HIV integrase strand-transfer inhibitor Pregnancy: Raltegravir 1,200 mg once daily is not recommended during pregnancy (no data at this dose). Data on raltegravir 400 mg twice daily indicate no malformative or increased feto/neonatal toxicity. Women living with HIV should not breast-feed to avoid HIV transmission; raltegravir is excreted in human milk (UK SPC §4.6).

Raltegravir

Brand names: Isentress

Raltegravir is an integrase strand transfer inhibitor (INSTI) used as part of combination antiretroviral therapy for HIV-1 infection.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 1,200 mg (two 600 mg tablets)

Route: Oral

Frequency: Once daily

For adults and paediatric patients weighing at least 40 kg who are treatment-naive or virologically suppressed on an initial regimen of raltegravir 400 mg twice daily; must be used in combination with other active anti-retroviral therapies. Therapy should be initiated by a physician experienced in HIV management. Raltegravir is also available as a 400 mg tablet for twice-daily use in adults or children/adolescents at least 25 kg; the 400 mg tablet must not be used to give the 1,200 mg once-daily regimen. The 600 mg film-coated tablet formulation should not be used in children weighing less than 40 kg. Take with or without food; tablets should not be chewed, crushed or split. Hepatic impairment: no adjustment for mild to moderate; use with caution in severe hepatic impairment (safety/efficacy not established). Elderly: limited data — use with caution.

Dose adjustments

Renal

No dosage adjustment is required for patients with renal impairment (§4.2).

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients

Side effects

Headache, nausea and abdominal pain (most frequently reported)
Immune reconstitution syndrome and rash (most frequently reported serious reactions)
Decreased appetite (common)
Insomnia, abnormal dreams, nightmare, depression, dizziness (common)
Rhabdomyolysis (uncommon; reported in post-marketing use of raltegravir 400 mg twice daily)

Clinical monograph

How it works

It inhibits HIV integrase, preventing integration of viral DNA into the host genome and thereby blocking establishment of productive infection.

Prescribing in practice

Always use within a fully suppressive combination antiretroviral regimen; never as monotherapy, as resistance develops rapidly.
Polyvalent cation-containing antacids and certain supplements can chelate the drug and reduce absorption, so separate administration carefully.
Rare but serious skin and hypersensitivity reactions, including severe cutaneous reactions, have been reported.

Monitoring

Monitor HIV viral load and CD4 count to confirm virological response, alongside periodic liver function and creatine kinase if myopathy is suspected.

Counselling the patient

Take every dose as prescribed to keep the virus suppressed and prevent resistance.
Tell your clinician about any antacids, indigestion remedies or mineral supplements before starting.
Seek urgent advice if you develop a rash, fever or muscle pain.

Evidence & guidelines

Raltegravir is a recommended first-line INSTI option in UK and international HIV treatment guidelines.

Reference: BHIVA; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways