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block 2 > DRUGS! > Flashcards

DRUGS! Flashcards

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
Q

phenylephrine side effects/cautions/contraindications

A

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

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26
Q

phenylephrine unique properties

A

related to midordrine which is used for orthostatic HTN

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27
Q

clonadine MOA and effects

A

selective a2 agonist
decreases:
* sympathetic nervous system effects
* NT release (feedback inhibition)
* PVR
* BP

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28
Q

clonidine therapeutic use

A
  • HTN
  • anesthesia (decreases CNS activity, pain)
  • ADHD
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29
Q

clonidine side effects/cautions/contraindications

A

side effects:
* sedation
* dry mouth
* orthostatic hypotension

cautions
* must discontinue slowly to avoid rebound HTN

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30
Q

clonidine unique properties

A

can produce transient initial vasocontriction but ultimately leads to decreased SNS tone and lowered BP

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31
Q

mirabegron MOA and effects

A

b3 agonist
* relaxes detrusor muscle to allow filling

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32
Q

mirabegron therapeutic use

A

overactive bladder

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33
Q

mirabegron side effects/caution/contraindications

A

side effects:
* HTN
* dizziness
* headaches

caution:
* in pts with poorly controlled HTN

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34
Q

mirabegron unique properties

A

alternative to antimuscarinics for OAB in pts w cognitive impairment

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35
Q

cocaine MOA and effects

A
  • blocks dopmine, norepinephrine, and serotonin transporters
  • inhibits voltage-gated sodium channels (local anesthetic)
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36
Q

cocaine therapeutic use

A
  • local anesthetic for ENT procedures
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37
Q

cocaine side effects/caution/contraindications

A
  • CV stimulation
  • arrythmias
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38
Q

amphetamine MOA and effects

A
  • 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
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39
Q

amphetamine therapeutic uses

A
  • ADHD
  • narcolepsy
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40
Q

amphetamine side effects/caution/contraindications

A

side effects
* appetite/growth suppression
* unmasking of motor tics
* HTN
* arrythmias
caution:
* reports of sudden death in pts w/ conduction defects

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41
Q

amphetamine unique properties

A

prone to abuse

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42
Q

tyramine MOA and effects

A
  • 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
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43
Q

tyramine therapeutic use

A

none

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44
Q

tyramine side effects/caution/contraindications

A

side effects:
* HTN crisis when combined with MAOI

caution:
* dietary restrictions in pts taking MAOIs

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45
Q

tyramine unique properties

A
  • normally metabolized by MAO
  • found in cheese, beer, wine, aged meats
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46
Q

ephedrine/pseudoephedrine MOA and effects

A
  • a and b agonist
  • moderately enhances NE release
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47
Q

ephedrine/pseudoephedrine therapeutic uses

A
  • decongestant
  • mydriatic
  • hypotension
  • (asthma)
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48
Q

ephedrine/pseudoephedrine side effects/caution/contraindications

A

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

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49
Q

ephedrine/pseudephedrine unique properties

A
  • herbal supplements w/ ephedra/ephedrine banned by FDA for adverse CV events
  • pseudoephedrine very limites OTC access
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50
Q

phentolamine MOA and effects

A

a1, a2 antagonist

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51
Q

phentolamine therapeutic use

A
  • pheochromocytoma (adrenal tumor)
  • HTN crisis
  • extravsation of vasoconstrictors
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52
Q

phentolamine side effects/caution/contraindications

A

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

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53
Q

phenoxybenzamine MOA

A

a1, a2 antagonist (nonselective)

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54
Q

phenoxybenzamine therapeutic use

A
  • HTN crises in pheochromocytoma pts
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55
Q

phenoxybenzamine side effects/caution/contraindications

A

side effects:
* orthostatic hypotension
* tachycardia (can lead to ischemia)
* nasal congestion
caution:
* in pts w/ angina, history of MI/coronary artery disease

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56
Q

phenoxybenzamine unique properties

A

irreversible/insurmountable antagonist of a1/a2 (permanent flattened curve)

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57
Q

prazosin MOA and effects

A

competitive a1 antagonist

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58
Q

prazosin therapeutic use

A
  • HTN
  • BPH
  • PTSD (off label)
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59
Q

prazosin side effects/caution/contraindications

A

side effects:
* orthostatic hypotension
* tachycardia

cautions:
* angina

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60
Q

tamsulosin MOA and effects

A

a1 a/d (most affinity) or a1b (secondary) antagonist

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61
Q

tamsulosin therapeutic use

A

BPH

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62
Q

tamsulosin side effects/caution/contraindications

A

side effects:
* orthostatic hypotension
* tachycardia

63
Q

tamsulosin unique properties

A

most selective for a1a receptor (in prostate)

