ALL THE DRUGS Flashcards

1
Q

muscarinic agonist

A

increase SLUDGE, decrease HR, miosis, dec dopamine. bronchoconstriction

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2
Q

acetylcholine

A

muscarinic agonist, quat, all synapses

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3
Q

methacholine

A

muscarinic agonist, B carbon methyl, quat, induces asthma attack

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4
Q

carbachol

A

muscarinic agonist, quat, carbamate, glaucoma

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5
Q

bethanechol

A

muscarinic agonist, carbamate and methyl on b carbon, treats urinary retention (non-obstructive) and dec symptoms of depression

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6
Q

muscarine

A

muscarinic agonist, quat,

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7
Q

pilocarpine

A

muscarinic agonist,, tert, glaucoma, miosis after eye exam

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8
Q

cevimeline

A

muscarinic agonist, tert, salivary gland issue

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9
Q

muscarinic antagonist

A

decreases slud, mydriasis, increases HR, bronchodilation

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10
Q

muscarinic agonist SAR

A
  1. N capable of being + , no huge groups dec methyls for H on N terminal = dec potency / increased carbons on N antagonist
  2. ethylene bridge (2C)
  3. alcoxyl group (ketone, ester, ether)/ Ing’s rule of 5/
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11
Q

SAR muscarinic antagonist

A
  1. N tertiary or quat
  2. R1 and R2 heterocyclic (can’t be naphthelene)
  3. R3 -H, -OH part of ring
  4. X=ester, ether
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12
Q

atropine

A

muscarinic antagonist, ophthalmic, tert

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13
Q

tropicamide

A

muscarinic antagonist, opthalmic, tert

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14
Q

cyclopentolate

A

muscarinic antagonist,, opthalmic, tert

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15
Q

iptratropium

A

COPD, muscarinic antagonist,, quat

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16
Q

tiotropium

A

COPD, tert, muscarinic antagonist,

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17
Q

umeclidinium

A

COPD, tert, muscarinic antagonist,

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18
Q

glycopyrrolate

A

COPD, tert, muscarinic antagonist,

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19
Q

acidinium

A

COPD, tert, muscarinic antagonist,

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20
Q

benztopine

A

parkinsons, tert, muscarinic antagonist,

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21
Q

trihexylphenydil

A

parkinsons, tert, muscarinic antagonist,

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22
Q

dicycloamine

A

IBS-D, tert, muscarinic antagonist,

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23
Q

scopolamine

A

motion sickness, tert, muscarinic antagonist,

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24
Q

oxybutynin

A

tert, OAB/urinary retention, muscurinic antagonist, cmax related to ADE/lipophillic/P450

