Indinavir

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Indinavir

Mechanism of action

• Competitive inhibitor of HIV protease
• preventing cleaving of gag & gag-pol protein precursors encoded by HIV genome in acutely & chronically infected cells,
• arresting maturation
• blocking infectivity of nascent virions.

Pharmacokinetics

• 65 % bioavailability with t_½ of 2 h.
• 60 – 65 % protein bound.
• Metabolised in the liver. However, it DOES NOT induce but inhibits hepatic cytochrome P _{450 3A4.}

Contra-indications

• breast-feeding

Side-effects

• Weakly active against human aspartyl-proteases.
• Gastrointestinal upset ( fewer than other protease inhibitors ).
• Hyperglycaemia.
• Hepatic dysfunction.
• Fat redistribution.

Drug interactions

• midazolam – increased prolonged sedation.
• terfenadine – risk of arrhythmias.
• ritonavir – increased indinavir [ plasma ] & thus greater toxicity.
• sildenafil – possibly increased sildenafil [ plasma ]

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