药理学教学课件：Chapter 11 Adrenoceptor Blocking Drugs.ppt

Nadolol The time for blocking effects last longer； Excretion mainly from kidney with the prototype. Timolol Strongest blocker of β R in known compounds; Inhibiting the production of aqueous water，used in the treatment of glaucoma. Pindolol Stronger ISA; Has certain activating effects of β2 R and useful to the treatment of hypertention. Selectively β1 R Blockers —— Atenolol Weaker blocking effects of β2 R, Milder effect of increasing breath-track resistance， Used mainly in the treatment of BP Metoprolol Shorter lasting time of effects than atenolol Labetalol 1. Can be absorbed by p.o. , larger individual differences in bioavailability; 2. β R blocking effects is stronger 5-10 times than α R blocking effects ; 3. Used often in moderate or severe hypertension and cardiac angina. Also used in hypertention crisis by i.v. Arotinolol 1. Stronger β R blocking effects than α R blocking effects compared with labetalol; 2. Used in the treatment of hypertention、cardiac angina、supraventricular tachycardia and essential tremor，especially in the patients with hypertention combinated with coronary heart disease; 3. Has synergistic effects combinated with the drugs reducing blood sugar, calcium channel blockers, etc. Carvedilol 1. Has the activity of blockingα1、β1、β2 R，and the effects of Anti-oxidation； 2. Was approved to be used in primary hypertention by FDA of USA in 1995，and in congestive heart failure in 1997. It can improve the symptoms and life quality obviously. 3. The drug is the first β R blocking drug approved formly in the treatment of heart failure. Chapter 11 Adrenoceptor Blocking Drugs Abstract Section 1 α-Adrenoceptor Blocking Drugs 1. Nonselectively α-Adrenoceptor Blockers Short acti