AMSDEN GW, FOULDS G; Interscience Conference on Antimicrobial Agents and Chemotherapy.
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2000 Sep 17-20; 40: 336.
Bassett Healthcare, Cooperstown, NY
BACKGROUND: Due to the common use of both agents in HIV infected patients, this study was done to characterize the potential for AZ to alter the PKs of NEL and/or its active metabolite, M8. A secondary objective was to characterize any effect that NEL may have on the PKs of AZ.METHODS: 12 healthy subjects were enrolled in this 2-way, open-label crossover study. During one study arm, subjects received a single 1200 mg dose of AZ. During the other, subjects received 11 days of NEL 750 mg q8h with a single 1200 mg oral dose of AZ given concurrently with the Day 9 morning NEL dose. Serum samples were collected after each AZ dose for 168 hours and after the Day 8 and 9 morning NEL doses for 8 hours to characterize AZ, NEL and M8 PK parameters during both control and test periods. Appropriate comparative statistical tests were conducted with significance defined as p # 0.05.RESULTS: 12 subjects (5M/7F, age 36.1+/-7.2 yrs., wgt 66.0+/-10.9 kg) completed the study. Regimens were well tolerated with mild/moderate GI symptoms being most frequently reported. AZ caused a statistically, not clinically, significant increase in NEL (24%) and M8 (23%) CLt/F and decrease in NEL (28%) and M8 (23%) AUC and NEL T[1/2] (23%). Also, NEL caused AZ Cmax and AUC values to increase >100%. Conclusion: While the decrease in NEL AUC is not thought to be of clinical significance, the increase in AUC of AZ may offer the potential to increase clinical efficacy without significantly increasing GI side effects. Further study of the mechanism and implications of this interaction is needed.KEYWORDS: Azithromycin; Nelfinavir; Pharmacokinetics
Publication Types:
Keywords:
- Acquired Immunodeficiency Syndrome
- Anti-HIV Agents
- Area Under Curve
- Azithromycin
- Drug Interactions
- HIV
- HIV Infections
- HIV Protease Inhibitors
- Humans
- Nelfinavir
- pharmacokinetics
Other ID:
UI: 102247126
From Meeting Abstracts