Piscitelli S, Rock-Kress D, Bertz R, Pau A, Davey R; Conference on Retroviruses and Opportunistic Infections.
Program Abstr 6th Conf Retrovir Oppor Infect Conf Retrovir Oppor Infect 6th 1999 Chic Ill. 1999 Jan 31-Feb 4; 6th: 137 (abstract no. 373).
National Institutes of Health, Bethesda, MD.
Meperidine is a narcotic analgesic commonly used in HIV-infected patients for symptomatic relief of chills, rigors, and pain. Its use is contraindicated with the HIV protease inhibitor RTV, an inhibitor of CYP3A4 metabolism, because of the theoretical potential for increased meperidine concentrations. Eight HIV-negative subjects received a 50 mg oral dose of meperidine and had serial blood samples collected for 48 hours. Subjects then received 500 mg BID of RTV for 10 days followed by administration of a second 50 mg meperidine dose and collection of serial samples. Plasma samples were assayed by HPLC methods for meperidine, normeperidine, and RTV. Pharmacokinetic parameters of meperidine with and without ritonavir are shown below (mean +/- SD): (Table: see text) The AUC of meperidine decreased in all subjects by a mean of 67 +/- 4% in the presence of RTV (p < 0.005). Normeperidine mean AUC was increased 47% suggesting induction of hepatic metabolism. RTV exposure was similar to previous reports with 500 mg BID doses, CL/F averaged 5.6 L/h. Meperidine AUC is significantly reduced, not increased, by concomitant RTV. Based on these findings, the risk of narcotic-related adverse effects from this combination appears to be minimal. This suggests that contraindication of meperidine is not necessary during RTV therapy.
Publication Types:
Keywords:
- Accidents
- Acquired Immunodeficiency Syndrome
- Analgesics, Opioid
- Anti-HIV Agents
- Area Under Curve
- HIV
- HIV Envelope Protein gp41
- HIV Fusion Inhibitors
- HIV Infections
- HIV Protease Inhibitors
- Humans
- Meperidine
- Ritonavir
- immunology
- injuries
- normeperidine
Other ID:
UI: 102189029
From Meeting Abstracts