Classifications: antiviral agent; protease inhibitor; Therapeutic: antiviral; protease inhibitor
Pregnancy Category: C
100 mg, 200 mg, 333 mg, 400 mg capsules
Indinavir is an HIV protease inhibitor. HIV protease is an enzyme required to produce the polyprotein precursors of the
functional proteins in infectious HIV. Indinavir binds to the protease active site and thus inhibits activity of the enzyme.
Protease inhibitors prevent cleavage of the HIV viral polyproteins, resulting in formation of immature noninfectious virus
Treatment of HIV infection, usually in combination with other antiretroviral agents or protease inhibitors.
Hypersensitivity to indinavir; pregnancy (category C), lactation.
Hepatic dysfunction, renal impairment, history of nephrolithiasis, diabetes mellitus; history of adverse responses to other
protease inhibitors. Safety and efficacy in children are not established.
Route & Dosage
Adult: PO 800 mg (2 x 400 mg) q8h 1 h before or 2 h after meal
With ritonavir: 800 mg b.i.d. plus 100200 mg ritonavir b.i.d.
- Give with water on an empty stomach 1 h before or 2 h after meal; if needed, may be given with a very light meal or beverage.
- Note: When didanosine and indinavir are ordered concurrently, give each on empty stomach at least 1 h apart.
- Do not administer concurrently with midazolam or triazolam.
- Store tightly closed with desiccant in original bottle.
Adverse Effects (≥1%)CNS: Fatigue
, headache, insomnia
, dizziness, somnolence, nervousness, agitation, anxiety, paresthesia
, peripheral neuropathy
tremor, vertigo. CV:
Palpitations. Hematologic: Anemia
, lymphadenopathy. GI: Nausea, diarrhea
, abdominal discomfort, dyspepsia, stomatitis
, anorexia, dry mouth, cholecystitis, cholestasis, constipation
, flatulence. Skin:
Body odor, rash, pruritus, seborrhea, skin ulceration, dry skin, sweating, urticaria. Other:
Myalgia, allergic reaction, bronchitis
, cough, rhinitis, taste alterations, visual disturbances, hyperglycemia, diabetes
InteractionsDrug: Rifabutin, rifampin
significantly decrease indinavir levels. Ketoconazole
significantly increases indinavir levels. Indinavir could inhibit the metabolism
and increase the toxicity
of midazolam, sildenafil, tadalafil, trazodone, triazolam, vardenafil.
Indinavir and didanosine
should be administered at least 1 h apart on empty stomach to permit full absorption of each; increased ergotamine toxicity
with indinavir. Herbal: St. John's wort,
garlic decreases antiretroviral
activity of indinavir.
Rapidly absorbed from GI tract; a meal high in calories, fat, and protein significantly reduces absorption. Distribution:
60% protein bound. Metabolism:
In liver by cytochrome P4503A4 (CYP3A4). Elimination:
Primarily in feces (>80%), 20% in urine.
Assessment & Drug Effects
- Lab tests: Monitor CBC with differential and platelet count, liver function tests, CPK, urinalysis, and serum amylase periodically.
- Assess for S&S of renal dysfunction, respiratory dysfunction, GI distress, and other common adverse effects.
Patient & Family Education
- Learn drug interactions and potential adverse reactions. Drink plenty of liquids to minimize risk of renal stones.
- Notify physician of flank pain, hematuria, S&S of jaundice, or other distressing adverse effects.