Proconvulsant potential of cyproheptadine in experimental animal models.

Abstract:

:In epileptic patients cyproheptadine is frequently prescribed as an appetite stimulant for the treatment of anorexia associated with anti-epileptic drugs and for the management of 'serotonin syndrome' in depressed epileptic patients. However, the study of serotonergic and histaminergic pathway shows that the decreased neurotransmission of serotonin and histamine in the brain reduces seizures threshold. Since, cyproheptadine interferes with these pathways via antagonizing subtypes of 5-HT(1/2) receptors and H(1) receptor, therefore the present study was undertaken to investigate its effect on seizures threshold, so as to substantiate its use in epileptics. In the present study convulsions were induced in mice by, maximum electroshock (MES), picrotoxin, and pentylenetetrazol (PTZ). Cyproheptadine (4 mg/kg, i.p.) was administered per se and along with clinically used anti-epileptic drugs (phenytoin 25 mg/kg, i.p. and diazepam 5 mg/kg, i.p.) in different groups of mice, onset and extent of convulsions in these groups were compared with that of vehicle control and anti-epileptics per se treated groups. Percentage mortality in all groups was also determined. Results depicted a significant increase in duration of tonic hind limb extension in MES and decrease in latency to clonic convulsions induced by PTZ and picrotoxin in cyproheptadine treated groups (per se and along with anti-epileptics), as compared to vehicle control and anti-epileptics per se treated groups respectively. Percentage mortality was also increased with cyproheptadine treatment. Therefore it is concluded that cyproheptadine pretreatment reduces threshold, increases severity of seizures and decreases the efficacy of clinically used anti-epileptic drugs in experimental animal models of convulsions.

journal_name

Fundam Clin Pharmacol

authors

Singh D,Goel RK

doi

10.1111/j.1472-8206.2009.00797.x

subject

Has Abstract

pub_date

2010-08-01 00:00:00

pages

451-5

issue

4

eissn

0767-3981

issn

1472-8206

pii

FCP797

journal_volume

24

pub_type

杂志文章
  • Effects of SR140333, a selective non-peptide NK1 receptor antagonist, on trigemino-thalamic nociceptive pathways in the rat.

    abstract::Trigeminal stimulation of C-fibers increased c-fos expression within the trigeminal nucleus caudalis (NtV) and thalamic neuronal activity which both reflect the transmission of a nociceptive message. We examined the effects on both these phenomena of the selective NK1 and NK2 receptor antagonists, SR140333 and SR48968...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.1998.tb00929.x

    authors: Michaud JC,Alonso R,Gueudet C,Fournier M,Calassi R,Brelière JC,Le Fur G,Soubrié P

    更新日期:1998-01-01 00:00:00

  • Effects of oxazepam and acetaminophen on cicletanine metabolism in rat hepatocytes and liver microsomes.

    abstract::Cicletanine, a racemic furopyridine derivative synthesized as racemate, is used as an antihypertensive agent. Its two enantiomers are involved in the pharmacological effects of the drug. Cicletanine is metabolized by conjugation enzyme systems (phase II) into sulfoconjugated or glucuroconjugated enantiomers. As oxazep...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.1999.tb00363.x

    authors: Menard C,Lamiable D,Vistelle R,Droy-Lefait MT,Ratanasavanh D

    更新日期:1999-01-01 00:00:00

  • N-Acetyl cysteine does not prevent liver toxicity from chronic low-dose plus subacute high-dose paracetamol exposure in young or old mice.

    abstract::Paracetamol is an analgesic commonly used by people of all ages, which is well documented to cause severe hepatotoxicity with acute overexposures. The risk of hepatotoxicity from nonacute paracetamol exposures is less extensively studied, and this is the exposure most common in older adults. Evidence on the effectiven...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12184

    authors: Kane AE,Huizer-Pajkos A,Mach J,McKenzie C,Mitchell SJ,de Cabo R,Jones B,Cogger V,Le Couteur DG,Hilmer SN

