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 was excreted in urine after i.v. and p.o. administration, 86% and 80% of the dose respectively, complete enteral absorption can be assumed. A considerable difference was seen in the fraction of free phenylephrine, i.v. 16% of the dose versus p.o. 2.6%, which suggested reduced bioavailability. This was confirmed by comparison of the areas under the serum curve, which showed a bioavailability factor of 0.38. The result for the patient with porto-caval anastomosis was comparable to that in the normal volunteers. The biological half-life of 2 to 3h was comparable to that of structurally related amines, as were the total clearance of 2 l/h, and the volume of distribution of 340 l. Metabolism to phenolic conjugates mainly after oral ingestion, and to m-hydroxymandelic acid after i.v. injection, again demonstrated that m-hydroxylated amines are predominantly conjugated during the "first-pass" metabolism.

journal_name

Eur J Clin Pharmacol

authors

Hengstmann JH,Goronzy J

doi

10.1007/BF00637623

subject

Has Abstract

pub_date

1982-01-01 00:00:00

pages

335-41

issue

4

eissn

0031-6970

issn

1432-1041

journal_volume

21

pub_type

杂志文章
  • Temporary reversal of serum to cerebrospinal fluid glycerol concentration gradient after intravenous infusion of glycerol.

    abstract::Glycerol 50 g infused i.v. over 2 to 6 h is widely used to treat cerebral oedema in patients with acute stroke. Its transit through the blood-cerebrospinal fluid barrier in subjects with uninflamed meninges has now been examined. In 7 patients with an external ventriculostomy for occlusive hydrocephalus, each of whom ...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00278481

    authors: Nau R,Prins FJ,Kolenda H,Prange HW

    更新日期:1992-01-01 00:00:00

  • Genetic polymorphism of CYP2C19 and lansoprazole pharmacokinetics in Japanese subjects.

    abstract:OBJECTIVE:We investigated whether interindividual differences in the pharmacokinetic disposition of lansoprazole are attributed to the genetic polymorphism of CYP2C19 which occurred by two mutations. CYP2C19m1 and CYP2C19m2, in 20 Japanese subjects. METHODS:Polymerase chain reaction (PCR) restriction fragment length p...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s002280050307

    authors: Katsuki H,Nakamura C,Arimori K,Fujiyama S,Nakano M

    更新日期:1997-01-01 00:00:00

  • Haemodynamic dose-response effects of i.v. metoprolol in coronary heart disease.

    abstract::The haemodynamic effects of intravenous metoprolol, over the dose-range 2.5--20 mg, were studied in 12 patients with coronary heart disease. The pharmacodynamic activity of the drug was confirmed by the suppression of exercise systolic pressure and tachycardia. There were statistically significant dose-response reduct...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00544581

    authors: Hendry WG,Silke B,Taylor SH

    更新日期:1981-01-01 00:00:00

  • Pharmacogenetic effects of regulatory nuclear receptors (PXR, CAR, RXRα and HNF4α) on docetaxel disposition in Chinese nasopharyngeal cancer patients.

    abstract:PURPOSE:This exploratory study was aimed at elucidating the pharmacogenetics of regulatory nuclear receptors (PXR, CAR, RXRα and HNF4α) and their implications on docetaxel pharmacokinetics and pharmacodynamics in local Chinese nasopharyngeal cancer patients. METHODS:A total of 59 single nucleotide polymorphisms (SNPs)...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00228-013-1596-3

    authors: Chew SC,Lim J,Singh O,Chen X,Tan EH,Lee EJ,Chowbay B

    更新日期:2014-02-01 00:00:00

  • Pinacidil, a new vasodilator, in the treatment of mild to moderate essential hypertension.

    abstract::Twenty three patients with essential hypertension who were uncontrolled on diuretic and/or beta-receptor antagonist therapy were treated additionally with the vasodilator, pinacidil, in an open study. Significant reduction in mean blood pressure was achieved. Supine and erect systolic and diastolic blood pressure fell...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00543335

    authors: D'Arcy V,Laher M,McCoy D,Sullivan P,Walsh CH,Hickey MP

    更新日期:1985-01-01 00:00:00

  • Haemodynamic effects of intravenous verapamil at rest and during exercise in subjectively healthy middle-aged men.

    abstract::Verapamil, 0.1 mg/kg body wt, was injected i.v. over 2 minutes in 8 subjectively healthy middle-aged men, followed by a continuous infusion of 0.007 mg/kg body wt per minute. Prior to the injection several of the subjects had raised pulmonary or systemic arterial pressures. At rest, the central pressures increased sli...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00562656

    authors: Atterhög JH,Ekelund LG

    更新日期:1975-06-13 00:00:00

  • Effect of fenofibrate on the level of asymmetric dimethylarginine in individuals with hypertriglyceridemia.

