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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. Acute anaphylactic reaction to expired chlorpheniramine injection

    Directory of Open Access Journals (Sweden)

    Beuy Joob

    2014-01-01

    Full Text Available 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.

  3. 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/chlorphenir...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 ... ...ST/Rat/in_vitro/chlorpheniramine.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATE...amine.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATE

  4. 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 ...

  5. Plasma cell gingivitis: treatment with chlorpheniramine maleate.

    Science.gov (United States)

    Ranganathan, Aravindhan Thiruputkuzhi; Chandran, Chitraa R; Prabhakar, Priya; Lakshmiganthan, Mahalingam; Parthasaradhi, Thakkalapati

    2015-01-01

    Plasma cell gingivitis is a benign lesion of unknown etiology characterized by massive and diffuse infiltration of plasma cells into the gingival connective tissue. Clinically, it can be seen as a diffuse, erythematous, and edematous swelling involving the marginal gingiva and extending into the attached gingiva. Although usually painless, the lesion can be esthetically unappealing, especially when anterior gingiva is involved. Although the usual line of management is removal of the offending agent, this report describes the treatment of plasma cell gingivitis with the topical application of chlorpheniramine maleate (25 mg) for a period of 10 days.

  6. Factitious urticaria (dermographism): treatment by cimetidine and chlorpheniramine in a randomized double-blind study.

    Science.gov (United States)

    Kaur, S; Greaves, M; Eftekhari, N

    1981-02-01

    The HI-antihistamine chlorpheniramine and the H2-antihistamine cimetidine, given alone and in combination, have been compared with placebo in twenty patients with factitious urticaria (dermographism), in a double-blind, randomized cross-over trial. Of these regimes, the combination was the only treatment which significantly reduced weal size, flare size and duration of weal, compared with placebo, although other treatments approached statistical significance. Continuation of the most effective of the four treatments in nineteen of the patients for a further 3 months without breaking the randomization code provided further evidence of the great effectivness of combined cimetidine and chlorpheniramine. No significant side effects were note.

  7. Chlorpheniramine facilitates inhibitory avoidance in teleosts submitted to telencephalic ablation

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    F.R. Faganello

    2008-05-01

    Full Text Available The present study investigated the involvement of H(1 histaminegic receptor on the acquisition of inhibitory avoidance in Carassius auratus submitted to telencephalic ablation. The fish were submitted to telencephalic ablation 5 days before the experiment. The inhibitory avoidance procedure included 1 day for habituation, 3 days for training composed of 3 trials each (1st day: T1, T2, T3; 2nd day: 2T1, 2T2, 2T3; 3rd day: 3T1, 3T2, 3T3 and 1 day for test. On training days, the fish were placed in a white compartment, after 30 s the door was opened. When the fish crossed to a black compartment, a weight was dropped (aversive stimuli. Immediately after the third trial, on training days, the fish received, intraperitoneally, one of the pharmacological treatments (saline (N = 20, 8 (N = 12 or 16 (N = 13 µg/g chlorpheniramine, CPA. On the test day, the time to cross to the black compartment was determined. The latency of the saline group increased significantly only on the 3rd trial of the 2nd training day (mean ± SEM, T1 (50.40 ± 11.69, 2T3 (226.05 ± 25.01; ANOVA: P = 0.0249, Dunn test: P < 0.05. The group that received 8 µg/g CPA showed increased latencies from the 2nd training day until the test day (T1 (53.08 ± 17.17, 2T2 (197.75 ± 35.02, test (220.08 ± 30.98; ANOVA: P = 0.0022, Dunn test: P < 0.05. These results indicate that CPA had a facilitating effect on memory. We suggest that the fish submitted to telencephalic ablation were able to learn due to the local circuits of the mesencephalon and/or diencephalon and that CPA interferes in these circuits, probably due an anxiolytic-like effect.

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

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

    2013-09-01

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

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

    Science.gov (United States)

    Chittrakarn, Somsmorn; Penjamras, Pimpimol; Keawpradub, Niwat

    2012-04-10

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

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

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    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.

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

    Science.gov (United States)

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

    2010-04-01

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

  12. 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.

  13. Preparation of codeine-resinate and chlorpheniramine-resinate sustained-release suspension and its pharmacokinetic evaluation in beagle dogs.

    Science.gov (United States)

    Zeng, Huan-Xiang; Cheng, Gang; Pan, Wei-San; Zhong, Guo-Ping; Huang, Min

    2007-06-01

    Using ion exchange resins (IERs) as carriers, a dual-drug sustained release suspension containing codeine, and chlorpheniramine had been prepared to elevate drug safety, effectiveness and conformance. The codeine resinate and chlorpheniramine resinate beads were prepared by a batch process and then impregnated with Polyethylene glycol 4000 (PEG 4000), respectively. The PEG impregnated drug resinate beads were coated with ethylcellulose as the coating polymer and di-n-butyl-phthalate as plasticizer in ethanol and methylene chloride mixture by the Wurster process. The coated PEG impregnated drug resinate beads were dispersed in an aqueous suspending vehicle containing 0.5% w/w xanthan gum and 0.5% w/w of hydroxypropylmethylcellulose of nominal viscosity of 4000 cps, obtaining codeine resinate and chlorpheniramine resinate sustained-release suspension (CCSS). Codeine phosphate and chlorpheniramine maleate were respectively loaded onto AMBERLITE IRP 69, and PEG 4000 was used to impregnate drug resinate beads to maintain their geometry. Ethylcellulose with di-n-butyl-phthalate in ethanol and methylene chloride mixture for the coating of drug resinate beads was performed in Glatt fluidized bed coater, where the coating solution flow rate was 8-12 g/min, the inlet air temperature was 50-60 degrees C, the outlet air temperature was 32-38 degrees C, the atomizing air pressure was 2.0 bar and the fluidized air pressure was adjusted as required. Few significant agglomeration of circulating drug resinate beads was observed during the operation. The film weight gained 20% w/w and 15% w/w were suitable for the PEG impregnated codeine resinate and chlorpheniramine resinate beads, respectively. Residual solvent content increased with coating level, but inprocess drying could reduce residual solvent content. In the present study, the rates of drug release from both drug resinate beads were measured in 0.05 M and 0.5M KCl solutions. The increased ionic strength generally accelerated

  14. RP-HPLC-DAD method for the determination of phenylepherine, paracetamol, caffeine and chlorpheniramine in bulk and marketed formulation

    Directory of Open Access Journals (Sweden)

    A.P. Dewani

    2014-11-01

    Full Text Available A simple, specific and accurate isocratic RP-HPLC-DAD method was developed for the simultaneous determination of phenylephrine, paracetamol, caffeine and chlorpheniramine in bulk and tablet dosage form. The four contents are present in variable concentrations and have variable chromatographic behavior making the process of analysis very difficult. For present studies a reversed-phase C-18 column (150 mm × 4.5 mm i.d., particle size 5 μm with mobile phase consisting of acetonitrile, methanol and 10 Mm phosphate buffer 16:22:62 (v/v (pH of buffer 2.5 ± 0.02, adjusted with ortho phosphoric acid was used. The flow rate was 1.0 ml/min and eluents were monitored at 280 nm. The mean retention times of phenylephrine, paracetamol, caffeine and chlorpheniramine were found to be 1.8, 3.1, 5.2 and 10.9 min, respectively. The method was validated in terms of linearity, range, specificity, accuracy, precision and robustness. The proposed method was successfully applied to the estimation of phenylephrine, paracetamol, caffeine and chlorpheniramine in combined tablet dosage form.

  15. [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.

  16. 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.

  17. 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.

  18. Simultaneous determination of pseudoephdrine, pheniramine, guaifenisin, pyrilamine, chlorpheniramine and dextromethorphan in cough and cold medicines by high performance liquid chromatography.

    Science.gov (United States)

    Louhaichi, M R; Jebali, S; Loueslati, M H; Adhoum, N; Monser, L

    2009-05-15

    A new simple, rapid and sensitive liquid chromatographic method has been developed and validated for the simultaneous determination of pseudoephdrine, pheniramine, guaifenisin, pyrilamine, chlorpheniramine and dextromethorphan in cough and cold pharmaceuticals. The separation of these compounds was achieved within 13 min on a Kromasil C18 column using an isocratic mobile phase consisting of methanol-dihydrogenphosphate buffer at pH 3 (45:55, v/v). The analysis was performed at a flow rate of 1 mL min(-1) and at a detection wavelength of 220 nm. The selectivity, linearity of calibration, accuracy, within and between-days precision and recovery were examined as parts of the method validation. The concentration-response relationship was linear over a concentration range of 5-50 microg mL(-1) for pseudoephdrine, pheniramine, chlorpheniramine and 50-600 microg mL(-1) for guaifenisin, pyrilamine, dextromethorphan, methylparaben and sodium benzoate with correlation coefficients better than 0.998. The standard deviations of the intraday and interday were all less than 2%. The proposed liquid chromatographic method was successfully applied for the routine analysis of these compounds in different cough and cold pharmaceutical preparations such as syrups, capsules, tablets and sachets. The presence of preservatives (sodium benzoate and methylparaben) and other excipients did not show any significant interference on the determination of these compounds.

  19. Validated Stability Indicating RP-HPLC Method for Simultaneous Estimation of Codeine Phosphate and Chlorpheniramine Maleate from Their Combined Liquid Dosage Form

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    Ramakrishna Kommana

    2013-01-01

    Full Text Available The present paper describes the development of quick stability indicating RP-HPLC method for the simultaneous estimation of codeine phosphate and chlorpheniramine maleate in the presence of its degradation products, generated from forced degradation studies. The developed method separates codeine phosphate and chlorpheniramine maleate in impurities/degradation products. Codeine phosphate and chlorpheniramine maleate and their combination drug product were exposed to acid, base, oxidation, dry heat, and photolytic stress conditions, and the stressed samples were analysed by proposed method. The proposed HPLC method utilizes the Shimadzu HPLC system on a Phenomenex C18 column (, 5 μ using a mixture of 1% o-phosphoric acid in water : acetonitrile : methanol (78 : 10 : 12 mobile phase with pH adjusted to 3.0 in an isocratic elution mode at a flow rate of 1 mL/min, at 23°C with a load of 20 μL. The detection was carried out at 254 nm. The retention time of codeine phosphate and chlorpheniramine maleate was found to be around 3.47 min and 9.45 min, respectively. The method has been validated with respect to linearity, robustness, precision, accuracy, limit of detection (LOD, and limit of quantification (LOQ. The developed validated stability indicating HPLC method was found to be simple, accurate, and reproducible for the determination of instability of these drugs in bulk and commercial products.

  20. 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.

  1. [Evaluation of short-time premedication with d-chlorpheniramine maleate injection for paclitaxel-induced hypersensitivity reaction].

    Science.gov (United States)

    Harada, Tomohiko; Doi, Masakazu; Yamada, Yasuhiko; Akase, Tomohide

    2008-08-01

    Paclitaxel(referred to hereinafter as PTX )is used in ovarian cancer, non-small cell lung cancer, breast cancer, gastric cancer, and endometrial cancer with positive treatment result reports. However, severe allergic reactions such as decreases in blood pressure and impaired breathing occur with relatively high frequency. For the prevention of such allergic reactions, administration of a premedication composed of the three components, dexamethasone sodium phosphate injection, diphenhydramine hydrochloride tablet, and ranitidine hydrochloride injection solution(or injectable famodine), is advised in the appended documentation. Administration is difficult because, among these three components, only diphenhydramine hydrochloride is administered orally and thus must be provided through the internal medicine department. Particularly when this combined dosage is administered as outpatient chemotherapy, the doctor must prescribe diphenhydramine hydrochloride tablets, and the patient must not forget to bring them on the day in which chemotherapy is administered. Also, checks by the medical staff such as pharmacists and nurses are required, complicating the administration of this therapy further. Taking this situation into consideration, our hospital uses a short-time premedication method wherein d-Chlorpheniramine Maleate injections are substituted for diphenhydramine hydrochloride tablets, and the time required for premedication is reduced to 15 minutes. This study investigated the allergic reaction ratio to consider the safety and usefulness of the short-time premedication method used at our hospital. The chemotherapy regimens conducted for the subject patients were 9 cases of PTX+CBDCA, 6 cases of biweekly- PTX, and 5 cases of weekly-PTX. A total of 67 PTX injections were given, 15 of them being first-time administrations. The ratio of allergic/hypersensitivity reactions was 10.0%(2 cases in 20). The short-time premedication method using d-Chlorpheniramine Maleate

  2. Study of the Capability of Niosomes that Used Maltodextrin from Garut Starch (Maranta arundinaceae Linn. as a Chlorpheniramine Maleate Carrier

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    Mahdi Jufri

    2004-08-01

    Full Text Available The aim of this research was to study the entrapment ability of ampiphylic drug, chlorpheniramine maleate (CTM, by niosome. Like liposomes, niosomes is an encapsulated drug carrier that has important role in a drug release system. Niosomes and liposomes are unstable, but niosomes could be handled by proniosomes. Proniosomes in this research was prepared using the combination of maltodextrin DE 5-10 from arrowroot starch (Maranta arundinaceae Linn., Span 60 and Cholesterol as non ionic surfactant in six formulas. The entrapment level of CTM depends on combination of surfactant in proniosomes, drug substance concentration and proniosomes quantity, temperature, and hydration times. Niosomes (10mM that was prepared by proniosomes in formula 3 has been hydrated at 80 oC for 2 minutes using demineralized water could entrapped 94,04%, of 1 mM CTM. The proniosomes in formula 3 was increased up to 30 mM surfactant and 10 mM CTM in niosomes, could increase the entrapment of CTM.

  3. Analysis of chlorpheniramine in human urine samples using dispersive liquid-liquid microextraction combined with high-performance liquid chromatography

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    Mehdi Maham

    2014-09-01

    Full Text Available A simple and environmentally friendly microextraction technique was used for determination of chlorpheniramine (CPM, an antihistamine drug, in human urine samples using dispersive liquid-liquid microextraction (DLLME followed by high performance liquid chromatography with diode array detection (HPLC-DAD. In this extraction technique, an appropriate mixture of acetonitrile (disperser solvent and carbon tetrachloride (extraction solvent was rapidly injected into the urine sample containing the target analyte. Tiny droplets of extractant were formed and dispersed into the sample solution and then sedimented at the bottom of the conical test tube by centrifugation. Under optimal conditions, the calibration curve was linear in the range of 0.055-5.5 µg mL-1, with a detection limit of 16.5 ng mL-1. This proposed method was successfully applied to the analysis of real urine samples. Low consumption of toxic organic solvents, simplicity of operation, low cost and acceptable figures of merit are the main advantages of the proposed technique.

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

    OpenAIRE

    Pinak M. Sanchaniya; Falgun A. Mehta; Uchadadiya, Nirav B.

    2013-01-01

    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 stati...

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

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    TO Ogungbamigbe

    2008-02-01

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

  6. 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.

  7. 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.

  8. Simultaneous determination of caffeine and chlorpheniramine in human plasma by LC-MS/MS%LC-MS/MS法同时测定人血浆中的咖啡因和氯苯那敏

    Institute of Scientific and Technical Information of China (English)

    赵婷; 张丹; 杨漫; 张娅喃; 韩静; 肖雪; 刘会臣

    2012-01-01

    OBJECTIVE To develop a method for simultaneous determination of caffeine and chlorpheniramine in human plasma by LC - MS/MS. METHODS After liquid - liquid extraction, caffeine, chlorpheniramine and diphenhydramine ( IS) were separated on an Inertsil ODS - SP analytical column using the mobile phase of methanol - 5 mmol · L-1 ammonium acetate ( containing 0.5% formic acid) (55 : 45) at a flow rate of 0. 3 mL·min-1. Detection was carried out by electrospray positive ionization mass spectrometry in the multiple reaction monitoring(MRM) mode. The MRM transitions of m/z 195.3→110.2, m/z 275. 2→230.2, m/z 256.2→167.3 were used to quantify caffeine, chlorpheniramine and IS, respectively. RESULTS The method was linear ( r > 0. 999 ) in the concentration ranges of 4.0 - 1. 2 × 103,0. 05 - 15. 0 μg·L-1 for caffeine and chlorpheniramine,respectively. Intra - batch and inter- batch RSD were both less than 13% ,and the RE were within ±5% . The mean extract recoveries were 67. 6% ±1.3% ,69.1% ±3.4% for caffeine and chlorpheniramine, respectively. CONCLUSION The method is a rapid, sensitive, selective and reliable method for the determination of caffeine and chlorpheniramine in human plasma. It was successfully applied to a bioequivalence study of the two analyses in healthy Chinese volunteers after administration of pediatric paracetamol and amantadine hydrochloride effervescent tablets.%目的 采用LC-MS/MS法同时测定人血浆中咖啡因和氯苯那敏的浓度.方法 人血浆样本经液液萃取后,选用Inertsil ODS-SP色谱柱(75 mm×2.1 mm,3μm),流动相为甲醇-5 mmol·L-1乙酸铵(含0.5%甲酸)(55∶45),流速0.3 mL·min-1,选用API3200型三重四极杆串联质谱仪的多重反应监测(MRM)扫描方式进行监测,电喷雾离子化源,正离子方式,选择监测离子反应分别为m/z 195.3→110.2(咖啡因)、m/z 275.2→230.2(氯苯那敏)和m/z256.2→167.3(苯海拉明内标).结果 血浆中咖啡因和氯苯那

  9. 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.

