CHF Medchem

What is left side heart failure

The left ventricle no longer pumps blood to body

What is ride sided heart failure

The righ ventricle of the heart is too weak to pump blood to the lungs

What is chronic heart failure

Long term develops gradually over time

Occurs when heart is unable to pump blood effectively due to damage or weakness in the heart muscle

What is symptoms of Chronic heart failure

Fluid builds up in the body

It occurs when the heart fails to pump blood adequately

Symptoms of congestive heart failure

Peripheral edema in legs

Pulmonary edema in the lungs

Which drugs are Nonglycosidic positive Inotropic

Milrinone

Dobutamine

What idoes Milrinone Inhibit

PDE3

What is the chemical name of Milrinone

Dihydro bipyridine derivative

What is the ideal torsion angle of Milrinone

21 degrees

Which group on Milrinone causes it to be noncoplanar

The methyl group

What groups must R1, 3 and 6 be in Milrinone

R1= N-CH3

R3= H

R6= H

What is Dobutamine

Synthetic Sympathomimetic amine

How does Dobutamine work

Causes B1 to increase heart contraction and stroke volume leading to increased cardiac output

What other activity does Dobutamine have

Inotropes that is also a dilator because of B2 receptors found in blood vessels and lungs

What is the MOA of Dobutamine

Dobutamine Binds to B1 receptors directly which stimulates CAMP which leads to phosphprylation and calcium channels openign and contraction for more cardiac output

What is the MOA of Milrinone

Inibitis PDE3 which would normally breakdown CAMP so with more CAMP levels there is more contraction and output

True or FAlse Dobutamine is direct while Milrinone is indirect

Trueee

True or False Milrinone is effective in patients with down regulated or desensitized D1 adrenergic response

True

What is ARNI

Angiotensin receptor/Neprilysin Receptor

What is Entresto

Valsartan/Sacubitril

What type of Drug is Sacubitirl

Prodrug and Neprylyssin Inhibitor

What activates Sacubitiril

Esterases

What is the MOA of Sacubitirl

Inhibits Neprylysin which is repsonsible for breaking down Naturietic peptides so by blocking this and increasing naturietic peptides leads to lower BP

What is the MOA of Valsartan

Blocks AT1 receptor of Angiotension 2 which would increase BP and stuff so it blocks that

Which drugs are Vasodilators

Hydralyzine

Potassium Channel opener=Minoxxidil and Diazoxide

Nitric oxide donors

What is the MOA of Vasodilator drugs

Stimulate nitric oxide production causing activation of guanylyl cyclase leading to increased CGMP and interfering with influx of Ca2+ ions

Whats the MOA of Minoxidil

Potassium channel opener that activates ATP sensitive K channel leading to decrease in intracellular Ca2+ hyperpolarization and reduces excitability of vascular smooth muscle

Used for androgenic alopecia

Which drugs are prodrugs of Nitric Oxide

Nitroglycerin

Isosorbide Dinitrate

Isosorbide mononitrate

What should minoxidil not be combined with

Sildenafil

What is the MOA of NO donors

they release Nitric oxide which activates guanylyl cyclase and increases cGMP levels which lowers intracellular calcium leading to muscle relaxation and dilation

What should organic nitrates not be combined with

PDE5 inhibitors because itll cause increased cGMP and marked drop in blood pressure

What does Beta 1 adrenergic receptor activation lead to

Increased heart rate, increased oxygen consumption and eventually heart failure

What is the first beta blocker

Propanolol

Explain the evolution of Propanolol

Started with Isoproterenol to Dichloroisoproterenol to pronethalol to Propanolol

What were the major advances for the creation of Propanolol

Insertion of oxymethylene bridge

Side chain moved from C2 to C1

S configuration

Became an Aryloxy propanolamine

What structure is Labetalol

What structure is Labetalol

Arylethanolamine e

What must the Y substituent be in Beta blockers

Para position and steric bulk group for best selectivity

What is the selectivity order of Y group for beta blockers

Para

meta

ortho

What is X in Beta blockers when its arylethanolamines

Nothing

What is X in beta blockers when Aryloxy propanolamines

Och2

What is optimal stereochemistry for Aryloxy propanolamines

S

What position must amine be in Beta blockers

Secondary

What is the solubility of Propanolol like

Very lipophillic can penetrate the CNS

What is the Beta directing group of Propanolol

isopropyl

What is the aryl group in propanolol

Naphthalene

Is propanolol selective or non selective

Non selective

What is NAdylol

Aryloxy propanoloamine

Non selective

What is Labetalol

Non selective aryl ethanolamines with 2 assymetric centers

What is carvedilol

Non selective aryloxy propanolamines

What is Metopropolo

Selective Aryloxy propanolamines

How does the selectivity change in Metoprolol

Higher doses are not selective

What does a larger substituent on the para position of beta blockers indicate

It is more selective

What is Bisprolol

Selective aryloxy propanolamines

Very selective

What is Atenolol

Selective aryloxypropanolamines

What are Loop diuretics derived from

Sulfamoylamino benzoic acid

What is toresemide and what is it derived from

Loop diuretic from pyridine sulfonylurea derivative

What is the MOA of Loop Diuretics

Block reabsorption of Na ions in TALH by blocking Na/kCL cotransporter

What structural replacement was done in furosemide and Bumetanide

1-sulfomyl replaced by carboxylix acid

What are the potassium sparing diuretics

Spirinolactone

Eplerenone

What is the MOA of Minceralcorticoid Antagonists

Decrease the amount of Na+ and Cl- reabsorbed from the renal tubules leading to diuresis while sparing K+ loss they competively inhibit Aldosterone

What is Spirinolactone

Synthetic analogue of Aldosterone where side chain replaced by spiro 5-membered lactone ring

7-position substituted with acetyl thio

What is Spirinolactone metabolized to

Canrenone by hydrolysis of ester bod

What are the side effects of Spirinolacton

Hyoerkalemia

Gynecomastia

Decreased Libido

Impotence

What is epleperone

Selective aldosterone-receptor antagonists

What contributes to the selectivity of epleperone

C9a and C11a epoxide leading to less antiandrogenic and antiprogesteone effects

What is Ivabradine

Novel heart rate lowering medicine

Benzocyclobutene derivative with S stereochemisty

What is the MOA of Ivabradine

If Channel blockers for angina and heart failure

Reduces spontaneous pacemaker activity of SA node by inhibiting If channel and Hyoerpolarization activated nucleotide-gated channel current to slow heart rate