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25
tolterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 2D6
26
solifenacin
tert, OAB/urinary retention, muscurinic antagonist, functional selectivity for M3 bladder/ 3A4
27
darifenacin
tert, OAB/urinary retention, muscurinic antagonist, , pharmacologically selective M3, cause dry mouth, 3A4 and 2D6
28
trospium
tert, OAB/urinary retention, muscurinic antagonist, P450/esterase/hydroxylation
29
fesoterodine
tert, OAB/urinary retention, muscurinic antagonist, prodrug 5-HMT
30
AChE inhibitors
increases the ACh, increase SLUDGE, decreases HR and miosis of the eye
31
neostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
32
phyostigmine
AChE inhibitor, tert, carbamate ester
33
pyridostigmine
AChE inhibitor, quat, carbamate ester, myasthenia gravis
34
rivastigmine
alzheimers, carbamate ester, tert
35
carbamate ester
"stigmine" temporary covalent modification, work through being metabolized
36
edrophenium
reversible inhibitor of AChE, quat
37
galantamine
reversible inhibitor of AChE, tert, alzheimers
38
doneprexil
reversible inhibitor of AChE, tert, alzheimers
39
echothiophate
irreversible inhibitor of AChE, quat, glaucoma
40
organophosphates
toxic/dephosphroylate = resistant to hydrolysis = too much ACh build up / use 2-PAM if hasn't aged
41
neuromusuclar blocking agent MOA
immobilize patients for surgery, procedures = work by causing paralysis
42
depolarizing agents
opens the cel membrane and becomes refractory and the muscle becomes resistant to further stimulation, fasciculations and then flaccid paralysis
43
succinylcholine
more ach wouldnt do anything because you are blocking to the binding site to cause muscle activation
44
mivacurium
benzylisoquinolines, non-depolarizing NMBA, shorter half life, quat
45
atracurium
shorter half life, benzylisoquinolines, quat, non-depolarizing, degradation/hoffman elimination
46
cisatrascurium
non-depolarizing NMBA, spontaneous degradation/hoffman elimination
47
rocuronium
amino steroid, hepatic and renal, intermediate half life, non-depolarizing NMBA, hepatic and renal
48
vecuronium
amino steroid, hepatic and renal, intermediate half life, non-depolarizing NMBA
49
pancuronium
amino steroid, hepatic and renal, longest half life, non-depolarizing NMBA
50
alpha 1 agonist
vasoconstriction, decongestant, red eye, inc BP
51
phenylephrine
alpha 1 agonist, decongestant
52
naphazoline
alpha 1 agonist
53
tetrahydrozoline
alpha 1 agonist
54
oxymethazoline
alpha 1 agonist
55
high dose DA
alpha 1 agonist
56
Epi high dose
alpha 1 agonist = B, vasoconstrict, inc TPR
57
Epi low dose
B, inc HR, dec insulin, dec digestion, inc lipolysis, dec uterine, dec urgency
58
NE
alpha, alpha 2, b1 (NO B2), vasoconstrict, cardiac dec (vagal), dec digestion, dec urine
59
alpha 2 agonist
dec SNS, dec HR, dec BP, dec TPR - upregulation of alpha 1 and b1
60
SAR alpha 2 agonist
2, 5 ortho substituents (cl)/ bridge / basic nitrogen grouping/ perpendicular
61
clonidine
alpha 2 agonist, with opioid for pain, causes xerostomia
62
guanacifine
alpha 2 agonist, ADHD
63
methyldopa
alpha 2 agonist
64
dexmedetomidine
sedative
65
b1 agonist
inc FOC, inc HR, used to preserve CO
66
dobutamine
B1
67
isoproterenol
nonselective B agonist
68
mid dose D1
D1, B1
69
B2 agonist MOA
bronchodilation
70
B2 agonist SAR
2 hydroxyl required, 3-hydroxymethyl, 3-formamido, carbostyril ethanolamine side chain (R conformation) / basic substituents
71
albuterol
B2 agonist, SA
72
tertbutaline
B2 agonist
73
salmeterol
B2 agonist, LA
74
fomoterol
B2 agonist
75
indacterol
B2 agonist
76
oldaterol
B2 agonist, LA
77
vilanterol
B2 agonist, LA
78
fenoldapam
D1 agonist - expensive
79
D1 MOA
low dose dopamine, mesenteric dilation, "renal dose"
80
cardioselective B1 antagonist MOA
dec HR, dec FOC, dec CO
81
cardioselective B1 antagonist SAR
SAR: adernergic side chain / ether group / para substituents with an H bond acceptor 1 to 2 atoms away
82
metroprolol
cardioselective B1 antagonist
83
atenolol
cardioselective B1 antagonist MOA, renal
84
bisoproprolol
cardioselective B1 antagonist MOA, renal
85
acebutolol
cardioselective B1 antagonist MOA, hepatic
86
esmolol
cardioselective B1 antagonist MOA, 10 min t1/2 bc esterase
87
alpha 1 antagonist
BPH, kidney stone, last option for decrease in HR
88
parazosin
non-selective alpha 1 antagonist
89
terazosin
non-selective alpha 1 antagonist
90
doxazosin
non-selective alpha 1 antagonist
91
alfuzosin
A alpha 1 antagonist- BPH/kidney stones
92
tamulosin
A alpha 1 antagonist- BPH/kidney stones
93
silodosin
A alpha 1 antagonist- BPH/kidney stones
94
pentoalimine
non-selective alpha, extraversion of vasculature
95
phenoxybenzamine
nonselective alpha = irrreversible= pneumocytoma
96
partial agonist
labetol (B2), acebutolol (B1), pinidol (B1)
97
nonselective B antagonists
pinidolol, propanolol, nadelol
98
labetalol
bblocker with vasodilation, alpha 1 antagonsit/ B1 antagonist / B2 ISA, glucuronidation, CYP450
99
nebivolol
bblocker with vasodilation, NO increased production
100
carvedilol
bblocker with vasodilation, block Ltype CC, antagonist at alpha 1, antioxidation, undergoes o-dealkylation
101
bblockers with vasodilation good for
asthma and COPD
102
renally metabolized bblockers are good for
patients with decreased liver function
103
renally metabolized bblocker
nadelol, atenolol, bisprolol
104
esmolol
quickly metabolized by plasma esterases
105
BBlockers elim by which enzyme
CYP2D6
106
random uses of BBlockers
glaucoma, thyrotoxosis, tremors, migraine
107
BBlockers adverse effects
``` lipid cns depression dec libido hypoglycemia mask overdose causes AV block ```
108
when do you not want to use a nonselective BBlocker?
pts with asthma/ COPD (constrict airways), diabetes - dec insulin secretion