  10. Effects of pyrimethamine-sulphadoxine, chloroquine plus chlorpheniramine, and amodiaquine plus pyrimethamine-sulphadoxine on gametocytes during and after treatment of acute, uncomplicated malaria in children

    Directory of Open Access Journals (Sweden)

    A Sowunmi

    2006-12-01

    Full Text Available The effects of pyrimethamine-sulphadoxine (PS, chloroquine plus chlorpheniramine, a H1 receptor antagonist that reverses chloroquine resistance in Plasmodium falciparum in vitro and in vivo (CQCP, and amodiaquine plus pyrimethamine-sulphadoxine (AQPS on gametocyte production were evaluated in 157 children with acute, symptomatic, uncomplicated falciparum malaria who were treated with these drugs. PS was significantly less effective than CQCP or AQPS at clearing asexual parasitaemia or other symptoms of malaria. Gametocyte carriage on days 3, 7, and 14 were significantly higher in those treated with PS. The ratio of the density (per µl blood of peripheral young gametocyte (PYG, that is, < stage III to peripheral mature gametocyte (PMG, that is, stage IV and V, an index of continuing generation of gametocytes, rose to 1 by day 7 of treatment in those treated with PS, but remained consistently below 1 in the other treatment groups. PYG-PMG density ratio increased significantly from day 0-14 in those treated with PS and CQCP (chi2 = 76, P = 0.000001 and chi2 = 42.2, P = 0.00001, respectively but decreased significantly in those treated with AQPS (chi2 = 53.2, P = 0.000001. Both PS-sensitive and -resistant infections generated PYG (18 of 29 vs 13 of 20, chi2 = 0.04, P = 0.93 but PYG was present only in those with resistant response to CQCP. Combination of PS with amodiaquine (AQ, that is, (AQPS resulted in less production of PYG, but in this setting, PYG was not indicative of response to AQPS. These data indicate that PS enhanced production or release of young gametocytes when used alone, but generated less young gametocytes when used in combination with AQ. PYG may be used as an indicator of response to CQCP but not PS or PS-based combination drugs.

  11. 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.

  12. Pharm GKB: chlorpheniramine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available hlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin fl...lopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetin...hlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...lopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetin... chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  13. 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

  14. 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

  15. 78 FR 14217 - Control of Alcohol and Drug Use: Addition of Post-Accident Toxicological Testing for Non...

    Science.gov (United States)

    2013-03-05

    ... and asked how FRA decided to select diphenhydramine, chlorpheniramine, bromenphiramine, and doxylamine..., chlorpheniramine, bromenphiramine, and doxylamine'' (77 FR at 29308, emphasis added). As explained below,...

  16. A Case of Thrombocytopenia Caused by Dextromethorphan-chlorpheniramine-pseudoephedrine Solution%美敏伪麻口服液引起血小板减少1例

    Institute of Scientific and Technical Information of China (English)

    李松杨

    2009-01-01

    @@ 1 临床资料 患者,男性,68岁,因咳嗽、咯痰3 d于2007年4月20日就诊.3 d前因受凉出现咳嗽、咯白色黏痰,自购美敏伪麻口服液(惠菲宁,惠氏制药有限公司,批号0612204),每日3次,每次10 mL,共服4次;未加服其他药物.因症状不缓解故来我院就诊,既往有高血压病及糖尿病10余年,服氯沙坦(科素亚)50 mg,每日1次,血压控制尚可;口服格列齐特片(达美康)80 mg每日1次,血糖控制良好.查体:T 36.8℃,R 20次·min-1,HR 84次·min-1、律齐,BP 140/90 mmHg(1 mmHg=0.133 kPa);皮肤黏膜未见出血点,右下肺呼吸音减低,未闻及干湿性啰音.

  17. Drug: D08694 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08694 Mixture, Drug dl-Methylephedrine hydrochloride - chlorpheniramine maleate mi...xt; Neoas (TN) dl-Methylephedrine hydrochloride [DR:D02109], (Chlorpheniramine maleate [DR:D00665] | d-Chlorpheniramine maleate [DR:D00668]) PubChem: 96025377 ...

  18. The effect of H1 and H2 histamine antagonists on symptomatic dermographism.

    Science.gov (United States)

    Matthews, C N; Boss, J M; Warin, R P; Storari, F

    1979-07-01

    In ten patients suffering from symptomatic dermographism the combined administration of chlorpheniramine + cimetidine produced a greater reduction in the weal and flare response provoked by a standardized scratch than the administration of chlorpheniramine alone. There was a statistically significant improvement in the overall assessment of the patient's skin condition with the combined administration of chlorpheniramine + cimetidine. Chlorpheniramine given alone produced no significant benefit whilst cimetidine alone produced a marked exacerbation in itching in nearly half the patients who initially entered the study and was sufficient to require withdrawal.

  19. 高效液相色谱法测定美敏伪麻溶液中3种成分的含量%Determination of three components in dextromethorphan-chlorpheniramine-pseudoephedrine solution by HPLC

    Institute of Scientific and Technical Information of China (English)

    解春文; 杨少辉; 史大勇

    2008-01-01

    目的 建立一种高效液相色谱法同时测定美敏伪麻溶液主成分(盐酸伪麻黄碱、马来酸氯苯那敏、氢溴酸右美沙芬)的含量.方法 使用Thermo C18色谱柱(4.6mm×250mm,10μm);以0.02%mol·L-1磷酸二氢钾溶液(磷酸调pH至4.0±0.1)-甲醇(20:80)为流动相A,0.02%mol·L-1磷酸二氢钾溶液(磷酸调pH至4.0±0.1)-甲醇(55:45)为流动相B进行梯度洗脱;流速为1mL·min-1;检测波长为257nm(盐酸伪麻黄碱)和264nm(马来酸氯苯那敏和氢溴酸右美沙芬).结果 盐酸伪麻黄碱线性范围0.96248~1.92496mg·mL-1,平均回收率为99.67%,RSD=0.83%(n=9);马来酸氯苯那敏线性范围0.06456~0.12912mg·mL-1,平均回收率为100.23%,RSD=0.87%(n=9);氢溴酸右美沙芬线性范围0.320088~0.64176mg·mL-1,平均回收率为99.70%,RSD=0.93%(n=9).结论 该方法准确、简单,快速,适用于美敏伪麻溶液中3种成分的同时测定.

  20. Pharm GKB: chlorpromazine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available tine carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ne citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxami...tine carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...lorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  1. Pharm GKB: gefitinib [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...heniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...mine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine g... carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...heniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  2. Pharm GKB: propafenone [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available e debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxa...xetine carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...zine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide ...omipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxa...xetine carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  3. Pharm GKB: thioridazine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available dilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine f...lozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefitin...dilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxe

  4. Pharm GKB: carvedilol [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available arvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ne citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fl...lomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvox...ine carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...romazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecain

  5. Drug: D04447 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 6 ANTIHISTAMINES FOR SYSTEMIC USE R06A ANTIHISTAMINES FOR SYSTEMIC USE R06AB Substituted alkylamines R06AB54 Chlorphenamine, combinat...ions D04447 Betamethasone - d-chlorpheniramine maleate mixt PubChem: 17398108 ...

  6. 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 hydrochloride - noscapine

  7. Epinephrine Injection

    Science.gov (United States)

    ... itching, swelling, skin redness, fast heartbeat, weak pulse, anxiety, confusion, stomach pain, losing control of urine or ... such as chlorpheniramine (Chlor-Trimeton) and diphenhydramine (Benadryl); beta blockers such as propranolol (Hemangeol, Inderal LA, Innopran XL); ...

  8. Dextromethorphan

    Science.gov (United States)

    Alka-Seltzer Plus Cold and Cough Formula® (as a combination product containing Aspirin, Chlorpheniramine, Dextromethorphan, Phenylephrine) ... Alka-Seltzer Plus Day and Night Cold Formulas® (as a combination product containing Aspirin, Dextromethorphan, Phenylephrine)

  9. 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.

  10. Drug: D04313 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04313 Mixture, Drug Dihydrocodeine phosphate - dl-methylephedrine hydrochloride - ...Chlorpheniramine maleate mixt; Huscode (TN) Dihydrocodeine phosphate [DR:D01481], dl-Methylephedrine hydroch...s 22 Respiratory organ agents 222 Antitussives 2229 Others D04313 Dihydrocodeine phosphate - dl-methylephedrine...e phosphate - dl-methylephedrine hydrochloride - Chlorpheniramine maleate mixt PubChem: 17398050 ... ...NES FOR SYSTEMIC USE R06AB Substituted alkylamines R06AB54 Chlorphenamine, combinations D04313 Dihydrocodein

  11. Immunoglobulin E anaphylaxis in rabbits: mechanisms of pulmonary resistance and compliance changes.

    Science.gov (United States)

    Habib, M P; Dunn, A M; Sobonya, R E; Baumgartener, C C; Newell, J D; Halonen, M

    1988-03-01

    Factors causing changes in pulmonary resistance and dynamic compliance with immunoglobulin (Ig) E anaphylaxis in spontaneously breathing rabbits were assessed in ventilated rabbits using tantalum bronchography and wet-to-dry wt ratios. Ventilated rabbits demonstrated changes in resistance and compliance similar to spontaneously breathing rabbits. Chlorpheniramine pretreatment prevented increases in resistance but not decreases in compliance. Anaphylaxis constricted small (less than 1 mm) airways 20.9 +/- 16.0% (mean +/- SD) and intermediate (between 1 and 3 mm) airways 21.8 +/- 19.8%. Chlorpheniramine (10 mg/kg) prevented small airway changes and attenuated those in intermediate airways. Chlorpheniramine prevented histamine-induced constriction of small (23.6 +/- 15.7%) and intermediate (17.6 +/- 15.0%) airways. Lung wet-to-dry wt ratios were unchanged. Changes in resistance and compliance during rabbit IgE anaphylaxis are not due to changes in tidal volume or frequency. Histamine, via H1 receptors, is the principal mediator of pulmonary resistance increases but not dynamic compliance reductions. Chlorpheniramine-sensitive increases in resistance are caused by constrictions of intermediate and small airways, whereas the chlorpheniramine-resistant decrease in compliance is not caused directly by constriction of the smallest measurable airways (0.25 mm) or changes in lung water.

  12. Central effect of histamine in a rat model of acute trigeminal pain.

    Science.gov (United States)

    Tamaddonfard, Esmaeal; Khalilzadeh, Emad; Hamzeh-Gooshchi, Nasrin; Seiednejhad-Yamchi, Sona

    2008-01-01

    In conscious rats implanted with an intracerebroventricular (icv) cannula, effect of icv injections of histamine, chlorpheniramine (H(1)-receptor antagonist) and ranitidine (H(2)-receptor blocker) was investigated in a rat model of acute trigeminal pain. Acute trigeminal pain was induced by putting a drop of 5 M NaCl solution on the corneal surface of the eye and the numbers of eye wipes were counted during the first 30 s. Histamine (20, 40 microg) and chlorpheniramine (80 microg) significantly decreased the numbers of eye wipes. Ranitidine alone had no effect. Pretreatment with chlorpheniramine did not change the histamine-induced analgesia, whereas the histamine effect on pain was inhibited with ranitidine pretreatment. These results indicate that the brain histamine, through central H(2) receptors, may be involved in the modulation of the acute trigeminal pain in rats.

  13. Central interaction between physostigmine and histamine during yawning in rats.

    Science.gov (United States)

    Tamaddonfard, Esmaeal; Soraya, Hamid; Hamzeh-Gooshchi, Nasrin

    2008-01-01

    In this study, the effects of intraperitoneal (ip) injection of physostigmine, subcutaneous (sc) injection of atropine, and intracerebroventricular (icv) injections of histamine, chlorpheniramine (H(1)-receptor antagonist), and ranitidine (H(2)-receptor antagonist) in separate and combined treatments were investigated during yawning in rats. Physostigmine at a dose of 0.25 mg/kg produced the highest number of yawns. Atropine, used alone, was without effect, but physostigmine (0.25 mg/kg, ip)-induced yawning was blocked by pretreatment with atropine (1 mg/kg, sc). Histamine at the doses of 10, 20 and 40 microg produced yawning. Chlorpheniramine and ranitidine, used alone, had no effect, whereas pretreatments with chlorpheniramine and ranitidine at the same dose of 80 microg prevented histamine (40 microg, icv)-induced yawning. The suppressive effect of chlorpheniramine was more than that of ranitidine. Histamine (10 and 40 microg, icv) enhanced, whereas chlorpheniramine and ranitidine at the same dose of 80 microg suppressed, physostigmine (0.25 mg/kg, ip)-induced yawning. Atropine (1 mg/kg, sc) not only suppressed histamine-induced yawning, but also enhanced the inhibitory effect of chlorpheniramine, but not of ranitidine on yawning induced by histamine. These results indicate that muscarinic receptors mediate yawning induced by physostigmine. Histamine central H(1), and to a lesser extent H(2) receptors, may be involved in histamine-induced yawning. Cholinergic muscarinic receptors, as well as histaminergic H(1) and to a lesser extent H(2) receptors, may lso be involved in the interaction between brain acetylcholine and histamine.

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

    Science.gov (United States)

    Nakasone, Tasuku; Sugimoto, Yumi; Kamei, Chiaki

    2016-04-15

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

  15. 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.

  16. Epidemiology of Toxicological Factors in Civil Aviation Accident Pilot Fatalities, 1999-2003

    Science.gov (United States)

    2005-11-01

    central nervous system (5−7). For example, fi rst-generation antihistaminics—brompheniramine, chlorpheniramine, diphenhydramine, and doxylamine— cause...1 3 5 Quinidine 0 0 1 1 Ranitidine 2 3 9 17 Sertraline /Desmethylsertraline 0 6 11 19 Sildenafil/Metabolite(s) 0 1 3 4 Theophylline 1 3 2 6

  17. 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.

  18. Drug: D04296 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04296 Mixture, Drug Diprophylline - methoxyphenamine hydrochloride - noscapine - c...al organs 22 Respiratory organ agents 222 Antitussives 2229 Others D04296 Diprophylline - methoxyphenamine hydrochloride - noscapine...04296 Diprophylline - methoxyphenamine hydrochloride - noscapine - chlorpheniramine maleate mixt PubChem: 17398046 ...

  19. 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.

  20. Pharm GKB: metoprolol [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available amine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan dox...e chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...vedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan... citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ilol codeine debrisoquine dextromethorphan metoprolol N/A N/A N/A VIP VA CYP2D6 *

  1. Pharm GKB: tamoxifen [PharmGKB

    Lifescience Database Archive (English)

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  2. Pharm GKB: tolterodine [PharmGKB

    Lifescience Database Archive (English)

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  3. Pharm GKB: doxepin [PharmGKB

    Lifescience Database Archive (English)

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  4. Pharm GKB: mianserin [PharmGKB

    Lifescience Database Archive (English)

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  5. Pharm GKB: clomipramine [PharmGKB

    Lifescience Database Archive (English)

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  6. Pharm GKB: flecainide [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available promazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...opram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine...ine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine ge...carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...zine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  7. Pharm GKB: zuclopenthixol [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine...vedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...opram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine... clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefit

  8. Pharm GKB: atomoxetine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine ...amine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan dox...romazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecain...lol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...ne chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepi

  9. Pharm GKB: paroxetine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available e citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...pram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan dox...rvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...e chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin...e citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide flu

  10. Pharm GKB: maprotiline [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available iramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan d...lomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin f...ine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefitinib ha...lol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan... citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  11. Pharm GKB: codeine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available pramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin fleca...lol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...alopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxeti...e chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin...ne clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide

  12. Pharm GKB: mexiletine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available lorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...opram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine...lorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...opram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine...arvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

  13. Pharm GKB: timolol [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available amine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine ...deine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefitinib haloperi... chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...pram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan dox...orpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flec

  14. Pharm GKB: imipramine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available ine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxep...clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefiti...l chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...opram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine...orpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan

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

    Directory of Open Access Journals (Sweden)

    Dr Sudip Parajuli

    2006-07-01

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

  16. 76 FR 1174 - Drugs for Human Use; Drug Efficacy Study Implementation; Oral Prescription Drugs Offered for...

