← Pharmacology (Exam 3 Spring 2012) Export Options Alphabetize Word-Def Delimiter Tab Comma Custom Def-Word Delimiter New Line Semicolon Custom Data Copy and paste the text below. It is read-only. Select All High levels of Atropine Antimuscarinic, Skin is dry, difficulty with vision and sympathetic discharge Alpha 1 Agonist Phenylephrine Phenylephrine Increases Ca (intracellularly)-->activates phospholipase-->vasoconstriction-->constrict smooth muscle Alpha 2 Agonists Clondidine, methyldopa, guanfacine Clondidine Decreases adenylate cyclase-->opens K channels-->decreases Ca channels, decreases blood pressure and sympathetics Beta 1 Agonist Increases Ca (intracellularly)--> on heart increases HR and contractility Beta 2 Agonist Stimulates adenylate cyclase activity-->decreases Ca (intracellularly)-->on lungs relaxes smooth muscle-->vasodilation Beta 2 Agonist Albuterol Beta 1 Agonist> Beta 2 Agonist Dobutamine Beta 1 = Beta 2 Isoproterenol Isoproterenol increases HR and bronchodilator D1 CNS and periphery increases in cAMP and CO D2-D4 decreases in cAMP in intra-renal arteries and arterioles, vasoconstriction A1A2B1 NE A1A2B1B2 Epi Potent D1 Agonist that increases CO and decreased TPR Fenoldopam Nonselective Alpha blockers Phentolamine Alpha 1 Blockers Prazosin Alpha 1 Blockers Vasodilation to decrease BP in hypertensive crisis Nonselective Beta Blocker Propanolol, timolol Selective B1 Blocker Atenolol Alpha and Beta Blocker Carvedilol Treats Pheochromocytoma Carvedilol Dopamine Directly stimulates alpha and beta receptors M1 CNS, Gq, increases cAMP by increasing IP3 M2 Heart, Gi, decreases cAMP, efflux of K M3 Smooth muscle, Gq increases Ca, smooth muscle contraction, NO synthase stimulated, not innervated Baroreceptor reflex carotid sinus and aortic sinus, primary response, increases stretch, fastest way to change HR. Chemoreceptor reflex Carotid Body and Aortic Body, secondary response Increase in HR always decreases duration of diastole HMG-CoA R Inhibitors Statins D1 Low dose dopamine D1b1 medium dose Dopamine D1B1A1 high dose dopamine statins block formation of fatty acids, decrease LDL Statin side effect Myositis and rhabdomyolysis Bile Acid binding resins "Cole" "Cole" reduces gastric reabsorption of cholesterol, increase TG Bile Acid binding resin side effect increased TG, vitamin k deficiency Cholesterol Absorption inhibitor Ezetimibe Ezetimibe prevents uptake of cholesterol from gut to liver Fibric Acid Derivatives Fenofibrate or gemfibrozil Fenofibrate breaks down fatty acid Fenofibrate side effect rhabdomyolysis Niacin Inhibits cholesterol--> VLDL, increases HDL Side effect of niacin high doses cause flushing and Gout Fish oil decreases TG (side effect: fish burp) Osmotic Diuretic Mannitol Mannitol increases osmotic pressure which retains water in tubule Mannitol side effect Volume expansion Carbonic Anhydrase Inhibitor prevents reabsorption of HCO3 from Proximal Tubules Carbonic Anhydrase Inhibitors Acetazolamide, Dorzolamide Carbonic Anhydrase Inhibitors Side Effect Hypokalemia, metabolic acidosis, reduced Ca reabsorption, not reccommended for use in people with sulfa drug allergies or sickel cell anemia Loop Diuretics inhibits Na/K/2Cl symporter in ascending loop of hendle, reduced Na reabsorption, dilute outside of tubule, reduced water reabsorption Loop Diuretics Ethacrynic Acid, Furosemide, Torsemide Loop Diuretic Side Affects Hypokalemia potentiates digitalis toxicity, metabolic alkalosis, hypomagnesemia and Ca loss from decreased luminal K, hyperuriecemia due to hypovolemia Thiazide Diuretic Hydrochlorothiazide Hydrochlorothiazide acts on distal tubule, treats HTN, excretes Na, blocks Na/Cl symporter Side effect of thiazide diuretic K wasting K Sparing Diuretics acts on Collecting duct, allows Na and water excretion by retains K K sparing diuretics Amiloride, Spironolactone, Triamterene Side effects of K sparing diuretics promotes hyperkalemia, ACE inhibitors make hyperkalemia worse and NSAIDS reduce diuretic effiacy ADH acts of cortical collecting duct, stimulates renal synthesis of aquaporin (V2) receptors, permits renal H2O reabsorption Treat scuba divers and astronauts with ADH Vasopressin Antagonist acts on cortical collecting duct, Conivaptan, treats hyponatremia from SIADH and causes nephrogenic diabetes insipidus Side affects of Vasopressin Antagonist hypovolemia and increased blood osmolarity Nitroglycerine is contraindicated in patients with glaucoma, anemia, pregnancy, or Viagra IV Nitroglycerine First line to improve cardiac flow, nitric oxide donor Sublingual Nitroglycerine treats Angina Disadvantage to Nitroglycerine Tolerance develops, headache, reflex tachycardia Sodium