RALTEGRAVIR
Background and Date of Approval
Raltegravir is an antiviral medication used to treat HIV infection. It belongs to the integrase inhibitor class of drugs, which work by reducing HIV viral load and supporting immune function. The drug represented a significant advance in HIV therapy owing to its distinct mechanism of action and rapid impact on viral load. The U.S. Food and Drug Administration approved it on October 12, 2007, establishing it as the first integrase inhibitor. Clinical trials demonstrated its capacity to substantially reduce HIV levels in both treatment-naïve and treatment-experienced patients when combined with other antiretroviral medicines. It typically forms part of a comprehensive HIV treatment regimen and has demonstrated favourable tolerability and efficacy across diverse patient populations.
Uses
Raltegravir is approved by the FDA for the following: Treatment of HIV-1 infection in adults and children aged 4 weeks and older, weighing at least 3 kg Used in combination with other antiretroviral drugs Effective for both treatment-naïve and treatment-experienced patients
How is it administered?
Raltegravir is taken by mouth and comes in tablet, chewable tablet, and oral suspension forms. The dosage depends on the patientâs age, weight, and specific medical needs. Adults are typically prescribed 400 mg twice daily or a 1200 mg once-daily dose. For children, the dose is adjusted according to body weight. It's important to follow the dosing schedule consistently and never skip doses, as doing so can affect treatment success.
Side Effects
Common Side Effects: Headache Trouble sleeping Dizziness Nausea Tiredness Diarrhea Itching or rash (usually mild) Serious Side Effects: Severe skin reactions (such as Stevens-Johnson syndrome) Liver problems (signs include yellowing of skin or eyes, dark urine) Muscle breakdown or weakness Depression or mood changes Allergic reactions like swelling of the face or lips If any serious symptoms appear, medical help should be sought immediately.
Warnings
Do not use with aluminium or magnesium-containing antacids as they reduce its effectiveness. Avoid combining with rifampin, as it can lower drug levels in the body. Use cautiously in people with a history of depression or mental illness. Not recommended in individuals with severe liver disease unless closely monitored. It may interact with warfarin and other blood thinners, so dose adjustments may be needed.
Precautions
Before starting this medicine, inform your doctor about any history of liver problems, mental health issues, or muscle disorders. If you are pregnant or planning to become pregnant, discuss the potential risks and benefits. Breastfeeding is not recommended as HIV can be passed to the baby through breast milk. Always inform your doctor about any other medications or supplements you are taking to avoid interactions. It is also important to attend regular check-ups and lab tests to monitor liver function and viral load during treatment.
Word of Advice
Take this medicine exactly as prescribed and do not discontinue even if symptoms improve. Skipped doses can permit viral replication and development of resistance. Store tablets in a dry location, protected from heat and moisture. Maintain a consistent dosing schedule to prevent missed doses; use reminders if helpful. Support treatment with adequate nutrition and regular communication with your healthcare provider regarding treatment response. This medicine is most effective when used as part of a comprehensive antiretroviral regimen that includes other antiretroviral agents.
References
https://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022145s029lbl.pdf https://www.thelancet.com/journals/laninf/article/PIIS1473-3099(13)70093-8/abstract https://eurjmedres.biomedcentral.com/articles/10.1186/2047-783X-14-S3-5 https://clinicaltrials.gov/study/NCT01767701
Frequently Asked Questions
What is the mechanism of action of Raltegravir?
Raltegravir works by blocking an enzyme called integrase, which HIV uses to insert its genetic material into human cells. By stopping this process, the virus cannot multiply or infect new cells. This helps reduce the amount of HIV in the body and improves immune function.
What is the difference between Raltegravir and Dolutegravir?
Both drugs are integrase inhibitors used to treat HIV, but Dolutegravir is newer and generally considered more potent with fewer side effects. It also has a higher barrier to resistance, meaning the virus is less likely to become resistant to it. Dolutegravir is often preferred for first-line therapy, while Raltegravir may be used in specific cases or when other drugs are not suitable.
Is Raltegravir a PEP?
Yes, Raltegravir can be used as part of post-exposure prophylaxis (PEP) to prevent HIV infection after a possible exposure. It is usually combined with two other antiretroviral drugs and must be started within 72 hours of exposure for maximum effectiveness. The typical duration of PEP is 28 days.
How much does Raltegravir cost?
In India, the cost of Raltegravir varies depending on the brand and dosage. On average, a 400 mg tablet may cost between â¹150 to â¹300 per tablet. A full monthâs supply can range from â¹9,000 to â¹18,000, depending on the prescribed dose and frequency.