    更新日期:2016-06-01 00:00:00

  • A nonpeptide vasopressin V(1a) receptor antagonist, SR 49059, does not prevent cisplatin-induced emesis in piglets.

    abstract::We determined the pharmacological and the antiemetic properties of SR 49059, a selective nonpeptide V(1a) receptor antagonist, on cisplatin-induced emesis in the piglet. Firstly, we clearly demonstrate that SR 49059 is a potent V(1a) receptor antagonist in vitro and in vivo in the piglet. In binding studies, [3H]-SR 4...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1472-8206.2001.00027.x

    authors: Grélot L,Girod V,Dapzol J,Maffrand JP,Serradeil-Le Gal C

    更新日期:2001-06-01 00:00:00

  • Beraprost sodium-fluindione combination in healthy subjects: pharmacokinetic and pharmacodynamic aspects.

    abstract::Beraprost sodium (BPS), an orally active PGI2 (prostaglandine 12) analogue possesses vasodilatating and platelet aggregation inhibiting properties. It is being developed in peripheral arterial occlusive disease. As in future clinical practice BPS might be co-prescribed with oral anticoagulants, we investigated its int...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1472-8206.2000.tb00021.x

    authors: Warot D,Berlin I,Aymard G,Ankri A,Fabry C,Besse B,Lechat P,Diquet B

    更新日期:2000-05-01 00:00:00

  • Factitious increases in serum testosterone concentrations related to phenylbutazone therapy.

    abstract::We report 6 additional observations of a drug/hormone assay interaction between serum testosterone and phenylbutazone intake. This interaction had been described previously only once. We discuss its potential mechanisms, based upon our experimental findings, and its clinical implications. ...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2007.00564.x

    authors: Uzzan B,Dumont-Fischer D,Lahlou N,Bihan H,Boissier MC,Alvarez JC,Perret GY,Cohen R

    更新日期:2008-04-01 00:00:00

  • Study of in vitro glucuronidation of hydroxyquinolines with bovine liver microsomes.

    abstract::Glucuronidation of drugs by UDP-glucuronosyltransferase (UGT) is a major phase II conjugation reaction. Defects in UGT are associated with Crigler-Najjar syndrome and Gilbert's syndrome with severe hyperbilirubinaemias and jaundice. We analysed the reactivities of some hydroxyquinoline derivatives, which are naturally...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1472-8206.2002.00097.x

    authors: Kanou M,Saeki K,Kato TA,Takahashi K,Mizutani T

    更新日期:2002-12-01 00:00:00

  • Surrogate endpoints in randomized cardiovascular clinical trials.

    abstract::Surrogate endpoints predict the occurrence and timing of a clinical endpoint of interest (CEI). Substitution of a surrogate endpoint for a CEI can dramatically reduce the time and cost necessary to complete a Phase III clinical trial. However, assurance that use of a surrogate endpoint will result in a correct conclus...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.2010.00865.x

    authors: Domanski M,Pocock S,Bernaud C,Borer J,Geller N,Revkin J,Zannad F

    更新日期:2011-08-01 00:00:00

  • Incidence of hospital admissions due to adverse drug reactions in France: the EMIR study.

    abstract::To assess the incidence of hospital admissions related to adverse drug reactions (ADRs) in France and the frequency of preventable ADRs in France, a prospective study was conducted among a representative randomly selected sample of medical wards in public hospitals between December 2006 and June 2007; all patients adm...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12088

    authors: Bénard-Laribière A,Miremont-Salamé G,Pérault-Pochat MC,Noize P,Haramburu F,EMIR Study Group on behalf of the French network of pharmacovigilance centres.

