MOA Flashcards

1
Q

Chloropheniramine

A

Inhibit H1 and cholinergic receptors

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2
Q

Diphenhydramine

A

Inhibit H1 and cholinergic receptors

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3
Q

Dimenhydrinate

A

Inhibit H1 and cholinergic receptors

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4
Q

Loratadine

A

Selective H1 inhibition

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5
Q

Cetirizine

A

Selective H1 inhibition

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6
Q

Fexofenadine

A

Selective H1 inhibition

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7
Q

Cromolyn Sodium

A

directly inhibits mast cell degranulation (ion channel blockers)

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8
Q

Aldosterone

A

Binds to mineralocorticoid receptor

↑Na Channels and Na uptake into the cell

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9
Q

Glucocorticoids

A

↑Annexan A1 (which inhibits PLA2)

↓cytokine synthesis (TNF α )

↓Production of prostaglandin/leukotriene products (Cox 2)

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10
Q

11β-HSD2

A

inactivates cortisol by converting it to cortisone

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11
Q

Omalizumab

A

Binds to FC portion of IgE to block its ability to bind to mast cell

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12
Q

Montelukast

A

leukotriene receptor antagonist inhibits bronchoconstriction

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13
Q

Theophylline

A

Inhibits cAMP phosphodiesterase in smooth muscle

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14
Q

Ipratropropium Bromide

A

Block affects of Ach release from vagus on M3

↓smooth muscle contraction and mucus secretion

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15
Q

Tiotropium

A

Block affects of Ach release from vagus on M3

↓smooth muscle contraction and mucus secretion

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16
Q

Albuterol (SABA)

A

Bind to β2 and prevents Ca from coming in cell to relax smooth muscle causing airways to open
Inhibit release of mast cell mediators

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17
Q

Salmeterol (LABA)

A

Bind to β2 and prevents Ca from coming in cell to relax smooth muscle causing airways to open
Inhibit release of mast cell mediators

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18
Q

Fluticasone

A

Blocks gene transcription (cytokines, chemokines)
↓Inflammatory cells (cytokines)
↑β2 receptors

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19
Q

Prazosin

A

reversible α1 receptor blocker only

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20
Q

Phenoxybenzamine

A

irreversible α1 receptor blocker

somewhat selective over α2

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21
Q

Phentolamine

A

non-selectively blocks α1 and α2

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22
Q

Pindolol

A

↓CO, ↓plasma renin release and ↓ central sympathetic tone

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23
Q

Acebutolol

A

↓CO, ↓plasma renin release and ↓ central sympathetic tone

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24
Q

Propanolol

A

↓CO, ↓plasma renin release and ↓ central sympathetic tone

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25
Q

Timolol

A

β receptors produce aqueous humor so you block and ↓ aqueous humor and ↓IOP

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26
Q

Atenolol

A

↓CO, ↓plasma renin release and ↓ central sympathetic tone

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27
Q

Esmolol

A

↓CO, ↓plasma renin release and ↓ central sympathetic tone

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28
Q

Labetalol

A

Blocks β2α1 in 4:1 rtio

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29
Q

Carvedilol

A

Blocks β2α1 in 10:1 ratio

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30
Q

Clonidine

A

works directly at α2 receptors to
1. Tells enough NE and stops release by acting at presymaptic receptors on postganglionic neurons

  1. ↓Sympathetic outflow in the brain
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31
Q

α-methyldopa

A

must be metabolized to α-methyl-NE to
1. Tells enough NE and stops release by acting at presymaptic receptors on postganglionic neurons

  1. ↓Sympathetic outflow in the brain
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32
Q

Dexmedetomide

A

α2 receptors n locus coeruleus to
1. Tells enough NE and stops release by acting at presymaptic receptors on postganglionic neurons

  1. ↓Sympathetic outflow in the brain
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33
Q

Guanethidine

A

enters via NET and concentrates in vesicle to ↓ NE over time

NE that escapes is metabolized by MAO

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34
Q

Reserpine

A

enters terminal, membrane blocks VMAT causin ↓NE

NE that escapes is metabolized by MAO

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35
Q

Fiber

A

Releases FA that inhibit hepatic FA synthesis

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36
Q

Omega-3 Fatty Acids

A

↑ clearance of TGs

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37
Q

Atrovastatin

A

Direct inhibition of HMG CoA reductase which leads to
↓ cholesterol→
↑ synthesis of hepatic LDL receptors→
↑ LDL clearance

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38
Q

Pravastatin

A

Direct inhibition of HMG CoA reductase which leads to
↓ cholesterol→
↑ synthesis of hepatic LDL receptors→
↑ LDL clearance

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39
Q

Cholestyramine

A

⊕charged so binds to bile acids (cholesterol metabolites) → prevents reabsorption of bile acids → ↑conversion of cholesterol to bile acids→ ↑LDL receptors and ↑LDL clearance from plasma

