Dosing & Uses
Dosage Forms & Strengths
tablet
- 250mg
- 625mg
HIV Infection
750 mg PO q8hr, OR
1250 mg PO q12hr
Dosage Modifications
Renal impairment: Dose adjustment not necessary
Hepatic impairment
- Mild impairment (Child-Pugh class A): Dose adjustment not necessary
- Severe impairment (Child-Pugh Class B or C): Not recommended
Multiple Myeloma (Orphan)
Orphan designation for treatment of multiple myeloma
Sponsor
- Swiss Group for Clinical Cancer Research (SAKK); Effingerstrasse 33; Bern, Switzerland
Dosage Forms & Strengths
tablet
- 250mg
- 625mg
HIV Infection
<2 years: Safety and efficacy not established
2-13 years: 45-55 mg/kg PO q12hr, OR 25-35 mg/kg PO q8hr
Not to exceed adult dose of 2,500 mg/day (q12hr dosing) or 1,875 mg/day (q8hr dosing)
Adolescents: 1,250 mg PO q12hr, OR 750 mg PO q8hr
Also see Administration
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
>10%
Diarrhea (14-20%)
1-10%
Nausea (3-7%)
Flatulence (1-5%)
Abdominal pain (1%)
Anemia (1%)
Allergic reaction (1%)
Impaired concentration (1%)
Lipodystrophy (1%)
Metabolic acidosis (1%)
Rash (1-3%)
Leukopenia (1%)
Thrombocytopenia (1%)
Weakness (1%)
<1%
QTc prolongation
Torsades de pointes
Diabetes mellitus, new onset and exacerbation
Hyperglycemia
Warnings
Contraindications
Hypersensitivity
Coadministration with major CYP3A4 substrates and/or inducers
Drugs that are contraindicated with nelfinavir include alpha1-adrenoreptor agonists (eg, alfuzosin), antiarrhythmics (amiodarone, bepridil, flecainide, propafenone, quinidine), rifampin, voriconazole, ergot derivatives (dihydroergotamine, ergonovine, ergotamine, methylergonovine), cisapride, St. John’s wort, lovastatin, simvastatin, lurasidone, pimozide, sildenafil (when used for PAH), midazolam, and triazolam
Cautions
Risk to pregnant/ pediatric pts: EMS (ethyl methanesulfonate) impurity shown to be teratogenic, mutagenic & carcinogenic in animal studies
Oral powder contains 11.2 mg of phenylalanine per gram of powder
Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs
Caution in patients with hemophilia A or B (risk of bleeding); increased bleeding, including spontaneous skin hematomas and hemarthrosis reported with protease inhibitors; in more than half of cases, administration of protease inhibitors was continued or reintroduced
Increased risks of fat redistribution, hemolytic anemia, hyperbilirubinemia if used in combination with other antiretroviral drugs
Increases risk of developing new onset diabetes mellitus; exacerbation of DM & hyperglycemia
Not for use in patients with moderate to- evere hepatic impairment
In pediatrics, drug exposure is highly variable
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to drug during pregnancy; healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263
Published reports of hepatic adverse events ranging from elevated liver enzymes to hepatic failure in pregnant patients exposed to drug and as part of combination treatment of HIV-1 infection reported; overall adverse event profile, including hepatic adverse events, and literature reports of decreased exposures in second and third trimesters, consider alternative antiretroviral drugs during pregnancy; if drug is used during pregnancy, clinical monitoring recommended
Therapy may reduce efficacy of estrogen-based oral contraceptives; advise patients to use alternative or additional contraceptive measures when oral contraceptives containing ethinyl estradiol or norethindrone and nelfinavir are coadministered
Lactation
The Centers for Disease Control and Prevention recommend that HIV-1 infected patients in the United States not breastfeed their infants to avoid risking potential transmission of HIV-1 infection
Based on limited published data, drug is present in low levels in human milk, and adverse effects in infants exposed to nelfinavir have been reported; because of potential for HIV-1 transmission (in HIV-negative infants), developing viral resistance (in HIV-positive infants), and the potential for serious adverse reactions in breastfed infants similar to those seen in adults, instruct mothers not to breastfeed if they are receiving therapy
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Protease Inhibitor; inhibits cleavage of Gag-Pol polyprotein precursors, which in turn causes the formation of immature, noninfectious viral particles.
Pharmacokinetics
Absorption: food increases AUC 2-3x
Vd: 2-7 L/kg
Protein Bound: >98%
Metabolism: hepatic via CYP3A4 & CYP2C19; major metabolite has activity comparable to parent drug
Half-life, plasma: 3.5-5 hr
Peak Plasma Time: 2-4 hr
Enzymes Inhibited: CYP3A4
Excretion: Feces: (87%); urine: (1-2%)
Administration
Oral Administration
Mix oral powder with small amount of water, milk, formula or dietary supplement and consume entire dose
Do not mix with acidic food or juice
If not consumed immediately, refrigerate no more than 6 hr
May use crushed 250 mg tablets instead of oral powder
Take all doses with high-fat meals
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Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.