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Sample records for chlorpheniramine

  1. Acute anaphylactic reaction to expired chlorpheniramine injection

    Institute of Scientific and Technical Information of China (English)

    Beuy Joob; Viroj Wiwanitkit

    2014-01-01

    Chlorpheniramine is a widely used drug for management of allergic reaction.The serious adverse reaction to this drug is extremely rare.In this report, the authors present a case of acute anaphylactic reaction to expired chlorpheniramine injection.

  2. Compound list: chlorpheniramine [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available chlorpheniramine CHL 00090 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in_vitro/chlorph...eniramine.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitro/chlorph...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 ...

  3. Chlorpheniramine

    Science.gov (United States)

    ... product you plan to use. Check the package label for a list of the ingredients.tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or ...

  4. 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.

  5. 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.

  6. 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

  7. Sensing of chlorpheniramine in pharmaceutical applications by sequential injector coupled with potentiometer

    Institute of Scientific and Technical Information of China (English)

    Tawfik A. Saleh

    2011-01-01

    This paper reports on development of a system consisting of a portable sequential injector coupled with potentiometric unit for sensing of chlorpheniramine (CPA), based on the reaction of CPA with potassium permanganate in acidic media. Various experimental conditions affecting the potential intensity were studied and incorporated into the procedure. Under the optimum conditions, linear relationship between the CPA concentration and peak area was obtained for the concentration range of 0.1-50 ppm. The method reflects good recovery with relative standard deviation (RSD)〈 3 %. The detection limit was 0.05 ppm. The developed method was successfully applied for determination of CPA in pure form and in pharmaceutical dosage forms. The results, obtained using the method, are in accord with the results of the British pharmacopoeia method. In addition to its accuracy and precision, the method has the advantages of being simple, inexpensive and rapid.

  8. 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

  9. 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...

  10. [Stevens-Johnson syndrome plus intrahepatic cholestasis caused by clindamycin or chlorpheniramine].

    Science.gov (United States)

    Sahagún Flores, J E; Soto Ortiz, J A; Tovar Méndez, C E; Cárdenas Ochoa, E C; Hernández Flores, G

    2009-05-15

    A 48-year-old woman was hospitalized with the diagnosis of hepatitis. She presented with symptoms of jaundice, headache, elevated bilirubin, and elevated hepatic enzymes. She related a recent episode of a bronchial infection that was treated during the previous eight days with paracetamol (500mg, 2 doses only), chlorpheniramine, betamethasone and clindamycin. After an initial clinical and laboratorial improvement, she began to complain of pruritus of the palms and soles. Thereafter, vesicles evolving to blisters developed and a deterioration of her general health ensued. Serologies for hepatitis A, B, and C viruses were negative. Intrahepatic cholestasis and Stevens Johnson Syndrome (SJS) were the final diagnosis. The association of the Stevens Johnson Syndrome and intrahepatic cholestasis simultaneously, related to adverse drug reactions, is very rare. The drugs reportedly involved are mainly antibiotics, such as ampicillin, vancomycin, amoxicillin/clavulinic acid and erythromycin. Other drugs involved are non-steroidal anti-inflamatory drugs, such as mefenamic acid, ibuprofen, and sulindac. The reactions can be minor or severe and can even cause death, an outcome that has been reported in patients of all races and ethnic groups, but appears to be more rare in patients of Latin origin. We present a discussion of this case and review the main characteristics of the Stevens Johnson Syndrome.

  11. 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

  12. Nonsteroidal management of canine pruritus: chlorpheniramine and a fatty acid supplement (DVM Derm Caps) in combination, and the fatty acid supplement at twice the manufacturer's recommended dosage.

    Science.gov (United States)

    Scott, D W; Miller, W H

    1990-10-01

    Forty-three dogs having pruritus associated with atopy, flea bite hypersensitivity, and idiopathy were randomly assigned to 1 of 2 treatment protocols. Twenty-three dogs received chlorpheniramine in combination with a fatty acid supplement (DVM Derm Caps). Twenty dogs received the fatty acid supplement at twice the manufacturer's recommended dosage. All 43 dogs were known to be unresponsive to chlorpheniramine and the manufacturer's recommended dosage of the fatty acid supplement when either drug was used alone. Pruritus was satisfactorily controlled in 34.8% of the dogs in the chlorpheniramine--DVM Derm Caps protocol. No dog in the double DVM Derm Caps protocol showed a beneficial response. Side effects were uncommon and mild with either protocol.

  13. 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

  14. 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.

  15. 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

  16. 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

  17. 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.

  18. 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...

  19. 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

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

    Directory of Open Access Journals (Sweden)

    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.

  1. 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

  2. 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。

  3. Dorsal hippocampal microinjection of chlorpheniramine reverses the anxiolytic-like effects of l-histidine and impairs emotional memory in mice.

    Science.gov (United States)

    Canto-de-Souza, L; Garção, D C; Romaguera, F; Mattioli, R

    2015-02-01

    Several findings have pointed to the role of histaminergic neurotransmission in the modulation of anxiety-like behaviors and emotional memory. The elevated plus-maze (EPM) test has been widely used to investigate the process of anxiety and also has been used to investigate the process of learning and memory. Visual cues are relevant to the formation of spatial maps, and as the hippocampus is involved in this task, experiment 1 explored this issue. Experiment 2 investigated the effects of intraperitoneal (i.p.) injections of l-histidine (LH, a precursor of histamine) and of intra-dorsal hippocampus (intra-DH) injections of chlorpheniramine (CPA, an H1 receptor antagonist) on anxiety and emotional memory in mice re-exposed to the EPM. Mice received saline (SAL) or LH i.p. and SAL or CPA (0.016, 0.052, and 0.16 nmol/0.1 μl) intra-DH prior to Trial 1 (T1) and Trial 2 (T2). No significant changes were observed in the number of enclosed-arm entries (EAE) in T1, an EPM index of general exploratory activity. LH had an anxiolytic-like effect that was reversed by intra-DH injections of CPA. T2 versus T1 analysis revealed that only the lower dose of CPA resulted in impaired emotional memory. Combined injections of LH and CPA revealed that higher doses of CPA impair emotional memory. Taken together, these results suggest that LH and H1 receptors present in the dorsal hippocampus are involved in anxiety-related behaviors and emotional memory in mice submitted to EPM.

  4. 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

  5. Clinical effect of dextromethorphan-chlorpheniramine-pseudoephedrine solution on postinfectious cough%美敏伪麻溶液治疗感染后咳嗽临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    许先荣; 李玉花; 柴秀娟

    2009-01-01

    目的:观察美敏伪麻溶液治疗感染后咳嗽的疗效.方法:78例感染后咳嗽的患者随机分为治疗组和对照组,对照组口服酮替芬片(1 mg,bid,7 d),阿奇霉素片(0.5 g,qd,3d);治疗组12'服美敏伪麻溶液(10 mL,tid,7 d),阿奇霉素片(0.5 g,qd,3 d);按咳嗽症状得分在7 d后评价疗效.结果:治疗组与对照组治疗前咳嗽症状得分分别为(5.4±1.2)分及(5.5±1.2)分,2组间差异无显著性(P>0.05),治疗后得分分别为(2.3±1.3)分及(3.2±1.3)分,与治疗前相比,差异均有显著性(P均0. 05). After 7-day's treatment, the cough symptom scores of the study group and control group were 2.3±1.3 and 3.2±1.3 respectively, there were significant differences between before and after treatment for both groups (P<0. 01 ). After treatment,symptom scores of the study group were lower than that of control group, there were significant differences between two groups (P<0.01). The efficiency rate were 76. 3% in study group and 45% in control group, there were significant differences between two groups (P<0.01). The clinical effects of study group was better than the control group. CONCLUSION Dextromethorphan-chlorpheniramine-pseudoephedrine solution has significant therapeutic effects on postinfectious cough,and can be a choose for the treatment of postinfeetious cough.

  6. 健康志愿者单次和多次口服美敏伪麻缓释胶囊的药动学研究%Pharmacokinetics of Dextromethorphan Chlorpheniramine Pseudoephedrine Controlled-release Capsule after single and multiple doses in healthy volunteers

    Institute of Scientific and Technical Information of China (English)

    刘东阳; 赵芊; 宗海军; 沈凯; 江骥; 胡蓓

    2015-01-01

    Objective To investigate pharmacokinetics of Dextromethorphan Chlorpheniramine Pseudoephedrine Controlled-release Capsule after single and multiple doses, and make an assessment on the security in healthy volunteers.Methods Random and open trial was carried out for 22 healthy volunteers. A single and multiple oral dose of Dextromethorphan Chlorpheniramine Pseudoephedrine Controlled-release Capsule were given. The concentrations of dextromethorphan, chlorpheniramine, pseudoephedrine, and dextrorphan in plasma were determined by LC-MS/MS method. Pharmacokinetic parameters were calculated using WinNonlin program. Safety was evaluated using observed adverse events.Results No observed severe adverse event was reported. For chlorpheniramine, pseudoephedrine, dextromethorphan, and dextrorphan, median oftmax were about 3.0 — 5.0 h,means of t1/2 were 6.30 ± 1.17, 23.3 ± 6.90, 10.4 ± 2.19, and 8.62 ± 3.04 h. Means ofCmax were 203 ± 40.4, 5.05 ± 1.39, 4.29 ± 3.95, and 1.9 5 ± 0.720 ng/mL. Means of AUClast were 2 055 ± 559, 137 ± 47.5, 61.3 ± 67.5, and 17.2 ± 6.58. Means of AUCinf were 2 140 ± 570, 161 ± 63.8, 17.6 ± 6.65, and 62.8 ± 69.3μg·h/L after single dose. After four-day continuous dosing, steady status was reached for all compounds. TheirCmax,Cmin, and AUCtau, ss increased by different extent, and FI were within the range of 107% — 271%.Conclusion Dextromethorphan Chlorpheniramine Pseudoephedrine Controlled-release Capsule reaches steady status after four-day continuous doses, plasma exposures of four compounds increase than those after single dose, and capsule are well tolerated in healthy volunteers.%目的:研究美敏伪麻缓释胶囊经单、多次给药后的药动学特征,评估其在健康志愿者体内的安全性。方法22例受试者随机、开放试验设计,研究单、多次给药药动学特征。血浆中氯苯那敏、伪麻黄碱、右美沙芬、右啡烷采用LC-MS/MS法测定,药动学参数采用WinNonlin软件

  7. 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.

