The effect of cimetidine and ranitidine administration with zidovudine.

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The effect of cimetidine and ranitidine administration with zidovudine.

Pharmacotherapy. 1995 Nov-Dec;15(6):701-8. Unique Identifier : AIDSLINE MED/96162732
Fletcher CV; Henry WK; Noormohamed SE; Rhame FS; Balfour HH Jr; Department of Pharmacy Practice, University of Minnesota Health; Sciences Center, Minneapolis 55455, USA.

Abstract: STUDY OBJECTIVE. To evaluate the possibility of a drug interaction with zidovudine and histamine2-receptor antagonists in individuals infected with the human immunodeficiency virus. DESIGN. Randomized crossover study. SETTING. University-affiliated research center. PATIENTS. Six HIV-infected individuals. INTERVENTIONS. The subjects received 7-day regimens of zidovudine 600 mg/day alone, zidovudine with cimetidine 1200 mg/day, and zidovudine with ranitidine 300 mg/day. MEASUREMENTS AND MAIN RESULTS. The renal clearance of zidovudine when given alone was 0.41 L/kg/hour, and was reduced to 0.18 L/kg/hour (p = 0.002) when given with cimetidine. In the presence of cimetidine the urinary excretion of zidovudine decreased from 89.5 to 53.7 microM (p = 0.01), the urinary ratio of metabolite to parent increased from 5.16 to 9.96 (p = 0.0001), and the fraction of zidovudine converted to metabolite increased from 0.86 to 0.92 (p = 0.0025). CONCLUSION. Cimetidine presumably inhibits the renal clearance of zidovudine by competing for tubular secretion. Based on the observation that neither cimetidine nor ranitidine had a significant effect on serum concentrations of zidovudine or zidovudine glucuronide, a change in the dosage of zidovudine is not warranted.

Keywords: Adolescence Adult Anti-Ulcer Agents/ADMINISTRATION & DOSAGE/*PHARMACOLOGY Antiviral Agents/*PHARMACOKINETICS/THERAPEUTIC USE Cimetidine/ADMINISTRATION & DOSAGE/*PHARMACOLOGY Cross-Over Studies CD4 Lymphocyte Count/*DRUG EFFECTS CD4-CD8 Ratio/DRUG EFFECTS Drug Interactions Histamine H2 Antagonists/ADMINISTRATION & DOSAGE/*PHARMACOLOGY Hospitals, University Human HIV Infections/DRUG THERAPY/METABOLISM Male Metabolic Clearance Rate Ranitidine/ADMINISTRATION & DOSAGE/*PHARMACOLOGY Support, Non-U.S. Gov't Support, U.S. Gov't, P.H.S. Zidovudine/ANALOGS & DERIVATIVES/BLOOD/*PHARMACOKINETICS/ THERAPEUTIC USE CLINICAL TRIAL JOURNAL ARTICLE RANDOMIZED CONTROLLED TRIAL
960730
M9670419

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