Can also lead to up regulation of HMG-CoA reductase

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40
Q

Niacin (vit B3)

A

Inhibits lipase and ↓ TG transport to liver→ ↓TG synthesis in liver

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41
Q

Gemfibrozil

A

Agonist for PPAR α receptor (a transcription factor)

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42
Q

Evolocumab

A

blocks degredation of LDL receptor

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43
Q

Nitroglycerin

A

Converted to NO →↑Guanylate cyclase →↑cGMP→dephosphorylates MLC→↓conractile smooth muscles

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44
Q

Verapamil

A

Block influx of Ca→↓contractile state of smooth muscle

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45
Q

Diltazem

A

Block influx of Ca→↓contractile state of smooth muscle

46
Q

Nifedipine

A

Block influx of Ca→↓contractile state of smooth muscle

more potent on vessel than heart

47
Q

Nimodipine

A

Block influx of Ca→↓contractile state of smooth muscle
more potent on vessel than heart
high affinity for cerebral vessels

48
Q

Propanolol

A

Block β1 R on heart→↓HR and ↓contraction due to ↓Calcium influx

Blocks β1 and β2

↓renin secretion→↓Ang II

49
Q

Hydrochlorothiazide

A

block Na Cl pump

↑Na in lumen→depolarizing luminal membrane→↑loss of K

50
Q

Captopril

A

Blocks ACE which blocks conversion of Ang I → Ang II (normally causes vasoconstriction)

51
Q

Losartan

A

Block pathway at receptor level AT1

52
Q

Hydralazine

A

Vasodilate arterial smooth muscle → baroreceptor reflex response

53
Q

Minoxidil

A

Vasodilate arterial smooth muscle → baroreceptor reflex response

54
Q

Sodium Nitroprusside

A

Vasodilate arterial smooth muscle → baroreceptor reflex response

55
Q

Prazosin

A

Blocks binding of NE to to α1 receptors

56
Q

Guanethidine

A

Transported into vesicles and replace NE and blocks exicatation secretion coupling at Post ganglionic peripheral nerurons

57
Q

Reserpine

A

Binds to storage vesicles and inhibits transmitter uptake→dysfunctional vesicles bc depletion of NE at Central and peripheral vesicles

58
Q

Methyldopa

A

↓sympathetic activity→vasoconstriction

59
Q

Clonidine

A

↓sympathetic activity→vasoconstriction

60
Q

Effect of nitroglycerin on the body

A

Vasodilates
Dilates large epicardial arteries →↓coronary steal→↓LV pressure
↓Preload
↓Wall tension

61
Q

Effect of Calcium Channel Blockers on the body

A

↓contractility

62
Q

Effect of Dihydropyridine Calcium Channel Blockers on the body

A

More coronary and peripheral vasodilation than non-dihydros
↓BP
↑HR
↑Contractility

63
Q

Effect of Propanolol on the body

A

↓HR
↓contraction

↑Preload and tension (might want to use in combo w/ ↓preload)

64
Q

Effect of Hydrochlorothiazide on the body

A

↓preload and blood volume

65
Q

Effect of Captopril on the body

A

vasodilation

↓preload and blood volume

↓LV hypertrophy

66
Q

Effect of Losartan on the body

A

↓preload and blood volume

67
Q

Effect of α2 Agonists on the body

A

Vasoconstriction
↓Sympathetic Activity
↓BP

68
Q

Lidocaine

A

Block Na channels→ ↑ERP
Inc K+ out→ ↓ AP
Selective for sick cells

69
Q

Mexiletine

A

Block Na channels→ ↑ERP
Inc K+ out→ ↓ AP
Selective for sick cells

70
Q

Flecainide

A

Selectively Na channel blocker→ ↑ERP

Inc K+ out→ ↓ AP

71
Q

Quinidine

A

Blocks Na channels in normal cells → ↑ERP

Anticholinergic ↓vagal influences

72
Q

Procainamide

A

Blocks Na channels in normal cells → ↑ERP

Anticholinergic ↓vagal influences

73
Q

Disopyramide

A

Blocks Na channels in normal cells → ↑ERP

Anticholinergic ↓vagal influences

74
Q

Amiodarone

A

Blocks K+ efflux → ↑APD and ↑QT

Blocks Na channels→ ↑ERP

75
Q

Dronedarone

A

Blocks K+ efflux → ↑APD and ↑QT

Blocks Na channels→ ↑ERP

76
Q

Sotalol

A

Blocks K+ efflux → ↑APD and ↑QT

Blocks Na channels→ ↑ERP

77
Q

Ibutalide

A

Blocks K+ efflux → ↑APD and ↑QT

Blocks Na channels→ ↑ERP

78
Q

Verapamil

A

L type Ca channel blockade
↓SA and AV node conduction
↓ contractility

79
Q

Diltiazem

A

L type Ca channel blockade
↓SA and AV node conduction
↓ contractility

80
Q

Metoprolol

A

↓AV node conduction
↓excitability
↓SA node rate
↓contractility

81
Q

Digoxin

A

Inhibits Na+/K+ ATPase→
↓resting mem potential
↓conduction velocity

↑vagal activity→ ↓recractory period and ↓conduction in AV node

82
Q

Adenosine

A

↑K+ efflux and hyperpolarizes cell→ ↓ability for Ca to enter→ ↓AV node conduction and ↓automaticity

