肾上腺素受体激动药adrenoceptor-activatingdrugs.ppt

Adrenoceptor agonists ③ Pharmacodynamics activate both ? - and β - receptors strongly Adrenoceptor agonists a. Heart ? Marked positive chronotropic effect on both normal and abnormal pacemaker activity ? Strong positive inotropic effect on intrinsic contractility Adrenoceptor agonists ? Promote conduction of heart ? Cardiac output ↑ ? Relaxate coronary arteries Adrenoceptor agonists b. Blood vessels ? Low dose can activate β 2 -R on the smooth muscles and cause relaxation ? Large dose can strong activate ? 1 -R on the smooth muscles, peripheral vascular resistance ↑ Adrenoceptor agonists c. Blood pressure ? Low dose systolic pressure ↑ and diastolic pressure normal or ↓ (heart β 1 -R and peripheral β 2 -R) ? Large dose marked increase blood pressure (peripheral ? 1 -R and β 1 - R of juxtaglomerular cells, excretion renin) Adrenoceptor agonists d. Smooth muscles (SM) ? Bronchial SM relaxation, β 2 - R(+), strongly ? Gastrointestinal tract tone ↓, β 1 -R(+) Adrenoceptor agonists e. Metabolism ? Lipolysis ↑, β 3 -R(+); ? glycogenolysis in liver ↑, ? - & β 2 - R (+), blood sugar ↑ markedly, ? ↓plasma K + when stress or exercise, β 2 -R (+) Adrenoceptor agonists ④ Clinical uses ? Cardiac arrest ? Anaphylactic shock: sc or im ? Bronchial asthma: sc or im ? Local application: local anaesthesia (1 ∶ 250000), stop bleeding Adrenoceptor agonists ⑤ Adverse effects ? BP marked elevation, cerebral hemorrhage or pulmonary edema ? Severe angina or myocardial infarction ? Sinus tachycardia or serious ventricular arrhythmias Adrenoceptor agonists ⑥ Contraindications Hypertension, sclerosis of cerebral artery, ischemic heart disease, congestive heart failure, hyperthyroidism, and diabetes. Use with care for old patients. Adrenoceptor agonists 2. Dopamine, DA ① Pharmacokinetics Dopamine is the precursor of NA and Adr. intravenous infusion, destroyed by MAO & COMT rapidly, t 1/2 =1- 2 min. can't across BBB, Adrenoceptor agonists ② Pharmacodynamic