第二十八章 抗心绞痛药
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教学内容II.Classification of antianginal agents1.Nitrates and Nitrites2. -adrenoceptor-blocking drugs3.Calcium channel blockersAll three of the drug groups useful inoxygen requirement by decreasingdemand. In variant angina, the nitrates & the calcium channel blockers may also increase myocardialcoronary arterial spasm.2.Pharmacokinetics①AbsorptionThe bioavailability of the traditional typically <10-20%. The sublingual achieving a therapeutic bloodOn other smooth muscle organsRelaxation ofgastrointestinalgenitourinary tract has been demonstrated experimentally.Because of theirnitrates are rarely of any clinical value.b.Effects on platelet aggregationNitric oxide released from nitroglycerin stimulates guanylyl cyclase in platelets as in smooth muscle.that results is responsible foraggregation.Unfortunately, recent prospective trials have established no②Mechanism of action in smooth muscleNitroglycerin appears to be denitrated,ion in the smooth muscle cell by glutathione S-transferase.Nitric oxide released from the parent drug molecule.Nitric oxide is a much more potent vasodilator than nitrite, which itself can release nitric oxide. Nitric oxide causes activation of guanylyl cyclase and an increaseClinical use2.classification①First generationa.Verapamilb.Nifedipinec.DiltiazemStabilizing Effects②Second generationBlood pressure is reduced with all calciumThe reduction in peripheral vascularmechanism by which these agents may benefitangina of effort. Reduction of coronary arterial tone has②Mechanism③Clinical use④Adverse effectsThe combination of antianginal agents1.Nitrates and β-blocking agents2.Nitrates and calcium channels-blocking agents3.β-blocking agents and calcium channels-blocking agents重点及难点:To master the classification of antianginal agents and pharmacological actions,。