Exam 3 Drug MOA

Question 1

Spironolactone
and
Eplerenone

Answer 1

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

Eplerenone more selective for aldosterone antagonist

Question 2

Captopril
and
Enalapril

Answer 2

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

Question 3

Candesartan
and
Valsartan

Answer 3

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

Question 4

Sacubitril/Valsartan (Entresto)

Answer 4

ARNI—> Blocks neprilysin & AT1 to enhance ARB effect

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

Increases: naturesis and diuresis

Question 5

Carvedilol

Answer 5

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

Question 6

Ivabradine

Answer 6

Inhibits I(f) channel to ↓ SA node rate

Question 7

Isosorbide Dinitrate

Answer 7

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

Question 8

Hydralazine

Answer 8

MOA unknown but results in dilated arterioles–> ↓ AFTERload

Question 9

Milrinone

Answer 9

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

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

Question 10

Digoxin

Answer 10

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

Question 11

Metoprolol

Answer 11

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

Question 12

Epinephrine

Answer 12

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

Question 13

Norepinephrine

Answer 13

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

Question 14

Isoproterenol

Answer 14

Selective Beta agonist to stimulate heart,
↓ BP
relaxes Bronchi

Question 15

Dopamine

Answer 15

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

Question 16

Dobutamine

Answer 16

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

Question 17

Phenylephrine

Answer 17

CNS penetration; Alpha 1 stimulator–> ↑ BP

Question 18

Ephedrine

Answer 18

CNS penetration; Alpha 1 stimulator–> ↑ BP

weak Beta agonist

Question 19

Terbutaline

Answer 19

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

Question 20

Albuterol

Answer 20

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

Question 21

Amphetamine

Answer 21

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

Question 22

Methylphenidate

Answer 22

CNS stimulant that increases NE in front of the brain

Question 23

Phenoxybenzamine

Answer 23

Irreversible selective Alpha 1 blocker

Question 24

Phentolamine

Answer 24

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

Question 25

Propranolol

Answer 25

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

Question 26

Atenolol

Answer 26

Selective B1 blocker

Question 27

Esmolol

Answer 27

Selective B1 blocker with short half life

Question 28

Timolol

Answer 28

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

Question 29

Prazosin

Answer 29

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

Question 30

Clonidine

Answer 30

Acts directly at Alpha 2 (agonist)

Question 31

Methyldopa

Answer 31

must be metabolized to alpha-methyl-NE to become alpha 2 agonist

Question 32

Fiber

Answer 32

Slows cholesterol and bile acid absorption and facilitates excretion Increases GI motility

Question 33

Omega-3 Fatty Acids

Answer 33

↑ TG clearance, ↓ Lipogenesis, ↑ beta-oxidation, ↓ VLDL Anti-inflammatory

Question 34

Atorvastatin

Answer 34

Inhibits HMG CoA Reductase--> ↓cholesterol synthesis--> ↑ synthesis of hepatic LDL receptors --> ↑ LDL and VLDL remnant clearance metabolized by CYP3A4

Question 35

Pravastatin

Answer 35

Inhibits HMG CoA Reductase--> ↓cholesterol synthesis--> ↑ synthesis of hepatic LDL receptors --> ↑ LDL and VLDL remnant clearance metabolized by sulfation and is NOT P450 dependent

Question 36

Ezetimibe

Answer 36

Blocks absorption of cholesterol from intestinal track by inhibiting Niemann-Pick C1-like 1--> ↓ delivery of intestinal cholesterol to liver which ↓ choelsterol in chylomicrons/remnants all leads to ↑ LDL receptors and ↑ LDL clearance

Question 37

Ezetimibe

Answer 37

Blocks absorption of cholesterol from intestinal track by inhibiting Niemann-Pick C1-like 1--> ↓ delivery of intestinal cholesterol to liver which ↓ choelsterol in chylomicrons/remnants all leads to ↑ LDL receptors and ↑ LDL clearance

Question 38

Cholestyramine

Answer 38

Binds bild, metabolites of cholesterol--> prevents reabsorption and promotes excretion--> ↑ conversion of cholesterol into bile acids --> ↑ LDL receptors and LDL clearance

Question 39

Niacin

Answer 39

Poorly understood mechanism inhibits lipase in adipose tissue and ↓ free fatty acids transport--> ↓ VLDL synthesis--> ↓ LDL production ↓ TG synthesis ↓ HDL catabolism --> ↑HDL levels

Question 40

Gemfibrozil

Answer 40

PPAR-alpha receptor agonist--> ↓ TGs

Question 41

Cholestyramine

Answer 41

Binds bild, metabolites of cholesterol--> prevents reabsorption and promotes excretion--> ↑ conversion of cholesterol into bile acids --> ↑ LDL receptors and LDL clearance

Question 42

Niacin

Answer 42

Poorly understood mechanism inhibits lipase in adipose tissue and ↓ free fatty acids transport--> ↓ VLDL synthesis--> ↓ LDL production ↓ TG synthesis ↓ HDL catabolism --> ↑HDL levels

Question 43

Gemfibrozil

Answer 43

PPAR-alpha receptor agonist--> ↓ TGs

Question 44

Evolocumab

Answer 44

Inhibit PCSK9 in order to upregulate the LDL receptor --> increase LDL clearance

Question 45

Lidocaine | and Mexiletine

Answer 45

Class 1B, Just VT, Blocks Na+ channels (primarily in depol cells) --> ↑ ERP increase K+ out--> ↓ AP duration

Question 46

Flecainide

Answer 46

Class 1C, VT>SVT, rhythm control, Na+

Question 47

Quinidine

Answer 47

Class 1A, VT>SVT, rhythm control, long QT

Question 48

Procainamide and Disopyramide

Answer 48

Class 1A, VT>SVT, rhythm control, long QT

Question 49

Lidocaine | and Mexiletine

Answer 49

Class 1B, Just VT, Blocks Na+ channels (primarily in depol cells) --> ↑ ERP increase K+ out--> ↓ AP duration

Question 50

Flecainide

Answer 50

Class 1C, VT>SVT rhythm control Blocks Na+ channels--> ↑ refractory period

Question 51

Quinidine

Answer 51

Class 1A, VT>SVT rhythm control Blocks Na+ channels, Blocks TEA-type K+ channel--> ↑ refractory period

Question 52

Procainamide and Disopyramide

Answer 52

Class 1A, VT>SVT rhythm control Blocks Na+ channels, Blocks TEA-type K+ channel--> ↑ refractory period

