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CVS Pharmacology

Cardiovascular system pharmacology-Ischemic Heart Disease

What is myocardial stunning? The reversible reduction of function of heart contraction after reperfusion not accounted for by tissue damage or reduced blood flow
The calcium combines with calmodulin to form: a complex that converts the enzyme myosin light-chain kinaseto its active form (MLCK)
Beta2 agonists may cause relaxation in smooth muscle by: accelerating the inactivation of MLCK
Calcium influx is inhibited by CCBs, leading to muscle relaxation
Organic nitrates release Nitric oxide
What is the function of nitric oxide? Activation of guanylyl cyclase and increases formation of cGMP
What is the function of cGMP? Smooth muscle relaxation by activating kinases that increase myosin phosphatase activity and decrease myosin phosphate levels
α 1-Adrenoceptor agonists activate phospholipase C (PLC)
What is the function Phospholipase C (PLC)? Increased formation of inositol triphosphate (IP3) from phosphatidyl inositol bisphosphate(PIP2), leading to increased release of calcium from the sarcoplasmic reticulum
Function of B2 receptor agonists: Increased formation of cyclic adenosine monophosphate (cAMP), which activates kinases that inhibit myosin light-chain kinase
What is the prototype of nitroglycerine? Nitroglycerine
What is the function of Nitroglycerine? Nonspecific smooth muscle relaxant General vasodilation
How is nitroglycerine administered? Usually, sublingual But can be administered by many routes
Onset of action of nitroglycerine? 1-3 minutes, Peaks at 10 minutes
DOA of nitroglycerine: 15-30 minutes Until reductase in the liver breaks down the drug
How long does arteriolar vasodilation last? 5-10 minutes
How long does venous vasodilation last? 30 minutes
Function of arteriolar vasodilation: Decreases systemic blood pressure (afterload) and causes reflex tachycardia and increased contractility (the last two are deleterious effects) Might increase MVO2
Function of venous vasodilation: Decreases venous return (preload) and decreases MVO2
Side effects of Nitroglycerine: Headache Hypotension Tachycardia Increased intraocular and intracranial pressures Methemoglobinemia Tolerance: only for the arteriolar effects Withdrawal: in workers in ammunition industry
Functions of Beta Adrenergic Blockers Cause subjective and objective improvement Decreased number of anginal episodes Nitroglycerine consumption Enhanced exercise tolerance Improved ECG
Advantages of taking Beta adrenergic blockers: Prevent actions of catecholamines, so more effective during exertion Do not dilate coronary arteries Do not increase collateral blood flow
Functions of CCBs: Beneficial in vasospasm
Harmful effects of CCBs: Can affect platelets aggregation May be dangerous in the presence of heart failure and in patients susceptible to hypotension
Side effects of CCBs: Hypotension Headache Dizziness Flushing Peripheral edema.
Function of Dipyridamole: Inhibits the uptake of adenosine and inhibits adenosine deaminase enzyme Thought to be a good coronary dilator Increases the blood flow to the normal area Still used as an antiplatelet drug
Other solutions for ischemic heart disease: ACEI Anticoagulants and/or Thrombolytic Therapy Cholesterol Lowering Agents Angioplasty Surgery
Newer anti-anginal drugs: Metabolic modulators Direct bradycardic agents Potassium channel activators Rho-kinase inhibitors Sulfonylureas Thiazolidinediones Vasopeptidase inhibitors Nitric oxide donors Capsaicin Amiloride
What is the newer metabolic modulator? Ranolazine
What is the newer bradycardiac agent? Ivabradine
What is the newer Potassium channel activators? Nicorandil
What is the newer Rho-kinase inhibitor? Fasudil
Newer sulfonylurea? Glibenclamide
Newest Nitric oxide donor: L- arginine
Additional Effects of CCBs: A direct effect on HR and contractility (decrease) Indirect effect (from high doses) Increase HR and contractility (reflex) Enhance collateral vessel diameter The ratio of epicardial to endocardial blood flow/endo is increased
Nifedpine is not used in cardiac arrhythmias , unlike verapmil which is effective in almost everything
Created by: Ulaisl



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