Drug reference

Dolutegravir

Antiretroviral

Also known as Dolutegravir sodium, Tivicay

Antiretroviral

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Manufacturer advises avoid. New safety recommendations due to neural tube defects in babies born to mothers taking dolutegravir. Should not be prescribed to women trying to become pregnant; pregnancy should be excluded before starting. Women of childbearing potential should use effective contraception. If pregnancy is confirmed in the first trimester, switch to an alternative unless no suitable alternative exists.

FDA category + note

Top interactionssee all 12 →

St John S WortContraindicatedTextbookG&G 14e · p1245-1266
Aluminum HydroxideSevereDatabaseDDInter
ApalutamideSevereDatabaseDDInter
AttapulgiteSevereDatabaseDDInter

Mechanism

Dolutegravir is an integrase strand transfer inhibitor that blocks the HIV integrase enzyme. This action prevents the integration of viral DNA into the host cell's genome, thereby inhibiting viral replication.

Indications

HIV-1 infectionHIV-1 and HIV-2 infection in HIV-infected adults and children older than 4 weeks of age and weighing at least 3 kg

Dosing

Hepatic adjustment: Manufacturer advises caution in severe impairment—no information available.

Pharmacokinetics

Half-life

Bioavailability

—

Protein binding

98.9%

Metabolism

Chiefly through UDP glucuronosyltransferase (UGT) and cytochrome P450 enzymes.

Excretion

<1% (renal, unchanged)

Contraindications

Women who are trying to become pregnant (due to risk of neural tube defects). Pregnancy should be excluded in women of childbearing potential before starting treatment.

Side effects

Common

Anxietydepressiondiarrhoeadizzinessfatigueflatulencegastrointestinal discomfortheadachenauseaskin reactionssleep disordersvomitinglong-term weight gain

Serious

Arthralgia
hepatic disorders
hypersensitivity reactions (including severe rash, or rash accompanied by fever, malaise, arthralgia, myalgia, blistering, oral lesions, conjunctivitis, angioedema, eosinophilia, or raised liver enzymes)
immune reconstitution inflammatory syndrome
myalgia
suicidal tendencies
Osteonecrosis
neural tube defects (potential increased risk in infants of mothers taking dolutegravir at conception)
hypersensitivity reactions (rash, organ dysfunction)