  8. 布洛伪麻那敏胶囊治疗成人普通感冒的多中心随机双盲对照临床研究%Multi center randomized double-blind clinical comparison of ibuprofen and pseudoephedrine chlorphenira-mine capsule in the treatment of adult common cold

    Institute of Scientific and Technical Information of China (English)

    邓俊; 王宋平; 张睢扬; 孙圣华; 肖贞良; 崔社怀

    2016-01-01

    Objective To evaluate the efficacy and safety of ibuprofen pseudoephedrine hydrochloride and chlorpheniramine maleate cpasules in the treatment of adult common cold. Methods A multicenter, randomized, double-blind, double-dummy, and positive drug parallel-controlled clinical trial was conducted. The trial group and the control group were administered with ibuprofen pseudoephedrine hydrochloride and chlorpheniramine maleate cpa-sules and paracetamol pseudoephedrine hydrochloride and chlorphenamine maleate tablets, respectively. The medi-cine was taken orally one cpasule (tablet), three times a day for 3 to 5days for each group. Results The total effec-tive rate and control rate of the trial group (n=119) and the control group (n=119) enrolled in the full analysis set (FAS) were 98. 32% vs. 97. 48% and 86. 55% vs. 93. 28%, respectively, while those of the trial group (n=117) and the control group (n=115) enrolled in the per protocol set (PPS) were 98. 29% vs. 98. 26% and 86. 32% vs. 93. 91%, respectively (P>0. 05). After the treatment, the effective rate and control rate of the individual symptom (fever, headache, limb ache, stuffy nose, sneezing, runny nose) showed no significant difference between the two groups ( P>0. 05 ) . The incidence of adverse drug reactions ( including mild drowsiness, dizziness, fatigue, and thirsty) in the trial group and the control group was 13. 45% and 11. 76%, respectively, with no statistical signifi-cant difference between the two groups ( P >0. 05 ) . Conclusion Ibuprofen pseudoephedrine hydrochloride and chlorpheniramine maleate cpasules is safe and effective in treating adult common cold. Its therapeufic efficacy and safety are similar to paracetamol pseudoephedrine hydrochloride and chlorphenamine maleate tablets.%目的:评价天圣制药集团股份有限公司研制生产的布洛伪麻那敏胶囊治疗成人普通感冒的疗效和安全性。方法采用多中心、随机、双盲、双模拟、阳性药物平行对照

  9. 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.

  10. Drug: D04323 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04323 Mixture, Drug dl-Methylephedrine hydrochloride - noscapine - chlorpheniramin...R SYSTEMIC USE R06AB Substituted alkylamines R06AB54 Chlorphenamine, combinations D04323 dl-Methylephedrine

  11. Dapsone versus corticosteroids in lichen planus

    Directory of Open Access Journals (Sweden)

    Chopra Adarsh

    1999-01-01

    Full Text Available Seventy five patients with Lichen Planus (LP were enrolled from out-patient department for screening the therapeutic effect of dapsone. Patients were divided into two groups of 50 and 25. In regimen - 1 (RI 25 patients were given local corticosteroids and oral chlorpheniramine maleate. In regimen - 2 (R2 50 patients were given oral dapsone and chlorpheniramine maleate and topical coconut oil. It was found that total efficacy of R2 was 18% higher than R1.

  12. 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.

  13. A role for the central histaminergic system in the leptin-mediated increase in cardiovascular dynamics.

    Science.gov (United States)

    Rao, Sumangala P; Dunbar, Joseph C

    2005-01-15

    The central nervous system (CNS) histaminergic neurons have been shown to regulate feeding behavior and are a target of leptin in the brain. The present study aimed to examine the involvement of the histaminergic system in the leptin-mediated regulation of cardiovascular dynamics. We investigated the cardiovascular responses to the CNS administration of histamine, leptin and alpha-melanocyte stimulating hormone (alpha-MSH) both in the presence and absence of the histamine H1 antagonist, chlorpheniramine. The intracerebroventricular (i.c.v.) administration of histamine resulted in an immediate increase in both mean arterial pressure (MAP) and heart rate (HR) and vasoconstricted the iliac, renal and superior mesenteric vessels. The i.c.v. pretreatment with chlorpheniramine attenuated the histamine-induced increase in MAP, HR and decreased vascular conductance. The i.c.v. administration of leptin increased MAP and HR and decreased vascular conductance. The i.c.v. pretreatment with chlorpheniramine decreased the leptin-induced increase in MAP and the leptin-mediated iliac vasoconstriction. The i.c.v. administration of alpha-MSH also increased MAP, HR and decreased vascular conductance. However, pretreatment with chlorpheniramine did not influence the central alpha-MSH-mediated increase in MAP, HR and decreased vascular conductance. These results indicate that the central histaminergic system mediated by H1 receptors have a role in the central signaling pathway and is involved in leptin's regulation of cardiovascular dynamics. It appears that leptin directly or indirectly stimulates histaminergic neurons that lead to increased cardiovascular activity.

  14. On the employment of lambda carrageenan in a matrix system. III. Optimization of a lambda carrageenan-HPMC hydrophilic matrix

    NARCIS (Netherlands)

    Bonferoni, MC; Rossi, S; Ferrari, F; Bertoni, M; Bolhuis, GK; Caramella, C

    1998-01-01

    The lambda carrageenan/HPMC ratio in matrix tablets has been optimized in order to obtain pH-independent release profiles of chlorpheniramine maleate, a freely soluble drug. Release profiles in acidic (pH 1.2) and neutral (pH 6.8) media were fitted according to the Weibull and the power law models.

  15. 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.

  16. Evaluation of Prosopis africana Seed Gum as an Extended Release Polymer for Tablet Formulation

    OpenAIRE

    Nadaf, Sameer; Nnamani, Petra; Jadhav, Namdeo

    2014-01-01

    In the present work, an attempt has been made to screen Prosopis africana seed gum (PG), anionic polymer for extended release tablet formulation. Different categories of drugs (charge basis) like diclofenac sodium (DS), chlorpheniramine maleate (CPM), and ibuprofen (IB) were compacted with PG and compared with different polymers (charge basis) like xanthan gum (XG), hydroxypropyl methyl cellulose (HPMC-K100M), and chitosan (CP). For each drug, 12 batches of tablets were prepared by wet granul...

  17. 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)...

  18. Quality research of Part Pediatric Paracetamol Atificial Cow-bezoar and Chlorphenamine Maleate Granules on the market%市场上部分小儿氨酚黄那敏颗粒的质量调研

    Institute of Scientific and Technical Information of China (English)

    郝晶晶; 李海亮; 李伟; 梁卓; 李金梅

    2013-01-01

    Objective To investigate the content uniformity of aceta minophen and chlorpheniramine maleate in Pediatric Paracetamol Atificial Cow-bezoar and Chlorphenamine Maleate Granules on the market. Methods Eight products of Pediatric Paracetamol Atificial Cow-bezoar and Chlorphenamine Maleate Granules on the market were sampled. The high performance liquid chromatography (HPLC) was used to measure the content uniformity of acetaminophen and chlorpheniramine maleate at the same time. Results Taking the content uniformity of acetaminophen and chlorpheniramine maleate as the measuring standards, the content uniformity of acetaminophen of 7 products was qualified and the content uniformity of chlorpheniramine maleate of 1 product was qualified. Conclusion Among the sampled products of Pediatric Paracetamol Atificial Cow-bezoar and Chlorphenamine Maleate Granules, only 1 product reaches the eligibility requirements.%目的 调研现市场上小儿氨酚黄那敏颗粒中对乙酰氨基酚和马来酸氯苯那敏的含量均匀度,考察该产品的质量情况.方法 通过抽查现市场上8个小儿氨酚黄那敏颗粒产品,采用高效液相色谱法(HPLC)同时测定对乙酰氨基酚和马来酸氯苯那敏的含量均匀度.结果 以对乙酰氨基酚和马来酸氯苯那敏的含量均匀度为衡量标准,有7个产品的对乙酰氨基酚的均匀度合格;有1个产品马来酸氯苯那敏的均匀度合格.结论 所抽查的小儿氨酚黄那敏颗粒质量只有1个达到合格要求.

