Autonomic Drugs Flashcards

1
Q

direct acting muscarinic receptor agonists

A

pilocarpine

bethanechol

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2
Q

direct acting nicotinic receptor agonists

A

succinylcholine

varenicline

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3
Q

indirect acting reversible AchE Inhibitors

A
edrophonium (short acting) 
neostigmine (intermediate acting)
pyridostigmine
physostigmine
donepezil
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4
Q

indirect acting irreversible AchE inhibitors

A

insecticides

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5
Q

AchE Inhibitor Drugs MOA

A

binds to activate site and inhibits AchE, undergoes hydrolysis and acidic portion slowly released. Prevents Ach from binding.

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6
Q

2 main types of reversible AchEI inhibitors

A
  1. alcohol (edrophonium)

2. carbamate (neostigmine)

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7
Q

Irreversible AchE Inhibitor Drugs MOA

A

enzyme active site is phosphorylated, requires synthesis of new AchE to overcome

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8
Q

Clinical Uses of AchE Inhibitors

A
  1. reverse NMB
  2. MG dx and tx
  3. glaucoma
  4. ileus tx
  5. postop urinary retention tx
  6. alzheimers tx
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9
Q

Autonomic AchE Inhibitor Drug Effects

A
  1. increased secretions
  2. increased GI motility
  3. bronchoconstriction
  4. bradycardia
  5. hypotension
  6. miosis
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10
Q

CNS AchE Inhibitor Drug Effects

A

used for dementia tx, toxicity can look like possible convulsions r/t excitation followed by a depression and unconsciousness

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11
Q

Edrophonium chemical structure, type of reversible AchE, effect, route of administration, onset, duration

A
quaternary amine (very polar)
alcohol
reversible blockade
IV, IM
onset 30-60sec
duration 10 minutes
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12
Q

Neostigmine chemical structure, type of reversible AchE, effect, route of administration, onset, duration

A
quaternary amine, moderately polar
carbamate
hydrolyzed by AchE, labile covalent bond
IV, PO?
onset 10-30 min
duration 2-4h
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13
Q

Physostigmine chemical structure, type of reversible AchE, effect, route of administration, onset, duration

A
tertiary amine, nonpolar (crosses BBB)
carbamate
hydrolyzed by AchE, labile covalent bond
PO, IM, IV
onset 3-8min
duration 1 hour
-useful for tx of anticholinergic toxicity
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14
Q

Cholinergic Crisis Pneumonic

A
DUMBELLS:
Diarrhea, Diaphoresis
Urination
Miosis
Bradycardia
Bronchoconstriction
Excitation (of skeletal muscle, CNS), Emesis
Lacrimation
Salivation
Sweating
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15
Q

antidote for cholinergic toxicity

A

atropine

can give pralidoxime to regenerate AchE enzyme if you catch it early

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16
Q

Muscarinic Agonist Drug Effects CV, GI, bladder, lungs, secretions, eye

A

CV: decreased HR, decreased CO and arterial pressure, vasodilation via NO on endothelium of BV
GI: increased motility
Bladder: contraction
Lungs: bronchoconstriction
Secretions: increased
Eye: miosis, accomodati for near vision, decreased IOP

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17
Q

Muscarinic Agonist SE’s Pneumonic

A
SLUDGE
Salivation
Lacrimation
Urination
Diarrhea
GI upset
Emesis
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18
Q

Nicotinic M Antagonist Examples

A
Pancuronium
Atracurium
Vecuronium
Rocuronium
Cisatracurium
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19
Q

Nicotinic N receptor effects, uses, adverse effects

A
  • stimulation of post ganglionic neuronal activity, CNS stimulation
  • smoking cessation (NRT)
  • CNS stimulation, skeletal muscle depolarization, hypertension, increased HR, n/v/diarrhea
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20
Q

Nicotinic M receptor effects, uses, adverse effects

A
  • activated neuromuscular endplates, contraction
  • depolarizing skeletal muscle paralysis
  • fasciculations
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21
Q

cholinergic drug adverse effects and contraindication

A
  • not indicated if GI/GU obstruction
  • CV disease (HTN, increased HR)
  • resp d/o (bronchoconstriction)
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22
Q

nonselective muscarinic antagonist examples

A

atropine
glycopyrrolate
scopalamine

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23
Q

Nicotinic M antagonists

A

Atracurium, Cisatracurium, Vecuronium, Rocuronium, Pancuronium

24
Q

muscarinic receptor antagonist effects (CV, lungs, GI, GU, glands, sweat glands, eye, CNS)

A
increased HR
bronchodilator
decreased GI stimulation
decreased GU stimulation
decreased sweat gland stimulation
mydriasis
sedation
25
Q

muscarinic antagonist uses

A
motion sickness
parkinsons
eye exams
decreased pulmonary secretions
COPD, asthma
GI hyper motility
urinary urgency
26
Q

would you expect effects from muscarinic receptor agonist at blood vessels or skeletal muscle

A

for BV, no with antagonist but yes with nAchR agonist

for skeletal muscle, no because theres only nAchR receptors

27
Q

atropine structure, half life, route of administration, uses

A

tertiary amine, lipophilic, crosses BBB
t1/2 about 4 hours (eye effects last for days)
IV, IM
used for ophthalmic, bradycardia, preop to inhibit secretions, NM reversal

28
Q

scopolamine structure, half life, route of administration, uses

A

tertiary amine, crosses BBB
half life 1-4h, onset 10 min, duration 2 hours
transdermal patch, IV, IM
uses include motion sickness, PONV, preop for amnesia or sedation

