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Pharmacology N929 > Autonomic Drugs > Flashcards

Autonomic Drugs Flashcards

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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

Study These Flashcards
A

Atracurium, Cisatracurium, Vecuronium, Rocuronium, Pancuronium

24
Q

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

Study These Flashcards
A 
increased HR
bronchodilator
decreased GI stimulation
decreased GU stimulation
decreased sweat gland stimulation
mydriasis
sedation
25
muscarinic antagonist uses
``` motion sickness parkinsons eye exams decreased pulmonary secretions COPD, asthma GI hyper motility urinary urgency ```
26
would you expect effects from muscarinic receptor agonist at blood vessels or skeletal muscle
for BV, no with antagonist but yes with nAchR agonist | for skeletal muscle, no because theres only nAchR receptors
27
atropine structure, half life, route of administration, uses
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
scopolamine structure, half life, route of administration, uses
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
glycopyrrolate structure, half life, route of administration, uses
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
anticholinergic effects memory aid
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
antimuscarinic drug potential concerns
hyperthermia risk (esp in infants, children) glaucoma GU obstruction prostatic hypertrophy CV: esp myocardial ischemia, HF, certain arrhythmias, HTN GI: ileus, UC
32
med classes with anticholinergic activity (7)
``` antihistamines antispasmodics antiparkinson drugs skeletal muscle relaxants antipsychotics antidepressants (usually older ones, not SSRI's) antimuscarinics for urinary incontinence ```
33
direct acting adrenergic alpha agonists (nonselective, a1, a2)
norepinephrine a1: phenylephrine a2: clonidine, dexmedetomidine
34
direct acting adrenergic beta agonists (nonselective, B1, B2)
isoproterenol B1: dobutamine B2: albuterol
35
direct acting adrenergic mixed receptor medications
epinephrine, norepinephrine
36
indirect acting adrenergic neurotransmitter releaser
amphetamines, or ephedrine (mixed action drug)
37
indirect acting adrenergic NE reuptake inhibitor
cocaine, SNRI
38
indirect acting adrenergic MAOI
tranylcypromine, slegiline (prevent NE breakdown, located within nerve terminal)
39
Ephedrine mixed action
displaces/releases stored catecholamine NT
40
Amphetamine mixed action
displaces/releases stored catecholamine NT, inhibits catecholamine reuptake (NE, DA) (uses in narcolepsy, ADHD, appetite suppression)
41
Cocaine MOA
blocks NE reuptake by inhibiting NE/DA transporters, blocks Na channels-local anesthetic actions
42
Tyramine MOA
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
MAOI effect on adrenergic drugs, types of MAO
prevents breakdown of catecholamines in presynaptic terminal-catecholamine accumulates in vescicles/ MAO-A metabolizes NE MAO-B metabolizes DA
44
epinephrine receptor action, uses
a1, a2, b1, b2, b3 | used in anaphylaxis, with local anesthetics, during cardiac arrest
45
NE (the actual drug) receptor action, uses
a1, b1 (little effect on B1) used in shock (tissue necrosis r/t extravasation possible)
46
Isoproterenol receptor action, uses
``` B1, B2 acute asthma (obsolete r/t B2 specific drugs), cardiac stimulant ```
47
dopamine receptor action, uses
D1 in renal, mesenteric, coronary, vascular beds (low dose) B1 medium doses, A1, high doses used in shock, HF, increased BF to kidneys
48
dobutamine receptor action, uses
B1 primarily | acute HF
49
alpha receptor affinity of epi, iso, NE
epi>NE>iso
50
beta receptor affinity of epi, iso, NE
iso>epi>NE
51
dexmedetomidine receptor affinity, MOA, effects, CV/resp SE, uses
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
adrenergic agonist potential concerns
``` CV disease cerebrovascular disease other r/t vasoconstriction DM or increase BG IV extravasation risks thyroid disease ```
53
adrenergic alpha blockers nonselective, a1, a2
nonselective: phenoxybenzamine, phentolamine a1: prazosin a2: yohimbine
54
adrenergic beta blockers nonselective, B1
nonselective: propanolol b1: metoprolol, esmolol
55
when are nonselective BB contraindicated?
COPD, asthma, airway diseases
56
a1 antagonist effects, clinical uses, SE
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
b1 (+B2) antagonist effects, clinical uses, SE:
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)

Pharmacology N929 (11 decks)

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