    更新日期:2015-02-01 00:00:00

  • Electrophysiology of ion channels of the heart.

    abstract::The contribution of Na+, Ca2+, and various K+ currents to the shape of the cardiac action potential is outlined based on the relation between electrophysiological properties and structure of channel molecules. These currents have also been found in human ventricular myocytes, where the most prominent K+ current is a t...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.1996.tb00582.x

    authors: Ravens U,Wettwer E,Ohler A,Amos GJ,Mewes T

    更新日期:1996-01-01 00:00:00

  • The mechanisms of vasorelaxant effect of leptin on isolated rabbit aorta.

    abstract::In the present study, we analysed the effects of leptin on rabbit aorta and the mechanisms underlying these effects. Leptin (10(-12)-10(-9) m) induced concentration-dependent relaxation in intact rabbit aorta rings precontracted with phenylephrine (10(-6) m). Removal of endothelium abolished the effects of leptin. Pre...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2007.00541.x

    authors: Sahin AS,Bariskaner H

    更新日期:2007-12-01 00:00:00

  • Systemic, regional and cerebral hemodynamic effects of a new angiotensin converting enzyme inhibitor, imidapril, in healthy volunteers.

    abstract::The effects of two single oral doses (5 mg and 20 mg) of a new angiotensin I-converting enzyme inhibitor, imidapril, on a) systemic hemodynamics (arterial pressure, heart rate, cardiac output), b) brachial and common carotid arteries' hemodynamics (diameter and blood flow, pulsed Doppler technique), c) cerebral hemody...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1472-8206.1994.tb00783.x

    authors: Démolis P,Annane D,Duhazé P,Giudicelli JF

    更新日期:1994-01-01 00:00:00

  • Discrepancies in pharmacokinetic analysis results obtained by using two standard population pharmacokinetics software programs.

    abstract::Multiple standard software packages for population pharmacokinetics (PK) modeling are currently available. These programs may significantly vary in the algorithms used for modeling plasma concentrations as a function of time course. We compared the population PK parameters obtained by using two standard software packa...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2008.00641.x

    authors: Finkelstein Y,Nava-Ocampo AA,Schechter T,Grant R,St Pierre E,Goldman R,Walker S,Koren G

    更新日期:2009-02-01 00:00:00

  • KATP channels modulate GABA release in hippocampal slices in the absence of glucose.

    abstract::We studied the effects of KATP channel blockers on [3H]GABA release in the absence of glucose in rat hippocampal slices. The omission of glucose induced a marked increase in the efflux of [3H]GABA, which was antagonized by TTX (1 microM), but not by MK 801 (1 microM) or DNQX (100 microM). Glibenclamide (10-100 microM)...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.1992.tb00123.x

    authors: Margaill I,Miquet JM,Doble A,Blanchard JC,Boireau A

    更新日期:1992-01-01 00:00:00

  • Sulforaphane protects SK-N-SH cells against antipsychotic-induced oxidative stress.

    abstract::Adverse reactions to antipsychotic drugs (APs) have been attributed to oxidative stress. Sulforaphane (SF) is a potent antioxidant that protects against dopaminergic cell death. We examined the protective properties of SF against AP-induced oxidative stress in dopaminergic neuroblastoma cells. Human neuroblastoma SK-N...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2011.00988.x

    authors: Mas S,Gassó P,Trias G,Bernardo M,Lafuente A

    更新日期:2012-12-01 00:00:00

  • Erythropoietin and myocardial protection: what's new?

    abstract::Erythropoietin (EPO), the principal hematopoietic cytokine produced by the kidney and the liver in fetuses, regulates mammalian erythropoiesis and exhibits diverse cellular effects in non-hematopoietic tissues. The introduction of recombinant human EPO (rhEPO) has marked a significant advance in the management of anem...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.2005.00347.x

    authors: Joyeux-Faure M,Godin-Ribuot D,Ribuot C

    更新日期:2005-08-01 00:00:00

  • Enhancement on reactive oxygen species and COX-1 mRNA levels modulate the vascular relaxation induced by sodium nitroprusside in denuded mice aorta.

