Products
Raltegravir is commercially available as film-coated tablets and chewable tablets (Isentress). It was approved in the United States in 2007 and in many countries in 2008 as the first integrase inhibitor.
Structure and properties
Raltegravir (C20H21FN6O5, Mr = 444.4 g/mol) is a hydroxypyrimidinone carboxamide. It is present in drugs in the form of the salt raltegravir potassium, a white powder that is soluble in water.
Effects
Raltegravir (ATC J05AX08) has antiviral properties. It is a specific inhibitor of HIV integrase, which is responsible for the integration of the HIV genome into the host cell genome at the onset of infection. This prevents replication of the virus.
Indications
In combination with other antiretroviral drugs for the treatment of human immunodeficiency virus (HIV-1) infection.
Dosage
According to the SmPC. The drug is taken twice daily, regardless of meals.
Contraindications
- Hypersensitivity
Full details of precautions and interactions can be found in the drug label.
Interactions
Raltegravir, unlike other HIV medications, does not interact with CYP450, but it is glucouronidated by the UDP-glucuronyltransferase UGT1A1. Inducers of this enzyme, such as rifampicin, may reduce plasma concentrations and necessitate a dose increase. UGT1A1 inhibitors such as atazanavir may conversely increase concentrations. Drugs that increase gastric pH (eg, omeprazole) may increase plasma concentrations because they improve the solubility of raltegravir.
Adverse effects
The most common potential adverse effects include diarrhea, nausea, headache, fatigue, upper respiratory tract infection, and fever. Dangerous skin reactions have been reported. Other adverse reactions are described in the SmPC.
