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Sample records for chlorpheniramine

  1. Compound list: chlorpheniramine [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available chlorpheniramine CHL 00090 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/H...uman/in_vitro/chlorpheniramine.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATE...ST/Rat/in_vitro/chlorpheniramine.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATE...ST/Rat/in_vivo/Liver/Single/chlorpheniramine.Rat.in_vivo.Liver.Single.zip ftp://f...tp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/chlorpheniramine.Rat.in_vivo.Liver.Repeat.zip ...

  2. Chlorpheniramine

    Science.gov (United States)

    ... in combination with fever and pain reducers, expectorants, cough suppressants, and decongestants. Ask your doctor or pharmacist for advice on which product is best for your symptoms. Check nonprescription cough and cold product labels carefully before using 2 ...

  3. Chlorpheniramine

    Science.gov (United States)

    Aller-Chlor® Syrup ... Chlor-Trimeton® Allergy Syrup ... Polaramine® Syrup ... in combination with fever and pain reducers, expectorants, cough suppressants, and decongestants. Ask your doctor or pharmacist ...

  4. N-Nitrosodimethylamine formation from ozonation of chlorpheniramine: Influencing factors and transformation mechanism.

    Science.gov (United States)

    Lv, Juan; Wang, Lin; Song, Yun; Li, Yongmei

    2015-12-15

    As a disinfection byproduct, the detection of N-nitrosodimethylamine (NDMA) in aquatic environments across the globe has caused widespread concern due to its potential carcinogenicity. In this study, the possibility of NDMA formation from chlorpheniramine ozonation was investigated. The influencing factors including the initial chlorpheniramine concentration, ozone dose, pH, and water matrix were quantified. Furthermore, the mechanisms for chlorpheniramine transformation and NDMA formation were explored. Our results demonstrate that ozonation is effective in removing chlorpheniramine. Generation of dimethylamine (DMA) and NDMA was observed during chlorpheniramine ozonation. Higher initial chlorpheniramine concentration and ozone dose resulted in higher production of NDMA. Acidic conditions (pH≤5) did not facilitate the production of NDMA. Ozone molecules played a dominant role in chlorpheniramine degradation, and influenced DMA release and NDMA formation. DMA and NDMA generations as well as their degradations were mainly attributed to hydroxyl radicals (·OH) produced by ozone decomposition. Water matrix properties such as HCO3(-) and humic acid affected DMA and NDMA generation due to ·OH competition. The degradation intermediates of chlorpheniramine were identified, among which only the intermediates with a DMA group were attributable to NDMA formation. A possible pathway for NDMA formation from chlorpheniramine ozonation is proposed. PMID:26261866

  5. Life-threatening overdose with lamotrigine, citalopram, and chlorpheniramine

    Directory of Open Access Journals (Sweden)

    Venkatraman N

    2008-01-01

    Full Text Available Lamotrigine is a commonly used agent for seizure control in epilepsy. There are limited data on the adverse effects of lamotrigine in overdose. We report a number of serious side-effects associated with a large overdose of lamotrigine. A 23-year-old female presented to the emergency department after taking an intentional overdose of 9.2 g of lamotrigine, 56 mg of chlorpheniramine, and 220 mg of citalopram. On admission, she had a reduced level of consciousness and electrocardiographic abnormalities; a widened QRS and a prolonged corrected QT (QTc interval. Prompt treatment with early intubation, along with the use of magnesium for cardioprotection and administration of sodium bicarbonate may have aided in a quick recovery with a short intensive care stay and good outcome.

  6. Chlorpheniramine impairs functional recovery in Carassius auratus after telencephalic ablation

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    D.C. Garção

    2009-04-01

    Full Text Available We determined the effect of an H1 receptor antagonist on the functional recovery of Carassius auratus submitted to telencephalic ablation. Five days after surgery the fish underwent a spatial-choice learning paradigm test. The fish, weighing 6-12 g, were divided into four groups: telencephalic ablation (A or sham lesion (S and saline (SAL or chlorpheniramine (CPA, ip, 16 mg/kg. For eight consecutive days each animal was trained individually in sessions separated by 24 h (alternate days. Training trials (T1-T8 consisted of finding the food in one of the feeders, which were randomly blocked for each subject. Animals received an intraperitoneal injection of SAL or CPA 10 min after the training trials. The time spent by the animals in each group to find the food (latency was analyzed separately at T1 and T8 by the Kruskal-Wallis test, followed by the Student Newman-Keuls test. At T1 the latencies (mean ± SEM of the A-SAL (586.3 ± 13.6 and A-CPA (600 ± 0 groups were significantly longer than those of the S-SAL (226.14 ± 61.15 and S-CPA (356.33 ± 68.8 groups. At T8, the latencies of the A-CPA group (510.11 ± 62.2 remained higher than those of the other groups, all of which showed significantly shorter latencies (A-SAL = 301.91 ± 78.32; S-CPA = 191.58 ± 73.03; S-SAL = 90.28 ± 41 compared with T1. These results support evidence that training can lead to functional recovery of spatial-choice learning in telencephalonless fish and also that the antagonist of the H1 receptor impairs it.

  7. SIMULTANEOUS ESTIMATION & VALIDATION OF PARACETAMOL, PHENYLEPHRINE HYDROCHLORIDE AND CHLORPHENIRAMINE MALEATE IN TABLETS BY SPECTROPHOTOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    R. SAWANT, R. JOSHI, P. LANKE L. BHANGALE

    2013-09-01

    Full Text Available The present work describes two methods for simultaneous estimation of phenylephrine hydrochloride and chlorpheniramine maleate in pure and solid dosage forms. First method employs the application of simultaneous equation and second, is a multi-wavelength spectrophotometric analysis method. Both methods utilize 0.1N NaOH as solvent. Simultaneous equation develops using 256.8 nm, 236.8 nm and 222.4 nm as the max of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate respectively. Calibration curves were linear over the concentration ranges of 0-35 μg/mL for all drugs. The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation < 1 %, while being simple, cheap and less time consuming, and hence can be suitably applied for simultaneous determination of three drugs in laboratory prepared mixtures and in commercial tablet preparation.

  8. Quantitative analysis of mitragynine, codeine, caffeine, chlorpheniramine and phenylephrine in a kratom (Mitragyna speciosa Korth.) cocktail using high-performance liquid chromatography.

    Science.gov (United States)

    Chittrakarn, Somsmorn; Penjamras, Pimpimol; Keawpradub, Niwat

    2012-04-10

    A simple HPLC technique for determining mitragynine, codeine, caffeine, chlorpheniramine and phenylephrine in 'kratom cocktail' was developed. The analytical method for mitragynine, codeine and caffeine used an Eclipse XDB-C8 column. A Lichrospher CN column was using for analysing chlorpheniramine and phenylephrine. The correlation coefficient of each standard was between 0.9957 and 0.9993. The precision of the methods were between 0.700 and 7.108% RSD. The concentration of mitragynine, codeine, caffeine, chlorpheniramine and phenylephrine in 'kratom cocktail' was 90.021, 234.174, 73.986, 7.053 and 1.486 mg/L, respectively. PMID:22018854

  9. Simultaneous determination of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate in pharmaceutical preparations using multivariate calibration 1

    Science.gov (United States)

    Samadi-Maybodi, Abdolraouf; Hassani Nejad-Darzi, Seyed Karim

    2010-04-01

    Resolution of binary mixtures of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate with minimum sample pre-treatment and without analyte separation has been successfully achieved by methods of partial least squares algorithm with one dependent variable, principal component regression and hybrid linear analysis. Data of analysis were obtained from UV-vis spectra of the above compounds. The method of central composite design was used in the ranges of 1-15 mg L -1 for both calibration and validation sets. The models refinement procedure and their validation were performed by cross-validation. Figures of merit such as selectivity, sensitivity, analytical sensitivity and limit of detection were determined for all three compounds. The procedure was successfully applied to simultaneous determination of the above compounds in pharmaceutical tablets.

  10. Abuse of "BRON": a Japanese OTC cough suppressant solution containing methylephedrine, codeine, caffeine and chlorpheniramine.

    Science.gov (United States)

    Ishigooka, J; Yoshida, Y; Murasaki, M

    1991-01-01

    1. The paper describes the mental disturbances of 44 abusive cases of "BRON," an over-the-counter (OTC) cough suppressant solution containing methylephedrine, codeine, caffeine, and chlorpheniramine. 2. Major psychiatric symptoms observed included hallucinatory-paranoid state and affective disorder. There also were groups which exhibited a combination of the two states and abuse only. 3. The hallucinatory-paranoid state group had a relatively small BRON usage amount, short usage term and few withdrawal symptoms. The affective disorder group, in contrast, had large usage amount, longer usage term, and showed significant autonomic nerve disorders during withdrawal. These tendencies were seen more clearly in the mixed state group. 4. The hallucinatory-paranoid state group showed little or no physical dependence, while that of the affective disorder group was thought to be firmly established. Thus, in the former group, methylephedrine was considered the major behavior modifying drug, while in the latter, it was thought to be codeine. PMID:1749828

  11. SIMULTANEOUS ESTIMATION AND VALIDATION OF PARACETAMOL, CHLORPHENIRAMINE MALEATE AND PHENYLEPHRINE HYDROCHLORIDE IN BULK AND TABLET DOSAGE FORM BY USING DIFFERENT SPECTROPHOTOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    Hapse Sandip Appasaheb

    2013-10-01

    Full Text Available A simple, precise, accurate and economic simultaneous UV spectrophotometric method has been developed for the estimation of Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride in combination in bulk mixture and tablet. The estimation was based upon measurement of absorbance at absorbance maxima of 258 nm, 262 nm and 239 nm for Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride in methanol, respectively in bulk mixture and tablet. The Beer Lambert's law obeyed in the concentration range 4-24 μg/ml, for Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride respectively. The estimation of bulk mixture and tablet was carried out by simultaneous equation, Q-analysis and area under curve method for estimation of Paracetamol, Chlorpheniramine Maleate and Phenylephrine Hydrochloride. Recovery study was performed to confirm the accuracy of the methods. The methods were validated as per ICH guidelines.

  12. Cardiovascular effects of a chlorpheniramine/paracetamol combination in hypertensive patients who were sensitive to the pressor effect of pseudoephedrine.

    Science.gov (United States)

    Chua, S S; Benrimoj, S I; Gordon, R D; Williams, G

    1991-03-01

    Twelve hypertensive patients who were classified as pseudoephedrine-sensitive in a preliminary trial were selected for further investigation with single doses of pseudoephedrine 60 mg, a combination of chlorpheniramine 4 mg with paracetamol 650 mg and placebo. A double-blind, randomised, crossover study design was followed. Treatment with pseudoephedrine produced significant effects on all the four variables measured (systolic, diastolic and mean arterial blood pressure, and heart rate). Effects of the chlorpheniramine/paracetamol combination were found to be not significantly different from placebo. It was concluded that the combination may be useful as a medication for 'colds' in hypertensive patients, since it does not induce cardiovascular effects such as those observed with pseudoephedrine. PMID:2054278

  13. Visible Spectrophotometric determination of Chlorpheniramine maleate and Diphenhydramine hydrochloride in raw and dosage form using Potassium permanganate

    OpenAIRE

    Mohammed Al Bratty

    2016-01-01

    Two simple, rapid and sensitive spectrophotometric methods developed for Chlorpheniramine Maleate (CPM) and Diphenhydramine Hydrochloride (DPH) determination in pure and pharmaceutical preparation using Potassium Permanganate. The solvent system used was potassium permanganate. The method developed by adding a known amount of permanganate to CPM and DPH in acid and alkaline medium, the unreacted permanganate was determined at 550 nm; method A and bluish green colour of Manganate at 610 nm; me...

  14. Simultaneous determination of phenylephrine hydrochloride, guaifenesin, and chlorpheniramine maleate in cough syrup by gradient liquid chromatography.

    Science.gov (United States)

    Amer, Sawsan M; Abbas, Samah S; Shehata, Mostafa A; Ali, Nahed M

    2008-01-01

    A simple and reliable high-performance liquid chromatographic method was developed for the simultaneous determination of mixture of phenylephrine hydrochloride (PHENYL), guaifenesin (GUAIF), and chlorpheniramine maleate (CHLO) either in pure form or in the presence of methylparaben and propylparaben in a commercial cough syrup dosage form. Separation was achieved on a C8 column using 0.005 M heptane sulfonic acid sodium salt (pH 3.4 +/- 0.1) and acetonitrile as a mobile phase by gradient elution at different flow rates, and detection was done spectrophotometrically at 210 nm. A linear relationship in the range of 30-180, 120-1800, and 10-60 microg/mL was obtained for PHENYL, GUAIF, and CHLO, respectively. The results were statistically analyzed and compared with those obtained by applying the British Pharmacopoeia (2002) method and showed that the proposed method is precise, accurate, and can be easily applied for the determination of the drugs under investigation in pure form and in cough syrup formulations. PMID:18476338

  15. Stability-indicating High-performance Liquid Chromatography Method for Simultaneous Determination of Aminophylline and Chlorpheniramine Maleate in Pharmaceutical Formulations.

    Science.gov (United States)

    Ali, A; Ahmed, M; Mahmud, T; Qadir, M A; Nadeem, K; Saleem, A

    2015-01-01

    The present work deals with the development and validation of method for simultaneous determination of antihistaminic drugs in pharmaceutical formulations. A precise, specific and accurate reverse phase-high-performance liquid chromatography method for the simultaneous measurement of aminophylline and chlorpheniramine maleate was developed. The separation of drugs was achieved on C-18 (5 μm, 250×4.6 mm) high-performance liquid chromatography column. The runtime for analysis was 10 min. Mobile phase is mixture containing dilute H2SO4:methanol (60:40% v/v) with flow rate adjusted at 1.5 ml/min. The detection of components was performed at a wavelength of 264 nm. Retention times of aminophylline and chlorphinramine maleate were found to be 2.00 and 3.25 min, respectively. Linearity was found in the range of 16-24 μg/ml for chlorpheniramine maleate and 102.4-153.6 μg/ml for aminophylline with a correlation coefficient of 0.9998 and 0.9996, respectively. High peak purity index of 99.99% indicated the complete separation of analytes in the presence of degradation products is justification of method stability. Linearity, accuracy, specificity, precision and robustness studies were performed for method validation. PMID:26798164

  16. Visible Spectrophotometric determination of Chlorpheniramine maleate and Diphenhydramine hydrochloride in raw and dosage form using Potassium permanganate

    Directory of Open Access Journals (Sweden)

    Mohammed Al Bratty

    2016-05-01

    Full Text Available Two simple, rapid and sensitive spectrophotometric methods developed for Chlorpheniramine Maleate (CPM and Diphenhydramine Hydrochloride (DPH determination in pure and pharmaceutical preparation using Potassium Permanganate. The solvent system used was potassium permanganate. The method developed by adding a known amount of permanganate to CPM and DPH in acid and alkaline medium, the unreacted permanganate was determined at 550 nm; method A and bluish green colour of Manganate at 610 nm; method B. In method A decrease in absorbance or method B increase in absorbance as concentrations of CPM and DPH was measured. Beer’s law was obeyed at a range of 2.5 to 20 μg / ml in both the methods A and B. The method was validated as per International Council for Harmonisation guideline. The proposed methods were effectively used for the determination of CPM and DPH in commercially available syrup. The average percentages of recoveries of CPM were 99.20 ± 1.29% (method A, 100.6% ± 1.43% (method B; DPH 98.50 ± 1.29% (method A and 100.20 ± 1.43% (method B. The methods were efficiently validated and used for quantitative determination of Chlorpheniramine maleate and Diphenhydramine Hydrochloride in pure and syrup preparations.

  17. Synergistic action of famotidine and chlorpheniramine on acetic acid-induced chronic gastric ulcer in rats

    Institute of Scientific and Technical Information of China (English)

    Zhen Qin; Chao Chen

    2005-01-01

    AIM: To assess the synergistic action of famotidine (FMD)and chlorpheniramine (CPA) on acetic acid-induced chronic gastric ulcer in rats.METHODS: Chronic gastric lesions were induced in male Sprague-Dawley (SD) rats by serosal application of the acetic acid. Forty SD rats were randomly divided into blank group (n = 8), control group (n = 8), FMD group (n= 8), CPA group (n = 8), and FMD+CPA group (n = 8).Each group was given intraperitoneally (i.p.) 0.5 mL/100g distilled water, 9 g/L NaCl saline, 4 mg/kg FMD, 10mg/kg CPA, 4 mg/kg FMD+10 mg/kg CPA, respectively,daily for 10 d. On d 10, ulcer area was determined by planimetry. The level of myeloperoxidase (MPO) in the liver homogenation was determined by biochemical methods and the plasma levels of 6-ketoprostaglandin F1 alpha (6-keto-PGF1a)and IL-8 were determined by radioimmunoassay.RESULTS: The synergistic effects of FMD+CPA group on the lesion, IL-8, 6-keto-PGF1a and MPO were confirmed.The effect of FMlD+CPA group was significantly different as compared to the control and FMD groups. The lesion (mm2) was reduced from 40.18±2.6 in control group to 6.83±2.97 in PMD+CPA group, P<0.01, and from 32.9±3.27 in FMD group to 6.83±2.97 in pMlD+CPA group,P<0.01. The plasma levels of IL-8 decreased from 0.69±0.11 ng/L in control group to 0.4±0.04 ng/L in PMD+CPA group, P<0.01, and from 0.51±0.08 ng/L in FMD group to 0.4±0.04 ng/L in PMD+CPA group, P<0.05. The level of 6-keto-PGF1a increased from 7.55±1.65 ng/L in control group to 16.62±0.97 ng/L in PMD+CPA group, P<0.01,and from 13.15±1.48 ng/L in FMD group to 16.62±0.97ng/L in PMD+CPA group, P<0.05. The levels of MPO in the liver homogenate decreased from 9.12±2.05 u/Lin control group to 4.33±0.95 u/L in PMD+CPA group,P<0.01, and from 8.3±1.29 u/L in FMD group to 4.33±0.95 u/L, P<0.01.CONCLUSION: The synergistic action of FMD and CPA on acetic acid-induced chronic gastric ulcer in rats decreases the incidence of ulcer and also enhances the

  18. Comparative Study of Apo-Cetirizine Single Therapy and Intermittent Sequential Therapy with Cetirizine, Loratadine and Chlorpheniramine in Allergic Rhinitis.

