WorldWideScience

Sample records for atropine

  1. Atropine and Other Anticholinergic Drugs

    Science.gov (United States)

    2007-01-01

    compromise near- who first analyzed the pharmacology and toxicol- vision in the case of accidental use. Military re- ogy of tabun obtained from captured...Lipp JA and Dola TJ (1978). Effect of atropine upon 290-293. the cerebrovascular system during soman-induced NakajimaT.Ohta S. Morita H etal. (1997...sarin: Clinical manifes- Wills JH (1963). Pharmacological antagonists of the tations and treatment of accidental poisoning by anticholinesterase agents

  2. Effect of atropine on sputum production.

    Science.gov (United States)

    Lopez-Vidriero, M T; Costello, J; Clark, T J; Das, I; Keal, E E; Reid, L

    1975-10-01

    The effect of atropine on sputum production has been studied in patients with asthama, chronic bronchitis, and bronchiectasis in some of whom there was bronchorrhoea. In three patients a reduction in sputum volume was observed after atropine but it would seem that the decrease was mainly due to the inhibitory effect on salivary secretion which facilitates spitting. The one patient treated with long-term oral atropine showed a marked reduction in sputum volume although chemical constituents and viscosity levels remained unchanged, suggesting that in this case atropine had an inhibitory effect on bronchial gland secretion.

  3. Refractory reverse amblyopia with atropine penalization

    Directory of Open Access Journals (Sweden)

    Preeti Ajit Patil

    2010-01-01

    Full Text Available Pharmacological penalization with atropine has been shown to be equally effective as conventional occlusion therapy in the treatment of amblyopia in children. Reverse amblyopia of the sound eye with atropine penalization has been reported before, but is more common in cases where the effect is augmented with optical penalization and is mostly reversible. We report a case of reverse amblyopia with atropine penalization, in a 4-year-old girl, which was refractory to treatment. This report highlights the need for strict monitoring of the vision in the sound eye and regular follow-up in children undergoing amblyopia treatment.

  4. Compliance and patching and atropine amblyopia treatments.

    Science.gov (United States)

    Wang, Jingyun

    2015-09-01

    In the past 20 years, there has been a great advancement in knowledge pertaining to compliance with amblyopia treatments. The occlusion dose monitor introduced quantitative monitoring methods in patching, which sparked our initial understanding of the dose-response relationship for patching amblyopia treatment. This review focuses on current compliance knowledge and the impact it has on patching and atropine amblyopia treatment. Copyright © 2015 Elsevier Ltd. All rights reserved.

  5. Extraction of atropine by ultrasounds in different solvent systems.

    Science.gov (United States)

    Djilani, A; Legseir, B

    2005-03-01

    The use of ultrasounds for extraction of atropine from Egyptian henbane (Hyoscyamus muticus) has been studied. The kinetic of extraction using various solvent systems was carried out. The results obtained have shown that the most efficient system of solvents was CH3OH/CH3CN (80:20). The amount of atropine was calculated by HPLC.

  6. [Cycloplegic effectiveness of cyclopentolate and tropicamide preparations compared with atropinization].

    Science.gov (United States)

    Proskurina, O V

    2002-01-01

    To gain a comparative estimate of cycloplegic agents with mild effect vs conventional atropinization, a study was performed on refraction in 57 children after instillations of cyclopentolate and atropine and in 57 children after instillations of tropicamide and atropine. A difference was determined in refraction after instillation of cycloplegic agents with mild effect and atropine. It turned out that by depth of cycloplegic effect cyclopentolate is reaching that of atropine. Cyclopentolate can be used in initial study of refraction in children with hypermetropic and myopic refraction and in repeated studies of any refraction. Tropicamide is less effective cycloplegic agent than cyclopentolate and thus it can be used in initial studies of refraction in children with myopia and in repeat studies of refraction in children with myopia and hypermetropia and also in cases of intolerance of other cycloplegic agents.

  7. The pharmacokinetics of intraosseous atropine in hypovolemic swine.

    Science.gov (United States)

    Yost, Jonathan; Baldwin, Phillip; Bellenger, Sarah; Bradshaw, Freida; Causapin, Edna; Demotica, Richelle; Livingston, Michael; Lee, Cynthia; Gegel, Brian; Burgert, James; Claessens, Adam; Johnson, Don; Loughren, Michael

    2015-01-01

    Compare the pharmacokinetics of atropine administered via the intravenous (IV), intramuscular (IM), and intraosseous (IO) routes in a normovolemic and hypovolemic swine model. Prospective, between subjects, experimental study. Vivarium. Yorkshire-cross swine (N = 36). Atropine was administered via IV, IM, or IO routes to normovolemic and hypovolemic swine. Blood samples were drawn at regular intervals after atropine administration and analyzed for plasma atropine concentration. Pharmacokinetic parameters were obtained from modeling the plasma concentrations. Pharmacokinetic parameters, maximum concentration (Cmax) and time to maximum concentration (Tmax). The IV and IO groups in both the normovolemic and hypovolemic models reached peak plasma concentration immediately and had a very rapid distribution phase with no apparent absorption phase for the IO groups. Peak plasma concentration and time to reach peak concentration were both significantly lower for the IM groups. There was a significant increase in absorption time with IM administration in the hypovolemic model compared to the normovolemic model. The IO route is an effective method of administering atropine and is comparable to the IV route even under conditions of significant hemorrhage. Therapeutic levels of atropine may be delayed and possibly difficult to obtain via IM injection in the presence of hypovolemic shock.

  8. Atropine exposure in adolescence predispose to adult memory loss ...

    African Journals Online (AJOL)

    Some of the brain malfunctions in adulthoods have been linked to the developmental process in their childhood, especially in most adolescent who have been exposed to one form of drug abuse or another. This study investigated the effect of atropine exposure at adolescence on the memory and histology of the frontal ...

  9. Atropine exposure in adolescence predispose to adult memory loss ...

    African Journals Online (AJOL)

    1 Department of Anatomy, University of Ilorin, P.M.B. 1515 Ilorin, Nigeria. 2 Department of Anatomy, Afe Babalola University, P.M.B. 5454 Ado-Ekiti, Nigeria. 3 Department of Physiology, ... study investigated the effect of atropine exposure at adolescence on the memory and histology of the frontal cortex of Wistar rats and its ...

  10. Influence of atropine and loperamide on reduced intestinal transit ...

    African Journals Online (AJOL)

    The effects of Calotropis procera latex alone and in the presence of loperamide and atropine on intestinal transit in rats were determined to elucidate the action of C. procera on intestinal transit. Six groups of rats containing ten rats per group were used. Each rat in the control group (I) received 0.5 ml of normal saline.

  11. Impurity profiling of atropine sulfate by microemulsion electrokinetic chromatography.

    Science.gov (United States)

    Bitar, Yaser; Holzgrabe, Ulrike

    2007-07-27

    An oil-in-water microemulsion electrokinetic chromatography (MEEKC) method has been developed and validated for the determination of atropine, its major degradation products (tropic acid, apoatropine and atropic acid) and related substances from plants material (noratropine, 6-hydroxyhyoscyamine, 7-hydroxyhyoscyamine, hyoscine and littorine). Separation of atropine and all impurities was optimized by varying the voltage, the nature of the oil droplet and the buffer, as well as the organic modifier (methanol, 2-propanol or acetonitrile) and the surfactant type and concentration. The optimum O/W microemulsion background electrolyte (BGE) solution consists of 0.8% (w/w) octane, 6.62% (w/w) 1-butanol, 2.0% (w/w) 2-propanol, 4.44% (w/w) SDS and 86.14% (w/w) 10 mM sodium tetraborate buffer pH 9.2. In order to shorten the analysis time a voltage gradient was applied. The validation was performed with respect to specificity, linearity, range, limit of quantification and detection, precision, accuracy and robustness. The established method allowed the detection and determination of atropine sulfate related substances at impurity levels given in the European Pharmacopoeia. Good agreement was obtained between the established MEEKC method and the traditional RP-HPLC method.

  12. Comparison of exercise, dobutamine-atropine and dipyridamole-atropine stress echocardiography in detecting coronary artery disease

    Directory of Open Access Journals (Sweden)

    Petrasinovic Zorica

    2006-05-01

    Full Text Available Abstract Background Dipyridamole and dobutamine stress echocardiography testing are most widely utilized, but their sensitivity remained suboptimal in comparison to routine exercise stress echocardiography. The aim of our study is to compare, head-to-head, exercise, dobutamine and dipyridamole stress echocardiography tests, performed with state-of-the-art protocols in a large scale prospective group of patients. Methods Dipyridamole-atropine (Dipatro: 0.84 mg/kg over 10 min i.v. dipyridamole with addition of up to 1 mg of atropine, dobutamine-atropine (Dobatro: up to 40 mcg/kg/min i.v. dobutamine with addition of up to 1 mg of atropine and exercise (Ex, Bruce were performed in 166 pts. Of them, 117 pts without resting wall motion abnormalities were enrolled in study (91 male; mean age 54 ± 10 years; previous non-transmural myocardial infarction in 32 pts, angina pectoris in 69 pts and atypical chest pain in 16 pts. Tests were performed in random sequence, in 3 different days, within 5 day period under identical therapy. All patients underwent coronary angiography. Results Significant coronary artery disease (CAD; ≥50% diameter stenosis was present in 69 pts (57 pts 1-vessel CAD, 12 multivessel CAD and absent in 48 pts. Sensitivity (Sn was 96%, 93% and 90%, whereas specificity (Sp was 92%, 92% and 87% for Dobatro, Dipatro and Ex, respectively (p = ns. Concomitant beta blocker therapy did not influence peak rate-pressure product and Sn of Dobatro and Dipatro (p = ns. Conclusion When state-of-the-art protocols are used, dipyridamole and dobutamine stress echocardiography have comparable and high diagnostic accuracy, similar to maximal post-exercise treadmill stress echocardiography.

  13. Comparison of exercise, dobutamine-atropine and dipyridamole-atropine stress echocardiography in detecting coronary artery disease

    Science.gov (United States)

    Nedeljkovic, Ivana; Ostojic, Miodrag; Beleslin, Branko; Djordjevic-Dikic, Ana; Stepanovic, Jelena; Nedeljkovic, Milan; Stojkovic, Sinisa; Stankovic, Goran; Saponjski, Jovica; Petrasinovic, Zorica; Giga, Vojislav; Mitrovic, Predrag

    2006-01-01

    Background Dipyridamole and dobutamine stress echocardiography testing are most widely utilized, but their sensitivity remained suboptimal in comparison to routine exercise stress echocardiography. The aim of our study is to compare, head-to-head, exercise, dobutamine and dipyridamole stress echocardiography tests, performed with state-of-the-art protocols in a large scale prospective group of patients. Methods Dipyridamole-atropine (Dipatro: 0.84 mg/kg over 10 min i.v. dipyridamole with addition of up to 1 mg of atropine), dobutamine-atropine (Dobatro: up to 40 mcg/kg/min i.v. dobutamine with addition of up to 1 mg of atropine) and exercise (Ex, Bruce) were performed in 166 pts. Of them, 117 pts without resting wall motion abnormalities were enrolled in study (91 male; mean age 54 ± 10 years; previous non-transmural myocardial infarction in 32 pts, angina pectoris in 69 pts and atypical chest pain in 16 pts). Tests were performed in random sequence, in 3 different days, within 5 day period under identical therapy. All patients underwent coronary angiography. Results Significant coronary artery disease (CAD; ≥50% diameter stenosis) was present in 69 pts (57 pts 1-vessel CAD, 12 multivessel CAD) and absent in 48 pts. Sensitivity (Sn) was 96%, 93% and 90%, whereas specificity (Sp) was 92%, 92% and 87% for Dobatro, Dipatro and Ex, respectively (p = ns). Concomitant beta blocker therapy did not influence peak rate-pressure product and Sn of Dobatro and Dipatro (p = ns). Conclusion When state-of-the-art protocols are used, dipyridamole and dobutamine stress echocardiography have comparable and high diagnostic accuracy, similar to maximal post-exercise treadmill stress echocardiography. PMID:16672046

  14. Effects of Atropine and Azaprophen on Matching and Detection in Rhesus Monkeys

    Science.gov (United States)

    1989-01-01

    substantially more potent than atropine for inhibiting termining whether atropine and azaprophen could be differ- carbachol-induced c,- amylase release (6. 7, 13...investigated the behavioral effects of azap- tion of daily fruit and vitamin supplements, was presented rophen and atropine in rhesus monkeys using...thank Jeffrey Witkin for helpful comments on the with results from carbachol-induced a- amylase release (6, 7, manuscript and Donald Conrad and Lisa King

  15. Efficacy of atropine and anisodamine eye drops for adolescent pseudomyopia

    Directory of Open Access Journals (Sweden)

    Hui-Jie Wang

    2017-03-01

    Full Text Available AIM:To investigate the effect and local influence of atropine and anisodamine eye drops on adolescent pseudomyopia. METHODS:Totally 110 cases of juvenile pseudomyopia were randomly divided into two groups, the control group was given 10g/L atropine sulfate eye gel, and the observation group was treated with 5g/L raceanisodamine eye drops. The efficacy of two methods, the changes of axial length and intraocular pressure before and after treatment, and the incidence of adverse reactions were compared. RESULTS: There was no significant difference in cure rate between the two groups(χ2=0.533, P=0.465, but the effective rate of observation group was significantly better than the control group(χ2=3.907, P=0.048. Compared with the same group before treatment, the length of the axial length of the two groups increased in different degrees,and the increase value of the observation group was significantly higher than that of the control group, the difference was statistically significant(PP>0.05. The intraocular pressure of the two groups was significantly lower than that of the same group before treatment, and the difference between the two groups after treatments was not statistically significant(P >0.05. The incidence of adverse reactions in the observation group was significantly lower than that in the control group(χ2=18.939, PCONCLUSION: Anisodamine eye drops in the treatment of juvenile pseudomyopia has obvious curative effect, its efficacy and safety are better than atropine eye gel.

  16. Split-dose atropine versus glycopyrrolate with neostigmine for reversal of gallamine-induced neuromuscular blockade

    DEFF Research Database (Denmark)

    Wetterslev, J; Jarnvig, I; Jørgensen, L N

    1991-01-01

    of glycopyrrolate (7 micrograms.kg-1) or two doses of atropine (8 micrograms.kg-1 each), given with an interval of 1 min. There were no differences between the two methods with respect to percentage heart rate changes, salivation or arousal time. Four patients demonstrated cardiac arhythmias in the atropine group...

  17. Efficacy and Adverse Effects of Atropine in Childhood Myopia: A Meta-analysis.

    Science.gov (United States)

    Gong, Qianwen; Janowski, Miroslaw; Luo, Mi; Wei, Hong; Chen, Bingjie; Yang, Guoyuan; Liu, Longqian

    2017-06-01

    Some uncertainty about the clinical value and dosing of atropine for the treatment of myopia in children remains. To evaluate the efficacy vs the adverse effects of various doses of atropine in the therapy for myopia in children. Data were obtained from PubMed, EMBASE, and the Cochrane Central Register of Controlled Trials, from inception to April 30, 2016. The reference lists of published reviews and clinicaltrials.gov were searched for additional relevant studies. Key search terms included myopia, refractive errors, and atropine. Only studies published in English were included. Randomized clinical trials and cohort studies that enrolled patients younger than 18 years with myopia who received atropine in at least 1 treatment arm and that reported the annual rate of myopia progression and/or any adverse effects of atropine therapy were included in the analysis. Two reviewers independently abstracted the data. Heterogeneity was statistically quantified by Q, H, and I2 statistics, and a meta-analysis was performed using the random-effects model. The Cochrane Collaboration 6 aspects of bias and the Newcastle-Ottawa Scale were used to assess the risk for bias. The primary outcome was a difference in efficacy and the presence of adverse effects at different doses of atropine vs control conditions. The secondary outcomes included the differences in adverse effects between Asian and white patients. Nineteen unique studies involving 3137 unique children were included in the analysis. The weighted mean differences between the atropine and control groups in myopia progression were 0.50 diopters (D) per year (95% CI, 0.24-0.76 D per year) for low-dose atropine, 0.57 D per year (95% CI, 0.43-0.71 D per year) for moderate-dose atropine, and 0.62 D per year (95% CI, 0.45-0.79 D per year) for high-dose atropine (P myopia progression (P = .15). High-dose atropine were associated with more adverse effects, such as the 43.1% incidence of photophobia compared with 6.3% for low

  18. Atropine and glycopyrrolate do not support bacterial growth-safety and economic considerations.

    Science.gov (United States)

    Ittzes, Balazs; Weiling, Zsolt; Batai, Istvan Zoard; Kerenyi, Monika; Batai, Istvan

    2016-12-01

    Evaluation of bacterial growth in atropine and glycopyrrolate. Laboratory investigation. Standard microbiological methods were used to evaluate the impact of atropine and glycopyrrolate on the growth of Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, and Escherichia coli. Bacterial count was checked at 0, 1, 2, 3, 4, 6, and 24 hours. Atropine or glycopyrrolate did not support the growth of the above bacteria at any examined time at room temperature. Glycopyrrolate killed all of the examined strains (P < .05), whereas in atropine, only the clinical isolates of Staphylococcus and Acinetobacter were killed (P < .05). Drawing up atropine or glycopyrrolate at the beginning of the operating list and use within 24 hours if needed are a safe practice and do not pose infection hazard. We can also reduce hospital costs if we do not throw away these unused syringes following each case. Copyright © 2016 Elsevier Inc. All rights reserved.

  19. Civilian adult self injections of atropine-trimedoxime (TMB4) auto-injectors.

    Science.gov (United States)

    Bentur, Yedidia; Layish, Ido; Krivoy, Amir; Berkovitch, Matitiahu; Rotman, Eran; Haim, Shmuel Bar; Yehezkelli, Yoav; Kozer, Eran

    2006-01-01

    The clinical effects of self injections of atropine-trimedoxime auto-injectors distributed to the civilian population as a field antidote for nerve agent attack were assessed. Data on self injections by adults (> or = 18 years) were collected from the Israel Poison Information Center and a hospital Emergency Department's records during a 2-year period. The data included demographics, time interval from injection, type of auto-injector, clinical manifestations and atropinization score. Sixty-five patients, all with unintentional self injections, were reported. Systemic atropine effects were observed in 24 patients, but no severe atropinization. The atropinization score was significantly higher in the 2 mg atropine dose group than in the two lower dose groups, which were in the normal range. No specific adverse effects attributable to trimedoxime were observed. Intravenous fluids and physostigmine were not required. Only mild reactions were observed following self-injection of atropine trimedoxime auto-injectors in adults, attesting to their relative safety under these conditions.

  20. A randomized trial of adding a plano lens to atropine for amblyopia.

    Science.gov (United States)

    Wallace, David K; Lazar, Elizabeth L; Repka, Michael X; Holmes, Jonathan M; Kraker, Raymond T; Hoover, Darren L; Weise, Katherine K; Waters, Amy L; Rice, Melissa L; Peters, Robert J

    2015-02-01

    Some children have residual amblyopia after treatment with atropine eyedrops for amblyopia due to strabismus and/or anisometropia. We conducted a randomized clinical trial to evaluate the effectiveness of augmenting the effect of atropine by changing the lens over the fellow eye to plano in children with residual amblyopia. A total of 73 children 3 to amblyopia (range, 20/32 to 20/160, mean 20/63(+1)) were enrolled after at least 12 weeks of atropine treatment of the fellow eye. Participants were randomly assigned to continuing weekend atropine alone or wearing a plano lens over the fellow eye (while continuing atropine). The primary outcome was assessed at 10 weeks, and participants were followed until improvement ceased. At the 10-week primary outcome visit, amblyopic-eye visual acuity had improved an average of 1.1 lines with the plano lens and 0.6 lines with atropine only (difference adjusted for baseline visual acuity = + 0.5 line; 95% CI, -0.1 to +1.2). At the primary outcome or later visit when the best-measured visual acuity was observed, the mean amblyopic-eye improvement from baseline was 1.9 lines with the plano lens and 0.8 lines with atropine only. When amblyopic-eye visual acuity stops improving with atropine treatment, there may be a small benefit to augmenting atropine therapy with a plano lens over the fellow eye. However, the effect was not statistically significant, and the large confidence interval raises the possibility of no benefit or a benefit larger than we observed. A larger study would be necessary to get a more precise estimate of the treatment effect. Copyright © 2015 American Association for Pediatric Ophthalmology and Strabismus. Published by Elsevier Inc. All rights reserved.

  1. Cytotoxicity of atropine to human corneal endothelial cells by inducing mitochondrion-dependent apoptosis.

    Science.gov (United States)

    Wen, Qian; Fan, Ting-Jun; Tian, Cheng-Lei

    2016-07-01

    Atropine, a widely used topical anticholinergic drug, might have adverse effects on human corneas in vivo. However, its cytotoxic effect on human corneal endothelium (HCE) and its possible mechanisms are unclear. Here, we investigated the cytotoxicity of atropine and its underlying cellular and molecular mechanisms using an in vitro model of HCE cells and verified the cytotoxicity using cat corneal endothelium (CCE) in vivo. Our results showed that atropine at concentrations above 0.3125 g/L could induce abnormal morphology and viability decline in a dose- and time-dependent manner in vitro. The cytotoxicity of atropine was proven by the induced density decrease and abnormality of morphology and ultrastructure of CCE cells in vivo. Meanwhile, atropine could also induce dose- and time-dependent elevation of plasma membrane permeability, G1 phase arrest, phosphatidylserine externalization, DNA fragmentation, and apoptotic body formation of HCE cells. Moreover, 2.5 g/L atropine could also induce caspase-2/-3/-9 activation, mitochondrial transmembrane potential disruption, downregulation of anti-apoptotic Bcl-2 and Bcl-xL, upregulation of pro-apoptotic Bax and Bad, and upregulation of cytoplasmic cytochrome c and apoptosis-inducing factor. In conclusion, atropine above 1/128 of its clinical therapeutic dosage has a dose- and time-dependent cytotoxicity to HCE cells in vitro which is confirmed by CCE cells in vivo, and its cytotoxicity is achieved by inducing HCE cell apoptosis via a death receptor-mediated mitochondrion-dependent signaling pathway. Our findings provide new insights into the cytotoxicity and apoptosis-inducing effect of atropine which should be used with great caution in eye clinic. © 2016 by the Society for Experimental Biology and Medicine.

  2. [Objective refraction in black children: cyclopentolate and tropicamide combination, a reliable alternative to atropine?].

    Science.gov (United States)

    Ka, A M; De Medeiros, M E; Sow, A S; Ndiaye, P A; Weladji, C; Diallo, H M; Wane, A M; Diagne, J P; Kane, A; Ndiaye, J M M; Ndoye Roth, P A; Ba, E A; Ndiaye, M R

    2014-11-01

    Cycloplegia allows for an objective refraction in children. Atropine is the gold standard but causes prolonged blurred vision. Cyclopentolate is less effective but less disabling. Tropicamide is a weak cycloplegic. The purpose of this study was to evaluate a cyclopentolate and tropicamide combination (CTA) versus atropine for refraction in black children. We performed a prospective study between October 2011 and July 2012 on all children seen in consultation. Objective refraction was performed after cycloplegia with cyclopentolate 0.5% combined with tropicamide 0.5%, and then after cycloplegia with atropine. Thirty-three patients were recruited, 14 boys and 19 girls. The average age was 9.9 years. The mean age of the patients was 9.9 years. Astigmatism was found in 96.9% of cases. It was 1.34±1.32 diopters with CTA and 1.35±1.22 diopters with atropine. The mean axis was 98.15 and 99.8, respectively. Hyperopia and myopia were found in 39 and 27 eyes, respectively with ACT (average 1.73 and 5.37 diopters), and in 41 and 19 eyes with atropine (average 2.06 and 6.11 diopters). There is a good correlation of results with regards to cylindrical and spherical refractive error between the two protocols. Atropine is the best cycloplegic, however ACT provides reliable results. The cyclopentolate-tropicamide combination is satisfactory for routine cycloplegia in children. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  3. Atropine unmasks bed-rest effect - A spectral analysis of cardiac interbeat intervals

    Science.gov (United States)

    Goldberger, Ary L.; Goldwater, Danielle; Bhargava, Valmik

    1986-01-01

    Heart rate spectral data obtained for 10 male subjects between 35-49 years following orthostatic tolerance testing with lower body negative pressure prebed rest and after 7-10 days of bed rest, while on placebo and after intravenous atropine are analyzed. Comparison of the spectral atropine rms for subjects prebed rest and after bed rest reveal a decrease from 63 + or - 24 ms to 40 + or - 23 ms. It is observed that heart rate interval variability for subjects after bed rest and with atropine is reduced; the heart rate at bed rest with atropine is increased from 70.4 + or - 12.4 beats/min prebed rest to 83.7 + or - 18.9 beats/min; and the exercise tolerance time for subjects in the atropine prebed-rest phase (658 + or - 352 s) is higher than the bed-rest phase (505 + or - 252 s). It is noted that bed rest impairs the cardiovascular capacity to adaptively modulate physiological responses, atropine exposes bed-rest deconditioning effects, and spectral analysis is useful for studying the effects of bed-rest deconditioning on cardiac dynamics.

  4. Atropine and Roscovitine Release from Model Silicone Hydrogels.

    Science.gov (United States)

    Lasowski, Frances; Sheardown, Heather

    2016-04-01

    Drug delivery to the anterior eye has a low compliance and results in significant drug losses. In pediatric patients, eye diseases such as myopia and retinoblastoma can potentially be treated pharmacologically, but the risk associated with high drug concentrations coupled with the need for regular dosing limits their effectiveness. The current study examined the feasibility of atropine and roscovitine delivery from model silicone hydrogel materials which could potentially be used to treat myopia and retinoblastoma, respectively. Model silicone hydrogel materials that comprised TRIS and DMA were prepared with the drug incorporated during synthesis. Various materials properties, with and without incorporated drug, were investigated including water uptake, water contact angle, and light transmission. Drug release was evaluated under sink conditions into phosphate buffered saline. The results demonstrate that up to 2 wt% of the drugs can be incorporated into model silicone hydrogel materials without adversely affecting critical materials properties such as water uptake, light transmission, and surface hydrophilicity. Equilibrium water content ranged from 15 to 32% and transmission exceeded 89% for materials with at least 70% DMA. Extended release exceeding 14 days was possible with both drugs, with the total amount of drug released from the materials ranging from 16% to over 76%. Although a burst effect was noted, this was thought to be due to surface-bound drug, and therefore storage in an appropriate packaging solution could be used to overcome this if desired. Silicone hydrogel materials have the potential to deliver drugs for over 2 weeks without compromising lens properties. This could potentially overcome the need for regular drop instillation and allow for the maintenance of drug concentration in the tear film over the period of wear. This represents a potential option for treating a host of ophthalmic disorders in children including myopia and retinoblastoma.

  5. Is oxygen required before atropine administration in organophosphorus or carbamate pesticide poisoning? – A cohort study

    Science.gov (United States)

    Konickx, L. A.; Bingham, K.

    2014-01-01

    Background Early and adequate atropine administration in organophosphorus (OP) or carbamate insecticide poisoning improves outcome. However, some authors advise that oxygen must be given before atropine due to the risk of inducing ventricular dysrhythmias in hypoxic patients. Because oxygen is frequently unavailable in district hospitals of rural Asia, where the majority of patients with insecticide poisoning present, this guidance has significant implications for patient care. The published evidence for this advice is weak. We therefore performed a patient cohort analysis to look for early cardiac deaths in patients poisoned by anticholinesterase pesticides. Methods We analysed a prospective Sri Lankan cohort of OP or carbamate-poisoned patients treated with early atropine without the benefit of oxygen for evidence of early deaths. The incidence of fatal primary cardiac arrests within 3 h of admission was used as a sensitive (but non-specific) marker of possible ventricular dysrhythmias. Results The cohort consisted of 1957 patients. The incidence of a primary cardiac death within 3 h of atropine administration was 4 (0.2%) of 1957 patients. The majority of deaths occurred at a later time point from respiratory complications of poisoning. Conclusion We found no evidence of a high number of early deaths in an observational study of 1957 patients routinely given atropine before oxygen that might support guidance that oxygen must be given before atropine. The published literature indicates that early and rapid administration of atropine during resuscitation is life-saving. Therefore, whether oxygen is available or not, early atropinisation of OP- and carbamate-poisoned patients should be performed. PMID:24810796

  6. The Effect of Atropine on Post-ECT Bradycardia in Patients with Major Depressive Disorder

    Directory of Open Access Journals (Sweden)

    Hassan Farashbandi

    2014-08-01

    Full Text Available Background: Electroconvulsive therapy (ECT is utilized for treatment of a range of psychiatric disorders including major depressive disorder (MDD. One of the major complications in using ECT is cardiovascular problems i.e., bradycardia. The present study was designed to investigate the effect of atropine on the pulse rate (PR of the patients under treatment with ECT. Materials and Methods: In this randomized clinical trial, 30 patients with diagnosis of MDD who received atropine before ECT treatment (control group were compared with 30 patients with the same diagnosis without receiving atropine (experimental group under ECT treatment. Both groups received ECT under the same term and condition. The PR of the patients were recorded 7 times (twice before anesthesia and ECT and 5 fixed one min intervals immediately after receiving ECT; for 10 sessions of treatment with ECT (3 times a week. The results were analyzed using repeated measure analysis of variance. The PR under 50 was the cut off point for differentiating the patients suffering from bradycardia and those without it. Results: Slight increment in PRs for experimental group (patient who did not receive atropine in contrast to control group were observed, but it did not reach a statistically significant level. The gender (male/female did not have different PR. The age of the patients and initial PR (regarded as co-variances did not show significant effect on PR for total sample. Conclusion: There seems to be not necessary to use atropine treatment for depressed patients receiving ECT.

  7. Haemodynamic effects of remifentanil in children with and without intravenous atropine. An echocardiographic study.

    Science.gov (United States)

    Chanavaz, C; Tirel, O; Wodey, E; Bansard, J Y; Senhadji, L; Robert, J C; Ecoffey, C

    2005-01-01

    Remifentanil is known to cause bradycardia and hypotension. We aimed to characterize the haemodynamic profile of remifentanil during sevoflurane anaesthesia in children with or without atropine. Forty children who required elective surgery received inhalational induction of anaesthesia using 8% sevoflurane. They were allocated randomly to receive either atropine, 20 microg kg(-1) (atropine group) or Ringer's lactate (control group) after 10 min of steady-state 1 MAC sevoflurane anaesthesia (baseline). Three minutes later (T0), all children received remifentanil 1 microg kg(-1) injected over a 60 s period, followed by an infusion of 0.25 microg kg(-1) min(-1) for 10 min then 0.5 microg kg(-1) min(-1) for 10 min. Haemodynamic variables and echocardiographic data were determined at baseline, T0, T5, T10, T15 and T20 min. Remifentanil caused a significant decrease in heart rate compared with the T0 value, which was greater at T20 than T10 in the two groups: however, the values at T10 and T20 were not significantly different from baseline in the atropine group. In comparison with T0, there was a significant fall in blood pressure in the two groups. Remifentanil caused a significant decrease in the cardiac index with or without atropine. Remifentanil did not cause variation in stroke volume (SV). In both groups, a significant increase in systemic vascular resistance occurred after administration of remifentanil. Contractility decreased significantly in the two groups, but this decrease remained moderate (between -2 and +2 sd). Remifentanil produced a fall in blood pressure and cardiac index, mainly as a result of a fall in heart rate. Although atropine was able to reduce the fall in heart rate, it did not completely prevent the reduction in cardiac index.

  8. Comparison of sugammadex and neostigmine–atropine on intraocular pressure and postoperative effects

    Directory of Open Access Journals (Sweden)

    Sedat Hakimoğlu

    2016-02-01

    Full Text Available During surgery, changes in intraocular pressure (IOP can be observed resulting from several factors, such as airway manipulations and drugs used. We aimed to investigate the effects of sugammadex and neostigmine on IOP, hemodynamic parameters, and complications after extubation. Our study comprised 60 patients, aged 18–65 years, with a risk status of the American Society of Anesthesiologists I–II who underwent arthroscopic surgery under general anesthesia. The patients were randomly assigned into two groups. At the end of the surgery, the neuromuscular block was reversed using neostigmine (50 μg/kg plus atropine (15 μg/kg in Group 1, and sugammadex (4 mg/kg in Group 2. Neuromuscular blockade was monitored using acceleromyography and a train-of-four mode of stimulation. IOP was measured before induction and at 30 seconds, 2 minutes, and 10 minutes after extubation. A Tono-Pen XL applanation tonometer was used to measure IOP. This showed that elevation in IOP of patients reversed using sugammadex was similar to that recorded in patients reversed using neostigmine–atropine. When heart rate was compared, there was a significant difference between basal values and those obtained at 30 seconds and 10 minutes after extubation in the neostigmine–atropine group. Extubation time (time from withdrawal of anesthetic gas to extubation was significantly shorter in the sugammadex group (p = 0.003 than in the neostigmine–atropine group. The postextubation IOP values of the sugammadex group were similar to the neostigmine–atropine group. Extubation time (time from withdrawal of anesthetic gas to extubation was significantly shorter in the sugammadex group (p = 0.003 than in the neostigmine–atropine group.

  9. Multiple eccrine hidrocystomas: Report of two cases treated unsuccessfully with atropine ointment

    Directory of Open Access Journals (Sweden)

    Khunger Niti

    2004-01-01

    Full Text Available Eccrine hidrocystomas are rare, benign, cystic lesions with a lining that resembles that of the eccrine sweat gland and may be solitary or multiple. Multiple eccrine hidrocystomas occur predominantly on the face as asymptomatic, skin-colored to bluish lesions associated with a chronic course and seasonal variability. Treatment of multiple lesions on the face is challenging. Efficacy with atropine ointment is variable. Botulinum toxin and pulsed dye laser are reported to be beneficial. Two cases of multiple eccrine hidrocystomas are reported who showed no response to 1% atropine ointment.

  10. Efficacy of atropine combined with paroxetine in vagus nerve excitatory panic disorder

    Directory of Open Access Journals (Sweden)

    Du N

    2015-07-01

    Full Text Available Na Du, Xue-Li Sun Department of Psychiatry, West China Hospital, Sichuan University, Chengdu, People’s Republic of China Abstract: Panic disorder is often associated with the autonomic nervous system pattern – sympathetic activation and parasympathetic (vagal withdrawal. However, we present one special case here to show a totally reversed pathogenesis – vagal activation occupying the leading role, which requires atropine to cure the patient’s symptoms. Through this report, it is reasonably proven that panic disorder may be a heterogeneous condition, whose mechanism might be the imbalance between the sympathetic and parasympathetic tone. Keywords: panic disorder, vagal activation, bradycardia, atropine

  11. Comparative study of oral and intramuscular atropine sulphate as a premedicant in paediatric age group.

    Directory of Open Access Journals (Sweden)

    Chaudhari L

    1989-01-01

    Full Text Available The use of atropine sulphate in the paediatric age group as a premedicant orally in a dosage of 0.02 mg/kg body weight 70 minutes prior to surgery was found to be as effective as atropine sulphate given intramuscularly 35 minutes prior to surgery in a dosage of 0.01 mg/kg body weight. This avoids the unpleasant memory of needle prick; The duration of effect as studied in the normal healthy children not subjected to surgery was found to be 2 1/2-3 hours.

  12. Treatment outcomes of myopic anisometropia with 1% atropine: a pilot study.

    Science.gov (United States)

    Lin, Lixia; Lan, Weizhong; Liao, Yunru; Zhao, Feng; Chen, Can; Yang, Zhikuan

    2013-12-01

    To investigate the safety and efficacy of the treatment of myopic anisometropia with 1% atropine. Twenty-two children with myopic anisometropia were prescribed 1% solution of atropine sulfate to the more myopic eye, one drop before sleep every 3 days. Children were visited every 3 to 4 months until the degree of anisometropia was no more than 0.5 diopters (D) ("Success") or unchanged after 9 months of treatment ("No effect"). The treatment effect was assessed by comparing the interocular imbalance in refraction and axial length before and after the treatment. A detailed questionnaire about subjective symptoms in each visit and an electroretinogram in the end were administered to evaluate the side effects of this treatment. The subjects were followed for 7 to 16 months. Six subjects withdrew participation on their own accord, and three were excluded because of inconstant usage of drug. Of the 13 remaining subjects, the refraction of the treated eyes decreased by 0.63 ± 0.59 D (p = 0.007), whereas that of the untreated eyes increased by -0.72 ± 0.65 D (p anisometropia was reduced from 1.82 ± 0.73 D to 0.47 ± 0.65 D (p anisometropia, although with some tolerable side effects. Nevertheless, an attenuated benefit was observed after cessation of atropine treatment. Thus, participants should be informed of a possible rebound effect before the administration of atropine for myopic anisometropia.

  13. Intravenous and inhalation toxicokinetics of sarin stereoisomers in atropinized guinea pigs

    NARCIS (Netherlands)

    Spruit, W.E.T.; Langenberg, J.P.; Trap, H.C.; Wiel, H.J. van der; Helmich, R.B.; Helden, H.P.M. van; Benschop, H.P.

    2000-01-01

    We report the first toxicokinetic studies of (±)-sarin. The toxicokinetics of the stereoisomers of this nerve agent were studied in anesthetized, atropinized, and restrained guinea pigs after intravenous bolus administration of a dose corresponding to 0.8 LD50 and after nose-only exposure to vapor

  14. Prophylactic administration of atropine attenuates the negative haemodynamic effects of propofol/remifentanil induction of anaesthesia.

    NARCIS (Netherlands)

    Poterman, Marieke; Scheeren, Thomas; van der Velde, M.I.; Struys, Michel; Kalmar, A.F.

    2013-01-01

    Background and Goal of Study:   Induction of anaesthesia with propofol and remifentanil often induces unwanted bradycardia and hypotension. This raises the concern for preserving haemodynamic stability and adequate tissue oxygenation. We previously demonstrated that atropine significantly

  15. [Research on whether atropine can be substituted by the powerful cycloplegic cyclopentolate].

    Science.gov (United States)

    Xu, Jiang-tao

    2012-09-01

    For a long time, atropine eye ointment has been widely used as the cycloplegic for children's optometry in China, while internationally, cyclopentolate gutta is widely used as the first choice for cycloplegic. In recent years, 1% cyclopentolate hydrochloride ocular humor has been introduced to our country. This effective and powerful cycloplegic has already been paid close attention to by domestic pedo-ophthalmologists. According to a serious of studies both home and abroad on the therapeutic effects of the own control drugs, the cycloplegia effect of cyclopentolate is close to the atropine. Cyclopentolate can be widely used for the cycloplegia before optometry for the Chinese children. However, the effect of cyclopentolate is still not as good as atropine. So, for the children with farsightedness within 7 years old, all esotropia children, Am children, and children who suffer from decreased vision acuteness and needs to be excluded from accommodative myopia, atropine eye ointment should be routinely used for cycloplegia before optometry. In this article, we also discuss the medication dosage, medication method, possible drug adverse reactions of cyclopentolate humor ocular and the coping measures at the same time.

  16. Cycloplegic effect of atropine compared with cyclopentolate-tropicamide combination in children with hypermetropia.

    Science.gov (United States)

    Sani, Rabi Yahaya; Hassan, Sadiq; Habib, Saudat Garba; Ifeanyichukwu, Ebisike Philips

    2016-01-01

    Cycloplegic refraction is important in assessing children with hypermetropia. Atropine, though the gold standard cycloplegic agent for refraction in children, has a long duration of action and more severe side effects compared to short-acting cycloplegic agents. The aim of the study was to compare the cycloplegic effect of atropine with cyclopentolate and tropicamide combination in children with hypermetropia. This was a crossover interventional study in children with hypermetropia. Cycloplegic refraction using two separate regimens of cycloplegic drugs was done on all subjects. Data were analyzed using the statistical software SPSS version 22.0. The mean spherical equivalent values of regimen 1 (atropine 1%) and regimen 2 (cyclopentolate 1% and tropicamide 1%) were presented as mean and standard deviation. A P ≤ 0.05 was considered statistically significant. One hundred and twenty-six eyes of 63 subjects aged 5-12 years were examined. The mean spherical equivalent values for regimen 1 and regimen 2 for the right eyes were 4.73 ± 2.1 DS and 4.54 ± 1.9 DS, respectively (P = 0.59). The mean spherical equivalent values for regimens 1 and 2 for the left eyes were 4.74 ± 2.0 DS and 4.54 ± 1.8 DS, respectively (P = 0.56). The combination of 1% cyclopentolate and 1% tropicamide could be a useful alternative to atropine 1% for cycloplegic refraction in children with hypermetropia.

  17. Effect of Pre-medication with Atropine on the Blood Pressure of ...

    African Journals Online (AJOL)

    Arterial blood pressure and heart rate were recorded every 3 minutes. The patients were asked to report any symptoms of nausea or fainting. Results: Both the incidence and severity of hypotension were reduced in the patients that had atropine prophylaxis (Group B) compared with the control group that received normal ...

  18. Efficacy of tropicamide, homatropine, cyclopentolate, atropine and hyoscine as mydriatics in Angora goats.

    Science.gov (United States)

    Whelan, N C; Castillo-Alcala, F; Lizarraga, I

    2011-11-01

    To document the efficacy of five commercially available mydriatics for their potential for diagnostic and therapeutic use in Angora goats. Over 8 weeks, the mydriatic effects of 1% tropicamide, 2% homatropine, 1% cyclopentolate, 1% atropine and 0.25% hyoscine were evaluated. Given as block treatments, drugs were applied randomly to one eye of 10 Angora goats, and the contralateral eye served as a control. Vertical and horizontal pupil diameters were measured to document onset of effect, time to reach a difference of 5 mm in the vertical/horizontal pupil diameter between eyes, time to maximum pupillary dilation, and duration of mydriatic action. Onset of mydriasis for all drugs occurred within 15 minutes. Time to reach a difference of 5 mm in the vertical pupil diameter between eyes was shortest for 1% tropicamide and 0.25% hyoscine (0.5 h), then 2% homatropine and 1% atropine (0.75 h), and longest for 1% cyclopentolate (1.5 h). The maximum vertical pupillary dilation occurred earliest with 1% tropicamide and 1% atropine (2 h), followed by 0.25% hyoscine (3 h), 2% homatropine (4 h), and latest with 1% cyclopentolate (8 h). The duration of vertical dilation of the pupil was shortest with 1% tropicamide (6 h), then 2% homatropine (12 h), 1% cyclopentolate (12 h), 1% atropine (24 h), and longest for 0.25% hyoscine (96 h). The time to reach maximum horizontal dilation of the pupil in treated eyes was shortest with 1% cyclopentolate (1 h), followed by 1% tropicamide (1.5 h), 0.25% hyoscine (3 h), 2% homatropine (3.5 h), and 1% atropine (4 h). The duration of horizontal pupil dilation was shortest with 1% tropicamide (4.5 h), and longest with 0.25% hyoscine (48 h). All five mydriatics induced clinical dilation. Tropicamide (1%) had the shortest duration of effect, but gave incomplete dilation. Good dilation was achieved with 1% cyclopentolate and 2% homatropine, but took too long to reach maximum dilation for routine mydriasis. The largest vertical dilation of the pupil

  19. Dose-response effects of atropine and HI-6 treatment of organophosphorus poisoning in guinea pigs

    Energy Technology Data Exchange (ETDEWEB)

    Koplovitz, I.; Menton, R.; Matthews, C.; Shutz, M.; Nalls, C.

    1995-12-31

    H1-6 (1-2-hydrnxyiminomethyl-1 pyridino-3-(4-carbameyl- 1--pyddino)-2- oxaprnpane dichioride) has been evaluated as an oxime alternative to pralidoxime, and toxogonin in the treatment of organophosphorus (OP) poisoning. The dose response effects of atropine (ATR) and HI-6 were investigated to more fully explore the interaction of these compounds in the treatment of OP poisoning. ATR, HI-6 and various combinations of the two drugs were evaluated against lethal poisoning by soman (GD) and tabun (GA) in guinea pigs. The effect of adjunctive diazepam treatment on the efficacy of atropine and HI-6 against soman was also investigated. Animals of either sex were challenged s.c. with OP and treated i.m. 1 min later with ATR and/or HI-6. When used, diazepam was injected immediately after ATR+HI6. LD50s of each treatment were calculated from probit models based on 24-hour survival against 5 levels of nerve agent and 6 animals per challenge level. A protective index (PI) was calculated by dividing the nerve agent LD50 in the presence of treatment by the LD50 in the absence of treatment. Treatment with HI-6 alone had little effect on the toxicity of either OP. Treatment with ATR alone was more effective than HI-6 alone and was significantly more effective against soman than against tabun. When used in combination atropine and HI-6 had a strong synergistic effect against both agents. The dose of atropine used with HI-6 was critical in determining the efficacy of HI-6 against either agent. The slopes of the dose-lethality curves were minimally affected by the dose of ATR or HI-6. Adjunctive treatment with diazepam enhanced the efficacy of HI-6 and atropine against soman.

  20. MRI findings in 6 cases of children by inadvertent ingestion of diphenoxylate-atropine

    Energy Technology Data Exchange (ETDEWEB)

    Xiao Lianxiang [Shandong University School of Medicine, Shandong Medical Imaging Research Institute , No. 44 West Wenhua Road, Jinan 250012 (China); Lin Xiangtao, E-mail: yishui1982@126.com [Shandong University School of Medicine, Shandong Medical Imaging Research Institute, No. 44 West Wenhua Road, Jinan 250012 (China); Cao Jinfeng [Shandong University School of Medicine, Shandong Medical Imaging Research Institute , No. 44 West Wenhua Road, Jinan 250012 (China); Wang Xueyu [Division of Pediatrics, Shandong Provincial Hospital, Shandong University, No. 324 Jingwu Road, Jinan 250021 (China); Wu Lebin [Shandong Medical Imaging Research Institute, No. 324 Jingwu Road, Jinan 250021 (China)

    2011-09-15

    Purpose: Compound diphenoxylate (diphenoxylate-atropine) poisoning can cause toxic encephalopathy in children, and magnetic resonance imaging (MRI) of the brain in this condition has not been reported. This study is to analyze brain MRI findings and to investigate the relations between MRI features and possible pathophysiological changes in children. Methods: Six children accidentally swallowed compound diphenoxylate, 4 males, 2 females, aged 20-46 months, average 33 months. Quantity of ingested diphenoxylate-atropine was from 6 to 30 tablets, each tablet contains diphenoxylate 2.5 mg and atropine 0.025 mg. These patients were referred to our hospital within 24 h after diphenoxylate-atropine ingestion, and underwent brain MRI scan within 24-72 h after emergency treatment. The characteristics of conventional MRI were analyzed. Results: These pediatric patients had various symptoms of opioid intoxication and atropine toxicity. Brain MRI showed abnormal low signal intensity on T1-weighted images (T1WI) and abnormal high signal intensity on T2-weighted images (T2WI) and fluid-attenuated inversion recovery (FLAIR) imaging in bilateral in all cases; abnormal high signal intensity on T1WI, T2WI and FLAIR in 4 cases. Encephalomalacia was observed in 3 cases during follow-up. Conclusion: In the early stage of compound diphenoxylate poisoning in children, multiple extensive edema-necrosis and hemorrhagic-necrosis focus were observed in basic nucleus, pallium and cerebellum, these resulted in the corresponding brain dysfunction with encephalomalacia. MRI scan in the early stage in this condition may provide evidences of brain impairment, and is beneficial for the early diagnosis, treatment and prognosis assessment.

  1. Minimizing E-factor in the continuous-flow synthesis of diazepam and atropine.

    Science.gov (United States)

    Bédard, Anne-Catherine; Longstreet, Ashley R; Britton, Joshua; Wang, Yuran; Moriguchi, Hideki; Hicklin, Robert W; Green, William H; Jamison, Timothy F

    2017-12-01

    Minimizing the waste stream associated with the synthesis of active pharmaceutical ingredients (APIs) and commodity chemicals is of high interest within the chemical industry from an economic and environmental perspective. In exploring solutions to this area, we herein report a highly optimized and environmentally conscious continuous-flow synthesis of two APIs identified as essential medicines by the World Health Organization, namely diazepam and atropine. Notably, these approaches significantly reduced the E-factor of previously published routes through the combination of continuous-flow chemistry techniques, computational calculations and solvent minimization. The E-factor associated with the synthesis of atropine was reduced by 94-fold (about two orders of magnitude), from 2245 to 24, while the E-factor for the synthesis of diazepam was reduced by 4-fold, from 36 to 9. Copyright © 2017 Elsevier Ltd. All rights reserved.

  2. Primacy and recency effects in rhesus monkeys (Macaca mulatta) using a serial probe recognition task: II. Effects of atropine sulfate.

    Science.gov (United States)

    Castro, C A

    1997-08-01

    Nonhuman primates display both a primacy and a recency effect when trained on a 6-item serial probe recognition task. The author has previously shown that in the rhesus monkey, diazepam (3.2 mg/kg im) interferes with the memory processes that mediate the recency effect without affecting those memory processes involved in the primacy effect (C. A. Castro, 1995). This study assessed the effects of atropine sulfate (0.2, 0.3, and 0.4 mg/kg im) on the primacy and recency effects in these same monkeys. Opposite the effects of diazepam, atropine disrupted the primacy component of the serial position curve and had no measurable effect on the recency component. In addition, the 2 highest doses of atropine disrupted accuracy on the nonmatching probe trials, whereas all 3 doses of atropine resulted in increased response latencies. These reports indicate that the primacy and recency effects in the nonhuman primate can be pharmacologically dissociated.

  3. Pharmacokinetics of IM,IV and IO Atropine in Normovolemic and Hypovolemic Swine

    Science.gov (United States)

    2016-06-12

    support the bioequivalence of intraosseous and intravenous administration of atropine. In theory , drug could distribute to the bone marrow of the...to humans; however, pigs are very similar in anatomy and physiology and should approximate results with humans. In fact, the tibia of a 70-kilogram...marrow volume and is made up of red marrow compared to the adult tibia which is made up of almost entirely yellow marrow. In theory , the sternal IO route

  4. Content of atropine and scopolamine in poisonous solanaceae plants from Slovenia

    Directory of Open Access Journals (Sweden)

    Javor Kac

    2006-03-01

    Full Text Available Background: Some species from the Solanaceae family are still the cause of serious poisoning among youth in Slovenia. Usually intoxication is due to abuse of these plants to provoke hallucinations. There is still not enough data about the alkaloid content of these plants growing in Slovenia.Methods: Different plant samples were analyzed for the content of atropine and scopolamine with capillary electrophoresis after solid phase extraction of alkaloids. Plants were gathered from different areas of Slovenia between April and September 2004.Results: Results were compared and possible correlations between the alkaloid content and species, plant parts, growth conditions, and time of harvest were suggested. Atropine and scopolamine contents were assessed in deadly nightshade (Atropa belladonna L., thorn apple (Datura stramonium L., scopolia (Scopolia carniolica Jacq. and angel trumpet. The common name angel trumpet is used for Datura inoxia Mill. as well as for different Brugmansia Pers. species. The most intriguing results were the variable alkaloid content in various Brugmansia species and generally great differences in alkaloid content among various plants and their plant parts.Conclusions: All investigated plants have noticeable atropine and/or scopolamine content. The content is variable between various plants and their plant parts and therefore special care should be taken in cases of possible intoxication. It was shown that smaller or greater amounts of ingested drug can cause the same level of intoxication due to the variability in alkaloid content.

  5. Physiological responses wearing MOPP-IV after atropine and pralidoxime administration in warm and cool environments

    Energy Technology Data Exchange (ETDEWEB)

    Kolka, M.A.; Cadarette, B.S.

    1988-04-01

    The effect of cholinolytic and oxime (2 mg atropine + 600 mg pralidoxime) therapy on temperature regulation was evaluated in 8 subjects wearing chemical warfare protective clothing (MOPP-level IV). Subjects were tested in two environments: 35 c, 60% rh and 13 C, 44% rh during very light physical activity (1-2 Met) over a six-hour period. Sweating was suppressed approximately 40% by atropine and pralidoxime, and heart rate increased approximately 30 beats/min with drug treatment. At 13 C, all eight subjects completed 350 minutes of exposure in both drug and control experiments. Rectal temperature (t sub re) averaged 38.24 C in both treatments when subjects terminated their exposure at 35 C. Mean skin temperature averaged 37.42 C for both groups at termination. The treatment of subjects with atropine and pralidoxime when wearing chemical protective clothing does not adversely affect the length of time individuals can remain in a cool environment during very light work. However, the wearing of chemical protective clothing will decrease exposure time significantly (approx. 40%) in both control and drug treated subjects in a warm environment.

  6. Sedation management during therapeutic hypothermia for neonatal encephalopathy: atropine premedication for endotracheal intubation causes a prolonged increase in heart rate.

    Science.gov (United States)

    Gill, Hannah; Thoresen, Marianne; Smit, Elisa; Davis, Jonathan; Liu, Xun; Dingley, John; Elstad, Maja

    2014-10-01

    Heart rate (HR) plays an important role in the assessment of stress during therapeutic hypothermia (TH) for neonatal encephalopathy; we aimed to quantify the effect on HR of endotracheal (ET) intubation and drugs given to facilitate it. If atropine premedication independently increased HR, the main indicator of effective sedation, we hypothesised that increased sedation would have been given. Thirty-two, term, neonates recruited into a randomised pilot study comparing TH and TH combined with 50% Xenon inhalation were studied. Indications for ET intubation included: resuscitation at delivery, clinical need and elective re-intubation with a cuffed ET tube if randomised to Xenon. Standard intubation drugs comprised one or more of intravenous morphine, atropine, and suxamethonium. Local cooling guidelines were followed including morphine infusion for sedation. At postnatal hours five to eight atropine increased HR in a linear regression model (psedation given up to 8h into the treatment period was significantly higher (psedation and total morphine dose for sedation during early TH was increased where more than one dose of atropine was given. Bradycardia was not reported in any neonate, even without atropine premedication. We suggest that the use of atropine as part of standard premedication for ET intubation of term neonates undergoing TH should be reconsidered. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  7. A comparative study of clonidine versus a combination of diazepam and atropine for premedication in orthopaedic patients.

    Directory of Open Access Journals (Sweden)

    Chaurasia S

    1999-07-01

    Full Text Available Sixty patients in the age group of 18-60 years of A.S.A. Grade I/II risk, scheduled for elective orthopaedic surgeries under general anaesthesia were studied for pre-medication with either oral clonidine or with combination of effects of diazepam & atropine. Patients in Group A (clonidine group received tablet clonidine 100 mcg (1 tablet if less than 50 kg in weight and 200 mcg if weighing more than 50 kg two hours before surgery. Patients in Group B (Diazepam-atropine group received one tablet of Diazepam (10 mg orally two hours before surgery and injection atropine-sulphate 0.01 mg/kg half an hour preoperatively by intramuscular route. In our study, the sedative and anti-sialogogue effects of clonidine were comparable to those of diazepam-atropine combination, which are commonly used premedicants. The anti-anxiety effect of clonidine was found to be better than that of diazepam-atropine combination. Clonidine also proved to be a better agent for the attenuation of pressor response to laryngoscopy and intubation. Thus, oral clonidine is a better premedicant compared to atropine-diazepam combination. Also, it is a more acceptable agent because of its oral route of administration.

  8. Systemic delivery of atropine sulfate by the MicroDose Dry-Powder Inhaler.

    Science.gov (United States)

    Corcoran, T E; Venkataramanan, R; Hoffman, R M; George, M P; Petrov, A; Richards, T; Zhang, S; Choi, J; Gao, Y Y; Oakum, C D; Cook, R O; Donahoe, M

    2013-02-01

    Inhaled atropine is being developed as a systemic and pulmonary treatment for the extended recovery period after chemical weapons exposure. We performed a pharmacokinetics study comparing inhaled atropine delivery using the MicroDose Therapeutx Dry Powder Inhaler (DPIA) with intramuscular (IM) atropine delivery via auto-injector (AUTO). The MicroDose DPIA utilizes a novel piezoelectric system to aerosolize drug and excipient from a foil dosing blister. Subjects inhaled a 1.95-mg atropine sulfate dose from the dry powder inhaler on one study day [5 doses × 0.4 mg per dose (nominal) delivered over 12 min] and received a 2-mg IM injection via the AtroPen® auto-injector on another. Pharmacokinetics, pharmacodynamic response, and safety were studied for 12 hr. A total of 17 subjects were enrolled. All subjects completed IM dosing. One subject did not perform inhaled delivery due to a skin reaction from the IM dose. Pharmacokinetic results were as follows: area under the curve concentration, DPIA=20.1±5.8, AUTO=23.7±4.9 ng hr/mL (means±SD); maximum concentration reached, DPIA=7.7±3.5, AUTO=11.0±3.8 ng/mL; time to reach maximum concentration, DPIA=0.25±0.47, AUTO=0.19±0.23 hr. Pharmacodynamic results were as follows: maximum increase in heart rate, DPIA=18±12, AUTO=23±13 beats/min; average change in 1-sec forced expiratory volume at 30 min, DPIA=0.16±0.22 L, AUTO=0.11±0.29 L. The relative bioavailability for DPIA was 87% (based on output dose). Two subjects demonstrated allergic responses: one to the first dose (AUTO), which was mild and transient, and one to the second dose (DPIA), which was moderate in severity, required treatment with oral and intravenous (IV) diphenhydramine and IV steroids, and lasted more than 7 days. Dry powder inhalation is a highly bioavailable route for attaining rapid and consistent systemic concentrations of atropine.

  9. Atropine for the Prevention of Myopia Progression in Children: A Report by the American Academy of Ophthalmology.

    Science.gov (United States)

    Pineles, Stacy L; Kraker, Raymond T; VanderVeen, Deborah K; Hutchinson, Amy K; Galvin, Jennifer A; Wilson, Lorri B; Lambert, Scott R

    2017-12-01

    To review the published literature on the efficacy of topical atropine for the prevention of myopic progression in children. Literature searches were last conducted in December 2016 in the PubMed database with no date restrictions, but were limited to studies published in English, and in the Cochrane Library database without any restrictions. The combined searches yielded 98 citations, 23 of which were reviewed in full text. Of these, 17 articles were deemed appropriate for inclusion in this assessment and subsequently were assigned a level of evidence rating by the panel methodologist. Seventeen level I, II, and III studies were identified. Most of the studies reported less myopic progression in children treated with atropine compared with various control groups. All 8 of the level I and II studies that evaluated primarily myopic progression revealed less myopic progression with atropine (myopic progression ranging from 0.04±0.63 to 0.47±0.91 diopters (D)/year) compared with control participants (myopic progression ranging from 0.38±0.39 to 1.19±2.48 D/year). In studies that evaluated myopic progression after cessation of treatment, a rebound effect was noted. Several studies evaluated the optimal dosage of atropine with regard to myopic progression, rebound after treatment cessation, and minimization of side effects. Lower dosages of atropine (0.5%, 0.1%, and 0.01%) were found to be slightly less effective during treatment periods of 1 to 2 years, but they were associated with less rebound myopic progression (for atropine 0.01%, mean myopic progression after treatment cessation of 0.28±0.33 D/year, compared with atropine 0.5%, 0.87±0.52 D/year), fewer side effects, and similar long-term results for myopic progression after the study period and rebound effect were considered. The most robust and well-designed studies were carried out in Asian populations. Studies involving patients of other ethnic backgrounds failed to provide sufficient evidence of an

  10. Clinical study of a new therapy for nerve agent poisoning: Ascending dose tolerance study of HI-6 + atropine

    Energy Technology Data Exchange (ETDEWEB)

    Clement, J.G.; Madill, H.D.; Bailey, D.; Spence, J.D.

    1994-04-01

    This report details a double-blind, placebo controlled, ascending dose tolerance and pharmacokinetic study of HI-6 + atropine sulfate 2 mg in 24 healthy male volunteers. HI-6 was rapidly absorbed from an IM injection site. Maximum HI-6 plasma concentrations of 1.88, 4.96, 8.31 and 15.0 micrograms/mL were found 30-36 min after administration and maintained above 4 micrograms/mL concentration for 0, 39, 112 and 172.5 min following injection of 62.5, 125, 250 or 500 mg HI-6 + atropine (2 mg), respectively. The calculated half life of HI-6 was 78.2 min following 62.5 mg HI-6 + atropine dose and approximately 64-67 min following 125-500 mg HI-6 + atropine doses. Approximately 50% of the total dose of HI-6 was eliminated unchanged in the urine. There were significant changes (p < 0.05) in AST, CPK, creatinine and gamma GT following the 500 mg HI-6 + atropine dose but they were not considered to be clinically significant. Urinalysis, hematology and semen analysis over the 24 hr observation period was uneventful. There were no clinically significant changes in heart rate or ECG trace, respiration or blood pressure, visual and mental acuity following HI-6 + atropine. The various doses of HI-6 + atropine were well tolerated by the subjects as no serious clinical complaints were reported. With the rapid absorption and the lack of clinically significant side effects, combined with the superior efficacy against all nerve agents, HI-6 shows great promise as a replacement oxime in the therapy of nerve agent poisoning.

  11. Oxime and atropine failure to prevent intermediate syndrome development in acute organophosphate poisoning

    Directory of Open Access Journals (Sweden)

    Vučinić Slavica

    2013-01-01

    Full Text Available Introduction. Intermediate syndrome (IMS was described a few decades ago, however, there is still a controversy regarding its exact etiology, risk factors, diagnostic parameters and required therapy. Considering that acute poisonings are treated in different types of medical institutions this serious complication of organophosphate insecticide (OPI poisoning is frequently overlooked. The aim of this paper was to present a case of IMS in organophosphate poisoning, which, we believe, provides additional data on the use of oxime or atropine. Case report. After a well-resolved cholinergic crisis, the patient developed clinical presentation of IMS within the first 72 h from deliberate malathion ingestion. The signs of IMS were weakness of proximal limb muscles and muscles innervated by motor cranial nerves, followed by the weakness of respiratory muscles and serious respiratory insufficiency. Malathion and its active metabolite were confirmed by analytical procedure (liquid chromatography-mass spectrometry. Pralidoxime methylsulphate, adiministered as a continuous infusion until day 8 (total dose 38.4 g, and atropine until the day 10 (total dose 922 mg did not prevent the development of IMS, hence the mechanical ventilation that was stopped after 27 h had to be continued until the day 10. Conclusion. Continuous pralidoxime methylsulphate infusion with atropine did not prevent the development of IMS, most likely due to the delayed treatment and insufficient oxime dose but also because of chemical structure and lipophilicity of ingested OPI. A prolonged intensive care monitoring and respiratory care are the key management for the intermediate syndrome. [Projekat Ministarstva nauke Republike Srbije, br. OI 176018, No. 46009

  12. Anesthesia of captive African wild dogs (Lycaon pictus) using a medetomidine-ketamine-atropine combination.

    Science.gov (United States)

    Ward, David G; Blyde, David; Lemon, John; Johnston, Steve

    2006-06-01

    Seven captive male African wild dogs (Lycaon pictus) weighing 25-32 kg each, were anesthetized by i.m. injection via hand syringe with a combination of 1.5 mg/kg ketamine, 40 microg/kg medetomidine, and 0.05 mg/kg atropine. Following endotracheal intubation, each animal was connected to a bain closed-circuit system that delivered 1.5% isoflurane and 2 L/min oxygen. Atipamezole (0.1 mg/kg i.v.; 0.1 mg/kg i.m.) was given at the end of each procedure (60 min following injection of medetomidine/ketamine/atropine). Time to sternal recumbency was 5-8 min. Times to standing after atipamezole administration were 8-20 min. This anesthetic regimen was repeated on three separate occasions (September 2000, February 2002, and October 2002) on all males to perform electroejaculation procedures. Each procedure was Dogs showed excellent muscle relaxation during the procedures. Arterial blood samples were collected at 10-min intervals for blood gases in one procedure (September 2000). Separate venous samples were taken from each dog during each procedure for hematology and biochemistry. These values were within the normal range for this species. Arterial hemoglobin oxygen saturation (SpO2) and heart rate (HR) were monitored continuously in addition to other anesthesia monitoring procedures (body temperature, respiratory rate [RR], capillary refill time, blink response, pupil position, deep pain perception reflex). All dogs maintained relatively stable SpO2 profiles during monitoring, with a mean (+/-SD) SpO2 of 92% +/-5.4%. All other physiological variables (HR, RR, body temperature, blood pressure) were within normal limits. Following each procedure, normal behavior was noted in all dogs. All the dogs were reunited into the pack at completion of their anesthetic procedures. An injectable medetomidine-ketamine-atropine combination with maintenance by gaseous isoflurane and oxygen provides an inexpensive, reliable anesthetic for captive African wild dogs.

  13. Atropine and ODQ antagonize tetanic fade induced by L-arginine in cats

    Directory of Open Access Journals (Sweden)

    J.M. Cruciol-Souza

    1999-10-01

    Full Text Available Although it has been demonstrated that nitric oxide (NO released from sodium nitrite induces tetanic fade in the cat neuromuscular preparations, the effect of L-arginine on tetanic fade and its origin induced by NO have not been studied in these preparations. Furthermore, atropine reduces tetanic fade induced by several cholinergic and anticholinergic drugs in these preparations, whose mechanism is suggested to be mediated by the interaction of acetylcholine with inhibitory presynaptic muscarinic receptors. The present study was conducted in cats to determine the effects of L-arginine alone or after pretreatment with atropine or 1H-[1,2,4]oxadiazole [4,3-a]quinoxalin-1-one (ODQ on neuromuscular preparations indirectly stimulated at high frequency. Drugs were injected into the middle genicular artery. L-arginine (2 mg/kg and S-nitroso-N-acetylpenicillamine (SNAP; 16 µg/kg induced tetanic fade. The Nw-nitro-L-arginine (L-NOARG; 2 mg/kg alone did not produce any effect, but reduced the tetanic fade induced by L-arginine. D-arginine (2 mg/kg did not induce changes in tetanic fade. The tetanic fade induced by L-arginine or SNAP was reduced by previous injection of atropine (1.0 µg/kg or ODQ (15 µg/kg. ODQ alone did not change tetanic fade. The data suggest that the NO-synthase-GC pathway participates in the L-arginine-induced tetanic fade in cat neuromuscular preparations. The tetanic fade induced by L-arginine probably depends on the action of NO at the presynaptic level. NO may stimulate guanylate cyclase increasing acetylcholine release and thereby stimulating presynaptic muscarinic receptors.

  14. Investigating and comparing effects of atropine and physostigmine in peripheral pain examination due to formalin injection on rats

    Directory of Open Access Journals (Sweden)

    Mohammad Pourahmadi

    2016-07-01

    Full Text Available There areseveral neurotransmittersat feel the pain and processing nervoussystem, and until now cholinergic system has not been well studied in this field. The purpose of this research is investigating effects of atropine and physostigmine on the response of formalin pain test. We divided 50 male wistar head rats into 5 groups , first group ( saline normal injection 5 µ , second group ( 1% formalin injection into 50 µ , third group ( physostigmine injection 0/1 mg / kg , fourth group (atropine injection 2 mg / kg , fifth group ( atropine injection 2 mg / kg and physostigmine 0/1 mg/kg , after formalin injection , the animals were placed inside mirror pain machine and it was recorded pain response at the time ranges 0-5 and 15-45 . Results investigated with spss software and ANOVA and Duncan’s test. Formalin injection causes pain response in both time ranges. Atropine injection alone had no effect on pain response. Physostigmine effect alone, with a significant reduction (p< 0/05 in the number of foot motions in both stage and duration causesof licking and biting in the 15-45 minutes stage . Atropine and physostigmine injections in fifth group cause significant reduction in the number of foot motions and duration of licking and biting in the time range of 15-45 minutes.Perhaps there is a close relationship between cholinergic system and peripheral pain that can be taken through the action of muscarinic receptors.

  15. Clinical study of a new therapy for nerve agent poisoning: Ascending dose tolerance study of HI-6 + atropine

    Energy Technology Data Exchange (ETDEWEB)

    Clement, J.G.; Bailey, D.G.; Madill, H.D.; Spence, J.D.

    1993-05-13

    HI-6 was rapidly absorbed from an IM injection site. Maximum HI-6 plasma concentrations of 1.88, 4.96, 8.31 15.0 ug/ml were found 28-36 min after administration and maintained above 4 ug/ml concentration for 0, 39, 112 172.5 min following administration of 62.5, 125, 250 or 500 mg HI-6 + atropine (2 mg), respectively. The calculated half life of HI-6 was 78.2 min following 62.5 mg HI-6 + atropine dose and approximately 64-67 min following 125-500 mg HI-6 + atropine doses. Approximately 50 % of the total dose of HI-6 was eliminated unchanged in the urine. There were significant changes (p < 0.05) in AST, CPK, creatinine and gamma GT following the 500 mg HI-6 + atropine dose but they were not considered to be clinically significant. Urinalysis, hematology and semen analysis over the 24 hr observation period was uneventful. There were no clinically significant changes in heart rate or ECG trace, respiration or blood pressure, visual and mental acuity following HI-6 + atropine.

  16. Atropine Ophthalmic

    Science.gov (United States)

    ... following symptoms, call your doctor immediately: fever irritability fast pulse irregular heartbeat mental confusion difficulty urinating If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting ...

  17. Intravenously administered oxotremorine and atropine, in doses known to affect pain threshold, affect the intraspinal release of acetylcholine in rats

    DEFF Research Database (Denmark)

    Abelson, Klas S P; Höglund, A Urban

    2002-01-01

    /kg). Spinal microdialysis probes were placed intraspinally at approximately the C2-C5 spinal level for sampling of acetylcholine and dialysis delivery of atropine (0.1, 1, 10 nM). Additionally, the tail-flick behaviour was tested on conscious rats injected intraperitoneally with saline, atropine (10, 100...... muscarinic agonists and antagonists modify nociceptive threshold by affecting intraspinal release of acetylcholine (ACh). Catheters were inserted into the femoral vein in rats maintained on isoflurane anaesthesia for administration of oxotremorine (10-300 microg/kg) and atropine (0.1, 10, 5000 microg...... and 5000 microg/kg), or subcutaneously with oxotremorine (30, 100, 300 microg/kg). Subcutaneous administration of oxotremorine (30, 100, 300 microg/kg) significantly increased the tail-flick latency. These doses of oxotremorine dose-dependently increased the intraspinal release of acetylcholine...

  18. Antimuscarinic-induced convulsions in fasted animals after food intake: evaluation of the effects of levetiracetam, topiramate and different doses of atropine.

    Science.gov (United States)

    Büget, Bahar; Türkmen, Aslı Zengin; Allahverdiyev, Oruc; Enginar, Nurhan

    2016-01-01

    This study evaluated the effects of different doses of atropine and new antiepileptics, levetiracetam and topiramate, on the development of convulsions triggered by food intake in antimuscarinic-treated fasted animals. Mice deprived of food for 24 h and treated i.p. with atropine at a dose of 2.4 or 24 mg/kg developed convulsions after being allowed to eat ad libitum. No convulsions were observed in fasted animals treated with 0.24 mg/kg atropine. There was no difference in the incidence of convulsions between the two atropine treatments, but latency to convulsions was longer in 24 mg/kg atropine treated animals. The lowest dose of atropine, 0.24 mg/kg, caused stage 1 and stage 2 activity, but did not provide the convulsive endpoint (stage 3, 4, 5 activity). Administration of levetiracetam (50 or 200 mg/kg) or topiramate (50 or 100 mg/kg) to another group of 24-h fasted mice was ineffective in reducing the incidence of convulsions developed in the animals after 2.4 mg/kg atropine treatment and food intake. However, the higher dose of levetiracetam prolonged the onset of convulsions. Present results demonstrated the efficacy of low and high doses of atropine on the development of convulsions in fasted animals and provided additional evidence for the ineffectiveness of antiepileptic treatment in these seizures.

  19. Electrochemical determination of atropine at multi-wall carbon nanotube electrode based on the enhancement effect of sodium dodecyl benzene sulfonate.

    Science.gov (United States)

    Dar, Riyaz Ahmad; Brahman, Pradeep Kumar; Tiwari, Sweety; Pitre, Krishna Sadashiv

    2012-03-01

    Herein, a new electrochemical method was described for the determination of atropine based on the enhancement effect of an anionic surfactant: sodium dodecyl benzene sulfonate (SDBS). In pH 10.5 tetramethyl ammonium hydroxide as supporting electrolyte and in the presence of 0.4×10(-4)M SDBS, atropine yields a well-defined and sensitive oxidation peak at the multi-wall carbon nanotube electrode (MWCNTE). Compared with that in the absence of SDBS, the oxidation peak current of atropine remarkably increases in the presence of SDBS. The experimental parameters, such as supporting electrolyte, concentration of SDBS, and accumulation time, were optimized for atropine determination. The oxidation peak current is proportional to the concentration of atropine over the range from 3.98 ng/ml to 27.23 ng/ml. The detection limit is 0.449 ng/ml after 2 min of accumulation. This new voltammetric method was successfully used to determine atropine in Indian traditional medicine (seeds and leaves of Datura stramonium) with satisfactory recoveries. The developed method was also used for the analysis of atropine in pharmaceutical formulation of ophthalmic solution (eye drop). The relative standard deviations of intraday and interday analyses for atropine were 0.67% and 0.86% respectively (n=3) for the accumulation time of 120 s. Copyright © 2011 Elsevier B.V. All rights reserved.

  20. Ready-to-use pre-filled syringes of atropine for anaesthesia care in French hospitals - a budget impact analysis.

    Science.gov (United States)

    Benhamou, Dan; Piriou, Vincent; De Vaumas, Cyrille; Albaladejo, Pierre; Malinovsky, Jean-Marc; Doz, Marianne; Lafuma, Antoine; Bouaziz, Hervé

    2017-04-01

    Patient safety is improved by the use of labelled, ready-to-use, pre-filled syringes (PFS) when compared to conventional methods of syringe preparation (CMP) of the same product from an ampoule. However, the PFS presentation costs more than the CMP presentation. To estimate the budget impact for French hospitals of switching from atropine in ampoules to atropine PFS for anaesthesia care. A model was constructed to simulate the financial consequences of the use of atropine PFS in operating theatres, taking into account wastage and medication errors. The model tested different scenarios and a sensitivity analysis was performed. In a reference scenario, the systematic use of atropine PFS rather than atropine CMP yielded a net one-year budget saving of €5,255,304. Medication errors outweighed other cost factors relating to the use of atropine CMP (€9,425,448). Avoidance of wastage in the case of atropine CMP (prepared and unused) was a major source of savings (€1,167,323). Significant savings were made by means of other scenarios examined. The sensitivity analysis suggests that the results obtained are robust and stable for a range of parameter estimates and assumptions. The financial model was based on data obtained from the literature and expert opinions. The budget impact analysis shows that even though atropine PFS is more expensive than atropine CMP, its use would lead to significant cost savings. Savings would mainly be due to fewer medication errors and their associated consequences and the absence of wastage when atropine syringes are prepared in advance. Copyright © 2016 Société française d'anesthésie et de réanimation (Sfar). Published by Elsevier Masson SAS. All rights reserved.

  1. Leaching of zinc compound from rubber stoppers into the contents of automatic atropine injectors.

    Science.gov (United States)

    Ellin, R I; Kaminskis, A; Zvirblis, P; Sultan, W E; Shutz, M B; Matthews, R

    1985-07-01

    This report describes how a material within the cartridge of an automatic injector contaminated its contents. On prolonged storage, a formulation that contained atropine produced lethality in mice. The toxic material originated from zinc compounds that were present in the rubber stopper and plunger of the container and that subsequently leached into the formulation. The contents of cartridges that contained greater than or equal to 0.75 mg/mL of solubilized zinc were lethal to at least 20% of the mice tested; those that contained 0.42 mg/mL showed no lethality. The problem resulted from the physicochemical properties of the rubber, not the concentration of zinc used in the vulcanization process.

  2. Effect of remifentanil with and without atropine on heart rate variability and RR interval in children.

    Science.gov (United States)

    Tirel, O; Chanavaz, C; Bansard, J Y; Carré, F; Ecoffey, C; Senhadji, L; Wodey, E

    2005-10-01

    Remifentanil can cause bradycardia either by parasympathetic activation or by other negative chronotropic effects. The high frequency (HF) component of heart rate variability (HRV) is a marker of parasympathetic activity. This study aimed to evaluate the effect of remifentanil on RR interval and on HRV in children. Forty children ASA I or II were studied after approval by the human studies committee and informed parental consent was obtained. After stabilisation at sevoflurane 1 MAC, they were randomly divided into two groups: one received a 20 microg.kg(-1) atropine injection (AT + REMI) and the other ringer lactate solution (REMI). Three minutes later, a 1 microg.kg(-1) bolus of remifentanil was administered over 1 min, followed by a continual infusion at 0.25 microg.kg(-1).min(-1) for 10 min increased to 0.5 microg.kg(-1).min(-1) for a further 10 min. A time varying, autoregressive analysis of RR sequences was used to estimate classical spectral parameters: low (0.04-0.15 Hz; LF) and high (0.15-0.45 Hz; HF) frequency, whereas the root mean square of successive differences of RR intervals (rmssd) was derived directly from the temporal sequence. Statistical analyses were conducted by means of the multiple correspondence analysis and with non parametrical tests. Remifentanil induced an RR interval lengthening, i.e. bradycardia, in both groups compared to pretreatment values and was associated with an increase of HF and rmssd only for the REMI group. The parasympathetic inhibition by atropine did not totally prevent remifentanil's negative chronotropic effect. A direct negative chronotropic effect of remifentanil is proposed.

  3. Pharmacokinetic analysis of pralidoxime after its intramuscular injection alone or in combination with atropine-avizafone in healthy volunteers.

    Science.gov (United States)

    Abbara, C; Rousseau, J M; Lelièvre, B; Turcant, A; Lallement, G; Ferec, S; Bardot, I; Diquet, B

    2010-12-01

    Treatment of organophosphate poisoning with pralidoxime needs to be improved. Here we have studied the pharmacokinetics of pralidoxime after its intramuscular injection alone or in combination with avizafone and atropine using an auto-injector device. The study was conducted in an open, randomized, single-dose, two-way, cross-over design. At each period, each subject received either intramuscular injections of pralidoxime (700 mg), or two injections of the combination: pralidoxime (350 mg), atropine (2 mg), avizafone (20 mg). Pralidoxime concentrations were quantified using a validated LC/MS-MS method. Two approaches were used to analyse these data: (i) a non-compartmental approach; and (ii) a compartmental modelling approach. The injection of pralidoxime combination with atropine and avizafone provided a higher pralidoxime maximal concentration than that obtained after the injection of pralidoxime alone (out of bioequivalence range), while pralidoxime AUC values were equivalent. Pralidoxime concentrations reached their maximal value earlier after the injection of the combination. According to Akaike and to goodness of fit criteria, the best model describing the pharmacokinetics of pralidoxime was a two-compartment with a zero-order absorption model. When avizafone and atropine were injected with pralidoxime, the best model describing pralidoxime pharmacokinetics becomes a two-compartment with a first-order absorption model. The two approaches, non-compartmental and compartmental, showed that the administration of avizafone and atropine with pralidoxime results in a faster absorption into the general circulation and higher maximal concentrations, compared with the administration of pralidoxime alone. © 2010 The Authors. British Journal of Pharmacology © 2010 The British Pharmacological Society.

  4. Addition of atropine to submaximal exercise stress testing in patients evaluated for suspected ischaemia with SPECT imaging: a randomized, placebo-controlled trial

    Energy Technology Data Exchange (ETDEWEB)

    Manganelli, Fiore; Sauro, Rosario; Di Lorenzo, Emilio; Rosato, Giuseppe [San Giuseppe Moscati Hospital, Department of Cardiology and Heart Surgery, Avellino (Italy); Spadafora, Marco; Varrella, Paola; Peluso, Giuseppina [San Giuseppe Moscati Hospital, Nuclear Medicine Unit, Avellino (Italy); Daniele, Stefania [Institute of Diagnostic and Nuclear Development (SDN), Naples (Italy); Cuocolo, Alberto [Institute of Diagnostic and Nuclear Development (SDN), Naples (Italy); University Federico II, Department of Biomorphological and Functional Sciences, Naples (Italy); National Council of Research, Institute of Biostructures and Bioimages, Naples (Italy)

    2011-02-15

    To evaluate the effects of the addition of atropine to exercise testing in patients who failed to achieve their target heart rate (HR) during stress myocardial perfusion imaging with single-photon emission computed tomography (SPECT). The study was a prospective, randomized, placebo-controlled design. Patients with suspected or known coronary artery disease who failed to achieve a target HR ({>=}85% of maximal predicted HR) during exercise SPECT imaging were randomized to receive intravenous atropine (n = 100) or placebo (n = 101). The two groups of patients did not differ with respect to demographic or clinical characteristics. A higher proportion of patients in the atropine group achieved the target HR compared to the placebo group (60% versus 3%, p < 0.0001). SPECT imaging was abnormal in a higher proportion of patients in the atropine group as compared to the placebo group (57% versus 42%, p < 0.05). Stress-induced myocardial ischaemia was present in more patients in the atropine group as compared to placebo (47% versus 29%, p < 0.01). In both groups of patients, no major side effects occurred. The addition of atropine at the end of exercise testing is more effective than placebo in raising HR to adequate levels, without additional risks of complications. The use of atropine in patients who initially failed to achieve their maximal predicted HR is associated with a higher probability of achieving a diagnostic myocardial perfusion study. (orig.)

  5. Assessment of drug content uniformity of atropine sulfate triturate by liquid chromatography-tandem mass spectrometry, X-ray powder diffraction, and Raman chemical imaging.

    Science.gov (United States)

    Moriyama, Kei; Takami, Yoichiro; Uozumi, Natsuki; Okuda, Akiko; Yamashita, Mayumi; Yokomizo, Rie; Shimada, Kenichi; Egawa, Takashi; Kamei, Takehito; Takayanagi, Kazunobu

    2016-01-01

    Atropine sulfate is an anticholinergic agent for treatment of hypertrophic pyloric stenosis and is orally administrated as a triturate with lactose hydrate. Because of the low safety margin of atropine sulfate, triturate uniformity is a key safety factor. In this study, we assessed the uniformity of atropine sulfate in 1000-fold triturates prepared by wet mixing and dry mixing methods and discussed the cause of the difference in uniformity between two preparation methods. A 1000-fold triturate of atropine sulfate with lactose hydrate was prepared by two different methods: wet mixing and dry mixing. The wet mixing was performed according to Kurashiki Central Hospital protocol and the dry mixing was a simple physical mixing by a rocking mixer. The uniformity of atropine sulfate content in aliquots of a 1000-fold triturate with lactate hydrate was assessed by liquid chromatography-tandem mass spectrometry (LC-MS/MS) quantification. Solid-state analyses of the triturates by Raman chemical imaging and X-ray powder diffraction (XRPD) were performed to investigate the difference in uniformity. The LC-MS/MS quantification showed that the uniformity of atropine sulfate in the 1000-fold triturate was excellent for wet mixing but was significantly variable for dry mixing. On the basis of the Raman chemical imaging and XRPD analyses, it was indicated that an amorphous thin film of atropine sulfate coated the surfaces of the lactose hydrate particles during wet mixing and contributed to the uniformity of the triturate. In contrast, clusters of the crystalline atropine sulfate were found in the dry mixing samples. The results showed that better atropine sulfate triturate uniformity was achieved using the wet mixing method rather than the dry method and the cause of the uniformity difference between two mixing methods was indicated by the multilateral assessment.

  6. Analysis of atropine, its degradation products and related substances of natural origin by means of reversed-phase high-performance liquid chromatography.

    Science.gov (United States)

    Kirchhoff, C; Bitar, Y; Ebel, S; Holzgrabe, U

    2004-08-13

    Chromatographic separation and quantification methods of tropa alkaloids were often described. In order to separate atropine from its degradation products ion-pair chromatography (IPC) has been frequently applied. Beside long equilibration times IPC often suffers from poor robustness. The aim of this study was to develop robust and simple HPLC methods for both stability testing of atropine solutions and limitation of related substances in atropine from plant material. Using a hydrophilic embedded RP18 column and a gradient elution gave baseline separation of all components.

  7. Isolation of atropine and scopolamine from plant material using liquid-liquid extraction and EXtrelut® columns.

    Science.gov (United States)

    Śramska, Paula; Maciejka, Artur; Topolewska, Anna; Stepnowski, Piotr; Haliński, Łukasz P

    2017-02-01

    Tropane alkaloids are toxic secondary metabolites produced by Solanaceae plants. Among them, plants from Datura genus produce significant amounts of scopolamine and hyoscyamine; the latter undergoes racemization to atropine during isolation. Because of their biological importance, toxic properties and commonly reported food and animal feed contamination by different Datura sp. organs, there is a constant need for reliable methods for the analysis of tropane alkaloids in many matrices. In the current study, three extraction and sample-clean up procedures for the determination of scopolamine and atropine in plant material were compared in terms of their effectiveness and repeatability. Standard liquid-liquid extraction (LLE) and EXtrelut® NT 3 columns were used for the sample clean-up. Combined ultrasound-assisted extraction and 24h static extraction using ethyl acetate, followed by multiple LLE steps was found the most effective separation method among tested. However, absolute extraction recovery was relatively low and reached 45-67% for atropine and 52-73% for scopolamine, depending on the compound concentration. The same method was also the most effective one for the isolation of target compounds from Datura stramonium leaves. EXtrelut® columns, on the other hand, displayed relatively low effectiveness in isolating atropine and scopolamine from such a complex matrix and hence could not be recommended. The most effective method was also applied to the extraction of alkaloids from roots and stems of D. stramonium. Quantitative analyses were performed using validated method based on gas chromatography with flame ionization detector (GC-FID). Based on the results, the importance of the proper selection of internal standards in the analysis of tropane alkaloids was stressed out. Copyright © 2016 Elsevier B.V. All rights reserved.

  8. Acute and chronic effects of glucose and carbachol on insulin secretion and phospholipase C activation: studies with diazoxide and atropine.

    Science.gov (United States)

    Yamazaki, Hanae; Philbrick, William; Zawalich, Kathleen C; Zawalich, Walter S

    2006-01-01

    The acute and chronic effects of 20 mM glucose and 10 microM carbachol on beta-cell responses were investigated. Acute exposure of rat islets to 20 mM glucose increased glucose usage rates and resulted in a large insulin-secretory response during a dynamic perifusion. The secretory, but not the metabolic, effect of 20 mM glucose was abolished by simultaneous exposure to 100 microM diazoxide. Glucose (20 mM) significantly increased inositol phosphate (IP) accumulation, an index of phospholipase C (PLC) activation, from [(3)H]inositol-prelabeled islets. Diazoxide, but not atropine, abolished this effect as well. Unlike 20 mM glucose, 10 microM carbachol (in the presence of 5 mM glucose) increased IP accumulation but had no effect on insulin secretion or glucose (5 mM) metabolism. The IP effect was abolished by 50 microM atropine but not by diazoxide. Chronic 3-h exposure of islets to 20 mM glucose or 10 microM carbachol profoundly reduced both the insulin-secretory and PLC responses to a subsequent 20 mM glucose stimulus. The adverse effects of chronic glucose exposure were abolished by diazoxide but not by atropine. In contrast, the adverse effects of carbachol were abolished by atropine but not by diazoxide. Prior 3 h of exposure to 20 mM glucose or carbachol had no inhibitory effect on glucose metabolism. Significant secretory responses could be evoked from 20 mM glucose- or carbachol-pretreated islets by the inclusion of forskolin. These findings support the concept that an early event in the evolution of beta-cell desensitization is the impaired activation of islet PLC.

  9. Highly sensitive determination of atropine using cobalt oxide nanostructures: Influence of functional groups on the signal sensitivity

    Energy Technology Data Exchange (ETDEWEB)

    Soomro, Razium Ali, E-mail: raziumsoomro@gmail.com [Interface Analysis Centre, School of Physics, University of Bristol, Bristol, BS8 1TL (United Kingdom); National Centre of Excellence in Analytical Chemistry, University of Sindh, Jamshoro, 76080 (Pakistan); Nafady, Ayman [Department of Chemistry, College of Science, King Saud University, Riyadh (Saudi Arabia); Department of Chemistry, Faculty of Science, Sohag University, Sohag (Egypt); Hallam, Keith Richard [Interface Analysis Centre, School of Physics, University of Bristol, Bristol, BS8 1TL (United Kingdom); Jawaid, Sana [National Centre of Excellence in Analytical Chemistry, University of Sindh, Jamshoro, 76080 (Pakistan); Al Enizi, Abdullah [Department of Chemistry, College of Science, King Saud University, Riyadh (Saudi Arabia); Sherazi, Syed Tufail Hussain; Sirajuddin [National Centre of Excellence in Analytical Chemistry, University of Sindh, Jamshoro, 76080 (Pakistan); Ibupoto, Zafar Hussain [Dr M.A. Kazi Institute of Chemistry, University of Sindh, Jamshoro, 76080 (Pakistan); Willander, Magnus [Department of Science and Technology, Campus Norrkoping, Linkoping University, SE-60174, Norrkoping (Sweden)

    2016-12-15

    This study describes sensitive determination of atropine using glassy carbon electrodes (GCE) modified with Co{sub 3}O{sub 4} nanostructures. The as-synthesised nanostructures were grown using cysteine (CYS), glutathione (GSH) and histidine (HYS) as effective templates under hydrothermal action. The obtained morphologies revealed interesting structural features, including both cavity-based and flower-shaped structures. The as-synthesised morphologies were noted to actively participate in electro-catalysis of atropine (AT) drug where GSH-assisted structures exhibited the best signal response in terms of current density and over-potential value. The study also discusses the influence of functional groups on the signal sensitivity of atropine electro-oxidation. The functionalisation was carried with the amino acids originally used as effective templates for the growth of Co{sub 3}O{sub 4} nanostructures. The highest increment was obtained when GSH was used as the surface functionalising agent. The GSH-functionalised Co{sub 3}O{sub 4}-modified electrode was utilised for the electro-chemical sensing of AT in a concentration range of 0.01–0.46 μM. The developed sensor exhibited excellent working linearity (R{sup 2} = 0.999) and signal sensitivity up to 0.001 μM of AT. The noted high sensitivity of the sensor is associated with the synergy of superb surface architectures and favourable interaction facilitating the electron transfer kinetics for the electro-catalytic oxidation of AT. Significantly, the developed sensor demonstrated excellent working capability when used for AT detection in human urine samples with strong anti-interference potential against common co-existing species, such as glucose, fructose, cysteine, uric acid, dopamine and ascorbic acid. - Highlights: • Template-assisted growth of Co{sub 3}O{sub 4} nanostructures. • Shape-dependent electro-catalysis of atropine. • Effect of functionalisation of signal sensitivity.

  10. Hawthorn (Crataegus monogyna Jacq.) extract exhibits atropine-sensitive activity in a cultured cardiomyocyte assay.

    Science.gov (United States)

    Salehi, Satin; Long, Shannon R; Proteau, Philip J; Filtz, Theresa M

    2009-01-01

    Hawthorn (Crataegus spp.) plant extract is used as a herbal alternative medicine for the prevention and treatment of various cardiovascular diseases. Recently, it was shown that hawthorn extract preparations caused negative chronotropic effects in a cultured neonatal murine cardiomyocyte assay, independent of beta-adrenergic receptor blockade. The aim of this study was to further characterize the effect of hawthorn extract to decrease the contraction rate of cultured cardiomyocytes. To test the hypothesis that hawthorn is acting via muscarinic receptors, the effect of hawthorn extract on atrial versus ventricular cardiomyocytes in culture was evaluated. As would be expected for activation of muscarinic receptors, hawthorn extract had a greater effect in atrial cells. Atrial and/or ventricular cardiomyocytes were then treated with hawthorn extract in the presence of atropine or himbacine. Changes in the contraction rate of cultured cardiomyocytes revealed that both muscarinic antagonists significantly attenuated the negative chronotropic activity of hawthorn extract. Using quinuclidinyl benzilate, L-[benzylic-4,4'-(3)H] ([(3)H]-QNB) as a radioligand antagonist, the effect of a partially purified hawthorn extract fraction to inhibit muscarinic receptor binding was quantified. Hawthorn extract fraction 3 dose-dependently inhibited [(3)H]-QNB binding to mouse heart membranes. Taken together, these findings suggest that decreased contraction frequency by hawthorn extracts in neonatal murine cardiomyocytes may be mediated via muscarinic receptor activation.

  11. Intravenous and inhalation toxicokinetics of sarin stereoisomers in atropinized guinea pigs.

    Science.gov (United States)

    Spruit, H E; Langenberg, J P; Trap, H C; van der Wiel, H J; Helmich, R B; van Helden, H P; Benschop, H P

    2000-12-15

    We report the first toxicokinetic studies of (+/-)-sarin. The toxicokinetics of the stereoisomers of this nerve agent were studied in anesthetized, atropinized, and restrained guinea pigs after intravenous bolus administration of a dose corresponding to 0.8 LD50 and after nose-only exposure to vapor concentrations yielding 0.4 and 0.8 LCt50 in an 8-min exposure time. During exposure the respiratory minute volume and frequency were monitored. Blood samples were taken for gas chromatographic analysis of the nerve agent stereoisomers and for measurement of the activity of blood acetylcholinesterase (AChE). In all experiments, the concentration of (+)-sarin was below the detection limit (sarin, after an intravenous bolus was adequately described with a two-exponential equation. (-)-Sarin is distributed ca. 10-fold faster than C(-)P(-)-soman, whereas its elimination proceeds almost 10-fold slower. During nose-only exposure to 0.4 and 0.8 LCt50 of (+/-)-sarin in 8 min, (-)-sarin appeared to be rapidly absorbed. The blood AChE activity decreased during the exposure period to ca. 15 and 70% of control activity, respectively. There were no effects on the respiratory parameters. A significant nonlinearity of the toxicokinetics with dose was observed for the respiratory experiments. Copyright 2000 Academic Press.

  12. Use of atropine to predict the accommodative component in esotropia with hypermetropia

    Directory of Open Access Journals (Sweden)

    Mihir Kothari

    2011-01-01

    Full Text Available This cohort study included children with esotropia and hypermetropia of ≥ +2.0 diopters (D. The deviation was measured at presentation, under atropine cycloplegia and 3 months after full refractive correction. Of 44 children with a mean age of 5.2 ± 2.4 years, 25 were males. Eighteen (41% had fully refractive accommodative esotropia (RAE, 10 (23% had partial accommodative esotropia (PAE, and 5 (11% had nonaccommodative esotropia (NAE. Eleven (25% had convergence excess (CE. Under cycloplegia, all with RAE and RAE with CE had orthotropia. There was no significant change in the deviation in the patients with NAE. The deviation under cycloplegia and that with full refractive correction in PAE and PAE with CE (with +3.0 D addition were not different. The intraclass correlation coefficient for deviation under cycloplegia and after full refractive correction (+3.0 D addition for CE was 0.89. It was concluded that ocular deviation under cycloplegia can help to predict the accommodative component in esotropia with hypermetropia.

  13. Determination of atropine sulfate using a novel sensitive DNA-biosensor based on its interaction on a modified pencil graphite electrode.

    Science.gov (United States)

    Ensafi, Ali A; Nasr-Esfahani, Parisa; Heydari-Bafrooei, Esmaeil; Rezaei, B

    2015-01-01

    A novel, selective, rapid and simple electrochemical method is developed for the determination of atropine sulfate. UV-Vis and differential pulse voltammetry are used to study the interaction of atropine sulfate with salmon sperm ds-DNA on the surface of salmon sperm ds-DNA modified-pencil graphite electrode (PGE). For this purpose, a pencil graphite electrode (PGE) modified with multiwall carbon nanotubes (MWCNTs), titanium dioxide nanoparticles (TiO2NPs), and poly-dialyldimethylammonium chloride (PDDA) decorated with ds-DNA is tested for the determination of atropine sulfate. The electrochemical oxidation peak current of adenine and guanine bonded on the surface of ds-DNA/PDDA-TiO2NPs-MWCNTs/PGE is used to obtain the analytical signal. Decreases in the intensities of guanine and adenine oxidation signals after their interaction with atropine sulfate are used as indicator signals for the sensitive determination of atropine sulfate. Using ds-DNA/PDDA-TiO2NPs-MWCNTs/PGE and based on the guanine signal, linear calibration curves were obtained in the range of 0.6 to 30.0 μmol L(-1) and 30.0 to 600.0 μmol L(-1) atropine sulfate with low detection limits of 30.0 nmol L(-1). The biosensor shows a good selectivity for the determination of atropine sulfate. Finally, the applicability of the biosensor is evaluated by measuring atropine sulfate in real samples with good accuracy. Copyright © 2014 Elsevier B.V. All rights reserved.

  14. Enantiomeric differentiation of atropine/hyoscyamine by (13) C NMR spectroscopy and its application to Datura stramonium extract.

    Science.gov (United States)

    Antoine Lanfranchi, Don; Tomi, Félix; Casanova, Joseph

    2010-01-01

    The two enantiomers of hyoscyamine, an alkaloid found in many plant species, have distinct pharmacological and biological properties. Methods for the discrimination of both enantiomers are almost exclusively based on chiral HPLC/UV. Determination of the enantiomeric ratio (e.r.) of hyoscyamine is a challenging problem since this compound tends to racaemise, forming atropine during acid-base extraction. To develop a protocol for the calculation of enantiomeric ratio of hyoscyamine in a plant extract using a (13) C NMR method. Samples were prepared by extraction of dried Datura stramonium seeds. Observation of C12 and C15 NMR signals of hyoscyamine in the presence of one equivalent of TFA and sub-stoichiometric amount of Yb(hfc)(3) allowed the calculation of the e.r. of S-(-) and R-(+)-hyoscyamine.The method was optimised with various mixtures of (+) and (-)-hyoscyamine ranging from 50:50 (racaemic mixture, i.e. atropine) to 98.5:1.5. The e.r. measured by NMR on the signals of aromatic C12 and C15 were in agreement with the gravimetrically prepared samples. The method was then applied to an extract of Datura stramonium and S-(-)-hyoscyamine was the unique enantiomer. The study showed that the e.r. determination of atropine/hyoscyamine was achieved with a routine NMR spectrometer, using CLSR/TFA on pure compounds as well as on the crude extract of Datura stramonium. Copyright © 2010 John Wiley & Sons, Ltd.

  15. Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.

    Science.gov (United States)

    Bhattacharjee, Apurba K; Pomponio, James W; Evans, Sarah A; Pervitsky, Dmitry; Gordon, Richard K

    2013-05-01

    Muscarinic acetylcholine receptors (mAChRs) have five known subtypes which are widely distributed in both the peripheral and central nervous system for regulation of a variety of cholinergic functions. Atropine is a well known muscarinic subtype non-specific antagonist that competitively inhibits acetylcholine (ACh) at postganglionic muscarinic sites. Atropine is used to treat organophosphate (OP) poisoning and resulting seizures in the warfighter because it competitively inhibits acetylcholine (ACh) at the muscarinic cholinergic receptors. ACh accumulates due to OP inhibition of acetylcholinesterase (AChE), the enzyme that hydrolyzes ACh. However, atropine produces several unwanted side-effects including dilated pupils, blurred vision, light sensitivity, and dry mouth. To overcome these side-effects, our goal was to find an alternative to atropine that emphasizes M1 (seizure prevention) antagonism but has minimum M2 (cardiac) and M3 (e.g., eye) antagonism so that an effective less toxic medical countermeasure may be developed to protect the warfighter against OP and other chemical warfare agents (CWAs). We adopted an in silico pharmacophore modeling strategy to develop features that are characteristics of known M1 subtype-selective compounds and used the model to identify several antagonists by screening an in-house (WRAIR-CIS) compound database. The generated model for the M1 selectivity was found to contain two hydrogen bond acceptors, one aliphatic hydrophobic, and one ring aromatic feature distributed in a 3D space. From an initial identification of about five hundred compounds, 173 compounds were selected through principal component and cluster analyses and in silico ADME/Toxicity evaluations. Next, these selected compounds were evaluated in a subtype-selective in vitro radioligand binding assay. Twenty eight of the compounds showed antimuscarinic activity. Nine compounds showed specificity for M1 receptors and low specificity for M3 receptors. The p

  16. Determination of tropane alkaloids atropine and scopolamine by liquid chromatography-mass spectrometry in plant organs of Datura species.

    Science.gov (United States)

    Jakabová, Silvia; Vincze, Lajos; Farkas, Agnes; Kilár, Ferenc; Boros, Borbála; Felinger, Attila

    2012-04-06

    Hyoscyamine (atropine) and scopolamine are the predominant tropane alkaloids in the Datura genus, occurring in all plant organs. The assessment of the alkaloid content of various plant parts is essential from the viewpoint of medical use, but also as a potential risk of toxicity for humans and animals. Therefore, a reliable method for the determination of tropane alkaloid content is of high importance. The present work aimed at the elaboration of a rapid method for determination of the most abundant Datura alkaloids by LC-MS technique using a new generation of core-shell particle packed column. Tropane alkaloid content was investigated in various plant organs of four Datura taxa (D. innoxia, D. metel, D. stramonium, and D. stramonium var. tatula), grown under the same conditions, in two developmental stages. We have developed a rapid LC-MS method for the quantitative determination of atropine and scopolamine, which was successfully applied to quantify the alkaloids in different plant organs (leaves, flowers, stems, seeds) of thorn apples after a simple sample preparation step. Elaboration and validation of the method and analysis of plant extracts were done by UFLC-MS technique, employing an Ascentis Express C18 column. Detection was done in positive ionization mode (ESI+) and the method suitability was evaluated by several validation characteristics. Quantitation limits are 333 and 167 pgmL(-1) for scopolamine and atropine, respectively, and the method shows very good repeatability. The analysis of Datura extracts revealed significant differences depending on the species, the organ and the sampling period. Atropine was found to be dominant over scopolamine in three out of the four taxa investigated. D. innoxia showed the highest concentrations of scopolamine in all organs examined, whereas D. metel accumulated the lowest scopolamine levels. Hyoscyamine, measured as atropine, was the highest in D. stramonium var. tatula, and the lowest in D. innoxia. Samples

  17. PERBANDINGAN WAKTU INDUKSI, DURASI DAN PEMULIHAN ANESTESI DENGAN PENAMBAHAN PREMEDIKASI ATROPIN-XYLAZIN DAN ATROPINDIAZEPAM UNTUK ANESTESI UMUM KETAMIN PADA BURUNG MERPATI (COLUMBA LIVIA

    Directory of Open Access Journals (Sweden)

    I Wayan Gorda

    2012-11-01

    Full Text Available The aim of this study is to determine the comparison of induction, duration and recoverytime of anaesthesia with addition of premedication atropine-xylazine and atropinediazepamfor anaesthesia of ketamine in pigeon (Columba livia.Complete Random Device (RAL was used to analisis. The total of eight teen of pigeonused for this study. They were divided into three groups i.e. (I treated with ketamine : 75mg/kg of body weight as a positive control, (II treated with combination of atropinexylazine-ketamine with dose 0,02 mg/kg of body weight, 4 mg/kg of body weight and 75mg/kg of body weight and (III treated with combination of atropine-diazepam-ketaminewith dose 0,02 mg/kg of body weight, 2,5 mg/kg of body weight and 75 mg/kg of bodyweight. Data were analized with Analysis of Variance. (Steel and Torrie, 1989. Theresult showed that the anaesthesia of ketamine and the combination of atropine-diazepamketaminewas not resulted the induction and duration time of anaesthesia. That mean,recovery time of anaesthesia ketamine and the combination of atropine-diazepam-ketamineare 114,4 minutes and 138,1 minutes. The combination of atropine-xylazine-ketamine wasresulting the mean of induction 13,4 minutes, duration 82,8 minutes and recovery 139,6minutes. The result showed that no significantly different (P > 0.05 the time of recoverybetween the anaesthesia of ketamine, combination of atropine-xylazine-ketamine andcombination of atropine-diazepam-ketamine.

  18. Visual hallucinations on eye closure associated with atropine toxicity. A neurological analysis and comparison with other visual hallucinations.

    Science.gov (United States)

    Fisher, C M

    1991-02-01

    Visual hallucinations of remarkable intensity began shortly after intravenous atropine and persisted for 11 days. They were present only when the eyes were closed and were associated with heightened dreaming and disturbed sleep. The patient remained lucid and described his experiences to his attendants. Our patient's hallucinations bore some resemblance to hypnagogic hallucinations and this became the basis for the hypothesis that the hallucinations originated in the sleep-dream system of the brain stem. It is speculated that a similar site--a metabolic locus minoris resistentiae may play a part in other types of visual hallucinations and in delirium.

  19. Measurement of atropine and scopolamine in hair by LC-MS/MS after Datura stramonium chronic exposure.

    Science.gov (United States)

    Ricard, Florian; Abe, Emuri; Duverneuil-Mayer, Charlotte; Charlier, Philippe; de la Grandmaison, Geoffroy; Alvarez, Jean Claude

    2012-11-30

    Datura stramonium is an herbaceous annual plant. All parts of the plant contain tropane alkaloids such as atropine and scopolamine. We report the case of a 22-year-old man admitted to a general hospital for visual and aural hallucinations. One week after his admission, as the hallucinations remained, the patient was transferred to a psychiatric hospital. Neither blood nor urine was conserved during his hospitalization, so a hair analysis was requested in order to identify a possible consumption of a Datura seed infusion. After decontamination and washing, hair strands were segmented into four pieces and grinded into a fine and homogeneous powder. We then incubated 20 mg for 10 min in 1 mL of phosphate buffer at pH 5.0 in the presence of 100 ng of ketamine-d4, used as internal standard (IS). Liquid-liquid extraction was performed with 4 mL of a mixture of hexane/ethyl acetate (1/1, v/v). The residue was reconstituted in 80 μL of mobile phase. A further 10 μL were injected into an 1.9 μm Hypersil GOLD PFP column (100 mm×2.1 mm) eluted with a gradient of acetonitrile and 2 mmol/L 0.1% formate buffer at a flow rate of 300 μL/min. Compounds were detected by a LCQ TSQ Vantage XP triple-quadripole mass spectrometer equipped with an electrospray ionization (ESI) source set in positive mode. SRM transitions m/z 290.2→124.1, m/z 304.2→138.1, and m/z 242.1→129.1 were optimized for atropine, scopolamine and IS, respectively. The assay was accurate and precise over the range of 1.0 (lower limit of quantification) to 1000.0 pg/mg (upper limit of quantification) in hair. Both atropine (from 8.4 to 15.0 pg/mg) and scopolamine (1.0-1.3 pg/mg) were identified in the four segment of the hair showing a regular consumption of Datura admitted by the patient himself. We report here the first description of atropine with scopolamine in a Caucasian dark man's hair after D. stramonium chronic exposure, using a validated LC-MS/MS method. Copyright © 2012 Elsevier Ireland Ltd. All

  20. Atropine sulfate for treatment of bradycardia in a patient with morbid obesity: what may happen when you least expect it

    OpenAIRE

    Carron, Michele; Veronese, Stefano

    2015-01-01

    A 74-year-old morbidly obese man was scheduled for surgical repair of an incisional ventral hernia. Anaesthesia was induced with propofol and fentanyl, and maintained with desflurane. A second dose of fentanyl 0.2 mg, given before starting surgery, resulted in sinus bradycardia and mild decrease of arterial blood pressure. Atropine sulfate 0.5 mg was administered. One minute later, the ECG rhythm on the monitor changed to third degree atrioventricular block with a ventricular response rate of...

  1. Effect of Intensive Atropine Doses (Rapid Incremental Loading and Titration for Management of Organophosphorus Pesticide Poisoning: a Case Series

    Directory of Open Access Journals (Sweden)

    Abu Saleh Ahmed

    2014-03-01

    Full Text Available Background:Acute poisoning with organophosphorus (OP pesticides is a common method of suicide and entails considerable mortality in Bangladesh. The objective of this study was to evaluate the effects and outcomes of a protocol for treatment of OP poisoning that included titrated incremental atropine as loading dose and slow infusion for maintenance.  Methods:In this prospective descriptive case series, definitive OP poisoned patients were enrolled in an adult medicine unit of Dhaka Medical College Hospital from April 2006 to April 2007. Clinical examinations were done as soon as the patient entered the ward. Patient’s demographics, comorbid conditions and the occurrence of specific clinical outcomes including death, need for assisted ventilation and clinical complications were recorded. The patients were treated according to the protocol. Results: A total of 56 patients were enrolled over the study period. The median age of the study population was 22.5 years. Most patients were men (67.8%. The most common clinical presentation was miosis (58.9%. In total, 11 patients died (19.6%. Intermediate syndrome developed in 12 patients (21.4% and 6 of them died. Assisted ventilation was required in 16 cases (28.5. Patients with diastolic blood pressure ≤ 70 mmHg and/or GCS ≤ 10 were significantly less likely to survive (P = 0.02, 0.006, respectively. Moreover, early respiratory failure (P < 0.001 and the need for assisted ventilation (P < 0.001 were significantly higher among deceased cases. The mortality rate in this study was similar to previous studies. The frequency of atropine toxicity in the present study (1.8% was considerably lower than conventional regimen used in previous studies. Conclusion:Using the new protocol, lower rate of atropine toxicity developed in victims. Hence, the new protocol appears to be safer and its effectiveness should be further evaluated in case control studies in Bangladesh.    How to cite this article: Ahmed AS

  2. In vitro activation of the medial septum-diagonal band complex generates atropine-sensitive and atropine-resistant hippocampal theta rhythm: an investigation using a complete septohippocampal preparation.

    Science.gov (United States)

    Goutagny, Romain; Manseau, Frédéric; Jackson, Jesse; Danik, Marc; Williams, Sylvain

    2008-01-01

    The medial septum and diagonal band complex (MS-DB) is believed to play a key role in generating theta oscillations in the hippocampus, a phenomenon critical for learning and memory. Although the importance of the MS-DB in hippocampal theta rhythm generation is generally accepted, it remains to be determined whether the MS-DB alone can generate hippocampal oscillations or is only a transducer of rhythmic activity from other brain areas. Secondly, it is known that hippocampal theta rhythm can be separated into an atropine-sensitive and insensitive component. However, it remains to be established if the MS-DB can generate both types of rhythm. To answer these questions, we used a new in vitro rat septohippocampal preparation placed in a hermetically separated two side recording chamber. We showed that carbachol activation of the MS-DB generated large theta oscillations in the CA1 and CA3 regions of the hippocampus. These oscillations were blocked by applying either the GABA(A) receptor antagonist bicuculline or the AMPA/kainate antagonist DNQX to the hippocampus. Interestingly, the application of the muscarinic receptor antagonist atropine produced only a partial decrease in the amplitude, without modification of the frequency, of theta. These results show for the first time, that upon optimal excitation, the MS-DB alone is able to generate hippocampal oscillations in the theta frequency band. Moreover, these MS-DB generated theta oscillations are mediated by muscarinic and nonmuscarinic receptors and have a pharmacological profile similar to theta rhythm observed in awake animals. (c) 2008 Wiley-Liss, Inc.

  3. Low level nose-only exposure to the nerve agent soman: Toxicokinetics of soman stereoisomers and cholinesterase inhibition in atropinized guinea pigs

    NARCIS (Netherlands)

    Benschop, H.P.; Trap, H.C.; Spruit, H.E.T.; Wiel, H.J. van der; Langenberg, J.P.; Jong, L.P.A. de

    1998-01-01

    In order to initiate a quantitative basis for the toxicology of low level exposure to nerve agents, the toxicokinetics of soman stereoisomers during nose-only exposure for 5 h to 20 ppb (160 μg/m3) of C(±)P(±)- soman in air were studied in restrained, anesthetized, and atropinized guinea pigs. The

  4. High spatial resolution myocardial perfusion imaging during high dose dobutamine/atropine stress magnetic resonance using k-t SENSE.

    Science.gov (United States)

    Gebker, R; Jahnke, C; Manka, R; Frick, M; Hucko, T; Kozerke, S; Schnackenburg, B; Fleck, E; Paetsch, I

    2012-07-26

    To prospectively evaluate the feasibility and diagnostic accuracy of high spatial resolution myocardial perfusion imaging during high dose dobutamine/atropine stress magnetic resonance (DSMR) for the detection of coronary artery disease (CAD). DSMR-wall motion was combined with perfusion imaging (DSMR-perfusion) in 78 patients prior to clinically indicated invasive coronary angiography. For DSMR-perfusion an in-plane spatial resolution of 1.5 × 1.5mm(2) was attained by using 8 × k-space and time sensitivity encoding (k-t SENSE). Image quality and extent of artifacts during perfusion imaging were evaluated. Wall motion and perfusion data were interpreted sequentially. Significant CAD (stenosis ≥ 70%) was present in 52 patients and involved 86 coronary territories. One patient did not reach target heart rate despite maximum infusion of dobutamine/atropine. Two studies (3%) were non-diagnostic due k-t SENSE related artifacts resulting from insufficient breathhold capability. Overall image quality was good. Dark-rim artifacts were limited to the endocardial border at a mean width of 1.8mm. The addition of DSMR-perfusion to DSMR-wall motion data improved sensitivity for the detection of CAD (92% vs. 81%, P=0.03) and accurate determination of disease extent (85% vs. 66% of territories, Pspatial resolution DSMR-perfusion imaging at maximum stress level was feasible, improved sensitivity over DSMR-wall motion for the detection of CAD and allowed an accurate determination of disease extent. Specificity of DSMR-perfusion with k-t SENSE improved compared to prior studies using lower spatial resolution. Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.

  5. Combinations of ketamine and atropine are neuroprotective and reduce neuroinflammation after a toxic status epilepticus in mice

    Energy Technology Data Exchange (ETDEWEB)

    Dhote, Franck, E-mail: franck.dhote@irba.fr [Département de Toxicologie et risques chimiques, Institut de Recherche Biomédicale des armées – Centre de recherches du Service de santé des armées IRBA-CRSSA, 24 avenue des Maquis du Grésivaudan, B.P. 87, 38702 La Tronche cedex (France); Carpentier, Pierre; Barbier, Laure [Département de Toxicologie et risques chimiques, Institut de Recherche Biomédicale des armées – Centre de recherches du Service de santé des armées IRBA-CRSSA, 24 avenue des Maquis du Grésivaudan, B.P. 87, 38702 La Tronche cedex (France); Peinnequin, André [Département Effets biologiques des rayonnements, Institut de Recherche Biomédicale des armées – Centre de recherches du Service de santé des armées IRBA-CRSSA, 24 avenue des Maquis du Grésivaudan, B.P. 87, 38702 La Tronche cedex (France); Baille, Valérie; Pernot, Fabien; Testylier, Guy; Beaup, Claire; Foquin, Annie [Département de Toxicologie et risques chimiques, Institut de Recherche Biomédicale des armées – Centre de recherches du Service de santé des armées IRBA-CRSSA, 24 avenue des Maquis du Grésivaudan, B.P. 87, 38702 La Tronche cedex (France); and others

    2012-03-01

    Epileptic seizures and status epilepticus (SE) induced by the poisoning with organophosphorus nerve agents (OP), like soman, are accompanied by neuroinflammation whose role in seizure-related brain damage (SRBD) is not clear. Antagonists of the NMDA glutamate ionotropic receptors are currently among the few compounds able to arrest seizures and provide neuroprotection even during refractory status epilepticus (RSE). Racemic ketamine (KET), in combination with atropine sulfate (AS), was previously shown to counteract seizures and SRBD in soman-poisoned guinea-pigs. In a mouse model of severe soman-induced SE, we assessed the potentials of KET/AS combinations as a treatment for SE/RSE-induced SRBD and neuroinflammation. When starting 30 min after soman challenge, a protocol involving six injections of a sub-anesthetic dose of KET (25 mg/kg) was evaluated on body weight loss, brain damage, and neuroinflammation whereas during RSE, anesthetic protocols were considered (KET 100 mg/kg). After confirming that during RSE, KET injection was to be repeated despite some iatrogenic deaths, we used these proof-of-concept protocols to study the changes in mRNA and related protein contents of some inflammatory cytokines, chemokines and adhesion molecules in cortex and hippocampus 48 h post-challenge. In both cases, the KET/AS combinations showed important neuroprotective effects, suppressed neutrophil granulocyte infiltration and partially suppressed glial activation. KET/AS could also reduce the increase in mRNA and related pro-inflammatory proteins provoked by the poisoning. In conclusion, the present study confirms that KET/AS treatment has a strong potential for SE/RSE management following OP poisoning. The mechanisms involved in the reduction of central neuroinflammation remain to be studied. -- Highlights: ► During soman-induced status epilepticus, ketamine-atropine limit brain damage. ► Molecular neuroinflammatory response is strongly decreased. ► Glial activation is

  6. Bioavailability of diazepam after intramuscular injection of its water-soluble prodrug alone or with atropine-pralidoxime in healthy volunteers.

    Science.gov (United States)

    Abbara, C; Rousseau, J M; Turcant, A; Lallement, G; Comets, E; Bardot, I; Clair, P; Diquet, B

    2009-08-01

    The aim of this study was to assess the relative bioavailability of diazepam after administration of diazepam itself or as a water-soluble prodrug, avizafone, in humans. The study was conducted in an open, randomized, single-dose, three-way, cross-over design. Each subject received intramuscular injections of avizafone (20 mg), diazepam (11.3 mg) or avizafone (20 mg) combined with atropine (2 mg) and pralidoxime (350 mg) using a bi-compartmental auto-injector (AIBC). Plasma concentrations of diazepam were quantified using a validated LC/MS-MS assay, and were analysed by both a non-compartmental approach and by compartmental modelling. The maximum concentration (C(max)) of diazepam after avizafone injection was higher than that obtained after injection of diazepam itself (231 vs. 148 ng.mL(-1)), while area under the curve (AUC) values were equal. Diazepam concentrations reached their maximal value faster after injection of avizafone. Injection of avizafone with atropine-pralidoxime (AIBC) had no effect on diazepam C(max) and AUC, but the time to C(max) was increased, relative to avizafone injected alone. According to the Akaike criterion, the pharmacokinetics of diazepam after injection as a prodrug was best described as a two-compartment with zero-order absorption model. When atropine and pralidoxime were injected with avizafone, the best pharmacokinetic model was a two-compartment with a first-order absorption model. Diazepam had a faster entry to the general circulation and achieved higher C(max) after injection of prodrug than after the parent drug. Administration of avizafone in combination with atropine and pralidoxime by AIBC had no significant effect on diazepam AUC and C(max).

  7. Atropine vs patching for treatment of moderate amblyopia: follow-up at 15 years of age of a randomized clinical trial.

    Science.gov (United States)

    Repka, Michael X; Kraker, Raymond T; Holmes, Jonathan M; Summers, Allison I; Glaser, Stephen R; Barnhardt, Carmen N; Tien, David R

    2014-07-01

    Initial treatment for amblyopia of the fellow eye with patching and atropine sulfate eyedrops improves visual acuity. Long-term data on the durability of treatment benefit are needed. To report visual acuity at 15 years of age among patients who were younger than 7 years when enrolled in a treatment trial for moderate amblyopia. In a multicenter clinical trial, 419 children with amblyopia (visual acuity, 20/40 to 20/100) were randomly assigned to patching (minimum of 6 h/d) or atropine sulfate eyedrops, 1% (1 drop daily), for 6 months. Treatment after 6 months was at the discretion of the investigator. Two years after enrollment, an unselected subgroup of 188 children were enrolled into long-term follow-up. Initial treatment with patching or atropine with subsequent treatment at investigator discretion. Visual acuity at 15 years of age with the electronic Early Treatment Diabetic Retinopathy Study test in amblyopic and fellow eyes. Mean visual acuity in the amblyopic eye measured in 147 participants at 15 years of age was 0.14 logMAR (approximately 20/25); 59.9% of amblyopic eyes had visual acuity of 20/25 or better and 33.3%, 20/20 or better. Mean interocular acuity difference (IOD) at 15 years of age was 0.21 logMAR (2.1 lines); 48.3% had an IOD of 2 or more lines and 71.4%, 1 or more lines. Treatment (other than spectacles) was prescribed for 9 participants (6.1%) aged 10 to 15 years. Mean IOD was similar at examinations at 10 and 15 years of age (2.0 and 2.1 logMAR lines, respectively; P = .39). Better visual acuity at the 15-year examination was achieved in those who were younger than 5 years at the time of entry into the randomized clinical trial (mean logMAR, 0.09) compared with those aged 5 to 6 years (mean logMAR, 0.18; P treatment with atropine or patching, no significant differences were observed in visual acuity of amblyopic and fellow eyes at 15 years of age (P = .44 and P = .43, respectively). At 15 years of age, most children treated

  8. Open-label randomized controlled study comparing continuous infusion versus intermittent bolus dose of atropine with or without pralidoxime in the treatment of organophosphorus poisoning in a teaching hospital

    Directory of Open Access Journals (Sweden)

    R C Kumaraswamy

    2014-01-01

    Full Text Available Background: Severe organophosphorus (OPC poisoning is one of the serious problems in developing world, taking great toll on life. Though Atropine is used as an antidote, there are no clear guidelines. We conducted an open label randomized controlled clinical study to compare the efficacy of continuous infusion of atropine to that of intermittent bolus dose in the treatment of OPC poisoning. Methods and Material: Patients aged above 12 years with clinical evidence of OPC poisoning were studied. Both the groups received initial bolus of 1to3 mg of atropine. Then, Group-A received intermittent bolus and group-B, continuous infusion, until adequately atropinized. Results: Out of 743 patients (group-A: 356 and group-B: 387, females were 54%. 83% had suicidal intent. Mean atropine dose was 126.6mg in group-A and 78mg in group-B (P < 0.0001 . 21.07% (group-A and 12.92% (group-B developed intermediate syndrome (P = 0.003 , mortality was 27.25%(97 in group-A v/s 13%(50 in group-B (P < 0.0001 . Ventilator support needed in 36%(group-A against 17% in group-B (P < 0.0001 and duration of ventilation was 1.5 days lesser in group B (P < 0.0001 . 23.03% had atropine toxicity in group-A as compared to 8% in group-B (P < 0.0001 . Hospital stay was 1.67 (P < 0.0001 days shorter for group-B. Conclusion: Continuous atropine infusion should be standard of care in treating OPC poisoning.

  9. Effects of beta-blockade and atropine on ischemic responses in left ventricular regions subtending coronary stenosis during dobutamine stress echocardiography.

    Science.gov (United States)

    Chen, L; Ma, L; de Prada, V A; Chen, M; Feng, Y J; Waters, D; Gillam, L; Chen, C

    1996-12-01

    This study was designed to examine the effects of a beta-adrenergic blocking agent on the ischemic response to dobutamine stress and to determine the degree to which these effects can be abolished by the addition of atropine. Whether beta-blockade affects the sensitivity of dobutamine stress echocardiography for the diagnosis of coronary artery disease has been controversial. In nine pigs, a left anterior descending coronary artery stenosis was created to reduce flow reserve (maximal/rest flow) to 1.1 to 1.9 without baseline regional wall motion abnormalities. This corresponded to a 50% to 90% diameter stenosis. Wall thickening was measured using epicardial echocardiography. Regional lactate production and coronary venous pH were monitored from an adjacent cardiac vein. A standard protocol of dobutamine stress echocardiography was first performed. After normalization of the ischemic abnormalities elicited with this infusion, esmolol was infused at 50 micrograms/kg body weight per min and the dobutamine test was repeated, with 1.0 mg of atropine added at the maximal dobutamine dose. Without esmolol, dobutamine stress induced myocardial ischemia with a reduction in regional wall thickening and lactate production in all nine pigs. Multiple regression analysis revealed that coronary flow per heartbeat (p rate and regional oxygen consumption and altered the relation between coronary flow per heartbeat and regional wall thickening (p heartbeat was demonstrated during baseline dobutamine stress. Beta-blockade shifted this relation so that dobutamine stress-induced myocardial ischemia was attenuated. The mechanisms by which beta-blockade prevents dobutamine-induced ischemia appeared to be mainly through decreases in heart rate and rate of rise in left ventricular pressure, improvement of regional coronary flow per heartbeat and attenuation of regional ischemic lactate production. Adding atropine in conventional doses enhanced the ability of dobutamine stress to induce

  10. COMPARISON OF THREE SHORT-TERM IMMOBILIZATION REGIMES IN WILD VERREAUX'S SIFAKAS (PROPITHECUS VERREAUXI): KETAMINE-XYLAZINE, KETAMINE-XYLAZINE-ATROPINE, AND TILETAMINE-ZOLAZEPAM.

    Science.gov (United States)

    Springer, Andrea; Razafimanantsoa, Léonard; Fichtel, Claudia; Kappeler, Peter M

    2015-09-01

    Although research on lemurid primates in Madagascar has been ongoing for several decades, reports on different drug regimes to immobilize wild lemurs are limited. This study compares the efficacy, reliability, and side effects of ketamine-xylazine, ketamine-xylazine-atropine, and tiletamine-zolazepam immobilization in wild Verreaux's sifakas (Propithecus verreauxi). In the course of a long-term study in Kirindy Forest, western Madagascar, eight animals each received a mixture of ketamine (5.32±1.71 mg/kg) and xylazine (0.56±0.19 mg/kg) (KX; 7 males, 1 female) and ketamine (6.58±1.36 mg/kg), xylazine (1.28±0.28 mg/kg), and atropine (0.013±0.003 mg/kg) (KXA; 5 males, 3 females), respectively, and 14 individuals received tiletamine-zolazepam (7.73±1.37 mg/kg) (TZ; 9 males, 5 females). Induction was smooth in all protocols, but showed considerable variation in duration when animals had received KXA. Immobilization as well as recovery lasted significantly longer with TZ than with KX (Pimmobilized with TZ. Heart rate measurement at 10 min after onset of complete immobilization yielded significantly higher values if the animals had been immobilized with TZ compared to KX (Pimmobilized animals, whereas immobilization with TZ resulted in an increase in heart rate. The results suggest that KX produces good, but short, immobilization in Verreaux's sifakas at approximately 5 mg/kg ketamine and 0.5 mg/kg xylazine and a smoother and shorter recovery phase than 5 to 10 mg/kg TZ, whereas adding atropine to KX did not provide any benefits.

  11. Comparing the preventive effect of 2 percent Topical Lidocaine and Intravenous Atropine on oculocardiac reflex in Ophthalmological Surgeries under General Anesthesia

    Directory of Open Access Journals (Sweden)

    Parvin Sajedi

    2013-01-01

    Full Text Available Background: The current study aimed to determine preventive effect of 2 percent topical xylocaine on oculocardiac reflex in ophthalmological surgeries except strabismus, including retinal detachment and vitrectomy with scleral buckling under general anesthesia. Methods: A randomized controlled clinical trial was carried out on 150 patients aged 18-90 years undergoing ophthalmological surgeries under general anesthesia. Samples randomly divided into the experimental group (received four drops of 2 percent topical xylocaine instilled in desired eye and control group (received 0.5 mg atropine sulfate injection. Systolic, diastolic and mean arterial blood pressure of patients and baseline heart rate were recorded. They were compared regarding the incidence of bradycardia, heart rate less than 60 beats/minute, hypotension and blood pressure less than 90 mm/Hg. Data were analyzed by Statistical Package for the Social Sciences software version 20 using Chi-square and ANOVA. Results: The difference between two groups was not statistically significant regarding demographic and basic variables. The incidence of bradycardia in both groups was respectively (90.7 percent vs. 17.3 percent, heart rate less than 60 beats/minute (40 percent vs. 13.3 percent, hypotension (76 percent vs. 32 percent and blood pressure less than 90 mmHg was (28 percent vs. 8 percent. Accordingly, the differences between both groups were statistically significant (P > 0.001. Conclusions: The preventive impact of topical xylocaine upon oculocardiac reflex in ophthalmological surgeries such as retinal detachment and vitrectomy with scleral buckling under general anesthesia was less effective than that of atropine injection. Therefore, to avoid this reflex in high-risk patients, injecting atropine would be safer.

  12. Evaluation of the use of atropine sulfate, a combination of butylscopolammonium bromide and metamizole sodium, and flunixin meglumine to ameliorate clinical adverse effects of imidocarb dipropionate in horses.

    Science.gov (United States)

    Abutarbush, Sameeh M; Alfaqeeh, Sameh M; Mustafa, Ghazi; Qura'n, Lara; Al-Majali, Ahmad M

    2013-11-01

    To evaluate the ability of atropine sulfate, butylscopolammonium bromide combined with metamizole sodium, and flunixin meglumine to ameliorate the clinical adverse effects of imidocarb dipropionate in horses. 28 horses with piroplasmosis. 28 horses were randomly assigned to 4 equal groups according to the pretreatment administered. Fifteen minutes before administration of 2.4 mg of imidocarb dipropionate/kg IM, horses in the first group were pretreated with 0.02 mg of atropine sulfate/kg IV, the second group with a combination of 0.2 mg of butylscopolammonium bromide/kg IV and 25 mg of metamizole sodium/kg IV, the third group with 1.1 mg of flunixin meglumine/kg IV, and the fourth (control) group with 1 mL of saline (0.9% NaCl) solution/50 kg IV. Physical examination, including evaluation of rectal temperature, heart and respiratory rates, capillary refill time, mucous membrane color, hydration status, abdominal sounds, signs of abdominal pain, salivation, diarrhea, and number of defecations, was performed. Imidocarb dipropionate use in the control group was associated with serious adverse effects including signs of abdominal pain (4/7 horses) and diarrhea (2/7). Horses pretreated with atropine had no diarrhea, but 6 had signs of abdominal pain. Only 1 horse that received butylscopolammonium-metamizole pretreatment had signs of abdominal pain and 3 had diarrhea, which was numerically but not significantly different than the control group. Of horses pretreated with flunixin, 3 had signs of abdominal pain and 3 had diarrhea. A combination of butylscopolammonium bromide and metamizole sodium may be useful to ameliorate the adverse effects of imidocarb dipropionate in horses, although group size was small and significant differences from the control group were not found.

  13. Lung lesions and anti-ulcer agents beneficial effect: anti-ulcer agents pentadecapeptide BPC 157, ranitidine, omeprazole and atropine ameliorate lung lesion in rats.

    Science.gov (United States)

    Stancic-Rokotov, D; Slobodnjak, Z; Aralica, J; Aralica, G; Perovic, D; Staresinic, M; Gjurasin, M; Anic, T; Zoricic, I; Buljat, G; Prkacin, I; Sikiric, P; Seiwerth, S; Rucman, R; Petek, M; Turkovic, B; Kokic, N; Jagic, V; Boban-Blagaic, A

    2001-01-01

    Anti-ulcer agents may likely attenuate lesions outside the gastrointestinal tract, since they had protected gastrectomized rats (a "direct cytoprotective effect"). Therefore, their therapeutic potential in lung/stomach lesions were shown. Rats received an intratracheal (i.t.) HCl instillation [1.5 ml/kg HCl (pH 1.75)] (lung lesion), and an intragastric (i.g.) instillation of 96% ethanol (gastric lesion; 1 ml/rat, 24 h after i.t. HCl instillation), then sacrificed 1 h after ethanol. Basically, in lung-injured rats, the subsequent ethanol-gastric lesion was markedly aggravated. This aggravation, however, in turn, did not affect the severity of the lung lesions in the further period, at least for 1 h of observation. Taking intratracheal HCl-instillation as time 0, a gastric pentadecapeptide, GEPPPGKPADDAGLV, M.W.1419, coded BPC 157 (10 microg, 10 ng, 10 pg), ranitidine (10 mg), atropine (10 mg), omeprazole (10 mg), were given [/kg, intraperitoneally (i.p.)] (i) once, only prophylactically [as a pre-treatment (at -1h)], or as a co-treatment [at 0)], or only therapeutically (at +18h or +24 h); (ii) repeatedly, combining prophylactic/therapeutic regimens [(-1 h)+(+24 h)] or [(0)+(+24 h)], or therapeutic/therapeutic regimens [(+18 h)+(+24 h)]. For all agents, combining their prophylactic and salutary regimens (at -1 h/+24 h, or at 0/+24 h) attenuated lung lesions; even if effect had been not seen already with a single application, it became prominent after repeated treatment. In single application studies, relative to controls, a co-treatment (except to omeprazole), a pre-treatment (at -1 h) (pentadecapeptide BPC 157 and atropine, but not ranitidine and omeprazole) regularly attenuated, while therapeutically, atropine (at +18 h), pentadecapeptide BPC 157 highest dose and omeprazole (at +24 h), reversed the otherwise more severe lung lesions.

  14. Comparison of the effects of atropine and labetalol on trigeminocardiac reflex-induced hemodynamic alterations during percutaneous microballoon compression of the trigeminal ganglion.

    Science.gov (United States)

    Chen, Chun-Yu; Luo, Chiao-Fen; Hsu, Yi-Chun; Chen, Jyi-Feng; Day, Yuan-Ji

    2012-12-01

    A significant abrupt drop in heart rate is the most frequent complication during percutaneous microballoon compression of the trigeminal ganglion. It is suggested that co-activation of the sympathetic and parasympathetic nervous systems plays an important role in this occurrence. We hypothesized that not only atropine, but also labetalol might be effective in preventing this cardiovascular reflex during percutaneous microballoon compression of the trigeminal ganglion. Patients who underwent percutaneous microballoon compression for trigeminal neuralgia between September 2007 and December 2009 were prospectively evaluated. The relationship between the hemodynamic changes and intraoperative use of atropine (0.01 mg/kg) or labetalol (0.05 mg/kg) was compared. One-way analysis of variance with Bartlett's and Tukey's post-tests was used, and a value of p labetalol, and 45 received normal saline as a control. Of the patients who received normal saline, 31.3% had moderate bradycardia (heart rate labetalol, 16.7% had moderate bradycardia, 5.6% had severe bradycardia, and 2.8% had arrhythmia. Systemic blood pressure was markedly elevated straight after compression in all groups and tended to normalize 3 minutes afterwards. Both atropine and labetalol were able to lower the frequency of bradycardia. Neither of them could abolish episodes of bradycardia during the procedure. Patients receiving labetalol before microballoon compression were subject to a smaller change in hemodynamics. Our findings verified that the sympathetic and parasympathetic nervous systems may be involved in the complex interneuronal interaction of the trigeminocardiac reflex. Copyright © 2012. Published by Elsevier B.V.

  15. NO system dependence of atropine-induced mydriasis and L-NAME- and L-arginine-induced miosis: Reversal by the pentadecapeptide BPC 157 in rats and guinea pigs.

    Science.gov (United States)

    Kokot, Antonio; Zlatar, Mirna; Stupnisek, Mirjana; Drmic, Domagoj; Radic, Radivoje; Vcev, Aleksandar; Seiwerth, Sven; Sikiric, Predrag

    2016-01-15

    We revealed an immediate and hours-lasting particular NO-specific parallel miotic effect of L-NAME and L-arginine in rats and guinea pigs and a stable gastric pentadecapeptide BPC 157 157-particular effect vs. that of atropine-induced mydriasis while examining the NO system role in the normal pupils responses and pupils with atropine-induced mydriasis. We also assessed the responses to BPC 157 and its possible modulation of the changes caused by L-NAME/L-arginine and atropine. We administered locally (two drops/eye) or systemically (intraperitoneally/kg) [BPC 157 (0.4µg/eye; 10µg, 10ng, 10pg/kg), L-NAME (0.1mg/eye; 5mg/kg), and L-arginine (2mg/eye; 100mg/kg) alone and combined] at 3min prior to assessment (normal pupils) or alternatively at maximal 1% atropine-induced mydriasis (30min after two drops were administered to each eye). L-NAME/L-arginine. Normal pupil. L-NAME-miosis and L-arginine-miosis shortened and attenuated each other's responses when combined (L-NAME+L-arginine) (except with guinea pigs treated locally) and were thereby NO-specific. Atropine-pupil. Both L-NAME and L-arginine counteracted atropine-induced mydriasis. With few exceptions, the atropine+L-NAME+L-arginine-animals showed a consistent shift toward the left. BPC 157. Normal pupil. Always, BPC 157 alone (both species; locally; systemically; all regimens) did not affect normal pupils. Despite specific exceptions, BPC 157 distinctively affects L-arginine-miosis (prolongation) and L-NAME-miosis (shortening). When L-arginine and L-NAME were combined (L-NAME+L-arginine+BPC 157), the effect was less pronounced. Atropine-pupil. BPC 157 alone counteracted atropine-induced mydriasis. With few exceptions (when administered with L-NAME or L-arginine or L-NAME+L-arginine), BPC 157 augments their counteracting effects. Thus, along with its l-NAME/L-arginine effects, BPC 157 participates in ocular control, potentially via NO-mediated and cholinergic mechanisms. Copyright © 2015 Elsevier B.V. All

  16. The effects of oxotremorine, epibatidine, atropine, mecamylamine and naloxone in the tail-flick, hot-plate, and formalin tests in the naked mole-rat (Heterocephalus glaber)

    DEFF Research Database (Denmark)

    Dulu, Thomas D; Kanui, Titus I; Towett, Philemon K

    2014-01-01

    in antinociception by investigating the involvement of muscarinic, nicotinic and opioid receptors in nociceptive tests in this species. The effects of systemic administration of the muscarinic receptor agonist oxotremorine and the nicotinic receptor agonist epibatidine were investigated in the tail-flick, the hot......-plate, and the formalin tests. The effects of co-administration of the muscarinic receptor antagonist atropine, the nicotinic receptor antagonist mecamylamine, and the opioid receptor antagonist naloxone were also investigated. Oxotremorine and epibatidine induced a significant, dose-dependent antinociceptive effect...

  17. Are tropane alkaloids present in organic foods? Detection of scopolamine and atropine in organic buckwheat (Fagopyron esculentum L.) products by UHPLC-MS/MS.

    Science.gov (United States)

    Cirlini, Martina; Demuth, Teresa M; Biancardi, Alberto; Rychlik, Michael; Dall'Asta, Chiara; Bruni, Renato

    2018-01-15

    A closer monitoring of tropane alkaloids (TA) in foods is now recommended by the European Commission, following a series of alerts related to the contamination of buckwheat with weeds of the genus Datura. A novel, accurate UHPLC-MS/MS method was developed and validated for the rapid detection of scopolamine and atropine in buckwheat foods. A suitable extraction protocol was set up to maximize recoveries and detection limits in different raw, processed and baked foods. The method offers good performances in terms of sensitivity, accuracy and precision, with LOQs at 0.04 and 0.10µg/kg. The established method is suitable for routine determination of trace levels of TA and was applied to 26 different buckwheat-derived organic foods, detecting TA in 3 samples (13.9-83.9µg/kg for atropine and 5.7-10.4µg/kg for scopolamine). Only in one case the level of contamination was relevant in terms of food safety. Copyright © 2017 Elsevier Ltd. All rights reserved.

  18. Simultaneous determination of atropine and scopolamine in buckwheat and related products using modified QuEChERS and liquid chromatography tandem mass spectrometry.

    Science.gov (United States)

    Chen, Hongping; Marín-Sáez, Jesús; Romero-González, Roberto; Garrido Frenich, Antonia

    2017-03-01

    A method was developed for the determination of atropine and scopolamine in buckwheat and related products. A modified QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) extraction procedure was evaluated. Dispersive solid phase extraction (d-SPE) was studied as clean-up step, using graphitized black carbon (GBC) and primary secondary amine (PSA). The extract was diluted with water (50:50, v/v) prior to chromatographic analysis. The method was validated and recoveries (except chia samples spiked at 10μg/kg) ranged from 75% to 92%. Intra and inter-day precision was lower than or equal to 17%. The limit of quantification of atropine and scopolamine was 0.4 and 2μg/kg, respectively. Eight types of samples (buckwheat, wheat, soy, buckwheat flour, buckwheat noodle, amaranth grain, chia seeds and peeled millet) were analyzed. Target compounds were not found above the detection limits of the method, but three transformation products of scopolamine (norscopine, hydroscopolamine and dihydroxyscopolamine) were putative identified in the tested samples using high resolution mass spectrometry (Exactive-Orbitrap). Copyright © 2016 Elsevier Ltd. All rights reserved.

  19. Identification of low and high frequency ranges for heart rate variability and blood pressure variability analyses using pharmacological autonomic blockade with atropine and propranolol in swine.

    Science.gov (United States)

    Poletto, Rosangela; Janczak, Andrew M; Marchant-Forde, Ruth M; Marchant-Forde, Jeremy N; Matthews, Donald L; Dowell, Carol A; Hogan, Daniel F; Freeman, Lynetta J; Lay, Donald C

    2011-05-03

    Understanding autonomic nervous system functioning, which mediates behavioral and physiological responses to stress, offers great potential for assessing farm animal stress and welfare. Evaluation of heart rate variability (HRV) and blood pressure variability (BPV), using time and frequency domain analyses may provide a sensitive and reliable measure of affective states and stress-mediated changes in sympathetic and parasympathetic tones. The aim of this research was to define low (LF) and high frequency (HF) power spectral ranges using pharmacological autonomic blockade, and to examine HRV and BPV parameter changes in response to atropine and propranolol in swine. Ten, 13-week old, barrows (n=6) and gilts (n=4) underwent surgery to place an intra-cardiac electrode and a blood pressure catheter attached to a biotelemetric transmitter; pigs had a 3-week recovery period prior to data collection. Each pig was subjected to administration of 4 intravenous (i.v.) drug treatments: a control treatment, 3 mL of saline, and 3 blockade treatments; 0.1 mg/kg of atropine, 1.0 mg/kg of propranolol, and .1 mg/kg of atropine together with 1.0 mg/kg of propranolol. All treatments were delivered by injection in the jugular vein with a minimum of 48 h between individual treatments. Behavior, ECG and blood pressure data were recorded continuously for a total of 1h, from 30 min pre-injection to 30 min post-injection. For data analyses, two 512-beat intervals were selected for each treatment while the pig was lying and inactive. The first interval was selected from the pre-injection period (baseline), and the second was selected between 10 and 30 min post-injection. Time and frequency domain (power spectral density) analyses were performed on each data interval. Subsequent, LF and HF bands from the power spectral densities were defined based on general linear and regression analyses. The HRV and BPV were computed with a covariate (baseline) factorial analysis of treatment by sex

  20. A rat model of nerve agent exposure applicable to the pediatric population: The anticonvulsant efficacies of atropine and GluK1 antagonists

    Energy Technology Data Exchange (ETDEWEB)

    Miller, Steven L., E-mail: stevenmiller17@gmail.com [Department of Anatomy, Physiology, and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Program in Neuroscience, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Aroniadou-Anderjaska, Vassiliki, E-mail: vanderjaska@usuhs.edu [Department of Anatomy, Physiology, and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Department of Psychiatry, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Program in Neuroscience, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Figueiredo, Taiza H., E-mail: taiza.figueiredo.ctr@usuhs.edu [Department of Anatomy, Physiology, and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Prager, Eric M., E-mail: eric.prager683@gmail.com [Department of Anatomy, Physiology, and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Program in Neuroscience, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Almeida-Suhett, Camila P., E-mail: camilapalmeida@gmail.com [Department of Anatomy, Physiology, and Genetics, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Program in Neuroscience, Uniformed Services University of the Health Sciences, 4301 Jones Bridge Road, Bethesda, MD 20814 (United States); Apland, James P., E-mail: james.p.apland.civ@mail.mil [Neurotoxicology Branch, U.S. Army Medical Research Institute of Chemical Defense, Aberdeen Proving Ground, MD 21010 (United States); and others

    2015-04-15

    Inhibition of acetylcholinesterase (AChE) after nerve agent exposure induces status epilepticus (SE), which causes brain damage or death. The development of countermeasures appropriate for the pediatric population requires testing of anticonvulsant treatments in immature animals. In the present study, exposure of 21-day-old (P21) rats to different doses of soman, followed by probit analysis, produced an LD{sub 50} of 62 μg/kg. The onset of behaviorally-observed SE was accompanied by a dramatic decrease in brain AChE activity; rats who did not develop SE had significantly less reduction of AChE activity in the basolateral amygdala than rats who developed SE. Atropine sulfate (ATS) at 2 mg/kg, administered 20 min after soman exposure (1.2 × LD{sub 50}), terminated seizures. ATS at 0.5 mg/kg, given along with an oxime within 1 min after exposure, allowed testing of anticonvulsants at delayed time-points. The AMPA/GluK1 receptor antagonist LY293558, or the specific GluK1 antagonist UBP302, administered 1 h post-exposure, terminated SE. There were no degenerating neurons in soman-exposed P21 rats, but both the amygdala and the hippocampus were smaller than in control rats at 30 and 90 days post-exposure; this pathology was not present in rats treated with LY293558. Behavioral deficits present at 30 days post-exposure, were also prevented by LY293558 treatment. Thus, in immature animals, a single injection of atropine is sufficient to halt nerve agent-induced seizures, if administered timely. Testing anticonvulsants at delayed time-points requires early administration of ATS at a low dose, sufficient to counteract only peripheral toxicity. LY293558 administered 1 h post-exposure, prevents brain pathology and behavioral deficits. - Highlights: • The LD{sub 50} of soman was determined in postnatal-day-21 rats. • Rats with no seizures after 1.2XLD{sub 50} soman had less reduction of AChE in the amygdala. • Atropine sulfate (ATS) at 2 mg/kg, given at 20 min after

  1. "Combined Occlusion and Atropine Therapy" Versus "Augmented Part-Time Patching" in Children with Refractory/Residual Amblyopia: A Pilot Study.

    Science.gov (United States)

    Sachdeva, Virender; Mittal, Vaibhev; Gupta, Varun; Gunturu, Rekha; Kekunnaya, Ramesh; Chandrasekharan, Anjali; Chabblani, Preeti Patil; Rao, Harsha L

    2016-01-01

    To compare the efficacy of combined occlusion and atropine therapy (COAT) and augmented part-time patching for the treatment of unilateral refractory/residual amblyopia. This retrospective study evaluated children between 4 and 11 years with refractory/residual amblyopia who were treated with either additional atropine (COAT group) or increased hours of patching (augmented group). Data were collected on improvement in best-corrected visual acuity (BCVA; logarithm of the minimum angle of resolution [logMAR] units) at each follow-up visit. There were 19 children in the COAT group and 17 children in the augmented group. The baseline BCVA of the amblyopic eye was 0.79 ± 0.36 logMAR in the COAT group and 0.72 ± 0.26 logMAR in augmented group. Children were statistically significantly younger in the COAT group (6.4 ± 2.2 years) compared to the augmented group (8.6 ± 3.3 years, P = 0.02). The mean duration of follow-up was statistically significantly longer in the augmented group (20.2 COAT group; 13.9 months augmented group) (P = 0.03). Compliance was similar in both groups. LogMAR BCVA (adjusted for difference in age and baseline BCVA) was statistically significantly better in the COAT group (0.56 ± 0.04) compared to the augmented group (0.80 ± 0.04) at 3 months (P = 0.000); 6 months (COAT group, 0.50 ± 0.04 vs. augmented group, 0.74 ± 0.04; P = 0.04) and at 1 year (COAT group, 0.42 ± 0.04 vs. augmented group, 0.67 ± 0.04, P = 0.000). There was statistically significantly greater improvement in logMAR BCVA at 6 months in COAT group (0.26 ± 0.15) compared to the augmented group (0.02 ± 0.14), (P = 0.0002). Age, gender, pretreatment BCVA, duration of follow-up, or compliance to patching did not affect improvement in BCVA. COAT may result in greater improvement in BCVA than augmented part-time patching in children with unilateral residual/refractory amblyopia.

  2. Enantiomeric determination and evaluation of the racemization process of atropine in Solanaceae seeds and contaminated samples by high performance liquid chromatography-tandem mass spectrometry.

    Science.gov (United States)

    Marín-Sáez, Jesús; Romero-González, Roberto; Garrido Frenich, Antonia

    2016-11-25

    A new method has been developed for the enantioselective separation of (-) and (+) hyoscyamine in Solanaceaes seeds and contaminated buckwheat. Chromatographic separation was optimized, evaluating two chiral columns, Chirobiotic V and Chiralpal-AY3. Better resolution was obtained using a Chiralpak-AY3 column, utilizing as mobile phase ethanol (0.1% diethanolamine). An extraction procedure based on a modified QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) was applied, using water and acetonitrile containing 1% of acetic acid, and a clean-up step utilizing primary secondary amine (PSA) and graphitized carbon black (GCB) as sorbents. The extract was diluted with ethanol (50/:50, v/v) prior to chromatographic analysis, and the separation was carried out avoiding the racemization during this stage. Enantiomerization process of atropine was studied in samples at different conditions such as temperature (30, 50 and 80°C) and pH (3, 5, 7 and 9), observing that racemization occurs at high pH (9) and temperature (80°C). Stramonium and Brugmansia seeds were analyzed and the concentration of (-)-hyoscyamine was 1500mg/kg and 320mg/kg respectively. Contaminated buckwheat was also determined and (-)-hyoscyamine was detected at 170μg/kg. Copyright © 2016 Elsevier B.V. All rights reserved.

  3. Midazolam and atropine alter theta oscillations in the hippocampal CA1 region by modulating both the somatic and distal dendritic dipoles.

    Science.gov (United States)

    Balakrishnan, Shilpashree; Pearce, Robert A

    2014-10-01

    Theta (4-12 Hz) oscillations in the hippocampus play an important role in learning and memory. They are altered by a wide variety of drugs that impair memory, and these effects may underlie or contribute to drug-induced amnesia. However, the network mechanisms linking drug actions with changes in memory formation remain poorly defined. Here, we used a multisite linear electrode array to measure local field potentials simultaneously across the CA1 layers of the hippocampus during active exploration, and employed current source density analysis and computational modeling to investigate how midazolam and atropine-two amnestic drugs that are used clinically and experimentally-change the relative timing and strength of the drivers of θ-oscillations. We found that two dipoles are present, with active inputs that are centered at the soma and the distal apical dendrite and passive return pathways that overlap in the mid-apical dendrite. Both drugs shifted the position of the phase reversal in the local field potential that occurred in the mid-apical dendritic region, but in opposite directions, by changing the strength of the dendritic pole, without altering the somatic pole or relative timing. Computational modeling showed that this constellation of changes, as well as an additional effect on a variably present mid-apical pole, could be produced by simultaneous changes in the active somatic and distal dendritic inputs. These network-level changes, produced by two amnestic drugs that target different types of receptors, may thus serve as a common basis for impaired memory encoding. © 2014 Wiley Periodicals, Inc.

  4. Haloperidol-stomach lesions attenuation by pentadecapeptide BPC 157, omeprazole, bromocriptine, but not atropine, lansoprazole, pantoprazole, ranitidine, cimetidine and misoprostol in mice.

