□
Coronary vascular dilators
TomasGonec 14.11.2011
Ischemic heart disease
B
□ when lumen of coronary artery is restricted (due to atherosclerotic changes, spasm or inflammatory reaction), supplying of myocard with oxygen and nutrients is insufficient
□ primary symptom is Angina pectoris -
sudden, severe pain originating in the chest and radiating to the left shoulder and arm
11
Ischemic heart disease therapy
□ vasodilators - direct (NO releasing agents, xanthine derivatives, nicotinic acid, chromone derivatives, Prostaglandines, trimetazidin) indirect (Ca2+inhibitors, ACE inhibitors, angiotensin II receptor antagonists)
□ drugs preventing myocardial infarction (anicoagulants, antithrombotics)
Organic nitrates
B
□ prodrugs releasing NO
□ NO is endotelial guanylatcyclase activator
□ increased intracelular cGMP decrease Ca2+ levels —► vessel wall smooth muscle relaxation —► vasodilatation
Organic nitrates
B
02NO^ y^ON02
02NO^VY^ON°2 )-(
ON02 02NO       ON02 ^ v ^ONO
Glyceryl Trinitrate     Erythrityl Tetranitrate      Amyl Nitrite
02NO^^-ON02 02NO^^-ON02
" ON02
Pentaerythritol Tetranitrate Isosorbide Dinitrate
Xanthin derivatives
B
□ nature xanthines - theophylin, theobromin, Coffein
□ all are central stimulants, vasodilators, bronchodilators, diuretics
□ theophylin has enhanced smooth muscle relaxing activity
□ synthetic analogues are vasodilators and bronchodilators
Xanthin derivatives
11
Nicotinic acid
□ low dosis - vasodilating effect on upper part of body
□ higher dosis - antihyperlipidemic effect
Chromone derivatives
B
□ PDE inhibitor, enhances anaerobic glycolysis
□ 2X increased coronary flow without affecting blood pressure
o
Karbokromen
Prostaglandines
B
□ various Prostaglandines has vasodilating effect
□ Alprostadil is used in some heart insufficiencies
alprostadil
a
Trimetazidine
□ decreases intracelular ATP
OMe
MeO
MeO