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DRUGS! Flashcards

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1
Q

Epinephrine MOA and effects

A

agonist of a1, a2, b1, b2
increases:
* heart rate
* contractility
* cardiac output
* blood pressure
* blood glucose
* bronchdilation
* blood glucose

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2
Q

epinephrine therapeutic use

A
  • anaphylactic shock
  • cardiac arrest
  • wide angle glaucoma
  • prolong duration of local anesthetics
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3
Q

epinephrine side effects/cautions/contraindications

A

side effects
* arrythmias
* tachycardia
* HTN
* hypokalemia
cautions/contraindications
* hyperthyroidism (increased CV effects)
* diabetes/hyperglycemia
* non-selective b-1 blockers will increase a-1 effects
* narrow angle glaucoma

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4
Q

unique properties of epinephrine

A

causes vasodilation at low dose (b2 receptors) and vasoconstriction at high dose (a1 receptors)

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5
Q

norepinephrine MOA and effects

A

a1, a2, b1 agonist
increases:
* cardiac output
* bronchodilation
* (BP)
decreases:
* peripheral vascular resistance
* (HR)

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6
Q

norepinephrine therapeutic uses

A
  • shock
  • hypotension
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7
Q

norepinephrine side effects/cautions/contraindications

A

side effects:
* phlebitis at injection site
* extravasation–> necrosis
* arrythmias
caution:
* hypertension

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8
Q

isopreterenol MOA and effects

A

b1, b2 agonist
increases
* cardiac output
* bronchodilation
decreases
* peripheral vascular resistance

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9
Q

isoproterenol therapeutic use

A
  • heart block
  • acute cardiac depression
  • bradycardia
  • long QT
  • asthma/COPD
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10
Q

isoproterenol side effects/caution/contraindications

A

side effects
* arrythmias
* tachycardia
* angina
* hypokalemia
* hyperglycemia
* increased renin release
cautions
* cardiac ischemia possible in pts with coronary artery disease
* caution in diabetics & hyperthyroid pts

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11
Q

dopamine MOA and effects

A

D1>b1>a1 agonist
increases
* contractility
* cardiac output
* moderate HR effects

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12
Q

dopamine therapeutic uses

A
  • shock
  • acute, decompensated heart failure
  • acute renal failure
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13
Q

dopamine side effects/cautions/contraindications

A

side effects:
* nausea
* vomiting
* arrythmias
contraindicaitons:
* monoamine oxidase inhibitors (MAOIs)

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14
Q

dopamine unique properties

A
  • increases blood flow to kidney, urine output
  • vasoconstrictor at high dose
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15
Q

albuterol MOA and effects

A

selective b2 agonist
* bronchodilation
* uterine relaxation

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16
Q

albuterol therapeutic uses

A
  • asthma
  • COPD
  • pre-term labor
  • hyperkalemia
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17
Q

albuterol unique properties

A

inhalational use limits CV side effects

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18
Q

albuterol side effects/cautions/contraindications

A

Side effects:
* tremors (b2 activation)
* cardiac stimulation (b1 overflow)

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19
Q

dobutamine MOA and effects

A

selective b1 agonist (with very minor effects on a and b2)
increases:
* contractility
* AV conduction
* heart rate (slight)

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20
Q

dobutamine therpeutic uses

A
  • nasal decongestant
  • hypotension
  • mydriasis
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21
Q

dobutamine side effects/cautions/contraindications

A

side effect:
* arrythmias

caution
* A-fib (due to AV conduction)
* HTN

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22
Q

dobutamine unique properties

A

increases contractility and cardiac output with only moderate effects on heart rate

