Tablets: 10 mg, 25 mg, and 50 mg.
In combination with other antiretroviral agents for the treatment of HIV-1 infections in adults and pediatric patients weighing at least 40 kg: 50 mg once daily.
In combination with other antiretroviral agents for the treatment of HIV-1 infection in pediatric patients weighing between 30-40 kg: 35 mg once daily.
In combination with rilpivirine as a complete regimen for the treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed on a stable antiretroviral regimen for at least 6 months: 50 mg once daily.
In patients who are coadministered with certain UGTIA or CYP3A4 inducers or who are INSTI resistant: 50 mg given twice daily.
Monitor: LFT, CD4+ cell count.
Pharmacology/Pharmacokinetics:
Dolutegravir inhibits the strand transfer activity of HIV-1 integrase which prevents the integration of HIV-1 DNA into host genomic DNA. This inhibition blocks the formation of the HIV-1 provirus and propagation of the viral infection. Resistance to integrase strand transfer inhibitors (INSTI) is possible and should be considered in treatment failures. After oral dosing, peak plasma levels are reached in 2-3 hours and steady state is reached in 5 days. Terminal half-life is approximately 14 hours. Metabolism is primarily via UGTA1A1 with 53% of an oral dose being excreted unchanged in the feces.
Drug Interactions:
Carbamazepine, oxcarbazepine, phenytoin, phenobarbital, rifampin, and St. John’s Wort will decrease concentration of dolutegravir. Coadministration with oral calcium, magnesium, aluminum, sucralfate, or iron supplements will decrease concentrations of dolutegravir. May increase concentration of metformin (dosage adjustment necessary). Will increase concentration of DOFETILIDE. Dosage increases of dolutegravir may be necessary when used with non-nucleoside reverse transcriptase inhibitors and protease inhibitors.
Contraindications/Precautions:
Contraindicated in patients receiving dofetilide. Do not use during the first trimester of pregnancy. Do not use in patients with severe hepatic impairment. Use may precipitate hepatitis B or C liver toxicity. Patients should be tested for hepatitis before initiating treatment.
Adverse Effects:
Rare cases of LIVER TOXICITY and IMMUNE RECONSTITUTION SYNDROME have occurred during use. The most common adverse effects are sleep disturbances, tiredness, and headache.
Do not take antacids or products containing calcium, zinc, or iron at the same time. Can be taken 2 hours before of 6 hours after these products.
Do not take St. John’s Wort with this medication.
If you miss a dose, take it as soon as you remember. If it is closer to the time of your next dose, skip the missed dose and carry on with your normal dosing schedule. Do not double doses.
Call your healthcare provider if you experience any symptoms of liver dysfunction (yellow eyes or skin, dark urine, light color stools, anorexia, stomach pain, or nausea).
This medication does not prevent you from transmitting HIV-1 to other people. Do not share needles, personal items that have blood or body fluids on them, and use a barrier protection (condom) during use.