Contraindicated in:
Use Cautiously in:
Derm: rash, ACUTE GENERALIZED EXANTHEMATOUS PUSTULOSIS, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN).
Endo: Graves' disease, hyperglycemia.
GI: abdominal pain, ACUTE EXACERBATION OF HBV, autoimmune hepatitis, diarrhea, flatulence, HEPATOTOXICITY, LACTIC ACIDOSIS/HEPATOMEGALY WITH STEATOSIS, nausea.
GU: Fanconi syndrome, acute renal failure, proximal renal tubulopathy.
Metab: body fat redistribution, hyperlipidemia.
MS: polymyositis.
Neuro: Guillain-Barré syndrome, fatigue, headache.
Misc: immune reconstitution syndrome.
Drug-Drug:
Drug-Natural Products:
Therapeutic Classification: antiretrovirals, pharmacoenhancers
Pharmacologic Classification: protease inhibitors, enzyme inhibitors, nucleoside reverse transcriptase inhibitors
Darunavir
Absorption: Food enhances oral absorption.
Distribution: Unknown.
Protein Binding: 95%.
Metabolism/Excretion: Extensively metabolized by the liver via the CYP3A isoenzyme; 41% excreted unchanged in feces, 8% in urine.
Half-life: 9.4 hr.
Cobicistat
Absorption: Absorption follows oral administration.
Distribution: Unknown.
Protein Binding: 9798%.
Metabolism/Excretion: Metabolized by the liver primarily by the CYP3A isoenzyme and to a lesser extent by the CYP2D6 isoenzyme; 86.2% excreted in feces, 8.2% in urine.
Half-life: 3.2 hr.
Emtricitabine
Absorption: 93% absorbed following oral administration.
Distribution: Unknown.
Metabolism/Excretion: Not significantly metabolized; 86% excreted in urine, 14% in feces.
Half-life: 7.5 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% in urine.
Half-life: 0.5 hr.
(plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
Darunavir (PO) | unknown | 3 hr | 24 hr |
Cobicistat (PO) | unknown | 3 hr | 24 hr |
Emtricitabine (PO) | rapid | 1.5 hr | 24 hr |
Tenofovir (PO) | unknown | 0.5 hr | 24 hr |