Nelfinavir is indicated for the treatment of HIV infection when antiretroviral therapy is clinically required.

Nelfinavir is a selective, competitive, reversible inhibitor of HIV-1 protease. It blocks the viral protease enzyme, preventing the cleavage of the gag-pol polyprotein, which leads to the formation of immature, non-infectious viral particles and inhibition of viral replication.

Adults: The recommended dose is 1250 mg (five 250 mg tablets) twice daily or 750 mg (three 250 mg tablets) three times daily. Nelfinavir should be taken with a meal. Antiviral activity is enhanced when Nelfinavir is administered in combination with nucleoside analogues. Therefore, it is recommended that Nelfinavir should be used in combination with nucleoside analogues.

Paediatric patients (2-13 years): The recommended oral dose of Nelfinavir for paediatric patients 2 to 13 years of age is 20-30 mg/kg per dose, three times daily with a meal.

Reduced levels/effects may occur with antacids, phenobarbital, carbamazepine, aminoglutethimide, phenytoin, rifampicin, nafcillin, nevirapine, omeprazole.
Increased serum levels/effects may occur with azole antifungals, cimetidine, and efavirenz. Nelfinavir may increase serum levels/effects of azithromycin, calcium channel blockers, clarithromycin, corticosteroids (e.g. fluticasone), mirtazapine, nateglinide, nefazodone, ciclosporin, sirolimus, tacrolimus, venlafaxine, eplerenone, fentanyl, atorvastatin, PDE-5 inhibitors, rifabutin, trazodone, and tricyclic antidepressants (TCAs).
It may reduce the effectiveness of hormonal contraceptives, methadone, and theophylline derivatives.

Nelfinavir is contraindicated in patients with known hypersensitivity to any of its components. Co-administration with drugs highly dependent on CYP3A metabolism and where increased plasma levels may lead to serious or life-threatening adverse effects is contraindicated.

The safety of Nelfinavir has been evaluated in more than 1500 patients receiving the drug alone or in combination with nucleoside analogues. Most adverse effects were mild in severity. The most commonly reported side effect was diarrhoea, usually mild to moderate in intensity. Adverse reactions occurring in less than 2% of patients in Phase II/III studies and considered possibly related or of unknown relationship to treatment and of at least moderate severity are listed below.

General: Abdominal pain, accidental injury, allergic reactions, asthenia, back pain, fever, headache, malaise, pain, and redistribution or accumulation of body fat.

Digestive system: Anorexia, dyspepsia, epigastric pain, gastrointestinal bleeding, hepatitis, mouth ulceration, pancreatitis, and vomiting.

Haemic/Lymphatic system: Anaemia, leukopenia, and thrombocytopenia.

Metabolic/Nutritional: Increased alkaline phosphatase, amylase, creatine phosphokinase, lactate dehydrogenase, SGOT, SGPT, and gamma-glutamyl transpeptidase; hyperlipidaemia, hyperuricaemia, hyperglycaemia, hypoglycaemia, dehydration, and abnormal liver function tests.

Musculoskeletal system: Arthralgia, arthritis, muscle cramps, myalgia, myasthenia, and myopathy.

Nervous system: Anxiety, depression, dizziness, emotional instability, hyperkinesia, insomnia, migraine, paraesthesia, seizures, sleep disorders, somnolence, and suicidal ideation.

Respiratory system: Dyspnoea, pharyngitis, rhinitis, and sinusitis.

Skin/Appendages: Dermatitis, folliculitis, fungal dermatitis, maculopapular rash, pruritus, sweating, and urticaria.

Ophthalmic: Acute iritis and other eye disorders.

Urogenital system: Kidney stones and sexual dysfunction.

Pregnancy Category B. There are no adequate and well-controlled studies in pregnant women.

Lactation: The US Public Health Service and CDC recommend that HIV-infected women should not breast-feed to prevent postnatal transmission of HIV to the infant.

Nelfinavir should not be used with terfenadine, astemizole, cisapride, triazolam, midazolam, ergot derivatives, amiodarone, or quinidine, as it may inhibit hepatic metabolism of these drugs and lead to serious or life-threatening adverse effects. New-onset diabetes mellitus, worsening of pre-existing diabetes, and hyperglycaemia have been reported during post-marketing use of protease inhibitors. Some patients required insulin or oral antidiabetic dose adjustment, and in some cases diabetic ketoacidosis occurred. Hyperglycaemia may persist even after discontinuation in some patients.

General: Nelfinavir is mainly metabolized in the liver; therefore, caution is required in patients with hepatic impairment.

Haemophilia: Increased bleeding events, including spontaneous haematomas and haemarthrosis, have been reported in haemophilia A and B patients receiving protease inhibitors. In some cases, factor VIII therapy was required, and protease inhibitors were continued or restarted. A direct causal relationship has not been confirmed.

Paediatric use: Safety, efficacy, and pharmacokinetics have not been established in children below 2 years of age.

Drugs for HIV / Anti-retroviral drugs

Store at 15–30°C.