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- Title
Clinical Pharmacology Profile of Raltegravir, an HIV-1 Integrase Strand Transfer Inhibitor.
- Authors
Brainard, Diana M.; Wenning, Larissa A.; Stone, Julie A.; Wagner, John A.; Iwamoto, Marian
- Abstract
Raltegravir is an HIV-1 integrase inhibitor approved to treat HIV infection in adults in combination with other antiretrovirals. Data from healthy volunteers demonstrate that raltegravir is rapidly absorbed with a mean half-life of approximately 7 to 12 hours, with steady state achieved in approximately 2 days. Raltegravir is characterized by both high intra- and interindividual variabilities, although neither gender, race, age, body mass index, food intake, nor renal or hepatic insufficiency has a clinically meaningful effect on raltegravir pharmacokinetics. Raltegravir lacks activity as a perpetrator of drug–drug interactions and demonstrates a low propensity to be subject to drug–drug interactions. Raltegravir is metabolized primarily by UGT1A1 and is not affected by P450 inhibitors or inducers. Inhibitors of UGT1A1 (eg, atazanavir) can increase plasma concentrations of raltegravir, although this increase has not been found to be clinically meaningful. Likewise, inducers of UGT1A1 (eg, rifampin) can reduce plasma concentrations of raltegravir, and the clinical significance of this reduction is being investigated in ongoing clinical studies. Raltegravir demonstrates favorable clinical pharmacology and a drug interaction profile that permits administration to a wide, demographically diverse patient population and coadministration with many other therapeutic agents, including antiretroviral agents and supportive medications, without restrictions or dose adjustment.
- Subjects
AGE distribution; ANTI-infective agents; ANTIHISTAMINES; ANTIULCER drugs; ANTIVIRAL agents; BIOPHYSICS; CEREBROSPINAL fluid; COMBINATION drug therapy; CHRONIC kidney failure; DRUG interactions; DRUG monitoring; DRUG-food interactions; ENZYME inhibitors; EXANTHEMA; GENITALIA; GENETIC polymorphisms; HIV infections; IMMUNOSUPPRESSIVE agents; LIVER diseases; RESEARCH methodology; METHADONE hydrochloride; MIDAZOLAM; ORAL contraceptives; HEALTH outcome assessment; RACE; RIFAMPIN; SEX distribution; LAMOTRIGINE; PROTON pump inhibitors; PRAVASTATIN; PROTEASE inhibitors; BODY mass index; TREATMENT effectiveness; ABACAVIR; ATAZANAVIR; DARUNAVIR; ETRAVIRINE (Drug); FOSAMPRENAVIR (Drug); LOPINAVIR-ritonavir; MARAVIROC (Drug); RALTEGRAVIR; TENOFOVIR; TIPRANAVIR (Drug)
- Publication
Journal of Clinical Pharmacology, 2011, Vol 51, Issue 10, p1376
- ISSN
0091-2700
- Publication type
Article
- DOI
10.1177/0091270010387428