Therapeutic Classification: antiretrovirals
Pharmacologic Classification: nucleoside reverse transcriptase inhibitors, integrase strand transfer inhibitors (INSTI)
REMS
Bictegravir
Absorption: Extent of absorption following oral administration unknown.
Distribution: Unknown.
Protein Binding: >99%.
Half-Life: 17.3 hr;
Emtricitabine
Absorption: Well absorbed (93%) following oral administration.
Distribution: Unknown.
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.
Half-Life: Tenofovir alafenamide: 0.51 hr; Tenofovir diphosphate: 150180 hr.
(plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
bictegravir PO | unknown | 24 hr | 24 hr |
emtricitabine PO | unknown | 1.52 hr | 24 hr |
tenofovir PO | unknown | 0.52 hr | 24 hr |
Contraindicated in:
Use Cautiously in:
GI: ↑amylase, ↑liver enzymes, ACUTE EXACERBATION OF HBV, diarrhea, LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, nausea
GU: ACUTE RENAL FAILURE/FANCONI SYNDROME
Hemat: neutropenia
MS: ↑creatine kinase
Neuro: abnormal dreams, dizziness, fatigue, headache, insomnia
Misc: immune reconstitution syndrome
Drug-drug:
Drug-Natural Products:
Renal Impairment
Lab Test Considerations: