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phcy 503 > Exam 1 Drugs > Flashcards

Exam 1 Drugs Flashcards

1
Q

aspirin drug class

A

antiplatelet agent, salicylates, NSAID

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2
Q

aspirin indication

A

secondary prevention after acute coronary syndrome

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3
Q

aspirin drug target

A

cyclooxygenase 1 enzyme (COX-1)

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4
Q

aspirin target family and location

A

oxioreductase enzyme in platelets

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5
Q

aspirin target normal role

A

COX-1 catalyzes the conversion of arachidonic acid to PGH2, in platelets PGH2 is the converted to TxA2, which is an autocrine and paracrine activator of platelet aggregation during hemostasis

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6
Q

aspirin pharmacologic activity

A

Irreversible, competitive inhibitor

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7
Q

aspirin MOA

A

aspirin irreversibly inhibits COX-1 enzyme to reduce formation of TxA2, thus blocking platelets aggregation and decreasing thrombus formation that could lead to ASCVD progression or a related CV event

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8
Q

clopidogrel brand name

A

Plavix

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9
Q

clopidogrel drug class

A

antiplatelet agent, thienopyridine

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10
Q

clopidogrel indication

A

Heart disease

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11
Q

clopidogrel target

A

P2Y12 receptor

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12
Q

clopidogrel target family and location

A

GPCR on platelets

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13
Q

clopidogrel target normal role

A

P2Y12R are activated by ADP and signal via Gi to activate the fibrinogen receptor (integrin alpha IIb-beta IIIa) that mediates the activation and aggreegation of platelets. this extends and stabilizes the initial platelet adhesion that leads to platelet aggregation, this is a necessary event in the formation of blood clots

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14
Q

clopidogrel pharmocologic activity

A

Irreversible, orthosteric antagonist

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15
Q

clopidogrel MOA

A

the active metabolite irreversibly blocks P2Y12R, preventing fibrinogen receptor activation and reducing platelet aggregation. this decreases thrombus formation that could lead to an ACS event

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16
Q

prasugrel brand name

A

Effient

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17
Q

prasugrel drug class

A

antiplatelet agent, thienopyridine

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18
Q

prasugrel indication

A

heart disease

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19
Q

prasugrel drug target

A

P2Y12R

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20
Q

prasugrel target family and location

A

GPCR on platelets

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21
Q

prasugrel target normal role

A

P2Y12 R are activated by ADP and signal via Gi to activate fibrinogen receptor (alpha IIb-beta IIIa) that mediates the activation and aggregation of platelets. this extends and stabilizes the initial platelet adhesion that leads to platelet aggregation. a necessary event in hemostatic blood clot formation.

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22
Q

prasugrel pharmacologic activity

A

irreversible, orthosteric antagonist

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23
Q

prasugrel MOA

A

the active metabolite irreversibly blocks P2Y12R, thereby preventing fibrinogen receptor activation and reducing platelet aggregation. this decreases thrombus formation that could lead to ACS event

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24
Q

losartan brand name

A

Cozaar

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25
Q

losartan drug class

A

ARB blocker, antihypertensive

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26
Q

losartan indication

A

hypertension management

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27
Q

losartan drug target

A

angiotensin II type 1 receptor (AT1R)

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28
Q

losartan drug family and location

A

GPCR on vascular smooth muscle

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29
Q

losartan target normal role

A

binding of angiotensin II type 1 to AT1R on SMC is signaled via Gq, resulting in increased intracellular Ca concentration to stimulate MLCK dependent cellular cantraction that results in vasoconstriction and increased blood pressure

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30
Q

losartan pharmacologic activity

A

reversible, orthosteric antagonist

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31
Q

losartan MOA

A

selectively blocks the activation of AT1R by angiotensin II, blocking the vasocinstrictor and aldosterone secreting effects to reduce elevated blood pressure in the treatment of hypertension

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32
Q

olmesartan brand name

A

Benicar

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33
Q

olmesartan drug class

A

ARB, antihypertensive

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34
Q

olmesartan indication

A

management of hypertension

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35
Q

olmesartan drug target

A

angiotensin II type 1 receptors

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36
Q

olmesartan target family and location

A

GPCR on vascular smooth muscle

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37
Q

olmesartan target normal role

A

binding of angiotensin II to AT1R is signaled via Gq, resulting in intracellular Ca concentration to stimulate MLCK dependent cellular contraction that results in vasoconstriction and increased blood pressure

