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TUSHAR MORANKAR, profile picture
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Congestive heart failure (chf) medicinal chemistry

The document discusses congestive heart failure (CHF), detailing its definition, diagnosis methods such as echocardiograms and blood tests, and treatment strategies aimed at improving cardiac output. It covers various drug classifications, including inotropic agents, diuretics, and vasodilators, along with their mechanisms of action. Additionally, it introduces specific medications like digoxin, bosentan, tezosentan, and nesiritide, explaining their roles in managing heart failure.

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Congestive Heart Failure (CHF) 1 Presented By- Morankar. Tushar D. (T.Y.B.Pharm) Guided By- Dr. Ghodage Mangesh G.
Content ▪ Introduction ▪ How Heart Failure Is Diagnosed ▪ Treatment strategies of CHF GOAL ▪ Classification.. ▪ Structure with IUPAC.. ▪ Mechanism of Action… 17-Oct-19 2 Mr.Morankar Tushar D.
Introduction A condition in which the heart is unable to pump sufficient blood to meet the metabolic demand of the body and also unable to receive it back because every time after a systole. 17-Oct-19 3 Mr.Morankar Tushar D.
Diagnosed Echo Chest X-ray ECG Blood tests How Heart Failure Is Diagnosed 17-Oct-19 4 Mr.Morankar Tushar D.
Treatment strategies of CHF GOAL Increase cardiac output Reduce preload and afterload increase myocardial contractility. Inotropic agents β adrenergic agonist β adrenergic antagonist Vasodilators: Ca2+ Channel Blocker Diuretic agents 17-Oct-19 5 Mr.Morankar Tushar D.
Classification.. 1. Inotropic drugs: (a)Cardiac glycosides: Digoxin, Digitoxin (b)Sympathomimetics: Dobutamine, Dopamine (c) Phosphodiesterase III inhibitors: Amrinone 2. Diuretics: (a) High ceiling diuretics: Furosemide, Bumetanide (b) Thiazide like diuretics: Hydrochlorothiazide, Metolazone. 3. Inhibitors of Renin-Angiotensin system- (a) ACE-inhibitors: Enalapril, Ramipril (b) Angiotensin (AT receptor) antagonists: Losartan 4. Aldosterone antagonist- Spironolactone, Eplerenone 5. Vasodilators- (a) Venodilators: Glyceryl trinitrate (b) Arteriolar dilator: Hydralazine (c) Arteriolar + Venodilator: Sod. Nitroprusside IDIA-V 17-Oct-19 6 Mr.Morankar Tushar D.
Mechanism of Action of Digoxin ▪ Inhibition of Na+/K ATPase pimp by Digitalis ▪ Increases Na+ concentration inside the cell ▪ Increases exchanges Na+ for ca++ ▪ Incresed intracellular Ca++ ▪ Incresed influx of Ca++ from sarcoplasmic reticulum ▪ Increases contractility of cardiac muscles. 17-Oct-19 7 Mr.Morankar Tushar D.
Bosentan 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy) -2-(pyrimidin-2- yl)pyrimidin-4-yl]benzene-1-sulfonamide  Bosentan is a competitive antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors.  Under normal conditions, endothelin-1 binding of ET-A receptors causes constriction of the pulmonary blood vessels.  Conversely, binding of endothelin-1 to ET-B receptors has been associated with both vasodilation and vasoconstriction of vascular smooth muscle, depending on the ET-B subtype (ET-B1 or ET-B2) and tissue.  Bosentan blocks both ET-A and ET-B receptors, but is thought to exert a greater effect on ET-A receptors, causing a total decrease in pulmonary vascular resistance 17-Oct-19 9 Mr.Morankar Tushar D.
Mechanism of Action… 17-Oct-19 Normal Endothelin -1 Endothelin -1 Endothelin –A Endothelin -B Vasoconstriction VasoconstrictionVasodilation (Pulmonary Blood Vessels) (Vascular Smooth Muscles) Bosentan Mr.Morankar Tushar D.
Tezosentan N-(2-(2-(2H-tetrazol-5-yl)pyridin-4-yl)-6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy) pyrimidin-4-yl)-5-isopropylpyridine-2-sulfonamide 1 5 3 4 5 6 1 2 3 4 2 62 1 3 4 5 6 2 3 4 5 6 1 2 3 4 5 2  Tezosentan is a non-selective ETA and ETB receptor antagonist.  It acts as a vasodilator and was designed as a therapy for patients with acute heart failure. 17-Oct-19 10 Mr.Morankar Tushar D.
Nesiritide ▪ Nesiritide (Natrecor) is the recombinant form of the 32 amino acid human B-type natriuretic peptide(BNP), which is normally produced by the ventricular myocardium. ▪ Nesiritide works to facilitate cardiovascular fluid homeostasis through counter regulation of the renin–angiotensin–aldosterone system, stimulating cGMP, leading to smooth muscle cell relaxation. Vasodilation NPR-A BNP GTP cGMP ▪ Recombinant human B-type natriuretic peptide (BNP) DiuresisNatriuresis NO 17-Oct-19 11 Mr.Morankar Tushar D.
17-Oct-19 12 Mr.Morankar Tushar D.