raltegravir: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
raltegravir: clinical details
Prescribing considerations
- Initiation and regimen selection should be supervised by a clinician experienced in HIV management.
- Use only within an active combination regimen; raltegravir has a relatively low genetic barrier to resistance.
- Review psychiatric history, previous myopathy or rhabdomyolysis, liver disease and interacting medicines.
- Use caution in severe hepatic impairment and older people because clinical information is limited.
- Review treatment promptly if pregnancy occurs because the selected formulation's regimen is not recommended during pregnancy.
Contraindications and cautions
- Hypersensitivity to raltegravir or any excipient in the selected product.
Monitoring
- Assess adherence and virological response because treatment interruption or an incompletely active regimen can promote resistance.
- Monitor liver function in people with pre-existing hepatic dysfunction or chronic hepatitis, and investigate evidence of worsening liver disease.
- Assess creatine kinase and renal function when clinically indicated by muscle symptoms or suspected rhabdomyolysis.
- Monitor promptly for severe rash, systemic hypersensitivity, immune-reconstitution phenomena and psychiatric deterioration.
Clinical pharmacology
Raltegravir inhibits HIV-1 integrase strand transfer. Clearance is mainly through UGT1A1-mediated glucuronidation, with little potential for clinically important CYP-mediated inhibition or induction.
Formulation and product differences
- Film-coated tablets, chewable tablets and granules have different pharmacokinetic profiles and should not be substituted directly.
- The selected film-coated formulation should be swallowed whole and is not licensed below its specified paediatric weight threshold.
raltegravir preparations and strengths
Tablet
Route: Oral
Strengths: 600 mg
raltegravir interactions
Tell the HIV team and pharmacist about prescribed, purchased and herbal products. Important examples include:
Aluminium-, magnesium- or calcium-containing antacids
They can substantially reduce raltegravir levels and are not recommended with the selected formulation.
Iron salts
Iron can reduce raltegravir absorption; take the products separately as directed by the HIV team or pharmacist.
Rifampicin, phenytoin or phenobarbital
Strong enzyme induction may lower raltegravir exposure, so use with the selected formulation is not recommended.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.