Probenecid Affects the Pharmacokinetics of Ofloxacin in Healthy Volunteers

Authors: Nataraj B.¹; Rao Mamidi N.V.S.¹; Krishna D.R.²

Source: Clinical Drug Investigation, Volume 16, Number 3, September 1998 , pp. 259-262(4)

Publisher: Adis International

Abstract:

Objective: The aim of this randomised, double-blind, crossover study was to evaluate the effect of single-dose probenecid on the pharmacokinetics of ofloxacin in eight healthy male volunteers.

Methods: After an overnight fast, and according to a randomised sequence, each volunteer received either single oral ofloxacin 200mg (Hoechst Marion Roussel Ltd., Mumbai, India) or both ofloxacin (1 × 200mg) and probenecid (1 × 500mg) [Geno Pharmaceutical Ltd., Mumbai, India]. Blood samples were collected at regular intervals until 24 hours. Serum concentration versus time profiles for ofloxacin were generated and pharmacokinetic parameters were calculated by noncompartmental model analysis.

Results: Elimination half-life, mean residence time and area under the curve were significantly increased (4.86 vs 5.26h; 7.23 vs 7.95h; 10.28 vs 11.9 mg/L · h) [p < 0.01], whereas the total clearance was decreased (19.66 vs 16.95 L/h) [p < 0.01] in the presence of probenecid. Other pharmacokinetic parameters were not significantly affected by coadministration of probenecid.

Conclusion: Concomitant administration of probenecid with ofloxacin may result in a decreased elimination half-life and consequently increased bioavailability of ofloxacin. Probenecid may be co-prescribed with ofloxacin; patients taking this combination should be closely monitored and dosage reduction should be considered if warranted in high-risk patients.

Keywords: Ofloxacin, drug-interactions; Drug-interactions; Randomised-controlled-trials; Probenecid, drug-interactions; Ofloxacin, pharmacokinetics; Antigouts, drug-interactions; Antibacterials, drug-interactions; Clinical-pharmacokinetics

Language: English

Document Type: Original article

Affiliations: 1: Drug Metabolism and Pharmacokinetic Laboratory, Dr Reddy's Research Foundation, Ameerpet, Hyderabad, India 2: Drug Metabolism Laboratory, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India *

Publication date: 1998-09-01

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• In this Subject: Pharmacology
• By this author: Nataraj B. ;  Rao Mamidi N.V.S. ;  Krishna D.R.

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