  19. 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...

  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. [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

  2. 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

  3. Preparation and Characterization of β-Cyclodextrin Derivatized Ovalbumin Used as Chiral Selector in Pressure Capillary Electrochromatography

    Institute of Scientific and Technical Information of China (English)

    YU Yu-hong; TANG Li; DAI Rong-ji; DENG Yu-lin; FU Ruo-nong

    2007-01-01

    Synthesis and properties of β-cyclodextrin derivatized ovalbumin used as chiral selector were investigated.β-cyclodextrin derivatized ovalbumin was synthesized using β-cyclodextrin and ovalbumin in the presence of ethylene glycol diglycidyl ether in boric acid buffer at pH value 8.7 at 37 ℃.Amino group was coated on the internal surface of the silica capillary by sol-gel technology with triethoxylmethylsiloxane and (3-arninopropyl)trimethoxysiloxane.Covalent binding of β-cyclodextrin derivatized ovalbumin was performed by glutaraldehyde.Enantiomers of chlorpheniramine,phenylalanine and atropine were separated by pressure capillary electrochromatography column coated with β-cyclodextrin derivatized ovalbumin.

  4. 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

    with 44 g/h of amino acid mixtures with or without His for 10 h. Infusates were administered in a 2 x 2 factorial arrangement within a 4 x 4 Latin square to 4 multiparous Holstein cows in mid lactation. Exclusion of His from the infusate decreased protein content in milk from the infused udder half from 3......) blocker decreased milk production in the infused udder half from 4.6 to 3.5 kg without affecting protein, fat, and lactose percentages, suggesting an inhibition of milk ejection. Cows on chlorpheniramine ate less feed during the infusion than saline-infused cows, which resulted in lower arterial...

  5. 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. ...

  6. Pharmacological characterisation of cardiovascular histamine receptors in man in vivo.

    Science.gov (United States)

    Boyce, M J

    1982-09-01

    Data from pharmacological studies carried out in healthy subjects using systemic histamine or impromidine and their antagonists are reviewed. Exogenous histamine by rapid injection appears to stimulate only H1-receptors. Chlorpheniramine alone antagonised the responses to histamine. The effects of cardiovascular H2-receptor stimulation are demonstrated best by a sustained and large dose of histamine given by infusion. If it be considered desirable to antagonise all the cardiovascular responses to endogenous histamine, the available pharmacological data in man suggest this would be achieved best by a combination of an H1-and H2-receptor antagonist.

  7. Cerebellar vermis H₂ receptors mediate fear memory consolidation in mice.

    Science.gov (United States)

    Gianlorenço, A C L; Riboldi, A M; Silva-Marques, B; Mattioli, R

    2015-02-01

    Histaminergic fibers are present in the molecular and granular layers of the cerebellum and have a high density in the vermis and flocullus. Evidence supports that the cerebellar histaminergic system is involved in memory consolidation. Our recent study showed that histamine injections facilitate the retention of an inhibitory avoidance task, which was abolished by pretreatment with an H2 receptor antagonist. In the present study, we investigated the effects of intracerebellar post training injections of H1 and H2 receptor antagonists as well as the selective H2 receptor agonist on fear memory consolidation. The cerebellar vermi of male mice were implanted with guide cannulae, and after three days of recovery, the inhibitory avoidance test was performed. Immediately after a training session, animals received a microinjection of the following histaminergic drugs: experiment 1, saline or chlorpheniramine (0.016, 0.052 or 0.16 nmol); experiment 2, saline or ranitidine (0.57, 2.85 or 5.07 nmol); and experiment 3, saline or dimaprit (1, 2 or 4 nmol). Twenty-four hours later, a retention test was performed. The data were analyzed using one-way analysis of variance (ANOVA) and Duncan's tests. Animals microinjected with chlorpheniramine did not show any behavioral effects at the doses that we used. Intra-cerebellar injection of the H2 receptor antagonist ranitidine inhibited, while the selective H2 receptor agonist dimaprit facilitated, memory consolidation, suggesting that H2 receptors mediate memory consolidation in the inhibitory avoidance task in mice.

  8. 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.

  9. 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

  10. Cardiovascular effects of histamine administered intracerebroventricularly in critical haemorrhagic hypotension in rats.

    Science.gov (United States)

    Jochem, J

    2000-06-01

    The study was designed to determine the cardiovascular effects of histamine administered intracerebroventricularly (icv) in a rat model of volume-controlled haemorrhagic shock. The withdrawal of approximately 50% of total blood volume resulted in the death of all control saline icv treated animals within 30 min. Icv injection of histamine produced a prompt dose-dependent (0.1-100 nmol) and long-lasting (10-100 nmol) increase in mean arterial pressure (MAP), pulse pressure (PP) and heart rate (HR), with a 100% survival of 2h after treatment (100 nmol). The increase in MAP and HR after histamine administration in bled rats in comparison to the normovolaemic animals was 2.7-3.3- and 1.3-3.6-fold higher, respectively. Pretreatment with chlorpheniramine (50 nmol icv), H1 receptor antagonist, inhibited the increase in MAP, PP, HR and survival rate produced by histamine, while chlorpheniramine given alone had no effect. Neither ranitidine (50 nmol icv), H2 histamine receptor antagonist, nor thioperamide (50 nmol icv), H3 receptor blocker, influenced the histamine action, however, when given alone, both evoked the pressor effect with elongation of survival time. It can be concluded that histamine administered icv reverses the haemorrhagic shock conditions, and histamine H1 receptors are involved.

  11. Effect of Two Histamine Receptor Antagonists on Hematology of Porcine Reproductive and Respiratory Syndrome%组胺受体拮抗剂对高致病性猪蓝耳病血液学的影响

    Institute of Scientific and Technical Information of China (English)

    刘芳; 高登慧; 欧德渊; 万文华; 向智龙; 禾采红; 黄露

    2011-01-01

    为探索组胺(HA)受体拮抗剂对高致病性蓝耳病(PRRS)病毒感染患猪血液学的影响,揭示内源性组胺在高致病性猪蓝耳病发生发展过程中的部分作用,通过人工使仔猪感染高致病性蓝耳病,并相应注射扑尔敏、西咪替丁后第5天采用RT-PCR方法检测仔猪血液中的PRRSV,第7天采用ETDA抗凝管颈静脉采血,全自动血液分析仪测定血液指标.结果表明,1)攻毒后第5天均扩出1条约1064 bp的特异性目的条带,表明攻毒成功;2)西咪替丁组、阳性组仔猪血液中白细胞总数、淋巴细胞数量、单核细胞数量极显著低于阴性组(P<0.01),而扑尔敏组均显著高于阳性组(P<0.05);3)阳性组仔猪血液中血红蛋白浓度、红细胞压积显著低于阴性组(P<0.05),西咪替丁组红细胞数显著高于阳性组;4)扑尔敏组、西咪替丁组仔猪血液中血小板含量、血小板压积极显著高于阴性组(P<0.0l),阳性组血小板含量极显著高于阴性组(P<0.01),阳性组血小板压积显著高于阴性组(P<0.05).说明,扑尔敏能抑制高致病性蓝耳病患猪血液中白细胞总数、白细胞中淋巴细胞数量和白细胞中单核细胞数量的下降,稳定红细胞相关指标的数量,具有增强机体免疫力的作用,但促进了血小板的升高,西咪替丁能维持高致病性蓝耳病患猪血液中红细胞相关指标的稳定.%The piglets artificially infected with porcine reproductive and respiratory syndrome were injected with two histamine receptor antagonists (Cimetidine and Chlorpheniramine) and then PRRSV in tested piglets was detected by RT-PCR after 5d and the blood indexes were determined by an automatic blood analyzer after 7 d to study the effect of histamine receptor antagonist on hematology of porcine reproductive and respiratory syndrome and to reveal the part effect of endogenous histamine on occurrence and development of porcine reproductive and respiratory syndrome. The

  12. The Synthesis and Characterization of β-cyclodextrin Derivated Pancreatin Used as Chiral Selector in Capillary Electrochromatography

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    The preparation of capillary electrochromatography column for chiral separation with β-cyclodextrin derivatized Pancreatin was investigated, which had three steps, synthesis ofβ-cyclodextrin derivated pancreatin, the modification of the capillary internal surface and the covalent binding of β-cyclodextrin derivated pancreatin on the capillary internal wall. β-cyclodextrin derivated pancreatin was synthesized using β-cyclodextrin and protein in the presence of ethylene glycol diglycidyl ether (EGDE) in boric acid buffer at pH = 8.7. Amino group was coated on the internal surface of the silica capillary by sol-gel technology using triethoxylmethylsiloxane and (3- aminopropyl ) trimethoxysiloxane . Covalent binding of β- cyclodextrin derivated pancreatin was performed by glutaraldehyde. Chlorpheniramine, phenylalanine and troopine were separated baseline by β-cyclodextrin derivated pancreatin in capillary electrochromatography.

  13. 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.