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23
Q

phenylephrine MOA and effects

A

a1 selective agonist
increases vasoconstriction

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24
Q

phenylephrine therapeutic uses

A
  • nasal decongestant
  • hypotension
  • mydriasis
  • tachycardia
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25
phenylephrine side effects/cautions/contraindications
**side effects:** * rebound hyperemia * nasal ischemia * headache * urinary retention * bradycardia (baroreceptor relfex) **cautions/contraindication:** * hypertension * BPH * pts w/ bradycardia, myocaridal disease, coronary artery disease, peripheral vasculardisease
26
phenylephrine unique properties
related to midordrine which is used for orthostatic HTN
27
clonadine MOA and effects
selective a2 agonist **decreases:** * sympathetic nervous system effects * NT release (feedback inhibition) * PVR * BP
28
clonidine therapeutic use
* HTN * anesthesia (decreases CNS activity, pain) * ADHD
29
clonidine side effects/cautions/contraindications
**side effects:** * sedation * dry mouth * orthostatic hypotension **cautions** * must discontinue slowly to avoid rebound HTN
30
clonidine unique properties
can produce transient initial vasocontriction but ultimately leads to decreased SNS tone and lowered BP
31
mirabegron MOA and effects
b3 agonist * relaxes detrusor muscle to allow filling
32
mirabegron therapeutic use
overactive bladder
33
mirabegron side effects/caution/contraindications
**side effects:** * HTN * dizziness * headaches **caution:** * in pts with poorly controlled HTN
34
mirabegron unique properties
alternative to antimuscarinics for OAB in pts w cognitive impairment
35
cocaine MOA and effects
* blocks dopmine, norepinephrine, and serotonin transporters * inhibits voltage-gated sodium channels (local anesthetic)
36
cocaine therapeutic use
* local anesthetic for ENT procedures
37
cocaine side effects/caution/contraindications
* CV stimulation * arrythmias
38
amphetamine MOA and effects
* competes w/ norepinephrine and dopamine for reuptake * substrate for VMAT (competes w/ NE and DA for uptake into vesicles * inhibits monoamine oxidase to increase NE and DA * causes transporters to efflux NE and DA
39
amphetamine therapeutic uses
* ADHD * narcolepsy
40
amphetamine side effects/caution/contraindications
**side effects** * appetite/growth suppression * unmasking of motor tics * HTN * arrythmias **caution:** * reports of sudden death in pts w/ conduction defects
41
amphetamine unique properties
prone to abuse
42
tyramine MOA and effects
* indirect pressor found in fermented and age foods * can displace NE from NT vesicles to increase NE relase similar to amphetamine whe combined with MAOI
43
tyramine therapeutic use
none
44
tyramine side effects/caution/contraindications
**side effects:** * HTN crisis when combined with MAOI **caution:** * dietary restrictions in pts taking MAOIs
45
tyramine unique properties
* normally metabolized by MAO * found in cheese, beer, wine, aged meats
46
ephedrine/pseudoephedrine MOA and effects
* a and b agonist * moderately enhances NE release
47
ephedrine/pseudoephedrine therapeutic uses
* decongestant * mydriatic * hypotension * (asthma)
48
ephedrine/pseudoephedrine side effects/caution/contraindications
**side effects:** * CV stimulation * arrythmias * anxiety/dizziness **caution:** * pts w/ HTN (a1) * pts w/ diabetes (b2) * pts w/ BPH (a1) * thyroid dysfunction (b1/2) | pseudoephedrine has fewer CNS effects
49
ephedrine/pseudephedrine unique properties
* herbal supplements w/ ephedra/ephedrine banned by FDA for adverse CV events * pseudoephedrine very limites OTC access
50
phentolamine MOA and effects
a1, a2 antagonist
51
phentolamine therapeutic use
* pheochromocytoma (adrenal tumor) * HTN crisis * extravsation of vasoconstrictors
52
phentolamine side effects/caution/contraindications
**side effects:** * orthostatic hypotension * tachycardia/arrythmias (drops MAP by blocking a1, blocks cardiac nerve presynaptic a2 receptors) * myocardial ischemia (blocks a2 reeptors in heart increasing NE release **caution:** * pts w/ angina * pts w/ history of MI, coronary artery disease
53
phenoxybenzamine MOA
a1, a2 antagonist (nonselective)
54
phenoxybenzamine therapeutic use
* HTN crises in pheochromocytoma pts
55
phenoxybenzamine side effects/caution/contraindications
