Indinavir

Indications
 Oral
HIV infection
Adult: 800 mg every 8 hr. Dose reduction may be required when used with delavirdine, itraconazole, ketoconazole and rifabutin.
Child: >4 yr: 500 mg/m2 every 8 hr without exceeding adult dose.
Hepatic impairment: Mild-moderate (due to cirrhosis): 600 mg every 8 hr.
Contraindications
 Hypersensitivity. Severe hepatic impairment.
Warnings / Precautions
 Increased risk of urolithiasis/nephrolithiasis. Ensure adequate hydration. Hyperbilirubinaemia may be exacerbated. Diabetes; haemophilia. Monitor for signs of lipodystrophy. Pregnancy and lactation.
Adverse Reactions
 Flank pain, abdominal pain, nephrolithiasis, malaise, nausea, vomiting, diarrhoea, elevated liver enzymes, hyperbilirubinaemia, raised creatinine phosphokinase and blood lipids, back pain, lipodystrophy, alopecia, acid regurgitation, dyspepsia, dry mouth, dysuria, dry skin, hyperpigmentation, headache, dizziness, somnolence, cough, dyspnoea.
Potentially Fatal: Acute haemolytic anemia; acute hepatitis.
Overdose Reactions
 Symptoms: Renal and GI disturbances (doses >2400 mg). Management: Supportive and symptomatic.
Drug Interactions
 Reduced absorption with antacids. Increased concentrations with ketoconazole, delavirdine, nelfinavir and ritonavir. Reduced efficacy with nevirapine, efavirenz or rifampicin. Increased risk of myopathy with statins. Increased concentrations of phosphodiesterase-5 inhibitors.
Potentially Fatal: Increased risk of cardiac arrhythmias with amiodarone, pimozide or cisapride. Increased sedation and respiratory depression with midazolam, alprazolam and triazolam. Increased risk of ergotism with ergot derivatives. Increased toxicity of drugs with narrow therapeutic index.
See Below for More indinavir Drug Interactions
Food Interactions
 Reduced concentrations with grapefruit juice. Reduced antiviral response with St. John's wort.
Mechanism of Actions
 Indinavir binds reversibly to HIV-protease which prevents cleavage of the viral precursor polyproteins. As a result, immature viral particles incapable of infecting other cells are formed.
Absorption: Absorbed rapidly from the GIT (oral); peak plasma concentrations after 0.8 hr. May be reduced by intake of high-calorie meals.
Distribution: Protein-binding: 60%
Metabolism: Oxidation by CYP3A4 and glucuronidation.
Excretion: Via urine (<20%, half as unchanged drug), via faeces (remaining dose); 1.8 hr (elimination half-life).
Storage Conditions
 Oral: Store at 15-30°C (59-86°F).
ATC Classification
 J05AE02 - indinavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
Storage
 Oral: Store at 15-30°C (59-86°F).
Available As
  • Indinavir 400 mg

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