Formulary Monographs [ELVITEGRAVIR, 08180812]
ELVITEGRAVIR
08180812
INTEGRASE INHIBITORS
The fixed combination of elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate (tenofovir DF) (EVG/c/FTC/TDF) is used for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral-naïve (have not previously received antiretroviral therapy) or antiretroviral-experienced (previously treated) adults and pediatric patients 12 years of age or older .
Lactic acidosis and hepatomegaly with steatosis, including fatalities, have been reported with Tenofovir DF in combination with other antiretrovirals; risk is increased in women, obese patients, prolonged exposure in patients with known risk for liver disease.
Elvitegravir is often given with a protease inhibitor, a pharmacokinetic enhancer such as low-dose ritonavir, and at least one other antiretroviral drug; the dose may need to be adjusted to manage drug interactions.
Drugs that induce these enzymes may decrease its plasma concentration and it should not be used with strong inducers of CYP3A which include the following:
antibacterials (rifampicin)
antidepressants (St John's Wort)
antiepileptics (carbamazepine, oxcarbazepine, phenobarbital, and phenytoin)
Moderate CYP3A inducers including efavirenz, nevirapine, and bosentan, should also be avoided.
Drugs that inhibit CYP3A, UGT1A1 or UGT1A3 may increase the plasma concentration of elvitegravir and when it is used with ritonavir-boosted atazanavir or lopinavir a lower dose is given, itself, is a modest inducer of CYP2C9 and may decrease the plasma
There are no or limited amount of data (less than 300 pregnancy outcomes) from the use of Stribild in pregnant women. However, a large amount of data in pregnant women (more than1,000 pregnancy outcomes) indicate no malformations or foetal/neonatal toxici
In order to avoid transmission of HIV to the infant it is recommended that HIV infected women do not breast-feed their infants under any circumstances.