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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Derm: rash ( in women and children)

Endo: hyperglycemia

GI: abdominal pain, diarrhea, nausea, vomiting, HEPATOTOXICITY

Hemat: bleeding

Metab: fat redistribution, hypercholesterolemia, hypertriglyceridemia

Neuro: fatigue, headache, INTRACRANIAL HEMORRHAGE

Misc: fever, immune reconstitution syndrome

Interactions

Drug-drug:

Drug-Natural Products:

Availability

Route/Dosage

US Brand Names

Aptivus

Action

  • Inhibits processing of viral polyproteins, preventing formation of mature virions.
Therapeutic effects:

Classifications

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: protease inhibitors

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unknown.

Protein Binding: >99.9%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme; requires coadministration with ritonavir as a metabolic inhibitor to achieve therapeutic blood levels; eliminated mostly in feces, minimal renal excretion.

Half-Life: 5.5–6 hr.

Time/Action Profile

(plasma concentrations*)

ROUTEONSETPEAKDURATION
POrapid2 hr12 hr

* With ritonavir.



Patient/Family Teaching

Pronunciation

ti-PRAN-a-veer