**side effects:** * orthostatic hypotension * tachycardia (can lead to ischemia) * nasal congestion **caution:** * in pts w/ angina, history of MI/coronary artery disease
56
phenoxybenzamine unique properties
irreversible/insurmountable antagonist of a1/a2 (permanent flattened curve)
57
prazosin MOA and effects
competitive a1 antagonist
58
prazosin therapeutic use
* HTN * BPH * PTSD (off label)
59
prazosin side effects/caution/contraindications
**side effects:** * orthostatic hypotension * tachycardia **cautions:** * angina
60
tamsulosin MOA and effects
a1 a/d (most affinity) or a1b (secondary) antagonist
61
tamsulosin therapeutic use
BPH
62
tamsulosin side effects/caution/contraindications
**side effects:** * orthostatic hypotension * tachycardia
63
tamsulosin unique properties
most selective for a1a receptor (in prostate)
64
propranolol MOA and effects
* b1 and b2 antagonist * inhibits Na+ channels at high doses
65
propranolol therapeutic use
* hypertension * angina * post-MI * some arrythmias * hyperthyroid * migraine * performance anxiety
66
propranolol side effects/caution/contraindications
**side effects:** * bradycardia * bronchostriction * lowered HDL:LDL * nightmares * impotence/ED * decreased exercise tolerance **caution:** * pts w/ asthma/COPD (extreme caution) * acute cardiac failure * delayed response to hypoglycemia in diabetic pts * CNS effects (nightmares, fatigue, lethargy) * decreased exercise tolerance * pts w/ severe bradycardia * pts w/ 2nd/3rd degree heart block * discontinue slowly to prevent further angina/arrythmias)
67
propanolol unique properties
inhibits sodium channels at high doses
68
timolol MOA and effects
b1/b2 antagonist
69
timolol therapeutic use
* wide angle glaucoma (decreases AH production) * HTN * post-MI * migraine
70
timolol side effects/caution/contraindications
**side effects:** * bradycardia * bronchoconstriction * lowered HDL:LDL * impotence/ED * decrease exercised tolerance **caution:** * pts w/ asthma/COPD * acute cardiac failure * severe bradycardia * 2nd/3rd degree heart block * delayed response to hypoglycemia in diabetics * discontinue slowly to prevent further angina/arrythmias)
71
metoprolol MOA
"cardioselective" b1 antagonist
72
metoprolol therapeutic use
* HTN * angina * post-MI * some arrythmias * congestive heart failure
73
metoprolol side effects/caution/contraindications
**side effects:** * bradycardia * bronchoconstriction * lowered HDL:LDL * impotence/ED * decrease exercised tolerance **caution:** * pts w/ asthma/COPD * acute cardiac failure * severe bradycardia * 2nd/3rd degree heart block * delayed response to hypoglycemia in diabetics * discontinue slowly to prevent further angina/arrythmias)
74
metoprolol unique properties
* proven to decrease CHF-related mortality * lower risk of lipid abnormalities * safer for diabetic pts * safer for pts w/ asthma/COPD
75
esmolol MOA
cardioselective b1 antagonist (very short acting)
76
esmolol therapeutic use
* intraoperative control of tachycardia/HTN * SVT (arrythmia)
77
esmolol side effects/caution/contraindications
**side effects:** * hypotension **cautions:** * pts w/ severe bradycardia, hypotension, 2nd/3rd degree heart block * lowered risk for pts w/ asthma/COPD but still must monitor
78
esmolol unique properties
* metabolized by esterases on RBCs * duration of action only 5-10 minutes
79
carvedilol/labetalol MOA
b1/b2/a1 antagonist
80
carvedilol/labetalol therapeutic use
* HTN * HTN emergency (labetalol) * heart failure/CHF (carvedilol) * post-MI
81
carvedilol/labetolol side effects/caution/contraindications
**side effects:** * orthostatic hypotension (a1 blockade) * bradycardia * decreased execise tolerance **caution:** * pts w/ asthma/COPD * pts w/ severe bradycardia * pts w/ 2nd/3rd degree heart block * discontinue slowly to avoid angina, arrythmias
82
labetalol unique properties
often used in pregnant pts w/ HTN (preeclampsia)
83
acetylcholine MOA
nonselective muscarinic agonist
84
acetylcholine therapeutic use
none (rapidly degraded by cholinesterases)
85
acetylcholine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB
86
acetylcholine unique properties
IV administration can cause transient vasodilation via NO produced by endothelium
87
bethanechol MOA
non-selective muscarinic agonist
88
bethanechol therapeutic use
* post-op ileus (bowel obstruction) * urinary retention
