Saquinavir

Saquinavir is a peptidomimetic HIV protease inhibitor that was designed to mimic the phenylalanine-proline cleavage site of the HIV Gag-Pol polyprotein, fitting into the active site of the HIV aspartyl protease and competitively blocking substrate access. This prevents the proteolytic processing of viral polyproteins into mature structural and enzymatic components, resulting in production of non-infectious, immature virions. Its oral bioavailability is poor (~4% alone) and it is used with ritonavir boosting.

Adult

For previously treated patients: 1 g every 12 hours (with low-dose ritonavir). For not previously treated patients: 500 mg every 12 hours for 7 days, then increased to 1 g every 12 hours (with low-dose ritonavir).

Renal adjustment

Use with caution if eGFR less than 30 mL/minute/1.73 m2.

Hepatic adjustment

Manufacturer advises caution in moderate impairment (limited information available); avoid in decompensated liver disease.

• Bradycardia
• Congenital QT prolongation
• Electrolyte disturbances
• Heart failure with reduced left ventricular ejection fraction
• History of symptomatic arrhythmias