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38
Q

olmesartan pharmacologic activity

A

reversible, orthosteric antagonist

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39
Q

olmesartan MOA

A

selectively blocks activation of AT1R by angiotensin II, therefore, blocking its vasoconstrictor and aldosterone secreting effects to reduce elevated blood pressure in the treatment of hypertension

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40
Q

valsartan brand name

A

Diovan

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41
Q

valsartan drug class

A

ARB, antihypertensive

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42
Q

valsartan indication

A

management of hypertension

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43
Q

valsartan drug target

A

angiotensin II type 1 receptor

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44
Q

valsartan target family and location

A

GPCR on SMC

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45
Q

valsartan target normal role

A

binding of angiotensin II to AT1 receptor on SMC is signaled via Gq, leading to an increase in Ca concentration leading to MLCK dependent cellular contraction that results in vasoconstriction and increased blood pressure

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46
Q

valsartan pharmacologic activity

A

reversible orthosteric antagonist

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47
Q

valsartan MOA

A

selectively block activation of AT1R activation by angiotensin II, thereby blocking its vasoconstrictor and aldosterone secreting effect to reduce blood pressure in the treatment of hypertension

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48
Q

benazepril brand name

A

Lotensin

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49
Q

benazepril drug class

A

ACE-I, antihypertensive

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50
Q

benazepril indication

A

hypertension

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51
Q

benazepril drug target

A

angiotensin converting enzyme (ACE)

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52
Q

benazepril target family and location

A

peptidase on surface of endothelial cells in kidney and lungs

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53
Q

benazepril target normal role

A

as part of RAAS, ACE converts angiotensin I to angiotensin II, which activates AT1R which results in vasoconstriction and aldosterone release, and sodium retention. ACE also degrades bradykinin into inactive peptides inhibiting nociception.

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54
Q

benazepril pharmacologic activity

A

reversible competitive inhibitor

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55
Q

benazepril MOA

A

blocks the production of angiotensin II, thereby activation of AT1 receptor and reducing angiotensin II vasoconstriction and aldosterone secreting effects to reduce elevated blood pressure in the treatment of hypertension

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56
Q

enalapril brand name

A

Vasotec

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57
Q

enalapril drug class

A

ACE-I, antihypertensive

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58
Q

enalapril indication

A

hypertension

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59
Q

enalapril drug target

A

angiotensin converting enzyme

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60
Q

enalapril target family and location

A

peptidase on surface of endothelial cells in kidney and lungs

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61
Q

enalapril target normal role

A

as part of RAAS, ACE converts angiotensin I to angiotensin II, which activates AT1 receptor, and results in vasoconstriction and aldosterone secretion and sodium retention, ACE also degrades bradykinin into inactive peptides, inhibiting nociception

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62
Q

enalapril pharmacologic activity

A

reversible, competitive inhibitor

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63
Q

enalapril MOA

A

blocks the production of angiotensin II, thereby preventing the activation of AT1R, therefore, reducing angiotensin II vasoconstrictor and aldosterone secreting effects to reduce blood pressure in the treatment of hypertension

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64
Q

lisinopril brand name and drug class

A

Zestril/Prinivil

ACE-I

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65
Q

ramipril brand name and drug target

A

Altace

ACE-I

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66
Q

clonidine brand name

A

Catapres

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67
Q

clonidine drug class

A

alpha-2 adrenergic receptor agonist, antihypertensive

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68
Q

clonidine indication

A

manage management of hypertension

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69
Q

clonidine drug target

A

alpha 2 adrenergic receptor

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70
Q

clonidine target family

A

GPCR on post synaptic CNS neurons

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71
Q

clonidine target normal role

A

NE binding to post synaptic alpha 2 Rs on select sympathetic neurons is signaled via Gi to activate ATP sensitive K channels, hyperpolarize the target neuron, and attenuate further neurotransmission

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72
Q

clonidine pharmacologic activiry

A

agonist

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73
Q

clonidine MOA

A

activates alpha-2 AR, resulting in hyperpolarization of key neurons in the medulla and decreased sympathetic outflow from the CNS, thereby producing a decrease in peripheral vascular resistance, HR, and BP

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74
Q

doxazosin brand name

A

Cardura

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75
Q

doxazosin drug class

A

alpha 1 blocker, antihypertensive

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76
Q

doxazosin indication

A

hypertension, BPH

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77
Q

doxazosin drug target

A

alpha-1 AR

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78
Q

doxazosin target family and location

A

GPCR on SMCs of peripheral vasculature and bladder sphicter

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79
Q

doxazosin target normal role

A

binding of NE to alpha-1 ARs on SMC of peripheral vasculature is signaled via Gq, resulting in increased intracellular Ca concentration to stimulate MLCK dependent cellular contraction that results in vasoconstriction and increased blood pressure

