Methylprednisolone pharmacokinetics after intravenous and oral administration.

Abstract:

:1. The pharmacokinetics of methylprednisolone (MP) were studied in five normal subjects following intravenous doses of 20, 40 and 80 mg methylprednisolone sodium succinate (MPSS) and an oral dose of 20 mg methylprednisolone as 4 x 5 mg tablets. Plasma concentrations of MP and MPSS were measured by both high performance thin layer (h.p.t.l.c.) and high pressure liquid chromatography (h.p.l.c.). 2. The mean values (+/- s.d.) of half-life, mean residence time (MRT), systemic clearance (CL) and volume of distribution at steady state (Vss) of MP following intravenous administration were 1.93 +/- 0.35 h, 3.50 +/- 1.01 h, 0.45 +/- 0.12 lh-1 kg-1 and 1.5 +/- 0.63 1 kg-1, respectively. There was no evidence of dose-related changes in these values. The plasma MP concentration-time curves were superimposable when normalized for dose. 3. The bioavailability of methylprednisolone from the 20 mg tablet was 0.82 +/- 0.11 (s.d.). 4. In vivo hydrolysis of MPSS was rapid with a half-life of 4.14 +/- 1.62 (s.d.) min, and was independent of dose. In contrast, in vitro hydrolysis in plasma, whole blood and red blood cells was slow; the process continuing for more than 7 days. Sodium fluoride did not prevent the hydrolysis of MPSS.

journal_name

Br J Clin Pharmacol

authors

Al-Habet SM,Rogers HJ

doi

10.1111/j.1365-2125.1989.tb05366.x

subject

Has Abstract

pub_date

1989-03-01 00:00:00

pages

285-90

issue

3

eissn

0306-5251

issn

1365-2125

journal_volume

27

pub_type

临床试验,杂志文章,随机对照试验
  • Use of an integrated modelling and simulation approach to develop a simplified peginterferon alfa-2a dosing regimen for children with hepatitis C.

    abstract:AIM:The aim of the study was to simplify the dosing regimen of peginterferon alfa-2a in paediatric patients with chronic hepatitis C. METHODS:A population pharmacokinetic (PK) model was developed using PK data from 14 children aged 2-8 years and 402 adults. Simulations were produced to identify a simplified dosing reg...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/bcp.12816

    authors: Brennan BJ,Lemenuel-Diot A,Snoeck E,McKenna M,Solsky J,Wat C,Mallalieu NL

    更新日期:2016-04-01 00:00:00

  • Metabolic effects of low-dose fluconazole in healthy female users and non-users of oral contraceptives.

    abstract::1. Azole antifungal agents such as ketoconazole act by inhibiting cytochrome P-450 mediated sterol synthesis in the fungal cell membrane and thus have the potential to interfere with mammalian steroidogenesis. Fluconazole is a novel orally-effective antifungal triazole which has been reported to have more specific eff...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1989.tb03449.x

    authors: Devenport MH,Crook D,Wynn V,Lees LJ

    更新日期:1989-06-01 00:00:00

  • Co-prescribing of SSRIs and TCAs in Australia: how often does it occur and who is doing it?

    abstract:AIMS:To determine the frequency with which the selective serotonin re-uptake inhibitor (SSRI) antidepressants are used as add-on therapy to the tricyclic antidepressants (TCA) rather than as replacement therapy. METHODS:The data analysed were profiles of prescription records by date of supply to the patient. From with...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.2001.01319.x

    authors: McManus P,Mant A,Mitchell P,Birkett D,Dudley J

    更新日期:2001-01-01 00:00:00

  • Effects of policosanol treatment on the susceptibility of low density lipoprotein (LDL) isolated from healthy volunteers to oxidative modification in vitro.

    abstract:AIMS:The aim of this study was to investigate the effect of policosanol on the susceptibility of LDL-C to in vitro lipid peroxidation in human healthy volunteers. METHODS:The effect of policosanol (5 and 10 mg day(-1) on LDL-C oxidation was studied in a double-blind, randomized, placebo-controlled trial conducted in 6...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1046/j.1365-2125.2000.00250.x

    authors: Menéndez R,Más R,Amor AM,González RM,Fernández JC,Rodeiro I,Zayas M,Jiménez S

    更新日期:2000-09-01 00:00:00

  • Marketing medicines: charting the rise of modern therapeutics through a systematic review of adverts in UK medical journals (1950-1980).