    Science.gov (United States)

    Safavi Naini, Ali; Ghorbani, Jahangir; Mazloom, Ebrahim

    2016-09-01

    There are limited numbers of articles, studying combined use of antihistamines. In this study, we compare single therapy of Apo-Cetirizine with a new regimen of intermittent sequential therapy with cetirizine, loratadine and chlorpheniramine in treatment of seasonal allergic rhinitis. This randomized clinical trial was performed between April and September at the peak prevalence of seasonal allergic rhinitis. Fifty-four eligible patients diagnosed clinically to have seasonal allergic rhinitis were randomized in two groups: 24 cases in single therapy arm, received Apo-Cetirizine 10 mg tablet daily and in other arm, 30 patients received sequential regimen of cetirizine 10 mg tablet, loratadine 10 mg tablet and chlorpheniramine 4 mg tablet, one tablet each day. Major Symptom Complex Score (MSCS) and Total Symptom Complex Score (TSCS) of patients were recorded before treatment and after 30 days of treatment in two groups. The average post-treatment MSCS and TSCS in combination therapy group showed better improvement than single therapy group but difference was not statistically significant (p value = 0.053 and p value = 0.104 respectively). Combination therapy regimen was better in improvement of nasal congestion (p value = 0.006). There were no significant difference between two groups in efficacy, side effects and patient's satisfaction. Combination therapy would be effective on a wide spectrum of symptoms with lower price and theoretically offers lower chance of tolerance and re-appearance of complaints. PMID:27508135

  19. Development and Validation of an RP-HPLC Method for Estimation of Chlorpheniramine Maleate, Ibuprofen, and Phenylephrine Hydrochloride in Combined Pharmaceutical Dosage Form

    Directory of Open Access Journals (Sweden)

    Pinak M. Sanchaniya

    2013-01-01

    Full Text Available The objective of this paper is to develope a simple, precise, accurate, and reproducible reversed phase high performance liquid chromatographic method for the quantitative determination of chlorpheniramine maleate, ibuprofen, and phenylephrine hydrochloride in combined pharmaceutical dosage form. Analysis was carried out using acetonitrile : mathanol : phoshphate buffer (50 : 20 : 30, v/v/v, pH 5.6 mobile phase at 1.0 mL/min flow rate and Sunfire C 18 column (5 μm × 250 mm × 4.6 mm as stationary phase with detection wavelength of 220 nm. The retention times of chlorpheniramine maleate (CPM, ibuprofen (IBU, and phenylephrine hydrochloride (PHE were 4.2 min, 13.6 min, and 2.7 min, respectively. The proposed method was validated with respect to linearity, accuracy, precision, specificity, and robustness. The linearity for chlorpheniramine maleate, ibuprofen, and phenylephrine hydrochloride was in the range of 0.5–2.5 μg/mL, 25–125 μg/mL, and 1.25–6.25 μg/mL, respectively. The % recoveries of all the three drugs were found to be 99.44–101.61%, 99.39–101.79%, and 98.66–101.83%. LOD were found to be 32, 120, and 68 ng/mL for CPM, IBU, and PHE, respectively. The method was successfully applied to the estimation of chlorpheniramine maleate, ibuprofen, and phenylephrine hydrochloride in combined pharmaceutical dosage form.

  20. A comparison of the in vivo effects of ketotifen, clemastine, chlorpheniramine and sodium cromoglycate on histamine and allergen induced weals in human skin.

    OpenAIRE

    Phillips, M. J.; Meyrick Thomas, R H; I. Moodley; Davies, R J

    1983-01-01

    The effect of ketotifen was compared with that of clemastine and chlorpheniramine, known antihistamines, and sodium cromoglycate, a drug considered to have mast cell "stabilizing' properties on histamine and allergen wealing reactions in human skin, in random order, double-blind, placebo controlled studies. Ketotifen was significantly more potent in the inhibition of both histamine (P less than 0.001) and allergen (P less than 0.001) skin wealing reactions than either clemastine or chlorpheni...

  1. Chloroquine resistant Plasmodium falciparum malaria in Osogbo Nigeria: efficacy of amodiaquine + sulfadoxine-pyrimethamine and chloroquine + chlorpheniramine for treatment

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    TO Ogungbamigbe

    2008-02-01

    Full Text Available Chloroquine (CQ resistance in Plasmodium falciparum contributes to increasing malaria-attributable morbidity and mortality in Sub-Saharan Africa. Despite a change in drug policy, continued prescription of CQ did not abate. Therefore the therapeutic efficacy of CQ in uncomplicated falciparum malaria patients was assessed in a standard 28-day protocol in 116 children aged between six and 120 months in Osogbo, Southwest Nigeria. Parasitological and clinical assessments of response to treatment showed that 72 (62.1% of the patients were cured and 44 (37.9% failed the CQ treatment. High initial parasite density and young age were independent predictors for early treatment failure. Out of the 44 patients that failed CQ, 24 received amodiaquine + sulphadoxine/pyrimethamine (AQ+SP and 20 received chlorpheniramine + chloroquine (CH+CQ combinations. Mean fever clearance time in those treated with AQ+SP was not significantly different from those treated with CH+CQ (p = 0.05. There was no significant difference in the mean parasite density of the two groups. The cure rate for AQ+SP group was 92% while those of CH+CQ was 85%. There was a significant difference in parasite clearance time (p = 0.01 between the two groups. The 38% treatment failure for CQ reported in this study is higher than the 10% recommended by World Health Organization in other to effect change in antimalarial treatment policy. Hence we conclude that CQ can no more be solely relied upon for the treatment of falciparum malaria in Osogbo, Nigeria. AQ+SP and CH+CQ are effective in the treatment of acute uncomplicated malaria and may be considered as useful alternative drugs in the absence of artemisinin-based combination therapies.

  2. Physicochemical properties and mechanisms of drug release from melt-extruded granules consisting of chlorpheniramine maleate and Eudragit FS.

    Science.gov (United States)

    Zhang, Feng

    2016-01-01

    The objective of this research project was to characterize the drug release profiles, physicochemical properties and drug-polymer interaction of melt-extruded granules consisting of chlorpheniramine maleate (CPM) and Eudragit® FS. Melt extrusion was performed using a single screw extruder at a processing temperature of 65-75 °C. The melt extrudate was milled, blended with lactose monohydrate and then filled into hard gelatin capsules. Each capsule contained 300 mg CPM granules. The release of CPM was determined with the United States Pharmacopeia dissolution apparatus II using a three-stage dissolution medium testing in order to simulate the pH conditions of the gastrointestinal tract. Pore structure, thermal properties and surface morphologies of CPM granules were studied using mercury and helium pycnometer, differential scanning calorimeter and scanning electron microscope. Sustained release of CPM over 10 h was achieved. The release of CPM was a function of drug loading and the size of the milled granules. The complexation between CPM and Eudragit® FS as the result of counterion condensation was observed, and the interaction was characterized using membrane dialysis and H(1) NMR techniques. In both 0.1 N HCl and phosphate buffer pH 6.8, CPM was released via a diffusion mechanism and the release rate was controlled by the pore structure of the melt-extruded granules. In phosphate buffer pH 7.4, CPM release was controlled by the low pH micro-environment created by CPM, the pore structure of the granules and the in situ complexation between CPM and Eudragit® FS. PMID:26065535

  3. Health outcome and safety assessment of a fixed dose combination of Amantadine, Paracetamol, Chlorpheniramine maleate, and Phenylephrine introduction in India: A prescription event monitoring study

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    K Krishnaprasad

    2012-01-01

    Full Text Available To assess the likely impact of a fixed dose combination (FDC of Amantadine, Paracetamol, Chlorpheniramine maleate, and Phenylephrine on the health outcome and safety profile arising from the complementary action of amantadine and other ingredients, we conducted a Prescription Event Monitoring study for patients with suspected Influenza symptoms who were prescribed this FDC in ′real life clinical settings′ or clinical practice. Between August 2010 and March 2011, Questionnaires were sent to doctors who provided data on the health outcome or safety profile. Sedation and allergy, including rash, were noted in few of the patients. None of the patients reported any major events. Most of the patients (60% were initiated on FDC therapy within the first 24 hours of symptom onset. Even as a significant proportion of the patients (24.9% had a concurrent history of allergy / rhinitis including asthma, few of them (4.1% reported lack of improvement and had to be complemented with antibiotics. The FDC of Amantadine, Chlorpheniramine, Paracetamol, and Phenylephrine was found to be safe and well-tolerated when administered to patients within the first 24 to 48 hours of symptom onset.

  4. Development and validation of RP-HPLC method for simultaneous estimation of nimesulide, phenylephrine hydrochloride, chlorpheniramine maleate and caffeine anhydrous in pharmaceutical dosage form.

    Science.gov (United States)

    Kumar, Ashok; Sharma, Rishbha; Nair, Anroop; Saini, Gautam

    2012-01-01

    In this study, a simple, specific and accurate reverse phase high performance liquid chromatographic method was developed for the simultaneous determination of nimesulide (NS), phenylephrine hydrochloride (PE), chlorpheniramine maleate (CPM) and caffeine anhydrous (CF) in pharmaceutical dosage forms. A reversed phase Hypersil phenyl column (4.6 mm x 25 cm) with mobile phase having pH 5.5 consisting of methanol and buffer (55:45, v/v) was used. The flow rate was 1.0 mL per minute and the effluents were monitored at 214 nm. The retention times of all the drugs were found to be 7.47 min (NS), 3.944 min (PE), 4.55 min (CF) and 17.15 min (CPM), respectively. The linearity for all the drugs was obtained in the range of 300-800 microg/mL (NS), 15-32 microg/mL (PE), 16-32 microg/mL (CPM) and 30-180 microg/mL (CF), respectively. The results of analysis have been well validated according to guidelines of International Conference of Harmonisation of technical requirements for registration of pharmaceuticals for human use. The method was found to be simple, precise, economical, less time consuming and reproducible. Hence, the suggested procedure could be used for the determination of all the four drugs in commercial preparations. PMID:23285660

  5. Rapid Discrimination of Chlorpheniramine Maleate and Assessment of Its Surface Content Uniformity in a Pharmaceutical Formulation by NIR-CI Coupled with Statistical Measurement

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    Luwei Zhou

    2014-01-01

    Full Text Available This study demonstrated that near infrared chemical imaging (NIR-CI was a rapid and nondestructive technique for discrimination of chlorpheniramine maleate (CPM and assessment of its surface content uniformity (SCU in a pharmaceutical formulation. The characteristic wavenumber method was used for discriminating CPM distribution on the tablet surface. To assess the surface content uniformity of CPM, binary image and statistical measurement were proposed. Furthermore, high-performance liquid chromatography (HPLC was used as reference method for accurately determining volume content of CPM in the sample. Moreover, HPLC was performed to assess volume content uniformity (VCU of CPM in whole region and part region of the tablets. The NIR-CI result showed that the spatial distribution of CPM was heterogeneous on the tablet surface. Through the comparison of content uniformity of CPM determined by NIR-CI and HPLC, respectively, it demonstrated that a high degree of VCU did not imply a high degree of SCU of the samples. These results indicate that HPLC method is not suitable for testing SCU, and this has been verified by NIR-CI. This study proves the feasibility of NIR-CI for rapid discrimination of CPM and assessment of its SCU, which is helpful for the quality control of commercial CPM tablets.

  6. 愈酚茶碱那敏片质量标准的改进研究%Study on the Improvement of Standard of Guaiacol Theophylline and Chlorpheniramine Maleate Tablets

    Institute of Scientific and Technical Information of China (English)

    冯国

    2014-01-01

    Objective To improve the standard of Guaiacol Theophylline and Chlorpheniramine Maleate Tablets and to establish an HPLC method for the assay of theophylline, guaifenesin and chlorpheniramine maleate in Guaiacol Theophylline and Chlorpheniramine Maleate Tablets.Methods The procedure was performed on the Insteril C8-3 column (250 mm×4.6 mm,5 μm)at 30 ℃,detected at 223 nm.The mobile phase was composed of 0.5% phosphate solution (in which 0.5% of triethylamine was added and the pH was adjusted to 5.5 by ammonia)and methanol (55 ∶ 45 ),fluxed at a rate of 1.0 mL·min-1 .Results Theophylline,guaifenesin and chlorpheniramine maleate were in good linear in the range of 0.097 5-1.560 0 μg (r=0.999 8),0.053 8-0.860 8 μg (r=1.000 0),0.050 9-0.815 1 μg (r=0.999 9),respectively.The mean recoveries were 99.31%,99.39%,99.27% with the RSD 0.55%, 0.68% and 0.44% (n = 9 ). Conclusion The method is proved to be simple, rapid and accurate, appropriate for the assay of theophylline, guaifenesin and chlorpheniramine maleate in Guaiacol Theophylline and Chlorpheniramine Maleate Tablets,and it can provide a reference for the improvement of current standard.%目的:改进愈酚茶碱那敏片质量标准,建立 HPLC 测定愈酚茶碱那敏片中茶碱、愈创甘油醚和马来酸氯苯那敏含量的方法。方法采用 Insteril C8-3色谱柱(250 mm×4.6 mm,5μm),流动相:0.5%磷酸溶液(0.5%三乙胺,氨水调 pH 至5.5)-甲醇(55∶45),柱温:30℃,检测波长:223 nm,流速:1.0 mL·min-1。结果茶碱、愈创甘油醚、马来酸氯苯那敏分别在0.0975~1.5600μg (r =0.9998)、0.0538~0.8608μg (r=1.0000)、0.0509~0.8151μg (r=0.9999)范围内线性关系良好,平均回收率分别为99.31%、99.39%、99.27%,RSD 分别为0.55%、0.68%、0.44%(n=9)。结论经方法学验证,所建立方法可用于愈酚茶碱那敏片中愈创甘油醚、茶碱和马来酸氯苯那敏的含量测定,为现行标准改进提供参考。

  7. Enhancement of on chip chemiluminescence signal intensity of tris(1,10-phenanthroline)-ruthenium(II) peroxydisulphate system for analysis of chlorpheniramine maleate in pharmaceutical formulations.

    Science.gov (United States)

    Al Lawati, Haider A J; Suliman, Fakhr Eldin O; Al Kindy, Salma M Z; Al-Lawati, Ali M; Varma, Gouri B; Nour, Imad Eldin M

    2010-10-15

    The effect of detection chip geometry on chemiluminescence (CL) signal intensity of tris(1,10-phenanthroline)-ruthenium(II) peroxydisulphate system for analysis of chlorpheniramine maleate (CPM) in pharmaceutical formulations was investigated. It was observed that the design of the detection chip is very crucial and can play an important role in enhancing the CL signal intensity in this system. The CL signal intensity was enhanced 250% when a teardrop micromixer chip was used, compared to the commonly used serpentine chip geometry. The study was conducted using a multi-chip device. In this device, chip 1 was used to prepare and pump the reagent mixture, whereas chip 3 was used for pumping the sample. The two chips were connected to the teardrop chip (2) via silica capillary where detection took place. Non-linear regression curve fitting of the calibration data revealed that the calibration curves are best described by third order polynomial equation with excellent correlation coefficients (R(2)=0.9998) for the concentration range 7.69 × 10(-8) to 5.12 ×1 0(-5)mol L(-1). A linear response is also observed over the range 7.69 × 10(-8) to 1.28 × 10(-5)mol L(-1) (R(2)=0.9996) and the detection limit was found to be 5.49 × 10(-8)mol L(-1). The device was successfully used for the analysis of CPM in tablets and a multi-component cough syrup. Results were reproducible with relative standard deviation (RSD) of 0.6-1.1%. PMID:20875608

  8. 法莫替丁与扑尔敏联合应用治疗乙酸致胃溃疡的协同作用%Synergistic Action of Famotidine and Chlorpheniramine of Acetic Acid-induced Chronic Gastric Ulcer in Rats

    Institute of Scientific and Technical Information of China (English)

    陈超; 覃珍

    2005-01-01

    Objective: Previous work demonstrates that H2 receptors antagonist shows gastroprotective effect in the ethanol, aspirin and pilorous ligature-induced gastric ulcer in rats as well as in the ethanol/hydrochloric acid-induced ulcer in rats ,and H1-receptor antagonists have been reported to be potent anti-inflammatory compounds. The aim of the present study was designed to assess the synergistic action of famotidine and chlorpheniramine in the acetic acid-induced chronic gastric ulcer model in rats. Methods:Chronic gastric lesions were induced in male Sprague-Dawley rats with serosal application of acetic acid. 40 SD rats were randomly divided into 5 groups:blank group,control group, famotidine (FMD) group, chlorpheniramine (CPA) group and FMD+CPA group; Every group was given intraperitoneally(i.p.) distilled water 0.5 ml/100 g、the same volume of 0.9% saline、FMD4 mg/kg、CPA10mg/kg、FMD+CPA (the same dose) respectivedly daily for 10 days. On days 10,the ulcer area was determined by planimetry, The levels of MPO in the liver homogenation was measured by bio-chemical methods and the plasma levels of 6-keto-PGF1a and IL-8 by radio-immune assay methods.Results:although FMD or CPA alone possess a potent antiulcer or anti-inflammatory activity. The synergistic effects of FMD+CPA were confirmed in the lesion area, IL-8,6-keto-PGF1a and MPO. The effect of FMD+CPA was significantly different as compared to the control and FMD reducing the lesion area (mm2) from 40.18+/-2.6 in controls to 6.83+/-2.97,P0.05),FMD+ CPA联合组与CPA组、FMD组有显著差异性(P<0.05).但是FMD+ CPA联合组与FMD组的大鼠血浆IL-8及肝组织MPO相比要明显低IL-8,P<0.05;MPO,P<0.01,提示扑尔敏有抗炎作用. 结论:联合应用H1、H2受体阻滞剂治疗胃溃疡能取得良好的疗效,尤其抗炎作用显著差异性.其机制与减少炎症因子的产生,减少对胃黏膜的损伤,改善胃黏膜血流有关.

  9. Drug: D04447 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04447 Mixture, Drug Betamethasone ... - d-chlorpheniramine maleate mixt; Celestamine (TN) Betamethasone ... 45 Adrenal hormone preparations 2459 Others D04447 Betamethasone ... - d-chlorpheniramine maleate mixt Anatomical Thera ... amines R06AB54 Chlorphenamine, combinations D04447 Betamethasone ... - d-chlorpheniramine maleate mixt PubChem: 1739810 ...

  10. Drug: D04044 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04044 Mixture, Drug Chlorpheniramine maleate - acetaminophen ... - salicylamide - anhydrous caffein ... ixt; LL (TN) Chlorpheniramine maleate [DR:D00665], Acetaminophen ... [DR:D00217], Salicylamide [DR:D01811], Anhydrous c ... 4 Mixture of Chlorpheniramine maleate [DR:D00665], Acetaminophen ... [DR:D00217], Salicylamide [DR:D01811] and Anhydrou ...

  11. Assay of Maleate Chlorpheniramine in Zinc Compound Coth Particles by HPLC%HPLC测定复方锌布颗粒中马来酸氯苯那敏含量

    Institute of Scientific and Technical Information of China (English)

    王文鹏; 赵志强

    2014-01-01

    目的:建立复方锌布颗粒中马来酸氯苯那敏含量的HPLC测定方法.方法:采用高效液相色谱法,色谱柱为Water RP18色谱柱(250mm×4.6mm,5μm),流动相为乙腈:0.3%十二烷基硫酸钠溶液:磷酸(60:40:0.02)(用三乙胺调pH值至3.3±0,1),流速为1.0mL/min,柱温:35℃,检测波长为224nm.结果:平均回收率为99.7%,相对标准偏差(RSD)为1.2%,马来酸氯苯那敏的线性范围为2.016~100.8μg/mL,系统精密度为0.6%.结论:用HPLC测定复方锌布颗粒中马来酸氯苯那敏的含量可以用于复方锌布颗粒的质量控制.

  12. A comparative study of various therapeutic regimens in urticaria

    Directory of Open Access Journals (Sweden)

    Mukhopadhyay Amiyakumar

    1995-01-01

    Full Text Available 127 patients of urticaria were treated with chlorpheniramine maleate alone and in combination with cyproheptadine hydrochloride, ranitidine and doxepin and levamisole. Chlorpheniramine and doxepin combination showed a satisfactory result in 88.46% of patients. Overall study showed that a combination regimen is better than the antihistaminics alone. Drowsiness was the commonest side effect. Levamisole and chlorpheniramine maleate combination was found to be more effective than the antihimstamine alone.

  13. 78 FR 14217 - Control of Alcohol and Drug Use: Addition of Post-Accident Toxicological Testing for Non...

    Science.gov (United States)

    2013-03-05

    ... certain non-controlled substances with potentially impairing side effects (77 FR 29307). As discussed in... moving heavy machinery because of their potential sedating effects. Furthermore, even prescription and..., chlorpheniramine, bromenphiramine, and doxylamine'' (77 FR at 29308, emphasis added). As explained below,...

  14. Cypermethrin Poisoning and Anti-cholinergic Medication- A Case Report

    Directory of Open Access Journals (Sweden)

    Dr Sudip Parajuli

    2006-07-01

    Full Text Available A 30 years old male was brought to emergency department of Manipal Teaching Hospital, Pokhara, Nepal with alleged history of consumption of pyrethroid compound ‘cypermethrin’. It was found to be newer insecticide poisoning reported in Nepal. We reported this case to show effectiveness of anti-cholinergic like hyosciane and chlorpheniramine maleate in the treatment of cypermethrin poisoning.

  15. Central histaminergic system interplay with suppressive effects of immune challenge on food intake in chicken.

    Science.gov (United States)

    Zendehdel, M; Baghbanzadeh, A; Aghelkohan, P; Hassanpour, S

    2016-04-01

    The aim of the current study was to investigate the interaction of the lipopolysaccharide (LPS) and histaminergic systems on appetite regulation in broilers. Effects of intracerebroventricular (ICV) injection of α-fluoromethylhistidine (α-FMH, histidine decarboxylase inhibitor), chlorpheniramine (histamine H1 receptor antagonist), famotidine (histamine H2 receptor antagonist) and thioperamide (histamine H3 receptor antagonist) on LPS-induced hypophagia in broilers were studied. A total of 128 broilers were randomly allocated into 4 experiments (4 groups and 8 replications in each experiment). A cannula was surgically implanted into the lateral ventricle. In Experiment 1, broilers were ICV injected with LPS (20 ng) prior to α-FMH (250 nmol). In Experiment 2, chickens were ICV injected with LPS followed by chlorpheniramine (300 nmol). In Experiment 3, broilers were ICV injected with famotidine (82 nmol) after LPS (20 ng). In Experiment 4, ICV injection of LPS was followed by thioperamide (300 nmol). Then, cumulative food intake was recorded until 4 h post-injection. According to the results, LPS significantly decreased food intake. Chlorpheniramine significantly amplified food intake, and LPS-induced hypophagia was lessened by injection of chlorpheniramine. α-FMH, famotidine and thioperamide had no effect on LPS-induced hypophagia. These results suggest that there is an interaction between central LPS and the histaminergic system where LPS-induced hypophagia is mediated by H1 histamine receptors in 3 h food-deprived broilers. PMID:26924422

  16. Effects of histamine and antihistamines on the kinetics of carbon dioxide in the rat

    Energy Technology Data Exchange (ETDEWEB)

    Russell, J.C.; Chambers, M.M.

    1981-01-01

    We have investigated the effects of chlorpheniramine (an H1 histamine inhibitor) and metiamide (an H2 inhibitor) on response to 14C pulse-labeling of carbon dioxide in the rat in the presence and absence of histamine. Neither chlorpheniramine nor metiamide alone had any effect upon the gastric venous/arterial ratio (VG/A) or the peripheral venous/arterial ratio (Vp/A). As in the case with no drug present, Vp/A rose with time following pulse-labeling to a value of 1.15-1.20. The presence of a preexisting steady-state infusion of histamine caused no changes in the ratios in the presence or absence of the inhibitors. The inhibitors did completely abolish the oscillations of both VG/A and Vp/A caused by initiation of histamine infusion coincident with the pulse-labeling. The results suggest that the histamine effects are largely mediated through H1 receptors.

  17. The interaction between histamine H1 receptor and μ- opioid receptor in scratching behavior in ICR mice.

    Science.gov (United States)

    Nakasone, Tasuku; Sugimoto, Yumi; Kamei, Chiaki

    2016-04-15

    In this study, we examined the interaction between histamine H1 receptor and μ-opioid receptor in scratching behavior in ICR mice. Both histamine and morphine caused scratching and simultaneous injection of histamine and morphine had an additive effect. Chlorpheniramine and naloxone inhibited histamine-induced scratching behavior. These two drugs also inhibited morphine-induced scratching behavior. Simultaneous injection of chlorpheniramine and naloxone caused a significant inhibition of histamine-induced scratching compared with separate injections. The same findings were also noted for morphine-induced scratching. These results strongly indicate a close relationship between histamine H1 receptor and μ-opioid receptor in scratching behavior in ICR mice. PMID:26948312

  18. Effects of histamine and antihistamines on the kinetics of carbon dioxide in the rat

    International Nuclear Information System (INIS)

    We have investigated the effects of chlorpheniramine (an H1 histamine inhibitor) and metiamide (an H2 inhibitor) on response to 14C pulse-labeling of carbon dioxide in the rat in the presence and absence of histamine. Neither chlorpheniramine nor metiamide alone had any effect upon the gastric venous/arterial ratio (VG/A) or the peripheral venous/arterial ratio (Vp/A). As in the case with no drug present, Vp/A rose with time following pulse-labeling to a value of 1.15-1.20. The presence of a preexisting steady-state infusion of histamine caused no changes in the ratios in the presence or absence of the inhibitors. The inhibitors did completely abolish the oscillations of both VG/A and Vp/A caused by initiation of histamine infusion coincident with the pulse-labeling. The results suggest that the histamine effects are largely mediated through H1 receptors

  19. Prophylaxis of anaphylactoid reactions to a polypeptidal plasma substitute by H1- plus H2-receptor antagonists: synopsis of three randomized controlled trials

    OpenAIRE

    Schöning, B.; Lorenz, Wilfried; Doenicke, A.

    1982-01-01

    To demonstrate the efficacy of a premedication with H1- + H2-receptor antagonists against histamine-release responses in anaesthesia and surgery 3 randomized controlled trials were conducted in patients, volunteers and experimental animals (dogs). Cutaneous anaphylactoid reactions following infusion of polygeline (Haemaccel) in orthopedic patients were successfully abolished by premedication with 0.1 mg/kg dimethpyrindene (Fenistil) and 5 mg/kg cimetidine (Tagamet). Chlorpheniramine (Piriton)...

  20. Excitatory effect of Clostridium perfringens alpha toxin on the rat isolated aorta.

    OpenAIRE

    Fujii, Y.; Nomura, S; Oshita, Y.; Sakurai, J

    1986-01-01

    Clostridium perfringens alpha toxin caused contraction of the isolated aorta of the rat in a dose-dependent manner. The contractile action caused by the toxin was inhibited or abolished by calcium antagonists such as nifedipine, verapamil and cinnarizine, or a Ca-free medium, but was not affected by phentolamine, chlorpheniramine, atropine, tetrodotoxin or a low Na medium. The toxin stimulated Ca uptake into the aorta in a dose-dependent manner. 8-N,N'-diethylaminooctyl-3,4,5-trimethoxybenzoa...

  1. The histomine H1 receptor is not involved in local control of mammary blood flow in dairy cows

    OpenAIRE

    Madsen, Torben Gosvig; Trout, D.R.; Cieslar, S.R.L.; Purdie, N.G.; Nielsen, Mette Benedicte Olaf; Cant, J.P.

    2008-01-01

    Low concentrations of the essential amino acid histidine in circulation have been shown to increase mammary blood flow and it has been suggested that this effect is mediated by histamine. The hypotheses tested in this experiment were that interstitial histamine concentrations in the mammary gland are related to arterial His concentrations and that mammary blood flow is reduced by extracellular histamine via H(1) receptors. The hypotheses were tested by infusing saline or chlorpheniramine, a b...

  2. The central effect of biological Amines on immunosuppressive effect of restraint stress in rat

    OpenAIRE

    Zeraati F; Ghafghazi T.; Adib M; Rezaei A

    2000-01-01

    The effects of some histaminergic agents were evaluated on stress- induced immunosuppression in immunized nale rats. In rat immunized with sheep red blood cells ( SRBCs). Restraint stress (RS) prevented the booster-induced rise in anti-SRBC antibody titre and cell immunity response. Intracerebroventicular (I.C>V) injection of histamine (150 µg/rat) induced a similar effect with RS. Pretreatment with chlorpheniramine (50 µg/rat) reduced the inhibitory effect of Ras on immune function. Also ...

  3. [Clinical study of BRON-L syrup (cough suppressant) abuse].

    Science.gov (United States)

    Miyatake, Ryosuke; Doi, Tomoko; Date, Kenji; Naitoh, Tomomichi; Suwaki, Hiroshi

    2002-02-01

    In 1980s, abuse and dependence of BRON-W syrup (cough suppressant), which contains methylephedrine, dihydrocodeine, chlorpheniramine and caffeine, were prevalent in Japan. Pharmacological and clinical studies suggest that methylephedrine and dihydrocodeine cause dependence. Although BRON-L syrup, newly modified cough suppressant contains only chlorpheniramine and caffeine, there still are abuse and dependence of this drug. In this report, three cases of BRON-L syrup abuse are demonstrated. All cases started using BRON-L syrup in the late teens in their peer groups, and dropped out from school. Case 1 misused only BRON-L syrup, but case 2 and 3 were multi-drug abusers (case 2: amphetamine, cocaine, and marijuana, case 3: solvent, alcohol, bromovalerylurea), and had kept in tough with the peer groups. Case 2 and 3 hospitalized more than 2 times. Withdrawal symptoms, such as headache, insomnia, and irritability were mild and improved in a few weeks after drug use was stopped. These findings suggest that 1) psychosocial backgrounds of these cases are in common with those of BRON-W syrup abusers, but 2) the clinical course and prognosis of multi-drug abusers are different from the BRON single abuser, 3) chlorpheniramine and caffeine possibly cause dependence, 4) abusers are likely to choose BRON brand although two main dependence-producing constituents are removed from it now. Therefore, prevention and care of BRON-L abusers requires both psychosocial and pharmacological aspects. PMID:11915306

  4. A kinetic study of the antihistaminic effect of terfenadine.

    Science.gov (United States)

    Cheng, H C; Woodward, J K

    1982-01-01

    Kinetics of the antihistaminic effect of alpha-[4-(1,1-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1- piperidinebutanol (terfenadine, RMI 9918, Triludan, Teldane, resp.) were examined in the isolated guinea pig ileum and spirally cut tracheal strip preparations. In the isolated guinea pig ileum, terfenadine produced a parallel or competitive shift (3.16 X 10(-8) and 10(-7) mol/l) as well as a nonparallel or unsurmountable shift (3.16 X 10(-7) and 10(-6) mol/l) of the histamine dose response curves. Using the dose ratio test, it was concluded that terfenadine competes at the same receptors as chlorpheniramine, namely, the histamine H1-receptors. The antihistaminic effects of terfenadine, both the competitive and unsurmountable effects, were difficult to reverse by washout techniques whereas the nonspecific effects (against acetylcholine and barium chloride) could be readily washed out. The unsurmountable antagonism of histamine by terfenadine may result from a slow dissociation of terfenadine from the histamine H1-receptor. When terfenadine (2 mg/kg) or chlorpheniramine (2 mg/kg) was administered systemically, either orally or intraperitoneally, to guinea pigs and the antihistaminic effect assessed in vitro (isolated ileal strips and tracheal strips) terfenadine consistently produced a longer duration of action than chlorpheniramine. It is concluded that terfenadine is a potent, selective histamine H1-receptor antagonist; the kinetics of association/dissociation of terfenadine with histamine H1-receptors may account for the long-lasting antihistaminic effect in various animal models. PMID:6129862

  5. The effect of intracerebroventricular injection of histamine in visceral nociception induced by acetic acid in rats

    Directory of Open Access Journals (Sweden)

    Zanboori Ali

    2010-01-01

    Full Text Available Objective : This study was designed to investigate the role of brain histamine and H1 and H2 receptors in mediating the central perception of visceral pain in rats. Materials and Methods : In conscious rats implanted with a lateral brain ventricle cannula, the effect of intracerebroventricular (i.c.v. injection of histamine (2.5, 10, and 40 μg, and chlorpheniramine and ranitidine at the same doses of 5, 20, and 80 μg were investigated on visceral pain. Visceral nociception induced by intraperitoneal (i.p. injection of acetic acid (1 mL, 1%, and the number of complete abdominal wall muscle contractions accompanied with stretching of hind limbs (writhes were counted for 1 h. Results : Histamine at doses of 10 and 40 μg and chlorpheniramine and ranitidine at the same doses of 20 and 80 μg, significantly decreased the numbers of writhes (P < 0.05. Pretreatment with chlorpheniramine and ranitidine at the same dose of 80 μg, significantly prevented histamine (40 μg-induced antinociception (P < 0.05. Conclusion : The results of this study suggest that brain histamine may be involved in modulation of visceral antinociception through both central H 1 and H 2 receptors.

  6. The central effect of biological Amines on immunosuppressive effect of restraint stress in rat

    Directory of Open Access Journals (Sweden)

    Zeraati F

    2000-10-01

    Full Text Available The effects of some histaminergic agents were evaluated on stress- induced immunosuppression in immunized nale rats. In rat immunized with sheep red blood cells ( SRBCs. Restraint stress (RS prevented the booster-induced rise in anti-SRBC antibody titre and cell immunity response. Intracerebroventicular (I.C>V injection of histamine (150 µg/rat induced a similar effect with RS. Pretreatment with chlorpheniramine (50 µg/rat reduced the inhibitory effect of Ras on immune function. Also histamine could inhibit the effect of RS on immune function. Also histamine could inhibitory the effect of chlorpheniramine when injected simultaneously. Pretreatment with ranidine (10 µg/rat had not a significant effect. Serotonin (3 µg/rat and dopamine (0.2 µg/rat could reverse the effects of chlorpheniromine when injected with chlorpheniramine (P<0.05. Epinephrine (0.2 µg/rat had not a significant effect. The results indicate that histamine mediates the immunosuppression of restraint stress by influencing the histamine H1 receptor in the brain and this effects of histamine may be modulated by serotoninergic and dopaminergic system.

  7. Effect of antihistaminic agents on the ATP-sensitive potassium channel activity in isolated mouse ventricular cardiomyocytes%组胺拮抗剂对小鼠ATP-敏感性钾离子通道的影响

    Institute of Scientific and Technical Information of China (English)

    朴伶华; 姜圣男; 柳贤德

    2013-01-01

    Objective The purpose of this study was to clarify the effect of the first generation histamine H1 receptor antagonists on adenosine triphosphate-sensitive potassium (KATP) channel in isolated mouse ventricular cardiomyocytes using excised inside-out and cell-attached patch clamp techniques. Methods Mouse heart ventricular cardiomyocytes were isolated, and excised inside-out and cell-attached patch clamp techniques were used to determine the effect of the antihistamines on the KATP channel activity. Results In the excised inside-out patch configuration, H1-antihistaminic agents (chlorpheniramine, pyrilamine and diphenhydramine), in a dose ranging from 1 to 100 μmol/L, inhibited KATP channel activity in a dose-dependent manner. The potency order reducing the channel activity was pyrilamine>diphenhydramine>chlorpheniramine. All the three antihistamines (100 μmol/L) also inhibited pinacidil-induced KATP channel activity in the cell-attached patch configuration. The potency order of the three antihistamines inhibiting KATP channel activity was pyrilamine>chlorpheniramine>diphenhydramine in the cell-attached configurations. Histamine did not affect the pinacidil-induced KATP channel activity by itself, in addition, did not influence the effects elicited by the three antihistamines on pinacidil-induced KATP channel activity in the cell-attached patches. Conclusions It is concluded that the first generation histamine H1 receptor antagonists are involved in the regulation of ATP-sensitive potassium channel activity in the mouse cardiac ventricular myocytes, and that the inhibitory action of the antihistaminic agents on the channel is not dependent on H1-receptors.%目的 观察比较3种组胺拮抗剂对缺血性心肌细胞的ATP-敏感性钾离子通道中的影响.方法 利用急性酶解法分离小鼠心室肌细胞.结果 组胺拮抗剂pyrilamine、chlorpheniramine及diphenhydramine均可抑制ATP-敏感性钾离子通道的活性,抑制程度为pyrilamine

  8. Crocin alleviates the local paw edema induced by histamine in rats

    OpenAIRE

    Esmaeal Tamaddonfard; Amir Abbas Farshid; Leila Hosseini

    2012-01-01

    Objective: Crocin, as an active constituent of saffron, has many biological functions including antioxidant and anti-inflammatory activities. The present study was aimed to investigate the effects of crocin and chlorpheniramine on local edema induced by histamine. Materials and Methods: Local edema was induced by subcutaneous injection of histamine (100 μl, 0.1%) in ventral surface of right hind paw. The thickness of paw was measured at 1 h before and 1, 2, 3 h after injection of histamine, u...

  9. The histomine H1 receptor is not involved in local control of mammary blood flow in dairy cows

    DEFF Research Database (Denmark)

    Madsen, Torben Gosvig; Trout, D.R.; Cieslar, S.R.L.;

    2008-01-01

    Low concentrations of the essential amino acid histidine in circulation have been shown to increase mammary blood flow and it has been suggested that this effect is mediated by histamine. The hypotheses tested in this experiment were that interstitial histamine concentrations in the mammary gland...... arterial concentrations and mammary uptakes of acetate. The efficiency of plasma triacylglycerol uptake across the mammary glands was decreased by chlorpheniramine but net uptake of long-chain fatty acids was not affected. The mechanism by which an amino acid deficiency influences mammary blood flow does...

  10. Scintigraphic assessment of the in vivo dissolution rate of a sustained release tablet

    International Nuclear Information System (INIS)

    The release of [sup(99m)Tc]diethylenetriaminepentaacetic acid ([sup(99m)Tc]DTPA) from a matrix tablet formulation was measured by external scintigraphy in 4 healthy male volunteers. The rate determined was compared with that observed in vitro using a U.S.P. dissolution apparatus. The in vitro release rate of [sup(99m)Tc]DTPA was similar to that of chlorpheniramine, and therefore the labelled compound was used to model the release of this drug in vivo. The in vitro release of [sup(99m)Tc]DTPA was pH-independent. (Auth.)

  11. Kid Goats are More Sensitive to Penicillin Overdose

    OpenAIRE

    A.A. Nikvand; H. Najafzadeh

    2011-01-01

    Hipracilina suspension contains benzyl penicillin (200000I U), dihydrostreptomycin sulfate (250 mg), chlorpheniramine maleate (15 mg) and dexamethasone sodium phosphate (0.6 mg). This drug is used for treatment infection in respiratory, urinary, reproductive, forelimb and hind limb systems in cattle, goats, sheep and rabbits. Hipracilina is intramuscularly injected at dose 1 mL/10 kg body weight once or twice in day for 3 days. Hipracilina was clinically used at dose 1.5 mL/B.W in kid goats. ...

