Trade Names:Crixivan- Capsules 100 mg- Capsules 200 mg- Capsules 333 mg- Capsules 400 mg
Inhibits human immunodeficiency virus (HIV) protease, the enzyme that cleaves viral polyprotein precursors into functional proteins in HIV-infected cells. Inhibition of this enzyme by indinavir results in formation of immature noninfectious viral particles.
T max is approximately 0.8 h (fasting). C max is approximately 12,617 nanomolars. The AUC at steady state is approximately 30,691 nanomolars•h. Administration with a high calorie, fat, and protein meal reduced AUC approximately 77% and C max approximately 84%.
60% is protein bound.
There are 7 metabolites: 1 glucuronide conjugate and 6 oxidative metabolites. CYP3A4 is major enzyme responsible for formation of oxidative metabolites.
The t ½ is approximately 1.8 h. Approximately 83% is excreted in the urine and approximately 19% in the feces.
Mild to moderate: decreased metabolism resulting in an approximate increase in AUC of 60% and increased t ½ to approximately 2.8 h.Children
AUC and C max slightly increased and trough concentration were considerably lower.Gender
Females have decreased AUC (13%) and C max (13%).
Treatment of HIV infection in combination with other antiretroviral agents.
Concomitant therapy with amiodarone, cisapride, ergot derivatives, midazolam, pimozide, or triazolam; hypersensitivity to any component of product.
PO 800 mg (two 400 mg capsules) every 8 h.Dosage Adjustment in Hepatic InsufficiencyAdults
PO Mild-to-moderate hepatic insufficiency caused by cirrhosis: 600 mg every 8 h.
Store in original container with desiccant at controlled room temperature (59° to 86°F). Keep tightly closed. Store unit-dose packages at controlled room temperature. Protect from moisture.
Because of potential life-threatening reactions, concomitant use with indinavir is contraindicated.Antiarrhythmic agents (eg, bepridil, quinidine, systemic lidocaine)
Concentrations of these agents may be elevated; monitoring of antiarrhythmic agent concentration is recommended.Anticonvulsant agents (carbamazepine, phenobarbital, phenytoin)
Indinavir concentrations may be decreased, reducing the therapeutic effect.Atazanavir
Coadministration with indinavir is not recommended because both agents are associated with indirect hyperbilirubinemia.Atorvastatin
Atorvastatin concentration may be elevated.Clarithromycin
Plasma concentration may be elevated by indinavir, increasing the risk of adverse effects.Clarithromycin, nelfinavir, ritonavir
Indinavir concentrations may be increased; the appropriate dose of indinavir is not known.Cyclosporine, sirolimus, tacrolimus
Plasma concentrations may be elevated by indinavir, increasing the therapeutic and adverse effects.Delavirdine, itraconazole, ketoconazole
Indinavir dosage reduction (600 mg every 8 h) should be considered because concentrations may be elevated.Didanosine
Administration of indinavir and didanosine formulations containing buffer should be separated by at least 1 h and given on an empty stomach.Dihydropyridine calcium channel blockers (eg, felodipine, nicardipine, nifedipine)
Concentrations of these agents may be increased by indinavir; clinical monitor is recommended.Efavirenz, nevirapine
Indinavir concentration may be reduced; the optimal dose of indinavir is not known.HMG-CoA Reductase inhibitors (eg, lovastatin, simvastatin)
Coadministration with indinavir is not recommended because of increased risk of myopathy including rhabdomyolysis.Rifabutin
When coadministered with indinavir, a dose reduction of rifabutin to 50% the standard dose and an increase of indinavir to 1,000 mg every 8 h is recommended.Rifampin, St. John's wort
Coadministration is not recommended because indinavir serum levels may be reduced, decreasing the clinical effect and possibly leading resistance to indinavir or the class of protease inhibitors.Ritonavir, saquinavir
Concentrations of these medications may be increased.Sildenafil, tadalafil, vardenafil
Indinavir may increase concentrations of these agents; dosage reduction is necessary.
None well documented.
Angina pectoris, cerebrovascular disorder, MI (postmarketing).
Headache (5%); dizziness (3%); asthenia/fatigue, malaise, somnolence (2%); oral paresthesia, depression (postmarketing).
Pruritus (4%); rash (1%); erythema multiforme, Stevens Johnson syndrome, hyperpigmentation, alopecia, ingrown toenails, paronychia (postmarketing).
Taste perversion (3%).
Abdominal pain (17%); nausea (12%); vomiting (8%); acid regurgitation, anorexia, diarrhea (3%); increased appetite, dyspepsia (2%); abdominal distension (postmarketing).
Nephrolithiasis/urolithiasis (9%); dysuria (2%); renal insufficiency, acute renal failure, pyelonephritis with or without bacteremia, interstitial nephritis sometimes with indinavir crystal deposits, crystalluria, dysuria (postmarketing).
Anemia (1%); increased spontaneous bleeding in patients with hemophilia (postmarketing).
Jaundice (2%); liver function abnormalities, hepatitis, hepatic failure, pancreatitis (postmarketing).
Anaphylactoid reactions, urticaria, vasculitis (postmarketing).
Increased serum bilirubin (12%); increased ALT (5%); increased AST (4%); decreased neutrophils, increased serum amylase (2%); decreased hemoglobin, decreased platelet count, increased glucose (1%); increased serum cholesterol and triglycerides (postmarketing).
New onset diabetes mellitus, exacerbation of preexisting diabetes mellitus, hyperglycemia (postmarketing).
Back pain (8%); arthralgia (postmarketing).
Fever (2%); redistribution/accumulation of body fat (postmarketing).
Category C .
Undetermined. HIV-infected mothers should not breast-feed to avoid risking potential transmission of HIV to infant.
Safety and efficacy not established.
Dose selection should be cautious, reflecting greater frequency of decreased hepatic, renal, or cardiac function.
Redistribution/accumulation of body fat including central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance have been reported.
Acute hemolytic anemia, including cases resulting in death, have been reported. Discontinue indinavir and treat appropriately if hemolytic anemia occurs.
Spontaneous bleeding and increased need for factor VIII has been reported in patients with hemophilia A and B treated with protease inhibitors.
Lower indinavir doses may be required because indinavir is hepatically metabolized.
Hepatitis, including cases resulting in death, have been reported during treatment with indinavir.
Indirect hyperbilirubinemia has occurred frequently during treatment with indinavir; increases in serum transaminases has occurred infrequently.
New onset diabetes mellitus, exacerbation of preexisting diabetes, and hyperglycemia have been reported in patients receiving protease inhibitor therapy.
Has been reported in patients treated with combination antiretroviral therapy.
Has occurred, more commonly in pediatric than adult patients. Temporarily interrupt therapy (eg, 1 to 3 days) if signs or symptoms of nephrolithiasis/urolithiasis occur (flank pain, with or without hematuria or microscopic hematuria).
Tubulointerstitial nephritis with medullary calcification and cortical atrophy have been reported in patients with asymptomatic severe leukocyturia (greater than 100 cells/high power field). Follow patients closely, frequently monitor with urinalysis, and consider discontinuing indinavir in patients who develop asymptomatic severe leukocyturia.
Nephrolithiasis/urolithiasis, flank pain, hematuria, nausea, vomiting, diarrhea.
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