Product Information
Registration Status: ActiveSIN14809P
OPSUMIT FILM-COATED TABLET 10MG is approved to be sold in Singapore with effective from 2015-07-15. It is marketed by JOHNSON & JOHNSON PTE LTD, with the registration number of SIN14809P.
This product contains Macitentan 10mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Patheon Italia S.p.A. in SWITZERLAND,Patheon France (Primary and Secondary Packager) in ITALY,Allpack Group AG (Primary and Secondary Packager) in FRANCE, andExcella GmbH & Co. KG in GERMANY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.
Indication
Macitentan is indicated for patients with pulmonary arterial hypertension.
Mechanism of Action
Macitentan is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitentan binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating the ETA and ETB receptors.
Pharmacokinetics
- Absorption
- Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.
- Distribution
- Macitentan has a volume of distribution of 50L.
- Metabolism
- Macitentan is metabolised to an active metabolite by CYP 3A4 (major) and CYP 2C19 (minor).
- Elimination
Clearance
Clearance data was not found.
Toxicity
Macitentan has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.
Active Ingredient/Synonyms
Macitentanum | Macitentan |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.