  12. Involvement of histamine released from mast cells in acute radiation dermatitis in mice

    International Nuclear Information System (INIS)

    A possible involvement of histamine in acute radiation dermatitis in mice was investigated. The dose of 40 Gy of gamma irradiation induced erythema and edema in C57BL/6 mice treated with vehicle. However, in C57BL/6 mice treated with chlorpheniramine and WBB6F1-W/WV mice, erythema and edema were not observed. In all of these mice, epilation and dry desquamation were induced, but bepotastine significantly reduced the extent of these areas. These results suggest that gamma irradiation-induced erythema and edema were caused by histamine released from mast cells via histamine H1 receptor, and epilation was induced by other inflammatory mediators. (author)

  13. Kid Goats are More Sensitive to Penicillin Overdose

    Directory of Open Access Journals (Sweden)

    A.A. Nikvand

    2011-10-01

    Full Text Available Hipracilina suspension contains benzyl penicillin (200000I U, dihydrostreptomycin sulfate (250 mg, chlorpheniramine maleate (15 mg and dexamethasone sodium phosphate (0.6 mg. This drug is used for treatment infection in respiratory, urinary, reproductive, forelimb and hind limb systems in cattle, goats, sheep and rabbits. Hipracilina is intramuscularly injected at dose 1 mL/10 kg body weight once or twice in day for 3 days. Hipracilina was clinically used at dose 1.5 mL/B.W in kid goats. The kids had 6 days age and 3kg weight. These animals had diarrhea after high milk eating. One kids died after 15 min. Fourteen kids had signs such as ataxia, depression, hind limb paralysis, hyperesthesia, mydriasis, decreasing of respiratory rate, tachycardia and falling. Two kids died after 4 h. Supportive treatment was carried by ORS powder and furosemide administration. The kids returned to normal state after 24 h. In another experimental study we divided kids 3 groups which received A: benzyl penicillin, B: benzyl penicillin+dihydrostreptomycin, and C: chlorpheniramine. Group A and B showed depression. Thus, Hipracilina can be toxic in kid goats at nearly 4-5 folds dose. It seems that this toxicity is related to penicillin compound.

  14. Optimization of wavelength range and data interval in chemometric analysis of complex pharmaceutical mixtures

    Directory of Open Access Journals (Sweden)

    Michele De Luca

    2016-02-01

    Full Text Available The performance of different chemometric approaches was evaluated in the spectrophotometric determination of pharmaceutical mixtures characterized by having the amount of components with a very high ratio. Principal component regression (PCR, partial least squares with one dependent variable (PLS1 or multi-dependent variables (PLS2, and multivariate curve resolution (MCR were applied to the spectral data of a ternary mixture containing paracetamol, sodium ascorbate and chlorpheniramine (150:140:1, m/m/m, and a quaternary mixture containing paracetamol, caffeine, phenylephrine and chlorpheniramine (125:6. 25:1.25:1, m/m/m/m. The UV spectra of the calibration samples in the range of 200–320 nm were pre-treated by removing noise and useless data, and the wavelength regions having the most useful analytical information were selected using the regression coefficients calculated in the multivariate modeling. All the defined chemometric models were validated on external sample sets and then applied to commercial pharmaceutical formulations. Different data intervals, fixed at 0.5, 1.0, and 2.0 point/nm, were tested to optimize the prediction ability of the models. The best results were obtained using the PLS1calibration models and the quantification of the species of a lower amount was significantly improved by adopting 0.5 data interval, which showed accuracy between 94.24% and 107.76%.

  15. Capillary electrophoretic enantioseparation of basic drugs using a new single-isomer cyclodextrin derivative and theoretical study of the chiral recognition mechanism.

    Science.gov (United States)

    Liu, Yongjing; Deng, Miaoduo; Yu, Jia; Jiang, Zhen; Guo, Xingjie

    2016-05-01

    A novel single-isomer cyclodextrin derivative, heptakis {2,6-di-O-[3-(1,3-dicarboxyl propylamino)-2-hydroxypropyl]}-β-cyclodextrin (glutamic acid-β-cyclodextrin) was synthesized and used as a chiral selector in capillary electrophoresis for the enantioseparation of 12 basic drugs, including terbutaline, clorprenaline, tulobuterol, clenbuterol, procaterol, carvedilol, econazole, miconazole, homatropine methyl bromide, brompheniramine, chlorpheniramine and pheniramine. The primary factors affecting separation efficiency, which include the background electrolyte pH, the concentration of glutamic acid-β-cyclodextrin and phosphate buffer concentration, were investigated. Satisfactory enantioseparations were obtained using an uncoated fused-silica capillary of 50 cm (effective length 40 cm) × 50 μm id with 120 mM phosphate buffer (pH 2.5-4.0) containing 0.5-4.5 mM glutamic acid-β-cyclodextrin as background electrolyte. A voltage of 20 kV was applied and the capillary temperature was kept at 20°C. The results proved that glutamic acid-β-cyclodextrin was an effective chiral selector for studied 12 basic drugs. Moreover, the possible chiral recognition mechanism of brompheniramine, chlorpheniramine and pheniramine on glutamic acid-β-cyclodextrin was investigated using the semi-empirical Parametric Method 3. PMID:26935589

  16. Effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin on scratching behavior in mice.

    Science.gov (United States)

    Ono, Rie; Kagawa, Yoto; Takahashi, Yuji; Akagi, Masaki; Kamei, Chiaki

    2010-03-01

    The present study was performed to study the effect of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) on scratching behavior in hairless mice, which are highly sensitive to pruritogens (mediators causing itching), except for histamine, and are suitable for time-course studies due to their hairless skin. TCDD is a well-known environmental pollutant that causes skin diseases with itching; therefore, we examined whether TCDD induced itching. Oral administration of TCDD caused no increase in scratching behavior when used alone, whereas TCDD in combination with distilled water or acetone/olive oil application caused a significant increase in scratching behavior. Furthermore, nerve growth factor (NGF) content in the skin increased significantly. A single administration of chlorpheniramine (histamine H1 receptor antagonist), tranilast (chemical mediator release inhibitor) and olopatadine (histamine H1 receptor antagonist) had no effect on scratching behavior induced by TCDD in combination with acetone/olive oil application. With repeated administration for 7 days, chlorpheniramine and tranilast had no effect on scratching behavior, whereas olopatadine significantly inhibited scratching behavior. In addition, only olopatadine significantly inhibited NGF content in the skin. From these findings, it can be concluded that TCDD is not a pruritogen but causes alloknesis (itchy skin) with the simultaneous use of trivial external stimulation. In addition, it was found that drugs which decreased skin NGF contents may inhibit this scratching behavior. PMID:19969104

  17. Thermodynamic and transport properties of some biologically active compounds in aqueous solutions at different temperatures

    Energy Technology Data Exchange (ETDEWEB)

    Dhondge, Sudhakar S., E-mail: s_dhondge@hotmail.co [P.G. Department of Chemistry, S.K. Porwal College, Kamptee, Nagpur 441 002 (India); Zodape, Sangesh P.; Parwate, Dilip V. [Department of Chemistry, R.T.M. Nagpur University, Nagpur 440 033 (India)

    2011-01-15

    The experimental data of density and viscosity have been obtained for aqueous solutions of biologically active compounds like salbutamol sulphate (SS), diethylcarbamazine citrate (DEC), and chlorpheniramine maleate (CPM) in the concentration range (0 to 0.15) mol . kg{sup -1} at three different temperatures. The derived parameters, such as apparent molar volume of solute ({phi}{sub V})), limiting apparent molar volume of solute ({phi}{sub V}{sup 0}), limiting apparent molar expansivity ({phi}{sub E}{sup 0}), thermal expansion coefficient ({alpha}*) and Jones-Dole equation viscosity A and B coefficients, were obtained using the density and viscosity results. It has been observed that the electrolyte-salt (SS) as well as adducts exhibit a positive viscosity B coefficient having negative ((dB)/(dT)). These results are interpreted in the light of possible solute-solute and solute-solvent interactions.

  18. TREATMENT OF 100 CASES OF ACUTE URTICARIA WITH ELECTROACUPUNCTURE

    Institute of Scientific and Technical Information of China (English)

    钟鸿; 武哲丽

    2004-01-01

    Objective: To observe the therapeutic effect of clinical treatment of acute urticaria chiefly by electroacupuncture (EA). Methods: A total of 180 outpatients with acute urticaria were randomized into treatment group and control group. 100 cases in the treatment group were were managed by chlorpheniramine maleate and Vitamin C. Results: After 3 days' treatment, of the 100 and 80 cases in treatment and control groups, 79 and 53 were cured, 10 and 6 markedly effective, 5 and 8 effective, and 6 and 13 failed, with the effective rates being 94.00% and 83.75% respectively. The therapeutic effect of electroacupunture was significantly superior to that of medication(P<0.05). Conclusion: The was a more effective therapy for acute urticaria.

  19. Dramatic Clinical Response of Relapsed Metastatic Extramammary Paget’s Disease to Trastuzumab Monotherapy

    Directory of Open Access Journals (Sweden)

    S. Wakabayashi

    2012-01-01

    Full Text Available We report the first case of 68-year-old Japanese woman with metastatic HER2-positive extramammary Paget’s disease that showed the validity of trastuzumab monotherapy. We administered trastuzumab at a loading dose of 8 mg/kg i.v., followed by a 6 mg/kg maintenance dose every three weeks according to a protocol for HER2-positive metastatic breast cancers and a near-complete response was achieved after the tenth infusion. The patient experienced a moderate headache and flushing during the first infusion, but had no advanced effects during subsequent infusions with ibuprofen and d-chlorpheniramine maleate. Given the dramatic response, the patient has had 17 infusions of trastuzumab with no disease progression. Thus, trastuzumab has few side effects and is well tolerated for elderly patients. It may become a new choice of the adjubant therapy of this disease.

  20. Thermodynamic and transport properties of some biologically active compounds in aqueous solutions at different temperatures

    International Nuclear Information System (INIS)

    The experimental data of density and viscosity have been obtained for aqueous solutions of biologically active compounds like salbutamol sulphate (SS), diethylcarbamazine citrate (DEC), and chlorpheniramine maleate (CPM) in the concentration range (0 to 0.15) mol . kg-1 at three different temperatures. The derived parameters, such as apparent molar volume of solute (φV)), limiting apparent molar volume of solute (φV0), limiting apparent molar expansivity (φE0), thermal expansion coefficient (α*) and Jones-Dole equation viscosity A and B coefficients, were obtained using the density and viscosity results. It has been observed that the electrolyte-salt (SS) as well as adducts exhibit a positive viscosity B coefficient having negative ((dB)/(dT) ). These results are interpreted in the light of possible solute-solute and solute-solvent interactions.

  1. Evaluation of histamine induced acute inflammation by 67Ga-citrate in conscious rats

    International Nuclear Information System (INIS)

    Radioactivity of 67Ga in the paw edema and the edema rate were measured after subcutaneous injection of histamine into the paw of the conscious rat. The radioactivity increased almost parallel with the edema rate following the injection of histamine. The increase in the radioactivity and edema were almost completely prevented by pretreatment with a 10 mg/kg dose of chlorpheniramine, an antihistaminic agent. A good correlation between the edema rate and the radioactivity was demonstrated. These results suggest that 67Ga-citrate is useful for monitoring the process of acute inflammation in the pharmacological evaluation of anti inflammatory drugs. Moreover, there is also a possibility that 67Ga-citrate may be useful in measuring vascular permeability. (orig.)

  2. Studies on in vitro release of CPM from semi-interpenetrating polymer network (IPN) composed of chitosan and glutamic acid

    Indian Academy of Sciences (India)

    K Kumari; P P Kundu

    2008-04-01

    Interpenetrating polymer network (IPN) beads consisting of chitosan–glutamic acid were prepared for in vitro study of controlled release of chlorpheniramine maleate (CPM). A viscous solution of chitosan–glutamic acid was prepared in 2% acetic acid solution, extruded as droplets through a syringe to alkali–methanol solution and the precipitated beads were crosslinked using glutaraldehyde solution. Swelling and drug release studies were carried out. Transport of release medium through the semi-IPN depended upon its pH and extent of crosslinking. The structural and morphological studies of beads were carried out by using a scanning electron microscope (SEM). The larger surface area of beads as well as their ease of handling makes them ideal agents of controlled release.

  3. Oral eosinophilic granulomas in tigers (Panthera tigris)--a collection of 16 cases.

    Science.gov (United States)

    Sykes, John M; Garner, Michael M; Greer, Leah L; Lung, Nancy P; Coke, Rob L; Ridgley, Frank; Bush, Mitch; Montali, Richard J; Okimoto, Ben; Schmidt, Robert; Allen, Jack L; Rideout, Bruce A; Pesavento, Patricia A; Ramsay, Edward C

    2007-06-01

    Oral eosinophilic granulomas were diagnosed in 16 tigers (Panthera tigris). All lesions were located on the hard or soft palate and typically consisted of flat or slightly raised circular ulcers. Histologic features of these lesions were essentially identical to those seen in oral eosinophilic granulomas of domestic cats and dogs. No clinical signs were noted in eight cases, though various degrees of inappetence, excessive salivation, and dysphagia were noted in the other eight tigers. Six cases were not treated. Treatment for the remaining 10 cases centered on corticosteroids and additional treatments included surgical removal, cryotherapy, antibiotics, and chlorpheniramine. Treatment with corticosteroids did appear to be effective in some cases, though lesions would worsen after cessation of therapy and no cases were cured. In addition, three cases developed complications possibly related to this corticosteroid therapy. The etiology of these lesions remains unknown, though an underlying allergic condition is likely. PMID:17679515

  4. Quantitation of cutaneous inflammation induced by reactive species generated by UV-visible irradiation of rose bengal

    International Nuclear Information System (INIS)

    The present studies were undertaken to quantitate the initial inflammatory response produced by the photo-generated reactive species in rabbit skin. Rose bengal (RB), a photosensitizer dye, was injected into the skin sites at various concentrations and exposed to UV-visible light for 30-120 min. The increase in vascular permeability and the accumulation of PMNs were investigated using 125I-labeled albumin and 51Cr-labeled PMNs. RB at a concentration of 1 nmol with 120-min exposure to light enhanced vascular permeability by 3.7 times and accumulation of PMNs by 3.3 times. As low as 0.01 nmol of RB produced discernible effects. beta-Carotene (0.1 nmole) inhibited the inflammatory response by 75-100%, suggesting that the reactive species involved in this response was predominantly singlet oxygen. The increase in vascular permeability was inhibited by 48-70% by 25 micrograms of chlorpheniramine maleate. It is therefore suggested that histamine plays a major role in the initial vascular response. The studies demonstrate that this rabbit model is suitable for the quantitation of photoinduced inflammatory response which is not observable by gross anatomic procedures

  5. A case of tongue edema associated with radiation-induced ulcer with low level of C1 inhibitor activity

    International Nuclear Information System (INIS)

    A 66-year-old man became aware of sudden swelling of the tongue with swallowing disturbance. He had a medical history of tongue cancer treated by interstitial radiotherapy and had undergone a cytological examination of an ulcer on the right side of the tongue three weeks earlier because of suspected recurrence. The cytological examination result was class I with no malignant findings. Angioneurotic edema, so-called ''Quincke's edema'', associated with radiation-induced ulcer of the tongue, was diagnosed. Tranexamic acid, d-chlorpheniramine maleate, and epinephrine were administered. After six days, the tongue edema had almost disappeared. Laboratory examination revealed a low level of C1 inhibitor activity with normal levels of CH50, C1, C3, and C4 at the time of swelling. Hereditary angioneurotic edema with absence of hereditary trait was suspected based on the sudden edema attack and low level of C1 inhibitor activity. The C1 inhibitor activity returned to normal after disappearance of the tongue edema. (author)

  6. Quantitation of cutaneous inflammation induced by reactive species generated by UV-visible irradiation of rose bengal

    Energy Technology Data Exchange (ETDEWEB)

    Ranadive, N.S.; Menon, I.A.; Shirwadkar, S.; Persad, S.D. (Univ. of Toronto, Ontario (Canada))

    1989-10-01

    The present studies were undertaken to quantitate the initial inflammatory response produced by the photo-generated reactive species in rabbit skin. Rose bengal (RB), a photosensitizer dye, was injected into the skin sites at various concentrations and exposed to UV-visible light for 30-120 min. The increase in vascular permeability and the accumulation of PMNs were investigated using 125I-labeled albumin and 51Cr-labeled PMNs. RB at a concentration of 1 nmol with 120-min exposure to light enhanced vascular permeability by 3.7 times and accumulation of PMNs by 3.3 times. As low as 0.01 nmol of RB produced discernible effects. beta-Carotene (0.1 nmole) inhibited the inflammatory response by 75-100%, suggesting that the reactive species involved in this response was predominantly singlet oxygen. The increase in vascular permeability was inhibited by 48-70% by 25 micrograms of chlorpheniramine maleate. It is therefore suggested that histamine plays a major role in the initial vascular response. The studies demonstrate that this rabbit model is suitable for the quantitation of photoinduced inflammatory response which is not observable by gross anatomic procedures.

  7. Liquid chromatography and chemometric-assisted spectrophotometric methods for the analysis of two multicomponent mixtures containing cough suppressant drugs.

    Science.gov (United States)

    El-Gindy, Alaa; Emara, Samy; Mesbah, Mostafa K; Hadad, Ghada M

    2005-01-01

    Three methods were applied for the analysis of 2 multicomponent mixtures containing dextromethorphan hydrobromide, phenylephrine hydrochloride, chlorpheniramine maleate, methylparaben, and propylparaben, together with either sodium benzoate (Mix 1) or ephedrine hydrochloride and benzoic acid (Mix 2). In the first method, liquid chromatography was used for their simultaneous determination using an ODS column with a mobile phase consisting of acetonitrile-phosphate buffer, pH 2.7 (40 + 60, v/v), containing 5mM heptanesulfonic acid sodium salt and ultraviolet (UV) detection at 214 nm. Also, 2 chemometric methods, principal component regression, and partial least squares were used. For both chemometric calibrations, a concentration set of the mixture consisting of each compound in each mixture was prepared in distilled water. The absorbance data in the UV spectra were measured for the 76 or 71 wavelength points in the spectral region 210-240 or 210-224 nm considering the intervals of deltagamma = 0.4 or 0.2 nm for Mix 1 and Mix 2, respectively. The 2 chemometric methods did not require any separation step. These methods were successfully applied for the analysis of the 2 multicomponent combinations in synthetic mixtures and in commercial syrups, and the results were compared with each other. PMID:16152922

  8. The simultaneous determination of active ingredients in cough-cold mixtures by isocratic reversed-phase ion-pair high-performance liquid chromatography.

    Science.gov (United States)

    Lau, O W; Chan, K; Lau, Y K; Wong, W C

    1989-01-01

    A simple, rapid and accurate method for the simultaneous determination of active ingredients in cough-cold mixtures using isocratic reversed-phase ion-pair high-performance liquid chromatography has been developed. It involves the use of an octadecylsilane column as the stationary phase with methanol, water, tetrahydrofuran, phosphoric acid mixtures as mobile phase including sodium dioctylsulphosuccinate as the ion-pair agent. The pH of the mobile phase was adjusted to 4.6 by means of phosphoric acid and ammonium hydroxide solutions. The proposed method involves the simple dilution of the samples with the mobile phase and the addition of metoclopramide hydrochloride as the internal standard. The active ingredients under investigation were chlorpheniramine, codeine, diphenhydramine, ephedrine, ethylmorphine, phenylephrine, phenylpropanolamine and pholcodine, which exist as various combinations in cough-cold mixtures. The optimum composition of the mobile phase and the optimum flow rate were determined and are reported. The method was applied to the determination of active ingredients in seven commercially available cough-cold mixtures. PMID:2577452

  9. Activation of the central histaminergic system mediates arachidonic-acid-induced cardiovascular effects.

    Science.gov (United States)

    Altinbas, Burcin; Topuz, Bora Burak; İlhan, Tuncay; Yilmaz, Mustafa Sertac; Erdost, Hatice; Yalcin, Murat

    2014-08-01

    The aim of this study was to explain the involvement of the central histaminergic system in arachidonic acid (AA)-induced cardiovascular effects in normotensive rats using hemodynamic, immunohistochemistry, and microdialysis studies. Intracerebroventricularly (i.c.v.) administered AA (0.25, 0.5, and 1.0 μmol) induced dose- and time-dependent increases in mean arterial pressure and decreased heart rate in conscious normotensive Sprague-Dawley rats. Central injection of AA (0.5 μmol) also increased posterior hypothalamic extracellular histamine levels and produced strong COX-1 but not COX-2 immunoreactivity in the posterior hypothalamus of rats. Moreover, the cardiovascular effects and COX-1 immunoreactivity in the posterior hypothalamus induced by AA (0.5 μmol; i.c.v.) were almost completely blocked by the H2 receptor antagonist ranitidine (50 and 100 nmol; i.c.v.) and partially blocked by the H1 receptor blocker chlorpheniramine (100 nmol; i.c.v.) and the H3-H4 receptor antagonist thioperamide (50 and 100 nmol; i.c.v.). In conclusion, these results indicate that centrally administered AA induces pressor and bradycardic responses in conscious rats. Moreover, we suggest that AA may activate histaminergic neurons and increase extracellular histamine levels, particularly in the posterior hypothalamus. Acting as a neurotransmitter, histamine is potentially involved in AA-induced cardiovascular effects under normotensive conditions. PMID:25065747

  10. Involvement of the histaminergic system in the resuscitating effect of centrally acting leptin in haemorrhagic shock in rats.