64
Q

propranolol MOA and effects

A
  • b1 and b2 antagonist
  • inhibits Na+ channels at high doses
65
Q

propranolol therapeutic use

A
  • hypertension
  • angina
  • post-MI
  • some arrythmias
  • hyperthyroid
  • migraine
  • performance anxiety
66
Q

propranolol side effects/caution/contraindications

A

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
Q

propanolol unique properties

A

inhibits sodium channels at high doses

68
Q

timolol MOA and effects

A

b1/b2 antagonist

69
Q

timolol therapeutic use

A
  • wide angle glaucoma (decreases AH production)
  • HTN
  • post-MI
  • migraine
70
Q

timolol side effects/caution/contraindications

A

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
Q

metoprolol MOA

A

“cardioselective” b1 antagonist

72
Q

metoprolol therapeutic use

A
  • HTN
  • angina
  • post-MI
  • some arrythmias
  • congestive heart failure
73
Q

metoprolol side effects/caution/contraindications

A

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
Q

metoprolol unique properties

A
  • proven to decrease CHF-related mortality
  • lower risk of lipid abnormalities
  • safer for diabetic pts
  • safer for pts w/ asthma/COPD
75
Q

esmolol MOA

A

cardioselective b1 antagonist (very short acting)

76
Q

esmolol therapeutic use

A
  • intraoperative control of tachycardia/HTN
  • SVT (arrythmia)
77
Q

esmolol side effects/caution/contraindications

A

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
Q

esmolol unique properties

A
  • metabolized by esterases on RBCs
  • duration of action only 5-10 minutes
79
Q

carvedilol/labetalol MOA

A

b1/b2/a1 antagonist

80
Q

carvedilol/labetalol therapeutic use

A
  • HTN
  • HTN emergency (labetalol)
  • heart failure/CHF (carvedilol)
  • post-MI
81
Q

carvedilol/labetolol side effects/caution/contraindications

A

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
Q

labetalol unique properties

A

often used in pregnant pts w/ HTN (preeclampsia)

83
Q

acetylcholine MOA

A

nonselective muscarinic agonist

84
Q

acetylcholine therapeutic use

A

none (rapidly degraded by cholinesterases)

85
Q

acetylcholine side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB

86
Q

acetylcholine unique properties

A

IV administration can cause transient vasodilation via NO produced by endothelium

87
Q

bethanechol MOA

A

non-selective muscarinic agonist

88
Q

bethanechol therapeutic use

A
  • post-op ileus (bowel obstruction)
  • urinary retention
89
Q

bethanechol side effects/caution/contraindications

A

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
Q

bethanechol unique properties

A
  • relatively insensitive to cholinesterases
  • short-acting
  • eliminated rapidly by kidneys
91
Q

carbachol MOA

A

non-selective muscarinc agonist

92
Q

carbachol therapeutic use

A

glaucoma

93
Q

carbachol side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* blurred vision
* lacrimation

caution:
* pts w/ asthma/COPD
* beta blockers (risk of bronchoconstriction, bradycardia)
* hyperthyroid (risk of a-fib)

94
Q

carbechol unique properties

A
  • relatively insensitive to cholinesterases
  • ophthalmic delivery lowers risk of side effects
  • short-acting
  • rapidly eliminated by kidneys
95
Q

methacholine MOA

A

non-selective muscarinic agonist

96
Q

methacholine therapeutic use

A

bronchial challenge test for asthma diagnosis

97
Q

methacholine side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* bronchoconstriction

caution:
* asthma
* COPS
* beta blockers (risk of bronchoconstriction, bradycardia)
* hyperthyroid (risk of a-fib)

98
Q

methacholine unique properties

A
  • somewhat insensitive to cholinesterases
  • short-acting
  • eliminated rapidly by kidneys
99
Q

pilocarpine MOA

A

non-selective muscarinic agonist

100
Q

pilocarpine therapeutic use

A
  • wide- and narrow-angle glaucoma
  • xerostomia (after head/neck radiation)
101
Q

pilocarpine side effects/caution/contraindications

A

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
Q

pilocarpine unique properties

A
  • insensitive to cholinesterases
  • tertiary amine (can cross BBB)
103
Q

edrophonium MOA

A

non-covalent acetylcholinesterase competitive inhibitor

104
Q

edrophonium therapeutic use

A
  • diagnostic test for myasthenia gravis
  • reversal of neuromuscular blockade
105
Q

edrophonium side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* salivation
* sweating
* nausea
* stimulate skeletal muscle

caution:
* asthma/COPD
* beta-blockers (bronchoconstriction/bradycardia risks)

106
Q

edrophonium unique properties

A
  • reversibly binds to acetylcholine anionic site
  • charged, cannot cross BBB
  • rapid onset, short duration of action
  • muscarinic effects reduced by atropine-like drugs
107
Q

neostigmine MOA

A

carbamate acetylcholinesterase inhibitor

108
Q

neostigmine therapeutic use

A
  • ileus and post-op atonic bladder
  • reversal of neuromuscular blockade
  • myasthenia gravis
109
Q

neostigmine side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* salivation
* sweating
* nausea
* skeletal muscle stimulation

cautions:
* asthma/COPD
* beta-blockers (bronchoconstriction/bradycardia)
* increase in gastric ulcer secretions

