País: Malasia
Idioma: inglés
Fuente: NPRA (National Pharmaceutical Regulatory Agency, Bahagian Regulatori Farmasi Negara)
BISOPROLOL FUMARATE
IMEKS PHARMA SDN. BHD.
BISOPROLOL FUMARATE
10 x 10tablet Tablets; 50 x 10tablet Tablets; 10 x 10 Tablets; 50 x 10 Tablets
Sriprasit Pharma Co. Ltd.
_PRODUCT DESCRIPTION _ Yellow heart shaped film coated tablet embossed with “S”, “5” and breakline on one side, and breakline on the other side. Each film coated tablet contains 5mg of bisoprolol fumarate. _PHARMACODYNAMICS _ Bisoprolol is a β1-selective adrenergic blocking agent. Bisoprolol is related structurally to acebutolol, atenolol, and metoprolol in that the drugs contain substituents in the para position of the benzene ring; the presence of large substituents in the para position is believed to account in part for the selective β1-adrenergic blocking effect of these drugs. It is devoid of intrinsic symphathomimetic, membrane-stabilizing properties and only shows shows low affinity to the β2- receptor of the smooth muscle of bronchi and vessels as well as the β2-receptors concerned with metabolic regulation. At therapeutic doses bisoprolol is not to be expected to influence airway resistance and β2-mediated metabolic effects. _PHARMACOKINETICS _ Bisoprolol is almost completely absorbed after oral administration, the absorption is not affected by the presence of food and it undergoes only minimal first-pass metabolism. Peak plasma concentrations are reached 2 to 4 h after oral administration. It is moderately lipid soluble and rapidly and widely distributed in the body. Plasma protein binding is around 30% to 36%. The bioavalability is 82% to 94%. The distribution volume is 3.5 l/kg. It has a plasma elimination half-life of 10 to 12 hours increased in patients with renal or liver impairment. Total clearance is approximately 15 l/h. Approximately 50% of a dose is metabolised in the liver to pharmacologically inactive polar metabolites that are then excreted by the kidneys; the remaining 50% is excreted unchanged. Bisoprolol is eliminated equally by both liver and renal and less than 2% by feces. _INDICATION _ Hypertension. Coronary Heart Disease (angina pectoris). Treatment of stable chronic moderate to severe heart failure with reduced systolic ventricular function (ejection fraction ≤ 35 %, Leer el documento completo