| Indication |
For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues. |
| Pharmacodynamics |
Saquinavir 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. Saquinavir
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. |
| Mechanism of action |
Saquinavir inhibits the HIV viral proteinase enzyme which prevents
cleavage of the gag-pol polyprotein, resulting in noninfectious,
immature viral particles. |
| Absorption |
Absolute bioavailability averages 4% |
| Volume of distribution |
|
| Protein binding |
98% |
| Metabolism |
Hepatic |
| Route of elimination |
In vitro studies using human liver microsomes have shown that the
metabolism of saquinavir is cytochrome P450 mediated with the specific
isoenzyme, CYP3A4, responsible for more than 90% of the hepatic
metabolism. Only 1% of saquinavir is excreted in the urine, so the
impact of renal impairment on saquinavir elimination should be minimal. |
| Half life |
Not Available |
| Clearance |
- 1.14 L/h/kg [Healthy volunteers receiving IV doses of 6, 36, and 72 mg]
|
| Toxicity |
Probably experience pain in the throat |
