Nelfinavir (PI)

	Protease Inhibitors: Nelfinavir

Contents Introduction Information card Pharmacokinetics Dosing Pediatric dose Side effects Drug interactions

Introduction

The information represented on this drug does not necessarily correspond with the information that can be found in the Belgian scientific leaflet.
Nelfinavir was the fourth HIV-1 protease inhibitor to be developed clinically. It was approved by the FDA in March of 1997. (106) It is the only protease inhibitor with a pediatric indication. (100)

Abbreviation(s):
Generic name:
Brand name:

NFV
nelfinavir
Viracept®

USA (FDA)

Adult approval date:
Pediatric approval date:

March 14, 1997
March 14, 1997

Pharmaceutical co.: Agouron Pharmaceuticals

Belgium:
Reimbursable since September 1998

Active
Ingredient

Dosage form;
Route

Strength

Tablets and Powder(not yet reimbursable)

Nelfinavir Mesylate

Tablet; Oral

250MG

Pharmacokinetics

The absolute bioavailability of nelfinavir is unknown.

Dosing

Currently, 750 mg is given three times daily with food (dosing exactly every 8 hours is not required). (106)

Pediatric dose: (111)

2 to 13 years: 20-30 mg/kg/dose three times daily.

Side effects

The most common adverse event associated with nelfinavir use was diarrhea. Unpublished data suggest the diarrhea was not associated with weight loss and was easy to control with over-the-counter antidiarrheal medications. Less common side effects included rash, asthenia, headache, and nausea. (100,106) Hyperglycemia and severe diabetes has been reported with neflinavir. (112)

Drug interactions

Neflinavir is metabolized by the cytochrome P450 3A4 enzyme system. Drugs that induce the activity of this system (such as rifampin) may lead to reduced plasma concentrations of neflinavir, and possibly the rapid development of drug resistance. Because ketoconazole inhibits the CYP3A4 pathway, it may increase the plasma concentrations of neflinavir, but dose modifications are not necessary. Neflinavir should not be used in conjunction with terfenadine, cisapride, astemizole and potent benzodiazepine. Neflinavir decreases the AUC of etinyl estradiol. (113) Rifampin will reduce the AUC of by 82%, and therefore should not be used concurrently with nelfinavir. (106,114)

Interactions with other antiretroviral agents

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