Enfuvirtide

Indications

Enfuvirtide is used for: HIV-1 infection

Adult Dose

Subcutaneous HIV-1 infection Adult: Combination therapy w/ other antiretroviral: 90 mg bid. Inject into the arm, thigh or abdomen as directed, at a different site from the preceding one.

Child Dose

Subcutaneous HIV-1 infection Child: 6-16 yr 2 mg/kg bid. Max: 90 mg bid; >16 yr Same as adult dose.

Renal Dose

Administration

Reconstitute w/ 1.1 mL water for inj, gently tap the vial and allow to stand for up to 45 min to dissolve into soln. Do not shake or invert vial. SC Administration Inject SC into the upper arm, anterior thigh, or abdomen

Contra Indications

Hypersensitivity. Lactation.

Precautions

Patient w/ coagulation disorders, high initial viral load, low initial CD4 cell count, history of lung disease. Smokers and patients receiving IV drugs. Not intended in antiretroviral therapy-naive individual. Hepatic impairment and moderate to severe renal impairment. Childn. Pregnancy.

Pregnancy-Lactation

Pregnancy Category: B Lactation: Unknown whether enfuvirtide is excreted in milk; avoid in breastfeeding women; the CDC advises HIV-infected women not to breast-feed to avoid postnatal transmission of HIV

Interactions

Increased serum concentration w/ protease inhibitors. Decreased serum concentration w/ orlistat. Increased risk of bleeding w/ anticoagulants.

Adverse Effects

Side effects of Enfuvirtide : >10% Difficult to separate from background regimen Multiple inj site rxn (98%) Pain & discomfort (96%) Erythema (91%) Induration (90%) Nodules and cysts (80%) Pruritis (65%) Ecchymosis (52%) Diarrhea (31%) Nausea (22%) Fatigue (20%) Periph. neuropathy Insomnia 1-10% Difficult to separate from background regimen Asthenia Depression Pruritis Abdominal pain Anorexia Decreased appetite Weight loss Myalgia Cough Herpes simplex Influenza-like illness Pneumonia Sinusitis Lymphadenopathy Pancreatitis

Mechanism of Action

Enfuvirtide, is an HIV fusion protein inhibitor which interferes w/ entry of HIV type 1 (HIV-1) into the host cell by binding to viral glycoprotein gp41 subunit, thereby inhibiting viral and cellular membrane fusion w/ the CD4 cell receptor.