    Science.gov (United States)

    Bilic, I; Zoricic, I; Anic, T; Separovic, J; Stancic-Rokotov, D; Mikus, D; Buljat, G; Ivankovic, D; Aralica, G; Prkacin, I; Perovic, D; Mise, S; Rotkvic, I; Petek, M; Rucman, R; Seiwerth, S; Sikiric, P

    2001-03-09

    The focus was on haloperidol (central dopamine antagonist)-stomach lesion, a longly described suitable counterpart of dopamine blocker cysteamine-duodenal lesion. In this, the contribution of blockade of central/peripheral dopamine receptors and prostaglandins synthesis, along with influence of antiulcer agents was evaluated in mice. Male NMRI Hannnover mice were sacrificed 24 h after haloperidol (25 mg/kg b.w. i.p., given alone or with saline (haloperidol+saline) (i) or in combination (ii,iii)). Supporting central dopamine predominance for haloperidol stomach lesion induction, co-administration of peripheral dopamine receptor antagonist domperidone (5 mg/kg i.p.) (haloperidol+ domperidone) (ii), or prostaglandin synthesis inhibitor indomethacin (10 mg/kg s.c.) (haloperidol+ indomethacin) (iii) did not aggravate this lesion. (i) In haloperidol+saline challenged mice the lesions were inhibited by co-administration (/kg i.p.) of a gastric pentadecapeptide BPC 157, GlyGluProProProGlyLysProAlaAspAspAlaGlyLeuVal, M.W. 1419 (10 microg, 10 ng, 10 pg, but not 1 pg, 100 fg, 10 fg), bromocriptine (10 mg), omeprazole (10 mg, 100 mg, but not 1 mg). Atropine (10, 100, 200 mg), pirenzepine (10, 100, 200 mg), misoprostol (10, 100, 200 microg), pantoprazole (1, 10, 100 mg), lansoprazole (0.1, 1, 10 mg), cimetidine (10, 100, 200 mg) and ranitidine (10, 100, 200 mg) were not effective. (ii) Dopamine peripheral blockade influence: in haloperidol+domperidone mice, previously effective bromocriptine, pentadecapeptide BPC 157 (10 microg) or omeprazole (10 mg) did not attenuate stomach lesions. (iii) Prostaglandins synthesis blockade effect: in haloperidol+indomethacin mice, previously effective agents, bromocriptine or omeprazole were not active, while BPC 157 effect was only lessened.

  5. Therapy for unhealed gastrocutaneous fistulas in rats as a model for analogous healing of persistent skin wounds and persistent gastric ulcers: stable gastric pentadecapeptide BPC 157, atropine, ranitidine, and omeprazole.

    Science.gov (United States)

    Skorjanec, Sandra; Dolovski, Zdravko; Kocman, Ivan; Brcic, Luka; Blagaic Boban, Alenka; Batelja, Lovorka; Coric, Marjana; Sever, Marko; Klicek, Robert; Berkopic, Lidija; Radic, Bozo; Drmic, Domagoj; Kolenc, Danijela; Ilic, Spomenko; Cesarec, Vedran; Tonkic, Ante; Zoricic, Ivan; Mise, Stjepan; Staresinic, Mario; Ivica, Mihovil; Lovric Bencic, Martina; Anic, Tomislav; Seiwerth, Sven; Sikiric, Predrag

    2009-01-01

    This study focused on unhealed gastrocutaneous fistulas to resolve whether standard drugs that promote healing of gastric ulcers may simultaneously have the same effect on cutaneous wounds, and corticosteroid aggravation, and to demonstrate why peptides such as BPC 157 exhibit a greater healing effect. Therefore, with the fistulas therapy, we challenge the wound/growth factors theory of the analogous nonhealing of wounds and persistent gastric ulcers. The healing rate of gastrocutaneous fistula in rat (2-mm-diameter stomach defect, 3-mm-diameter skin defect) validates macro/microscopically and biomechanically a direct skin wound/stomach ulcer relation, and identifies a potential therapy consisting of: (i) stable gastric pentadecapeptide BPC 157 [in drinking water (10 microg/kg) (12 ml/rat/day) or intraperitoneally (10 microg/kg, 10 ng/kg, 10 pg/kg)], (ii) atropine (10 mg/kg), ranitidine (50 mg/kg), and omeprazole (50 mg/kg), (iii) 6-alpha-methylprednisolone (1 mg/kg) [intraperitoneally, once daily, first application at 30 min following surgery; last 24 h before sacrifice (at postoperative days 1, 2, 3, 7, 14, and 21)]. Greater anti-ulcer potential and efficiency in wound healing compared with standard agents favor BPC 157, efficient in inflammatory bowel disease (PL-14736, Pliva), given in drinking water or intraperitoneally. Even after 6-alpha-methylprednisolone aggravation, BPC 157 promptly improves both skin and stomach mucosa healing, and closure of fistulas, with no leakage after up to 20 ml water intragastrically. Standard anti-ulcer agents, after a delay, improve firstly skin healing and then stomach mucosal healing, but not fistula leaking and bursting strength (except for atropine). We conclude that BPC 157 may resolve analogous nonhealing of wounds and persistent gastric ulcers better than standard agents.

  6. Segurança e exeqüibilidade do ecocardiograma sob estresse com dobutamina e atropina em pacientes octogenários Safety and feasibility of dobutamine-atropine stress echocardiography in octogenarian patients

    Directory of Open Access Journals (Sweden)

    José Sebastião de Abreu

    2005-09-01

    Full Text Available OBJETIVO: Verificar a exeqüibilidade e segurança do ecocardiograma sob estresse com dobutamina e atropina (EED em octogenários. MÉTODOS: Avaliaram-se 5.467 EED, distribuídos entre grupo dos octogenários (GI=203 e grupo controle (GII=5.264. A idade média no GI=83±3 (80-95 e no GII=59±11 (17-79 anos. Os parâmetros resultantes do EED, coletados prospectivamente, foram comparados e analisados. RESULTADOS: O percentual de pacientes que atingiram freqüência cardíaca máxima foi em GI=63,5% e GII=41% (GI vs. GII; pOBJECTIVE: To assess the feasibility and safety of dobutamine-atropine stress echocardiography (DASE in octogenarians. METHODS: We evaluated 5,467 DASE which were distributed in two groups: group I (GI with 203 DASE performed in octogenarians, and group II (GII, the control group, with 5,264 DASE. The mean age of GI and GII was 83±3 (80-95 and 59±11 (17-79 years, respectively. DASE parameters that were prospectively collected, were compared and analyzed. RESULTS: The percentage of patients that achieved maximum heart rate was 63.5% in GI and 41% in GII (p<0.001, and GI patients required less atropine compared to GII (GI=47%, GII=78%, p<0.001.The presence of chest pain (GI=13%, GII=15.6%, p=0.429 and DASE positive for myocardial ischemia (GI=20.7%, GII=16.9%, p=0.296 were not statistically different between the two groups. However, concomitant positive DASE and absence of chest pain (GI=17%, GII=11%, p=0.029 was higher in GI. The incidence of premature beats in GI was higher than in GII (GI=47.8%, GII=27.6%, p<0.001, and there were more supraventricular tachyarrhythmias (ST in GI than in GII (GI=5.9%, GII=1.9%, p=0.001. Out of 11 ST that happened in GI, 9 reverted spontaneously. There weren't either deaths or acute myocardial infarction. Ventricular fibrillation only happened in GII (2 cases, 0.03%. CONCLUSION: In the present study, octogenarians achieved maximum heart rate more frequently despite the lesser amount of atropine

  7. Sulfato de atropina nos parâmetros hemodinâmicos e hemogasométricos de cães anestesiados com clorpromazina, dexmedetomidina e isoflurano Hemodynamic and hemogasometric in the atropine administration in dogs anesthetized with chlorpromazine and dexmedetomidine and isoflurane

    Directory of Open Access Journals (Sweden)

    Fabíola Niederauer Flôres

    2008-08-01

    , at least 7 days apart, in randomized blinded manner. Anesthesia was induced and maintained with isoflurane in mechanical ventilation. After instrumentation, the end-tidal isoflurane was maintained at 1,3%V throughout the study. After a 30 minutes stabilization period (M -15, baseline hemodynamic parameters and arterial blood gases were recorded and atropine (atropine group or 0.9% NaCl (saline group were administered. Fifteen minutes later, data were recorded again (M0 and a chlorpromazine- dexmedetomidine (Chlor-Dex combination was administered. Variables were measured for an additional 65 minutes after Chlor-Dex. A one-way ANOVA-Student-Newman-Keuls was used for comparisons within groups, while a paired t test was used for comparisons between groups (P£0,05. Heart rate was higher in atropine group after Chlor-Dex administration. Cardiac index (CI was reduced from baseline after Chlor-Dex in both treatments. Although mean CI values tended to be higher in atropine group, CI did not differ between groups. Chlor-Dex administration caused increased arterial blood pressure in dogs treated with atropine. Mean arterial pressure (MAP was significantly higher in the atropine group from 5 to 65 min after Chlor-Dex. The systemic vascular resistance index (SVRI increased from baseline in both groups after Chlor-Dex administration. No significant differences were observed for arterial blood gases. Atropine administration prior to Chlor-Dex resulted in increased arterial blood pressure. Bradycardia induced by the administration of these drugs was prevented by the anticholinergic given, however decrease in cardiac output was not prevented.

  8. Alterações cardiovasculares de gatos submetidos à toracotomia intercostal, pré-medicados com associação de tramadol, butorfanol e atropina e anestesiados com propofol e halotano Cardiovascular changes in cats submitted to intercostal thoracotomy, premedication with association tramadol, butorphanol, atropine, anesthetised with propofol and halothane

    Directory of Open Access Journals (Sweden)

    Juliana Tabarelli Brondani

    2003-10-01

    Full Text Available A toracotomia é um procedimento cirúrgico que produz estímulo doloroso intenso. O objetivo deste estudo foi avaliar o efeito cardiovascular da associação tramadol, butorfanol e atropina na medicação pré-anestésica de gatos anestesiados com propofol e halotano. Doze animais, SRD, machos ou fêmeas, com peso médio de 2,7 ± 0,62kg receberam como medicação pré-anestésica (MPA, a associação de tramadol (2,0mg kg-1, butorfanol (0,4mg kg-1 e atropina (0,044mg kg-1, via intramuscular. Trinta minutos após MPA, a indução foi realizada com propofol (5,0mg kg-1 por via intravenosa. A manutenção anestésica foi obtida com halotano e oxigênio 100% sob ventilação artificial manual. Os gatos foram submetidos à toracotomia intercostal para implante de um segmento autólogo de pericárdio no diafragma. As variáveis avaliadas foram: freqüência cardíaca (bpm, saturação de oxigênio da hemoglobina (%, pressão arterial sistólica (mmHg e vaporização de halotano (%. As variáveis foram mensuradas 20 minutos após a MPA (TMPA, 10 minutos após indução e a cada 10 minutos até o final do procedimento cirúrgico (T10 a T100.Os dados obtidos foram analisados estatisticamente através de ANOVA e teste de Bonferroni (pIntercostal thoracotomy is a very painful procedure that deserves proper prevention and treatment. In this study we aimed to investigate the cardiovascular effect of the association of tramadol, butorphanol and atropine in the premedication of cats anesthetised with propofol and halothane. Twelve cats of mixed breed, female and male, with mean body weight of 2.7 ± 0.62kg were premedicated with 2.0mg kg-1 tramadol and 0.4mg kg-1 butorphanol and 0.044mg kg-1 atropine combined in the same syringe intramuscularly administered. After 30 minutes of premedication, anesthetic induction was obtained with 5.0mg kg-1 propofol intravenously. Anesthetic maintenance was done with halothane and 100% oxygen with manual artificial

  9. Sublingual atropine for the treatment of severe and hyoscine ...

    African Journals Online (AJOL)

    antagonism and impaired deglutition have been hypothesised as probable underlying mechanisms.3 A few ... Oral hyoscine hydrobromide was administered for 4 weeks (titrated gradually up to 900 mcg/day) without notable improvement in the patient's hypersalivation. This restricted any further increase in the dose of ...

  10. A comparative study of the haemodynamic effects of atropine and ...

    African Journals Online (AJOL)

    Background:Bradycardia following administration of halothane and suxamethonium in children leads to reduced cardiac output, which can be prevented with prophylactic anticholinergics. Anticholinergics may result in tachycardia and arrhythmias. This study was designed to compare haemodynamic changes and incidence ...

  11. Atropine Pharmacokinetics are Affected by Moderate Hemorrhage and Hypothyroidism

    Science.gov (United States)

    1989-12-01

    Moderate Hemorrhage and Hypothyroidism 12. PERSONAL AUTHOR(S) R.C. Smallridge, B. Chernow, S. Teich, C. Kinzer, C. Umstott, G. Geelhoed, _ Ppmnl i n 13a...moderate hemorrhage and hypothyroidism ROBERT C. SMALLRIDGE, MD: BART CHERNOW, MD: STEVEN TEICH, MD, CAROL KINZER: CAROLYN UMSTOTT: GLEN GEELHOED. MD...under resting conditions. logic responses (heart rate, mydriasis, inhibition of Pharmacokinetic studies were performed in mongrel logi reo (a rat . dogs

  12. The Effects of Atropine Sulfate on Aviator Performance

    Science.gov (United States)

    1985-03-01

    subject received a pre-experimental physical including an ECG and test for glaucoma ; each subject was scheduled for a post-experimental physical...D., Schoor, N., & Bossetti, L. P. (1976). S ulated flying performance after marihuana intoxication. Av ation, Apace, and Environmental Medilnel, 1(2

  13. Atropine exposure in adolescence predispose to adult memory loss ...

    African Journals Online (AJOL)

    The memory index was calculated using the expression: Memory index. (%). = ×. 100. (Liet al., 2013). Y-maze test. This is done to check the spatial working memory of the rats. A “Y” maze of. 75 cm x 25 cm x 15 cm was constructed. The rats were placed facing the edge and were left to make their own decisions of the arms ...

  14. Exeqüibilidade, segurança e acurácia do ecocardiograma sob estresse com dobutamina/ atropina para detecção de doença arterial coronariana em candidatos a transplante renal Feasibility, safety and accuracy of dobutamine/atropine stress echocardiography for the detection of coronary artery disease in renal transplant candidates

    Directory of Open Access Journals (Sweden)

    Pedro Antonio Muniz Ferreira

    2007-01-01

    Full Text Available OBJETIVO: Avaliar a exeqüibilidade, a segurança e a acurácia diagnóstica do ecocardiograma sob estresse (EEDA com dobutamina/atropina em candidatos a transplante renal. MÉTODOS: Pacientes candidatos a transplante renal com e sem nefropatia diabética realizaram EEDA e cineangiocoronariografia. Consideraram-se dois pontos de corte para doença arterial coronariana (DAC: > 50% e > 70% de obstrução de uma artéria epicárdica. RESULTADOS: Cento e quarenta e oito pacientes realizaram o EEDA e a angiografia coronariana. A média de idade foi de 52±9 anos, 69% eram do sexo masculino, 27% tinham nefropatia diabética, e 73%, HVE; 63% estavam assintomáticos, 36% e 22% apresentaram obstruções coronarianas > 50% e > 70%, respectivamente. A exeqüibilidade foi de 91% e houve 2,7% de complicações maiores. Obtiveram-se as seguintes médias de sensibilidade, especificidade e acurácia, considerando obstrução coronariana > 50%: 53% (IC:45-61, 87% (IC:81-93, e 75% (IC:63-83, respectivamente. Para obstrução >70%, 71% (IC:64-92, 85% (IC:79-91 e 81% (IC:75-87. A sensibilidade para diagnosticar doença uniarterial foi 41% (IC:19-63 e doença multiarterial, 78% (IC:64-92. CONCLUSÃO: O EEDA foi exeqüível e seguro; entretanto, foi ineficiente para rastreamento de DAC, considerando obstruções > 50%, mas pode ser útil para detecção de DAC em pacientes com obstruções > 70% e doença multiarterial.OBJECTIVE: To evaluate the feasibility, safety and accuracy of dobutamine/atropine stress echocardiography (DASE for the detection of coronary artery desease (CAD in renal transplant candidates. METHODS: Patients candidates to renal transplant were submitted consecutively to DASE and coronary angiography. The adopted angiographic criteria for CAD were an obstructive lesion of > 50% and > 70%. RESULTS: 148 patients underwent the DASE and the coronary angiography. Mean age was 52 ± 9 years, 69% of the patients were males; 27% had diabetic nephropathy

  15. Atropine’s Effects upon the Heart and Its Systemic Output,

    Science.gov (United States)

    1986-01-01

    Nerve fibers run parallel to the Purkinje fibers in humans, 75 sheep , oxen and pigs,󈧒 whereas they tend to envelop the Purkinje fibers of the dog...1962. 154. JAMES, TN. Pericarditis and the sinus node. Arch. Int. Med. 110:305-311, 1962. 155. JAMES, TN. The connecting pathways between the sinus

  16. Combined Atropine and 2-PAM Cl Effects on Tracking Performance and Visual, Physiological, and Psychological Functions

    Science.gov (United States)

    1988-12-01

    tracking task reveals the magnitude Akitrihm. Spare. and Environmental Medicine • December. I$ II I ANTIDOTE EFFECTS--PEN ETAR ET AL. and duration of the... marihuana on dynamic visual acu- blood pressure following the combination of 2-PAM Cl ity: I. Threshold measurements. Perception Psychophys. 1975

  17. Equilibrium Performance Changes Produced by Atropine in M. mulatta and M. fascicularis.

    Science.gov (United States)

    1981-09-01

    species similar, so) was their behavior after injection of the saline control. This is consistent with ethological and neuroanatomical studies. In addition... cat . At to - )Ito Iarvlug(, I (Stockhi) 80:422-428 (1975). 18. Mat suoka, I,, Y . Ch ikamori , M. Sasa, and S. I’akaori . Influence o? mono- am inergic...neurons on the vestibular and cochlear nuclei in cats . In Vestibular Mechanisms in lealth & I) i sases. Ed., I . D. Hood . London Academic Press, 1978

  18. Prognostic value of dobutamine-atropine stress myocardial perfusion imaging in patients with diabetes

    NARCIS (Netherlands)

    A.F.L. Schinkel (Arend); A. Elhendy (Abdou); J.J. Bax (Jeroen); E.C. Vourvouri (Eleni); F. Sozzi (Fabiola); R. Valkema (Roelf); D. Poldermans (Don); J.R.T.C. Roelandt (Jos); R.T. van Domburg (Ron)

    2002-01-01

    textabstractOBJECTIVE: Exercise tolerance in patients with diabetes is frequently impaired due to noncardiac disease such as claudication and polyneuropathy. This study assesses the prognostic value of dobutamine stress myocardial perfusion imaging in patients with diabetes.

  19. Anticonvulsants for Nerve Agent-Induced Seizures: The Influence of the Therapeutic Dose of Atropine

    National Research Council Canada - National Science Library

    Shih, Tsung-Ming; Rowland, Tami C; McDonough, John H

    2007-01-01

    Two guinea pig models were used to study the anticonvulsant potency of diazepam, midazolam, and scopolamine against seizures induced by the nerve agents tabun, sarin, soman, cyclosarin, O-ethyl S-(2-(diisopropylamino)ethyl...

  20. Effects of neostigmine and atropine on basal and handling-induced acetylcholine output from ventral hippocampus

    NARCIS (Netherlands)

    Moor, E; Schirm, Eric; Jacsó, J; Westerink, B.H.C.

    The involvement of muscarinic autoreceptors in the regulation of hippocampal acetylcholine levels during acetylcholinesterase inhibition was examined by perfusing the acetylcholinesterase inhibitor neostigmine bromide(10, 100 or 1000 nM) alone and in the presence of the muscarinic receptor

  1. The Effects of Anticholinesterases and Atropine Derivatives on Visual Function in Human Subjects

    Science.gov (United States)

    1988-02-01

    formation and may be involved in arousal responses (Singer, 1979). The reticular formation also appears to be the source of cholinergic fibres to the...1960). La transmission des contrastes par le syst~me optique de l’oeil et les seuils de contraste ret~niens. Comptes Rendus de l’Acadtmie des Sciences

  2. Extraction from ox retractor penis of an inhibitory substance which mimics its atropine-resistant neurogenic relaxation.

    Science.gov (United States)

    Ambache, N; Killick, S W; Aboo Aar, M

    1975-01-01

    The inhibitory post-ganglionic transmission in the retractor penis of the ox resembles that of the dog and is not cholinergic or adrenergic. Acid extracts of this tissue have yielded an unidentified, labile, inhibitory substance which mimics the effect of its inhibitory nerves. PMID:169935

  3. Toxicokinetics of the nerve agent (+/-)-VX in anesthetized and atropinized hairless guinea pigs and marmosets after intravenous and percutaneous administration.

    Science.gov (United States)

    van der Schans, Marcel J; Lander, Brenda J; van der Wiel, Herma; Langenberg, Jan P; Benschop, Hendrik P

    2003-08-15

    In continuation of our investigations on the toxicokinetics of the volatile nerve agents C(+/-)P(+/-)-soman and (+/-)-sarin, we now report on the toxicokinetics of the rather nonvolatile agent (+/-)-VX. A validated method was developed to determine blood levels of (+/-)-VX by means of achiral gas chromatography at blood levels > or =10 pg/ml. The ratio of the two enantiomers of VX in blood could be measured at levels > or =1 ng/ml by using chiral HPLC in combination with off-line gas chromatographic analysis. In order to obtain basic information on the toxicokinetics of (+/-)-VX, i.e., under conditions of 100% bioavailability, the blood levels of this agent were measured in hairless guinea pigs at iv doses corresponding with 1 and 2 LD50. The derived AUCs indicate a reasonable linearity of the toxicokinetics with dose. Also, the toxicokinetics in marmoset primates was studied at an absolute iv dose corresponding with 1 LD50 in the hairless guinea pig which led to approximately the same levels of (+/-)-VX in blood as observed at 2 LD50 in the hairless guinea pig. Finally, the toxicokinetics of (+/-)-VX were measured in hairless guinea pigs via the most relevant porte d' entrée for this agent, which is the percutaneous route at a dose corresponding with 1 LD50 (pc). Large variations were observed between individual animals in the rate of penetration of (+/-)-VX and in concomitant progression of AChE inhibition in blood of these animals. Blood levels of (+/-)-VX increased gradually over a 6-h period of time. After a 7-h penetration period, the total AUC corresponded with 2.5% bioavailability relative to iv administration. In contrast with the G-agents C(+/-)P(+/-)-soman and (+/-)-sarin, stereospecificity in the sequestration of the two enantiomers of (+/-)-VX is not a prominent phenomenon. It appears that (+/-)-VX is substantially more persistent in vivo than the two G-agents. This persistence may undermine the efficacy of pretreatment with carbamates of percutaneous intoxication in particular due to gradual replacement of carbamate on AChE by (+/-)-VX, whereas classical treatment of intoxication with oximes is hampered by the short persistence of oximes relative to the agent.

  4. Toxicokinetics of the nerve agent (±)-VX in anesthetized and atropinized hairless guinea pigs and marmosets after intravenous and percutaneous administration

    NARCIS (Netherlands)

    Schans, M.J. van der; Lander, B.J.; Wiel, H. van der; Langenberg, J.P.; Benschop, H.P.

    2003-01-01

    In continuation of our investigations on the toxicokinetics of the volatile nerve agents C(±)P(±)-soman and (±)-sarin, we now report on the toxicokinetics of the rather nonvolatile agent (±)-VX. A validated method was developed to determine blood levels of (±)-VX by means of achiral gas

  5. Identification of low and high frequency ranges for heart rate variability and blood pressure variability analyses using pharmacological autonomic blockade with atropine and propranolol in swine.

    Science.gov (United States)

    Understanding autonomic nervous system functioning, which mediates behavioral and physiological responses to stress, offers great potential for evaluation of farm animal stress and welfare. Evaluation of heart rate variability (HRV) and blood pressure variability (BPV), using time and frequency doma...

  6. An Efficacy and Pharmacokinetic Evaluation of a Dose of Diazepam That Will Reduce the Incidence of Convulsions in Indian Rhesus Monkeys Pretreated with Pyridostigmine Bromide, Challenged with Soman, and Treated with Atropine and Pralidoxime Chloride with the Diazepam

    Science.gov (United States)

    1990-12-01

    cord (three sections), peripheral nerve (sciatic, brachial- plexus , ulnar, radial, phrenic), adrenal gland, liver, kidney, lung, ileum, stomach...hydroxide (10 percent solution) for G agents. E. Equipment: Safety equipped cart, freezer ( locked ), refrigerator ( locked ), tatx gloves, labels, first...solutions should be kept frozen when not in use. All XCSM samples and standard solutions are stored double contained at -70 C in a locked Revcofreezer4 6

  7. Task 89-06: Determination of the Bioequivalence of HI-6 and Atropine When Delivered by Wet/Dry Autoinjector or Syringe in Sheep: A Pharmacokinetic and Efficacy Evaluation

    Science.gov (United States)

    1991-04-01

    ORGAMLZflON WEORT NUMBSER(S) 6&. ftAAM OF PEFORAiNG ORGANUAlMN 61L OPF4C1 SYMSOL 7S. MAMA Of MO~ITORIMG ORGAJ.LATION Battelle Coluus Operations / U.S. Army...excess leukemia. Containers must say *DANGEP CONTAINS BENZENE CANCER HAZARD." OSHA 8-hr permissible exposure limit (PEL) I ppm, Action Level - 0.5 ppm

  8. Drug: D07477 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available PLAIN A03BA Belladonna alkaloids, tertiary amines A03BA01 Atropine D07477 Atropine oxide (INN) USP drug clas...DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS A03B BELLADONNA AND DERIVATIVES,

  9. Sensible Heat Loss After Systemic Anticholinergic Treatment

    Science.gov (United States)

    1994-01-01

    thermosensitivity to esophageal temperature drive following atropine administration. Introduction Atropine or atropine-like antimuscarinic drugs block the action of...943 29 018 166 M.A. Kolka•a l. Materials and Methods The effects of anticholinergic therapy, in this case intramuscular atropine sulfate (2 mg), on dry...Sinn, Cherry Hill, NJ, USA) and once after the injection of an equal volume of sterile saline. Test days were separated by a minimum of 48 h, and the

  10. Drug: D03863 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03863 Mixture, Drug Opium alkaloids and atropine injection (JP16); Opium alkaloids... hydrochloride - atropine sulfate hydrate mixt; Opiato (TN) Opium alkaloids hydrochlorides [DR:D03445], Atro...8301] 8 Narcotics 81 Alkaloidal narcotics 811 Opium alkaloids 8119 Others D03863 Opium alkaloids and atropine injection (JP16) PubChem: 17397948 ...

  11. Comparative study of cycloplegic drugs in clinical refraction1

    Directory of Open Access Journals (Sweden)

    Hashemi H

    2001-07-01

    Full Text Available Accurate measurement of refractive error in uncooperative patients and young children, requires cycloplegia. The aim of the present study was to determine whethere cyclopentolate by itself or in combination with 4 times instillation of atropine can be used as a substitute for 10 times instillation of atropine. From 1994 to 1996, 39 patients aged 2-12 years were included in this study. Cycloplegia was undertaken by four different methods in subsequent visits: cyclopentolate 1%, 4 times instillation of atropine, 10 times instillation of atropine plus tropicamide and 10 times instillation of atropine. 26 patients (53% male, mean age: 6.4 years completed the four stages of the study. Spheric refraction was significantly different between cyclopentolate and 4 times and 10 times atropine groups, but we didn't find any significant difference in cylindric refraction between groups. It seems that 10 times instillation of atropine is still the best method of cycloplegia in pediatric eye examination.

  12. Comparative study of cycloplegic drugs in clinical refraction

    Directory of Open Access Journals (Sweden)

    Hashemi H

    2000-07-01

    Full Text Available Accurate measurement of refractive error in uncooperative patients and young children, requires cycloplegia. The aim of the present study was to determine whethere cyclopentolate by itself or in combination with 4 times instillation of atropine can be used as a substitute for 10 times instillation of atropine. From 1994 to 1996, 39 patients aged 2-12 years were included in this study. Cycloplegia was undertaken by four different methods in subsequent visits: cyclopentolate 1%, 4 times instillation of atropine, 10 times instillation of atropine plus tropicamide and 10 times instillation of atropine. 26 patients (53% male, mean age: 6.4 years completed the four stages of the study. Spheric refraction was significantly different between cyclopentolate and 4 times and 10 times atropine groups, but we didn't find any significant difference in cylindric refraction between groups. It seems that 10 times instillation of atropine is still the best method of cycloplegia in pediatric eye examination.

  13. Se requiere una evidencia más sólida para afirmar que la premedicación, antes de una intubación no urgente en neonatos, favorece un mejor resultado de ésta

    National Research Council Canada - National Science Library

    Puebla Molina, Sergio Francisco; Carvajal Encina, Fernando

    2010-01-01

    Authors conclusions: atropine, fentanyl and succinylcholine as premedication for non urgent intubation in newborns favors a minor number of attempts and better conditions of intubation, without adverse events...

  14. An unusual case of anisocoria by vegetal intoxication: a case report

    National Research Council Canada - National Science Library

    Macchiaiolo, Marina; Vignati, Elettra; Gonfiantini, Michaela V; Grandin, Annalisa; Romano, Maria Teresa; Salata, Michele; Valentini, Diletta; Villani, Alberto

    2010-01-01

    ...". Datura and Brugmansia are well known toxic plant; all Datura and Brugmasia plants contain, primarily in their seeds and flowers, tropane alkaloids such as scopolamine, hyoscyamine and atropine...

  15. Mexiletine

    Science.gov (United States)

    ... Diamox); aluminum-magnesium hydroxide (Gaviscon, Maalox, Mylanta, others); amiodarone (Cordarone, Pacerone); atropine (in Lomotil, in Lonox, in ... sensation slow, fast, or irregular heartbeat coma sudden death

  16. Blood pressure lowering effect of Tylophora hirsuta wall | Ahmad ...

    African Journals Online (AJOL)

    Crude hydromethanolic extract of Tylophora hirsuta (Th.Cr) was studied in spontaneous hypertensive Wistar rats for possible effects on high blood pressure and heart rate. In the absence of atropine, fall in arterial blood pressure was 64±7 mmHg at the dose of 100 mg/kg while in the presence of atropine, there was no effect ...

  17. Drug: D02069 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ETABOLISM A03 DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS A03B BELLADONNA AND DERIVATIVES, PLAIN A03BA Belladonna alkaloids, tert...iary amines A03BA01 Atropine D02069 Atropine sulfate (JP16/USP) S SENSORY ORGANS S0

  18. Some aspects of the pharmacology of the methanolic extract of ...

    African Journals Online (AJOL)

    These inhibitions are thought to be anti-muscarinic or atropine-like, since the contractions of the jejunal segment is believed to be through muscarinic receptors and could be blocked by atropine and related compounds. Phytochemical spot tests of MEPAF revealed the presence of alkaloids, carbohydrates, saponins, tannins ...

  19. Oxytocic effects of the water extract of Musanga cecropioides R ...

    African Journals Online (AJOL)

    ... activity of the extract while pre-treating the tissue with either atropine or salbutamol before administering the water extract showed the inhibitory effects of the drugs on the activity of the extract. The inhibition effect showed by atropine suggests the probable stimulation of the muscarinic receptors of the uterus by the extract.

  20. Pharmacological Effects of a Fraction of the Methanolic Extract of ...

    African Journals Online (AJOL)

    These inhibitions are thought to be antimuscarinic or atropine-like, since the contractions of the jejunal segment is believed to be through muscarinic receptors and could be blocked by atropine and related compounds . Phytochemical spot tests of the fraction G revealed the presence of alkaloids, carbohydrates, saponins, ...

  1. The human thoracic duct is functionally innervated by adrenergic nerves

    DEFF Research Database (Denmark)

    Telinius, Niklas; Baandrup, Ulrik; Rumessen, Jüri Johs.

    2013-01-01

    and immunohistochemistry suggested scarce diffuse distribution of nerves in the entire vessel wall, but nerve-mediated contractions could be induced with EFS and were sensitive to the muscarinic receptor blocker atropine and the α-adrenoceptor blocker phentolamine. The combination of phentolamine and atropine resulted...

  2. ORIGINAL ARTICLES Paediatric organophosphate poisoning - a ...

    African Journals Online (AJOL)

    organophosphate poisoning (OPP) in children and to record the frequency of atropine ... additional support for respiratory muscle paralysis/weakness and convulsions, etc.' Atropine's biochemical structure allows it to pass through the blood-brain barrier, potentially reversing some of the CNS effects of the OPP; however it ...

  3. Risk assessment of buckwheat flour contaminated by thorn-apple (Datura stramonium L.) alkaloids: a case study from Slovenia.

    Science.gov (United States)

    Perharič, Lucija; Koželj, Gordana; Družina, Branko; Stanovnik, Lovro

    2013-01-01

    In Slovenia, a mass poisoning incident involving 73 consumers with symptoms such as dry mouth, hot red skin, blurred vision, tachycardia, urinary retention, ataxia, speech disturbance, disorientation and visual hallucinations occurred in 2003. In all cases, consumers had eaten buckwheat flour food products within the last few hours. Investigations by responsible authorities identified the contamination of a range of buckwheat food products with thorn-apple (Datura stramonium L.) seeds containing toxic alkaloids, atropine and scopolamine. To ensure the safe consumption of buckwheat food products, we carried out risk characterisation and proposed provisional maximum residue levels (MRLs) of atropine and scopolamine mixture in buckwheat flour. In the absence of critical "no observed adverse effect levels" for atropine and scopolamine, we based our estimation of the acute reference doses on the lowest recommended therapeutic doses. Taking into account the additive effect of the two alkaloids, we calculated acute reference doses of the mixture, that is 0.05 µg/kg of body mass for atropine and 0.03 µg/kg of body mass for scopolamine. MRLs for atropine and scopolamine mixture in buckwheat flour were estimated in a worst-case scenario, that is consumption of 100 g of flour by a child weighing 10 kg and taking into account a range of atropine/scopolamine ratio in implicated food products, that is 0.85-3.3. We proposed the national MRLs for atropine/scopolamine mixture in buckwheat food products: 4.0 µg/kg (atropine) and 2.0 µg/kg(scopolamine). However, in view of the large variability in the alkaloid content, depending on the origin of the Datura, we propose that risk assessment should be carried out on a case-by-case basis, taking into account the ratio between atropine and scopolamine content in a particular sample.

  4. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... Peligros asociados con los lentes de contacto de color Sep. 26, 2013 It started as an impulsive ... more kids are being diagnosed with the condition. Studies show that a low-dose of atropine, typically ...

  5. Medications (for IBS)

    Medline Plus

    Full Text Available ... atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people with ... Privacy & Security | Terms of Use | Contact Us This information is in no way intended to replace the ...

  6. Sedation of Pediatric Patients in Magnetic Resonance Imaging

    National Research Council Canada - National Science Library

    Ricks, Alesia

    2000-01-01

    .... The purpose of this study was to explore the combination sedative of ketamine, midazolam, and atropine administered intramuscularly and determine if it is safe and effective for pediatric patients...

  7. Effect of autonomic blocking agents and structurally related substances on the “salt arousal of drinking”

    NARCIS (Netherlands)

    Wied, D. de

    The effect of autonomic blocking agents and structurally related substances was studied in rats in which thirst was produced by the administration of a hypertonic sodium chloride solution. Scopolamine, methamphetamine, amphetamine, chlorpromazine, atropine, mecamylamine, hexamethonium, nethalide,

  8. The clinical diagnosis of brain death

    African Journals Online (AJOL)

    -~": 1 Deep coma without any kind of response. 2 Irreversible and irreparable brain injury. 3 Absence of brainstem and spinal integrated reflexes. 4 Negative atropine test. 5 Proved apnoea with an apnoea test. 6 Electroencephalogram results ...

  9. Effects of alpha-adrenoceptor and of combined sympathetic and parasympathetic blockade on cardiac performance and vascular resistance

    DEFF Research Database (Denmark)

    Kelbaek, H; Frandsen, Henrik Lund; Hilsted, J

    1992-01-01

    1. Cardiac performance and vascular resistance was studied in seven healthy men by radionuclide cardiography and venous plethysmography before and after alpha-adrenoceptor blockade with phentolamine and after combined alpha-adrenoceptor, beta-adrenoceptor (propranolol) and parasympathetic (atropine...

  10. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... not safe. Low-Dose Atropine for Kids with Myopia AUG 31, 2017 By Kate Rauch A promising treatment for childhood near-sightedness (myopia) is welcome news at a time when more ...

  11. Development of contractile properties in the fetal porcine urinary bladder

    DEFF Research Database (Denmark)

    Jakobsen, Lotte K; Trelborg, Karina F; Simonsen, Ulf

    2017-01-01

    completely blocked by atropine.ConclusionSpontaneous myogenic contractions become irregular and contractile responses to muscarinic receptor stimulation increase during gestation, as the bladder reservoir and voiding functions develop.Pediatric Research advance online publication, 4 October 2017; doi:10...

  12. New generic approach to the treatment of organophosphate poisoning : Adenosine receptor mediated inhibition of ACh-release

    NARCIS (Netherlands)

    van Helden, HPM; Moor, E; Westerink, BHC; Bruijnzeel, PLB

    1998-01-01

    Current treatment of acute organophosphate (OP) poisoning includes a combined administration of a cholinesterase reactivator (oxime), a muscarinic receptor antagonist (atropine) and an anticonvulsant (diazepam). This treatment is not adequate since it does not prevent neuronal brain damage and

  13. Phase 1 Clinical Pharmacology Studies

    National Research Council Canada - National Science Library

    Lasseter, Kenneth

    1997-01-01

    .... Task Order 90-01 produced data suggesting that the Mark I auto-injector produced effective and desirable blood levels and effects of atropine and 2-PAM compared to other prototype auto-injectors...

  14. Medications (for IBS)

    Medline Plus

    Full Text Available ... atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people with ... treatment of IBS symptoms is not linked to depression, but rather likely to effects on the brain ...

  15. Medications (for IBS)

    Medline Plus

    Full Text Available ... atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people with ... to Do and What to Avoid Foods That Cause Cramping and Diarrhea Foods that Cause Gas and ...

  16. Pilocarpine

    Science.gov (United States)

    ... by radiotherapy in people with head and neck cancer and to treat dry mouth in people with ... Mytelase); antihistamines; atropine (Motofen, in Lomotil, in Lonox); beta blockers such as atenolol (Tenormin), labetalol (Normodyne), metoprolol (Lopressor, ...

  17. Journal of Special Operations Medicine, Volume 2, Edition 3

    Science.gov (United States)

    2002-01-01

    chlorpheniramine Anticholinergics-atropine Antiparkinsonian-- procyclidine Phenothiazines-- chlorpromazine Hyperpyrexia Hyperpyrexia Hyperpyrexia Hyperpyrexia...hypoxemia, causes activation of the inflammatory cascade producing eicosanoids through arachidonic acid synthesis . It is this inflammatory cascade which

  18. Medications (for IBS)

    Medline Plus

    Full Text Available ... atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people with ... There are other medications that are either under study, or have been shown to be effective in ...

  19. Augmentation of the pressor response to octapressin by autonomic blocking agents in the pithed rat

    NARCIS (Netherlands)

    Leenen, F.H.H.; Jong, Wybren de

    The effect of octapressin on blood pressure was studied in anesthetized pithed male rats, pretreated with autonomic blocking agents. Phenoxybenzamine and chlorpromazine induced an augmentation of the blood pressure response to octapressin, whereas atropine, propranolol and hexamethonium had no

  20. Effect of autonomic blocking agents on the cardiovascular effects of octapressin in the rat

    NARCIS (Netherlands)

    Jong, Wybren de; McLeod, Stuart M.

    Cardiovascular effects of Octapressin were studied in anesthetized male albino rats. The effect of pretreatment with the following blocking agents was evaluated: atropine, phenoxybenzamine, propranolol, hexamethonium and chlorpromazine. A decrease in blood pressure and in heart rate was induced by

  1. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... lenses, remove the lenses and seek immediate medical attention from an ophthalmologist. Related resources: Learn how to ... more kids are being diagnosed with the condition. Studies show that a low-dose of atropine, typically ...

  2. The role of protein kinase-G in the antidepressant-like response of sildenafil in combination with muscarinic acetylcholine receptor antagonism

    DEFF Research Database (Denmark)

    Liebenberg, Nico; Wegener, Gregers; Brink, Christiaan

    2010-01-01

    .c.v.) ± atropine (1 mg/kg, i.p.), Rp-8-Br-PET-cGMP or atropine. Antidepressant-like activity was scored in terms of a reduction of immobility (in seconds) relative to vehicle-treated controls. Swimming and climbing behaviours were scored as an indication of serotonergic and noradrenergic mechanisms, respectively....... This was in contrast to sildenafil + atropine which, like imipramine, selectively increased climbing. Infusion of Rp-8-Br-PET-cGMP prevented the 8-Br-cGMP-induced increase in swimming, whereas Rp-8-Br-PET-cGMP also attenuated the increase in climbing induced by sildenafil + atropine. Rp-8-Br-PET-cGMP alone did...... not affect swimming or climbing. Lastly, locomotor activity was unaltered by all treatment conditions. Conclusions These results confirm cholinergic-cGMP-PK-G interactions in the antidepressant-like effects of sildenafil, putatively acting via noradrenergic mechanisms, whereas direct PK-G activation induces...

  3. Drug: D08653 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Neuropsychiatric agent ... DG01745 ... Anticholinergic antiparkinson agent ... DG01967 ... Antiparkinson agent ... DG01745 ... Anticholinergic antipar...kinson agent ATC code: N04AA12 Chemical group: DG00858 ... Atropine [CPD:C01479] deri

  4. Novel neuroprotective and hepatoprorective effects of citric acid in acute malathion intoxication

    National Research Council Canada - National Science Library

    Omar M.E.Abdel-Salam Eman R.Youness Nadia A.Mohammed Noha N.Yassen Yasser A.Khadrawy Safinaz Ebrahim El-Toukhy Amany A.Sleem

    2016-01-01

    Objective: To study the effect of citric acid given alone or combined with atropine on brain oxidative stress, neuronal injury, liver damage, and DNA damage of peripheral blood lymphocytes induced in the rat...

  5. Biodegradation of an Organophosphate Chemical Warfare Agent Simulant by Activated Sludge with Varying Solid Retention Times

    Science.gov (United States)

    2013-03-21

    exposure consists of properly administering three drugs: atropine, pralidoxime chloride (2-PAM-Cl), and diazepam . Two mg of atropine acts to bind to...make the MARK I kit which is the current field use treatment for nerve agent exposures (Lillie, 2005). Diazepam is an anticonvulsant which is used...the synthesis of tetraethyl pyrophosphate (TEPP) in the De Clermont laboratory in France (Chauhan, 2008). However, their highly toxic capabilities

  6. Direct muscarinic cholinergic inhibition of hepatic glucose production in humans.

    OpenAIRE

    Boyle, P. J.; Liggett, S B; Shah, S D; Cryer, P E

    1988-01-01

    To explore the potential role of the parasympathetic nervous system in human glucoregulatory physiology, responses to the muscarinic cholinergic agonist bethanechol (5.0 mg s.c.) and antagonist atropine (1.0 mg i.v.) were measured in normal humans. There were no changes in the plasma glucose concentration or rates of glucose production or utilization following atropine administration. After bethanechol administration there were no changes in the plasma glucose concentration or fluxes despite ...

  7. Subtypes of muscarinic receptors in vagal inhibitory pathway to the lower esophageal sphincter of the opossum.

    Science.gov (United States)

    Gilbert, R J; Dodds, W J

    1987-10-01

    We assessed the characteristics of muscarinic neural transmission in the vagal inhibitory pathway to the lower esophageal sphincter (LES) of anesthetized opossums. LES relaxation was induced by electrical stimulation of the cervical vagus. Measurements were made of LES relaxation before and after intravenous administration of nicotinic (hexamethonium), serotonergic (5-Meo-DMT), nonselective muscarinic (atropine), and selective muscarinic (pirenzepine-M1 and 4-DAMP-M2) antagonists. The latency of LES relaxation was increased substantially by pirenzepine and atropine, increased slightly by hexamethonium, but was not affected by 4-DAMP or 5-Meo-DMT. Given as concurrent intravenous infusions, hexamethonium, 5-Meo-DMT and 4-DAMP added to pirenzepine or atropine did not significantly increase LES relaxation latency above that caused by pirenzepine or atropine alone. None of the antagonists alone had a significant effect on percent LES relaxation. The combination of pirenzepine or 4-DAMP with hexamethonium and 5-Meo-DMT did not affect percent LES relaxation. The combination of atropine with hexamethonium and 5-Meo-DMT reduced LES relaxation to 18%. The combination of pirenzepine and 4-DAMP with hexamethonium and 5-Meo-DMT, however, had no effect on percent LES relaxation. We conclude that muscarinic participation in vagally induced LES relaxation exhibits two functional receptor subtypes: (1) M1 receptors that determine LES relaxation latency and are antagonized by pirenzepine or atropine, and (2) non-M1, non-M2 receptors (Mx receptors) that contribute to the magnitude of LES relaxation and are antagonized by atropine, but not by pirenzepine or 4-DAMP.

  8. Molecular pharmacological approaches to effects of capsaicinoids and of classical antisecretory drugs on gastric basal acid secretion and on indomethacin-induced gastric mucosal damage in human healthy subjects (mini review).

    Science.gov (United States)

    Szabó, Imre Laszlo; Czimmer, Jozsef; Szolcsányi, Janos; Mózsik, Gyula

    2013-01-01

    Actions of various drugs have been tested on the gastric acid basal secretion and on the drug (Indomethacin)- induced gastric mucosal damage; however their physiological and pharmacological mechanisms have not been compared. The effects of capsaicinoids, atropine, cimetidine, omeprazole, famotidine and ranitidine were studied on gastric basal acid output, whereas the gastric mucosal preventive effects of capsaicinoids (capsaicin), atropine and cimetidine were tested on the indomethacin-induced gastric mucosal microbleedings in human healthy subjects. Results were presented by molecular pharmacological method; affinity (pD) and intrinsic activity (α-values) were calculated. Intrinsic activity curves are based on comparison to atropine effect (α(atropine)= 1.00). For evaluation of physiological and pharmacological effects of compounds molar doses of pD(2) (necessary doses to produce 50% inhibition) and pA(2) (50% inhibion on intrinsic activity) were calculated from affinity and intrinsic activity curves. The pD(2) values for compounds were as follows: 5.88 for capsaicinoids, 5.40 for atropine , 2.23 for cimetidine, 3.33 for ranitidine, 3.77 for famotidine and 3.97 for omeprazole. α - value results for compounds were: 0.76 for capsaicinoids, and 1.00 for atropine, cimetidine, ranitidine, famotidine and omeprazole all equal to 1.00 on gastric acid basal secretion. The pD(2) values on indomethacin-induced gastric mucosal microbleeding were found as follows: 6.00 for capsaicinoids, 5.50 for atropine, and 3.50 for cimetidine, meanwhile α-values resulted 0.76 for capsaicinoids, 1.00 for atropine and cimetidine. Comparison classical antisecretory drugs acting on different pathways but in much more higher molar concentrations. The atropine and capsaicinoids act in about the same molar concentration which suggests a significant physiological role for capsaicin sensitive afferent nerves in the regulation of gastric basal acid secretion and in the prevention of chemically

  9. A comparison of the neuroprotective efficacy of newly developed oximes (K117, K127) and currently available oxime (obidoxime) in tabun-poisoned rats

    Science.gov (United States)

    Kassa, Jiri; Karasova, Jana Zdarova; Musilek, Kamil; Kuca, Kamil; Jung, Young-Sik

    2009-01-01

    The potency of newly developed bispyridinium compounds (K117, K127) to reduce tabun-induced acute neurotoxic signs and symptoms was compared with currently available oxime (obidoxime) using functional observational battery. The neuroprotective effects of atropine alone and atropine combined with one of three bispyridinium oximes (K117, K127, obidoxime) on rats poisoned with tabun at a sublethal dose (180 μg/kg i.m.; 80% of LD50 value) were studied. Tabun-induced neurotoxicity was monitored using a functional observational battery and automatic measurement of motor activity at 24 h following tabun challenge. The results indicated that all tested oximes combined with atropine enabled tabun-poisoned rats to survive 24 h following tabun challenge while one tabun-poisoned rats died within 24 h after tabun poisoning when the rats were treated with atropine alone. Newly developed oxime K127 combined with atropine was the most effective in decreasing tabun-induced neurotoxicity in the case of sublethal poisonings among all oximes tested. Nevertheless, the differences of neuroprotective efficacy between K127 and obidoxime are not sufficient to replace obidoxime by K127 for the treatment of acute tabun poisonings. PMID:19730756

  10. Electroacupuncture at Zusanli Prevents Severe Scalds-Induced Gut Ischemia and Paralysis by Activating the Cholinergic Pathway

    Directory of Open Access Journals (Sweden)

    Huan Wang

    2015-01-01

    Full Text Available Severe burn injuries may result in gastrointestinal paralysis, and barrier dysfunction due to gut ischemia and lowered vagus excitability. In this study we investigate whether electroacupuncture (EA at Zusanli (ST36 could prevent severe scalds-induced gut ischemia, paralysis, and barrier dysfunction and whether the protective role of EA at ST36 is related to the vagus nerve. 35% burn area rats were divided into six groups: (a EAN: EA nonchannel acupoints followed by scald injury; (b EA: EA at ST36 after scald injury; (c VGX/EA: vagotomy (VGX before EA at ST36 and scald injury; (d VGX/EAN: VGX before EAN and scald injury; (e atropine/EA: applying atropine before scald injury and then EA at ST36; (f atropine/EAN: applying atropine before scald injury and then EA at nonchannel acupoints. EA at the Zusanli point significantly promoted the intestinal impelling ratio and increased the amount of mucosal blood flow after scald injury. The plasma diamine oxidase (DAO and intestinal permeability decreased significantly after scald injury in the EA group compared with others. However, EA after atropine injection or cervical vagotomy failed to improve intestinal motility and mucosa blood flow suggesting that the mechanism of EA may be related to the activation of the cholinergic nerve pathway.

  11. A case of pediatric age anticholinergic intoxication due to accidental Datura stramonium ingestion admitting with visual hallucination.

    Science.gov (United States)

    Şanlıdağ, Burçin; Derinöz, Okşan; Yıldız, Nagehan

    2014-01-01

    Datura stramonium (DS) is a hallucinogenic plant that can produce anticholinergic toxicity because of its significant concentrations of toxic alkaloids, such as atropine, hyoscyamine, and scopolamine. DS grows in both rural and urban areas in Turkey. Clinical findings of toxicity are similar to those of atropine toxicity. DS abuse is common among adolescents because of its hallucinatory effects. However, accidental DS poisoning from contaminated food is very rare. Accidental poisonings are commonly seen among children. Children are more prone to the toxic effects of atropine; ingestion of even a small amount can cause serious central nervous system symptoms. Treatment is supportive; antidote treatment is given rarely. An eight-year-old male with accidental DS poisoning who presented to the Pediatric Emergency Department with aggression, agitation, delirium, and visual hallucinations is reported.

  12. A retrospective survey of the causes of bracket- and tube-bonding failures.

    Science.gov (United States)

    Roelofs, Tom; Merkens, Nico; Roelofs, Jeroen; Bronkhorst, Ewald; Breuning, Hero

    2017-01-01

    To investigate the causes of bonding failures of orthodontic brackets and tubes and the effect of premedicating for saliva reduction. Premedication with atropine sulfate was administered randomly. Failure rate of brackets and tubes placed in a group of 158 consecutive patients was evaluated after a mean period of 67 weeks after bonding. The failure rate in the group without atropine sulfate premedication was 2.4%. In the group with premedication, the failure rate was 2.7%. The Cox regression analysis of these groups showed that atropine application did not lead to a reduction in bond failures. Statistically significant differences in the hazard ratio were found for the bracket regions and for the dental assistants who prepared for the bonding procedure. Premedication did not lead to fewer bracket failures. The roles of the dental assistant and patient in preventing failures was relevant. A significantly higher failure rate for orthodontic appliances was found in the posterior regions.

  13. [The effects of cycloplegic eyedrops on corneal tomography].

    Science.gov (United States)

    Kalezic, T; Vukovic, I; Andjelkovic, M; Gajic, M; Potic, J; Stojkovic, M

    2016-12-01

    Whether cycloplegics affect standard keratorefractometric and tomographic measurements is unknown. The purpose of our study was to compare the effects of cycloplegics (cyclopentolate and atropine) on corneal shape and refractive power of the eye. This study was performed on 84 eyes of 49 study participants. Patients were randomized into two groups: atropine 1% (32 eyes) and cyclopentolate 1% (52 eyes). Corneal tomography was performed with the Orbscan IIz. To evaluate the corneal shape, simulated keratometry values, anterior and posterior best-fit sphere, white-to-white and tangential and axial corneal power were performed for the anterior and posterior corneal surfaces before and during cycloplegia. Pupil diameter, anterior chamber depth, corneal thickness at the 3, 5 and 7mm optical zones, thinnest area of the cornea and corneal thickness at the visual axis were examined. Data were analyzed using an SPSS statistical package. The anterior and posterior BFS (in the atropine 1% group, anterior BFS was P=0.188; anterior BFS in the cyclopentolate group was P=0.227) and tangential and axial corneal power showed no change during cycloplegia in either group. SimK showed no statistical significance. The ACD was deeper when using atropine than cyclopentolate. Corneal thickness remained unchanged during cycloplegia in both groups. Pupil diameter was larger in light-colored irides in the cyclopentolate group than the atropine group. There was no change in W to W before (P=0.473) and during cycloplegia (P=0.287) in either group. Our results suggest that usage of atropine or cyclopentolate does not alter corneal shape. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  14. Medical countermeasure against respiratory toxicity and acute lung injury following inhalation exposure to chemical warfare nerve agent VX.

    Science.gov (United States)

    Nambiar, Madhusoodana P; Gordon, Richard K; Rezk, Peter E; Katos, Alexander M; Wajda, Nikolai A; Moran, Theodore S; Steele, Keith E; Doctor, Bhupendra P; Sciuto, Alfred M

    2007-03-01

    To develop therapeutics against lung injury and respiratory toxicity following nerve agent VX exposure, we evaluated the protective efficacy of a number of potential pulmonary therapeutics. Guinea pigs were exposed to 27.03 mg/m(3) of VX or saline using a microinstillation inhalation exposure technique for 4 min and then the toxicity was assessed. Exposure to this dose of VX resulted in a 24-h survival rate of 52%. There was a significant increase in bronchoalveolar lavage (BAL) protein, total cell number, and cell death. Surprisingly, direct pulmonary treatment with surfactant, liquivent, N-acetylcysteine, dexamethasone, or anti-sense syk oligonucleotides 2 min post-exposure did not significantly increase the survival rate of VX-exposed guinea pigs. Further blocking the nostrils, airway, and bronchioles, VX-induced viscous mucous secretions were exacerbated by these aerosolized treatments. To overcome these events, we developed a strategy to protect the animals by treatment with atropine. Atropine inhibits muscarinic stimulation and markedly reduces the copious airway secretion following nerve agent exposure. Indeed, post-exposure treatment with atropine methyl bromide, which does not cross the blood-brain barrier, resulted in 100% survival of VX-exposed animals. Bronchoalveolar lavage from VX-exposed and atropine-treated animals exhibited lower protein levels, cell number, and cell death compared to VX-exposed controls, indicating less lung injury. When pulmonary therapeutics were combined with atropine, significant protection to VX-exposure was observed. These results indicate that combinations of pulmonary therapeutics with atropine or drugs that inhibit mucous secretion are important for the treatment of respiratory toxicity and lung injury following VX exposure.

  15. The relationship between respiratory sinus arrhythmia and heart rate during anesthesia in rat

    DEFF Research Database (Denmark)

    Moldovan, M; Spulber, S; Saravan, V

    2004-01-01

    rats, slowing of HR is associated with an increase in HF. The aim of this study was to investigate whether this relationship between HF and HR is preserved during anesthesia in rat. A 15 minutes long ECG signal was recorded from rats (N=15) under moderate chloral hydrate (CHL) anesthesia. Recordings......) the decrease in HR that occurs during CHL anesthesia in rat correlates with an increase in RSA; (2) atropine reduces RSA and the time-dependent decrease in HR; (3) the time-dependent increase in RSA is preserved after atropine. We conclude that the correlation between RSA and HR reflects the cardio...

  16. 76 FR 79701 - Bristol-Myers Squibb Co. et al.; Withdrawal of Approval of 70 New Drug Applications and 97...

    Science.gov (United States)

    2011-12-22

    ... approval of the following three ANDAs after receiving a request from the ANDA holder, A.H. Robins Co., c/o Wyeth Pharmaceuticals, Inc., P.O. Box 8299, Philadelphia, PA 19101- 8299: ANDA 086661, DONNATAL (phenobarbital, hyoscyamine sulfate, atropine sulfate, scopolamine (HBr)) Elixir; ANDA 086676, DONNATAL...

  17. Electrophysiological effects of the solitary bee "Anthophora

    African Journals Online (AJOL)

    Atropine and nicotine decreased these effects. Perfusion of the gastrocnemius muscle-sciatic nerve preparation of toads with lug/m1 venom solution decreased the mechanical contraction of the muscle without recovery. The electric activity of the rabbit's duodenum was recorded before and after the application of venom ...

  18. Management of Treatment and Prevention of Acute OP Pesticide Poisoning by Medical Informatics, Telemedicine and Nanomedicine

    Directory of Open Access Journals (Sweden)

    Ganesh Chandra Sahoo

    2013-10-01

    Full Text Available Acute organophosphorous pesticide (OP poisoning kills a lot of people each year. Treatment of acute OP poisoning is of very difficult task and is a time taking event. Present day informatics methods (telemedicine, bioinformatics methods (data mining, molecular modeling, docking, cheminformatics, and nanotechnology (nanomedicine should be applied in combination or separately to combat the rise of death rate due to OP poisoning. Use of informatics method such as Java enabled camera mobiles will enable us early detection of insecticidal poisoning. Even the patients who are severely intoxicated (suicidal attempts can be diagnosed early. Telemedicine can take care for early diagnosis and early treatment. Simultaneously efforts must be taken with regard to nanotechnology to find lesser toxic compounds (use less dose of nanoparticle mediated compounds: nano-malathion as insecticides and find better efficacy of lesser dose of compounds for treatment (nano-atropine of OP poisoning. Nano-apitropine (atropine oxide may be a better choice for OP poisoning treatment as the anticholinergic agent; apitropine and hyoscyamine have exhibited higher binding affinity than atropine sulfate. Synthesis of insecticides (malathion with an antidote (atropine, apitropine in nanoscale range will prevent the lethal effect of insecticides.

  19. Timing of decontamination and treatment in case of percutaneous VX poisoning: A mini review

    NARCIS (Netherlands)

    Joosen, M.J.A.; Schans, M.J. van der; Kuijpers, W.C.; Helden, H.P.M. van; Noort, D.

    2013-01-01

    Low volatile organophosphorous nerve agents such as VX, will most likely enter the body via the skin. The pharmacokinetics of drugs such as oximes, atropine and diazepam, are not aligned with the variable and persistent toxicokinetics of the agent. Repeated administration of these drugs showed to

  20. Some Gastrointestinal Effects of the Aqueous Root Extract of ...

    African Journals Online (AJOL)

    African Journal of Biomedical Research ... The latter observed effect was similar to that produced by adrenaline (3.9×10-7 M) and the adrenergic antagonists- prazosin and propranolol used together with the herbal drug, revealed that PLZ effect is partly mediated through the adrenergic mechanism. The effects of atropine ...

  1. Medications (for IBS)

    Medline Plus

    Full Text Available ... and hyoscyamine (Levsin). Read more about anticholinergics/antispasmodics. Anti-diarrheal agents – can be effective in preventing and ... and atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people ...

  2. Non-enzymatic pretreatment of nerve agent (soman) poisoning: A brief state-of-the-art review

    NARCIS (Netherlands)

    Helden, H.P.M. van; Joosen, M.J.A.; Philippens, I.H.C.H.M.

    2011-01-01

    The rapid onset of toxic signs following nerve agent intoxication and the apprehension that current therapy (atropine, oxime, diazepam) may not prevent brain damage, requires supportive pretreatment. Since the current pretreatment drug pyridostigmine fails in protecting brain-AChE, more effective

  3. Nigerian Veterinary Jeurnal list. 25 (it), @962 (2064)

    African Journals Online (AJOL)

    produce the muscarinic (dyspnea, gastrointestinal hypermotility, salivation, sweating, etc) and nicotinic (tremour, spasm, convulsion etc) responses similar to that of acetylcholine overdoses (Hunter,. 1994; Radostits er al., 1997). Anticholinergic agents such as atropine and oximes are the specific antidotes of OPC poisoning.

  4. Intensive Care Management of Organophosphate Poisoned Patient ...

    African Journals Online (AJOL)

    The management of organophosphate poisoning is challenging, more so in the setting of poor critical care facilities. The management requires the administration of atropine, an antidote (oxime) and supportive care often provided in the ICU. We report a 35year old male who presented with a history of ingestion of an ...

  5. Malathion Administration: Effects on Physiological and Physical Performance in the Heat,

    Science.gov (United States)

    1982-12-09

    was diluted with a mixture of acetone , 70% ethyl alcohol, physiological saline (1:4.2:6.2) aseptically to achieve a final concentration of 7.5 mg...Heyl, C. N. Lieske, 3. R. Lowe, 3. H. Clark, and C. A. Broomfield. The effects of atropine- oxime therapy on cholinesterase activity and survival of

  6. Effect of aqueous leaf extract of Solanum aethiopicum on isolated ...

    African Journals Online (AJOL)

    Pharmacological reactivity of guinea pig ileum to aqueous extract of Solanum aethiocpicum was determined in vitro. Extract of the vegetable contracted the isolated ileum in a dose dependent fashion. These contractions were inhibited by mepyramine (5x10-5M) cimetidine (5 x 10-5M )and atropine (5x10-5M) inferring that ...

  7. Effects of Chloramphenicol Pretreatment on Xylazine/ketamine ...

    African Journals Online (AJOL)

    Keyword: Chloramphenicol, xylazine, ketamine, anaesthesia, cats. The effect of pretreatment with a single intramuscular (im) dose of chloramphenicol (10mg/kg) on the anaethesia induced with im injection of ketamine (25mg/kg) was investigated in five cats premedicated with im xylazine (1.0mg/kg) and atropine ...

  8. Pharmacological Studies of p, N-(3, 4-Methylenedioxy phenyl Benzoic Acid (RRL-1364 - Part-I

    Directory of Open Access Journals (Sweden)

    Dahanukar Sharadini

    1978-01-01

    Full Text Available Detailed pharmacological investigations of p-N-(3, 4-methylene dioxy phenyl benzoic acid revealed marked hypotensive action which was dose dependent and most marked in cats; it was absent in rats. Atropine could block this hypotensive action, thus suggest-ing cholinomimetic mechanism. Further studies indicated that the hypotension produced was central and possibly medullary in origin.

  9. Sex-specific peculiarities of cholinergic regulation of the cardiovascular system in normal and hypertensive rats.

    Science.gov (United States)

    Semyachkina-Glushkovskaya, O V; Anishchenko, T G; Berdnikova, V A; Najdyonova, O S

    2008-07-01

    Cardiovascular sensitivity to atropine and acetylcholine is reduced in renal hypertension. Hypertension in females is more benign and the hypotensive effects of acetylcholine in them are less attenuated than in males. Cardiovascular sensitivity to cholinergic effects in females is higher in health and hypertension, which improves their resistance to cardiovascular pathology.

  10. Multi-analysis determination of tropane alkaloids in cereals and solanaceaes seeds by liquid chromatography coupled to single stage Exactive-Orbitrap.

    Science.gov (United States)

    Marín-Sáez, Jesús; Romero-González, Roberto; Garrido Frenich, Antonia

    2017-10-06

    Tropane alkaloids are a wide group of substances that comprises more than 200 compounds occurring especially in the Solanaceae family. The main aim of this study is the development of a method for the analysis of the principal tropane alkaloids as atropine, scopolamine, anisodamine, tropane, tropine, littorine, homatropine, apoatropine, aposcopolamine, scopoline, tropinone, physoperuvine, pseudotropine and cuscohygrine in cereals and related matrices. For that, a simple solid-liquid extraction was optimized and a liquid chromatographic method coupled to a single stage Exactive-Orbitrap was developed. The method was validated obtaining recoveries in the range of 60-109% (except for some compounds in soy), precision values (expressed as relative standard deviation) lower than 20% and detection and quantification limits equal to or lower than 2 and 3μg/kg respectively. Finally, the method was applied to the analysis of different types of samples as buckwheat, linseed, soy and millet, obtaining positives for anisodamine, scopolamine, atropine, littorine and tropinone in a millet flour sample above the quantification limits, whereas atropine and scopolamine were detected in a buckwheat sample, below the quantification limit. Contaminated samples with Solanaceaes seeds (Datura Stramonium and Brugmansia Arborea) were also analysed, detecting concentrations up to 693μg/kg (scopolamine) for contaminated samples with Brugmansia seeds and 1847μg/kg (atropine) when samples were contaminated with Stramonium seeds. Copyright © 2017 Elsevier B.V. All rights reserved.

  11. Butyrylcholinesterase as a Therapeutic Drug for Protection Against Percutaneous VX

    Science.gov (United States)

    2010-01-01

    ard therapy of atropine, oxime or diazepam . While all of these nimals displayed mild signs of poisoning following VX, the signs ad resolved in 5h and by...Zheng, C.B. Gilley,M.MacDonald, K. Okolotowicz, J.R. Cashman, S.Vyas, J.M.Beck, C.M.Hadad, J. Zhang, Chemical synthesis of twoseriesofnerve agent

  12. The Acute Phase Response and Soman-Induced Status Epilepticus: Temporal, Regional and Cellular Changes in Rat Brain Cytokine Concentrations

    Science.gov (United States)

    2010-07-22

    factors such as IL-1is not surprising. Fur- thermore, IL-6 expression begins the synthesis of corti- cotrophin and glucocorticoids [50], initiating an...L, Cassel G: Effects of HI 6, diazepam and atropine on soman-induced IL-1 beta protein in rat brain. Neurotoxicology 2005, 26:173-181. 24. Shih TM

  13. Comparison of the efficacy of HI6 and 2-PAM against soman, tabun, sarin, and VX in the rabbit

    Energy Technology Data Exchange (ETDEWEB)

    Koplovitz, I.; Stewart, J.R.

    1994-12-31

    This study compared the efficacy of H16 and 2-PAM against nerve agent (soman tabun sarin and VX) -induced lethality in the atropinesterase-free rabbits pretreated with vehicle (controls) or pyridostigmine. Treatment was administered at signs or 2 min after agent challenge and consisted ofoxime (l00umol/lkg) + atropine 13 mg(kg) (alone or together with diazepam). Twenty-four-h LD50 values were calculated for soman- and tabun-intoxicated animals, whereas 24-h survival was noted in animals given 10 LD50s of sarin or VX. In pyridostigmine and control rabbits intoxicated with soman and treated with oxime + atropine (alone or together with diazepam), HI6 was 35 times more effective than 2-PAM. In contrast 1116 was less effective than 2-PAM against tabun poisoning. In pyridostigmine-pretreated animals exposed to tabun, efficacy was increased more than 3-fold when compare to tabun-challenged animals treated with atropine + H16 alone. Both oximes were highly effective against satin and VX. These findings suggest that Hifi could replace 2-PAM as therapy for nerve agent poisoning because it is superior to 2-PAM against soman, and when used in pyridostigmine-pretreated animals it affords excellent protection against all four nerve agents when used in combination with atropine (alone or together with diazepam) therapy.

  14. 75 FR 19213 - Use of Ozone-Depleting Substances; Removal of Essential-Use Designation (Flunisolide, etc.)

    Science.gov (United States)

    2010-04-14

    ... a cannula is used for application; (2) metered-dose atropine sulfate aerosol human drugs... organic compounds that contain carbon, chlorine, and fluorine atoms. CFCs were first used commercially in... addition to the ODS-containing Aerobid, Aerospan Inhalation Aerosol, a new drug application (NDA) for a...

  15. In vivo and in vitro hypotensive effect of aqueous extract of Moringa ...

    African Journals Online (AJOL)

    Administrator

    not cause contraction of guinea pig ilea unlike acetylcholine, ruling out the involvement of muscarinic receptor activation12. M. oleifera aqueous extract caused dose dependent negative inotropic effect in isolated frog heart at concentration of 0.1-. 1 µg and atropine failed to block the negative inotropic effect of the extract16.

  16. Relaxant effect of Enantia clorantha on the gastrointestinal smooth ...

    African Journals Online (AJOL)

    The extract was found to exert inhibitory action on the GIT, which resulted in reduced percentage transit in the herbal-drug-treated animals, when compared with controls (p<0.05). While atropine (0.25mgkg-1) produced a greater reduction in the rate of intestinal transit, 0.1mgkg-1 carbachol enhanced intestinal motility.

  17. Comparative studies of the effects of some antimuscarinic agents on gastric damage and pupillary reflex in the rat.

    OpenAIRE

    Daniotti, S; Del Soldato, P

    1984-01-01

    The effects of some antimuscarinic compounds on oxotremorine-induced gastric damage, the pupil size and the pupillary light reflex have been studied in the rat. Unlike atropine, propantheline and methylscopolamine, pirenzepine is effective in preventing gastric erosions at doses much lower than those that affect pupillary reflex.

  18. Pilocarpine-induced seizure-like activity with increased BNDF and neuropeptide Y expression in organotypic hippocampal slice cultures

    DEFF Research Database (Denmark)

    Poulsen, Frantz Rom; Jahnsen, Henrik; Blaabjerg, Morten

    2002-01-01

    with the muscarinic receptor antagonist atropine (100 microM). Regardless of dose and exposure time, the pilocarpine treatment induced very limited neuronal cell death, recorded as cellular propidium iodide uptake. Cultures exposed to 5 mM pilocarpine for up to 7 days displayed increased BDNF expression when analyzed...

  19. Molecular Targets for Organophosphates in the Central Nervous System

    National Research Council Canada - National Science Library

    Albuquerque, Edson

    1996-01-01

    ...%, when exposed to VX from 10 nM to 1 pM. The effect of VX was observed in the presence of TTX and atropine, indicating that it was a presynaptic effect unrelated to the activation of muscarinic receptors...

  20. Effect of Sulfadoxine-Pyrimethamine and Artesunate on Gastric Acid ...

    African Journals Online (AJOL)

    Further assessment of the roles of histaminergic and muscarinic receptors were done using ranitidine (H2 antagonist) and atropine (M3 antagonist) in the treated animals. PCM and GMP were determined in the stomach samples by histometry. The basal acid output was 0.70 + 0.01 mmol/10 mins. Normal saline and SP ...

  1. Pharmacological evidence of hypotensive activity of Somina (herbal ...

    African Journals Online (AJOL)

    Acetylcholine (Ach, 10-4 M) was used as positive control for comparison while the receptor activity of Ach and somina was assessed using atropine (muscarinic receptor antagonist) on rat heart. Results: Somina caused dose-dependent significant (p < 0.05) reduction in mean arterial pressure blood pressure (MABP). The 35 ...

  2. Drug: D02273 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available rapeutic category: 2259 Therapeutic category of drugs in Japan [BR:br08301] 2 Agent...mixt; Stmerin D (TN) Isoproterenol sulfate [DR:D02066], Atropine methylbromide [DR:D03814], Dexamethasone [DR:D00292] [DS:H00010] The

  3. Effect of Orally Administered Zingiber Officinale on the Intra Ocular ...

    African Journals Online (AJOL)

    PURPOSE: To determine the therapeutic effect of Ginger (Zingiber officinale) on increased intraocular pressure (IOP). METHODS: Twenty male and female New Zealand rabbits divided into 5 groups (A, B, C, D and E) were used. Groups B and D were administered with topical atropine 1% for 2 weeks while groups A and C ...

  4. Changes in intraocular pressure and horizontal pupil diameter ...

    African Journals Online (AJOL)

    The objective of this study was to determine the effects of topical 0.5% tropicamide, 1% atropine sulphate and 10% phenylephrine hydrochloride ophthalmic solutions on intraocular pressure (IOP) and horizontal pupil diameter (HPD) in the dog during the first hour after treatment. Forty clinically and ophthalmologically ...

  5. Endophthalmitis in a Child with Meningococcal Meningitis

    African Journals Online (AJOL)

    Endophthalmitis in a Child with Meningococcal Meningitis. BA Wills, S Lewallen. CASE REPORT. An eleven year old ... sis of meningococcal meningitis was made. She was commenced on intravenous Benzylpenicillin ... The left eye was treated with topical steroids (1 % hydrocortisone every two hours) and topical atropine.

  6. Browse Title Index

    African Journals Online (AJOL)

    Items 1 - 50 of 623 ... Vol 24, No 2 (2005), A comparative study of the haemodynamic effects of atropine and glycopyrrolate at induction of anaesthesia in children, Abstract PDF. I Desalu ... Vol 30, No 1 (2011), Adult Learning Principles for Effective Teaching in Radiology Programmes: A Review of the Literature, Abstract PDF.

  7. In vivo and in vitro hypotensive effect of aqueous extract of Moringa ...

    African Journals Online (AJOL)

    The effect might have been mediated by non-autonomic nervous system as the effect is not altered by atropine and propranolol. The extract also caused significant dose and time dependent inhibition of K+ induced contraction on guinea pig aorta. Conclusion: M.stenopetala has blood pressure lowering effect substantiating ...

  8. carpal arthrodesis for the management of experimentally induced ...

    African Journals Online (AJOL)

    flumethrin Bayticol Pour-on_® (Bayer. Germany). Surgery: Standard general and orthopedic sterile packs were utilized for all surgeries. Atropine sulphate at 0.02 mg/kg and. Chlorpromazine at 2 mg/kg were used as preanesthetic agents. Sodium. Pentobarbitone at 10 — 15 mg/kg intravenously, was administered to achieve.

  9. The role of the tractus diagonalis in drinking behaviour induced by central chemical stimulation, water deprivation and salt injection

    NARCIS (Netherlands)

    Terpstra, G.K.; Slangen, J.L.

    The role of the tractus diagonalis in drinking behaviour induced by central chemical stimulation, 23-hr water deprivation and injection of a hypertonic sodium chloride solution was investigated by means of central and peripheral administration of atropine and methylatropine. The effect of the same

  10. Life-threatening angio-oedema after the first dose of an ACE inhibitor-not an anaphylactic reaction

    DEFF Research Database (Denmark)

    Krogh Nielsen, Troels; Bygum, Anette; Rye Rasmussen, Eva

    2016-01-01

    severe angio-oedema of the upper airways. Neither adrenaline inhalations, intravenously administrated corticosteroids, atropine nor furosemide were effective and the patient soon become bradycardic. A tracheotomy was performed and the patient was placed on a ventilator. She eventually made a full...

  11. Review of the U.S. Army Aeromedical Research Laboratory Conference on Aeromedical Evacuation Held on 15-16 January 1974

    Science.gov (United States)

    1974-08-01

    standard cardiac arrest drugs--sodium bicarbonate, atropine, lidocaine, epinephrine , and calcium chloride. We utilize a system whereby the drugs are...included a portable liquid oxygen system, an electronic nebulizer , ECG monitor, defibrillator, a portable incubator, and intravenous infusion pumps

  12. An investigation into the presence of a vagal tachycardia and the effect of vasoactive intestinal polypeptide on rat heart rate in vitro.

    Science.gov (United States)

    Hogan, K; Markos, F

    2006-01-01

    The presence of the vagal tachycardia and the effect of vasoactive intestinal polypeptide in the isolated innervated rat atrium were investigated. The right vagus, or cardiac branch, were stimulated at 4, 8, 16 and 32 Hz, pulse duration 1 ms, 20 V, 30 s before atropine and for 1 min after atropine (3 micromol/l), experiments were carried out in the presence of atenolol (4 micromol/l). No significant vagal tachycardia was observed in the presence of atropine, the greatest increase in heart rate was at 16 Hz which was 3+/-1 beats/min (n = 12 rats) (p = 0.052). Baseline heart rates for the control, 226+/-11 beats/min (n = 12 rats) and atropine experiments, 210+/-8 beats/min (n = 12 rats), were not significantly different (p = 0.24). VIP (0.06, 0.12, 0.24 micromol/l) caused a maximum increase of 27+/-13 beats/min (n = 5 rats) after 6 micromol/l VIP which was not significant, two higher concentrations of VIP failed to increase heart rate further. These results show that the vagal tachycardia is not present and that VIP does not cause a significant tachycardia in the rat. Copyright (c) 2006 S. Karger AG, Basel.

