Vigabatrin-induced decrease in serum phenytoin concentration does not involve a change in phenytoin bioavailability.

Abstract:

:The possibility that vigabatrin (VGB) decreases serum phenytoin (PHT) concentration by lowering the oral bioavailability of PHT was investigated in 21 patients with epilepsy. Each patient was switched from oral to intravenous PHT for 5 days before and after combined treatment with VGB. After VGB (2-3.5 g day(-1) for at least 5 weeks), serum PHT concentrations decreased slightly from 87 +/- 25 to 76 +/- 31 micromol l(-1) (means +/- s.d., P < 0.05), but in a subgroup of seven patients the decrease was more prominent (from 72 +/- 22 to 49 +/- 17 micromol l(-1), P < 0.005). At baseline (before VGB), serum PHT remained unaffected (85 +/- 30 micromol l(-1)) after switching PHT dosage to the intravenous route, indicating that the oral availability of the drug was virtually complete. During VGB treatment, serum PHT was also unchanged (74 +/- 34 micromol l(-1)) after switching from oral to intravenous therapy, and this was also true for the subgroup of patients showing a prominent interaction (48 +/- 18 micromol l(-1)). The urinary recoveries of PHT and its metabolites pHPPH and mHPPH remained constant throughout the study. It is concluded that the oral availability of PHT is unaffected by VGB and that the VBG-induced decrease in serum PHT is mediated by alternative mechanisms.

journal_name

Br J Clin Pharmacol

authors

Gatti G,Bartoli A,Marchiselli R,Michelucci R,Tassinari CA,Pisani F,Zaccara G,Timmings P,Richens A,Perucca E

doi

10.1111/j.1365-2125.1993.tb00422.x

keywords:

subject

Has Abstract

pub_date

1993-12-01 00:00:00

pages

603-6

issue

6

eissn

0306-5251

issn

1365-2125

journal_volume

36

pub_type

杂志文章
  • A double-blind crossover comparison of pindolol, metoprolol, atenolol and labetalol in mild to moderate hypertension.

    abstract::1 This study was designed to compare in a double-blind randomized crossover trial, atenolol, labetalol, metoprolol and pindolol. Considerable differences in dose (atenolol 138 +/- 13 mg daily; labetalol 308 +/- 34 mg daily; metoprolol 234 +/- 22 mg daily; and pindolol 24 +/-2 mg daily were required to produce similar ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1979.tb04774.x

    authors: McNeil JJ,Louis WJ

    更新日期:1979-04-01 00:00:00

  • The pharmacodynamics of single doses of prorenoate potasssium and spironolactone in fludrocortisone treated normal subjects.

    abstract::1 The pharmacodynamic profile of single oral doses of prorenoate potassium (40 mg) and spironolactone (100 mg), as judged by reversal of the effects of fludrocostisone on the urinary electrolyte composition, was compared to that of placebo in a double-blind crossover study in six healthy subjects. 2 Both drugs showed ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1976.tb00624.x

    authors: Ramsay LE,Shelton JR,Tidd MJ

    更新日期:1976-06-01 00:00:00

  • Towards a better use of scientific advice for developers of advanced therapies.

    abstract::Scientific advice (SA) is an important tool offered by regulators to help developers generate robust evidence on a medicine's benefits and risks. Drawing on accumulated experience and looking at the SA provided by the European Medicines Agency in 2018 to advanced therapy medicinal products originally developed by publ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.14672

    authors: Tavridou A,Rogers D,Bonelli M,Schiel A,Hidalgo-Simon A

    更新日期:2020-11-25 00:00:00

  • Prazosin disposition in young and elderly subjects.

    abstract::1 The disposition of prazosin following oral and intravenous administration has been studied in seven young and seven elderly men, all of whom were in good health and living independently in the community. 2 The elimination half-life (min) of prazosin was 123 +/- 19.4 (s.d.) in the young and 194 +/- 36 in the elderly ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1981.tb01234.x

    authors: Rubin PC,Scott PJ,Reid JL

    更新日期:1981-09-01 00:00:00

  • Effect of indomethacin on the pharmacokinetics and pharmacodynamics of felodipine.

    abstract::1. We studied the effects of pre-treatment with oral indomethacin (25 mg four times daily for 3 days) on the pharmacokinetics, haemodynamics and diuretic properties of oral felodipine (10 mg single dose) in 12 healthy male volunteers using a placebo controlled double-blind four-way crossover protocol. 2. Felodipine wi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1988.tb05295.x

    authors: Hardy BG,Bartle WR,Myers M,Bailey DG,Edgar B

    更新日期:1988-11-01 00:00:00

  • The induction effect of rifampicin on activity of mephenytoin 4'-hydroxylase related to M1 mutation of CYP2C19 and gene dose.

