Drug Detail

Raltegravir

Last Updated June 10, 2016

Trade Names

Isentress

Drug Classification

Integrase strand transfer inhibitor antiretroviral

Formulations

400 mg tablets

Indications and Pharmacology

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.

Dosage

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*:

  • No dose adjustment required for mild to moderate hepatic insufficiency; no recommendation for patients with severe hepatic insufficiency.
  • No dose adjustments needed for patients with renal insufficiency.

Use in Pregnancy and Breastfeeding*: Category C. Excretion into breast milk unknown.

Use in Children: No recommendation in South African Formulary.

Warnings

Rifampicin decreases raltegravir concentrations; raltegravir 800 mg twice daily should be used.*

Drug–Drug Interactions

See Warnings. Minimal drug interactions.

Considerations for Special Populations

See above for pregnancy and lactation.

Adverse Effects

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.