    Science.gov (United States)

    2011-01-07

    ..., dosage forms, salts, and esters of the same drug moiety as well as of any drug moiety related in chemical... its IRS products Chlorpheniramine Maleate S.R. Capsules and Efedra-PA Tablets, and KV Pharmaceutical... Midway Blvd., Broomfield, CO 80020. On December 4, 2009, KV Pharmaceutical Co. also withdrew its...

  17. Separation of cold medicine ingredients by capillary electrophoresis.

    Science.gov (United States)

    Suntornsuk, L

    2001-01-01

    This study demonstrates the separation of cold medicine ingredients (e.g., phenylpropanolamine, dextromethorphan, chlorpheniramine maleate, and paracetamol) by capillary zone electrophoresis and micellar electrokinetic chromatography. Factors affecting their separations were the buffer pH and the concentrations of buffer, surfactant and organic modifiers. Optimum results were obtained with a 10 mM sodium dihydrogen-phosphate-sodium tetraborate buffer containing 50 mM sodium dodecyl sulfate (SDS) and 5% methanol (MeOH), pH 9.0. The carrier electrolyte gave a baseline separation of phenylpropanolamine, dextromethorphan, chlorpheniramine maleate, and paracetamol with a resolution of 1.2, and the total migration time was 11.38 min.

  18. Automated drug dissolution monitor that uses a UV-visible diode array spectrophotometer.

    Science.gov (United States)

    Lo, S C; Donahue, S M; Brown, C W

    1993-04-01

    A method for performing multicomponent analysis in drug dissolution testing without chromatographic separation is presented. Aliquots from dissolution vessels are automatically transferred to a UV-visible diode array spectrophotometer, spectra are measured, and the aliquots are returned to the testing vessels. A full-spectrum calibration method based on principal-component regression is used to simultaneously determine the concentrations of active ingredients and to account for interferences due to excipients in a tablet formulation. The system was evaluated with two commercial pharmaceutical formularies; the first contained pseudoephedrine hydrochloride and chlorpheniramine maleate, whereas the second was a mixture of phenylpropanolamine hydrochloride and chlorpheniramine maleate. The selections of standard mixtures for calibration and validation were based on a factorial design.

  19. Phentolamine-induced rhythmic contractions in bladder detrusor muscle of guinea-pig.

    OpenAIRE

    Satake, N; Shibata, S.; Ueda, S.

    1984-01-01

    Phentolamine caused a rhythmic contraction concentration-dependently without affecting resting tone in the detrusor muscle. Prazosin, yohimbine, propranolol, noradrenaline, clonidine or isoprenaline failed to cause the rhythmic contraction. These agents did not modify the response to phentolamine suggesting no involvement of alpha- or beta-adrenoceptors in the response to phentolamine. Chlorpheniramine, cimetidine, methysergide, SK&F 83566, atropine, bretylium, hemicholinium or tetrodotoxin f...

  20. 阿斯美胶囊4个组分的HPLC测定法

    Institute of Scientific and Technical Information of China (English)

    章苏玲

    1999-01-01

    @@ 阿斯美胶囊(Asmeton"strong")为日本进口,临床上用于治疗咳嗽、痰、哮喘.其主要成分是由氨茶碱(Aminophylline)、盐酸甲氧那明(Methoxyph-enamine Hydrochloride)、那可汀(Noscapine)、马来酸氯苯那敏(Chlorpheniramine Maleate)组成.

  1. 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...

  2. Sensory responses of human skin to synthetic histamine analogues and histamine.

    OpenAIRE

    Davies, M. G.; Greaves, M W

    1980-01-01

    The potential for itch production in human skin of the synthetic analogues of histamine, 2-methyl histamine (an H1-receptor agonist) and 4-methyl histamine and dimaprit (H2-receptor agonists) has been studied in vivo and compared with histamine. Itch thresholds for 2-methyl histamine were consistently much higher than for histamine (P < 0.001). The H1-receptor antagonist chlorpheniramine raised the itch thresholds to 2-methyl histamine and histamine significantly (P < 0.001). Pruritus was not...

  3. Formulasi Tablet Klorfeniramin Maleat Menggunakan Selulosa Mikrokristal dengan Metode Cetak Langsung

    OpenAIRE

    Sihaloho, Jandri Duvico

    2011-01-01

    Microcrystalline cellulose is an exipient which often used in the manufacture of tablets by direct compression. The purpose of this research is to apply the use of microcrystalline cellulose isolated from nata de coco as a diluent in the manufacture of chlorpheniramin maleate tablets by direct compression. Microcrystalline cellulose obtained by isolation from nata de coco. Isolation was carried out by extraction using 18% sodium hydroxide to produce α-cellulose and α-cellulose is hydrol...

  4. Pharm GKB: sparteine [PharmGKB

    Lifescience Database Archive (English)

    Full Text Available *21, CYP2D6 *44, CYP2D6 *5 and debrisoquine, dextromethorphan, sparteine Level of Evidence Level 4 Type Othe...lozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxamine gefitin... carvedilol chlorpheniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...heniramine chlorpromazine citalopram clomipramine clozapine codeine debrisoquine desipramine dextromethorphan...omipramine clozapine codeine debrisoquine desipramine dextromethorphan doxepin flecainide fluoxetine fluvoxa

  5. Development of screening assays to test novel integrin antagonists in allergic inflammation

    OpenAIRE

    Spartà, Antonino Maria

    2009-01-01

    Aim of the research: to develop a prototype of homogeneous high-throughput screening (HTS) for identification of novel integrin antagonists for the treatment of ocular allergy and to better understand the mechanisms of action of integrin-mediated levocabastine antiallergic action. Results: This thesis provides evidence that adopting scintillation proximity assay (SPA) levocabastine (IC50=406 mM), but not the first-generation antihistamine chlorpheniramine, displaces [125I]fibronectin (F...

  6. 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.

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

    Directory of Open Access Journals (Sweden)

    Zeraati F

    2000-10-01

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

  8. Investigation of Peripheral Effects of Citrus Limon Essential Oil on Somatic Pain in Male Wistar Rats: Role of Histaminergic System

    Directory of Open Access Journals (Sweden)

    Ali Mojtahedin

    2016-12-01

    Full Text Available Background & Objective: One of the plants used in traditional medicine is lemon which has analgesic effect. However, little research has been performed on the analgesic effect of lemon and mechanisms of action with an emphasis on neurotransmitters systems. Therefore, the present study set to investigate the peripheral effects of lemon essential oil on somatic pain using formalin test with an emphasis on histaminergic system in male Wistar rats. Materiala & Methods: Sixty male rats weighing approximately 200-250g and aged 14-16 wk were divided into 10 groups: sham (Salin + Formalin 1% intraplantar, three treatment groups with lemon essential oil (EO (12.5, 25 and 50 mg/kg, three treatment groups with Chlorpheniramine (5, 10 and 20 mg/kg, 1 treatment group with Histamine (10 mg/kg, 1 pretreatment group with Chlorpheniramine (20 mg/kg + EO (50mg/kg, and 1 pretreatment group with Histamine (10 mg/kg + EO (50 mg/kg. Formalin test was used to assess somatic pain. Data analysis was performed using one-way ANOVA. Results:  Intraperitoneal injection of lemon essential oil reduced the pain response induced by formalin in both phases (P<0.05. Pretreatment with chlorpheniramine and lemon essential oil enhanced the analgesic response in both phases (P<0.05. Conclusion: Lemon essential oil had analgesic effects, probably caused by the histaminergic system.

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

    Directory of Open Access Journals (Sweden)

    Zanboori Ali

    2010-01-01

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

  10. Efficacy of anti-pruritis drugs in chronic renal failure: a comparative study

    Directory of Open Access Journals (Sweden)

    "H. Khalili

    2006-07-01

    Full Text Available Background: Pruritus is one of the most common problems in patients suffering chronic renal failure. Twenty five - 35% of predialysis patients and 60-80% of patients during dialysis complain pruritus. The exact pathophysiology of pruritus is unknown; however, some possible interactive factors include: histamine release from mast cells and basophiles, uremic skin, cutaneous mast cells proliferation, adipose cells atrophy, electrolyte imbalance, and accumulation of bile acids. Since histamine is the main proposed mediator in pruritus, the goal of this study was to evaluate the role of antihistamines in controling of pruritus of patients with chronic renal failure. This study was done as a before - after study during one year period in dialysis department of Imam Khomeini hospital. Methods: Thirty patients complied with inclusion criteria were entered in the study. Treatment strategy was: 2 weeks treatment with hydroxyzine 25 mg TDS, followed by one week wash-out period, then 2 weeks ketotifen therapy 1mg BID and finally two weeks treatment with chlorpheniramine 4mg BD following one week washout period after ketotifen therapy. Pruritus severity before and after each treatment period was evaluated with Pruritus Severity Score (PSS chart. Results: The mean PSS reduction by hydroxyzine, ketotifen and chlorpheniramine, were 33%, 4.5% and 20%, respectively. Conclusion: PSS improvement with hydroxyzine and chlorpheniramine was statistically significant (p<0.001. However, ketotifen induced pruritus reduction was not considerably significant.

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

    OpenAIRE

    Zanboori Ali; Tamaddonfard Esmaeal; Mojtahedin Ali

    2010-01-01

    Objective : This study was designed to investigate the role of brain histamine and H1 and H2 receptors in mediating the central perception of visceral pain in rats. Materials and Methods : In conscious rats implanted with a lateral brain ventricle cannula, the effect of intracerebroventricular (i.c.v.) injection of histamine (2.5, 10, and 40 μg), and chlorpheniramine and ranitidine at the same doses of 5, 20, and 80 μg were investigated on visceral pain. Visceral nociception induce...

  12. Evaluation of in vivo selective binding of [{sup 11}C]doxepin to histamine H{sub 1} receptors in five animal species

    Energy Technology Data Exchange (ETDEWEB)

    Ishiwata, Kiichi E-mail: ishiwata@pet.tmig.or.jp; Kawamura, Kazunori; Wang Weifang; Tsukada, Hideo; Harada, Norihiro; Mochizuki, Hideki; Kimura, Yuichi; Ishii, Kenji; Iwata, Ren; Yanai, Kazuhiko

    2004-05-01

    The specific binding of [{sup 11}C]doxepin, which has been used as a radioligand for mapping histamine H{sub 1} receptors in human brain by positron emission tomography, was evaluated in five animal species. In mice the [{sup 11}C]doxepin uptake was reduced by treatment with cold doxepin and two H{sub 1} receptor antagonists, but not with H{sub 2}/H{sub 3} antagonists. The specific binding evaluated with treatment with (+)-chlorpheniramine (H{sub 1} antagonist) was in the range of 10-30% in mouse, rat, rabbit, and monkey, but was not detected in guinea pig.

  13. 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.

  14. 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.

  15. Involvement of central histamine in amygdaloid kindled seizures in rats.

    Science.gov (United States)

    Kamei, C

    2001-10-15

    The involvement of central histamine in amygdaloid kindled seizures in rats was investigated using histamine-related compounds. Histamine contents in the amygdala of electrical stimulation site was significantly decreased after development of amygdaloid kindling. Intracerebroventricular (i.c.v.) injection of histamine resulted in inhibition of amygdaloid kindled seizures. The H(1)-agonists 2-methylhistamine and 2-thiazolylethylamine also inhibited amygdaloid kindled seizures. In addition, intraperitoneal (i.p.) injection of histidine and metoprine inhibited amygdaloid kindled seizures at doses that caused increases in histamine contents of the brain. H(1)-antagonists (diphenhydramine and chlorpheniramine) attenuated histamine (i.c.v.)-induced inhibition of amygdaloid kindled seizures, however, no significant antagonism was observed with H(2)-antagonists (cimetidine, ranitidine or zolantidine). Intracerebroventricular injection of H(3)-antagonists (thioperamide and AQ 0145) resulted in a dose-related inhibition of amygdaloid kindled seizures. The same findings were observed when thioperamide and clobenpropit were injected i.p. The effects of thioperamide (i.p.) and AQ 0145 (i.p.) were inhibited by an H(3)-agonist [(R)-alpha-methylhistamine] and H(1)-antagonists (diphenhydramine and chlorpheniramine). On the other hand, H(2)-antagonists (cimetidine and ranitidine) showed no antagonistic effects. These findings suggested that a histaminergic mechanism plays an important role in suppressing amygdaloid kindled seizures through histamine H(1)-receptors.

  16. Effects of alpha-adrenoceptor agonists and antagonists on histamine-induced impairment of memory retention of passive avoidance learning in rats.

    Science.gov (United States)

    Zarrindast, Mohammad-Reza; Ahmadi, Ramesh; Oryan, Shahrbanoo; Parivar, Kazem; Haeri-Rohani, Ali

    2002-11-15

    The effect of alpha-adrenoceptor agents on the impairment induced by histamine was measured for memory retention of passive avoidance learning in rats. Post-training intracerebroventricular (i.c.v.) injection was carried out in all the experiments. Histamine (5, 10 and 20 microg/rat) reduced, while a histamine H(1) receptor antagonist, chlorpheniramine (0.1, 1 and 10 microg/rat), increased memory retention. The histamine H(2) receptor antagonist, ranitidine (0.1, 1, 10 and 20 microg/rat), did not elicit any response in this respect. Different doses of chlorpheniramine but not ranitidine reversed the histamine-induced impairment of memory. Clonidine and prazosin decreased, but yohimbine and phenylephrine increased, memory retention. Yohimbine decreased the inhibitory response to histamine. Phenylephrine, clonidine and prazosin did not alter the histamine effect. It is concluded that a histamine-induced impairment of memory retention through histamine H(1) receptors and an alpha(2)-adrenoceptor mechanism may be involved in the histamine response.

  17. State-dependent interaction in the antihistamine-induced disruption of a radiation-induced conditioned taste aversion

    Energy Technology Data Exchange (ETDEWEB)

    Rabin, B.M. (Armed Forces Radiobiology Research Inst., Bethesda, MD); Hunt, W.A.; Lee, J.

    1982-06-01

    Two experiments were run to evaluate the possibility that injection of antihistamine can produce a state-dependent acquisition of a radiation-induced conditioned taste aversion. In the first experiment, pretreating rats with the antihistamine chlorpheniramine maleate prior to their initial exposure to sucrose and to low-level irradiation on the conditioning day did not prevent the acquisition of a taste aversion to sucrose when the antihistamine was also administered prior to a subsequent preference test. In the second experiment, rats were both conditioned and tested for a radiation-induced aversion in a drug-free state. Under these condtions, the rats continued to show an aversion to sucrose despite pretreating them with chlorpheniramine prior to irradiation. Since rats conditioned under the antihistamine do not show the radiation-induced conditioned taste aversion when tested for sucrose preference in a nondrug state, it would seem that pretreating rats with an antihistamine prior to conditioning affects only the retrieval of the previously learned response and not its acquisition.

  18. Applying patient centered approach in management of pulmonary tuberculosis: A case report from Malaysia.

    Science.gov (United States)

    Atif, M; Sulaiman, Sas; Shafi, Aa; Muttalif, Ar; Ali, I; Saleem, F

    2011-06-01

    A 24 year university student with history of productive cough was registered as sputum smear confirmed case of pulmonary tuberculosis. During treatment, patient suffered from itchiness associated with anti tuberculosis drugs and was treated with chlorpheniramine (4mg) tablet. Patient missed twenty eight doses of anti tuberculosis drugs in continuation phase claiming that he was very busy in his studies and assignments. Upon questioning he further explained that he was quite healthy after five months and unable to concentrate on his studies after taking prescribed medicines. His treatment was stopped based on clinical improvement, although he did not complete six months therapy. Two major reasons; false perception of being completely cured and side effects associated with anti TB drugs might be responsible for non adherence. Non sedative anti histamines like fexofenadine, citrizine or loratidine should be preferred over first generation anti histamines (chlorpheniramine) in patients with such lifestyle. Patient had not completed full course of chemotherapy, which is preliminary requirement for a case to be classified as "cure" and "treatment completed". Moreover, patient had not defaulted for two consecutive months. Therefore, according to WHO treatment outcome categories, this patient can neither be classified as "cure" or "treatment completed" nor as "defaulter". Further elaboration of WHO treatment outcome categories is required for adequate classification of patients with similar characteristics. Likelihood of non adherence can be significantly reduced by applying the WHO recommended "Patient Centered Approach" strategy. Close friend, class mate or family member can be selected as treatment supporter to ensure adherence to treatment.

