Last Updated June 10, 2016
Integrase strand transfer inhibitor antiretroviral
400 mg tablets
Indication: treatment of HIV infection in combination with other antiretrovirals in treatment-experienced patients who have evidence of viral replication despite ongoing treatment or who have multiple drug–resistant viruses.
Mechanism of action*: inhibits the catalytic activity of HIV-1 integrase, the enzyme responsible for inserting the viral DNA into the human genome, thereby preventing integration of the proviral gene into the human DNA.
Pharmacokinetics*: metabolized in the liver by glucuronidation, primarily UGT1A1. 32T excreted in the urine; half-life: ~9 hours.
Adult Dose: 400 mg twice daily; take without regard to meals.*
With rifampicin, increase dose to 800 mg twice daily.*
Use in Renal or Hepatic Insufficiency*:
Use in Pregnancy and Breastfeeding*: Category C. Excretion into breast milk unknown.
Use in Children: No recommendation in South African Formulary.
Rifampicin decreases raltegravir concentrations; raltegravir 800 mg twice daily should be used.*
See Warnings. Minimal drug interactions.
See above for pregnancy and lactation.
Rash including Stevens-Johnson syndrome, hypersensitivity syndrome, and toxic epidermal necrolysis; nausea; diarrhoea; headache; pyrexia; creatinine phosphokinase elevation; muscle weakness; rhabdomyolysis.*
*Information from US prescribing information.
†Recommendation from Southern African HIV Clinician Society Guidelines.