Exam 1 Drugs Flashcards
1
Q
aspirin drug class
A
antiplatelet agent, salicylates, NSAID
2
Q
aspirin indication
A
secondary prevention after acute coronary syndrome
3
Q
aspirin drug target
A
cyclooxygenase 1 enzyme (COX-1)
4
Q
aspirin target family and location
A
oxioreductase enzyme in platelets
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
6
Q
aspirin pharmacologic activity
A
Irreversible, competitive inhibitor
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
8
Q
clopidogrel brand name
A
Plavix
9
Q
clopidogrel drug class
A
antiplatelet agent, thienopyridine
10
Q
clopidogrel indication
A
Heart disease
11
Q
clopidogrel target
A
P2Y12 receptor
12
Q
clopidogrel target family and location
A
GPCR on platelets
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
14
Q
clopidogrel pharmocologic activity
A
Irreversible, orthosteric antagonist
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
16
Q
prasugrel brand name
A
Effient
17
Q
prasugrel drug class
A
antiplatelet agent, thienopyridine
18
Q
prasugrel indication
A
heart disease
19
Q
prasugrel drug target
A
P2Y12R
20
Q
prasugrel target family and location
A
GPCR on platelets
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.
22
Q
prasugrel pharmacologic activity
A
irreversible, orthosteric antagonist
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
24
Q
losartan brand name
A
Cozaar
25
losartan drug class
ARB blocker, antihypertensive
26
losartan indication
hypertension management
27
losartan drug target
angiotensin II type 1 receptor (AT1R)
28
losartan drug family and location
GPCR on vascular smooth muscle
29
losartan target normal role
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
30
losartan pharmacologic activity
reversible, orthosteric antagonist
31
losartan MOA
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
32
olmesartan brand name
Benicar
33
olmesartan drug class
ARB, antihypertensive
34
olmesartan indication
management of hypertension
35
olmesartan drug target
angiotensin II type 1 receptors
36
olmesartan target family and location
GPCR on vascular smooth muscle
37
olmesartan target normal role
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
38
olmesartan pharmacologic activity
reversible, orthosteric antagonist
39
olmesartan MOA
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
40
valsartan brand name
Diovan
41
valsartan drug class
ARB, antihypertensive
42
valsartan indication
management of hypertension
43
valsartan drug target
angiotensin II type 1 receptor
44
valsartan target family and location
GPCR on SMC
45
valsartan target normal role
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
46
valsartan pharmacologic activity
reversible orthosteric antagonist
47
valsartan MOA
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
48
benazepril brand name
Lotensin
49
benazepril drug class
ACE-I, antihypertensive
50
benazepril indication
hypertension
51
benazepril drug target
angiotensin converting enzyme (ACE)
52
benazepril target family and location
peptidase on surface of endothelial cells in kidney and lungs
53
benazepril target normal role
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.
54
benazepril pharmacologic activity
reversible competitive inhibitor
55
benazepril MOA
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
56
enalapril brand name
Vasotec
57
enalapril drug class
ACE-I, antihypertensive
58
enalapril indication
hypertension
59
enalapril drug target
angiotensin converting enzyme
60
enalapril target family and location
peptidase on surface of endothelial cells in kidney and lungs
61
enalapril target normal role
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
62
enalapril pharmacologic activity
reversible, competitive inhibitor
63
enalapril MOA
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
64
lisinopril brand name and drug class
Zestril/Prinivil
| ACE-I
65
ramipril brand name and drug target
Altace
| ACE-I
66
clonidine brand name
Catapres
67
clonidine drug class
alpha-2 adrenergic receptor agonist, antihypertensive
68
clonidine indication
manage management of hypertension
69
clonidine drug target
alpha 2 adrenergic receptor
70
clonidine target family
GPCR on post synaptic CNS neurons
71
clonidine target normal role
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
72
clonidine pharmacologic activiry
agonist
73
clonidine MOA
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
74
doxazosin brand name
Cardura
75
doxazosin drug class
alpha 1 blocker, antihypertensive
76
doxazosin indication
hypertension, BPH
77
doxazosin drug target
alpha-1 AR
78
doxazosin target family and location
GPCR on SMCs of peripheral vasculature and bladder sphicter
79
doxazosin target normal role
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
80
doxazosin pharmacologic activity
reversible, orthosteric antagonist
81
doxazosin MOA
blocks sympathetic activation of alpha-1 AR by NE, thereby relaxing vasoconstriction to reduce elevated blood pressure in the treatment of hypertension
82
propranolol brand name
Inderal LA
83
propanolol drug class
beta blocker, nonselective, antihypertensive
84
propranolol indication
hypertension
85
propanolol drug target
beta-1 and beta-2 ARs
86
propranolol target family and location
GPCRs on cardiomyocytes and bronchiolar SMCs
87
propranolol target normal role
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.
