Pharmacokinetics of the selective benzodiazepine antagonist Ro 15-1788 in man.

Abstract:

:The pharmacokinetics of the selective benzodiazepine antagonist Ro 15-1788 has been studied in 6 healthy male volunteers following a single intravenous dose of 2.5 mg. The drug was only slightly bound to plasma proteins (40 +/- 8%, mean +/- SD). A negligible amount (less than 0.2% of the dose) of unchanged drug was recovered in urine. Hepatic elimination was rapid, as shown by a short t1/2 of 0.9 +/- 0.2 h, and high total plasma and blood clearances of 691 +/- 216 ml/min and 716 +/- 199 ml/min, respectively. The fast decline of plasma levels from about 60 to 2 ng/ml accounts for the short-lasting reversal of benzodiazepine-induced sedation by Ro 15-1788.

journal_name

Eur J Clin Pharmacol

authors

Klotz U,Ziegler G,Reimann IW

subject

Has Abstract

pub_date

1984-01-01 00:00:00

pages

115-7

issue

1

eissn

0031-6970

issn

1432-1041

journal_volume

27

pub_type

杂志文章
  • Lack of relationship between quinidine pharmacokinetics and the sparteine oxidation polymorphism.

    abstract::Quinidine is a very potent inhibitor of CYP2D6, but the role of the enzyme in the biotransformation of quinidine has only been investigated in a single in vitro study and in two small in vivo experiments, with contradictory results. The present investigation was designed to present definite evaluation of whether quini...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00194341

    authors: Nielsen F,Rosholm JU,Brøsen K

    更新日期:1995-01-01 00:00:00

  • Clinical and therapeutic use of probucol.

    abstract::Previous studies showed that probucol significantly lowered both LDL cholesterol and HDL cholesterol. In addition, there is evidence that as an essential antioxidant probucol causes variations in cellular interactions and cardiovascular functions in patients. Therefore, 14 hypercholesterolemic men were investigated be...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:

    authors: Berg A,Baumstark MW,Frey I,Halle M,Keul J

    更新日期:1991-01-01 00:00:00

  • Absorption and metabolism in man of 16-epi-gitoxin, a new semi-synthetic cardioactive glycoside.

    abstract::The pharmacokinetics of 3H-16-epi-gitoxin have been investigated after oral administration: The peak serum level occurred after 30-60 min, and its subsequent decline was in two phases with half-lives of 3.5 and 19.5 h, respectively. Within 3 days 66-70% of the administered radioactivity were eliminated by renal excret...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00562938

    authors: Haustein KO

    更新日期:1977-07-19 00:00:00

  • Pharmacokinetics of 3H-phenylephrine in man.

    abstract::7-3H-phenylephrine was given to 15 volunteers by a short-infusion n = 4) or p.o. (10 volunteers, 1 patient with porto-caval anastomosis). Analysis of serum for free 3H-phenylephrine and fractionation of urinary radioactivity was performed by ion-exchange and thin-layer chromatography. As almost the same 3H-activity wa...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00637623

    authors: Hengstmann JH,Goronzy J

    更新日期:1982-01-01 00:00:00

  • Arginine vasopressin (AVP) and treatment with arginine vasopressin receptor antagonists (vaptans) in congestive heart failure, liver cirrhosis and syndrome of inappropriate antidiuretic hormone secretion (SIADH).

    abstract::Arginine vasopressin (AVP) is the major physiological regulator of renal water excretion and blood volume. The AVP pathways of V(1a)R-mediated vasoconstriction and V(2)R-induced water retention represent a potentially attractive target of therapy for edematous diseases. Experimental and clinical evidence suggests bene...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00228-011-1006-7

    authors: Gassanov N,Semmo N,Semmo M,Nia AM,Fuhr U,Er F

    更新日期:2011-04-01 00:00:00

  • Use of anti-asthmatic drugs during pregnancy. 1. Maternal characteristics, pregnancy and delivery complications.

    abstract:OBJECTIVE:To study, in a large cohort, the association between the use of anti-asthmatic drugs during pregnancy and pregnancy complications. METHODS:Using the Swedish Medical Birth Register, we identified 24,369 women who reported the use of anti-asthmatic drugs in early pregnancy and 7778 women who were prescribed su...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-006-0257-1

    authors: Källén B,Otterblad Olausson P

    更新日期:2007-04-01 00:00:00

  • Network meta-analyses of antiepileptic drug efficacy and tolerability in drug-resistant focal epilepsies: a clinical perspective.

