Overview:
Enfuvirtide is a prescription medication authorized by the U.S. (United States). Food and Drug Administration (FDA) for treating HIV (human immunodeficiency virus) infection in grown-ups and in kids of six years of age and older weighing at least 11 kilograms whose condition (infection) is not well-controlled by ongoing therapy with additional HIV drugs. Enfuvirtide is constantly utilized in combination with other HIV drugs.
How Does Enfuvirtide Work?
Enfuvirtide interrupts the entrance of HIV-1 into cells by interfering with the fusion of viral and cellular membranes. Enfuvirtide attaches to the first heptad-repeat (HR1) in the gp41 subunit of the envelope glycoprotein (viral) and controls the conformational differences needed for the fusion of viral membranes and cellular membranes.
Antiviral activity in vitro - Enfuvirtide in vitro antiviral action was evaluated by infecting additional CD4+ cell kinds with laboratory and clinical isolates of HIV-1.
Indications and Usage:
Enfuvirtide, combined with additional antiretroviral agents, is indicated for treating HIV-1 infection in therapy-experienced cases with proof of HIV-1 replication despite continuous antiretroviral treatment.
Dosage and Administration:
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Adults - The suggested dose of Enfuvirtide is 90 milligrams two times every day, injected subcutaneously into the upper arm region, anterior thigh region, or abdomen. Each injection must be delivered at a location separate from the preceding injection area and only where there is no recent injection site response from an earlier dose. Enfuvirtide should not be injected around any anatomical regions where big nerves course adjacent to the skin, like the elbow, knee, groin, or the inferior section or medial section of the buttocks, skin anomalies, involving directly over a blood vessel, into moles, scar tissue, or around the navel, surgical scars, or burn areas.
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Pediatric Patients - Inadequate data are known to demonstrate a dose recommendation of Enfuvirtide in pediatric cases below the age of six years. In pediatric cases of six years via 16 years of age, the suggested dosage of Enfuvirtide is two milligrams per kilogram two times daily up to a maximum dosage of 90 milligrams two times every day injected subcutaneously into the upper arm region, anterior thigh, or abdomen. All injections must be delivered at a location separate from the preceding injection area and only where there is no recent injection area response from an earlier dose. Enfuvirtide must not be injected into moles, scar tissue areas, the navel, or bruises.
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Directions for Use - Parenteral medication products must be examined visually for particulate issues and discoloration before administration.
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For Subcutaneous Administration - Enfuvirtide must only be reconstituted with one milliliter of sterile water for injection delivered in the convenience kit. Following the addition of sterile water, the vial must be gently swabbed for 10 seconds and then slowly rolled between the hands to prevent foaming and ensure all medicine particles are in contact with the liquid and no medicine stays on the vial wall. The vial must then be permitted to stand till the powder reaches a complete solution. This may take up to 45 minutes. The reconstitution period can be decreased by slowly rolling the vial between the hands till the derivative is totally dissolved. Before the solution is removed for administration, the vial must be examined visually to confirm that the contents are thoroughly dissolved in the solution and that the solution is transparent and without particulate matter.
If the Enfuvirtide is foamy, allow more period for it to dissolve. If there is evidence of particulate matter, the vial should not be used and must return to the pharmacy. It has no preservatives. One time reconstituted, Enfuvirtide must be injected immediately or refrigerated in the real vial until use. Reconstituted Enfuvirtide must be utilized within 24 hours. The subsequent dose of Enfuvirtide can be reconstituted in advance and should be kept in the refrigerator in the real vial and used within 24 hours. The refrigerated reconstituted solution must be taken to room temperature before the injection, and the vial must be inspected visually again to ensure that the contents are totally dissolved in the solution and that they must be transparent and without color and bubbles.
Contraindications:
Enfuvirtide is contraindicated in cases with known hypersensitivity to Enfuvirtide or any of its elements.
Warnings and Precautions:
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Local Injection Site Reactions - Most subjects obtaining Enfuvirtide in randomized, controlled, open-label, multicenter clinical practices had at least one local injection site response; it happened throughout therapy with Enfuvirtide. Symptoms may possess ache, induration, erythema, nodules, pruritus, and ecchymosis. Responses are usually current at more than one injection area. Cases must be knowledgeable about Enfuvirtide injection education to understand how to inject Enfuvirtide properly and observe carefully for manifestations of cellulitis or local infection.
