Enfuvirtide

Subcutaneous
HIV-1 infection

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.

Hypersensitivity. Lactation.

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.

Significant: Hypersensitivity reactions (e.g. rash, fever, nausea and vomiting, chills, rigors, hypotension, elevated serum liver transaminases), immune reconstitution syndrome, bacterial pneumonia, inj site reaction (e.g. mild to moderate pain/discomfort, induration, erythema, pruritus, ecchymosis).
Nervous: Anxiety, flu-like symptoms, peripheral neuropathy, weakness, insomnia, depression, nightmare, irritability, hypoaesthesia, tremor, vertigo, asthenia.
GI: Abdominal pain, anorexia, dry mouth, nausea, diarrhoea, constipation, pancreatitis, GERD.
Resp: Cough, sinusitis.
Genitourinary: Nephrolithiasis.
Endocrine: Wt loss, hyperglycaemia, hypertriglyceridaemia, DM.
Haematologic: Lymphadenopathy, eosinophilia, haematuria.
Musculoskeletal: Limb pain, myalgia, osteonecrosis.
Ophthalmologic: Conjunctivitis.
Otic: Ear infection.
Dermatologic: Dry skin, seborrheic eczema, acne.
Potentially Fatal: Guillain-Barre syndrome.

Parenteral/SC: B

Monitor viral load, CD4 count, hypersensitivity and inj site reactions, pediatric wt (periodically). Monitor for signs and symptoms of pneumonia, neuropathy and CNS changes.

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

May cross react w/ HIV glycoprotein 41(gp41) resulting to false-positive HIV result in ELISA test.

Description:
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.
Pharmacokinetics:
Absorption: Almost completely absorbed following SC inj. Bioavailability: 84%. Time to peak plasma concentration: 8 hr.
Distribution: Volume of distribution: 5.5 ± 1.1 L. Plasma protein binding: 92%.
Metabolism: Undergoes catabolism in the liver and kidney by peptidase into amino acids and proteinase via hydrolysis to form deaminated metabolite.
Excretion: Elimination half-life: 3.8 hr.

Store at 25°C.
Any unused medicinal product should be disposed of in accordance w/ local requirement.

Antivirals

J05AX07 - enfuvirtide ; Belongs to the class of other antivirals. Used as a direct acting antiviral in the systemic treatment of viral infections.

Anon. Enfuvirtide (Briggs Drugs in Pregnancy and Lactation). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/09/2017.

Anon. Enfuvirtide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 06/09/2017.

Buckingham R (ed). Enfuvirtide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2017.

Joint Formulary Committee. Enfuvirtide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/09/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Enfuvirtide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 06/09/2017.