Effect of calcium channel blockers on theophylline disposition

Susan M. Sirmans, John A. Pieper, Richard L. Lalonde, David G. Smith, Timothy H. Self

Research output: Contribution to journalArticle

32 Citations (Scopus)

Abstract

Twolve healthy subjects received a single oral dose of theophylline, 5 mg/kg alone, and after 7 days of oral verapamil, 120 mg every 8 hours, diltiazem, 90 mg every 8 hours, and nifedipine, 20 mg every 8 hours, in randomized crossover fashion. Mean theophylline oral clearance decreased 18% and 12% after verapamil and diltiazem, respectively (p < 0.05). No significant change in theophylline oral clearance was observed after nifedipine. Increases in mean theophylline half-life were observed after verapamil (10.8 ± 3.2 hours) and diltiazem (9.9 ± 2.4 hours) (p < 0.05) but not after nifedipine (8.6 ± 2.4 hours) when compared with control (8.6 ± 1.9 hours). Apparent volume of distribution was unchanged. Urinary excretion data showed that the relative formation rate constants of 3-methylxanthine and 1,3-dimethyluric acid were: decreased during verapamil and diltiazem (p < 0.05) but not during nifedipine. No change in 1-methyluric acid excretion was observed. Increases in urinary elimination of unchanged theophylline were observed after verapamil, diltiazem, and nifedipine. The modest reduction in theophylline clearance observed after verapamil and diltiazem is not likely to produce clinically significant increases in theophylline concentrations in most patients.

Original languageEnglish (US)
Pages (from-to)29-34
Number of pages6
JournalClinical Pharmacology and Therapeutics
Volume44
Issue number1
DOIs
StatePublished - Jan 1 1988

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Calcium Channel Blockers
Theophylline
Diltiazem
Verapamil
Nifedipine
Half-Life
Healthy Volunteers

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

Cite this

Sirmans, S. M., Pieper, J. A., Lalonde, R. L., Smith, D. G., & Self, T. H. (1988). Effect of calcium channel blockers on theophylline disposition. Clinical Pharmacology and Therapeutics, 44(1), 29-34. https://doi.org/10.1038/clpt.1988.108

Effect of calcium channel blockers on theophylline disposition. / Sirmans, Susan M.; Pieper, John A.; Lalonde, Richard L.; Smith, David G.; Self, Timothy H.

In: Clinical Pharmacology and Therapeutics, Vol. 44, No. 1, 01.01.1988, p. 29-34.

Research output: Contribution to journalArticle

Sirmans, SM, Pieper, JA, Lalonde, RL, Smith, DG & Self, TH 1988, 'Effect of calcium channel blockers on theophylline disposition', Clinical Pharmacology and Therapeutics, vol. 44, no. 1, pp. 29-34. https://doi.org/10.1038/clpt.1988.108
Sirmans, Susan M. ; Pieper, John A. ; Lalonde, Richard L. ; Smith, David G. ; Self, Timothy H. / Effect of calcium channel blockers on theophylline disposition. In: Clinical Pharmacology and Therapeutics. 1988 ; Vol. 44, No. 1. pp. 29-34.
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