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Pharmacokinetic interaction between diltiazem and tolbutamide
1Centre for Biopharmaceutics and Pharmacokinetics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.
Drug Metabolism and Drug Interactions
|March 15, 2000
Summary
Co-administration of tolbutamide and diltiazem had no effect on diltiazem pharmacokinetics. Tolbutamide showed a minor increase in Cmax and AUC0-24 when given with diltiazem.
Area of Science:
- Pharmacology
- Drug Interactions
- Clinical Pharmacology
Background:
- Tolbutamide and diltiazem are commonly prescribed medications.
- Understanding potential drug-drug interactions is crucial for patient safety.
- Assessing the pharmacokinetic impact of co-administration is essential.
Purpose of the Study:
- To investigate the pharmacokinetic interaction between tolbutamide and diltiazem.
- To determine the effect of co-administration on the absorption, distribution, metabolism, and excretion of each drug.
Main Methods:
- A randomized crossover study involving eight healthy male volunteers.
- Oral administration of tolbutamide (500 mg) and diltiazem hydrochloride (60 mg) individually and concurrently.
- Serum drug concentrations measured by High-Performance Liquid Chromatography (HPLC).
- Pharmacokinetic analysis using a non-compartmental model.
Main Results:
- Diltiazem pharmacokinetics remained unchanged when co-administered with tolbutamide.
- Tolbutamide exhibited a modest increase of approximately 10% in AUC0-24 and Cmax in the presence of diltiazem.
- No significant alterations in diltiazem's pharmacokinetic profile were observed.
Conclusions:
- Co-administration of tolbutamide and diltiazem does not significantly alter diltiazem pharmacokinetics.
- A minor increase in tolbutamide exposure (AUC0-24, Cmax) occurs when given with diltiazem.
- These findings suggest a generally low pharmacokinetic interaction potential between these two drugs.