    Science.gov (United States)

    Jochem, J; Altinbas, B; Yalcin, M; Ottani, A; Giuliani, D; Savci, V; Kasperska-Zajac, A; Guarini, S

    2016-02-01

    Leptin, acting centrally as a neuromodulator, induces the activation of the sympathetic nervous system, which may lead to a pressor action in normotensive animals. In haemorrhagic shock, leptin administered intracerebroventricularly (icv.) evokes the resuscitating effect, with long-lasting rises in mean arterial pressure (MAP) and heart rate (HR), subsequent increase in peripheral blood flows, and a 100% survival at 2 h. Since leptin is able to activate histaminergic neurons, and centrally acting histamine also induces the resuscitating effect with the activation of the sympathetic nervous system, in the present study, we investigated an involvement of the histaminergic system in leptin-evoked cardiovascular effects in haemorrhagic shock. The model of irreversible haemorrhagic shock, with MAP decreased to and stabilised at 20 - 25 mmHg, has been used. Leptin (20 μg) given icv. at 5 min of critical hypotension evoked 181.5% increase in extracellular hypothalamic histamine concentration during the first 10 min after injection. Rises in MAP, HR and renal, mesenteric and hindquarters blood flows induced by leptin were inhibited by icv. pre-treatment with histamine H1 receptor antagonist chlorpheniramine (50 nmol). In contrast, there was no effect of H2, H3 and H4 receptor antagonists ranitidine (25 nmol), VUF 5681 (25 nmol) and JNJ 10191584 (25 nmol), respectively. In conclusion, the histaminergic system is involved in centrally-acting leptin-induced resuscitating effect in haemorrhagic shock in rats. PMID:27010896

  11. Effect of Taurine on The Respiratory System of Rats

    Directory of Open Access Journals (Sweden)

    Ammer E.M

    2013-08-01

    Full Text Available The present study was designed to investigate the effect of taurine on isolated trachea and pulmonary artery of rats and the possible mechanism(s of action. The possible antioxidant effect of taurine was also studied by measuring its protective effect against cyclophosphamide induced lung injuiry. Taurine produced a concentration dependent relaxation in the isolated tracheal strips and pulmonary arterial rings precontracted by serotonin (2x10-4 mM. The relaxing effect of taurine was not influenced by pretreatment with nitric oxide synthase inhibitor (L-NAME , cysteinyl leukotreines receptor 1 blocker (montelukast , H1 receptor blocker (chlorpheniramine , β-adrenoceptor blocker (propranolol, potassium channel blocker (amiodarone , cyclo-oxygenase inhibitor (indomethacin or muscarinic receptor blocker (atropine. Preincubation with adenosine receptor blocker (aminophylline significantly potentiated the relaxing effect of taurine in the tracheal strips and pulmonary arterial rings. Cyclophosphamide (CYP, 150 mg/kg administerated i.p. in a single dose was used to produce lung injuiry in rats. CYP caused marked increase in lung lipid peroxides (MDA and decrease in lung reduced glutathione (GSH. Administration of taurine (1% in drinking water starting 7 days before CYP and continuing throughout the duration of the experiment (24 hours improved significantly the lung GSH and MDA. It can be concluded that taurine relaxes precontracted rat tracheal strips and pulmonary arterial rings probably by direct effect on the smooth muscles. Also, the observed antioxidant activity of taurine which may contribute to its relaxant effect suggesting the usefulness of turine in pulmonary hypertension.

  12. A case of levocetirizine-induced fixed drug eruption and cross-reaction with piperazine derivatives.

    Science.gov (United States)

    Kim, Mi-Yeong; Jo, Eun-Jung; Chang, Yoon-Seok; Cho, Sang-Heon; Min, Kyung-Up; Kim, Sae-Hoon

    2013-10-01

    Fixed drug eruption is an uncommon adverse drug reaction caused by delayed cell-mediated hypersensitivity. Levocetirizine is an active (R)-enatiomer of cetirizine and there have been a few reports of fixed drug eruption related to these antihistamines. We experienced a case of levocetirizine-induced fixed drug eruption and cross-reaction with other piperazine derivatives confirmed by patch test. A 73-year-old female patient presented with recurrent generalized itching, cutaneous bullae formation, rash and multiple pigmentation at fixed sites after taking drugs for common cold. She took bepotastine besilate (Talion®) and levocetirizine (Xyzal®) as antihistamine. She took acetaminophen, pseudoephedrine 60 mg / triprolidine 2.5 mg (Actifed®), dihydrocodeinebitartrate 5 mg / di-methylephedrine hydrochloride 17.5 mg / chlorpheniramine maleate 1.5 mg / guaifenesin 50 mg (Codening®) and aluminium hydroxide 200 mg / magnesium carbonate 120 mg (Antad®) at the same time. Patch test was done with suspected drugs and the result was positive with levocetirizine. We additionally performed patch test for other antihistamines such as cetirizine, hydroxyzine, fexofenadine and loratadine. Piperazine derivatives (cetirizine and hydroxyzine) were positive, but piperidine derivatives (fexofenadine and loratadine) were negative to patch test. There was no adverse drug reaction when she was challenged with fexofenadine. We report a case of levocetirizine-induced fixed drug eruption confirmed by patch test. Cross-reactions were only observed in the piperazine derivatives and piperidine antihistamine was tolerant to the patient. PMID:24260733

  13. Characteristics of scratching behavior in ADJM mice (atopic dermatitis from Japanese mice).

    Science.gov (United States)

    Nakasone, Tasuku; Sato, Takumi; Matsushima, Yoshibumi; Inoue, Toshio; Kamei, Chiaki

    2015-04-01

    In order to elucidate the characteristics of scratching behavior in atopic dermatitis from Japanese mice (ADJM) mice, the effects of some antagonists of pruritogens on this behavior were studied. Both male and female ADJM mice showed frequent scratching behavior around the face, abdomen and back. The number of scratching behavior around the face was greater than on the abdomen and back, and scratching behavior in female mice was significantly more frequent than in male mice. Histamine H1 antagonist, chlorpheniramine, p.o., inhibited this behavior potently and dose-dependently. Histamine H1 antagonist with serotonin 5-TH(5-hydroxytryptamine)2 antagonist, cyproheptadine, also inhibited this behavior. However, NK1 antagonist, aprepitant, p.o., had no significant inhibitory effect even at a dose of 100 mg/kg, p.o., Mu antagonist, naloxone, and kappa agonist, nalfurafine, significantly inhibited this behavior at doses of 0.3 mg/kg, s.c., and 0.01 mg/kg, p.o., respectively. Histamine contents in the skin of ADJM mice were significantly higher than in BALB/c mice. These results strongly indicate that scratching behavior in ADJM mice is related with histamine H1, opioid mu and opioid kappa receptors. PMID:25578901

  14. Preparation and evaluation of monodispersed, submicron, non-porous silica particles functionalized with β-CD derivatives for chiral-pressurized capillary electrochromatography.

    Science.gov (United States)

    Yangfang, Lu; Hui, Wang; Yun, Xue; Xue, Gu; Yan, Wang; Chao, Yan

    2015-09-01

    Submicron, non-porous, chiral silica stationary phase has been prepared by the immobilization of functionalized β-CD derivatives to isocyanate-modified silica via chemical reaction and applied to the pressurized capillary electrochromatography (pCEC) enantio-separation of various chiral compounds. The submicron, non-porous, cyclodextrin-based chiral stationary phases (sub_μm-CSP2) exhibited excellent chiral recognition of a wide range of analytes including clenbuterol hydrochloride, mexiletine hydrochloride, chlorpheniramine maleate, esmolol hydrochloride, and metoprolol tartrate. The synthesized submicron particles were regularly spherical and uniformly non-porous with an average diameter of around 800 nm and a mean pore size of less than 2 nm. The synthesized chiral stationary phase was packed into 10 cm × 100 μm id capillary columns. The sub_μm-CSP2 column used in the pCEC system showed better separation of the racemates and at a higher rate compared to those used in the capillary liquid chromatography mode (cLC) system. The sub_μm-CSP2 possessed high mechanical strength, high stereoselectivity, and long lifespan, demonstrating rapid enantio-separation and good resolution of samples. The column provided an efficiency of up to 170,000 plates/m for n-propylbenzene. PMID:25990895

  15. A Case of Anaphylaxis Induced by Contact with Young Radish (Raphanus sativus L).

    Science.gov (United States)

    Lee, Yung-Hee; Lee, Jae-Hyoung; Kang, Hye-Ran; Ha, Jung-Hoon; Lee, Byoung-Hoon; Kim, Sang-Hoon

    2015-01-01

    Young radish (Raphanus sativus L), a member of the mustard family (Cruciferae), is a common ingredient of Kimchi. Although few reports have described anaphylaxis to cruciferous vegetables, we report the case of anaphylaxis induced by contact with young radish. A 46-year-old female with a history of contact allergy to metal presented to our emergency room (ER) with dizziness, generalized eruption and gastrointestinal upset. Her symptoms developed after re-exposure to young radish while chopping it. Hypotensive blood pressures were noted. Three days prior, the patient had experienced generalized urticaria with pruritus immediately after chopping the fresh young radish, which resolved spontaneously. In the ER, her symptoms improved by the administration of epinephrine (0.3 mL), antihistamine (chlorpheniramine) and isotonic saline hydration. A skin prick test with young radish extract showed positive reactivity. The same skin test was negative in five adult controls. IgE-mediated hypersensitivity could be an important immunologic mechanism in the development of young radish-induced anaphylaxis. PMID:25553270

  16. A solid-state electrochemiluminescence composite modified electrode based on Ru(bpy)32+/PAHNSA: Characterization and pharmaceutical applications

    International Nuclear Information System (INIS)

    A composite electrochemiluminescence (ECL) sensor was constructed by electrochemical polymerization of 4-amino-3-hydroxynaphthalene sulfonic acid (AHNSA) and tris(2,2′-bipyridyl) ruthenium(II), [Ru(bpy)3]2+, from their aqueous solutions at glassy carbon electrode (GCE). The proposed one-step electrochemical synthesis of the composite film (Ru/PAHNSA/GCE) provides a stable and reactive luminescent for the quantification of chlorpheniramine maleate (CPM) in its pharmaceutical preparations. The properties and the structure of the modified surface were studied using typical voltammetric, Electrochemical Impedance Spectroscopy (EIS), X-Ray Photoelectron Spectroscopy (XPS) and Atomic Force Microscopy (AFM) methods. The intensity of the ECL as a function of [CPM] is linear for the range between 0.2 and 32 μg mL−1 with a detection limit of 0.023 μg mL−1. The performance of the sensor was tested in the presence of interference species and for real sample analysis under optimal conditions

  17. Amino-functionalized silica nanoparticles for improved enantiomeric separation in capillary electrophoresis using carboxymethyl-β-cyclodextrin (CM-β-CD) as a chiral selector

    International Nuclear Information System (INIS)

    We report on the use of amino-modified silica nanoparticles (SiNPs) as an additive to the background electrolyte solution to enhance the chiral selectivity of in capillary electrophoresis that is induced by the presence of a small quantity of carboxymethyl-β-cyclodextrin (CM-β-CD). The modified SiNPs were characterized by transmission electron microscopy, elemental analysis and their zeta potential. The method was applied to the separation of four alkaline drugs (ephedrine, chlorpheniramine, propranolol and amlodipine). The addition of the modified SiNPs to the background electrolyte results in a distinct improvement in the separation power, especially when the capillary was pretreated with high concentration of particle suspensions prior to separation. The effects of fractions of modified SiNPs and organic modifier, of the thickness of the SiNP coating layer on the capillary wall were investigated. Under optimum experimental conditions, all the racemates investigated were separated with improved resolution, thus indicating the potential of the method in the field of enantiomeric separation. (author)

  18. Preliminary observation with dronabinol in patients with intractable pruritus secondary to cholestatic liver disease.

    Science.gov (United States)

    Neff, Guy W; O'Brien, Christopher B; Reddy, K Rajender; Bergasa, Nora V; Regev, Arie; Molina, Enrique; Amaro, Rafael; Rodriguez, Miguel J; Chase, VeEtta; Jeffers, Lennox; Schiff, Eugene

    2002-08-01

    Pruritus due to cholestatic liver disease can be particularly difficult to manage and frequently is intractable to a variety of medical therapies. The aim of our study is to evaluate the efficacy of delta-9-tetrahydrocannabinol (delta-9-THC) for intractable cholestatic related pruritus (ICRP) that has failed conventional (and unconventional) remedies. Three patients were evaluated for plasmapheresis because of ICRP. All 3 patients had previously been extensively treated with standard therapies for ICRP including: diphenhydramine, chlorpheniramine, cholestyramine, rifampicin, phenobarbital, doxepin, naltrexone, UV therapy, and topical lotions. Even multiple courses of plasmapheresis were performed without any benefit for the intractable pruritus. All patients reported significant decreases in their quality of life, including lack of sleep, depression, inability to work, and suicidal ideations. All patients were started on 5 mg of delta-9-THC (Marinol) at bedtime. All 3 patients reported a decrease in pruritus, marked improvement in sleep, and eventually were able to return to work. Resolution of depression occurred in two of three. Side effects related to the drug include one patient experiencing a disturbance in coordination. Marinol dosage was decreased to 2.5 mg in this patient with resolution of symptoms. The duration of antipruritic effect is approximately 4-6 hrs in all three patients suggesting the need for more frequent dosing. Delta-9-tetrahydrocannabinol may be an effective alternative in patients with intractable cholestatic pruritus. PMID:12190187

  19. Involvement of serotonin and eicosanoids in the rat paw oedema response to the essential oil of Pilocarpus spicatus.

    Science.gov (United States)

    Silva, J C; Rao, V S

    1992-01-01

    Subplantar injection of Pilocarpus spicatus essential oil (PSEO), induced rat hindpaw oedema in a dose-dependent manner. The time course study revealed that when compared to carrageenan-induced oedema, the oedema response to PSEO was greater at 1 h post-injection, and thereafter remained relatively constant until 5 h post-injection. By 24 h, it was still at almost the 50% level. This effect of PSEO was characterized using several inhibitors of oedema formation. Pretreatment with the H(1)-receptor antagonist chlorpheniramine did not affect this response, while a significant reduction of paw oedema was achieved with the serotonin antagonist methysergide, but only 1 h and 2 h after injection of PSEO. The oedemagenic activity of PSEO was also suppressed by pretreating the rats with the eicosanoid synthesis inhibitors, phenylbutazone, EP 10161 and dexamethasone. This last drug showed the greatest potency. These findings suggested a probable injury to dermal mast cells and liberation of arachidonate metabolites and eicosanoids at the late phase of oedema induced by PSEO. PMID:18475456

  20. Involvement of serotonin and eicosanoids in the rat paw oedema response to the essential oil of Pilocarpus spicatus

    Directory of Open Access Journals (Sweden)

    J. C. R. Silva

    1992-01-01

    Full Text Available Subplantar injection of Pilocarpus spicatus essential oil (PSEO, induced rat hindpaw oedema in a dose-dependent manner. The time course study revealed that when compared to carrageenan-induced oedema, the oedema response to PSEO was greater at 1 h post-injection, and thereafter remained relatively constant until 5 h post-injection. By 24 h, it was still at almost the 50% level. This effect of PSEO was characterized using several inhibitors of oedema formation. Pretreatment with the H1-receptor antagonist chlorpheniramine did not affect this response, while a significant reduction of paw oedema was achieved with the serotonin antagonist methysergide, but only 1 h and 2 h after injection of PSEO. The oedemagenic activity of PSEO was also suppressed by pretreating the rats with the eicosanoid synthesis inhibitors, phenylbutazone, EP 10161 and dexamethasone. This last drug showed the greatest potency. These findings suggested a probable injury to dermal mast cells and liberation of arachidonate metabolites and eicosanoids at the late phase of oedema induced by PSEO.

  1. Responses of the L5178Y mouse Lymphoma cell forward mutation assay. V: 27 coded chemicals.

    Science.gov (United States)

    McGregor, D B; Brown, A G; Howgate, S; McBride, D; Riach, C; Caspary, W J

    1991-01-01

    Twenty-seven chemicals were tested for their mutagenic potential in the L5178Y tk+/tk- mouse lymphoma cell forward mutation assay using procedures based upon those described by McGregor et al. (McGregor DB, Martin R, Cattanach P, Edwards I, McBride D, Caspary WJ (1987): Environ Mol Mutagen 9:143-160). Cultures were exposed to the chemicals for 4 hr, then cultured for 2 days before plating in soft agar with or without trifluorothymidine (TFT), 3 micrograms/ml. The chemicals were tested at least twice. Statistically significant responses were obtained with acid orange 10, aniline, benzaldehyde, o-chloroaniline, chlorodibromomethane, cytembena, 1,2-dibromo-4-(1,2-dibromomethyl) cyclohexane, dieldrin, lithocholic acid, oxytetracycline, phenazopyridine HCl, 1-phenyl-3-methyl-5-pyrazolone, sodium diethyldithiocarbamate, solvent yellow 14, tetraethylthiuram disulfide (disulfiram), 2,4-toluene diisocyanate, and 2,6-toluene diisocyanate. Apart from phenazopyridine HCl, acid orange 10, and solvent yellow 14, rat liver S9 mix was not a requirement for the mutagenic activity of these compounds. Chemical not identified as mutagens were N-4-acetylaminofluorene, chlorpheniramine maleate, chloropropamide, 1,4-dioxane, endrin, ethylene glycol, iron dextran, methapyrilene, sodium(2-ethylhexyl)alcohol PMID:1902415

  2. Psychogenic Itch Management.

    Science.gov (United States)

    Szepietowski, Jacek C; Reszke, Radomir

    2016-01-01

    Pruritus is a bothersome and prevalent symptom reported by patients suffering from both cutaneous and extracutaneous diseases. Psychogenic pruritus, also referred to as functional itch disorder, is a distinct clinical entity. According to the definition proposed by the French Psychodermatology Group (FPDG) in 2007, the disorder is characterized by pruritus which is the chief complaint and psychologic factors that contribute to eliciting, worsening, and sustaining the symptoms. Specific diagnostic criteria were proposed, including 3 compulsory and 7 optional, of which 3 have to be met in order to establish the diagnosis. Psychogenic pruritus may require cooperation between dermatologists, psychiatrists, and psychologists. Psychotherapy and psychopharmacotherapy are mainstays of managing the disease. However, publications regarding psychogenic itch management are uncommon. Initially, general measures have to be taken, including avoiding irritating factors, preventing skin dryness, and frequent application of emollients. As in pruritus of other causes, several drugs are used, with more emphasis on substances that influence central nervous system: H1-antihistamines (hydroxyzine, chlorpheniramine, cyproheptadine, diphenhydramine, promethazine), tricyclic antidepressants (doxepin), tetracyclic antidepressants (mirtazapine), selective serotonin reuptake inhibitors (citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline), antipsychotic drugs (pimozide), anticonvulsants (topiramate), and benzodiazepines (alprazolam), preferably depending on the coexisting symptoms. PMID:27578081

  3. Antihistamines suppress upregulation of histidine decarboxylase gene expression with potencies different from their binding affinities for histamine H1 receptor in toluene 2,4-diisocyanate-sensitized rats.

