Indinavir

CRIXIVAN

What it isHIV protease inhibitor; HIV.

Why this oneAn early potent protease inhibitor central to the first effective combination therapy.

What limits itNephrolithiasis requires high fluid intake, and dosing is three times daily on an empty stomach. Largely obsolete.

FDA-approved for

FDA dosing	Population	Start	Target	Max
HIV-1 infection	Adults	800 mg q8h	800 mg q8h

Renal Undefined

Hepatic Mild-to-moderate insufficiency due to cirrhosis: reduce to 600 mg q8h; severe not studied

Must be taken at 8-hour intervals; interrupt 1–3 days for nephrolithiasis/urolithiasis

Take without food, with water, 1 h before or 2 h after a meal (or with a light low-fat meal/other liquids)
Drink at least 1.5 L of fluids per 24 h to maintain hydration
Separate from didanosine by ≥1 h on an empty stomach

Coadministration with drugs whose CYP3A4-mediated metabolism indinavir inhibits, causing elevated levels with potentially serious or life-threatening reactions: alfuzosin; amiodarone; ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine); cisapride; lovastatin, simvastatin; pimozide; sildenafil for pulmonary arterial hypertension (Revatio); oral midazolam; triazolam; alprazolam

Pregnancy Optimal dosing not established; markedly reduced plasma levels during pregnancy

Lactation Undefined

NO BOXED WARNINGS

Principal riskNephrolithiasis; three-times-daily fasting dosing

Direct muscarinic antagonism0 / 4