    abstract:PURPOSE:Network meta-analysis (NMA) is a new technique that allows multiple treatment comparisons and provides estimates of effect sizes for all possible pair-wise comparisons. Several NMAs of antiepileptic drug (AED) efficacy and tolerability in individuals with refractory focal epilepsy, however, came to non-specific...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1007/s00228-014-1669-y

    authors: Zaccara G,Giovannelli F,Bell GS,Sander JW

    更新日期:2014-06-01 00:00:00

  • HTR1B as a risk profile maker in psychiatric disorders: a review through motivation and memory.

    abstract:PURPOSE:Serotonin receptor 1B (HTR1B) is involved in the regulation of the serotonin system, playing different roles in specific areas of the brain. We review the characteristics of the gene coding for HTR1B, its product and the functional role of HTR1B in the neural networks involved in motivation and memory; the cent...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00228-009-0724-6

    authors: Drago A,Alboni S,Brunello N,De Ronchi D,Serretti A

    更新日期:2010-01-01 00:00:00

  • Corticosteroid therapy and need for hospital care in wheezing preschool children.

    abstract:OBJECTIVES:To study the frequency of corticosteroid therapy and the use of inpatient care for preschool children with wheezing in two regions in Finland. METHODS:The Finnish Social Insurance Institution database on refundable asthma medication indicated that 1.18% of children in Tampere and 2.37% in Turku used inhaled...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002280000199

    authors: Csonka P,Mertsola J,Klaukka T,Kaila M,Ståhlberg MR,Ashorn P

    更新日期:2000-11-01 00:00:00

  • Single- and multiple-dose pharmacokinetics of terodiline in geriatric patients.

    abstract::As a target group, geriataric patients were selected for pharmacokinetic studies with terodiline (Mictrol), an anticholinergic and calcium antagonist drug effective in the treatment of urinary incontinence. The single-dose kinetics in the geriatric patients (mean age 82 years) differed significantly from that previous...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00540958

    authors: Hallén B,Magnusson A,Bogentoft S,Ekelund P

    更新日期:1988-01-01 00:00:00

  • Utilization of oral antihyperglycemic drugs over a 7-year period (1998-2004) in a Hungarian population and adherence to drug therapy.

    abstract:OBJECTIVE:To describe the quantitative and qualitative changes in the utilization of oral antihyperglycemic drugs (OAHDs) between 1998 and 2004 and to analyze patients' adherence to OAHD therapy. METHODS:We conducted a retrospective analysis of the electronic database of the Hungarian National Health Fund Administrati...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-005-0031-9

    authors: Doró P,Benko R,Kosik E,Matuz M,Tóth K,Soós G

    更新日期:2005-12-01 00:00:00

  • Genetic variability at COMT but not at OPRM1 and UGT2B7 loci modulates morphine analgesic response in acute postoperative pain.

    abstract:PURPOSE:To investigate interindividual variability in response to pain treatment, we characterized postoperative patients for morphine metabolism and for COMT, OPRM1 and UGT2B7 polymorphisms. METHODS:A total of 109 patients treated with morphine were genotyped by DNA sequencing for 12 DNA polymorphisms of the COMT, OP...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00228-013-1523-7

    authors: De Gregori M,Garbin G,De Gregori S,Minella CE,Bugada D,Lisa A,Govoni S,Regazzi M,Allegri M,Ranzani GN

    更新日期:2013-09-01 00:00:00

  • Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function.

    abstract::We have studied pharmacokinetics of a new H2-receptor antagonist, TZU-0460, in patients with varying degrees of renal impairment. The apparent volume of distribution at steady-state was 1.70 l/kg, and the plasma protein binding of TZU-0460 or its active metabolite, desacetyl TZU-0460 was less than 10% in normal subjec...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00608220

    authors: Takabatake T,Ohta H,Yamamoto Y,Ishida Y,Hara H,Nakamura S,Ushiogi Y,Satoh S,Hattori N

    更新日期:1986-01-01 00:00:00

  • Ambulatory blood pressure monitoring during sustained treatment with conventional and extended-release felodipine in mild-to-moderate hypertension.

    abstract::To assess the duration of the antihypertensive effect of the dihydropiridine calcium antagonist felodipine in conventional (C-F) and slow-release (ER-F) formulations, 12 patients with essential hypertension underwent ambulatory blood pressure monitoring (ABPM) at the end of a 2-week treatment period with C-F 5 mg b.d....

