Exam 3 Drug MOA Flashcards Preview

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Flashcards in Exam 3 Drug MOA Deck (84)
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1

Spironolactone
and
Eplerenone

Aldosterone Antagonist—> Acts on the RAAS system;
↓ Na+ reabsorption,
↑ Na+, Cl+, H2O excretion;
↓ K+ excretion
↓ decreases myocardial fibrosis

Eplerenone more selective for aldosterone antagonist

2

Captopril
and
Enalapril

Blocks the conversion of Ang I to Ang II;
↓ preload and afterload; Protects heart against adverse remodeling

Captopril is active drug w/ renal excretion
Enalapril is prodrug hydrolyzed in liver, renal and fecal excretion

3

Candesartan
and
Valsartan

Blocks Ang II binding to the AT1 receptor

On arteries —> ↓ vasoconstriction & therefore ↓ AFTERload
On adrenals —> ↓ aldosterone secretion, ↓ Na+ reabsorption —> ↓ PREload

Protects against adverse myocardial remodeling

Valsartan has lower bioavailability

4

Sacubitril/Valsartan (Entresto)

ARNI—> Blocks neprilysin & AT1 to enhance ARB effect

Decreases: BP, sympathetic tone, aldosterone seretion, fibrosis, hypertrophy

Increases: naturesis and diuresis

5

Carvedilol

ARB--> beta (non-specific) and alpha1
Beta effect--> at juxtaglomerular cells ↓ renin secretion, angiotension ii and vasoconstriction --> ↓ AFTERload; ↓ NA+ reabsorption and PREload;
at CNS ↓ BP;
at SA node ↓ HR;
at myocardium ↓ contractility;
at AV node ↓ conduction velocity
*Blocks adverse remodeling*
Alpha1 block contributes to vasoconstriction

6

Ivabradine

Inhibits I(f) channel to ↓ SA node rate

7

Isosorbide Dinitrate

releases NO--> increases cGMP--> ↓ MLC--> vasodilation of veins (↓ preload) > arteries (↓ afterload)

8

Hydralazine

MOA unknown but results in dilated arterioles--> ↓ AFTERload

9

Milrinone

↑ cAMP in heart leads to ↑Ca2+--> ↑contractility--> ↑CO

↑cAMP in artery --> ↑vasodilation--> ↓ AFTERload

10

Digoxin

Inhibits Na+/K+ ATPase which then has effect on Na+/Ca2+ exchanger
results in: Na+ is stuck outside the cell, Ca2+ stuck inside cell, decreased K+ inside cell
1) ↑ myocardium contractility dt increased Ca inside cell
2) ↑ risk of arrhythmias dt decreased K+
3) ↑ vagal tone and ↓ HR and conduction velocity
4) improved CO

11

Metoprolol

Same effects as Carvedilol
except sustained-release and
*Beta-1 specific
Rate control
Give this to asthma and COPD patients over carvedilol

12

Epinephrine

released from adrenal medulla; not very selective
at low doses prefers beta > alpha
at high doses strong preference for Alpha1 and Betas
At Beta 1--> vasodilation, ↑ HR and contractility
At Alpha 1--> vasoconstriction and leads to reflex decrease in HR

13

Norepinephrine

Postganglionic sympathetic neuron binds to alpha and beta receptors;
At presynaptic alpha2 receptors for feedback inhibition of NE release
At Alpha 1--> ↑ BP
At Beta1 that activates Gs--> ↑ Ca2+ into heart and ↑ rate and contractility

14

Isoproterenol

Selective Beta agonist to stimulate heart,
↓ BP
relaxes Bronchi

15

Dopamine

CNS transmitter
↓ BP in renal and mesenteric bends at low dose by beta activation; ↑ BP at high doses by Alpha activation
↑ HR by Beta 1 stimulation

16

Dobutamine

at low doses acts at Beta 1 and some Beta2; at high doses acts at Beta 1 and some Beta 2 and Alpha1
At Beta 1--> ↑ contractility without affecting rate
↑ BP at high doses via Alpha1

17

Phenylephrine

CNS penetration; Alpha 1 stimulator--> ↑ BP

18

Ephedrine

CNS penetration; Alpha 1 stimulator--> ↑ BP

weak Beta agonist

19

Terbutaline

Beta 2 selective; opens airways, inhibits allergic response in anaphylactic shock, relaxes pregnant uterus

20

Albuterol

Beta 2 selective; opens airways, inhibits allergic response in anaphylactic shock, relaxes pregnant uterus

21

Amphetamine

Substrate for NET and kicks out NE leading to increased synaptic NE via Facilitated Exchange Diffusion
CNS penetration

22

Methylphenidate

CNS stimulant that increases NE in front of the brain

23

Phenoxybenzamine

Irreversible selective Alpha 1 blocker

24

Phentolamine

Non-selective alpha Antagonist; Blocks NE from alpha receptor; ↓ BP resulting in reflex tachycardia

25

Propranolol

Non-selective beta Blocker; Blocks NE--> ↓ HR and CO; ↓ conduction velocity, oxygen demand

26

Atenolol

Selective B1 blocker

27

Esmolol

Selective B1 blocker with short half life

28

Timolol

Non-selective Beta blocker used to decrease aqueous humor production for glaucoma

29

Prazosin

Reversible selective Alpha 1 blocker --> ↓ BP resulting in reflex tachy

30

Clonidine

Acts directly at Alpha 2 (agonist)