  13. Selection mosaic exerted by specialist and generalist herbivores on chemical and physical defense of Datura stramonium.

    Directory of Open Access Journals (Sweden)

    Guillermo Castillo

    Full Text Available Selection exerted by herbivores is a major force driving the evolution of plant defensive characters such as leaf trichomes or secondary metabolites. However, plant defense expression is highly variable among populations and identifying the sources of this variation remains a major challenge. Plant populations are often distributed across broad geographic ranges and are exposed to different herbivore communities, ranging from generalists (that feed on diverse plant species to specialists (that feed on a restricted group of plants. We studied eight populations of the plant Datura stramonium usually eaten by specialist or generalist herbivores, in order to examine whether the pattern of phenotypic selection on secondary compounds (atropine and scopolamine and a physical defense (trichome density can explain geographic variation in these traits. Following co-evolutionary theory, we evaluated whether a more derived alkaloid (scopolamine confers higher fitness benefits than its precursor (atropine, and whether this effect differs between specialist and generalist herbivores. Our results showed consistent directional selection in almost all populations and herbivores to reduce the concentration of atropine. The most derived alkaloid (scopolamine was favored in only one of the populations, which is dominated by a generalist herbivore. In general, the patterns of selection support the existence of a selection mosaic and accounts for the positive correlation observed between atropine concentration and plant damage by herbivores recorded in previous studies.

  14. Selection mosaic exerted by specialist and generalist herbivores on chemical and physical defense of Datura stramonium.

    Science.gov (United States)

    Castillo, Guillermo; Cruz, Laura L; Tapia-López, Rosalinda; Olmedo-Vicente, Erika; Olmedo-Vicente, Eika; Carmona, Diego; Anaya-Lang, Ana Luisa; Fornoni, Juan; Andraca-Gómez, Guadalupe; Valverde, Pedro L; Núñez-Farfán, Juan

    2014-01-01

    Selection exerted by herbivores is a major force driving the evolution of plant defensive characters such as leaf trichomes or secondary metabolites. However, plant defense expression is highly variable among populations and identifying the sources of this variation remains a major challenge. Plant populations are often distributed across broad geographic ranges and are exposed to different herbivore communities, ranging from generalists (that feed on diverse plant species) to specialists (that feed on a restricted group of plants). We studied eight populations of the plant Datura stramonium usually eaten by specialist or generalist herbivores, in order to examine whether the pattern of phenotypic selection on secondary compounds (atropine and scopolamine) and a physical defense (trichome density) can explain geographic variation in these traits. Following co-evolutionary theory, we evaluated whether a more derived alkaloid (scopolamine) confers higher fitness benefits than its precursor (atropine), and whether this effect differs between specialist and generalist herbivores. Our results showed consistent directional selection in almost all populations and herbivores to reduce the concentration of atropine. The most derived alkaloid (scopolamine) was favored in only one of the populations, which is dominated by a generalist herbivore. In general, the patterns of selection support the existence of a selection mosaic and accounts for the positive correlation observed between atropine concentration and plant damage by herbivores recorded in previous studies.

  15. Effects of drugs and ionic variations on contractions of rat smooth ...

    African Journals Online (AJOL)

    ... Rat Stomach Strip (RSS), and Rat Vas Deferens (RVD) using known Ca2+ channel and specific receptor blockers. Atropine and Phentolamine respectively blocked Ach and NA competitively. While effect on K+- induced contraction was unaffected. The Rat ileum and Rat Stomach Strip has more pool of intracellular Ca2+ ...

  16. Environ: E00010 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available E00010 Belladonna root (JP16) Crude drug Hyoscyamine [CPD:C02046], Atropine [CPD:C0...1479], Norhyoscyamine [CPD:C10862], Scopolamine [CPD:C01851] Atropa belladonna [TAX:33113] Same as: D03224 S...olanaceae (nightshade family) Belladonna root Major component: Hyoscyamine [DR:D00147] CAS: 8007-93-0 ...

  17. Environ: E00008 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available E00008 Belladonna extract (JP16) Belladonna (USP) Crude drug Hyoscyamine [CPD:C0204...6], Atropine [CPD:C01479], Norhyoscyamine [CPD:C10862], Scopolamine [CPD:C01851] Atropa belladonna [TAX:3311...3] Same as: D03069 Solanaceae (nightshade family) Belladonna root extract Major component: Hyoscyamine [DR:D00147] CAS: 8007-93-0 ...

  18. Biomedical Effects of Chemical-Threat-Agent Antidote and Pretreatment Drugs. An Abstracted Bibliography. Volume 1.

    Science.gov (United States)

    1986-04-01

    route [expired air]." Or (Cont’d) 500 "An effective reabsorption from the gut prevents atropine or its metabolic products from being excreted in the...Cats were injected with HS-6, and the pressor response of carotid artery occlusion was measured. The results of selective superior cervical ganglion

  19. Effect of an Aqueous Extract of Allium Sativum Linn on the Intestinal ...

    African Journals Online (AJOL)

    The effects of acetylcholine, atropine and propranolol were also studied in the presence of the extract in the organ bath. The results show strong correlation between the log concentration of the extract and the percentage relaxation of the ileum, with r = 0.930325. This correlation was highly significant (p<0.01). Also ...

  20. The role of the tractus diagonalis in drinking behaviour induced by central chemical stimulation, water deprivation and salt injection

    NARCIS (Netherlands)

    Terpstra, G.K.; Slangen, J.L.

    1972-01-01

    The role of the tractus diagonalis in drinking behaviour induced by central chemical stimulation, 23-hr water deprivation and injection of a hypertonic sodium chloride solution was investigated by means of central and peripheral administration of atropine and methylatropine. The effect of the same

  1. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... more kids are being diagnosed with the condition. Studies show that a low-dose of atropine, typically ... EyeSmart Embed EyeSmart videos on your website Promotional materials for eye health observances EyeSmart resources are also ...

  2. Effects of Pyridostigmine Bromide on A-10 Pilots During Execution of a Simulated Mission: Physiology

    Science.gov (United States)

    1990-04-01

    warfare began at an early date in hurnan history . There is evidence that various ancient societies--used chemicals much as do certain contemporary...atropine and 2-PAM chloride, to be administered coordinately with an anticonvulsart and muscle relaxant, such as Valium , after exposure to a toxic nerve

  3. Acute angle closure glaucoma following ileostomy surgery

    Directory of Open Access Journals (Sweden)

    Mariana Meirelles Lopes

    2015-02-01

    Full Text Available Angle-closure glaucoma can be induced by drugs that may cause pupillary dilatation. We report a case of a patient that developed bilateral angle closure glaucoma after an ileostomy surgery because of systemic atropine injection. This case report highlights the importance of a fast ophthalmologic evaluation in diseases with ocular involvement in order to make accurate diagnoses and appropriate treatments.

  4. Tension Empyema Thoracis

    African Journals Online (AJOL)

    evaluation, he deteriorated and had cardio- respiratory arrest. Basic and advanced life support were initiated, and the airway secured with an endotracheal tube. Resumption of spontaneous cardiac activity was noted after three rounds of atropine and epinephrine. The patient's blood pressure was still unrecordable, but the ...

  5. Efficacy assessment of various anticholinergic agents against topical sarin-induced miosis and visual impairment in rats.

    Science.gov (United States)

    Gore, Ariel; Brandeis, Rachel; Egoz, Inbal; Peri, David; Turetz, Joseph; Bloch-Shilderman, Eugenia

    2012-04-01

    Eye exposure to the organophosphorus (OP) irreversible acetylcholinesterase inhibitor sarin results in long-term miosis and reduction in visual function. Anticholinergic drugs, such as atropine or homatropine, which are used topically in order to counter these effects may produce mydriasis and partial cycloplegia, which may worsen visual performance. This study was aimed to test the efficacy of short-acting anticholinergic drugs against sarin-induced miosis and visual impairment, which will minimally insult vision. Long-Evans rats, exposed topically to various sarin doses from 0 to 10 μg, showed a dose-dependent miosis, which returned to pre-exposure levels within 24-48 h. Tropicamide treatment rapidly widened the miotic effect to a different extent depending on time following treatment and dosage given. Cyclopentolate, however, showed a delayed response that finally widened the pupils in a dose-dependent manner. Atropine treatment showed a rapid widening of the pinpoint pupils exceeding baseline level finally causing mydriasis. Light reflex test showed that the contraction ability of the iris following atropine treatment was impaired, as opposed to the use of tropicamide which facilitated the iris contraction, similar to control. Finally, tropicamide and atropine treatments ameliorated the visual impairment, as opposed to cyclopentolate, which worsened visual performance. Considering that tropicamide treatment against sarin exposure did not cause mydriasis nor did it impair the iris contraction flexibility as a response to light, the use of this drug should be taken into consideration as a first-choice topical treatment against OP intoxication.

  6. A comparison of the neuroprotective efficacy of individual oxime (HI-6) and combinations of oximes (HI-6+trimedoxime, HI-6+K203) in soman-poisoned rats.

    Science.gov (United States)

    Kassa, Jiri; Karasova, Jana Zdarova; Tesarova, Sandra

    2011-07-01

    The ability of two combinations of oximes (HI-6+trimedoxime, HI-6+K203) to reduce soman-induced acute neurotoxic signs and symptoms was compared with the neuroprotective efficacy of the oxime HI-6 alone, using a functional observational battery. Soman-induced neurotoxicity and the neuroprotective effects of HI-6 alone and HI-6 combined with trimedoxime or K203 in rats poisoned with soman at a sublethal dose (90 μg/kg intramuscularly, i.m.; 80% of LD₅₀ value) were monitored by the functional observational battery at 24 hours following soman administration. The results indicate that both tested oxime mixtures combined with atropine were able to allow soman-poisoned rats to survive 24 hours following soman challenge, while 4 nontreated soman-poisoned rats and 1 soman-poisoned rat treated with oxime HI-6 alone combined with atropine died within 24 hours following soman poisoning. While the oxime HI-6 alone combined with atropine treatment was able to eliminate a few soman-induced neurotoxic signs and symptoms, both oxime mixtures showed higher neuroprotective efficacy in soman-poisoned rats. Especially, the combination of HI-6 with trimedoxime was able to eliminate most soman-induced neurotoxic signs and symptoms and markedly reduce acute neurotoxicity of soman in rats. Thus, both tested mixtures of oximes combined with atropine were able to increase the neuroprotective effectiveness of antidotal treatment of acute soman poisonings, compared to the individual oxime.

  7. The efficacy of HI-6 DMS in a sustained infusion against percutaneous VX poisoning in the guinea-pig.

    Science.gov (United States)

    Whitmore, C; Cook, A R; Mann, T; Price, M E; Emery, E; Roughley, N; Flint, D; Stubbs, S; Armstrong, S J; Rice, H; Tattersall, J E H

    2017-11-10

    Post-exposure nerve agent treatment usually includes administration of an oxime, which acts to restore function of the enzyme acetylcholinesterase (AChE). For immediate treatment of military personnel, this is usually administered with an autoinjector device, or devices containing the oxime such as pralidoxime, atropine and diazepam. In addition to the autoinjector, it is likely that personnel exposed to nerve agents, particularly by the percutaneous route, will require further treatment at medical facilities. As such, there is a need to understand the relationship between dose rate, plasma concentration, reactivation of AChE activity and efficacy, to provide supporting evidence for oxime infusions in nerve agent poisoning. Here, it has been demonstrated that intravenous infusion of HI-6, in combination with atropine, is efficacious against a percutaneous VX challenge in the conscious male Dunkin-Hartley guinea-pig. Inclusion of HI-6, in addition to atropine in the treatment, improved survival when compared to atropine alone. Additionally, erythrocyte AChE activity following poisoning was found to be dose dependent, with an increased dose rate of HI-6 (0.48mg/kg/min) resulting in increased AChE activity. As far as we are aware, this is the first study to correlate the pharmacokinetic profile of HI-6 with both its pharmacodynamic action of reactivating nerve agent inhibited AChE and with its efficacy against a persistent nerve agent exposure challenge in the same conscious animal. Copyright © 2017. Published by Elsevier B.V.

  8. Cardiovascular Effects of Acute Organophosphate Poisoning

    Directory of Open Access Journals (Sweden)

    Shankar Laudari

    2014-06-01

    Conclusion:Cardiac effects of OP poisoning can be life-threatening. Prompt diagnosis, early supportive and definitive therapies with atropine and oximes along with vigilant monitoring of the patients for prominent cardiac effects such as QT prolongation, VT or VF during hospital stay can definitely save lives of the victims.

  9. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... more kids are being diagnosed with the condition. Studies show that a low-dose of atropine, typically given as eye drops at bedtime, can significantly slow the progression o… ... EyeSmart Resources for Professionals Link your website to EyeSmart Embed EyeSmart videos on your website Promotional materials for eye health ...

  10. The progressive onset of cholinergic and adrenergic control of heart rate during development in the green iguana, Iguana iguana.

    Science.gov (United States)

    Sartori, Marina R; Leite, Cleo A C; Abe, Augusto S; Crossley, Dane A; Taylor, Edwin W

    2015-10-01

    The autonomic control of heart rate was studied throughout development in embryos of the green iguana, Iguana iguana by applying receptor agonists and antagonists of the parasympathetic and sympathetic systems. Acetylcholine (Ach) slowed or stopped the heart and atropine antagonized the response to Ach indicating the presence of muscarinic cholinoceptors on the heart of early embryos. However, atropine injections had no impact on heart rate until immediately before hatching, when it increased heart rate by 15%. This cholinergic tonus increased to 34% in hatchlings and dropped to 24% in adult iguanas. Although epinephrine was without effect, injection of propranolol slowed the heart throughout development, indicating the presence of β-adrenergic receptors on the heart of early embryos, possibly stimulated by high levels of circulating catecholamines. The calculated excitatory tonus varied between 33% and 68% until immediately before hatching when it fell to 25% and 29%, a level retained in hatchlings and adults. Hypoxia caused a bradycardia in early embryos that was unaffected by injection of atropine indicating that hypoxia has a direct effect upon the heart. In later embryos and hatchlings hypoxia caused a tachycardia that was unaffected by injection of atropine. Subsequent injection of propranolol reduced heart rate both uncovering a hypoxic bradycardia in late embryos and abolishing tachycardia in hatchlings. Hypercapnia was without effect on heart rate in late stage embryos and in hatchlings. Copyright © 2015 Elsevier Inc. All rights reserved.

  11. Colored Contact Lens Dangers

    Medline Plus

    Full Text Available ... the American Academy of Ophthalmology has said many times. Projectile toys are not safe. Low-Dose Atropine for Kids with ... near-sightedness (myopia) is welcome news at a time when more and more kids are being diagnosed with the condition. Studies show that ...

  12. cardiovascular effects of allium sativum bulb in laboratory mammals

    African Journals Online (AJOL)

    The negative inotropic and chronotropic effects of plant extract on guinea-pig atrial muscle strips were not modified by exogenous administration of atropine ... garlic methanolic extract (GME, 50 — 800 mg/kg p.o.) dose-dependently and significantly (P<0.05-0.001) reduced systemic arterial blood pressures and heart rates ...

  13. Experience of thoracic surgery performed under difficult conditions ...

    African Journals Online (AJOL)

    We simply used ketamine, Suxamethonium, Diazepam and Atropine. We did not use post-operative suction drainage but simple "under water seal" bottle drainage. Results: Thoracic surgery was performed in 32 patients in Medina Hospital. Most of these cases underwent pleural decortications for chronic empyema (18 ...

  14. Medications (for IBS)

    Medline Plus

    Full Text Available ... atropine (Lomotil) Read more about antidiarrheal agents. Anti-anxiety medications – can be helpful for some people with IBS, mainly those with emotional distress. There are also effective medications available that relieve the pain and improve the changes in bowel habit. They may need to be taken on ...

  15. Systemic Administration of the Potential Countermeasure Huperzine Reversibly Inhibits Central and Peripheral Acetylcholinesterase Activity Without Adverse Cognitive-Behavioral Effects

    Science.gov (United States)

    2010-01-01

    urination at current therapeutic levels (Dunn and Sidell, 1989). Even slight performance decrements could be significant in a battlefield scenario. The...Schuster CR, Seiden LS. Methamphetamine , physostigmine, atropine and mecamylamine: effects on force lever performance. Pharmacol BiochemBehav1985;23: 781–8

  16. Synergism Between Anticholinergic and Oxime Treatments Against Sarin-Induced Ocular Insult in Rats.

    Science.gov (United States)

    Gore, A; Brandeis, R; Egoz, I; Turetz, J; Nili, U; Grauer, E; Bloch-Shilderman, E

    2015-08-01

    Eye exposure to the extremely toxic organophosphorus sarin results in long-term miosis and visual impairment. As current treatment using atropine or homatropine eye drops may lead to considerable visual side effects, alternative combined treatments of intramuscular (im) oximes (16.8 µmol/kg, im) with atropine (0.5 mg/kg, im) or with the short acting antimuscarinic tropicamide (0.5%; w/v) eye drops were thus evaluated. The combined treatments efficacy following topical exposure to sarin (1 µg) was assessed by measuring pupil width and light reflex using an infra-red based digital photographic system. Results showed that the combined treatment of various oximes with atropine or with topical tropicamide eye drops rapidly reversed the sarin-induced miosis and presented a long-term improvement of 67-98% (oxime+tropicamide) or 84-109% (oxime+atropine) in pupil widening as early as 10-min following treatment. This recovery was shown to persist for at least 8-h following exposure. All combined treatments facilitated the ability of the iris to contract following sarin insult as tested by a light reflex response.Our findings emphasize the high efficacy of im oxime treatment combined with either atropine im or tropicamide eye drops in counteracting sarin-induced ocular insult. Therefore, in a mass casualty scenario the systemic combined treatment may be sufficient to ameliorate sarin-induced ocular insult with no need for additional, topical anticholinergic treatment at least in the initial stage of intoxication. For very mild casualties, who are unlikely to receive im treatment, the combined oxime (im) with topical tropicamide treatment may be sufficient in ameliorating the ocular insult. © The Author 2015. Published by Oxford University Press on behalf of the Society of Toxicology. All rights reserved. For Permissions, please e-mail: journals.permissions@oup.com.

  17. The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors.

    Science.gov (United States)

    Betz, Adrienne J; McLaughlin, Peter J; Burgos, Melissa; Weber, Suzanne M; Salamone, John D

    2007-10-01

    Nonselective muscarinic acetylcholine antagonists have been used for several years as antiparkinsonian drugs. However, there are at least five subtypes of muscarinic receptor (M1-5). Neostriatal M4 receptors have been implicated in aspects of motor function, and it has been suggested that M4 antagonists could be used as treatments for parkinsonism. Currently, there is a lack of highly selective M4 antagonists that readily penetrate the blood brain barrier. Thus, the present studies focused upon the effects of tropicamide, a muscarinic acetylcholine receptor antagonist with moderate binding selectivity for the M4 receptor subtype. Tremulous jaw movements were used as a model of parkinsonian tremor in these studies, and the effects of tropicamide were compared with those of the nonselective muscarinic antagonist atropine. Tropicamide suppressed the tremulous jaw movements induced by the muscarinic agonist pilocarpine and the dopamine antagonist pimozide. Analysis of the dose-response curves indicated that tropicamide showed approximately the same potency as atropine for suppression of pilocarpine-induced jaw movements but was more potent than atropine on the suppression of pimozide-induced jaw movements. In contrast, atropine was more potent than tropicamide in terms of impairing performance on visual stimulus detection and delayed nonmatch-to-position tasks. These studies demonstrate that tropicamide, which currently is used clinically for ophthalmic purposes, can exert actions that are consistent with antiparkinsonian effects. Moreover, the different pattern of effects shown by tropicamide compared to those of atropine on motor vs cognitive tasks could be due to the modest M4 selectivity shown by tropicamide.

  18. The role of sympathetic and vagal cardiac control on complexity of heart rate dynamics.

    Science.gov (United States)

    Silva, Luiz Eduardo Virgilio; Silva, Carlos Alberto Aguiar; Salgado, Helio Cesar; Fazan, Rubens

    2017-03-01

    Analysis of heart rate variability (HRV) by nonlinear approaches has been gaining interest due to their ability to extract additional information from heart rate (HR) dynamics that are not detectable by traditional approaches. Nevertheless, the physiological interpretation of nonlinear approaches remains unclear. Therefore, we propose long-term (60 min) protocols involving selective blockade of cardiac autonomic receptors to investigate the contribution of sympathetic and parasympathetic function upon nonlinear dynamics of HRV. Conscious male Wistar rats had their electrocardiogram (ECG) recorded under three distinct conditions: basal, selective (atenolol or atropine), or combined (atenolol plus atropine) pharmacological blockade of autonomic muscarinic or β1-adrenergic receptors. Time series of RR interval were assessed by multiscale entropy (MSE) and detrended fluctuation analysis (DFA). Entropy over short (1 to 5, MSE1-5) and long (6 to 30, MSE6-30) time scales was computed, as well as DFA scaling exponents at short (αshort, 5 ≤ n ≤ 15), mid (αmid, 30 ≤ n ≤ 200), and long (αlong, 200 ≤ n ≤ 1,700) window sizes. The results show that MSE1-5 is reduced under atropine blockade and MSE6-30 is reduced under atropine, atenolol, or combined blockade. In addition, while atropine expressed its maximal effect at scale six, the effect of atenolol on MSE increased with scale. For DFA, αshort decreased during atenolol blockade, while the αmid increased under atropine blockade. Double blockade decreased αshort and increased αlong Results with surrogate data show that the dynamics during combined blockade is not random. In summary, sympathetic and vagal control differently affect entropy (MSE) and fractal properties (DFA) of HRV. These findings are important to guide future studies.NEW & NOTEWORTHY Although multiscale entropy (MSE) and detrended fluctuation analysis (DFA) are recognizably useful prognostic/diagnostic methods, their physiological

  19. In vitro release of two anti-muscarinic drugs from soft contact lenses

    Directory of Open Access Journals (Sweden)

    Hui A

    2017-09-01

    Full Text Available Alex Hui,1 Magdalena Bajgrowicz-Cieslak,2 Chau-Minh Phan,3 Lyndon Jones3 1School of Optometry and Vision Science, UNSW Sydney, Sydney, NSW, Australia; 2Department of Mechanics, Material Science and Engineering, Wroclaw University of Technology, Wroclaw, Poland; 3Centre for Contact Lens Research, School of Optometry & Vision Science, University of Waterloo, Waterloo, ON, Canada Abstract: The purpose of this study was to investigate the release of the anti-myopia drugs atropine sulfate and pirenzepine dihydrochloride from commercially available soft contact lenses. Standard ultraviolet (UV absorbance–concentration curves were generated for atropine and pirenzepine. Ten commercially available contact lenses, including four multifocal lenses, were loaded by soaking in atropine or pirenzepine solutions at two different concentrations (10 mg/mL and 1 mg/mL. The release of the drugs into phosphate-buffered saline was determined over the course of 24 hours at 34°C using UV absorbance. Materials with surface charge released the greatest amount of atropine when loaded with either concentration when compared to the other lens types (p<0.05, releasing upward of 1.026±0.035 mg/lens and 0.979±0.024 mg/lens from etafilcon A and ocufilcon A, respectively. There were no significant differences in the amount of atropine or pirenzepine released from the multifocal and non-multifocal lenses made from the same lens materials. Narafilcon A material demonstrated prolonged release of up to 8 hours when loaded with pirenzepine, although the overall dose delivered from the lens into the solution was among the lowest of the materials investigated. The rest of the lenses reached a plateau within 2 hours of release, suggesting that they were unable to sustain drug release into the solution for long periods of time. Given that no single method of myopia control has yet shown itself to be completely effective in preventing myopia progression, a combination of

  20. Enantioseparation of tropa alkaloids by means of anionic cyclodextrin-modified capillary electrophoresis.

    Science.gov (United States)

    Wedig, M; Holzgrabe, U

    1999-06-01

    Anionic cyclodextrins (CDs), i.e., sulfated CD, sulfobutylether beta-CD (SBE-beta-CD) and heptakis(2,3-di-O-acetyl-6-sulfato)-beta-CD (HDAS-beta-CD), were used to separate the isomers of atropine, homatropine, ipratropium, scopolamine and butylscopolamine. Variations in the pH value and the concentration of the various CDs revealed the sulfated beta-CD to be superior to the other derivatives. In a basic medium at low concentrations of sulfated CD the enantiomers of atropine, homatropine and ipratropium were well resolved in a short migration time, which is appropriate for the routine analysis of the enantiomeric excess. Scopolamine and butylscopolamine compounds could not be separated with either CD.

  1. Gastrin-releasing peptide is a transmitter mediating porcine gallbladder contraction

    DEFF Research Database (Denmark)

    Schjoldager, Birgit; Poulsen, S.S.; Schmidt, P.

    1991-01-01

    We studied the role of gastrin-releasing peptide (GRP) for porcine gallbladder motility. Immunohistochemistry visualized nerve fibers containing GRP-like immunoreactivity in muscularis. GRP concentration dependently stimulated contractions of muscularis strips (ED50, 2.9 nM). Neuromedin B was less...... potent (ED50, 0.1 microM), suggesting existence of GRP-preferring receptors. GRP-induced contractions were unaffected by muscarinic antagonism (1 microM atropine), axonal blockade (1 microM tetrodotoxin), cholecystokinin (CCK) receptor antagonism (10 microM MK-329), or substance P desensitization (1......-(6-13)PA interacted specifically with GRP receptors; while abolishing responses to GRP (1 nM), responses to substance P (0.1 microM) and CCK-8 (1 nM) were unchanged. Electrical stimulation (10 Hz, 0.5 ms, 10 V) caused a rapid onset-slow offset, tetrodotoxin-sensitive excitation. Atropine reduced...

  2. [Effect of physiologically-significant stimula on Ca2+/H+ exchange by myometrial cell membrane].

    Science.gov (United States)

    Danylovych, Iu V; Tuhaĭ, V A

    2001-01-01

    The effect of membrane potential, acetylcholine, carbachol and atropine on the myometrium plasmatic membrane Ca2+/H+ exchange was estimated. The change of artificially directed membrane potential from -40 to +20 mV was defined to provide for increasing the input of Ca2+ into vesicules and output of H+ from them in their concentration gradients. The similar changes of cations in membranes were registered under acetylcholine (10(-8)-10(-4) M) and carbachol (0.1 mM) action. Atropine displayed itself as decreasing the cholinomimetics effect to the tested ions transport. The exogenous 0.5 mM Ca2+ free of directed membrane potential as well stimulated the output of protons from vesicles. The supposition was made regarding H output strengthening and pH possible local increase of cytoplasm under the smooth cells activation by the membrane potential and acetylcholine.

  3. Migrating Motor Complex in Colectomized Ileo Stoma Patients

    DEFF Research Database (Denmark)

    Berner-Hansen, Mark; Wallin, Lene; Husebye, Einar

    2011-01-01

    muscarinic receptors. We aimed to evaluate the effect of 5-hydroxytryptamine (5-HT), ondansetron and atropine on fasting and stimulated antro-duodeno-jejunal migrating motor complex (MMC) in colectomized patients with ileo stoma compared with healthy subjects. Manometric recordings were obtained in a blinded...... also evaluated. 5-HT increased the frequency (threefold) and migration velocity (twofold) of MMC phase III in both experimental groups. Ondansetron reduced 5-HT-induced frequency of MMC phase III in patients (p MMC phase...... III in healthy subjects (p MMC in either experimental group (p > 0.05). Atropine did not change fasting MMC in healthy subjects (p > 0.05). We conclude that 5-HT is a stimulator of MMC phase III and that ondansetron reduces the 5-HT...

  4. Determination of the main tropane alkaloids from transformed Hyoscyamus muticus plants by capillary zone electrophoresis.

    Science.gov (United States)

    Eeva, M; Salo, J P; Oksman-Caldentey, K M

    1998-01-01

    A capillary zone electrophoretic method (CZE) was developed using an uncoated fused silica capillary for the separation and determination of the main tropane alkaloids. The applicability of the developed method for analysis of plant samples was examined by analyzing samples of transgenic Egyptian henbane Hyoscyamus muticus (L.) plants. A simple 40 mM phosphate buffer at pH 7.8 using a voltage of 20 kV was found the best for this purpose. The main tropane alkaloids, atropine and scopolamine as well as nor-(-)-scopolamine, and tropic acid, the precursor of tropane alkaloids, could be separated in less than 13 min. The linear concentration range for atropine was 5.00-140 microg ml(-1), for scopolamine 7.50-210 microg ml(-1) and for tropic acid 2.50-70.0 microg ml(-1).

  5. [Sedation using ketamine for pain procedures in Pediatric Oncology.].

    Science.gov (United States)

    Ricard, C; Tichit, R; Troncin, R; Bernard, F

    2009-09-01

    Procedural sedation and analgesia for children is widely practiced. Since 2005 to 2007, we evaluated the safety and efficacy of ketamine to control pain induced by diagnostic procedures in pediatric oncology patients. Eight hundred fifty procedures were carried out in 125 patients aged 2 to 16 years. We associated EMNO (inhaled equimolar mixture of nitrous oxide and oxygen), atropin (oral or rectal), midazolam (oral or rectal) and ketamin (intravenous). An anesthesiologist injected ketamin. Average dose of ketamine was 0.33 to 2 mg/kg depending on number and invasiveness of procedures. This method requires careful monitoring and proper precautions. With these conditions, no complication was observed. All patients were effectively sedated. These results indicate that ketamine - in association with EMNO, atropine and midazolam - is safe and effective in pain management induced by diagnostic procedures in pediatric oncology patients. The sedative regimen of intravenous ketamine has greatly reduced patient, family and practitioners anxiety for diagnostic and therapeutic procedures.

  6. [Condition of patients after surgical wisdom tooth extraction under general anesthesia with different premedication variants--a prospective study based on a post-anesthesia questionnaire].

    Science.gov (United States)

    Markus, H; Schwarz, A

    2001-01-01

    Evaluation of the modified "postanaesthesiological questionnaire" pointed to a subtle influencing of the condition of patients who had undergone 3rd molar surgery in general anaesthesia by using different premedication variants: "Atropine, Pethidine and Midazolam" (group A) and "Atropine, Midazolam and S-Ketamin" (group B). The combination in group B seems to be more suitable. On the one hand, a lower incidence of unwanted side-effects was found and, on the other hand, remarkable positive effects were observed. Of particular significance with this combination was also the more effective suppression of postoperative pain. The Propofol-supplemented general anaesthesia prepared in this way and administered using a nasal intubation technique found the full approval of the patients. Postoperative pain therapy was effective and also inexpensive, costing just 8.20 DM per patient, according to current prices calculated by Magdeburg University Hospital.

  7. Cephalic phase secretion of insulin and other enteropancreatic hormones in humans

    DEFF Research Database (Denmark)

    Veedfald, Simon; Plamboeck, Astrid; Deacon, Carolyn F

    2016-01-01

    Enteropancreatic hormone secretion is thought to include a cephalic phase, but the evidence in humans is ambiguous. We studied vagally induced gut hormone responses with and without muscarinic blockade in 10 glucose-clamped healthy men (age: 24.5 ± 0.6 yr, means ± SE; body mass index: 24.0 ± 0.5 kg...... and abolished the MSF response. Neither insulin, C-peptide, glucose-dependent insulinotropic polypeptide (GIP), nor glucagon-like peptide-1 (GLP-1) levels changed in response to MSF or atropine. Glucagon and ghrelin levels were markedly attenuated by atropine prior to and during the clamp: at t = 105 min...... and 3.7 ± 21 pg/ml (means ± SE), P insulin, glucagon, GLP-1, GIP, and ghrelin....

  8. Datura stramonium poisoning in a child.

    Science.gov (United States)

    Özkaya, Ahmet Kağan; Güler, Ekrem; Karabel, Nihal; Namlı, Ali Rıza; Göksügür, Yalçın

    2015-01-01

    Hallucinogenic plant poisoning in children is a significant problem for the emergency physician. We describe the case of a boy who had slurred speech, fever, hallucinations, tachycardia, dilated pupils, confusion and disorientation. He had no history of drug use or toxin intake. All signs and symptoms were improved by supportive therapy within 48 hours. It turned out that the patient had ingested seeds of Datura stramonium in a neighbor's garden two days previously. The medical history should be taken repeatedly in cases of unknown etiology, and physicians should keep in mind the possibility that unexplained anticholinergic toxidromes could be the result of exposure to toxic plants, in particular those containing atropine and atropine derivates.

  9. Vasoactive intestinal polypeptide (VIP) in the pig pancreas

    DEFF Research Database (Denmark)

    Poulsen, Steen Seier

    1984-01-01

    Vasoactive intestinal polypeptide (VIP) in the pig pancreas is localized to nerves, many of which travel along the pancreatic ducts. VIP stimulates pancreatic fluid and bicarbonate secretion like secretin. Electrical vagal stimulation in the pig causes an atropine-resistant profuse secretion...... of bicarbonate-rich pancreatic juice. In an isolated perfused preparation of the pig pancreas with intact vagal nerve supply, electrical vagal stimulation caused an atropine-resistant release of VIP, which accurately parallelled the exocrine secretion of juice and bicarbonate. Perfusion of the pancreas...... with a potent VIP-antiserum inhibited the effect of vagal stimulation on the exocrine secretion. It is concluded, that VIP is responsible for (at least part of) the neurally controlled fluid and bicarbonate secretion from the pig pancreas....

  10. Parameters for Estimation of Casualties from Ammonia (NH3), Tabun (GA), Soman (GD),Cyclosarin (GF) and Lewisite (L)

    Science.gov (United States)

    2015-09-01

    Dilli et al., “A Non-Accidental Poisoning with Ammonia in Adolescence,” Child : Care, Health and Development 31, no. 6 (November 2005): 737–739. 100... paralysis of the diaphragm, and asphyxiation due to constriction of the bronchial tubes combine with excessive secretions in the air passages. A brief...glands, and the brain and prevents ACh from stimulating the synapse. Because atropine does not bind to nicotinic receptors, neuromuscular symptoms

  11. Pharmacognosy: Science of natural products in drug discovery.

    Science.gov (United States)

    Orhan, Ilkay Erdogan

    2014-01-01

    Pharmacognosy deals with the natural drugs obtained from organisms such as most plants, microbes, and animals. Up to date, many important drugs including morphine, atropine, galanthamine, etc. have originated from natural sources which continue to be good model molecules in drug discovery. Traditional medicine is also a part of pharmacognosy and most of the third world countries still depend on the use of herbal medicines. Consequently, pharmacognosy always keeps its popularity in pharmaceutical sciences and plays a critical role in drug discovery.

  12. Development of Optimized Guidelines for Therapeutic Strategies for Organophosphate Poisoning

    Science.gov (United States)

    2011-03-01

    atropine, oxime, and diazepam . Controversy exists over the use of oxime to treat organophosphate poisoning and various studies have concluded that...exposures to high doses (Cannard, 2006). The anticonvulsant typically used for the treatment of seizures is diazepam (Cannard, 2006). Most armed forces... synthesis of organophosphate insecticides began in the 1930s by German chemist Gerhard Schrader (Szinicz, 2005; Cannard, 2006). Schrader’s work led

  13. [Intoxication with henbane].

    Science.gov (United States)

    Vidović, Domagoj; Brecić, Petrana; Haid, Aleksander; Jukić, Vlado

    2005-01-01

    Henbane, Hyoscyamus niger, is a hallucinogenic plant, widely spread and easy accessible, which contains anticholinergic substances. Ingestion, intentional or accidental, can provoke serious worsening of psychophysical state and can cause even death. Intoxication resembles the one with atropine. Symptoms like mydriasis, tachycardia, arrhythmia, agitation, convulsion and coma can appear. Diagnosis is made by clinical symptomatology and history. Therapeutic acts include stomach lavage, supportive therapy and physostigmine as a specific antidote. Prognosis is usually good.

  14. Black henbane and its toxicity – a descriptive review

    OpenAIRE

    Alizadeh, Anahita; Moshiri, Mohammad; Alizadeh, Javad; Balali-Mood, Mahdi

    2014-01-01

    Black henbane (BH) or Hyoscyamus niger, has been used as a medicine since last centuries and has been described in all traditional medicines. It applies as a herbal medicine, but may induce intoxication accidentally or intentionally. All part of BH including leaves, seeds and roots contain some alkaloids such as Hyoscyamine, Atropine, Tropane and Scopolamine. BH has pharmacological effects like bronchodilating, antisecretory, urinary bladder relaxant, spasmolytic, hypnotic, hallucinogenic, pu...

  15. Antiemetics With Concomitant Sedative Use in Civil Aviation Pilot Fatalities: From 2000 to 2006

    Science.gov (United States)

    2007-10-01

    prescribed to treat motion sickness as well as the adverse side effects of opioid analgesics, general anesthetics , and chemotherapy directed against... lidocaine , and atropine were detected in blood, liver, and lung. Morphine and acet- aminophen were both detected in blood, and morphine was also...containing drug paraphernalia including a green leaf-type substance, which local law enforcement offi cials determined to be consistent with marijuana

  16. [Mystery of mydriatic pupils].

    Science.gov (United States)

    Stefánek, J; Dufincová, J; Vychytil, P; Holmes, S

    2000-11-01

    The authors describe the case of a 27-year-old man who was examined on account of vertigo and blurred vision. In the objective case-history there was mild confusion, in the physical examination broad symmetrical mydriasis dominated. Later other similar patients were found. Atropine intoxication was proved. The source of the alkaloid was poppy seed contaminated with seeds of henbane (Hyoscyamus niger), in bakery goods served in the works canteen.

  17. Acute effects of a sarin-like organophosphorus agent, bis(isopropyl methyl)phosphonate, on cardiovascular parameters in anaesthetized, artificially ventilated rats

    Energy Technology Data Exchange (ETDEWEB)

    Watanabe, Yoshimasa [Department of Pharmacology, Graduate School of Medical Sciences, Nagoya City University, Nagoya (Japan); Itoh, Takeo, E-mail: titoh@med.nagoya-cu.ac.jp [Department of Pharmacology, Graduate School of Medical Sciences, Nagoya City University, Nagoya (Japan); Shiraishi, Hiroaki [Department of Forensic Medicine, Institute of Biomedical and Health Sciences, Hiroshima University, Hiroshima (Japan); Maeno, Yoshitaka [Department of Forensic Medical Science, Graduate School of Medical Sciences, Nagoya City University, Nagoya (Japan); Arima, Yosuke; Torikoshi, Aiko; Namera, Akira [Department of Forensic Medicine, Institute of Biomedical and Health Sciences, Hiroshima University, Hiroshima (Japan); Makita, Ryosuke [Department of Nursing, Faculty of Health Sciences, Hiroshima Cosmopolitan University, Hiroshima (Japan); Yoshizumi, Masao [Department of Cardiovascular Physiology and Medicine, Institute of Biomedical and Health Sciences, Hiroshima University, Hiroshima (Japan); Nagao, Masataka [Department of Forensic Medicine, Institute of Biomedical and Health Sciences, Hiroshima University, Hiroshima (Japan)

    2013-10-01

    The organophosphorus compound sarin irreversibly inhibits acetylcholinesterase. We examined the acute cardiovascular effects of a sarin-like organophosphorus agent, bis(isopropyl methyl)phosphonate (BIMP), in anaesthetized, artificially ventilated rats. Intravenous administration of BIMP (0.8 mg/kg; the LD50 value) induced a long-lasting increase in blood pressure and tended to increase heart rate. In rats pretreated with the non-selective muscarinic-receptor antagonist atropine, BIMP significantly increased both heart rate and blood pressure. In atropine-treated rats, hexamethonium (antagonist of ganglionic nicotinic receptors) greatly attenuated the BIMP-induced increase in blood pressure without changing the BIMP-induced increase in heart rate. In rats treated with atropine plus hexamethonium, intravenous phentolamine (non-selective α-adrenergic receptor antagonist) plus propranolol (non-selective β-adrenergic receptor antagonist) completely blocked the BIMP-induced increases in blood pressure and heart rate. In atropine-treated rats, the reversible acetylcholinesterase inhibitor neostigmine (1 mg/kg) induced a transient increase in blood pressure, but had no effect on heart rate. These results suggest that in anaesthetized rats, BIMP induces powerful stimulation of sympathetic as well as parasympathetic nerves and thereby modulates heart rate and blood pressure. They may also indicate that an action independent of acetylcholinesterase inhibition contributes to the acute cardiovascular responses induced by BIMP. - Highlights: • A sarin-like agent BIMP markedly increased blood pressure in anaesthetized rats. • Muscarinic receptor blockade enhanced the BIMP-induced increase in blood pressure. • Ganglionic nicotinic receptor blockade attenuated the BIMP-induced response. • Blockade of α- as well as β-receptors attenuated the BIMP-induced response.

  18. Role of M1 receptor in regulation of gastric fundus smooth muscle contraction

    Directory of Open Access Journals (Sweden)

    Marta Gajdus

    2011-09-01

    Full Text Available Background:The subject of this study is determination of the influence of drugs on gastric fundus smooth muscle contraction induced by activation of muscarinic receptors M1. Experiments tested interactions between a receptor agonist, carbachol and muscarinic receptor antagonists, atropine and pirenzepine.Material/Methods:Testing was conducted on tissues isolated from rat’s stomach. Male Wistar rats with weight between 220 g and 360 g were anesthetized by intraperitoneal injection of urethane (120 mg/kg. The stomach was dissected, and later the gastric fundus was isolated. Tissue was placed in a dish for insulated organs with 20 ml in capacity, filled with Krebs fluid. Results contained in the study are average values ± SE. In order to determine statistical significance, the principles of receptor theory were used (Kenakin modification.Results:According to tests, carbachol, in concentrations ranging between 10–8 M to 10–4 M, in a dosage-dependent way induces gastric fundus smooth muscle contraction. Presented results indicate that carbachol meets the conditions posed to full agonists. On the other hand, atropine, a non-selective muscarinic receptor antagonist, causes a concentration-dependent shift of concentration-effect curve (for carbachol to the right, maintaining maximum reaction. According to analysis of the curve determined, we can deduce that atropine meets the conditions posed to competitive antagonists. The use of pirenzepine, a competitive receptor agonist M1, causes shift of concentration-effect curve (for carbachol to the right, maintaining maximum reaction.Conclusions:From the testing conducted on the preparation of the gastric fundus we can deduce that atropine causes shift of concentration-effect curves for carbachol to the right. A similar effect is released by pirenzepine, selectively blocking muscarinic receptors of M1 type. The results indicate that in the preparation of the gastric fundus smooth muscle, M1 type

  19. Interactions between anticholinesterases in an in vitro central nervous system preparation

    OpenAIRE

    Scott, Iain Ratcliffe

    2008-01-01

    Organophosphate compounds have been widely developed as pesticides (e.g. paraoxon) and also as chemical warfare agents (nerve agents, e.g. sarin). These compounds rapidly inhibit the enzyme acetylcholinesterase (AChE), causing overstimulation within the cholinergic nervous system. If left untreated, this can be fatal. Current medical countermeasures to nerve agent poisoning consist of pretreatment with pyridostigmine and an emergency therapy comprising atropine, diazepam and pr...

  20. A Characterization of Carboxylesterases in Rat and Guinea Pig - Their Heterogeneity and Role in Detoxication of Organophosphorus Compounds

    Science.gov (United States)

    1993-09-01

    serine esterases in man, rat and guinea pig capable of hydrolysing acetylsalicylic acid with different properties from the microsomal enzymes...e.g., acetylsalicylic acid , cocaine, procaine or atropine is terminated by enzymatic cleavage of their ester bond. Other examples are hydro- lysis of... properties [181. They possess an identical E 25 25 amino acid sequence, but possibly these two forms differ a in their glycosylation [2[. Robbi and

  1. 1231-IJBCS-Article-Aklesso Mouzou

    African Journals Online (AJOL)

    KODJIO NORBERT

    métacholine (MTC) (40 mM), Trema guineensis (Celtidacea) provoquerait une relaxation dose-dépendante. L'extrait aurait une action sur les canaux calciques. En outre, cette solution semi-éthanolique aurait une action similaire (diminution de la contracture) à celle de l'atropine sur l'iléon de rat précontracturé à la MTC.

  2. Searching for the Cases of Acute Organophosphorus Pesticides Poisoning by JOIS

    Science.gov (United States)

    Futagami, Kojiro; Fujii, Toshiyuki; Horioka, Masayoshi; Asakura, Hajime; Fukagawa, Mitsuro

    Cholinesterase reactivator PAM (Pralidoxime) is used in the treatment of organophosphates poisoning with anticholinergic agent atropine. However, some reports demonstrated recently that PAM has inefficacy in some cases of so-called low toxicity organophosphates poisoning. So, to atempt to discuss the efficacy of PAM in clinical treatment, we searched for the case reports of these poisoning by JOIS. In this time, we compared with the specificity of each data bases and presented some examples in this on-line information retrieval.

  3. [Acute poisoning by pesticides in children].

    Science.gov (United States)

    Leveau, P

    2016-07-01

    Acute pesticide poisoning in children is rare but potentially serious. Some clinical patterns (toxidromes) are suggestive of the drug class: cholinergic crisis for organophosphate or carbamate insecticides; neurological syndrome for rodenticides; digestive and respiratory syndrome for herbicides. Treatment is symptomatic and only a few patients are treated with an antidote: atropine and pralidoxime for organophosphate insecticides, vitamin K for anticoagulant rodenticides. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  4. EPULIS AND ITS SURGICAL TREATMENT IN A SPITZ BITCH

    Directory of Open Access Journals (Sweden)

    A.K. Maji

    2015-12-01

    Full Text Available One Spitz bitch of about 7 years of age with pedunculated soft tissue mass at upper left corner molar teeth was presented. Local excision under Atropine - Xylazine - Ketamine - Diazepam combined administration was performed with red hot iron thermo-cauterization. The excised mass on histopathology showed squamous hyperplasia with fibrous network and angiogenesis interpreting fibrous epulis. No recurrence was observed or no chemotherapy was needed up to one year post operation.

  5. Datura stramonium L. poisoning in a geophagous child: a case report.

    Science.gov (United States)

    Bouziri, Asma; Hamdi, Asma; Borgi, Aida; Hadj, Sarra Bel; Fitouri, Zohra; Menif, Khaled; Ben Jaballah, Nejla

    2011-06-15

    Datura stramonium L. (DS) is a wild-growing plant widely distributed and easily accessible. It contains a variety of toxic anticholinergic alkaloids such as atropine, hyoscamine, and scopolamine. Voluntary or accidental ingestion can produce severe anticholinergic poisoning. We report an unusual case of DS intoxication occurring in a geophagous young child after accidental ingestion of the plant. Our case is original because of the young age of the victim and the underlying geophagia facilitating the occurrence of poisoning.

  6. Optimization of Quantitative Proteomics Using 2-Dimensional Difference Gel Electrophoresis to Characterize Molecular Mechanisms of Chemical Warfare Nerve Agent Exposure in the Rat Brain

    Science.gov (United States)

    2010-11-01

    sodium cacodylate buffer, post-fixed in 1% osmium tetroxide/0.1M sodium cacodylate buffer, dehydrated in graded ethanol , and embedded in PolyBed 812...and J.H. McDonough, Efficacy of biperiden and atropine as anticonvulsant treatment for organophosphorus nerve agent intoxication . Archives of...Methods in Toxicology, 1993. 2: p. 41-50. 18. Venkatraman, A., et al., Modification of the mitochondrial proteome in response to the stress of ethanol

  7. Dopamine-induced amylase secretion from rat parotid salivary gland in vitro: an effect mediated via noradrenergic and cholinergic nerves.

    OpenAIRE

    Hata, F.; Ishida, H.; Kondo, E

    1986-01-01

    The effect of dopamine on amylase secretion by rat parotid tissue was examined in vitro. Dopamine induced marked amylase secretion from the tissue in a dose-dependent manner. Its EC50 value was about 4 microM and the maximal response was obtained at a concentration of 100 microM. The dopamine-induced secretion was inhibited by the dopamine-antagonists haloperidol, (+)-butaclamol and spiroperidol. Atropine reduced the dopamine-induced secretion significantly, and physostigmine enhanced the sec...

  8. Novel neuroprotective and hepatoprotective effects of citric acid in acute malathion intoxication.

    Science.gov (United States)

    Abdel-Salam, Omar M E; Youness, Eman R; Mohammed, Nadia A; Yassen, Noha N; Khadrawy, Yasser A; El-Toukhy, Safinaz Ebrahim; Sleem, Amany A

    2016-12-01

    To study the effect of citric acid given alone or combined with atropine on brain oxidative stress, neuronal injury, liver damage, and DNA damage of peripheral blood lymphocytes induced in the rat by acute malathion exposure. Rats were received intraperitoneal (i.p.) injection of malathion 150 mg/kg along with citric acid (200 or 400 mg/kg, orally), atropine (1 mg/kg, i.p.) or citric acid 200 mg/kg + atropine 1 mg/kg and euthanized 4 h later. Malathion resulted in increased lipid peroxidation (malondialdehyde) and nitric oxide concentrations accompanied with a decrease in brain reduced glutathione, glutathione peroxidase (GPx) activity, total antioxidant capacity (TAC) and glucose concentrations. Paraoxonase-1, acetylcholinesterase (AChE) and butyrylcholinesterase activities decreased in brain as well. Liver aspartate aminotransferase and alanine aminotransferase activities were raised. The comet assay showed increased DNA damage of peripheral blood lymphocytes. Histological damage and increased expression of inducible nitric oxide synthase (iNOS) were observed in brain and liver. Citric acid resulted in decreased brain lipid peroxidation and nitric oxide. Meanwhile, glutathione, GPx activity, TAC capacity and brain glucose level increased. Brain AChE increased but PON1 and butyrylcholinesterase activities decreased by citric acid. Liver enzymes, the percentage of damaged blood lymphocytes, histopathological alterations and iNOS expression in brain and liver was decreased by citric acid. Meanwhile, rats treated with atropine showed decreased brain MDA, nitrite but increased GPx activity, TAC, AChE and glucose. The drug also decreased DNA damage of peripheral blood lymphocytes, histopathological alterations and iNOS expression in brain and liver. The study demonstrates a beneficial effect for citric acid upon brain oxidative stress, neuronal injury, liver and DNA damage due to acute malathion exposure. Copyright © 2016 Hainan Medical University. Production

  9. Poisoned after Dinner: Dolma with Datura Stramonium

    OpenAIRE

    Disel, Nezihat Rana; Yilmaz, Mustafa; Kekec, Zeynep; KARANLIK, Meryem

    2016-01-01

    SUMMARY: Datura stramonium, which is also known as Thorn Apple or Jimson Weed, is an alkaloid containing plant that is entirely toxic. The active toxic constituents of the plant are atropine, scopolamine and hyoscyamine. It has been abused worldwide for hundreds of years because of its hallucinogenic properties. Previous reports have shown that herbal medication overdose and accidental food contamination are ways it can cause poisoning. Herein we present a family that had three of its members...

  10. Modulation of the Cholinergic Mechanisms in the Bronchial Smooth Muscle.

    Science.gov (United States)

    1984-06-01

    recent studies with radiotracer tech- niques suggest a moderate enhanchement of transmitter release during atropine inhibition in the absence of...INTRODUCTION Intoxications with organophosphorus cholinesterase inhibitors used as insecticides constitute an increasing problem in industrial and agri...part of the airflow is passed through the diffusion cell and one part through a bypass. Traces of oil residues and water vapour were removed from the

  11. Intrinsic Cholinergic Mechanisms Regulating Cerebral Blood Flow as a Target for Organophosphate Action.

    Science.gov (United States)

    1985-10-01

    will facilitate the vasodilation associated with cortical arousal or hypercapnia, an effect blocked by atropine (see Scremin 1982, for review ) and that...stimulation of the fastiglal nucleus (FN) on ICBF (mean S.E.M.) int d ralyzed tanesthetized pral rat. n_ -31- Pons - Vestibular comp. R 189 +- 15 346...sources for the cholinergic link in this pathway are local cholinergic neurons of the cortex, or nerve terminals of afferent cholinergic fibers arising

  12. Beta-Blockers: An Abstracted Bibliography.

    Science.gov (United States)

    1989-04-04

    32 Acetylcholine increased tie 3p labeling of Phosphatidic acid (140-205%) and Phosphatidylinositol (175%-229%). Acety holine stimulation was blocked... Muscle . REFERENC-E Advance& ir Expeaim~ental Medicine and BI&1q.&.y, Vol. 72, pp. 227-256,1976. DRUGS: Eserine di-Propranolol So taM ol Norepinephrine...NE) Acetyicholine (Ach) Atropine SUBJECT: Rabbit iris muscle PREDJKDURE: Labeling study on incubated mixtures containing the iris muscle . FINDINGS

  13. Estimating 'lost heart beats' rather than reductions in heart rate during the intubation of critically-ill children.

    Science.gov (United States)

    Jones, Peter; Ovenden, Nick; Dauger, Stéphane; Peters, Mark J

    2014-01-01

    Reductions in heart rate occur frequently in children during critical care intubation and are currently considered the gold standard for haemodynamic instability. Our objective was to estimate loss of heart beats during intubation and compare this to reduction in heart rate alone whilst testing the impact of atropine pre-medication. Data were extracted from a prospective 2-year cohort study of intubation ECGs from critically ill children in PICU/Paediatric Transport. A three step algorithm was established to exclude variation in pre-intubation heart rate (using a 95%CI limit derived from pre-intubation heart rate variation of the children included), measure the heart rate over time and finally the estimate the numbers of lost beats. 333 intubations in children were eligible for inclusion of which 245 were available for analysis (74%). Intubations where the fall in heart rate was less than 50 bpm were accompanied almost exclusively by less than 25 lost beats (n = 175, median 0 [0-1]). When there was a reduction of >50 bpm there was a poor correlation with numbers of lost beats (n = 70, median 42 [15-83]). During intubation the median number of lost beats was 8 [1]-[32] when atropine was not used compared to 0 [0-0] when atropine was used (pheart rate during intubation of heart rate was >50 bpm the heart rate was poorly predictive of lost beats. A study looking at the relationship between lost beats and cardiac output needs to be performed. Atropine reduces both fall in heart rate and loss of beats. Similar area-under-the-curve methodology may be useful for estimating risk when biological parameters deviate outside normal range.

  14. Changes in intraocular pressure and horizontal pupil diameter during use of topical mydriatics in the canine eye

    Directory of Open Access Journals (Sweden)

    Liga Kovalcuka

    2017-01-01

    Full Text Available The objective of this study was to determine the effects of topical 0.5% tropicamide, 1% atropine sulphate and 10% phenylephrine hydrochloride ophthalmic solutions on intraocular pressure (IOP and horizontal pupil diameter (HPD in the dog during the first hour after treatment. Forty clinically and ophthalmologically normal canine patients (between the ages of 2 and 6 years of varying breed and sex were used in this study. Animals were randomly divided into four groups of ten and given one drop of tropicamide, atropine, phenylephrine or saline into one eye. IOP and HPD were measured in both eyes every 5 minutes for 60 minutes. Tropicamide increased IOP by 8.8±4.0 mmHg 35 minutes post-treatment compared to pre-treatment (P<0.01 only in treated eye. IOP in the contralateral eye did not increase. With atropine the maximum increase in IOP was 2.6±2.8 mmHg at 20 minutes post treatment in the treated eye (P<0.01. IOP in the contralateral eye did not increase. Phenylephrine increased IOP by 2.3±2.1 mmHg (P<0.05 10 minutes after treatment. Also in the untreated eye IOP increased by 2.3±2.1 mmHg, 20 minutes post-treatment. Maximum HPD in eyes treated with tropicamide occurred at 55 minutes and with atropine at 60 minutes. There were no HPD changes in the contralateral, untreated eye. Topical 10% phenylephrine showed maximal pupil dilation 60 minutes after treatment, but the HPD of the – untreated eye slightly decreased at 15 minutes, but this change only reached statistical significance at 40 min post- treatment (P<0.05. Normal saline showed no influence on IOP or HPD. The drugs investigated here show a significant increase in IOP after mydriatics.

  15. Self-generated theta oscillations in the hippocampus.

    Science.gov (United States)

    Goutagny, Romain; Jackson, Jesse; Williams, Sylvain

    2009-12-01

    Hippocampal theta rhythm is crucial for spatial memory and is thought to be generated by extrinsic inputs. In contrast, using a complete rat hippocampus in vitro, we found several intrinsic, atropine-resistant theta generators in CA1. These oscillators were organized along the septotemporal axis and arose independently from CA3. Our results suggest that CA1 theta rhythm can emerge from the coupling of multiple autonomous hippocampal theta oscillators.

  16. Posterior reversible encephalopathy syndrome in a patient of organophosphate poisoning

    OpenAIRE

    Rajesh Phatake; Sameer Desai; Manikanth Lodaya; Shrinivas Deshpande; Nagaraj Tankasali

    2014-01-01

    A 32-year-old male presented with a history of consuming some organophosphorous compound with suicidal intention. He was treated with atropine, pralidoxime, ventilator support. During stay patient had persistent irritability, tachycardiaand hypertension despite sedation and labetalol infusion. He developed headache, visual blurring hemiparesis and focal seizures. Magnetic resonance imaging of the brain revealed multifocal hyperintensities mainly in subcortical areas of parietal and occipital ...

  17. Pilot experiments on the actions of drugs injected into the human corpus cavernosum penis.

    OpenAIRE

    Brindley, G. S.

    1986-01-01

    Seven drugs that are known to relax smooth muscle (phenoxybenzamine, phentolamine, thymoxamine, imipramine, verapamil, papaverine, naftidrofuryl) caused erection when injected intracavernosally. Salbutamol, hydralazine, lignocaine and bupivacaine caused tumidity but not erection. Metaraminol and guanethidine caused shrinkage followed by tumidity. Neostigmine, atropine, propranolol and idazoxan had no effect in the doses tried. It is argued that the seven drugs that cause erection do so by rel...

  18. Identification and treatment of amblyopia.

    Science.gov (United States)

    Bradfield, Yasmin S

    2013-03-01

    Amblyopia is the leading cause of vision loss in children. It is treatable if diagnosed early, making identification of affected children critical. The American Association for Pediatric Ophthalmology and Strabismus and the American Academy of Pediatrics recommend that clinicians routinely perform age-appropriate vision chart testing, red reflex testing, and examination for signs of strabismus. The U.S. Preventive Services Task Force recommends vision screening for all children at least once between three and five years of age to detect the presence of amblyopia or its risk factors. Photoscreening may be a useful adjunct to traditional vision screening, but there is limited evidence that it improves visual outcomes. Treatments for amblyopia include patching, atropine eye drops, and optical penalization of the nonamblyopic eye. In children with moderate amblyopia, patching for two hours daily is as effective as patching for six hours daily, and daily atropine is as effective as daily patching. Children older than seven years may still benefit from patching or atropine, particularly if they have not previously received amblyopia treatment. Amblyopia recurs in 25 percent of children after patching is discontinued. Tapering the amount of time a patch is worn each day at the end of treatment reduces the risk of recurrence.

  19. Respiratory mechanics and lung histology in normal rats anesthetized with sevoflurane.

    Science.gov (United States)

    Correa, F C; Ciminelli, P B; Falcão, H; Alcântara, B J; Contador, R S; Medeiros, A S; Zin, W A; Rocco, P R

    2001-08-01

    Respiratory system, lung, and chest wall mechanical properties were subdivided into their resistive, elastic, and viscoelastic/inhomogeneous components in normal rats, to define the sites of action of sevoflurane. In addition, we aimed to determine the extent to which pretreatment with atropine modified these parameters. Twenty-four rats were divided into four groups of six animals each: in the P group, rats were sedated (diazepam) and anesthetized with pentobarbital sodium; in the S group, sevoflurane was administered; in the AP and AS groups, atropine was injected 20 min before sedation/anesthesia with pentobarbital and sevoflurane, respectively. Sevoflurane increased lung viscoelastic/inhomogeneous pressures and static elastance compared with rats belonging to the P group. In AS rats, lung static elastance increased in relation to the AP group. In conclusion, sevoflurane anesthesia acted not at the airway level but at the lung periphery, stiffening lung tissues and increasing mechanical inhomogeneities. These findings were supported by the histological demonstration of increased areas of alveolar collapse and hyperinflation. The pretreatment with atropine reduced central and peripheral airway secretion, thus lessening lung inhomogeneities.

  20. Protection by tacrine and some adjuncts against the depressant effects of soman in guinea-pig atrium. (Reannouncement with new availability information)

    Energy Technology Data Exchange (ETDEWEB)

    Lau, W.M.

    1993-12-31

    The negative inotropic effects of soman have been reported previously. It was suggested that the depression in atrial force of contraction was a consequence of continuous muscarinic receptor activation by excessive acetylcholine (ACh) accumulation and also possibly through direct interactions at the receptor-associated K+ channels by organophosphate (OP). In this study, the protective effects of tacrine (THA), an antimuscarinic as well as a K+ channel blocker, against soman in guinea-pig atrium were investigated. It was found that tacrine could antagonize the negative inotropic effects of soman. This antagonism occurred in a concentration dependent manner, with effective concentrations (ECs) for tacrine ranging from 1.7 to 12.1 micrometers when the atrium was equilibrated with 0.05-10 micrometers soman. Inclusion of an oxime HI-6 (100 micrometers) in the regimen improved the efficacy of tacrine against soman (1 micrometer) by 16.1 fold. Addition of a potent antimuscarinic, either atropine or glycopyrrolate with tacrine also improved tacrine`s efficacy against soman significantly. Atropine, at equivalent concentration, appeared to be the most effective of the three. At 0.1 micrometers concentration, atropine was 4.25 and 3.47 times more potent than HI-6 and glycopyrrolate respectively in enhancing THA efficacy.

  1. Feeding on toxic prey. The praying mantis (Mantodea) as predator of poisonous butterfly and moth (Lepidoptera) caterpillars.

    Science.gov (United States)

    Mebs, Dietrich; Wunder, Cora; Pogoda, Werner; Toennes, Stefan W

    2017-06-01

    Caterpillars of the monarch butterfly, Danaus plexippus, feed on milkweed plants, Asclepias spp. (Apocynaceae), and sequester their toxic cardenolides aimed at deterring predators. Nevertheless, Chinese praying mantids, Tenodera sinensis, consume these caterpillars after removing the midgut ("gutting") including its plant content. In the present study, monarch caterpillars raised on A. curassavica, and those of the death's-head hawkmoth, Acherontia atropos, raised on Atropa belladonna containing atropine, were fed to mantids, Hierodula membranacea, which removed the gut of both species discarding about 59% of cardenolides and more than 90% of atropine, respectively. The ingestion of these compounds produced no apparent ill effects in the mantids and both were excreted with faeces. On the other hand, when mantids were fed with larvae of two moth species, Amata mogadorensis and Brahmaea certia, raised on non-poisonous host plants, the mantids showed the same gutting behaviour, thereby discarding indigestible plant material. As polar compounds, e.g. cardenolides and atropine, are not absorbed from the mantids midgut and do not pass the gut membrane, this enables the mantids to feed on toxic prey. Copyright © 2017 Elsevier Ltd. All rights reserved.

  2. Role of glutamatergic system in nerve agent intoxication

    Energy Technology Data Exchange (ETDEWEB)

    Blanchet, G.; Lallement, G.; Carpentier, P.; De Groot, D.; Bodjarian, N.

    1993-05-13

    Our recent studies concerning soman-induced seizures mechanisms and subsequent brain damage are reviewed. (1) Seizure activity was associated with transient increases of extracellular concentrations of acetylcholine (ACh) and with long-lasting releases of glutamate (Glu) in all limbic areas studied. (2) Preventive intraseptal application of atropine abolished the hippocampal increases of extracellular AChi and Glu indicating a key role of septum in triggering seizure activity. (3) Early increases of hippocampal AMPA receptor binding occurred before activation of NMDA receptors. (4) Pretreatment with NBQX, an antagonist of AMPA receptor, prevented convulsions and brain damage even without atropine. In the same conditions, no protection was afforded by TCP, a non-competitive antagonist of the NMDA receptor. (5) On the contrary, in the presence of pyridostigmine and atropine, TCP blocked the seizures induced by 2 x LD50 of soman. The anticonvulsant potency of TCP was particularly obvious when administered curatively. (6) Mossy fibers sprouting takes place in the supragranular-molecular layers of rat hippocampus long after brain injury associated with abnormal neuronal excitability. (7) Altogether, it appears that an AMPA component is involved in combination with cholinergic mechanisms in initiating seizures. A subsequent and long-lasting recruitment of NMDA receptors is then essential in sustaining the seizures. New anticonvulsant and neuroprotective approaches using Glu antagonists against nerve agents intoxication are discussed.

  3. Effect of Urea Fertilizer on the Weight of Different Parts of Datura stramonium and their Alkaloidal Contents at Different Developmental Stages

    Directory of Open Access Journals (Sweden)

    S. Afsharypuor

    1997-08-01

    Full Text Available Plants of Datura Stramonium var. stramonium were cultivated in pots at different nitrogen levels (60,120, 180, 240, and 300 kg/ha using urea fertilizer as the nitrogen source. At various developmental stages, the weights of different parts of the plants which recieved 60-240 kg N/ha were significantly increased as compared with the relevant parts of untreated (control plants. The 240 kg N/ha usually caused the highest increases in the weights of different parts of the plant."nAtropine and scopolamine contents of each dried part of the plant were determined by a previously published TLC-spectrophotometric method. The stem of 80 days old pretreated plants with 180 kg N/ha accumulated significantly the highest percentages of atropine and scopolamine. However, the 120 kg N/ha level caused the highest enhancement in the yield of atropine (65.24 % and scopolamine (40.38% in the whole plant during the reproductive (80 days old stage as compared with the yield of these alkaloids in the relevant controls.

  4. [Toxicological analysis of a case of Datura stramonium poisoning].

    Science.gov (United States)

    Matsuda, Kimiko; Morinaga, Mutsuko; Okamoto, Misao; Miyazaki, Shuhei; Isimaru, Tsuyoshi; Suzuki, Kouichiro; Tohyama, Kaoru

    2006-10-01

    We encountered a patient in a restless excitable state after eating boiled jimson weed grown in the patient's garden. The patient mistook the weed for Angelica keiskei. Pupillary dilation (7/7mm), weak light reflex, body temperature of 37 degrees C, respiratory frequency of 19/min, blood pressure of 138/88 mmHg, pulse rate of 108/min, and hot feeling were observed. No abnormalities nor special findings were detected by general examination of the peripheral blood, biochemical examination of the blood, general examination of the urine, or electrocardiography. Atropine and scopolamine, which are tropane alkaloids, were detected by the GC/MS. The retention time of atropine-TMS was 17.0 min, and the mass spectra were m/z 124, 82, and 140. The retention time of scopolamine-TMS was 17.7 min, and the mass spectra were m/z 138, 108, 154 and 375. At the time of consultation, the serum concentrations of atropine and scopolamine were 31.3 ng/ml, and 30.6 ng/ml, respectively, and decreased to 6.7 ng/ml and 8.5 ng/ml, respectively, after 2 hours. The patient underwent injection of activated carbon after gastrolavage with 2,000 ml warm water, and neostigmine was administered. The patient awoke the following morning, and was discharged with mild pupillary dilation 2 days after poisoning.

  5. Role of the thalamic parafascicular nucleus cholinergic system in the modulation of acute corneal nociception in rats

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    Esmaeal Tamaddonfard

    2011-11-01

    Full Text Available The present study investigated the effects of microinjections of acetylcholine (a cholinergic agonist, physostigmine (a cholinesterase inhibitor, atropine (an antagonist of muscarinic cholinergic receptors and hexamethonium (an antagonist of nicotinic cholinergic receptors into the parafascicular nucleus of thalamus on the acute corneal nociception in rats. Acute corneal nociception was induced by putting a drop of 5 M NaCl solution onto the corneal surface of the eye and the number of eye wipes was counted during the first 30s. Both acetylcholine and physostigmine at the same doses of 0.5, 1 and 2 μg significantly (P < 0.05 reduced the number of eye wipes. The intensity of corneal nociception was not changed when atropine and hexamethonium were used alone. Atropine (4 μg, but not hexamethonium (4 μg significantly (P < 0.05 prevented acetylcholine (2 μg- and physostigmine (2 μg-induced antinociceptive effects. The results indicated that at the level of the parafascicular nucleus of thalamus, the muscarinic cholinergic receptors might be involved in the antinociceptive effects of acetylcholine and physostigmine.

  6. Inhibitory effect of the nucleus reticularis pontis oralis on the pontine micturition center and pontine urine storage center in decerebrate cats.

    Science.gov (United States)

    Sugaya, Kimio; Nishijima, Saori; Miyazato, Minoru; Oda, Masami; Ogawa, Yoshihide

    2006-10-01

    The influence of the nucleus reticularis pontis oralis (PoO) on the pontine micturition center (PMC) and pontine urine storage center (PUSC) was examined in decerebrate cats by electrical and chemical stimulations of the PMC, PUSC or PoO. Microinjection of carbachol into the rostral and dorsolateral part of the PoO rapidly inhibited reflex micturition and external urethral sphincter (EUS) activity. After confirming the inhibition of reflex micturition and EUS activity by microinjection of carbachol into the PoO, intravenous injection of atropine sulfate or its microinjection into the PoO recovered both reflex micturition and EUS activity. Microinjection of carbachol into the PMC evoked micturition and then inhibited reflex micturition, but intravenous injection of atropine or its microinjection into the PoO recovered reflex micturition. After confi rming the inhibition of reflex micturition and EUS activity by microinjection of carbachol into the PoO, electrical stimulation of the PUSC enhanced EUS activity, but electrical stimulation of the PMC failed to evoke micturition. However, electrical stimulation of the PMC evoked micturition after microinjection of atropine into the PoO. These results suggest that the PoO strongly inhibits the PMC and less strongly inhibits the PUSC. Therefore, the PoO seems to be the pontine micturition inhibitory area.

  7. Effects of topical fucosyl-lactose, a milk oligosaccharide, on dry eye model: an example of nutraceutical candidate

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    Claudio eBucolo

    2015-11-01

    Full Text Available Purpose: Colostrum has been proposed to treat severe dryness and problematic eye lesions showing a beneficial effect. The aim of the study was to investigate the effect of 2-fucosyl-lactose, a natural sugar present in the human colostrum, in an experimental dry eye. Methods: Dry eye was induced in adult male New Zealand albino rabbits by topical administration of 1% atropine. Tear volume (Schirmer’s test, tear film breakup time (TBUT, corneal staining and tear osmolarity were assessed. Fucosyl-lactose eye drops was instilled at different concentrations (0.01%, 0.1%, 1%. Results: After 24 hours from first atropine administration, tear volume and TBUT values were significantly improved in groups treated with 2-flucosyl-lactose in a dose-dependent manner. Tear volume increased from 5.25 to 10.75 mm and TBUT values from 8.75 to 34.5 seconds with 0.01% or 1% 2-flucosyl-lactose treatment, respectively. No changes were observed in terms of corneal staining among the all groups treated with 2-fucosyl-lactose. Atropine instillation caused an increase of tear osmolarity (428 mOsm/L, which was reversed by topical treatment with 2-fucosyl-lactose at all doses.Conclusions: The present study demonstrated that 2-fucosyl-lactose, a human milk oligosaccharide, has protective effect on tear film stability.

  8. [Treatment of spontaneous dissociated vertical deviation with the pharmacological penalization of the fixing eye].

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    Arroyo-Yllanes, María Estela; Galicia-Castillo, Blanca Adriana; Pérez-Pérez, José Fernando

    2005-01-01

    Dissociated vertical deviation (DVD) is a common innervational entity frequently found in patients with congenital endotropia. It is characterized as being bilateral, asymmetric, and to a greater extent, in the non-fixating eye. It can be compensatory or non-compensatory. In the majority of cases, surgery is the treatment of choice, but spontaneous appearance of DVD is a common occurrence after surgery, sometimes to a degree similar to that prior to surgery. Our aim was to evaluate the behavior of dissociated vertical deviation with penalization of the fixating eye. An experimental and longitudinal study was conducted in which patients with spontaneous DVD were included, whether or not associated with horizontal deviation, with or without previous surgery. Atropine (1%) was applied every 24 h in the fixating eye for 3 months and DVD presence, magnitude, and spontaneity were evaluated at 15 days, 1 month, 3 months, and 1 month after penalization suspension. Eight patients were included. DVD magnitude decreased with penalization (p = 0.02) and remained unchanged when atropine was suspended (p = 0.6). With regard to decompensatory phases, DVD shifted from spontaneous to non-spontaneous during penalization (p = 0.01); when this was eliminated, deviation showed decompensation again (p = 0.03). Fixating eye penalization with 1% atropine reduces DVD magnitude and decompensatory phases during follow-up.

  9. Anticonvulsant actions of anticholinergic drugs in soman poisoning.

    Science.gov (United States)

    Capacio, B R; Shih, T M

    1991-01-01

    The acute effects of the organophosphorus cholinesterase inhibitor soman include hypersecretions, convulsions, and death. The purpose of this study was to evaluate the anticholinergic compounds aprophen, atropine sulfate, azaprophen, benactyzine, benztropine, biperiden, scopolamine HBr, and trihexyphenidyl for their efficacy in preventing soman-induced hypersecretions and convulsions. Male rats were injected with the oxime HI-6 (125 mg/kg, i.p.), to increase survival time, along with various intramuscular doses of the anticholinergics 30 min prior to a dose of soman (180 micrograms/kg, s.c.; equivalent to 1.6 x the median lethal dose) that produced 100% convulsions. Signs of intoxication as well as the time-to-onset of convulsions were observed. The calculated anticonvulsant median effective dose values were 0.18, 0.33, 0.36, 0.55, 2.17, 2.30, 2.45, and 31.09 mumol/kg for scopolamine HBr, biperiden, trihexyphenidyl, benactyzine, benztropine, azaprophen, aprophen, and atropine sulfate, respectively. The same rank order of potency for inhibition of hypersecretions among these compounds was observed. Parallel studies with quaternary analogs of atropine sulfate and scopolamine HBr demonstrated, however, that these charged compounds afford no protection against soman-induced hypersecretions and convulsions. The results indicate that tertiary anticholinergic compounds afford protection against soman-induced convulsions and hypersecretions and that the beneficial anticonvulsant effects are mediated through the central cholinergic system. Excitatory amino acid neurotransmitter systems may be involved in the effectiveness of these compounds.

  10. Effect of oral administration of Terminalia chebula on gastric emptying: an experimental study.

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    Tamhane M

    1997-01-01

    Full Text Available Terminalia chebula is a commonly advocated agent in Ayurveda for improving gastrointestinal motility. Charles Foster rats (150-200 gms of either sex were divided into four groups as follows--Group 1 (n = 15 normal animals; Group II (n = 6 rats administered metoclopramide (1.35 mg/kg; Group III (n = 8 rats given atropine (0.45 mg/kg. These agents were injected intramuscularly, 30 mins before the experiment. Rats from Group IV (n = 8 were administered Terminalia chebula (100 mg/kg/day for 15 days orally. Metoclopramide and atropine have established prokinetic and antikinetic activities respectively and are therefore included for comparison. All rats were then given a test meal of methyl cellulose (1.5% mixed with phenol red (50 mg/100 ml orally and gastric emptying was measured 20 mins later. Gastric emptying of normal rats (Group I was found to be 51.6 +/- 7.79%. Metoclopramide significantly increased the gastric emptying (76.33 +/- 12.37%; p < 0.01 and atropine inhibited the motility (% gastric emptying being 7.26 +/- 19.76%; p < 0.01. Terminalia chebula was found to increase the percent gastric emptying (86.57 +/- 6.65%; p < 0.01. Thus from this study it appears that Terminalia chebula can serve as an useful alternative to prokinetic drugs available today.

