Raltegravir – HIV-1 Integrase Inhibitor Therapy

Raltegravir is a potent antiviral medication and the first representative of the human immunodeficiency virus (HIV-1) integrase strand transfer inhibitor class. The drug revolutionized antiretroviral therapy (ART) by offering a unique viral suppression mechanism that differs from traditional methods.

The mechanism of action involves blocking the catalytic activity of HIV integrase, an enzyme required for viral replication. Integrase is responsible for inserting (integrating) the HIV genetic material into the genome of the host cell (T-lymphocyte). By blocking this process, raltegravir prevents the formation of the integrated provirus, making further production of new viral particles impossible. Consequently, the viral load in the patient's blood rapidly decreases to undetectable levels. The drug is active against HIV strains resistant to other classes of medications, such as protease inhibitors or nucleoside reverse transcriptase inhibitors.

The drug is administered orally and is always used only as part of combination therapy to prevent the development of drug resistance.

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Raltegravir

Indications

Raltegravir is indicated for the treatment of HIV-1 infection in adults, adolescents, and children in the following clinical scenarios:

  • Combination ART: in combination with other antiretroviral medications for the treatment of HIV-1 infection.
  • Treatment-naïve Patients: for the treatment of patients who have not previously received antiretroviral therapy.
  • Treatment-experienced Patients: for the treatment of patients with prior therapy experience, including those with resistance to other antiviral classes.

Dosage and administration

The raltegravir dosing regimen depends on the formulation and the patient's age.

  • Standard Adult Dose: typically 400 mg twice daily or 1200 mg (two 600 mg tablets) once daily (depending on the specific formulation prescribed).
  • Administration: tablets are taken orally, with or without food. Tablets must not be chewed, broken, or crushed.
  • Pediatric Considerations: the dose is calculated based on the child's body weight; chewable tablets and powder for oral suspension are available.
  • Antacid Interaction: avoid taking antacids containing aluminum and magnesium, as they can decrease raltegravir levels in the blood.
  • Consistency: to achieve maximum efficacy, it is crucial to adhere to a strict dosing schedule and avoid missing doses.

The use of raltegravir is restricted in the following cases:

  • Hypersensitivity: known allergy to raltegravir or any of its excipients.
  • Pediatric Use: the 400 mg and 600 mg formulations are not intended for children weighing less than 25 kg and 40 kg, respectively.
  • Pregnancy and Lactation: use is only possible under strict medical supervision if the benefits outweigh the risks; HIV-infected women are advised not to breastfeed.
  • Severe Hepatic Impairment: safety data for this patient population are limited.

Most patients tolerate raltegravir well, but the following side effects may occur:

  • Neurologic: headache, insomnia, abnormal dreams, and dizziness.
  • Gastrointestinal: nausea, flatulence (bloating), diarrhea, and epigastric pain.
  • Dermatologic: skin rash (in rare cases, serious reactions such as Stevens-Johnson syndrome).
  • General: fatigue, asthenia, and fever.
  • Laboratory: increased levels of creatine kinase (may indicate muscle damage) and liver enzymes (ALT, AST).

Frequently Asked Questions

Raltegravir is an antiviral medication and the first in its class of integrase inhibitors. It works by blocking the integrase enzyme, which the HIV virus uses to insert its genetic material into the DNA of human cells (T-lymphocytes). Without this step, the virus cannot complete its replication cycle, effectively halting the spread of the infection within the body.
No, raltegravir must always be used as part of a combined antiretroviral therapy (ART) regimen, typically alongside two other medications. Using it as a monotherapy rapidly leads to the development of viral resistance, making future treatment efforts ineffective.
To effectively suppress the virus, a consistent concentration of the drug must be maintained in the bloodstream. Missing even a few doses can allow the virus to mutate and develop resistance to raltegravir. Patients are advised to take the medication at the same time every day.
In rare cases, raltegravir can cause severe skin reactions (such as Stevens-Johnson syndrome) or rhabdomyolysis (breakdown of muscle tissue). Patients should seek immediate medical attention if they experience unexplained muscle pain, weakness, or an extensive skin rash accompanied by fever.
Yes, antacids containing aluminum or magnesium can significantly decrease the absorption of raltegravir, reducing its effectiveness. If antacids are necessary, they should be taken several hours before or after raltegravir, following a consultation with a physician regarding the safe timing interval.

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Ralmac 400 mg McNeil & Argus
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McNeil & Argus

Ralmac

Raltegravir
400 mg 60 tablets
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