Classifications: antiretroviral agent; protease inhibitor; Therapeutic:antiretroviral; protease inhibitor
Pregnancy Category: B
250 mg, 625 mg tablets; 50 mg/g powder
Inhibits HIV-1 protease, which is responsible for the production of HIV-1 viral particles in an infected individual. Inhibition
of the viral protease prevents the cleavage of the viral polypeptide, resulting in the production of an immature, noninfectious
Effectiveness is indicated by decreased viral load.
Treatment of HIV infection in combination with a nucleoside analog.
Hypersensitivity to nelfinavir; concurrent administration with amiodarone, quinidine, rifampin, triazolam, or midazolam;
lactation. Safety and effectiveness in children <2 y are not established.
Liver function impairment, hemophilia; pregnancy (category B).
Route & Dosage
Adult: PO 750 mg t.i.d. or 1250 mg (2 x 625 mg) b.i.d. with food
Child (213 y): PO 2030 mg/kg t.i.d. with food (max: 750 mg/dose)
- Give with a meal or light snack.
- Oral powder may be mixed with a small amount of water, milk, soy milk, or dietary supplements; liquid should be consumed
immediately. Do not mix oral powder in original container nor with acid food or juice (e.g., orange or apple juice, or applesauce).
- Store at 15°30° C (59°86° F).
Adverse Effects (≥1%)Body as a Whole:
Allergic reactions, back pain, fever, malaise, pain, asthenia, myalgia, arthralgia. CNS:
Headache, anxiety, depression
, dizziness, insomnia
, seizures. GI:
Abdominal pain, diarrhea,
nausea, flatulence, anorexia, dyspepsia, GI bleeding,
hepatitis, vomiting, pancreatitis, increased liver function tests. Hematologic:
Anemia, leukopenia, thrombocytopenia. Respiratory:
Dyspnea, pharyngitis, rhinitis. Skin:
Rash, pruritus, sweating, urticaria.
Other protease inhibitors
may increase nelfinavir levels; rifabutin, rifampin
may decrease nelfinavir levels; nelfinavir will decrease oral contraceptive
levels; may increase levels of atorvastatin, simvastatin;
increase risk of ergotamine
toxicity with dihydroergotamine, ergotamine. Herbal: St. John's wort, garlic
may decrease antiretroviral activity.
Food increases the amount of drug absorbed. Distribution:
>98% protein bound. Metabolism:
In the liver (CYP3A). Elimination:
Primarily in feces. Half-Life:
Assessment & Drug Effects
- Monitor hemophiliacs (type A or B) closely for spontaneous bleeding.
- Monitor carefully patients with hepatic impairment for toxic drug effects.
Patient & Family Education
- Drug must be taken exactly as prescribed. Do not alter dose or discontinue drug without consulting physician.
- Use a barrier contraceptive even if using hormonal contraceptives.
- Be aware that diarrhea is a common adverse effect that can usually be controlled by OTC medications.