  14. Effect of restraint stress on nociceptive responses in rats: role of the histaminergic system.

    Science.gov (United States)

    Ibironke, G F; Mordi, N E

    2011-12-20

    Stress induced analgesia (SIA) is well known, but the reverse phenomenon, hyperalgesia is poorly documented. This study investigated the role of the histaminergic system in restraint stress hyperalgesia in rats, using thermal stimulation method (hot plate and tail flick tests). Paw licking and tail withdrawal latencies were taken before and after restraint for about one hour. Significant decreases (p<0.05) were obtained in these latencies after the restraint in both tests. Administration of H1 and H2 receptor blockers, chlorpheniramine and cimetidine respectively 30 mins before the restraint still resulted in significant reductions (p<0.05) in these latencies, connoting the persistence of hyperalgesia, showing that histamine H1 and H2 receptors did not participate in the mechanism of restraint stress hyperalgesia. We therefore suggest a histaminergic independent mechanism for restraint stress induced hyperalgesia.

  15. Treatment of Urticaria with Cupping at Back-Shu Points - A Report of 40 Cases

    Institute of Scientific and Technical Information of China (English)

    李丽梅; 丁杰

    2001-01-01

    @@Urticaria is a common and frequently encountered disease, which is mainly manifested by extreme pruritus and lumpish eruption of the skin. Acute urticaria with a short disease course can be cured, while the chronic one with repeated attacks is a lingering disorder. In the past few years, 40 cases of urticaria were treated by cupping at the back-shu points of the five zang-organs and Geshu (BL 17). Another 20 cases in the control group were treated with Fang Feng Tong Sheng Wan (防风通圣丸Miraculous Pills of Ledebouriella) and chlorpheniramine maleate. The therapeutic effect in the treatment group was significantly superior to that in the control group. The results are reported as follows.

  16. 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

  17. 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.

  18. Antihistaminic activity of Clitoria ternatea L. roots.

    Science.gov (United States)

    Taur, Dnyaneshwar J; Patil, Ravindra Y

    2010-12-01

    Clonidine, a α2 adrenoreceptor agonist induces dose dependent catalepsy in mice, which was inhibited by histamine H1 receptor antagonists but not by H2 receptor antagonist. Clonidine releases histamine from mast cells which is responsible for different asthmatic conditions. Clitoria ternatea L. (Family: Fabaceae) is a perimial twing herb. The roots have anti-inflammatory properties and are useful in severe bronchitis, asthma. In present study ethanol extract of Clitoria ternatea root (ECTR) at doses 100, 125 and 150 mg/kg i.p were evaluated for antihistaminic activity using clonidine and haloperidol induced catalepsy in mice. Finding of investigation showed that chlorpheniramine maleate (CPM) and ECTR inhibit clonidine induced catalepsy significantly P < 0.001 when compare to control group, while CPM and ECTR fail to inhibit haloperidol induced catalepsy. Present study concludes that ECTR possesses antihistaminic activity. PMID:24826001

  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. Correlation Analysis of Common Cold Medicine Ingredients Based on Principal Component Analysis%基于主成份分析法的常用抗感冒药成分相关性分析

    Institute of Scientific and Technical Information of China (English)

    汤宏明

    2013-01-01

    本文对常用抗感冒药进行调查统计的基础上,运用主成份分析的方法,对样本的成分进行分类分析。分析结果表明:抗感冒药一般成分主要有主要乙酰胺基酚、盐酸伪麻黄碱、氢溴酸右美沙芬、扑尔敏、盐酸金刚烷胺、人工牛黄、咖啡因。乙酰胺基酚、盐酸伪麻黄碱、氢溴酸右美沙芬为同一类;扑尔敏为一类;盐酸金刚烷胺、人工牛黄、咖啡因也是一类。此结论基本上是正确合理的,对家庭或医生抗感冒药的选择具有一定的指导作用。%In this paper, commonly used anti-cold medicine survey based on the use of principal component analysis, classification analysis of the composition of the sample. Analysis showed that: the general composition of the anti-cold medicine the major acetaminophen, pseudoephedrine hydrochloride, hydrogen bromideacid dextromethorphan, chlorpheniramine, amantadine hydrochloride, artificial bezoar, caffeine. Acetaminophen, pseudoephedrine hydrochloride, hydrobromide right dextromethorphan same class; chlorpheniramine as a class; amantadine hydrochloride artificial bezoar, caffeine, is also a class. This conclusion is basically correct and reasonable, and has a guiding role in the family or doctors the choice of anti-cold medicine.

  1. 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

  2. Multiple unit gastroretentive drug delivery systems: a new preparation method for low density microparticles.

    Science.gov (United States)

    Streubel, A; Siepmann, J; Bodmeier, R

    2003-01-01

    The aim of this study was to develop a new preparation method for low density foam-based, floating microparticles and to demonstrate the systems' performance in vitro. Major advantages of the novel preparation technique include: (i) short processing times, (ii) no exposure of the ingredients to high temperatures, (iii) the possibility to avoid toxic organic solvents, and (iv) high encapsulation efficiencies close to 100%. Floating microparticles consisting of polypropylene foam powder, model drug [chlorpheniramine maleate (CPM), diltiazem HCl, theophylline or verapamil HCl] and polymer [Eudragit RS or polymethyl methacrylate (PMMA)] were prepared by soaking the microporous foam carrier with an organic solution of drug and polymer and subsequent drying. The effects of various formulation and processing parameters on the resulting in vitro floating behaviour, internal and external particle morphology, drug loading, in vitro drug release and physical state of the incorporated drug were studied. Good in vitro floating behaviour was observed in most cases and a broad variety of drug release patterns could be achieved by varying the drug loading and type of polymer. Interestingly, PMMA-based microparticles showed incomplete drug release with verapamil HCl. This restriction could be overcome by forming the free base of the drug prior to microparticle preparation. In contrast to the salt, the free base acted as a plasticizer for PMMA, resulting in sufficiently high diffusion coefficients and, consequently, complete drug release. The low density microparticles were compressed into rapidly disintegrating tablets in order to provide an administrable oral dosage form.

  3. 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

  4. Involvement of the histaminergic system in cytidine 5'-diphosphocholine-induced reversal of critical haemorrhagic hypotension in rats.

    Science.gov (United States)

    Jochem, J; Savci, V; Filiz, N; Rybus-Kalinowska, B; Fogel, W A; Yalcin, M

    2010-02-01

    Cytidine 5'-diphosphocholine (CDP-choline) is an endogenously synthesized mononucleotide which exerts a variety of physiological effects by altering central cholinergic transmission. Administered intracerebroventricularly (i.c.v.) or intravenously, it reverses haemorrhagic hypotension in rats, apparently by the activation of central cholinergic receptors. The study was undertaken to investigate the involvement of the central histaminergic system in CDP-choline-mediated reversal of haemorrhagic hypotension. Experiments were carried out in male ketamine/xylazine-anaesthetised Wistar rats subjected to haemorrhagic hypotension of 20-26 mmHg. CDP-choline (2 micromol; i.c.v.) administered at 5 min of critical hypotension produced a long-lasting pressor effect with increases in mean arterial pressure (MAP), heart rate (HR), and renal, hindquarters and mesenteric blood flows, resulting in a 100% survival at 2 h. The action was accompanied by approximately a 26% increase in extracellular histamine concentration at the posterior hypothalamus, as measured by microdialysis. Cardiovascular effects mediated by CDP-choline were almost completely blocked by pretreatment with H(1) receptor antagonist chlorpheniramine (50 nmol; i.c.v.), but not with H(2) receptor blocker ranitidine (25 nmol; icv) or H(3)/H(4) receptor antagonist thioperamide (50 nmol; i.c.v.). In conclusion, the present results show that he central histaminergic system, through the activation of H(1) histaminergic receptors, is involved in CDP-choline-induced resuscitating effect in haemorrhage-shocked rats.

  5. The mediation of the central histaminergic system in the pressor effect of intracerebroventricularly injected melittin, a phospholipase A2 activator, in normotensive rats.

    Science.gov (United States)

    Altinbas, Burcin; Topuz, Bora B; Yilmaz, Mustafa S; Aydin, Cenk; Savci, Vahide; Jochem, Jerzy; Aydin, Sami; Yalcin, Murat

    2012-01-01

    Melittin is a polypeptide component of bee venom that leads to an increase in arachidonic acid release and subsequently in prostaglandin synthesis by activating phospholipase A(2). Recently we demonstrated that centrally or peripherally administrated melittin caused pressor effect and central thromboxane A(2) (TXA(2)) and cholinergic system mediated these effects of melittin. Also centrally injected histamine leads to pressor and bradycardic response by activating central histamine receptors in normotensive rats and central cholinergic system involved the effects of histamine. The present study demonstrates an involvement of the central histaminergic system in melittin-induced cardiovascular effect in normotensive rats. Experiments were carried out in male Sprague Dawley rats. Intracerebroventricularly (i.c.v.) injected melittin (0.5, 1 and 2 nmol) caused dose- and time-dependent increases in mean arterial pressure (MAP) and decrease in heart rate (HR) as we reported previously. Moreover, H(2) receptor antagonist ranitidine (50 nmol; i.c.v.) almost completely and H(3)/H(4) receptor antagonist thioperamide (50 nmol; i.c.v.) partly blocked melittin-evoked cardiovascular effects, whereas H(1) receptor blocker chlorpheniramine (50 nmol; i.c.v.) had no effect. Also centrally injected melittin was accompanied by 28% increase in extracellular histamine concentration in the posterior hypothalamus, as shown in microdialysis studies. In conclusion, results show that centrally administered melittin causes pressor and bradycardic response in conscious rats. Moreover, according to our findings, there is an involvement of the central histaminergic system in melittin-induced cardiovascular effects.

