Isentress 400 mg is a prescription antiretroviral medication containing raltegravir, an integrase strand transfer inhibitor (INSTI), used to manage HIV-1 infection in adults and pediatric patients weighing at least 2 kg. It works by blocking the HIV integrase enzyme, preventing the virus from multiplying and reducing viral load, which helps strengthen the immune system and lower the risk of HIV-related complications. Isentress is not a cure for HIV or AIDS but is a critical component of combination antiretroviral therapy (ART). Manufactured by Merck Sharp & Dohme Corp., it is trusted for its efficacy and safety when used as prescribed.

Key Features

• Active Ingredient: Raltegravir (400 mg per film-coated tablet).

• Indications: Used in combination with other antiretroviral drugs to treat HIV-1 infection in treatment-naïve or treatment-experienced patients. Additionally approved for use as post-exposure prophylaxis (PEP) if started within 72 hours of potential HIV exposure.

• Form: Pink, oval, film-coated tablet marked with “227” on one side, supplied in bottles of 60 tablets.

• Dosage:

  • Adults: Typically 400 mg twice daily, with or without food. The dosage of rifampin may be increased to 800 mg twice daily for patients.

  • Pediatric (≥25 kg and able to swallow tablets): 400 mg twice daily.

  • Always follow your healthcare provider’s dosing instructions.

• NDC: 00006-0227-61.

Benefits

• Effective HIV Management: Reduces viral load and increases CD4 cell counts, improving immune function and reducing the risk of AIDS-related illnesses.

• Flexible Administration: Can be taken with or without food, offering convenience for daily use.

• Pediatric Use: Chewable tablets or oral suspension are available for children who are unable to swallow tablets and are suitable for children weighing at least 2 kg.

• Well-Tolerated: Most side effects are mild and temporary, making it suitable for long-term use under medical supervision.

How It Works
Isentress 400 mg contains raltegravir, which inhibits the HIV integrase enzyme, preventing the integration of viral DNA into human cells. This action stops HIV from replicating, reducing the viral load and supporting immune system recovery. It is most effective when used in combination with other HIV medications as part of a comprehensive ART regimen.

Usage Instructions

• Administration:  Take the tablet whole with a glass of water for administration.  Do not crush, chew, or break the tablet, as this may affect its efficacy.

• Timing: Take at the same time daily to maintain consistent drug levels. If you miss a dose, take it as soon as you remember, unless the next dose is almost due.

• Precautions:

  • Avoid antacids containing aluminum or magnesium within 2 hours before or after taking Isentress, as they may reduce its absorption.

  • Do not take with St. John’s Wort, phenobarbitone, carbamazepine, or fosphenytoin, as these may decrease effectiveness.

• Storage: Store the bottle tightly closed at room temperature (below 30°C), away from moisture.

Side Effects
The majority of side effects are not severe and go away as the body adjusts. Common side effects include:

• Nausea, headache, fatigue, diarrhea, dizziness, insomnia, rash, and elevated liver enzymes. Side effects that are rare but serious (seek immediate medical attention):

• Allergic reactions (fever, rash, swelling, trouble breathing).

• Severe liver issues (yellowing of skin/eyes, dark urine).

• Muscle pain or weakness (possible rhabdomyolysis).

Precautions and Warnings

• Allergies: Inform your doctor if you have allergies to raltegravir or any tablet ingredients (contains lactose monohydrate).

• Medical Conditions: Use with caution if you have liver disease, kidney issues, or a history of mental health problems. No dose adjustment is needed for mild to moderate liver or kidney impairment, but caution is advised for severe liver disease.

• Pregnancy/Breastfeeding: Not recommended unless benefits outweigh risks; consult your doctor. HIV-positive women should avoid breastfeeding to prevent transmission.

• Drug Interactions: Inform your doctor about all medications, including antacids, rifampin, or other antiretrovirals, to avoid interactions.

• Driving: May cause dizziness or fatigue; avoid driving or operating machinery if affected.

Who Should Use Isentress 400 mg?

• Adults and children (≥2 kg) with HIV-1 infection, as part of combination therapy.

• Individuals requiring PEP after potential HIV exposure (within 72 hours).

• Not suitable for those with hypersensitivity to raltegravir or severe liver disorders without medical guidance.