Cardiovascular system Drugs - HEART FAILURE (Chapter 1 / 7)

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 HEART FAILURE

HF=complex, progressive disorder in which the heart is unable to pump sufficient blood to meet the needs of the body.

Symptoms; Dyspnea, Fatigue, Fluid retention.

Also called” Congestive Heart failure (C.H.F)

Action Potential=

Phase 0:Fast Upstroke:

Na+ channels open (fast channel) resulting in afast inward current ……Sodium current is blocked by Quinidine

Phase l: Repolarization:

inactivation of Na+ channel…K+ channels rapidly open & close…outward current

Phase ll: Plateau:

Voltage sensitive Ca++ channels open…Slow inward current(depolarizing)…. Slow outward current (Polarizing) leak of K+

Phase lll: Repolarization

Ca++ channels close…K+ channels open…outward current lead to repolarization… net gain of Na+ & Loss of K+….corrected by Na+/K+-ATPase

Phase lV: Forward Current

Increase depolarization from gradual increase in sodium….bring the cell to Threshold of next action potential.

Cardiovascular drugs heart failure and mcqs interview important points for revision

Angiotensin-Converting Enzyme Inhibitor

Angiotensinogen (α2-globulin in blood)…Renin (in kidney) acton Angiotensinogen & convert into Angiotensin l(inactive)…ACE convert Angiotensin into Angiotensin ll…

MOA=ACEI inhbit ACE and block conversion of Angiotensin l into Angiotensin ll….leads to increase Vasodilation…Decreased output of sympathetic nervous system..

Decrease ALDOSTERONE secretion…decrease retention of Na+ & H2O..

ACEI ϴ degradation of BRADYKININ….Increase level of Bradykinin….vasodilation occur


Actions= decrease PRELOAD & increase AFTERLOAD…increase cardiac output..

T.E= DOC in Left Ventricular Failure & Lowest Ejection Fraction

P.K= food decreases their Absorption…Except for CAPTOPRIL, all are prodrugs…..

Fosinopril only eliminate through Feces, O.D administer

S.E= Hyperkalemia, Dry cough (due to increase level of Bradykinin) , Angioedema,Hypotension, Renal insufficiency

Angiotensin Receptor Blocker

Non-peptide…orally active..Losartan is Prototype..Candesartan have large Vd..

MOA= competitive Antagonist of Angiotensin receptor type 1…complete blockade of Angiotensin action

S.E=same to ACEI...do not produce Cough...Contraindicated in Pregnancy

 β-Blocker

-Ve ionotropic effect, increase systolic functioning …reverse cardiac remodeling...prevent the changes produced by Sympathetic nervous sys..decrease heart rate & inhibition of Renin..

Carvedilol and Metoprolol= mostly used

Diuretics

Relieve Pulmonary congestion and Peripheral edema… reducing Volume Overload & Venous return…decrease O2 demand…Loop Diuretics mostly used

Direct Vasodilator

Dilation of Venous blood vessels…decrease cardiac preload & increase Venous Capacitance

Dilation of Arterials vessels reduce arteriolar resistance & afterload

Nitrates common vasodilator decrease Preload…Hydralazine reduce Afterload

Ca++ channel blocker should be avoided

Inotropic Drugs

+Ve inotropic agentsenhance Cardiac muscle contractility…increase cardiac output…

Digoxin= obtained from Digitalis Glycoside (Foxglove)…..low therapeutic index

MOA= inhibit Na+/K+ exchange by Na+/K+ ATPase….conc. of intracellular Na+ increases..Conc. gradient across the memb decreases… inceased Na+ conc. 

Decreases driving force Na+/Ca++ exchanger…decrease extrusion of Ca++ into extracellular space 

more Ca++ inside the cell for contractility 

Increases Force of contraction increase cardiac output..decrease end-diastolic Volume.. 

increase efficiency of contraction(Ejection-fraction)…improved circulation

T.E= Pt. with Left Ventricular Systolic Dysfunction & HF with atrial Fibrillation….do not indicated in Pt. with Diastolic or Right sided HF…

Dobutamine another Inotropic agent , available as Direct Intra Cardiac inj. 

P.K=t1/2 of Digoxin 36hr, large Vd, accumulate in Muscle…Dosage based on Lean Body Weight…

S.E= decrease COLOR PERCEPTION...Halos on Dark objects...HYPOKALEMIA. 

PhosphoDiesterase Inhibitor= Milrinone & Amrinone inhibit Phosphodiesterase.. 

increase cAMP…increase Ca++… increase cardiac contractility..

Aldosterone Antagonists 

Spiranolactone= direct Antagonist of Aldosterone..prevent salt retention, Myocardial  hypertrophy and Hypokalemia…

Eplerenone= competitive Antagonist of Aldosterone at Mineralocorticoid receptor…

Cardiovascular drugs mcqs screening point and test interview



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