  6. 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.

  7. 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.

  8. Effects of histamine H(1) receptor antagonists on depressive-like behavior in diabetic mice.

    Science.gov (United States)

    Hirano, Shoko; Miyata, Shigeo; Onodera, Kenji; Kamei, Junzo

    2006-02-01

    We previously reported that streptozotocin-induced diabetic mice showed depressive-like behavior in the tail suspension test. It is well known that the central histaminergic system regulates many physiological functions including emotional behaviors. In this study, we examined the role of the central histaminergic system in the diabetes-induced depressive-like behavior in the mouse tail suspension test. The histamine contents in the hypothalamus were significantly higher in diabetic mice than in non-diabetic mice. The histamine H(1) receptor antagonist chlorpheniramine (1-10 mg/kg, s.c.) dose-dependently and significantly reduced the duration of immobility in both non-diabetic and diabetic mice. In contrast, the selective histamine H(1) receptor antagonists epinastine (0.03-0.3 microg/mouse, i.c.v.) and cetirizine (0.01-0.1 microg/mouse, i.c.v.) dose-dependently and significantly suppressed the duration of immobility in diabetic mice, but not in non-diabetic mice. Spontaneous locomotor activity was not affected by histamine H(1) receptor antagonists in either non-diabetic or diabetic mice. In addition, the number and affinity of histamine H(1) receptors in the frontal cortex were not affected by diabetes. In conclusion, we suggest that the altered neuronal system mediated by the activation of histamine H(1) receptors is involved, at least in part, in the depressive-like behavior seen in diabetic mice.

  9. 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.

  10. Management of horn gore injury and urticaria in a dairy cow: A case report

    Directory of Open Access Journals (Sweden)

    Abdul Nasir Tijjani

    2015-09-01

    Full Text Available This paper reports how a 4-year old Friesien-Sahiwal cross cow weighing 380 kg with horn gore injury on the left labia of the vulva was managed at the Large Animal Clinic, University Putra Malaysia. The lacerated wound measuring about 4-cm long was originated as a result of horn goring from another cow two weeks prior presentation of the cow to the clinic. Physical examination of the cow incidentally revealed urticaria on the left ventro-lateral aspect of the neck suspected to be sequel of hypersensitivity. The wound was treated by topical application of a mixture of Iodine, Benacillin LA, Biomectin 1% and Ilium Dermapred made into cream. While the uticaria was treated by intramuscular injection of Chlorpheniramine maleate at 0.5 mg/kg bwt. Animal management, housing design and presence of sharp horns are some of the factors that can lead to physical traumatic injuries in dairy cows. [J Adv Vet Anim Res 2015; 2(3.000: 366-368

  11. 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

  12. 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

  13. Single-walled carbon nanotube-based polymer monoliths for the enantioselective nano-liquid chromatographic separation of racemic pharmaceuticals.

    Science.gov (United States)

    Ahmed, Marwa; Yajadda, Mir Massoud Aghili; Han, Zhao Jun; Su, Dawei; Wang, Guoxiu; Ostrikov, Kostya Ken; Ghanem, Ashraf

    2014-09-19

    Single-walled carbon nanotubes were encapsulated into different polymer-based monolithic backbones. The polymer monoliths were prepared via the copolymerization of 20% monomers, glycidyl methacrylate, 20% ethylene glycol dimethacrylate and 60% porogens (36% 1-propanol, 18% 1,4-butanediol) or 16.4% monomers (16% butyl methacrylate, 0.4% sulfopropyl methacrylate), 23.6% ethylene glycol dimethacrylate and 60% porogens (36% 1-propanol, 18% 1,4-butanediol) along with 6% single-walled carbon nanotubes aqueous suspension. The effect of single-walled carbon nanotubes on the chiral separation of twelve classes of pharmaceutical racemates namely; α- and β-blockers, antiinflammatory drugs, antifungal drugs, dopamine antagonists, norepinephrine-dopamine reuptake inhibitors, catecholamines, sedative hypnotics, diuretics, antihistaminics, anticancer drugs and antiarrhythmic drugs was investigated. The enantioselective separation was carried out under multimodal elution to explore the chiral recognition capabilities of single-walled carbon nanotubes using reversed phase, polar organic and normal phase chromatographic conditions using nano-liquid chromatography. Baseline separation was achieved for celiprolol, chlorpheniramine, etozoline, nomifensine and sulconazole under multimodal elution conditions. Satisfactory repeatability was achieved through run-to-run, column-to-column and batch-to-batch investigations. Our findings demonstrate that single-walled carbon nanotubes represent a promising stationary phase for the chiral separation and may open the field for a new class of chiral selectors.

  14. 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

  15. 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

  16. A Facile Electrochemical Preparation of Reduced Graphene Oxide@Polydopamine Composite: A Novel Electrochemical Sensing Platform for Amperometric Detection of Chlorpromazine

    Science.gov (United States)

    Palanisamy, Selvakumar; Thirumalraj, Balamurugan; Chen, Shen-Ming; Wang, Yi-Ting; Velusamy, Vijayalakshmi; Ramaraj, Sayee Kannan

    2016-01-01

    We report a novel and sensitive amperometric sensor for chlorpromazine (CPZ) based on reduced graphene oxide (RGO) and polydopamine (PDA) composite modified glassy carbon electrode. The RGO@PDA composite was prepared by electrochemical reduction of graphene oxide (GO) with PDA. The RGO@PDA composite modified electrode shows an excellent electro-oxidation behavior to CPZ when compared with other modified electrodes such as GO, RGO and GO@PDA. Amperometric i-t method was used for the determination of CPZ. Amperometry result shows that the RGO@PDA composite detects CPZ in a linear range from 0.03 to 967.6 μM. The sensor exhibits a low detection limit of 0.0018 μM with the analytical sensitivity of 3.63 ± 0.3 μAμM–1 cm–2. The RGO@PDA composite shows its high selectivity towards CPZ in the presence of potentially interfering drugs such as metronidazole, phenobarbital, chlorpheniramine maleate, pyridoxine and riboflavin. In addition, the fabricated RGO@PDA modified electrode showed an appropriate recovery towards CPZ in the pharmaceutical tablets. PMID:27650697

  17. 甲泼尼龙引起皮肤过敏反应1例报告

    Institute of Scientific and Technical Information of China (English)

    夏明倩

    2014-01-01

    1 case of hand,foot and mouth disease were summarized merger encephalitis patients still point a prednisolone treatment measures and experience of skin allergy reaction process.Measures immediately stop drug,chlorpheniramine maleate allergy symptoms after treatment.Analysts say a prednisolone are leading to the possibility of an anaphylactic reaction,should control the transfusion speed in clinical application,strengthen the observation of adverse drug reactions.%总结了1例手足口病合并脑炎患者静点甲泼尼龙过程发生皮肤过敏反应的处理措施及体会。处理措施为立即停药,予以扑尔敏抗过敏治疗后症状缓解。分析认为甲泼尼龙也有导致患者发生过敏反应的可能,临床应用中应控制输液速度,加强药物不良反应的观察。

  18. 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

  19. 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

  20. 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.

  1. 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

  2. Inhibitory Effect on β-Hexosaminidase Release from RBL-2H3 Cells of Extracts and Some Pure Constituents of Benchalokawichian, a Thai Herbal Remedy, Used for Allergic Disorders

    Directory of Open Access Journals (Sweden)

    Thana Juckmeta

    2014-01-01

    Full Text Available Introduction. Benchalokawichian (BCW, a Thai traditional herbal formulation, has long been used as antipyretic and to treat skin disorders. It comprises roots from five herbs: Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. This polyherbal remedy has recently been included in the Thailand National List of Essential Medicines (Herbal Products list. Methodology. A Bioassay-guided fractionation technique was used to evaluate antiallergy activities of crude extracts, and those obtained by the multistep column chromatography isolation of pure compounds. Inhibitory effect on the release of β-hexosaminidase from RBL-2H3 cells was used to determine antiallergic activity. Results. Two pure compounds from BCW formulation showed higher antiallergic activity than crude or semipure extracts. Pectolinarigenin showed the highest antiallergic activity, followed by O-methylalloptaeroxylin, with IC50 values of 6.3 μg/mL and 14.16 μg/mL, respectively. Moreover, the highest activities of pure compounds were significantly higher than chlorpheniramine (16.2 μg/mL. Conclusions. This study provides some support for the use of BCW in reducing itching and treatment of other skin allergic disorders. The two isolated constituents exhibited high antiallergic activity and it is necessary to determine their mechanism of action. Further phytochemical and safety studies of pure compounds are required before development of these as antiallergy commercial remedies.

  3. Inhibitory Effect on β -Hexosaminidase Release from RBL-2H3 Cells of Extracts and Some Pure Constituents of Benchalokawichian, a Thai Herbal Remedy, Used for Allergic Disorders.