    abstract:AIMS:To examine how pharmaceutical products that were first marketed between 1950 and 1980 were promoted to physicians through advertisements and briefly review advertising regulations and accuracy of the advertisements in the light of modern knowledge. METHODS:We systematically reviewed advertisements promoting drugs...

    journal_title:British journal of clinical pharmacology

    pub_type: 历史文章,杂志文章

    doi:10.1111/bcp.13549

    authors: Green AR,Haddad PM,Aronson JK

    更新日期:2018-08-01 00:00:00

  • Absorption of cyclosporin from conventional and new microemulsion oral formulations in liver transplant recipients with external biliary diversion.

    abstract::1. Less than 5% of a dose of the conventional oral formulation of cyclosporin, Sandimmun, is absorbed in liver transplant recipients with external biliary drainage, necessitating intravenous administration of the drug and exposing the patient to increased risk of severe side-effects. 2. We compared the pharmacokinetic...

    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.1365-2125.1995.tb05722.x

    authors: Trull AK,Tan KK,Tan L,Alexander GJ,Jamieson NV

    更新日期:1995-06-01 00:00:00

  • Sources of variability in nicotine and cotinine levels with use of nicotine nasal spray, transdermal nicotine, and cigarette smoking.

    abstract:AIMS:Nicotine nasal spray and transdermal nicotine are effective aids to smoking cessation, and are being evaluated for treatment of other medical diseases. Wide variation in levels of nicotine and its metabolite, cotinine, have been observed with such therapies. This study aimed primarily to assess sources of individu...

    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.1365-2125.1997.00566.x

    authors: Benowitz NL,Zevin S,Jacob P 3rd

    更新日期:1997-03-01 00:00:00

  • Effects of diazepam and chlormethiazole on ventilatory control in normal subjects.

    abstract::We have studied the effects of chlormethiazole and diazepam given orally on the ventilatory and mouth occlusion pressure (P0.1) responses to CO2 in a placebo controlled study in 10 healthy volunteers. Diazepam 10 mg produced a significant reduction in both the ventilatory and P0.1 responses to CO2, and this was not as...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.1988.tb05266.x

    authors: Gilmartin JJ,Corris PA,Stone TN,Veale D,Gibson GJ

    更新日期:1988-06-01 00:00:00

  • Selective effects of low doses of apomorphine on spatiotemporal contrast sensitivity in healthy volunteers: a double-blind placebo-controlled study.

    abstract::1. Apomorphine (1 and 5 micrograms kg-1) and placebo were given to nine normal volunteers, using a Latin-square design and double-blind procedures. The visual perception of static and moving patterns (static and motion contrast sensitivity) was evaluated before and 15 min after the dose administration. 2. Apomorphine ...

    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.1365-2125.1991.tb03950.x

    authors: Blin O,Mestre D,Masson G,Serratrice G

    更新日期:1991-11-01 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

  • Inhibition of artificially induced cough in man by bronchodilators.

    abstract::1. The antitussive properties of bronchodilators were evaluated in a total of 47 normal volunteers. 2. Cough was induced by inhalation of ultrasonically nebulized solutions of distilled water and hypotonic saline. 3. Inhaled fenoterol hydrobromide (360 micrograms; 20 volunteers) and inhaled ipratropium bromide (72 mic...

    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.1365-2125.1987.tb03204.x

    authors: Lowry R,Higenbottam T,Johnson T,Godden D

    更新日期:1987-10-01 00:00:00

  • Drug induced liver injury with analysis of alternative causes as confounding variables.

    abstract:AIMS:Drug-induced liver injury (DILI) is rare compared to the worldwide frequent acute or chronic liver diseases. Therefore, patients included in series of suspected DILI are at high risk of not having DILI, whereby alternative causes may confound the DILI diagnosis. The aim of this review is to evaluate published case...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.13593

    authors: Teschke R,Danan G

    更新日期:2018-07-01 00:00:00

  • 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 a...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1993.tb00422.x

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

    更新日期:1993-12-01 00:00:00

  • Prescription patterns of diuretics in Dutch community-dwelling elderly patients.

    abstract:AIMS:To describe age- and gender-related prescription patterns of diuretics in community-dwelling elderly, and to compare diuretics to other cardiovascular (CV) medications. METHODS:Cross-sectional study of patient-specific prescription data derived from a panel of 10 Dutch community pharmacies. Determination of propo...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1046/j.1365-2125.1998.00793.x

    authors: van Kraaij DJ,Jansen RW,de Gier JJ,Gribnau FW,Hoefnagels WH

    更新日期:1998-10-01 00:00:00

  • Usage of paracetamol-containing combination analgesics remains high in primary care.