    Science.gov (United States)

    Mizuguchi, Hiroyuki; Das, Asish K; Maeyama, Kazutaka; Dev, Shrabanti; Shahriar, Masum; Kitamura, Yoshiaki; Takeda, Noriaki; Fukui, Hiroyuki

    2016-04-01

    Antihistamines inhibit histamine signaling by blocking histamine H1 receptor (H1R) or suppressing H1R signaling as inverse agonists. The H1R gene is upregulated in patients with pollinosis, and its expression level is correlated with the severity of nasal symptoms. Here, we show that antihistamine suppressed upregulation of histidine decarboxylase (HDC) mRNA expression in patients with pollinosis, and its expression level was correlated with that of H1R mRNA. Certain antihistamines, including mepyramine and diphenhydramine, suppress toluene-2,4-diisocyanate (TDI)-induced upregulation of HDC gene expression and increase HDC activity in TDI-sensitized rats. However, d-chlorpheniramine did not demonstrate any effect. The potencies of antihistamine suppressive effects on HDC mRNA elevation were different from their H1R receptor binding affinities. In TDI-sensitized rats, the potencies of antihistamine inhibitory effects on sneezing in the early phase were related to H1R binding. In contrast, the potencies of their inhibitory effects on sneezing in the late phase were correlated with those of suppressive effects on HDC mRNA elevation. Data suggest that in addition to the antihistaminic and inverse agonistic activities, certain antihistamines possess additional properties unrelated to receptor binding and alleviate nasal symptoms in the late phase by inhibiting synthesis and release of histamine by suppressing HDC gene transcription. PMID:26980430

  4. Preparation of tablets rapidly disintegrating in saliva containing bitter taste-masked granules by compression method

    Directory of Open Access Journals (Sweden)

    Shishu

    2007-01-01

    Full Text Available The aim of this study was to prepare, using taste masked granules, rapidly disintegrating tablets of chlorpheniramine maleate, a bitter drug. The taste masked granules were prepared using aminoalkyl methacrylate copolymers (Eudragit E-100 by the extrusion method. In vitro release profile obtained at pH 6.8 indicate that perceivable amount of drug will not be released in saliva while high percent release (more than 80% in 30 min would be obtained at acidic pH 1.2 of the stomach. These taste masked granules were directly compressed into tablets using sodium starch glycolate as a super-disintegrant. The prepared tablets containing the taste masked granules having sufficient strength of 3.5 kg/cm were evaluated for taste by both spectrophotometric method and through panel testing. Panel testing data collected from 20 healthy volunteers indicate successful formulation of oral fast disintegrating tablets which had good taste and disintegrated in the oral cavity within 30s.

  5. Membrane transport of andrographolide in artificial membrane and rat small intestine.

    Science.gov (United States)

    Daodee, Supawadee; Wangboonskul, Jinda; Jarukamjorn, Kanokwan; Sripanidkulchai, Bung-orn; Murakami, Teruo

    2007-06-15

    In the present study, the possible drug interactions of andrographolide with co-administering drugs such as acetaminophen, amoxycillin, aspirin, chlorpheniramine and norfloxacin to treat various infectious and inflammatory diseases that may be induced during absorption process were examined using artificial lipophilic membrane and everted rat intestine. The membrane transport of andrographolide across the artificial membrane was not affected by different pH of the medium (simulated gastric and intestinal fluids), different concentrations of andrographolide and co-administered drugs examined. In everted rat intestine, above co-administered drugs examined showed no significant effect on andrographolide membrane transport. The participation of efflux transporters such as P-glycoprotein and MRP2 in andrographolide transport was then examined, since andrographolide is a diterpene compound and some diterpene compounds are known as P-glycoprotein substrates. Cyclosporine, a P-glycoprotein/MRP2 inhibitor, significantly suppressed the efflux transport of andrographolide in distal region of intestine, whereas probenecid, an MRP inhibitor, showed no significant effect in both proximal and distal regions of intestine. These results suggest that P-glycoprotein, but not MRP, is participated in the intestinal absorption of andrographolide and P-glycoprotein-mediated drug interactions occur depending on the co-administered drugs and its concentrations. PMID:19093450

  6. Changes in nasal resistance and nasal geometry using pressure and acoustic rhinometry in a feline model of nasal congestion

    DEFF Research Database (Denmark)

    McLeod, R.L.; Mingo, G.G.; Herczku, C.; Corboz, M.R.; DeGennaro-Culver, F.; Pedersen, Ole Finn; Hey, J.A.

    1999-01-01

    , increased nasal airway resistance (NAR) 1.2 +/- 0.6, 5.8 +/- 0.5, 8.6 +/- 1.1 and 7.9 +/- 1.5 cmH2O.L/minute, respectively. Increases in NAR produced by compound 48/80 were associated with a 395% increase in histamine concentration found in the nasal lavage fluid. Pretreatment with the alpha......-adrenoreceptor agonist, phenylpropanolamine (PPA; 0.1-3.0 mg/kg, i.v.), and the NO synthetase inhibitor, NG-nitro-L-arginine (L-NAME; 10 mg/kg, i.v.) attenuated the increases in NAR produced by compound 48/80. The histamine H1 antagonist chlorpheniramine (1.0 mg/kg, i.v.) and the H2 antagonist, ranitidine (1.0 mg/kg, i.......v.) had no decongestant activity. Also without decongestant activity were the muscarinic antagonist atropine, the cyclooxygenase inhibitor indomethacin, and the 5-HT blocker methysergide. Aerosolized histamine (0.1-1.0%) also produced a dose dependent increase in NAR. In studies using acoustic rhinometry...

  7. Simultaneous determination of some active ingredients in cough and cold preparations by gas chromatography, and method validation.

    Science.gov (United States)

    Harsono, Thresiana; Yuwono, Mochammad; Indrayanto, Gunawan

    2005-01-01

    A simple and rapid gas chromatographic (GC) method has been developed for the simultaneous determination of combinations of acetaminophen, phenylpropanolamine hydrochloride, guaifenesin, pseudoephedrine hydrochloride, caffeine, chlorpheniramine maleate, and dextromethorphan hydrobromide in cough and cold tablets and syrups. After extraction of the analyte with alkaline ethyl acetate, 2 microL extract was injected (splitting ratio of 50:1) into a gas chromatograph equipped with a CBP1-M25-025 fused silica capillary column (25 m x 0.22 mm; film thickness, 0.25 microm). The column temperature was held at 150 degrees C for 5 min, increased to 175 degrees C at 3 degrees C/min, and increased to 270 degreesC at 10 degrees C/min. The temperatures of the flame ionization detector and injector were maintained at 300 degrees C. The GC method is inexpensive, rapid, accurate, and precise, and thus it can be used for routine analysis of tablet and syrup preparations in quality control laboratories of pharmaceutical companies. PMID:16152925

  8. Evaluation of postmortem drug concentrations in cerebrospinal fluid compared with blood and pericardial fluid.

    Science.gov (United States)

    Tominaga, Mariko; Michiue, Tomomi; Ishikawa, Takaki; Inamori-Kawamoto, Osamu; Oritani, Shigeki; Maeda, Hitoshi

    2015-09-01

    In forensic toxicology, body fluids are important materials not only as alternatives to blood but also for investigation of postmortem drug redistributions and pharmaco-/toxicokinetic analysis; however, there are limited data on postmortem drug distributions in cerebrospinal fluid (CSF). The present study reviewed toxicological data of autopsy cases (n=103), in which drugs were detected in CSF using gas chromatography/mass spectrometry (GC/MS), to investigate drug concentrations in CSF, compared with blood and pericardial fluid (PCF) concentrations. Oral/injected amphetamines (n=23) showed similar CSF and blood/PCF concentrations with partly lower CSF concentrations (about ×0.5-1.1). CSF concentrations of the venous anesthetic midazolam (n=7) were lower with poor correlations. Oral caffeine (n=15), acetaminophen (n=7), chlorpheniramine (n=6), dihydrocodeine (n=6), and phenobarbital (n=21) showed equivalent to lower CSF concentrations (about ×0.2-1.2), compared with blood and PCF concentrations; however, CSF phenobarbital concentrations were high in a fatal intoxication case. CSF concentrations of phenothiazine derivatives (n=29) were markedly lower (about ×0.1) than blood/PCF concentrations. The distribution of the local anesthetic lidocaine used in critical medical care (n=49) markedly varied by case. These findings suggest that CSF is useful in routine forensic toxicology as an alternative to blood as well as for investigating pharmaco-/toxicokinetics and postmortem redistributions. PMID:26218406

  9. Dexamethasone: a potent blocker for radiation-induced taste aversion in rats

    International Nuclear Information System (INIS)

    Rats, trained to drink water during a single 30-min period each day, were then given 0.1% saccharin twice a week and water on other days for 30 min. If 20 rad of radiation (0.2 Gy) were given each time 30 to 40 min after the saccharin the rats developed a profound aversion to saccharin during the course of three weeks, whereas control groups failed to do so. This paradigm was then used to test the ability of drugs, given twice weekly immediately after the saccharin, to prevent the development during three weeks of an aversion when 20 rad was given, 30 to 40 min later. Insulin, domperidone, haloperidol, acetylsalicylic acid, naloxone, chlorpheniramine, cimetidine, and dimethyl sulphoxide were tested without notable success. However dexamethasone, at doses ranging from 0.013 mg/kg to 1.3 mg/kg, significantly attenuated the conditioned taste aversion by up to 60 percent. The results are discussed in terms of a search for an antinauseant and antiemetic drug effective against radiation in man

  10. Detection of drugs in 275 alcohol-positive blood samples of Korean drivers.

    Science.gov (United States)

    Kim, Eunmi; Choe, Sanggil; Lee, Juseon; Jang, Moonhee; Choi, Hyeyoung; Chung, Heesun

    2016-08-01

    Since driving under the influence of drugs (DUID) is as dangerous as drink-driving, many countries regulate DUID by law. However, laws against the use of drugs while driving are not yet established in Korea. In order to investigate the type and frequency of drugs used by drivers in Korea, we analyzed controlled and non-controlled drugs in alcohol-positive blood samples. Total 275 blood samples were taken from Korean drivers, which were positive in roadside alcohol testing. The following analyses were performed: blood alcohol concentrations by GC; screening for controlled drugs by immunoassay and confirmation for positive samples by GC-MS. For the detection of DUID related drugs in blood samples, a total of 49 drugs were selected and were examined by GC-MS. For a rapid detection of these drugs, an automated identification software called "DrugMan" was used. Concentrations of alcohol in 275 blood samples ranged from 0.011 to 0.249% (average 0.119%). Six specimens showed positive results by immunoassay: one methamphetamine and five benzodiazepines I. By GC-MS confirmation, only benzodiazepines in four cases were identified, while methamphetamine and benzodiazepine in two cases were not detected from the presumptive positive blood samples. Using DrugMan, four drugs were detected; chlorpheniramine (5)*, diazepam (4), dextromethorphan (1) and doxylamine (1). In addition, ibuprofen (1), lidocaine (1) and topiramate (1) were also detected as general drugs in blood samples ('*' indicates frequency). The frequency of drug abuse by Korean drivers was relatively low and a total 14 cases were positive in 275 blood samples with a ratio of 5%. However it is necessary to analyze more samples including alcohol negative blood, and to expand the range of drug lists to get the detailed information. PMID:27015372

  11. Utility of rotational thromboelastometry for the diagnosis of asymptomatic hyperfibrinolysis secondary to anaphylaxis.

    Science.gov (United States)

    Koami, Hiroyuki; Sakamoto, Yuichiro; Furukawa, Takashi; Imahase, Hisashi; Iwamura, Takashi; Inoue, Satoshi

    2016-06-01

    We present a case of hyperfibrinolysis induced by oxaliplatin-derived anaphylactic shock, which was diagnosed with rotational thromboelastometry (ROTEM). A 57-year-old male patient underwent a second course of oxaliplatin (126 mg/m/course)-based chemotherapy for stage IV metastatic rectal cancer. Two minutes after the infusion of oxaliplatin, the patient lost consciousness and developed generalized urticarial lesions, followed by hemodynamic instability and respiratory insufficiency. He was diagnosed anaphylactic shock and transported to emergency department (ED) after intramuscular injection of 0.2 mg of adrenaline, an intravenous injection of 100 mg of hydrocortisone, and 500 mg of methylprednisolone. After arriving in the ED, the patient remained in shock and early resuscitation with administration of 5 mg of D-chlorpheniramine maleate and 20 mg of famotidine was performed. He recovered from his state of shock 30 min after the resuscitation. ROTEM findings showed fulminant hyperfibrinolysis with minimal changes in standard coagulation tests (SCTs) and no remarkable coagulopathy. Seven hours after the attack, he became asymptomatic and follow-up ROTEM revealed values within normal limits with the exception of sustained slight abnormalities of SCTs. He was discharged the next day without any signs of spontaneous bleeding and has continued his outpatient chemotherapy uneventfully. A review of the literature on anaphylaxis-induced hyperfibrinolysis and a discussion of the mechanism between anaphylactic shock and hyperfibrinolysis were performed. Although administration of tissue-type plasminogen activator can play a vital role in anaphylactic shock-induced hyperfibrinolysis, early effective resuscitation is imperative to prevent severe hemorrhagic complications. Therefore, ROTEM is a useful tool that can detect these dynamic changes faster and more accurately than SCTs. PMID:26569513

  12. [A case study of BRON (cough suppressant) tablet dependence--its social psychiatric and biological aspects].

    Science.gov (United States)

    Kitabayashi, Y; Ueda, H; Narumoto, J; Kita, H; Nakamura, K; Tsuchida, H; Tani, N; Fukui, K

    2000-10-01

    A case of BRON tablet dependence is demonstrated. BRON is an over-the-counter (OTC) cough suppressant, which contains methylephedrine, dihydrocodeine, chlorpheniramine and caffeine. He took BRON tablet for the first time at the age of 16. In progress, he developed psychomotor excitement twice and finally manifested amotivational syndrome 3 years later from his first use. Longitudinal 123I-IMP SPECT (autoradiography method) findings demonstrated diffuse cerebral blood flow (CBF) decrease and relative hyperactivity in the lower frontal lobe. Diffuse decreased regional CBF, which was unchanged through its course for about 4 months, may show irreversible brain damage due to chronic BRON abuse. The findings of relative hyperactivity in the lower frontal lobe (orbitofrontal lobe) may reflect "craving for BRON" based on abnormal dopaminergic neural system activity. Based on the evidence that orbitofrontal hyperactivity is also seen in cases of cocaine abuse, methylephedrine, which is a cocaine-like central nervous system stimulant, may play the main role in BRON dependence formation. In Japan, BRON syrup abuse and dependence were in fashion for youth in 1980s. After the legal regulation of the market in 1988, it has gone out of fashion. While it is still easy to acquire OTC cough suppressant, reports of BRON tablet abuse and dependence are quite rare through 1980s and 1990s. This case suggests that BRON tablet abuse also could lead to dependence and come into new vogue for youth in the future. We should pay attention to the trend of OTC cough suppressant abuse and may need to regulate the market by law more severely. PMID:11144150

  13. Antitussive activity of Vasa Avaleha formulations on sulfur dioxide-induced coughing in mice

    Directory of Open Access Journals (Sweden)

    Ankit M Paneliya

    2015-01-01

    Full Text Available Objective: Vasa Avaleha is a well-known Ayurvedic compound formulation, known for its usefulness in respiratory disorders like cough, cold, bronchitis, bronchial asthma, etc. Though Adhatoda vasica individually studied for antitussive activity in animals, no scientific evidence was available for Vasa Avaleha. This prompted us to initiate a comparative antitussive activity of Vasa Avaleha and granules of Vasa Avaleha in sulfur dioxide-induced coughing in mice. Materials and Methods: The test drugs were prepared as per classical guidelines and standards in the Departmental Laboratory of the Institute. The test drugs were administered orally at a dose of 1.56 g/kg and tested against sulfur dioxide-induced coughing in mice for 5 min. Results : Vasa Avaleha significantly (P < 0.001 inhibited the sulfur dioxide-induced cough reflexes in mice compared to control group. The effect was comparable to the standard drug Recodex, which contain codeine phosphate and chlorpheniramine maleate. Granules of Vasa Avaleha also produced significant (P < 0.001 decrease in cough reflexes compared to control group. The magnitude of the antitussive effect was more pronounced and significant in Vasa Avaleha treated group in comparison to granules of Vasa Avaleha. Conclusions: From the present study, it is concluded that Vasa Avaleha and granules of Vasa Avaleha may prove as useful and an effective antitussive agent which provides experimental evidence in support of the Ayurvedic ancient claim. Further, Avaleha form of test formulation can be converted to granule form and further evaluated in clinical studies for better human therapeutic uses.

  14. Centrally injected histamine increases posterior hypothalamic acetylcholine release in hemorrhage-hypotensive rats.

    Science.gov (United States)

    Altinbas, Burcin; Yilmaz, Mustafa S; Savci, Vahide; Jochem, Jerzy; Yalcin, Murat

    2015-01-01

    Histamine, acting centrally as a neurotransmitter, evokes a reversal of hemorrhagic hypotension in rats due to the activation of the sympathetic and the renin-angiotensin systems as well as the release of arginine vasopressin and proopiomelanocortin-derived peptides. We demonstrated previously that central nicotinic cholinergic receptors are involved in the pressor effect of histamine. The aim of the present study was to examine influences of centrally administrated histamine on acetylcholine (ACh) release at the posterior hypothalamus-a region characterized by location of histaminergic and cholinergic neurons involved in the regulation of the sympathetic activity in the cardiovascular system-in hemorrhage-hypotensive anesthetized rats. Hemodynamic and microdialysis studies were carried out in Sprague-Dawley rats. Hemorrhagic hypotension was induced by withdrawal of a volume of 1.5 ml blood/100 g body weight over a period of 10 min. Acute hemorrhage led to a severe and long-lasting decrease in mean arterial pressure (MAP), heart rate (HR), and an increase in extracellular posterior hypothalamic ACh and choline (Ch) levels by 56% and 59%, respectively. Intracerebroventricularly (i.c.v.) administered histamine (50, 100, and 200 nmol) dose- and time-dependently increased MAP and HR and caused an additional rise in extracellular posterior hypothalamic ACh and Ch levels at the most by 102%, as compared to the control saline-treated group. Histamine H1 receptor antagonist chlorpheniramine (50 nmol; i.c.v.) completely blocked histamine-evoked hemodynamic and extracellular posterior hypothalamic ACh and Ch changes, whereas H2 and H3/H4 receptor blockers ranitidine (50 nmol; i.c.v.) and thioperamide (50 nmol; i.c.v.) had no effect. In conclusion, centrally administered histamine, acting via H1 receptors, increases ACh release at the posterior hypothalamus and causes a pressor and tachycardic response in hemorrhage-hypotensive anesthetized rats. PMID:25468497

  15. Application of RP-HPLC method in dissolution testing and statistical evaluation by NASSAM for simultaneous estimation of tertiary combined dosages forms

    Institute of Scientific and Technical Information of China (English)

    Yogesh Upadhyay; Nitin Sharma; G.S. Sarma; Ravindra K. Rawal

    2015-01-01

    A dissolution method with robust high performance liquid chromatographic (HPLC) analysis for im-mediate release tablet formulation was developed and validated to meet the requirement as per Inter-national Conference on Harmonization (ICH) and United States Food and Drug Administration (USFDA) guidelines. The method involved the use of Agilent ZORBAX Eclipse XDB C18 column, and temperature was maintained at 30 °C. After optimization, the mobile phase was selected as phosphate buffer (KH2PO4, 30 mM):ACN (60:40, v/v) with pH 3.0, and retention time Rt was found as 3.24, 4.16, and 2.55 min for paracetamol (PCM), chlorpheniramine maleate (CPM) and phenylephrine hydrochloride (PH) respec-tively at 265 nm and at a flow rate of 1 mL/min. The relative standard deviation (%RSD) for 6 replicate measurements was found to be less than 2%. Furthermore net analyte signal standard addition method (NASSAM) with spectrophotometer was performed for standard and liquid oral suspension. On the basis of selectivity, sensitivity and accuracy analysis, it was confirmed that this novel method could be useful for simultaneous estimation of the given drug combinations. Two-way analysis of variance (ANOVA) was applied for evaluating the statistical difference between the assay results obtained via both NASSAM and RP-HPLC methods and ultimately no significant difference was found between both the methods. All the methods and results were acceptable and confirmed that the method was suitable for intended use.

