Nelfinavir Mesylate
Pronouncation: (nell-FIN-ah-veer)Class: Protease inhibitor
Trade Names:
Viracept
- Tablets 250 mg
- Powder 50 mg/g
Pharmacology
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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 h and C max was 3 to 4 h.
Distribution
Nelfinavir's Vd is 2 to 7 L/kg and protein binding is greater than 98%.
Metabolism
Nelfinavir is metabolized by multiple CYP-450 isoforms, including CYP3A. Major metabolite has activity comparable with parent drug.
Elimination
The t ½ is 3.5 to 5 h; 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 of age)PO 1,250 mg twice daily or 750 mg 3 times daily in combination with nucleoside analogs.
Children (2 to 13 yr of age)PO 20 to 30 mg/kg/dose 3 times daily.
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 h 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, zolpidemNelfinavir 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, tacrolimusNelfinavir may elevate blood levels of these drugs, which may increase the risk of arrhythmias or other potential serious adverse reactions.
Carbamazepine, phenobarbital, St. John's wortMay decrease nelfinavir plasma concentrations.
IndinavirNelfinavir may increase indinavir blood levels.
Indinavir, ritonavirMay increase nelfinavir plasma concentrations.
MethadoneMay decrease methadone concentration.
Oral contraceptivesConcentrations of ethinyl estradiol, a component of oral contraceptives, may be reduced.
PhenytoinNelfinavir may decrease blood levels of phenytoin.
RifabutinMay increase rifabutin concentration and decrease nelfinavir concentration.
RifampinMay 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; CPK; 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 of age.
Hepatic Function
Use caution in patients with hepatic function impairment; decreased nelfinavir Cl 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 reaction and that it can usually be controlled by OTC antidiarrheals such as loperamide.
- Inform patient to report serious or bothersome adverse reactions 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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HIV Infection, Nonoccupational Exposure, Occupational Exposure