  11. Effect of tricyclic antidepressants on transmitter-stimulated inositol phosphate production in rat brain cortex in vitro

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    Nomura, S.; Enna, S.J.

    1986-03-01

    Tricyclic antidepressants (TCAs) have anticholinergic and ..cap alpha..-adrenergic blocking properties. The present study was undertaken to examine the effects of amitriptyline, imipramine, and desipramine on inositol phosphate accumulation, a brain second messenger system associated with cholinergic and adrenergic receptors. Whereas the TCAs were 28 to 400-fold weaker than atropine as inhibitors of /sup 3/H-QNB binding to brain cholinergic receptors, they were 600 to 2000-fold less active than atropine as inhibitors of carbachol-stimulated IP accumulation in brain. In contrast, the relative potencies of the TCAs and prazosin to inhibit norepinephrine-stimulated IP accumulation and /sup 3/H-prazosin binding appeared to be similar in the two assays. The results suggest pharmacological differences between the cholinergic receptors labeled in the ONB binding assay and those mediating the IP response, whereas the ..cap alpha../sub 1/-adrenergic receptors appear to be similar in the two systems. Since atropine is considered a nonselective muscarinic antagonist, it is possible that the TCAs may differentiate between cholinergic receptor subtypes, which may be an important component of their clinical response.

  12. EVALUATION OF IRIDOCILIARY AND LENTICULAR ELASTICITY USING SHEAR-WAVE ELASTOGRAPHY IN RABBIT EYES

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    Efstathios T. Detorakis

    2014-01-01

    Full Text Available Introduction: A previous study has employed shear-wave ultrasound elastographic imaging to assess corneal rigidity in an ex-vivo porcine eye model. This study employs the same modality in vivo in a rabbit eye model in order to assess lens, ciliary body and total ocular rigidity changes following the instillation of atropine and pilocarpine. Methods: Ten non-pigmented female rabbits were examined. Measurements of the lens, ciliary body and total ocular rigidity as well as lens thickness and anterior chamber depth were taken with the Aixplorer system (SuperSonic Imagine, Aix-en-Provence, France with the SuperLinear™ SL 15-4 transducer in both eyes at baseline as well as after pilocarpine and atropine instillation. The IOP was also measured with the TonoPen tonometer. Results: Changes in rigidity in the examined areas following atropine instillation were statistically not significant. Ciliary body rigidity was significantly increased whereas lens and total ocular rigidity were significantly reduced following pilocarpine instillation. The decrease in lens rigidity following pilocarpine was significantly associated with the respective increase in ciliary body rigidity. Conclusions: Shear-wave ultrasound elastography can detect in vivo rigidity changes in the anterior segment of the rabbit eye model and may potentially be applied in human eyes, providing useful clinical information on conditions in which rigidity changes play an important role, such as glaucoma, pseudoexfoliation syndrome or presbyopia.

  13. Parenteral ophthalmic tropicamide or cyclopentolate protects rats from lethal organophosphate poisoning.

    Science.gov (United States)

    Bryant, Sean M; Rhee, James W; Thompson, Trevonne M; Lu, Jenny J; Aks, Steven E

    2009-01-01

    We determine the efficacy of parenteral ophthalmic antimuscarinic agents (tropicamide ophthalmic 1% and cyclopentolate hydrochloride ophthalmic 1%) on survivability in a rat model of acute, lethal organophosphate pesticide (OP) poisoning. After obtaining an appropriate dose-response for study comparison, rodents were randomized to receive 1 of 4 intraperitoneal antidotes; (1) 0.3 mL normal saline, (2) atropine 10 mg/kg, (3) ophthalmic tropicamide 20 mg/kg, or (4) ophthalmic cyclopentolate 20 mg/kg. Five minutes after pretreatment, 15 mg/kg of dichlorvos was administered subcutaneously. Mortality rates and time to death were compared using Fisher exact test and the Kaplan-Meier method with log-rank test, respectively. If alive at 120 minutes, survival was assumed and the study was terminated. Survival in rats pretreated with atropine (10 mg/kg) was 90%. Survival in rats pretreated with tropicamide (20 mg/kg) and cyclopentolate (20 mg/kg) were 90% [P tropicamide or cyclopentolate) was equivalent to standard atropine in preventing lethality in this rat model of acute, lethal OP poisoning.

  14. Changes in intraocular pressure and horizontal pupil diameter during use of topical mydriatics in the canine eye

    Science.gov (United States)

    Kovalcuka, Liga; Ilgazs, Agris; Bandere, Dace; Williams, David L.

    2017-01-01

    The objective of this study was to determine the effects of topical 0.5% tropicamide, 1% atropine sulphate and 10% phenylephrine hydrochloride ophthalmic solutions on intraocular pressure (IOP) and horizontal pupil diameter (HPD) in the dog during the first hour after treatment. Forty clinically and ophthalmologically normal canine patients (between the ages of 2 and 6 years) of varying breed and sex were used in this study. Animals were randomly divided into four groups of ten and given one drop of tropicamide, atropine, phenylephrine or saline into one eye. IOP and HPD were measured in both eyes every 5 minutes for 60 minutes. Tropicamide increased IOP by 8.8±4.0 mmHg 35 minutes post-treatment compared to pre-treatment (Ptropicamide occurred at 55 minutes and with atropine at 60 minutes. There were no HPD changes in the contralateral, untreated eye. Topical 10% phenylephrine showed maximal pupil dilation 60 minutes after treatment, but the HPD of the – untreated eye slightly decreased at 15 minutes, but this change only reached statistical significance at 40 min post- treatment (P<0.05). Normal saline showed no influence on IOP or HPD. The drugs investigated here show a significant increase in IOP after mydriatics. PMID:28210543

  15. Determination of tropicamide in pharmaceutical formulations using high-performance liquid chromatography.

    Science.gov (United States)

    Amanlou, Massoud; Asmardi, Gholamreza; Andalibi, Pedram C; Javadi, Nahid; Khodadady, Farank; Omarny, Zinat Bahrampour

    2005-09-23

    An isocratic, reversed-phase liquid chromatographic method was developed for determination of tropicamide using atropine as an internal standard in a pharmaceutical dosage form. Tropicamide and atropine sulfate were separated using a microBondapak ODS (C18) column by isocratic elution of mobile phase with flow rate of 2.0 ml/min. The mobile phase composition was methanol-50 mM phosphate buffer (pH 4; 30:70, v/v). The eluate was monitored at 257 nm with detector range setting fixed at 0.01 AUFS. Under these conditions, the retention times were 4.81 min for atropine and 11.89 min for tropicamide. The standard calibration curve was linear over a sample concentration range from 2 to 300 microg/ml, with limit of detection of 0.15 microg/ml. The assay linearity was good (typically r2 = 0.9992) and the standard curves were linear in the detection range. The precision of the method (expressed by relative standard deviation) and the accuracy (mean error in percent) were tropicamide. The proposed method was satisfactorily applied to the determination of tropicamide in pharmaceutical preparation and stability indicating studies.

  16. Effect of pilocarpine on the formalin-induced orofacial pain in rats

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    Esmaeal Tamaddonfard

    2012-06-01

    Full Text Available In this study, the effects of subcutaneous (SC injection of pilocarpine (a cholinomimetic agent and atropine (a muscarinic receptors antagonist were investigated on a tonic model of orofacial pain in rats. The contribution of the endogenous analgesic opioid system was assessed using naloxone (an opioid receptors antagonist. Tonic orofacial pain was induced by SC injection of a diluted formalin solution (1%, 50 μL in the right upper lip, and the time spent face rubbing was measured in five min blocks for 1 h. Formalin induced a biphasic (first phase: 0-5 min and second phase: 15-35 min pain response. Pilocarpine significantly (P < 0.05 suppressed both phases of orofacial pain. Atropine did not have any effect and naloxone non-significantly increased the intensity of pain when used alone. In the pre-injection examinations, atropine prevented, but naloxone did not reverse the antinociceptive effect of pilocarpine. The results indicated that SC injection of formalin in the orofacial region induced a marked biphasic pain. Pilocarpine via muscarinic cholinergic receptors produced antinociceptive effect in the orofacial formalin-induced pain. The endogenous opioid analgesic system may not have a role in pilocarpine-induced antinociception.

  17. Is abandonment of nonoperative management of hypertrophic pyloric stenosis warranted?

    Science.gov (United States)

    Lukac, Marija; Antunovic, Sanja Sindjic; Vujovic, Dragana; Pavicevic, Polina; Jesic, Milos; Krstajic, Tamara; Petronic, Ivana; Nikolic, Dejan

    2013-02-01

    Evaluation of the effectiveness of oral atropine versus surgical therapy for hypertrophic pyloric stenosis (HPS). A total of 66 consecutive patients with HPS were treated at the University Children's Hospital between January 2006 and December 2011. The diagnosis was initially based on medical history and confirmed by ultrasonography (US). The patients were divided into two groups according to the treatment preferred by their parents. The conservatively treated group, consisting of 33 boys and 7 girls, mean age 22.25 days, was given water-soluble atropine sulfate therapy at an initial dose of 0.05 mg/kg/day divided into 8 single doses, and administered after stomach decompression, 20 minutes prior to feeding. If vomiting persisted, the daily dose was progressively increased up to 0.18 mg/kg. If vomiting did not stop and full oral feeding was not reestablished in a week, surgery was done. The second group of 26 patients, mean age 20.86 days, underwent an operative procedure, Ramstedt extramucosal pyloromyotomy after the initial resuscitation. US evaluation was performed on days 7, 14, and 21. The outcome of the treatment was tested by Yates modification of the χ2 test. In the group of patients treated with atropine sulfate, 10 (25%) failed to respond to therapy, therefore, 8 boys and 2 girls underwent surgical treatment between the fifth and seventh day following institution of therapy. The remaining patients who received atropine sulfate (75%) were discharged when vomiting ceased, between the sixth and eighth day. They continued to take oral medication for 4 to 6 weeks, and were followed up by an ultrasound examination. The operated patients were discharged between the third and fifth day after surgery. There was a significant statistical difference between the groups regarding the outcome at a significance level of p < 0.05 (Yates χ2 = 5.839), with no complications regardless of the treatment option. However, at the significance level of p < 0.01 (Yates χ2 = 7

  18. Alterations in ZENK and glucagon RNA transcript expression during increased ocular growth in chickens.

    Science.gov (United States)

    Ashby, Regan; Kozulin, Peter; Megaw, Pam L; Morgan, Ian G

    2010-04-13

    To examine in detail the time-course of changes in Zif268, Egr-1, NGFI-A, and Krox-24 (ZENK) and pre-proglucagon (PPG) RNA transcript levels in the chick retina during periods of increased ocular growth induced by form-deprivation and negative-lens wear. To further elucidate the role of ZENK in the modulation of ocular growth, we investigated the effect of intravitreal injections of the muscarinic antagonist atropine and the dopamine agonist 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene hydrobromide (ADTN), both of which block the development of experimental myopia, on the expression of ZENK in eyes fitted with negative-lenses. Myopia was induced by fitting translucent diffusers or -10D polymethyl methacrylate (PMMA) lenses over one eye of the chicken. At times from 1 h to 10 days after fitting of the diffusers or negative lenses, retinal RNA transcript levels of the selected genes were determined by semi-quantitative real-time reverse transcriptase polymerase chain reaction (RT-PCR). For the pharmacology experiments, -10D lenses were fitted over the left eye of chicks for a period of 1h. Intravitreal injections of atropine (10 mul-25 mM), ADTN (10 mul-10 mM), or a vehicle solution were made immediately before fitting of the lenses. ZENK RNA transcript levels were rapidly and persistently down-regulated following the attachment of the optical devices over the eye. With a delay relative to ZENK, PPG transcript levels were also down-regulated. Induced changes in gene expression were similar for both form-deprivation and negative-lens wear. When atropine or ADTN were administered immediately before lens attachment, the rapid down-regulation in ZENK RNA transcript levels normally seen following 1 h of negative-lens wear was not seen, and ZENK transcript levels rose above those values seen in control eyes. However, injection of atropine or ADTN into untreated eyes had no effect on ZENK transcript levels. Both form-deprivation and negative-lens wear modulated the

  19. Cholinergic mechanisms in canine narcolepsy--I. Modulation of cataplexy via local drug administration into the pontine reticular formation.

    Science.gov (United States)

    Reid, M S; Tafti, M; Geary, J N; Nishino, S; Siegel, J M; Dement, W C; Mignot, E

    1994-04-01

    Cataplexy in the narcoleptic canine has been shown to increase after systemic administration of cholinergic agonists. Furthermore, the number of cholinergic receptors in the pontine reticular formation of narcoleptic canines is significantly elevated. In the present study we have investigated the effects of cholinergic drugs administered directly into the pontine reticular formation on cataplexy, as defined by brief episodes of hypotonia induced by emotions, in narcoleptic canines. Carbachol and atropine were perfused through microdialysis probes implanted bilaterally in the pontine reticular formation of freely moving, narcoleptic and control Doberman pinschers. Cataplexy was quantified using the Food-Elicited Cataplexy Test, and analysed using recordings of electroencephalogram, electrooculogram and electromyogram. Cataplexy was characterized by a desynchronized electroencephalogram and a drop in electromyogram and electrooculogram activity. In narcoleptic canines, both unilateral and bilateral carbachol (10(-5) to 10(-3) M) produced a dose-dependent increase in cataplexy, which resulted in complete muscle tone suppression at the highest concentration. In control canines, neither bilateral nor unilateral carbachol (10(-5) to 10(-3) M) produced cataplexy, although bilateral carbachol, did produce muscle atonia at the highest dose (10(-3)). The increase in cataplexy after bilateral carbachol (10(-4) M) was rapidly reversed when the perfusion medium was switched to one containing atropine (10(-4) M). Bilateral atropine (10(-3) to 10(-2) M) alone did not produce any significant effects on cataplexy in narcoleptic canines; however, bilateral atropine (10(-2) M) did reduce the increase in cataplexy produced by systemic administration of physostigmine (0.05 mg/kg, i.v.). These findings demonstrate that cataplexy in narcoleptic canines can be stimulated by applying cholinergic agonists directly into the pontine reticular formation. The ability of atropine to inhibit

  20. Prognostic Factors of Organophosphate Poisoning Between the Death and Survival Groups

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    Tzeng-Jih Lin

    2007-04-01

    Full Text Available In this prospective case series study, we consider the different factors between death and survival groups of organophosphate poisoning. Patients in tertiary-care medical center who had been exposed to organophosphate were included in the study. Pralidoxime (PAM was discontinued after atropine had controlled the clinical situation. We recorded the demographic data, amount of organophosphate consumption, duration of coma, duration of ventilator use, duration of hospitalization, findings of chest X-ray, white blood cell count, acetylcholinesterase concentration, plasma cholinesterase concentration, total atropine amount, duration of atropine use, total PAM amount, duration of PAM use, urine organophosphate peak concentration, duration of urine organophosphate and mortality rate. Urine was collected every 8 hours and was analyzed by gas chromatography equipped with a flame photometric detector and gas chromatography with mass spectrometer detector for organophosphate determination. The urine organophosphate peak concentration was recorded. Wilcoxon rank sum test was used to compare the factors between death and survival groups. Fisher's exact test was used to compare the different findings of chest X-ray between the death and survival groups. Evidently, the death group had a higher amount of organophosphate consumption, duration of coma, and higher white blood cell count than those in the survival group. Also, the death group had lower duration of hospitalization, and decreased concentrations of acetylcholinesterase and plasma cholinesterase. Total PAM amount use and duration of PAM use were lower. However, the duration of ventilator use, findings of chest X-ray, total atropine amount, duration of atropine, urine organophosphate peak concentration and duration of urine organophosphate were similar in both groups. The mortality rate of our 50 cases was 20%. As stated earlier, the cases of the death group had insufficient PAM therapy. The maximum

  1. Pharmacological basis for the medicinal use of psyllium husk (Ispaghula) in constipation and diarrhea.

    Science.gov (United States)

    Mehmood, Malik Hassan; Aziz, Nauman; Ghayur, Muhammad Nabeel; Gilani, Anwarul-Hassan

    2011-05-01

    The objective of this study was to determine the pharmacological basis of the medicinal use of psyllium husk (Ispaghula) in gastrointestinal motility disorders. In-vivo studies were conducted on mice, and isolated rabbit jejunum and guinea-pig ileum were used in in-vitro experiments. The crude extract of Ispaghula (Po.Cr) had a laxative effect in mice at 100 and 300 mg/kg, which was partially sensitive to atropine or SB203186 (5-HT(4) antagonist). At higher doses (500 and 1,000 mg/kg), Po.Cr had antisecretory and antidiarrheal activity. In guinea-pig ileum, Po.Cr (1-10 mg/ml) had a stimulatory effect, which was partially sensitive to atropine or SB203186. In rabbit jejunum, Po.Cr had a partially atropine-sensitive stimulatory effect followed by relaxation at 10 mg/ml. The relaxation was inhibited by the presence of L-NAME, a nitric oxide (NO) synthase inhibitor, or methylene blue, a guanylyl cyclase inhibitor. Similarly, the relaxant effect of Po.Cr on K(+) (80 mM)-induced contractions, was attenuated in the presence of L-NAME or methylene blue. Activity-directed fractionation of Po.Cr revealed that the gut stimulatory and inhibitory constituents were widely distributed in the aqueous and organic fractions. This study demonstrates that Ispaghula has a gut-stimulatory effect, mediated partially by muscarinic and 5-HT(4) receptor activation, which may complement the laxative effect of its fiber content, and a gut-inhibitory activity possibly mediated by blockade of Ca(2+) channels and activation of NO-cyclic guanosine monophosphate pathways. This may explain its medicinal use in diarrhea. It is, perhaps, also intended by nature to offset an excessive stimulant effect.

  2. The diagnostic accuracy of pharmacological stress echocardiography for the assessment of coronary artery disease: a meta-analysis

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    Molinaro Sabrina

    2008-06-01

    Full Text Available Abstract Background Recent American Heart Association/American College of Cardiology guidelines state that "dobutamine stress echo has substantially higher sensitivity than vasodilator stress echo for detection of coronary artery stenosis" while the European Society of Cardiology guidelines and the European Association of Echocardiography recommendations conclude that "the two tests have very similar applications". Who is right? Aim To evaluate the diagnostic accuracy of dobutamine versus dipyridamole stress echocardiography through an evidence-based approach. Methods From PubMed search, we identified all papers with coronary angiographic verification and head-to-head comparison of dobutamine stress echo (40 mcg/kg/min ± atropine versus dipyridamole stress echo performed with state-of-the art protocols (either 0.84 mg/kg in 10' plus atropine, or 0.84 mg/kg in 6' without atropine. A total of 5 papers have been found. Pooled weight meta-analysis was performed. Results the 5 analyzed papers recruited 435 patients, 299 with and 136 without angiographically assessed coronary artery disease (quantitatively assessed stenosis > 50%. Dipyridamole and dobutamine showed similar accuracy (87%, 95% confidence intervals, CI, 83–90, vs. 84%, CI, 80–88, p = 0.48, sensitivity (85%, CI 80–89, vs. 86%, CI 78–91, p = 0.81 and specificity (89%, CI 82–94 vs. 86%, CI 75–89, p = 0.15. Conclusion When state-of-the art protocols are considered, dipyridamole and dobutamine stress echo have similar accuracy, specificity and – most importantly – sensitivity for detection of CAD. European recommendations concluding that "dobutamine and vasodilators (at appropriately high doses are equally potent ischemic stressors for inducing wall motion abnormalities in presence of a critical coronary artery stenosis" are evidence-based.

  3. ChAT-positive neurons participate in subventricular zone neurogenesis after middle cerebral artery occlusion in mice.

    Science.gov (United States)

    Wang, Jianping; Fu, Xiaojie; Zhang, Di; Yu, Lie; Li, Nan; Lu, Zhengfang; Gao, Yufeng; Wang, Menghan; Liu, Xi; Zhou, Chenguang; Han, Wei; Yan, Bo; Wang, Jian

    2017-01-01

    The mechanisms of post-stroke neurogenesis in the subventricular zone (SVZ) are unclear. However, neural stem cell-intrinsic and neurogenic niche mechanisms, as well as neurotransmitters, have been shown to play important roles in SVZ neurogenesis. Recently, a previously unknown population of choline acetyltransferase (ChAT) + neurons residing in rodent SVZ were identified to have direct control over neural stem cell proliferation by indirectly activating fibroblast growth factor receptor (FGFR). This finding revealed possible neuronal control over SVZ neurogenesis. In this study, we assessed whether these ChAT + neurons also participate in stroke-induced neurogenesis. We used a permanent middle cerebral artery occlusion (MCAO) model produced by transcranial electrocoagulation in mice, atropine (muscarinic cholinergic receptor [mAchR] antagonist), and donepezil (acetylcholinesterase inhibitor) to investigate the role of ChAT + neurons in stroke-induced neurogenesis. We found that mAchRs, phosphorylated protein kinase C (p-PKC), and p-38 levels in the SVZ were upregulated in mice on day 7 after MCAO. MCAO also significantly increased the number of BrdU/doublecortin-positive cells and protein levels of phosphorylated-neural cell adhesion molecule and mammalian achaete scute homolog-1. FGFR was activated in the SVZ, and doublecortin-positive cells increased in the peri-infarction region. These post-stroke neurogenic effects were enhanced by donepezil and partially decreased by atropine. Neither atropine nor donepezil affected peri-infarct microglial activation or serum concentrations of TNF-α, IFN-γ, or TGF-β on day 7 after MCAO. We conclude that ChAT + neurons in the SVZ may participate in stroke-induced neurogenesis, suggesting a new mechanism for neurogenesis after stroke. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Tramadol state-dependent memory: involvement of dorsal hippocampal muscarinic acetylcholine receptors.

    Science.gov (United States)

    Jafari-Sabet, Majid; Jafari-Sabet, Ali-Reza; Dizaji-Ghadim, Ali

    2016-08-01

    The effects on tramadol state-dependent memory of bilateral intradorsal hippocampal (intra-CA1) injections of physostigmine, an acetylcholinesterase inhibitor, and atropine, a muscarinic acetylcholine receptor antagonist, were examined in adult male NMRI mice. A single-trial step-down passive avoidance task was used for the assessment of memory retention. Post-training intra-CA1 administration of an atypical μ-opioid receptor agonist, tramadol (0.5 and 1 μg/mouse), dose dependently impaired memory retention. Pretest injection of tramadol (0.5 and 1 μg/mouse, intra-CA1) induced state-dependent retrieval of the memory acquired under the influence of post-training tramadol (1 μg/mouse, intra-CA1). A pretest intra-CA1 injection of physostigmine (1 μg/mouse) reversed the memory impairment induced by post-training administration of tramadol (1 μg/mouse, intra-CA1). Moreover, pretest administration of physostigmine (0.5 and 1 μg/mouse, intra-CA1) with an ineffective dose of tramadol (0.25 μg/mouse, intra-CA1) also significantly restored retrieval. Pretest administration of physostigmine (0.25, 0.5, and 1 μg/mouse, intra-CA1) by itself did not affect memory retention. A pretest intra-CA1 injection of the atropine (1 and 2 μg/mouse) 5 min before the administration of tramadol (1 μg/mouse, intra-CA1) dose dependently inhibited tramadol state-dependent memory. Pretest administration of atropine (0.5, 1, and 2 μg/mouse, intra-CA1) by itself did not affect memory retention. It can be concluded that dorsal hippocampal muscarinic acetylcholine receptor mechanisms play an important role in the modulation of tramadol state-dependent memory.

  5. Aldrin-induced locomotor activity: possible involvement of the central GABAergic-cholinergic-dopaminergic interaction.

    Science.gov (United States)

    Jamaluddin, S; Poddar, M K

    2001-01-01

    Aldrin (5 mg/kg/day, p.o.) under nontolerant condition, administered either for a single day or for 12 consecutive days, enhanced locomotor activity (LA) of rats. The increase in LA was greater in rats treated with aldrin for 12 consecutive days than that observed with a single dose. The aim of the present study is to evaluate the involvement of possible interactions of central GABAergic, cholinergic and dopaminergic systems using their agonist(s) and antagonist(s) in the regulation of LA in aldrin nontolerant rats. Administration of either L-DOPA along with carbidopa or bicuculline potentiated aldrin-induced increase in LA under nontolerant condition as well as LA of the control rats. Treatment with muscimol, haloperidol, atropine or physostigmine all decreased the LA of both aldrin nontolerant and control rats. Further, the application of (a) haloperidol along with bicuculline, atropine or physostigmine and (b) physostigmine along with bicuculline or L-DOPA + carbidopa significantly reduced LA but L-DOPA + carbidopa along with atropine or bicuculline increased LA of the control rats. These agonist(s)/antagonist(s)-induced decrease or increase in LA of the control rats were attenuated or potentiated, respectively, when those agonist(s)/antagonist(s) under abovementioned condition were administered to aldrin nontolerant rats. The attenuating or potentiating effects of aldrin on agonist(s)/antagonist(s) (either individually or in different combinations)-induced change in LA were greater in rats treated with aldrin for 12 consecutive days than that observed with a single-dose aldrin treatment. These results suggest that aldrin, under nontolerant condition, reduces central GABAergic activity and increases LA by activating dopaminergic system via inhibition of cholinergic activity. The treatment with aldrin for 12 consecutive days produces greater effect than that caused by a single-day treatment.

  6. Scopolamine in racing horses: trace identifications associated with dietary or environmental exposure.

    Science.gov (United States)

    Brewer, Kimberly; Dirikolu, Levent; Hughes, Charlie G; Tobin, Thomas

    2014-03-01

    Scopolamine (L-hyoscine) identifications, often in small-number clusters, have been reported worldwide in performance horses over the last 30 years. Scopolamine is an Association of Racing Commissioners International (ARCI) class 3, penalty class B, substance with potential to affect performance. As such, scopolamine identification(s) in race or performance horses can result in significant penalties for the connections of the horse(s). Reviewed here is the worldwide distribution of scopolamine containing plants (primarily Datura spp.), with estimates of their potential toxicity to horses through dietary and/or environmental exposure. Also reviewed are the basic pharmacology of scopolamine and its precursor, urinary concentrations following feedstuff exposure, and the probable pharmacological/forensic significance of such findings. Based on an overview of the world literature on scopolamine, the expected characteristics of inadvertent environmental exposure are also presented with a view to making clear the potential of scopolamine identifications, with or without atropine, as a direct and expected outcome of both the worldwide distribution of scopolamine-containing plants and the sensitivity of modern equine drug testing. It is of particular interest that only 2/30 reported post-event equine identifications of scopolamine have been associated with atropine, suggesting that failure to identify atropine is not a biomarker of pharmaceutical administration of scopolamine. Available quantitative information associated with scopolamine identifications is consistent with the 75 ng/mL regulatory threshold for scopolamine currently used in Louisiana racing in the USA and the 30 ng/mL reporting threshold in effect in European racing. Copyright © 2013 Elsevier Ltd. All rights reserved.

  7. Bioavailability of diazepam after intramuscular injection of its water-soluble prodrug alone or with atropine–pralidoxime in healthy volunteers

    Science.gov (United States)

    Abbara, C; Rousseau, JM; Turcant, A; Lallement, G; Comets, E; Bardot, I; Clair, P; Diquet, B

    2009-01-01

    Background and purpose: The aim of this study was to assess the relative bioavailability of diazepam after administration of diazepam itself or as a water-soluble prodrug, avizafone, in humans. Experimental approach: The study was conducted in an open, randomized, single-dose, three-way, cross-over design. Each subject received intramuscular injections of avizafone (20 mg), diazepam (11.3 mg) or avizafone (20 mg) combined with atropine (2 mg) and pralidoxime (350 mg) using a bi-compartmental auto-injector (AIBC). Plasma concentrations of diazepam were quantified using a validated LC/MS–MS assay, and were analysed by both a non-compartmental approach and by compartmental modelling. Key results: The maximum concentration (Cmax) of diazepam after avizafone injection was higher than that obtained after injection of diazepam itself (231 vs. 148 ng·mL−1), while area under the curve (AUC) values were equal. Diazepam concentrations reached their maximal value faster after injection of avizafone. Injection of avizafone with atropine–pralidoxime (AIBC) had no effect on diazepam Cmax and AUC, but the time to Cmax was increased, relative to avizafone injected alone. According to the Akaike criterion, the pharmacokinetics of diazepam after injection as a prodrug was best described as a two-compartment with zero-order absorption model. When atropine and pralidoxime were injected with avizafone, the best pharmacokinetic model was a two-compartment with a first-order absorption model. Conclusion and implications: Diazepam had a faster entry to the general circulation and achieved higher Cmax after injection of prodrug than after the parent drug. Administration of avizafone in combination with atropine and pralidoxime by AIBC had no significant effect on diazepam AUC and Cmax. PMID:19681868

  8. Effect of acetylcholine receptors on the pain-related electrical activities in the hippocampal CA3 region of morphine-addicted rats

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    Guan Zeng Li

    2015-07-01

    Full Text Available Objective(s:To determine the effect of acetylcholine (ACh, pilocarpine, and atropine on pain evoked responses of pain excited neurons (PEN and pain inhibited neurons (PIN in hippocampal CA3 region of morphine addicted rats. Materials and Methods:Female Wistar rats, weighing between 230-260 g were used in this study. Morphine addicted rats were generated by subcutaneous injection of increasing concentrations of morphine hydrochloride for six days. Trains of electrical impulses applied to the sciatic nerve were used as noxious stimulation and the evoked electrical activities of PEN or PIN in hippocampal CA3 area were recorded using extracellular electrophysiological recording techniques in hippocampal slices. The effect of acetylcholine receptor stimulation byACh, the muscarinic agonist pilocarpine, and the muscarinic antagonist atropine on the pain evoked responses of pain related electrical activities was analyzed in hippocampal CA3 area of morphine addicted rats. Results:Intra-CA3 microinjection of ACh (2 μg/1 μl or pilocarpine (2 μg/1 μl decreased the discharge frequency and prolonged the firing latency of PEN, but increased the discharge frequency and shortened the firing inhibitory duration (ID of PIN. The intra-CA3 administration of atropine (0.5 μg/1 μl produced opposite effect. The peak activity of cholinergic modulators was 2 to 4 min later in morphine addicted rats compared to peak activity previously observed in normal rats. Conclusion: ACh dependent modulation of noxious stimulation exists in hippocampal CA3 area of morphine addicted rats. Morphine treatment may shift the sensitivity of pain related neurons towards a delayed response to muscarinergic neurotransmission in hippocampal CA3 region.

  9. Cholinergic modulation of narcoleptic attacks in double orexin receptor knockout mice.

    Directory of Open Access Journals (Sweden)

    Mike Kalogiannis

    2011-04-01

    Full Text Available To investigate how cholinergic systems regulate aspects of the sleep disorder narcolepsy, we video-monitored mice lacking both orexin (hypocretin receptors (double knockout; DKO mice while pharmacologically altering cholinergic transmission. Spontaneous behavioral arrests in DKO mice were highly similar to those reported in orexin-deficient mice and were never observed in wild-type (WT mice. A survival analysis revealed that arrest lifetimes were exponentially distributed indicating that random, Markovian processes determine arrest lifetime. Low doses (0.01, 0.03 mg/kg, i.p., but not a high dose (0.08 mg/kg, i.p. of the cholinesterase inhibitor physostigmine increased the number of arrests but did not alter arrest lifetimes. The muscarinic antagonist atropine (0.5 mg/kg, i.p. decreased the number of arrests, also without altering arrest lifetimes. To determine if muscarinic transmission in pontine areas linked to REM sleep control also influences behavioral arrests, we microinjected neostigmine (50 nl, 62.5 µM or neostigmine + atropine (62.5 µM and 111 µM respectively into the nucleus pontis oralis and caudalis. Neostigmine increased the number of arrests in DKO mice without altering arrest lifetimes but did not provoke arrests in WT mice. Co-injection of atropine abolished this effect. Collectively, our findings establish that behavioral arrests in DKO mice are similar to those in orexin deficient mice and that arrests have exponentially distributed lifetimes. We also show, for the first time in a rodent narcolepsy model, that cholinergic systems can regulate arrest dynamics. Since perturbations of muscarinic transmission altered arrest frequency but not lifetime, our findings suggest cholinergic systems influence arrest initiation without influencing circuits that determine arrest duration.

  10. Using pharmacokinetic modeling to determine the effect of drug and food on gastrointestinal transit in dogs.

    Science.gov (United States)

    Sjödin, Linnea; Visser, Sandra; Al-Saffar, Ahmad

    2011-01-01

    The gastrointestinal (GI) tract is one of the target organs of adverse drug effects in different phases of drug development. This study aimed to investigate the feasibility of population pharmacokinetic modeling to quantify the rate of gastric emptying (GE) and small intestinal transit time (SITT) in response to drugs that affect GI motility in fed and fasted dogs. Paracetamol and sulfapyridine (sulfasalazine metabolite) pharmacokinetics were used as markers for GE and SITT, respectively. In two separate studies, under fed and fasted conditions, six male beagle dogs received a 15min intravenous infusion of vehicle, atropine (0.06mg/kg) or erythromycin (1mg/kg) followed by an intragastric administration of a mixture of paracetamol (24mg/kg) and sulfasalazine (20mg/kg). Food was given just before or at 6h after drug administration in the fed and fasted study, respectively. Blood samples were collected for analysis of paracetamol and sulfapyridine in plasma. Population pharmacokinetic analysis of paracetamol and sulfapyridine in plasma was used to determine the rate of GE and SITT. The quantitative parameter estimates demonstrated a detailed and significant influence of atropine, erythromycin and food on GE and SITT. Compared to fasted conditions food intake delayed GE in pharmacologically treated dogs and SITT was shortened after treatment with vehicle or erythromycin. Atropine substantially delayed GE in fed and fasted conditions but the effect on SITT was evident only under fed condition. Erythromycin, in contrast, increased GE only in fasted conditions, and generally delayed SITT. Population pharmacokinetic modeling of paracetamol and sulfapyridine provides a suitable preclinical non-invasive experimental method for quantification of drug- and food-induced changes in the rate of GE and SITT in conscious beagle dogs for use in safety evaluations to predict changes in GI transit and/or to explain the pharmacokinetic profile of drugs under development. Copyright

  11. 4R-cembranoid protects against diisopropylfluorophosphate-mediated neurodegeneration.

    Science.gov (United States)

    Ferchmin, P A; Andino, Myrna; Reyes Salaman, Rebeca; Alves, Janaina; Velez-Roman, Joyce; Cuadrado, Brenda; Carrasco, Marimeé; Torres-Rivera, Wilmarie; Segarra, Annabell; Martins, Antonio Henrique; Lee, Jae Eun; Eterovic, Vesna A

    2014-09-01

    Many organophosphorous esters synthesized for applications in industry, agriculture, or warfare irreversibly inhibit acetylcholinesterase, and acute poisoning with these compounds causes life-threatening cholinergic overstimulation. Following classical emergency treatment with atropine, an oxime, and a benzodiazepine, surviving victims often suffer brain neurodegeneration. Currently, there is no pharmacological treatment to prevent this brain injury. Here we show that a cyclic diterpenoid, (1S,2E,4R,6R,7E,11E)-cembra-2,7,11-triene-4,6-diol (4R) ameliorates the damage caused by diisopropylfluorophosphate (DFP) in the hippocampal area CA1. DFP has been frequently used as a surrogate for the warfare nerve agent sarin. In rats, DFP is lethal at the dose used to cause brain damage. Therefore, to observe brain damage in survivors, the death rate was reduced by pre-administration of the peripherally acting antidotes pyridostigmine and methyl atropine or its analog ipratropium. Pyridostigmine bromide, methyl atropine nitrate, and ipratropium bromide were dissolved in saline and injected intramuscularly at 0.1mg/kg, 20mg/kg, and 23mg/kg, respectively. DFP (9mg/kg) dissolved in cold water was injected intraperitoneally. 4R (6mg/kg) dissolved in DMSO was injected subcutaneously, either 1h before or 5 or 24h after DFP. Neurodegeneration was assessed with Fluoro-Jade B and amino cupric silver staining; neuroinflammation was measured by the expression of nestin, a marker of activated astrocytes. Forty-eight hours after DFP administration, 4R decreased the number of dead neurons by half when injected before or after DFP. 4R also significantly decreased the number of activated astrocytes. These data suggest that 4R is a promising new drug that could change the therapeutic paradigm for acute poisoning with organophosphorous compounds by the implementation of a second-stage intervention after the classical countermeasure treatment. Copyright © 2014 Elsevier Inc. All rights reserved.

  12. In vivo binding, pharmacokinetics and metabolism of the selective M{sub 2} muscarinic antagonists [{sup 3}H]AF-DX 116 and [{sup 3}H]AF-DX 384 in the anesthetized rat

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    Mickala, Patrick; Boutin, Herve; Bellanger, Cecile; Chevalier, Cyril; MacKenzie, Eric T.; Dauphin, Francois

    1996-02-01

    The pharmacokinetics, in vivo binding and metabolism of two M{sub 2} muscarinic receptor antagonists, [{sup 3}H]AF-DX 116 and [{sup 3}H]AF-DX 384, were studied in anesthetized rats, which received either the tracer alone or following a saturating injection of atropine. Both radioligands were cleared from the circulation with distribution half-lives of 17 and 14 sec and elimination half-lives of 17 and 40 min for [{sup 3}H]AF-DX 116 and [{sup 3}H]AF-DX 384, respectively. A radioactive distribution, predominant in peripheral organs when compared to brain, was found at each time studied after tracer injection. Atropine-displaceable tracer uptake was evidenced at 20-40 min in brain (31%), submandibular glands (26%), spleen (37%) and notably heart (55%) for [{sup 3}H]AF-DX 116 but only in heart (50%) for [{sup 3}H]AF-DX 384 at 10-20 min. Regional brain sampling revealed a relatively uniform distribution of [{sup 3}H]AF-DX 384 and a -45% atropine saturation effect (i.e., specific binding) in the thalamus 20 min after injection. Sequential thin-layer chromatographic studies performed on tissue extracts demonstrated the rapid appearance of labeled metabolites of both radiotracers in brain (but less so in liver) and especially in cardiac tissues, where almost 70% of total radioactivity still corresponded to authentic tracer 40 min after injection. Thus, based on their low blood-brain barrier permeability and the high presence of labeled metabolites in the central nervous system, AF-DX 116 and AF-DX 384 might be more helpful in the study of M{sub 2} muscarinic receptors present in heart rather than brain. Labeled with positron emittors, these M{sub 2} antagonists might be applicable to the pathophysiological study of disease states, such as cardiomyopathies.

  13. Relaxant effect of Curcuma longa on rat tracheal smooth muscle and its possible mechanisms.

    Science.gov (United States)

    Emami, Bahman; Shakeri, Farzaneh; Ghorani, Vahideh; Boskabady, Mohammad Hossein

    2017-12-01

    Turmeric is a spice obtained from the root of Curcuma longa L. (Zingiberaceae) with anti-aging, anticancer, anti-Alzheimer's disease, antioxidant and other medicinal properties. The relaxant effect of C. longa on rat tracheal smooth muscle and its possible mechanisms were investigated in this study. The relaxant effects of four cumulative concentrations of hydro-ethanol extract of C. longa (6.25, 12.5, 25, 50 mg/mL) were studied on tracheal smooth muscle precontracted by methacholine or KCl in non-incubated or incubated with different substances including propranolol, diltiazem, L-NAME, glibenclamide, atropine, chlorpheniramine, indomethacin and papaverine. The duration of the study was 84 days. In non-incubated tracheal smooth muscle, the extract of C. longa showed significant concentration-dependent relaxant effects (p longa and theophylline in both methacholine and KCl-induced contraction conditions. In tissues incubated with propranolol, diltiazem, L-NAME and glibenclamide on methacholine-induced contraction and in tissues incubated with atropine, chlorpheniramine, indomethacin and papaverine on KCl-induced contraction, the extract also showed significant concentration-dependent relaxant effects (p longa between non-incubated (16.22 ± 0.62) and incubated tissues (atropine: 13.03 ± 0.55, chlorpheniramine: 12.94 ± 0.68, indomethacin: 14.80 ± 0.57 and papaverine: 16.16 ± 1.42) were not significantly different. Tracheal smooth muscle relaxant effects of C. longa, were comparable to those of theophylline, which could be due to the presence of methylxanthines or its possible interaction with non-adrenergic non-cholinergic nervous system.

  14. Cardiovascular effects of Tacca integrifolia Ker-Gawl. extract in rats

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    Prakart Sawangchote

    2005-03-01

    Full Text Available Rhizome of Tacca integrifolia, a Thai folk medicinal herb, has been used for controlling blood pressure and improving sexual function in humans. However, the biological activities of this herb on the cardiovascular system have not yet been documented. In the present study, we investigated the cardiovascular effects of methanolic extract from the rhizome of this herb (Tacca extract. In the in vivo study, intravenous injection of the Tacca extract (0.04-40 mg/kg caused a decrease in both mean arterial blood pressure and heart rate of anesthetized rats (Nembutal sodium, 60 mg/kg, i.p. in a dose dependent manner. Pretreatment of the animals with muscarinic receptor antagonist, atropine (1 mg/kg, i.v., significantly reduced the hypotensive and the negative chronotropic activities of the Tacca extract. In the in vitro preparation, the Tacca extract (0.001-3 mg/ml caused a decrease in both force and rate of spontaneous contraction of isolated atria in a dose dependent manner. These effects were reduced by preincubation of the atria with atropine (10-7 or 10-6 M. For isolated blood vessels, the Tacca extract (0.003-3 mg/ ml caused vasodilation of endothelium-intact thoracic aortic rings pre-constricted with phenylephrine (3× 10-6 M. This effect disappeared after pre-incubation of blood vessels with atropine (10-6 M or with Nω-nitro- L-arginine (3×10-4 M, or by removing the vascular endothelium. The results obtained suggest that the hypotensive and negative chronotropic effects of the Tacca extract in the rat are due to the active components acting via the muscarinic receptors at the blood vessel to cause vasodilatation by stimulating the release of nitric oxide, as well as on the muscarinic receptors at the atria to cause the decrease of both rate and force of the atrial contraction.

  15. Attempts to reduce the progression of myopia and spectacle prescriptions during childhood: a survey of eye specialists.

    Science.gov (United States)

    Jung, Jong Jin; Lim, Eun-Hae; Baek, Seung-Hee; Kim, Yong Ran; Gong, Sang Mook; Kim, Ungsoo Samuel

    2011-12-01

    To determine methods tried in clinical trials to reduce the progression of myopia in children, and spectacle prescribing patterns of hospital ophthalmologists. A multi-sectioned survey composed of Likert items relating to the methods of reducing myopia progression (orthokeratology lenses [O-K lenses], undercorrected glasses, and topical atropine) and the patterns of prescribing spectacles for children (including two cases involving a 5-year-old girl and an 8-year-old boy) were distributed to members of the Korean Ophthalmological Society, and the collected data was statistically analyzed. A total of 78 out of 130 ophthalmologists returned the survey. On a scale of 1 to 5, the mean rates of whether the ophthalmologists think O-K lenses arrest myopia progression, and whether they recommend their patients to wear O-K lenses if indicative, were 3.06 and 2.75, respectively. Moreover, the mean rates of whether they consider that wearing glasses which are undercorrected would slow down the progression of the myopia, or if they think topical atropine helps in arresting myopia progression in children, were 2.34 and 1.27, respectively. In response to the case studies, the majority of practitioners preferred to prescribe the full amount found in cycloplegic refraction to pediatric patients with myopia. Ophthalmologists in clinical practice encouraged children to wear O-K lenses more than undercorrected glasses as a way to retard myopia progression. However, the application of atropine is rarely tried in clinical trials. In managing pediatric patients with myopia (case specific), the majority of the practitioners chose to prescribe glasses with full cycloplegic correction.

  16. N-acetylcysteine in Acute Organophosphorus Pesticide Poisoning: A Randomized, Clinical Trial.

    Science.gov (United States)

    El-Ebiary, Ahmad A; Elsharkawy, Rasha E; Soliman, Nema A; Soliman, Mohammed A; Hashem, Ahmed A

    2016-08-01

    Organophosphorus poisoning is a major global health problem with hundreds of thousands of deaths each year. Research interest in N-acetylcysteine has grown among increasing evidence of the role of oxidative stress in organophosphorus poisoning. We aimed to assess the safety and efficacy of N-acetylcysteine as an adjuvant treatment in patients with acute organophosphorus poisoning. This was a randomized, controlled, parallel-group trial on 30 patients suffering from acute organophosphorus poisoning, who were admitted to the Poison Control Center of Tanta University Emergency Hospital, Tanta, Egypt, between April and September 2014. Interventions included oral N-acetylcysteine (600 mg three times daily for 3 days) as an added treatment to the conventional measures versus only the conventional treatment. Outcome measures included mortality, total dose of atropine administered, duration of hospitalization and the need for ICU admission and/or mechanical ventilation. A total of 46 patients were screened and 30 were randomized. No significant difference was found between both groups regarding demographic characteristics and the nature or severity of baseline clinical manifestations. No major adverse effects to N-acetylcysteine therapy were reported. Malondialdehyde significantly decreased and reduced glutathione significantly increased only in the NAC-treated patients. The patients on NAC therapy required less atropine doses than those who received only the conventional treatment; however, the length of hospital stay showed no significant difference between both groups. The study concluded that the use of N-acetylcysteine as an added treatment was apparently safe, and it reduced atropine requirements in patients with acute organophosphorus pesticide poisoning. © 2016 Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).

  17. [Acute Datura stramonium poisoning in an emergency department].

    Science.gov (United States)

    Marc, Bernard; Martis, Antoine; Moreau, Céline; Arlie, Gilles; Kintz, Pascal; Leclerc, Johan

    2007-10-01

    The toxic effects of Datura stramonium most often include visual and auditory hallucinations, confusion and agitation. Severe and even fatal complications (coma, respiratory distress or death in more than 5% of cases) are not rare since the lethal concentration of the drug's toxic substances (i.e., atropine and scopolamine) is close to the level at which delirium occurs. A 17-year-old man was admitted to our emergency department with agitation, delirium with persecutory ideation and frightening hallucinations of being assaulted by animals. Blood samples taken 12 hours after Datura stramonium ingestion and analyzed with liquid chromatography and mass spectrometry (LC-MS/MS) found 1.7 ng/mL of atropine, close to the lethal level. After restraint and treatment with the antipsychotic drug cyamemazine, the young man returned to normal 36 hours after drug ingestion. A 17-year-old woman was admitted to our emergency department after losing consciousness on a public thoroughfare. At the emergency department, 2 hours after she had ingested Datura stramonium, she was agitated, with delirium, anxiety, and frightening visual and tactile hallucination of green turtles walking on her as well as auditory hallucinations. Blood samples at D0, D1 and D2 after Datura stramonium ingestion, analyzed with LC-MS/MS, found: 1.4, 1.0, and 0.2 ng/mL of scopolamine, respectively. Atropine was massively eliminated in urine on D1 (114 ng/mL). After restraint and cyamemazine treatment, the young woman returned to normal 40 hours after she had first ingested this hallucinogen. These cases of intoxication with Datura stramonium are, to our knowledge, the first clinical reports correlated with toxicologic analysis by the reference method (LC-MS/MS) in an emergency setting. Since neither the drug-users nor those accompanying them usually volunteer information about drug use, it is important to consider this specific risk in cases of agitation and confusion in adolescents or young adults.

  18. Central command does not suppress baroreflex control of cardiac sympathetic nerve activity at the onset of spontaneous motor activity in the decerebrate cat.

    Science.gov (United States)

    Matsukawa, Kanji; Ishii, Kei; Asahara, Ryota; Idesako, Mitsuhiro

    2016-10-01

    Our laboratory has reported that central command blunts the sensitivity of the aortic baroreceptor-heart rate (HR) reflex at the onset of voluntary static exercise in animals. We have examined whether baroreflex control of cardiac sympathetic nerve activity (CSNA) and/or cardiovagal baroreflex sensitivity are altered at the onset of spontaneously occurring motor behavior, which was monitored with tibial nerve activity in paralyzed, decerebrate cats. CSNA exhibited a peak increase (126 ± 17%) immediately after exercise onset, followed by increases in HR and mean arterial pressure (MAP). With development of the pressor response, CSNA and HR decreased near baseline, although spontaneous motor activity was not terminated. Atropine methyl nitrate (0.1-0.2 mg/kg iv) with little central influence delayed the initial increase in HR but did not alter the response magnitudes of HR and CSNA, while atropine augmented the pressor response. The baroreflex-induced decreases in CSNA and HR elicited by brief occlusion of the abdominal aorta were challenged at the onset of spontaneous motor activity. Spontaneous motor activity blunted the baroreflex reduction in HR by aortic occlusion but did not alter the baroreflex inhibition of CSNA. Similarly, atropine abolished the baroreflex reduction in HR but did not influence the baroreflex inhibition of CSNA. Thus it is likely that central command increases CSNA and decreases cardiac vagal outflow at the onset of spontaneous motor activity while preserving baroreflex control of CSNA. Accordingly, central command must attenuate cardiovagal baroreflex sensitivity against an excess rise in MAP as estimated from the effect of muscarinic blockade. Copyright © 2016 the American Physiological Society.

  19. INVESTIGATIONS INTO THE MECHANISM OF REDUCTION OF ETHANOL SLEEP BY THYROTROPIN - RELEASING HORMONE (TRH)1

    Science.gov (United States)

    COTT, JERRY M.; BREESE, GEORGE R.; COOPER, BARRETT R.; BARLOW, T. STEVEN; PRANGE, ARTHUR J.

    2010-01-01

    Thyrotropin-releasing hormone (TRH), administered intraperitoneally, was found to antagonize ethanol-induced sleep and hypothermia in mice without affecting brain ethanol content. This reduction of the actions of ethanol was also apparent after oral or intracisternal administration of TRH. In addition, TRH reduced ethanol-induced sleep in rats, hamsters, gerbils and guinea pigs. Evidence that the pituitary-thyroid axis is not necessary for the effects of TRH was provided by observations that hypophysectomy did not reduce TRH antagonism of ethanol narcosis and findings that neither triiodothyronine nor thyrotropin mimicked its action. Certain analogs of TRH, which have little effect on the pituitary, were also found to antagonize ethanol-induced sleep and hypothermia. Pretreatment with the antiadrenergic drugs, α-methyltyrosine, phentolamine and propranolol did pot antagonize the ability of TRH to reduce sleep induced by ethanol. However, after intracisternal administration of atropine methyl nitrate, TRH no longer caused a significant reduction of sleep, even though TRH antagonism of the ethanol-induced hypothermia was still apparent. In contrast, central administration of other anticholinergic drugs, such as d-tubocurarine and hexamethonium, reduced ethanol-induced sleep and this effect was additive with TRH. Carbachol also reduced ethanol sleeping time and this effect was also blocked by atropine methyl nitrate. The antagonism of ethanol-induced sleep by dibutyryl cyclic adenosine 3′,5′-monophosphate was significantly reduced but not blocked by atropine methyl nitrate. Results provide evidence that TRH has a direct extrapituitary action on brain and that both TRH and ethanol may interact with central cholinergic systems. PMID:177753

  20. Antinociception induced by systemic administration of local anaesthetics depends on a central cholinergic mechanism.

    Science.gov (United States)

    Bartolini, A; Galli, A; Ghelardini, C; Giotti, A; Malcangio, M; Malmberg-Aiello, P; Zucchi, P L

    1987-12-01

    1 The antinociceptive effects of systemically-administered procaine, lignocaine and bupivacaine were examined in mice and rats by using the hot-plate, writhing and tail flick tests. 2 In both species all three local anaesthetics produced significant antinociception which was prevented by atropine (5 mg kg-1, i.p.) and by hemicholinium-3 (1 microgram per mouse, i.c.v.), but not by naloxone (3 mg kg-1, i.p.), alpha-methyl-p-tyrosine (100 mg kg-1, s.c.), reserpine (2 mg kg-1, i.p.) or atropine methylbromide (5.5 mg kg-1, i.p.). 3 Atropine (5 mg kg-1, i.p.) which totally antagonized oxotremorine (40 micrograms kg-1, s.c.) antinociception did not modify morphine (5 mg kg-1, s.c.) or baclofen (4 mg kg-1, s.c.) antinociception. On the other hand, hemicholinium, which antagonized local anaesthetic antinociception, did not prevent oxotremorine, morphine or baclofen antinociception. 4 Intracerebroventricular injection in mice of procaine (200 micrograms), lignocaine (150 microgram) and bupivacaine (25 micrograms), doses which were largely ineffective by parenteral routes, induced an antinociception whose intensity equalled that obtainable subcutaneously. Moreover, the i.c.v. injection of antinociceptive doses did not impair performance on the rota-rod test. 5 Concentrations below 10(-10) M of procaine, lignocaine and bupivacaine did not evoke any response on the isolated longitudinal muscle strip of guinea-pig ileum, or modify acetylcholine (ACh)-induced contractions. On the other hand, they always increased electrically-evoked twitches. 6 The same concentrations of local anaesthetics which induced antinociception did not inhibit acetylcholinesterase (AChE) in vitro. 7 On the basis of the above findings and the existing literature, a facilitation of cholinergic transmission by the local anaesthetics is postulated; this could be due to blockade of presynaptic muscarinic receptors.

  1. A key role for the caudoventral pontine tegmentum in the simultaneous generation of eye saccades in bursts and associated ponto-geniculo-occipital waves during paradoxical sleep in the cat.

    Science.gov (United States)

    Vanni-Mercier, G; Debilly, G

    1998-09-01

    Ponto-geniculo-occipital waves and rapid eye movements (eye saccades) are two prominent phasic events of paradoxical sleep which occur in conjunction. Although they have been studied intensively, the neuronal link between these two events is still poorly understood. On the basis of our previous results, combining brainstem transections and carbachol microinjections, we postulated that the oculomotor and ponto-geniculo-occipital systems do not work in series, but in parallel, and that the caudoventral pontine tegmentum might represent a structure controlling and/or co-ordinating the simultaneous production of the two phenomena. This hypothesis was further supported by the demonstration that, during paradoxical sleep, the instantaneous velocity of eye saccades in bursts is higher than that of isolated ones which, in turn, are more rapid than waking saccades. This acceleration of eye saccades in bursts also seems to be under the cholinergic control of the caudoventral pontine tegmentum. In order to test the hypothesis that this area may be a prime mover leading to the simultaneous appearance of these two phasic events as a whole, we investigated, in the present study, the effects of pharmacological stimulation (with carbachol) and inhibition (with atropine) of the caudoventral pontine tegmentum on the production and the characteristics of eye saccades and ponto-geniculo-occipital waves. Cats' eye movements were recorded using the technique of the scleral search coil in a magnetic field, together with sleep-waking parameters. We found that: (i) unilateral microinjections of carbachol (0.4 microg) induced, during waking, a majority of long bursts of ponto-geniculo-occipital waves (i.e. bursts containing at least five waves) which had intra-burst intervals similar to natural ones (48-259 ms) and decreased the frequency of isolated ponto-geniculo-occipital waves; (ii) unilateral microinjections of atropine (2.4 microg) strongly decreased, during paradoxical sleep, the

  2. Isotretinoin-induced Angle Closure and Myopic Shift.

    Science.gov (United States)

    Park, Young-Myoung; Lee, Tae-Eun

    2017-11-01

    To report and describe the management a rare case of transient bilateral angle closure with increased intraocular pressure (IOP) and myopic shift while on isotretinoin therapy for acne. A 28-year-old woman presented with bilateral myopic shift, angle closure with IOP increase, and supraciliary effusion 1 week after acne therapy with isotretinoin. Two weeks after stopping isotretinoin, and treatment with topical prednisolone acetate, atropine, and fixed combination of timolol and dorzolamide, refraction, IOP returned to normal and supraciliary effusions was decreased on ultrasound biomicroscopy. Oral isotretinoin for acne treatment may be associated with an adverse reaction, resulting in bilateral transient myopia and angle closure with IOP elevation.

  3. Dual action of antimuscarinic agents on the intestinal smooth muscle

    Directory of Open Access Journals (Sweden)

    Acharya SRK

    1979-01-01

    Full Text Available Propantheline, oxyphenonium, isoproponaide, epidosine, adiphe-nine and atropine were studied for their effect on the superfused infesting of guinea pig and rat. In small, concentrations, all drugs produced a contraction, which with increasing concentration, was Hocked. Occasionally, a contraction and a relaxation or vice versa was recorded. A partial antagonism and a potentiation on the action of acetylcholine (Ach during recovery was observed. In very high concentrations, all drugs produced a graded contraction of intestine, except adiphenine which produced a sustained contraction. Some- times, a contraction and a relaxation was also observed.

  4. The Effects of Exercise on Pharmacokinetics and Pharmacodynamics of Physostigmine in Rats

    Science.gov (United States)

    1989-02-15

    present in whole blood, which comprises true ChE (ACHE) and "pseudocholines- terase", i.e., butylcholinesterase ( BuChE ). It is understandable that our...unsteadiness, incoordina- tion or salivati3n). The maximum sign-free dose of Phy without atropine was 0.16 mg/kg in chicken and guinea pig; 0.1 mg/kg...activity; however, they observed an increase in total ChE and BuChE in diaphragm after moderate physical exercise. Physostigmine reduced the ChE

  5. Asystole Following Profound Vagal Stimulation During Hepatectomy

    Directory of Open Access Journals (Sweden)

    Preeta John

    2008-01-01

    Full Text Available Asystole in a non laparoscopic upper abdominal surgery following intense vagal stimulation is a rare event. This case report highlights the need for awareness of such a complication when a thoracic epidural anaesthetic has been given in addition to a general anaesthetic for an upper abdominal procedure. A combined thoracic epidural and general anaesthetic was given. The anterior abdominal wall was retracted forty minutes after administration of the epidural bolus. This maneuver resulted in a profound vagal response with bradycardia and asystole. The patient was resuscitated successfully with a cardiac massage, atropine and adrenaline and the surgery was resumed. Surgery lasted eleven hours and was uneventful.

  6. Bölgemizde hyoscyamus niger ( Henbane = Banotu ) zehirlenmeleri

    OpenAIRE

    ORBAK, Zerrin; TAN, Hüseyin; KARAKELLEOĞLU, Cahit; ALP, Handan; AKDAĞ, Recep

    1998-01-01

    in the region of Erzurum in East Anatolia, in Spring, typical atropine poisoning is seen in children who eat the roots and leaves of henbane (Hyoscyamus niger) known here as "Deli Bat Bat", in this article we have discussed 216 patients who were admitted to our hospital during the years 1981-1995. VVİthin 24 hours the most patients were out of danger from the intoxication and showed improvement due to the use of only sufficient amounts of intravenous fluid to force diuresis. AH the ...

  7. Plasma volume changes during hypoglycaemia

    DEFF Research Database (Denmark)

    Hilsted, J; Frandsen, Henrik Lund; Christensen, N J

    1991-01-01

    -induced hypoglycaemia with total autonomic blockade (alpha-adrenoceptor blockade combined with beta-adrenoceptor blockade and atropine); and insulin-induced hypoglycaemia without any autonomic blockade. In the experiments without autonomic blockade the peripheral venous hematocrit increased, plasma volume decreased......, intravascular albumin content decreased and the transcapillary escape rate of albumin increased. In both experiments with autonomic blockade the increase in venous haematocrit was abolished, yet plasma volume decreased, intravascular albumin content decreased and the transcapillary escape rate of albumin...... increased in these experiments. Thus, the changes in plasma volume and composition in response to hypoglycaemia are due to the combined actions of adrenaline and of insulin....

  8. Organophosphate exposure with pseudocholinesterase deficiency.

    Science.gov (United States)

    Lurati, Ann R

    2013-06-01

    A 36-year-old correctional officer was exposed to lice while at work and self-treated with chlorpyrifos, an organophosphate. The correctional officer applied chlorpyrifos to her entire body and did not wash it off for 8 to 12 hours. Eight hours after the initial application, the correctional officer developed abdominal cramps, diarrhea, sweating, excessive salivation, frequent urination, and increased bronchial secretions. After a phone consultation with the occupational health clinic, the correctional officer reported to the emergency department, was diagnosed with organophosphate toxicity, and was treated with atropine. Later testing revealed that the correctional officer had pseudocholinesterase deficiency. Copyright 2013, SLACK Incorporated.

  9. Cutaneous allergic reaction due to alprazolam in a child

    Directory of Open Access Journals (Sweden)

    Meryem Ozlem Kutuk

    2016-06-01

    Full Text Available Cutaneous allergic reactions due to drug intake may be triggered by many types of drugs such as atropine, anticonvulsants and benzodiazepines. But allergic reactions due to benzodiazepines are extremely rare. Alprazolam is a benzodiazepine which may be useful for refractory idiopathic urticaria due to antihistaminergic effect. Although antihistaminergic effect of alprazolam, a cold urticaria case and an angioedema case induced by alprazolam are known in the literature. In the case, we present a child suffering from cutaneous allergic reaction due to alprazolam at the first dose taken. [Cukurova Med J 2016; 41(2.000: 400-402

  10. Anisocoria Secondary to Anticholinergic Mydriasis from Homeopathic Similasan Pink-Eye-Relief Drops.

    Science.gov (United States)

    Chen, Lin; Yeung, Joseph C; Anderson, Dennis R

    2017-10-17

    A 70-year-old-woman developed anisocoria after applying homeopathic eye drops (Similasan Pink Eye Relief) to her left eye. Her pupil was dilated for two weeks and did not respond to light or near stimuli for one week. Both 0.1 % and 1% pilocarpine failed to constrict her left pupil, and magnetic resonance imaging of her brain did not reveal any abnormality. The eye drops she had used contain belladonna extracts, which have a natural atropine component. This case demonstrates the importance, when evaluating a patient presenting with anisocoria, of knowing the chemical ingredients of the homeopathic eye drops, which often are not listed. © 2017 Marshfield Clinic.

  11. Datura Stramonium Abuse: A Case Report

    Directory of Open Access Journals (Sweden)

    Muhittin Yilmaz

    2013-10-01

    Full Text Available Datura stramonium, known as devils apple or tatula by the people of Turkey, is a plant known member of a belladonna alkaloid family contains atropine, hyoscyamine and scopolamine having hallucinogenic and anticholinergic effects. 19 years old male patient admitted to emergency department (ED by his relatives with the complaints of altered mental status, and meaningless speech. History revealed that patient consumed %u201CDatura stramonium%u201D for entertainment about 4 hours before the development of symptoms. In our study we described a case presented by delirium to our emergency department later diagnosed as Datura stramonium poisoning.

  12. An unusual case of altered sensorium in a young child: Datura poisoning

    Directory of Open Access Journals (Sweden)

    Bindu T Nair

    2014-01-01

    Full Text Available Datura stramonium (DS is a wildly growing plant which is widely distributed and easily accessible. It contains a variety of toxic anticholinergic alkaloids such as atropine, hyoscamine, and scopolamine. Voluntary or accidental ingestion can produce severe anticholinergic poisoning. We report an unusual case of DS intoxication occurring in a young child after accidental ingestion of the plant fruit. Our case is unusual because of the young age of the victim and the underlying inquisitiveness of children facilitating the occurrence of such poisoning.

  13. Datura Stramonium Zehirlenmesi: Olgu Sunumu

    OpenAIRE

    DENİZ,, Dr. Turgut; NARĞİS,, Dr. Cemil; GÜVEN, Dr. Hakan; TANYERİ, Dr. Fulya

    2009-01-01

    Yazımızda; antikolinerjik bulgularla acil servise başvuran, hikaye ve fizik muayene ile datura stramonium zehirlenme tanısı konan bir hasta sunulmaktadır. Datura stramonium, Türkiye'nin hemen her yerinde doğal florada yaygın olarak bulunabilen bir bitkidir. Bitkinin oral olarak alımı atropin, skopolamin ve hiyosiyamin içermesinden dolayı antikolinerjik etkilere neden olmaktadır. Datura ile olan zehirlenme olgularındaki antikolinerjik etkilerin klasik belirti ve bulgularını bilmek, klinisyenin...

  14. Drug: D03069 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03069 Crude, Drug Belladonna extract (JP16); Belladonna (USP) Hyoscyamine [CPD:C02...046], Atropine [CPD:C01479], Norhyoscyamine [CPD:C10862], Scopolamine [CPD:C01851] Atropa belladonna [TAX:33...113] Anticholinergic Same as: E00008 ATC code: A03BA04 Solanaceae (nightshade family) Belladonna root extrac...RDERS A03B BELLADONNA AND DERIVATIVES, PLAIN A03BA Belladonna alkaloids, tertiary amines A03BA04 Belladonna ...total alkaloids D03069 Belladonna extract (JP16); Belladonna (USP) Crude drugs [B

  15. Drug: D03223 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03223 Crude, Drug Belladonna leaf (USP) Hyoscyamine [CPD:C02046], Atropine [CPD:C0...1479], Norhyoscyamine [CPD:C10862], Scopolamine [CPD:C01851] Atropa belladonna [TAX:33113] Same as: E00229 A...TC code: A03BA04 Solanaceae (nightshade family) Belladonna leaf Anatomical Therapeutic Chemical (ATC) classi...GASTROINTESTINAL DISORDERS A03B BELLADONNA AND DERIVATIVES, PLAIN A03BA Belladonna alkaloids, tertiary amines A03BA04 Belladonna... total alkaloids D03223 Belladonna leaf (USP) PubChem: 17397376 ...

  16. Etude des effets pharmacologiques de l'extrait aqueux de ...

    African Journals Online (AJOL)

    L'inhibition de ces effets, par l'atropine à 10-8 mg/ml et par le propranolol à 10-10 mg/ml, suggère la présence concomitante de substances cholinomimétiques et adrénomimétiques de type b dans HEL. Sur l'aorte isolée, ce concentré naturel provoque une vasorelaxation endothélium-dépendante entre 10-6 et 10-1 mg/ml.

  17. Sedative and cardiovascular effects of Aloysia citriodora Palau, on mice and rats

    OpenAIRE

    Ragone, María Inés; Sella, Mariana; Pastore, Agustín; Consolini, Alicia E.

    2010-01-01

    Aloysia citriodora Palau, Verbenaceae ("cedrón") is widely used as infusion or decoction in South America to treat indigestion, tachycardia and anxiety. We previously demonstrated its antispasmodic effect on rat duodenum. Now, its aqueous extract (AEC) from 1 to 10 mg/kg was sedative in mice on the open-field, effect which was potentiated by diazepam and sensitive to flumazenil. In normotensive rats, 1 to 30 mg AEC/kg induced a transitory hypotension, insensitive to atropine and L-NAME. Regar...

  18. Anticonvulsants for poisoning by the organophosphorus compound soman: pharmacological mechanisms.

    Science.gov (United States)

    Shih, T M; Koviak, T A; Capacio, B R

    1991-01-01

    Exposure to high doses of organophosphorus nerve agents such as soman, even with carbamate pretreatment, produces a variety of toxic cholinergic signs, including secretions, convulsions and death. Evidence suggests that soman-induced convulsions may be associated with postexposure brain neuropathology. The purpose of this study was to investigate the pharmacologic mechanism of action of soman-induced convulsions and of anticonvulsant drugs. Various classes of compounds were evaluated for their efficacy in preventing soman-induced convulsions in rats pretreated with the oxime HI-6 to increase survival time, along with various doses of the test compounds (IM) either in the absence or presence of atropine sulfate (16 mg/kg, IM) 30 minutes prior to a soman challenge dose (180 micrograms/kg, SC; equivalent to 1.6 x LD50) that produced 100% convulsions. Without atropine sulfate, only tertiary anticholinergics (scopolamine, trihexyphenidyl, biperiden, benactyzine, benztropine, azaprophen and aprophen), caramiphen, carbetapentane and MK-801 were effective anticonvulsants. In the presence of atropine sulfate, the benzodiazepines (diazepam, midazolam, clonazepam, loprazolam and alprazolam), mecamylamine, flunarizine, diphenylhydantoin, clonidine, CGS 19755 and Organon 6370 studied were effective. We have examined the possibility that diazepam may exert some of its anticonvulsant effects through cholinergic mechanisms and found that a reduced release of ACh into synapses after diazepam and atropine treatment may account for diazepam's anticonvulsant activity against soman. We also found that at anticonvulsant doses biperiden and trihexyphenidyl each significantly reversed the effects of soman on striatal levels of DOPAC and HVA, the metabolites of dopamine, and have concluded that in addition to actions on muscarinic receptors, the anticonvulsant effects of these anticholinergics in soman poisoning may be partially related to their actions on the striatal dopaminergic system

  19. Anesthetic consideration in downs syndrome--a review.

    Science.gov (United States)

    Bhattarai, B; Kulkarni, A H; Rao, S T; Mairpadi, A

    2008-09-01

    Downs syndrome constitutes to be the most common chromosomal disorder. Patients with Downs's syndrome are posted for several surgeries including dental procedures and even for facial reconstruction. They are associated with several congenital anomalies in different organ system. There is also increased incidence of atlanto axial instability and risk of spinal cord injury. These children are susceptible to infection and they are also considered to be hypersensitive to the effect or atropine. These all factors modify the anesthetic implication and also anesthetic management in these cases. We have highlighted all these factors and reviewed the anesthetic implication of these child posted for several procedures under anesthesia.

  20. Posterior reversible encephalopathy syndrome in a patient of organophosphate poisoning.

    Science.gov (United States)

    Phatake, Rajesh; Desai, Sameer; Lodaya, Manikanth; Deshpande, Shrinivas; Tankasali, Nagaraj

    2014-04-01

    A 32-year-old male presented with a history of consuming some organophosphorous compound with suicidal intention. He was treated with atropine, pralidoxime, ventilator support. During stay patient had persistent irritability, tachycardiaand hypertension despite sedation and labetalol infusion. He developed headache, visual blurring hemiparesis and focal seizures. Magnetic resonance imaging of the brain revealed multifocal hyperintensities mainly in subcortical areas of parietal and occipital regions in T2-weighted images, with increased values of Apparent Diffusion Coefficient, suggesting posterior reversible encephalopathy syndrome (PRES). The possibilities of PRES caused by organophosphorous poisoning either due to hypertension caused by autonomic deregulation or direct neurological toxicity has been discussed.

  1. Antinociceptive and anti-inflammatory potentials of kolaviron: mechanisms of action.

    Science.gov (United States)

    Onasanwo, Samuel A; Rotu, Rume A

    2016-06-01

    Major attention has been on dietary and medicinal phytochemicals that inhibit or reverse abnormal conditions caused by nociceptive and inflammatory stimuli. Garcinia kola (Guttiferae) seed, known as "bitter kola", plays an important role in African ethno-medicine and traditional hospitality like in the treatment of inflammation, colds, bronchitis, bacterial, and viral infections. A number of useful phytochemicals have been isolated from the seed, and the most prominent of them is kolaviron (Garcinia bioflavonoid), which has been suggested to have antinociceptive and anti-inflammatory potentials. The aim of this experiment is to explore the mechanisms of action of the antinociceptive and anti-inflammatory potentials of kolaviron. The probable mechanisms of action of kolaviron were assessed by using naloxone, prazosin, and atropine to investigate the involvement of adrenergic, opioidergic, and cholinergic systems, respectively, using tail flick, the acetic acid-induced writhing, formalin-induced paw licking, and carrageenan-induced paw edema models. Also, hematoxylin and eosin (H&E) staining was used to analyze the level of inflammation. In the acetic acid-induced writhing test in mice, pretreatment with naloxone, prazosin, and atropine significantly reversed the antinociception effects of kolaviron (200 mg/kg) when compared with control and kolaviron groups. In the formalin-induced paw licking test in mice, there was a significant decrease on the antinociceptive effects of kolaviron in the late phase when compared with the control, while the pretreatment with naloxone and prazosin significantly reversed the antinociception of kolaviron but atropine did not have any significant decrease when compared with the kolaviron group. In the tail flick latency assay in rats, pretreatment with naloxone and prazosin significantly reversed the antinociception of kolaviron but atropine; however, did not have any significant increase when compared with the control and kolaviron

  2. Digoxinforgiftning hos et spædbarn grundet forveksling af flasker med magistrelt fremstillet medicin

    DEFF Research Database (Denmark)

    Hansen, Louise Lindholdt; Herskind, Anne Maria

    2014-01-01

    We hereby describe a case report of a 9-month-old girl, who was accidentally intoxicated with digoxin since her parents by mistake gave her digoxin instead of propranolol. At admission sinusbradycardia and a first-degree atrioventricular block was found and she was treated with antidigitalis Fab......-fragment and atropine. After three days of hospitalization she was discharged well-being. We suspect that the explanation for this intoxication is due to confusion of bottles of magistral preparations of medicine, as they were very identical. Therefore we call for increased attention in children receiving this type...

  3. The Organophosphate Paraoxon and Its Antidote Obidoxime Inhibit Thrombin Activity and Affect Coagulation In Vitro.

    Directory of Open Access Journals (Sweden)

    Valery Golderman

    Full Text Available Organophosphates (OPs are potentially able to affect serine proteases by reacting with their active site. The potential effects of OPs on coagulation factors such as thrombin and on coagulation tests have been only partially characterized and potential interactions with OPs antidotes such as oximes and muscarinic blockers have not been addressed. In the current study, we investigated the in vitro interactions between coagulation, thrombin, the OP paraoxon, and its antidotes obidoxime and atropine. The effects of these substances on thrombin activity were measured in a fluorescent substrate and on coagulation by standard tests. Both paraoxon and obidoxime but not atropine significantly inhibited thrombin activity, and prolonged prothrombin time, thrombin time, and partial thromboplastin time. When paraoxon and obidoxime were combined, a significant synergistic effect was found on both thrombin activity and coagulation tests. In conclusion, paraoxon and obidoxime affect thrombin activity and consequently alter the function of the coagulation system. Similar interactions may be clinically relevant for coagulation pathways in the blood and possibly in the brain.

  4. The poison center as a reservoir for antidotes for veterinary poisoning emergencies.

    Science.gov (United States)

    Krenzelok, E P; Drake, T; Dean, B S

    1992-04-01

    Animal poisonings account for a significant number of the cases responded to by poison centers. The majority of consultations involve small animals and do not necessitate the use of large amounts of pharmacologic antagonists, such as atropine to treat anticholinesterase pesticide poisonings. However, large animals such as cattle present unique management problems, since phenomenal amounts of antidotes may be needed to treat a herd of cattle, creating a significant economic impact. The most challenging dilemma is providing 24-h availability and a means of acquisition of sufficient quantities of antidotes to reduce the economic impact of large-animal poisonings. In conjunction with a state veterinary medical association, a RPIC serves as a depot for the storage and distribution of emergency veterinary antidotes. Sufficient quantities of atropine, methylene blue, calcium EDTA, sodium nitrite and thiosulfate, and activated charcoal are available via the RPIC to treat a herd of 200 cattle. The antidotes are available only for emergency treatment and with a veterinary prescription. The 24-h nature of the poison center makes it an ideal location to serve the needs of veterinarians.

  5. Randomized trial of laryngeal mask airway versus endotracheal intubation for surfactant delivery.

    Science.gov (United States)

    Pinheiro, J M B; Santana-Rivas, Q; Pezzano, C

    2016-03-01

    To compare the effectiveness of surfactant delivery via endotracheal tube (ETT) using an intubation-surfactant-rapid extubation approach with premedication) vs laryngeal mask airway (LMA) in preventing the need for mechanical ventilation in preterm neonates with moderate respiratory distress syndrome (RDS). Moderately preterm infants diagnosed with RDS, receiving nasal continuous positive airway pressure with FiO2 0.30 to 0.60, were randomized to two groups at age 3 to 48 h. Those in the ETT group were intubated following premedication with atropine and morphine, whereas the LMA group received only atropine. Both groups received calfactant before a planned reinstitution of nasal continuous positive airway pressure, and had equivalent pre-specified criteria for subsequent mechanical ventilation and surfactant retreatment. The primary outcome was failure of surfactant treatment strategy to avoid mechanical ventilation; we differentiated early from late failures to assess the contribution of potential mechanisms such as respiratory depression versus less-effective surfactant delivery. Secondary outcomes addressed efficacy and safety end points. Sixty-one patients were randomized, one excluded and 30 analyzed in each group, with similar baseline characteristics. Failure rate was 77% in the ETT group and 30% in the LMA group (Psedation. The efficacy of surfactant in decreasing RDS severity appears similar with both methods. Morphine premedication likely contributed to early post-surfactant failures.

