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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: pruritus

GI: HEPATOTOXICITY ( WITH HEPATITIS B OR C)

GU: renal impairment

MS: myositis

Neuro: headache, insomnia, fatigue

Misc: hypersensitivity reactions (including rash, constitutional symptoms, and liver injury), immune reconstitution syndrome

Interactions

Drug-drug:

Drug-Natural Products:

Availability

(Generic available)

Route/Dosage

Tablets (Tivicay) and tablets for oral suspension (Tivicay PD) are not interchangeable.

US Brand Names

Tivicay, Tivicay PD

Action

  • Inhibits HIV-1 integrase, which is required for viral replication.
Therapeutic effects:
  • Evidence of decreased viral replication and reduced viral load with slowed progression of HIV and its sequelae.

Classifications

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: integrase strand transfer inhibitors (INSTI)

Pharmacokinetics

Absorption: 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 UGT1A1 metabolizers have dolutegravir concentrations and an risk of adverse effects.

Half-Life: 14 hr

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown2–3 hr12–24 hr

Depends on concurrent use of metabolic inducers.

Patient/Family Teaching

Pronunciation

doe-loo-TEG-ra-vir

Code

NDC Code