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Indications

REMS

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: MI.

F and E: LACTIC ACIDOSIS.

GI: exacerbation of hepatitis B, HEPATOMEGALY (WITH STEATOSIS), HEPATOTOXICITY ( WITH HEPATITIS B OR C).

Neuro: fatigue, headache, insomnia.
Misc: HYPERSENSITIVITY REACTIONS, immune reconstitution syndrome.

Interactions

Drug-Drug:

Drug-Natural Products:

Availability

(Generic available)

Route/Dosage

Tablets and tablets for oral suspension are NOT interchangeable on a milligram-per-milligram basis.

US Brand Names

Triumeq, Triumeq PD

Action

Therapeutic Effects:

Classifications

Therapeutic Classification: antiretrovirals (combination)

Pharmacologic Classification: integrase strand transfer inhibitors (INSTI) (dolutegravir), nucleoside reverse transcriptase inhibitors (abacavir, lamivudine)

Pharmacokinetics

Abacavir

Absorption: Rapidly and extensively (83%) absorbed.

Distribution: Distributes into extravascular space and readily distributes into erythrocytes.

Metabolism/Excretion: Mostly metabolized by the liver; 1.2% excreted unchanged in urine.

Half-life: 1.5 hr.

Dolutegravir

Absorption: Absorption follows oral administration; bioavailability is unknown.

Distribution: Enters CSF.

Protein Binding: >98.9%.

Metabolism/Excretion: Metabolized primarily by the UGT1A1 enzyme system with some metabolism by the CYP3A4 isoenzyme. 53% excreted unchanged in feces. Metabolites are renally excreted; minimal renal elimination of unchanged drug. Poor metabolizers of dolutegravir have levels and clearance.

Half-life: 14 hr.

Lamivudine

Absorption: Well absorbed after oral administration (86% in adults, 66% in infants and children).

Distribution: Distributes into the extravascular space. Some penetration into CSF; remainder of distribution unknown.

Metabolism/Excretion: Mostly excreted unchanged in urine; <5% metabolized by the liver.

Half-life: 13–19 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknownunknown24 hr

Patient/Family Teaching

Pronunciation

ah-BACK-ah-veer/doe-loo-TEG-ra-vir/la-MI-vyoo-deen