Antianginal Drugs Flashcards
Organic nitrites and nitrates
Amyl nitrite
Nitroglycerin
Isosorbide dinitrate
Isosorbide mononitrate
Organic nitrites and nitrates - MoA
Act by releasing nitric oxide in vascular smooth muscle cells. Nitric oxide activates guanylyl cyclase forming cGMP, cGMP activates cGMP dependent kinases that appear to cause relaxation of vascular smooth muscle by phosphorylating proteins that decrease intracellular calcium mobilization and decrease myosin light chain-phosphatase. They relax venous smooth muscle, with small effect on arteriolar. This leads to venous pooling of blood, a decrease in venous blood return to the heart and a decrease in ventricular volume, pressure, and wall tension. The nitrites reduce cardiac preload and output, which leads to reduction in BP
Organic nitrites and nitrates - Adverse effects
Hypotension Reflex tachycardia (to prevent this, can give B-blocker) Headache Dizziness Euphoria Increased libido
Methemoglobinemia (Only nitrites, not nitrates)
Pharmacodynamics tolerance to their vasodilate effects (transdermal patches should be removed for at least 10h every day, while drugs should be adm no more than two times per day)
Organic nitrites and nitrates - Interactions
Phosphodiesterase-V inhibitors (sildenafil)- potentiate the hypotensive effect
Amyl nitrite - Clincal use
Treatment of acute angina attacks
Initial management of cyanide poisoning (given iv, thiosulfate is also given to convert cyanide to inactive thiocyanate)
Nitroglycerin - Clinical use
Prevent and treat angina attacks
Reduce preload and afterload in pat who have acute heart failure associated with MI or other(iv)
Isosorbide dinitrate and Isosorbide mononitrate - Clinical use
Prevent and treat angina attacks
Calcium Channel Blockers
Amlodipine Felodipine Isradipine Nicardipine Nifedipine Nimodipine Diltiazem Verapamil
Calcium Channel Blockers - MoA
By blocking calcium ion channels in the plasma membranes of smooth muscle, the CCBs relax vascular smooth muscle and causes vasodilation. They have greater effect on arteriolar smooth muscle then venous, effect on BP is mainly because a reduction in PVR.
Calcium Channel Blockers - Adverse effects
Fatigue Headache Dizziness Flushing Peripheral edema Gingival hyperplasia (not diltiazem and verapamil) Constipation
Amlodipine, Felodipine and Nicardipine - Clinical use
Hypertension
Treatment of angina pectoris
Isradipine - Clinical use
Hypertension
Nimodipine - MoA
Dilates small cerebral vessels and increases collateral circulation to the affected areas of the brain.
It also reduces neuronal damage caused by the excessive release of calcium that is evoked by cerebral ischemia
Nimodipine - Clinical use
Reducing neurologic complications of Subarachnoid hemorrhage
Nimodipine - Contraindications
IV administration causes severe hypotension, cardiac arrest and fatalities