  19. Histamine mediates the pro-inflammatory effect of latex of Calotropis procera in rats.

    Science.gov (United States)

    Shivkar, Yatin M; Kumar, Vijay L

    2003-01-01

    INTRODUCTiON: Calotropis procera is known to produce contact dermatitis and the latex of this plant produces intense inflammation when injected locally. However, the precise mode of its pro-inflammatory effect is not known. In present study we have pharmacologically characterized the inflammation induced by latex of C. procera in a rat paw edema model and determined the role of histamine in latex-induced inflammation. METHODS: Inflammation was induced in the hind paw of rats by injecting different doses of dried latex (DL) of C. procera. The inhibitory effect of phenylbutazone, dexamethasone, celecoxib, cyproheptadine, chlorpheniramine and compound 48/80 on edema volume was evaluated and compared with that against carrageenan. The histamine content of DL was measured fluorometrically. RESULTS: DL produced dose-dependent inflammation of the rat paw. Cyproheptadine and chlorpheniramine effectively inhibited DL-induced inflammation (90%; p phenylbutazone, dexamethasone and celecoxib were more effective against carrageenan-induced inflammation. Depletion of mast cell histamine by compound 48/80 produced a significant decrease in DL-induced inflammation as compared with carrageenan (500% versus 25%). DL was also found to contain about 6 microg/g of histamine. CONCLUSIONS: Thus, our study shows that the biogenic amines play a significant role in C. procera latex-induced inflammation and antihistaminic drugs could be effectively used to inhibit inflammatory response elicited by exposure to latex. PMID:14760937

  20. 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.

  1. Participation of histamine in the step-through active avoidance response and its inhibition by H1-blockers.

    Science.gov (United States)

    Kamei, C; Tasaka, K

    1991-12-01

    The effects of intravenous and intracerebroventricular administrations of certain H1-blockers on the active avoidance response in rats were studied. Among the classic H1-blockers used in this study: pyrilamine, diphenydramine, promethazine and chlorpheniramine, promethazine was the most effective and chlorpheniramine the least in inhibiting the active avoidance response; namely, a variation of prolongation in the response latency of the avoidance response. Meanwhile, ketotifen most potently inhibited the active avoidance response when the drugs were administered intracerebroventricularly. Mequitazine, astemizole and oxatomide were weak depressants when administered by either route. Azelastine was less effective than the classic H1-blockers by intravenous injection, while by intracerebroventricular injection, the inhibition was almost identical to those induced by the classic H1-blockers. Intracerebroventricular injection of histamine was antagonized the prolonged latency in the avoidance response induced by pyrilamine or diphenhydramine. A similar effect was also produced by 2-methylhistamine, but 4-methylhistamine had no effect. Intracerebroventricular injection of acetylcholine was restored the retarded avoidance response induced by pyrilamine, but a dose 20 times greater than that of histamine was required. From these findings, it can be concluded that inhibition of the active avoidance response induced by H1-blockers may be exerted through interaction with H1-receptors in the brain.

  2. 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.

  3. 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

  4. 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.

  5. Three-dimensional solubility parameters and their use in characterising the permeation of drugs through the skin.

    Science.gov (United States)

    Groning, R; Braun, F J

    1996-05-01

    The physico-chemical properties of drug substances are major determinants of their transdermal absorption. In the present study the concept of the three-dimensional solubility parameters of Hansen was applied in conjunction with the Bagley projection to describe the permeation of drugs and model substances through the skin. Drug permeation data from the literature were compared with the calculated solubility parameters of the drugs. It was demonstrated that the permeation of drugs can be estimated by their position in the Bagley diagram. There is a linear correlation between the logarithm of the skin permeation of drugs and the exchange cohesive energy for the steroids testosterone, progesterone, hydrocortisone acetate, corticosterone, cortisone, and dexamethasone. A linear correlation can be confirmed for the permeation of glyceryl trinitrate, digitoxin, oestradiol, scopolamine, atropine, diethylcarbamazine, fentanyl, and chlorpheniramine. In the case of morphine, codeine, sufentanil, meperidine and hydromorphone there is a linear relationship, too.

  6. Effects of intracerebroventricular injection of histamine and its related compounds on rectal temperature in mice.

    Science.gov (United States)

    Chen, Z; Sugimoto, Y; Kamei, C

    1995-12-01

    Effects of intracerebroventricular injection of histamine and its related compounds on rectal temperature were studied in mice. Histamine (0.1-1.0 mu g) and histidine (500-1,000 mg/kg) caused a dose-related hypothermia. H1 agonist, 2-methylhistamine and 2-thiazolylethylamine also displayed a dose-dependent hypothermia. In addition, H2 agonists, 4-methylhistamine and dimaprit elicited a decrease in body temperature. Preinjection of not only H1-antagonists (diphenhydramine and chlorpheniramine) but also H2 antagonists (cimetidine and ranitidine) abolished histamine-induced hypothermia. Either intracerebroventricular or intraperitoneal injection of thioperamide, a histamine H3 antagonist, showed hypothermia. The hypothermic effect produced by intracerebroventricular injection of thioperamide was significantly blocked by (R)-alpha-methylhistamine, a selective H3 agonist. In addition, the effect induced by thioperamide was inhibited by H1 and H2 antagonists, indicating that the H3 receptor also participates in histamine-induced hypothermia.

  7. Radiation-released histamine in the rhesus monkey as modified by mast cell depletion and antihistamine. Scientific report

    Energy Technology Data Exchange (ETDEWEB)

    Doyle, T.F.; Strike, T.A.

    1975-06-01

    Changes in blood histamine concentrations of rhesus monkeys were measured after a 4000-rad dose of mixed gamma-neutron radiation. All animals were pretreated with amino-guanidine to retard histamine catabolism. Histamine concentrations increased from 26 + or - 13.5 to 235 + or - 16 ng/ml after irradiation. When the animals were pretreated with an antihistamine, chlorpheniramine (3 mg/kg), histamine concentrations changed from 25.7 + or - 13.5 to 462 + or - 226 ng/ml after irradiation. When the monkeys were pretreated with a specific mast cell histamine depleter, compound 48/80 (1mg/kg per day) for four consecutive days and then irradiated (4000 rads), histamine concentrations did not change significantly. When 48/80 was given 20 min after irradiation, histamine concentrations changed from 18 + or - 2 ng/ml to a maximum of 35 + or - 9 ng/ml after 48/80 injection. (Author) (GRA)

  8. HPLC双波长法同时测定复方维A酸软膏中2主药的含量%Simultaneous Content Determination of 2 Components in Compound Tretinoin Ointment by Dual Wavelength HPLC

    Institute of Scientific and Technical Information of China (English)

    魏立明; 宋霞; 宋三孔; 杨效宇; 焦海胜

    2012-01-01

    OBJECTIVE: To establish the method for the simultaneous determination of tretinoin and chlorpheniramine maleate in compound tretinoin ointment. METHODS: HPLC method was adopted. Luna da column was used with mobile phase consisted of methanol-phosphate buffer (0.02 mol-L-1 potassium dihydrogen phosphate, pH adjusted to 7.0 using 1 mol·L-1 sodium hydroxide, F/K=80:20) at a flow rate of 1.0 mL·min-1. The column temperature was 30 °C and injection volume was 20 μL. The detection wavelength was set at 350 nm and 262 nm for tretinoin and chlorpheniramine maleate, respectively. The content of tretinoin and chlorpheniramine maleate was determined by external standard method. RESULTS: The liner range of tretinoin was 20~100 μg·mL-1 (t-=0.999 9) with an average recovery rates of it at low, medium and high concentrations were 98.48% , 97.15%, 98.88% (RSD=0.92%). The liner range of chlorpheniramine maleate was 30-150 μg·mL-1 (r=0.999 9) with an average recovery rates of it at low, medium and high concentrations were 100.47% , 99.01% , 99.75% (RSD=0.83% ). CONCLUSION: The established method is simple, accurate and reproducible. It can be used for the quality control of compound tretinoin ointment.%目的:建立同时测定复方维A酸软膏中维A酸和马来酸氯苯那敏含量的方法.方法:采用高效液相色谱法.色谱柱为Luna C1.柱,流动相为甲醇-磷酸盐缓冲液(0.02 mol· L-1磷酸二氢钾,用1 mol·L-1氢氧化钠调节pH至7.0,V/V) =80:20,流速为1.0 mL· min-1,进样量为20μL,柱温为30℃,维A酸的检测波长为350 nm,马来酸氯苯那敏的检测波长为262 nrn.采用外标法计算含量.结果:维A酸检测浓度在20~100 μg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.999 9),低、中、高平均加样回收率分别为98.48%、97.15%、98.88% (RSD=0.92%);马来酸氯苯那敏检测浓度在30~150 μg·mL-1范围内与峰面积积分值呈良好的线性关系(r=0.999 9),低、中、高平

  9. 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.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    2011-01-15

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

  11. 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.

  12. Analysis of pharmaceutical preparations containing antihistamine drugs by micellar liquid chromatography.

    Science.gov (United States)

    Martínez-Algaba, C; Bermúdez-Saldaña, J M; Villanueva-Camañas, R M; Sagrado, S; Medina-Hernández, M J

    2006-02-13

    Rapid chromatographic procedures for analytical quality control of pharmaceutical preparations containing antihistamine drugs, alone or together with other kind of compounds are proposed. The method uses C18 stationary phases and micellar mobile phases of cetyltrimethylammonium bromide (CTAB) with either 1-propanol or 1-butanol as organic modifier. The proposed procedures allow the determination of the antihistamines: brompheniramine, chlorcyclizine, chlorpheniramine, diphenhydramine, doxylamine, flunarizine, hydroxyzine, promethazine, terfenadine, tripelennamine and triprolidine, in addition to caffeine, dextromethorphan, guaifenesin, paracetamol and pyridoxine in different pharmaceutical presentations (tablets, capsules, suppositories, syrups and ointments). The methods require minimum handling sample and are rapid (between 3 and 12 min at 1 mLmin(-1) flow rate) and reproducible (R.S.D. values<5%). Limits of detection are lower than 1 microgmL(-1) and the recoveries of the analytes in the pharmaceutical preparations are in the range 100+/-10%.

  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. 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.

  15. Evaluation of extended-release applications for solid dispersion hot-melt fluid bed coatings utilizing hydrophobic coating agents.

    Science.gov (United States)

    Kennedy, J P; Niebergall, P J

    1998-02-01

    A new hot-melt fluid bed coating method was evaluated for potential extended-release applications. Chlorpheniramine maleate (CPM) USP was chosen as a model drug. The assays for drug release and content uniformity were dictated by the USP Official Monograph for a Chlorpheniramine Maleate Extended-Release Capsule. The fluid bed chamber was charged with CPM-loaded nonpareils and hydrophobic coating agents in the solid state. The method consists of four processing stages: (a) warming, (b) preheating, (c) melting-spreading, and (d) cooling-congealing. Various hydrophobic coating agent candidates were evaluated for extended-release potential by a preliminary screen at a coating agent level of 1.5% (w/w). A beeswax coating agent was identified as the most promising candidate of the preliminary screen. After the level of beeswax was increased to 2.0%, the dissolution profile met all of the specifications of the USP Drug Release Test 1 for a CPM Extended-Release Capsule. The potency and content uniformity remained unchanged by the process. Dual coatings demonstrated a cumulative extension of release superior to the capability of a single coat. The new method is a viable alternative to hot-melt spray-coating methodologies. Organic solvents, spraying equipment, steam jackets, and/or heating tape are eliminated from the process. A reduction of equipment costs, setup time, and cleanup time may be realized. The method has demonstrated extended-release capabilities. No excessive attrition of potency or content uniformity has been noted. Additive, multiple coatings that have a cumulative effect on release retardation are feasible.

  16. Prescription writing trends of antihistamines at the university health centre

    Directory of Open Access Journals (Sweden)

    Kumar Anil

    2009-01-01

    Full Text Available The aim of the present study was to establish antihistamines drug prescribing pattern in order to improve the rational prescribing of antihistamines by physicians at Panjab University Health Centre. The study was performed in between the months of November 2005 to April 2006. Five hundred out patients were monitored and data was collected on WHO-based prescription-auditing performa. Demographic analysis of this prospective study revealed that out of the 500 patients, 293 (58.6 % were male and 207 (41.4 % were female and maximum patients were in the age group of 21-40 (34.8 %. Chlorpheniramine maleate (235 prescriptions was the highest prescribed among antihistamine prescriptions (36.89 % followed by diphenhydramine hydrochloride (186 prescriptions, 29.19%, cetirizine (175 prescriptions, 27.47 % and promethazine (41 prescriptions, 6.4%. In comparison to generic drugs (169 prescriptions, 26.54%, branded were more prescribed at PUHC. Majority of antihistamines were in form of tablets (414 prescriptions, 64.99% followed by liquid formulations (195 prescriptions, 30.61% and injections (28 prescriptions, 4.40%. The average cost of different antihistamine drugs prescribed was as follows: diphenhydramine hydrochloride Rs. 34.74 followed by promethzine Rs. 22.46, chlorpheniramine maleate Rs. 15.30, and cetirizine Rs. 13.50. Average numbers of drugs prescribed per prescription were 1.27. The average consulting and dispensing time was 4.82 and 3.56 min, respectively. Out of the 500 university patients, 258 (51.6% had the knowledge regarding the medication prescribed and 242 (48.4% were unaware of the medication prescribed.

  17. 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.

  18. Simultaneous determination of ten antihistamine drugs in human plasma using pipette tip solid-phase extraction and gas chromatography/mass spectrometry.

    Science.gov (United States)

    Hasegawa, Chika; Kumazawa, Takeshi; Lee, Xiao-Pen; Fujishiro, Masaya; Kuriki, Ayako; Marumo, Akemi; Seno, Hiroshi; Sato, Keizo

    2006-01-01

    Ten antihistamine drugs, diphenhydramine, orphenadrine, chlorpheniramine, diphenylpyraline, triprolidine, promethazine, homochlorcyclizine, cyproheptadine, cloperastine and clemastine, have been found to be extractable from human plasma samples using MonoTip C18 tips, inside which C18- bonded monolithic silica gel was fixed. Human plasma (0.1 mL) containing the ten antihistamines was mixed with 0.4 mL of distilled water and 25 microL of a 1 M potassium phosphate buffer (pH 8.0). After centrifugation of the mixture, the supernatant fraction was extracted to the C18 phase of the tip by 25 repeated aspirating/dispensing cycles using a manual micropipettor. The analytes retained on the C18 phase were then eluted with methanol by five repeated aspirating/dispensing cycles. The eluate was injected into a gas chromatography (GC) injector without evaporation and reconstitution steps, and was detected by a mass spectrometer with selected ion monitoring in the positive-ion electron impact mode. The separation of the ten drugs from each other and from impurities was generally satisfactory using a DB-1MS column (30 m x 0.32 mm i.d., film thickness 0.25 microm). The recoveries of the ten antihistamines spiked into plasma were 73.8-105%. The regression equations for the ten antihistamines showed excellent linearity with detection limits of 0.02-5.0 ng/0.1 mL. The within-day and day-to-day coefficients of variation for plasma were not greater than 9.9%. The data obtained from determination of diphenhydramine and chlorpheniramine in human plasma after oral administration of the drugs are also presented.

  19. Contribution of alpha4beta1 integrin to the antiallergic effect of levocabastine.

    Science.gov (United States)

    Qasem, Ahmed R; Bucolo, Claudio; Baiula, Monica; Spartà, Antonino; Govoni, Paolo; Bedini, Andrea; Fascì, Domenico; Spampinato, Santi

    2008-09-15

    Levocabastine is an antiallergic drug acting as a histamine H1-receptor antagonist. In allergic conjunctivitis (AC), it may also antagonize up-regulation of the intercellular adhesion molecule-1 (ICAM-1) expressed on epithelial conjunctival cells. However, little is known about its effects on eosinophils, important effector cells in AC. The adhesion molecule integrin alpha(4)beta(1) is expressed in eosinophils; it interacts with the vascular cell adhesion molecule-1 (VCAM-1) and fibronectin (FN) in vascular endothelial cells and contributes to eosinophil activation and infiltration in AC. This study provides evidence that in a scintillation proximity assay levocabastine (IC(50) 406 microM), but not the first-generation antihistamine chlorpheniramine, displaced (125)I-FN binding to human integrin alpha(4)beta(1) and, in flow cytometry analysis, levocabastine antagonized the binding of a primary antibody to integrin alpha(4) expressed on the Jurkat cell surface. Levocabastine, but not chlorpheniramine, binds the alpha(4)beta(1) integrin and prevents eosinophil adhesion to VCAM-1, FN or human umbilical vascular endothelial cells (HUVEC) in vitro. Similarly, levocabastine affects alpha(L)beta(2)/ICAM-1-mediated adhesion of Jurkat cells. In a model of AC levocabastine eye drops reduced the clinical aspects of the late-phase reaction and the conjunctival expression of alpha(4)beta(1) integrin by reducing infiltrated eosinophils. We propose that blockade of integrin-mediated cell adhesion might be a target of the antiallergic action of levocabastine and may play a role in preventing eosinophil adhesion and infiltration in AC.