    abstract::This study aimed to investigate the modulation of nitric oxide/reactive oxygen species in sodium nitroprusside relaxation in mice aorta. Sodium nitroprusside induced relaxation in endothelium-intact (e+) and endothelium-denuded (e-) aortas with greater potency in e+ than in e-. The nitric oxide synthase inhibitor did ...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12103

    authors: Kangussu LM,Olivon VC,Arifa RD,Araújo N,Reis D,Assis MT,Soriani FM,de Souza Dda G,Bendhack LM,Bonaventura D

    更新日期:2015-04-01 00:00:00

  • Controlled ingestion of kaolinite (5%) modulates enteric nitrergic innervation in rats.

    abstract::We have previously shown that kaolinite slowed down gastric emptying and intestinal transit and induced changes in enteric mechanical activities. As gastric emptying and intestinal transit have been shown to be regulated by nitric oxide (NO), the effect of an imposed ingestion of kaolinite on enteric nitrergic innerva...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12040

    authors: Voinot F,Fischer C,Schmidt C,Ehret-Sabatier L,Angel F

    更新日期:2014-08-01 00:00:00

  • Spontaneous adverse event notifications by patients subsequent to the marketing of a new formulation of Levothyrox® amidst a drug media crisis: atypical profile as compared with other drugs.

    abstract::Since patients may report spontaneously adverse events associated with their medications, such notifications are constantly on the rise. In 2017, an unexpected rise of notifications associated with the marketing of a new formula of Levothyrox, differing from the 30-year-old drug only by minor elements, occurred in Fra...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12446

    authors: Viard D,Parassol-Girard N,Romani S,Van Obberghen E,Rocher F,Berriri S,Drici MD

    更新日期:2019-08-01 00:00:00

  • Differential sensitivities of pyrogenic chemokine fevers to CC chemokine receptor 5 antibodies.

    abstract::Macrophage inflammatory protein (MIP)-1beta and RANTES (regulated on activation, normal T-cells expressed and secreted) are members of the CC-family of chemokines. Although these two peptides are structurally and functionally related to one another, each exhibits distinct features, which allows it to independently reg...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2003.00227.x

    authors: Tavares E,Miñano FJ

    更新日期:2004-04-01 00:00:00

  • Pharmacology and drug development in rare diseases: the attractiveness and expertise of the French medical pharmacology.

    abstract::Developing drugs for rare disease can be challenging due to specific rare disease characteristics. The French Medical Pharmacology is structured and positioned to play a major role in orphan drug research and development due to the required expertise concentrated into pharmacology departments, exclusively implemented ...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/fcp.12314

    authors: Micallef J,Boutouyrie P,Blin O

    更新日期:2017-12-01 00:00:00

  • Extracting numerical data from published reports of pharmacokinetics investigations: method description and validation.

    abstract::A method has been proposed for extracting numerical data when only graphical results are presented. Reports with both graphical and tabular data were identified and the graphs were electronically scanned. The coordinates of each point were read using the cross-hair facility of Adobe Photoshop 7.0. To improve the preci...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1472-8206.2003.00180.x

    authors: de Oliveira IR,Santos-Jesus R,Po AL,Poolsup N

    更新日期:2003-08-01 00:00:00

  • Prevention of CCL4-induced liver cirrhosis by silymarin.

    abstract::The efficacy of silymarin treatment in preventing biochemical and histological alterations in CCL4-induced liver cirrhosis in rats was studied. Four groups of rats were treated with: (1) CCL4; (2) mineral oil; (3) CCL4 + silymarin; and (4) silymarin. All animals were sacrificed 72 h after the end of treatments. The ac...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.1989.tb00449.x

    authors: Mourelle M,Muriel P,Favari L,Franco T

    更新日期:1989-01-01 00:00:00

  • Microparticles from apoptotic monocytes enhance nitrosative stress in human endothelial cells.

