1. Pharmacokinetics of and short-term virologic response to low-dose 400-milligram once-daily raltegravir maintenance therapy
- Author
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Jintanat, Ananworanich, Meena, Gorowara, Anchalee, Avihingsanon, Stephen J, Kerr, Nadine, van Heesch, Chuleeporn, Khongpetch, Anuntaya, Uanithirat, Andrew, Hill, Kiat, Ruxrungtham, David M, Burger, and Noor van Ewijk-Beneken, Kolmer
- Subjects
Adult ,Male ,HIV Infections ,Pharmacology ,Drug Administration Schedule ,Raltegravir Potassium ,Cohort Studies ,Pharmacokinetics ,Medicine ,Humans ,Pharmacology (medical) ,Dosing ,HIV Integrase Inhibitors ,Aged ,Likelihood Functions ,Cross-Over Studies ,Dose-Response Relationship, Drug ,business.industry ,Body Weight ,Age Factors ,Half-life ,Liter ,Middle Aged ,Viral Load ,Raltegravir ,Thailand ,Crossover study ,Pyrrolidinones ,Infectious Diseases ,Area Under Curve ,HIV-1 ,RNA, Viral ,Regression Analysis ,Female ,business ,Poverty-related infectious diseases Infectious diseases and international health [N4i 3] ,Viral load ,Software ,medicine.drug ,Half-Life - Abstract
Because studies showed similar viral suppression with lower raltegravir doses and because Asians usually have high antiretroviral concentrations, we explored low-dose raltegravir therapy in Thais. Nineteen adults on raltegravir at 400 mg twice daily (BID) with HIV RNA loads of 0-12 ) was 15.6 mg/liter-h and the minimum plasma drug concentration ( C trough ) was 0.22 mg/liter; for raltegravir given at 800 mg QD, the AUC 0-24 was 33.6 mg/liter-h and the C trough was 0.06 mg/liter; and for raltegravir given at 400 mg QD, the AUC 0-24 was 18.6 mg/liter-h and the C trough was 0.08 mg/liter. The HIV RNA load was 0-24 for Westerners on raltegravir at 400 mg BID, Thais on the same dose had double the AUC 0-24 and those on raltegravir at 400 mg QD had a similar AUC 0-24 . More patients had a C trough of C trough values. Low-dose raltegravir could be a cost-saving option for maintenance therapy in Asians or persons with low body weight. However, raltegravir at 400 mg QD was associated with a low C trough and with a risk for HIV viremia. Raltegravir at 200 or 300 mg BID should be studied, but new raltegravir formulations will be needed.
- Published
- 2012