    abstract:AIMS:To determine the induction effect of rifampicin on the activity of 4'-hydroxylase in poor metabolizers (PMs) with m1 mutation of S-mephenytoin 4'-hydroxylation and the relationship of the effect with gene dose. METHODS:Seven extensive metabolizers (EMs) of S-mephenytoin 4'-hydroxylation and five PMs with m1 mutat...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.1998.00643.x

    authors: Feng HJ,Huang SL,Wang W,Zhou HH

    更新日期:1998-01-01 00:00:00

  • Assessment of endothelial function: comparison of the pulse wave response to beta 2-adrenoceptor stimulation with flow mediated dilatation.

    abstract:AIMS:To assess the reproducibility of the digital pulse wave response to beta(2)-adrenoreceptor stimulation and to determine if an attenuated response to beta(2)-adrenoceptor stimulation is associated with impaired flow mediated dilatation (FMD). METHODS:Subjects (n = 20) with endothelial dysfunction (ED), were compar...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2007.03006.x

    authors: Rambaran C,Jiang B,Ritter JM,Shah A,Kalra L,Chowienczyk PJ

    更新日期:2008-02-01 00:00:00

  • Inhibition of vasoconstriction by AJ-2615, a novel calcium antagonist with alpha(1)-adrenergic receptor blocking activity in human conduit arteries used as bypass grafts.

    abstract:AIMS:Graft spasm may develop during coronary artery bypass grafting and reversal of spasm is still challenging. The purpose of this study was to investigate the in vitro vascular relaxant properties of AJ-2615 in human internal mammary artery (IMA). METHODS:We studied 264 IMA rings taken from 65 patients undergoing co...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.0306-5251.2001.01444.x

    authors: Liu MH,Floten SH,Yang Q,He GW

    更新日期:2001-09-01 00:00:00

  • The effect of isoxicam on neutrophil and monocyte function.

    abstract::1 Isoxicam was found to inhibit monocyte and neutrophil cell chemotaxis at therapeutic concentrations. 2 The effect was observed after in vitro incubation of normal cells and in vivo in patients with rheumatoid arthritis. 3 Compared to other NSAIDs studied in our laboratory, isoxicam was shown to have a broader spectr...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1986.tb02991.x

    authors: Martinez JG,Murakami SI,Scheinberg MA

    更新日期:1986-01-01 00:00:00

  • Antidepressant use and risk of coronary heart disease: meta-analysis of observational studies.

    abstract:AIMS:Our goal was to evaluate the association between antidepressant use and the risk of coronary heart disease (CHD) among subjects with no history of coronary heart disease. METHODS:A search of Medline, EMBASE, PsycINFO and the Cochrane Library was performed in January 2013. Two authors independently reviewed and se...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/bcp.12383

    authors: Oh SW,Kim J,Myung SK,Hwang SS,Yoon DH

    更新日期:2014-10-01 00:00:00

  • Comparative efficacy and tolerability of anti-epileptic drugs for refractory focal epilepsy: systematic review and network meta-analysis reveals the need for long term comparator trials.

    abstract:AIMS:To evaluate the comparative efficacy (50% reduction in seizure frequency) and tolerability (premature withdrawal due to adverse events) of anti-epileptic drugs (AEDs) for refractory epilepsy. METHODS:We searched Cochrane Central Register of Controlled Trials (Cochrane Library 2009, issue 2) including Epilepsy Gro...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究,评审

    doi:10.1111/bcp.12083

    authors: Bodalia PN,Grosso AM,Sofat R,Macallister RJ,Smeeth L,Dhillon S,Casas JP,Wonderling D,Hingorani AD

    更新日期:2013-11-01 00:00:00

  • The disposition of amodiaquine in man after oral administration.

    abstract::A method is described for the simultaneous determination of amodiaquine (AQ) and desethylamodiaquine (AQm) in plasma, urine, whole blood and packed red cells. After oral administration of AQ (600 mg) to seven healthy subjects, absorption of AQ was rapid, reaching peak concentrations in plasma, whole blood, and packed ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1987.tb03002.x

    authors: Winstanley P,Edwards G,Orme M,Breckenridge A

    更新日期:1987-01-01 00:00:00

  • Contrasting effects of fluconazole and ketoconazole on phenytoin and testosterone disposition in man.

    abstract::Nine healthy male subjects received oral fluconazole 400 mg daily, ketoconazole 200 mg twice daily or no treatment for 6 days according to a randomized, cross-over design. A single 250 mg oral dose of phenytoin suspension was administered on day 5 and serum phenytoin concentrations were measured over the following 48 ...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1992.tb04111.x

    authors: Touchette MA,Chandrasekar PH,Milad MA,Edwards DJ

    更新日期:1992-07-01 00:00:00

  • Acute management of severe hypertension with oral labetalol.