    Science.gov (United States)

    Juckmeta, Thana; Thongdeeying, Pakakrong; Itharat, Arunporn

    2014-01-01

    Introduction. Benchalokawichian (BCW), a Thai traditional herbal formulation, has long been used as antipyretic and to treat skin disorders. It comprises roots from five herbs: Ficus racemosa, Capparis micracantha, Clerodendrum petasites, Harrisonia perforata, and Tiliacora triandra. This polyherbal remedy has recently been included in the Thailand National List of Essential Medicines (Herbal Products list). Methodology. A Bioassay-guided fractionation technique was used to evaluate antiallergy activities of crude extracts, and those obtained by the multistep column chromatography isolation of pure compounds. Inhibitory effect on the release of β-hexosaminidase from RBL-2H3 cells was used to determine antiallergic activity. Results. Two pure compounds from BCW formulation showed higher antiallergic activity than crude or semipure extracts. Pectolinarigenin showed the highest antiallergic activity, followed by O-methylalloptaeroxylin, with IC50 values of 6.3 μg/mL and 14.16 μg/mL, respectively. Moreover, the highest activities of pure compounds were significantly higher than chlorpheniramine (16.2 μg/mL). Conclusions. This study provides some support for the use of BCW in reducing itching and treatment of other skin allergic disorders. The two isolated constituents exhibited high antiallergic activity and it is necessary to determine their mechanism of action. Further phytochemical and safety studies of pure compounds are required before development of these as antiallergy commercial remedies. PMID:25580152

  4. Antiinflammatory Efficacy of Extracts of Latex of Calotropis procera Against Different Mediators of Inflammation

    Directory of Open Access Journals (Sweden)

    Soneera Arya

    2005-01-01

    Full Text Available The latex of the plant Calotropis procera has been reported to exhibit potent antiinflammatory activity against carrageenin and formalin that are known to release various mediators. In the present study, we have evaluated the efficacy of extracts prepared from the latex of C procera against inflammation induced by histamine, serotonin, compound 48/80, bradykinin (BK, and prostaglandin E(PGE in the rat paw oedema model. The paw oedema was induced by the subplantar injection of various inflammagens and oedema volume was recorded using a plethysmometer. The aqueous and methanol extracts of the dried latex (DL and standard antiinflammatory drugs were administered orally 1 hour before inducing inflammation. The inhibitory effect of the extracts was also evaluated against cellular influx induced by carrageenin. The antiinflammatory effect of aqueous and methanolic extracts of DL was more pronounced than phenylbutazone (PBZ against carrageenin while it was comparable to chlorpheniramine and PBZ against histamine and PGE, respectively. Both extracts produced about 80%, 40%, and 30% inhibition of inflammation induced by BK, compound 48/80, and serotonin. The histological analysis revealed that the extracts were more potent than PBZ in inhibiting cellular infiltration and subcutaneous oedema induced by carrageenin. The extracts of DL exert their antiinflammatory effects mainly by inhibiting histamine and BK and partly by inhibiting PGE.

  5. 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.

  6. Posterior hypothalamic receptors involved in the cardiovascular changes elicited by electrical stimulation of the rostral ventrolateral medulla.

    Science.gov (United States)

    Bachelard, H; Rivest, R; Marsden, C A

    1991-07-01

    The posterior hypothalamic receptors involved in the cardiovascular responses to electrical stimulation of the rostral ventrolateral medulla were investigated in urethane-anaesthetized rats. Electrical stimulation of the rostral ventrolateral medulla produced a significant increase in systolic blood pressure. This response was significantly attenuated by the prior administration of d,l-propranolol (20 micrograms), clonidine (8 micrograms), atropine (8 micrograms) or methysergide (10 micrograms) into the posterior hypothalamus, but not by cimetidine (11 micrograms), chlorpheniramine (12 micrograms), naloxone (10 micrograms) or a vasopressin V1 antagonist (100 ng). The effect of clonidine (8 micrograms) on the pressor response to stimulation of the rostral ventrolateral medulla was antagonized by idazoxan (66 micrograms). These results confirm that the cardiovascular changes elicited by stimulation of the rostral ventrolateral medulla area are, in part, centrally modulated by alpha 2 and beta-adrenoceptors in the posterior hypothalamus which exert respectively, inhibitory and stimulatory effect. Furthermore the results indicate the involvement of posterior hypothalamic cholinergic and serotonergic receptors in the pressor response produced by stimulation of the rostral ventrolateral medulla.

  7. Mechanism of central histamine in rats with asthma induced by psychological stress%中枢组胺在心理应激致大鼠哮喘发病中的作用机制

    Institute of Scientific and Technical Information of China (English)

    张红叶; 宋佳贤; 杨莉亚; 杨八双; 黄旭; 董榕

    2011-01-01

    目的 探讨中枢组胺在心理应激致大鼠哮喘发病中的中枢免疫调节作用及其机制.方法 SD大鼠随机分为5组(每组n=10):对照组、哮喘组、应激组、应激哮喘组及侧脑室注射扑尔敏组,测定肺通气功能,放免法测定血清皮质酮(CORT)含量,ELISA测定IL-4及IFN-γ水平,并计算Th1/Th2比值;HE染色观察肺组织形态;高效液相法测定下丘脑内组胺含量;侧脑室注射H1受体拮抗剂扑尔敏观察应激哮喘组肺通气功能、Th1/Th2比值的变化.结果与哮喘组相比:应激哮喘组肺通气功能下降(P<0.05);血清Th1 /Th2比值下降(P<0.05),肺组织炎性浸润加重;下丘脑内组胺从231 ±32 nmol/g升高至287±44 nmol/g(P<0.05).侧脑室注射H1受体拮抗剂扑尔敏后可减轻上述变化.结论 心理应激可致哮喘大鼠中枢组胺含量升高,后者作用于H1受体,加重哮喘气道高反应性及气道炎性反应.%Objective This study aims to investigate the mechanism of central histamine on psychological stress rats with asthma. Methods Healthy SD rats were randomly assigned as 4 test groups and me control group. Asthma and psychological stress rat models were established. Pulmonary function was tested by Powlab biological signal processing system. Serum corticosterone ( CORT) was tested by radioimmunoassay. Serum IL-4, IFN-γ were tested by enzyme-linked immunosorbent assay, which were used to calculate the ratio of Thl/Th2. Lung tissues were stained with HE. Histamine content in the hypothalamus was determined by HPLC. And through intracerebroven-tricular injection of histamine H1 receptor antagonist,chlorpheniramine,to observe pulmonary function and Thl/Th2 ratio in rats with asthma. Results After the psychological stress, compared with the asthma model group, pulmonary function of stress asthmatic rats decreased ( P < 0. 05 ). Serum Thl/Th2 ratio were decreased ( P < 0. 05 ). Besides, peripheral inflammation of lung tissue were worse. Histamine in

  8. 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

  9. [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

  10. Involvement of the histaminergic system on appetitive learning and its interaction with haloperidol in goldfish.

    Science.gov (United States)

    Medalha, Carla Christina; Mattioli, Rosana

    2007-05-17

    This study investigated the actions of the histaminergic system on appetitive learning and memory, and its interaction with the dopaminergic system in goldfish. It consisted of nine sessions, in which fish were tested in a four-arm tank. On day 1, the animals were habituated for 10 min. On day 2, they were placed in one arm and had to find food at the left or the right arm. Time to begin feeding was recorded, and the procedure repeated for more 3 days (training phase). On training day 4, seven groups were injected with saline, seven with haloperidol (2.0 mg/kg) and one with DMSO solution before training and after feeding, three groups received saline, six chlorpheniramine (CPA) (1.0, 4.0 and 8.0 mg/kg), and six l-histidine (LH) (25, 50 and 100 mg/kg). Saline groups were considered as control of CPA and LH treated groups and DMSO as control of haloperidol. A non-injected group was also included. Testing occurred after 24 h. A reversal procedure was conducted 24h after testing and repeated for 3 days. The groups receiving CPA at 1.0 and 8.0 mg/kg and LH at 25, 50 and 100 mg/kg differed between Test and Reversal day 1. Pre-treatment with haloperidol plus 8.0 mg/kg of CPA and 25 and 50 mg/kg of LH reverted the treatment effect. However, in the groups treated with 1.0 mg/kg of CPA and 100 mg/kg of LH, the difference remained. This study confirmed the interaction between the histaminergic and the dopaminergic systems on memory process in goldfish.

  11. 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.