110
Q

neostigmine unique properties

A
  • carbamylates the active site of acetylcholinesterase for 0.5-2 hrs
  • muscarinic effects can be reduced by atropine-like drugs
111
Q

pyridostigmine MOA

A

carbamate acetylcholinesterase inhibitor

112
Q

pyridostigmine therapeutic use

A

myasthenia gravis

113
Q

pyridostigmine side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* salivation
* sweating
* nausea
* skeletal muscle stimulation

cautions:
* asthma/COPD
* bets-blockers (bronchoconstriction/bradycardia)
* increased gastric ulcer secretions

114
Q

pyridostigmine unique properties

A
  • carbamylates active site of acetylcholinesterase for 3-6 hrs
  • muscarinic effects can be reduced by atropine-like drugs
115
Q

physostigmine MOA

A

carbamate acetylcholinesterase inhibitor that can cross BBB

116
Q

physostigmine therapeutic use

A
  • glaucoma
  • reversal of anticholinergic intoxication
117
Q

physostigmine side effects/caution/contraindications

A

side effects:
* SLUDGE
* BBB
* salivation
* sweating
* nausea
* skeletal muscle stimulation

cautions:
* asthma/COPD
* bets-blockers (bronchoconstriction/bradycardia)
* increased gastric ulcer secretions

118
Q

physostigmine unique properties

A
  • 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
Q

echothiophate MOA

A

organophosphate irreversible acetylcholinesterase inhibitor

120
Q

echothiophate therapeutic use

A

glaucoma

121
Q

echothiophate side effects/cautions/contraindications

A

side effects:
* SLUDGE
* BBB

122
Q

echothiophate unique properties

A
  • forms stable phosphorylated intermediate in acetylcholinesterase active site
  • 100 hr half life
123
Q

malathion MOA

A

organophosphate irreversible acetylcholinesterase inhibitor

124
Q

malathion therapeutic use

A

none; insecticide

125
Q

malathion side effects/cautions/contraindications

A

side effects:
* SLUDGE
* BBB
* muscle fasciculation, paralysis
* convulsions
* respiratory depression

126
Q

malathion unique properties

A
  • 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
Q

sarin MOA

A

irreversible organophosphate acetylcholinesterase inhibitor

128
Q

sarin therapeutic use

A

none; nerve gas/war agent

129
Q

sarin side effects/cautions/contraindications

A

side effects:
* SLUDGE
* BBB
* muscle fasciculation, paralysis
* convulsions
* respiratory depression

130
Q

sarin unique properties

A
  • forms stable phosphorylated intermediate in acetylcholinesterase active site
  • rapid aging of phosphorylated acetylcholinesterase
  • treat poisoning with atropine
  • 2-PAM/pralidoxime not effective
131
Q

Pralidoxime/2-PAM MOA

A

acetylcholinesterase reactivator

132
Q

pralidoxime/2-PAM therapeutic use

A

protection against poisoning of acetylcholinesterase

133
Q

pralidoxime/2-PAM unique properties

A
  • 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
Q

atropine MOA

A

muscarinic antagonist

135
Q

atropine therapeutic use

A
  • bradycardia/AV block
  • mydriasis/cycloplegia
  • overactive bladder
  • antisialogogue
  • antidote for organophosphate poisoning
  • adjunct in reversal of neuromuscular blockade
136
Q

atropine side effects/cautions/contraindications

A

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
Q

atropine unique properties

A
  • forget all contraindications if using for organophosphate poisoning
  • treat atropine OD w/ physostigmine
138
Q

scopolamine MOA

A

muscarinic antagonist

139
Q

scopolamine therapeutic use

A

motion sickness

140
Q

scopolamine side effects/cautions/contraindications

A

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
Q

scopolamine unique properties

A
  • greater CNS action than atropine
  • faster onset and longer duration than atropine
  • treat OD w/ physostigmine
142
Q

ipratropium MOA

A

muscarinic antagonist

143
Q

ipratropopium therapeutic use

A

inhaled for COPD/asthma

144
Q

ipratropium side effects/cautions/contraindications

A

side effects
* anhidrosis
* increase in body temperature
* blurred vision
* dry mouth/eyes
* delirium
* tachycardia
* urinary retention

cautions
* glaucoma
* BPH

145
Q

ipratropium unique properties

A

inhalation reduces severity of side effects when compared to atropine

146
Q

tropicamide MOA

A

muscarinic antagonist

147
Q

tropicamide therapeutic use

A

mydriasis/cycloplegia for opththalmic diagnostic procedures

148
Q

tropicamide side effects/cautions/contraindications

A

side effects
* anhidrosis
* increase in body temperature
* blurred vision
* dry mouth/eyes
* delirium
* tachycardia
* urinary retention

cautions
* glaucoma (increases intraocular pressure)

149
Q

tropicamide unique properties

A

topical ophthalmic delivery reduces severity of side effects relative to atropine

150
Q

oxybutynin MOA

A

muscarinic antagonist

151
Q

oxybutinin therapeutic use

A

overactive bladder

152
Q

oxybutynin side effects/cautions/contraindications

A

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
Q

nicotine MOA

A

nicotinic acetylcholine receptor agonist/desensitizer

block 2 (5 decks)

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