  20. Possible role of pseudoephedrine and other over-the-counter cold medications in the deaths of very young children.

    Science.gov (United States)

    Wingert, William E; Mundy, Lisa A; Collins, Gary L; Chmara, Edward S

    2007-03-01

    The Philadelphia Medical Examiners Office has reported a series of 15 deaths between February 1999 and June 2005 of infants and toddlers 16 months and younger in which drugs commonly found in over-the-counter (OTC) cold medications were present. A total of 10 different drugs were detected: pseudoephedrine, dextromethorphan, acetaminophen, brompheniramine, carbinoxamine, chlorpheniramine, ethanol, doxylamine and the anticonvulsants, phenobarbital, and phenytoin. The drugs were confirmed and quantified by gas chromatography (GC)-mass spectrometry, with the exception of ethanol, which was analyzed by headspace GC and of phenobarbital and phenytoin that were quantified by GC with a nitrogen phosphorus detector. The most predominant drug was pseudoephedrine, which was found in all of the cases (blood concentration, n=14, range=0.10-17.0 mg/L, mean=3.34 mg/L) and was the sole drug detected in three cases. Acetaminophen was detected in blood from each of the five cases with sufficient sample. Other drugs (with frequency of detection) were dextromethorphan (five cases), carbinoxamine (four cases), chlorpheniramine (two cases) and brompheniramine, doxylamine, and ethanol (one case each). In the majority of the cases, toxicity from drugs found in easily available OTC medications was listed either as the direct cause of death or as a contributory factor. The manner of death was determined to be natural in only two of the cases. This postmortem study supports previous evidence that the administration of OTC cold medications to infants may, under some circumstances, be an unsafe practice and in some cases may even be fatal. The treating physicians and the general public need to be made more aware of the dangers of using OTC cold medications to treat very young children so that these types of tragedies might be avoided.

  1. The Mexican asthma cure. Systemic steroids for gullible gringos.

    Science.gov (United States)

    Rubin, B K; LeGatt, D F; Audette, R J

    1990-04-01

    Asthmatic patients from western Canada and the United States have reported that after visits to an asthma clinic in Mexicali, Mexico, they return home substantially improved or cured having received "a bronchodilator medication unavailable in the United States or Canada because of the big drug companies." Analysis of these medications reveals that the most commonly prescribed combination is the glucocorticoid triamcinolone (unscored white tablets) and the antihistamine chlorpheniramine (coated biconvex orange or red tablets). Occasionally benzodiazepines are added to these medications. The patients are assured that the medications which they have been given are free of side effects and specifically, that corticosteroids are not used. Such therapy is dangerous to the patient who not only is unaware of the medications that he or she is taking, but is unlikely to mention this therapy to his or her physician. These patients risk drug interactions, medication side effects, and the possibility of adrenal failure either with a stress to their system or on withdrawal of drug treatment. Patients are also at risk of abandoning safer forms of asthma therapy for the miracle cure. We, too, are partially responsible for these unethical practices by avoiding the use of steroids and undertreating our patients at times, leaving them unnecessarily restricted and eager for any form of relief.

  2. Development and validation of an MEKC method for determination of nitrogen-containing drugs in pharmaceutical preparations.

    Science.gov (United States)

    Buiarelli, Francesca; Coccioli, Franco; Jasionowska, Renata; Terracciano, Alessandro

    2008-09-01

    A fast and accurate micellar electrokinetic capillary chromatography method was developed for quality control of pharmaceutical preparations containing cold remedies as acetaminophen, salicylamide, caffeine, phenylephrine, pseudoephedrine, norephedrine and chlorpheniramine. The method optimization was realized on a Beckman P/ACE System MDQ instrument. The baseline separation of seven analytes was performed in an uncoated fused silica capillary internal diameter (ID)=50 microm using tris-borate (20 mM, pH=8.5) containing sodium dodecyl sulphate 30 mM BGE. On line-UV detection at 214 nm was performed and the applied voltage was 10 kV. The operating temperature was 25 degrees C. After experimental conditions optimization, the proposed method was validated. The evaluated parameters were: precision of migration time and of corrected peak area ratio, linearity range, limit of detection, limit of quantification, accuracy (recovery), ruggedness and applicability. The method was then successfully applied for the analysis of three pharmaceutical preparations containing some of the analytes listed before.

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

    Energy Technology Data Exchange (ETDEWEB)

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

    1989-10-01

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

  4. Velocity gap mode of capillary electrophoresis developed for high-resolution chiral separations.

    Science.gov (United States)

    Li, Xue; Li, Youxin; Zhao, Lumeng; Shen, Jianguo; Zhang, Yong; Bao, James J

    2014-10-01

    A new CE method based on velocity gap (VG) theory has been developed for high-resolution chiral separations. In VG, two consecutive electric fields are adopted to drive analytes passing through two capillaries, which are linked together through a joint. The joint is immersed inside another buffer vial which has conductivity communication with the buffer inside the capillary. By adjusting the field strengths onto the two capillaries, it is possible to observe different velocities of an analyte when it passes through those two capillaries and there would be a net velocity change (NVC) for the same analyte. Different analytes may have different NVC which may be specifically meaningful for enantioseparations because enantiomers are usually hard to resolve. By taking advantage of this NVC, it is possible to enhance the resolution of a chiral separation if a proper voltage program is applied. The feasibility of using NVC to enhance chiral separation was demonstrated in the separations of three pairs of enantiomers: terbutaline, chlorpheniramine, and promethazine. All separations started with partial separation in a conventional CE and were significantly improved under the same experimental conditions. The results indicated that VG has the potential to be used to improve the resolving power of CE in chiral separations.

  5. H(1) and H(2) receptors in the locus ceruleus are involved in the intracerebroventricular histamine-induced carotid sinus baroreceptor reflex resetting in rats.

    Science.gov (United States)

    Wang, Guo-Qing; Sun, Wan-Ping; Zhu, Yong-Jin; Zou, Rong; Zhou, Xi-Ping

    2006-07-01

    Objective To investigate the role of H(1) and H(2) 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 H(1) or H(2) 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 mu l) significantly shifted the ISP-MAP relationship curve upwards (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 H(1) and H(2) receptors activities in the LC, especially by H(1) receptors. Moreover, the effects of the central HA on CSR might be related to a histaminergic descending pathway from the hypothalamus to LC.

  6. [Roles of histamine receptors in pain perception: a study using receptors gene knockout mice].

    Science.gov (United States)

    Yanai, Kazuhiko; Mobarakeh, Jalal Izadi; Kuramasu, Atsuo; Sakurada, Shinobu

    2003-11-01

    To study the participation of histamine H1- and H2-receptors in pain perception, H1 and H2 receptor knockout (KO) mice were examined for pain threshold by means of three kinds of nociceptive tasks. These included assays for thermal, mechanical, and chemical nociception. H1KO mice showed significantly fewer nociceptive responses to the hot-plate, tail-flick, tail-pressure, paw-withdrawal, formalin, capsaicin, and abdominal constriction tests. Sensitivity to noxious stimuli in H1KO mice was significantly decreased when compared to wild-type mice. The antinociceptive phenotypes of H2KO were relatively less prominent when compared to H1KO mice. We also examined the antinociceptive effects of intrathecally-, intracerebroventricularly-, and subcutaneously-administered morphine in H1KO and H2KO mice. In these nociceptive assays, the antinociceptive effects produced by morphine were more enhanced in both H1KO and H2KO mice. The effects of histamine H1- and H2-receptor antagonists on morphine-induced antinociception were studied in ICR mice. The intrathecal, intracerebroventricular and subcutaneous co-administrations of d-chlorpheniramine enhanced the effects of morphine in all nociceptive assays examined. In addition, intrathecal co-administrations of cimetidine enhanced the antinociception of morphine in the hot plate tests. These results suggest that existing H1 and H2 receptors play an inhibitory role in morphine-induced antinociception in the spinal and supra-spinal levels.

  7. [Role of central histamine in amygdaloid kindled seizures].

    Science.gov (United States)

    Kamei, C; Okuma, C

    2001-05-01

    The role of central histamine in amygdaloid kindled seizures in rats was studied. Histamine content in the amygdala was significantly decreased after development of amygdaloid kindling. Intracerebroventricular (i.c.v.) injection of histamine resulted in inhibition of amygdaloid kindled seizures. The H1-agonists 2-methylhistamine and 2-thiazolylethylamine also inhibited amygdaloid kindled seizures. In addition, intraperitoneal (i.p.) injection of histidine and metoprine inhibited amygdaloid kindled seizures at doses that caused increases in histamine contents of the brain. H1-antagonists (diphenhydramine and chlorpheniramine) attenuated histamine- or histidine-induced inhibition of amygdaloid kindled seizures. Both i.c.v. and i.p. injections of H3-antagonists (thioperamide, AQ0145 and clobenpropit) resulted in a dose-related inhibition of amygdaloid kindled seizures. The effects of thioperamide and AQ0145 were inhibited by an H3-agonist (R)-alpha-methylhistamine and H1-antagonists. On the other hand, H2-antagonists showed no antagonistic effect. GABAmimetic drugs, diazepam, sodium valproate and muscimol potentiated the effect of clobenpropit. Bicuculline caused significant antagonism of the inhibition of amygdaloid kindled seizures induced by clobenpropit. These findings suggested that a histaminergic mechanism plays an important role in suppressing amygdaloid kindled seizures through histamine H1-receptors. In addition, an inhibition of amygdaloid kindled seizures induced by histamine is closely related with the action of GABA.

  8. Development and Validation of a Precise and Stability Indicating LC Method for the Determination of Benzalkonium Chloride in Pharmaceutical Formulation Using an Experimental Design

    Directory of Open Access Journals (Sweden)

    Harshal K. Trivedi

    2010-01-01

    Full Text Available A simple, precise, shorter runtime and stability indicating reverse-phase high performance liquid chromatographic method has been developed and validated for the quantification of benzalkonium chloride (BKC preservative in pharmaceutical formulation of sparfloxacin eye drop. The method was successfully applied for determination of benzalkonium chloride in various ophthalmic formulations like latanoprost, timolol, dexametasone, gatifloxacin, norfloxacin, combination of moxifloxacin and dexamethasone, combination of nepthazoline HCl, zinc sulphate and chlorpheniramine maleate, combination of tobaramycin and dexamethasone, combination of phenylephrine HCl, naphazoline HCl, menthol and camphor. The RP-LC separation was achieved on an Purospher Star RP-18e 75 mm × 4.0 mm, 3.0 μ in the isocratic mode using buffer: acetonitrile (35: 65, v/v, as the mobile phase at a flow rate of 1.8 mL/min. The methods were performed at 215 nm; in LC method, quantification was achieved with PDA detection over the concentration range of 50 to 150 μg/mL. The method is effective to separate four homologs with good resolution in presence of excipients, sparfloxacin and degradable compound due to sparfloxacin and BKC within five minutes. The method was validated and the results were compared statistically. They were found to be simple, accurate, precise and specific. The proposed method was validated in terms of specificity, precision, recovery, solution stability, linearity and range. All the validation parameters were within the acceptance range and concordant to ICH guidelines.

  9. Combined use of ionic liquid and hydroxypropyl-β-cyclodextrin for the enantioseparation of ten drugs by capillary electrophoresis.

    Science.gov (United States)

    Cui, Yan; Ma, Xiaowei; Zhao, Min; Jiang, Zhen; Xu, Shuying; Guo, Xingjie

    2013-07-01

    In the present study, hydroxypropyl-β-cyclodextrin and an ionic liquid (1-ethyl-3-methylimidazolium-l-lactate) were used as additives in capillary electrophoresis for the enantioseparation of 10 analytes, including ofloxacin, propranolol hydrochloride, dioxopromethazine hydrochloride, isoprenaline hydrochloride, chlorpheniramine maleate, liarozole, tropicamide, amlodipine benzenesulfonate, brompheniramine maleate, and homatropine methylbromide. The effects of ionic liquid concentrations, salt effect, cations, and anions of ionic liquids on enantioseparation were investigated and the results proved that there was a synergistic effect between hydroxypropyl-β-cyclodextrin and the ionic liquid, and the cationic part of the ionic liquid played an important role in the increased resolution. With the developed dual system, all the enantiomers of 10 analytes were well separated in resolutions of 5.35, 1.76, 1.85, 2.48, 2.88, 1.43, 5.45, 4.35, 2.76, and 2.98, respectively. In addition, the proposed method was applied to the determination of the enantiomeric purity of S-ofloxacin after validation of the method in terms of selectivity, repeatability, linearity range, accuracy, precision, limit of detection (LOD), and limit of quality (LOQ).

  10. 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.

  11. 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.

  12. Molecular pharmacology of antihistamines in inhibition of oxidative burst of professional phagocytes.

    Science.gov (United States)

    Nosáľ, Radomír; Jančinová, Viera; Drábiková, Katarína; Perečko, Tomáš

    2015-04-01

    Antihistamines of the H₁and H₃/H₄groups interfere with oxidative burst of human professional phagocytes in vitro. In the concentration of 10 μM, H₁antihistamines of the 1st and 2nd generation inhibited oxidative burst of human neutrophils in the rank order of potency: dithiaden > loratadine > brompheniramine > chlorpheniramine > pheniramine. Of the H₁antihistamines, the most effective was dithiaden in suppressing oxidative burst of whole human blood and dose-dependently the chemiluminescence of isolated neutrophils at extra- and intracellular level. Inhibition of free oxygen radical generation in isolated neutrophils by dithiaden resulted from the inhibition of protein kinase C activation. The potentiation of recombinant caspase-3 by dithiaden is supportive of the antiinflammatory effect of dithiaden and suggestive of increasing the apoptosis of professional phagocytes. Of the H₃/H₄antihistamines, the most effective was JNJ7777120 in decreasing chemiluminescence in whole blood and also at extra- and intracellular sites of isolated neutrophils. JNJ 10191584 and thioperamide were less effective and the latter significantly potentiated free oxygen radical generation intracellularly. The results demonstrated that, compared with the H₃/H₄antihistamines investigated, H₁antihistamines were much more potent in inhibiting free oxygen radical generation in human professional phagocytes. This finding should be taken into account therapeutically.

  13. Effects of antihistamines on the function of human α7-nicotinic acetylcholine receptors.

    Science.gov (United States)

    Sadek, Bassem; Khanian, Seyedeh Soha; Ashoor, Abrar; Prytkova, Tatiana; Ghattas, Mohammad A; Atatreh, Noor; Nurulain, Syed M; Yang, Keun-Hang Susan; Howarth, Frank Christopher; Oz, Murat

    2015-01-05

    Effects of the histamine H₁ receptor (H1R) antagonists (antihistamines), promethazine (PMZ), orphenadrine (ORP), chlorpheniramine (CLP), pyrilamine (PYR), diphenhydramine (DPH), citerizine (CTZ), and triprolidine (TRP) on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes were investigated. Antihistamines inhibited the α7-nicotinic acetylcholine receptor in the order PYR>CLP>TRP>PMZ>ORP≥DPH≥CTZ. Among the antihistamines, PYR showed the highest reversible inhibition of acetylcholine (100 µM)-induced responses with IC₅₀ of 6.2 µM. PYR-induced inhibition was independent of the membrane potential and could not be reversed by increasing the concentration of acetylcholine. Specific binding of [¹²⁵I] α-bungarotoxin, a selective antagonist for α7-nicotinic acetylcholine receptor, was not changed in the presence of PYR suggesting a non-competitive inhibition of nicotinic receptors. In line with functional experiments, docking studies indicated that PYR can potentially bind allosterically with the α7 transmembrane domain. Our results indicate that the H₂-H₄ receptor antagonists tested in this study (10 µM) showed negligible inhibition of α7-nicotinic acetylcholine receptors. On the other hand, H₁ receptor antagonists inhibited the function of human α7-nicotinic acetylcholine receptor, with varying potencies. These results emphasize the importance of α7-nicotinic acetylcholine receptor for future pharmacological/toxicological profiling.

  14. Combined histamine H1/H2 receptor antagonists: part I. Pharmacological hybrids with pheniramine- and roxatidine-like substructures.

