Drug information of nelfinavir


nelfinavir

Drug group:

Nelfinavir is a potent HIV-1 protease inhibitor. It is used in combination with other antiviral drugs in the treatment of HIV in both adults and children.

Mechanism of effect

Nelfinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature 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%)

Dosage

Adult

HIV Infection

750 mg PO q8hr, OR

1250 mg PO q12hr

Pediatric

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

Drug contraindications

Hypersensitivity

Alerts

Risk to pregnant/ pediatric pts: EMS (ethyl methanesulfonate) impurity shown to be teratogenic, mutagenic & carcinogenic in animal studies

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

Points of recommendation

  • This medicine interacts with many other drugs. The chance of this medicine (nelfinavir tablets)'s side effects may be raised or how well this medicine (nelfinavir tablets) works may be lowered. The chance of the other drugs' side effects may also be raised. This may include very bad, life-threatening, or deadly side effects. Check with your doctor and pharmacist to make sure that it is safe for you to take this medicine (nelfinavir tablets) with all of your other drugs (prescription or OTC, natural products, vitamins).
  • If you have high blood sugar (diabetes), talk with your doctor. This medicine may raise blood sugar.
  • Some people with hemophilia have had times of more bleeding when taking drugs like this one. If you have hemophilia, talk with your doctor.
  • This medicine is not a cure for HIV. Stay under the care of your doctor.
  • This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors.
  • Birth control pills and other hormone-based birth control may not work as well to prevent pregnancy. Use some other kind of birth control also like a condom when taking this medicine (nelfinavir tablets).
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine (nelfinavir tablets) while you are pregnant.
  • Do not breast-feed if you have HIV disease unless your doctor tells you to.
  • Take with meals.
  • Do not take didanosine within 2 hours of this medicine (nelfinavir tablets).
  • Keep taking this medicine (nelfinavir tablets) as you have been told by your doctor or other health care provider, even if you feel well.
  • It is important that you do not miss or skip a dose of this medicine (nelfinavir tablets) during treatment.
  • If you cannot swallow this medicine (nelfinavir tablets) whole, you may melt it in water. Once your dose is melted, mix well and drink right away. Rinse the glass with more water and drink.
  • Take a missed dose as soon as you think about it. If it is close to the time for your next dose, skip the missed dose and go back to your normal time. Do not take 2 doses at the same time or extra doses.
  • If you miss taking this medicine (nelfinavir tablets) for a few days in a row, call your doctor before you start taking it again.

Pregnancy level

B


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