enfuvirtide


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Related to enfuvirtide: Maraviroc

enfuvirtide

Fuzeon

Pharmacologic class: Human immunodeficiency-1 (HIV-1) fusion inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category B

Action

Interferes with entry of HIV-1 into cells by inhibiting fusion of viral and cellular membranes

Availability

Powder for injection: 90 mg/1-ml vial

Indications and dosages

HIV-1 infection in adults in combination with other antiretrovirals

Adults: 90 mg subcutaneously b.i.d. in upper arm, anterior thigh, or abdomen

Children ages 6 to 16: 2 mg/kg subcutaneously b.i.d. in upper arm, anterior thigh, or abdomen. Maximum dosage is 90 mg b.i.d.

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• increased risk of pneumonia

• injection site reaction

• concurrent use of anticoagulants

• hemophilia or other coagulant disorders

• elderly patients

• children younger than age 6 (safety and efficacy not established).

Administration

• Rotate injection sites.

• Be aware that preferred injection sites are upper arm, anterior thigh, and abdomen.

• Reconstitute with 1.1 ml of sterile water for injection, and gently tap vial for 10 seconds. Then gently roll vial between hands or allow vial to stand until product dissolves completely (could take up to 45 minutes).

• Know that drug is usually given with other antiretrovirals.

• Use reconstituted solution immediately.

Adverse reactions

CNS: fatigue, asthenia, insomnia, depression, anxiety, peripheral neuropathy

EENT: conjunctivitis, sinusitis

GI: nausea, diarrhea, upper abdominal pain, dry mouth, anorexia, pancreatitis

Hematologic: lymphadenopathy

Musculoskeletal: limb pain, myalgia

Respiratory: cough, pneumonia

Skin: folliculitis

Other: taste disturbance, decreased appetite, weight loss, herpes simplex infection, injection site reactions (erythema, induration, nodules, cysts, mild to moderate pain, infection), flulike illness, hypersensitivity reactions

Interactions

Drug-diagnostic tests. Alanine aminotransferase, amylase, aspartate aminotransferase, creatine kinase, eosinophils, gamma-glutamyltransferase, lipase, triglycerides: increased levels

Hemoglobin: decreased level

Patient monitoring

• Inspect injection sites frequently for adverse reactions.

• Monitor CBC with white cell differential, lipid panel, liver function test results, and gastric enzymes levels.

• Watch for hypersensitivity reactions.

• Monitor nutritional and hydration status in light of GI adverse effects and underlying disease.

Patient teaching

• Teach patient (or caregiver) how to reconstitute and self-administer drug, as appropriate.

Instruct patient not to change dosage or stop taking drug unless prescriber approves.

Tell patient to immediately report signs or symptoms of hypersensitivity reaction (such as rash, fever, nausea and vomiting, and chills).

• Teach patient how to recognize signs and symptoms of injection site reaction. Tell him to contact prescriber if these occur, especially if they last more than 7 days.

• Advise female patient to notify prescriber if she is pregnant or plans to become pregnant.

• Tell HIV-infected patient not to breastfeed.

• If patient misses a dose, instruct him to take it as soon as he remembers. However, if it's almost time for next dose, tell him to skip the missed dose and take next dose on schedule.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the tests mentioned above.

enfuvirtide

(ĕn-fyo͞o′vîr-tīd′)
n.
An antiretroviral drug of the fusion inhibitor class used in combination with other drugs to treat HIV infection.

enfuvirtide

The first of a new class of anti-HIV drugs. Enfuvirtide (Fuzeon) interferes with the mechanism by which the membranes of HIV and of the target T cell fuse together so as to allow insertion of the viral genome. The drug is currently unique in that it attacks the virus before the T cell is infected. It does so by binding to a region of the envelope and blocking the conformational change necessary for fusion. Unfortunately, the drug, which requires twice-daily injections, is extremely expensive. A brand name is Fuzeon.
References in periodicals archive ?
O'Hearn et al., "Enfuvirtide, an HIV 1 fusion inhibitor, for drug-resistant HIV infection in North and South America," The New England Journal of Medicine, vol.
Enfuvirtide, an HIV-1 fusion inhibitor, for drug-resistant HIV infection in North and South America.
The above findings suggest that a CD4 molecule, CD4 domain, or small-molecule CD4 mimetic can trigger the HIV-1 Env conformation change, resulting in the exposure of some conserved epitopes or region in gp120 or gp41, which can serve as a target for antibodies with a neutralizing effect of ADCC effect, or for peptide-based HIV-1 fusion inhibitors, such as enfuvirtide. These strategies have potential for use in clinics towards a functional HIV cure.
Gourmel et al., "Decreases in inflammatory and coagulation biomarkers levels in HIV-infected patients switching from enfuvirtide to raltegravir: ANRS 138 substudy," Journal of Infectious Diseases, vol.
During the study, in the event of discontinuation of lopinavir/ritonavir because of treatment failure or adverse events, a large range of antiretroviral drugs have been utilized in this population, including other protease inhibitors, efavirenz and more recently raltegravir and enfuvirtide.
[33] The nucleoside reverse-transcriptase inhibitors (NRTIs), as well as the newer fusion inhibitor (enfuvirtide) and integrase inhibitor (raltegravir) are not metabolised significantly by the CYP system, making them less vulnerable to interactions with psychotropic medications.
Due to disadvantages of enfuvirtide (fuzeon), scientists have tried to discover small molecules which inhibit fusion process.
The first protease inhibitor (saquinavir) was approved in 1995 and the first fusion inhibitor (enfuvirtide) in 2003.
Enfuvirtide (T20) fue comprado a Roche (Palo Alto, CA).
These studies have included the addition of agents, such as enfuvirtide, additional protease inhibitors (ritonavir-boosted atazanavir or lopinavir) or raltegravir, to an already suppressive regimen Disappointingly, none of these studies have demonstrated any decline in low-level viraemia, IUPM or cell-associated HIV DNA.
FDA-Approved Antiretroviral Agents Nucleoside RTIs Nonnucleoside RTIs Protease inhibitors abacavir (ABC) delavirdine (DLV) atazanavir (ATV) didanosine (ddl) efavirenz (EFZ) darunavir (DRV) emtricitabine (FTC) etravirine (ETV) fosamprenavir (Fos-APV) lamivudine (3TC) nevirapine (NVP) indinavir (IDV) stavudine (d4T) lopinavir/r (LPV/r) zidovudine (ZDV) nelfinavir (NFV) ritonavir (RTV) saquinavir (SQV) tipranavir (TPV) Nucleotide RTI Integrase inhibitor Fusion inhibitor tenofovir DF (TDF) raltegravir (RAL) enfuvirtide (T-20) CCR5 antagonist maraviroc (MVC) Notes: Six fixed-dose combinations are approved by the Food and Drug Administration.
Emergence and Evolution of Enfuvirtide Resistance following Long-Term Therapy Involves Heptad Repeat 2 Mutations within gp41.