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/BF00562543

    authors: Porcellati C,Verdecchia P,Gatteschi C,Benemio G,Guerrieri M,Boldrini F,Pollavini G

    更新日期:1989-01-01 00:00:00

  • Do pharmacokinetic polymorphisms explain treatment failure in high-risk patients with neuroblastoma?

    abstract:PURPOSE:Neuroblastoma is the most common extracranial solid tumour in childhood. It accounts for 15% of all paediatric oncology deaths. In the last few decades, improvement in treatment outcome for high-risk patients has not occurred, with an overall survival rate <30-40%. Many reasons may account for such a low surviv...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00228-010-0966-3

    authors: Bellanti F,Kågedal B,Della Pasqua O

    更新日期:2011-05-01 00:00:00

  • Non-steroidal anti-inflammatory drugs: use and co-treatment with potentially interacting medications in the elderly.

    abstract:BACKGROUND:Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used in the elderly. NSAIDs may cause a series of adverse drug reactions, of which gastrointestinal, renovascular/cardiovascular and bleeding complications are of particular concern. Concomitant use of several other drugs may further increase the risk...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-010-0825-2

    authors: Vandraas KF,Spigset O,Mahic M,Slørdal L

    更新日期:2010-08-01 00:00:00

  • Fabry disease and treatment with agalsidase alpha: unsuspected cardiac arrhythmia in two heterozygous women. In reference to pharmacovigilance.

    abstract:CASE REPORTS:Two women treated with agalsidase alpha for Fabry disease developed severe heart dysfunctions a few months after the beginning of enzyme replacement therapy (ERT). An adverse effect caused by the treatment was suspected; therefore we informed the French pharmacovigilance authorities about these two events....

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-007-0460-8

    authors: Mougenot P,Lidove O,Caillaud C,Arnaud P,Papo T

    更新日期:2008-06-01 00:00:00

  • A real or apparent decrease in glomerular filtration rate in patients using olaparib?

    abstract:PURPOSE:Olaparib is a poly (ADP-ribose) polymerase (PARP) inhibitor indicated for ovarian and metastatic breast cancer. Increased serum creatinine levels have been observed in patients taking olaparib, but the underlying mechanism is unknown. This study aimed to investigate if patients receiving olaparib have increased...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-020-03070-0

    authors: Bruin MAC,Korse CM,van Wijnen B,de Jong VMT,Linn SC,van Triest B,Rosing H,Beijnen JH,van den Broek D,Huitema ADR

    更新日期:2021-02-01 00:00:00

  • Acute effect of prednisone and deflazacort on glucose tolerance in prediabetic subjects.

    abstract::The diabetogenic effect of deflazacort (DF), an oxazolinic synthetic corticosteroid, was studied in 12 healthy adult subjects with a positive family history of diabetes mellitus. Three oral glucose tests (oGTT) were performed at 9.00 a.m., after a 12 h fast, following randomized administration of Placebo (PL), or Defl...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/BF00542555

    authors: Pagano G,Lombardi A,Ferraris GM,Imbimbo B,Cavallo Perin P

    更新日期:1982-01-01 00:00:00

  • Single nucleotide polymorphisms of ABCB1 (MDR1) gene and distinct haplotype profile in a West Black African population.

    abstract:OBJECTIVE:The ABCB1 (MDR1) multidrug transporter plays a key role in determining drug bioavailability. Differences in drug response exist among different ethnic groups. However, until now, no haplotype data are available in a Black African population. METHODS:Exons 2, 7, 10, 11, 12, 14, 17, 21, 26, and the surrounding...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-004-0879-0

    authors: Allabi AC,Horsmans Y,Issaoui B,Gala JL

    更新日期:2005-04-01 00:00:00

  • Antidepressant drug prescribing in Italy, 2000: analysis of a general practice database.

    abstract:OBJECTIVE:Databases of subjects receiving antidepressants provide evidence on the use of drugs in typical patients and settings under real-world conditions. This study analysed a general practice database to estimate the prevalence of antidepressant drug use, describe the use of these compounds by gender and age and es...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002280100361

    authors: Pietraru C,Barbui C,Poggio L,Tognoni G

    更新日期:2001-10-01 00:00:00

  • Long-term nicotine substitution after application of a 16-hour nicotine patch in smoking cessation.

    abstract::The purpose of the study was to examine long-term nicotine substitution and its variability during use of a nicotine patch. In two smoking cessation studies a 16-h nicotine patch, releasing 15 mg nicotine, was applied daily for 16 h over 12 weeks, to 167 smokers. Salivary cotinine was highly correlated with plasma cot...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1007/BF02280755

    authors: Nørregaard J,Tønnesen P,Simonsen K,Säwe U

    更新日期:1992-01-01 00:00:00

  • Trends in opioid analgesics consumption, Israel, 2000-2008.

