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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: QT interval prolongation

Derm: rash, pruritus, sweating

Endo: Graves' disease, hypercholesterolemia, hypertriglyceridemia

GI: nausea, abdominal pain, anorexia, autoimmune hepatitis, diarrhea, dyspepsia, flatulence, HEPATOTOXICITY

GU: hematuria, renal calculi

Metab: fat redistribution

MS: polymyositis

Neuro: Guillain-Barré syndrome, abnormal dreams, ataxia, catatonia, delusions, depression, dizziness, drowsiness, encephalopathy, fatigue, headache, hypoesthesia, impaired concentration, insomnia, nervousness, psychoses, SUICIDAL THOUGHTS/BEHAVIORS

Misc: immune reconstitution syndrome

Interactions

Drug-drug:

Drug-Food:

Availability

(Generic available)

Route/Dosage

Action

  • Inhibits HIV reverse transcriptase, which results in disruption of DNA synthesis.
Therapeutic effects:
  • Slowed progression of HIV infection and decreased occurrence of sequelae.
  • Increases CD4 cell counts and decreases viral load.

Classifications

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: non nucleoside reverse transcriptase inhibitors

Pharmacokinetics

Absorption: 50% absorbed when ingested following a high-fat meal.

Distribution: 99.5–99.75% bound to plasma proteins; enters CSF.

Metabolism/Excretion: Mostly metabolized by the liver via the CYP3A4 and CYP2B6 isonezymes. Excreted in urine and feces, primarily as metabolites.

Half-Life: Following single dose: 52–76 hr. Following multiple doses: 40–55 hr.

Canadian Brand Names

Sustiva

Time/Action Profile

(blood levels)

ROUTEONSETPEAKDURATION
POrapid3–5 hr24 hr

Patient/Family Teaching

Pronunciation

e-FAV-e-renz

Code

NDC Code