INDIVIR-400 400MG CAPSULE

Indications

• HIV-1 infection
• AIDS-related conditions

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Indinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Pharmacodynamics

Indinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). It binds to the active site of the HIV-1 protease enzyme, inhibiting its activity. This inhibition prevents the proteolytic cleavage of viral polyproteins, which is essential for the production of infectious virus. As a result, the formation of non-infectious viral particles occurs, contributing to decreased viral replication and overall viral load. Protease inhibitors like indinavir are typically used in combination with other antiretroviral medications to enhance efficacy and reduce the risk of resistance.

Pharmacokinetics

Indinavir is absorbed orally and reaches peak plasma concentrations typically within 1 to 2 hours after administration. It is metabolized primarily in the liver, involving cytochrome P450 3A4 enzymes. The elimination half-life of indinavir is approximately 1.5 to 2 hours, requiring multiple daily dosing to maintain therapeutic levels. The drug is excreted mainly through the feces and, to a lesser extent, in urine. The pharmacokinetics of indinavir can be influenced by food intake, with a high-fat meal decreasing its absorption.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Fatigue
• Nephrolithiasis (kidney stones)
• Hyperbilirubinemia
• Rash

Interactions

• Rifampicin may reduce indinavir levels
• Other protease inhibitors may lead to additive side effects
• Concomitant use with certain antifungals (e.g., ketoconazole) may increase indinavir levels

Precautions

• Renal impairment may require dose adjustment
• Monitor for signs of nephrolithiasis
• Caution in patients with hepatic impairment
• Regular liver function tests are recommended

Pregnancy

Indinavir is categorized as FDA pregnancy category C. Use should be considered only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Indinavir is excreted in human breast milk; therefore, a decision should be made to discontinue nursing or the drug, taking into account the importance of the drug to the mother.

Storage

Store at controlled room temperature (20 to 25 degrees Celsius), protect from moisture and light.

Formulations

• Capsules

Mechanism of action

Indinavir inhibits the HIV viral protease enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Pharmacodynamics

Indinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Indinavir 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 non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.