88
atenolol brand name
Tenormin
89
atenolol drug class
selective beta-1 blocker, antihypertensive
90
atenolol indication
hypertension
91
atenolol drug target
beta-1 AR
92
atenolol target family and location
GPCR on cardiomyocytes
93
atenolol target normal role
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)
94
atenolol pharmacologic activity
reversible, orthosteric antagonist
95
atenolol MOA
selectively blocks beta-1 AR activation by NE or Epi, thereby reducing heart rate and stroke volume that lead to hypertension
96
metroprolol brand name and drug class (explain other parts too)
Lopressor, Toprol XL
Beta-1 selective blocker,
antihypertensive
97
nebivolol brand name and drug class (explain other parts too)
Bystolic
| beta-1 selective blocker, antihypertensive
98
carvedilol brand name
Coreg
99
carvedilol drug class
beta blocker with alpha blocking activity, antihypertensive
100
carvedilol indication
hypertension, HF
101
carvedilol drug target
alpha-1, beta-1,2
102
carvedilol target family
GPCRs on vascular SMCs, cardiomyocytes, bronchiolar SMCs
103
carvedilol target normal role
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.
104
carvedilol pharmacologic activity
reversible orthosteric antagonist
105
carvedilol MOA
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.
106
atrovastatin brand name
Lipitor
107
atrovastatin drug class
antilipemic agent, HMG-CoA reductase inhibitor
108
atrovastatin indication
Hypercholesterolemia
109
atrovastatin drug target
HMG-CoA reductase
110
atrovastatin target family and location
oxioreductase enzyme expressed in hepatocytes (liver cells)
111
atrovastatin target normal role
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
112
atrovastatin pharmacologic activity
reversible competitive inhibitor
113
atrovastatin MOA
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
114
lovastatin brand name
Altoprev or Mevacor
115
lovastatin drug class
antilipemic agent, HMG CoA reductase inhibitor
116
lovastatin indication
hypercholesterolemia
117
lovastatin target
HMG CoA reductase
118
lovastatin target location and family
oxioreductase enzyme expressed in hepatocytes
119
lovastatin target normal role
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
lovastatin pharmacologic activity
reversible competitive inhibitor
121
lovastatin MOA
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
pravastatin brand name and drug class
Pravachol
| antilipemic agent, HMG-CoA reductase inhibitor
123
rosuvastatin brand name and drug class
Crestor
antilipemic agent
HMG-CoA reductase inhibitor
124
simvastatin brand name and drug class
Zocor
| antilipemic agent, HMG Co-A reductase inhibitor
125
fenofibrate brand name
Tricor
126
fenofibrate drug class
antilipemic agent, fibric acid
127
fenofibrate indication
hypercholesterolemia
128
fenofibrate drug target
PPAR-alpha
129
fenofibrate target family and location
heterodimeric nuclear receptor expressed in liver cells and other cells
130
fenofibrate target normal role
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
fenofibrate pharmacologic activity
agonist
132
fenofibrate MOA
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
gemfibrozil brand name and drug class
Lopid
| antilipemic agent, fibric acid
134
ezetimibe brand name
Zetia
135
ezetimibe drug class
antilipemic agent, 2-azetidinone
136
ezetimibe indication
hypercholesterolemia
137
ezetimibe drug target
NPC1L1
138
ezetimibe target family and location
transporter expressed on epithelial cells of the small intestine
139
ezetimibe target normal role
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
ezetimibe pharmacologic activity
reversible, non-competitive inhibitor
141
ezetimibe MOA
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
simvastatin/ezetimibe brand name
Vytorin
143
hydrochlorothiazide brand name
Microzide
144
hydrochlorothiazide drug class
thiazide diuretic, antihypertensive
145
hydrochlorothiazide indication
HTN, edema
146
hydrochlorothiazide target
NCC symporter
147
hydrochlorothiazide target family and location
symporter on the distal convoluted tubule of the nephron
148
hydrochlorothiazide target normal role
in the distal convoluted tubule, the Na/Cl symport helps reabsorb about 5% of the Na and Cl ions back into the bloodstream
149
hydrochlorothiazide target pharmacologic activity
blocker
150
hydrochlorothiazide MOA
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
chlorthialidone brand name and drug class
N/A