Nitroprusside Nitric oxide donor, arterial/venous dilation, can cause cyanide poisoning Sodium Nitroprusside is contraindicated in patients with pre-eclampsia, hyponatremia, pregnancy, viagra Phosphodiesterase inhibitor Type 3 Aminophylline increases cAMP, dilates, even during alpha and beta blockade, amplify sympathetic activators, catastrophic if used with sympathetic mimetics Phosphodiesterase inhibitor Type 5 Sildenafil increases cGMP, vasodilation, DO NOT MIX WITH NITRATES OR CIRCULATORY COLLAPSE WILL HAPPEN! Hydralazine opens K channels, vasodilates Minoxidil opens K channels, vasodilates, unwanted body hair is a negative side effect Non-selective Ca channel blocker blocks blood vessels only Selective Ca channel blocker blocks blood vessels and heart All Ca channel blockers promote vasodilation and coronary blood flow Verapamil and Diltiazem Ca channel blocker, negative inotropic Nifedipine, dihydropyridine Ca channel blocker, vasodilator, CONTRAINDICATED IN HEART FAILURE CA channel blocker side effect breast enlargement alpha 1 receptor antagonist Doxazosin Beta 1 Blocker can be taken with Doxazosin to control the heart rate ACE Inhibitor "prils" and protects against cardiac remodeling, vasodilation Angiotensin II receptor Antagonist "artans" and protects against cardiac remodeling with less of a cough, vasodilation Aldosterone receptor antagonist/blocker (ARB) Spironolactone Spironolactone Spares K, protects against cardiac edema and remodeling, promotes Na loss Direct renin antagonist aliskire(causes vasodilation) Vasodilators all cause headaches, orthostatic hypotension, and hypotensive episodes Na channel blocker class 1A prolonged repolarization, procainamide Na channel blocker class 1B shorten time for repolarization, Lidocaine First line of treatment for arrhythmias Lidocaine (IV) Na channel blocker class 1C Flecainide Class 2 Beta blockers, Esmolol Class 3 block K channels Amiodarone Class 3, turns patient blue Class 4 slow ca channel blocker, cardioselective Ca channel blocker Diltiazem and Verapamil Class 4 Digoxin increases Ca storage in SR, slows HR and force of contraction, narrow therapeutic index, DANGEROUS WITH VERAPAMIL, AMIODARONE, ERYTHROMYCIN, and Epi Magnesium Sulfate controls torsades de pointes Treatment for arrhythmias IV Lidocaine, Class 1A to capture heart rate, if wolff parkinson white try class 1A with beta blocker, if fibrillation or torsade de Pointes try Magnesium Sulfate Cardiac Glycosides Digoxin, Digitoxin, Digoxin Immune Fab Digoxin Increase Ca storage in SR, slows HR, increases F of contraction, CLEARED THRU KIDNEY with a narrow therapeutic index Adverse affects of Digoxin arrthythmias, ventricular tachycardia, fibrillation, overdose in renal failure, women have 33% more fatalities than untreated Digoxin directly blocks Na/K ATPase Digitoxin Metabolized by liver Digoxin Immune Fab Treats digoxin overdose, not reccommended in patients with sheep allergies Adrenoreceptor agonists Epi, NE, Isoproterenol, Dopamine and Dobutamine Epi and NE are used to treat cardiac arrest Low dose Dopamine D1 (vasodilation) Medium dose Dopamine B1 (increased cardiac contractility) High dose Dopamine A1 (vasoconstriction) Dopamine is best used for Shock! Can you use Epi and NE to treat shock? No! Lactic acidosis causes the catecholamine receptors to loose their shape. Phosphodiesterase Inhibitor 3 Milrinone, Inamrinone, Vesnarinone Milrinone Treats CHF, slow degradation of cAMP, restrores sympathetic drive in presence of adrenergic receptor antagonists, DON'T use with B agonists! Ca Sensitizing Agent Levosimendan Hypertension treatment 1. Therapeutic lifestyle change. 2. hydrochlorthiazides or ACE inhibitors Hydrochlorothiazide acts of distal tubule to promote Na, H2O excretion, K wasting, Ca sparing and tachycardia Use Hydrochlorothiazide with Selective Beta 1 Blockers (to control tachycardia) ACE Inhibitor Protects against cardiac remodeling, vasodilator, Na/H2O excretion and limits K loss ARB Like ACE Inhibitor but LESS COUGHING Use the following drugs in a Hypertensive Crisis Esmolol, Nitroglycerin, Sodium Nitroprusside Acute Coronary Syndrome Ischemic heart disease How to treat Acute Coronary Syndrome MONA (Morphone, Oxygen, Nitrates, Aspirin) Chronic Cardiac ischemia treatment Nitrates, B-Blockers, non-selective Ca channel blockers Should you use Beta-Blocker to treat CHF? No! That would promote pulmonary edema. How do you treat CHF? ARB (Spironolactone) and ACE Inhibitor How do you treat an emergency Beta-2 Blockade? PDE-3 Inhibitor High levels of ANP is diagnostic of heart failure Flow is the name of the game! Why use Spironolactone to treat CHF? It counteracts aldosterone escape.