    Science.gov (United States)

    Schulze, F R; Buschauer, A; Schunack, W

    1998-07-01

    A series of hybrid compounds combining the pharmacophores of both pheniramine-type histamine H1 receptor antagonists and roxatidine-type H2 receptor antagonists have been synthesized and tested for histamine antagonism at the isolated ileum (H1) and the spontaneously beating right atrium (H2) of the guinea pig. The 'polar group' of the H2 antagonist moiety (cyanoguanidine, nitroethenediamine or urea) and the side chain amino group of the H1 antagonist portion have been linked by a polymethylene spacer or by a piperazine system. The incorporation of a flexible spacer (2-7 methylene groups) resulted in H1 antagonists achieving up to 2.4 times the activity of pheniramine. Depending on the nature of the polar group the highest H2 antagonist potency resides in compounds with spacers ?2 methylene groups. Nitroethenediamine 24c with a seven-membered chain and a chlorpheniramine substructure proved to be approximately equipotent with pheniramine at the H1 and with ranitidine at the H2 receptor (pKB values 7.82 and 7.1, respectively).

  15. 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.

  16. 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.

  17. 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.

  18. 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

  19. Prejunctional inhibition of sympathetically evoked pupillary dilation in cats by activation of histamine H3 receptors.

    Science.gov (United States)

    Koss, M C; Hey, J A

    1993-08-01

    Frequency-dependent pupillary dilations were evoked by electrical stimulation of the pre- or post-ganglionic cervical sympathetic nerve (sympatho-excitation) or the hypothalamus (parasympatho-inhibition) in sympathectomized anesthetized cats. Systemic administration of the selective histamine H3 receptor agonist (R)-alpha-methylhistamine (R alpha MeHA) produced a dose-dependent depression of mydriasis due to direct neural sympathetic activation but had no effect on responses elicited by parasympathetic withdrawal. The histamine H2 receptor agonist, dimaprit, was inactive. R alpha MeHA was much more effective in depressing sympathetic responses obtained at lower frequencies when compared to higher frequencies of stimulation. Responses evoked both pre- and postganglionically were inhibited by R alpha MeHA. This peripheral sympatho-inhibitory action of R alpha MeHA was antagonized by the histamine H3 receptor blocker thioperamide but not by intravenous pretreatment with the histamine H1 receptor antagonist chlorpheniramine. Histamine H2 receptor blockers cimetidine and ranitidine were also without effect. R alpha MeHA did not depress pupillary responses elicited by i.v. (-)-adrenaline. The results demonstrate that histamine H3 receptors modulate sympathetic activation of the iris at a site proximal to the iris dilator muscle. The predominant mechanism of action appears to the prejunctional inhibition of noradrenaline release from postganglionic sympathetic nerve endings. However, a concomitant ganglionic inhibitory action cannot be excluded.

  20. 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.

  1. 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.

  2. 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.

  3. 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.

  4. 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.

  5. 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

  6. Immunoassay screening of diphenhydramine (Benadryl®) in urine and blood using a newly developed assay.

    Science.gov (United States)

    Rodrigues, Warren C; Castro, Catherine; Catbagan, Philip; Moore, Christine; Wang, Guohong

    2012-03-01

    Diphenhydramine (DPH) is a common over the counter antihistamine that produces drowsiness and has the potential to cause driving under the influence of drugs-related accidents. To date there are no commercially available immunoassay screening kits for its detection in biological fluids such as urine and/or blood. We describe a newly developed enzyme-linked immunosorbent assay (ELISA) screen and report on its utility in the analysis of authentic specimens taken from volunteers. The assay is specific for detection of DPH and does not detect closely related antihistamines like brompheniramine, chlorpheniramine, and doxylamine. There is a varying amount of cross-reactivity seen with certain tricyclic compounds, due to similarities in side chain structure with DPH. Intra- and interday precision of the assay were determined to be less than 10%. The assay is highly sensitive and has a working range from 1 to 500 ng/mL for urine and 1 to 250 ng/mL for blood. The assay was further validated with authentic urine and blood specimens obtained from volunteers and coroner's laboratories.

  7. Chemometrics optimization of six antihistamines separations by capillary electrophoresis with electrochemiluminescence detection.

    Science.gov (United States)

    Zhu, Derong; Li, Xia; Sun, Jinying; You, Tianyan

    2012-01-15

    This work expanded the knowledge of the use of chemometric experimental design in optimizing of six antihistamines separations by capillary electrophoresis with electrochemiluminescence detection. Specially, central composite design was employed for optimizing the three critical electrophoretic variables (Tris-H(3)PO(4) buffer concentration, buffer pH value and separation voltage) using the chromatography resolution statistic function (CRS function) as the response variable. The optimum conditions were established from empirical model: 24.2mM Tris-H(3)PO(4) buffer (pH 2.7) with separation voltage of 15.9 kV. Applying theses conditions, the six antihistamines (carbinoxamine, chlorpheniramine, cyproheptadine, doxylamine, diphenhydramine and ephedrine) could be simultaneous separated in less than 22 min. Our results indicate that the chemometrics optimization method can greatly simplify the optimization procedure for multi-component analysis. The proposed method was also validated for linearity, repeatability and sensitivity, and was successfully applied to determine these antihistamine drugs in urine.

  8. Comparison of chiral recognition capabilities of cyclodextrins for the separation of basic drugs in capillary zone electrophoresis.

    Science.gov (United States)

    Jin, L J; Li, S F

    1998-04-24

    The enantiomeric separation of some racemic anti-histamines and anti-malarials, namely (+/-)-pheniramine, (+/-)-brompheniramine, (+/-)-chlorpheniramine, (+/-)-doxylamine, and (+/-)-chloroquine, was investigated by capillary zone electrophoresis. The enantiomeric separation of five compounds was obtained by addition of approximately 7 mM (1%, w/v) sulfated-beta-cyclodextrin into the buffer as a chiral selector. The effects of sulfated-beta-cyclodextrin concentration and buffer pH on migration and resolution are discussed. Two other cyclodextrins, carboxyethylated-beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin were also investigated. Four of the racemic compounds were resolved using 14 mM (2%, w/v) carboxyethylated-beta-cyclodextrin while 28 mM (4%, w/v) hydroxypropyl-beta-cyclodextrin resolved only two of them. It was found that the type of substituent and the degree of substitution on the rim of the CD structure played an important role in enhancing the chiral recognition. Cyclodextrins with negatively charged substituents and higher degree of substitution on the rim of the structure proved to give better resolution to the cationic racemic compounds compared with cyclodextrin with neutral substituents. This is due to the countercurrent mobility of the negatively charged cyclodextrin relative to the cationic analytes thus allowing for a smaller difference in interaction constants to achieve a successful resolution of enantiomers. Furthermore, lower concentrations of negatively charged cyclodextrins were necessary to achieve the equivalent resolutions as compared with the neutral ones.

  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. Characterization of soy polysaccharide and its in vitro and in vivo evaluation for application in colon drug delivery.

    Science.gov (United States)

    Ursekar, B M; Soni, P S; Date, Abhijit A; Nagarsenker, M S

    2012-09-01

    The objective of the present investigation was to establish potential of commercially available soy polysaccharide (Emcosoy®) for colon drug delivery. The soy polysaccharide-ethyl cellulose films were fabricated and characterized. The effect of the pectinase enzyme on the tensile strength and surface morphology of the film was evaluated. The permeation of chlorpheniramine maleate (CPM), a model hydrophilic drug from pectinase enzyme treated and untreated films was measured in pH 7.4 buffer. The soy polysaccharide-ethyl cellulose films were also incubated with Lactobacillus sp. culture for a specific duration, and effect on the CPM permeation was evaluated. The CPM capsules were coated with the soy polysaccharide-ethyl cellulose mixture, and Eudragit S100 was applied as a secondary coat. The coated CPM capsules were radiolabelled, and their in vivo transit was evaluated in human volunteers on oral administration. The pectinase enzyme had a significant influence on the tensile strength and surface morphology of the soy polysaccharide-ethyl cellulose films. The permeability of pectinase enzyme-treated and Lactobacillus sp.-treated films was significantly higher than that of untreated films. The CPM capsules were coated with the soy polysaccharide-ethyl cellulose mixture and Eudragit S100 and were successfully radiolabelled by a simple method. Gamma scintigraphic studies in human volunteers showed that the radiolabelled capsules maintained integrity for at least 9 h after oral administration. Thus, the soy polysaccharide has a potential in colon drug delivery.

  11. 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.

  12. 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.

  13. Operator care and eco-concerned development of a fast, facile and economical assay for basic nitrogenous drugs based on simplified ion-pair mini-scale extraction using safer solvent combined with drop-based spectrophotometry.

    Science.gov (United States)

    Plianwong, Samarwadee; Sripattanaporn, Areerut; Waewsa-nga, Kwanrutai; Buacheen, Parin; Opanasopit, Praneet; Ngawhirunpat, Tanasait; Rojanarata, Theerasak

    2012-08-30

    A fast, facile, and economical assay for basic nitrogenous drugs has been developed based on the mini-scale extraction of the drug-dye ion pair complex combined with the use of safe-for-analyst and eco-friendlier organic extractant and drop-based micro-spectrophotometry. Instead of using large volume devices, the extraction was simply carried out in typical 1.5 mL microcentrifuge tubes along with the use of micropipettes for accurate transfer of liquids, vortex mixer for efficient partitioning of solutes and benchtop centrifuge for rapid phase separation. In the last step, back-extraction was performed by using the microvolume of acidic solution in order to concentrate the colored species into a confined aqueous microdrop and to keep the analyst away from unwanted contact and inhalation of organic solvents during the quantitation step which was achieved by using cuvetteless UV-vis micro-spectrophotometry without any prior dilutions. Using chlorpheniramine maleate as a representative analyte and n-butyl acetate as a less toxic and non-ozone depleting extractant, the miniaturized method was less laborious and much faster. It was accurate, precise and insensitive to the interferences from common excipients. Notably, it gave the assay results of drug in tablets and oral solution comparable to the large-scale pharmacopeial method while the consumption of organic solvents and the release of wastes were lowered by 200-400 folds.

  14. 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.

  15. 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

  16. Relaxant effect of Pimpinella anisum on isolated guinea pig tracheal chains and its possible mechanism(s).

    Science.gov (United States)

    Boskabady, M H; Ramazani-Assari, M

    2001-01-01

    We have studied the relaxant effect of Pimpinella anisum on isolated guinea pig tracheal chains and its possible mechanism(s). The bronchodilatory effects of aqueous and ethanol extracts and essential oil were examined on precontracted isolated tracheal chains of the guinea pig by 10 microM methacholine in two different conditions including: non-incubated tissues (group 1) and incubated tissues with 1 microM propranolol and 1 microM chlorpheniramine (group 2). In addition, the anticholinergic effects of essential oil and 10 nM atropine were tested by comparing the cumulative log concentration-response curves of methacholine induced contraction of tracheal chains and the effective concentration of methacholine, causing 50% of maximum response (EC(50)) in the presence of essential oil or atropine. Aqueous and ethanol extracts, essential oil and theophylline (1 mM) showed significant relaxant effects compared to those of controls. Although relaxant effect of essential oil was lower than theophylline, there was no significant difference between the effect of aqueous and ethanol extracts and that of theophylline. There was also no significant difference between the relaxant effects obtained in group 1 and 2 experiments. The results also showed parallel rightward shifts of methacholine-response curves and significant increase in EC(50) with the presence of atropine or essential oil. These results indicated bronchodilatory effects of essential oil, aqueous, and ethanol extracts from P. anisum. The results also showed that the relaxant effect of this plant is not due to an inhibitory effect of histamine (H(1)) or stimulatory effect of beta(2)-adrenergic receptors, but due to inhibitory effects on muscarinic receptors.

  17. Antidiabetic properties of the histamine H3 receptor protean agonist proxyfan.

    Science.gov (United States)

    Henry, Melanie B; Zheng, Shuqin; Duan, Chenxia; Patel, Bhuneshwari; Vassileva, Galya; Sondey, Christopher; Lachowicz, Jean; Hwa, Joyce J

    2011-03-01

    Proxyfan is a histamine H3 receptor protean agonist that can produce a spectrum of pharmacological effects including agonist, inverse agonist, and antagonist. We have discovered that proxyfan (10 mg/kg orally) significantly improved glucose excursion after an ip glucose tolerance test in either lean or high-fat/cholesterol diet-induced obese mice. It also reduced plasma glucose levels comparable to that of metformin (300 mg/kg orally) in a nongenetic type 2 diabetes mouse model. The dose-dependent decrease in glucose excursion correlated with inhibition of ex vivo H3 receptor binding in the cerebral cortex. In addition, glucose levels were significantly reduced compared with vehicle-treated mice after intracerebroventricular administration of proxyfan, suggesting the involvement of central H3 receptors. Proxyfan-induced reduction of glucose excursion was not observed in the H3 receptor knockout mice, suggesting that proxyfan mediates this effect through H3 receptors. Proxyfan reduced glucose excursion by significantly increasing plasma insulin levels in a glucose-independent manner. However, no difference in insulin sensitivity was observed in proxyfan-treated mice. The H1 receptor antagonist chlorpheniramine and the H2 receptor antagonist zolantidine had modest effects on glucose excursion, and neither inhibited the glucose excursion reduced by proxyfan. The H3 receptor antagonist/inverse agonist, thioperamide, had weaker effects on glucose excursion compared with proxyfan, whereas the H3 receptor agonist imetit did not affect glucose excursion. In conclusion, these findings demonstrate, for the first time, that manipulation of central histamine H3 receptor by proxyfan can significantly improve glucose excursion by increasing plasma insulin levels via a glucose-independent mechanism.

  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. 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.

  20. 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.

  1. Excitatory effect of histamine on neuronal activity of rat cerebellar fastigial nucleus in vitro

    Institute of Scientific and Technical Information of China (English)

    TANG Biao; ZHANG Jun; LI HongZhao; ZHU JingNing; WANG JianJun

    2007-01-01

    The cerebellar fastigial nucleus (FN) holds an important role in motor control and body balance. Previous studies have revealed that the nucleus is innervated by direct hypothalamocerebellar histaminergic fibers. However, the functional role of histaminergic projection in cerebellar FN has never been established. In this study, we investigated the effect of histamine on neuronal firing of cerebellar FN by using slice preparations. Sixty-five FN cells were recorded from 47 cerebellar slices, and a vast majority of the cells responded to histamine stimulation with an excitatory response (58/65, 89.2%). Perfusing slices with low-Ca2+/high-Mg2+ medium did not block the histamine-induced excitation (n=10), supporting a direct postsynaptic action of histamine on the cells. Furthermore, the excitatory effect of histamine on FN neurons was not blocked by selective histamine H1 receptor antagonist triprolidine (n=15) or chlorpheniramine (n=10), but was effectively suppressed by ranitidine (n=15), a highly selective histamine H2 receptor antagonist. On the other hand, highly selective histamine H2 receptor agonist dimaprit (n=20) instead of histamine H1 receptor agonist 2-pyridylethylamine (n=16) mimicked the excitatory effect of histamine on FN neurons. The dimaprit-induced FN neuronal excitation was effectively antagonized by selective histamine H2 receptor antagonist ranitidine (n=13) but not influenced by selective histamine H1 receptor antagonist triprolidine (n=15). These results demonstrate that histamine excites cerebellar FN cells via the histamine H2 receptor mechanism and suggest that the hypothalamocerebellar histaminergic fibers may modulate cerebellar FN-mediated sensorimotor integration through their excitatory innervations on FN neurons.

  2. 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.

  3. 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.

  4. [Role of serotonin and histamine in the effects of degranulation of mast cells on the colonic motility and the transit. Experimental study in rats].

    Science.gov (United States)

    Castex, N; Fioramonti, J; Fargeas, M J; Bueno, L

    1993-01-01

    The aim of this work was to describe the alterations of colonic motility and transit induced by an experimental, histologically verified, degranulation of mast cells, provoked by the compound BrX-537A, and to determine the role of serotonin and histamine by specific antagonists, in the rat. Colonic myoelectrical activity was inhibited by BrX-537A (2 mg/kg IP) in a biphasic manner. The initial profound inhibition, lasting 30 min, during which the frequency of spike bursts decreased from 9.2 +/- 1.1 to 1.4 +/- 0.5/10 min, was followed by a sustained (5 h) period of moderate inhibition (5.2 +/- 0.5 spike bursts/10 min). In the same way, BrX-537A increased the mean retention time of a marker injected in the proximal colon (10.8 +/- 1.4 h vs 7.4 +/- 0.4 h). Neither serotoninergic nor histaminergic antagonists, at a dose of 1 mg/kg IP, modified the primary drastic inhibition of colonic motility during the first 20 minutes. After, a selective time-related blockade of this inhibition was observed. Granisetron blocked the inhibition from the 30th minute on, methysergide from the 120th minute on, and chlorpheniramine, between the 20th and 60th minutes. In conclusion, the inhibitory effect of mast cell degranulation depends on serotonin and histamine release, in a time-related manner, and implicates the H1, 5-HT3 and 5-HT1 or 2 receptors.