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Pneumonia - An improved rate of bacterial pneumonia was seen in cases managed with Enfuvirtide in phase three clinical tests corresponding to the control arm.
It is undefined if the improved incidence of pneumonia is connected to Enfuvirtide usage. Nevertheless, due to these findings, cases with HIV-1 infection must be carefully observed for manifestations of pneumonia, particularly if they have underlying circumstances which might predispose them to pneumonia. Hazard elements for pneumonia possessed low initial CD4 cell count, increased initial viral load, intravenous drug usage, smoking, and a previous history of lung condition.
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Hypersensitivity Reactions - Systemic hypersensitivity responses have been connected with Enfuvirtide treatment and may recur on re-challenge. Hypersensitivity responses are seen as combinations of rash, fever, nausea, vomiting, rigors, hypotension, and raised serum liver transaminases. Additional adverse circumstances that may be immune-mediated and have been noted in cases obtaining Enfuvirtide possess primary immune complex response, respiratory distress, and Guillain-Barre syndrome. Cases that may develop manifestations representative of a systemic hypersensitivity response should discontinue Enfuvirtide and seek medical assessment instantly. Treatment with Enfuvirtide must not be continued following systemic manifestations compatible with a hypersensitivity response. Risk characteristics that may indicate the happening or severity of hypersensitivity to Enfuvirtide have not been specified.
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Non-HIV Infected Individuals - There is a hypothetical risk that Enfuvirtide usage may direct the production of anti-enfuvirtide antibodies, which cross-react with HIV gp41. This may cause a false positive HIV examination with an ELISA assay; a confirmatory western blot examination would be expected to be negative. Enfuvirtide has not been examined in non-HIV-infected people.
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Immune Reconstitution Syndrome - Immune reconstitution syndrome has been noted in cases managed with combination antiretroviral treatment, including Enfuvirtide. During the initial stage of combination antiretroviral therapy, cases whose immune system reacts may create an inflammatory reaction to residual opportunistic infections, which might increase the need for additional assessment and therapy.
For Patients:
What Is HIV?
HIV refers to the human immunodeficiency virus. It affects the immune system by destroying a kind of white blood cell that supports the body in fighting infection. This makes an individual at the chance for severe infections and particular cancers.
What Is AIDS?
AIDS refers to acquired immunodeficiency syndrome. It is the last stage of infection with HIV. It occurs when the body's immune system is impaired due to the virus. Not all with HIV develop AIDS.
Who Is at Risk for HIV Infection?
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People with other sexually transmitted diseases. Having an STD can improve the risk of spreading HIV.
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Drugs injected with shared needles.
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Gay men and bisexual men.
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African Americans and Latino Americans.
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People who are in risky sexual behaviors.
How Is Enfuvirtide Supplied, Stored, and Handled?
Enfuvirtide for injection is a white color to off-white colored, sterile, lyophilized powder packed in a single-usage transparent glass vial holding 108 mg of Enfuvirtide for the delivery of around 90 mg/1 mL when reconstituted with one mL of sterile water for Injection. Enfuvirtide is available in a convenience kit, including 60 single-use vials of Enfuvirtide that are 90 mg strength, 60 vials that are two cartons of 30 each of sterile water for injection, 60 reconstitution syringes, 60 administration syringes. Store at 25 degrees Celsius excursions authorized to 15 to 30 degrees Celsius. The reconstituted solution must be kept in the actual vial under refrigeration at two to eight-degree celsius and utilized within 24 hours.
How Should This Medicine Be Used?
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Enfuvirtide is a powder that can be combined with sterile water and can be injected subcutaneously. It is typically injected two times a day. Track the directions on the prescription label thoroughly, and ask the doctor or pharmacist to clarify any section that is not understood. Use Enfuvirtide precisely as directed. Enfuvirtide controls HIV but does not heal it. Resume using Enfuvirtide even if feeling well. Do not quit using Enfuvirtide without discussing it with the doctor. In case of missed doses or stopping using Enfuvirtide, the condition may evolve more challenging to treat. When the supply of Enfuvirtide begins to run low, get more from the doctor or pharmacist. The first dose of Enfuvirtide is delivered to the patient in the doctor's office. Afterward, the patient can inject Enfuvirtide themselves or have a friend or relative conduct the injections. The doctor will train the individual to inject the medicine and train him to be sure he can deliver the injection accurately. Be sure that the patient and the person providing the injections have read and understood the manufacturer's details for the patient with Enfuvirtide prior to the usage for the first time at home.
