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Triazolam kinetics: interaction with cimetidine, propranolol, and the combination
H Friedman1, D J Greenblatt, E S Burstein
1Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts 02111.
Journal of Clinical Pharmacology
|March 1, 1988
Summary
Cimetidine significantly inhibits triazolam clearance, increasing its peak concentration and overall exposure. Propranolol does not affect triazolam kinetics or potentiate cimetidine’s effects.
Area of Science:
- Pharmacology
- Clinical Pharmacology
- Drug Interactions
Background:
- Triazolam is a commonly prescribed benzodiazepine.
- Understanding drug interactions is crucial for patient safety.
- Cimetidine and propranolol are frequently co-administered medications.
Purpose of the Study:
- To investigate the pharmacokinetic interaction between triazolam and cimetidine.
- To evaluate the effect of propranolol on triazolam pharmacokinetics.
- To determine the combined effect of cimetidine and propranolol on triazolam.
Main Methods:
- Healthy volunteers received oral triazolam alone and with cimetidine, propranolol, or both.
- Plasma triazolam concentrations were measured over 24 hours.
- Pharmacokinetic parameters including Cmax, AUC, and clearance were calculated.
Main Results:
- Cimetidine significantly increased triazolam's peak concentration (Cmax) and area under the curve (AUC), while decreasing oral clearance.
- Propranolol alone did not significantly alter triazolam pharmacokinetics.
- Combined cimetidine and propranolol yielded similar triazolam kinetics as cimetidine alone.
- Plasma free fraction of triazolam remained unchanged.
Conclusions:
- Cimetidine significantly inhibits triazolam clearance, leading to increased exposure.
- Propranolol does not affect triazolam clearance or potentiate cimetidine's inhibitory effect.
- These findings highlight the importance of considering cimetidine when prescribing triazolam.