    abstract:OBJECTIVE:To test whether treatment with fenofibrate decreases asymmetric dimethylarginine (ADMA) level in hypertriglyceridemic individuals. METHODS:In the present study, 45 subjects with hypertriglyceridemia were recruited to receive treatment with fenofibrate (200 mg/d). Serum concentrations of ADMA, malondialdehyde...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s00228-005-0095-6

    authors: Yang TL,Chen MF,Xia X,Luo BL,Li YJ

    更新日期:2006-03-01 00:00:00

  • Pharmacodynamics and arteriovenous difference of intravenous naloxone in healthy volunteers exposed to remifentanil.

    abstract:PURPOSE:Pharmacodynamic studies of naloxone require opioid agonism. Steady state condition may be achieved by remifentanil TCI (target controlled infusion). Opioid agonism can be measured by pupillometry. It is not known whether there are arteriovenous concentration differences for naloxone. The aim was thus to further...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-018-2545-y

    authors: Tylleskar I,Skulberg AK,Skarra S,Nilsen T,Dale O

    更新日期:2018-12-01 00:00:00

  • Plasma theophylline and caffeine and plasma clearance of theophylline during theophylline treatment in the first year of life.

    abstract::Plasma concentrations of caffeine and theophylline were simultaneously determined in 17 preterm infants after oral administration of aminophylline for treatment of apnoea. The ratio of caffeine/theophylline concentration in plasma increased during the first 2 weeks of treatment, owing to the longer time required for c...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00610057

    authors: Lönnerholm G,Lindström B,Paalzow L,Sedin G

    更新日期:1983-01-01 00:00:00

  • Tocilizumab in transplantation.

    abstract:PURPOSE:Tocilizumab, a monoclonal antibody directed against the IL-6 receptor, might block detrimental effects of IL-6 on transplantation. IL-6 plays a considerable role in cytokine storm after stem cell transplantation as well as graft versus host disease, and it has also been shown to be involved in solid organ allog...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,评审

    doi:10.1007/s00228-020-02864-6

    authors: Mosharmovahed B,Fatahi Y,Mohebbi B,Ghorbanian SA,Assadiasl S

    更新日期:2020-06-01 00:00:00

  • The use of a cyclosporin-ketoconazole combination: making renal transplantation affordable in developing countries.

    abstract:OBJECTIVES:The costs of immunosuppressive drugs in renal transplant recipients remains prohibitively high. Ketoconazole (KZ) has, in limited studies, been shown to significantly reduce the dose of cyclosporin (CyA) after renal transplantation. We report our long-term experience with the use of KZ in a large group of re...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-004-0745-0

    authors: Gerntholtz T,Pascoe MD,Botha JF,Halkett J,Kahn D

    更新日期:2004-05-01 00:00:00

  • Interaction between valproate formulation and phenytoin concentrations.

    abstract::Changes in phenytoin concentrations caused by switching valproate formulations with different absorption rates were retrospectively investigated in eleven epileptic patients receiving treatment with both drugs. Total plasma phenytoin concentrations were measured before and after a standard tablet of valproate was repl...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00202174

    authors: Suzuki Y,Nagai T,Mano T,Arai H,Kodaka R,Matsuoka T,Itagaki Y,Ono J,Okada S

    更新日期:1995-01-01 00:00:00

  • Grapefruit juice has no effect on quinine pharmacokinetics.

    abstract:OBJECTIVE:As quinine is mainly metabolised by human liver CYP3A4 and grapefruit juice inhibits CYP3A4, the effect of grapefruit juice on the pharmacokinetics of quinine following a single oral dose of 600 mg quinine sulphate was investigated. METHODS:The study was carried out in ten healthy volunteers using a randomis...

    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/s002280050646

    authors: Ho PC,Chalcroft SC,Coville PF,Wanwimolruk S

    更新日期:1999-07-01 00:00:00

  • Pharmacokinetics of the placental transfer and distribution of clorazepate and its metabolite nordiazepam in the feto-placental unit and in the neonate.

    abstract::Clorazepate 20 mg was given i.m. to 49 mothers during the first stage of labour. The elimination of the drug was studied in 27 newborns produced by these mothers. The same dose was given to 13 women who underwent amniocentesis and to 7 women who were breast-feeding. "Total nordiazepam", i.e. the sum of clorazepate and...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00563103

    authors: Rey E,Giraux P,d'Athis P,Turquais JM,Chavinie J,Olive G

    更新日期:1979-04-17 00:00:00

  • Unwanted symptoms in depressed patients treated with viloxazine: an algorithm for identification of illness-related symptoms.