89
bethanechol side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * nausea/vomiting **caution:** * pts w/ asthma/COPD * beta blockers (risk of bronchoconstriction/bradycardia) * gastric ulcers (due to increased secretion) * pts w/ hyperthyroid (risk of A fib)
90
bethanechol unique properties
* relatively insensitive to cholinesterases * short-acting * eliminated rapidly by kidneys
91
carbachol MOA
non-selective muscarinc agonist
92
carbachol therapeutic use
glaucoma
93
carbachol side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * blurred vision * lacrimation **caution:** * pts w/ asthma/COPD * beta blockers (risk of bronchoconstriction, bradycardia) * hyperthyroid (risk of a-fib)
94
carbechol unique properties
* relatively insensitive to cholinesterases * ophthalmic delivery lowers risk of side effects * short-acting * rapidly eliminated by kidneys
95
methacholine MOA
non-selective muscarinic agonist
96
methacholine therapeutic use
bronchial challenge test for asthma diagnosis
97
methacholine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * bronchoconstriction **caution:** * asthma * COPS * beta blockers (risk of bronchoconstriction, bradycardia) * hyperthyroid (risk of a-fib)
98
methacholine unique properties
* somewhat insensitive to cholinesterases * short-acting * eliminated rapidly by kidneys
99
pilocarpine MOA
non-selective muscarinic agonist
100
pilocarpine therapeutic use
* wide- and narrow-angle glaucoma * xerostomia (after head/neck radiation)
101
pilocarpine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * nausea/vomiting * lacrimation * blurred vision * sweating **cautions:** * pts w/ asthma/COPD * in combo w/ beta-blockers (bronchoconstriction, bradycardia) * gastric ulcers due to increased secretions * hyperthyroid pts (risk of A fib)
102
pilocarpine unique properties
* insensitive to cholinesterases * tertiary amine (can cross BBB)
103
edrophonium MOA
non-covalent acetylcholinesterase competitive inhibitor
104
edrophonium therapeutic use
* diagnostic test for myasthenia gravis * reversal of neuromuscular blockade
105
edrophonium side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * salivation * sweating * nausea * stimulate skeletal muscle **caution:** * asthma/COPD * beta-blockers (bronchoconstriction/bradycardia risks)
106
edrophonium unique properties
* reversibly binds to acetylcholine anionic site * charged, cannot cross BBB * rapid onset, short duration of action * muscarinic effects reduced by atropine-like drugs
107
neostigmine MOA
carbamate acetylcholinesterase inhibitor
108
neostigmine therapeutic use
* ileus and post-op atonic bladder * reversal of neuromuscular blockade * myasthenia gravis
109
neostigmine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * salivation * sweating * nausea * skeletal muscle stimulation **cautions:** * asthma/COPD * beta-blockers (bronchoconstriction/bradycardia) * increase in gastric ulcer secretions
110
neostigmine unique properties
* carbamylates the active site of acetylcholinesterase for 0.5-2 hrs * muscarinic effects can be reduced by atropine-like drugs
111
pyridostigmine MOA
carbamate acetylcholinesterase inhibitor
112
pyridostigmine therapeutic use
myasthenia gravis
113
pyridostigmine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * salivation * sweating * nausea * skeletal muscle stimulation **cautions:** * asthma/COPD * bets-blockers (bronchoconstriction/bradycardia) * increased gastric ulcer secretions
114
pyridostigmine unique properties
* carbamylates active site of acetylcholinesterase for 3-6 hrs * muscarinic effects can be reduced by atropine-like drugs
115
physostigmine MOA
carbamate acetylcholinesterase inhibitor that **can cross BBB**
116
physostigmine therapeutic use
* glaucoma * reversal of anticholinergic intoxication
117
physostigmine side effects/caution/contraindications
**side effects:** * SLUDGE * BBB * salivation * sweating * nausea * skeletal muscle stimulation **cautions:** * asthma/COPD * bets-blockers (bronchoconstriction/bradycardia) * increased gastric ulcer secretions
118
physostigmine unique properties
* carbamylates acetylcholinesterase active site for 0.5-2 hrs * muscarinic effects can be reduced by atropine-like drugs * **crosses BBB; best choice to treat anticholinergic OD**
119
echothiophate MOA
organophosphate irreversible acetylcholinesterase inhibitor