  6. Pengaruh Pemberian Minyak Atsiri Daun Kemangi (Ocimum americanum L. Terhadap Motilitas Usus Mencit Putih Jantan

    Directory of Open Access Journals (Sweden)

    Dewi Sriyani

    2016-04-01

    Full Text Available Kemangi (Ocimum americanum L. is a well known plant that contains essential oils with citral as a major compound. Citral is reported to have beneficial effect on intestinal motility. This reseach investigated the effect of essential oil of kemangi leaves (Ocimum americanum L. on male DDY mices intestinal motility. Thirty mices were divided into six groups and each group was pretreated with 0,2 ml of 0,5% CMC (negative control, 1 mg/kg BW of atropine sulfate (positive control, 5 mg/kg BW of citral (comparative control, and three dose variation of volatile oil of kemangi leaves (25 mg/kg BW; 50 mg/kg BW; 100 mg/kg BW orally. All mices were given charcoal meal suspension 0,2 ml orally, and the animals were sacrificed. The percentage ratio and inhibition were analysed by measure the intestinal transit of charcoal. The results showed that the essential oil of kemangi leaves dose 100 mg/kg BW significantly (p 0.05 compared with citral and atropine sulfate. This research concluded that the essential oil of kemangi leaves has potential effect as antispasmodic agent.

  7. The effect of cimetidine on basal and stimulated pepsin secretion in the isolated whole stomach of the rat.

    Science.gov (United States)

    Bunce, K. T.; Grewal, M.; Parsons, M. E.

    1981-01-01

    1 The isolated stomach preparation of the immature rat has been used to study the stimulation and inhibition of pepsin secretion. 2 The isolated stomach secretes a basal level of pepsin. High concentrations (10(-3)M) of the H2-receptor antagonist, cimetidine, and the muscarinic receptor blocking drug, atropine, did not affect this secretion in a manner which was consistently of statistical significance. 3 Concentrations of histamine of 10(-5)M, 10(-4)M and 10(-3) M stimulated maximum levels of pepsin output of 126%, 155% and 299% respectively of control. There was no evidence that this secretion was secondary to the stimulation of acid secretion. 4 Cimetidine (10(-4)M and 10(-3)M) produced a dose-related inhibition of the pepsin output to 10(-3)M histamine, suggesting that histamine H2-receptors mediate this response. 5 Atropine (10(-3)M) had no effect on the pepsin response to 10(-3)M histamine, suggesting that muscarinic mechanisms play no part, even modulatory, in this secretion. PMID:6793118

  8. Electroacupuncture at ST37 Enhances Jejunal Motility via Excitation of the Parasympathetic System in Rats and Mice

    Directory of Open Access Journals (Sweden)

    Mengqian Yuan

    2016-01-01

    Full Text Available Background. The roles of the sympathetic and parasympathetic systems in mediating the effect of electroacupuncture (EA at ST37 on jejunal motility have yet to be demonstrated. Aim. We used rats and mice to investigate the effect and mechanism of action of EA at ST37 on jejunal motility. Methods. Jejunal motility was recorded by a balloon placed in the jejunum and connected to a biological signal collection system through a transducer. The effects of EA (3 mA at ST37 were evaluated in Sprague-Dawley rats without drugs and with the administration of clenbuterol, propranolol, acetylcholine, and atropine. Further, the efficacy of EA at different intensities (1/2/4/6/8 mA was measured in wild-type mice and β1β2-/- mice and M2M3-/- mice. Results. In Sprague-Dawley rats, the excitatory effect of EA at ST37 on jejunal motility disappeared in the presence of the muscarinic receptor antagonist atropine. EA at ST37 was less effective in M2M3-/- mice than in wild-type mice. Furthermore, to a certain extent, there existed “intensity-response” relationship between jejunal motility and EA. Conclusions. EA at ST37 can enhance jejunal motility in rats and mice mainly via excitation of the parasympathetic pathway. There is an “intensity-response” relationship between EA and effect on jejunal motility.

  9. In vitro production of secondary metabolite using Atropa komarovii Bline&Shal (Solanaceae hairy root culture via Agrobacterium rhizogenes ATCC15834

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    Ofelia Banihashemi

    2017-07-01

    Full Text Available Background & Aim:A new sustainable tissue-based system is presented by plant hairy roots, preserving all of the several specialized types of cell with critical roles in allowing bioactive secondary molecules to be synthesized more consistently as usual. The system is also essential for studying the production of alkaloid in culture. Experimental: The Atropa komarovii leaves were wounded and infected with soil gram-negative bacterium Agrobacterium rhizogenes ATCC15834. After three weeks, the transformation roots and control roots without infection, appeared, and for confirming that T-DNA Ri plasmid fragments were transformed and integrated to plant genome, the rolB gene region, was amplified using PCR. HPLC method was then used for assaying how two tropane alkaloids such as atropine (hyosciamine and scopolamine (hyoscine were produced in hairy roots,control roots, leaves and roots of plantlet. Results: The data indicated that diagnostic 500bp rol B product amplification was exhibited to be present by all the transformed hairy roots. Scopolamine content in hairy roots was considerably greater than that in control roots but greatest (Hyoscyamine atropine content was observed in control roots. Analysis of DW, FW and root length showed that fresh and dry root weight increased in hairy roots compared with that in non transformed root. Recommended applications/industries: The present study demonstrated that secondary metabolite production using medicinal plants concerns many researchers worldwide today and hairy root culture is a useful method for producing tropane alkaloids in solanaceae.

  10. Identification of Medication Errors with Similar Pronunciation, Spelling and Packaging in Tabriz Shahid Madani Hospital -1392

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    Gisoo Alizadeh

    2015-08-01

    Full Text Available Background and objectives: Evidence suggests that medication errors are among the most common types of medical errors, and over fifty percent of them are preventable. Since a significant proportion of these errors are related to the similarity between drug names, this study was designed to evaluate drugs with similar spelling, spelling and packaging. Material and Methods: This is a qualitative study with phenomenological approach. Participants were selected by purposive sampling. Data were collected through semi-structured interviews and with the help of previously designed guide. Data were analyzed using content analysis. Results: The central themes of the findings of this study include: the accuracy of drug use, the way of recording and monitoring used medication, the storage, reporting, and notification of similar medications, verbal or telephone orders, medication lists with similar spelling, pronunciation and packaging and recommendations of the participants. The most errors in the Heparin-Atropine pair was the packaging of the drugs, spelling was the highest error in Dopamine- Dobutamine pair drug and spelling was the highest error in Atropine and Atorvastatin pair drug. Conclusion: The study findings indicate that there is no certain system for recording, monitoring and storage of similar drugs. Therefore, identifying the medication list with similar pronunciation, spelling and packaging is an opportunity to reduce these types of errors with appropriate interventions. ​

  11. Mass spectrometry study of increased breakdown of an anticonvulsivant drug substance

    Science.gov (United States)

    Buret, D.; Breton, D.; Clair, P.; Lafosse, M.

    2006-06-01

    The French Military Health Service (SSA) developed a new pharmaceutic speciality as a treatment against neurotoxic organophosphate poisoning (NSP), as a substitute for existing therapeutics. The Armed Forces Central Pharmacy (PCA) is in charge of the development of therapeutic formulation and stability studies. This product includes three drug substances: atropine, pralidoxime and avizafone, an amine prodrug of diazepam, soluble in water. The PCA performed a stability study of this formulation according to the International Conference on Harmonization (ICH) recommendations: it was used to display interaction between the molecules and the plastic of the cartridge (the container turned yellow). Since no degradation product of atropine and pralidoxime was observed, a complementary evaluation of avizafone and its main known degradation products (diazepam, carbostyril and methylaminobenzochlorophenone [MACB]) was initiated. The results were used to determine the degradation products obtained under different conditions and the kind of mechanisms, which may occur as the formulation ages: adsorption or absorption by the bulk and/or increasing degradation products. The analytical methods developed here are a direct sample analysis by mass spectrometry (MS) using different ionization modes and liquid chromatography (LC) with UV detection to confirm the results obtain with MS.

  12. Analisis Gas Darah pada Kucing yang Mengalami Laparohisterotomi dengan Anestesi Xylazin-Ketamin dan Xylazin-Propofol (BLOOD GAS ANALYSIS OF XYLAZIN- KETAMIN AND XYLAZIN-PROPOFOL FOR ANESTHESIA TO LAPARO-HISTEROTOMY SURGERY IN CAT

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    Ira Sari Yudaniayanti

    2012-03-01

    Full Text Available The aim of this research was to study the safety application of xylazine-ketamine and xylazinepropofolrecurrent dosage combination as anesthesia for laparo-histerotomy surgery in cat. Thisresearch used 10 female cats, 12-18 months of age, followed randomly divided into two groups, P1:atropine 0,04 mg/kgBW/SC + xylazine 2 mg/kg BW/IM + ketamine 20 mg/kg BW/IM; P2 : atropine0,04mg/kg BW/SC + xylazine 2 mg/kg BW/IM + Propofol 20 mg/kg BW/IV. The blood of the allgroups was taken from vena femuralis at 0 minute (before treatment, 15, 30, 45 and 60 minutesduring anesthesia for measurement of blood gas value pH, pCO2 and HCO3. After all animals wereanesthetized, the animals were treated laparo-histerotomy surgery. The data were analyzed byusing Randomized Complete Block Design (RCBD. The result showed both of groups were notsignificantly difference (p>0,05 to blood gas values for pH, pCO2 dan HCO3. Besides, both groupsanaesthetic agent perfectly caused metabolic acidosis with respiratory alkalosis compensationperfectly, therefore it is relatively safe to use as anaesthetic agent for surgery that needs long timeprocedure, as laparo-histerotomy.

  13. [Effect of change in levels of motor activity and innervation on basic and secondary rhythms of rat heart rate and respiration in ontogenesis].

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    Bursian, A V; Dmitrieva, L E; Sizonov, V A

    2011-01-01

    Changes in the heart basic rhythm, its rhythmical variations on periodograms, and level of spontaneos motor activity were studied on offspring of white rats from newborn to 3-week age at transition from the state of active wakefulness to narcosis as well as under conditions of blockade of M-cholinoreceptors with atropine. It is shown that the endogenous rhythmical activity can be regulated not only by a change in frequency of basic rhythms, but also by action on all parameters and properties of their rhythmical variations and secondary rhythms. The changes in power of the heart secondary rhythms exceed considerably the frequency oscillations of basic rhythms during blockade of cholinergic innervation or a change in the motor activity level that affects both the basic rhythm circulation and respiration and their variations--secondary rhythms. The atropine blockade of M-cholinoreceptors at the studied ages changes the heart beating rhythm within the limits of 10% of bradicardia in newborns to tachycardia in the 3-week old animals. At the same time, power of the cardiac rhythm secondary oscillations changes several times. These data indicate that the cholinergic mechanisms play the key role in formation of the secondary rhythms and their correlation with motor activity.

  14. Development and validation of a rapid and sensitive assay for the determination of anisodamine in 50 μL of beagle dog plasma by LC-MS/MS.

    Science.gov (United States)

    Li, Wenxue; Wen, Jun; He, Jingyu; Cao, Di; Sun, Fanlu; Li, Jinying; Fan, Guorong

    2013-10-01

    A simple, rapid, high-throughput, and highly sensitive LC-MS/MS was developed to determine anisodamine in a small volume (50 μL) of beagle dog plasma using atropine sulfate as the internal standard. The analyte and internal standard were isolated from 50 μL plasma samples after a one-step protein precipitation using Sirocco 96-well protein precipitation filtration plates. The separation was accomplished on a Hanbon Hedera CN column (100 × 4.6 mm, 5 μm) and the run time was 4 min. A Micromass Quatro Ultima mass spectrometer equipped with an ESI source was operated in the multiple reaction monitoring mode with the precursor-to-product ion transitions m/z 306.0→140.0 (anisodamine) and 290.0→123.9 (atropine) used for quantitation. The method was sensitive with a low LOQ of 0.05 ng/mL, and good linearity in the range 0.05-50 ng/mL for anisodamine (r(2) ≥ 0.995). All the validation data, such as accuracy, intra- and interrun precision, were within the required limits. The method was successfully applied to the pharmacokinetic study of anisodamine hydrochloride injection in beagle dogs. © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  15. Ketamine-propofol sedation in circumcision

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    Handan Gulec

    2015-10-01

    Full Text Available ABSTRACTBACKGROUND AND OBJECTIVE: To compare the therapeutic effects of ketamine alone or ketamine plus propofol on analgesia, sedation, recovery time, side effects in premedicated children with midazolam-ketamine-atropin who are prepared circumcision operation.METHODS: 60 American Society of Anaesthesiologists physical status I-II children, aged between 3 and 9 years, undergoing circumcision operations under sedation were recruited according to a randomize and double-blind institutional review board-approved protocol. Patients were randomized into two groups via sealed envelope assignment. Both groups were administered a mixture of midazolam 0.05 mg/kg + ketamine 3 mg/kg + atropine 0.02 mg/kg intramuscularly in the presence of parents in the pre-operative holding area. Patients were induced with propofol-ketamine in Group I or ketamine alone in Group II.RESULTS: In the between-group comparisons, age, weight, initial systolic blood pressure, a difference in terms of the initial pulse rate was observed (p > 0.050. Initial diastolic blood pressure and subsequent serial measurements of 5, 10, 15, 20th min, systolic blood pressure, diastolic blood pressure and pulse rate in ketamine group were significantly higher (p < 0.050.CONCLUSION: Propofol-ketamine (Ketofol provided better sedation quality and hemodynamy than ketamine alone in pediatric circumcision operations. We did not observe significant complications during sedation in these two groups. Therefore, ketofol appears to be an effective and safe sedation method for circumcision operation.

  16. Adenotomy under general anesthesia.

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    Vokurka, J; Jakoubková, S; Vít, Z; Drahokoupilová, M

    1989-01-01

    Experience obtained from adenotomy (AT) under general anesthesia using Ketamin hydrochloride (Ketalar, Narkamon) in children are presented in this paper. The authors had used intramuscular premedication with Prothazin, Dolsin and Atropin at the first stage, then they shifted to oral administration of a combination of Diazepam, Theadryl and Atropin. Ketamin may be applied intravenously in the dosage of 1.0 to 1.5 mg/kg of body weight in most children. Where it is not possible, a triple dose into the muscle is used. A total of 2,266 AT were performed. About 70% of patients were calm during the operation, once a suspected aspiration was considered but it was not confirmed. The main contribution of the method is 100% amnesia of the surgery made. The procedure is a compromise between a requirement for minimal traumatization of the child's psyche by the intervention and the resources available, particularly the need of personnel at the majority of otorhinolaryngo-logical departments nowadays.

  17. Prokinetic effects of large-dose lubiprostone on gastrointestinal transit in dogs and its mechanisms.

    Science.gov (United States)

    Song, Jun; Yin, Jieyun; Xu, Xiaohong; Chen, Jiande

    2015-01-01

    To systemically explore effects of large dose of lubiprostone on gastrointestinal (GI) transit and contractions and its safety in dogs. 12 healthy dogs were studied. 6 dogs were operated to receive duodenal cannula and colon cannula and the other 6 dogs received gastric cannula. Lubiprostone was orally administrated at a dose of 24 µg or 48 µg 1 hr prior to the experiments. Gastric emptying (GE) of solids and small bowel transit were evaluated by collecting the effluents from the duodenal cannula and from the colon cannula. Gastric accommodation was measured by barostat. Gastric and intestinal contractions were by manometry. Colon transit was by X-ray pictures. 1) Lubiprostone 48 µg not 24 µg accelerated GE. Atropine could block the effect; 2) Average motility index (MI) of gastric antrum in lubiprostone 48 µg session was significantly higher in both fasting state (P = 0.01) and fed state (P = 0.03). Gastric accommodation was not significantly different; 3) Lubiprostone 48 µg accelerated small bowel and colon transit. Atropine could block the effect on small bowel transit; 4) Lubiprostone 48 µg increased postprandial small bowel MI (P = 0.0008) and colon MI (P = 0.002). 5) No other adverse effects except for diarrhea were observed. Acute administration of lubiprostone at a dose of 48 µg accelerates GI motility and enhances GI contractions in the postprandial state. The findings suggest that lubiprostone may have an indirect prokinetic effects on the GI tract and vagal activity may be involved. Lubiprostone may be safely used.

  18. Salvia miltiorrhiza Induces Tonic Contraction of the Lower Esophageal Sphincter in Rats via Activation of Extracellular Ca2+ Influx

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    Ching-Chung Tsai

    2015-08-01

    Full Text Available Up to 40% of patients with gastroesophageal reflux disease (GERD suffer from proton pump inhibitor refractory GERD but clinically the medications to strengthen the lower esophageal sphincter (LES to avoid irritating reflux are few in number. This study aimed to examine whether Salvia miltiorrhiza (SM extracts induce tonic contraction of rat LES ex vivo and elucidate the underlying mechanisms. To investigate the mechanism underlying the SM extract-induced contractile effects, rats were pretreated with atropine (a muscarinic receptor antagonist, tetrodotoxin (a sodium channel blocker, nifedipine (a calcium channel blocker, and Ca2+-free Krebs-Henseleit solution with ethylene glycol tetraacetic acid (EGTA, followed by administration of cumulative dosages of SM extracts. SM extracts induced dose-related tonic contraction of the LES, which was unaffected by tetrodotoxin, atropine, or nifedipine. However, the SM extract-induced LES contraction was significantly inhibited by Ca2+-free Krebs-Henseleit solution with EGTA. Next, SM extracts significantly induce extracellular Ca2+ entry into primary LES cells in addition to intracellular Ca2+ release and in a dose-response manner. Confocal fluorescence microscopy showed that the SM extracts consistently induced significant extracellular Ca2+ influx into primary LES cells in a time-dependent manner. In conclusion, SM extracts could induce tonic contraction of LES mainly through the extracellular Ca2+ influx pathway.

  19. Sudden unexpected death in a mouse model of Dravet syndrome

    Science.gov (United States)

    Kalume, Franck; Westenbroek, Ruth E.; Cheah, Christine S.; Yu, Frank H.; Oakley, John C.; Scheuer, Todd; Catterall, William A.

    2013-01-01

    Sudden unexpected death in epilepsy (SUDEP) is the most common cause of death in intractable epilepsies, but physiological mechanisms that lead to SUDEP are unknown. Dravet syndrome (DS) is an infantile-onset intractable epilepsy caused by heterozygous loss-of-function mutations in the SCN1A gene, which encodes brain type-I voltage-gated sodium channel NaV1.1. We studied the mechanism of premature death in Scn1a heterozygous KO mice and conditional brain- and cardiac-specific KOs. Video monitoring demonstrated that SUDEP occurred immediately following generalized tonic-clonic seizures. A history of multiple seizures was a strong risk factor for SUDEP. Combined video-electroencephalography-electrocardiography revealed suppressed interictal resting heart-rate variability and episodes of ictal bradycardia associated with the tonic phases of generalized tonic-clonic seizures. Prolonged atropine-sensitive ictal bradycardia preceded SUDEP. Similar studies in conditional KO mice demonstrated that brain, but not cardiac, KO of Scn1a produced cardiac and SUDEP phenotypes similar to those found in DS mice. Atropine or N-methyl scopolamine treatment reduced the incidence of ictal bradycardia and SUDEP in DS mice. These findings suggest that SUDEP is caused by apparent parasympathetic hyperactivity immediately following tonic-clonic seizures in DS mice, which leads to lethal bradycardia and electrical dysfunction of the ventricle. These results have important implications for prevention of SUDEP in DS patients. PMID:23524966

  20. [Effect of prokinetic agents on the electrical activity of stomach and duodenum in rats].

    Science.gov (United States)

    Li, Fujun; Zou, Yiyou; Huang, Tianhui

    2009-07-01

    To determine the effect of prokinetic agents such as domperidone, mosapride, clarithromycin, and itopride on the electrical activity of the stomach and duodenum in SD rats,and also to explore the mechanism. The organism functional experiment system BL-420E was used to record the myoelectrical activity in the stomach and duodenum of SD rats in all groups using domperidone, mosapride, itopride, clarithromycin, and physiological saline on the interdigestive phase. The effect of the prokinetic agents on the amplitude and frequency of gastric and duodenal electromyogram in the SD rats was compared. The antagonists such as atropine, phentolamine, and propranolol were added to investigate the mechanism of action with all prokinetic agents. All prokinetic agents increased the amplitude and frequency of gastric and duodenal fast waves in the SD rats(Pitopride was the most obvious among the 3 groups (Pitopride, and physiological saline were inhibited by atropine(PItopride, mosapride, domperidone, and clarithromycin can increase the amplitude and frequency of gastric and duodenal fast waves in the SD rats. The mechanism may be related to cholinergic receptors, but not adrenergic receptors.

  1. A New Wavelet-Based ECG Delineator for the Evaluation of the Ventricular Innervation.

    Science.gov (United States)

    Cesari, Matteo; Mehlsen, Jesper; Mehlsen, Anne-Birgitte; Sorensen, Helge Bjarup Dissing

    2017-01-01

    T-wave amplitude (TWA) has been proposed as a marker of the innervation of the myocardium. Until now, TWA has been calculated manually or with poor algorithms, thus making its use not efficient in a clinical environment. We introduce a new wavelet-based algorithm for the delineation QRS complexes and T-waves, and the automatic calculation of TWA. When validated in the MIT/BIH Arrhythmia database, the QRS detector achieved sensitivity and positive predictive value of 99.84% and 99.87%, respectively. The algorithm was validated also on the QT database and it achieved sensitivity of 99.50% for T-peak detection. In addition, the algorithm achieved delineation accuracy that is similar to the differences in delineation between expert cardiologists. We applied the algorithm for the evaluation of the influence in TWA of anticholinergic and antiadrenergic drugs (i.e., atropine and metoprolol) for healthy subjects. We found that the TWA decreased significantly with atropine and that metoprolol caused a significant increase in TWA, thus confirming the clinical hypothesis that the TWA is a marker of the innervation of the myocardium. The results of this paper show that the proposed algorithm can be used as a useful and efficient tool in clinical practice for the automatic calculation of TWA and its interpretation as a non-invasive marker of the autonomic ventricular innervation.

  2. Antidiarrheal activity of ethanolic extract of Manihot esculenta Crantz leaves in Wistar rats

    Science.gov (United States)

    Bahekar, Satish E.; Kale, Ranjana S.

    2015-01-01

    Background: Use of Manihot esculenta Crantz (MEC) plant has been mentioned in literature of Food and Agriculture Organization of United Nations, Central Tuber Crops Research Institute and many others. It is also known commonly as tapioca, continues to be a crop of food security for the millions of people, especially in the developing countries of the globe including India. Medicinal uses of this plant including diarrhea have been mentioned in literature, but scientific evidence is lacking. Objective: The objective was to study antidiarrheal activity of ethanolic leaf extract of MEC in Wistar rats. Materials and Methods: Ethanolic extract of MEC leaves in the doses of 50 mg/kg, 100 mg/kg and 200 mg/kg were used in Wistar rats of either sex. Experimental models used were castor oil-induced intestinal fluid accumulation and charcoal passage test. Loperamide and atropine sulfate were the standard drugs used in these models respectively. Results: MEC extracts decreased intestinal fluid volume in dose dependent manner no extract group was comparable with standard drug loperamide (5 mg/kg). MEC extracts also significantly inhibited gastrointestinal motility in dose dependent manner. MEC (100 mg/kg) and MEC (200 mg/kg) were comparable with standard drug atropine sulfate (5 mg/kg) in this aspect. <0.05 were considered to be significant. Conclusions: Ethanolic extract of MEC leaves exhibited significant antidiarrheal activity by decreasing intestinal fluid accumulation and the gastrointestinal motility in Wistar rats. PMID:25878462

  3. Orthostatic Dysregulation during Postural Change on the Dental Chair and Intraoperative Monitoring by Heart Rate Variability Analysis

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    Yukihiro Momota

    2014-01-01

    Full Text Available This is the first case report of orthostatic dysregulation (OD manifested during postural change on the dental chair and intraoperatively monitored by heart rate variability (HRV analysis. OD-associated autonomic dysfunction is induced by postural changes and easily leads to disturbance in circulatory dynamics; however, most dental practices have not yet realized the importance of managing OD. We measured autonomic activity in a patient with OD during dental therapy and assessed the clinical significance of HRV analysis for OD. The patient was a 17-year-old Japanese female. She was diagnosed with impacted wisdom teeth and had no previous history of a distinct systemic disease. A surgical procedure to extract the teeth was safely performed under both local anesthesia and sedation with nitrous oxide and midazolam. After the surgery, her postural change to sitting induced orthostatic hypotension. HRV variables showed parasympathetic dominance due to the upright position. Subsequently, her posture was returned to supine, and atropine sulfate administration for the immediate treatment of OD returned her blood pressure to normal levels. HRV variables showed relative sympathetic dominance due to an atropine-derived parasympathetic blockade. HRV analysis revealed OD-associated autonomic dysfunction and should become a standard tool for safe and secure dental management of OD.

  4. Pentobarbital Toxicity after Self-Administration of Euthasol Veterinary Euthanasia Medication

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    Steven Jason Crellin

    2016-01-01

    Full Text Available Suicide attempt via sodium pentobarbital is uncommon. A 48-year-old woman with a history of depression and prior suicide attempt was found unresponsive by her veterinarian spouse near a syringe containing pink solution. Upon EMS’ arrival, the patient was experiencing apnea, hypoxemia, and miotic pupils; her blood glucose level measured 73 mg/dL. She was bradycardic and administered atropine with transient improvement in heart rate and transported to an emergency department; 2 mg of intravenous naloxone was administered without effect. She was endotracheally intubated via rapid sequence intubation. Rapid urine drug screening detected both benzodiazepines and barbiturates. The patient was transferred to an intensive care unit where she demonstrated a nearly absent radial pulse. Emergent fasciotomy to the left forearm and carpal tunnel was performed for acute compartment syndrome; “Euthasol” had been self-administered into the antecubital fossa. Expanded toxicological analysis via liquid chromatography/mass spectroscopy detected caffeine, atropine, 7-aminoclonazepam, phenytoin, citalopram, and naproxen. The patient’s coma resolved over 48 hours and she was successfully extubated without complication. Emergency physicians must closely monitor patients exposed to veterinary euthanasia agents who develop central nervous system and respiratory depression, hypothermia, bradycardia, hypotension, or skin injury. Consultation with a regional poison center and medical toxicologist is recommended.

  5. Pyridinium oximes: rationale for their selection as causal antidotes against organophosphate poisonings and current solutions for auto-injectors.

    Science.gov (United States)

    Stojiljković, Milos P; Jokanović, Milan

    2006-12-01

    During the last five decades, five pyridinium oximes were found to be worthy of use as antidotes against nerve agents in humans: pralidoxime, in a form of chloride or PAM-2 Cl and mesylate or P2S (against sarin, cyclosarin and VX), trimedoxime or TMB-4 and obidoxime or LüH-6 (both against tabun, sarin and VX), HI-6 (against sarin, soman, cyclosarin and VX) and HLö-7 (against all the five nerve agents). In order to provide the auto-injector with the best and most potent acetylcholinesterase reactivator, the Defence Research and Development Canada (DRDC) received in the 1990s a core funding from the federal government's CBRN research and Technology Initiative (CRTI). Its ultimate result should be three products: (1) 3-in-1 auto-injector (atropine, HI-6 dimethanesulphonate and avizafone, as anticonvulsant), (2) 2-in-1 auto-injector (atropine and HI-6 dimethanesulphonate) and (3) HI-6 dimethanesulphonate in a vial for administration by the medically trained personnel. Previous experimental and clinical experience suggests that, among the oximes mentioned, only trimedoxime and obidoxime can be used for acetylcholinesterase reactivation and antidotal protection against most of the organophosphorus insecticides. The search for an "omnipotent" oxime, effective in reactivation of AChE inhibited with both nerve agents and organophosphorus insecticides, is still ongoing.

  6. Acetylcholine produces contractions mediated by the cyclooxygenase pathway in arterial vessels in the Chilean frog (Calyptocephalella gayi

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    F. A. Moraga

    2017-05-01

    Full Text Available Abstract Previous studies performed in marine fish (I. conceptionis and G. laevifrons showed that indomethacin blocked arterial contraction mediated by acetylcholine (ACh. The objective of this study was to determine if contraction induced by acetylcholine is mediated by the cyclooxygenase pathway in several arterial vessels in the Chilean frog Calyptocephalella gayi. Arteries from the pulmonary (PA, dorsal (DA, mesenteric (MA and iliac (IA regions were dissected from 6 adult specimens, and isometric tension studies were done using dose response curves (DRC for ACh (10-13 to 10-3 M in presence of a muscarinic antagonist (Atropine 10-5 M and an unspecific inhibitor of cyclooxygenases (Indomethacin, 10-5M. All the studied arteries exhibited vasoconstriction mediated by ACh. This vasoconstriction was abolished in the presence of atropine in DA, MA and IA and attenuated in PA. Indomethacin abolished the vasoconstriction in MA and attenuated the response in PA, DA and IA. Similar to marine fish, C. gayi have an ACh-mediated vasoconstrictor pattern regulated by muscarinic receptors that activate a cyclooxygenase contraction pathway. These results suggest that the maintenance in vasoconstrictor mechanisms mediated by ACh→COX →vasoconstriction is conserved from fish to frogs.

  7. Unilateral anterior uveitis complicating zoledronic acid therapy in breast cancer

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    El Saghir Nagi S

    2005-12-01

    Full Text Available Abstract Background Zoledronic acid is very widely used in patients with metastatic bone disease and osteoporosis. Only one case of bilateral uveitis was recently reported related to its use. Case presentation We report the first case of severe unilateral anterior uveitis in a patient with breast cancer and an intraocular lens. Following zoledronic acid infusion, the patient developed severe and dramatic right eye pain with decreased visual acuity within 24 hours and was found to have a fibrinous anterior uveitis of moderate severity The patient was treated with topical prednisone and atropine eyedrops and recovered slowly over several months. Conclusion Internists, oncologists, endocrinologists, and ophtalmologists should be aware of uveitis as a possible complication of zoledronic acid therapy. Patients should be instructed to report immediately to their physicians and treatment with topical prednisone and atropine eyedrops should be instituted immediately at the onset of symptoms. This report documents anterior uveitis as a complication of zoledronic acid therapy. This reaction could be an idiosyncratic one but further research may shed more light on the etiology.

  8. Absence of cholinergic airway tone in normal BALB/c mice.

    Science.gov (United States)

    Larcombe, Alexander N; Zosky, Graeme R; Bozanich, Elizabeth M; Turner, Debra J; Hantos, Zoltan; Sly, Peter D

    2008-05-31

    Basal airway smooth muscle (ASM) tone has not been demonstrated in mice in vivo. To determine whether basal ASM tone is present in mouse airways we measured respiratory system impedance (Zrs) before and after either atropine or bilateral vagotomy. Zrs was measured using forced oscillations delivered via a wave-tube during slow ( approximately 35s) inflation-deflation maneuvers between transrespiratory pressures (Prs) of 0 and 20 cm H2O. A constant-phase tissue model was applied to the Zrs to calculate airway resistance (R aw), tissue damping (G) and elastance (H). Thoracic gas volume (TGV) was determined plethysmographically at Prs=0 cm H2O and by integration of the inspiratory flow. The relationship between conductance (G aw=1/R aw) and TGV during inflation was also examined. Neither atropine nor vagotomy produced any change in R aw, H, eta (=G/H), TGV or the slope of G aw vs. TGV that was different to that observed in the relevant control groups. These data show that BALB/c mice do not have cholinergic ASM tone in vivo.

  9. Cases of poisoning with organophosphates treated at the University Clinical Centre of Kosova.

    Science.gov (United States)

    Gashi, Musli; Gashi, Sanije; Berisha, Merita; Mekaj, Agon; Gashi, Goneta

    2010-01-01

    Everywhere today, poisonings present a significant and continuous increase of incidence in illness. Poisonings with organophosphates are more and more often. We do not have accurate statistics for this problem. The aim of this work was to present the clinical characteristics of poisoning with organophosphates, treated in University Clinical Centre in Prishtina. With the retrospective method, 23 patients were analyzed, 18 female and 5 male. Out of these, to (43.5%) have had tentative suicide, while 13 (56%) were accidentally exposed to poison. Poisoning with organophosphates was present in 3.8% of the overall number of poisonings. Organophosphate that was found in the analyzed poisoned patients was malathion (known here as Etiol). Average hospitalization time was 8.8 days (1 - 50 days range), average age of the patients was 27.1 years. Mortality scale was 52.1%. All these patients were treated with atropine. Atropine was given in intravenous way during 4.2 +/- 3.5 days and the average total dose was 82 +/- 61.5 mg. Pralidoxime antidote was not given to any of the patients. In adults, the poisoning was done mainly with the aim of suicide. Poisoned children with Etiol are in larger numbers from rural areas.

  10. [Transfer factor of immune reactivity to diphtheria-tetanus anatoxin modulates the action of neurotransmitters in the intestinal smooth muscle].

    Science.gov (United States)

    Melenevs'ka, N V; Miroshnychenko, M C; Filippov, I B; Kholodna, L S; Shuba, M F

    2007-01-01

    Transfer factor (TF) of immune reactivity (10(-5) - 10(-3) mg/ml) to diphtheria-tetanus anatoxin modulates slow waves and spontaneous contractile activity of non-atropinized smooth muscle stripes (SMS) of guinea-pig taenia coli. TF (10(-4) mg/ml) transforms slow waves into stable depolarization and tonic contraction. After SMS atropinization, the substance acts in the same way. In the presence of methylene blue (10(-5) M), a guanylatecyclase blocker, FT induces transitory increase of SMS muscle tone, which is followed by their stable relaxation. ATP and UTP, purinoceptors agonists, evoke substantial hyperpolarization of smooth muscle cells membrane and their relaxation. FT enhances post-inhibitory excitation in SMS. In the presence of acetylcholine (10(-5) M) FT (10(-4) mg/ml) transforms the inhibitory ATP action on tonic contraction into excitative. This substance (10(-5), 10(-4) mg/ml) enhances Ca2+ mobilization from ryanodine-sensitive calcium store, inhibits the release of these cations from IP3-sensitive calcium store of sarcoplasmic reticulum. TF demolishes the inhibitory actions of sodium nitroprusside (nitric oxide donor), and noradrenaline in taenia coli smooth muscles.

  11. The Organophosphate Paraoxon and Its Antidote Obidoxime Inhibit Thrombin Activity and Affect Coagulation In Vitro

    Science.gov (United States)

    Golderman, Valery; Shavit-Stein, Efrat; Tamarin, Ilia; Rosman, Yossi; Shrot, Shai; Rosenberg, Nurit

    2016-01-01

    Organophosphates (OPs) are potentially able to affect serine proteases by reacting with their active site. The potential effects of OPs on coagulation factors such as thrombin and on coagulation tests have been only partially characterized and potential interactions with OPs antidotes such as oximes and muscarinic blockers have not been addressed. In the current study, we investigated the in vitro interactions between coagulation, thrombin, the OP paraoxon, and its antidotes obidoxime and atropine. The effects of these substances on thrombin activity were measured in a fluorescent substrate and on coagulation by standard tests. Both paraoxon and obidoxime but not atropine significantly inhibited thrombin activity, and prolonged prothrombin time, thrombin time, and partial thromboplastin time. When paraoxon and obidoxime were combined, a significant synergistic effect was found on both thrombin activity and coagulation tests. In conclusion, paraoxon and obidoxime affect thrombin activity and consequently alter the function of the coagulation system. Similar interactions may be clinically relevant for coagulation pathways in the blood and possibly in the brain. PMID:27689805

  12. Involvement of Cholinergic and Opioid System in γ-Terpinene-Mediated Antinociception

    Directory of Open Access Journals (Sweden)

    Flávia Franceli de Brito Passos

    2015-01-01

    Full Text Available The literature shows that the monoterpenes are great candidates for the development of new drugs for the treatment of various pathological processes, including painful conditions. The gamma terpinene (γ-TPN is a monoterpene present in plant species that have multiple pharmacological properties and has structural similarity to antinociceptive monoterpenes, such as limonene and alpha-phellandrene. The γ-TPN molecular mass was evaluated by mass spectrometry and showed a pseudomolecular ion with m/z 137.0 Da. The animals did not present any signs of acute toxicity at 2 g/kg, p.o. γ-TPN (1.562 to 50 mg/kg, p.o. showed an antinociceptive effect in the formalin, capsaicin, and glutamate tests. γ-TPN has antinociceptive action when administered by others routes in glutamate test. To eliminate a possible sedative effect of γ-TPN, the open field and rota-rod test were conducted and the γ-TPN did not show muscle relaxant activity or central depressant effect. To investigate the mechanisms of action, the animals were pretreated with naloxone, glibenclamide, atropine, mecamylamine, or L-arginine in the glutamate test. γ-TPN antinociception was inhibited in the presence of naloxone, glibenclamide, atropine, and mecamylamine. The results suggest that the γ-TPN (p.o. produced antinociceptive effect in models of chemical nociception through the cholinergic and opioid systems involvement.

  13. Confirmed Datura poisoning in a horse most probably due to D. ferox in contaminated tef hay : clinical communication

    Directory of Open Access Journals (Sweden)

    R. Gerber

    2006-06-01

    Full Text Available Two out of a group of 23 mares exposed to tef hay contaminated with Datura ferox (and possibly D. stramonium developed colic. The 1st animal was unresponsive to conservative treatment, underwent surgery for severe intestinal atony and had to be euthanased. The 2nd was less seriously affected, responded well to analgesics and made an uneventful recovery. This horse exhibited marked mydriasis on the first 2 days of being poisoned and showed protracted, milder mydriasis for a further 7 days. Scopolamine was chemically confirmed in urine from this horse for 3 days following the colic attack, while atropine could just be detected for 2 days. Scopolamine was also the main tropane alkaloid found in the contaminating plant material, confirming that this had most probably been a case of D. ferox poisoning. Although Datura intoxication of horses from contaminated hay was suspected previously, this is the 1st case where the intoxication could be confirmed by urine analysis for tropane alkaloids. Extraction and detection methods for atropine and scopolamine in urine are described employing enzymatic hydrolysis followed by liquid-liquid extraction and liquid chromatography tandem mass spectrometry (LC/MS/MS.

  14. Adaptive divergence in resistance to herbivores in Datura stramonium

    Directory of Open Access Journals (Sweden)

    Guillermo Castillo

    2015-11-01

    Full Text Available Defensive traits exhibited by plants vary widely across populations. Heritable phenotypic differentiation is likely to be produced by genetic drift and spatially restricted gene flow between populations. However, spatially variable selection exerted by herbivores may also give rise to differences among populations. To explore to what extent these factors promote the among-population differentiation of plant resistance of 13 populations of Datura stramonium, we compared the degree of phenotypic differentiation (PST of leaf resistance traits (trichome density, atropine and scopolamine concentration against neutral genetic differentiation (FST at microsatellite loci. Results showed that phenotypic differentiation in defensive traits among-population is not consistent with divergence promoted by genetic drift and restricted gene flow alone. Phenotypic differentiation in scopolamine concentration was significantly higher than FST across the range of trait heritability values. In contrast, genetic differentiation in trichome density was different from FST only when heritability was very low. On the other hand, differentiation in atropine concentration differed from the neutral expectation when heritability was less than or equal to 0.3. In addition, we did not find a significant correlation between pair-wise neutral genetic distances and distances of phenotypic resistance traits. Our findings reinforce previous evidence that divergent natural selection exerted by herbivores has promoted the among-population phenotypic differentiation of defensive traits in D. stramonium.

  15. Adaptive divergence in resistance to herbivores in Datura stramonium.

    Science.gov (United States)

    Castillo, Guillermo; Valverde, Pedro L; Cruz, Laura L; Hernández-Cumplido, Johnattan; Andraca-Gómez, Guadalupe; Fornoni, Juan; Sandoval-Castellanos, Edson; Olmedo-Vicente, Erika; Flores-Ortiz, César M; Núñez-Farfán, Juan

    2015-01-01

    Defensive traits exhibited by plants vary widely across populations. Heritable phenotypic differentiation is likely to be produced by genetic drift and spatially restricted gene flow between populations. However, spatially variable selection exerted by herbivores may also give rise to differences among populations. To explore to what extent these factors promote the among-population differentiation of plant resistance of 13 populations of Datura stramonium, we compared the degree of phenotypic differentiation (P ST) of leaf resistance traits (trichome density, atropine and scopolamine concentration) against neutral genetic differentiation (F ST) at microsatellite loci. Results showed that phenotypic differentiation in defensive traits among-population is not consistent with divergence promoted by genetic drift and restricted gene flow alone. Phenotypic differentiation in scopolamine concentration was significantly higher than F ST across the range of trait heritability values. In contrast, genetic differentiation in trichome density was different from F ST only when heritability was very low. On the other hand, differentiation in atropine concentration differed from the neutral expectation when heritability was less than or equal to 0.3. In addition, we did not find a significant correlation between pair-wise neutral genetic distances and distances of phenotypic resistance traits. Our findings reinforce previous evidence that divergent natural selection exerted by herbivores has promoted the among-population phenotypic differentiation of defensive traits in D. stramonium.

  16. Acetylcholine Attenuates Hydrogen Peroxide-Induced Intracellular Calcium Dyshomeostasis Through Both Muscarinic and Nicotinic Receptors in Cardiomyocytes

    Directory of Open Access Journals (Sweden)

    Siripong Palee

    2016-06-01

    Full Text Available Background/Aims: Oxidative stress induced intracellular Ca2+ overload plays an important role in the pathophysiology of several heart diseases. Acetylcholine (ACh has been shown to suppress reactive oxygen species generation during oxidative stress. However, there is little information regarding the effects of ACh on the intracellular Ca2+ regulation in the presence of oxidative stress. Therefore, we investigated the effects of ACh applied before or after hydrogen peroxide (H2O2 treatment on the intracellular Ca2+ regulation in isolated cardiomyocytes. Methods: Single ventricular myocytes were isolated from the male Wistar rats for the intracellular Ca2+ transient study by a fluorimetric ratio technique. Results: H2O2 significantly decreased both of intracellular Ca2+ transient amplitude and decay rate. ACh applied before, but not after, H2O2 treatment attenuated the reduction of intracellular Ca2+ transient amplitude and decay rate. Both atropine (a muscarinic acetylcholine receptor blocker and mecamylamine (a nicotinic acetylcholine receptor blocker significantly decreased the protective effects of acetylcholine on the intracellular Ca2+ regulation. Moreover, the combination of atropine and mecamylamine completely abolished the protective effects of acetylcholine on intracellular Ca2+ transient amplitude and decay rate. Conclusion: ACh pretreatment attenuates H2O2-induced intracellular Ca2+ dyshomeostasis through both muscarinic and nicotinic receptors.

  17. The A- and B-type muscarinic acetylcholine receptors from Drosophila melanogaster couple to different second messenger pathways

    DEFF Research Database (Denmark)

    Ren, Guilin Robin; Folke, Jonas; Hauser, Frank

    2015-01-01

    to classical antagonists such as atropine. Here, we find that the D. melanogaster A-type mAChR is coupled to Gq/11 and D. melanogaster B-type mAChR to Gi/0. Furthermore, by comparing the second and third intracellular loops of all animal mAChRs for which the G protein coupling has been established, we could......Muscarinic acetylcholine receptors (mAChRs) are G protein-coupled receptors (GPCRs) that are activated by the agonists acetylcholine and muscarine and blocked by several antagonists, among them atropine. In mammals five mAChRs (m1-m5) exist of which m1, m3, and m5 are coupled to members of the Gq...... identify several amino acid residues likely to be specific for either Gq/11 or Gi/0 coupling. Using these hallmarks for specific mAChR G protein interaction we found that all protostomes with a sequenced genome have one mAChR coupled to Gq/11 and one to four mAChRs coupled to Gi/0. Furthermore...

  18. Influence of dopaminergic, adrenergic and cholinergic blockade and TRH administration on GH responses to GRF 1-29.

    Science.gov (United States)

    Jordan, V; Dieguez, C; Lafaffian, I; Rodriguez-Arnao, M D; Gomez-Pan, A; Hall, R; Scanlon, M F

    1986-03-01

    In order to establish the influence of dopaminergic, alpha-adrenergic and cholinergic pathways on GRF-mediated GH release we have studied the GH responses to GRF 1-29 (100 or 50 micrograms as i.v. bolus) alone and in combination with metoclopramide (MCP, 10 mg, i.v.), thymoxamine (THYM, 210 micrograms/min, 150 min infusion), and atropine (1.2 mg, i.v.). We have also investigated any possible interaction between TRH and GRF in view of the reported inhibitory effects of TRH infusion on stimulated GH release. Dopaminergic and alpha-adrenergic blockade with MCP and THYM respectively, did not have any effect on the GH responses to GRF. This lack of effect strongly suggests that any action which these neurotransmitters may exert on GH secretion is not at a pituitary level. TRH did not modify the GH response to GRF suggesting that the inhibitory effect on stimulated GH secretion is exerted at a hypothalamic level. In contrast, GH responses to GRF were significantly reduced by prior administration of atropine. These data support the view that cholinergic pathways play an important role in the regulation of GH secretion and such control may be exerted at both hypothalamic and pituitary levels.

  19. Current approaches to myopia control.

    Science.gov (United States)

    Leo, Seo Wei

    2017-05-01

    Myopia is a global problem, being particularly prevalent in the urban areas of east and southeast Asia. In addition to the direct economic and social burdens, associated ocular complications may lead to substantial vision loss. With prevalence of myopia above 80% and high myopia over 20%, it is crucial to control myopia. The aim of this review to is provide an update on the interventions to slow the onset of myopia and retard its progression. The epidemic of myopia is characterized by increasingly early onset, combined with high myopia progression rates. There are two pathways for myopia control: firstly to slow the onset of myopia and secondly to reduce or prevent progression. Increased time outdoors can reduce the onset of myopia. Atropine 0.01% dose offers an appropriate risk-benefit ratio, with no clinically significant visual side effects balanced against a significant 50% reduction in myopia progression. Orthokeratology contact lenses can slow axial length elongation, but infective keratitis is a risk. Peripheral defocussing lenses may both have a role in slowing myopic progression in a subset of children and further help our understanding of the physiologic control of ocular growth. Myopia control can be achieved by slowing the onset of myopia, which now appears to be possible through increasing time outdoors and slowing the progression of myopia with interventions like atropine and orthokeratology.

  20. Interventions to Reduce Myopia Progression in Children.

    Science.gov (United States)

    Tay, Su Ann; Farzavandi, Sonal; Tan, Donald

    2017-03-01

    Efforts to reduce the progression of myopia in childhood are on the rise, due to an increasing incidence of myopia worldwide and its associated sight-threatening complications. Interventions are aimed at reducing myopia in childhood and include environmental considerations, spectacles, contact lenses, and pharmacological agents. We reviewed recent literature with interventions aimed at reducing myopia progression in children and found that a number of interventions were significant in reducing the progression of myopia. Of these interventions, atropine showed the largest dose-related effect on myopia progression control. Although higher doses are associated with side effects of pupil dilatation, loss of accommodation, near vision blur, and rebound phenomenon, low-dose atropine has also been shown to provide effective myopia control with minimal side effects and rebound. To a lesser degree, bifocal soft contact lenses have also been shown to be effective in reducing the progression of myopia, though compliance is an issue. Similarly, orthokeratology lenses have also been shown to be effective in reducing axial length elongation and myopia progression, though long-term data on its rebound effects are unavailable.

  1. [Clinical effect of alanyl glutamine in the treatment of patients with gastrointestinal function obstacle caused by severe phorate poisoning].

    Science.gov (United States)

    Yu, Z K; Gong, Z J; Jian, X D; Qu, A J

    2017-07-20

    Objective: To observe the therapeutic efficacy of alanyl glutamine injection on patients with gastrointestinal function obstacle caused by severe phorate poisoning. Methods: A total of 80 eligible patients with gastrointestinal function obstacle caused by severe phorate poisoning were randomly divided into the control group (n=40) and treatment group (n=40) . The control group was treated with the conventional therapy, which included forbidden diet, atropine, pralidoxime iodide, anti-inflammatory, albumin infusion, ω-3 fish oil fat emulsion, protection of organs function, blood perfusion, and Fat Emulsion, Amino Acids (17) and Glucose Injection. The treatment group was treated with alanyl glutamine injection plus the conventional therapy. To observe the time of recovering to normal of gastrointestinal function between the two groups, compared the AChE activity and changes of prealbumin, albumin and total protein of the two groups respectively. Furthermore, the total atropine dosage, the total pralidoxime iodide dosage and ICU stay time between the two groups were also compared. Results: The gastrointestinal function recovery time of patients in the treatment group was less than the control group, the difference was statistically significant (Ppoisoning.

  2. Effect of aqueous fraction of Rosa damascena on ileum contractile response of guinea pigs.

    Science.gov (United States)

    Dolati, Karim; Rakhshandeh, Hassan; Shafei, Mohammad Naser

    2013-01-01

    The use of drugs with herbal origin is increasing for treatment of gastrointestinal (GI) disorders. Rosa damascena (R. damascena) is a well-known plant suggested to have beneficial effect on GI system. In this study, the effect of aqueous fraction of R. damascena on the contractions of isolated guinea pig ileum was investigated. Aqueous fraction of plant was obtained from ethanolic extract after ethyl acetate and n-butanol fractions were discarded. To evaluate effect of this fraction on ileum contraction, guinea pig ileum was removed and mounted on organ bath and its contraction was recorded. Effect of various concentrations (0.66, 0.83, and 1.3 mg/ml) of aqueous fraction on ileum contraction in comparison with Ach in presence and absence of atropine, a muscarinic antagonist of cholinergic, was evaluated. The response of ileum to 1 µg/ml of acetylcholine was considered as 100% response. Our results showed that aqueous fractions of R. damascena dose-dependently increased basal guinea pigs ileum contractions (p<0.05 to p<0.001). Maximal contraction of fraction (1.3 mg/ml) induced 23.4 % of maximal Ach response. The contraction of ileum to aqueous fraction was significant decreased in presence 0.001 µg/ml of atropine. It is concluded that aqueous fraction of R. damascena has mild excitatory effect on ileum contraction and this fraction may be beneficial as a mild laxative agent.

  3. Appearance of antidepressant-like effect by sildenafil in rats after central muscarinic receptor blockade: evidence from behavioural and neuro-receptor studies.

    Science.gov (United States)

    Brink, C B; Clapton, J D; Eagar, B E; Harvey, B H

    2008-01-01

    The phosphodiesterase (PDE) 5 inhibitor sildenafil has been shown to display psychotropic actions in humans and animals, and has been used for the treatment of antidepressant-associated erectile dysfunction. However, its effects on the neurobiology of depression are unknown. Nitric oxide (NO)-cyclic guanosine monophosphate (cGMP) inhibition is anti-depressant in animals, and increasing cGMP with sildenafil is anxiogenic in rodents. Substantial cholinergic-nitrergic interaction exists in the brain, while sildenafil shows modulatory actions on cholinergic transmission. Depression is also associated with increased cholinergic drive. Here we report that sildenafil increases muscarinic acetylcholine receptor (mAChR) signaling in human neuroblastoma cells. We also show that fluoxetine (20 mg/kg/day x 7 days), as well as a combination of sildenafil (10 mg/kg/day x 7 days) plus the antimuscarinic atropine (1 mg/kg/day x 7 days) demonstrates significant, comparable antidepressant-like effects in the rat forced swim test (FST) and also reduces cortical beta-adrenergic receptor (beta-AR) density, while sildenafil or atropine alone did not. Importantly, sildenafil did not modify fluoxetine's response. Sildenafil thus demonstrates antidepressant-like effects but only after central muscarinic receptor blockade, providing evidence for cholinergic-nitrergic interactions in the neurobiology of depression.

  4. Anticonvulsant actions of anticholinergic drugs in soman poisoning. (Reannouncement with new availability information)

    Energy Technology Data Exchange (ETDEWEB)

    Capacio, B.R.; Shih, T.M.

    1991-12-31

    The acute effects of the organophosphorus cholinesterase inhibitor soman include hypersecretions, convulsions, and death. The purpose of this study was to evaluate the anticholinergic compounds, aprophen, atropine sulfate, azaprophen, benactyzine, benztropine, biperiden, scopolamine HBr, and trihexyphenidyl for their efficacy in preventing soman-induced hypersecretions and convulsions. Male rats were injected with the oxime HI-6 (125 mg/kg, i.p.), to increase survival time, along with various intramuscular doses of the anticholinergics 30 min prior to a dose of soman that produced 100% convulsions. Signs of intoxication as well as the time-to-onset of convulsions were observed. The calculated anticonvulsant median effective dose values were 0.18, 0.33, 0.36, 0.55, 2.17, 2.30, 2.45, and 31.09 micro mol per kilogram for scopolamine HBr, biperiden, trihexyphenidy, benactyzine, benztropine, azaprophen, aprophen, and atropine sulfate, respectively. The same rank order by potency for inhibition of hypersecretions among these compounds was observed.

  5. The role of muscarinic cholinergic signaling in cost-benefit decision making

    Science.gov (United States)

    Fobbs, Wambura

    Animals regularly face decisions that affect both their immediate success and long term survival. Such decisions typically involve some form of cost-benefit analysis and engage a number of high level cognitive processes, including learning, memory and motivational influences. While decision making has been a focus of study for over a century, it's only in the last 20 years that researchers have begun to identify functional neural circuits that subserve different forms of cost-benefit decision making. Even though the cholinergic system is both functionally and anatomically positioned to modulate cost-benefit decision circuits, the contribution of the cholinergic system to decision making has been little studied. In this thesis, I investigated the cognitive and neural contribution of muscarinic cholinergic signaling to cost-benefit decision making. I, first, re-examined the effects of systemic administration of 0.3 mg/kg atropine on delay and probability discounting tasks and found that blockade of muscarinic acetylcholine receptors by atropine induced suboptimal choices (impulsive and risky) in both tasks. Since the effect on delay discounting was restricted to the No Cue version of the delay discounting task, I concluded that muscarinic cholinergic signaling mediates both forms of cost-benefit decision making and is selectively engaged when decisions require valuation of reward options whose costs are not externally signified. Second, I assessed the impact of inactivating the nucleus basalis (NBM) on both forms decision making and the effect of injecting atropine locally into the orbitofrontal cortex (OFC), basolateral amygdala (BLA), or nucleus accumbens (NAc) core during the No Cue version of the delay discounting task. I discovered that although NBM inactivation failed to affect delay discounting, it induced risk aversion in the probability discounting task; and blockade of intra- NAc core, but not intra-OFC or intra-BLA, muscarinic cholinergic signaling lead to

  6. Protection against the lethal effects of organophosphates by pyridine-2-aldoxime methiodide.

    Science.gov (United States)

    HOBBIGER, F

    1957-12-01

    The mechanism responsible for the protection against lethal organophosphate poisoning by pyridine-2-aldoxime methiodide (P-2-AM) was studied in the mouse. Two types of organophosphates were used: ethyl pyrophosphate (TEPP), E 600, Ro 3-0340, and Ro 3-0422 which form with true cholinesterase a diethylphosphoryl enzyme (1) and DFP, D 600, and Ro 3-0351 which form with true cholinesterase a diisopropylphosphoryl enzyme (2).In vitro and under the experimental conditions used more than 50% reactivation of (1) was obtained within 1 hr. by concentrations of P-2-AM ranging from 0.5 to 1x10(-5) M; 30 times higher concentrations of the oxime were required to achieve the same effect with (2). In vivo reactivation of phosphorylated true cholinesterases in blood amounted to 10 to 24% within the first 30 min. if 25 mg./kg. P-2-AM was injected (i.p.) 5 min. before a sublethal dose of TEPP, E 600, Ro 3-0340, or Ro 3-0422 and reactivation reached a maximum within 1 to 2 hr. after the injection of the oxime. P-2-AM was more effective when given 30 min. after the organophosphate. The effect of 25 mg./kg. P-2-AM on the phosphorylated true cholinesterase in brain (experiments with TEPP and E 600) was negligible. A dose of 25 mg./kg. P-2-AM had no consistent effect on the phosphorylated true cholinesterases in blood and brain of mice injected with sublethal doses of DFP, D 600, or Ro 3-0351.The protection by 25 mg./kg. P-2-AM against lethal doses of TEPP, E 600, Ro 3-0422, and Ro 3-0340 was greater than that obtained with 50 mg./kg. atropine sulphate, but the degree of protection was determined by the organophosphate itself and not its dialkylphosphoryl group. Protection by 25 mg./kg. P-2-AM against lethal doses of DFP, D 600, and Ro 3-0351 was negligible. The antidotal effect of P-2-AM was potentiated by atropine. Mice which were injected with atropine and P-2-AM were protected to a greater extent against DFP than against Ro 3-0422, and protection against DFP was only slightly less

  7. Role of the autonomic nervous system in the thermogenic response to food in lean individuals.

    Science.gov (United States)

    De Jonge, L; Garrel, D R

    1997-05-01

    The aim of this study was to determine the role of the autonomic nervous system (ANS) in obligatory and facultative components of the thermogenic response to food (TRF). Nineteen lean, healthy subjects participated in this study, which comprised two protocols, each exploring one component of the ANS. In the first experimental group, propranolol (prime: 80 micrograms/kg; continuous: 1 microgram.kg-1.min-1) was infused intravenously to inhibit sympathetic nervous activity (SNA), whereas in the second group atropine (prime: 5 micrograms/kg; continuous: 5 micrograms.kg-1.min-1) was used to inhibit parasympathetic nervous activity (PNA). The TRF was measured on four occasions: 1) after oral ingestion of a breakfast, during 0.9% NaCl perfusion, 2) after oral ingestion of the same breakfast, during the perfusion of one of the drugs, 3) after intragastric injection of a pureed form of the same meal as in part 1, during 0.9% NaCl perfusion, and 4) after intragastric feeding, during the administration of one of the drugs. Energy expenditure was measured by indirect calorimetry for 30 min before and 6 h after ingestion of the meal. Facultative TRF was defined as the difference between oral and intragastric TRF. Intragastric feeding significantly reduced TRF in both studies: 6.6 +/- 1.0 vs. 8.7 +/- 0.8% of the ingested energy in the SNA study and 5.5 +/- 1.6 vs. 7.4 +/- 3.1% in the PNA study. During propranolol infusion, TRF was significantly lower than it was during saline infusion after oral feeding (6.9 +/- 1.0% vs. 8.7 +/- 0.8% of ingested energy) but not after intragastric feeding. During atropine administration, TRF was reduced after both oral and intragastric feeding, although statistical significance was not reached in the latter. Atropine administration decreased gastric emptying (measured with an isotopic method) 2 h postingestion by 50%. These results show that the SNA is necessary for the facultative component of TRF to occur in humans. The role of the PNA appears

  8. Diazepam in the treatment of organophosphorus ester pesticide poisoning.

    Science.gov (United States)

    Marrs, Timothy C

    2003-01-01

    Although the main site of action of diazepam, as with other benzodiazepines, is at the gamma-aminobutyric acid A (GABAA) receptor, the degree to which the beneficial actions of diazepam in organophosphorus (OP) ester pesticide poisoning are mediated through the GABAA receptor has been a matter of controversy. Although in most series of OP intoxications, convulsions have been relatively uncommon, it is probable that convulsions produce long-term sequelae in the central nervous system by causing structural damage. Animal studies have demonstrated that diazepam prevents and treats convulsions produced by OPs and may prevent the late effects caused by damage to the central nervous system induced by such convulsions. Consequently, the use of diazepam is an important part of the treatment regimen of severe OP poisoning as it prevents, or at least reduces the duration of, convulsions. In addition, case reports suggest that diazepam will also ameliorate muscle fasciculation, a subjectively unpleasant feature of OP pesticide poisoning. There are no data, either experimental or clinical, demonstrating any clear effect of diazepam alone on lethality in OP poisoning. In fact, in one study of large animals, diazepam, given alone, increased lethality. In animals experimentally poisoned with OPs, combined treatment with atropine and diazepam significantly lowered lethality compared with atropine treatment alone, indicating a clear beneficial effect. There are numerous case reports of the use of diazepam, generally as an adjunct to other more specific OP antidotes such as atropine and/or pyridinium oximes. Based on this evidence and pharmacodynamic studies in experimental animals, diazepam should be given to patients poisoned with OPs whenever convulsions or pronounced muscle fasciculation are present. In severe poisoning, diazepam administration should be considered even before these complications develop. Although diazepam has a large therapeutic index, there appears to be no

  9. Cardiovascular actions of the venom from the Irukandji (Carukia barnesi) jellyfish: effects in human, rat and guinea-pig tissues in vitro and in pigs in vitro.

    Science.gov (United States)

    Winkel, Kenneth D; Tibballs, James; Molenaar, Peter; Lambert, Gavin; Coles, Peter; Ross-Smith, Mark; Wiltshire, Carolyn; Fenner, Peter J; Gershwin, Lisa-Ann; Hawdon, Gabrielle M; Wright, Christine E; Angus, James A

    2005-09-01

    1. We have investigated the cardiovascular pharmacology of the crude venom extract (CVE) from the potentially lethal, very small carybdeid jellyfish Carukia barnesi, in rat, guinea-pig and human isolated tissues and anaesthetized piglets. 2. In rat and guinea-pig isolated right atria, CVE (0.1-10 microg/mL) caused tachycardia in the presence of atropine (1 micromol/L), a response almost completely abolished by pretreatment with tetrodotoxin (TTX; 0.1 micromol/L). In paced left atria from guinea-pig or rat, CVE (0.1-3 microg/mL) caused a positive inotropic response in the presence of atropine (1 micromol/L). 3. In rat mesenteric small arteries, CVE (0.1-30 microg/mL) caused concentration-dependent contractions that were unaffected by 0.1 micromol/L TTX, 0.3 micromol/L prazosin or 0.1 micromol/L omega-conotoxin GVIA. 4. Neither the rat right atria tachycardic response nor the contraction of rat mesenteric arteries to CVE were affected by the presence of box jellyfish (Chironex fleckeri) antivenom (92.6 units/mL). 5. In human isolated driven right atrial trabeculae muscle strips, CVE (10 microg/mL) tended to cause an initial fall, followed by a more sustained increase, in contractile force. In the presence of atropine (1 micromol/L), CVE only caused a positive inotropic response. In separate experiments in the presence of propranolol (0.2 micromol/L), the negative inotropic effect of CVE was enhanced, whereas the positive inotropic response was markedly decreased. 6. In anaesthetized piglets, CVE (67 microg/kg, i.v.) caused sustained tachycardia and systemic and pulmonary hypertension. Venous blood samples demonstrated a marked elevation in circulating levels of noradrenaline and adrenaline. 7. We conclude that C. barnesi venom may contain a neural sodium channel activator (blocked by TTX) that, in isolated atrial tissue (and in vivo), causes the release of transmitter (and circulating) catecholamines. The venom may also contain a 'direct' vasoconstrictor component

  10. Interactions between biomaterials and the sclera: Implications on myopia progression

    Science.gov (United States)

    Su, James

    injectable materials. Fourth, the muscarinic antagonist drug, atropine, was encapsulated within the edsIPNs and delivered to the chick eye posterior pole to evaluate the local effect of atropine release. This fourth study offered an alternative method of ocular drug delivery for treatment of myopia, with the potential to elucidate the actual location of the inhibitive effect of atropine on myopia progression. In summary, this dissertation contributes to the design and use of biomaterials specific to myopia therapy and adds novel insights to scleral tissue engineering.

  11. Effects of intraocular mescaline and LSD on visual-evoked responses in the rat.

    Science.gov (United States)

    Eells, J T; Wilkison, D M

    1989-01-01

    The effects of mescaline and LSD on the flash-evoked cortical potential (FEP) were determined in unrestrained rats with chronically-implanted electrodes. Systemic administration of mescaline or LSD significantly attenuated the primary component of the FEP at three stimulus intensities with the greatest effect observed 60-90 minutes following drug administration. The magnitude and specificity of the effects of these agents on the primary response suggest that they produce deficits in conduction through the retino-geniculato-cortical system. The serotonin receptor antagonists, cyproheptadine and methysergide, antagonized the mescaline-induced depression of the FEP in accordance with neurochemical and behavioral evidence that mescaline acts as a partial agonist on serotonin receptors. Topical or intraocular administration of atropine antagonized the actions of systemically-administered mescaline. In addition, intraocular administration of mescaline or LSD attenuated the FEP indicative of an action of these hallucinogens on visual processing in the retina which is modulated by muscarinic receptor activity.

  12. Asystole following positive pressure insufflation of right pleural cavity: a case report

    Directory of Open Access Journals (Sweden)

    Konia Mojca R

    2011-06-01

    Full Text Available Abstract Introduction Adverse hemodynamic effects with severe bradycardia have been previously reported during positive pressure insufflation of the right thoracic cavity in humans. To the best of our knowledge, this is the first report of asystole during thoracoscopic surgery with positive pressure insufflation. Case presentation A 63-year-old Caucasian woman developed asystole at the onset of positive pressure insufflation of her right hemithorax during a thoracoscopic single-lung ventilation procedure. Immediate deflation of pleural cavity, intravenous glycopyrrolate and atropine administration returned her heart rhythm to normal sinus rhythm. The surgery proceeded in the absence of positive pressure insufflation without any further complications. Conclusions We discuss the proposed mechanisms of hemodynamic instability with positive pressure thoracic insufflation, and anesthetic and insufflation techniques that decrease the likelihood of adverse hemodynamic events.

  13. The inhibition of phosphodiesterase type 5 as a novel target for antidepressant action

    DEFF Research Database (Denmark)

    Liebenberg, Nico

    2010-01-01

    therapy of depression. A recent study from our laboratory reported an antidepressant-like response in the rat forced swim test (FST) following chronic (11 day) co-administration of the phosphodiesterase type 5 (PDE5) inhibitor sildenafil and the muscarinic acetylcholine (mACh) receptor antagonist atropine...... rats were treated with vehicle/drug(s) for 14 days, whereafter immobility, swimming and climbing behaviours were measured in the FST, or time spent in social interaction in the social interaction test. Following decapitation, saturation binding studies were performed for the measurement of m...... not involve up-regulation of frontal cortical and hippocampal mACh receptors. In summary, this project emphasises the potential of PDE5 inhibition as a novel antidepressant and anxiolytic strategy, and provides important insight into the specific neuronal mechanism(s) that may be involved...

  14. Ulcers in restrained rats: Study of protective substances

    Science.gov (United States)

    Buche, L.; Gallaire, D.

    1980-01-01

    The genesis of ulcers in restrained rats is discussed through an investigation of the relationship between the protective effects of nervous system effectual substances examined vis-a-vis ulcers in restrained rats and their elective or secondary pharmacologic effects. The substances used were capable of either peripheral parasympatholytic, sympatholytic, ganglioplegic, spasmolytic effects or central, hypnotic, tranquilizing, neuroleptic, analgesic effects. The regular and considerable protection observed with parasympatholytics (atropine sulfate, benzylonium bromide, dihexyverine, J.L. 1344) and a ganglioplegic (pentamethonium) is a function of their anticholinergic properties. It is of less importance with dibenamine, a sympatholytic action on the adrenergic receptors. Among the central depressive substances tested (hypnotics, tranquilizers, neuroleptics, analgesic), phenobarbital at a nonhypnotic dose, and dextromoramide at a nonanalgesic dose, show antiulcerous effects, which are found with chlorpromazine only at cataleptogenic doses.

  15. Mannich Bases: An Important Pharmacophore in Present Scenario

    Directory of Open Access Journals (Sweden)

    Suman Bala

    2014-01-01

    Full Text Available Mannich bases are the end products of Mannich reaction and are known as beta-amino ketone carrying compounds. Mannich reaction is a carbon-carbon bond forming nucleophilic addition reaction and is a key step in synthesis of a wide variety of natural products, pharmaceuticals, and so forth. Mannich reaction is important for the construction of nitrogen containing compounds. There is a number of aminoalkyl chain bearing Mannich bases like fluoxetine, atropine, ethacrynic acid, trihexyphenidyl, and so forth with high curative value. The literature studies enlighten the fact that Mannich bases are very reactive and recognized to possess potent diverse activities like anti-inflammatory, anticancer, antifilarial, antibacterial, antifungal, anticonvulsant, anthelmintic, antitubercular, analgesic, anti-HIV, antimalarial, antipsychotic, antiviral activities and so forth. The biological activity of Mannich bases is mainly attributed to α, β-unsaturated ketone which can be generated by deamination of hydrogen atom of the amine group.

  16. Antidiarrheal activity of Pterocarpus erinaceus methanol leaf extract in experimentally-induced diarrhea.

    Science.gov (United States)

    Ezeja, I Maxwell; Ezeigbo, Ihechiluru I; Madubuike, Kelechi G; Udeh, Nkiru E; Ukweni, Iheanacho A; Akomas, Stella C; Ifenkwe, Daniel C

    2012-02-01

    To investigate the antidiarrheal activity of the methanol leaf extract of Pterocarpus erinaceus in vivo. The methanol leaf extract of Pterocarpus erinaceus was evaluated using different doses (100, 200 and 400 mg/kg body weight) orally for antidiarrheal activity using castor oil-induced diarrhea, charcoal meal transit time and castor oil-induced enteropooling in different groups of albino Wistar mice. The activity of the extract at different doses were compared to diphenoxylate (5 mg/kg) and atropine sulphate (3 mg/kg) which were used as standard reference drugs and also to the distilled water administered negative control group of mice. The extract at the doses used caused a significant (PPterocarpus erinaceus extract produced significant antidiarrheal activity and the action may attribute to inhibition of gastrointestinal movement and fluid secretion. Copyright © 2012 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

  17. Oximes: Inhibitors of Human Recombinant Acetylcholinesterase. A Structure-Activity Relationship (SAR) Study

    Science.gov (United States)

    Sepsova, Vendula; Karasova, Jana Zdarova; Korabecny, Jan; Dolezal, Rafael; Zemek, Filip; Bennion, Brian J.; Kuca, Kamil

    2013-01-01

    Acetylcholinesterase (AChE) reactivators were developed for the treatment of organophosphate intoxication. Standard care involves the use of anticonvulsants (e.g., diazepam), parasympatolytics (e.g., atropine) and oximes that restore AChE activity. However, oximes also bind to the active site of AChE, simultaneously acting as reversible inhibitors. The goal of the present study is to determine how oxime structure influences the inhibition of human recombinant AChE (hrAChE). Therefore, 24 structurally different oximes were tested and the results compared to the previous eel AChE (EeAChE) experiments. Structural factors that were tested included the number of pyridinium rings, the length and structural features of the linker, and the number and position of the oxime group on the pyridinium ring. PMID:23959117

  18. [Myopia, a growing health problem].

    Science.gov (United States)

    Tideman, J W L; Polling, J R; van der Schans, A; Verhoeven, V J M; Klaver, C C W

    2016-01-01

    - Myopia is the eye disorder with the most rapid increase in prevalence worldwide. It develops in childhood, with a peak incidence between the ages of 13 to 15 years. - Especially high myopia, i.e. a refractive error of -6 diopters or more, increases the risk of permanent visual impairment during adulthood due to structural abnormalities of the retina and optic nerve.- The cause of myopia is complex. Lifestyle factors in childhood, such as limited time spent outdoors and close work - such as reading and smartphone usage - are risk factors. Furthermore, genetic studies have revealed more than 100 factors associated with the development of myopia. - Pharmacological and optical interventions to inhibit myopia progression are increasingly applied. The use of atropine eye drops in children and has shown to be an effective treatment.

  19. [Mechanism of action of parenterally administered protein hydrolysates on gastric secretion].

    Science.gov (United States)

    Sysoev, Iu A; Sidorenko, V I

    1976-01-01

    Tests were conducted on dogs with a gastric fistula and removal of the structure associated with the formation of antral gastrin (mucosectomy of the antral portion of the stomach). In another series of experiments use was made of dogs with Basov's fistula, isolated Pavlov's and Haidenhain's pouches. The basic mechanism of action exerted by apparently introduced proteinic hydrolysates on the gastric secretion was found to be of nervous nature. This is evidenced by the fact of an abrupt suppression of secretion following a preliminary injection of atropine, by a less abundant secretion in dogs with a vagus-denervated isolated pouch and, finally, by the absence of any significant differences in the gastric secretion of dogs with mucosectomized antral segment of the stomach and in control ones.

  20. Post-thoracotomy dysrhythmia.

    Science.gov (United States)

    Haverkamp, Wilhelm; Hachenberg, Thomas

    2016-02-01

    This article reviews and summarizes the pathophysiology, risk factors, and the management of arrhythmias in patients undergoing noncardiac thoracic surgery. Cardiac arrhythmias are common findings in the perioperative period, particularly with increasing age. They often complicate the course of the patient's recovery after operation. The most common postoperative arrhythmia is atrial fibrillation. It requires either a rate or rhythm control strategy, and the need for anticoagulation has to be assessed depending on the duration of the arrhythmia and risk factors. Fortunately, malign sustained ventricular tachyarrhythmias (ventricular tachycardia, ventricular fibrillation) are rare. Acute treatment and, in the absence of a reversible cause, a long-term preventive strategy may be warranted. Transient bradyarrhythmias can be managed by atropine or with temporary pacing. Arrhythmias are common after thoracotomy. Physicians treating patients with postoperative arrhythmias should bear in mind that arrhythmia management does not only comprise a specific therapy for the arrhythmia itself, but also includes the correction of transient and correctable predisposing and causative factors.

  1. Intrabiliary pressure changes produced by narcotic drugs and inhalation anesthetics in guinea pigs.

    Science.gov (United States)

    Arguelles, J E; Franatovic, Y; Romo-Salas, F; Aldrete, J A

    1979-01-01

    The effects of narcotic agents and two inhalation anesthetics on intrabiliary pressure (IBP) were measured before and after morphine (0.2 mg/kg), meperidine (2 mg/kg), fentanyl (0.002 mg/kg), or pentazocine (1 mg/kg) given intramuscularly to guinea pigs, and after halothane (0.5, 1.0, 1.5, or 2.0 MAC) or enflurane (same range of MAC) administered by inhalation. All narcotics except pentazocine significantly increase IBP, the increases ranging from 85.7% for meperidine to 143.4% for fentanyl. Pentazocine had no effect on IBP. Peak IBP increases occurred between 9 and 18 minutes after administration. The elevation of IBP produced by narcotics was reversed by atropine (0.05 mg/kg). No statistically significant alterations of IBP were noted during halothane or enflurane anesthesia.

  2. Diverse presentation of breath holding spells: two case reports with literature review.

    Science.gov (United States)

    Rathore, Geetanjali; Larsen, Paul; Fernandez, Cristina; Parakh, Manish

    2013-01-01

    Breath holding spells are a common and dramatic form of syncope and anoxic seizure in infancy. They are usually triggered by an emotional stimuli or minor trauma. Based on the color change, they are classified into 3 types, cyanotic, pallid, and mixed. Pallid breath holding spells result from exaggerated, vagally-mediated cardiac inhibition, whereas the more common, cyanotic breathholding spells are of more complex pathogenesis which is not completely understood. A detailed and accurate history is the mainstay of diagnosis. An EKG should be strongly considered to rule out long QT syndrome. Spontaneous resolution of breath-holding spells is usually seen, without any adverse developmental and intellectual sequelae. Rare cases of status epilepticus, prolonged asystole, and sudden death have been reported. Reassurance and education is the mainstay of therapy. Occasionally, pharmacologic intervention with iron, piracetam; atropine may be of benefit. Here we present 2 cases, one of each, pallid and cyanotic breath holding spells.