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80
Q

doxazosin pharmacologic activity

A

reversible, orthosteric antagonist

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81
Q

doxazosin MOA

A

blocks sympathetic activation of alpha-1 AR by NE, thereby relaxing vasoconstriction to reduce elevated blood pressure in the treatment of hypertension

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82
Q

propranolol brand name

A

Inderal LA

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83
Q

propanolol drug class

A

beta blocker, nonselective, antihypertensive

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84
Q

propranolol indication

A

hypertension

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85
Q

propanolol drug target

A

beta-1 and beta-2 ARs

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86
Q

propranolol target family and location

A

GPCRs on cardiomyocytes and bronchiolar SMCs

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87
Q

propranolol target normal role

A

beta beta 1 and 2 ARs are GPCRs coupled to Gs. normally, activation by NE in heart or Epi in lunc increases cAMP concentration, activates PKA, increases Ca permeability. In cardiomyocytes, this activates troponin C and the actin-myosin system, leading to increased HR (chronotopy) and force of contraction (ionotropy). In bronchiolar SMCs, this deactivates MLCK and myosin, leading to SMC relaxation and bronchodilation.

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88
Q

atenolol brand name

A

Tenormin

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89
Q

atenolol drug class

A

selective beta-1 blocker, antihypertensive

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90
Q

atenolol indication

A

hypertension

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91
Q

atenolol drug target

A

beta-1 AR

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92
Q

atenolol target family and location

A

GPCR on cardiomyocytes

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93
Q

atenolol target normal role

A

NE secreted by sympathetic neuron activates beta-1 receptors, the signal is transferred via Gs, which increases cAMP concentration, activates PKA, increases Ca premeability, activates troponin C, and activates actin myosin system in the heart muscle, leading to increased heart rate and force of contraction (ionotropy)

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94
Q

atenolol pharmacologic activity

A

reversible, orthosteric antagonist

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95
Q

atenolol MOA

A

selectively blocks beta-1 AR activation by NE or Epi, thereby reducing heart rate and stroke volume that lead to hypertension

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96
Q

metroprolol brand name and drug class (explain other parts too)

A

Lopressor, Toprol XL
Beta-1 selective blocker,
antihypertensive

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97
Q

nebivolol brand name and drug class (explain other parts too)

A

Bystolic

beta-1 selective blocker, antihypertensive

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98
Q

carvedilol brand name

A

Coreg

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99
Q

carvedilol drug class

A

beta blocker with alpha blocking activity, antihypertensive

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100
Q

carvedilol indication

A

hypertension, HF

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101
Q

carvedilol drug target

A

alpha-1, beta-1,2

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102
Q

carvedilol target family

A

GPCRs on vascular SMCs, cardiomyocytes, bronchiolar SMCs

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103
Q

carvedilol target normal role

A

binding of NE to alpha-1 ARs on SMCs of peripheral vasculature is signaled via Gq, resulting in increased intracellular Ca concentration to stimulate MLCK dependent cellular contraction that result in vasoconstriction and increased blood pressure.
beta-1,2 ARs are Gs coupled GPCRs. they normally get activated by NE in heart and Epi in lunc, increase cAMP conccentration, activate PKA, increase Ca permeability. in cardiomyocytes this activates troponin C and the actin-myosin system leading to increased HR and force of contraction. in bronchiolar SMC this leads to deactivation of MLCK and myosin, that relaxes SMC and result in bronchiodilation.

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104
Q

carvedilol pharmacologic activity

A

reversible orthosteric antagonist

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105
Q

carvedilol MOA

A

as a beta-1 AR, carvedilol blocks receptor activation by NE or Epi, thereby reducing heart rate and stroke volume that contribute to hypertension. in addition, as an alpha-1 AR antagonist, carvedilol blocks symphathetic receptor activation by NE, thereby relaxing vasoconstriction to reduce elevated blood pressure in the treatment of hypertension.

