Raltegravir 💊
💊 About
Raltegravir is a first-in-class HIV-1 integrase strand transfer inhibitor (INSTI).
It blocks the integration of viral DNA into the host genome — a key step in the HIV replication cycle.
Always 🔗 check the BNF entry for current dosing, cautions, and interactions.
🧠 Mode of Action
- Acts as a selective integrase inhibitor.
- Prevents strand transfer — the final step of integration of HIV DNA into host DNA.
- By halting integration, viral replication is disrupted and new virions cannot form.
📋 Indications & Dosing
- Used in combination antiretroviral therapy (ART) for treatment of HIV-1 infection.
- Particularly useful in patients with resistance to other classes of antivirals.
- Typical adult dose: 400 mg twice daily (check BNF for paediatric and once-daily formulations).
⚠️ Interactions
- Antacids containing aluminium or magnesium reduce raltegravir absorption — separate by ≥2 hours.
- Rifampicin induces UGT1A1 metabolism and may lower plasma concentrations (higher dose may be needed).
- Check for other interactions in the BNF.
🚧 Cautions
- Monitor for immune reconstitution syndrome during initiation of ART.
- Use with caution in moderate/severe hepatic impairment.
- Rare reports of myopathy and rhabdomyolysis — advise patients to report muscle pain.
⛔ Contraindications
- No absolute contraindications beyond known hypersensitivity.
- Relative: avoid co-administration with strong enzyme inducers without expert advice.
💥 Side Effects
- Headache, insomnia, fatigue.
- Raised liver enzymes or creatine kinase (CK).
- Occasional rash or gastrointestinal disturbance.
- Rare: depression, suicidal ideation (monitor mental health in at-risk groups).
📚 References
- BNF: Raltegravir
- Public Health England. HIV treatment guidelines (latest update).
- European AIDS Clinical Society (EACS) Guidelines, 2023.