  3. Can We Find Better Bronchodilators to Relieve Asthma Symptoms?

    Directory of Open Access Journals (Sweden)

    Elizabeth A. Townsend

    2012-01-01

    Full Text Available Bronchodilators are the first line therapy during acute asthmatic exacerbations to reverse airway obstruction primarily by relaxing airway smooth muscle. Only three categories of bronchodilators exist in clinical practice: -adrenergic agonists, anticholinergics, and methylxanthines. Each of these categories have specific drugs dating back to the early 20th century, raising the question of whether or not we can find better bronchodilators. While caffeine, theophylline, atropine, and epinephrine were the first generations of therapeutics in each of these drug classes, there is no question that improvements have been made in the bronchodilators in each of these classes. In the following editorial, we will briefly describe new classes of potential bronchodilators including: novel PDE inhibitors, natural phytotherapeutics, bitter taste receptor ligands, and chloride channel modulators, which have the potential to be used alone or in combination with existing bronchodilators to reverse acute airway obstruction in the future.

  4. Adolf Hitler's medical care.

    Science.gov (United States)

    Doyle, D

    2005-02-01

    For the last nine years of his life Adolf Hitler, a lifelong hypochondriac had as his physician Dr Theodor Morell. Hitler's mood swings, Parkinson's disease, gastro-intestinal symptoms, skin problems and steady decline until his suicide in 1945 are documented by reliable observers and historians, and in Morell's diaries. The bizarre and unorthodox medications given to Hitler, often for undisclosed reasons, include topical cocaine, injected amphetamines, glucose, testosterone, estradiol, and corticosteroids. In addition, he was given a preparation made from a gun cleaner, a compound of strychnine and atropine, an extract of seminal vesicles, and numerous vitamins and 'tonics'. It seems possible that some of Hitler's behaviour, illnesses and suffering can be attributed to his medical care. Whether he blindly accepted such unorthodox medications or demanded them is unclear.

  5. Involvement of NMDA receptors in soman-induced neuropathology

    Energy Technology Data Exchange (ETDEWEB)

    De Groot, D.M.; Bierman, E.P.; Van Huygevoort, A.H.; Bruijnzeel, P.L.

    1993-05-13

    Our current working hypothesis with regard to soman-induced neuropathology is that accumulated ACh, resulting from soman-inhibited ACHE potentiates glutamate-induced neuronal degeneration, most likely by lowering the threshold for glutamate excitation at the NMDA-receptor sites. The activation of the NMDA-ionic channels may lead to massive Ca2+ fluxes into the postsynaptic cell, causing cell degeneration. In this concept the NMDA receptor plays a crucial role. In the present study, the involvement of NMDA receptors in soman-induced convulsions is tested by injecting NMDA receptor antagonists MK801, AP5 and TCP, whether or not in combination with atropine and/or diazepam, either directly into the hippocampal CA1 area or in the lateral ventricle very near to CA1. This area is predominantly affected by soman and contains high concentrations of NMDA receptors. Also the effect of injection with a non-NMDA receptor antagonist is tested.

  6. Effects of Naja haje (Egyptian cobra), Naja naja (hooded cobra), Naja nigricollis (spitting cobra) and Naja mossambica mossambica (Mozambique spitting cobra) venoms on the isolated guinea-pig tracheal muscle.

    Science.gov (United States)

    Tilmisany, A K; Abdel Aziz, A; Osman, O H; Mustafa, A A

    1986-01-01

    Venoms from N. haje, N. naja, N. nigricollis and N. mossambica were tested on the isolated guinea-pig trachea. The four venoms (1-30 micrograms/ml) contracted the tracheal smooth muscle after a delay of 40-60 sec. A second challenge with the venoms caused either no or a much reduced contraction or a relaxant effect. The contraction could be prevented by pretreatment with antihistaminics, but not by atropine, methysergide or indomethacin, indicating that it is due to histamine release by the venoms. This release requires extracellular Ca2+, as it could be prevented by pretreatment with verapamil. Under conditions which prevented histamine release or its effect, each of the four venoms resulted in a reproducible relaxant effect which was not blocked by propranolol. It is concluded that the venoms have one or more component(s) causing histamine release which masks the relaxation caused by another component(s) of the venoms.

  7. Effect of calcitonin gene-related peptide (CGRP) on motility and on the release of substance P, neurokinin A, somatostatin and gastrin in the isolated perfused porcine antrum

    DEFF Research Database (Denmark)

    Rasmussen, T N; Schmidt, P; Poulsen, S S

    2001-01-01

    We studied the effect of porcine CGRP (pCGRP) in concentrations from 10(-10) to 10(-8) mol L(-1) on the motility and on the release of substance P, neurokinin A, somatostatin and gastrin in the antrum using the isolated perfused porcine antrum as experimental model. In addition, we studied...... release. The effect of pCGRP was unaffected by the addition of the nonpeptide antagonists for the NK-1 (CP-99994) and NK-2 receptors (SR48968), both at 10(-6) mol L(-1), whereas atropine (10(-6) mol L(-1)) completely abolished the motor effect of pCGRP. The release of somatostatin was significantly....... in addition, pCGRP increases the release of somatostatin but has no effect on gastrin release in the isolated perfused porcine antrum....

  8. GRP-producing nerves control antral somatostatin and gastrin secretion in pigs

    DEFF Research Database (Denmark)

    Holst, J J; Orskov, C; Poulsen, Steen Seier

    1987-01-01

    of isolated perfused pig antrum with intact vagus nerve supply. Electrical stimulation of the vagus nerves at 4 Hz increased the antral release of GRP up to 10-fold and increased SS output 2- to 3-fold. Atropine at 10(-6) M had no effect on these responses. Intra-arterial GRP increased SS secretion...... significantly at 10(-10) M and eightfold at 10(-8) M, whereas gastrin secretion was stimulated significantly at 10(-11) M and maximally at 10(-10) M and inhibited at 10(-8) M. Preperfusion with a GRP antagonist ([D-Arg1,D-Pro2,D-Trp7,9,Leu11]substance P) or Fab fragments of antibodies against GRP abolished...

  9. Reducing by 50% the incidence of maternal hypotension during elective caesarean delivery under spinal anesthesia: Effect of prophylactic ondansetron and/or continuous infusion of phenylephrine - a double-blind, randomized, placebo controlled trial

    Directory of Open Access Journals (Sweden)

    Jose Ramon Ortiz-Gomez

    2017-01-01

    Results: There were differences (P = 0.0001 in the number of patients with hypotension (50.8% control, 44.6% O, 20.9% P, 25.0% OP, the percentage of time points (P = 0.0001 with systolic hypotension per patient (17.4% control, 8.7% O, 2.1% P, 6.7% OP and the number of patients requiring supplementary boluses of ephedrine (P = 0.003, phenylephrine (P = 0.017 or atropine (P = 0.0001. Conclusions: A 50 μg/min phenylephrine infusion reduces by 50%, the incidence of maternal hypotension compared with placebo, but infusions of phenylephrine are still not routine in our environment. Prophylactic ondansetron 8 mg might be considered in this situation, because it does not reduce the incidence of maternal hypotension but diminishes its severity, reducing the number of hypotensive events per patient by 50%.

  10. Update and review of Urrets-Zavalia syndrome

    Directory of Open Access Journals (Sweden)

    Otavio A. Magalhães

    2016-06-01

    Full Text Available ABSTRACT For more than half a century, Urrets-Zavalia syndrome (fixed dilated pupil has been described as a postoperative complication of ophthalmic surgery. Since first reported as a complication of penetrating keratoplasty for keratoconus in patients receiving atropine, the characteristic features of Urrets-Zavalia syndrome have been expanded. In previous literature, a total of 110 cases resulted in a fixed and dilated pupil. Increased intraocular pressure (IOP in the immediate postoperative period, phakia, and air or gas in the anterior chamber appear to be the most important risk factors for Urrets-Zavalia syndrome following ophthalmic procedures. Mannitol, IOP control, the removal of air or gas in the anterior chamber, and iridectomy have all demonstrated utility in managing Urrets-Zavalia syndrome.

  11. Effects of Acupuncture on Heart Rate Variability in Beagles; Preliminary Results

    Directory of Open Access Journals (Sweden)

    Huan Wang

    2013-01-01

    Full Text Available Evidence-based animal experimental research concerning the effects of acupuncture on autonomic function was performed by two research teams from China and Austria. This study describes measurements in beagles. Heart rate variability (HRV recordings were performed under stable conditions in Beijing, China, and the data analysis and interpretation were completed in Graz, Austria. The electrocardiograms were recorded during bilateral body acupuncture (PC6, Neiguan. Power of the low frequency (LF, high frequency (HF, and the ratio (LF/HF changed significantly during acupuncture stimulation in beagles after injection of atropine and β-blocker. However, there was no significant change in HF power after needling the Neiguan acupoint when a cervical vagotomy has been performed. Our findings show that acupuncture can mediate the HRV even after pharmaceutical blocking of autonomic function. Acupuncture effects on HRV should rely not only on autonomic nervous system but on complete central nervous system.

  12. [The esophagus in Chagas' disease: physiologic, pharmacologic and clinical studies].

    Science.gov (United States)

    Meneghelli, U G

    1987-01-01

    Intramural denervation confirmed anatomopathologically and by means of a pharmacological test is the main factor responsible for achalasia of the cardia and for the absence of peristalsis in the esophageal body in Chagas' disease. The resulting difficulty in transit and stasis cause the main symptoms and complications of megaesophagus. Among the recent phenomena observed in the physiopathology and pharmacology of megaesophagus by the manometric method, we may mention: delayed pharyngo-esophageal time, concomitance of peristalsis and aperistalsis and abnormal responses of the lower sphincter to caerulein, atropine, nifedipine and isosorbitol dinitrate. Gammascintillography was shown to be useful in the study of esophageal transit in megaesophagus by permitting the detection of unsuspected abnormalities, especially when deglution is done with the patient lying down, and by affording a dynamic and quantitative view of the changes in esophageal emptying.

  13. Role of central alpha-1 adrenoceptors in canine narcolepsy.

    Science.gov (United States)

    Mignot, E; Guilleminault, C; Bowersox, S; Rappaport, A; Dement, W C

    1988-09-01

    The role of central alpha-1 adrenergic receptors in cataplexy was investigated in genetically narcoleptic Doberman pinschers. Treatment of narcoleptic dogs with 25-600 micrograms/kg prazosin, a selective alpha-1 adrenergic receptor blocker, exacerbated cataplexy, whereas treatment with the alpha-1 agonist, methoxamine, ameliorated it. Subsequent studies showed that the beneficial effects of classical treatments of human narcolepsy (amphetamines and tricyclic antidepressants) are antagonized by prazosin, suggesting that these drugs are active through an indirect alpha-1 stimulation (via an increase of norepinephrine in the synaptic cleft). Other studies confirmed that the observed effects were not due to peripheral alpha-1 cardiovascular involvement. Atropine, a central anticholinergic agent, but not methylatropine, a peripheral one, completely suppressed the prazosin effect, which suggests that adrenergic and cholinergic systems act sequentially and not independently to generate cataplexy. Little is known about the physiological role of central alpha-1 adrenoceptors. This series of experiments implicates these receptors in narcolepsy-cataplexy.

  14. M sub 1 muscarinic antagonists interact with. sigma. recognition sites

    Energy Technology Data Exchange (ETDEWEB)

    Hudkins, R.L. (Virginia Commonwealth Univ., Richmond (United States)); DeHaven-Hudkins, D.L. (Sterling Research Group, Malvern, PA (United States))

    1991-01-01

    The M{sub 1}-selective muscarinic antagonists aprophen, caramiphen, carbetapentane, 2-DAEX, dicyclomine, hexahydrosiladifenidol, iodocaramiphen, nitrocaramiphen, oxybutynin and trihexyphenidyl potently inhibited binding to {sigma} sites in brain. Both basic ester and non-ester structural type compounds which exhibit affinity for the muscarinic receptor also demonstrated affinity for the {sigma} site, while the classical antimuscarinic agents atropine and QNB, and the tricyclic pirenzepine, were ineffective in binding to this site. The authors also observed a significant correlation between the K{sub i} values for {sigma}compounds to inhibit ({sup 3}H)pirenzepine binding and their IC{sub 50} values to inhibit carbachol-stimulated phosphoinositide turnover. These observations may aid in elucidating the relationship of {sigma} binding to inhibition of phosphoinositide turnover stimulated by cholinergic agonists.

  15. Effects of Swertia japonica extract and its main compound swertiamarin on gastric emptying and gastrointestinal motility in mice.

    Science.gov (United States)

    Kimura, Yoshiyuki; Sumiyoshi, Maho

    2011-09-01

    The Swertia japonica is used clinically as a remedy for gastrointestinal symptoms in Japan. We examined the effects of a S. japonica and swertiamarin on gastric emptying and gastrointestinal motility in atropine-, dopamine-, and 5-hydroxytryptamine (5-HT)-treated mice. All three preparations inhibited reductions in gastric emptying and gastrointestinal motility induced by dopamine (1mg/kg, intraperitoneal injection, ip). Neither the powder, swertiamarin, nor itopride had any effect on the reductions in gastric emptying and gastrointestinal motility caused by 5-HT (4 mg/kg, ip). These findings suggest that the powder and swertiamarin stimulate gastric emptying and gastrointestinal motility by inhibiting the dopamine D(2) receptor. Copyright © 2011 Elsevier B.V. All rights reserved.

  16. Intravenously administered lidocaine in therapeutic doses increases the intraspinal release of acetylcholine in rats

    DEFF Research Database (Denmark)

    Abelson, Klas S P; Höglund, A Urban

    2002-01-01

    The local anesthetic lidocaine suppresses different pain conditions when administered systemically. Part of the antinociceptive effect appears to be mediated via receptor mechanisms. We have previously shown that muscarinic and nicotinic agonists that produce antinociception increase the intraspi......The local anesthetic lidocaine suppresses different pain conditions when administered systemically. Part of the antinociceptive effect appears to be mediated via receptor mechanisms. We have previously shown that muscarinic and nicotinic agonists that produce antinociception increase...... the intraspinal release of acetylcholine. In the present study it was hypothesized that systemically administered lidocaine is acting through the same mechanisms as cholinergic agonists and affects the intraspinal release of acetylcholine. Microdialysis probes were placed in anesthetized rats for sampling...... of acetylcholine. Ten and 30 mg/kg lidocaine injected intravenously significantly increased the intraspinal release of acetylcholine. The effect of lidocaine could be reduced by pretreatment with intraspinally administered atropine or mecamylamine. Our results suggest that the antinociceptive effect produced...

  17. [Successful treatment by 4--aminopyridine of three cases of severe verapamil poisoning].

    Science.gov (United States)

    Magdalan, Jan; Kochman, Krystyna; Antończyk, Andrzej; Przewłocki, Michal; Smolarek, Małgorzata

    2003-01-01

    Three cases of verapamil intoxication were presented. In all cases shock and circulatory insufficiency were observed. In case no. 1 respiratory insufficiency and confusion were observed, in case no. 3 second-degree atrioventricular block was noted. The protracted hypotension (shock), circulatory insufficiency and atrioventricular block did not respond to calcium therapy, high dose of vasopressor amines and atropine. The addition of 4-aminopyridine (4-AP) infusion resulted in fast receding of poisoning symptoms; receding of atrioventricular block, cardiogenic shock and circulatory insufficiency. These cases suggest the usefulness of 4-AP in the treatment of verapamil poisoning. However, confirmation of the effectiveness of this substance for pharmacotherapy of calcium antagonists poisoning requires further clinical research. The influence of 4-AP on calcium channels is indirect. It blocks potassium channels K1 in cytoplasm side which makes potassium to stay inside the cell leading to depolarisation and opening of voltage-dependent calcium channels.

  18. Assessment of Mechanisms Involved in Antinociception Produced by the Alkaloid Caulerpine

    Directory of Open Access Journals (Sweden)

    Luiz Henrique Agra Cavalcante-Silva

    2014-09-01

    Full Text Available In previous works we showed that oral administration of caulerpine, a bisindole alkaloid isolated from algae of the genus Caulerpa, produced antinociception when assessed in chemical and thermal models of nociception. In this study, we evaluated the possible mechanism of action of this alkaloid in mice, using the writhing test. The antinociceptive effect of caulerpine was not affected by intraperitoneal (i.p. pretreatment of mice with naloxone, flumazenil, l-arginine or atropine, thus discounting the involvement of the opioid, GABAergic, l-arginine-nitric oxide and (muscarinic cholinergic pathways, respectively. In contrast, i.p. pretreatment with yohimbine, an α2-adrenoceptor antagonist, or tropisetron, a 5-HT3 antagonist, significantly blocked caulerpine-induced antinociception. These results suggest that caulerpine exerts its antinociceptive effect in the writhing test via pathways involving α2-adrenoceptors and 5-HT3 receptors. In summary, this alkaloid could be of interest in the development of new dual-action analgesic drugs.

  19. Acute poisoning due to ingestion of Datura stramonium - a case report.

    Science.gov (United States)

    Trancă, Sebastian Daniel; Szabo, Robert; Cociş, Mihaela

    2017-04-01

    Datura stramonium (DS) is a widespread annual plant, containing atropine, hyoscyamine, and scopolamine, which can produce poisoning with a severe anticholinergic syndrome. Teenagers ingest the roots, seeds or the entire plant to obtain its hallucinogenic and euphoric effects. We presented the case of a 22 year old male who was admitted to the Emergency Room in a coma after consuming Datura stramonium, 2 hours earlier. The patient presented with fever, tachycardia with right bundle branch block, and urinary retention. Rapid sequence induction and intubation was performed immediately, with sedation and assisted-control mechanical ventilation, after being transferred to the Intensive Care Unit. The patient received activated charcoal, in repeated doses, external and internal cooling was applied, and an infusion of neostigmine was started. The biological assessment revealed rhabdomyolysis and prevention of renal failure was initiated. After a proper neurological evaluation, 36 hours after using Datura stramonium, the patient was extubated and transferred to the Psychiatric ward for further assessment and care.

  20. Poisoned after Dinner: Dolma with Datura Stramonium.

    Science.gov (United States)

    Disel, Nezihat Rana; Yilmaz, Mustafa; Kekec, Zeynep; Karanlik, Meryem

    2015-03-01

    Datura stramonium, which is also known as Thorn Apple or Jimson Weed, is an alkaloid containing plant that is entirely toxic. The active toxic constituents of the plant are atropine, scopolamine and hyoscyamine. It has been abused worldwide for hundreds of years because of its hallucinogenic properties. Previous reports have shown that herbal medication overdose and accidental food contamination are ways it can cause poisoning. Herein we present a family that had three of its members poisoned after eating a traditional meal "dolma" made of datura flowers. None had fatal complications and all were discharged healthy. Datura stromonium may be used accidentally as a food ingredient. Since its poisonous effects are not known, people should be informed and warned about the effects of this plant.

  1. Poisoned after Dinner: Dolma with Datura Stramonium

    Directory of Open Access Journals (Sweden)

    Nezihat Rana DISEL

    2015-03-01

    Full Text Available SUMMARY: Datura stramonium, which is also known as Thorn Apple or Jimson Weed, is an alkaloid containing plant that is entirely toxic. The active toxic constituents of the plant are atropine, scopolamine and hyoscyamine. It has been abused worldwide for hundreds of years because of its hallucinogenic properties. Previous reports have shown that herbal medication overdose and accidental food contamination are ways it can cause poisoning. Herein we present a family that had three of its members poisoned after eating a traditional meal “dolma” made of datura flowers. None had fatal complications and all were discharged healthy. Datura stromonium may be used accidentally as a food ingredient. Since its poisonous effects are not known, people should be informed and warned about the effects of this plant. Key words: Anticholinergic effects, Datura stramonium, plant poisoning, rhabdomyolysis

  2. Deep halothane anaesthesia compared with halothane-suxamethonium anaesthesia for tracheal intubation in young children.

    Science.gov (United States)

    Hansen, D; Heitz, E; Toussaint, S; Schaffartzik, W; Striebel, H W

    1997-01-01

    A double-blind and randomized study design was used to investigate 100 healthy children, aged 1-5 years. Intubating conditions and cardiovascular changes during deep halothane anaesthesia, defined as an end-tidal concentration of 2%, were compared with those changes during 1% halothane and suxamethonium relaxation. Intubating conditions were graded according to the ease of laryngoscopy, vocal cord position, coughing and jaw relaxation. In each group 96% of the children demonstrated acceptable intubating conditions. Jaw relaxation was worse in the 1% halothane/-suxamethonium group (P < 0.01). When anaesthesia with 2% or 1% halothane was compared there was a more pronounced decrease in systolic blood pressure (18 vs. 8%, P < 0.001). Junctional rhythm occurred more frequently during deep halothane anaesthesia (46 vs. 18%, P < 0.01). Intravenously (i.v.) administered atropine attenuated blood pressure depression significantly and reinstituted sinus rhythm in most cases.

  3. [Hypothalamic stimulation effects on duodenal motility of rat. IV) Vias hypothalamo-duodenal (author's transl)].

    Science.gov (United States)

    De Vergueiro Forjaz, S

    1975-01-01

    Changes in duodenal motility, induced by electrical stimulation of hypothalamus, have been studied in rats, and registered by the baloon method. Localization of stimulated points was made by stereotaxic method, or by hostological control. Four animals were previously adrenalectomized. In 13 rats, the experiment has been repeated after bilateral cervical vagotomy. In 5 animals after total spinal cord transection, in the first dorsal segment. In 7 rats the experiment was reproduced after venous injections of atropine solution. In 5 rats after venous injections of dibenamine solution, and in other 5, after venous injection of hexamethonium solution. 1) Impulses that produced excitatory duodenal effects were mediated by the vagi nerves. 2) Impulses that produied inhibitory duodenal effects were not transmitted by the vagi nerves, but by sympathetic pathways.

  4. Diastolic and autonomic dysfunction in early cirrhosis

    DEFF Research Database (Denmark)

    Dahl, Emilie Kristine; Møller, Søren; Kjær, Andreas

    2014-01-01

    cirrhosis during maximal β-adrenergic drive. MATERIAL AND METHODS. Nineteen patients with Child A (n = 12) and Child B cirrhosis (n = 7) and seven matched controls were studied during cardiac stress induced by increasing dosages of dobutamine and atropine. RESULTS. Pharmacological responsiveness was similar...... fraction was similar in patients and controls. Peak filling rate was longer in cirrhosis compared to controls (1.8 ± 0.4 and 1.4 ± 0.2 end-diastolic volume/s, p stress by 13% compared to 0% in controls, p ... indicate that patients with early stage cirrhosis exhibit early diastolic and autonomic dysfunction as well as elevated pro-ANP. However, the cardiac chronotropic and inotropic responses to dobutamine stress were normal. The dynamics of ventricular repolarization appears normal in patients with early stage...

  5. Antidepressant-like properties of sildenafil in a genetic rat model of depression: Role of cholinergic cGMP-interactions

    DEFF Research Database (Denmark)

    Liebenberg, Nico; Brink, Christiaan; Brand, Linda

    2008-01-01

    any antidepressant-like effect when administered alone. In the current study, we investigated these findings in a genetic animal model of depression, the Flinders Sensitive Line (FSL) rats. In addition, we evaluated the dose-dependency and onset of action for sildenafil + atropine, as well....... Conclusions: Using a genetic animal model of depression, we have confirmed the antidepressant-like property of sildenafil following “unmasking” by concomitant block of muscarinic receptors. These findings hint at a novel interaction between the cGMP and cholinergic systems in depression, and suggest...... was scored during five minutes swim in the FST. In addition, locomotor activity was evaluated in the Open Field Test 2 hours prior to the FST. Results: Fluoxetine and imipramine separately decreased immobility in FSL rats, comparable to that of FRL control rats, after 14 but not after 7 days. Likewise, when...

  6. Pharmacological actions of tentacle extract of the jellyfish, Acromitus rabanchatu, occurring in the Bay of Bengal.

    Science.gov (United States)

    Ghosh, T K; Gomes, A; Chaudhuri, A K

    1990-01-01

    Tentacle extract of A.rabanchatu, produced a fall of blood pressure in cat, rat and guinea pig. Hypotension produced in cat remained unantagonized by blockers of acetylcholine, histamine and 5-HT. On isolated guinea pig heart, the extract significantly reduced the rate and amplitude of contraction leading to irreversible cardiac arrest. In cats and rats, the respiratory rate and amplitude was decreased significantly and resulted in temporary apnoea. The extract also produced vasoconstriction in perfused rat hindquarter preparation and increased cutaneous capillary permeability. The extract produced contraction in several isolated smooth muscle preparations. Contraction on guinea pig ileum was partly antagonized by atropine and cyproheptadine. On isolated rat phrenic nerve diaphragm and chick biventer cervicis, the extract produced irreversible blockade of the electrical stimulation-induced twitch responses. Haemolytic and myonecrotic activity was exhibited by the extract. LD50 was found to be 7.7 mg/kg (iv, mice).

  7. The left ventricular contractility of the rat heart is modulated by changes in flow and a1-adrenoceptor stimulation

    Directory of Open Access Journals (Sweden)

    P.F. Vassallo

    1998-10-01

    Full Text Available Myocardial contractility depends on several mechanisms such as coronary perfusion pressure (CPP and flow as well as on a1-adrenoceptor stimulation. Both effects occur during the sympathetic stimulation mediated by norepinephrine. Norepinephrine increases force development in the heart and produces vasoconstriction increasing arterial pressure and, in turn, CPP. The contribution of each of these factors to the increase in myocardial performance needs to be clarified. Thus, in the present study we used two protocols: in the first we measured mean arterial pressure, left ventricular pressure and rate of rise of left ventricular pressure development in anesthetized rats (N = 10 submitted to phenylephrine (PE stimulation before and after propranolol plus atropine treatment. These observations showed that in vivo a1-adrenergic stimulation increases left ventricular-developed pressure (Pa1-adrenoceptors and increased flow, increased cardiac performance acting simultaneously and synergistically.

  8. Pharmacodynamic Study of Interaction of Aqueous Leaf Extract of Psidium Guajava Linn. (Myrtaceae) with Receptor Systems Using Isolated Tissue Preparations.

    Science.gov (United States)

    Mahaseth, R K; Kumar, S; Dutta, Shagun; Sehgal, Ratika; Rajora, Preety; Mathur, Rajani

    2015-01-01

    The present study investigates the interaction of aqueous leaf extract of Psidium guajava with muscarinic, serotonergic and adrenergic receptor system using isolated rat ileum, gastric fundus and trachea, respectively. The concentration-dependent contractile response of aqueous leaf extract of Psidium guajava was parallel and rightward of standard agonists, ACh and 5-HT indicating agonistic activity on muscarinic and serotonergic receptor systems. The inhibition of aqueous leaf extract of Psidium guajava mediated contractions in presence of atropine (10(-7) M) and ketanserin (10(-6) M) confirmed the activity. Relaxant effect of PG (0.2 mg/ml) on carbachol induced pre-contracted rat tracheal chain indicated its agonistic action on adrenergic receptor system. Inhibition (P<0.05) of the action in the presence of propranolol (1 ng/ml) confirmed the activity. It may be concluded that PG possesses agonistic action on muscarinic, serotonergic and adrenergic receptor systems.

  9. Determinantes genéticos de las variables psicofisiológicas

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    Kaz Abe

    1972-01-01

    Full Text Available Studies of the genetic influence on varíous physiological functions related to the activity of the autonomic nervous system, on response to drugs and on sleep behaviors were reviewed. Genetic factor appears to play a significant role in; heart beat, electrocardíogramm, heart beat and respiratory response to startling events, or adrenalin or atropin injectíon, in predísposítíon to cardiac neurosis, peripheral vasomotor activity, (acrocyanosis, frost-bite sweat gland activity (hyperidrosis, galvaníc skin reflex, salivarysecretion rate, motion síckness, basal metabolism, blood sugar level, response to antídepressants, drug-induced Parkinsonism, sleepwalking, sleeptalking, childhood insomnia, and major shifts of sleep stages as observed by electroencephalogramm during sleep.

  10. Anesthetic management of a child with Down's syndrome having atlanto axial instability.

    Science.gov (United States)

    Bhattarai, B; Kulkarni, A H; Kalingarayar, S; Upadya, M P

    2009-01-01

    Down's syndrome is the most commonly encountered congenital anomaly in medical practice. These patients are of special concern to medical practice because of their associated problems with regard to respiratory, cardiovascular and other systemic problems. As these patients present for repeated surgeries like dental extraction, facial reconstruction and fixation of cervical spine, these patients pose challenges to the anesthesiologist because of their unique set of problems, namely atlantoaxial instability, small trachea, congenital heart disease and repeated chest infections due to lowered immunity. Their reactivity to inhalational anesthetics and atropine is variable. Here we present an interesting case report of a child with Down's syndrome who presented with atlantoaxial instability for MRI of cervical spine under general anesthesia.

  11. Diverse Presentation of Breath Holding Spells: Two Case Reports with Literature Review

    Science.gov (United States)

    Rathore, Geetanjali; Larsen, Paul; Fernandez, Cristina; Parakh, Manish

    2013-01-01

    Breath holding spells are a common and dramatic form of syncope and anoxic seizure in infancy. They are usually triggered by an emotional stimuli or minor trauma. Based on the color change, they are classified into 3 types, cyanotic, pallid, and mixed. Pallid breath holding spells result from exaggerated, vagally-mediated cardiac inhibition, whereas the more common, cyanotic breathholding spells are of more complex pathogenesis which is not completely understood. A detailed and accurate history is the mainstay of diagnosis. An EKG should be strongly considered to rule out long QT syndrome. Spontaneous resolution of breath-holding spells is usually seen, without any adverse developmental and intellectual sequelae. Rare cases of status epilepticus, prolonged asystole, and sudden death have been reported. Reassurance and education is the mainstay of therapy. Occasionally, pharmacologic intervention with iron, piracetam; atropine may be of benefit. Here we present 2 cases, one of each, pallid and cyanotic breath holding spells. PMID:24191206

  12. An Important Chemical Weapon Group: Nerve Agents

    Directory of Open Access Journals (Sweden)

    Hakan Yaren

    2007-12-01

    Full Text Available As a result of developing modern chemistry, nerve agents, which are one of the most important group of efficient chemical warfare agents, were developed just before Second World War. They generate toxic and clinical effects via inhibiting acetylcholinesterase irreversibly and causing excessive amounts of acetylcholine at cholinergic synapses in the body. Clinical symptoms are occurred as a result of affected muscarinic (stimulation of secretuar glands, miosis, breathing problems etc., nicotinic (stimulation of skeletal muscles, paralyse, tremors etc. and central nerve system (convulsions, loss of consciousness, coma etc. areas. In case of a nerve agent exposure, treatment includes the steps of ventilation, decontamination, antidotal treatment (atropine, oximes, diazepam and pyridostigmine bromide and supportive theraphy. Because of arising possibility of using chemical warfare agents due to current conjuncture of the world, medical staff should know about nerve agents, their effects and how to treat the casualties exposured to nerve agents. [TAF Prev Med Bull. 2007; 6(6: 491-500

  13. Amitraz: a mimicker of organophosphate poisoning.

    Science.gov (United States)

    Dhooria, Sahajal; Behera, Digambar; Agarwal, Ritesh

    2015-10-01

    Amitraz is used as an ectoparasiticide for dogs and cattle. Human poisoning due to amitraz may be misdiagnosed as organophosphate/carbamate (OPC) toxicity, since amitraz poisoning shares several clinical features (miosis, bradycardia and hypotension) encountered with OPC poisoning. A 19-year-old man with an alleged history of suicidal ingestion of a pesticide presented with drowsiness and was found to have constricted pupils, hypotension and bradycardia. He was diagnosed as a case of OPC poisoning and was treated with atropine and pralidoxime prior to presentation to our centre. Absence of a hypersecretory state, and the presence of hyperglycaemia and hypothermia along with a normal serum cholinesterase level suggested an alternate possibility. Retrieval of the poison container confirmed the diagnosis of amitraz poisoning. The patient made a rapid recovery with supportive management. Clinician awareness is key to successful management of this poisoning, which carries a good prognosis. 2015 BMJ Publishing Group Ltd.

  14. An Important Chemical Weapon Group: Nerve Agents

    Directory of Open Access Journals (Sweden)

    Hakan Yaren

    2007-12-01

    Full Text Available As a result of developing modern chemistry, nerve agents, which are one of the most important group of efficient chemical warfare agents, were developed just before Second World War. They generate toxic and clinical effects via inhibiting acetylcholinesterase irreversibly and causing excessive amounts of acetylcholine at cholinergic synapses in the body. Clinical symptoms are occurred as a result of affected muscarinic (stimulation of secretuar glands, miosis, breathing problems etc., nicotinic (stimulation of skeletal muscles, paralyse, tremors etc. and central nerve system (convulsions, loss of consciousness, coma etc. areas. In case of a nerve agent exposure, treatment includes the steps of ventilation, decontamination, antidotal treatment (atropine, oximes, diazepam and pyridostigmine bromide and supportive theraphy. Because of arising possibility of using chemical warfare agents due to current conjuncture of the world, medical staff should know about nerve agents, their effects and how to treat the casualties exposured to nerve agents. [TAF Prev Med Bull 2007; 6(6.000: 491-500

  15. Toxic Anterior Segment Syndrome following a Triple Descemet’s Stripping Automated Endothelial Keratoplasty Procedure

    Directory of Open Access Journals (Sweden)

    Nir Sorkin

    2012-11-01

    Full Text Available Purpose: To present a unique case of a 58-year-old female with toxic anterior segment syndrome (TASS, following a triple procedure: Descemet’s stripping automated endothelial keratoplasty (DSAEK, phacoemulsification and posterior chamber intraocular lens implantation. Methods: The patient was treated with topical dexamethasone sodium phosphate 0.1% and topical atropine sulfate 1%. Due to a slow improvement in her clinical status, oral prednisone 1 mg/kg/day was added. Results: The anterior chamber reaction improved gradually, with tapering down of topical and oral treatment, until a complete resolution of the anterior chamber reaction was observed. Conclusions: Taking into account the estimated volume of DSAEK triple procedures performed worldwide, we would expect an annual incidence of several TASS cases, following triple DSAEK procedures. However, we were unable to find any such previous reports in the literature. This fact raises questions regarding the cause of reduced TASS incidence following triple DSAEK procedures.

  16. Experimental pharmacokinetics and toxicology of acrylonitrile

    Energy Technology Data Exchange (ETDEWEB)

    Peter, H.; Bolt, H.M.

    1984-05-01

    Pharmacokinetic experiments in rats and Rhesus monkeys show that inhaled acrylonitrile is nearly completely retained and metabolized. Metabolism, according to the literature, proceeds via direct reaction of acrylonitrile with biological sulfhydryl compounds and, to a much lesser extent, via glycidonitrile as a DNA-reactive oxidative metabolite. Clinical symptoms of acute acrylonitrile intoxication are in favour of an increased parasympathetic activity. This is confirmed by increased release of acetylcholine, in presence of acrylonitrile, from isolated chicken hearts of which the N. vagus is electrically stimulated. This explains an antidotal effect of atropine. The effectiveness of N-acetyl-cysteine as an acrylonitrile antidote may be explained by decreased alkylation and inactivation of acetylcholine-esterase.

  17. Gallbladder emptying response to sham feeding in humans

    Energy Technology Data Exchange (ETDEWEB)

    Fisher, R.S.; Rock, E.; Malmud, L.S.

    1986-06-01

    Cholescintigraphy, using 99mTc-HIDA, was employed to determine the gallbladder emptying response to sham feeding of a steak and potato meal, and to compare it with the emptying responses to direct cholinergic stimulation by bethanechol and to ingestion of the test meal. The maximal cumulative gallbladder emptying response to sham feeding was 44.1% + 10.1%, which was not significantly different from the response to bethanechol. Cholinergic blockade with atropine eliminated the emptying response to sham feeding. Also, sham feeding did not stimulate gallbladder emptying in patients with vagotomy. This study suggests that intact vagus nerves and cholinergic pathways are required in order for the gallbladder to respond to sham feeding. The precise mechanism for this effect has not been elucidated.

  18. PENGARUH EKSTRAK BEBERAPA TANAMAN OBAT TERHADAP USUS TERISOLASI

    Directory of Open Access Journals (Sweden)

    B. Dzulkarnain

    2012-09-01

    Full Text Available The extraction of Anacardium occidentale L.leaves, Aegle marmelos Corr leaves and wood bark, Acorus calamus L. tuber and Desmodium triquetrum D.C. leaves has been tested on the isolated rabbit and guinea pig intestine. The extraction of A. occidentale L. leaves stimulated the isolated rabbit and guinea pig intestine which may due to the anacardic acid content. No consistent influence was seen by the extraction of A.marmelos Corr. leaves and wood bark. The A. calamus L. tuber extraction decreases the isolated intestine activities which is of the atropine-like type not antihistamin one. This may explain the use as antidysentri agent from the motility point of view. The D. triquetrum D.C. leaves extraction stimulated the isolated intestine which has a pilocarpine and histamine-like activity but does not exclude a seretonine-like action.

  19. Vestibular dysfunction in a child with embryonic exposure to accutane.

    Science.gov (United States)

    Westerman, S T; Gilbert, L M; Schondel, L

    1994-05-01

    Children with a history of embryonic exposure to Accutane (isotretinoin) are at great risk for major physical malformations, brain malformations, and decreased intelligence. A case is presented of a 4-year 7-month-old black male with a history of embryonic exposure to Accutane who was born with embryopathy that includes bilateral major ear deformities. The child has a significant bilateral conductive hearing loss, and, in addition, a left sided sensorineural loss. Vestibular function testing revealed evidence of peripheral and central vestibular dysfunction. A course of diphenhydramine hydrochloride and Donnatal (phenobarbital, hyoscyamine sulfate, atropine sulfate, and scopolamine hydrobromide) significantly alleviated the symptoms of vestibular dysfunction. Otologic management of these children should include clinical documentation of the external deformities, evaluation of cochlear function, and early auditory habilitation. Vestibular function should also be evaluated in all children with a history of embryonic exposure to isotretinoin.

  20. Repeated anaesthesia with isoflurane and medetomidine-midazolam-fentanyl in guinea pigs and its influence on physiological parameters.

    Directory of Open Access Journals (Sweden)

    Sabrina Schmitz

    Full Text Available Repeated anaesthesia may be required in experimental protocols and in daily veterinary practice, but anaesthesia is known to alter physiological parameters in GPs (Cavia porcellus, GPs. This study investigated the effects of repeated anaesthesia with either medetomidine-midazolam-fentanyl (MMF or isoflurane (Iso on physiological parameters in the GP. Twelve GPs were repeatedly administered with MMF or Iso in two anaesthesia sets. One set consisted of six 40-min anaesthesias, performed over 3 weeks (2 per week; the anaesthetic used first was randomized. Prior to Iso anaesthesia, atropine was injected. MMF anaesthesia was antagonized with AFN (atipamezole-flumazenil-naloxone. Abdominally implanted radio-telemetry devices recorded the mean arterial blood pressure (MAP, heart rate (HR and core body temperature continuously. Additionally, respiratory rate, blood glucose and body weight were assessed. An operable state could be achieved and maintained for 40 min in all GPs. During the surgical tolerance with MMF, the GPs showed a large MAP range between the individuals. In the MMF wake- up phase, the time was shortened until the righting reflex (RR returned and that occurred at lower MAP and HR values. Repeated Iso anaesthesia led to an increasing HR during induction (anaesthesias 2-6, non-surgical tolerance (anaesthesias 3-6 and surgical tolerance (anaesthesias 4, 6. Both anaesthetics may be used repeatedly, as repeating the anaesthesias resulted in only slightly different physiological parameters, compared to those seen with single anaesthesias. The regular atropine premedication induced HR increases and repeated MMF anaesthesia resulted in a metabolism increase which led to the faster return of RR. Nevertheless, Iso's anaesthesia effects of strong respiratory depression and severe hypotension remained. Based on this increased anaesthesia risk with Iso, MMF anaesthesia is preferable for repeated use in GPs.

  1. Change in Odor Identification Impairment is Associated with Improvement with Cholinesterase Inhibitor Treatment in Mild Cognitive Impairment.

    Science.gov (United States)

    Devanand, D P; Lentz, Cody; Chunga, Richard E; Ciarleglio, Adam; Scodes, Jennifer M; Andrews, Howard; Schofield, Peter W; Stern, Yaakov; Huey, Edward D; Bell, Karen; Pelton, Gregory H

    2017-01-01

    Anticholinergic challenge can induce odor identification impairment that indicates Alzheimer's disease pathology. To determine if decline in odor identification ability with anticholinergic challenge can predict improvement with donepezil, a cholinesterase inhibitor (ChEI), in patients with mild cognitive impairment (MCI). At baseline, the University of Pennsylvania Smell identification Test (UPSIT) was administered before and after an anticholinergic atropine nasal spray challenge. Donepezil was started at 5 mg daily, increased to 10 mg daily if tolerated, and then the dose was kept constant for 52 weeks. Main outcomes were change in Selective Reminding Test (SRT) total immediate recall and ADAS-Cog total score from baseline to 26 and 52 weeks. In 37 participants, mean age 70.4 (SD 9.8) y, greater atropine-induced decrease in UPSIT score at baseline was associated with greater improvement in SRT total recall score from baseline to 26 and 52 weeks (p < 0.03). This effect remained after adjusting for time, age, education, gender, APOE ɛ4 status, and baseline cognitive score (p < 0.05). Decrease in UPSIT score was associated with global improvement (CIBIC-plus) over 52 weeks (p < 0.02). After excluding patients with congential anosmia, increase in UPSIT score from 0 to 8 weeks showed a trend-level association with improvement on the ADAS-Cog (p = 0.07). Anticholinergic challenge-induced odor identification decline was associated with cognitive improvement, and short-term improvement in odor identification tended to predict longer term cognitive improvement. These simple inexpensive strategies have the potential to improve selection of patients with MCI for ChEI treatment.

  2. Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study

    Science.gov (United States)

    Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

    2017-01-01

    Objectives: The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. Materials and Methods: ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. Results: ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC50) of ACh in the presence of atropine (10−6 M; P < 0.05) and ZAHE (1000 μg/ml; P < 0.01) was significantly higher than EC50of ACh alone. The EC50of 5-HT in the presence of ketanserin (10−5 M; P < 0.01) and ZAHE (1000 μg/ml; P < 0.05) was higher than EC50of 5-HT alone. Similarly, the EC50of histamine in the presence of pheniramine maleate (10−6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC50of histamine alone. Conclusion: From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims. PMID:28458421

  3. Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract ofZanthoxylum alatumseeds on isolated tissue preparations: Anex vivostudy.

    Science.gov (United States)

    Saikia, Beenita; Barua, Chandana Choudhury; Haloi, Prakash; Patowary, Pompy

    2017-01-01

    The aim of this study was to evaluate anticholinergic, antihistaminic, and antiserotonergic activity of the n-hexane extract of the seeds of Zanthoxylum alatum (ZAHE) on isolated ileum of rat and guinea pig and fundus of rat. ZAHE was prepared using soxhlet extraction and cumulative concentration response curves were constructed using various doses on the tissues for acetylcholine (ACh), 5-hydroxytryptamine (5-HT), and histamine with or without n-hexane extract. Atropine, ketanserin, and pheniramine maleate were used as antagonists for ACh, serotonin, and histamine, respectively. ZAHE-induced concentration-dependent inhibition of isolated ileum and fundus in rat and ileum of guinea pig. The half maximal effective concentration (EC 50 ) of ACh in the presence of atropine (10 -6 M; P < 0.05) and ZAHE (1000 μg/ml; P < 0.01) was significantly higher than EC 50 of ACh alone. The EC 50 of 5-HT in the presence of ketanserin (10 -5 M; P < 0.01) and ZAHE (1000 μg/ml; P < 0.05) was higher than EC 50 of 5-HT alone. Similarly, the EC 50 of histamine in the presence of pheniramine maleate (10 -6 M; P < 0.01) and ZAHE (300 μg/ml; P < 0.01 and 1000 μg/ml; P < 0.05) was also significantly higher than EC 50 of histamine alone. From the study, it was observed that ZAHE shows significant anticholinergic, antiserotonergic, and antihistaminic activity. The study provides sufficient evidence that the seeds can be used in gastric disorders, cough, chest infection, etc., as per folklore claims.

  4. A Comprehensive Evaluation of the Efficacy of Leading Oxime Therapies in Guinea Pigs Exposed to Organophosphorus Chemical Warfare Agents or Pesticides

    Science.gov (United States)

    Wilhelm, Christina M.; Snider, Thomas H.; Babin, Michael C.; Jett, David A.; Platoff, Gennady E.; Yeung, David T.

    2014-01-01

    The currently fielded pre-hospital therapeutic regimen for the treatment of organophosphorus (OP) poisoning in the United States (U.S.) is the administration of atropine in combination with an oxime antidote (2-PAM Cl) to reactivate inhibited acetylcholinesterase (AChE). Depending on clinical symptoms, an anticonvulsant, e.g., diazepam, may also be administered. Unfortunately, 2-PAM Cl does not offer sufficient protection across the range of OP threat agents, and there is some question as to whether it is the most effective oxime compound available. The objective of the present study is to identify an oxime antidote, under standardized and comparable conditions, that offers protection at the FDA approved human equivalent dose (HED) of 2-PAM Cl against tabun (GA), sarin (GB), soman (GD), cyclosarin (GF), and VX, and the pesticides paraoxon, chlorpyrifos oxon, and phorate oxon. Male Hartley guinea pigs were subcutaneously challenged with a lethal level of OP and treated at approximately 1 min post challenge with atropine followed by equimolar oxime therapy (2-PAM Cl, HI-6 DMS, obidoxime Cl2, TMB-4, MMB4-DMS, HLö-7 DMS, MINA, and RS194B) or therapeutic-index (TI) level therapy (HI-6 DMS, MMB4-DMS, MINA, and RS194B). Clinical signs of toxicity were observed for 24 hours post challenge and blood cholinesterase [AChE and butyrylcholinesterase (BChE)] activity was analyzed utilizing a modified Ellman’s method. When the oxime is standardized against the HED of 2-PAM Cl for guinea pigs, the evidence from clinical observations, lethality, quality of life (QOL) scores, and cholinesterase reactivation rates across all OPs indicated that MMB4 DMS and HLö-7 DMS were the two most consistently efficacious oximes. PMID:25448441

  5. Presence of cholinomimetic and acetylcholinesterase inhibitory constituents in betel nut.

    Science.gov (United States)

    Gilani, Anwar H; Ghayur, M Nabeel; Saify, Zafar S; Ahmed, Shahida P; Choudhary, M Iqbal; Khalid, Asaad

    2004-10-01

    In this investigation, we report the presence of cholinomimetic and acetylcholinesterase (AChE) inhibitory constituents in betel nut, the most commonly used drug in the world after tobacco, ethanol and caffeine. The crude extract of betel nuts or Areca catechu (Ac.Cr) caused a dose-dependent (0.3-300 microg/mL) spasmogenic effect in the isolated rabbit jejunum. The spasmogenic effect was blocked by atropine, similar to that of acetylcholine (ACh), suggestive of muscarinic receptor mediated effect. Both the extract (0.3-10 microg/mL) and physostigmine (0.1-3.0 microM) potentiated the effect of a fixed dose of ACh (10 microM) in a dose-dependent fashion, suggesting acetylcholinesterase (AChE) inhibitory effect. This effect was confirmed in the in vitro assay where both the crude extract (1-100 microg/mL) and physostigmine inhibited the enzyme. In the in vivo model of gastrointestinal transit, Ac.Cr (10-30 mg/kg) enhanced the travel of charcoal meal and also exhibited a laxative effect in mice. The plant extract was subjected to activity-directed fractionation and all resultant fractions showed atropine-sensitive spasmogenicity in rabbit jejunum and also AChE inhibitory effect at doses similar to that for the parent crude extract, the ethyl acetate fraction being slightly less potent. Some of the known constituents of betel nut, including arecoline, were tested for the possible inhibitory effect on AChE, none were found active. The study provides first evidence for the presence of AChE inhibitory constituents in betel nut, though additional direct muscarinic stimulatory effect cannot be ruled out and this study provides sound scientific basis for some of the folkloric uses associated with betel nut chewing.

  6. Effect of Agonist and Antagonist on the In Vitro Contractility of Inflamed Vermiform Appendix

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    Singh, Phani Bhushan; Tiwary, Pushpakant; Singh, Sanjeev K; Pandey, Ratna; Roy, Atanu; Kar, Amrita Ghosh; Basu, Somprakas

    2017-01-01

    Introduction Appendicitis poses a great health problem worldwide. Previous studies demonstrated structural damage to neuronal network and interstitial cell of Cajal in appendicitis. Above observations suggest for the alterations in appendicular motility/contractility in appendicitis. But the mechanisms involved in mediating the contractility in inflamed vermiform appendix is not known till date. Aim The present in vitro study was performed to find out the mechanisms responsible for contractility in the inflamed human vermiform appendix. Materials and Methods Contractions of the longitudinal muscle strips of inflamed appendix were recorded in vitro at 37±0.5°C. Control contractions were recorded for 30 min after an initial tension of 0.5 gram. Initially dose-response experiments of agonists (acetylcholine, serotonin and histamine) were performed separately and the dose that produced maximum contraction was determined with each agonist. This maximal dose of agonist was used to elicit contractions in next series of experiments before and after pre-treatment with appropriate antagonists like atropine, ondansetron (5-HT3 antagonist) and chlorpheniramine maleate respectively. Results Acetylcholine (ACh) and serotonin (5-HT) elicited maximum amplitude of contraction at 10 µM and 1 µM concentration respectively. These contractions were significantly blocked by prior exposure of muscle strips with atropine (100 µM) and ondansetron (10 µM). Histamine produced very low amplitude of contractions in comparison to ACh or 5-HT and did not exhibit dose-response relations. The histamine induced contractions were blocked by H1 antagonist chlorpheniramine maleate (100 µM). Conclusion The observations suggested that the contractility of longitudinal muscle strips of inflamed vermiform appendix in human beings was predominantly mediated by muscarinic and serotonergic (5-HT3) mechanisms, whereas, histaminergic mechanisms played a minor role in mediating the contractility. PMID

  7. The involvement of the central cholinergic system in the pressor and bradycardic effects of centrally administrated melittin in normotensive conscious rats.

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    Yalcin, Murat; Erturk, Melih

    2007-04-01

    Recently we demonstrated that centrally administrated melittin, a phospholipase A(2) (PLA(2)) activator, caused pressor and bradycardic effect in the normotensive conscious rats. In the current study we aimed to determine the mediation of central cholinergic system in the pressor and bradycardic effect of centrally administrated melittin. Studies were performed in normotensive male Sprague-Dawley rats. 1.5, 3.0 or 6.0microg/5.0microl doses of melittin were injected intracerebroventricularly (i.c.v.). Melittin caused dose- and time-dependent increases in mean arterial pressure (MAP) and decrease in heart rate (HR). In order to test the mediation of central cholinergic system on the pressor and bradycardic effect of melittin, the rats were pretreated with mecamylamine (50microg; i.c.v.), cholinergic nonselective nicotinic receptor antagonist, atropine sulfate (10microg; i.c.v.), a cholinergic nonselective muscarinic receptor antagonist, hemicholinium-3 (20microg; i.c.v.), a high affinity neuronal choline uptake inhibitor, methyllycaconitine (10 and 25microg; i.c.v.) or alpha-bungarotoxin (10 and 25microg; i.c.v.), selective antagonists of alpha-7 subtype nicotinic acetylcholine receptors (alpha7nAChRs), 15min prior to melittin (3.0microg) injection. Pretreatment with mecamylamine, hemicholinium-3, methyllycaconitine or alpha-bungarotoxin partially attenuated the pressor and bradicardia effect of elicited by melittin in the normotensive conscious rats whereas pretreatment with atropine had no effect. In conclusion, i.c.v. administration of melittin increases MAP and decreases HR in conscious rats. The activation of central nicotinic cholinergic receptors, predominantly alpha7nAChRs, partially acts as a mediator in the pressor responses to i.c.v. injection of melittin in the normotensive conscious rats. Moreover, decreased uptake of choline to the cholinergic terminals may consider that melittin activates central choline and acetylcholine release, as well.

  8. Pharmacological basis for medicinal use of Lens culinaris in gastrointestinal and respiratory disorders.

    Science.gov (United States)

    Khan, Munasib; Khan, Arif-ullah; Najeeb-ur-Rehman; Gilani, Anwarul-Hassan

    2014-09-01

    Crude extract of Lens culinaris (Lc.Cr), which tested positive for presence of anthraquinones, flavonoids, saponins, sterol, tannins, and terpenes exhibited protective effect against castor oil-induced diarrhea in mice at 100-1000 mg/kg. In rabbit jejunum preparations, Lc.Cr caused relaxation of spontaneous contractions at 0.03-5.0 mg/mL. Lc.Cr inhibited carbachol (CCh, 1 μM) and K(+) (80 mM)-induced contractions in a pattern similar to dicyclomine, but different from verapamil and atropine. Lc.Cr shifted the Ca(++) concentration-response curves to the right, like dicyclomine and verapamil. Pretreatment of tissues with Lc.Cr (0.03-0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In guinea-pig ileum, Lc.Cr produced rightward parallel shift of CCh curves, followed by non-parallel shift at higher concentration with suppression of maximum response, similar to dicyclomine, but different from verapamil and atropine. Lc.Cr (3.0-30 mg/kg) caused suppression of carbachol (CCh, 100 µg/kg)-induced increase in inspiratory pressure of anesthetized rats. In guinea-pig trachea, Lc.Cr relaxed CCh and high K(+) -induced contractions, shifted CCh curves to right and potentiated isoprenaline response. These results suggest that L. culinaris possesses antidiarrheal, antispasmodic, and bronchodilator activities mediated possibly through a combination of Ca(++) antagonist, anticholinergic, and phosphodiesterase inhibitory effects, and this study provides sound mechanistic background to its medicinal use in disorders of gut and airways hyperactivity, like diarrhea and asthma. Copyright © 2014 John Wiley & Sons, Ltd.

  9. Amblyopia Treatment Knowledge Cognition of Iranian Practitioners in 2012.

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    Zhale Rajavi

    2015-02-01

    Full Text Available Background: Amblyopia is considered as one of the most prevalent vision problems in pediatrics age (1-5%. Recently, new methods in amblyopia treatment were reported in Amblyopia Treatment Study (ATS’.The objective of this study was to recognize amblyopia treatment knowledge of Iranian ophthalmologists and optometrists which are responsible for amblyopia treatment in our and other countries.Materials and Methods: This cross sectional study was performed during the Iranian Society of Ophthalmology annual meeting in Tehran in 2012 through questionnaire containing demographic information and 20 closed-answer questions based on ATS results. The questions were classified into seven categories and the sum of correct scores was 100. Optometrists and pediatric ophthalmologists were considered as the group 1 (153 participants, other practitioners (general ophthalmologists and other subspecialists were regarded as the group 2 (256 participants. Criteria for inadequate, fair and good knowledge were considered by scores of < 50, 50 to 70, and >70 respectively.Results: Overall, 409 out of a total of 600 questionnaires were completed (response rate: 68.1%.  Mean scores of the group 1 were significantly higher than the group 2 in all 7 categories of questions and in 5 of them the differences were statistically significant. The worst and best scores were related to prescription of atropine (12% and visual acuity improvement with glasses alone (93%, respectively. Scores for other questions were about 50%. There was no relationship between practice status and the number of referral amblyopic cases per week with the level of knowledge. In all categories except prescription of Atropine and recurrence, mean scores of females were more than the male participants.Conclusion: knowledge about amblyopia therapy seems to be overall inadequate and should be improved by more education. We suggest paying more attention to new modified methods of amblyopia treatment and

  10. Utility of prehospital electrocardiogram characteristics as prognostic markers in out-of-hospital pulseless electrical activity arrests.

    Science.gov (United States)

    Ho, Michael L; Gatien, Mathieu; Vaillancourt, Christian; Whitham, Veronica; Stiell, Ian G

    2017-10-21

    It is unclear if there are predictors of survival, including ECG characteristics, that can guide resuscitative efforts in pulseless electrical activity (PEA) cardiac arrests. We studied the predictive potential of presenting prehospital ECGs on survival for patients with out-of-hospital cardiac arrest (OHCA) with PEA. We studied prehospital ECGs of patients with OHCA prospectively enrolled between June 2007 and November 2009 at the Ottawa/OPALS (Ontario Prehospital Advanced Life Support Study) site of the Resuscitation Outcomes Consortium PRIMED study (Prehospital Resuscitation using an IMpedance valve and Early versus Delayed analysis). We included adult non-traumatic OHCA with PEA rhythm where resuscitation was attempted. We measured HR, QRS interval and presence of P waves, and determined their impact on return of spontaneous circulation (ROSC) and survival to hospital discharge (SHD) using multivariate regression analysis. The demographic characteristics of the 332 included cases were the following: mean age 71.8, male 58.4%, SHD 5.4% and ROSC at ED arrival 26.5%. Survivors had similar HR (56.8 vs 52.0 beats per minute (bpm), p=0.53) and QRS intervals (128.7 vs 129.6 ms, p=0.95) compared with non-survivors. Prehospital ECG characteristics did not predict SHD or ROSC on multivariate analyses. Patients with initial HR prehospital ECG characteristics did not predict SHD or ROSC in OHCA PEA victims and should not be used to guide termination of resuscitation. Location of arrest was a positive predictor for SHD; atropine use was a negative predictor. ALS paramedic on scene and successful intubation were positive predictors of ROSC; atropine use was a negative predictor. NCT00394706; post-results. © Article author(s) (or their employer(s) unless otherwise stated in the text of the article) 2017. All rights reserved. No commercial use is permitted unless otherwise expressly granted.

  11. Evaluation of the cholinomimetic actions of trimethylsulfonium, a compound present in the midgut gland of the sea hare Aplysia brasiliana (Gastropoda, Opisthobranchia

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    C.M. Kerchove

    2002-04-01

    Full Text Available Trimethylsulfonium, a compound present in the midgut gland of the sea hare Aplysia brasiliana, negatively modulates vagal response, indicating a probable ability to inhibit cholinergic responses. In the present study, the pharmacological profile of trimethylsulfonium was characterized on muscarinic and nicotinic acetylcholine receptors. In rat jejunum the contractile response induced by trimethylsulfonium (pD2 = 2.46 ± 0.12 and maximal response = 2.14 ± 0.32 g was not antagonized competitively by atropine. The maximal response (Emax to trimethylsulfonium was diminished in the presence of increasing doses of atropine (P<0.05, suggesting that trimethylsulfonium-induced contraction was not related to muscarinic stimulation, but might be caused by acetylcholine release due to presynaptic stimulation. Trimethylsulfonium displaced [³H]-quinuclidinyl benzilate from rat cortex membranes with a low affinity (Ki = 0.5 mM. Furthermore, it caused contraction of frog rectus abdominis muscles (pD2 = 2.70 ± 0.06 and Emax = 4.16 ± 0.9 g, which was competitively antagonized by d-tubocurarine (1, 3 or 10 µM with a pA2 of 5.79, suggesting a positive interaction with nicotinic receptors. In fact, trimethylsulfonium displaced [³H]-nicotine from rat diaphragm muscle membranes with a Ki of 27.1 µM. These results suggest that trimethylsulfonium acts as an agonist on nicotinic receptors, and thus contracts frog skeletal rectus abdominis muscle and rat jejunum smooth muscle via stimulation of postjunctional and neuronal prejunctional nicotinic cholinoreceptors, respectively.

  12. Pulmonary function, cholinergic bronchomotor tone, and cardiac autonomic abnormalities in type 2 diabetic patients

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    E. Melo

    2003-03-01

    Full Text Available This prospective study analyzed the involvement of the autonomic nervous system in pulmonary and cardiac function by evaluating cardiovascular reflex and its correlation with pulmonary function abnormalities of type 2 diabetic patients. Diabetic patients (N = 17 and healthy subjects (N = 17 were evaluated by 1 pulmonary function tests including spirometry, He-dilution method, N2 washout test, and specific airway conductance (SGaw determined by plethysmography before and after aerosol administration of atropine sulfate, and 2 autonomic cardiovascular activity by the passive tilting test and the magnitude of respiratory sinus arrhythmia (RSA. Basal heart rate was higher in the diabetic group (87.8 ± 11.2 bpm; mean ± SD than in the control group (72.9 ± 7.8 bpm, P<0.05. The increase of heart rate at 5 s of tilting was 11.8 ± 6.5 bpm in diabetic patients and 17.6 ± 6.2 bpm in the control group (P<0.05. Systemic arterial pressure and RSA analysis did not reveal significant differences between groups. Diabetes intragroup analysis revealed two behaviors: 10 patients with close to normal findings and 7 with significant abnormalities in terms of RSA, with the latter subgroup presenting one or more abnormalities in other tests and clear evidence of cardiovascular autonomic dysfunction. End-expiratory flows were significantly lower in diabetic patients than in the control group (P<0.05. Pulmonary function tests before and after atropine administration demonstrated comparable responses by both groups. Type 2 diabetic patients have cardiac autonomic dysfunction that is not associated with bronchomotor tone alterations, probably reflecting a less severe impairment than that of type 1 diabetes mellitus. Yet, a reduction of end-expiratory flow was detected.

  13. Urinary elimination kinetics of acephate and its metabolite, methamidophos, in urine after acute ingestion.

    Science.gov (United States)

    Chang, Arthur; Montesano, M Angela; Barr, Dana; Thomas, Jerry; Geller, Robert

    2009-06-01

    Acephate (AP) is a widely available organophosphorus (OP) insecticide considered to have low mammalian toxicity. In plants and insects, AP is metabolized extensively to methamidophos (MP), a more potent OP insecticide. The limited mammalian metabolism of AP to MP has been studied in laboratory rat models and suggests that initial formation of MP from AP may inhibit further formation. No case reports of human ingestion with urine AP and MP levels have been previously published. A 4-year-old male being evaluated for altered mental status and head trauma was noted to have muscarinic and nicotinic cholinergic signs. Further history suggested possible ingestion of a commercial AP product at an unknown time. Ingestion of AP was confirmed by the presence of urinary AP and MP and severely depressed red blood cell (RBC) cholinesterase and pseudocholinesterase activity levels. The patient initially received atropine in two 0.02 mg/kg IV boluses, then was started on 0.05 mg/kg IV per hour and titrated accordingly to clinical signs of cholinergic toxicity. Pralidoxime was also given at 20 mg/kg IV bolus, followed by an infusion of 10 mg/kg per hour. The patient required mechanical ventilation for 18 days and atropine infusion for 20 days. After a complicated intensive care unit course, he recovered and was discharged after a total of 32 days of hospitalization. Four urine samples collected at different times were analyzed for AP and MP by using high-performance liquid chromatography-atmospheric pressure chemical ionization tandem mass spectrometry. Kinetic calculations were performed by using standard equations. Suspected ingestion was confirmed by the presence of AP and MP in urine. The amount of MP found in urine suggests some limited human metabolism to this more toxic compound. Urinary elimination kinetics of AP demonstrates low metabolic conversion of AP to MP in humans.

  14. Recent Advances in the Treatment of Organophosphorous Poisonings

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    Mahdi Balali-Mood

    2012-06-01

    Full Text Available Organophosphorous compounds have been employed as pesticides and chemical warfare nerve agents. Toxicity of organophosphorous compounds is a result of excessive cholinergic stimulation through inhibition of acetyl cholinesterase. Clinical manifestations include cholinergic syndromes, central nervous system and cardiovascular disorders. Organophosphorous pesticide poisonings are common in developing worlds including Iran and Sri Lanka. Nerve agents were used during the Iraq-Iran war in 1983-1988 and in a terrorist attack in Japan in 1994-1995. Following decontamination, depending on the severity of intoxication the administration of atropine to counteract muscarinic over-stimulation, and an oxime to reactivate acetyl cholinesterase are indicated. Supportive and intensive care therapy including diazepam to control convulsions and mechanical respiration may be required. Recent investigations have revealed that intravenous infusion of sodium bicarbonate to produce mild to moderate alkalinization is effective. Gacyclidine; an antiglutamatergic compound, was also proved to be beneficial in conjunction with atropine, pralidoxime, and diazepam in nerve agent poisoning. Intravenous magnesium sulfate decreased hospitalization duration and improved outcomes in patients with organophosphorous poisoning. Bio-scavengers including fresh frozen plasma or albumin have recently been suggested as a useful therapy through clearing of free organophosphates. Hemofiltration and antioxidants are also suggested for organophosphorous poisoning. Recombinant bacterial phosphotriesterases and hydrolases that are able to transfer organophosphorous-degrading enzymes are very promising in delayed treatment of organophosphorous poisoning. Recently, encapsulation of drugs or enzymes in nanocarriers has also been proposed. Given the signs and symptoms of organophosphorous poisoning, health professionals should remain updated about the recent advances in treatment of

  15. The influence of midazolam on heart rate arises from cardiac autonomic tones alterations in Burmese pythons, Python molurus.

    Science.gov (United States)

    Lopes, Ivã Guidini; Armelin, Vinicius Araújo; Braga, Victor Hugo da Silva; Florindo, Luiz Henrique

    2017-12-01

    The GABA A receptor agonist midazolam is a compound widely used as a tranquilizer and sedative in mammals and reptiles. It is already known that this benzodiazepine produces small to intermediate heart rate (HR) alterations in mammals, however, its influence on reptiles' HR remains unexplored. Thus, the present study sought to verify the effects of midazolam on HR and cardiac modulation in the snake Python molurus. To do so, the snakes' HR, cardiac autonomic tones, and HR variability were evaluated during four different experimental stages. The first stage consisted on the data acquisition of animals under untreated conditions, in which were then administered atropine (2.5mgkg -1 ; intraperitoneal), followed later by propranolol (3.5mgkg -1 ; intraperitoneal) (cardiac double autonomic blockade). The second stage focused on the data acquisition of animals under midazolam effect (1.0mgkg -1 ; intramuscular), which passed through the same autonomic blockade protocol of the first stage. The third and fourth stages consisted of the same protocol of stages one and two, respectively, with the exception that atropine and propranolol injections were reversed. By comparing the HR of animals that received midazolam (second and fourth stages) with those that did not (first and third stages), it could be observed that this benzodiazepine reduced the snakes' HR by ~60%. The calculated autonomic tones showed that such cardiac depression was elicited by an ~80% decrease in cardiac adrenergic tone and an ~620% increase in cardiac cholinergic tone - a finding that was further supported by the results of HR variability analysis. Copyright © 2017 Elsevier B.V. All rights reserved.

  16. Autonomic cardiovascular control in methyl-CpG-binding protein 2 (Mecp2) deficient mice.

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    Bissonnette, John M; Knopp, Sharon J; Maylie, James; Thong, Tran

    2007-10-30

    Methyl-CpG-binding protein 2 is a transcription factor that is involved in gene silencing. It is mutated in the majority of cases of Rett syndrome. This X-linked neurodevelopmental disorder is reported to involve abnormalities in autonomic cardiovascular regulation. As an initial step in understanding the basis for these abnormalities we have characterized autonomic cardiovascular function in Mecp2 deficient mice. Arterial pressure waves were recorded in freely moving animals using telemetry. Baseline blood pressure and pulse interval (PI) as well as indices of heart rate variability (HRV): standard deviation of PI (SDNN), range encompassing 90% of PIs (PI90) and standard deviation of adjacent PIs (SDSD) were similar in Mecp2(+/+) and Mecp2(+/-) animals. Spectral analysis of mean arterial pressure (MAP) and PI in the frequency domain showed similar relative power in low frequency 1 (LF1, 08-0.4 Hz), low frequency 2 (LF2, 0.4-1.0 Hz), middle frequency (MF, 1-3 Hz) and high frequency (HF, 3.0-10.0 Hz) bands. Autonomic blockade with atropine or propranolol as well as elevation in ambient temperature to 32 degrees C resulted in changes in blood pressure, PI and HRV that did not differ between the strains. Atropine, propranolol and elevated temperature resulted in similar changes in both MAP and PI spectral power. Baroreceptor function was tested using intravenous injections of nitroprusside followed by phenylephrine. Maximum gain was not different. These results do reveal any disturbance of autonomic cardiovascular regulation in the Mecp2 deficient mouse genotype.

  17. Acetylcholine Attenuates Hypoxia/ Reoxygenation-Induced Mitochondrial and Cytosolic ROS Formation in H9c2 Cells via M2 Acetylcholine Receptor

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    Yi Miao

    2013-02-01

    Full Text Available Background: The anti-infammatory and cardioprotective effect of acetylcholine (ACh has been reported; nevertheless, whether and how ACh exhibits an antioxidant property against ischemia/reperfusion (I/R-induced oxidative stress remains obscure. Methods: In the present study, H9c2 rat cardiomyocytes were exposed to hypoxia/reoxygenation (H/R to mimic I/R injury. We estimated intracellular different sources of reactive oxygen species (ROS by measuring mitochondrial ROS (mtROS, mitochondrial DNA (mtDNA copy number, xanthine oxidase (XO and NADPH oxidase (NOX activity and expression of rac 1. Cell injury was determined by lactate dehydrogenase (LDH release and cleaved caspase-3 expression. The siRNA transfection was performed to knockdown of M2 acetylcholine receptor (M2 AChR expression. Results: 12-h hypoxia followed by 2-h reoxygenation resulted in an abrupt burst of ROS in H9c2 cells. Administration of ACh reduced the levels of ROS in a concentration-dependent manner. Compared to the H/R group, ACh decreased mtROS, recovered mtDNA copy number, diminished XO and NOX activity, rac 1 expression as well as cell injury. Co- treatment with atropine rather than hexamethonium abolished the antioxidant and cardioprotective effect of ACh. Moreover, knockdown of M2 AChR by siRNA showed the similar trends as atropine co-treatment group. Conclusions: ACh inhibits mitochondria-, XO- and NOX-derived ROS production thus protecting H9c2 cells against H/R-induced oxidative stress, and these benefcial effects are mainly mediated by M2 AChR. Our findings suggested that increasing ACh release could be a potential therapeutic strategy for treatment and prevention of I/R injury.

  18. Evaluation the effect of hydro-alcoholic extract of GlycyrrhizaGlabra rhizome on the isolated colon contractions of male rats

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    N Ghayedi

    2016-10-01

    Full Text Available Introduction:The licorice (Glycyrrhizaglabra rhizome has been widely used in traditional medicine for treatment of gastrointestinal diseases such as gastric ulcer and relieve intestinal spasms. In the present study, the effect of hydro-alcoholic extract of licoricerhizome on mechanical activity of isolated colon of male rats has been studied. Methods: Adult male rats were anesthetized by ethyl ether, their abdomen opened, and colon tissues were removed and divided into 1 cm segments. The segments were connected to a force transducer longitudinally and inserted to an organ bathe contained oxygenated Tyrode solution (37 °C, pH=7.4. Their mechanical activity of ileum was recorded by power lab AD instrument in basal condition, and after administration of L-NAME (10-4M, acetylcholine (4×10-5M and Atropine (10-5M drugs in the presence and absence of licorice rhizome extract were recorded (0.036mg/ml. Also, the mechanical activity of control group segments were recorded at the same condition with extract solvent (ethanol %70. Results: A significant decrease in mechanical activity of the isolated colon occurred after administration of hydro-alcoholic extract of licorice rhizome compared to the control group (p≤0.05. Also, a significant decrease was seen in mechanical activity occurredin the co-administration of extract and acetylcholine compared to the control group. The mechanical activity of tissue was not significantly changed in the presence of Atropine and extract between experimental and control groups. The mechanical activity of ileum tissue was not significantly changed in the co-administration of L-NAME and extract between experimental and control groups. Conclusion: We can conclude that hydro-alcoholic extract of licorice has modifying effect on colon motility, and this activity may be occurred independently in the nitrergic and cholinergic systems.

  19. Modulating activity of M1 receptor to the reaction of ileal smooth muscle

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    Izabela Glaza

    2011-08-01

    Full Text Available Background:The subject of the study was determination of the effect of drugs on ileal smooth muscle contraction induced by activation of M1 type muscarinic receptors. Drugs that have an effect on muscarinic receptors are divided to agonists, with close ties to the receptor and high internal activity and antagonists, with no internal activity. Conducted experiments tested interactions between a broad-spectrum agonist of muscarinic receptors, carbachol and a selective muscarinic receptor antagonist of M1 type, pirenzepine.Material/Methods:Testing was conducted on tissues isolated from rat’s intestine. Male Wistar rats with weight between 220 g and 360 g were anesthetized by intraperitoneal injection of urethane (120 mg/kg. Concentration-effect curves were determined with the use of cumulated concentration method, in accordance with the van Rossum method (1963 in Kenakin modification (2006.Results:The purpose of the study was determination of concentration-effect curves for carbachol. This curve was compared with the curve of receptor occupation depending on concentration of this drug. Based on concentration-effect curves, the average value of EC50 was calculated for carbachol, amounting to 2.44×10–6 [M/l].Conclusions:The results confirmed that atropine is effective in stopping contractions caused by carbachol, meeting the conditions of competitive antagonists. Atropine caused the shift of curves for carbachol to the right. Pirenzepine, selectively blocking muscarinic receptors of M1 type gave similar results. It was proved that in the preparation of gastric fundus smooth muscle, M1 type receptors occur not only presynaptically, but also postsynaptically.

  20. Cardiovascular effects of the intracerebroventricular injection of adrenomedullin: roles of the peripheral vasopressin and central cholinergic systems

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    B. Cam-Etoz

    2012-03-01

    Full Text Available Our objective was to investigate in conscious Sprague-Dawley (6-8 weeks, 250-300 g female rats (N = 7 in each group the effects of intracerebroventricularly (icv injected adrenomedullin (ADM on blood pressure and heart rate (HR, and to determine if ADM and calcitonin gene-related peptide (CGRP receptors, peripheral V1 receptors or the central cholinergic system play roles in these cardiovascular effects. Blood pressure and HR were observed before and for 30 min following drug injections. The following results were obtained: 1 icv ADM (750 ng/10 µL caused an increase in both blood pressure and HR (DMAP = 11.8 ± 2.3 mmHg and ΔHR = 39.7 ± 4.8 bpm. 2 Pretreatment with a CGRP receptor antagonist (CGRP8-37 and ADM receptor antagonist (ADM22-52 blocked the effect of central ADM on blood pressure and HR. 3 The nicotinic receptor antagonist mecamylamine (25 µg/10 µL, icv and the muscarinic receptor antagonist atropine (5 µg/10 µL, icv prevented the stimulating effect of ADM on blood pressure. The effect of ADM on HR was blocked only by atropine (5 µg/10 µL, icv. 4 The V1 receptor antagonist [β-mercapto-β-β-cyclopentamethylenepropionyl¹, O-me-Tyr²,Arg8]-vasopressin (V2255; 10 µg/kg, that was applied intravenously, prevented the effect of ADM on blood pressure and HR. This is the first study reporting the role of specific ADM and CGRP receptors, especially the role of nicotinic and muscarinic central cholinergic receptors and the role of peripheral V1 receptors in the increasing effects of icv ADM on blood pressure and HR.