  16. Analgesic Effects of 1st Generation Anti-histamines in Mice.

    Science.gov (United States)

    Takahashi, Mebae; Shima, Kazuhiro; Tsuchiya, Masahiro; Hagiwara, Yoshihiro; Mizoguchi, Hirokazu; Sakurada, Shinobu; Sugawara, Shunji; Fujita, Takuo; Tadano, Takeshi; Watanabe, Makoto; Fukumoto, Satoshi; Endo, Yasuo

    2016-01-01

    Pain is sensed, transmitted, and modified by a variety of mediators and receptors. Histamine is a well-known mediator of pain. In addition to their anti-histaminic effects, the classical, or 1st generation, anti-histamines (1st AHs) possess, to various degrees, anti-muscarinic, anti-serotonergic, anti-adrenergic, and other pharmacologic effects. Although there have been attempts to use 1st AHs as analgesics and/or analgesic adjuvants, the advent of non-steroidal anti-inflammatory drugs (NSAIDs) discouraged such trials. We previously reported that in patients with temporomandibular disorders, osteoporosis, and/or osteoarthritis, the analgesic effects of certain 1st AHs (chlorpheniramine and diphenhydramine) are superior to those of the NSAIDs flurbiprofen and indomethacin. Here, we compared analgesic effects among 1st AHs and NSAIDs against responses shown by mice to intraperitoneally injected 0.7% acetic acid. Since 1st AHs are water soluble, we selected water-soluble NSAIDs. For direct comparison, drugs were intravenously injected 30 min before the above tests. Histamine-H1-receptor-deficient (H1R-KO) mice were used for evaluating H1-receptor-independent effects. The tested 1st AHs (especially cyproheptadine) displayed or tended to display analgesic effects comparable to those of NSAIDs in normal and H1R-KO mice. Our data suggest that the anti-serotonergic and/or anti-adrenergic effects of 1st AHs make important contributions to their analgesic effects. Moreover, combination of a 1st AH with an NSAID (cyclooxygenase-1 inhibitor) produced remarkably potent analgesic effects. We propose that a 1st AH, by itself or in combination with a cyclooxygenase-1 inhibitor, should undergo testing to evaluate its usefulness in analgesia. PMID:27040636

  17. A possible trend suggesting increased abuse from Coricidin exposures reported to the Texas Poison Network: comparing 1998 to 1999.

    Science.gov (United States)

    Baker, S David; Borys, Douglas J

    2002-06-01

    Coricidin products seemed to be one of the over-the-counter medications being reportedly abused by adolescents, as observed from the Texas Poison Center Network data. This retrospective chart review investigated the occurrence of abuse, developed a patient profile, and defined the clinical effects resulting from the abuse of Coricidin products. Data collected from the Texas Poison Center Network Toxic Exposure Surveillance System database included human exposures between 1998 and 1999, patients > or = 10y old, intentional use or abuse, and single substance ingestion of I of the tablet formulations of Coricidin. Thirty-three cases from 1998 and 59 cases from 1999 were reviewed. Of these cases, 85% met the inclusion criteria. Of the 7 medications searched, only 4 substances were coded for: Coricidin D, Coricidin D (long acting), Coricidin D (cold, flu & sinus) and Coriciding HBP. These contain a combination of dextromethorphan hydrobromide, chlorpheniramine maleate, phenylpropanolamine hydrochloride, and acetaminophen. Of the 78 cases, 63% were male and 38% were female. The mean age was 14.67 years, 77% being between 13 to 17 years old. Eighteen different symptoms were reported: tachycardia 50%, somnolence 24.4%, mydriasis and hypertension 16.7%, agitation 12.8%, disorientation 10.3%, slurred speech 9%, ataxia 6.4%, vomiting 5.1%, dry mouth and hallucinations 3.9%, tremor 2.6%, and headache, dizziness, syncope, seizure, chest pain, and nystagmus each 1.3%; 12.8% of the calls originated from the school nurse. The incidence of abuse reported increased 60% from 1998 to 1999. This worrisome trend suggests increased abuse of these products. PMID:12046973

  18. Effect of histamine H1 and H2 receptor antagonists, microinjected into cerebellar vermis, on emotional memory consolidation in mice

    International Nuclear Information System (INIS)

    This study investigated the effects of histamine H1 or H2 receptor antagonists on emotional memory consolidation in mice submitted to the elevated plus maze (EPM). The cerebellar vermis of male mice (Swiss albino) was implanted using a cannula guide. Three days after recovery, behavioral tests were performed in the EPM on 2 consecutive days (T1 and T2). Immediately after exposure to the EPM (T1), animals received a microinjection of saline (SAL) or the H1 antagonist chlorpheniramine (CPA; 0.016, 0.052, or 0.16 nmol/0.1 µL) in Experiment 1, and SAL or the H2 antagonist ranitidine (RA; 0.57, 2.85, or 5.7 nmol/0.1 µL) in Experiment 2. Twenty-four hours later, mice were reexposed to the EPM (T2) under the same experimental conditions but they did not receive any injection. Data were analyzed using one-way ANOVA and the Duncan test. In Experiment 1, mice microinjected with SAL and with CPA entered the open arms less often (%OAE) and spent less time in the open arms (%OAT) in T2, and there was no difference among groups. The results of Experiment 2 demonstrated that the values of %OAE and %OAT in T2 were lower compared to T1 for the groups that were microinjected with SAL and 2.85 nmol/0.1 µL RA. However, when animals were microinjected with 5.7 nmol/0.1 µL RA, they did not show a reduction in %OAE and %OAT. These results demonstrate that CPA did not affect behavior at the doses used in this study, while 5.7 nmol/0.1 µL RA induced impairment of memory consolidation in the EPM

  19. Oxidative stress induces itch via activation of transient receptor potential subtype ankyrin 1 in mice

    Institute of Scientific and Technical Information of China (English)

    Tong Liu; Ru-Rong Ji

    2012-01-01

    Objective To investigate the role of oxidative stress in itch-indicative scratching behavior in mice,and furthermore,to define the cellular and molecular mechanisms underlying oxidative stress-mediated itch.Methods Scratching behavior was induced by intradermal injection of the oxidants hydrogen peroxide (H2O2) or tert-butylhydroperoxide (tBHP) into the nape of the neck in mice.The mice were observed for 30 min.Results Intradermal H2O2 (0.03%-1%) or tBHP (1-30 μmol) elicited robust scratching behavior,displaying an inverted U-shaped dose-response curve.Naloxone,an opioid receptor antagonist,but not morphine,largely suppressed the oxidant-induced scratching.Chlorpheniramine,a histamine H 1 receptor antagonist,blocked histamine-but not oxidant-induced scratching,indicating the involvement of a histamine-independent mechanism in oxidant-evoked itch.Further,resiniferatoxin treatment abolished oxidant-induced scratching,suggesting an essential role of C-fibers.Notably,blockade of transient receptor potential subtype ankyrin 1 (TRPA1) with the selective TRPA1 antagonist HC-030031,or genetic deletion of Trpal but not Trpvl (subfamily V,member 1) resulted in a profound reduction in H2O2-evoked scratching.Finally,systemic administration of the antioxidant Nacety1-L-cysteine or trolox (a water-soluble vitamin E analog) attenuated scratching induced by the oxidants.Conclusion Oxidative stress by different oxidants induces profound scratching behavior,which is largely histamine-and TRPV1-independent but TRPA1-dependent.Antioxidants and TRPA1 antagonists may be used to treat human itch conditions associated with oxidative stress.

  20. Application of RP–HPLC method in dissolution testing and statistical evaluation by NASSAM for simultaneous estimation of tertiary combined dosages forms

    Directory of Open Access Journals (Sweden)

    Yogesh Upadhyay

    2015-10-01

    Full Text Available A dissolution method with robust high performance liquid chromatographic (HPLC analysis for immediate release tablet formulation was developed and validated to meet the requirement as per International Conference on Harmonization (ICH and United States Food and Drug Administration (USFDA guidelines. The method involved the use of Agilent ZORBAX Eclipse XDB C18 column, and temperature was maintained at 30 °C. After optimization, the mobile phase was selected as phosphate buffer (KH2PO4, 30 mM : ACN (60:40, v/v with pH 3.0, and retention time Rt was found as 3.24, 4.16, and 2.55 min for paracetamol (PCM, chlorpheniramine maleate (CPM and phenylephrine hydrochloride (PH respectively at 265 nm and at a flow rate of 1 mL/min. The relative standard deviation (%RSD for 6 replicate measurements was found to be less than 2%. Furthermore net analyte signal standard addition method (NASSAM with spectrophotometer was performed for standard and liquid oral suspension. On the basis of selectivity, sensitivity and accuracy analysis, it was confirmed that this novel method could be useful for simultaneous estimation of the given drug combinations. Two-way analysis of variance (ANOVA was applied for evaluating the statistical difference between the assay results obtained via both NASSAM and RP–HPLC methods and ultimately no significant difference was found between both the methods. All the methods and results were acceptable and confirmed that the method was suitable for intended use.

  1. Influence of processing parameters and formulation factors on the drug release from tablets powder-coated with Eudragit L 100-55.

    Science.gov (United States)

    Sauer, Dorothea; Zheng, Weijia; Coots, Lonique B; McGinity, James W

    2007-09-01

    The aim of this study was to develop a dry powder coating process for chlorpheniramine maleate (CPM) tablets using Eudragit L 100-55 as the delayed release polymer. Powder coating, a water and organic solvent-free process, was investigated as a method to prevent the migration of an ionizable, highly water soluble model drug into the polymeric film during the coating process. Eudragit L 100-55 was pre-plasticized with triethyl citrate (TEC) using hot-melt extrusion at levels of 20%, 30%, and 40%, based on the polymer weight. The extrudate was subsequently cut into pellets and cryogenically ground into a fine powder. Talc was incorporated into the coating powder as an anti-tack agent. PEG 3350 was used as a primer for the powder coating of tablets with pre-plasticized Eudragit L 100-55. The addition of polyethylene glycol 3350 (PEG 3350) to the pre-plasticized Eudragit L 100-55 was necessary to enhance the adhesion of the coating powder to the tablet cores. PEG 3350 also improved film formation and coalescence of the polymeric particles due to its plasticization effects on the acrylic polymer. For comparison, theophylline tablets were also coated with pre-plasticized Eudragit L 100-55. Theophylline was selected as a less water soluble model drug. The powder coating process was performed in a modified laboratory scale spheronizer. The drug release rate was dependent both on TEC content and the coating level. The stability of the powder-coated CPM tablets was confirmed at 25 degrees C/60% RH over a storage time of 12 weeks. PMID:17451929

  2. Bee Pollen-Induced Anaphylaxis: A Case Report and Literature Review.

    Science.gov (United States)

    Choi, Jeong Hee; Jang, Young Sook; Oh, Jae Won; Kim, Cheol Hong; Hyun, In Gyu

    2015-09-01

    Bee pollen is pollen granules packed by honey bees and is widely consumed as natural healthy supplements. Bee pollen-induced anaphylaxis has rarely been reported, and its allergenic components have never been studied. A 40-year-old male came to the emergency room with generalized urticaria, facial edema, dyspnea, nausea, vomiting, abdominal pain, and diarrhea 1 hour after ingesting one tablespoon of bee pollen. Oxygen saturation was 91%. His symptoms resolved after injection of epinephrine, chlorpheniramine, and dexamethasone. He had seasonal allergic rhinitis in autumn. Microscopic examination of the bee pollen revealed Japanese hop, chrysanthemum, ragweed, and dandelion pollens. Skin-prick with bee pollen extracts showed positive reactions at 0.1 mg/mL (A/H ratio > 3+). Serum specific IgE to ragweed was 25.2, chrysanthemum 20.6, and dandelion 11.4 kU/L; however, Japanese hop, honey-bee venom and yellow-jacket venom were negative (UniCAP®, Thermo Fisher Scientific, Uppsala, Sweden). Enzyme-linked immunosorbent assay (ELISA) confirmed serum specific IgE to bee-pollen extracts, and an ELISA inhibition assay for evaluation of cross-allergenicity of bee pollen and other weed pollens showed more than 90% of inhibition with chrysanthemum and dandelion and ~40% inhibition with ragweed at a concentration of 1 μg/mL. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and IgE-immunoblot analysis revealed 9 protein bands (11, 14, 17, 28, 34, 45, 52, 72, and 90 kDa) and strong IgE binding at 28-34 kDa, 45 and 52 kDa. In conclusion, healthcare providers should be aware of the potential risk of severe allergic reactions upon ingestion of bee pollen, especially in patients with pollen allergy. PMID:25749764

  3. Thermal, mechanical and drug release characteristics of an acrylic film using active pharmaceutical ingredient as non-traditional plasticizer.

    Science.gov (United States)

    Wiranidchapong, Chutima; Kieongarm, Waraporn; Managit, Chittima; Phrompittayarat, Watoo

    2016-04-01

    The objective of this study was to investigate thermal and mechanical properties as well as in vitro drug release of Eudragit® RL (ERL) film using chlorpheniramine maleate (CPM) as either active pharmaceutical ingredient or non-traditional plasticizer. Differential scanning calorimeter was used to measure the glass transition temperature (Tg) of 0-100% w/w CPM in ERL physical mixture. Instron testing machine was used to investigate Young's modulus, tensile stress and tensile strain (%) of ERL film containing 20-60% w/w CPM. Finally, a Franz diffusion cell was used to study drug release from ERL films obtained from four formulations, i.e. CRHP0/0, CRHP0/5, CRHP2/0 and CRHP2/5. The Tg of ERL was decreased when the weight percentage of CPM increased. The reduction of the Tg could be described by Kwei equation, indicating the interaction between CPM and ERL. Modulus and tensile stress decreased whereas tensile strain (%) increased when weight percentage of CPM increased. The change of mechanical properties was associated with the reduction of the Tg when weight percentage of CPM increased. ERL films obtained from four formulations could release the drug in no less than 10 h. Cumulative amount of drug release per unit area of ERL film containing only CPM (CRHP0/0) was lower than those obtained from the formulations containing traditional plasticizer (CRHP0/5), surfactant (CRHP2/0) or both of them (CRHP2/5). The increase of drug release was a result of the increase of drug permeability through ERL film and drug solubility based on traditional plasticizer and surfactant, respectively. PMID:26133082

  4. Effect of histamine H1 and H2 receptor antagonists, microinjected into cerebellar vermis, on emotional memory consolidation in mice

    Energy Technology Data Exchange (ETDEWEB)

    Gianlorenço, A.C.L.; Serafim, K.R. [Laboratório de Neurociências, Departamento de Fisioterapia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de São Carlos, São Carlos, SP, Brasil, Laboratório de Neurociências, Departamento de Fisioterapia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de São Carlos, São Carlos, SP (Brazil); Canto-de-Souza, A. [Laboratório de Psicologia da Aprendizagem, Departamento de Psicologia, Centro de Educação e Ciências Humanas, Universidade Federal de São Carlos, São Carlos, SP, Brasil, Laboratório de Psicologia da Aprendizagem, Departamento de Psicologia, Centro de Educação e Ciências Humanas, Universidade Federal de São Carlos, São Carlos, SP (Brazil); Programa de Pós-Graduação em Ciências Fisiológicas, Universidade Federal de São Carlos, São Carlos, SP, Brasil, Programa de Pós-Graduação em Ciências Fisiológicas, Universidade Federal de São Carlos, São Carlos, SP (Brazil); Instituto de Neurociências e Comportamento, Universidade de São Paulo, Ribeirão Preto, SP, Brasil, Instituto de Neurociências e Comportamento, Universidade de São Paulo, Ribeirão Preto, SP (Brazil); Mattioli, R. [Laboratório de Neurociências, Departamento de Fisioterapia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de São Carlos, São Carlos, SP, Brasil, Laboratório de Neurociências, Departamento de Fisioterapia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de São Carlos, São Carlos, SP (Brazil)

    2014-02-17

    This study investigated the effects of histamine H1 or H2 receptor antagonists on emotional memory consolidation in mice submitted to the elevated plus maze (EPM). The cerebellar vermis of male mice (Swiss albino) was implanted using a cannula guide. Three days after recovery, behavioral tests were performed in the EPM on 2 consecutive days (T1 and T2). Immediately after exposure to the EPM (T1), animals received a microinjection of saline (SAL) or the H1 antagonist chlorpheniramine (CPA; 0.016, 0.052, or 0.16 nmol/0.1 µL) in Experiment 1, and SAL or the H2 antagonist ranitidine (RA; 0.57, 2.85, or 5.7 nmol/0.1 µL) in Experiment 2. Twenty-four hours later, mice were reexposed to the EPM (T2) under the same experimental conditions but they did not receive any injection. Data were analyzed using one-way ANOVA and the Duncan test. In Experiment 1, mice microinjected with SAL and with CPA entered the open arms less often (%OAE) and spent less time in the open arms (%OAT) in T2, and there was no difference among groups. The results of Experiment 2 demonstrated that the values of %OAE and %OAT in T2 were lower compared to T1 for the groups that were microinjected with SAL and 2.85 nmol/0.1 µL RA. However, when animals were microinjected with 5.7 nmol/0.1 µL RA, they did not show a reduction in %OAE and %OAT. These results demonstrate that CPA did not affect behavior at the doses used in this study, while 5.7 nmol/0.1 µL RA induced impairment of memory consolidation in the EPM.

