Product image of Isentress (Raltegravir) supplied by GNH India

Isentress

Active Ingredient:
Raltegravir
Origin:
EU

Isentress (Raltegravir)

Raltegravir, the active ingredient in Isentress, is an integrase strand transfer inhibitor presented as a tablet for oral use. It belongs to the antiretroviral therapeutic class and is indicated for the treatment of HIV-1 infection in combination with other antiretroviral agents, helping to suppress viral replication in adults and adolescents. The medication is formulated to provide consistent plasma concentrations, supporting adherence to daily regimens and reducing the risk of resistance development.

GNH India supplies Isentress as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide.

Manufacturer / TM Owner

Merck Sharp & Dohme B.V.

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Indications & Clinical Uses

  • Isentress (raltegravir) is used in antiretroviral therapy targeting the HIV integrase pathway to control viral replication.
  • HIV‑1 infection (adults): Used with other antiretrovirals to achieve and maintain viral suppression.
  • HIV‑1 infection (adolescents): Combined with a full regimen to control viral load and improve immune function.
  • HIV‑1 infection (treatment‑experienced patients): Provides an alternative integrase inhibitor option for those with resistance to other classes.

How It Works

  • Raltegravir binds to the active site of the HIV‑1 integrase enzyme, blocking the strand transfer step required for integration of viral DNA into the host genome. By preventing this critical step, the drug stops the establishment of proviral DNA, thereby inhibiting replication of HIV and allowing the immune system to recover when used as part of combination antiretroviral therapy.

Side Effects

Common and serious adverse reactions have been reported with raltegravir use.

Common Side Effects

  • Nausea
  • Diarrhea
  • Headache
  • Fatigue
  • Insomnia
  • Rash

Serious or Rare Side Effects

  • Severe allergic reactions (anaphylaxis)
  • Hepatotoxicity (elevated liver enzymes)
  • Rhabdomyolysis (muscle breakdown)
  • Stevens‑Johnson syndrome or toxic epidermal necrolysis
  • Depression or mood changes
  • Elevated creatine kinase levels

Precautions & Warnings

  • When prescribing raltegravir, clinicians should consider several safety and handling precautions.
  • Assess renal function: Adjust use in patients with severe renal impairment.
  • Monitor liver enzymes: Watch for signs of hepatotoxicity during therapy.
  • Check for drug resistance: Ensure viral susceptibility before initiating raltegravir.
  • Avoid in patients with known hypersensitivity to raltegravir or any tablet components.
  • Pregnancy considerations: Discuss potential risks and benefits with the prescriber.
  • Store at room temperature: Keep in the original container, protect from moisture and heat.

Avoid Interactions

Raltegravir may interact with other medicines, affecting its effectiveness or safety.

Major Interactions (Avoid)

  • Co‑administration with strong CYP3A inducers (e.g., rifampin) can markedly reduce raltegravir exposure.
  • Use with antacids containing aluminum or magnesium may decrease absorption of raltegravir.

Moderate Interactions (Monitor Closely)

  • Concurrent use with other integrase inhibitors may increase risk of overlapping toxicity.
  • Combination with certain statins (e.g., rosuvastatin) may raise statin plasma levels.
  • Use with hormonal contraceptives may reduce contraceptive efficacy.

Frequently Asked Questions

Isentress, containing raltegravir, is used as part of combination antiretroviral therapy to treat HIV‑1 infection. It helps suppress viral replication by targeting the integrase enzyme, and is prescribed for adults, adolescents, and treatment‑experienced patients when a potent regimen is required.

Raltegravir inhibits the HIV‑1 integrase enzyme, specifically blocking the strand‑transfer step that inserts viral DNA into the host genome. By preventing this integration, the drug stops the formation of proviral DNA, thereby halting HIV replication and allowing the immune system to recover when used with other antiretrovirals.

The dose of Isentress is individualized by the prescribing healthcare professional based on factors such as the patient’s age, weight, renal function, and the composition of the accompanying antiretroviral regimen. No fixed dose is provided here; the prescriber sets the appropriate regimen.

Safety data for raltegravir in pregnancy and lactation are limited. The drug should only be used if the potential benefit to the mother outweighs any possible risk to the fetus or infant. Clinicians should discuss individual circumstances with the patient and consider alternative options when appropriate.

To order Isentress, submit an enquiry on the product page at gnhindia.com, specifying the required quantity. GNH India supplies hospitals, pharmacies and procurement teams worldwide, and will request verification of trade or institutional credentials before providing pricing, availability, shipping details and any necessary import documentation.

Isentress (raltegravir) was the first integrase strand transfer inhibitor approved and is known for a favorable safety profile and rapid viral suppression. Compared with newer agents such as dolutegravir, raltegravir may require twice‑daily dosing and has a lower barrier to resistance, but it remains an effective option for patients with specific resistance patterns.

Isentress tablets should be stored at room temperature, below 25 °C, in the original blister pack to protect them from moisture and light. Keep the product out of reach of children and avoid exposure to extreme heat or humidity, which could affect tablet integrity.

Isentress is taken orally, usually as a tablet swallowed with water. The exact dosing schedule—once or twice daily—depends on the prescriber’s instructions and the overall antiretroviral regimen. Patients should follow the healthcare provider’s guidance and not alter the dosing without medical advice.

Serious risks include severe allergic reactions such as anaphylaxis, liver toxicity indicated by elevated transaminases, muscle breakdown (rhabdomyolysis) with high creatine kinase levels, and rare but life‑threatening skin conditions like Stevens‑Johnson syndrome. Patients should seek immediate medical attention if they experience symptoms such as rash, jaundice, muscle pain, or breathing difficulties.

Isentress should be avoided in individuals with known hypersensitivity to raltegravir or any of the tablet excipients. Caution is also advised for patients with severe renal impairment, uncontrolled liver disease, or those taking medications that significantly reduce raltegravir exposure, unless the prescriber determines the benefits outweigh the risks.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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