  12. Evaluation of Prosopis africana Seed Gum as an Extended Release Polymer for Tablet Formulation.

    Science.gov (United States)

    Nadaf, Sameer; Nnamani, Petra; Jadhav, Namdeo

    2015-06-01

    In the present work, an attempt has been made to screen Prosopis africana seed gum (PG), anionic polymer for extended release tablet formulation. Different categories of drugs (charge basis) like diclofenac sodium (DS), chlorpheniramine maleate (CPM), and ibuprofen (IB) were compacted with PG and compared with different polymers (charge basis) like xanthan gum (XG), hydroxypropyl methyl cellulose (HPMC-K100M), and chitosan (CP). For each drug, 12 batches of tablets were prepared by wet granulation technique, and granules were evaluated for flow properties, compressibility, and compactibility by Heckel and Leuenberger analysis, swelling index, in vitro dissolution studies, etc. It has been observed that granules of all batches showed acceptable flowability. According to Heckel and Leuenberger analysis, granules of PG-containing compacts showed similar and satisfactory compressibility and compactibility compared to granules of other polymers. PG showed significant swelling (P < 0.05) compared to HPMC, and better than CP and XG. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Fourier transform infrared (FTIR) study showed no interaction between drugs and polymers. From all PG-containing compacts of aforesaid drugs, drug release was sustained for 12 h following anomalous transport. Especially, polyelectrolyte complex formation retarded the release of oppositely charged drug (CPM-PG). However, extended release was noted in both anionic (DS) and nonionic (IB) drugs, maybe due to swollen gel. All compacts were found to be stable for 3-month period during stability study. This concludes that swelling and release retardation of PG has close resemblance to HPMC, so it can be used as extended release polymer for all types of drugs.

  13. 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

  14. Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells.

    Science.gov (United States)

    Kim, Ji-Hyun; Park, Seong-Hae; Moon, Young Wha; Hwang, Sungmin; Kim, Donghoon; Jo, Su-Hyun; Oh, Seog Bae; Kim, Joong Soo; Jahng, Jeong Won; Lee, Jong-Ho; Lee, Sung Joong; Choi, Se-Young; Park, Kyungpyo

    2009-08-01

    One of the common side effects of antihistamine medicines is xerostomia (dry mouth). The current consensus is that antihistamine-induced xerostomia comes from an antimuscarinic effect. Although the effect of antihistamines on salivary secretion is both obvious and significant, the cellular mechanism whereby this happens is still unclear because of the lack of knowledge of histamine signaling in human salivary glands. Here, we have studied histamine receptors and the effect of antihistamines on human submandibular acinar cells. In primary cultured human submandibular gland and a HSG cell line, histamine increased the intracellular Ca(2+) concentration. The histamine-induced cytosolic free Ca(2+) concentration ([Ca(2+)](i)) increase was inhibited by histamine H1 receptor-specific antagonists, and the expression of the functional histamine H1 receptor was confirmed by reverse transcription-polymerase chain reaction. Interestingly, histamine pretreatment did not inhibit a subsequent carbachol-induced [Ca(2+)](i) rise without "heterologous desensitization." Chlorpheniramine inhibited a carbachol-induced [Ca(2+)](i) increase at a 100-fold greater concentration than histamine receptor antagonism, whereas astemizole and cetrizine showed more than 1000-fold difference, which in part explains the xerostomia-inducing potency among the antihistamines. Notably, histamine resulted in translocation of aquaporin-5 to the plasma membrane in human submandibular gland cells and green fluorescent protein-tagged aquaporin-5 expressing HSG cells. We found that histidine decarboxylase and the histamine H1 receptor are broadly distributed in submandibular gland cells, whereas choline acetyltransferase is localized only at the parasympathetic terminals. Our results suggest that human salivary gland cells express histamine H1 receptors and histamine-synthesizing enzymes, revealing the cellular mechanism of antihistamine-induced xerostomia. PMID:19443731

  15. 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.

  16. Indirect fluorescent determination of selected nitro-aromatic and pharmaceutical compounds via UV-photolysis of 2-phenylbenzimidazole-5-sulfonate.

    Science.gov (United States)

    Zhang, Wei; Wilson, Christopher R; Danielson, Neil D

    2008-02-15

    An indirect fluorescence (FL) detection method via the reactivity of UV-photolyzed 2-phenylbenzimidazole-5-sulfonate (PBSA) has been developed for non-fluorescent aromatic compounds. At high pH with UV photolysis, PBSA in the excited state is known to be quenched by reaction with oxygen species and analyte compounds that are reactive toward these oxygen species produced during photolysis can lessen the loss of PBSA FL. After off-line photolysis of PBSA in the presence of various nitro-aromatic test compounds, the increase in PBSA FL is clearly evident. A flow injection (FI) instrument using a PBSA mobile phase propelled through a Teflon coil wrapped around a Hg lamp is optimized and modified for use for liquid chromatography (LC). For the on-line FI determination of the non-fluorescent nitro-aromatic compounds such as 4-nitroaniline, 2-nitrophenol, 3-nitrophenol, 4-nitrophenol, and alpha-nitronaphthalene, a positive linear response for PBSA FL from about 0.5 to 15 microM and detection limits generally between 0.2 and 1 microM (4-20 pmol) are found. Linear responses and detection limits of selected pharmaceutical compounds such as the antibacterial nitrofurantoin, antihistamines chlorpheniramine and brompheniramine, and other compounds were similar. In general, detection limits using UV detection at about 214 nm were not as good in the 1-2 microM range but linearity extended up to 100 microM. The amino acid phenylalanine and small peptides containing this aromatic amino acid were also determined using this method. Application of this detection method for the liquid chromatography determination of 4-nitroaniline, 2-nitrophenol, nitrofurantoin, and salicylate is shown.

  17. 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.

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

    Science.gov (United States)

    Gianlorenço, A C L; Serafim, K R; Canto-de-Souza, A; Mattioli, R

    2014-02-01

    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. 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.

  20. H₁ but not H₂ histamine antagonist receptors mediate anxiety-related behaviors and emotional memory deficit in mice subjected to elevated plus-maze testing.

    Science.gov (United States)

    Serafim, K R; Kishi, M S; Canto-de-Souza, A; Mattioli, R

    2013-05-01

    This study investigated the role of H₁ and H₂ receptors in anxiety and the retrieval of emotional memory using a Trial 1/Trial 2 (T1/T2) protocol in an elevated plus-maze (EPM). Tests were performed on 2 consecutive days, designated T1 and T2. Before T1, the mice received intraperitoneal injections of saline (SAL), 20 mg/kg zolantidine (ZOL, an H2 receptor antagonist), or 8.0 or 16 mg/kg chlorpheniramine (CPA, an H1 receptor antagonist). After 40 min, they were subjected to the EPM test. In T2 (24 h later), each group was subdivided into two additional groups, and the animals from each group were re-injected with SAL or one of the drugs. In T1, the Student t-test showed no difference between the SAL and ZOL or 8 mg/kg CPA groups with respect to the percentages of open arm entries (%OAE) and open arm time (%OAT). However, administration of CPA at the highest dose of 16 mg/kg decreased %OAE and %OAT, but not locomotor activity, indicating anxiogenic-like behavior. Emotional memory, as revealed by a reduction in open arm exploration between the two trials, was observed in all experimental groups, indicating that ZOL and 8 mg/kg CPA did not affect emotional memory, whereas CPA at the highest dose affected acquisition and consolidation, but not retrieval of memory. Taken together, these results suggest that H₁ receptor, but not H₂, is implicated in anxiety-like behavior and in emotional memory acquisition and consolidation deficits in mice subjected to EPM testing.

  1. Possible Mechanism of Action of the Antiallergic Effect of an Aqueous Extract of Heliotropium indicum L. in Ovalbumin-Induced Allergic Conjunctivitis

    Directory of Open Access Journals (Sweden)

    Samuel Kyei

    2015-01-01

    Full Text Available Heliotropium indicum is used traditionally as a remedy for conjunctivitis in Ghana. This study therefore evaluated the antiallergic potential of an aqueous whole plant extract of Heliotropium indicum (HIE in ovalbumin-induced allergic conjunctivitis and attempted to predict its mode of action. Clinical scores for allergic conjunctivitis induced by intraperitoneal ovalbumin sensitization (100 : 10 μg OVA/Al(OH3 in phosphate-buffered saline [PBS] and topical conjunctival challenge (1.5 mg OVA in 10 μL PBS in Dunkin-Hartley guinea pigs were estimated after a week’s daily treatment with 30–300 mg kg−1 HIE, 30 mg kg−1 prednisolone, 10 mg kg−1 chlorpheniramine, or 10 mL kg−1 PBS. Ovalbumin-specific IgG and IgE and total IgE in serum were estimated using Enzyme-Linked Immunosorbent Assay. Histopathological assessment of the exenterated conjunctivae was also performed. The 30 and 300 mg kg−1 HIE treatment resulted in a significantly (p≤0.001 low clinical score of allergic conjunctivitis. Ovalbumin-specific IgG and IgE as well as total serum IgE also decreased significantly (p≤0.01–0.001. The conjunctival tissue in HIE treated guinea pigs had mild mononuclear infiltration compared to the PBS-treated ones, which had intense conjunctival tissue inflammatory infiltration. HIE exhibited antiallergic effect possibly by immunomodulation or immunosuppression.

  2. 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

  3. 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.

  4. Influence of SKF 91488, histamine N-methyltransferase inhibitor, on the central cardiovascular regulation during controlled, stepwise hemorrhagic hypotension in rats.