  1. Cardiovascular effects of the intracerebroventricular injection of adrenomedullin: roles of the peripheral vasopressin and central cholinergic systems

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    Cam-Etoz, B.; Isbil-Buyukcoskun, N.; Ozluk, K. [Department of Physiology, Uludag University Medical Faculty, Gorukle/Bursa (Turkey)

    2012-03-02

    Our objective was to investigate in conscious Sprague-Dawley (6-8 weeks, 250-300 g) female rats (N = 7 in each group) the effects of intracerebroventricularly (icv) injected adrenomedullin (ADM) on blood pressure and heart rate (HR), and to determine if ADM and calcitonin gene-related peptide (CGRP) receptors, peripheral V{sub 1} receptors or the central cholinergic system play roles in these cardiovascular effects. Blood pressure and HR were observed before and for 30 min following drug injections. The following results were obtained: 1) icv ADM (750 ng/10 µL) caused an increase in both blood pressure and HR (ΔMAP = 11.8 ± 2.3 mmHg and ΔHR = 39.7 ± 4.8 bpm). 2) Pretreatment with a CGRP receptor antagonist (CGRP{sub 8-37}) and ADM receptor antagonist (ADM{sub 22-52}) blocked the effect of central ADM on blood pressure and HR. 3) The nicotinic receptor antagonist mecamylamine (25 µg/10 µL, icv) and the muscarinic receptor antagonist atropine (5 µg/10 µL, icv) prevented the stimulating effect of ADM on blood pressure. The effect of ADM on HR was blocked only by atropine (5 µg/10 µL, icv). 4) The V{sub 1} receptor antagonist [β-mercapto-β-β-cyclopentamethylenepropionyl{sup 1}, O-me-Tyr{sup 2},Arg{sup 8}]-vasopressin (V2255; 10 µg/kg), that was applied intravenously, prevented the effect of ADM on blood pressure and HR. This is the first study reporting the role of specific ADM and CGRP receptors, especially the role of nicotinic and muscarinic central cholinergic receptors and the role of peripheral V{sub 1} receptors in the increasing effects of icv ADM on blood pressure and HR.

  2. Pharmacological basis for the medicinal use of black pepper and piperine in gastrointestinal disorders.

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    Mehmood, Malik Hassan; Gilani, Anwarul Hassan

    2010-10-01

    Dried fruits of Piper nigrum (black pepper) are commonly used in gastrointestinal disorders. The aim of this study was to rationalize the medicinal use of pepper and its principal alkaloid, piperine, in constipation and diarrhea using in vitro and in vivo assays. When tested in isolated guinea pig ileum, the crude extract of pepper (Pn.Cr) (1–10 mg/mL) and piperine (3–300 μM) caused a concentration-dependent and atropine-sensitive stimulant effect. In rabbit jejunum, Pn.Cr (0.01–3.0 mg/mL) and piperine (30–1,000 μM) relaxed spontaneous contractions, similar to loperamide and nifedipine. The relaxant effect of Pn.Cr and piperine was partially inhibited in the presence of naloxone (1 μM) similar to that of loperamide, suggesting the naloxone-sensitive effect in addition to the Ca(2+) channel blocking (CCB)-like activity, which was evident by its relaxant effect on K+ (80 mM)-induced contractions. The CCB activity was confirmed when pretreatment of the tissue with Pn.Cr (0.03–0.3 mg/mL) or piperine (10–100 μM) caused a rightward shift in the concentration–response curves of Ca(2+), similar to loperamide and nifedipine. In mice, Pn.Cr and piperine exhibited a partially atropine-sensitive laxative effect at lower doses, whereas at higher doses it caused antisecretory and antidiarrheal activities that were partially inhibited in mice pretreated with naloxone (1.5 mg/kg), similar to loperamide. This study illustrates the presence of spasmodic (cholinergic) and antispasmodic (opioid agonist and Ca(2+) antagonist) effects, thus providing the possible explanation for the medicinal use of pepper and piperine in gastrointestinal motility disorders.

  3. Intragastric Dai-Kenchu-To, a Japanese herbal medicine, stimulates colonic motility via transient receptor potential cation channel subfamily V member 1 in dogs.

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    Kikuchi, Daisuke; Shibata, Chikashi; Imoto, Hirofumi; Naitoh, Takeshi; Miura, Koh; Unno, Michiaki

    2013-08-01

    Japanese herbal medicine, also known as Kampo, is used for various diseases in Japan. One of those medicines, Dai-Kenchu-To (DKT), is considered clinically effective for adhesive bowel obstruction and chronic constipation. Although scientific evidence of DKT to improve adhesive bowel obstruction was shown in several previous reports, mechanism of DKT to improve constipation remains unknown. Our aim was to study the effect of intragastric DKT on colonic motility and defecation, and the involvement of various receptors in DKT-induced colonic contractions. Five beagle dogs were instructed with serosal strain-gauge force transducers to measure circular muscle activity at the proximal, middle, and distal colon. Dogs are suitable for a present study to administer the drugs repeatedly to the same individual and look at its effect on colonic motility. We studied the effects of DKT (2.5 or 5 g) administered into the stomach on colonic motility. Muscarinic receptor antagonist atropine, nicotinic receptor antagonist hexamthonium, or 5-hydroxytryptamine-3 receptor antagonist ondansetron was injected intravenously 10 min before DKT administration. Capsazepine, an antagonist to transient receptor potential cation channel subfamily V member 1 (TRPV1), was administered into the stomach 5 min before DKT administration. Intragastric DKT (2.5 or 5 g) induced colonic contractions within 10 min after administration but did not induce defecation. Pretreatment with atropine, hexamthonium, ondansetron, or capsazepine inhibited DKT-induced colonic contractions. These results indicate that orally administered DKT stimulates colonic motility via TRPV1, muscarinic, nicotinic, and 5-hydroxytryptamine-3 receptors, thereby providing scientific support for the efficacy of oral DKT in chronic constipation.

  4. Advances in toxicology and medical treatment of chemical warfare nerve agents.

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    Moshiri, Mohammd; Darchini-Maragheh, Emadodin; Balali-Mood, Mahdi

    2012-11-28

    Organophosphorous (OP) Nerve agents (NAs) are known as the deadliest chemical warfare agents. They are divided into two classes of G and V agents. Most of them are liquid at room temperature. NAs chemical structures and mechanisms of actions are similar to OP pesticides, but their toxicities are higher than these compounds. The main mechanism of action is irreversible inhibition of Acetyl Choline Esterase (AChE) resulting in accumulation of toxic levels of acetylcholine (ACh) at the synaptic junctions and thus induces muscarinic and nicotinic receptors stimulation. However, other mechanisms have recently been described. Central nervous system (CNS) depression particularly on respiratory and vasomotor centers may induce respiratory failure and cardiac arrest. Intermediate syndrome after NAs exposure is less common than OP pesticides poisoning. There are four approaches to detect exposure to NAs in biological samples: (I) AChE activity measurement, (II) Determination of hydrolysis products in plasma and urine, (III) Fluoride reactivation of phosphylated binding sites and (IV) Mass spectrometric determination of cholinesterase adducts. The clinical manifestations are similar to OP pesticides poisoning, but with more severity and fatalities. The management should be started as soon as possible. The victims should immediately be removed from the field and treatment is commenced with auto-injector antidotes (atropine and oximes) such as MARK I kit. A 0.5% hypochlorite solution as well as novel products like M291 Resin kit, G117H and Phosphotriesterase isolated from soil bacterias, are now available for decontamination of NAs. Atropine and oximes are the well known antidotes that should be infused as clinically indicated. However, some new adjuvant and additional treatment such as magnesium sulfate, sodium bicarbonate, gacyclidine, benactyzine, tezampanel, hemoperfusion, antioxidants and bioscavengers have recently been used for OP NAs poisoning.

  5. Advances in toxicology and medical treatment of chemical warfare nerve agents

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    Moshiri Mohammd

    2012-11-01

    Full Text Available Abstract Organophosphorous (OP Nerve agents (NAs are known as the deadliest chemical warfare agents. They are divided into two classes of G and V agents. Most of them are liquid at room temperature. NAs chemical structures and mechanisms of actions are similar to OP pesticides, but their toxicities are higher than these compounds. The main mechanism of action is irreversible inhibition of Acetyl Choline Esterase (AChE resulting in accumulation of toxic levels of acetylcholine (ACh at the synaptic junctions and thus induces muscarinic and nicotinic receptors stimulation. However, other mechanisms have recently been described. Central nervous system (CNS depression particularly on respiratory and vasomotor centers may induce respiratory failure and cardiac arrest. Intermediate syndrome after NAs exposure is less common than OP pesticides poisoning. There are four approaches to detect exposure to NAs in biological samples: (I AChE activity measurement, (II Determination of hydrolysis products in plasma and urine, (III Fluoride reactivation of phosphylated binding sites and (IV Mass spectrometric determination of cholinesterase adducts. The clinical manifestations are similar to OP pesticides poisoning, but with more severity and fatalities. The management should be started as soon as possible. The victims should immediately be removed from the field and treatment is commenced with auto-injector antidotes (atropine and oximes such as MARK I kit. A 0.5% hypochlorite solution as well as novel products like M291 Resin kit, G117H and Phosphotriesterase isolated from soil bacterias, are now available for decontamination of NAs. Atropine and oximes are the well known antidotes that should be infused as clinically indicated. However, some new adjuvant and additional treatment such as magnesium sulfate, sodium bicarbonate, gacyclidine, benactyzine, tezampanel, hemoperfusion, antioxidants and bioscavengers have recently been used for OP NAs poisoning.

  6. Determination of anti-convulsant and life-preserving capacities of three types of auto-injector therapies against soman intoxication in rats.

    Science.gov (United States)

    Myhrer, Trond; Enger, Siri; Aas, Pål

    2013-08-01

    More effective countermeasures against nerve-agent poisoning are needed, because current ones do not protect sufficiently, particularly the central nervous system (CNS). The purpose of the present study was to make a comparison of the antidotal capabilities of atropine/obidoxime/diazepam (termed the obidoxime regimen), atropine/HI-6 (1-[([4-(aminocarbonyl)pyridinio]methoxy)methyl]-2-[(hydroxyimino)methyl]pyridinium)/avizafone (termed the HI-6 regimen), and scopolamine/HI-6/physostigmine (termed the physostigmine regimen) against various doses of soman (2, 3, 4 x LD50 ). The results showed that each regimen administered twice (1 min and 5 min after exposure) effectively prevented or terminated epileptiform activity within 10 min. However, the regimens differed markedly in life-saving properties with the physostigmine regimen ranking highest followed in descending order by the HI-6 and obidoxime regimens. Pretreatment with pyridostigmine increased the potency of the HI-6 regimen, but not the obidoxime regimen. The latter regimen administered thrice (1 min, 5 min, and 9 min after exposure) did not compensate for the insufficiency. In half of the rats that lived for 7 days, neuropathology was unexpectedly observed predominantly in the left hemisphere unrelated to whether they seized or not. Local glutamatergic excitotoxic activity may occur even if manifest toxic signs are absent. The physostigmine regimen has excellent antidotal capacity, but the very narrow therapeutic window (< 10 min) makes it unsuitable for use in the field. The HI-6 regimen appears to constitute an efficacious therapy against lower doses of soman (2 and 3 x LD50). Copyright © 2012 John Wiley & Sons, Ltd.

  7. A functional study on small intestinal smooth muscles in jejunal atresia

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    Preeti Tyagi

    2016-01-01

    Full Text Available Aim: The present study was aimed to assess the contractile status of neonatal small intestinal smooth muscle of dilated pre-atretic part of intestinal atresia to resolve debatable issues related to mechanisms of persistent dysmotility after surgical repair. Materials and Methods: A total of 34 longitudinally sectioned strips were prepared from pre-atretic dilated part of freshly excised 8 jejunal atresia type III a cases. Spontaneous as well as acetylcholine- and histamine-induced contractions were recorded in vitro by using organ bath preparations. Chemically evoked contractions were further evaluated after application of atropine (muscarinic blocker, pheniramine (H1 blocker, and lignocaine (neuronal blocker to ascertain receptors and neuronal involvement. Histological examinations of strips were made by using Masson trichrome stain to assess the fibrotic changes. Results: All 34 strips, except four showed spontaneous contractions with mean frequency and amplitude of 5.49 ± 0.26/min and 24.41 ± 5.26 g/g wet tissue respectively. The response to ACh was nearly twice as compared to histamine for equimolar concentrations (100 μM. ACh (100 μM induced contractions were attenuated (by 60% by atropine. Histamine (100 μM-induced contractions was blocked by pheniramine (0.32 μM and lignocaine (4 μM by 74% and 78%, respectively. Histopathological examination showed varying degree of fibrotic changes in muscle layers. Conclusions: Pre-atretic dilated part of jejunal atresia retains functional activity but with definitive histopathologic abnormalities. It is suggested that excision of a length of pre-atretic part and early stimulation of peristalsis by locally acting cholinomimetic or H1 agonist may help in reducing postoperative motility problems in atresia patients.

  8. Effect of Fentanyl with Lidocaine on Hemodynamical Stability of Patients with History of Hypertension in TURP Surgery: A Double Blind Controlled Clinical Trial

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    M. Saheban Maleki

    2016-09-01

    Full Text Available Aims: Some severe hemodynamic changes are known as problems due to 5% lidocaine spinal anesthesia at the elderly. Such changes, also, may lead to the cardio-vascular or renal problems. The aim of this study was to compare between the hemodynamic changes in two spinal-cord anesthesia methods with 5% lidocaine (the current method and with low 5% lidocaine dose with 50μg fentanyl in the elderly patients with a systemic blood-pressure increase history in the transurethral resection of the prostate (TURP. Materials & Methods: In the two-blinded clinical trial, 148 patients aged more than 50 years with benign prostate hypertrophy, who had referred to 15th of Khordad Hospital of Gonabad for TURP between 2011 and 2012, were studied. The subjects, selected via simple random sampling method, were randomly divided into two groups (n=74 per group. The first and the second groups underwent spinal-cord anesthesia with the administrations of 5% lidocaine (2cc; 100mg and 5% lidocaine (1cc; 50mg + fentanyl (1cc; 50μg, respectively. Blood-pressure and heart-rate were recorded immediately after the anesthesia and at every 5 minutes. Data was analyzed by SPSS 21 software using independent T and Fisher’s exact tests. Findings: Mean reductions in the systolic and the diastolic blood-pressures (p<0.001 and mean reduction in the heart-rate (p=0.009 in lidocaine+fentanyl group were significantly lower than lidocaine group. In lidocaine group, ephedrine and atropine administrations were required in 26 and 19 patients, respectively. Nevertheless, no administration either of ephedrine or of atropine was required in lidocaine + fentanyl group (p<0.001. Conclusion: Without any hemodynamic instability, low lidocaine dose (50mg with fentanyl (50μg may result in sufficient anesthesia and no-pain in the elderly patients with a history of controlled high-pressure, who undergo TURP.

  9. Changes in cholinergic and nitrergic systems of defunctionalized colons after colostomy in rabbits.

    Science.gov (United States)

    Moralıoğlu, Serdar; Vural, İsmail Mert; Özen, İbrahim Onur; Öztürk, Gökçe; Sarıoğlu, Yusuf; Başaklar, Abdullah Can

    2017-01-01

    This study was designed to assess smooth muscle function and motility in defunctionalized colonic segments and subsequent changes in pathways responsible for gastrointestinal motility. Two-month-old New Zealand rabbits were randomly allocated into control and study groups. Sigmoid colostomies were performed in the study group. After a 2-month waiting period, colonic segments were harvested in both groups. For the in vitro experiment, the isolated circular muscle strips which were prepared from the harvested distal colon were used. First, contraction responses were detected using KCl and carbachol; relaxation responses were detected using papaverine, sodium nitroprusside, sildenafil, and l-arginine. The neurologic responses of muscle strips to electrical field stimulation (EFS) were evaluated in an environment with guanethidine and indomethacin. EFS studies were then repeated with atropine, Nω-nitro-l-arginine methyl ester, atropine, and Nω-nitro-l-arginine methyl ester-added environments. Although macroscopic atrophy had developed in the distal colonic segment of the colostomy, the contraction and relaxation capacity of the smooth muscle did not change. EFS-induced nitrergic-peptidergic, cholinergic-peptidergic, and noncholinergic nonnitrergic responses significantly decreased at all frequencies (0.5-32 Hz) in the study group compared with those in the control group (P < 0.05). Although the contraction capacity of the smooth muscle was not affected, the motility of the distal colon deteriorated owing to the defective secretion of presynaptic neurotransmitters such as acetylcholine, nitric oxide, and neuropeptides. Copyright © 2016 Elsevier Inc. All rights reserved.

  10. Repeated anaesthesia with isoflurane and medetomidine-midazolam-fentanyl in guinea pigs and its influence on physiological parameters.

    Science.gov (United States)

    Schmitz, Sabrina; Tacke, Sabine; Guth, Brian; Henke, Julia

    2017-01-01

    Repeated anaesthesia may be required in experimental protocols and in daily veterinary practice, but anaesthesia is known to alter physiological parameters in GPs (Cavia porcellus, GPs). This study investigated the effects of repeated anaesthesia with either medetomidine-midazolam-fentanyl (MMF) or isoflurane (Iso) on physiological parameters in the GP. Twelve GPs were repeatedly administered with MMF or Iso in two anaesthesia sets. One set consisted of six 40-min anaesthesias, performed over 3 weeks (2 per week); the anaesthetic used first was randomized. Prior to Iso anaesthesia, atropine was injected. MMF anaesthesia was antagonized with AFN (atipamezole-flumazenil-naloxone). Abdominally implanted radio-telemetry devices recorded the mean arterial blood pressure (MAP), heart rate (HR) and core body temperature continuously. Additionally, respiratory rate, blood glucose and body weight were assessed. An operable state could be achieved and maintained for 40 min in all GPs. During the surgical tolerance with MMF, the GPs showed a large MAP range between the individuals. In the MMF wake- up phase, the time was shortened until the righting reflex (RR) returned and that occurred at lower MAP and HR values. Repeated Iso anaesthesia led to an increasing HR during induction (anaesthesias 2-6), non-surgical tolerance (anaesthesias 3-6) and surgical tolerance (anaesthesias 4, 6). Both anaesthetics may be used repeatedly, as repeating the anaesthesias resulted in only slightly different physiological parameters, compared to those seen with single anaesthesias. The regular atropine premedication induced HR increases and repeated MMF anaesthesia resulted in a metabolism increase which led to the faster return of RR. Nevertheless, Iso's anaesthesia effects of strong respiratory depression and severe hypotension remained. Based on this increased anaesthesia risk with Iso, MMF anaesthesia is preferable for repeated use in GPs.

  11. Management of acute organophosphorus pesticide poisoning

    Science.gov (United States)

    Eddleston, Michael; Buckley, Nick A; Eyer, Peter; Dawson, Andrew H

    2008-01-01

    Summary Organophosphorus pesticide self-poisoning is an important clinical problem in rural regions of the developing world, and kills an estimated 200 000 people every year. Unintentional poisoning kills far fewer people but is a problem in places where highly toxic organophosphorus pesticides are available. Medical management is difficult, with case fatality generally more than 15%. We describe the limited evidence that can guide therapy and the factors that should be considered when designing further clinical studies. 50 years after first use, we still do not know how the core treatments—atropine, oximes, and diazepam—should best be given. Important constraints in the collection of useful data have included the late recognition of great variability in activity and action of the individual pesticides, and the care needed cholinesterase assays for results to be comparable between studies. However, consensus suggests that early resuscitation with atropine, oxygen, respiratory support, and fluids is needed to improve oxygen delivery to tissues. The role of oximes is not completely clear; they might benefit only patients poisoned by specific pesticides or patients with moderate poisoning. Small studies suggest benefit from new treatments such as magnesium sulphate, but much larger trials are needed. Gastric lavage could have a role but should only be undertaken once the patient is stable. Randomised controlled trials are underway in rural Asia to assess the effectiveness of these therapies. However, some organophosphorus pesticides might prove very difficult to treat with current therapies, such that bans on particular pesticides could be the only method to substantially reduce the case fatality after poisoning. Improved medical management of organophosphorus poisoning should result in a reduction in worldwide deaths from suicide. PMID:17706760

  12. Spatiotemporal characteristics and pharmacological modulation of multiple gamma oscillations in the CA1 region of the hippocampus

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    Shilpa eBalakrishnan

    2015-01-01

    Full Text Available Multiple components of γ-oscillations between 30-170 Hz in the CA1 region of the hippocampus have been described, based on their coherence with oscillations in other brain regions and on their cross-frequency coupling with local θ-oscillations. However, it remains unclear whether the different sub-bands are generated by a single broadband oscillator coupled to multiple external inputs, or by separate oscillators that incorporate distinct circuit elements. To distinguish between these possibilities, we used high-density linear array recording electrodes in awake behaving mice to examine the spatiotemporal characteristics of γ-oscillations and their responses to midazolam and atropine. We characterized oscillations using current source density (CSD analysis, and measured θ-γ phase-amplitude coupling by cross frequency coupling (CFC analysis. Prominent peaks were present in the CSD signal in the mid- and distal apical dendritic layers at all frequencies, and at stratum pyramidale for γslow (30-45 Hz and γmid (50-90 Hz, but not γfast (90-170 Hz oscillations. Differences in the strength and timing of θ-γslow and θ-γmid cross frequency coupling, and a lack of coupling at the soma and mid-apical region for γfast oscillations, indicated that separate circuit components generate the three sub-bands. Midazolam altered CSD amplitudes and cross-frequency coupling in a lamina- and frequency specific manner, providing further evidence for separate generator circuits. Atropine altered CSD amplitudes and θ-γ CFC uniformly at all locations. Simulations using a detailed compartmental model were consistent with γslow and γmid oscillations driven primarily by inputs at the mid-apical dendrites, and γfast at the distal apical dendrite. Our results indicate that multiple distinct local circuits generate γ-oscillations in the CA1 region of the hippocampus, and provide detailed information about their spatiotemporal characteristics.

  13. Isoflurane depresses baroreflex control of heart rate in decerebrate rats.

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    Lee, Jong S; Morrow, Don; Andresen, Michael C; Chang, Kyoung S K

    2002-05-01

    Isoflurane inhibits baroreflex control of heart rate (HR) by poorly understood mechanisms. The authors examined whether suprapontine central nervous system cardiovascular regulatory sites are required for anesthetic depression. The effects of isoflurane (1 and 2 rat minimum alveolar concentration [MAC]) on the baroreflex control of HR were determined in sham intact and midcollicular-transected decerebrate rats. Intravenous phenylephrine (0.2-12 microg/kg) and nitroprusside (1-60 microg/kg) were used to measure HR responses to peak changes in mean arterial pressure (MAP). Sigmoidal logistic curve fits to HR-MAP data assessed baroreflex sensitivity (HR/MAP), HR range, lower and upper HR plateau, and MAP at half the HR range (BP50). Four groups (two brain intact and two decerebrate) were studied before, during, and after isoflurane. To assess sympathetic and vagal contributions to HR baroreflex, beta-adrenoceptor (1 mg/kg atenolol) or muscarinic (0.5 mg/kg methyl atropine) antagonists were administered systemically. Decerebration did not alter resting MAP and HR or baroreflex parameters. Isoflurane depressed baroreflex slope and HR range in brain-intact and decerebrate rats. In both groups, 1 MAC reduced HR range by depressing peak reflex tachycardia. Maximal reflex bradycardia during increases in blood pressure was relatively preserved. Atenolol during 1 MAC did not alter maximum reflex tachycardia. In contrast, atropine during 1 MAC fully blocked reflex bradycardia. Therefore, 1 MAC predominantly depresses sympathetic components of HR baroreflex. Isoflurane at 2 MAC depressed both HR plateaus and decreased BP50 in both groups. Isoflurane depresses HR baroreflex control by actions that do not require suprapontine central nervous system sites. Isoflurane actions seem to inhibit HR baroreflex primarily by the sympathetic nervous system.

  14. The pharmacology of Malo maxima jellyfish venom extract in isolated cardiovascular tissues: A probable cause of the Irukandji syndrome in Western Australia.

    Science.gov (United States)

    Li, Ran; Wright, Christine E; Winkel, Kenneth D; Gershwin, Lisa-Ann; Angus, James A

    2011-03-25

    The in vitro cardiac and vascular pharmacology of Malo maxima, a newly described jellyfish suspected of causing Irukandji syndrome in the Broome region of Western Australia, was investigated in rat tissues. In left atria, M. maxima crude venom extract (CVE; 1-100μg/mL) caused concentration-dependent inotropic responses which were unaffected by atropine (1μM), but significantly attenuated by tetrodotoxin (TTX; 0.1μM), propranolol (1μM), Mg(2+) (6mM) or calcitonin gene-related peptide antagonist (CGRP(8-37); 1μM). CVE caused no change in right atrial rate until 100μg/mL, which elicited bradycardia. This was unaffected by atropine, TTX, propranolol or CGRP(8-37). In the presence of Mg(2+), CVE 30-100μg/mL caused tachycardia. In small mesenteric arteries CVE caused concentration-dependent contractions (pEC(50) 1.03±0.07μg/mL) that were unaffected by prazosin (0.3μM), ω-conotoxin GVIA (0.1μM) or Mg(2+) (6mM). There was a 2-fold increase in sensitivity in the presence of CGRP(8-37) (3μM). TTX (0.1μM), box jellyfish Chironex fleckeri antivenom (92.6U/mL) and benextramine (3μM) decreased sensitivity by 2.6, 1.9 and 2.1-fold, respectively. CVE-induced maximum contractions were attenuated by C. fleckeri antivenom (-22%) or benextramine (-49%). M. maxima CVE appears to activate the sympathetic, but not parasympathetic, nervous system and to stimulate sensory nerve CGRP release in left atria and resistance arteries. These effects are consistent with the catecholamine excess thought to cause Irukandji syndrome, with additional actions of CGRP release. Copyright © 2011 Elsevier Ireland Ltd. All rights reserved.

  15. Participation of the cholinergic system in the ethanol-induced suppression of paradoxical sleep in rats

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    L.A. Papale

    2008-09-01

    Full Text Available Sleep disturbance is among the many consequences of ethanol abuse in both humans and rodents. Ethanol consumption can reduce REM or paradoxical sleep (PS in humans and rats, respectively. The first aim of this study was to develop an animal model of ethanol-induced PS suppression. This model administered intragastrically (by gavage to male Wistar rats (3 months old, 200-250 g 0.5 to 3.5 g/kg ethanol. The 3.5 g/kg dose of ethanol suppressed the PS stage compared with the vehicle group (distilled water during the first 2-h interval (0-2 h; 1.3 vs 10.2; P < 0.001. The second aim of this study was to investigate the mechanisms by which ethanol suppresses PS. We examined the effects of cholinergic drug pretreatment. The cholinergic system was chosen because of the involvement of cholinergic neurotransmitters in regulating the sleep-wake cycle. A second set of animals was pretreated with 2.5, 5.0, and 10 mg/kg pilocarpine (cholinergic agonist or atropine (cholinergic antagonist. These drugs were administered 1 h prior to ethanol (3.5 g/kg or vehicle. Treatment with atropine prior to vehicle or ethanol produced a statistically significant decrease in PS, whereas pilocarpine had no effect on minutes of PS. Although the mechanism by which ethanol induces PS suppression is not fully understood, these data suggest that the cholinergic system is not the only system involved in this interaction.

  16. Comparison between fish and linseed oils administered orally for the treatment of experimentally induced keratoconjunctivitis sicca in rabbits

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    Danielle Alves Silva

    2017-09-01

    Full Text Available The objective of this study was to compare the efficacy of two sources of omega 3 and 6, fish oil (FO and linseed oil (LO, orally administered, alone or in combination, for treating experimentally induced keratoconjunctivitis sicca (KCS in rabbits. Twenty-eight New Zealand rabbits were used in this study. Seven animals were allocated to the C group (negative control, and KCS was induced in 21 animals by topically applying 1% atropine sulfate drops for 7 days. Treatment with atropine was maintained throughout the study period (12 weeks. The rabbits were divided into 3 treatment groups containing 7 animals each: FO group, LO group and FLO group (FO and LO. The animals were evaluated using the Schirmer Tear Test I (STT I, Rose Bengal Test (RBT, fluorescein test (FT, tear film break-up time (TBUT, and conjunctival and histopathological analysis. There was a significant increase in STT I and TBUT values in treatment groups, but the increase occurred earlier in the FO group. The results of the RBT and FT were similar among treatment groups, except FT, in the FLO group, negative staining was only in 12 weeks. There was a significant decrease in the number of goblet cells in the FLO group compared with the other groups. The results demonstrated that orally administered of FO and LO improved the clinical signs of KCS. However, improvement occurred earlier in the FO group. Using oils in combination did not provide additional benefits. These results contribute to the future development of new oral formulations as adjuvant therapies for KCS.

  17. Intravenous granisetron attenuates hypotension during spinal anesthesia in cesarean delivery: A double-blind, prospective randomized controlled study

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    Ahmed A Eldaba

    2015-01-01

    Full Text Available Background and Aims: This study was conducted to determine the effectiveness of intravenous (IV granisetron in the prevention of hypotension and bradycardia during spinal anesthesia in cesarean delivery. Material and Methods: A total of 200 parturients scheduled for elective cesarean section were included in this study. They were randomly divided into two groups. Group I was given 1 mg granisetron diluted in 10 ml normal saline slowly IV, 5 min before spinal anesthesia. Group II was given 10 ml of normal saline, 5 min before spinal anesthesia. Mean arterial blood pressure and heart rate (HR were recorded every 3 min until the end of surgery (for 45 min. The total consumption of vasopressors and atropine were recorded. Apgar scores at 1 and 5 min were also assessed. Results: Serial mean arterial blood pressure and HR values for 45 min after onset of spinal anesthesia were decreased significantly in group II, P < 0.0001. The incidence of hypotension after spinal anesthesia was 64% in group II and 3% in group I (P < 0.0001. The total doses of ephedrine (4.07 ± 3.87 mg vs 10.7 ± 8.9 mg, P < 0.0001, phenylephrine (0.0 microg vs 23.2 ± 55.1 microg, P < 0.0001, and atropine (0.0 mg vs 0.35 ± 0.49 mg P < 0.0001 consumed in both the groups respectively, were significantly less in group I versus group II. Conclusion: Premedication with 1 mg IV granisetron before spinal anesthesia in an elective cesarean section significantly reduces hypotension, bradycardia and vasopressors usage.

  18. Nitrergic Pathway Is the Main Contributing Mechanism in the Human Gastric Fundus Relaxation: An In Vitro Study.

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    Yang Won Min

    Full Text Available Human gastric fundus relaxation is mediated by intrinsic inhibitory pathway. We investigated the roles of nitrergic and purinergic pathways, two known inhibitory factors in gastric motility, on spontaneous and nerve-evoked contractions in human gastric fundus muscles.Gastric fundus muscle strips (12 circular and 13 longitudinal were obtained from patients without previous gastrointestinal motility disorder who underwent gastrectomy for stomach cancer. Using these specimens, we examined basal tone, peak, amplitude, and frequency of spontaneous contractions, and peak and nadir values under electrical field stimulation (EFS, 150 V, 0.3 ms, 10 Hz, 20 s. To examine responses to purinergic and nitrergic inhibition without cholinergic innervation, atropine (muscarinic antagonist, 1 μM, MRS2500 (a purinergic P2Y1 receptor antagonist, 1 μM, and N-nitro-L-arginine (L-NNA, a nitric oxide synthase inhibitor, 100 μM were added sequentially for spontaneous and electrically-stimulated contractions. Tetrodotoxin was used to confirm any neuronal involvement.In spontaneous contraction, L-NNA increased basal tone and peak in both muscle layers, while amplitude and frequency were unaffected. EFS (up to 10 Hz uniformly induced initial contraction and subsequent relaxation in a frequency-dependent manner. Atropine abolished initial on-contraction and induced only relaxation during EFS. While MRS2500 showed no additional influence, L-NNA reversed relaxation (p = 0.012 in circular muscle, and p = 0.006 in longitudinal muscle. Tetrodotoxin abolished any EFS-induced motor response.The relaxation of human gastric fundus muscle is reduced by nitrergic inhibition. Hence, nitrergic pathway appears to be the main mechanism for the human gastric fundus relaxation.

  19. Mechanism of action of honey bee (Apis mellifera L.) venom on different types of muscles.

    Science.gov (United States)

    Nabil, Z I; Hussein, A A; Zalat, S M; Rakha, M Kh

    1998-03-01

    1. The effect of crude honeybee (Apis mellifera) venom on the skeletal, smooth as well as cardiac muscles were studied in this investigation. 2. Perfusion of gastrocnemius-sciatic nerve preparation of frogs with 1 microgram/ml venom solution has weakened the mechanical contraction of the muscle without recovery. Blocking of nicotinic receptors with 3 micrograms/ml flaxedil before bee venom application sustained normal contraction of gastrocnemius muscle. 3. The electrical activity of duodenum rabbits was recorded before and after the application of 1 microgram/ml venom solution. The venom has depressed the amplitude of the muscle contraction after 15 min pretreatment with atropine nearly abolished the depressor effect of the venom on smooth muscle. 4. In concentrations from 0.5-2 micrograms/ml, bee venom caused decrease of heart rate of isolated perfused toad heart. This bradycardia was accompanied by elongation in the P-R interval. A gradual and progressive increase in the R-wave amplitude reflected a positive inotropism of the venom. Application of 5 micrograms/ml verapamil, a calcium channels blocking agent, abolished the noticed effect of the venom. 5. Marked electrocardiographic changes were produced within minutes of the venom application on the isolated perfused hearts, like marked injury current (elevation or depression of the S-T segment), atrioventricular conduction disturbances and sinus arrhythmias. Atropine and nicotine could decrease the toxic effect of the venom on the myocardium. 6. Results of the present work lead to the suggestion that bee venom is mediated through the peripheral cholinergic neurotransmitter system. General neurotoxicity of an inhibitory nature involving the autonomic as well as neuromuscular system are established as a result of the venom, meanwhile a direct effect on the myocardium membrane stabilization has been suggested.

  20. Antidiarrhoeal activity of the ethyl acetate extract of Baphia nitida (Papilionaceae).

    Science.gov (United States)

    Adeyemi, O O; Akindele, A J

    2008-03-28

    In our search for plants useful in the treatment of diarrhoea, we investigated the ethyl acetate extract of Baphia nitida (BN) using intestinal transit, enteropooling and gastric emptying tests in mice and rats. In the castor oil intestinal transit test, BN produced a significant (P400mg/kg vs. 89.33+/-6.28% for control. The effect at 400mg/kg was significantly lower than that of morphine, 10mg/kg, s.c. (20.29+/-3.78%), and was antagonized by isosorbide dinitrate, IDN (150mg/kg, p.o.) but not by yohimbine (1mg/kg, s.c.). This effect was not potentiated by atropine (1mg/kg, s.c.). In the castor oil-induced diarrhoea test, BN produced a significant increase in onset of diarrhoea (103.40+/-8.74, 138.80+/-17.04 and 174.8+/-29.04min, 100 to 400mg/kg, vs. 47.60+/-8.76min for control and 226.10+/-12.57min for morphine). The severity of diarrhoea (diarrhoea score) was dose dependently reduced (19.00+/-2.26, 17.04+/-1.89, 15.00+/-2.05, 100 to 400mg/kg, vs. 31.40+/-2.11 for control and 7.7+/-2.2 for morphine). This effect was not antagonized by IDN or yohimbine. The effect on severity was, however, potentiated by atropine. BN also reduced the number and weight of wet stools but did not have any significant effect on intestinal fluid accumulation and gastric emptying. Results obtained suggest that the ethyl acetate extract of Baphia nitida is endowed with antidiarrhoeal activity possibly mediated by interference with the l-arginine nitric oxide pathway and synergistic with antagonistic action on muscarinic receptors.

  1. Inhibitory effect of Rosa damascena Mill flower essential oil, geraniol and citronellol on rat ileum contraction.

    Science.gov (United States)

    Sadraei, H; Asghari, G; Emami, S

    2013-01-01

    Flower of Rosa damascena Mill is widely used in Iran for gastrointestinal (GI) disorders. However, its pharmacological action on ileum contraction has not been studied. In this research we have investigated ileum motility effect of essential oil of flower petals of R. damascena growing in Kashan, Iran, and two of its constituents. The essential oils obtained by hydrodistillation were investigated by a combination of GC and GC/MS. More than 34 compounds have been identified. The main constituents of the essential oil were β-citronellol (23%), nonadecane (16%), geraniol (16%) and heneicosane (5%). A portion of rat isolated ileum was suspended under 1g tension in Tyrode's solution at 37°C and gassed with O2. Effect of the R. damascena essential oil (2.5-160 μg/ml), geraniol (0.2-3.2 μg/ml) and citronellol (0.8-6.4 μg/ml) were studied on ileum contractions induced by KCl, acetylcholine (ACh) and electrical field stimulation (EFS) and compared with standard drugs atropine and loperamide. The contractile response of EFS was mediated mainly through the intramural nerve plexuses, because its response was inhibited by loperamide and partially reduced by atropine. The essential oil concentration dependently inhibited the response to KCl (IC50=67 ± 8.4μg/ml) and EFS (IC50=47 ± 10.6 μg/ml). Geraniol (IC50=1.7 ± 0.15 μg/ml for KCl) and citronellol (IC50=2.9 ± 0.3 μg/ml for KCl) also had inhibitory effect of ileum contraction and both were more potent than the essential oil. It was concluded that R. damascena essential oil mainly had an inhibitory effect on ileum contractions and geraniol and citronellol had a major role in inhibitory effect of the essential.

  2. Evidence for activation of both adrenergic and cholinergic nervous pathways by yohimbine, an alpha 2-adrenoceptor antagonist.

    Science.gov (United States)

    Bagheri, H; Chale, J J; Guyen, L N; Tran, M A; Berlan, M; Montastruc, J L

    1995-01-01

    Adrenoceptors are involved in the control of the activity of the autonomic nervous system and especially the sympathetic nervous system. Activation of alpha 2-adrenoceptors decreases sympathetic tone whereas their blockade has an opposite effect. However, previous investigations have shown that yohimbine (a potent alpha 2-adrenoceptor antagonist) increases salivary secretion through activation of cholinergic pathways. The aim of the present experiment was to investigate the involvement of both the sympathetic and the parasympathetic system in several pharmacological effects of yohimbine. For this purpose, salivary secretion and various endocrino-metabolic parameters (noradrenaline and insulin secretions, lipomobilization) were evaluated in conscious fasting dogs before and after blockade of either the sympathetic (with the beta-adrenoceptor antagonist agent nadolol) or the parasympathetic (with the anticholinergic agent atropine) systems. Yohimbine alone (0.4 mg.kg-1, i.v.) increased within 5-15 minutes, plasma noradrenaline (600%), insulin levels (300%), free-fatty acids (79%) and salivary secretion (143%). Atropine (0.2 mg.kg-1, i.v.) suppressed yohimbine-induced salivary secretion (90%) but did not significantly modify the yohimbine induced changes in noradrenaline (312%), insulin (277%) and free-fatty acids (102%) plasma levels. Administration of nadolol (1 mg.kg-1, i.v.) did not change the magnitude of the increase in both noradrenaline plasma levels (550%) and salivary secretion (300%) induced by yohimbine. However, nadolol totally blunted the increase in insulin (15%) and free-fatty acids (4%) plasma levels. These results show that yohimbine-induced increase in salivary secretion is a cholinergic effect whereas the increase in insulin and free fatty acids can be explained by an increase in sympathetic tone.(ABSTRACT TRUNCATED AT 250 WORDS)

  3. HYPOTENSIVE AND CARDIOINHIBOTORY EFFECTS OF THE AQUEOUS AND ETHANOL EXTRACTS OF CELERY (APIUM GRAVEOLENS, APIACEAE

    Directory of Open Access Journals (Sweden)

    Dragana Pavlović

    2010-03-01

    Full Text Available In this study we present the effects of aqueous and ethanol extracts of celery (Apium graveolens L., Apiaceae investigated on the mean blood pressure of anaesthetized rabbits and contractility of isolated atria of the rats. In our experiments were used rabbits and Wistar albino rats. The effects of extracts (0.5-15 mg/kg on blood pressure were recorded directly from the carotid artery. Rat isolated atria was mounted in 10 ml tissue bath. An equilibrium period of 30 min was given before the application of the extracts (0.02-0.75 mg/ml. In anesthetized rabbit, intravenous administration of aqueous extracts induced least hypotensive effects (14.35±2.94%, while the ethanol extract caused the greatest fall in the blood pressure (45.79±10.86%. Hypotensive effects of the extracts were partially blocked by atropine (0.3 mg/kg, an unselective muscarinic receptor antagonist. In isolated rat atria both aqueous and ethanolic extracts of celery, exhibit a negative chronotropic and an inotropic action. Aqueous extract decreased rate of contractions for 12.88±2.74% and amplitude for 8.73±0.89%. Ethanol extract inhibited rate of the atria contractions for 34.26±5.69%, and amplitude for 25.40±3.61%. Pretreatment of the atria with atropine (1μM partially blocked inhibitory response of aqueous and ethanol extracts. Ethanol extract of celery exhibited significantly greater hypotensive and cardio-depressant activities then aqueous extract (p<0.05. These data suggest that the aqueous and ethanol extracts of celery caused the hypotensive, negative inotropic and chronotropic effects, which could partially be mediated possibly via stimulation of muscarinic receptors. Inhibitory effect of ethanol extract was significant comparing to aqueous extract of celery.

  4. Role of ventrolateral orbital cortex muscarinic and nicotinic receptors in modulation of capsaicin-induced orofacial pain-related behaviors in rats.

    Science.gov (United States)

    Tamaddonfard, Esmaeal; Erfanparast, Amir; Abbas Farshid, Amir; Delkhosh-Kasmaie, Fatmeh

    2017-09-29

    Acetylcholine, as a major neurotransmitter, mediates many brain functions such as pain. This study was aimed to investigate the effects of microinjection of muscarinic and nicotinic acetylcholine receptor antagonists and agonists into the ventrolateral orbital cortex (VLOC) on capsaicin-induced orofacial nociception and subsequent hyperalgesia. The right side of VLOC was surgically implanted with a guide cannula in anaesthetized rats. Orofacial pain-related behaviors were induced by subcutaneous injection of a capsaicin solution (1.5µg/20µl) into the left vibrissa pad. The time spent face rubbing with ipsilateral forepaw and general behavior were recorded for 10min, and then mechanical hyperalgesia was determined using von Frey filaments at 15, 30, 45 and 60min post-capsaicin injection. Alone intra-VLOC microinjection of atropine (a muscarinic acetylcholine receptor antagonist) and mecamylamine (a nicotinic acetylcholine receptor antagonist) at a similar dose of 200ng/site did not alter nocifensive behavior and hyperalgesia. Microinjection of oxotremorine (a muscarinic acetylcholine receptor agonist) at doses of 50 and 100ng/site and epibatidine (a nicotinic acetylcholine receptor agonist) at doses of 12.5, 25, 50 and 100ng/site into the VLOC suppressed pain-related behaviors. Prior microinjections of 200ng/site atropine and mecamylamine (200ng/site) prevented oxotremorine (100ng/site)-, and epibatidine (100ng/site)-induced antinociception, respectively. None of the above-mentioned chemicals changed general behavior. These results showed that the VLOC muscarinic and nicotinic acetylcholine receptors might be involved in modulation of orofacial nociception and hypersensitivity. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. In a non-human primate model, aging disrupts the neural control of intestinal smooth muscle contractility in a region-specific manner.

    Science.gov (United States)

    Tran, L; Greenwood-Van Meerveld, B

    2014-03-01

    Incidences of gastrointestinal (GI) motility disorders increase with age. However, there is a paucity of knowledge about the aging mechanisms leading to GI dysmotility. Motility in the GI tract is a function of smooth muscle contractility, which is modulated in part by the enteric nervous system (ENS). Evidence suggests that aging impairs the ENS, thus we tested the hypothesis that senescence in the GI tract precipitates abnormalities in smooth muscle and neurally mediated contractility in a region-specific manner. Jejunal and colonic circular muscle strips were isolated from young (4-10 years) and old (18+ years) baboons. Myogenic responses were investigated using potassium chloride (KCl) and carbachol (CCh). Neurally mediated contractile responses were evoked by electrical field stimulation (EFS) and were recorded in the absence and presence of atropine (1 μM) or NG-Nitro-l-arginine methyl ester (l-NAME; 100 μM). The myogenic responses to KCl in the jejunum and colon were unaffected by age. In the colon, but not the jejunum, CCh-induced contractile responses were reduced in aged animals. Compared to young baboons, there was enhanced EFS-induced contractility of old baboon jejunal smooth muscle in contrast to the reduced contractility in the colon. The effect of atropine on the EFS response was lower in aged colonic tissue, suggesting reduced participation of acetylcholine. In aged jejunal tissue, higher contractile responses to EFS were found to be due to reduced nitregic inhibition. These findings provide key evidence for the importance of intestinal smooth muscle and ENS senescence in age-associated GI motility disorders. © 2014 The Authors. Neurogastroenterology & Motility published by John Wiley & Sons Ltd.

  6. Effectiveness of sub-Tenon's block in pediatric strabismus surgery

    Directory of Open Access Journals (Sweden)

    Kasim Tuzcu

    2015-10-01

    Full Text Available ABSTRACTBACKGROUND AND OBJECTIVES: Strabismus surgery is a frequently performed pediatric ocular procedure. A frequently occurring major problem in patients receiving this treatment involves the oculocardiac reflex. This reflex is associated with an increased incidence of postoperative nausea, vomiting, and pain. The aim of this study was to investigate the effects of a sub-Tenon's block on the oculocardiac reflex, pain, and postoperative nausea and vomiting.METHODS: 40 patients aged 5-16 years with American Society of Anesthesiologists status I-II undergoing elective strabismus surgery were included in this study. Patients included were randomly assigned into two groups by using a sealed envelope method. In group 1 (n = 20, patients did not receive sub-Tenon's anesthesia. In group 2 (n = 20, following intubation, sub-Tenon's anesthesia was performed with the eye undergoing surgery. Atropine use, pain scores, oculocardiac reflex, and postoperative nausea and vomiting incidences were compared between groups.RESULTS: There were no significant differences between groups with regard to oculocardiac reflex and atropine use (p > 0.05. Pain scores 30 min post-surgery were significantly lower in group 2 than in group 1 (p < 0.05. Additional analgesic needed during the postoperative period was significantly lower in group 2 compared to group 1 (p < 0.05.CONCLUSIONS: In conclusion, we think that a sub-Tenon's block, combined with general anesthesia, is not effective and reliable in decreasing oculocardiac reflex and postoperative nausea and vomiting. However, this method is safe for reducing postoperative pain and decreasing additional analgesia required in pediatric strabismus surgery.

  7. [Effectiveness of sub-Tenon's block in pediatric strabismus surgery].

    Science.gov (United States)

    Tuzcu, Kasim; Coskun, Mesut; Tuzcu, Esra Ayhan; Karcioglu, Murat; Davarci, Isil; Hakimoglu, Sedat; Aydın, Suzan; Turhanoglu, Selim

    2015-01-01

    Strabismus surgery is a frequently performed pediatric ocular procedure. A frequently occurring major problem in patients receiving this treatment involves the oculocardiac reflex. This reflex is associated with an increased incidence of postoperative nausea, vomiting, and pain. The aim of this study was to investigate the effects of a sub-Tenon's block on the oculocardiac reflex, pain, and postoperative nausea and vomiting. 40 patients aged 5-16 years with American Society of Anesthesiologists status I-II undergoing elective strabismus surgery were included in this study. Patients included were randomly assigned into two groups by using a sealed envelope method. In group 1 (n=20), patients did not receive sub-Tenon's anesthesia. In group 2 (n=20), following intubation, sub-Tenon's anesthesia was performed with the eye undergoing surgery. Atropine use, pain scores, oculocardiac reflex, and postoperative nausea and vomiting incidences were compared between groups. There were no significant differences between groups with regard to oculocardiac reflex and atropine use (p>0.05). Pain scores 30min post-surgery were significantly lower in group 2 than in group 1 (p<0.05). Additional analgesic needed during the postoperative period was significantly lower in group 2 compared to group 1 (p<0.05). In conclusion, we think that a sub-Tenon's block, combined with general anesthesia, is not effective and reliable in decreasing oculocardiac reflex and postoperative nausea and vomiting. However, this method is safe for reducing postoperative pain and decreasing additional analgesia required in pediatric strabismus surgery. Copyright © 2014 Sociedade Brasileira de Anestesiologia. Publicado por Elsevier Editora Ltda. All rights reserved.

  8. Effectiveness of sub-Tenon's block in pediatric strabismus surgery.

    Science.gov (United States)

    Tuzcu, Kasim; Coskun, Mesut; Tuzcu, Esra Ayhan; Karcioglu, Murat; Davarci, Isil; Hakimoglu, Sedat; Aydın, Suzan; Turhanoglu, Selim

    2015-01-01

    Strabismus surgery is a frequently performed pediatric ocular procedure. A frequently occurring major problem in patients receiving this treatment involves the oculocardiac reflex. This reflex is associated with an increased incidence of postoperative nausea, vomiting, and pain. The aim of this study was to investigate the effects of a sub-Tenon's block on the oculocardiac reflex, pain, and postoperative nausea and vomiting. Forty patients aged 5-16 years with American Society of Anesthesiologists status I-II undergoing elective strabismus surgery were included in this study. Patients included were randomly assigned into two groups by using a sealed envelope method. In group 1 (n=20), patients did not receive sub-Tenon's anesthesia. In group 2 (n=20), following intubation, sub-Tenon's anesthesia was performed with the eye undergoing surgery. Atropine use, pain scores, oculocardiac reflex, and postoperative nausea and vomiting incidences were compared between groups. There were no significant differences between groups with regard to oculocardiac reflex and atropine use (p>0.05). Pain scores 30min post-surgery were significantly lower in group 2 than in group 1 (p<0.05). Additional analgesic needed during the postoperative period was significantly lower in group 2 compared to group 1 (p<0.05). In conclusion, we think that a sub-Tenon's block, combined with general anesthesia, is not effective and reliable in decreasing oculocardiac reflex and postoperative nausea and vomiting. However, this method is safe for reducing postoperative pain and decreasing additional analgesia required in pediatric strabismus surgery. Copyright © 2014 Sociedade Brasileira de Anestesiologia. Published by Elsevier Editora Ltda. All rights reserved.

  9. Extraction and phytochemical investigation of Calotropis procera: effect of plant extracts on the activity of diverse muscles.

    Science.gov (United States)

    Moustafa, A M Y; Ahmed, S H; Nabil, Z I; Hussein, A A; Omran, M A

    2010-10-01

    isolated toad heart. The different extracts increased the power of contraction of the duodenum (trace a). Pretreatment with atropine sulfate as a muscarinic receptor blocker abolished the stimulatory effect of the different plant extracts and latex of C. procera (trace b). The present data suggest that ethanol, butanol, and EtOAc extracts of Calotropis procera have negative chronotropism and positive inotropism. Verapamil could abolish the inotropic effect of ethanol as well as that of butanol and EtOAc extracts. Meanwhile, atropine did not abolish the observed negative chronotropic effect. The ethanol extract increased the power of contraction of rabbit duodenum, but atropine abolished this effect. It also decreased the skeletal muscle contraction; this effect could be through blocking of the nicotinic receptors. Butanol and EtOAc extract data for smooth and skeletal muscles are very close to those for the corresponding ethanol extract of the studied plant. The present data for C. procera indicate its direct action on the myocardium, its increase of smooth muscle motility, and its relaxation of skeletal muscle contraction. The chemical constituents could directly affect the cell membrane probably through receptors coupling to G proteins. They regulate the ion channel physiology as in the myocardium. The present data on the extracts of C. procera indicate a direct action on the myocardium, stimulatory effect on smooth muscle motility, and relaxant action on skeletal muscle contraction. Chemical constituents could directly affect the cell membrane probably through receptors coupling to G proteins. They regulate the ion channel physiology as in the myocardium.

  10. Development of novel encapsulated formulations using albumin-chitosan as a polymer matrix for ocular drug delivery

    Science.gov (United States)

    Addo, Richard Tettey

    Designing formulations for ophthalmic drug delivery is one of the most challenging endeavors facing the pharmaceutical scientist due to the unique anatomy, physiology, and biochemistry of the eye. Current treatment protocols for administration of drugs in eye diseases are primarily solution formulations, gels or ointments. However, these modes of delivery have several drawbacks such as short duration of exposure, need for repeated administrations and non-specific toxicity. We hypothesize that development of ocular drugs in microparticles will overcome the deficiencies of the current modalities of treatment. We based the hypothesis on the preliminary studies conducted with encapsulated tetracaine, an anesthetic used for surgical purposes and atropine, a medication used for several ophthalmic indications including mydriatic and cycloplegic effects. However, atropine is well absorbed into the systemic circulation and has been reported to exert severe systemic side effects after ocular administration (Hoefnagel D. 1961, Morton H. G. 1939 and Lang J. C. 1995) and may lead to serious side effects including death in extreme cases with pediatric use. Based on these observations, the focus of this dissertation is to formulate microparticulate drug carrier for treatment of various conditions of the eye. Purpose: To prepare, characterize, study the in vitro and in vivo interaction of albumin-chitosan microparticles (BSA-CSN MS), a novel particulate drug carrier for ocular drug delivery. Method: Microparticle formulations were prepared by method of spray drying. The percentage drug loading and efficiency were assessed using USP (I) dissolution apparatus. Using Malvern Zeta-Sizer, we determined size and surface charge of the fabrication. Surface morphology of the microparticles was examined using Scanning Electron Microscopy. Microparticles were characterized in terms of thermal properties using Differential Scanning Calorimetry. Human corneal epithelial cells (HCET-1) were

  11. The early toxicology of physostigmine: a tale of beans, great men and egos.

    Science.gov (United States)

    Proudfoot, Alex

    2006-01-01

    Fraser did not get as close to the mode of action of physostigmine as Harley, he reigns supreme when it comes to antagonism between physostigmine and atropine. By this time, the 1870s had dawned and although the concept of antagonism between therapeutic agents was not new, it had little, if any, reliable scientific foundation. This was about to change; antagonism was becoming exciting and rational. Fraser's firm belief that physostigmine and atropine were mutually antagonistic at a physiological level was contrary to the conventional wisdom of his contemporaries. This alone would earn him a place in history but his contribution goes much, much further. Unlike any other at the time, he investigated it with scientific rigour, experimenting on only one species, ensuring as best he could the animals were the same weight, adjusting the doses of drugs he gave them for bodyweight, determining the minimum lethal dose of each drug before assessing their antagonistic effects, adopting a single, incontrovertible endpoint for efficacy and carrying out sufficient numbers of experiments to appear convincing in a later era where the statistical power of studies is all-important. To crown it all, he presented his results graphically. Fraser never claimed to have discovered the antagonism between physostigmine and atropine. Bartholow in 1873 did, based on work done in 1869. But his data hardly justify it. If anyone can reasonably claim this particular scientific crown it is an ophthalmologist, Niemetschek, working in Prague in 1864. His colleague in the same discipline, Kleinwächter, was faced with treating a young man with atropine intoxication. Knowing of the contrary actions of the two drugs on the pupil, Niemetschek suggested that Calabar bean extract might be useful. Kleinwächter had the courage to take the advice and his patient improved dramatically. Clearly, this evidence is nothing more than anecdotal, but the ophthalmologists were correct and, to the present day

  12. Effect on blood pressure of a dietary supplement containing traditional medicinal plants of Côte d'Ivoire.

    Science.gov (United States)

    Abrogoua, Danho Pascal; Dano, Djédjé Sébastien; Manda, Pierre; Adepo, Aholia Jean-Baptiste; Kablan, Brou Jérôme; Goze, Nomane Bernard; Ehoulé, Kroa

    2012-06-14

    A medicinal composition containing salt (sodium chloride) is given as a traditional dietary supplement to hypertensive patients (TDSHP) in Côte d'Ivoire. It consists of whole plant of Bidens pilosa (Asteraceae) and fresh leaves of Moringa oleifera (Moringaceae). The aim of this study was to establish the scientific basis for the use of this traditional recipe rich in sodium chloride in hypertension settings. We used a total aqueous extract of this traditional dietary supplement containing medicinal plants (Bidens pilosa, Moringa oleifera) and salt (sodium chloride). Experiment was carried out to evaluate its effect on arterial blood pressure of rabbits. The experimental device used for recording blood pressure in rabbits is based on the principle of Ludwig mercury manometer. TDSHP between 5×10(-8) and 5×10(-2) mg/kg caused a dose-dependent hypotension. TDSHP elicited drops in blood pressure ranging between 7.14±4 and 100±7.5%, compared to normal blood pressure of rabbits. Fifty percent effective dose of TDSHP was 3.95×10(-4) mg/kg. Similarly as the hypotension induced by acetylcholine, the one caused by TDSHP at dose of 3.95×10(-4) mg/kg in rabbit was progressively inhibited by atropine, dosed between 5×10(-4) to 5×10(-2) mg/kg. The percentage drop of recorded blood pressure ranged from 50.3±1.87 to 3.71±1.09% compared to the normal value of blood pressure. In the presence of atropine, TDSHP effect was partially inhibited. The same increasing doses of TDSHP reduced significantly the increase of blood pressure induced by adrenaline dosed at 4.76×10(-4) mg/kg from 89.3±2.19 to 1.19±0.59%. The consumption of this traditional dietary supplement is justified in hypertensive patients according to its composition and its ability to reduce blood pressure has been demonstrated experimentally. TDSHP should not be considered as an antihypertensive drug, it remains to us a salt substitute to be taken with moderation with strict adherence to the traditional dose

  13. Propofol for procedural sedation/anaesthesia in neonates.

    Science.gov (United States)

    Shah, Prakeshkumar S; Shah, Vibhuti S

    2011-03-16

    Elective medical or surgical procedures are commonplace for neonates admitted to NICU. Agents such as opioids are commonly used for achieving sedation/analgesia/anaesthesia for such procedures; however, these agents are associated with adverse effects. Propofol is used widely in paediatric and adult populations for this purpose. The efficacy and safety of the use of propofol in neonates has not been defined. To determine the efficacy and safety of propofol treatment compared to placebo or no treatment or alternate active agents in neonates undergoing sedation or anaesthesia for procedures. To conduct subgroup analyses according to method of propofol administration (bolus or continuous infusion), type of active control agent (neuromuscular blocking agents with or without the use of sedative, analgesics or anxiolytics), type of procedure (endotracheal intubation, eye examination, other procedure), and gestational age (preterm and term). We searched MEDLINE (1950 to September 30, 2010), EMBASE (1980 to September 30, 2010) and the Cochrane Central Register of Controlled Trials (CENTRAL, The Cochrane Library 2010, Issue 2) for eligible studies without language restriction. We searched reference lists of identified articles and abstracts submitted to Pediatric Academic Societies (2002 to 2009), and international trials registries for eligible articles. We included randomised or quasi-randomised controlled trials of propofol versus placebo, no treatment or other sedative/anaesthetic/analgesic agents in isolation or combination used in neonates for procedures. We collected and analysed data in accordance with the standard methods of the Cochrane Neonatal Review Group. One open-label randomised controlled trial of 63 neonates was eligible for inclusion. Thirty-three neonates in the propofol group were compared to 30 infants in the morphine-atropine-suxamethonium group. There was no statistically significant difference in the number of infants who required multiple

  14. Assessing the therapeutic efficacy of oxime therapies against percutaneous organophosphorus pesticide and nerve agent challenges in the Hartley guinea pig

    Science.gov (United States)

    Snider, Thomas H.; Wilhelm, Christina M.; Babin, Michael C.; Platoff, Gennady E.; Yeung, David T.

    2016-01-01

    Given the rapid onset of symptoms from intoxication by organophosphate (OP) compounds, a quick-acting, efficacious therapeutic regimen is needed. A primary component of anti-OP therapy is an oxime reactivator to rescue OP-inhibited acetylcholinesterases. Male guinea pigs, clipped of hair, received neat applications of either VR, VX, parathion, or phorate oxon (PHO) at the 85th percentile lethal dose, and, beginning with presentation of toxicosis, received the human equivalent dose therapy by intramuscular injection with two additional follow-on treatments at 3-hr intervals. Each therapy consisted of atropine free base at 0.4 mg/kg followed by one of eight candidate oximes. Lethality rates were obtained at 24 hr after VR, VX and PHO challenges, and at 48 hr after challenge with parathion. Lethality rates among symptomatic, oxime-treated groups were compared with that of positive control (OP-challenged and atropine-only treated) guinea pigs composited across the test days. Significant (p ≤ 0.05) protective therapy was afforded by 1,1-methylene bis(4(hydroxyimino- methyl)pyridinium) dimethanesulfonate (MMB4 DMS) against challenges of VR (p ≤ 0.001) and VX (p ≤ 0.05). Lethal effects of VX were also significantly (p ≤ 0.05) mitigated by treatments with oxo-[[1-[[4-(oxoazaniumylmethylidene)pyridin-1-yl] methoxymethyl]pyridin-4-ylidene]methyl]azanium dichloride (obidoxime Cl2) and 1-(((4-(aminocarbonyl) pyridinio)methoxy)methyl)-2,4-bis((hydroxyimino)methyl)pyridinium dimethanesulfonate (HLö-7 DMS). Against parathion, significant protective therapy was afforded by obidoxime dichloride (p ≤ 0.001) and 1,1′-propane-1,3-diylbis{4-[(E)-(hydroxyimino)methyl]pyridinium} dibromide (TMB-4, p ≤ 0.01). None of the oximes evaluated was therapeutically effective against PHO. Across the spectrum of OP chemicals tested, the oximes that offered the highest level of therapy were MMB4 DMS and obidoxime dichloride. PMID:26558457

  15. Spasmogenic and spasmolytic activities of Agastache mexicana ssp. mexicana and A. mexicana ssp. xolocotziana methanolic extracts on the guinea pig ileum.

    Science.gov (United States)

    Ventura-Martínez, Rosa; Rodríguez, Rodolfo; González-Trujano, María Eva; Ángeles-López, Guadalupe E; Déciga-Campos, Myrna; Gómez, Claudia

    2017-01-20

    Agastache mexicana has been used in traditional medicine for relief of abdominal pain and treatment of other diseases. Two subspecies have been identified: A. mexicana ssp. mexicana (AMM) and A. mexicana ssp. xolocotziana (AMX) and both are used traditionally without distinction or in combination. To determine the effect of methanol extracts of A. mexicana ssp. mexicana and A. mexicana ssp. xolocotziana on gut motility and their possible mechanism of action. The effect of AMM and AMX methanol extracts were tested on the spontaneous activity in the isolated guinea pig ileum and on tissues pre-contracted with KCl, electrical field stimulation (EFS) or ACh. In addition, the possible mechanism of action of each subspecies on gut motility was analyzed in the presence of hexametonium, indomethacin, L-NAME, verapamil, atropine or pyrylamine. A comparative chromatographic profile of these extracts was also done to indicate the most abundant flavonoids presents in methanol extracts of both subspecies. AMM, but not AMX, induced a contractile effect in the guinea pig ileum. This spasmogenic effect was partially inhibited by atropine, antagonist of muscarinic receptors; and pyrilamine, antagonist of H 1 receptors. In contrast, AMX, but not AMM, diminished the contractions induced by KCl, EFS or ACh. The spasmolytic activity of AMX was partially inhibited by hexamethonium, ganglionic blocker; and indomethacin, inhibitor of the synthesis of prostaglandins; but not by L-NAME, inhibitor of nitric oxide synthase. In addition, AMX diminished the maximal contraction induced by CaCl 2 in a calcium-free medium. Chromatographic analyses of these methanol extracts showed the presence of acacetin and tilanin in both. These results suggest that in folk medicine only AMX should be used as spasmolytic, and not in combination with AMM as traditionally occurs, due to the spasmogenic effects of the latter. In addition, activation of nicotinic receptors, prostaglandins and calcium channels, but

  16. [A preliminary study on the role of substance P in histamine-nasal-spray-induced allergic conjunctivitis in guinea pigs].

    Science.gov (United States)

    Li, Tong; Zhao, Changqing

    2015-10-01

    To investigate the effect of the non adrenergic non cholinergic nerve (NANC) and substance P (SP) in allergic rhinoconjunctivitis by observing histamine nasal provocation induced conjunctivitis in guinea pigs. Forty male guinea pigs were randomly divided into five groups with each group consisting of eight guinea pigs. All anesthetized guinea pigs were exposed either to histamine (0.2%, 5 µl) (group B~E) or saline (5 µl, group A) via unilateral nostril. No pretreatment was done in group A and B while pretreatment was done in groups C~E through injection into the unilateral common carotid artery with cholinergic nerve inhibitor (atropine, 1 mg/kg, group C), cholinergic nerve inhibitor plus adrenergic nerve inhibitors (atropine, 1 mg/kg, phentolamine, 1 mg/kg plus Esmolol, 1 mg/kg, group D) and cholinergic nerve inhibitor, adrenergic nerve inhibitors plus SP receptor antagonist (the same treatment with group D plus D-SP 10(-6) mol/L, 1 µl/g, group E), respectively. To assess the ipsilateral conjunctival inflammatory reaction, conjunctiva leakage with Evans blue dye assessments and HE staining of conjunctival tissues were performed. The SP expression in ipsilateral conjunctival tissue in different groups of guinea pigs were assessed by immunofluorescence and RT-PCR. The activity of eosinophils was assessed by eosinophil major basic protein 1 (MBP1) with RT-PCR, meanwhile, the activity of mast cells was assessed by tryptase with RT-PCR. SPSS 17.0 software was used to analyze the data. At 30 min after nasal application of histamine, ipsilateral conjunctivitis was successfully induced as shown by the change of conjunctiva leakage and histology. The content of Evans blue in ipsilateral conjunctival tissue of group A~E was (13.78 ± 2.48), (29.62 ± 3.31), (19.03 ± 1.47), (18.42 ± 2.52), (14.83 ± 2.14) µg/ml, respectively. There was statistically significant difference between group A and B (t = -10.66, P 0.05). Histamine nasal provocation induced allergic

  17. Catheter ablation of severe neurally meditated reflex (neurocardiogenic or vasovagal) syncope: cardioneuroablation long-term results.

    Science.gov (United States)

    Pachon, Jose Carlos M; Pachon, Enrique Indalecio M; Cunha Pachon, Maria Zelia; Lobo, Tasso Julio; Pachon, Juan Carlos M; Santillana, Tomas Guilhermo P

    2011-09-01

    Neurally meditated reflex or neurocardiogenic or vasovagal syncope (NMS) is usually mediated by a massive vagal reflex. This study reports the long-term outcome of NMS therapy based on endocardial radiofrequency (RF) catheter ablation of the cardiac vagal nervous system aiming permanent attenuation or elimination of the cardioinhibitory reflex (cardioneuroablation). A total of 43 patients (18F/25M, 32.9 ± 15 years) without apparent cardiopathy (left ventricular ejection fraction=68.6 ± 5%) were included. All had recurrent NMS (4.7 ± 2 syncope/patient) with important cardioinhibition (pauses=13.5 ± 13 s) at head-up tilt test (HUT), normal electrocardiogram (ECG), and normal atropine test (AT). The patients underwent atrial endocardial RF ablation using spectral mapping to track the neurocardiac interface (AF Nest Mapping). The follow-up (FU) consisted of clinical evaluation, ECG (1 month/every 6 months/or symptoms), Holter (every 6 months/or symptoms), HUT (≥ 4 months/or symptoms), and AT (end of ablation and ≥ 6 months). A total of 44 ablations (48 ± 9 points/patient) were performed. Merely three cases of spontaneous syncope occurred in 45.1 ± 22 months (two vasodepressor, one undefined). Only four partial cardioinhibitory responses occurred in post-ablation HUT without pauses or asystole (sinus bradycardia). Long-term AT (21.7 ± 11 months post) was negative in 33 (76.7%, P < 0.01), partially positive in 7(16.3%), and normal in three patients only (6.9%) reflecting long-term vagal denervation (AT-Δ%HR pre 79.4% × 23.2% post). The post-ablation stress test and Holter showed no abnormalities. No major complications occurred. Endocardial RF catheter ablation of severe neurally meditated reflex syncope prevented pacemaker implantation and showed excellent long-term results in well selected patients. Despite no action in vasodepression it seems to cause enough long-term vagal reflex attenuation, eliminating the cardioinhibition, and keeping most patients

  18. A comprehensive evaluation of the efficacy of leading oxime therapies in guinea pigs exposed to organophosphorus chemical warfare agents or pesticides

    Energy Technology Data Exchange (ETDEWEB)

    Wilhelm, Christina M., E-mail: wilhelmc@battelle.org [Battelle, 505 King Avenue, JM-7, Columbus, OH 43201-2693 (United States); Snider, Thomas H., E-mail: snidert@battelle.org [Battelle, 505 King Avenue, JM-7, Columbus, OH 43201-2693 (United States); Babin, Michael C., E-mail: babinm@battelle.org [Battelle, 505 King Avenue, JM-7, Columbus, OH 43201-2693 (United States); Jett, David A., E-mail: jettd@ninds.nih.gov [National Institutes of Health/National Institute of Neurological Disorders and Stroke, Bethesda, MD 20892 (United States); Platoff, Gennady E., E-mail: platoffg@niaid.nih.gov [National Institutes of Health/National Institute of Allergy and Infectious Diseases, Bethesda, MD 20892 (United States); Yeung, David T., E-mail: dy70v@nih.gov [National Institutes of Health/National Institute of Neurological Disorders and Stroke, Bethesda, MD 20892 (United States)

    2014-12-15

    The currently fielded pre-hospital therapeutic regimen for the treatment of organophosphorus (OP) poisoning in the United States (U.S.) is the administration of atropine in combination with an oxime antidote (2-PAM Cl) to reactivate inhibited acetylcholinesterase (AChE). Depending on clinical symptoms, an anticonvulsant, e.g., diazepam, may also be administered. Unfortunately, 2-PAM Cl does not offer sufficient protection across the range of OP threat agents, and there is some question as to whether it is the most effective oxime compound available. The objective of the present study is to identify an oxime antidote, under standardized and comparable conditions, that offers protection at the FDA approved human equivalent dose (HED) of 2-PAM Cl against tabun (GA), sarin (GB), soman (GD), cyclosarin (GF), and VX, and the pesticides paraoxon, chlorpyrifos oxon, and phorate oxon. Male Hartley guinea pigs were subcutaneously challenged with a lethal level of OP and treated at approximately 1 min post challenge with atropine followed by equimolar oxime therapy (2-PAM Cl, HI-6 DMS, obidoxime Cl{sub 2}, TMB-4, MMB4-DMS, HLö-7 DMS, MINA, and RS194B) or therapeutic-index (TI) level therapy (HI-6 DMS, MMB4-DMS, MINA, and RS194B). Clinical signs of toxicity were observed for 24 h post challenge and blood cholinesterase [AChE and butyrylcholinesterase (BChE)] activity was analyzed utilizing a modified Ellman's method. When the oxime is standardized against the HED of 2-PAM Cl for guinea pigs, the evidence from clinical observations, lethality, quality of life (QOL) scores, and cholinesterase reactivation rates across all OPs indicated that MMB4 DMS and HLö-7 DMS were the two most consistently efficacious oximes. - Highlights: • First comprehensive evaluation of leading AChE oxime reactivators • All oximes are compared against current U.S. therapy 2-PAM Cl. • Relative therapeutic oxime efficacies against OP CWNA and pesticides • Contribution to more effective

  19. Changes in the response to excitatory antagonists, agonists, and spasmolytic agents in circular colonic smooth muscle strips from patients with diverticulosis.

    Science.gov (United States)

    Alvarez-Berdugo, D; Espín, F; Arenas, C; López, I; Clavé, P; Gallego, D

    2015-11-01

    Colonic samples from asymptomatic diverticulosis (DS) patients presented enhanced electrical field stimulation (EFS)-contractions, in an earlier study of ours, suggesting increased endogenous responses. The aim of this study was to explore changes in excitatory neuromuscular transmission and to assess the pharmacodynamics of spasmolytic agents in DS. Circular muscle strips from sigmoid colon of DS patients (n = 30; 69.5 ± 14.8 years) and controls (n = 32; 64.7 ± 16.2 years) were studied using organ baths to evaluate the direct effect of excitatory agonists (carbachol, neurokinin A [NKA] and substance P [SP]), and the effect of antagonists (atropine and NK2 antagonist GR94800) and spasmolytic drugs (otilonium bromide [OB] and N-butyl-hyoscine) on the contractions induced by EFS-stimulation of excitatory motorneurons. qRT-PCR was also performed to compare mRNA expression of M2 , M3 , NK2 receptors and L-type calcium channels. Contractions to carbachol (Emax : 663.7 ± 305.6% control vs 2698.0 ± 439.5% DS; p curves for atropine (pIC50  = 8.56 ± 0.15 control vs pIC50  = 9.95 ± 0.18 DS group; p < 0.005) and slightly higher for GR94800 (pIC50  = 7.21 ± 0.18 control vs pIC50  = 7.97 ± 0.32 group; p < 0.0001). Lower efficacy (Emax ) and potency (pIC50 ) was observed for spasmolytic drugs in DS, whereas no differences were found regarding the relative expression of the receptors evaluated between groups. The greater response to cholinergic and tachykinergic agonists and greater potency for muscarinic and NK2 antagonists observed in DS might play a role in the spasticity found in diverticular disease. © 2015 John Wiley & Sons Ltd.

  20. Early differential cell death and survival mechanisms initiate and contribute to the development of OPIDN: A study of molecular, cellular, and anatomical parameters

    Energy Technology Data Exchange (ETDEWEB)

    Damodaran, T.V., E-mail: tdamodar@nccu.edu [Dept of Medicine, Duke University Medical Center, Durham, NC (United States); Pharmacology and Cancer biology, Duke University Medical Center, Durham, NC (United States); Dept of Biology, North Carolina Central University, Durham, NC 27707 (United States); Attia, M.K. [Pharmacology and Cancer biology, Duke University Medical Center, Durham, NC (United States); Abou-Donia, M.B., E-mail: donia@mc.duke.edu [Pharmacology and Cancer biology, Duke University Medical Center, Durham, NC (United States)

    2011-11-15

    Organophosphorus-ester induced delayed neurotoxicity (OPIDN) is a neurodegenerative disorder characterized by ataxia progressing to paralysis with a concomitant central and peripheral, distal axonapathy. Diisopropylphosphorofluoridate (DFP) produces OPIDN in the chicken that results in mild ataxia in 7-14 days and severe paralysis as the disease progresses with a single dose. White leghorn layer hens were treated with DFP (1.7 mg/kg, sc) after prophylactic treatment with atropine (1 mg/kg, sc) in normal saline and eserine (1 mg/kg, sc) in dimethyl sulfoxide. Control groups were treated with vehicle propylene glycol (0.1 ml/kg, sc), atropine in normal saline and eserine in dimethyl sulfoxide. The hens were euthanized at different time points such as 1, 2, 5, 10 and 20 days, and the tissues from cerebrum, midbrain, cerebellum, brainstem and spinal cord were quickly dissected and frozen for mRNA (northern) studies. Northern blots were probed with BCL2, GADD45, beta actin, and 28S RNA to investigate their expression pattern. Another set of hens was treated for a series of time points and perfused with phosphate buffered saline and fixative for histological studies. Various staining protocols such as Hematoxylin and Eosin (H and E); Sevier-Munger; Cresyl echt Violet for Nissl substance; and Gallocynin stain for Nissl granules were used to assess various patterns of cell death and degenerative changes. Complex cell death mechanisms may be involved in the neuronal and axonal degeneration. These data indicate altered and differential mRNA expressions of BCL2 (anti apoptotic gene) and GADD45 (DNA damage inducible gene) in various tissues. Increased cell death and other degenerative changes noted in the susceptible regions (spinal cord and cerebellum) than the resistant region (cerebrum), may indicate complex molecular pathways via altered BCL2 and GADD45 gene expression, causing the homeostatic imbalance between cell survival and cell death mechanisms. Semi quantitative