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It is an inhibitor of the enzyme human immunodeficiency virus protease.
Nelfinavir is a peptide analogue. It reversibly binds to the HIV encoded aspartyl protease enzyme which is involved in the degradation of poly protein into structural protein and subsequent maturation of virus particle. Binding of Nelfinavir to the enzyme results in immature noninfectious viral progeny.
Pharmacokinetics
Absorption: It is rapidly absorbed after oral administration.
Distribution: About half of the drug is distributed as protein bound form.
Metabolism: It undergoes metabolism in the liver.
Excretion: The metabolites are excreted through faeces.
On Set of Action
2 - 4 hours
Half Life
90 - 120 minutes
Adverse Effects
1. Diarrhoea
2. Vomiting
3. Nausea
4. Abdominal pain
5. Confusion
6. Itching
7. Fatigue
8. Leucopenia
9. Thrombocytopenia
ContraIndications
Hypersensitivity to Nelfinavir
Special Precautions
1. Hepatic dysfunction
2. Haemophilia
3. Diabetes mellitus
4. Renal impairment
Pregnancy
Use with caution
Breast Feeding
Contraindicated
Elderly
Use with caution
Children
Use with caution
Neonates
Contraindicated
Interactions
Anti-arrhythmics : Increased risk of arrhythmias with amiodarone and quinidine (avoid concomitant use).
Antibacterials : Rifampicin significantly reduces plasma concentration of nelfinavir (avoid concomitant use).
Antidepressants: Plasma concentration reduced by St. John`s Wort.
Antiepileptics : Carbamazepine and phenytoin possibly reduce plasma concentration of nelfinavir.
Antihistamine: Increased risk of arrhythmias with terfenadine.
Antipsychotics: Possibly increased risk of arrhythmias with pimozide.
Anxiolytics and Hypnotics: Risk of prolonged sedation with midazolam.
Barbiturates and Primidone: Phenobarbital possibly reduces plasma concentration of nelfinavir.
Indications
HIV infection
Dosage
Adult: 2.25 g / day in 3 divided dose
Children: 60 - 90 mg / kg body weight / day in 3 divided dose.
Storage
Store at 15 - 30 degree C.Protect away from heat and light. Keep out of the reach of Children.
Missed Dose
Take the missed dose as soon as noticed and if it is the time to take the next dose then skip the missed dose.
Over Dose
Give supportive measures and treatment. Induce emesis or gastric lavage has to be done followed by charcoal administration.
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