Introduction
Nelfinavir is a potent HIV-1 protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children. Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Uses
Nelfinavir is a viral protease inhibitor used in the treatment of HIV infection.
Used in combination with other antiviral drugs in the treatment of HIV in both adults and children.
Associated Conditions
Pharmacodynamics
Nelfinavir 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. Nelfinavir 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
Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Absorption
Well absorbed following oral administration.
Volume of Distribution
- 2 to 7 L/kg
Protein Binding
>98%
Route of Elimination
The terminal half-life in plasma was typically 3.5 to 5 hours. The majority (87%) of an oral 750 mg dose containing 14C-nelfinavir was recovered in the feces; fecal radioactivity consisted of numerous oxidative metabolites (78%) and unchanged nelfinavir (22%). Only 1–2% of the dose was recovered in urine, of which unchanged nelfinavir was the major component.
Half Life
3.5 - 5 hours
Toxicity
Oral LD50 is over 5g/kg in rats. Side effects include thirst and hunger, unexplained weight loss, increased urination, fatigue, and dry, itchy skin.
Food Interactions
- Take with food. Food increases exposure and decreases pharmacokinetic variability.
Dosage
Paediatric patients (2-13 years): The recommended oral dose of Nelfinavir for paediatric patients 2 to 13 years of age is 20-30 mg/kg per dose, three times daily with a meal.