Crixivan (indinavir sulfate)
Treatment of HIV infection in combination w/ other antiretroviral agents.
Combination w/ Other Antiretrovirals:
Consider dose reduction to 600mg q8h when administering delavirdine 400mg tid
Administer at least 1 hr apart on an empty stomach
Reduce dose to 600mg q8h when administering itraconazole 200mg bid
Reduce dose to 600mg q8h when administering ketoconazole
Reduce rifabutin dose to half the standard dose and increase indinavir dose to 1000mg q8h
Mild-to-Moderate Insufficiency Due to Cirrhosis:
Reduce dose to 600mg q8h
May temporarily interrupt (eg, 1-3 days) or d/c therapy
Administer w/o food but w/ water 1 hr ac or 2 hrs pc
May administer w/ other liquids (eg, skim milk, juice, coffee, tea) or w/ a light meal
Drink at least 1.5L of liquids during the course of 24 hrs to ensure adequate hydration
Cap: 200mg, 400mg
Coadministration w/ CYP3A4 substrates for which elevated concentrations potentially cause serious or life-threatening reactions (eg, alfuzosin, amiodarone, dihydroergotamine, ergonovine, ergotamine, methylergonovine, cisapride, lovastatin, simvastatin, pimozide, sildenafil [for treatment of pulmonary arterial HTN], oral midazolam, triazolam, alprazolam).
Nephrolithiasis/urolithiasis reported. Ensure adequate hydration in all patients. Acute hemolytic anemia, including cases resulting in death, reported; once a diagnosis is apparent, institute appropriate measures, including discontinuation of therapy. Hepatitis, including cases resulting in hepatic failure and death, reported. New onset or exacerbation of diabetes mellitus (DM), hyperglycemia, and diabetic ketoacidosis reported; initiation or dose adjustments of insulin or oral hypoglycemic agents may be required. Indirect hyperbilirubinemia reported frequently during treatment, and infrequently associated w/ increases in serum transaminases. Tubulointerstitial nephritis w/ medullary calcification and cortical atrophy observed in patients w/ asymptomatic severe leukocyturia (>100 cells/high power field); closely follow patients w/ asymptomatic severe leukocyturia and monitor frequently w/ urinalyses. Consider discontinuation of therapy in all patients w/ severe leukocyturia. Immune reconstitution syndrome reported. Autoimmune disorders (eg, Graves' disease, polymyositis, Guillain-Barre syndrome) reported in the setting of immune reconstitution and can occur many months after initiation of treatment. Spontaneous bleeding in patients w/ hemophilia A and B reported. Redistribution/accumulation of body fat reported. Caution in elderly.
Nephrolithiasis/urolithiasis, hyperbilirubinemia, abdominal pain, headache, N/V, dizziness, pruritus, diarrhea, back pain.
See Contraindications and Dose Modification. Caution w/ atorvastatin, rosuvastatin, parenteral midazolam, sildenafil (for treatment of erectile dysfunction), tadalafil, or vardenafil. Do not coadminister w/ rifampin. Not recommended w/ St. John's wort, atazanavir, salmeterol, or fluticasone (when indinavir is coadministered w/ a potent CYP3A4 inhibitor [eg, ritonavir]). Avoid w/ colchicine in patients w/ renal/hepatic impairment. May increase levels of CYP3A/CYP3A4 substrates, ritonavir, saquinavir, antiarrhythmics, trazodone, colchicine, quetiapine, dihydropyridine calcium channel blockers, clarithromycin, bosentan, atorvastatin, rosuvastatin, immunosuppressants, salmeterol, fluticasone, parenteral midazolam, rifabutin, sildenafil, tadalafil, and vardenafil. CYP3A/CYP3A4 inducers, St. John's wort, efavirenz, nevirapine, anticonvulsants, rifabutin, and venlafaxine may decrease levels. CYP3A/CYP3A4 inhibitors, delavirdine, nelfinavir, ritonavir, clarithromycin, itraconazole, and ketoconazole may increase levels. Refer to PI for dosing modifications when used w/ certain concomitant therapies.
PREGNANCY AND LACTATION
Category C, not for use in nursing.
MECHANISM OF ACTION
HIV-1 protease inhibitor; binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious viral particles.
Absorption: Rapid (fasted). Cmax=12,617nM; Tmax=0.8 hrs; AUC=30,691nM•hr. Distribution: Plasma protein binding (60%). Metabolism: Oxidation (via CYP3A4 [major]) and glucuronide conjugation. Elimination: Urine (<20%, unchanged); T1/2=1.8 hrs.
Assess for hypersensitivity to drug, hepatic insufficiency, DM, hemophilia, pregnancy/nursing status, and possible drug interactions.
Monitor for nephrolithiasis/urolithiasis, hemolytic anemia, hepatitis, new onset or exacerbation of DM, hyperglycemia, diabetic ketoacidosis, hyperbilirubinemia, serum transaminase elevations, immune reconstitution syndrome, autoimmune disorders, fat redistribution/accumulation, and other adverse reactions. Closely follow patients w/ asymptomatic severe leukocyturia and monitor frequently w/ urinalyses. In patients w/ hemophilia, monitor for bleeding events.
Instruct to take drug ud. Inform that drug is not a cure for HIV-1 infection and that illnesses associated w/ HIV may continue. Advise to avoid doing things that can spread HIV to others. Instruct not to modify or d/c therapy w/o consulting physician. Instruct to report to physician the use of any other prescription/nonprescription medication or herbal products (eg, St. John's wort). Inform that fat redistribution/accumulation may occur. Instruct to notify physician if pregnant or nursing.
15-30°C (59-86°F). Protect from moisture.
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