| thiazide-like diuretic, antihypertensive
152
triamterene brand name
Maxizide, Diazide
153
triamterene drug class
K+ sparing diuretic; antihypertensive
154
triamterene indication
HTN or edema for patients who develope hypokalemia on HCTZ alone
155
triamterene drug target
ENaC and NCC
156
triamterene target family and location
sodium ion channel in epithelial cells of the collecting duct and distal convoluted tubule
157
triamterene target normal role
in the collecting duct, ENaC is activated by aldosterone and reabsorbs a small amount of sodium
158
triamterene pharmacologic activity
blocker
159
triamterene MOA
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
spironolactone brand name
Aldactone
161
spironolactone drug class
K+ sparing diuretic; antihypertensive; mineralocorticoid receptor antagonist
162
spironolactone indication
edema, hypokalemia, HTN, HF
163
spironolactone drug target
aldosterone receptor (MR)
164
spironolactone target family and location
nuclear receptor in epithelial cells of the collecting duct and late distal tubule
165
spironolactone target normal role
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
spironolactone pharmacologic activity
reversible orthosteric antagonist
167
spironolactone MOA
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
lisinopril/HCTZ brand name
Zestoretic
169
esomeprazole brand name
Nexium
170
esomeprazole drug class
PPI
171
esomeprazole indication
GERD, PUD
172
esomeprazole drug target
H+/K+ ATPase (protone pump
173
esomeprazole target family and location
transporter on parietal cells
174
esomeprazole target normal role
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
esomeprazole pharmacologic activity
irreversible inhibitor
176
esomeprazole MOA
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
lansoprazole brand name and drug class
Prevacid
| PPI
178
omeprazole brand name and drug class
Prilosec
| PPI
179
pantoprazole brand name and drug class
Protonix
| PPI
180
famotidine brand name
Pepcid
181
famotidine drug class
H2R antagonist
182
famotidine indication
GERD, PUD, heartburn
183
famotidine drug target
H2R
184
famotidine target family and location
GPCRs expressed on parietal cells
185
famotidine target normal role
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
ranitidine brand name and drug class
Zantac
| H2RA
187
ondansetron brand name
Zofran
188
ondansetron drug class
selective 5HT3RA, antiemetic
189
ondansetron indication
nausea and vomiting
190
ondansetron drug target
serotonin 5-HT3R
191
ondansetron target family and location
ligand gated ion channels on enteric neurons and neurons of chemoreceptor trigger zone in AP
192
ondansetron target normal role
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
ondansetron pharmacologic activity
reversible orthosteric antagonist
194
ondansetron MOA
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
metoclopramide brand name
Reglan
196
metoclopramide drug class
serotinin 5-HT4 Receptor agonist; antiemetic; dopamine antagonist' GI agent; prokinetic
197
metoclopramide indication
nausea and vomiting
198
metoclopramide drug target
serotonin 5-HT4 R
199
metoclopramide target family and location
GPCR expressed on enteric neurons
200
metoclopramide target normal role
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
metoclopramide pharmacologic activity
agonist
202
metoclopramide MOA
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
meclizine brand name
Antivert
204
meclizine drug class
first gen histamine H1 receptor antagonist; antiemetic
205
meclizine indication
nausea and vomiting
206
meclizine drug target
H1R
207
meclizine target family and location
GPCRs expressed on neurons in the vestibular nuclei of the CNS
208
meclizine target normal role
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
meclizine pharmacologic activity
reversible, orthosteric antagonist
210
meclizine MOA
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
promethazine brand name and drug class
Phenergan
| first gen H1R
212
bethanechol brand name
Urecholine
213
bethanechol drug class
cholinergic agonist
214
bethanechol indication
urinary retention
215
bethanechol drug target
muscarinic acetylcholine receptor
216
bethanechol target family and location
GPCR on SMCs of the bladder wall
217
bethanechol target normal role
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
bethanochol pharmacologic activity
agonist
219
bethanechol MOA