    abstract:OBJECTIVE:To describe trends in opioid consumption in Israel (morphine, methadone, oxycodone, pethidine, fentanyl, buprenorphine, codeine, and dextropropoxyphene) over the 9 years, 2000-2008, and to explore explanations for changes in consumption, in amounts and the pattern. METHODS:Data for the 2000-2008 period (all ...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-010-0932-0

    authors: Ponizovsky AM,Marom E,Zeldin A,Cherny NI

    更新日期:2011-02-01 00:00:00

  • Nicorandil suppressed myocardial purine metabolism during exercise in patients with angina pectoris.

    abstract::To elucidate the effect of Nicorandil on myocardial energy metabolism and myocardial sympathetic activity, we administered Nicorandil orally to eight patients with angina pectoris prior to exercise testing. Arterial and coronary sinus levels of lactate, ammonia, hypoxanthine (HX), adrenaline and noradrenaline were mea...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00198297

    authors: Ogino K,Osaki S,Noguchi N,Kitamura H,Omodani H,Kato M,Hisatome I,Matsumoto T,Kinugawa T,Miyakoda H

    更新日期:1995-01-01 00:00:00

  • Prevalence of UGT1A9 and UGT2B7 nonsynonymous single nucleotide polymorphisms in West African, Papua New Guinean, and North American populations.

    abstract:OBJECTIVE:UDP-glucuronosyltransferases (UGTs) UGT1A9 and UGT2B7 are involved in the metabolism of antimalarial dihydroartemisinin and antiretroviral zidovudine. Our aim was to analyze the prevalence of UGT1A9 (chromosome 2) and UGT2B7 (chromosome 4) nonsynonymous single nucleotide polymorphisms (SNPs) in West African (...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-006-0206-z

    authors: Mehlotra RK,Bockarie MJ,Zimmerman PA

    更新日期:2007-01-01 00:00:00

  • Risks for stroke and bleeding with warfarin or aspirin treatment in patients with atrial fibrillation at different CHA(2)DS(2)VASc scores: experience from the Stockholm region.

    abstract:PURPOSE:This study evaluated the benefits of and possible contraindications to warfarin treatment in patients with atrial fibrillation (AF) prior to the introduction of new oral anticoagulants using health registry data from inpatient care, specialist ambulatory care, and primary care. METHODS:This is a cohort study i...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-014-1739-1

    authors: Forslund T,Wettermark B,Wändell P,von Euler M,Hasselström J,Hjemdahl P

    更新日期:2014-12-01 00:00:00

  • Effects of grapefruit juice on the stereoselective disposition of nicardipine in humans: evidence for dominant presystemic elimination at the gut site.

    abstract:OBJECTIVES:To assess relative roles of the intestinal and hepatic stereoselective metabolism of nicardipine in an oral first-pass disposal with and without grapefruit juice intake. METHODS:The kinetic profiles of (+)- and (-)-nicardipine were studied in the six normal healthy male volunteers who received oral (40 mg) ...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002280000235

    authors: Uno T,Ohkubo T,Sugawara K,Higashiyama A,Motomura S,Ishizaki T

    更新日期:2000-12-01 00:00:00

  • Slower onset of vasodilating action of brain natriuretic peptide (BNP) compared to atrial natriuretic peptide (ANP) in human forearm resistant vessels.

    abstract:PURPOSE:To investigate possible differences in the time course of vasodilating effects of atrial natriuretic peptide (ANP) and brain natriuretic peptide (BNP) in humans. METHODS:We measured forearm blood flow (FBF) by strain gauge plethymography and cyclic GMP spillover during and after intra-arterial infusions of BNP...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00228-008-0516-4

    authors: Minami H,Yasu T,Tagawa T,Yamakawa K,Ueda S

    更新日期:2008-09-01 00:00:00

  • On the absorption and metabolism of 35S-ampicillin.

    abstract::An aqueous solution of 35S-ampicillin and polyethylene glycol (PEG 4000, unabsorbable marker) was administered orally to 6 healthy subjects with gastrointestinal tubes. The minimal absorption of radioactive material, as shown by urinary excretion of label, differed markedly between subjects and averaged 44% (25-67). A...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00614007

    authors: Swahn A

    更新日期:1975-12-19 00:00:00

  • Effect of quinidine on digoxin bioavailability.

    abstract::To evaluate the possible effect of quinidine on digoxin bioavailability, the steady state digoxin kinetics was examined with and without concomitant quinidine therapy, in 7 cardiac patients after simultaneous administration of oral digoxin and intravenous [3H]-digoxin. In the presence of quinidine, the absorption rate...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00613925

    authors: Pedersen KE,Christiansen BD,Klitgaard NA,Nielsen-Kudsk F

    更新日期:1983-01-01 00:00:00