抗心绞痛药和降血脂药 by yurtgc548

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									     Antianginal drugs
n   Angina pectoris is the severe chest
    pain that occurs when coronary blood
    flow is inadequate to supply the
    oxygen required by the heart.
n   The primary cause of angina pectoris
    is an imbalance between the oxygen
    requirement of the heart and the
    oxygen supplied to it.
    Backgrounds of angina pectoris
n   Classification: stable; unstable;variant
n   Mechanism:
n   Methods for treatment:
Ø   To improve perfusion:
Ø   To reduce metabolic demand
n   Drugs
Ø   organic nitrates;
Ø   calcium antagonists
Ø   β-Receptor blockers
      Organic nitrates
n   Pharmacological effects and mechanism:
v   dilate peripheral vein   preload
                                       Oxygen
v   dilate peripheral artery afterload consumption
v   Dilate coronary artery         perfusion of
                             ischemic myocardium
      Mechanism of action in VSM
n   NO(EDRF)         activate GC       increase c-GMP
    activate cGMP- dependent kinase            decrease
    Ca      induce de-phosphorylation of the myosin
    light chain       relaxation
n   Pharmacokinetics: very low bioavailability per os
                         Subligual Rapid onset(2~5min)
n   Acute adverse effects: postural hypotensiom,
    throbbing headache
n   Tolerance : because of depletion of free –SH
    groups
n   Clinic use: to treat and prevent all of the angina
    β-Receptor blockers
n   Pharmacological effects:
Ø   Myocardial constriction                    Oxygen
                                               consumption
Ø   Heart rate
§   Clinic use : stable and unstable angina
§   Propranolol      not for variant angina because of coronary
    artery contraction due to its β-receptor blocked and α -
    receptor relatively activated.
§   Propranolol + nitroglycerin
    Calcium channel blockers
n   Pharmacological effects :              Myocardial
                                           oxygen
Ø   Cardiac contractility,
                                           consumption
Ø   heart rate
Ø   Peripheral vessels dilation ,afterload
Ø   dilate coronary artery, release its spasm
Ø   Ca2+ overload              apoptosis,necrosis
n   Clinic use : variant angina
v   Nifedipine not for unstable angina,+ β-Receptor blockers
     Other drugs for angina

n   Anti-platelet drugs:
         aspirin, persantin
n   Chinese medicine:
         salvia miltiorrhiza,panax notogenseng
n   ATP sensitive potassium channel openers

								
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