Product image of Isentress (Raltegravir) supplied by GNH India

Isentress

Active Ingredient:
Raltegravir
Origin:
EU

Isentress (Raltegravir)

Raltegravir, the active ingredient in Isentress, is a integrase strand transfer inhibitor presented as an oral tablet for oral use. It is used to treat HIV-1 infection in combination with other antiretroviral agents in adults and children. It is indicated for patients with HIV-1 infection, including those who are treatment‑naïve or have experienced resistance to other antiretrovirals.

GNH India supplies Isentress as a licensed, GDP‑compliant international pharmaceutical supplier serving hospitals, pharmacies and clinics worldwide, with robust quality assurance and regulatory compliance.

Manufacturer / TM Owner

Merck Sharp & Dohme B.V.

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Indications & Clinical Uses

  • Isentress (raltegravir) is used in the management of HIV‑1 infection, a viral disease that requires combination antiretroviral therapy.
  • HIV‑1 infection (treatment‑naïve): reduces plasma viral load when combined with a backbone regimen of two nucleoside reverse transcriptase inhibitors.
  • HIV‑1 infection (treatment‑experienced): provides an effective option for patients with resistance to other drug classes.
  • Pediatric HIV‑1 infection (≥2 years of age): approved for use in combination therapy to achieve virologic suppression.

How It Works

  • Raltegravir selectively inhibits the HIV‑1 integrase enzyme, which catalyzes the insertion of viral DNA into the host cell genome. By binding to the active site of integrase, it blocks the strand‑transfer step required for integration, preventing the establishment of proviral DNA and halting subsequent viral replication. This action is independent of reverse transcriptase or protease activity.

Side Effects

Common adverse reactions to raltegravir are generally mild and transient, while rare events may be serious.

Common Side Effects

  • Nausea
  • Diarrhea
  • Headache
  • Fatigue

Serious or Rare Side Effects

  • Severe hypersensitivity reactions (e.g., Stevens‑Johnson syndrome)
  • Elevated liver enzymes or hepatic injury
  • Lactic acidosis or severe metabolic disturbances

Precautions & Warnings

  • When prescribing raltegravir, clinicians should consider several safety and handling precautions.
  • Assess renal function: adjust therapy in patients with severe renal impairment.
  • Monitor liver enzymes: watch for signs of hepatic toxicity during treatment.
  • Check for hypersensitivity: discontinue if severe rash or allergic reaction occurs.
  • Avoid use in patients with known hypersensitivity to integrase inhibitors.
  • Pregnancy and breastfeeding: discuss potential risks with the prescriber before use.
  • Store at room temperature: keep tablets in the original container, protect from moisture and heat.

Avoid Interactions

Raltegravir may interact with other medicines, affecting its plasma concentration or safety profile.

Major Interactions (Avoid)

  • Rifampin (strong CYP3A inducer): markedly reduces raltegravir exposure, compromising efficacy.
  • Co‑administration with other integrase inhibitors: may increase risk of overlapping toxicity.

Moderate Interactions (Monitor Closely)

  • Antacids containing aluminum or magnesium: can lower raltegravir absorption; separate dosing by at least 2 hours.
  • Proton pump inhibitors (e.g., omeprazole): may modestly decrease drug levels; monitor viral load.
  • Certain statins (e.g., rosuvastatin): potential for increased statin exposure; observe for muscle symptoms.

Frequently Asked Questions

Isentress, containing the active ingredient raltegravir, is used as part of combination antiretroviral therapy to treat HIV‑1 infection in adults, adolescents and children. It helps lower the amount of virus in the blood and supports immune system recovery when used with other approved HIV medicines.

Raltegravir blocks the HIV integrase enzyme, which is essential for inserting viral DNA into the host cell’s genome. By preventing this strand‑transfer step, the drug stops the virus from establishing a permanent infection in the cell, thereby inhibiting further replication of HIV.

The specific dose of Isentress is determined by the prescribing healthcare professional based on the patient’s age, weight, treatment history and the other antiretroviral agents being used. Only a qualified prescriber can set the appropriate dosing regimen.

Safety data for raltegravir in pregnancy are limited. The drug should only be used during pregnancy or while breastfeeding if the potential benefits outweigh the potential risks, and this decision must be made by the treating physician in consultation with the patient.

To order Isentress, submit an enquiry on the product page at gnhindia.com, specifying the required quantity. GNH India works with hospitals, pharmacies and procurement teams worldwide, verifies trade or institutional credentials, and then provides pricing, availability, shipping details and any necessary import documentation.

Isentress (raltegravir) is a first‑generation integrase strand transfer inhibitor, offering a well‑characterised safety profile and rapid viral suppression. Compared with newer agents such as dolutegravir, raltegravir may require twice‑daily dosing and has a slightly lower barrier to resistance, but it remains an effective option for many treatment‑naïve and treatment‑experienced patients.

Isentress tablets should be stored at room temperature, below 25 °C, in their original packaging to protect them from moisture and light. Keep the product out of reach of children and do not use if the packaging is damaged or the tablets appear discoloured.

Isentress is taken orally, usually as a tablet, with or without food. The exact timing relative to other antiretroviral medicines should follow the prescriber’s instructions, and patients should not crush or chew the tablets unless specifically directed to do so.

Serious risks include severe hypersensitivity reactions such as Stevens‑Johnson syndrome, significant liver enzyme elevations indicating hepatic injury, and rare metabolic disturbances like lactic acidosis. Patients should seek immediate medical attention if they develop rash, jaundice, unexplained fatigue, or abdominal pain.

Isentress should be avoided in individuals with known hypersensitivity to raltegravir or any other integrase strand transfer inhibitor. It is also contraindicated in patients who cannot safely take the required combination of antiretroviral agents as prescribed by their healthcare provider.

Published by

GNH India Pharmaceuticals Limited

Licensed pharmaceutical supplier

Last updated:

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