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20 Cards in this Set
- Front
- Back
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By which pathophysiological mechanisms can we improve the symptoms of angina? |
By decreasing the hearts oxygen demand and/or by increasing hearts oxygen supply. |
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Name organic nitrates |
Glycerol trinitrate, isosorbide dinitrate and isosorbide mononitrate. |
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Mechanism of action of organic nitrates? |
They get converted into NO inside the body by consuming -SH from glutathione. NO stimulates the guanylyl cyclase inside the smooth muscle cells, causing them to produce more cGMP. The increased cGMP activates protein kinase G, leading to dephosphorylation of myosin light chains. This gives smooth muscle relaxation and vasodilation. |
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Where do the organic nitrates induce vasodilation and why is this good? |
In veins and coronary arteries. Arterioles are not dilated. The preload and afterload is decreased, and the work of heart is decreased. The myocardial oxygen demand decreases. |
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Describe the tachyphylaxis in organic nitrates and how it can be avoided. |
Development of tachyphylaxis may occur since they can deplete the available -SH groups to react with. This tachyphylaxis appears after 24 hours of continuous administration. Can be avoided by taking the patients off the nitrates for 6-8 hours every day. |
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Indications of glycerol trinitrate? |
- Stable Angina - Unstable angina - Prinzmetals - Hypertensive crisis - Acute left ventricular failure - AMI - Coronary vasodilation during angiography. |
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Side effects of organic nitrates? |
Headache, dizziness and orthostatic hypotension |
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Pharmacokinetics of glycerol trinitrate? |
Can be absorbed in intestine, oral mucosa and skin. Since it has a significant first-pass metabolism and oral bioavailability varies very, it is preferred to give it as IV, sublingual spray, buccal tablet or transdermal patch. Half-life of glycerol trinitrate is 1-3 minutes, and it takes 1 min to work (transdermal takes 1 hour) |
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Indications for transdermal patch with glycerol trinitrate? |
Given as maintenance treatment of angina or for chronic treatment of congestive heart failure when standard therapy fails. It is only worn for 12 hours. |
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Contraindication of organic nitrates? |
- Hypotension - Combination with PDE5 inhibitors sildenafil, tadalafil and vardenafil (viagra) - Increased ICP - Closed-angle glaucoma - Hypertrophic obstructive cardiomyopathy - Primary pulmonary hypertension - Combined with alcohol |
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Pharmacokinetics of Isosorbide mononitrate (ISMN)? |
Has 100 % bioavailability, and can be taken orally. Good for chronic maintenance of angina. |
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When are calcium channel blockers used as antianginal treatment? |
Used in treatment of stable angina together with beta blockers. They can improve anginal symptoms by giving vasodilation of periphery and coronaries and reducing myocardial contractility. |
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When are beta-blockers used? |
Used for maintenance of stable angina. They relieve anginal symptoms by reducing heart rate, contractility and therefore oxygen demand. |
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Action and use of Ranolazine? |
Inhibits late Na+ current in myocardial cells by unknown mechanism. Indicated in stable angina when b-blockers and Ca2+ channel blockers are not tolerated or work. |
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Action of Trimetazidine? (its unique) |
Inhibits carnitine so fatty acids are not transported into the mitochondrion. This shifts the myocardial metabolism towards glycolysis which uses less oxygen than fatty acid oxidation. The myocardial oxygen demand is now decreased. |
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How to treat acute symptoms of stable angina? |
Sublingual glycerol trinitrate or ISDN. |
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Maintenance therapy of stable angina? |
Beta blockers is first choice, but organic nitrates or ca2+ channel blockers can be used as well if no effect with B-blockers. |
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How to treat unstable angina or NSTEMI? |
MONA treatment (Morphine, O2, GTN and aspirin). |
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What to give to prevent ischemic heart disease?(which leads to angina ofc) |
Aspirin, statins, B-blockers, ACEIs and exercise. |
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Second-line drugs in angina? |
Ranolazine, trimetazine |