  5. Evaluation of Calendula mucilage as a mucoadhesive and controlled release component in buccal tablets.

    Science.gov (United States)

    Sabale, V; Patel, V; Paranjape, A

    2014-01-01

    Mucoadhesive drug delivery systems were developed to sustain drug delivery via various mucus membranes for either local or systemic delivery of poorly absorbed drugs such as peptides and proteins as well as drugs that are subjected to high first-pass metabolism. The present study was undertaken to use isolated Calendula mucilage as a mucoadhesive agent and to formulate controlled release buccoadhesive tablets with an intention to avoid hepatic first-pass metabolism as well as to enhance residence time of drug in the buccal cavity. The mucilage was isolated from the Calendula petals by aqueous extraction method and characterized for various physiochemical parameters as well as for its adhesive properties. By using direct compression technique, tablets were prepared containing dried mucilage and chlorpheniramine maleate (CPM) as a model drug. Three batches of tablets were prepared and evaluated containing three mucoadhesive components namely Methocel K4M, Carbopol 974P and isolated Calendula mucilage in 16.66%, 33.33 % and 50 % (1:2:3 ratio) resulting in 9 different formulations. FTIR studies between mucilage and CPM suggested the absence of a chemical interaction between CPM and Calendula mucilage. The results of the study showed that the isolated mucilage had good physicochemical and morphological characteristics and tablets conformed to the pharmacopoeial specifications. Also in vitro release studies showed controlled action of drug with increasing the concentration of the isolated Calendula mucilage as a mucoadhesive agent in the formulations. Permeability studies indicated that permeability behavior was not statistically different (P>0.05) by changing the mucoadhesive component. The formulated mucoadhesive tablets for buccal administration containing 75 mg Calendula mucilage showed controlled drug release. Thus, mucoadhesive natural Calendula mucilage based buccal tablets for controlled release were successfully formulated.

  6. Drug release-modulating mechanism of hydrophilic hydroxypropylmethylcellulose matrix tablets: distribution of atoms and carrier and texture analysis.

    Science.gov (United States)

    Park, Jun-Bom; Lim, Jisung; Kang, Chin-Yang; Lee, Beom-Jin

    2013-12-01

    Although release profiles of drug from hydrophilic matrices have been well recognized, the visual distribution of hydroxypropylmethylcellulose (HPMC) and atoms inside of internal structures of hydrophilic HPMC matrices has not been characterized. In this paper, drug release mechanism from HPMC matrix tablet was investigated based on the release behaviors of HPMC, physical properties of gelled HPMC tablet and atomic distributions of formulation components using diverse instruments. A matrix tablet consisting of hydroxypropyl methylcellulose (HPMC 6, 4,000 and 100,000 mPa·s), chlorpheniramine maleate (CPM) as a model and fumed silicon dioxide (Aerosil(®) 200) was prepared via direct compression. The distribution of atoms and HPMC imaging were characterized using scanning electron microscope (SEM)/ energy-dispersive X-ray spectroscopy (EDX), and near-infrared (NIR) analysis, respectively as a function of time. A texture analyzer was also used to characterize the thickness and maintenance of gel layer of HPMC matrix tablet. The HPMC matrix tablets showed Higuchi release kinetics with no lag time against the square root of time. High viscosity grades of HPMC gave retarded release rate because of the greater swelling and gel thickness as characterized by texture analyzer. According to the NIR imaging, low-viscosity-grade HPMC (6 mPa·s) quickly leached out onto the surface of the tablet, while the high-viscosity-grade HPMC (4000 mPa·s) formed much thicker gel layer around the tablet and maintained longer via slow erosion, resulting in retarded drug release. The atomic distribution of the drug (chlorine, carbon, oxygen), HPMC (carbon, oxygen) and silicon dioxide (silica, oxygen) and NIR imaging of HPMC corresponded with the dissolution behaviors of drug as a function of time. The use of imaging and texture analyses could be applicable to explain the release- modulating mechanism of hydrophilic HPMC matrix tablets.

  7. Characterization of hydroxypropylmethylcellulose films using microwave non-destructive testing technique.

    Science.gov (United States)

    Anuar, Nor Khaizan; Wui, Wong Tin; Ghodgaonkar, Deepak K; Taib, Mohd Nasir

    2007-01-17

    The applicability of microwave non-destructive testing (NDT) technique in characterization of matrix property of pharmaceutical films was investigated. Hydroxypropylmethylcellulose and loratadine were selected as model matrix polymer and drug, respectively. Both blank and drug loaded hydroxypropylmethylcellulose films were prepared using the solvent-evaporation method and were conditioned at the relative humidity of 25, 50 and 75% prior to physicochemical characterization using microwave NDT technique as well as ultraviolet spectrophotometry, differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR) techniques. The results indicated that blank hydroxypropylmethylcellulose film exhibited a greater propensity of polymer-polymer interaction at the O-H and C-H domains of the polymer chains upon conditioned at a lower level of relative humidity. In the case of loratadine loaded films, a greater propensity of polymer-polymer and/or drug-polymer interaction via the O-H moiety was mediated in samples conditioned at the lower level of relative humidity, and via the C-H moiety when 50% relative humidity was selected as the condition for sample storage. Apparently, the absorption and transmission characteristics of both blank and drug loaded films for microwave varied with the state of polymer-polymer and/or drug-polymer interaction involving the O-H and C-H moieties. The measurement of microwave NDT test at 8GHz was sensitive to the chemical environment involving O-H moiety while it was greatly governed by the C-H moiety in test conducted at a higher frequency band of microwave. Similar observation was obtained with respect to the profiles of microwave NDT measurements against the state of polymer-polymer and/or drug-polymer interaction of hydroxypropylmethylcellulose films containing chlorpheniramine maleate. The microwave NDT measurement is potentially suitable for use as an apparent indicator of the state of polymer-polymer and drug

  8. 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.

  9. Stimulatory effect of Crocus sativus (saffron) on beta2-adrenoceptors of guinea pig tracheal chains.

    Science.gov (United States)

    Nemati, H; Boskabady, M H; Ahmadzadef Vostakolaei, H

    2008-12-01

    To study the mechanism(s) of the relaxant effects of Crocus sativus (Iridaceae), the stimulatory effect of aqueous-ethanolic extracts of this plant and one of its constituent, safranal was examined on beta-adrenoceptors in tracheal chains of guinea pigs. The beta(2)-adrenergic stimulatory was tested by performing the cumulative concentration-response curves of isoprenaline-induced relaxation of pre-contracted isolated guinea pig tracheal chains. The studied solutions were included two concentrations of aqueous-ethanolic extract from Crocus sativus (0.1 and 0.2g%), safranal (1.25 and 2.5 microg), 10nM propranolol, and saline. The study was done in two different conditions including: non-incubated (group 1, n=9) and incubated tissues with 1 microM chlorpheniramine (group 2, n=6). The results showed clear leftward shifts in isoprenaline curves obtained in the presence of only higher concentration of the extract in group 1 and its both concentrations in group 2 compared with that of saline. The EC(50) (the effective concentration of isoprenaline, causing 50% of maximum response) obtained in the presence of both concentrations of the extract (0.17+/-0.06 and 0.12+/-0.02) and safranal (0.22+/-0.05 and 0.22+/-0.05) in group 1 and only in the presence of two concentrations of the extract (1.16+/-0.31 and 0.68+/-0.21) in group 2 was significantly lower compared to saline (1.00+/-0.22 and 4.06+/-1.04 for groups 1 and 2, respectively) (pCrocus sativus on beta(2)-adrenoceptors which is partially due to its constituent, safranal. A possible inhibitory effect of the plant on histamine (H(1)) receptors was also suggested.

  10. 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.

  11. Activation of histamine H3 receptors produces presynaptic inhibition of neurally evoked cat nictitating membrane responses in vivo.

    Science.gov (United States)

    Koss, M C; Hey, J A

    1992-08-01

    This study was undertaken in order to determine the potential role of prejunctional histamine H3 receptors in an in vivo adrenergic model system. Frequency-dependent nictitating membrane responses were elicited by sympathetic nerve stimulation in anesthetized cats. Systemic administration of the selective histamine H3 receptor agonist, (R)-alpha-methylhistamine (R alpha MeHA) produced a dose-related depression of amplitude of the evoked nictitating membrane responses with a threshold of about 10 micrograms/kg and maximal effect (50% depression at the lowest frequency; 0.5 Hz) seen at 100-300 micrograms/kg. Responses obtained with low frequency stimulation were more sensitive to depression by R alpha MeHA than were responses evoked with higher frequencies of stimulation. Larger doses of R alpha MeHA given to the same animals, failed to produce additional inhibition. R alpha MeHA depressed the amplitude of nictitating membrane responses evoked by either pre- or postganglionic nerve stimulation to an equivalent degree. This depressant action of R alpha MeHA was antagonized by pretreatment with the specific histamine H3 antagonist, thioperamide (3 mg/kg), but not by combined pretreatment with histamine H1 and H2 blockers chlorpheniramine (300 micrograms/kg) and cimetidine (5 mg/kg). Intravenous administration of adrenaline (1-30 micrograms/kg) also produced graded nictitating membrane responses that were not altered by subsequent administration of R alpha MeHA. These results suggest that histamine H3 receptors are involved in the modulation of neurally evoked noradrenaline release in the cat nictitating membrane by an inhibitory presynaptic action.(ABSTRACT TRUNCATED AT 250 WORDS)

  12. 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.

  13. Histamine H1-receptor antagonists against Leishmania (L.) infantum: an in vitro and in vivo evaluation using phosphatidylserine-liposomes.

    Science.gov (United States)

    Pinto, Erika G; da Costa-Silva, Thais A; Tempone, Andre Gustavo

    2014-09-01

    Considering the limited and toxic therapeutic arsenal available for visceral leishmaniasis (VL), the drug repositioning approach could represent a promising tool to the introduction of alternative therapies. Histamine H1-receptor antagonists are drugs belonging to different therapeutic classes, including antiallergics and anxyolitics. In this work, we described for the first time the activity of H1-antagonists against L. (L.) infantum and their potential effectiveness in an experimental hamster model. The evaluation against promastigotes demonstrated that chlorpheniramine, cinnarizine, hydroxyzine, ketotifen, loratadine, quetiapine and risperidone exerted a leishmanicidal effect against promastigotes, with IC50 values in the range of 13-84μM. The antihistaminic drug cinnarizine demonstrated effectiveness against the intracellular amastigotes, with an IC50 value of 21μM. The mammalian cytotoxicity was investigated in NCTC cells, resulting in IC50 values in the range of 57-229μM. Cinnarizine was in vivo studied as a free formulation and entrapped into phosphatidylserine-liposomes. The free drug was administered for eight consecutive days at 50mg/kg by intraperitoneal route (i.p.) and at 100mg/kg by oral route to L. infantum-infected hamsters, but showed lack of effectiveness in both regimens, as detected by real time PCR. The liposomal formulation was administered by i.p. route at 3mg/kg for eight days and reduced the parasite burden to 54% in liver when compared to untreated group; no improvement was observed in the spleen of infected hamsters. Cinnarizine is the first antihistaminic drug with antileishmanial activity and could be used as scaffold for drug design studies for VL.

  14. Multiple H1-antihistamine-induced urticaria.

    Science.gov (United States)

    Inomata, Naoko; Tatewaki, Satoko; Ikezawa, Zenro

    2009-04-01

    H(1)-antihistamines are widely used in the treatment of various allergic diseases. Particularly, a cornerstone of the management of chronic idiopathic urticaria is treatment with H(1)-antihistamines. However, a few cases of H(1)-antihistamine-induced urticaria have been reported. A 34-year-old woman presented with a 4-month history of recurrent urticaria, which was prominently exacerbated by the administration of H(1)-antihistamines. The patient consented to a provocation test of fexofenadine among drugs including cetirizine and hydroxyzine, which were suspected of inducing severe symptoms in episodes. One hour after challenge with 12 mg fexofenadine (one-fifth of the therapeutic dose), a urticarial reaction rapidly developed on nearly the entire body with remarkably increased levels of plasma histamine (190 nmol/L) and plasma leukotriene B4 (150 pg/mL). In challenge tests with other antihistamines, generalized urticaria occurred 5 and 1 h after intake of 10 mg loratadine and 10 mg bepotastine, respectively, whereas challenges with chlorpheniramine, mequitazine and azelastine were all negative. Skin prick tests with H(1)-antihistamines used in the challenges were all negative, indicating that the urticarial reactions after challenges with the causative drugs might not be immunoglobulin E-mediated. Among the causative drugs in our case, cetirizine and hydroxyzine are the piperazine derivatives, whereas fexofenadine, bepotastine, ebastine and loratadine are the piperidine derivatives. The chemical structures of both derivatives are very similar. Therefore, in this case, H(1)-antihistamine-induced urticaria may have been due to cross-reactivity between metabolites of these drugs, but not to drugs before metabolization. Hypersensitivity to H(1)-antihistamines should be considered when urticarial lesions worsen after H(1)-antihistamine treatment.

  15. Deaths due to abuse of dextromethorphan sold over-the-counter in Pakistan

    Directory of Open Access Journals (Sweden)

    Humera Shafi

    2016-09-01

    Full Text Available Dextromethorphan is the most commonly used over-the-counter anti-tussive and expectorant medicine at therapeutic doses. Due to easy availability, euphoric high and hallucinogenic effects at larger doses, dextromethorphan popularity amongst the drug abusers is growing day by day. It is often mixed with alcohol, opiates, cannabinoids or other drugs of abuse for recreational purposes despite their lethal synergistic effects. More than 50 deaths were reported the first time in Pakistan after consuming cough syrups containing dextromethorphan, manufactured by two local pharmaceutical industries. All deceased had the history of drug abuse. We report the deaths of nineteen males, ages ranged from 17 to 45 years, in two major cities of Pakistan who purposefully ingested large doses of dextromethorphan for recreational purposes and died as a result of direct toxic effects of the drug. Toxicological analysis revealed high levels of dextromethorphan ranging from 7.3 to 41.7 mg/L in the peripheral blood, 4.2–92.6 mg/kg in the liver and 9.9–349.6 mg/L in the gastric content by high performance liquid chromatography. The dextromethorphan concentrations in all subjects significantly exceeded the therapeutic range and were consistent with concentrations reported in other cases of dextromethorphan abuse and toxicity. Besides dextromethorphan other drugs of abuse like cannabinoids, opiates, benzodiazepines, ethanol and chlorpheniramine were also detected. The cause of death was determined to be acute dextromethorphan intoxication with lethal synergistic effect of other co-ingested drugs of abuse. The deaths resulted in the prosecution of all individuals involved in manufacturing, distribution or sale of the cough syrup.

  16. Synthesis of SB-β-CD and its application in nonaqueous capillary electrophoresis separation of basic chiral drugs%6-O-磺丁基-β-环糊精的合成及在非水毛细管电泳拆分碱性手性药物中的应用

    Institute of Scientific and Technical Information of China (English)

    邢文国; 孟宪兴; 冯维春; 李继宾; 何海林

    2013-01-01

    A new β-cyclodextrin (β-CD) derivative, SB-β-CD, was successfully synthesized and used as a chiral selector in nonaqueous capillary electrophoresis ( NACE ). The effects of organic solvents, the electrolytes, the concentrations of SB-p-CD and the pH of the buffer were investigated. Four basic chiral drugs, including chlorpheniramine, doxylamine, meclozine, and mianserin, were resolved, while the four basic chiral drugs can not be separated by β-CD under the same conditions. It demonstrated that SB-p-CD as a chiral selector had the special ability in the separation of basic chiral drugs. It was a rapid and accurate method for the separation of basic chiral drugs.%合成了新型环糊精衍生物6-O-磺丁基-β-环糊精(SB-β-CD),并以其作为手性选择剂,对扑尔敏、多西拉敏、美克洛嗪和米安舍林4种碱性手性药物进行非水毛细管电泳拆分.考察了有机溶剂、电解质、手性选择剂浓度以及pH对分离度的影响.研究结果表明:扑尔敏、多西拉敏、美克洛嗪和米安舍林4种碱性手性药物全部达到基线分离.可见SB-β-CD在碱性药物拆分方面具有特殊能力,为碱性手性药物的拆分提供了一种准确、简便的分析方法.

  17. 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.

  18. 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.

  19. 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.

  20. Construction and evaluation of PVC conventional and tubular tripelennamine-selective electrodes: their application in pharmaceutical preparations.

