section name header

Pronunciation

ti-PRAN-a-veer

Classifications

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: protease inhibitors

Indications

REMS

Action

Therapeutic Effects:

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.

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:

Route/Dosage

Availability

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Aptivus