    Science.gov (United States)

    Jochem, Jerzy; Zwirska-Korczala, Krystyna; Rybus-Kalinowska, Barbara; Jagodzińska, Julia; Korzonek-Szlacheta, Ilona

    2002-01-01

    The histaminergic system influences various activities of the central nervous system, including cardiovascular regulation. Histamine administered intracerebroventricularly (i.c.v.) in anesthetized rats produces the increase in mean arterial pressure (MAP) and heart rate (HR), however, in contrast to normotensive animals, histamine-induced rises in MAP and HR in critically hypotensive animals are significantly higher. Similarly to exogenous histamine, inhibition of the central histamine N-methyltransferase (HNMT) activity (the enzyme catabolizing histamine in the central nervous system) resulting in the increase in endogenous histamine concentration, also leads to the pressor effect in normotensive rats. The present study was designed to determine the role of endogenous central histamine in cardiovascular regulation in a rat model of blood volume-blood pressure controlled hemorrhagic hypotension. In normotensive animals, HNMT inhibitor SKF 91488 produced dose-dependent (20-100 microg i.c.v.) pressor effect accompanied by tachycardia, similarly as exogenous histamine (0.5-5 microg i.c.v.) did. The subpressor dose of SKF 91488 (10 microg) evoked the increase in blood volumes necessary to induce hypotension of 40 and 20 mmHg and the action was accompanied by the rise in histamine concentrations in the hypothalamus (5.18 +/- 0.45 vs 4.23 +/- 0.41 nmol/g; p histamine concentrations (0.84 +/- 0.18 vs 0.75 +/- 0.17 nmol/g), compared to the control i.c.v. saline-treated group. The effect of SKF 91488 was inhibited by H1 histamine receptor antagonist chlorpheniramine, whereas neither H2 receptor blocker ranitidine, nor H3 receptor antagonist thioperamide affected the action. In conclusion, the study demonstrates that the histaminergic system influences the central cardiovascular regulation during pronounced hemorrhagic hypotension, probably as a result of the activation of compensatory mechanisms.

  5. Effects of pirarubicin, an antitumor antibiotic, on the cardiovascular system.

    Science.gov (United States)

    Hirano, S; Agata, N; Hara, Y; Iguchi, H; Shirai, M; Tone, H; Urakawa, N

    1991-01-01

    In the present study we examined the effects of pirarubicin [(2"R)-4'-O-tetrahydropyranyladriamycin, THP] on a cardiovascular system. An injection of THP (0.39-3.13 mg/kg, i.v.) reduced the mean blood pressure and caused an increase in the respiratory air rate in anesthetized rats. At 1.5 x 10(-6)-1.5 x 10(-5) M, THP markedly relaxed a contraction induced by 10(-7) M norepinephrine in rat aorta with endothelium but not in that without endothelium. At a dose of 0.02-0.5 mg, THP produced an increase in the contractile force and the perfusion flow of isolated perfused guinea pig hearts. At a higher concentration (4.5 x 10(-5)-1.5 x 10(-4) M), it produced a slight increase in the contractile force of the left atria in guinea pigs. This positive inotropic action of THP was inhibited by diphenhydramine (10(-6)-5 x 10(-5) M), chlorpheniramine (3 x 10(-7)-3 x 10(-5) M), and tripelennamine (3 x 10(-7)-3 x 10(-5) M) but not by propranolol (10(-6) M), cimetidine (10(-5) M), diltiazem (10(-6) M), or ryanodine (10(-8) M). THP given i.v. at 2.5 mg/kg elevated the plasma histamine level in anesthetized dogs. From these data, we conclude that THP mainly relaxed the rat aorta in the presence of endothelium and that at higher concentrations, it increased the contractile force in the cardiac muscle, probably mediated through the release of histamine.

  6. 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.

  7. Study of the Effect of Hydro-Alcoholic Extract of Lactuca sativa on Arterial Blood Pressure and Heart Rate in Rats

    Directory of Open Access Journals (Sweden)

    R. Dehbooreh

    2013-04-01

    Full Text Available Introduction & Objective: Cardiovascular diseases are main causes of mortality and morbidity in the current world. Hypertension is one of the most important risk factors for the cardiovas-cular diseases. Herbal medicine is much regarded because of their natural source and less side effects. This study was done to evaluate the effects of hydro- alcoholic extract of Luc-tuca-Sativa (LS on blood pressure in rats. Materials & Methods: Hypertension was induced in the rats by Desoxycorticosterone (DOCA-Salt then the hypertension induction was confirmed by tail-cuff method before treatment. The effects of one week treatment by LS hydro-alcoholic extract (100 mg/kg/day on blood pressure; Heart Rate (HR and Plasma Renin Activity (PRA were investigated and compared with the control groups. Under anesthesia (urethane 1gr/kg Mean Arterial blood Pressure (MAP and HR were measured directly from Femoral Artery. In order to investigate the extract effects on MAP and HR, also possible mechanisms of these effects, intravenous injection of differ-ent concentrations of extract with and without pretreatment with histamine H1 receptor an-tagonist (Chlorpheniramine 10 mg/kg were performed. PRA was measured by radio-immuonoassay method. Urine volume was also measured during the treatment Results: The results of this study show that DOCA-Salt induced hypertension and decreased PRA in the rats. LS hydro- alcoholic extract treatment causes significant decrease of MAP in hypertension- treated group in comparison with non-treated group and also the level of PRA and urine volume increased by extract treatment. Our Findings showed that LS extract has no significant effect on HR. Conclusion: The results of this study indicated hat LS hydro- alcoholic extract due to interac-tion with kidney and diuretic effects decreased MAP and normalized PRA in the DOCA- Salt hypertensive. (Sci J Hamadan Univ Med Sci 2013; 20 (1:66-76

  8. H1 and H2 receptors in the locus ceruleus are involved in the intracerebroventricular histamine-induced carotid sinus baroreceptor reflex resetting in rats

    Institute of Scientific and Technical Information of China (English)

    Guo-Qing WANG; Wan-Ping SUN; Yong-Jin ZHU; Rong ZOU; Xi-Ping ZHOU

    2006-01-01

    Objective To investigate the role of H1 and H2 receptors in the locus ceruleus (LC) in carotid sinus baroreceptor reflex (CSR) resetting induced by intracerebroventricular (i.c.v.) injection of histamine (HA). Methods The left and right carotid sinus regions were isolated from the systemic circulation in 18 male Sprague-Dawley rats anesthetized with pentobarbital sodium. The intracarotid sinus pressure (ISP) was altered in a stepwise manner in vivo. ISP-mean arterial pressure (MAP) relationship curve and its characteristic parameters were constructed by fitting to the logistic function with five parameters. The changes in CSR performance induced by i.c.v. HA and the effects of pretreatment with H1 or H2 receptors selective antagonist, chlorpheniramine (CHL) or cimetidine (CIM) into the LC, on the responses of CSR to HA were examined. Results I.c.v. HA (100 ng in 5 μl) significantly shifted the ISP-MAP relationship curve upwards (P < 0.05) and obviously decreased the value of the reflex parameters such as MAP range and maximum gain (P < 0.05), but increased the threshold pressure, saturation pressure and ISP at maximum gain (P < 0.05). The pretreatment with CHL (0.5 μg in 1 μl) or CIM (1.5 μg in 1 μl) into the LC could obviously attenuate the changes mentioned above in CSR performance induced by HA, but the alleviative effect of CIM was less remarkable than that ofCHL (P < 0.05). Respective microinjection of CHL or CIM alone into the LC with the corresponding dose and volume did not change CSR performance significantly (P > 0.05). Conclusion Intracerebroventricular administration of HA results in a rapid resetting of CSR and a decrease in reflex sensitivity, and the responses of CSR to HA may be mediated, at least in part, by H1 and H2 receptors activities in the LC, especially by H1 receptors. Moreover, the effects of the central HA on CSR might be related to a histaminergic descending pathway from the hypothalamus to LC.

  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. 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

  11. 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.

  12. 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

  13. 预防服药对减少荧光素眼底血管造影不良反应的作用%Effect of preventive medicine on reducing adverse reaction of fundus fluorescein angiography

    Institute of Scientific and Technical Information of China (English)

    欧阳结颜; 邓桂英; 黄龙淳; 李翠久

    2012-01-01

    Objective:To evalute the effect of preventive medication to reduce untoward effect in fandus fluorescein angiog-raphy(FFA). Methods:Total 3640 cases with FFA were divided into two groups randomly. The patients in control group( n = 1820) were given topical mydriasis without oral medication, while patients in the research group( n = 1820)were given vitamin B6 20 mg and chlorpheniramine maleate tablets 4 mg except for giving topical mydriasis. Both groups received follow - up examination with untoward effect. Results :The rates of untoward effect in the research group and control group were 2.31 % and 6.78%.There was significant difference with each other in the two groups(P <0.05). Conclusion;Preventive medication before FFA is effective in preventing the untoward effect.%目的:探讨预防服药对减少荧光素眼底血管造影过程中发生不良反应的疗效.方法:将3640例行荧光素钠眼底血管造影检查的患者随机分为观察组和对照组各1820例.对照组在造影检查前只散瞳不服药,观察组则在造影检查前除散瞳外,造影前20 min给予维生素B6 20mg,马来酸氯苯那敏片4 mg口服,观察造影过程中出现的不良反应情况.结果:观察组中不良反应发生率为2.31%,对照组为6.76%,两组相比差异有统计学意义.结论:荧光素钠眼底血管造影检查前予预防服药可减少不良反应的发生.

  14. 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

  15. 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

  16. 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