120
echothiophate therapeutic use
glaucoma
121
echothiophate side effects/cautions/contraindications
**side effects:** * SLUDGE * BBB
122
echothiophate unique properties
* forms stable phosphorylated intermediate in acetylcholinesterase active site * 100 hr half life
123
malathion MOA
organophosphate irreversible acetylcholinesterase inhibitor
124
malathion therapeutic use
none; insecticide
125
malathion side effects/cautions/contraindications
**side effects:** * SLUDGE * BBB * muscle fasciculation, paralysis * convulsions * respiratory depression
126
malathion unique properties
* forms stable phosphorylated intermediate in acetylcholinesterase active site * can be detoxified by hydrolysis by plasma carboxylases * can treat poisoing with atropine and pralidoxime (2-PAM)
127
sarin MOA
irreversible organophosphate acetylcholinesterase inhibitor
128
sarin therapeutic use
none; nerve gas/war agent
129
sarin side effects/cautions/contraindications
**side effects:** * SLUDGE * BBB * muscle fasciculation, paralysis * convulsions * respiratory depression
130
sarin unique properties
* forms stable phosphorylated intermediate in acetylcholinesterase active site * rapid aging of phosphorylated acetylcholinesterase * treat poisoning with atropine * 2-PAM/pralidoxime not effective
131
Pralidoxime/2-PAM MOA
acetylcholinesterase reactivator
132
pralidoxime/2-PAM therapeutic use
protection against poisoning of acetylcholinesterase
133
pralidoxime/2-PAM unique properties
* displaces phosphate group of organophosphate to reactivate acetylcholinesterase * **cannot reactivate acetylcholinesterase after aging has occured** * must be given with atropine * cannot cross BBB * can also inhibit acetylcholinesterase itself
134
atropine MOA
muscarinic antagonist
135
atropine therapeutic use
* bradycardia/AV block * mydriasis/cycloplegia * overactive bladder * antisialogogue * antidote for organophosphate poisoning * adjunct in reversal of neuromuscular blockade
136
atropine side effects/cautions/contraindications
**side effects** * anhidrosis * increase in body temperature * blurred vision * dry mouth/eyes * delirium * tachycardia * urinary retention **cautions** * glaucoma * BPH * bladder/GI obstruction * increased sensitivity in children
137
atropine unique properties
* forget all contraindications if using for organophosphate poisoning * treat atropine OD w/ physostigmine
138
scopolamine MOA
muscarinic antagonist
139
scopolamine therapeutic use
motion sickness
140
scopolamine side effects/cautions/contraindications
**side effects** * anhidrosis * increase in body temperature * blurred vision * dry mouth/eyes * delirium * tachycardia * urinary retention **cautions** * glaucoma * BPH * bladder/GI obstruction * increased sensitivity in children
141
scopolamine unique properties
* greater CNS action than atropine * faster onset and longer duration than atropine * treat OD w/ physostigmine
142
ipratropium MOA
muscarinic antagonist
143
ipratropopium therapeutic use
inhaled for COPD/asthma
144
ipratropium side effects/cautions/contraindications
**side effects** * anhidrosis * increase in body temperature * blurred vision * **dry mouth**/eyes * delirium * tachycardia * urinary retention **cautions** * glaucoma * BPH
145
ipratropium unique properties
inhalation reduces severity of side effects when compared to atropine
146
tropicamide MOA
muscarinic antagonist
147
tropicamide therapeutic use
mydriasis/cycloplegia for opththalmic diagnostic procedures
148
tropicamide side effects/cautions/contraindications
**side effects** * anhidrosis * increase in body temperature * blurred vision * dry mouth/eyes * delirium * tachycardia * urinary retention **cautions** * glaucoma (increases intraocular pressure)
149
tropicamide unique properties
topical ophthalmic delivery reduces severity of side effects relative to atropine
150
oxybutynin MOA
muscarinic antagonist
151
oxybutinin therapeutic use
overactive bladder
152
oxybutynin side effects/cautions/contraindications
**side effects** * anhidrosis * increase in body temperature * blurred vision * dry mouth/eyes * delirium * tachycardia * urinary retention **cautions** * **glaucoma** * BPH * bladder/GI obstruction * increased sensitivity in children
153
nicotine MOA
nicotinic acetylcholine receptor agonist/desensitizer

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