    Science.gov (United States)

    Lima, J L; Montenegro, M C; Sales, M G

    1996-06-01

    The construction and evaluation of tripelennamine conventionally-shaped ion-selective electrodes and tubular detectors for the determination of this compound in pharmaceutical formulations are described. Electrodes with conventional configuration have been constructed without an internal reference solution, using several types of immobilized ionic sensors in PVC. The different electrode membranes were prepared by using tripelennamine tetraphenylborate as ionic-exchanger, dissolved in 2-nitrophenyl octyl ether (type A), dibutylphthalate (type B) and bis-(2-ethylhexyl)sebacate (type C) as plasticizer solvents. The general working characteristics of the different types of conventional electrodes were evaluated in tripelennamine solutions, with adjusted ionic strength, showing a linear response in the concentration range of about 4 x 10(-5) - 1 x 10(-1) M and a slope near the theoretical value. The electrodes presented a fast response (> 20 s) and a high reproducibility (> or = 0.2 mV per day). The electrode selectivity in the presence of some interferents, such as sodium, potassium, lithium, ammonium, chlorpheniramine, diphenydramine, promethazine, meclizine and pentazocine, was good, particularly for those whose sensor membrane was prepared with tripelennamine tetraphenylborate dissolved in 2-nitrophenyl octyl ether (type A). Tubular detectors were also prepared using the same sensor membrane and were evaluated in a low-dispersion flow-injection manifold. Under these conditions the detectors presented response characteristics similar to those of the corresponding conventionally-shaped electrodes. The analysis of different pharmaceutical forms (creams, syrups and gels) gave good results with mean recoveries of 99.8-100.6% when the experiments were conducted by direct potentiometry and 99.9-100.4% where the same determinations were conducted by flow-injection analysis with tubular detectors.

  1. 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.

  2. 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.

  3. 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

  4. Electrochemiluminescence of SDBS-Ru(bpy)2+-CPM System and Its Application%Electrochemiluminescence of SDBS-Ru(bpy)2+-CPM System and Its Application

    Institute of Scientific and Technical Information of China (English)

    李利军; 高文燕; 黄文艺; 蔡卓; 胡大春; 李彦青

    2012-01-01

    When the concentration of dodecyl benzene sulfonic acid sodium salt (SDBS) is 0.7 mmol.L-l, the electrochemical and electrochemiluminescence (ECL) intensity of Ru(bpy)23+ -chlorpheniramine maleate (CPM) system at the Au electrode were studied, The results showed that compared with the absence of SDBS, enhancement of the ECL intensity was 14-fold at Au electrode. Base on this, an ECL method was established for efficient and simple determination of CPM at Au electrode. Under the optimum experimental condition, the enhanced ECL intensities had good linear relationship with the concentration of CPM in the range of 1.0× 10 4--1,0× 10 7 tool.L-I, and a linear regression equation was obtained as follows: I (counts)=48.805×106c+394.03 (r=0.9975), the detection limit for CPM was 1.4~ 10 8 mol.L ~. The RSD for 5 times determinations of 1.0× 10 5 mol.mol·L-1 CPM was 3.2%. The results of recovery test were between 96.3%-102.5%, and the RSD of recovery test (n=5) was 2.7%. In addition, eleven kinds of tertiary amines- Ru(bpy)23+ systems were investigated in the absence and presence of SDBS. The results showed that the enbancement of SDBS on ECL intensity of tertiary amines- Ru(bpy)2+ systems was universal.

  5. [Effect of intracerebroventricular injection of histamine on carotid sinus baroreceptor reflex in anesthetized rats and its mechanism].

    Science.gov (United States)

    Wang, Guo-Qing; Zhou, Xi-Ping; Huang, Wei-Qiu

    2002-12-25

    The changes in carotid sinus baroreceptor reflex (CSR) performance induced by intracerebroventricular injection (i.c.v.) of histamine (HA) were investigated. The effects of pretreatment with HA receptors antagonists into the cerebroventricle or nucleus of solitary tract (NTS) on the responses of CSR to HA were also examined. Intracarotid sinus pressure (ISP)-mean arterial pressure (MAP) relationship curve was constructed by fitting to the logistic function with five parameters in 50 Wistar rats anesthetized with pentobarbital sodium. The left and right carotid sinus regions were isolated from the systemic circulation and the ISP was altered in a stepwise manner. The main results obtained are as follows. (1) i.c.v. injection of HA (100 ng) significantly shifted the ISP-MAP relationship curve upwards and moved the middle part of ISP-Gain relationship curve downwards, and reduced the MAP range and maximum gain (G(max)), but increased the threshold pressure (TP), saturation pressure (SP) and ISP at G(max) (ISP (Gmax)). (2) The pretreatment with H(1) or H(2) receptors antagonist, chlorpheniramine (CHL, 5 microg) or cimetidine (CIM, 15 microg), could obviously diminish the above-mentioned changes in CSR performance induced by HA, but the effect of CIM was less remarkable than that of CHL. (3) The pretreatment with both CHL and CIM (5 microg and 15 microg) at the same time abolished the responses of CSR performance to HA completely. (4) After microinjection of CHL (0.5 microg) or CIM (1.5 microg) into the NTS, the responses of CSR to HA were similar to those after i.c.v. CHL or CIM, but the change in TP was significantly decreased. These findings suggest that the intracerebroventricular administration of HA results in a rapid resetting of CSR and a decrease in reflex sensitivity. The response of CSR to HA might be mediated by both central H(1) and H(2) receptors, especially by H(1) receptors. The effects of the central HA on CSR might be related to a histaminergic

  6. 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.

  7. Selective serotonin reuptake inhibitor exposure.

    Science.gov (United States)

    Fitzgerald, Kevin T; Bronstein, Alvin C

    2013-02-01

    more desirable than other antidepressants. The prognosis in animals that receive treatment is excellent. In one retrospective study, there were no deaths in 313 SSRI-poisoned dogs. No characteristic or classic histopathologic lesions result from SSRI toxicosis. Differential diagnoses for SSRI overdose must include ingestions of other serotonergic medications such as phenylpiperidine opioids (fentanyl and tramadol), mirtazapine, buspirone, amitraz, and chlorpheniramine.

  8. Production by R-alpha-methylhistamine of a histamine H3 receptor-mediated decrease in basal vascular resistance in guinea-pigs.

    Science.gov (United States)

    McLeod, R L; Gertner, S B; Hey, J A

    1993-10-01

    1. The effect of the selective histamine H3 receptor agonist, R-alpha-methylhistamine given intravenously (10-100 micrograms kg-1) was examined on baseline total peripheral resistance (TPR), and cardiovascular haemodynamics in bilaterally vagotomized, anaesthetized guinea-pigs. 2. R-alpha-methylhistamine produced a dose-dependent hypotension and fall in TPR at 30 and 100 micrograms kg-1. A decrease in heart rate (HR) was observed at a dose of 100 micrograms kg-1. R-alpha-methylhistamine (10-100 micrograms kg-1) also produced a dose-dependent fall in rate pressure product (RPP). There was no effect on cardiac output (CO) or stroke volume (SV) at these doses. 3. Histamine H1 and H2 blockade in animals pretreated with a combination of chlorpheniramine (0.3 mg kg-1) and cimetidine (3.0 mg kg-1) did not alter the haemodynamic actions of R-alpha-methyl-histamine (100 micrograms kg-1, i.v.). Pretreatment with the selective H3 antagonist, thioperamide (1 mg kg-1), completely blocked the action of R-alpha-methylhistamine on haemodynamic parameters. 4. To study the mechanism of action of R-alpha-methylhistamine, the vasodilator hydralazine (1 mg kg-1, i.v.) was used. Hydralazine lowered BP, TRP and RPP in guinea-pigs pretreated with ipratropium (50 micrograms kg-1, i.v.). Hydralazine had no effect on HR, SV or CO. 5. R-alpha-methylhistamine (100 micrograms kg-1) did not affect the vasopressor action and increases in TPR produced by adrenaline (1 and 3 micrograms kg-1). On the other hand, the vasodilator hydralazine (1 mg kg-1, i.v.) inhibited the effects of adrenaline (3 micrograms kg-1) on TPR and RPP. The effect of both doses of adrenaline on BP were attenuated by hydralazine. Therefore, the inhibitory effects of R-alpha-methylhistamine are not mediated through a direct action on vascular smooth muscle.6. In adrenalectomized guinea-pigs, R-alpha-methylhistamine (100 microg kg-1) produced a drop in BP and HR.There was no difference between the effects of R

  9. Investigation of endogenous blood plasma phospholipids, cholesterol and glycerides that contribute to matrix effects in bioanalysis by liquid chromatography/mass spectrometry.

    Science.gov (United States)

    Ismaiel, Omnia A; Zhang, Tianyi; Jenkins, Rand G; Karnes, H Thomas

    2010-12-01

    Matrix effects caused by compounds endogenous to the biological sample are a primary challenge in quantitative LC/MS/MS bioanalysis. Many approaches have been developed to minimize matrix effects such as optimization of sample extraction procedures and use of isotopically labeled internal standards. Unexpected matrix components may still remain undetected, however, because of the selective mass transitions monitored during MS/MS analysis. Glycerophosphocholines are the major phospholipids in plasma that have been widely shown to cause significant matrix effects on electrospray ionization efficiencies for target analytes. The purpose of this work was to investigate potential matrix effects resulting from different endogenous lipid classes, including phospholipids, acylglycerols and cholesterols, in order to establish a library for the relative presence of these components in biological sample extracts obtained by commonly used sample preparation techniques. Thirteen compounds were selected which were representatives of eight phospholipids classes, mono, di, triacylglycerols, cholesterol and cholesterol esters. Post-column infusion experiments were carried out to compare relative ion suppression effects of these compounds. Chlorpheniramine and loratadine were selected as model test analytes. A Concentration Normalized Suppression Factor (%CNSF) was defined to allow comparison of ion suppression effects resulting from different endogenous lipids according to their typical concentrations in human plasma and erythrocytes. A simple LC/MS/MS method was developed to monitor these endogenous components in sample extracts and their extraction recoveries from a plasma pool were compared using protein precipitation, liquid-liquid extraction, supported-liquid extraction, solid phase extraction and Hybrid SPE-precipitation methods. Endogenous lipid components other than GPChos, such as cholesterols and triacylglycerols, may result in significant matrix effects and should be

  10. 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

  11. Histamine H3 receptors regulate ACTH release by AtT-20 cel ls%组胺H3受体对垂体瘤AtT-20细胞分泌ACTH的调节作用

    Institute of Scientific and Technical Information of China (English)

    谢建军; 罗晓星; 赵德化

    2001-01-01

    AIM To investigate the signal transduction mechanism of histamine H3 r eceptor. METHODS The adrenocorticotropic hormone (ACTH) levels of supernatants on AtT- 20 cells from the pituitary gland tumor were measured by radioimmunoassa y at the given time after histamine agonists were administrated and the effects o f R-(α)-methylhistamine on the cells proliferation were observed. RES ULTS The H3 receptor specific agonist, R-(α)-methylhistamine incre ased the release of A CT H in time-dependent manner. It increased significantly after administrated r e agents 8 h which reached 1920 μg*L-1 compared to the control group 7 80 μg*L-1 . while the H1 receptor agonist 2-methylhistamine and the H2 agonist impro midine were significantly less potent. Furthermore, this response was blocked by thiop eramide, an H3 receptor specific antagonist, but not by the H1 and H2 anta gonist chlorpheniramine and cimetidine. R-(α)- methylhistamine had no significant i nf luence on cell proliferation within 24 h. Pretreatment with N-ethylmaleimide (N EM ) could abolish the effects of R-(α)-methylhistamine on the release of ACTH. CO NCLUSION Specific activation of H3 receptor could evoke the excitatio n-secreti on coupling process, and G protein might be involved in the signal transdu ction.%目的 观察组胺受体激动剂对AtT-20细胞分泌ACTH的影响,并探讨G蛋 白在组胺H3 受体信号转导机制中的作用. 方法 选用文献报道的高表达组胺H3受体 的垂体细胞瘤AtT-20 作为观察系统,用放免分析法测定给予组胺受体激动剂后各时间点细胞上清液中ACTH分泌量 的变化,并观察药物对细胞增殖的影响. 结果 组胺H3受体激动剂R- (α)- MeHA(0.1 μmol*L-1)作用8 h能明显促进ACTH的释放,释放量为1920 μg * L-1,与同时间对照组(780 μg*L-1)相比,明显增高(P<0.01);H 1和H2激动剂则无此作用. 且R-(α)-MeHA引起ACTH分泌 的效应能被H3受体特异

  12. [Involvement of cross interaction between central cholinergic and histaminergic systems in the nucleus tractus solitarius in regulating carotid sinus baroreceptor reflex].

    Science.gov (United States)

    Hu, Li-Xun; Zhang, Guo-Xing; Zhang, Yu-Ying; Zhao, Hong-Fen; Yu, Kang-Ying; Wang, Guo-Qing

    2013-12-25

    possible modulatory mechanism of preceding microinjection with different histaminergic receptor antagonists, the selective histaminergic H1 receptor antagonist, i.e., chlorpheniramine (CHL) or the H2 receptor antagonist, i.e., cimetidine (CIM) into the NTS on the changes in function of CSR resulted from the i.c.v. cholinesterase inhibitor, physostigmine (PHY) were also examined in order to confirm and to analyze effects of cross interaction between central histaminergic and cholinergic systems on CSR. The main results obtained are as follows. (1) Standalone microinjection of different selective cholinergic receptor antagonists (PRZ, MTR or HEX) or different selective histaminergic receptor antagonists (CHL or CIM) into the NTS with each given dose had no effects on the CSR function and on the basic levels of the artery blood pressure, respectively (P > 0.05). (2) The pretreatment of PRZ or MTR into the NTS with each corresponding dose could attenuate CSR resetting resulted from i.c.v. HA in some degrees, which remarkably moved the posterior half range of ISP-MAP relationship curve downwards (P 0.05). (3) The effects of pretreatment of CHL or CIM into the NTS with each corresponding dose on CSR resetting made by i.c.v. PHY were similar to those of pretreatment of PRZ or MTR into the NTS on CSR resetting resulted from i.c.v. HA, and the decreasing effects of pretreatment with CHL into the NTS on CSR resetting induced by i.c.v. PHY were more remarkable than those with CIM (P < 0.05). These findings suggest that CSR resetting resulted from either HA or PHY into the lateral ventricle may partly involve the descending histaminergic or cholinergic pathway from the hypothalamus to NTS, which might evoke a cross activation of the cholinergic system in the NTS, via cholinergic M1 and M2 receptors mediation, especially the M2 receptors showing actions, or trigger another cross activation of the histaminergic system in the NTS, by histaminergic H1 and H2 receptors mediation

  13. 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

  14. Determination of twelve chemical drugs illegally added in herbal tea by ultra high performance liquid chromatography-tandem mass spectrometry coupled with modified QuEChERS%QuEChERS-超高效液相色谱-串联质谱法快速测定凉茶中非法添加的12种化学药物

    Institute of Scientific and Technical Information of China (English)

    宋宁宁; 张科明; 刘向红; 桑彤; 孙煜; 滕南雁

    2015-01-01

    An ultra high performance liquid chromatography-tandem mass spectrometry method with modified QuEChERS procedure for sample preparation was developed for the simultaneous determination of 12 chemical drugs(chlorpheniramine,piroxicam,α-asarone etc)illegally added in herbal tea. The samples were extracted with acetonitrile,purified with QuEChERS procedure and filtrated by 0. 22 μm microporous filters. The separation was carried on an XBridge BEH C18 column(100 mm×2. 1 mm,3. 5 μm)by a gradient elution using acetonitrile/0. 1%( v/v)formic acid aqueous solution as mobile phases. The analytes were detected by tan-dem mass spectrometry with positive electrospray ionization( ESI+)in multiple reaction moni-toring( MRM)mode,and quantified by external standard calibration method. The correlation coefficients of the standard calibration curves for the 12 analytes were all above 0. 997. The lim-its of detection ranged from 0. 1 μg/L to 2. 1 μg/L,and the limits of quantification ranged from 0. 4 μg/L to 8. 0 μg/L. The average recoveries of the 12 analytes spiked at three levels in blank samples ranged from 62. 7% to 95. 2% with the RSDs from 1. 3% to 10. 8%. The samples bought from markets were screened,and some of the samples showed positive for these analytes. The method developed is easy to operate,sensitive,and with good purification effect. It can be applied to the rapid determination of the 12 chemical drugs illegally added in herbal tea.%建立了凉茶中马来酸氯苯那敏、吡罗昔康、α-细辛脑等12种非法添加的化学药物的 QuEChERS 结合超高效液相色谱-串联质谱( UPLC-MS/MS)的检测方法。样品经乙腈提取,应用 QuEChERS 技术净化,经0.22μm 微孔滤膜过滤后进行 UPLC-MS/MS 测定,以乙腈-0.1%( v/v)乙酸水溶液为流动相梯度洗脱,在 XBridge BEH C18柱(100 mm×2.1 mm,3.5μm)上实现12种化学药物的基线分离。该方法采用多反应监测(MRM)正离子模式扫描