Company: GlaxoSmithKline.
Legal category: Prescription. Hospital. Sport permitted.
Active ingredient: Dolutegravir (sodium) 50mg.
Description: Yellow, round, biconvex film-coated tablets marked SV 572 on one side and 50 on reverse.
Presentation: Price available on request.
Indication: In combination with other anti-retrovirals for the treatment of human immunodeficiency virus (HIV) infected adults and adolescents above 12 years.
Pharmacology: Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral deoxyribonucleic acid integration which is essential for the HIV replication cycle.
Dosage: Adult: Patients without integrase class resistance: 50mg once daily. Take twice daily when co-administered with some drugs (e.g. efavirenz, nevirapine, tipranavir/ritonavir or rifampicin). Patients with integrase class resistance: 50mg twice daily (decision should be informed by the integrase resistance pattern); take with food to enhance exposure (especially in patients with Q148 mutations). Elderly: ≥65 years, limited data. Children: 12-17 years and ≥40 kg without integrase class resistance, 50mg once daily. <12 years or <40kg, safety and efficacy not established.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Lactation.
Special precautions: Viral strains harbouring Q14 plus >2 secondary mutations from G140A/C/S, E138A/K/T, L74I (treatment efficacy uncertain). Caution: Severe hepatic impairment, hepatitis B and/or C co-infection (monitor liver biochemistries), initiation or maintenance of effective hepatitis B therapy during treatment. Reported: Hypersensitivity reactions (discontinue immediately if develop, monitor clinical status including liver aminotransferases and bilirubin), immune reactivation syndrome (e.g. cytomegalovirus retinitis, generalised and/or focal mycobacterial infections, Pneumocystis jirovecii pneumonia), autoimmune disorders (such as Graves’ disease), osteonecrosis. Monitor for opportunistic infections and other complications of HIV infection. Pregnancy (only if benefit outweighs risk). Driving/using machines. Contains mannitol.
Drug interactions: Contraindicated: Dofetilide. Avoid (in both populations): Certain anti-epileptic drugs, St. John’s wort, etravirine (without co-adminstered atazanavir/ritonavir, darunavir/ritonavir or lopinavir/ritonavir). Also avoid (in patients with integrase class resistance): Factors that decrease dolutegravir exposure (e.g. magnesium/ aluminium-containing antacid, iron and calcium supplements, multivitamins and inducing agents), efavirenz, nevirapine, tipranavir/ ritonavir, fosamprenavir/ ritonavir, rifampicin. Metformin. In patients without integrase class resistance: Magnesium/ aluminium-containing antacid, iron and calcium supplements or multivitamins (minimum 2 hours after or 6 hours before).
Adverse drug reactions: Insomnia, abnormal dreams, headache, dizziness, GI upset, rash, pruritus, fatigue, elevations in creatine phosphokinase, alanine aminotransferase and/or aspartate aminotransferase.
Full prescribing information and references available from GlaxoSmithKline. Telephone: (01) 4955000.