Indinavir information from DrugsUpdate  

Pharmacodynamics

Pharmacokinetics

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 hours. 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 hours (elimination half-life).

Indinavir Indications / Indinavir Uses

Information Not Available

Indinavir Adverse Reactions / Indinavir Side Effects

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.

Precautions

Information Not Available

Special Precautions

Increased risk of urolithiasis/nephrolithiasis. Ensure adequate hydration. Hyperbilirubinaemia may be exacerbated. Diabetes; haemophilia. Monitor for signs of lipodystrophy. Pregnancy and lactation.

Other 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.

Other Interactions

Food Interaction
Reduced concentrations with grapefruit juice. Reduced antiviral response with St. John's wort.

Dosage

Oral
HIV infection
Adult: 800 mg every 8 hours. Dose reduction may be required when used with delavirdine, itraconazole, ketoconazole and rifabutin.
Child: >4 years: 500 mg/m2 every 8 hours without exceeding adult dose.
Hepatic impairment: Mild-moderate (due to cirrhosis): 600 mg every 8 hours.

Food(before/after)

Information Not Available

Indinavir and Pregnancy

Caution when used during pregnancy

Indinavir and Lactation

Caution when used during lactation

Indinavir and Children

Safety and efficacy not established.

Indinavir and Geriatic

Dose selection should be cautious, reflecting greater frequency of decreased hepatic, renal, or cardiac function.

Indinavir and Other Contraindications

Hypersensitivity. Severe hepatic impairment.

Storage

Oral
Store at 15-30°C (59-86°F).

Lab interference

Oral
Store at 15-30°C (59-86°F).