CARDIOVASCULAR DRUGS Methyldopa Use SE Sympathoplegic HTN Sedation

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? • Vasodilator—angina, pulm edema, aphrodisiac/erection enhancer • Releases NO from smooth muscle: increased c. GMP relaxation. Veins> Arteries – Which does Arteries > Veins? – HYDRALAZINE • Decreased Preload or • PRELOAD Afterload? • Tachycardia, Flushing, HA, • Toxicity 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 c. GMP 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 Ltype 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? – Dopamine 1 Receptor Agonist: relaxes vascular smooth muscle – #3: Nitroprusside • MOA? – Increased c. GMP 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 Ltype 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 Co. A 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 CLASS Class III Class IV General MOA

Anti-arrhythmics—BIG PICTURE CLASS General MOA Class I Block FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class III Class IV

Anti-arrhythmics—BIG PICTURE CLASS General MOA Class I Block FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class II Beta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class III Class IV

Anti-arrhythmics—BIG PICTURE CLASS General MOA Class I Block FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class II Beta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class III Prolong 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 CLASS General MOA Class I Block FAST sodium channels responsible for phase 0 depolarization Quinidine, Flecanide, Procainamide… Class II Beta Adrenergic Receptor Antagonists Propranolol, Metoprolol… Class III Prolong action potential with little effect on phase 0 depolarization, mostly via blocking the K repolarizing current Amiodarone, Sotalol, Ibutilide… Class IV Block slow L-type Calcium Channels Verapamil, Diltiazem

Class I Drugs: Broken up by degree of Na channel blockade and effect on AP duration • MOA? CLASS IA Drugs – 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 • MOA? CLASS IB Drugs – 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 • MOA? CLASS IC Drugs – 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 c. AMP 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? • SE • ESMOLOL – 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? • SE • Amiodarone – 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