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Pharm - Angina
Saba - Basic Sciences - Semester 4 - Pharm - Blk3 - Lect06
Question | Answer |
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Ischemic Heart Disease – 2 types | Angina (Transient coronary ischemia, chieft manifestation) & Myocardial infarction (Complete occlusion) are the manifestations of this disease |
Ischemic Heart Disease – Angina pectoris – Cause | Imbalance between Oxygen supply & demand results in this cardiac condition |
Ischemic Heart Disease – Angina pectoris – Stable | MC Angina, occuring in effort or exericse d/t coronary atherosclerotic occlusion |
Ischemic Heart Disease – Angina pectoris – Variant/Prinzmetal | Vasospastic angina, due to a reversible decrease in coronary blood flow. |
Ischemic Heart Disease – Angina pectoris – Risk Factors | Risk factors for this cardiac condition include Hypertension, Diabetes, Hyperlipidemia, Smoking |
Ischemic Heart Disease – Angina pectoris – Px | This cardiac disorder is seen more commonly in adult males and in post-menopausal females |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy | Incease oxygen delivery by reducing vasospasm (nitrates & CCBs). Decrease oxygen requirement by decreasing TPR/CO (+B-blockers) |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Types | Classes of drugs used in this condition include nitrates, calcium channel blockers, and beta blockers. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates | Prodrugs of nitrous oxide that decreases pre-load & O2 requirement by dilating veins. Also reduces infarct size & improves post-MI mortality. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Pathway | In Endothelial cells, upon binding of ACh, bradykinin, 5-HT etc: L-arg → NO (NO Synthase). Smooth muscle cells: Nitroglycerin activates guanylyl cyclase with creates cGMP. This activates phosphatase which acts on MLCK, leading to vasodilatation. |
Anti-Anginal Drugs – Nitrates – Effects | Decrease pre-load (most import…(-) end-diastolic size and pr, (+) subendocardial perfusion), cardiac work & O2 demand by dilating VEINS. (+) coronary collateral circulation. Relieve vasospasm of coronary vessels. (-) infarct size, (+) post-MI mortality |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types | There are both nitrates and nitrites used in the treatment of this disorder |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types - Classic - Subtypes | "This class of antianginals includes nitroglycerin (GTN), isosorbide dinitrate, isosorbide mononitrate, Erithrityl tetranitrate |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types - Nitrates | This class of antianginals includes amyl nitrite |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types- Classic - RoA (4) | RoA's for this drug class include short acting: sublingual (GTN, Isosorbide dinitrate), long acting: oral (isosorbide mononitrate, isosorbide dinitrate, Erithrityl tetranitrate), and ointment and transdermal preparations. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types- GTN - | This Nitrate is the DOC in acute anginal attack b/c it onsets in <1min d/t sublingual or spray RoA. Undergoes high first pass metab. transdermal or IV preparations are prophylactic |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates -Types-Isosorbide - Pharmacokinetics | The dinitrate form of this drug onsets in 5 min, while the mononitrate in 30 min. Timed/Extended release formulas have d/a 8-12hrs. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Indications | In stable angina, these drugs are used synergistically w B blockers to improve exercise tolerance. In variant angina, they are used in combination with CCBs/ |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Adverse Reactions | Adverse reactions of this drug include tachyphylaxis w repeated use, For variant angina, morning is worst period d/t catecholamine surge, also headache, flushing, postural hypotension, reflex tachycardia and fluid retention, and metHBemia at large doses) |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Adverse Reactions - Tachyphylaxis - Antidote | This adverse reaction to nitrates is overcome with a drug holiday of 10-12 hrs/overnight, when demand of heart is increased. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Adverse Reactions - Drug Interactions - Drugs | This drug class interacts with Sildenafil and Cocaine |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Adverse Reactions - Drug Interactions - Sildenafil | Nitrates interact with this drug, aka Viagra, tor/I potentiation of their hypotensive effect, leads to SEVERE hypotension, tachycardia and heart attack |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrates - Adverse Reactions - Drug Interactions - cocaine | the result of cocaines interact with this drug class includes increases oxygen demand by increasing HR & decreases O2 supply by vasoconstriction |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Nitrites - Nitrites - Amyl Nitrites | This is an organic nitrite, not used for angina, but for tx of CN- poisoning (converts Hb to methemoglobin which has affinity for cyanide). Followed by administration of sodium thiosulfate for excretion. Not used as much dt unpleasant odour and short d/a. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers | This class of anti-anginals works by (-) after-load by arteriolar dilation |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers (CCBs) – Mechanism of Action | This class of drugs blocks L-type channels in heart & blv's. This (-) contractile F and o2 reqmts. Lack of Ca2+ results in vasodilation. Predominantly, arteriolar dilation. Coronary dilation relieves vasospasm. Peripheral vasodilation reduces afterload. |
Anti-Anginal Drugs – Ca2+ channel blockers (CCBs) – Indications | All drugs of this class are indicated for angina pectoris. -Dipines better for vasospastic - good coronary dilators. They are usually give in combo w nitrate. Also used in HTN (even w PVD, DM, Angina, Asthma), peripheral vascular disease, arrythmia (V/D) |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers (CCBs) – Classification | This class of drugs includes 1) Verapamil and Diltiazem – 2) DihydropyriDINES |
Anti-Anginal Drugs – Ca2+ channel blockers (CCBs) – Verapamil/Diltiazem | These anti-anginal drugs have effect on cardiac & vascular Ca channels, no change in preload & ventricular arrhythmias. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers (CCBs) – 'Dines' | These anti-anginal drugs, particularly dihydropyri - have much greater affinity for vascular Ca2+ channels only. Affect only afterload, O2 consumption, both anginas & HTN. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers (CCBs) – Adverse Effects | Adverse effects of these drugs include Constipation (Vera), Flushing, dizziness, headache & fatigue, peripheral edema, reflex tachy & gingival hyperplasia (-dipines), cardiac depression |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Ca2+ channel blockers (CCBs) – Contraindications | Verapamil/Diltiazem should be used cautiously in patients w/ cardiac failure & heart blocks, as they increase supraventricular tachycardia (too much work, 02 demand). But before failure, they are very useful (increase work helps perfusion) |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - B-Blockers - Mechanism of Action | This drug class works in the tx of angine by(-) HR (+ perfusion), F of Contraction, time to onset of angina → decrease O2 demand |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - B-Blockers - Indications | Combo tx w nitrates and CCBs preferred for this drug class in txg classic angina d/t (-) adverse effects of both agents (inhibit reflex tachycardia). Carvedilol clinically equivt to isosorbide. also prophylactic of sudden death d/t arrhythmias (post-mi). |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - B-Blockers - Adverse Reactions | Adverse effects of these drugs include fatigure, depression, insomnia, hallucinations, deranged lipid profile, bronchospasm, masking of hypoglycemic conditions of DM, and sexual dysfunction |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - B-Blockers - Adverse Reactions - Drug Interactions | These should not be used with Verapamil/Diltiazem |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - B-Blockers - Contraindications | These drugs are contraindicated in variant/prinzmetal angina and in CAD px w asthma, diabetes mellitus and HF. |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - Best combo for Vasospastic | Nitrates increase preload while CCBs decrease afterload and so their combination is ideal for this condition |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - New | This class of drugs includes potassium channel activators (nicorandil), dipyramidole, trimetazidine and ranolazine (cytoprotective antiischemic), ivabradine |
Ischemic Heart Disease – Angina pectoris – Pharmacotherapy - New - Dipyramidole | This drug results in coronary steal phenomenon, diverting flow to non-ischemic areas only, giving it pharmacological success but therapeutic failure. Further exacerbates angina. |
Ischemic Heart Disease – MI – Pharmacotherapy | Pharmacotherapy for this condition involves aspirin, oxygen, GTN, morphine (opiod analgesic), beta blockers (metoprolol), antiarrhythmics, thrombolytics and percutaneous coronary interventions, heparin, lipid lowering agents, ACE inhibitors if EF <40% |