pharmacopeia
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/api/v1/drug/nelfinavir

Mechanism of action

Sourced from openFDA

Nelfinavir is an inhibitor of the HIV-1 protease [see Microbiology (12.4) ] .

Cytochrome P450 3AHIV Protease

Indications

Sourced from openFDA
  • VIRACEPT in combination with other antiretroviral agents is indicated for the treatment of HIV-1 infection. VIRACEPT is a protease inhibitor indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents.ICD-10: B20

Contraindications

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  • Coadministration of VIRACEPT is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. These drugs and other contraindicated drugs (which may lead to reduced efficacy of nelfinavir) are listed in Table 3 [also see Drug Interactions (7) , Table 6 ] .contraindicated

Dosage & administration

Sourced from openFDA

• See full prescribing information for administration instructions ( 2 ) • Adults and adolescents 13 years and older (tablets): 1250 mg twice daily or 750 mg three times daily with a meal ( 2.1 ) • Children 2 to less than 13 years (oral powder or 250 mg tablets): 45 to 55 mg/kg twice daily or 25 to 35 mg/kg three times daily with a meal. Refer to Tables 1 and 2 of the full prescribing information for specific dosing guidelines based on age and body weight ( 2.2 ) 2.1 Adults and Adolescents (13 years and older) The recommended dose is 1250 mg (five 250 mg tablets or two 625 mg tablets) twice daily or 750 mg (three 250 mg tablets) three times daily. VIRACEPT should be taken with a meal. Patients unable to swallow the 250 or 625 mg tablets may dissolve the tablets in a small amount of water [see Dosage and Administration (2.3) ] . 2.2 Pediatric Patients (2 to less than 13 years) In children 2 years of age and older, the recommended oral dose of VIRACEPT Oral Powder or 250 mg tablets is 45 to 55 mg/kg twice daily or 25 to 35 mg/kg three times daily. All doses should be taken with a meal . Doses higher than the adult maximum dose of 2500 mg per day have not been studied in children. For children unable to swallow tablets, VIRACEPT 250 mg tablet(s) may be dissolved in a small amount of water or, VIRACEPT Oral Powder may be administered [see Dosage and Administration (2.3) ] . The healthcare provider should assess appropriate formulation and dosage for each patient. Tables 1 and 2 provide dosing guidelines for VIRACEPT tablets and powder based on age and body weight.

Warnings & precautions

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ALERT: Find out about medicines that should not be taken with VIRACEPT. This statement is included on the product's bottle label. ALERT: Find out about medicines that should not be taken with VIRACEPT. • The concomitant use of VIRACEPT and certain other drugs may result in known or potentially significant drug interactions. Consult the full prescribing information prior to and during treatment for potential drug interactions ( 5.1 , 7.3 ) • Hepatic impairment: should not be used in patients with either moderate or severe hepatic impairment ( 2.4 , 5.2 ) • Phenylketonuria: the oral powder contains 11.2 mg phenylalanine per gram of powder ( 5.3 ) • Diabetes mellitus/hyperglycemia: new onset or exacerbation of pre-existing diabetes mellitus and hyperglycemia reported with protease inhibitors. In some cases after treatment discontinuation, hyperglycemia persisted ( 5.4 ) • Hemophilia: increased bleeding, including spontaneous skin hematomas and hemarthrosis reported with protease inhibitors. In more than half of the cases, protease inhibitors was continued or reintroduced ( 5.5 ) • Fat redistribution: observed with antiretroviral therapy ( 5.6 ) • Immune reconstitution syndrome: reported with combination antiretroviral therapy, including VIRACEPT.

Adverse reactions

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Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. • Most common adverse reactions (≥2%) of moderate or severe intensity in adults and adolescents (13 years and older) are diarrhea, nausea, rash, and flatulence ( 6.1 ) • Most common adverse reactions in pediatric patients (2 to less than 13 years) are diarrhea, leukopenia/neutropenia, rash, anorexia, and abdominal pain. ( 6.2 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience: Adults and Adolescents (13 years and older) The safety of VIRACEPT was studied in over 5000 patients who received drug either alone or in combination with nucleoside analogues. The majority of adverse events were of mild intensity. The most frequently reported adverse event among patients receiving VIRACEPT was diarrhea, which was generally of mild to moderate intensity. Drug-related clinical adverse experiences of moderate or severe intensity in ≥2% of patients treated with VIRACEPT coadministered with d4T and 3TC (Study 542) for up to 48 weeks, or with ZDV plus 3TC (Study 511) for up to 24 weeks are presented in Table 4.

