卡维地洛片（carvedilol）.docVIP

卡维地洛片（carvedilol） Carvedilol Tablets (Carvedilol Tablets) [traits] This product is white. [pharmacology and toxicology] Carvedilol has both A1 and nonselective B receptor blockade within the therapeutic dose range and has no intrinsic pseudo sympathetic activity. This product blocks the postsynaptic membrane A1 receptors, thereby dilating the blood vessels and reducing peripheral vascular resistance, blocking the B receptor, inhibiting the secretion of renin by the kidney, and blocking the renin angiotensin aldosterone system, resulting in a hypotensive effect. Carvedilol can reduce blood pressure rapidly and maintain blood pressure for a long time. Left ventricular ejection fraction, heart function, renal function, renal blood perfusion, peripheral blood flow, plasma electrolyte and blood lipid levels did not affect the heart rate or make it slightly slowed down, rarely produce water retention. [pharmacokinetics] Carvedilol is easy to absorb after oral administration, and absolute bioavailability (F) is about 25% to 35%. There are obvious first pass effects, and the elimination of phase half-life (t1/2b) is about 7~10 hours. When taken with food, the absorption slows down, but has no significant effect on bioavailability, and reduces the risk of orthostatic hypotension. Carvedilol is an alkaline lipophilic compound, and the binding rate with plasma proteins is more than 98%. Its steady-state distribution volume is about 1.5L, and the plasma clearance rate is 500 ~ 700ml/min. Carvedilol is metabolized completely, and its metabolites are excreted by bile and then excreted through the stool, less than 2% of which is excreted in the urine. 8 healthy subjects received a single dose of 30mg, and the pharmacokinetics were measured. The peak concentration of blood concentration (Cmax) was 89.89ng/ml, the elimination phase half-life (t1/2b) was 2.01 hours, and the area under curve (AUC) was 233.1 (ng. H) /ml. It can be absorbed quickly and completely. Food can slow down the