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106
Q

atrovastatin brand name

A

Lipitor

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107
Q

atrovastatin drug class

A

antilipemic agent, HMG-CoA reductase inhibitor

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108
Q

atrovastatin indication

A

Hypercholesterolemia

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109
Q

atrovastatin drug target

A

HMG-CoA reductase

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110
Q

atrovastatin target family and location

A

oxioreductase enzyme expressed in hepatocytes (liver cells)

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111
Q

atrovastatin target normal role

A

HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate limiting step in the mevalonate biosynthetic pathway that provides cholesterol in other isoprenoids

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112
Q

atrovastatin pharmacologic activity

A

reversible competitive inhibitor

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113
Q

atrovastatin MOA

A

as a competitive HMG-CoA reductase inhibitor, a statin blocks cholesterol biosynthesis. this induces the expression of LDL receptors in the liver to increase reuptake of LDL, increases the catabolism of plasma LDL, and lowers the plasma concentration of cholesterol

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114
Q

lovastatin brand name

A

Altoprev or Mevacor

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115
Q

lovastatin drug class

A

antilipemic agent, HMG CoA reductase inhibitor

116
Q

lovastatin indication

A

hypercholesterolemia

117
Q

lovastatin target

A

HMG CoA reductase

118
Q

lovastatin target location and family

A

oxioreductase enzyme expressed in hepatocytes

119
Q

lovastatin target normal role

A

HMG-CoA reductase catalyzes the conversion of HMG-CoA to mevalonic acid, the rate limiting step in the mevalonate biosynthetic pathway the provides cholesterol and other isoprenoids

120
Q

lovastatin pharmacologic activity

A

reversible competitive inhibitor

121
Q

lovastatin MOA

A

as a competitive HMG-CoA reductase inhibitor, a statin blocks cholesterol biosynthesis. this induces the expression of LDL receptors in the liver in increase LDL reuptake, increases catabolism of plasma LDL, and lowers the plasma concentration of cholesterol

122
Q

pravastatin brand name and drug class

A

Pravachol

antilipemic agent, HMG-CoA reductase inhibitor

123
Q

rosuvastatin brand name and drug class

A

Crestor
antilipemic agent
HMG-CoA reductase inhibitor

124
Q

simvastatin brand name and drug class

A

Zocor

antilipemic agent, HMG Co-A reductase inhibitor

125
Q

fenofibrate brand name

A

Tricor

126
Q

fenofibrate drug class

A

antilipemic agent, fibric acid

127
Q

fenofibrate indication

A

hypercholesterolemia

128
Q

fenofibrate drug target

A

PPAR-alpha

129
Q

fenofibrate target family and location

A

heterodimeric nuclear receptor expressed in liver cells and other cells

130
Q

fenofibrate target normal role

A

as a nuclear receptor PPAR-alpha is a ligand activated transcription factor and a major regulator of lipid metabolism in the liver. Normally, its activation by endogenous ligands such as arachidoinic acid and poly unsaturated fatty acids results in reuptake, utilization and catabolism of fatty acids by upregulation of genes involved in fatty acid transport, binding, and activation, and peroxisomal and mitochondrial fatty acid beta oxidation

131
Q

fenofibrate pharmacologic activity

A

agonist

132
Q

fenofibrate MOA

A

as an agonist, fibrates promote uptake, utilization, and catabolism of fatty acids by upregulation of genes involved in fatty acid transport binding and activatioin, and peroxisomal and mitochondrial fatty acid beta oxidation. this results in decreased LDL and TG concentrations and increased HDL concentration to counter hypercholesterolemia and hyperlipidemia

133
Q

gemfibrozil brand name and drug class

A

Lopid

antilipemic agent, fibric acid

134
Q

ezetimibe brand name

A

Zetia

135
Q

ezetimibe drug class

A

antilipemic agent, 2-azetidinone

136
Q

ezetimibe indication

A

hypercholesterolemia

137
Q

ezetimibe drug target

A

NPC1L1

138
Q

ezetimibe target family and location

A

transporter expressed on epithelial cells of the small intestine

139
Q

ezetimibe target normal role

A

NPC1L1 transports dietary cholesterol from the intestinal lumen into the membrane of the epithelial cells from which the cholesterol can be transported to the liver

140
Q

ezetimibe pharmacologic activity

A

reversible, non-competitive inhibitor

141
Q

ezetimibe MOA

A

as an inhibitor, ezetimibe binds to the extracellular loop of NPC1L1 to prevent the conformational changes required for the N-terminal domain to deposit cholesterol into microdomains. this reduces the transport of dietary cholesterol to the liver and decreases total cholesterol, LDL, ApoB, and TG, while increasing HDL to encounter hypercholesterolemia

142
Q

simvastatin/ezetimibe brand name

A

Vytorin

143
Q

hydrochlorothiazide brand name

A

Microzide

144
Q

hydrochlorothiazide drug class

A

thiazide diuretic, antihypertensive

145
Q

hydrochlorothiazide indication

A

HTN, edema

146
Q

hydrochlorothiazide target

A

NCC symporter

147
Q

hydrochlorothiazide target family and location

A

symporter on the distal convoluted tubule of the nephron

148
Q

hydrochlorothiazide target normal role

A

in the distal convoluted tubule, the Na/Cl symport helps reabsorb about 5% of the Na and Cl ions back into the bloodstream

149
Q

hydrochlorothiazide target pharmacologic activity

A

blocker

150
Q

hydrochlorothiazide MOA

A

as a thiazide diuretic, HCTZ competes for the Cl binding site of the Na/Cl symporter and inhibits the reabsorption of Na and Cl ions back into the bloodstream

151
Q

chlorthialidone brand name and drug class

A

N/A

thiazide-like diuretic, antihypertensive

152
Q

triamterene brand name

A

Maxizide, Diazide

153
Q

triamterene drug class

A

K+ sparing diuretic; antihypertensive

154
Q

triamterene indication

A

HTN or edema for patients who develope hypokalemia on HCTZ alone

155
Q

triamterene drug target

A

ENaC and NCC

156
Q

triamterene target family and location

A

sodium ion channel in epithelial cells of the collecting duct and distal convoluted tubule

157
Q

triamterene target normal role

A

in the collecting duct, ENaC is activated by aldosterone and reabsorbs a small amount of sodium

158
Q

triamterene pharmacologic activity

A

blocker

159
Q

triamterene MOA

A

as a K+ sparing diuretic, triamterene blocks ENaC in the collecting duct causing a small increase in Na reabsorption in the collecting duct means that K+ excretion is not increased to balance the cations.

160
Q

spironolactone brand name

A

Aldactone

161
Q

spironolactone drug class

A

K+ sparing diuretic; antihypertensive; mineralocorticoid receptor antagonist

162
Q

spironolactone indication

A

edema, hypokalemia, HTN, HF

163
Q

spironolactone drug target

A

aldosterone receptor (MR)

164
Q

spironolactone target family and location

A

nuclear receptor in epithelial cells of the collecting duct and late distal tubule

165
Q

spironolactone target normal role

A

aldosterone is a hormone produced by the adrenal gland and acts on the MR in the distal tubules and collecting ducts of the nephron. it causes changes in the expression of proteins that lead to the reabsorption of sodium and excretion of potassium, thereby increasing fluid retention, blood volume, and blood pressure

166
Q

spironolactone pharmacologic activity

A

reversible orthosteric antagonist

167
Q

spironolactone MOA

A

competes with aldosterone for MR sites in the distal tubule, blocking increased expression of aldosterone-induced proteins (AP), thereby increasing Na and water excretion, while conserving K and H

168
Q

lisinopril/HCTZ brand name

A

Zestoretic

169
Q

esomeprazole brand name

A

Nexium

170
Q

esomeprazole drug class

A

PPI

171
Q

esomeprazole indication

A

GERD, PUD

172
Q

esomeprazole drug target

A

H+/K+ ATPase (protone pump

173
Q

esomeprazole target family and location

A

transporter on parietal cells

174
Q

esomeprazole target normal role

A

after feeding, paretal cells are stimulated by histamine, gastrin, or acetylcholine to phosphorylate cytoskeletal proteins that facilitate the fusion of H+/K+ ATPase tubulovesicles with the luminal cell membrane. the proton pump moves H+ into the stomach lumen as part of the gastric juice that initiates digestion

175
Q

esomeprazole pharmacologic activity

A

irreversible inhibitor

176
Q

esomeprazole MOA

A

by irreversibly inhibiting the H+/K+ ATPase, PPI drugs suppress both basal and stimulated gastric acid secretion to reduce irritation/damage in the stomach that is symptomatic of acid peptic diseases like GERD and PUD

177
Q

lansoprazole brand name and drug class

A

Prevacid

PPI

178
Q

omeprazole brand name and drug class

A

Prilosec

PPI

179
Q

pantoprazole brand name and drug class

A

Protonix

PPI

180
Q

famotidine brand name

A

Pepcid

181
Q

famotidine drug class

A

H2R antagonist

182
Q

famotidine indication

A

GERD, PUD, heartburn

183
Q

famotidine drug target

A

H2R

184
Q

famotidine target family and location

A

GPCRs expressed on parietal cells

185
Q

famotidine target normal role

A

histamine secreted by ECL cells activates H2R on parietal cells. this activation is coupled to Gs subunits increasing cAMP to activate PKA. PKA phospharylates cytoskeletal proteins to facilitate the fusion of H+/K+ ATPase tubulovesicles with the luminal cell membrane to increase gastric acid secretion.

186
Q

ranitidine brand name and drug class

A

Zantac

H2RA

187
Q

ondansetron brand name

A

Zofran

188
Q

ondansetron drug class

A

selective 5HT3RA, antiemetic

189
Q

ondansetron indication

A

nausea and vomiting

190
Q

ondansetron drug target

A

serotonin 5-HT3R

191
Q

ondansetron target family and location

A

ligand gated ion channels on enteric neurons and neurons of chemoreceptor trigger zone in AP

192
Q

ondansetron target normal role

A

5-HT3 receptor is activated by 5-HT secreted by EC cells in the GI tract. It allows Na+ into the neurons resulting in depolarization and further neurotransmission. In ENS neurons, the neurotransmission to inhibitory vagal afferents ultimately stimulates distal NO release as part of peristalsis. in CNS neurons in the chemoreceptor trigger zone of the AP, the neurotransmission is involved in nausea and the initiation of the vomiting reflex

193
Q

ondansetron pharmacologic activity

A

reversible orthosteric antagonist

194
Q

ondansetron MOA

A

as a 5-HT3R antagonist, ondanseetron blocks 5-HT from activating 5-HT3R located on enteric neurons connecting to inhibitory vagal afferents and thereby, prevents depolarization of the neuron and increases normal HI contractility to reduce the reverse contraction necessary for vomiting. Ondansetron also blocks activation of 5-HT3R located on CTZ neurons to prevent depolarization of the neurons and reduce vomiting signaling in the CNS.

195
Q

metoclopramide brand name

A

Reglan

196
Q

metoclopramide drug class

A

serotinin 5-HT4 Receptor agonist; antiemetic; dopamine antagonist’ GI agent; prokinetic

197
Q

metoclopramide indication

A

nausea and vomiting

198
Q

metoclopramide drug target

A

serotonin 5-HT4 R

199
Q

metoclopramide target family and location

A

GPCR expressed on enteric neurons

200
Q

metoclopramide target normal role

A

serotonin acts as an agonist at 5-HT4R’s thereby activating Gs to increase cAMP and stimulating ACh release from enteric neurons that leads to GI smooth muscle contraction as part of peristalsis.

201
Q

metoclopramide pharmacologic activity

A

agonist

202
Q

metoclopramide MOA

A

by acting as an agonist at 5-HT4Rs on enteric neurons, metoclopramide enhances GI smooth muscle cell contraction, which accelerates gastric emptying, enhances GI motility, and suppresses vomitting.

203
Q

meclizine brand name

A

Antivert

204
Q

meclizine drug class

A

first gen histamine H1 receptor antagonist; antiemetic

205
Q

meclizine indication

A

nausea and vomiting

206
Q

meclizine drug target

A

H1R

207
Q

meclizine target family and location

A

GPCRs expressed on neurons in the vestibular nuclei of the CNS

208
Q

meclizine target normal role

A

H1R is activated by histamine to mediate neurotransmission in the vestibular system. Activation of this system communicates signaling from five distinct end organs in the inner ear to provide information about spatial orientation and allow neural control of both body and head posture

209
Q

meclizine pharmacologic activity

A

reversible, orthosteric antagonist

210
Q

meclizine MOA

A

as an H1R antagonist, meclizine blocks H1R activation by histamine, thereby suppressing neurotransmission in the vestibular system that results in motion sickness, including nausea and vomiting.

211
Q

promethazine brand name and drug class

A

Phenergan

first gen H1R

212
Q

bethanechol brand name

A

Urecholine

213
Q

bethanechol drug class

A

cholinergic agonist

214
Q

bethanechol indication

A

urinary retention

215
Q

bethanechol drug target

A

muscarinic acetylcholine receptor

216
Q

bethanechol target family and location

A

GPCR on SMCs of the bladder wall

217
Q

bethanechol target normal role

A

ACh secreteed by parasympathetic neurons activates mACHRs on SMCs of the bladder wall resulting in Gq signaling to increase the Ca concentration. the intracellular Ca binds to calmodulin and the complex activates MLCK which phophorylates myosin which interacts with actin to induce SMC contraction. in the bladder wall SMC contractin is responsible for bladder emptying

218
Q

bethanochol pharmacologic activity

A

agonist

219
Q

bethanechol MOA

A

as an mAChR agonist, bethanechol activates mAChR, thereby stimulating smooth muscle contractions and bladder emptying to treat urinary retention

220
Q

solifenacin brand name

A

Vesicare

221
Q

solifenacin drug class

A

anticholinergic agent

222
Q

solifenacin indication

A

overactive bladder

223
Q

solifenacin drug target

A

mAChR

224
Q

solifenacin target family and location

A

GPCR on SMCs of the bladder wall

225
Q

solifenacin target normal role

A

ACh secreted by parasympathetic neurons activates mAChRs on SMCs of the bladder wall resulting in Gq signaling to increase the Ca concentration. the intracellular Ca binds to calmodulin and the complex activates MLCK, which phosphorylates myosin, which interacts with actin to induce SMC contraction. in the bladder wall, SMC contraction is responsible for bladder emptying.

226
Q

solifenacin pharmacologic activity

A

reversible, orthosteric antagonist

227
Q

solifenacin MOA

A

as an mAChR antagonist, solifenacin blocks parasympathetic activation of the receptor by ACh. In SMCs of the bladder contraction that results in OAB-associated LUTS such as urinary frequency.

228
Q

tolterodine brand name and drug class

A

Detrol

OAB

229
Q

oxybutynin brand name and drug class

A

Ditropan XL

antispasmodic agent, urinary

230
Q

tamsulosin brand name

A

Flomax

231
Q

tamsulosin class

A

alpha-1 blocker

232
Q

tamsulosin indication

A

LUTS associated with BPH

233
Q

tamsulosin drug target

A

alpha-1 adrenergic receptors

234
Q

tamsulosin target family and location

A

GPCR on SMCs on bladder internal urethral sphincter

235
Q

tamsulosin target normal role

A

NE serves as the endogenous agonist to activate alpha-1 ARs, which signal through Gq to increase intracellular Ca concentration, activate MLCK, and cause smooth muscle contraction. In the bladder’s lower urethral sphincter, SMC contraction closes or restricts the bladder outlet.

236
Q

tamsulosin pharmacologic activity

A

reversible orthosteric antagonist

237
Q

tamsulosin MOA

A

as an alpha-1 AR antagonist, tamsulosin blocks sympathetic activation of the receptor by NE. In SMCs of the bladder’s lower urethral sphincter, this reduces the sympathetic tone-induced constriction of the sphincter that contributes to the increased outlet resistance associated with BPH

238
Q

doxazosin brand name

A

Cardura

239
Q

doxazosin class

A

alpha-1 blocker; antihypertensive

240
Q

doxazosin indication

A

hypertension; LUTS associated with BPH

241
Q

doxazosin drug target

A

alpha-1 AR

242
Q

doxazosin target family and location

A

GPCR on SMCs in peripheral vasculature and bladder’s internal sphincter

243
Q

doxazosin target normal role

A

NE serves as the endogenous agonist to activate alpha-1 ARs, which signal through Gq to increase the intracellular Ca concentration, activate MLCK, and cause smooth muscle contraction. In the peripheral vasculature, SMC contraction results in vasoconstriction and increased blood pressure. In the bladder’s lower urethral sphincter, SMC contraction closes or restricts the bladder outlet

244
Q

doxazosin pharmacologic activity

A

reversible orthosteric antagonist

245
Q

doxazosin MOA

A

as an alpha-1 AR antagonist, doxazosin blocks sympathetic activation of the receptor by NE. In vascular SMCs, this causes a relaxation of vasoconstriction to reduce elevated blood pressure in the treatment of hypertension. In SMCs of the bladder’s lower urethral sphincter, this reduces the sympathetic tone-induced constriction of the sphincter that contributes to the increased outlet resistance associated with BPH

246
Q

abiraterone brand name

A

Zytiga, Yonsa

247
Q

abiraterone class

A

antiandrogen; antineoplastic agent, antiandrogen

248
Q

abiraterone indication

A

metastatic prostate cancer

249
Q

abiraterone target

A

17-alpha-hydroxylase and C-17,20-lyase

250
Q

abiraterone target family and location

A

oxidoreductase enzyme expressed in testicular, adrenal, and prostatic tissue

251
Q

abiraterone target normal role

A

in steroidogenesis, 17 alpha-hydroxylase converts progestagens pregnenolone and progesterone to their 17-alpha-hydroxypregnenolone to dehydroepiandrosterone (DHEA) and 17-alpha-hydroxyprogesteerone to androstenedione. DHEA and androstenedione are androgens and precursors of testosterone. Androgens binding to AR affects gene transcription to promote the growth and development of the male sex organs and maintain male secondary sex characcteristics.

252
Q

abiraterone pharmacologic activity

A

irreversible inhibitor

253
Q

abiraterone MOA

A

as an irreversible inhibitor of 17 alpha-hydroxylase and C17,20-lyase abiraterone blocks the formation or the testosterone precursors DHEA and androstenedione. In turn, the reduced production of androgens decreases the growth-stimulating effects on prostatic tumors.

254
Q

anastrozole brand name

A

Arimidex

255
Q

anastrozole class

A

antineoplastic agent, aromatase inhibitor

256
Q

anastrozole indication

A

breast cancer, estrogen receptor positive

257
Q

anastrozole target

A

aromatase

258
Q

anastrozole target family and location

A

oxidoreductase enzyme expressed in many tissues, including gonads, brain, and bone

259
Q

anastrozole target normal role

A

in steroidogenesis, aromatase converts androgens androstenedione and testosterone to estrone and estradiol, respectively. estrogen binding to ER affects gene trandcription to influence the development and secondary sexual characteristics

260
Q

anastrozole pharmacologic activity

A

reversible, competitive inhibitor

261
Q

anastrozole MOA

A

as an inhibitor of aromatase, anastrozole blocks the conversion of androstenedione to estrone and testosterone to estradiol. In turn, the reduced production of estrogens decreases tumor mass or delays progression in patients with ER-positive tumors responsive.

262
Q

dutasteride brand name

A

Avodart

263
Q

dutasteride class

A

5 alpha reductase inhibitor

264
Q

dutasteride indication

A

BPH

265
Q

dutasteride drug target

A

5 alpha reductase type 1 and 2

266
Q

dutasteride target family and location

A

oxidoreductase enzyme in reproductive tissue

267
Q

dutasteride target normal role

A

in steroidogenesis, 5-alpha-reductase converts testosterone to DHT. DHT binding to AR affects gene transcription to promote the normal development of the prostate and external genitalia in men

268
Q

dutasteride pharmacologic activity

A

irreversible inhibitor

269
Q

dutasteride MOA

A

as an inhibitor of type 2-5AR, dutasteride blocks the conversion of testosterone to DHT. in turn, the reduced production of DHT decreases the growth stimulating effects on prostatic tumors

270
Q

finasteride brand name

A

Proscar; Propecia

271
Q

finasteride drug class

A

5-alpha-reductse inhibitor

272
Q

finasteride indication

A

male pattern hair loss (androgenic alopecia); BPH

273
Q

finasteride drug target

A

5 alpha reductase type 2

274
Q

finasteride drug target location and family

A

oxidoreductase enzyme in liver and skin (type 1), and reproductive tissue (type 2)

275
Q

finasteride target normal role

A

in steroidogenesis, 5 alpha reductase converts testosterone to DHT. DHT binding to AR affects gene transcription to promote the normal development of the prostate and external genitalia in men. DHT also contribute to the regulation of the hair follicle cycle

276
Q

finasteride pharmacologic activity

A

irreversible inhibitor

277
Q

finasteride MOA

A

as an inhibitor of 5AR, finasteride blocks the conversion of testosterone to DHT. in turn, the reduced production of DHT decreases the growth-stimulating effect on prostatic tumors. the reduced concentration of circulating DHT also influences the hair follicle cycle to decrease hair loss and increase hair regrowth

278
Q

sildenafil brand name

A

Viagra; Revatio

279
Q

sildenafil class

A

PDE-5 inhibitor

280
Q

sildenafil indication

A

ED (viagra); pulmonary arterial hypertension (Revatio)

281
Q

sildenafil target

A

PDE-5

282
Q

sildenafil family and location

A

hydrolase enzyme in vascular SMCs

283
Q

sildenafil target normal role

A

During sexual stimulation, NO is released from endothelial cells of the corpus cavernosum. NO then diffusees across membranes to activate the enzyme soluble guanylate cyclase in vascular SMCs which catalyzes the formation of cGMP, producing muscle relaxation and inflow of blood to the corpus cavernosum. PDE-5 hydrolyzes cGMP to GMP deactivate the erection producing signal

284
Q

sildenafil pharmacologic activity

A

reversible competitive inhibitor

285
Q

sildenafil MOA

A

as an inhibitor of PDE-5, sildenafil enhances the effects of NO by maintaining an increased concentration of cGMP in the vascular SMCs of the corpus cavernosum. this results in smooth muscle relaxation and inflow of blood to the corpus cavernosum

286
Q

tadalafil brand name and drug class

A

Cialis; Adcirca

PDE5 inhibitor

phcy 503 (2 decks)

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