section name header

Pronunciation

bik-TEG-ra-vir/em-trye-SYE-ta-been/ten-OF-oh-veer al-a-FEN-a-mide

Classifications

Therapeutic Classification: antiretrovirals

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

Indications

REMS

Action

Therapeutic Effects:

Pharmacokinetics

Bictegravir

Absorption: Extent of absorption following oral administration unknown.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Primarily metabolized by the CYP3A4 isoenzyme and UGT1A1 in the liver; 60% excreted in feces, 35% excreted in urine.

Half-life: 17.3 hr;.

Emtricitabine

Absorption: Well absorbed (93%) following oral administration.

Distribution: Unknown.

Metabolism/Excretion: Undergoes some metabolism, 70% excreted in urine, 14% excreted in feces.

Half-life: 10.4 hr.

Tenofovir Alafenamide

Absorption: Tenofovir alafenamide is a prodrug, which is hydrolyzed into tenofovir, the active component; absorption enhanced by high-fat meals.

Distribution: Unknown.

Metabolism/Excretion: Tenofovir is phosphorylated to tenofovir diphosphate (active metabolite); 32% excreted in feces, <1% excreted in urine.

Half-life: Tenofovir alafenamide: 0.51 hr; Tenofovir diphosphate: 150–180 hr.

Time/Action Profile

(plasma concentrations)

ROUTEONSETPEAKDURATION
bictegravir POunknown2–4 hr24 hr
emtricitabine POunknown1.5–2 hr24 hr
tenofovir POunknown0.5–2 hr24 hr

Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

GI: amylase, liver enzymes, ACUTE EXACERBATION OF HBV, diarrhea, LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, nausea.

GU: ACUTE RENAL FAILURE/FANCONI SYNDROME.

Hemat: neutropenia.

Metab: hyperlipidemia.

MS: creatine kinase.

Neuro: abnormal dreams, dizziness, fatigue, headache, insomnia.
Misc: immune reconstitution syndrome.

Interactions

Drug-Drug:

Drug-Natural Products:

Route/Dosage

Renal Impairment

Availability

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Biktarvy