Raltegravir Dosing for HIV Treatment
The recommended dose of raltegravir for the treatment of HIV infection in adults is 400 mg administered orally twice daily. 1
Standard Dosing Recommendations
- Adults: 400 mg film-coated tablet twice daily 1
- Pediatric patients:
- If ≥25 kg: 400 mg film-coated tablet twice daily
- If <25 kg: Weight-based dosing (approximately 6 mg/kg/dose twice daily)
- Alternative options for those who cannot swallow tablets include chewable tablets or oral suspension 1
Special Dosing Considerations
Tuberculosis Co-infection
When coadministered with rifampin for tuberculosis treatment:
- Adults: Increase raltegravir dose to 800 mg twice daily 1
- Pediatric patients <18 years: No data available to guide dosing with rifampin 1
For patients with HIV and active tuberculosis receiving rifamycin-based treatment:
- Raltegravir 400 mg twice daily (in combination with 2 NRTIs) is recommended 2
- Integrase strand transfer inhibitor (InSTI)-based regimens are preferred over protease inhibitor-based regimens for tuberculosis co-infection 2
Maximum Dosing
- Maximum dose for chewable tablets: 300 mg twice daily
- Maximum dose for oral suspension: 100 mg twice daily 1
Administration Considerations
- Raltegravir can be administered with or without food 1
- Film-coated tablets must be swallowed whole
- Chewable tablets may be chewed or swallowed whole
- Oral suspension requires preparation (100 mg packet suspended in 5 mL water) 1
Formulation Considerations
Different formulations of raltegravir are not bioequivalent:
- Do not substitute chewable tablets or oral suspension for the 400 mg film-coated tablet 1
- Each formulation has specific dosing requirements
Drug Interactions
- No cytochrome P450-related drug interactions are expected as raltegravir is not a CYP substrate, inducer, or inhibitor 3
- Important caution: Raltegravir should not be coadministered with rifampin to prevent treatment failure 3
- When used with rifapentine for latent tuberculosis infection, raltegravir exposure may be increased but the regimen is generally well tolerated 2
Once-Daily Dosing Option
While the standard dosing is twice daily, research has explored once-daily dosing:
- A 1200 mg (two 600 mg tablets) once-daily formulation (Isentress HD) is available for treatment-naïve adults 4
- Once-daily dosing simplifies treatment regimens and may improve convenience 4
- In some studies, raltegravir 800 mg once daily plus 2 NRTIs has shown efficacy, particularly in virologically suppressed patients 5
Clinical Efficacy
Raltegravir has demonstrated high efficacy in both treatment-naïve and treatment-experienced patients:
- In treatment-naïve patients, raltegravir shows similar efficacy to standard initial therapies 3
- In treatment-experienced patients with drug-resistant HIV, adding raltegravir to an optimized background regimen significantly lowered HIV RNA compared to optimized background treatment alone (62.1% vs 32.9%) 3
- Raltegravir treatment is associated with a lower impact on serum lipid levels compared to efavirenz 6
Safety Profile
Raltegravir is generally well tolerated. Common adverse effects include:
- Diarrhea (16.6%)
- Nausea (9.9%)
- Headache (9.7%) 3
Summary
For standard HIV treatment in adults, raltegravir 400 mg twice daily is the recommended dose. Special dosing considerations apply for tuberculosis co-infection, pediatric patients, and those unable to swallow tablets. A once-daily formulation (1200 mg) is also available for treatment-naïve adults.