enfuvirtide (Rx)

>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

<1% (selected)

Unstable angina

Toxic hepatitis

Renal failure

Respiratory distress

Guillain-Barre syndrome

Hypersensitivity rxn

Primary immune complex reaction

Suicide attempt

Postmarketing Reports

Cutaneous amyloidosis at the injection site

Contraindications

Hypersensitivity

Cautions

Use only in combination with other antiretrovirals

Each injection should be in a different site than the previous one (upper arm, anterior thigh, abdomen)

Monitor for signs and symptoms of pneumonia

Low initial CD4+ T-cell count and high initial viral load

Pulmonary disease, smoking

If pt becomes pregnant, call Antiretroviral Pregnancy Registry 1-800-258-4263

The possibility exists that this drug could result in a false-positive HIV test using (ELISA); use of a confirmatory test (Western blot) is advised

Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs; patients may develop an inflammatory response to indolent or residual opportunistic infection

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

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Synthetic peptide; inhibits fusion of HIV-1 with CD4+ cell membrane

Combination use recommended

Pharmacokinetics

Half-Life: 3.8 hr

Peak Plasma Time: 4-8 hr

Peak Plasma Concentration: 4.59 +/- 1.5 mcg/mL

AUC: 55.8 +/- 12.1 mcg.hr/mL

Bioavailability: 84%

Vd: 5.5L

Protein Bound: 92%

Metabolism: Hydrolysis

Total Body Clearance: 21-29 mL/hr/kg

SC Administration

Inject SC into the upper arm, anterior thigh, or abdomen