    abstract::1 Six previously untreated emergency admissions to hospital with severe hypertension were given oral treatment with labetalol. 2 Pre-treatment diastolic BP exceeded 130 mmHg, and clinical evidence of either accelerated hypertension or encephalopathy was present. 3 Hypotensive response after treatment followed two patt...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Ghose RR

    更新日期:1979-01-01 00:00:00

  • L-643.441: an H2-receptor antagonist with potent and long-lasting effects in man.

    abstract::Submaximal dose pentagastrin tests conducted in normal male volunteers with L-643.441, a novel histamine H2-receptor antagonist, indicate that it is a potent and long-acting inhibitor of gastric acid secretion. The effect appears dose-dependent and single doses of 50 mg are sufficient to reduce secretory potential by ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1985.tb05043.x

    authors: Henry DA,Somerville KW,Kitchingman GK,Holmes IB,Tobert JA,Langman MJ

    更新日期:1985-08-01 00:00:00

  • Inhaled histamine increases the rate of absorption of sodium cromoglycate from the lung.

    abstract::Since many factors may alter lung epithelial permeability (LEP) to water soluble molecules, the effect of histamine on the absorption and clearance of inhaled sodium cromoglycate was examined in seven mildly asthmatic patients with hyperresponsive airways and eight normal subjects. The subjects underwent histamine cha...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1992.tb04048.x

    authors: Richards R,Fowler C,Simpson S,Renwick AG,Holgate ST

    更新日期:1992-03-01 00:00:00

  • Comparison of the acute vascular effects of frusemide and bumetanide.

    abstract::The acute peripheral vascular and diuretic effects of intravenous frusemide 10 mg and 20 mg were compared with those of bumetanide 250 micrograms and 500 micrograms in a group of 10 salt depleted volunteers. Significant reductions in forearm blood flow (FBF) were observed after frusemide 10 mg (-0.77 ml 100 ml-1 min-1...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1986.tb05207.x

    authors: Johnston GD,Nicholls DP,Kondowe GB,Finch MB

    更新日期:1986-04-01 00:00:00

  • Morphine-like insomnia from heroin in nondependent human addicts.

    abstract::1 This study was performed because dose-related effects of heroin on human sleep had not been described previously, and to discover if heroin produces a morphine-like insomnia. 2 After three adaptation nights, the sleep of seven male nondependent opiate addicts was studied following i.m. doses of heroin (3, 6, 12 mg/7...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1981.tb01120.x

    authors: Kay DC,Pickworth WB,Neider GL

    更新日期:1981-02-01 00:00:00

  • Clinical and pharmacological study of a novel controlled release preparation of salbutamol.

    abstract::This study compared the efficacy of 8 mg controlled release (CR) salbutamol tablets twice daily with standard 4 mg salbutamol tablets four times daily in patients with chronic obstructive airways disease. There was significant bronchodilation in both treatment groups as measured by standard spirometry (P less than 0.0...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1990.tb03683.x

    authors: Milroy R,Carter R,Carlyle D,Boyd G

    更新日期:1990-05-01 00:00:00

  • Effects of the 5-HT3 antagonist cilansetron vs placebo on phasic sigmoid colonic motility in healthy man: a double-blind crossover trial.

    abstract:AIMS:5-hydroxytryptamine3 receptor antagonists act antiemetically and slow colonic transit. This study evaluated effects of the high-affinity 5-HT3 antagonist, cilansetron, on fasting, meal-and anticholinesterase-stimulated phasic contractile activity of the human sigmoid colon as well as on bowel habits and stool cons...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1046/j.1365-2125.2000.00180.x

    authors: Stacher G,Weber U,Stacher-Janotta G,Bauer P,Huber K,Holzäpfel A,Krause G,Steinborn C

    更新日期:2000-05-01 00:00:00

  • The impact of new insights and revised practice guidelines on prescribing drugs in the treatment of Type 2 diabetes mellitus.

    abstract:AIMS:The aim of this study was to investigate the impact of new insights and revised guidelines on initial and follow-up treatment with antihyperglycaemic drugs over the period 1998-2003. METHODS:The InterAction Database (IADB), which contains pharmacy dispensing data from 53 community pharmacies in the Northern and E...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2006.02711.x

    authors: Lub R,Denig P,van den Berg PB,Hoogenberg K,de Jong-van den Berg LT

    更新日期:2006-12-01 00:00:00

  • Drug-induced liver injury: results from the hospital-based Berlin Case-Control Surveillance Study.

    abstract:AIM:Drug-induced liver injury (DILI) is often responsible for acute liver failure, drug withdrawal, boxed warnings or drug non-approval. Therefore, we conducted a case-control study to determine the hepatotoxic risk of a wide range of drugs. METHODS:The Berlin Case-Control Surveillance Study FAKOS included all 51 Berl...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.12565

    authors: Douros A,Bronder E,Andersohn F,Klimpel A,Thomae M,Sarganas G,Kreutz R,Garbe E