  5. Effect of histamine H1 and H2 receptor antagonists, microinjected into cerebellar vermis, on emotional memory consolidation in mice

    Directory of Open Access Journals (Sweden)

    A.C.L. Gianlorenco

    2014-02-01

    Full Text Available This study investigated the effects of histamine H1 or H2 receptor antagonists on emotional memory consolidation in mice submitted to the elevated plus maze (EPM. The cerebellar vermis of male mice (Swiss albino was implanted using a cannula guide. Three days after recovery, behavioral tests were performed in the EPM on 2 consecutive days (T1 and T2. Immediately after exposure to the EPM (T1, animals received a microinjection of saline (SAL or the H1 antagonist chlorpheniramine (CPA; 0.016, 0.052, or 0.16 nmol/0.1 µL in Experiment 1, and SAL or the H2 antagonist ranitidine (RA; 0.57, 2.85, or 5.7 nmol/0.1 µL in Experiment 2. Twenty-four hours later, mice were reexposed to the EPM (T2 under the same experimental conditions but they did not receive any injection. Data were analyzed using one-way ANOVA and the Duncan test. In Experiment 1, mice microinjected with SAL and with CPA entered the open arms less often (%OAE and spent less time in the open arms (%OAT in T2, and there was no difference among groups. The results of Experiment 2 demonstrated that the values of %OAE and %OAT in T2 were lower compared to T1 for the groups that were microinjected with SAL and 2.85 nmol/0.1 µL RA. However, when animals were microinjected with 5.7 nmol/0.1 µL RA, they did not show a reduction in %OAE and %OAT. These results demonstrate that CPA did not affect behavior at the doses used in this study, while 5.7 nmol/0.1 µL RA induced impairment of memory consolidation in the EPM.

  6. Evaluation of Anti-Inflammatory and Antioxidant Potential of Ixora coccinea, Linn Ethanolic Root Extract

    Directory of Open Access Journals (Sweden)

    Kawade Rajendra

    2013-03-01

    Full Text Available The aim of this study was to investigate the anti-inflammatory potential of an ethanolic root extract (ERE of Ixora coccinea, Linn (Rubiaceae in rats by oral administration (500, 1000 and 1500 mg/kg. This was carried out by using carrageenan induced paw edema (acute inflammatory model and cotton pellet granuloma tests (chronic inflammatory model. In the former all the doses of ERE tested caused a significant (p < 0.05 to 0.001 and marked reduction in paw edema (28-59% compared to control at each time point measured. Overall, this anti-inflammatory effect seemed dose related. Indomethacin also impaired the edema formation, but this anti-inflammatory effect was much stronger (77-90%. In the latter test, ERE caused a significant (p < 0.05 and marked inhibition (36.1% of granuloma weight as compared to control (control vs. treatment: 29.2±9.6 vs. 18.6±7.1 mg. Collectively, these data show promising anti-inflammatory activity against both acute and chronic inflammation. ERE induced a significant (p < 0.05 and profound impairment by (42.6% of the area of wheal formed by the subcutaneous injection of histamine was comparable to that produced by Chlorpheniramine. It also showed promising antioxidant activity compared to Butylated hydroxyl toluene (BHT as control and dose dependent (r2 =0.9; p < 0.05 that can account for its anti-inflammatory potential. In addition, inhibition of prostaglandins and bradykinins may play a role.

  7. H1 + H2-receptor antagonists for premedication in anaesthesia and surgery: a critical view based on randomized clinical trials with Haemaccel and various antiallergic drugs.

    Science.gov (United States)

    Lorenz, W; Doenicke, A; Schöning, B; Mamorski, J; Weber, D; Hinterlang, E; Schwarz, B; Neugebauer, E

    1980-04-01

    Histamine release by drugs used in anaesthesia and surgery has been often demonstrated in human volunteers, but only occassionally in patients. Three questions arose from these studies. (1) Is the incidence of histamine release high in patients during routine anaesthesia and surgery? (2) Can the clinical effects of histamine release in man be prevented by H1 + H2-receptor antagonists? (3) Are there any side-effects of such a premedication? These problems were investigated in patients and volunteers by randomized controlled clinical trials using only one of the histamine-liberating drugs in man, the plasma substitute Haemaccel. This drug was chosen because it causes a reproducible histamine release in man and because its mechanism of action in man is largely known. (1) Out of 600 orthopaedic patients 30 (5%) showed anaphylactoid reactions following Haemaccel infusion. 26 of these had a histamine release of more than 1 ng histamine/ml plasma. Using predictive values this gives an efficiency of the test by nearly 98%. (2) In volunteers the combination of an H1-plus H2-receptor antagonist (dimethypyrindene and cimetidine) completely prevented the clinical effects of histamine release by Haemaccel (9 allergoid and anaphylactoid reactions in the control group, none in the H1 + H2-group). The incidence of histamine release, however, remained unchanged. (3) The premedication was found to release histamine itself. Cimetidine was effective when given alone but especially in combination with chlorpheniramine (4 events out of 7 applications). The clinical side-effects of these premedication were mild since apparently the free histamine was largely blocked at the receptor sites. It is concluded that premedication with a combination of H1- and H2-receptor antagonists is indicated due to the high incidence of histamine release during anaesthesia and surgery induced by various drugs and treatments. Such premedication is effective but associated with mild side-effects. For this

  8. Hypersensitivity to intravenous ondansetron: a case report

    Directory of Open Access Journals (Sweden)

    Mehra Karishma K

    2008-08-01

    Full Text Available Abstract Introduction Ondansetron, a 5-hydroxytryptamine3 receptor antagonist widely used in the prevention and treatment of chemotherapy-induced nausea and vomiting, is associated with various unusual adverse drug reactions. In this paper, we describe a hypersensitivity reaction to a single intravenous dose of ondansetron. Case presentation A 19-year-old woman presented to the emergency department of our institute with 3–4 episodes of nausea, vomiting and epigastric distress. She had a diagnosis of polycystic ovarian disease and had been on treatment with cyproterone acetate 2 mg, ethinyl estradiol 0.035 mg, finasteride 5 mg and metformin 500 mg for a month. She had been taking oral roxithromycin 500 mg per day for the past 3 days for treatment of a mild upper respiratory tract infection. She also occasionally took rabeprazole 10 mg for gastritis which had worsened after treatment with roxithromycin. She was treated with a single 4 mg dose of ondansetron intravenously. She immediately developed urticaria, which was treated with intravenous dexamethasone 4 mg and chlorpheniramine maleate 20 mg. The reaction abated within a few minutes and she was discharged within an hour. She was asymptomatic at 72 hours of follow-up. She had no history of ondansetron exposure, or drug or food allergies. On the Naranjo's causality assessment scale, the adverse event was 6 indicating a "probable" reaction to ondansetron. Conclusion 5-hydroxytryptamine3 receptor antagonists have been associated with life-threatening adverse reactions such as hypotension, seizures and anaphylaxis. The wide availability of these drugs in India has promoted their off label use in the treatment of gastritis, migraine and so on. Our case represents an off label use in a patient who could have been treated with a safer drug. Some authors have suggested that anaphylaxis may be a class effect while others think it may be drug specific. In our case, the reaction could be either

  9. 毛细管电泳法测定复方磷酸可待因口服制剂的含量%Determination of Compound Codeine Phosphate Oral Preparations by Capillary Electrophoresis

    Institute of Scientific and Technical Information of China (English)

    周震宇; 顾炳仁

    2015-01-01

    To establish a method for the simultaneous determination of the active ingredients ( codeine phosphate, brompheniramine maleate, chlorpheniramine maleate, ephedrine hydrochloride and guaifenesin) in compound codeine phosphate oral preparations by capillary electrophoresis ( CE) . Methods:The method employed an uncoated capillary column ( eCAPTM ) from Beck-mann company (50 cm × 75 μm);the electrophoresis voltage was at 10 kV;20 mmol·L-1 phosphate buffer solution (pH 7. 5) was used;the UV measurement was at the wavelength of 214 nm. Results: The studied components had good linear ranges (r≥0. 995) within the range of the investigated concentrations. The recovery was no less than 96%. Conclusion:The presented method can be ap-plied in the content determination of active ingredients in compound codeine phosphate oral preparations from different enterprises. It is simple, efficient and universal, which facilitates the market supervision in a fast and valid manner.%目的::建立毛细管电泳法( CE)法同时测定复方磷酸可待因口服制剂中磷酸可待因、盐酸麻黄碱、马来酸溴苯那敏、马来酸氯苯那敏、愈创甘油醚等有效成分的含量。方法:色谱柱为贝克曼eCAPTM未涂层石英毛细管柱(50 cm ×75μm);分离电压为10 kV;缓冲溶液为20 mmol·L-1磷酸盐缓冲液(pH 7.5);检测波长为214 nm。结果:各测定组分在考察浓度范围内线性关系良好(r≥0.995),回收率均≥96%。结论:该方法可用于不同复方磷酸可待因口服制剂中有效成分的含量测定,简单有效,具有通用性,便于快速有效的市场监督。

  10. Anaphylactic shock due to compound paracetamol and amantadine hydrochloride%复方氨酚烷胺致过敏性休克

    Institute of Scientific and Technical Information of China (English)

    任培培; 付莹

    2016-01-01

    1例68岁女性患者在右眼小梁切除+羊膜覆盖术后第2天因出现咳嗽、流涕而自行服用复方氨酚烷胺1片(每片含对乙酰氨基酚250 mg,盐酸金刚烷胺100 mg,人工牛黄10 mg,咖啡因15 mg,马来酸氯苯那敏2 mg)。服药后约30 min,患者出现头晕、恶心、呕吐,尿失禁,上肢及小腿瘙痒,面色苍白,血压80/44 mmHg(1 mmHg =0.133 kPa),脉搏90次/ min。立即给予抗过敏、扩充血容量及吸氧等处理。约30 min 后患者血压90/62 mmHg,2 h 后头晕、恶心等症状逐渐减轻,6 h 后血压106/69 mmHg。%A 68-year-old female patient self-medicated with 1 tablet of compound paracetamol and amantadine hydrochloride(each tablet contained acetaminophen 250 mg,amantadine hydrochloride 100 mg, calculus bovis factitious 10 mg,caffeine 15 mg,and chlorpheniramine maleate 2 mg)because of nasal discharge and cough on the second day of trabeculectomy with covering of amniotic membrane in her right eye. About 30 minutes after administration, she developed dizziness, nausea, vomiting, urinary incontinence,itching on her arms and calves,and pale. Her blood pressure was 80 / 44 mmHg and heart rate was 90 beats/ min. Anti-allergic treatments,blood volume expansion,and oxygen mask were given. Thirty minutes later,her blood pressure increased to 90 / 62 mmHg. The patient's symptoms gradually alleviated 2 hours later and the blood pressure increased to 106 / 69 mmHg 6 hours later.

  11. Intrathecal high-dose histamine induces spinally-mediated nociceptive behavioral responses through a polyamine site of NMDA receptors.

    Science.gov (United States)

    Watanabe, Chizuko; Orito, Tohru; Watanabe, Hiroyuki; Mizoguchi, Hirokazu; Yonezawa, Akihiko; Yanai, Kazuhiko; Mobarakeh, Jalal Izadi; Onodera, Kenji; Sakurada, Tsukasa; Sakurada, Shinobu

    2008-02-26

    Previous research has demonstrated that a high dose of histamine (1600 pmol) injected i.t. in mice can evoke nociceptive behaviors consisting of biting/licking along with occasional scratching. The present study was undertaken to examine the involvement of spinal N-methyl-d-aspartate (NMDA) and histamine H(1) and H(2) receptors in the nociceptive behaviors evoked by high-dose histamine. Co-administration of the histamine H(1) receptor antagonists, d-chlorpheniramine and pyrilamine, or the histamine H(2) receptor antagonists, ranitidine and zolantidine, failed to suppress the histamine-evoked nociceptive behaviors. Moreover, following histamine administration, nociceptive behaviors in histamine H(1) receptor-knockout and histamine H(2) receptor-knockout mice were indistinguishable from those in wild-type mice, suggesting that histamine-induced nociceptive behaviors are not mediated through histamine H(1) and H(2) receptors in the spinal cord. The histamine-induced nociceptive behaviors were inhibited by co-administration of the competitive NMDA receptor antagonists, d-(-)-2-amino-5-phosphonovaleric acid (D-APV) and 3-((+)-2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPPA), and the ion channel blocker, (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5,10-imine maleate (MK-801). Co-administration of ifenprodil, an antagonist for both the polyamine site and the NR2B subunit of NMDA receptors, also inhibited the histamine-induced nociceptive behaviors. (R-[R, S])-alpha-(4-hydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidinepropanol hydrochloride (Ro25-6981), an antagonist of the NMDA receptor subtype containing the NR2B subunit, did not inhibit histamine-induced nociceptive behaviors, whereas these behaviors were attenuated by pretreatment with an antisense oligodeoxynucleotide against the mRNA for the NR1 subunit of the NMDA receptor. Moreover, agmatine and arcaine, antagonists for a polyamine site on the NMDA receptor, inhibited nociceptive

  12. Investigation on situation of potentially inappropriate medication before and after pharmacist intervention in elderly patients in Beijing primary health care institutions%北京地区基层医疗机构药师干预前后老年患者潜在不适当用药情况调查

    Institute of Scientific and Technical Information of China (English)

    李星炜; 沈芊; 李晓玲; 刘琛; 王雅葳; 王育琴

    2015-01-01

    Objective To explore the impact of pharmacist intervention on the potentially inappropriate drug application in the elderly patients in the primary health care institutions. Methods Twenty four primary health care institutions in Beijing were selected. The researchers selected 15 kinds of potentially inappropriate drugs according to the Beers criteria and lists of potentially inappropriate drugs of USA,UK,and Japanese and organized a training of medication safety for pharmacists in above primary health care institutions. From February 10th,2014 to February 20th,2014,education on the risks of potentially inappropriate drug application in the elderly patients was carried out among the doctors in above mentioned institutions and relevant documents were distributed. Prescriptions for the elderly outpatients in the 24 primary health care institutions before(from June 3,2013 to June 7,2013)and after(from March 12,2014 to March 16,2014)the intervention were collected and the proportions of prescriptions containing 15 kinds of potentially inappropriate drugs in the prescriptions containing the appropriate diagnosis before and after the intervention were calculated and compared. Results The number of collected prescriptions in the elderly patients before and after the intervention was 12 243 and 11 571, respectively. Before the intervention,there were 10 kinds of inappropriate drugs, including estazolam, diazepam, ibuprofen, diclofenac, belladonna, theophylline, aminophylline, chlorpheniramine, digoxin, compound reserpine triamterene,and glyburide. After pharmacist intervention,the proportions of prescriptions of 5 kinds of potentially inappropriate drugs in the elderly patients decreased significantly,including ibuprofen(5. 92% vs. 27. 43%),diclofenac(5. 92% vs. 13. 17%),chlorpheniramine(1. 08% vs. 4. 86%),digoxin(2. 40% vs. 7. 56%)and glyburide(1. 61% vs. 8. 03%),all P<0. 001. Conclusion Pharmacist intervention has a positive effect on improving the potentially

  13. Clinical Study on the Chronic Urticaria Treatment by Fasting and spell%禁食轮替疗法在慢性荨麻疹中的临床研究

    Institute of Scientific and Technical Information of China (English)

    黎昌强; 李竹; 张璐; 杨碧坤; 李俏丽; 余媛

    2014-01-01

    Objective:To investigate the nearlyand long-term effect of fasting and spell combined with drugs therapy on the chronic urticaria with food specific IgG positive.Methods:The selected cases positive allergen specific IgG antibodies of food of 60 cases of chronic urticaria, were randomly divided into experimental group 30 cases and control group of 30 cases, two groups were treated with chlorpheniramine 4mg 3 times a day, cetirizine 1 tablets 1 times a day. In the experimental group was treated simultaneously fasting and spell.The effects and adverse reactions of two groups were observed after 3 months of treatment, the recurrence were observed after 6 months. Results:After 3 months treatment,the cure rate of experimental group was 53.33%,it higher than 26.67%of control group,two groups have significant difference compared (P<0.05).After 6 months treatment,the recurrence rate of experimental group was 16.67%,it lower than 43.33%of control group, two groups have significant difference compared(P<0.05).The serum food specific IgG level of experimental group decreased significantly (P<0.05)before and after treatment. Conclusion:A fast rotation therapy can effectively reduce symptoms of patients caused by food allergen specific IgG with chronic urticaria and reducing the positive rate of intolerance food. This treatment was worth popularizing.%目的:探讨禁食轮替疗法联合药物治疗由食物不耐受引起的慢性荨麻疹的近、远期疗效。方法:选取慢性荨麻疹食物特异性IgG抗体阳性病例60例,随机分为实验组30例与对照组30例,两组均采用扑尔敏4mg每天3次,西替利嗪1片每晚1次。实验组除与对照组相同的治疗外,加用禁食、轮替的方法,3个月后观察疗法疗效及不良反应,6个月后观察复发情况。结果:3个月后实验组痊愈率53.33%,高于对照组26.67%,两组比较差异有显著性(P<0.05)。6个月后复发率实验组16.67%,对照组43.33%,两

  14. 孤束核胆碱能与组胺能系统对颈动脉窦压力感受器反射调节的交互作用%Involvement of cross interaction between central cholinergic and histaminergic systems in the nucleus tractus solitarius in regulating carotid sinus baroreceptor reflex

    Institute of Scientific and Technical Information of China (English)

    胡力旬; 张国兴; 张玉英; 赵红芬; 于康英; 王国卿

    2013-01-01

    脑胆碱能系统与组胺能系统影响颈动脉窦压力感受器反射(carotid sinus baroreceptor reflex,CSR)活动,然而二者是否在孤束核(nucleus tractus solitarius,NTS)水平相互作用,跨转调节CSR,尚不清楚.本文在麻醉Sprague-Dawley (SD)大鼠孤离的一侧颈动脉窦区,通过窦内逐级加压引发CSR和动脉血压变化,经Logistic五参数曲线拟合,求得窦内压(intracarotid sinus pressure,ISP)-平均动脉压(mean arterial pressure,MAP)关系曲线及其特征参数,观察预先在NTS微量注射各选择性胆碱能受体拮抗剂[M1受体拮抗剂哌仑西平(pirenzepine,PRZ)、M2受体拮抗剂美索曲明(methoctramine,MTR)或N1受体拮抗剂六烃季胺(hexamethonium,HEX)]对侧脑室微量注射(intracerebroventricular injection,i.c.v.)组胺(histamine,HA)所致CSR变化的影响,以及预先在NTS微量注射组胺能H1受体拮抗剂氯苯吡胺(chlorpheniramine,CHL)或H2受体拮抗剂西咪替丁(cimetidine,CIM)对i.c.v.拟胆碱药毒扁豆碱(physostigmine,PHY)所致CSR变化的影响,以期解析中枢两大系统对CSR是否具有跨转调节机制.结果显示:(1)单独NTS内注射所给剂量的各选择性胆碱能受体拮抗剂或组胺能受体拮抗剂对CSR均无明显作用(P>0.05),也不引起动脉血压水平明显变动;(2)预先NTS内注射PRZ或MTR可部分翻转i.c.v.HA所致的CSR重调定,表现为ISP-MAP关系曲线在高窦压区明显左下移位(P<0.05),ISP-Gain关系曲线在中窦压区显著上移(P<0.05),反射参数平均动脉压变动范围和最大增益加大(P<0.05),最大增益时的窦内压值与饱和压减少(P<0.05),上述效应中PRZ的作用不如MTR的显著(P<0.05),但HEX对i.c.v.HA所致的CSR变化无明显作用(P>0.05);(3)预先NTS内注射CHL或CIM对i.c.v.PHY所致CSR变化的影响,类似于NTS内注射PRZ或MTR对i.c.v.HA所致CSR变化的作用,且CHL的效应强于CIM (P< 0.05).上述结果表明:侧脑室注射HA所致的CSR重调定机制