83
Q

Alcohol

A

↑GABA binding at inhibitory GABAaR
↓Glutamate activation of excitatory NMDAR

Facilitate release of endogenous opioids in VTA

84
Q

Barbiturates

A

↑GABA binding at inhibitory GABAaR

Can directly open GABAa at high concentrations

85
Q

Benzodiazepines

A

↑GABA binding at inhibitory GABAaR

Abuse w/ faster acting BZ (alprazolam, diazepam)

86
Q

Heroin/Opioids

A

Activity mu-opioid receptor

87
Q

Nicotine

A

Nicotine stimulates nAchRs in reward pathway

88
Q

Marijuana, hashish, oils

A

THC binds to cannabinoid receptors (GPCR) and activates the reward pthwy

89
Q

Amphetamines
and
Methamphetamine

A

↑ DA and NE release and block MAO

90
Q

Cocaine

A

Blocks reuptake of NA so ↓ NE and serotonin

91
Q

Psychedelics related to serotonin

LSD, Psilocybin, DMT

A

Agonist at 5HTR, DA receptors and adrengeric receptors

92
Q

Psychedelics related to dopamine and aphetamines

MDA, MDMA, mescaline

A

Induce 5HT and DA release
5HT reuptke inhibitor
Agonist at 5HT, DA & adrenergic receptor

93
Q

Dissociatives

PCP, ketamine

A

Inhibit glutamatergic NMDA receptors

94
Q

Acetazolamide

A

CAH inhibitor→↓HCO3⁻ in → ↓ Na⁺ resoprtion→ ↑ luminal Na⁺ concentration (which will retain water and Cl⁻)
↓ H⁺ in

Secondary: ↑tubular Na⁺→TGF activation → ↓GFR

95
Q

Osmotic diuretics

A

↑ conc in tubule that cant be resorbed so holds onto more water

↑plasma osmolality, ↑ECFV→ ↑ RBF & ↓ osmotic gradient

96
Q

Na⁺/K⁺/2Cl⁻ Blockers (Loop diuretics)

A

↓ Na⁺/K⁺/2Cl⁻ Symporter → ↓ osmotic gradient

Changes in macula densa sensing of Na is duiretic braking

97
Q

Na⁺/Cl⁻ Blockers (Thiazide diuretics)

A

Inhibits Na⁺/Cl⁻ cotransporter

98
Q

ENaC Inhibitors

A

Block ENaC → ↓ Na resoprtion and ↓ K backleak & excretion

99
Q

Aldosterone Antagonists

A

Prevents aldosterone & blocks production of ENaC channel, Na/K ATPase and K channel→ ↑Na resportion→ ↑K+ excretion

100
Q

Vasopressin (ADH) Antagonists

A

Block V2 receptor → block aquaporins→ ↓ water resorption

101
Q

Captopril

A

Block conversion of ang I to ang II → ↓ preload by ↓ vasoconstriction

↓aldosterone stimulation → ↓ preload

102
Q

Enalapril

A

Block conversion of ang I to ang II → ↓ preload by ↓ vasoconstriction

↓aldosterone stimulation → ↓ preload

103
Q

ARBs

A

Blocks after ang II so no cough but still ↓afterload by ↓ vasoconstriction

104
Q

Ivabradine

A

↓ HR

Blocks Na funny current in SA node which determines HR and ↓ leak

105
Q

Isosorbide

A

Releases organic nitrates→release of NO→ ↑cGMP→ uphosphorylated Myosin LC→ vasodilation

106
Q

Dinitrate/hydralazine

A

Dilates arterioles → ↓ afterload

107
Q

Ivabradine

A

↓ HR

Blocks Na funny current in SA node which determines HR and ↓ leak

108
Q

Isosorbide

A

Releases organic nitrates→release of NO→ ↑cGMP→ uphosphorylated Myosin LC→ vasodilation

109
Q

Dinitrate/hydralazine

A

Dilates arterioles → ↓ afterload

110
Q

Milirinone

A

Myocardium: Blocks cAMP destruction → ↑ Ca⁺⁺ levels → ↑ contraction

Also affects arterioles → MLCK inactivated → relaxation→ ↓ afterload

111
Q

Digoxin

A

Blocks Na⁺/K⁺ ATPase → ↓ Na⁺ outside the cell → ↓ driving force → ↑ Ca⁺⁺ inside cell → ↑ contractility