Indinavir sulfate
Indinavir sulfate
Indinavir sulfate
(in- DIN-ah-veer)
Pregnancy Category: C Crixivan (Rx)

Classification: Antiviral drug, protease inhibitor

See Also: See also Anitiviral Drugs .

Action/Kinetics: Binds to active sites on the HIV protease enzyme resulting in inhibition of enzyme activity. Inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious viral particles. Varying degrees of cross resistance have been noted between indinavir and other HIV-protease inhibitors. Rapidly absorbed in fasting clients; time to peak plasma levels: Approximately 0.8 hr. Administration with a meal high in calories, fat, and protein results in a significant decrease in the amount absorbed and in the peak plasma concentration. Approximately 60% bound to plasma proteins. t 1/2: 1.8 hr. Metabolized in the liver with both parent drug and metabolites excreted through the feces (over 80%) and the urine.

Uses: Treatment of HIV infection in adults when antiretroviral therapy is indicated. May be used with other anti-HIV drugs.

Contraindications: Lactation. Use with astemizole, cisapride, midazolam, rifampin, terfenadine, and triazolam. Mild to moderate liver or kidney disease.

Special Concerns: Not a cure for HIV infections; clients may continue to develop opportunistic infections and other complications of HIV disease. Not been shown to reduce the risk of transmission of HIV through sexual contact or blood contamination. No data on the effect of indinavir therapy on clinical progression of HIV infection, including survival or the incidence of opportunistic infections. Hemophiliacs treated for HIV infections with protease inhibitors may manifest spontaneous bleeding episodes. Safety and efficacy have not been determined in children.

Side Effects: GI: N&V;, diarrhea, abdominal pain, abdominal distention, acid regurgitation, anorexia, dry mouth, aphthous stomatitis, cheilitis, cholecystitis, cholestasis, constipation, dyspepsia, eructation, flatulence, gastritis, gingivitis, glossodynia, gingival hemorrhage, increased appetite, infectious gastroenteritis, jaundice, liver cirrhosis. CNS: Headache, insomnia, dizziness, somnolence, agitation, anxiety, bruxism, decreased mental acuity, depression, dream abnormality, dysesthesia, excitement, fasciculation, hypesthesia, nervousness, neuralgia, neurotic disorder, paresthesia, peripheral neuropathy, sleep disorder, tremor, vertigo. CV: CV disorder, palpitation. Musculoskeletal: Back pain, arthralgia, leg pain, myalgia, muscle cramps, muscle weakness, musculoskeletal pain, shoulder pain, stiffness. Body as a whole: Asthenia, fatigue, flank pain, malaise, chest pain, chills, fever, flu-like illness, fungal infection, malaise, pain, syncope. Hematologic: Anemia, lymphadenopathy, spleen disorder. Respiratory: Cough, dyspnea, halitosis, pharyngeal hyperemia, pharyngitis, pneumonia, rales, rhonchi, respiratory failure sinus disorder, sinusitis, URI. Dermatologic: Body odor, contact dermatitis, dermatitis, dry skin, flushing, folliculitis, herpes simplex, herpes zoster, night sweats, pruritus, seborrhea, skin disorder, skin infection, sweating, urticaria. GU: Nephrolithiasis, dysuria, hematuria, hydronephrosis, nocturia, PMS, proteinuria, renal colic, urinary frequency, UTI, uterine abnormality, urine sediment abnormality, urolithiasis. Ophthalmic: Accommodation disorder, blurred vision, eye pain, eye swelling, orbital edema. Miscellaneous: Asymptomatic hyperbilirubinemia, food allergy, taste disorder.

Laboratory Test Alterations: Serum transaminases (ALT, AST), total serum bilirubin, serum amylase. Hemoglobin, platelet count, neutrophils. Hyperbilirubinemia.

Drug Interactions: Aldesleukin / Plasma indinavir levels R/T liver metabolism Amiodarone / Possible amiodarone plasma levels R/T liver metabolism Astemizole / Astemizole metabolism possibility of cardiac arrhythmias and prolonged sedation Cisapride / Cisapride metabolism possibility of cardiac arrhythmias and prolonged sedation Clarithromycin / Plasma levels of both indinavir and clarithromycin Didanosine / pH Dependent in absorption Fluconazole / Plasma levels of indinavir Isoniazid / Plasma isoniazid levels Ketoconazole / Plasma levels of indinavir Midazolam / Midazolam metabolism possibility of cardiac arrhythmias and prolonged sedation Oral contraceptives / Plasma levels of both estrogen and progestin components of product Quinidine / Plasma indinavir levels Rifabutin / Plasma rifabutin levels; dose by 50% Rifampin / Plasma levels of indinavir Stavudine / Plasma stavudine levels Triazolam / Triazolam metabolism possibility of cardiac arrhythmias and prolonged sedation Trimethoprim/Sulfamethoxazole / Plasma levels of trimethoprim (no change in sulfamethoxazole levels) AZT / Plasma levels of both indinavir and AZT

How Supplied: Capsules: 200 mg, 333 mg, 400 mg.

Dosage
?Capsules HIV infections.
Adults: 800 mg (two 400-mg capsules) q 8 hr ATC. The dosage is the same whether the drug is used alone or in combination with other retroviral agents. Reduce the dose to 600 mg q 8 hr with mild to moderate hepatic insufficiency due to cirrhosis.