Using Isentress in treatment-naïve adults with HIV-1

Approved for use in treatment-naïve adults with HIV-1

ISENTRESS can be used in adults with HIV-1: treatment-naïve or -experienced

ISENTRESS is used in combination with other antiretroviral (ARV) agents for the treatment of HIV-1 infection in adult patients
This indication is based on analyses of plasma HIV-1 RNA levels up through 48 weeks in 3 double-blind controlled studies of ISENTRESS. Two of these studies were conducted in clinically advanced, 3-class antiretroviral—nonnucleoside reverse transcriptase inhibitor (NNRTI), nucleoside reverse transcriptase inhibitor (NRTI), and protease inhibitor (PI)—treatment-experienced adults and 1 was conducted in treatment-naïve adults
The use of other active agents with ISENTRESS is associated with a greater likelihood of treatment response
The safety and efficacy of ISENTRESS have not been established in pediatric patients

For the treatment of patients with HIV-1 infection, the dosage of ISENTRESS is 400 mg administered orally, twice daily with or without food. During coadministration with rifampin, the recommended dosage of ISENTRESS is 800 mg twice daily with or without food

During the initial phase of treatment, patients responding to ARV therapy may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium complex, cytomegalovirus, Pneumocystis jiroveci pneumonia, Mycobacterium tuberculosis, or reactivation of varicella zoster virus), which may necessitate further evaluation and treatment
Coadministration of ISENTRESS with drugs that are strong inducers of uridine diphosphate glucuronosyltransferase (UGT) 1A1 may result in reduced plasma concentrations of raltegravir
Rifampin, a strong inducer of UGT1A1, reduces plasma concentrations of ISENTRESS. Therefore, the dose of ISENTRESS should be increased during coadministration with rifampin
The impact of other inducers of drug metabolizing enzymes, such as phenytoin and phenobarbital, on UGT1A1 is unknown
In drug interaction studies, raltegravir did not have a clinically meaningful effect on the pharmacokinetics of the following: hormonal contraceptives, methadone, lamivudine, tenofovir, etravirine
Coadministration of ISENTRESS with drugs that inhibit UGT1A1 may increase plasma levels of raltegravir
The most common adverse reactions of moderate to severe intensity^a (>2%) that occurred at a higher rate than the comparator were insomnia in treatment-naïve patients and headache, nausea, asthenia, and fatigue in treatment-experienced patients
Creatine kinase elevations were observed in subjects who received ISENTRESS. Myopathy and rhabdomyolysis have been reported; however, the relationship of ISENTRESS to these events is not known. Use with caution in patients at increased risk of myopathy or rhabdomyolysis, such as patients receiving concomitant medications known to cause these conditions
ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus
To monitor maternal-fetal outcomes of pregnant patients exposed to ISENTRESS, an Antiretroviral Pregnancy Registry has been established. Physicians are encouraged to register patients by calling 1-800-258-4263

Intensities were defined as follows: Moderate (discomfort enough to cause interference with usual activity); or Severe (incapacitating with inability to work or do usual activity).

Before prescribing ISENTRESS, please read the Prescribing Information and Patient Information.

For additional copies of the Prescribing Information, call 1-800-672-6372, visit isentress.com, or contact your Merck representative.