Company: MSD.
Legal category: Prescription. Hospital only. Sport permitted.
Active ingredient: Raltegravir (as potassium) 25mg, 100mg.
Description: Pale yellow or orange, round or oval, orange-banana flavoured chewable tablet, respectively. 25mg: Merck logo on one side and 473 on reverse. 100mg: Scored on both sides, Merck logo and 477 on one side, can be divided into equal doses.
Presentation: 25mg-60, €46.10; 100mg-60, €184.40.
Indications: In combination with other anti-retroviral therapies (ART) for HIV-1 infection in children >2 years.
Pharmacology: Raltegravir inhibits the catalytic activity of integrase, an HIV-encoded enzyme that is required for viral replication. Inhibition of integrase prevents the covalent insertion, or integration, of the HIV genome into the host cell genome. HIV genomes that fail to integrate cannot direct the production of new infectious viral particles.
Dosage: Children: 2-11 years, weight based to maximum dose 300mg twice daily. 12 to <14kg , 75mg twice daily; 14 to <20kg, 100mg twice daily; 20 to <28kg, 150mg twice daily; 28 to <40kg, 200mg twice daily; ≥40kg, 300mg twice daily; see SPC. Under 2 years, safety and efficacy not established.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy, lactation.
Special precautions: Caution: Severe hepatic impairment, chronic hepatitis B or C (monitor), history of depression or psychiatric illness. Reported: Severe, potentially fatal skin/ hypersensitivity reactions (discontinue promptly), osteonecrosis (monitor for signs of joint aches), immune reactivation syndrome (monitor for inflammatory symptoms), autoimmune disorders (such as Grave’s disease), myopathy, rhabdomyolysis. Driving/using machines. Contains fructose, phenylalanine and sorbitol.
Drug interactions: Caution: Strong uridine diphosphate glucuronosyltransferase (UGT) 1A1 inducers, e.g. rifampicin; strong enzyme inducers, eg. phenytoin, phenobarbital (no data).
Adverse drug reactions: Decreased appetite, abnormal dreams, insomnia, nightmares, depression, dizziness, headache, vertigo, GI disorders, rash, fatigue, pyrexia. Increases in alanine aminotransferase, aspartate aminotransferase, atypical lymphocytes, triglycerides, lipase and pancreatic amylase.
Full prescribing information and references available from MSD. Telephone: (01) 2998700. Fax: (01) 2998701.