Literature DB >> 8483846

Clinical pharmacokinetics and relative bioavailability of oral procaterol.

M A Eldon1, M M Battle, M J Coon, G D Nordblom, A J Sedman, W A Colburn.   

Abstract

The pharmacokinetics and relative oral bioavailability of procaterol, an orally active beta 2-adrenergic agonist bronchodilator were evaluated in healthy volunteers. Procaterol was rapidly absorbed after oral administration. Mean plasma procaterol concentration-time profiles and pharmacokinetic parameters for both formulations were essentially superimposable. Following tablet administration, the mean Cmax was 358 pg/mL and the corresponding mean tmax was 1.6 hr. Mean renal clearance was 163 mL/min and accounted for approximately one-sixth of the mean apparent oral plasma clearance (988 mL/min). The mean apparent elimination half-life of procaterol was 4.2 hr. Hepatic metabolism appears to be the primary mechanism for elimination of procaterol from the body, and first-pass metabolism may limit systemic bioavailability.

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Year:  1993        PMID: 8483846     DOI: 10.1023/a:1018966506819

Source DB:  PubMed          Journal:  Pharm Res        ISSN: 0724-8741            Impact factor:   4.200


  9 in total

1.  Metabolic fate of a new beta2-adrenergic stimulant procaterol (OPC-2009). Absorption, distribution, metabolism and excretion in the beagle dog.

Authors:  Y Yasuda; N Fujisawa; S Morita; H Kohri
Journal:  Arzneimittelforschung       Date:  1979

2.  Pharmacokinetics of procaterol in the rat, rabbit and beagle dog.

Authors:  M Ishigami; K Saburomaru; K Niino; M Kido; S Morita; G Miyamoto; H Kohri
Journal:  Arzneimittelforschung       Date:  1979

3.  The utility of a long-acting sympathomimetic agent, procaterol, for nocturnal asthma.

Authors:  R P Baughman; R G Loudon
Journal:  Chest       Date:  1988-02       Impact factor: 9.410

4.  A comparison of the two one-sided tests procedure and the power approach for assessing the equivalence of average bioavailability.

Authors:  D J Schuirmann
Journal:  J Pharmacokinet Biopharm       Date:  1987-12

5.  The metabolites of procaterol HCl in urine and faeces of dog and man.

Authors:  T Shimizu; H Mori; E Tabusa; K Nakagawa
Journal:  Xenobiotica       Date:  1978-11       Impact factor: 1.908

6.  A placebo-controlled trial of procaterol: a new long-acting oral beta 2-agonist in bronchial asthma.

Authors:  S C Siegel; R M Katz; G S Rachelefsky; M L Brandon; L A Borgen
Journal:  J Allergy Clin Immunol       Date:  1985-06       Impact factor: 10.793

7.  [Pharmacological properties of procaterol, a newly synthetized, specific beta 2-adrenoceptor stimulant. Part I. Effects on the CNS (author's transl)].

Authors:  K Hashimoto; S Shintani; S Yamashita; S Tei; M Takai; M Tsutsui; K Kawamura; T Ohkawa; T Hiyama; Y Yabuuchi
Journal:  Nihon Yakurigaku Zasshi       Date:  1979-04-20

8.  [Pharmacological properties of procaterol, a newly synthesized, specific beta 2-adrenoceptor stimulant. Part II. Effects on the peripheral organs (author's transl)].

Authors:  K Hashimoto; S Shintani; S Yamashita; S Tei; M Takai; M Tsutsui; K Kawamura; T Ohkawa; T Hiyama; Y Yabuuchi
Journal:  Nihon Yakurigaku Zasshi       Date:  1979-05

9.  Efficacy and duration of action of procaterol, a new bronchodilator.

Authors:  C L Zanetti; H H Rotman; A J Dresner
Journal:  J Clin Pharmacol       Date:  1982 May-Jun       Impact factor: 3.126

  9 in total

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