nelfinavir

Contraindicated in:

Hypersensitivity
Concurrent amiodarone, ergot derivatives, quinidine, lurasidone, pimozide, alfuzosin, sildenafil (Revatio), simvastatin, lovastatin, triazolam, or rifampin
OB: Pregnancy (may lead to hepatic failure)
Lactation: Breastfeeding should be avoided in mothers infected with HIV.

Use Cautiously in:

Hemophiliacs (↑ risk of bleeding)
Diabetes mellitus (may exacerbate condition)
Hepatic impairment.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: pruritus, rash, sweating, urticaria.

EENT: acute iritis, pharyngitis, rhinitis, sinusitis.

Endo: fat redistribution, hyperglycemia, hyperuricemia.

F and E: dehydration.

GI: diarrhea, anorexia, dyspepsia, ↑ liver enzymes, epigastric pain, flatulence, GI bleeding, hepatitis, nausea, oral ulcerations, pancreatitis, vomiting.

GU: nephrolithiasis, sexual dysfunction.

Hemat: anemia, leukopenia, thrombocytopenia.

Metab: hyperlipidemia.

MS: arthralgia, arthritis, back pain, myalgia, myopathy.

Neuro: SEIZURES, anxiety, depression, dizziness, drowsiness, emotional lability, headache, hyperkinesia, insomnia, malaise, migraine headache, myasthenia, paresthesia, sleep disorders, suicidal ideation, weakness.

Resp: dyspnea.

Misc: allergic reactions, fever, immune reconstitution syndrome.

Interactions ⬆ ⬇

Drug-Drug:

↑levels and risk of toxicity from amiodarone, ergot derivatives (dihydroergotamine, ergotamine, methylergonovine), lovastatin, lurasidone, pimozide, quinidine, sildenafil (Revatio), simvastatin, alfuzosin, or triazolam; concurrent use contraindicated.
.
Rifampin may ↓ levels and promote resistance to its effects; concurrent use contraindicated.
↑risk of myopathy with atorvastatin; do not exceed atorvastatin dose of 40 mg/day.
↓metabolism may ↑ effects of rifabutin (dose of rifabutin should be ↓ by 50%), carbamazepine, phenobarbital, or phenytoin (concurrent use with rifampin should be avoided).
Plasma levels and effectiveness may be ↑ by ketoconazole, indinavir, or ritonavir.
May ↓ levels of methadone; dose of methadone may need to be ↑.
↑plasma levels of indinavir, saquinavir, cyclosporinetacrolimus, sirolimus, and azithromycin.
↑levels and effects of sildenafil (sildenafil dose should not exceed 25 mg in 48 hr).
Blood levels may be ↓ by nevirapine and omeprazole.
Should not be given at the same time as didanosine.
May ↓ plasma levels and effectiveness of hormonal contraceptives.
May ↑ concentrations of phosphodiesterase type 5 inhibitors (PDE5) causing hypotension, visual changes, priapism; ↓ starting doses not to exceed 25 mg within 48 hr for sildenafil, 2.5 mg every 24 hr for vardenafil and 10 mg every 72 hr for tadalafil.
May ↑ risk of adverse effects with salmeterol; concurrent use not recommended.
May ↑ bosentan levels; initiate bosentan at 62.5 mg once daily or every other day.
May ↑ tadalafil (Adcirca) levels; initiate tadalafil (Adcirca) at 20 mg once daily.
May ↑ colchicine levels; ↓ dose of colchicine; do not administer colchicine if patients have renal or hepatic impairment.
May ↑ levels of warfarinand the risk of bleeding; routinely monitor INR.
May ↑ quetiapine levels; ↓ quetiapine dose to 1/6 of current dose

Drug-Natural Products:

St. John's wort induces metabolism of nelfinavir, ↓ blood levels and may promote resistance to its effects.

Drug-Food:

Food↑ absorption.

Availability ⬆ ⬇

Tablets: 250 mg; 625 mg;

Route/Dosage ⬆ ⬇

PO (Adults and Children 13 yr): 750 mg 3 times daily or 1250 mg twice daily.
PO (Children 2–13 yr): 44–55 mg/kg twice daily or 25–35 mg/kg 3 times daily (not to exceed 2500 mg/day).

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Inhibits HIV protease and prevents cleavage of viral polyproteins.

Therapeutic Effects:

Increased CD4 cell count and decreased viral load.
Slowed progression of HIV infection with less sequelae.

Classifications ⬆ ⬇

Therapeutic Classification: antiretrovirals

Pharmacologic Classification: protease inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed after oral administration.

Distribution: Unknown.

Protein Binding: >98%.

Metabolism/Excretion: Mostly metabolized (CYP3A4 enzyme system) (CYP2C19 and CYP3A4); the CYP2C19 enzyme system exhibits genetic polymorphism; 15–20% of Asian patients and 3–5% of Caucasian and Black patients may be poor metabolizers and may have significantly ↑ nelfinavir concentrations and an ↑ risk of adverse effects. Excreted in feces as metabolites (78%) or unchanged drug (22%); minimal renal excretion.

Half-life: 3.5–5 hr.

Time/Action Profile ⬆ ⬇

(plasma levels)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	2–4 hr	8 hr

Patient/Family Teaching ⬆ ⬇

Emphasize the importance of taking nelfinavir exactly as directed at evenly spaced times throughout the day. Do not take more than prescribed amount and do not stop taking without consulting health care professional. Take missed doses as soon as remembered; do not double doses.
Instruct patient that nelfinavir should not be shared with others.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications, especially St. John's Wort. Advise patient to find out which medications cannot be taken with nelfinavir.
Inform patient that nelfinavir does not cure AIDS or prevent associated or opportunistic infections. Nelfinavir may reduce the risk of transmission of HIV to others through sexual contact or blood contamination. Caution patient to avoid sexual contact or to use a condom and to avoid sharing needles or donating blood to prevent spreading the AIDS virus to others. Advise patient that the long-term effects of nelfinavir are unknown at this time.
Inform patient that nelfinavir may cause hyperglycemia. Advise patient to notify health care professional if increased thirst or hunger; unexplained weight loss; increased urination; fatigue; or dry, itchy skin occurs.
Advise patient that if diarrhea occurs, it can usually be controlled with OTC antidiarrheals, such as loperamide, which slow GI motility.
Inform patient that redistribution and accumulation of body fat may occur, causing central obesity, dorsocervical fat enlargement (buffalo hump), peripheral wasting, breast enlargement, and cushingoid appearance. The cause and long-term effects are not known.
Immune reconstitution syndrome may trigger opportunistic infections or autoimmune disorders. Notify health care professional if symptoms occur.
Rep: May cause fetal harm. May cause liver failure in pregnant patients; consider alternative antiretroviral drugs. Advise females of reproductive potential taking oral contraceptives to use a nonhormonal method of birth control during nelfinavir therapy. If pregnancy is suspected notify health care professional promptly. Inform pregnant women of the Antiretroviral Pregnancy Registry that monitors pregnancy outcomes in women exposed to nelfinavir during pregnancy. Enroll patient by calling 1-800-258-4263. Advise female patient to avoid breastfeeding during therapy.
Emphasize the importance of regular follow-up and blood counts to determine progress and monitor for side effects.

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Indications ⬇

Contraind./Precautions ⬆ ⬇