Use in specific populations

Sourced from openFDA

• Use during pregnancy if the potential benefit justifies the potential risk to the fetus ( 8.1 ) • Lactation: Patients infected with HIV should be instructed not to breastfeed due to the potential for HIV transmission ( 8.2 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to VIRACEPT during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Published reports of hepatic adverse events ranging from elevated liver enzymes to hepatic failure in pregnant patients exposed to nelfinavir have been reported (see Clinical Considerations ). Due to VIRACEPT's 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. Available data from the APR suggests a statistically significant increase in overall risks of major birth defects with first trimester exposure with nelfinavir (3.9%) when compared with the background rate of 2.7% in one U.S. reference population (the Metropolitan Atlanta Congenital Defects Program [MACDP]), but the risk is similar to the background rate of 4.2% reported in another U.S. reference population (the Texas Birth Defects Registry [TBDR]).

Pharmacokinetics

Sourced from openFDA
Metabolism
The pharmacokinetic properties of nelfinavir were evaluated in healthy volunteers and HIV-infected patients; no substantial differences were observed between the two groups. Absorption Pharmacokinetic parameters of nelfinavir (area under the plasma concentration-time curve during a 24-hour period at steady-state [AUC 24 ], peak plasma concentrations [C max ], morning and evening trough concentrations [C trough ]) from a pharmacokinetic study in HIV-positive patients after multiple dosing with 1250 mg (five 250 mg tablets) twice daily (BID) for 28 days (10 patients) and 750 mg (three 250 mg tab…

Overdosage

Sourced from openFDA

Human experience of acute overdose with VIRACEPT is limited. There is no specific antidote for overdose with VIRACEPT. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Administration of activated charcoal may also be used to aid removal of unabsorbed drug. Since nelfinavir is highly protein bound, dialysis is unlikely to significantly remove drug from blood.

Approval history

Sourced from openFDA
  • Mar 14, 1997NDANDA020779Agouron Pharms
  • Apr 30, 2003NDANDA021503Agouron Pharms

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
2,088 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Drug Exposure During Pregnancy41320%
  2. 2Pain24412%
  3. 3Anxiety23611%
  4. 4Emotional Distress23611%
  5. 5Anhedonia21010%
  6. 6Foetal Exposure During Pregnancy2039.7%
  7. 7Chronic Kidney Disease1406.7%
  8. 8Osteoporosis1376.6%
  9. 9Anaemia1205.7%
  10. 10Premature Baby1165.6%
  11. 11Bone Density Decreased1155.5%
  12. 12Depression1105.3%
  13. 13Renal Failure1004.8%
  14. 14Pregnancy954.5%
  15. 15Osteopenia914.4%

Literature

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Recent PubMed references pinned to Nelfinavir as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 149 ClinicalTrials.gov registrations naming Nelfinavir as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Nelfinavir work?
Nelfinavir is an inhibitor of the HIV-1 protease [see Microbiology (12.4) ] .
What is Nelfinavir used for?
According to FDA labeling, Nelfinavir carries indications including: VIRACEPT in combination with other antiretroviral agents is indicated for the treatment of HIV-1 infection. VIRACEPT is a protease inhibitor indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Nelfinavir?
Nelfinavir is classified as Protease inhibitors, Protease Inhibitor, Cytochrome P450 3A Inhibitors, HIV Protease Inhibitors, Decreased Protein Synthesis, Increased Immunologically Active Molecule Activity.
What are the brand names for Nelfinavir?
Nelfinavir is marketed under brand names including Viracept.
What are the contraindications for Nelfinavir?
Nelfinavir labeling lists contraindications including: Coadministration of VIRACEPT is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. These drugs and other contraindicated drugs (which may lead to reduced efficacy of nelfinavir) are listed in Table 3 [also see Drug Interactions (7) , Table 6 ] .. Always consult the full prescribing information and a clinician.
Note. Data for nelfinavir is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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