Raltegravir

What is Raltegravir?

• Raltegravir (Isentress) is a human immunodeficiency virus integrase strand transfer inhibitor (HIV-1 INSTI) used in combination with other antiretroviral agents for the treatment of HIV-1 infection.

Raltegravir structure

Raltegravir-3D-balls

Raltegravir-3D-spacefill

What are the uses of this medicine?

• Raltegravir (ISENTRESS) is a prescription HIV medicine used with other HIV medicines to treat adults and children 2 years of age and older with human immunodeficiency virus (HIV-1) infection. HIV is the virus that causes AIDS (Acquired Immune Deficiency Syndrome).

How does this medicine work?

• Raltegravir (ral teg' ra vir) is relatively new antiretroviral drug that targets the HIV integrase, one of the three enzymes involved in viral replication.
• Raltegravir blocks the binding site of the HIV integrase and prevents the strand transfer activity and integration of the provirus into the host genome.
• Raltegravir has both in vitro and in vivo activity against HIV, and several randomized controlled trials have shown that it leads to significant decline in HIV RNA levels and rises in peripheral CD4 T cell counts.
• When used with other HIV medicines, ISENTRESS may reduce the amount of HIV in your blood (called "viral load").
• ISENTRESS may also help to increase the number of CD4 (T) cells in your blood which help fight off other infections.
• Reducing the amount of HIV and increasing the CD4 (T) cell count may improve your immune system.
• This may reduce your risk of death or infections that can happen when your immune system is weak (opportunistic infections).

Who Should Not Use this medicine ?

• This medicine have no usage limitations.

What drug interactions can this medicine cause?

Coadministration of ISENTRESS with drugs that are strong inducers of UGT1A1 may result in reduced plasma concentrations of raltegravir. In drug interaction studies, raltegravir did not have a clinically meaningful effect on the pharmacokinetics of the following: hormonal contraceptives, methadone, lamivudine, tenofovir, etravirine, darunavir/ritonavir.

Taking ISENTRESS and certain other medicines may affect each other causing serious side effects. ISENTRESS may affect the way other medicines work and other medicines may affect how ISENTRESS works. Especially tell your doctor if you take:

• rifampin (Rifadin, Rifamate, Rifater, Rimactane), a medicine commonly used to treat tuberculosis.

Is this medicine FDA approved?

• Raltegravir was given accelerated approval for use in HIV infection in the United States in 2007 and is currently used in an increasing proportion of antiretroviral regimens.

How should this medicine be used?

Recommended dosage: Adults

• 400 mg film-coated tablet orally, twice daily.
• During coadministration with rifampin in adults, 800 mg twice daily.

Children and Adolescents

• 12 years of age and older: One 400 mg film-coated tablet orally, twice daily.

6 to less than 12 years of age:

• If at least 25 kg in weight:

One 400 mg film-coated tablet orally, twice daily OR Chewable tablets: weight based to maximum dose 300 mg twice daily.

• If less than 25 kg in weight:

Chewable tablets: weight based to maximum dose 300 mg twice daily.

2 to less than 6 years of age: If at least 10 kg in weight: Chewable tablets: weight based to maximum dose 300 mg twice daily

Recommended Dose for ISENTRESS Chewable Tablets in Pediatric Patients 2 to Less Than 12 Years of Age

Body Weight(kg)	Dose	Number of Chewable Tablets
10 to less than 14	75 mg twice daily	3 × 25 mg twice daily
14 to less than 20	100 mg twice daily	1 × 100 mg twice daily
20 to less than 28	150 mg twice daily	1.5 × 100 mg twice daily
28 to less than 40	200 mg twice daily	2 × 100 mg twice daily
at least 40	300 mg twice daily	3 × 100 mg twice daily

Administration:

• Take ISENTRESS exactly as prescribed by your doctor.
• You should stay under the care of your doctor while taking ISENTRESS.
• Do not change your dose of ISENTRESS, switch between the film-coated tablet and the chewable tablet or stop your treatment without talking with your doctor first.
• Take ISENTRESS by mouth, with or without food.
• If your child is taking ISENTRESS, your child's doctor will decide the right dose based on your child's age and weight.
• ISENTRESS Chewable Tablets may be chewed or swallowed whole.
• ISENTRESS Film-Coated Tablets must be swallowed whole.
• If you miss a dose, take it as soon as you remember. If you do not remember until it is time for your next dose, skip the missed dose and go back to your regular schedule. Do not double your next dose or take more than your prescribed dose.
• If you take too much ISENTRESS, call your doctor or go to the nearest emergency room right away.
• Do not run out of ISENTRESS. Get your ISENTRESS refilled from your doctor or pharmacy before you run out.

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

This medicine is available in fallowing doasage form:

• As Film-Coated Tablets: 400 mg.
• Chewable Tablets: 100 mg scored and 25 mg

This medicine is available in fallowing brand namesː

• ISENTRESS

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• trouble sleeping

Less common side effects include:

• nausea
• tiredness
• weakness
• stomach pain
• dizziness
• depression
• suicidal thoughts and actions

ISENTRESS can cause serious side effects including:

• Serious skin reactions and allergic reactions
• Immune Reconstitution Syndrome
• Phenylketonuria (PKU)

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 and toxic epidermal necrolysis. Immediately discontinue treatment with ISENTRESS and other suspect agents if severe hypersensitivity, severe rash, or rash with systemic symptoms or liver aminotransferase elevations develops and monitor clinical status, including liver aminotransferases closely.
• Monitor for Immune Reconstitution Syndrome .
• Inform patients with phenylketonuria that the 100 mg and 25 mg chewable tablets contain phenylalanine. Each 100 mg ISENTRESS Chewable Tablet contains approximately 0.10 mg phenylalanine. Phenylalanine can be harmful to patients with phenylketonuria.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• No specific information is available on the treatment of overdosage with ISENTRESS.

Management of overdosage:

• In the event of an overdose, it is reasonable to employ the standard supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.
• The extent to which ISENTRESS may be dialyzable is unknown.

Can this medicine be used in pregnancy?

• ISENTRESS should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
• There are no adequate and well-controlled studies in pregnant women.
• Pregnancy Category C.

Can this medicine be used in children?

• Safety and effectiveness of ISENTRESS in children under 2 years of age have not been established.
• It is not known if ISENTRESS is safe and effective in children under 2 years of age.

What are the active and inactive ingredients in this medicine?

ISENTRESS Film-Coated Tablets:

• Active ingredient: raltegravir
• Inactive ingredients: microcrystalline cellulose, lactose monohydrate, calcium phosphate dibasic anhydrous, hypromellose 2208, poloxamer 407 (contains 0.01% butylated hydroxytoluene as antioxidant), sodium stearyl fumarate, magnesium stearate.
• The film coating contains: polyvinyl alcohol, titanium dioxide, polyethylene glycol 3350, talc, red iron oxide and black iron oxide.

ISENTRESS Chewable Tablets:

• Active ingredient: raltegravir
• Inactive ingredients: hydroxypropyl cellulose, sucralose, saccharin sodium, sodium citrate dihydrate, mannitol, red iron oxide (100 mg tablet only), yellow iron oxide, monoammonium glycyrrhizinate, sorbitol, fructose, natural and artificial flavors (orange, banana, and masking that contains aspartame), crospovidone, magnesium stearate, sodium stearyl fumarate, ethylcellulose 20 cP, ammonium hydroxide, medium chain triglycerides, oleic acid, hypromellose 2910/6cP, PEG 400.

Who manufactures and distributes this medicine?

Distributed by:

• Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc.

Whitehouse Station, NJ , USA

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

Film-Coated Tablets:

• Store ISENTRESS Film-Coated Tablets at room temperature between 68°F to 77°F (20°C to 25°C).

Chewable Tablets:

• Store ISENTRESS Chewable Tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Store ISENTRESS Chewable Tablets in the original package with the bottle tightly closed.
• Keep the drying agent (desiccant) in the bottle to protect from moisture.

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 Raltegravir
• FDA Raltegravir

Raltegravir Resources
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