Cardiovascular And Renal Pharmacology Flashcards
Altepase
Serine protease - catalyses the conversion of plasminogen to plasmin. Helps clot breakdown - localised action. Myocardial infarction and acute ischaemic stroke.
Acetazolamide
Carbonic anhydrase inhibitor. Weak diuretic to treat oedema. Now more to treat glaucoma.
Alpha-methylnoradrenaline
Selective A2 agonist. Inhibits sympathetic nervous system output and lower blood pressure. Antihypertensive.
Amiloride
Blocks ENaC - inhibits Na+ reabsorption, promotes H20 loss. Potassium sparing diuretic. Hypertension and congestive heart failure.
Aminocaproic acid
Lysine analogue. Effective inhibitor for enzymes that bind to that it. Including plasmin (fibrinolysis). Treat excessive postoperative bleeding (eg. Cardiac surgery).
Amiodarone
Class III antiarrhythmic agent - ventricular and atrial dysrhythmias. Prolongs phase III of the cardiac action potential (depolarisation phase). Very common use.
Bisoprolol
Selective B1 blocker. Limit damaging effects of chronic catecholamine stimulation to improve cardiac function.
Captopril
ACE inhibitor. Inhibits conversion of ATI to ATII. Prevents vasoconstriction and aldosterone secretion. Prevents increase in blood pressure.
Clonidine
Centrally acting A2 agonist. Treat hypertension.
Clopidogrel
Irreversibly binds to P2Y12 receptor on platelet cell membranes. Inhibits blood clots. Used in coronary artery disease, vascular disease and the prevention of myocardial infarction.
Dabigatran
Thrombin inhibitor. Used in atrial fibrillation and stroke. Prophylactically to prevent thromboembolism.
Digoxin
Cardiac glycoside. Inhibits Na/K/ATPase. Lots of Na+, Ca2+ cannot be pumped out so stronger contractions. Used to alleviate oedema and antidysrhythmias.
Diltiazem
Calcium channel blocker. Potent vasodilator. Class IV antiarrhythmic. Hypertension, angina and some arrhythmias.
Enalapril
ACE inhibitor. Prodrug, activated in the liver. Used in hypertension and in heart failure (decrease pre and after load)
Eptifibatide
Inhibitor of glycoprotein IIb/IIIa receptor normally needed for fibrinogen bridging between platelets -> aggregation. Prevention of myocardial infarction.
Furosemide
Loop diuretic - high ceiling as high rate of diuresis. Sulphonamides. Blocks the Na+-K+-2Cl- co trasporter in the apical membrane of the cells.Reduces reabsorption of these ions so water is drawn out and excreted. Also causes venodilation which reduces atrial filling pressure which increases renal blood flow withouth a change in GFR.
Heparin
Naturally occuring anticoagulant produced by basophils and mast cells. Binds to enzyme inhibitor antithrobin III -> conformational change exposes active site. This inactivates thrombin and proteases involved in blood clotting (eg. Factor Xa). Used in unstable angine, myocardial infarction, deep vein thrombosis and prophylactic to prevent clots forming.
Hydrochlorothiazide
Thiazide diuretics. Some inhbition of carbonic anhydrase Act on corical segment of TAL - block the Na+-Cl- cotransporter (binding to the Nl- site), reduceing reabsorption and increases water excreted. Also have vasodilatory effects. Hypokalaemia a problem
Levosimendan
Inodilator (calcium snesitiser) used in hospitals for heart failure.Also has a vasodilatory effect by opening ATP-sensitive ptassium channels in vascular smooth muscle to cause smooth muscle relaxation. Increase force of contraction, decrease preload and afterload.
Losartan
First non-peptide angiotensin II antagonist (angiotensin receptor blocker). Acts on the AT1 angiotensin II receptor - these are the receptors involved in normal response.
Mannitol
Osmotic diuretic. Filtered in glomerulus but not reabsorbed, retain osmotic equivalent of waer so increase urine volume. Decrease Na+ reabsorption. Useful where urine flow is reduced. If used for a long time, screws up electrolyte balance. Used if want to get rid of a lot of fluid in a short space of time eg. cerebral oedema.
Milrinone
Type III phosphodiesterase inhibitor is the mst often used inodilator in heart failure. Limited use as can cause dysrythmias. Short term treatment of severe heart fialure unresponsive to more conventional therapy.
Minoxidil
Contains nitric oxide functional group so may act as a nitric oxide agonist. Also a potassium channel opener (KCO) - acts on ATP-sensitive K+ channels in vascular smooth muscle -> causing hyperpolarisation of cell membranes and relaxation. Antihypertensive vasodilatory medication, can be used to treat severe refractory hypertension. Slows/stops/promotes hair regrwoth. Treatment of androgenic alopecia.
Ouabain
Also a Na+-K+ pump inhibit causing the Na+ gradient to decrease and therefore unable to pump Ca2+ out of cardiomyocytes so stronger contractions. Too powerful for clinical use but used experimentally.
Pimobendan
Calcium sensitiser - snesitise and increase the cardiac Ca2+ binding efficiency to troponin without a requirement for more energy consumption. Cause peripheral vasodlatation by inhibiting PDEII. Veterinary used.
Propranolol
Non-selective beta blocker. Used to treat hypertension, angina, myocardial infarction etc.
Reserpine
Depletes catecholamines from peripheral sympathetic nerve endings Blocks the VMAT so neurotransmitters can’t be transported into vesicles or released. Long lasting effects.
Rivaroxaban
Factor Xa inhibitor - prevent clotting, atrial fibrillation and stroke patients.
Saralasin
Angiotensin II receptor partial agonist - peptide socan’t be given orally. IV administration.
Sildenafil
(Viagra). Phosphodiesterase V inhibitor (cGMP specific). AN inodilator , by increase intracellular levels this mimics the effects of B-receptor stimulation. Vasodilatation decreases the after load on the heart.
Streptokinase
Binds to plasminogen activator and causes generation of plasmin - leads to degradation of the fibrin in cloths and also breaksdown clotting factors II, V and VII.
Tirofiban
Antiplatelet drug - glycoprotein Iib/IIIa inhibitors - which is needed for fibronigen bridging between platelets that causes aggregation. Used for prevention of myoardial infarction.
Tranexamic Acid
Analogue of aminocaproic acid so competitively inhibits plasminogen activation. Used to prevent excessive clot lysis which could lead to severe bleeding.
Triamterene
Potassium sparing diuretic used in combinationiwth thiazide diuretics for the treatment of hypertension and oedema. Blocks the ENaC - increases concentration of Na+ in the urine without affecting K+ too much.
Warfarin
Orally given clot inhibitor. Inhibits synthesis of clotting factors II, VII, IX and X and regulation factors - protein C, S and Z. Prophylactic and also prevent clot formation on prostehtic heart valves.
