Nelfinavir

VIRACEPT

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Pronunciation: nel-FIN-a-veer

Nelfinavir ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Nelfinavir ballicule

What it isHIV protease inhibitor; HIV.

Why this oneIt requires no ritonavir boosting, which simplified early regimens.

What limits itDiarrhea in most patients and a low resistance barrier; it is now rarely used. It induces and inhibits CYP3A4.

Nelfinavir molecular structure (skeletal formula) — Molecular structure: Nelfinavir

FDA-approved for

HIV infection (1997)

FDA label

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FDA dosing	Population	Start	Target	Max
HIV-1 infection	Adults & adolescents ≥13 yr	1250 mg BID or 750 mg TID with a meal	1250 mg BID or 750 mg TID	2500 mg/day
HIV-1 infection	Children 2 to <13 yr	45–55 mg/kg BID or 25–35 mg/kg TID with a meal	weight-based (see label tables)	2500 mg/day

Renal Undefined (not established in renal impairment)

Hepatic Mild (Child-Pugh A): no adjustment; do not use in moderate-severe (Child-Pugh B/C)

Instructions

Take with a meal
Tablets may be dissolved in a small amount of water if unable to swallow
Oral powder may be mixed in water/milk/formula (not acidic juice); contains phenylalanine (caution in PKU)

Available strengths

tab 250, 625 mg

Cautions

Serious CYP3A-mediated drug interactions
Do not use in moderate-severe hepatic impairment
Oral powder contains phenylalanine (phenylketonuria)
New-onset or worsening diabetes mellitus / hyperglycemia
Increased bleeding in hemophilia
Fat redistribution
Immune reconstitution syndrome
QTc prolongation / torsades (postmarketing)

Adverse reactions

Diarrhea
Nausea
Rash
Flatulence
Leukopenia/neutropenia (pediatric)
Anorexia (pediatric)
Abdominal pain (pediatric)

Pregnancy Consider alternative antiretrovirals; hepatic adverse events reported; APR birth-defect signal of uncertain significance

Lactation Do not breastfeed (HIV-1 transmission risk; present in human milk)

Cost

Nelfinavir (VIRACEPT)

Strength		#/mo	generic $/mo	CostPlus
250 mg	tab	60 BID		not offered
625 mg	tab	60 BID		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Nelfinavir is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entryNo US generic

NO BOXED WARNINGS

Principal riskDiarrhea in most patients; a low resistance barrier

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityAgent-specific renal, hepatic, hematologic, metabolic and drug-interaction toxicity.

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