CARDIOVASCULAR DRUGS!!!!!

Methyldopa Use? SE? Sympathoplegic, HTN Sedation, positive coombs test

Reserpine Use? SE? Sympathoplegic, HTN Sedation, depression, nasal stuffiness, diarrhea

Hydrochlorothiazide Use? SE? Diuretic, HTN Hypo-K, Hyperlipidemia, hyperuricemia, lassitude, Hyper-Ca, Hyperglycemia

Clonidine Use? SE? Sympathoplegic, HTN Dry mouth, sedation, severe rebound HTN

Guanethidine Use? SE? Sympathoplegic, HTN Orthostatic & exercise hypotension, diarrhea, sexual dysfxn 

Nitroglycerin, Isosorbide Dinitrate Use? MOA? Decreased Preload or Afterload? Toxicity Vasodilator—angina, pulm edema, aphrodisiac/erection enhancer Releases NO from smooth muscle: increased cGMP  relaxation. Veins> Arteries – Which does Arteries > Veins? – HYDRALAZINE PRELOAD Tachycardia, Flushing, HA, hypotension, Monday Disease— decreased tolerance over weekend  tach, dizziness and HA on reexposure

Prazosin Use? SE? Sympathoplegic, HTN Orthostatic hypotension with 1 st dose, dizziness, headache

Diazoxide Use? SE? Vasodilator, HTN Hyperglycemia, decreased insulin release, hypotension

Beta blockers Use? SE? Sympathoplegic, HTN Impotence , asthma, cardiovascular effects (bradycardia, CHF, AV block), CNS effects— sedation and changes in sleep

Hydralazine Use? Mechanism of Action? Reduces preload or afterload? SE? Vasodilator, severe HTN, CHF Increased cGMP  smooth muscle relaxation. Arterioles > veins. AFTERLOAD (Vasodilator!) Nausea, Headache, Lupus-like syndrome, reflex tachycardia (don’t use in agina or CAD!), angina, salt retention Use with beta blocker to avoid tachycardia and with a diuretic to avoid salt retention

Minoxidil Use? Mechanism of Action? SE? Vasodilator, HTN K channel opener, hyperpolarizes smooth muscle cells HAIRY MONSTER, pericardial effusion, reflex tachycardia, angina, salt retention Use with beta blocker to avoid tachycardia and with a diuretic to avoid salt retention

Captopril Use? Other Examples? SE? ACE Inhibitor, HTN Enalapril, Fosinopril Hyper-K, cough, angioedema, taste changes, hypotension, fetal renal damage, rash, increased renin

Hexamethonium Use? SE? Sympathoplegic, HTN Severe orthostatic hypotension, blurry vision, constipation, sexual dysfxn 

Verapamil Use? MOA? More cardiac or smooth muscle effects? SE? Toxicity? Calcium Channel Blocker, HTN, angina, arrhythmias, Raynaud’s Blocks Voltage Dependant L- type Ca channels, decreasing contractility Cardiac, but also vasodilator Dizziness, flushing, constipation, AV block, Nausea Cardiac depression, peripheral edema, flushing, dizziness, constipation

HOW DO YOU TREAT MALIGNANT HYPERTENSION??? Three drugs in alphabetical order – #1: DIAZOXIDE MOA? – K channel opener—hyperpolarizes smooth muscle – #2: Fenoldopam MOA? – Dopamine1 Receptor Agonist: relaxes vascular smooth muscle – #3: Nitroprusside MOA? – Increased cGMP via direct NO release SE? – CYANIDE POISONING!!!

Nitroprusside Use? SE? Vasodilator, HTN Cyanide Poisoning (Releases CN!)

WHICH TWO DRUGS ARE THE HYPERTENSION IN PREGNANCY SUPERSTAR MEDS? (Which are ok to use in Pregnancy?) HYDRALAZINE & METHYLDOPA This, on the other hand is NOT safe in pregnancy…. 

Diltiazem Use? MOA? More cardiac or smooth muscle effects? SE? Toxicity? Calcium Channel Blocker, HTN, angina, arrhythmias, Raynaud’s Blocks Voltage Dependant L- type Ca channels, decreasing contractility Somewhere in the middle Dizziness, flushing, constipation, AV block, Nausea Cardiac depression, peripheral edema, flushing, dizziness, constipation

Losartan Use? Good alternative to what? SE? Angiotensin II Receptor Blocker, HTN ACE Inhibitors Fetal renal toxicity, Hyper-K

Nifedipine Use? MOA? More Cardiac or Smooth Muscle Effects? SE? Toxicity? Calcium Channel Blocker, HTN, angina, Raynaud’s Blocks Voltage Dependant L-type Ca channels, decreasing contractility Smooth muscle—vasodilator Dizziness, flushing Cardiac depression, peripheral edema, flushing, dizziness, constipation

CHOLESTEROL DRUGS Which is best for decreased triglycerides? – Fibrates – Examples? Gemfibrozil, Clofibrate, Bezafibrate, Fenofibrate Which are best for decreasing LDL? – Statins – MOA? HMG CoA reductase inhibitors—inhibit cholestrol precursor: mevalonate Which do patients hate taking because of GI disturbances? – Bile Acid Resins: Cholestyramine & Colestipol What are two other possible drugs you could use? – Cholesterol Absorption Blockers (Ezetimibe) and Niacin

Anti-arrhythmics—BIG PICTURE CLASSGeneral MOA Class I Class II Class III Class IV

Anti-arrhythmics—BIG PICTURE CLASSGeneral MOA Class IBlock FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class II Class III Class IV

Anti-arrhythmics—BIG PICTURE CLASSGeneral MOA Class IBlock FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class IIBeta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class III Class IV

Anti-arrhythmics—BIG PICTURE CLASSGeneral MOA Class IBlock FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class IIBeta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class IIIProlong action potential with little effect on phase 0 depolarization, mostly via blocking the K repolarizing current Amiodarone, Sotalol, Ibutilide… Class IV

Anti-arrhythmics—BIG PICTURE CLASSGeneral MOA Class IBlock FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class IIBeta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class IIIProlong action potential with little effect on phase 0 depolarization, mostly via blocking the K repolarizing current Amiodarone, Sotalol, Ibutilide… Class IVBlock slow L-type Calcium Channels Verapamil, Diltiazem

Class I Drugs: Broken up by degree of Na channel blockade and effect on AP duration CLASS IA Drugs MOA? – Moderate blockade of Na channels = raise AP threshold and slow AP upstroke. Also depress slope of phase 4 depolarization. Uses? – Ectopic foci and reentrant rhythms – Atrial AND Ventricular Arrhythmias Examples? – Quinidine, Amiodarone, Procainamide, Disopyramide SE – Quinidine Cinconchism: HA, tinnitus, thrombocytopenia Increase AP duration, increased effective refractory period, increase QT interval (increased risk of what?) Torsades de points – Procainamide Reversible SLE-like syndrome

Class I Drugs: Broken up by degree of Na channel blockade and effect on AP duration CLASS IB Drugs MOA? – Bold Na channels, but unlike IA’s shorten duration of AP and refractory period Uses? – Preferentially act on diseased tissue: ischemic or depolarized Purkinje/ventricular tissue. – Great post-MI and for dig-induced arrhythmias Examples? – Lidocaine, Mexiletine, Tocainide, Phenytoin? SE – CNS depression/stim and cardiovasc depression

Class I Drugs: Broken up by degree of Na channel blockade and effect on AP duration CLASS IC Drugs MOA? – Most potent sodium channel blockers! Decrease upstroke of AP and conduction velocity everywhere! – No change in AP duration Uses? – Vtachs that progress to VF and intractable SVT – LAST RESORT FOR REFRACTORY TACHYARRHYTHMIAS Examples? – Flecanide, Encainide, Propafenone SE – Proarrhythmic, esp post MI: avoid in those with heart disease  increased mortality! – Prolonged refractory period in AV node.

Class II Drugs MOA? – Beta blockers: decreased cAMP and Ca currents. Decrease slope of phase 4 depolarization. AV node very sensitive. Uses? – Abnormal pacemakers, Vtach, SVT, slow ventricular rate in a-fib or a-flutter Examples? – Propranolol, Esmolol, Metoprolol, Atenolol, Timolol – Which one is super short acting? ESMOLOL SE – Impotence , asthma exacerbation, bradycardia, AV block, CHF,sedation, sleep changes – Why use with caution in diabetics? Mask effects of hypoglycemia – Metoprolol Dyslipidemia

Class III Drugs MOA? – Potassium Channel Blockers: increase AP duration Uses? – used when other drugs fail Examples? – Sotalol, Ibutilide, Bretylium, Amiodarone – Which is good for Wolf-Parkinson-White? Amiodarone SE – Sotalol Increased QT Interval—why is this bad? – Increased risk of torsades de points Excessive beta block – Ibutilide Torsades – Bretylium Arrhythmias, hypotension – Amiodarone Pulm fibrosis, corneal deposits, Hepatotoxicity, photodermatitis, Neuro SE, constipation, bradycardia, heart block, hypothyroid, hyperthyroid CHECK PFT’s, LFTs, and TFTs!!

Class IV Drugs MOA? – Calcium Channel Blockers: AV node: decreased conduction. – Uses? Especially good for? – SVTs Examples? – Verapamil and Diltiazem for Anti-arrhythmics SE – Constipation, flushing, edema, CV effects, torsades

Adenosine MOA – Increased K efflux: hyperpolarization. Drug of choice for which conditions? – AV nodal arrhythmias. Short or long acting? – Very short (~15 Seconds) Toxicity – Flushing, Hypotension, Chest pain

Potassium MOA – Decreases ectopic pacers in hypokalemia Drug of choice for which conditions? – Dig toxicity

Magnesium Drug of choice for which conditions? – Torsades and dig toxicity