Question 53

Amiodarone

Answer 53

``` Class III, VT & SVT, rhythm control Blocks K+ efflux, ↑ AP duration Blocks Na+ channels, ↑ refractory period Blocks Ca2+ channels Blocks beta receptors ```

Question 54

Sotalol and Ibutalide

Answer 54

Class III, VT & SVT, rhythm control Blocks K+ efflux, ↑ AP duration

Question 55

Verapamil and Diltiazem

Answer 55

Class IV, SVT only (fibrillation and flutter), rate control | Ca2+ channel blocker, slows SA and AV node conduction. ↓automaticity

Question 56

Metoprolol

Answer 56

Class II, SVT only, rate control | Beta blocker--> ↓ AV node conduction, ↓excitability, ↓ SA node rate, ↓contractility

Question 57

Digozin

Answer 57

used for SVT only rate control Inhibits Na+/K+ ATPase--> ↓ resting potential, ↓ conduction velocity indirect: ↑ vagal activity--> ↑ refractory period, ↓ conduction in AV node

Question 58

Adenosine

Answer 58

Increases K+ eflux--> hyperpolarizes--> ↓ Ca2+--> ↓ AV node conduction, ↓ SA pacemaker, ↓automaticity

Question 59

Ethanol

Answer 59

CNS depressant, enhances GABA binding to GABA-A Inhibits glutamate binding to NMDA facilitates release of endogenous opiods in VTA

Question 60

Benzodiazepines

Answer 60

CNS depressant, enhances GABA binding to GABA-A

Question 61

Barbiturates

Answer 61

CNS depressant, GABA binding and directly activate GABA-A

Question 62

Opioids

Answer 62

Activation of mu opioid receptor reward pathway

Question 63

Nicotine

Answer 63

Activation of nicotinic acetylcholine receptors in reward pathway

Question 64

Cannabinoids (THC)

Answer 64

Activation of cannabinoid receptors in reward pathway

Question 65

Stimulants (cocaine, amphetamine, methamphetamine)

Answer 65

Amphetamine and Methamphetamine enhance synaptic release of DA Cocaine blocks reuptake of DA

Question 66

LSD and psilocybin

Answer 66

Act as agonists at DA receptors- weak effects in reward pathway

Question 67

MDMA or ecstasy

Answer 67

Induce DA release; act as agonists at DA receptors- weak effects

Question 68

Dissociatives (PCP, ketamine)

Answer 68

Inhibit NMDA receptors in reward pathway

Question 69

Disulfiram

Answer 69

Inhibits acetaldehyde dehydrogenase, leading to accumulation of acetaldehyde upon alcohol consumption. Acetylaldehyde causes facial flushing, nausea, headache, vomiting, hypotension

Question 70

Acamprosate, Topiramate

Answer 70

Anti-craving mechanism unknown; known to increase activity of GABA-A receptors and inhibit glutamatergic NMDA receptor activity

Question 71

Naloxone (Narcan)

Answer 71

Inhibits mu opioid receptors in ventral tegmental (VTA) of brain; short acting antagonist

Question 72

Naltrexone

Answer 72

Inhibits mu opioid receptors in VTA of brain; long acting antagonist

Question 73

Methadone

Answer 73

High efficacy agonist at mu opioid and receptor suppresses symptoms of craving and withdrawal produces plasma opioid levels that remain stable over time

Question 74

LAAM

Answer 74

High efficacy agonist at mu opioid and receptor suppresses symptoms of craving and withdrawal produces plasma opioid levels that remain stable over time

Question 75

Buprenorphine

Answer 75

Partial agonist at mu opioid receptor and antagonist at kappa opioid receptor

Question 76

Nicotine replacement therapy

Answer 76

different kinetics from smoking; slower absorption and longer nicotine plasma levels, therefore less rewarding, alleviates craving and less frequent withdrawal symptoms

Question 77

Bupropion

Answer 77

Antidepressant; unknown MOA; non-competitive antogonist of nicotinic acetylcholine receptors in reward pathway; weak inhibitor of DA, NE and 5HT reuptake in reward pathway

Question 78

Varenicline

Answer 78

Partial agonist at alpha4beta2 nicotinic acetylcholine receptors (nAChRs) in ventral tegmental area (VTA) and nucleus accumbens region of brain Inhibits nicotine full agonist activation at nAChRs

Question 79

Diphenhydramine

Answer 79

H1 Antihistamine; Competitive antagonist to histamine's effects on smooth muscles "inverse agonist"; penetrate the BBB

Question 80

Diphenhydramine (Benadryl)

Answer 80

H1 Antihistamine; Competitive antagonist to histamine's effects on smooth muscles "inverse agonist"; penetrate the BBB

Question 81

Dimenhydrinate (Dramamine)

Answer 81

H1 Antihistamine Competitive antagonist to histamine's effects on smooth muscles "inverse agonist", Penetrate the BBB

Question 82

Loratadine (Claritin)

Answer 82

Second Generation H1 Antihistamine; Competitive antagonist to histamine's effects on smooth muscles "inverse agonist; Little BBB

Question 83

Cetirizine (zyrtec)

Answer 83

Second Generation H1 Antihistamine; Competitive antagonist to histamine's effects on smooth muscles "inverse agonist; Little BBB

Question 84

Fexofenadine (Allegra)

Answer 84

Second Generation H1 Antihistamine; Competitive antagonist to histamine's effects on smooth muscles "inverse agonist; Little BBB