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Enfuvirtide can be injected anywhere on the front of the thighs, stomach, or upper arms. Do not inject Enfuvirtide inside or near the navel or in any location directly under a belt or waistband; around the elbow, knee, groin, buttocks; or straight over a blood vessel. Choose another area for each injection to decrease the possibility of soreness. Maintain track of the sites where the Enfuvirtide is injected, and do not deliver an injection into the exact area twice in a row. Never reuse needles, syringes, and Enfuvirtide vials. Dispose of utilized needles and syringes in a puncture-resistant receptacle. Ask the doctor for a document of the manufacturer's injection details for the patient. Carefully follow the manufacturer's instructions to prepare and inject the dose. Ask the doctor or pharmacist in case of inquiries about how to inject Enfuvirtide.
What Are the Side Effects of Enfuvirtide?
Enfuvirtide may induce side effects. Inform the doctor if any of these manifestations are extreme.
Enfuvirtide may cause a range of side effects, including
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The injection site's local reactions include itching, inflammation, ache, tingling, distress, bruising, or bumps.
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Hardship in falling asleep or staying asleep, depression, nervousness, tiredness, muscle ache, nausea, appetite loss, changes in the ability to taste food, weight loss, diarrhea, constipation, flu-like manifestations, and runny nose with sinus aches.
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Warts or cold sores, swollen glands, painful, red, or teary eyes.
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Some side effects can be severe and demand immediate medical attention, such as:
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Severe aches, oozing, warmth, or redness at the injection area.
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Rash, fever, vomiting, nausea with rash and fever, chills, fainting, dizziness, blurred vision, cough, hardship breathing, blood in urine, inflamed feet, quick breathing, shortness of breath, burning, numbness in the feet, pale stools, yellowing of the skin or eyes.
For Doctors:
Clinical Pharmacology:
Mechanism of Action - Enfuvirtide is an antiretroviral medicine.
Pharmacokinetics - The pharmacokinetic effects of Enfuvirtide were assessed in HIV-1 infected grown-up and pediatric cases.
Enfuvirtide interrupts the entry of HIV-1 into cells by interfering with fusion of viral membranes and cellular membranes. Enfuvirtide attaches to the first heptad-repeat in the gp41 subunit of the viral envelope glycoprotein and controls the conformational differences needed for the fusion of viral membranes and cellular membranes.
Nonclinical Toxicology:
Carcinogenesis, Mutagenesis, and Impairment of Fertility:
Carcinogenesis and Mutagenesis - Carcinogenicity investigations have not been performed with Enfuvirtide. Enfuvirtide was not genotoxic in vivo and in vitro assays involving a bacterial reverse mutation assay and an in vivo mouse micronucleus assay.
Impairment of Fertility - In a fertility developmental study and early embryonic development study done in rats, no outcomes of Enfuvirtide on male fertility or female fertility were seen at Enfuvirtide exposures up to 1.6 times more elevated than human exposure at the recommended human dose.
Use in Specific Populations:
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Pregnancy - A pregnancy exposure registry that observes pregnancy outcomes in people exposed to Enfuvirtide during pregnancy. In animal reproduction examinations, no adverse developmental outcomes were seen with subcutaneous administration of Enfuvirtide at exposures more significant than or equal to around two times higher than human exposure at the recommended human dose found on the surface area.
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Lactation - No human data is known about the presence of Enfuvirtide or its metabolites in human milk, the consequences on the breastfed baby, or the results on milk production. When Enfuvirtide was distributed to lactating rats, Enfuvirtide was probably present in the milk because of both the potential for HIV-1 transmission in HIV-negative infants, generating viral resistance in HIV-positive infants, and adverse responses in breastfed infants compared to those seen in grown-ups, advise mothers stop breastfeeding if they are taking Enfuvirtide.
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Pediatric Use - The use of Enfuvirtide in pediatric cases weighing at least 11 kilograms is supported by proof from acceptable and well-controlled analyses of Enfuvirtide in grown-up and by two pediatric examinations assessing the safety, pharmacokinetics, and efficacy of Enfuvirtide in subjects six years of age and more aged.
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Hepatic and Renal Impairment - No dosage alteration of Enfuvirtide is required in cases with hepatic impairment.
