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All about: Nelfinavir Mesylate

Big Image Pronouncation: (nell-FIN-ah-veer)
Class: Protease inhibitor

Trade Names:
Viracept
- Tablets 250 mg
- Powder 50 mg/g

Mechanism of Action

Pharmacology

Inhibits human immunodeficiency virus (HIV) protease, the enzyme required to form functional proteins in HIV-infected cells.

Pharmacokinetics

Absorption

Food increased maximum plasma concentration and AUC by 2- to 3-fold. T max was 2 to 4 hr and C max was 3 to 4 hr.

Distribution

Nelfinavir's Vd is 2 to 7 L/kg and protein binding is greater than 98%.

Metabolism

Nelfinavir is metabolized by multiple cytochrome P450 isoforms, including CYP3A. Major metabolite has activity comparable to parent drug.

Elimination

The t 1/ 2 is 3.5 to 5 hr; 87% excreted in feces (78% metabolites, 22% unchanged) and 1% to 2% in urine (unchanged).

Indications and Usage

Treatment of HIV infection in combination with other antiretroviral agents.

Contraindications

Hypersensitivity to nelfinavir or any component of the product. Concomitant therapy with amiodarone, ergot derivatives, quinidine, lovastatin, midazolam, pimozide, simvastatin, and triazolam.

Dosage and Administration

Adults and Children (older than 13 yr)

PO 1250 mg bid or 750 mg tid in combination with nucleoside analogs.

Children (2 to 13 yr)

PO 20 to 30 mg/kg/dose tid.

General Advice

  • Administer with food.
  • The oral powder may be mixed with a small amount of water, milk, formula, soy formula, soy milk, or dietary supplement. If mixture is not consumed immediately, it must be stored under refrigeration and used within 6 hr of mixing.
  • Do not mix oral powder with acidic food or juice because of bitter taste.

Storage/Stability

Store tablets and powder at controlled room temperature (59° to 86°F).

Drug Interactions

Alprazolam, clorazepate, diazepam, estazolam, flurazepam, midazolam, triazolam, zolpidem

Nelfinavir may increase blood levels of these drugs, which may produce extreme sedation and respiratory depression. Do not coadminister.

Amiodarone, cisapride, cyclosporine, lovastatin, pimozide, quinidine, rifabutin, sildenafil, simvastatin, sirolimus, tacrolimus

Nelfinavir may elevate blood levels of these drugs, which may increase the risk of arrhythmias or other potential serious adverse effects.

Carbamazepine, phenobarbital, St. John's wort

May decrease nelfinavir plasma concentrations.

Indinavir

Nelfinavir may increase indinavir blood levels.

Indinavir, ritonavir

May increase nelfinavir plasma concentrations.

Methadone

May decrease methadone concentration.

Oral contraceptives

Concentrations of ethinyl estradiol, a component of oral contraceptives, may be reduced.

Phenytoin

Nelfinavir may decrease blood levels of phenytoin.

Rifabutin

May increase rifabutin concentration and decrease nelfinavir concentration.

Rifampin

May decrease plasma concentrations of nelfinavir.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache; paresthesia; dizziness; insomnia; somnolence; anxiety; depression; seizures; emotional lability; hyperkinesia; migraine; sleep disorder.

Dermatologic

Rash (2%); pruritus; sweating; urticaria; dermatitis folliculitis.

EENT

Pharyngitis; rhinitis; sinusitis; acute iritis; eye disorder.

GI

Anorexia; diarrhea (20%); dyspepsia; flatulence; nausea (3%); vomiting; abdominal pain; pancreatitis; bleeding; mouth ulcerations.

Genitourinary

Sexual dysfunction; kidney calculus; urine abnormality.

Hematologic

Anemia; leukopenia; thrombocytopenia.

Hepatic

Hepatitis.

Metabolic

Increased alkaline phosphatase; LFTs; creatine phosphokinase; hyperlipidemia; amylase; lactic dehydrogenase; hyperuricemia; hyperglycemia; hypoglycemia; dehydration; gamma glutamyl transpeptidase.

Respiratory

Dyspnea.

Miscellaneous

Asthenia; fever; myalgia; back pain; malaise; arthralgia; myasthenia; myopathy; accidental injury; allergic reaction; arthralgia; cramps.

Precautions

Pregnancy

Category B .

Lactation

Undetermined. HIV-infected mothers should not breast-feed their infants.

Children

Safety and efficacy not established for children younger than 2 yr.

Hepatic Function

Use caution in patients with hepatic impairment; decreased nelfinavir clearance may occur.

Diabetes

New onset diabetes and exacerbation of pre-existing diabetes mellitus has been reported in postmarking surveillance.

Fat redistribution

Redistribution/accumulation of body fat has been observed in patients receiving antiretroviral therapy.

Hemophilia

There have been reports of increased bleeding, including skin hematomas and hemarthrosis in patients with hemophilia type A and B treated with protease inhibitors. A causal relationship not established.

Phenylketonuria

Nelfinavir powder contains 11.2 mg phenylalanine/g of powder.

Patient Information

  • Advise patient to take medication exactly as prescribed, including taking each dose with food to increase absorption.
  • Warn patient not to alter dose or discontinue the medication without consulting health care provider.
  • Advise patient that if a dose is missed, to take it as soon as possible and then return to normal dose. However, if a dose is skipped, the patient should not double the next dose.
  • Instruct patient not to take any other medications, including OTC medications, without checking with health care provider. This medication interacts with a wide range of all types of medications.
  • Explain that the patient will be required to have frequent follow-up blood and urine tests during the course of treatment and to keep appointments.
  • Inform patient that this medication is not a cure for HIV infection and that the patient may continue to acquire secondary illnesses associated with the disease.
  • Emphasize to patient, family, and significant others that this medication does not reduce the risk of transmitting HIV to others through sexual contact or blood contamination.
  • Inform patient that diarrhea is the most common adverse effect and that it can usually be controlled by OTC antidiarrheals such as loperamide.
  • Inform patient to report serious or bothersome side effects to the health care provider.
  • Explain that the long-term effects of this medication are not known at this time.
  • Inform patients taking oral contraceptives that alternate or additional contraceptive measures should be used during therapy with nelfinavir.

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