29
Q

glycopyrrolate structure, half life, route of administration, uses

A

quaternary amine, decreased CNS effects
half life 1 hour, onset 1 minute, duration 7 hours (IV)
IV, PO
uses preop: dysrhythmia, or reversal of NMB adjunct

30
Q

anticholinergic effects memory aid

A

dry as a bone (dry mouth, urinary run), hot as a pistol, red as a beet (cannot sweat so hyperthermic), blind as a bat (r/t pupil dilation), mad as a hatter (r/t confusion and delirium)

31
Q

antimuscarinic drug potential concerns

A

hyperthermia risk (esp in infants, children)
glaucoma
GU obstruction
prostatic hypertrophy
CV: esp myocardial ischemia, HF, certain arrhythmias, HTN
GI: ileus, UC

32
Q

med classes with anticholinergic activity (7)

A
antihistamines
antispasmodics
antiparkinson drugs
skeletal muscle relaxants
antipsychotics
antidepressants (usually older ones, not SSRI's)
antimuscarinics for urinary incontinence
33
Q

direct acting adrenergic alpha agonists (nonselective, a1, a2)

A

norepinephrine

a1: phenylephrine
a2: clonidine, dexmedetomidine

34
Q

direct acting adrenergic beta agonists (nonselective, B1, B2)

A

isoproterenol
B1: dobutamine
B2: albuterol

35
Q

direct acting adrenergic mixed receptor medications

A

epinephrine, norepinephrine

36
Q

indirect acting adrenergic neurotransmitter releaser

A

amphetamines, or ephedrine (mixed action drug)

37
Q

indirect acting adrenergic NE reuptake inhibitor

A

cocaine, SNRI

38
Q

indirect acting adrenergic MAOI

A

tranylcypromine, slegiline (prevent NE breakdown, located within nerve terminal)

39
Q

Ephedrine mixed action

A

displaces/releases stored catecholamine NT

40
Q

Amphetamine mixed action

A

displaces/releases stored catecholamine NT,
inhibits catecholamine reuptake (NE, DA)
(uses in narcolepsy, ADHD, appetite suppression)

41
Q

Cocaine MOA

A

blocks NE reuptake by inhibiting NE/DA transporters, blocks Na channels-local anesthetic actions

42
Q

Tyramine MOA

A

displaces/releases stored catecholamines. not a drug, in fermented foods (pickled things, aged wine). this gets taken up by storage vesicles and pushes out NE. hypertensive crisis possible.

43
Q

MAOI effect on adrenergic drugs, types of MAO

A

prevents breakdown of catecholamines in presynaptic terminal-catecholamine accumulates in vescicles/
MAO-A metabolizes NE
MAO-B metabolizes DA

44
Q

epinephrine receptor action, uses

A

a1, a2, b1, b2, b3

used in anaphylaxis, with local anesthetics, during cardiac arrest

45
Q

NE (the actual drug) receptor action, uses

A

a1, b1 (little effect on B1)
used in shock
(tissue necrosis r/t extravasation possible)

46
Q

Isoproterenol receptor action, uses

A
B1, B2
acute asthma (obsolete r/t B2 specific drugs), cardiac stimulant
47
Q

dopamine receptor action, uses

A

D1 in renal, mesenteric, coronary, vascular beds (low dose)
B1 medium doses, A1, high doses
used in shock, HF, increased BF to kidneys

48
Q

dobutamine receptor action, uses

A

B1 primarily

acute HF

49
Q

alpha receptor affinity of epi, iso, NE

A

epi>NE>iso

50
Q

beta receptor affinity of epi, iso, NE

A

iso>epi>NE

51
Q

dexmedetomidine receptor affinity, MOA, effects, CV/resp SE, uses

A

selective a2 receptor agonist, suppresses SNS activity
sedative effects in locus coeruleus, analgesic effects (SC)
CV: decrease in HR and SVR, hypotension, transient HTN with bolus dose
Resp: some decrease in TV
tolerance, tachyphylaxis, withdrawal sx possible
used in ICU for sedation, adjunct to general anesthesia

52
Q

adrenergic agonist potential concerns

A
CV disease
cerebrovascular disease
other r/t vasoconstriction
DM or increase BG
IV extravasation risks
thyroid disease
53
Q

adrenergic alpha blockers nonselective, a1, a2

A

nonselective: phenoxybenzamine, phentolamine
a1: prazosin
a2: yohimbine

54
Q

adrenergic beta blockers nonselective, B1

A

nonselective: propanolol
b1: metoprolol, esmolol

55
Q

when are nonselective BB contraindicated?

A

COPD, asthma, airway diseases

56
Q

a1 antagonist effects, clinical uses, SE

A

smooth muscle relaxation, decrease in PVR, decrease in BP
uses: HTN, BPH, pheochromocytoma
SE: reflex tachycardia, first dose effect r/t major orthostatic hypotension, nasal congestion

57
Q

b1 (+B2) antagonist effects, clinical uses, SE:

A

decreased HR, force of contraction, renin release. antidysrhythmic effects
uses: HTN, angina, arrhythmia, MI, thyrotoxicosis (r/t hyperthyroidism), HR (chronic, stable), glaucoma, anxiety
SE: B2 bronchoconstricts, arrhythmia or bradycardia possible, sedation CNS, decreased sexual fxn, B2 blocks glycogenolysis (liver)