Raltegravir
- Atc Codes:J05AX08
- CAS Codes:871038-72-1#518048-05-0
- PHARMGKB ID:871038-72-1#518048-05-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Isentress; Belgium: Isentress; Bulgaria: Isentress; Czech Republic: Isentress; Denmark: Isentress; Estonia: Isentress; Finland: Isentress; France: Isentress; Germany: Isentress; Greece: Isentress; Hungary: Isentress; Ireland: Isentress; Italy: Isentress; Latvia: Isentress; Lithuania: Isentress; Luxembourg: Isentress; Malta: Isentress; Netherlands: Isentress; Poland: Isentress; Portugal: Isentress; Romania: Isentress; Slovakia: Isentress; Slovenia: Isentress; Spain: Isentress; Sweden: Isentress; UK: Isentress.
North America
Canada: Isentress; USA: Isentress.
Asia
Japan: Isentress.
Drug combinations
Chemistry
Raltegravir Potassium: C~20~H~20~FKN~6~O~5~. Mw: 482.51. (1) 4-Pyrimidinecarboxamide, N-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-, monopotassium salt; (2) Potassium 4-[(4-fluorobenzyl)carbamoyl]-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-1,6-dihydropyrimidin-5-olate. CAS-871038-72-1; CAS-518048-05-0 (raltegravir). (2007)
Pharmacologic Category
Antiretrovirals; Integrase Inhibitors. (ATC-Code: J05AX08).
Mechanism of action
Viral cDNA strand produced by reverse transcriptase is processed and inserted into human genome by enzyme HIV-1 integrase. Raltegravir inhibits catalytic activity of integrase, thus preventing integration of proviral gene into human DNA.
Therapeutic use
Treatment of HIV-1 infection in combination with other antiretroviral agents in treatment-experienced patients with virus that shows multidrug resistance and active replication.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women; available data insufficient to recommend use in pregnancy. Excretion in breast milk unknown (contraindicated in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to raltegravir or any other component of the formulation.
Warnings and precautions
Patients may develop immune reconstitution syndrome resulting in occurrence of inflammatory response to indolent or residual opportunistic infection. Grade 2-4 creatine kinase (CK) increases observed and myopathy and rhabdomyolysis reported (use caution in risk factors for CK elevations and/or skeletal muscle abnormalities). Use caution with medications known to induce (e.g. rifampin) or inhibit (e.g. atazanavir) UGT1A1 glucuronidation, as serum levels/therapeutic effects may be reduced or increased, respectively.