as an mAChR agonist, bethanechol activates mAChR, thereby stimulating smooth muscle contractions and bladder emptying to treat urinary retention
220
solifenacin brand name
Vesicare
221
solifenacin drug class
anticholinergic agent
222
solifenacin indication
overactive bladder
223
solifenacin drug target
mAChR
224
solifenacin target family and location
GPCR on SMCs of the bladder wall
225
solifenacin target normal role
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
solifenacin pharmacologic activity
reversible, orthosteric antagonist
227
solifenacin MOA
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
tolterodine brand name and drug class
Detrol
| OAB
229
oxybutynin brand name and drug class
Ditropan XL
| antispasmodic agent, urinary
230
tamsulosin brand name
Flomax
231
tamsulosin class
alpha-1 blocker
232
tamsulosin indication
LUTS associated with BPH
233
tamsulosin drug target
alpha-1 adrenergic receptors
234
tamsulosin target family and location
GPCR on SMCs on bladder internal urethral sphincter
235
tamsulosin target normal role
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
tamsulosin pharmacologic activity
reversible orthosteric antagonist
237
tamsulosin MOA
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
doxazosin brand name
Cardura
239
doxazosin class
alpha-1 blocker; antihypertensive
240
doxazosin indication
hypertension; LUTS associated with BPH
241
doxazosin drug target
alpha-1 AR
242
doxazosin target family and location
GPCR on SMCs in peripheral vasculature and bladder's internal sphincter
243
doxazosin target normal role
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
doxazosin pharmacologic activity
reversible orthosteric antagonist
245
doxazosin MOA
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
abiraterone brand name
Zytiga, Yonsa
247
abiraterone class
antiandrogen; antineoplastic agent, antiandrogen
248
abiraterone indication
metastatic prostate cancer
249
abiraterone target
17-alpha-hydroxylase and C-17,20-lyase
250
abiraterone target family and location
oxidoreductase enzyme expressed in testicular, adrenal, and prostatic tissue
251
abiraterone target normal role
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
abiraterone pharmacologic activity
irreversible inhibitor
253
abiraterone MOA
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
anastrozole brand name
Arimidex
255
anastrozole class
antineoplastic agent, aromatase inhibitor
256
anastrozole indication
breast cancer, estrogen receptor positive
257
anastrozole target
aromatase
258
anastrozole target family and location
oxidoreductase enzyme expressed in many tissues, including gonads, brain, and bone
259
anastrozole target normal role
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
anastrozole pharmacologic activity
reversible, competitive inhibitor
261
anastrozole MOA
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
dutasteride brand name
Avodart
263
dutasteride class
5 alpha reductase inhibitor
264
dutasteride indication
BPH
265
dutasteride drug target
5 alpha reductase type 1 and 2
266
dutasteride target family and location
oxidoreductase enzyme in reproductive tissue
267
dutasteride target normal role
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
dutasteride pharmacologic activity
irreversible inhibitor
269
dutasteride MOA
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
finasteride brand name
Proscar; Propecia
271
finasteride drug class
5-alpha-reductse inhibitor
272
finasteride indication
male pattern hair loss (androgenic alopecia); BPH
273
finasteride drug target
5 alpha reductase type 2
274
finasteride drug target location and family
oxidoreductase enzyme in liver and skin (type 1), and reproductive tissue (type 2)
275
finasteride target normal role
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
finasteride pharmacologic activity
irreversible inhibitor
277
finasteride MOA
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
sildenafil brand name
Viagra; Revatio
279
sildenafil class
PDE-5 inhibitor
280
sildenafil indication
ED (viagra); pulmonary arterial hypertension (Revatio)
281
sildenafil target
PDE-5
282
sildenafil family and location
hydrolase enzyme in vascular SMCs
283
sildenafil target normal role
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
sildenafil pharmacologic activity
reversible competitive inhibitor
285
sildenafil MOA
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
tadalafil brand name and drug class
Cialis; Adcirca
| PDE5 inhibitor
