Etravirine

What is Etravirine?

• Etravirine (INTELENCE) is a human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitor (NNRTI).

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Etravirine

Etravirine molecule ball

What are the uses of this medicine?

INTELENCE is a prescription HIV medicine that:

• is used with other HIV medicines to treat HIV (Human Immunodeficiency Virus) infection in adults and children 6 years of age and older. HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome). INTELENCE® is a type of HIV medicine called a non-nucleoside reverse transcriptase inhibitor (NNRTI).
• is used in people who are already taking or have taken NNRTI and other HIV medicines and these medicines are not controlling their HIV infection.

How does this medicine work?

• Etravirine is an antiviral drug.
• Etravirine is an NNRTI of human immunodeficiency virus type 1 (HIV-1).
• Etravirine binds directly to reverse transcriptase (RT) and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site.
• Etravirine does not inhibit the human DNA polymerases α, β, and γ.

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

INTELENCE® should not be co-administered with the following antiretrovirals:

• Tipranavir/ritonavir, fosamprenavir/ritonavir, atazanavir/ritonavir
• Protease inhibitors administered without ritonavir
• NNRTIs

• Co-administration of INTELENCE® with drugs that inhibit or induce CYP3A, CYP2C9, and/or CYP2C19 is not recommended.
• Co-administration of INTELENCE® with drugs that are substrates of CYP3A, CYP2C9, and/or CYP2C19 is not recommended.

Is this medicine FDA approved?

• Initial U.S. Approval: 2008

How should this medicine be used?

Recommended dosage: Adult Patients

• The recommended oral dose of INTELENCE® tablets is 200 mg (one 200 mg tablet or two 100 mg tablets) taken twice daily following a meal.

Pediatric Patients (6 years to less than 18 years of age)

• The recommended dose of INTELENCE® for pediatric patients 6 years to less than 18 years of age and weighing at least 16 kg is based on body weight as shown below not exceeding the recommended adult dose. INTELENCE tablet(s) should be taken orally, following a meal.

Weight
kilograms (kg)	Dose
greater than or equal to 16 kg to less than 20 kg	100 mg twice daily
greater than or equal to 20 kg to less than 25 kg	125 mg twice daily
greater than or equal to 25 kg to less than 30 kg	150 mg twice daily
greater than or equal to 30 kg	200 mg twice daily

Administration:

• Take INTELENCE® tablets every day exactly as prescribed by your doctor.
• Your doctor will tell you how many INTELENCE® tablets to take and when to take them. Talk to your doctor if you have questions about when to take INTELENCE®.
• INTELENCE® is taken two times each day.

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• If your child takes INTELENCE®, your doctor will prescribe the right dose based on your child's weight.
• Always take INTELENCE® following a meal. Do not take INTELENCE® on an empty stomach. INTELENCE® may not work as well if you take it on an empty stomach.
• Do not change your dose or stop taking INTELENCE® without first talking with your doctor. See your doctor regularly while taking INTELENCE®.
• Swallow INTELENCE® whole, with a glass of water. Do not chew the tablet(s).
• If you are unable to swallow INTELENCE® tablets whole, you may take your dose of INTELENCE® as follows:

• Step 1: Measure approximately 5 mL (1 teaspoon) of water and pour into a cup.
• Step 2: Place the tablets in the cup containing 5 mL of water. If needed, add more water to cover the tablets. Do not put the tablets in other liquids.
• Step 3: Stir well until the water looks milky.
• Step 4: At this step, you may add a small amount of water, orange juice or milk to make it easier to take.
• Step 5: Drink right away.

• Step 6: Add more water, orange juice or milk to the cup to rinse the cup several times and completely swallow each time to make sure you take your entire dose of INTELENCE®.

• Avoid using grapefruit juice or warm (more than 104°F or 40°C) or carbonated beverages when taking INTELENCE® tablets.
• When your supply of INTELENCE® starts to run low, get more from your doctor or pharmacy. It is important not to run out of INTELENCE®. The amount of HIV in your blood may increase if the medicine is stopped even for a short time.
• If you miss a dose of INTELENCE® within 6 hours of the time you usually take it, take your dose of INTELENCE® following a meal as soon as possible. Then, take your next dose of INTELENCE® at the regularly scheduled time. If you miss a dose of INTELENCE® by more than 6 hours of the time you usually take it, wait and then take the next dose of INTELENCE® at the regularly scheduled time.
• Do not take more than your prescribed dose to make up for a missed dose.
• If you take too much INTELENCE®, contact your local poison control center or go to the nearest emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 25 mg tablets, 100 mg tablets and 200 mg tablets

This medicine is available in fallowing brand namesː

• INTELENCE®

What side effects can this medication cause?

• In adults, common side effects include tingling, numbness, or pain in the hands or feet.
• In children, diarrhea

INTELENCE® can cause serious side effects including:

• Severe skin rash and allergic reactions
• Changes in body fat
• Changes in your immune system (Immune Reconstitution Syndrome)

What special precautions should I follow?

• Severe, potentially life threatening and fatal skin reactions have been reported. This includes cases of Stevens-Johnson syndrome, hypersensitivity reaction, toxic epidermal necrolysis and erythema multiforme. Immediately discontinue treatment if severe hypersensitivity, severe rash or rash with systemic symptoms or liver transaminase elevations develops and monitor clinical status, including liver transaminases closely.

What to do in case of emergency/overdose?

• Human experience of overdose with INTELENCE® is limited. The highest dose studied in healthy volunteers was 400 mg once daily.

Management of overdosage:

• Treatment of overdose with INTELENCE® consists of general supportive measures including monitoring of vital signs and observation of the clinical status of the patient.
• If indicated, elimination of unabsorbed active substance is to be achieved by emesis or gastric lavage.
• Administration of activated charcoal may also be used to aid in removal of unabsorbed active substance.
• Because etravirine is highly protein bound, dialysis is unlikely to result in significant removal of the active substance.

Can this medicine be used in pregnancy?

• INTELENCE® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Treatment with INTELENCE® is not recommended in children less than 6 years of age.

What are the active and inactive ingredients in this medicine?

• Active ingredient: etravirine.

• 25 mg and 100 mg INTELENCE® tablets contain the following inactive ingredients: hypromellose, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium, magnesium stearate and lactose monohydrate

• 200 mg INTELENCE® tablets contain the following inactive ingredients: hypromellose, silicified microcrystalline cellulose, microcrystalline cellulose, colloidal silicon dioxide, croscarmellose sodium and magnesium stearate.

Who manufactures and distributes this medicine?

• Product of Belgium
• Finished Product Manufactured by:

Janssen Cilag S.p.A., Latina, Italy

• Manufactured for:

Janssen Therapeutics, Division of Janssen Products, LP, Titusville NJ

What should I know about storage and disposal of this medication?

• Store INTELENCE® tablets at 59°F to 86°F (15°C to 30°C).
• Keep INTELENCE® in the original bottle given to you by your pharmacist. After opening, keep the bottle tightly closed to protect INTELENCE® from moisture.
• The INTELENCE® bottle contains a desiccant packet to help keep your medicine dry (protect it from moisture). The bottle of 25 mg tablets contains 2 desiccant packets. The bottles of 100 mg and 200 mg tablets contain 3 desiccant packets. Keep the desiccant packets in the bottle. Do not eat the desiccant packets.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Etravirine
• FDA Etravirine

Etravirine Resources
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