    更新日期:2015-06-01 00:00:00

  • Growth factors for diabetic foot ulcers: mixed treatment comparison analysis of randomized clinical trials.

    abstract:AIMS:Topical growth factors accelerate wound healing in patients with diabetic foot ulcers (DFU). Due to the absence of head-to-head comparisons, we carried out Bayesian network meta-analysis to compare the efficacy and safety of growth factors. METHODS:Using an appropriate search strategy, randomized controlled trial...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1111/bcp.13470

    authors: Sridharan K,Sivaramakrishnan G

    更新日期:2018-03-01 00:00:00

  • Development of anti-migraine therapeutics using the capsaicin-induced dermal blood flow model.

    abstract::The efficacy of calcitonin gene-related peptide (receptor) (CGRP-(R)) blocking therapeutics in the treatment of acute migraine headache provided proof-of-concept for the involvement of CGRP in the pathophysiology of this disorder. One of the major hurdles for the development of any class of drugs, including CGRP block...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.12704

    authors: Buntinx L,Vermeersch S,de Hoon J

    更新日期:2015-11-01 00:00:00

  • Enalapril (MK421) activation in man: importance of liver status.

    abstract::The in vitro conversion of enalapril (MK421) to enalaprilic acid (MK422) in human autopsy tissues was examined. MK422 was measured by radioimmunoassay. Human cadaver liver was the only tissue in which significant conversion was demonstrated. The esterase activity was stable after post mortem. Autopsy liver tissues fro...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1985.tb02699.x

    authors: Larmour I,Jackson B,Cubela R,Johnston CI

    更新日期:1985-05-01 00:00:00

  • Preliminary assessment of RX 72601, a new anticholinesterase in man: reversal of competitive neuromuscular blockade.

    abstract::1 The effect of RX 72601, neostigmine plus atropine, or saline on neuromuscular blockade with (+)-tubocurarine was studied in a double blind trial in four healthy male volunteers. 2 The methods used to assess neuromuscular function were voluntary grip strength and indirectly evoked muscle twitches. The muscarinic acti...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1974.tb00239.x

    authors: Dettmar PW,Metcalf G,Smith MH,Gillett GB,Hedges A,Richens A

    更新日期:1974-06-01 00:00:00

  • Cato Guldberg and Peter Waage, the history of the Law of Mass Action, and its relevance to clinical pharmacology.

    abstract::We have traced the historical link between the Law of Mass Action and clinical pharmacology. The Law evolved from the work of the French chemist Claude Louis Berthollet, was first formulated by Cato Guldberg and Peter Waage in 1864 and later clarified by the Dutch chemist Jacobus van 't Hoff in 1877. It has profoundly...

    journal_title:British journal of clinical pharmacology

    pub_type: 传,历史文章,杂志文章,评审

    doi:10.1111/bcp.12721

    authors: Ferner RE,Aronson JK

    更新日期:2016-01-01 00:00:00

  • The effect of age on the pharmacokinetics of metoprolol and its metabolites.

    abstract::1 Plasma concentrations of metoprolol and a pharmacologically active metabolite, H119/66, have been measured in young and elderly volunteers after a single dose of 100 mg metoprolol tartrate and after repeated administrated over a period of 1 week. Whilst concentrations of metoprolol are similar in each group, concent...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1981.tb00536.x

    authors: Quarterman CP,Kendall MJ,Jack DB

    更新日期:1981-03-01 00:00:00

  • Effects of MHRA drug safety advice on time trends in prescribing volume and indices of clinical toxicity for quinine.

    abstract:AIMS:To ascertain the effects of the Medicines and Healthcare products Regulatory Agency's (MHRA) safety update in June 2010 on the volume of prescribing of quinine and on indices of quinine toxicity. METHODS:We analysed quarterly primary care total and quinine prescribing data for England and quinine prescribing volu...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.12130

    authors: Acheampong P,Cooper G,Khazaeli B,Lupton DJ,White S,May MT,Thomas SH

    更新日期:2013-12-01 00:00:00

  • Comparison of digoxin and medigoxin in normal subjects.

    abstract::1 The properties of a recently introduced digitalis glycoside, 4-beta-methyl digoxin (medigoxin) were compared to those of a standard digoxin preparation. Using a radioimmunoassay (RIA) technique, serial plasma levels were recorded for 8 h following a single oral dose in five fasting volunteer subjects, and urinary gl...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1111/j.1365-2125.1978.tb01686.x

    authors: Hayward RP,Greenwood H,Hamer J

    更新日期:1978-07-01 00:00:00