3/13/2019 Clinical pharmacokinetics of beta-agonists.

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Clin Pharmacokinet. 1990 Apr;18(4):270-94.

Clinical pharmacokinetics of beta-agonists.

Morgan DJ1.

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Abstract
The beta-agonists have found wide clinical use as racemic mixtures for 20 years, but information
on their pharmacokinetics is not comprehensive. They are well absorbed orally, but have low
systemic availability due to extensive first-pass sulphation. When administered by inhalation, very
little of the administered dose reaches the lungs, but the small amount that does produces
effective bronchodilatation. Plasma protein binding of most beta-agonists is negligible, and there
is substantial extravascular distribution of the administered dose. Elimination of intravenous drug
is predominantly renal, whereas oral doses are mostly eliminated by biotransformation. Renal
clearance correlates with creatinine clearance; therefore, dose reduction should be considered if
renal function is impaired, such as in the elderly or in cardiac failure. The elimination half-life of
most beta-agonists is relatively short, and pharmacokinetics are independent of dose and
duration of treatment. Differences in the pharmacokinetics of the enantiomers are evident. There
is very large variation in pharmacodynamic response for a given plasma beta 2-agonist
concentration among different subjects, and as treatment proceeds in an individual subject.
Therefore, in most cases therapeutic response and side effects are more useful for the monitoring
of beta 2-agonist treatment than measurement of plasma drug concentrations. The
pharmacokinetics of beta 2-agonists are not greatly altered in pregnancy although these agents
cause a marked reduction in maternal renal function. Placental transfer is relatively rapid, and
side effects are observed in fetus and neonate. Elimination may be somewhat faster in children (8
to 15 years) than in young adults. Asthma does not appear to influence the pharmacokinetics of
beta 2-agonists; the only recorded drug interaction of clinical significance is an increase in
theophylline clearance by intravenous isoprenaline (isoproterenol). Controlled release oral
preparations do not reduce side effects, but may improve compliance due to less frequent dosing.
The application of pharmacokinetic principles may improve the clinical usage of beta-agonists, at
least when they are used in premature labour and in cardiac failure.

PMID: 1969785 DOI: 10.2165/00003088-199018040-00002

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https://www.ncbi.nlm.nih.gov/pubmed/1969785 1/2
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https://www.ncbi.nlm.nih.gov/pubmed/1969785 2/2