    abstract::Microparticles are membrane vesicles with procoagulant and proinflammatory properties released during cell activation or apoptosis. Microparticles from monocytes have been implicated in atherosclerosis and vascular inflammation, but their direct effects on endothelial cells are not completely elucidated. The present s...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.2010.00898.x

    authors: Mastronardi ML,Mostefai HA,Soleti R,Agouni A,Martínez MC,Andriantsitohaina R

    更新日期:2011-12-01 00:00:00

  • Clinical effects and outcomes with new P2Y12 inhibitors in ACS.

    abstract::Thienopyridines have become the cornerstone of treatment for percutaneous coronary intervention although no survival benefit has ever been shown with clopidogrel despite increasing loading doses. Newly developed P2Y12 inhibitors are more potent, more predictable, and have a faster onset of action than clopidogrel, cha...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.2011.00984.x

    authors: Collet JP,O'Connor S

    更新日期:2012-02-01 00:00:00

  • Plasma antioxidative activity during atorvastatin and fluvastatin therapy used in coronary heart disease primary prevention.

    abstract::We estimated the effect of atorvastatin and fluvastatin on plasma antioxidative activity used in coronary heart disease (CHD) primary prevention. Anti-oxidative activity of blood plasma was determined by Bartosz et al. method [Curr. Top. Biophys. (1998)22:11-13], based on reduction of preformed cation radical of 2,2,a...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.0767-3981.2003.00208.x

    authors: Kowalski J,Pawlicki L,Grycewicz J,Błaszczyk J,Irzmański R,Cegliński T,Kowalczyk E

    更新日期:2004-02-01 00:00:00

  • Plasma iron status and lipid peroxidation following thrombolytic therapy for acute myocardial infarction.

    abstract::Free radical species have been implicated as important agents involved in myocardial ischemic and reperfusion injuries. Superoxide is capable of mobilizing iron from ferritin and the released iron can cause hydroxyl formation from H2O2. The aim of this study was to evaluate the time-dependent increase in lipid peroxid...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1472-8206.1998.tb00947.x

    authors: Cottin Y,Doise JM,Maupoil V,Tannière-Zeller M,Dalloz F,Maynadié M,Walker MK,Louis P,Carli PM,Wolf JE,Rochette L

    更新日期:1998-01-01 00:00:00

  • Experimental models of torsades de pointes.

    abstract::Torsades de pointes is the most typical ventricular tachycardia involving QT-interval prolongation. It is a rather unusual but potentially lethal ventricular tachycardia with a distinctive morphology favored by bradycardia, antiarrhythmic drugs and hypokalemia and requires specific treatment. Torsades de pointes has b...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.1993.tb00215.x

    authors: Weissenburger J,Davy JM,Chézalviel F

    更新日期:1993-01-01 00:00:00

  • Effects of calcium entry blockers on blood pressure and heart rate in neurogenic hypertensive dogs.

    abstract::The hypotensive and negative chronotropic effects of 5 calcium entry blockers (verapamil 200 micrograms/kg IV; diltiazem 300 micrograms/kg IV; nifedipine 5 micrograms/kg IV; nicardipine 50 micrograms/kg IV; and bepridil 5 mg/kg IV) were compared in control normotensive and acute neurogenic hypertensive anaesthetized d...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1472-8206.1987.tb00548.x

    authors: Montastruc P,Valet P,Dang Tran L,Gaillard G,Montastruc JL

    更新日期:1987-01-01 00:00:00

  • Dopaminergic and non-dopaminergic pharmacological hypotheses for gait disorders in Parkinson's disease.

    abstract::Gait disorders form one component of the axial disorders observed in Parkinson's disease (PD). Indeed, short steps with a forward-leaning stance are diagnostic criteria for PD in the early stages of the condition. Gait disorders also represent a major source of therapeutic failure in the advanced stages of PD (with th...

    journal_title:Fundamental & clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1472-8206.2009.00798.x

    authors: Devos D,Defebvre L,Bordet R

    更新日期:2010-08-01 00:00:00