    abstract:AIMS:Paracetamol-containing combination analgesics are widely prescribed but the use of paracetamol/dextropropoxyphene (co-proxamol) is particularly controversial. We aim to examine the prescribing patterns of the paracetamol-containing analgesics in Ireland. METHODS:A national primary care prescribing database was us...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,多中心研究

    doi:10.1111/j.1365-2125.2005.02500.x

    authors: Usher C,Teeling M,Bennett K,McGowan B,Feely J

    更新日期:2005-12-01 00:00:00

  • Social media and pharmacovigilance: A review of the opportunities and challenges.

    abstract::Adverse drug reactions come at a considerable cost on society. Social media are a potentially invaluable reservoir of information for pharmacovigilance, yet their true value remains to be fully understood. In order to realize the benefits social media holds, a number of technical, regulatory and ethical challenges rem...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.12717

    authors: Sloane R,Osanlou O,Lewis D,Bollegala D,Maskell S,Pirmohamed M

    更新日期:2015-10-01 00:00:00

  • Reduced platelet aggregation after fluvastatin therapy is associated with altered platelet lipid composition and drug binding to the platelets.

    abstract:AIMS:High plasma cholesterol concentration and increased platelet activity are two major risk factors for atherosclerosis. Lovastatin, the lipophilic drug was shown to inhibit platelet aggregation whereas pravastatin, the hydrophilic drug had no such effect. Analysis of the effect of fluvastatin which is both a lipophi...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1046/j.1365-2125.1997.00625.x

    authors: Osamah H,Mira R,Sorina S,Shlomo K,Michael A

    更新日期:1997-07-01 00:00:00

  • Topical minoxidil: cardiac effects in bald man.

    abstract::Systemic cardiovascular effects during chronic treatment with topical minoxidil vs placebo were evaluated using a double-blind, randomized design for two parallel groups (n = 20 for minoxidil, n = 15 for placebo). During 6 months of follow-up, blood pressure did not change, whereas minoxidil increased heart rate by 3-...

    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.1365-2125.1988.tb03410.x

    authors: Leenen FH,Smith DL,Unger WP

    更新日期:1988-10-01 00:00:00

  • CYP2D6 variation, behaviour and psychopathology: implications for pharmacogenomics-guided clinical trials.

    abstract::Individual and population differences in polymorphic cytochrome P450 enzyme function have been known for decades. The biological significance of these differences has now been deciphered with regard to drug metabolism, action and toxicity as well as disposition of endogenous substrates, including neuroactive compounds...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bcp.12227

    authors: Peñas-Lledó EM,Llerena A

    更新日期:2014-04-01 00:00:00

  • Use of statins and risk of haematological malignancies: a meta-analysis of six randomized clinical trials and eight observational studies.

    abstract:AIMS:Statins have been suggested to prevent haematological malignancies. Several epidemiological studies have evaluated this association, while randomized controlled trials (RCTs) on cardiovascular outcomes have provided relevant data as secondary end-points. Our aim was to examine the strength of this association thro...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,meta分析,评审

    doi:10.1111/j.1365-2125.2007.02959.x

    authors: Bonovas S,Filioussi K,Tsantes A,Sitaras NM

    更新日期:2007-09-01 00:00:00

  • Pharmacokinetics of hydrochlorothiazide in patients with congestive heart failure.

    abstract::1. Hydrochlorothiazide (HCT, 50-75 mg) was administered orally to seven patients with cardiac failure. 2. Plasma levels and urinary concentration of HCT were determined by GLC. 3. The gastrointestinal uptake of the diuretic in three patients was reduced to approximately half that seen in healthy controls. 4. Plasma ha...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1979.tb04646.x

    authors: Beermann B,Groschinsky-Grind M

    更新日期:1979-06-01 00:00:00

  • A simple collection method for saliva in children: potential for home monitoring of carbamazepine therapy.

    abstract::We have developed a method of monitoring plasma concentrations of antiepileptic drugs which uses salivary samples, and is suitable for home monitoring in children. To validate the method, paired plasma and saliva samples from 39 children aged between 2 and 15 years were assayed for carbamazepine and its active metabol...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.1993.tb05700.x

    authors: Chee KY,Lee D,Byron D,Naidoo D,Bye A

    更新日期:1993-03-01 00:00:00

  • The roles of clinical pharmacologists in UK universities.

