Raltegravir is an integrase inhibitor used in HIV treatment. It works by blocking the integrase enzyme, preventing integration of viral DNA into the host cell genome.
Also known as: Isentress, RAL
Raltegravir may slightly elevate serum creatinine via inhibition of tubular secretion (no effect on actual GFR). No metformine dose adjustment required.
Raltegravir inhibits the OCT2/creatinine transporter in the proximal renal tubule, raising serum creatinine by 0.1-0.3 mg/dL without actual change in glomerular filtration rate (GFR). This elevation is apparent and does not reflect renal dysfunction. Metformine is eliminated by tubular secretion via OCT2, but the effect of raltegravir on creatinine does not translate to clinically significant metformine accumulation. No metformine dose adjustment is required. However, serum creatinine interpretation should account for the raltegravir effect — use calculated GFR (eGFR) instead of creatinine alone to assess renal function.
Raltegravir + metformine: apparent creatinine elevation (inhibits tubular secretion). No effect on actual GFR — no adjustment needed.
Raltegravir inhibits the OCT2/creatinine transporter in the kidney, raising serum creatinine by 0.1-0.3 mg/dL without actual renal function change.
Serum creatinine (interpret with caution).
None clinically significant.
No dose adjustment required. Interpret serum creatinine in the context of raltegravir — the elevation is apparent, not real.
DailyMed/FDA (NIH/NLM) — approved Raltegravir (Isentress) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3
Food does not significantly affect raltegravir absorption.
Can be taken with or without food.
DailyMed/FDA (NIH/NLM) — approved Raltegravir (Isentress) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3
No documented disease interactions.
Animal studies did not demonstrate teratogenicity. Limited human data. Can be used when indicated.
Can be used in all trimesters when indicated.
Excreted in breast milk. Artificial feeding is recommended for HIV-positive mothers.
Reliable contraceptive methods are recommended.
DailyMed/FDA (NIH/NLM) — approved Raltegravir (Isentress) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=89a5ec53-d956-4329-8004-0f40f51c88a3
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Raltegravir is an integrase inhibitor used in HIV treatment, with UGT1A1-dependent metabolism.
Blocks HIV-1 integrase by binding to the active site, preventing strand transfer of viral DNA and consequently integration into the host cell genome.
Oral bioavailability: ~60%. Tmax: 1-2 hours (400mg tablets); 2-5 hours (600mg tablets). Food does not significantly affect absorption.
Metabolised primarily by UGT1A1 (glucuronidation). Not metabolised by CYP3A4. Induced by rifampicin (via UGT1A1). Elevated serum creatinine (inhibits tubular secretion — no effect on actual GFR).
9 hours. Elimination: 51% faeces (metabolites), 32% urine (metabolites). Only ~2% excreted unchanged.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
