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CARDIOVASCULAR AGENTS for use in arrythmia: contraction of ventricle and atrium is not synchronized. Antiarythmia agents will block sodium channel, potassium channel, calcium channel or adrenergic receptor(adreneline,noradrenaline, dopamine). membrane stabilizing agents--aka Class 1 sodium channel blockers The class I antiarrhythmic agents interfere with the sodium channel . Class I agents are divided into three groups (Ia(lengthens action potential),

Cardiovascularagents

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Page 1: Cardiovascularagents

CARDIOVASCULAR AGENTSfor use in arrythmia:

contraction of ventricle and atrium is not synchronized.

Antiarythmia agents will block sodium channel, potassium channel, calcium channel or

adrenergic receptor(adreneline,noradrenaline, dopamine).

membrane stabilizing agents--aka

Class 1 sodium channel blockers

The class I antiarrhythmic agents interfere with the sodium channel.

Class I agents are divided into three groups (Ia(lengthens action potential),

Ib(shortens) and Ic( no effect and increased sodium current depression)---based upon their effect on the length of

the action potential.

Page 2: Cardiovascularagents

• MOA----depresses cardiac conduction and excitabiltity. action potential depends on the opening of sodium ion channels, a blockade of these channels will slow the spread of impulse conduction across the myocardium. mainly for tachycardia.

• Side effects:• diarrhea, naseau, dizziness• examples----• lidocaine/Xylocaine• mexiletine/Mextil• procainamide/Pronestyl• quinidine/Quinaglute• tocainide/Tonocard

CLASS 1--- Vaughan Williams Classification I-IV

Page 3: Cardiovascularagents

Class II--Beta blockersused after heart attack.moa---- blocks adrenaline and noradrenaline from cardiac cells. Beta-adrenergic blockers reduce heart rate and conduction velocity through the AV node. mainly for atrial dysrythmia. side effects---bronchoconstriction, impotence, fatigue, bradycardia, alopecia, depression

examples---atenolol/Tenormincarvedilol/Coregpropanolol/Inderalsotalol/Betapacemetaprolol/Lopressor

Page 4: Cardiovascularagents

class III---potassium channelblockers

moa---prolong the action potential duration (APD) and refractoriness and have been found effective to prevent/suppress cardiac arrhythmias. Cardiac K+ channels are membrane-spanning proteins that allow the passive movement of K+ ions across the cell membrane along its electrochemical gradient. K+ channels affect plateau and repolarization time.side effects---possible pulmonary fibrosis, blue skin deposit, liver damage

examples-- amiodarone, bretylium, sotalol, ibutilide amiodarone, bretylium, sotalol, ibutilide

Page 5: Cardiovascularagents

class IV---calcium channelblockers

calcium allows myosin heads to bind to actin filaments and pull them to get a power stroke. Cardiac muscle requires extracellular calcium ions for contraction to occur.

Page 6: Cardiovascularagents

class IV

moa--Slow conduction velocityProlongs the refractory periodeffective against supraventricular dysrhythmiasside effects----bradycardia, hypotension, constipation,headache, dizziness, heart failureconsider----keep dilitazem from lightexamples--dilitazem/Cardizemverapamil/Veralan

Page 7: Cardiovascularagents

ACE inhibitors-Angiotensin Converting Enzyme

mainly used in congestive heart failure----heart cannot meet oxygen needs for the body. chambers of the heart may respond by stretching to hold more blood to pump through the body or by becoming stiff and thickened. heart muscle walls may eventually weaken and become unable to pump as efficiently.The body keeps high blood pressure by--- the protein renin fromkidneys finds protein angiotensinogen(453 amino acids) from the liver and removes first 10 amino acids, this yields angiotensin I(no biological activity). ACE removes another 2 amino acids to yield angiotensin II. This increases blood pressure by increasing the amount of salt and water the body retains. Also a vasoconstrictor.side effects---hypotension, cough, hyperkalemia, headache, dizziness, fatigue, nausea, and renal impairment.examples---benazapril,enalapril, lisinopril, quinapril, ramipril,perinopril, captopril

Page 8: Cardiovascularagents

Angiotensin II antagonistsfor patients who don’t tolerate ACE inhibitors.Angiotensin II is allowed to be made but blocked atreceptor site by the drug, yields reduced blood pressure.

side effects----dizziness, headache, and/or hyperkalemia

examples-----losartan, olmesartan, valsartan, irbesartan, eprosartan,telmisartan, candesartan

Page 9: Cardiovascularagents

Nitratesused for angina pectoris----coronary blood flow is inadequate for heart oxygen needs. chest pain with exertion.

moa----nitrates are converted quickly to nitric acid and yields decreased venous return and reduced ventricular pressure, coronary vessel dilation.side effects----orthostatic hypotension, flushing, nitroglygerininhalant is flammable, projection liquid from light.

examples---isosorbide dinitrated/Isodilisosorbide monomitrate/Imdurnitroglygerin/Nitrostat

Page 10: Cardiovascularagents

Vasodilatorsmoa---relax smooth muscle atrerioles, yields decreasedvascular resistance.recommend with diuretics and sympathoplegic drugs.

side effects----headache, naseau, tachycardia, palpitations

examples----minoxidil/Lonitenhydralazine/Apresolinefendolapam/Corlopam

Page 11: Cardiovascularagents

CNS agentsmoa----reduce sympathetic outflow from vasomotor center in the brain, yields reduced heart rate, cardiac output, peripheral resistance.side effects----drowsiness, fatigue, fluid retention

examples----clonodine/Catapresguanfacine/tenexmethyldopa/Aldomet

Page 12: Cardiovascularagents

combination drugs

moa-----additive effect to lower blood pressure.lower dosages yield less side effects

examples------Lotensin/benazepril&HCTZHyzaar/ losartan&HCTZAvalide/irbesartan&HCTZ