    abstract::Ninety-six depressed outpatients from 5 centres were given viloxazine 200-400 mg/day. The treatment produced significant clinical improvement as evaluated by the Hamilton Rating Scale for Depression. Thirteen patients dropped-out because of possible side effects. Many untoward symptoms were described by all the patien...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00613832

    authors: Maistrello I,Grassi G,Bertolino A,Valerio P,Pistollato G,Soverini S

    更新日期:1983-01-01 00:00:00

  • Use of prescription forgeries in a drug abuse surveillance network.

    abstract::Data on forged prescriptions in Sweden in 1982-1986 were studied as an indicator in an epidemiological survey of medication abuse. The annual number of prescription forgeries doubled during the 5-year period. Psychotropic drugs accounted for 62% and analgesics for 25% of all forgeries. Benzodiazepines were the major s...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00637747

    authors: Bergman U,Dahl-Puustinen ML

    更新日期:1989-01-01 00:00:00

  • Underuse of lipid-lowering drugs and factors associated with poor adherence: a real practice analysis in Italy.

    abstract:BACKGROUND:Many studies have indicated the adequate use of lipid-lowering drugs (LLDs) as a factor in reducing the risk of cardiovascular disease. However, in clinical practice, a very high percentage of patients are not adequately treated. OBJECTIVE:To analyze the management of hypercholesterolemia in a non-experimen...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-005-0911-z

    authors: Di Martino M,Degli Esposti L,Ruffo P,Bustacchini S,Catte A,Sturani A,Degli Esposti E

    更新日期:2005-05-01 00:00:00

  • Distribution and metabolism of N(G)-nitro-L-arginine methyl ester in patients with septic shock.

    abstract:OBJECTIVE:The pharmacokinetics of N(G)-nitro-L-arginine methyl ester (L-NAME), an inhibitor of nitric oxide (NO) synthesis, was investigated in patients with septic shock. METHODS:Blood was sampled at intervals before, during and after 12-h infusion of L-NAME 1 mg x kg(-1) x h(-1) in nine septic shock patients for det...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/s002280050525

    authors: Avontuur JA,Buijk SL,Bruining HA

    更新日期:1998-10-01 00:00:00

  • Inhibition of thrombocyte aggregation by oral motapizone and other drugs.

    abstract::Ten healthy subjects took single oral doses of placebo, 8.8 +/- 1.8 mg motapizone, 40 +/- 13 mg captopril, 25 mg dihydralazine, 20 mg nifedipine and 4.5 +/- 1.1 mg prazosin in random order, and, as the last preparation 500 mg acetylsalicylic acid. Thrombocyte aggregation induced "ex-vivo" with collagen, ADP and adrena...

    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/BF00613515

    authors: Schulz V,Fischer W,Hanselle U,Huhmann W,Zietsch V

    更新日期:1986-01-01 00:00:00

  • Frequency of S-mephenytoin hydroxylation deficiency in 373 Spanish subjects compared to other Caucasian populations.

    abstract::We have investigated the prevalence of poor metabolisers (PM) of S-mephenytoin in 373 unrelated, healthy Spanish Caucasian subjects, based on the enantiomeric S/R mephenytoin ratio in urine collected 0-8 h and 24-32 h after intake of the racemic drug. Five of the subjects were PM (1.34%, 95% confidence interval 0.18-2...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF02440867

    authors: Reviriego J,Bertilsson L,Carrillo JA,Llerena A,Valdivielso MJ,Benítez J

    更新日期:1993-01-01 00:00:00

  • Controlled clinical investigation of trimeprazine as a sleep-inducer in normal subjects.

    abstract::The effects of acute introduction and withdrawal of trimeprazine (Vallergan), an antihistaminic phenothiazine derivative with known sedative effects, were investigated by a single blind polygraphic study in 8 healthy volunteers. A baseline placebo was given on Nights 1-3, followed either by 10 mg or 20 mg of the drug ...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00606405

    authors: Kayed K,Hansen T,Godtlibsen OB

    更新日期:1977-03-11 00:00:00

  • Effects of FCE20700, a new PGE2 derivative, on gastric acid secretion and cytoprotective processes in man.

    abstract::The pharmacodynamic effects of FCE20700, a new PGE2 derivative, have been investigated in 6 healthy volunteers given single intragastric (i.g.) and intraduodenal (i.d.) doses of 1 and 2 mg and placebo, according to a double-blind, within-subjects design. For 30-270 min following i.g. administration the effect of FCE20...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00606626

    authors: Caldara R,Guslandi M,Carbone M,Masci E,Cantù A,Ferrari C,Barbieri C,Dubini A

    更新日期:1987-01-01 00:00:00

  • Association of in-hospital intensive statins dosage and death in arteriosclerotic cardiovascular disease with percutaneous coronary intervention: insights of multicentre cohort from China.

