Overview
What is Raltegravir?
Raltegravir was the first HIV integrase inhibitor approved for clinical use. It works by blocking the integration of HIV DNA into the human cell's DNA — a completely different target from reverse transcriptase or protease inhibitors. It is generally well tolerated and has few drug interactions.
Mechanism
How Does It Work?
1
Integrase binding
Raltegravir binds the integrase active site alongside the viral DNA ends and magnesium co-factors, displacing the necessary metal ions.
2
Strand transfer inhibition
Prevents the viral DNA from being inserted (integrated) into host CD4+ cell DNA, blocking proviral establishment.
3
Provirus prevention
Without integration, HIV cannot establish a permanent reservoir in that cell or produce new virions from it.
Dosage
How to Use
Timing
Twice daily (standard tablet) or once daily (HD formulation)
How to Take
Swallow whole. Can be taken with or without food. HD tablets must not be crushed or split.
Frequency
400 mg twice daily (standard) or 1200 mg once daily (HD tablets, naïve adults only)
With Food
No significant food interaction
Alcohol
Avoid excessive alcohol
Missed Dose
Take as soon as remembered. If close to next dose, skip the missed dose. Never double dose.
Safety
Side Effects & Precautions
Common Side Effects
- Insomnia
- Headache
- Nausea
- Fatigue
- Dizziness
- Elevated CPK
Serious Side Effects — seek help immediately
- Severe skin reactions (Stevens-Johnson syndrome)
- Rhabdomyolysis
- Psychiatric events (depression, suicidal ideation)
- Immune reconstitution syndrome
Who Should Not Take This
- Known hypersensitivity to raltegravir
- Use with caution in severe hepatic impairment
Value
Generic vs Brand
Generic (OnlineMeds)
Isentress
Price per unit
—
$1200–$1800/month
Active ingredient
Identical
Identical
Storage
Storage & Handling
Temperature
Room temperature 15–30°C
Light
Keep in original container
Humidity
Protect from moisture
Children
Keep out of reach of children.
Why OnlineMeds
Why Buy From Us
Manufacturer Direct
Sourced directly from WHO-GMP certified manufacturers.
Quality Verified
Every batch tested for purity and bioequivalence.
Global Delivery
Discreet shipping to UK, US, AU, EU and beyond.
Licensed Pharmacy
Regulated and compliant with international pharmacy standards.
FAQ
Frequently Asked Questions
How is Zepdon Tablets different from other HIV drugs?
Raltegravir was the first integrase inhibitor — it blocks a different step in HIV replication (integration) compared to NRTIs (reverse transcription) or protease inhibitors (viral maturation). This means it can work even when resistance to other drug classes has developed.
Does Raltegravir require a booster drug?
No. Unlike some protease inhibitors, raltegravir does not require ritonavir or cobicistat boosting. It reaches therapeutic levels on its own, which also means it has far fewer drug interactions than boosted regimens.
Can I take Zepdon Tablets with antacids?
Aluminium- and magnesium-containing antacids can reduce raltegravir absorption. If you need antacids, separate them from your raltegravir dose by at least 2 hours. Calcium carbonate antacids do not appear to have the same effect.
How quickly does Raltegravir lower viral load?
Raltegravir produces rapid declines in viral load — studies show significant reductions within 2 weeks. Most patients achieve undetectable viral load within 24 weeks as part of a complete ART regimen.
Drug Interactions
| Drug / Substance | Effect | Action |
|---|
| Rifampicin |
Reduces raltegravir levels significantly |
Avoid or double raltegravir dose to 800 mg twice daily |
| Aluminium/magnesium antacids |
Reduce raltegravir absorption by chelation |
Separate administration by at least 2 hours |
| UGT1A1 inducers (e.g. rifampicin) |
Increased glucuronidation of raltegravir |
Dose adjustment required |
Approved Indications
-
HIV-1 infection in adults and children ≥ 4 weeks of age FDA / EMA
References
-
Merck. FDA Prescribing Information: Isentress (raltegravir). ↗
-
WHO. WHO Consolidated Guidelines on HIV Treatment, 2021. ↗
Disclaimer: This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before starting, stopping, or changing any medication. Used as prescribed by a licensed medical professional.
