国家: 马来西亚
语言: 英文
来源: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)
Bosentan Monohydrate
MEDISPEC (M) SDN.BHD
Bosentan Monohydrate
60 Tablets; 10 Tablets
UNISON LABORATORIES CO.LTD
_ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _ _CONSUMER MEDICATION INFORMATION LEAFLET (RIMUP) _ SILKAY 125 MG TABLET Bosentan monohydrate eq. to Bosentan (125 mg) 1 WHAT IS IN THIS LEAFLET 1. What Silkay 125 is used for 2. How Silkay 125 works 3. Before you use Silkay 125 4. How to use Silkay 125 5. While you are using it 6. Side effects 7. Storage and Disposal of Silkay 125 8. Product Description 9. Manufacturer and Product Registration Holder 10. Date of revision WHAT SILKAY 125 IS USED FOR Silkay 125 is a prescription medicine used to treat people with certain types of pulmonary arterial hypertension (PAH), which is high blood pressure in the vessels of the lungs. HOW SILKAY 125 WORKS Silkay 125 tablets contain Bosentan, which belongs to the class of medicines called “endothelin receptor antagonists”. Bosentan blocks a naturally occurring hormone called endothelin-1 (ET-1), which causes blood vessels to narrow. Thus, it acts to reduce abnormally high blood pressure by widening these blood vessels. BEFORE YOU USE SILKAY 125 _- When you must not use it _ Do not take Silkay 125: • if you are allergic to bosentan or any of the other ingredients of this medicine • if you have liver problems (ask your doctor) • if you are pregnant, or could get pregnant because you are not using reliable contraceptive methods. Please read the information under “Contraceptives” and “Taking other medicines” • if you are taking cyclosporine A (a medicine used after a transplant) PREGNANCY AND LACTATION DO NOT take Silkay 125 if you are pregnant or planning to become pregnant. _PREGNANCY TESTS _ Silkay 125 may harm unborn babies conceived before starting or during treatment. If you are a woman who could become pregnant, your doctor will ask you to take a pregnancy test before you start taking Silkay 125, and regularly while you are taking it. _CONTRACEPTIVES _ If it is possible that you could become pregnant, use a reliable form of birth control (contraception) while you are taking Silkay 125. Your doctor or gynecologist will 阅读完整的文件
ANTIHYPERTENSIVE Each film coated tablet contains: BOSENTAN MONOHYDRATE EQ. TO BOSENTAN 125 MG PRODUCT DESCRIPTION: Orange-white, oval, biconvex, film coated tablet with engraved 125 on one side and plain on the other side MECHANISM OF ACTION: _PHARMACOLOGY_ Bosentan is a dual endothelin receptor antagonist (ERA) with affinity for both endothelin A and B (ET A and ET B ) receptors. Bosentan decreases both pulmonary and systemic vascular resistance resulting in increased cardiac output without increasing heart rate. The neurohormone endothelin-1 (ET-1) is one of the most potent vasoconstrictors known and can also promote fibrosis, cell proliferation, cardiac hypertrophy and remodelling, and is pro-inflammatory. These effects are mediated by endothelin binding to ET A and ET B receptors located in the endothelium and vascular smooth muscle cells. ET-1 concentrations in tissues and plasma are increased in several cardiovascular disorders and connective tissue diseases, including PAH, scleroderma, acute and chronic heart failure, myocardial ischemia, systemic hypertension and atherosclerosis, suggesting a pathogenic role of ET-1 in these diseases. In PAH and heart failure, in the absence of endothelin receptor antagonism, elevated ET-1 concentrations are strongly correlated with the severity and prognosis of these diseases. Bosentan competes with the binding of ET-1 and other ET peptides to both ET A and ET B receptors, with a slightly higher affinity for ET A receptors (K i = 4.1–43 nanomolar) than for ET B receptors (K i = 38–730 nanomolar). Bosentan specifically antagonises ET receptors and does not bind to other receptors. _PHARMACOKINETICS_ Absorption In healthy individual, the absolute bioavailability of Bosentan is approximately 50% and is not affected by food. The maximum plasma concentrations are attained within 3–5 hours. Distribution Bosentan is highly bound (> 98%) to plasma proteins, mainly albumin. Bosentan does not penetrate into erythrocytes. A volume of distribution (V ss ) of about 18 liters w 阅读完整的文件