    abstract:PURPOSE:In-hospital statin dosage-related effect remains unknown for patients with arteriosclerotic cardiovascular disease (ASCVD). This study aimed to determine the associations of different in-hospital intensive statins dosages with the prognosis for patients in the era of percutaneous coronary intervention (PCI). M...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-020-02966-1

    authors: Chen PY,Liu YH,Duan CY,Fan HL,Zeng LH,Guo W,Jiang L,Wei XB,He WF,Tao S,Guo ZQ,Chen JY,Tan N,He PC

    更新日期:2020-12-01 00:00:00

  • Expression of fibroblast growth factor receptor 4 and clinical response to lenvatinib in patients with anaplastic thyroid carcinoma: a pilot study.

    abstract:PURPOSE:Fibroblast growth factor receptor 4 (FGFR4) expression has association with tumor malignancy. In thyroid cancers, FGFR4 has been reported to be characteristically expressed in aggressive thyroid tumors, such as anaplastic thyroid carcinoma (ATC). METHODS:We investigated FGFR4 expression in patients with ATC an...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-020-02842-y

    authors: Yamazaki H,Yokose T,Hayashi H,Iwasaki H,Osanai S,Suganuma N,Nakayama H,Masudo K,Rino Y,Masuda M

    更新日期:2020-05-01 00:00:00

  • Modelling circadian variation in the pharmacokinetics of non-steroidal anti-inflammatory drugs.

    abstract::A one-compartment model with first-order absorption has provided good fits to five sets of indomethacin data and four sets of ketoprofen data taken at different times of day. There was substantial variation in the model parameters with time of administration and most of the features of this variation applied equally t...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00265955

    authors: Aronson JK,Chappell MJ,Godfrey KR,Yew MK

    更新日期:1993-01-01 00:00:00

  • Elevated serum parathyroid hormone concentration during treatment with high ceiling diuretics.

    abstract::Serum concentrations of parathyroid hormone (s-PTH) calcium, phosphorus and alkaline phosphatase were measured during treatment with furosemide or bumetanide for congestive heart failure. Significant elevations both of s-PTH and alkaline phosphatase were found, whereas serum calcium concentration was decreased. The ch...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00561397

    authors: Elmgreen J,Tougaard L,Leth A,Christensen MS

    更新日期:1980-10-01 00:00:00

  • Capecitabine plus oxaliplatin (XELOX) compared with 5-fluorouracil/leucovorin plus oxaliplatin (FOLFOXs) in advanced gastric cancer: meta-analysis of randomized controlled trials.

    abstract:PURPOSE:The study aims to compare the efficacy and safety of capecitabine plus oxaliplatin (XELOX) with 5-fluorouracil/leucovorin plus oxaliplatin (FOLFOXs) in patients with advanced gastric cancer. METHODS:Five databases were searched up to June 2014, without language restrictions. The outcomes included overall respo...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章,meta分析

    doi:10.1007/s00228-015-1828-9

    authors: Xu HB,Huang F,Su R,Shen FM,Lv QZ

    更新日期:2015-05-01 00:00:00

  • Trends in paediatric macrolide use in five European countries-a population-based study.

    abstract:PURPOSE:The study aims to analyse overall as well as subgroup-specific outpatient paediatric macrolide use in five European countries, including time trends of macrolide prescription rates, and to provide potential targets for future interventions aiming to promote judicious macrolide use. METHODS:Macrolide prescripti...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/s00228-015-1870-7

    authors: Holstiege J,Enders D,Schink T,Innocenti F,Oteri A,Bezemer I,Kaguelidou F,Molokhia M,Poluzzi E,Puccini A,Ulrichsen SP,Sturkenboom MC,Trifirò G,Garbe E

    更新日期:2015-08-01 00:00:00

  • Combination therapy of essential hypertension with pindolol (Visken) and hydralazine.

    abstract::Thirty patients suffering from essential hypertension were treated successively with placebo, hydralazine alone, and pindolol (Visken) combined with hydralazine. Hydralazine caused a statistically significant reduction in blood pressure and an increase in pulse rate as compared with the placebo: palpitations were an i...

    journal_title:European journal of clinical pharmacology

    pub_type: 临床试验,杂志文章

    doi:10.1007/BF00614002

    authors: Persson I

    更新日期:1975-12-19 00:00:00

  • Chloroquine levels in blood during chronic treatment of patients with rheumatoid arthritis.

    abstract::Blood levels of racemic chloroquine and its main metabolites desethylchloroquine and bisdesethylchloroquine were measured in 29 patients treated chronically for rheumatoid arthritis. In six patients, the concentrations were followed during a one day dosage interval. There was considerable intersubject variability in t...

    journal_title:European journal of clinical pharmacology

    pub_type: 杂志文章

    doi:10.1007/BF00280130

    authors: Augustijns P,Geusens P,Verbeke N

    更新日期:1992-01-01 00:00:00