    abstract::Clinical pharmacologists in universities play major roles in research and teaching and provide important contributions to National Health Service (NHS) activities, such as work for research ethics, drug and therapeutics, and clinical governance committees. Their research extends from preclinical studies using drugs to...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2012.04228.x

    authors: Webb DJ

    更新日期:2012-06-01 00:00:00

  • A controlled trial of labetalol (Trandate), propranolol and placebo in the management of mild to moderate hypertension.

    abstract::1. Labetalol, a new drug combining alpha-and beta-adrenoceptor blocking properties, has been compared with placebo in a double-blind crossover study of a group of patients with mild to moderate essential hypertension (blood pressure 150/100 to 189/114 mmHg). 2. Labetalol and propranolol lowered blood pressure satisfac...

    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.1365-2125.1979.tb00898.x

    authors: Pugsley DJ,Nassim M,Armstrong BK,Beilin L

    更新日期:1979-01-01 00:00:00

  • Effect of labetalol in hypertension during exercise and postural changes.

    abstract::1 Fourteen hypertensive patients were studied by intra-arterial BP monitoring to quantify the effects of standardized physiological stresses: Valsalva manoeuvre, isometric, treadmill and bicycle exercise, and 60 degree tilting before and after labetalol treatment. 2 The dose of labetalol ranged from 100--600 mg three ...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Balasubramanian V,Mann S,Millar-Craig MW,Raftery EB

    更新日期:1979-01-01 00:00:00

  • SLCO1B1 521T-->C functional genetic polymorphism and lipid-lowering efficacy of multiple-dose pravastatin in Chinese coronary heart disease patients.

    abstract:AIMS:Pravastatin is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor, which is widely used both in primary and secondary prevention of coronary heart disease (CHD). Pravastatin is not subject to metabolism by cytochrome P450s, but it is actively transported from blood into target tissues (e.g. hepa...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/j.1365-2125.2007.02892.x

    authors: Zhang W,Chen BL,Ozdemir V,He YJ,Zhou G,Peng DD,Deng S,Xie QY,Xie W,Xu LY,Wang LC,Fan L,Wang A,Zhou HH

    更新日期:2007-09-01 00:00:00

  • A signal of increased risk of hypoglycaemia with angiotensin receptor blockers caused by confounding.

    abstract:AIMS:To study reporting of hypoglycaemia in angiotensin receptor blocker (ARB) users, and to investigate the possibility of confounding. METHODS:The French pharmacovigilance database was examined for an association between hypoglycaemia and ARBs or other drugs using reports notified between 1996 and 2005. This associa...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1365-2125.2008.03176.x

    authors: Grégoire F,Pariente A,Fourrier-Reglat A,Haramburu F,Bégaud B,Moore N

    更新日期:2008-07-01 00:00:00

  • Therapeutic drug monitoring: antiarrhythmic drugs.

    abstract::Antiarrhythmic agents are traditionally classified according to Vaughan Williams into four classes of action. Class I antiarrhythmic agents include most of the drugs traditionally thought of as antiarrhythmics, and have as a common action, blockade of the fast-inward sodium channel on myocardium. These agents have a v...

    journal_title:British journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1046/j.1365-2125.2001.0520s1021.x

    authors: Campbell TJ,Williams KM

    更新日期:2001-01-01 00:00:00

  • Pharmacokinetics of lamotrigine and its metabolite N-2-glucuronide: Influence of polymorphism of UDP-glucuronosyltransferases and drug transporters.

    abstract:AIMS:This study aimed to develop a population pharmacokinetic model for quantitative evaluation of the influence of genetic variants in metabolic enzymes and transporters on lamotrigine pharmacokinetics while taking into account the influence of various clinical, biochemical and demographic factors. METHODS:We include...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1111/bcp.12984

    authors: Milosheska D,Lorber B,Vovk T,Kastelic M,Dolžan V,Grabnar I

    更新日期:2016-08-01 00:00:00

  • Effect of beta-adrenoceptor blockade on atrial natriuretic peptide levels during exercise in angina pectoris.

    abstract::The effects of epanolol (200 mg once daily) and diltiazem (60 mg three times daily) on the response of atrial natriuretic peptide (ANP) to exercise were investigated in a double-blind placebo-controlled crossover study in 16 patients with angina pectoris. Exercise tolerance as assessed by peak oxygen consumption was s...

    journal_title:British journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:

    authors: Riley M,Elborn JS,Onuoha G,Erwin C,Shaw C,Khan MM,Stanford CF,Nicholls DP

    更新日期:1993-02-01 00:00:00