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Year 2 Pharmacology > Autonomic pharmacology II > Flashcards

Autonomic pharmacology II Flashcards

1
Q

what is the effect of M3 receptor activation on glands?

A

secretion - sweat, salivation, lacrimation

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2
Q

what is the effect of M3 receptor activation on sphincters?

A

mostly relaxation with the exception of lower esophageal sphincter

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3
Q

what is the effect of Nn receptor activation on the adrenal medulla?

A

secretion of EPI and NE

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4
Q

what is the effect of Nn receptor activation on the autonomic ganglia?

A

stimulation - net effects dependent on PANS/SNS innervation and dominance

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5
Q

what is the effect of Nm receptor activation on the neuromuscular junction?

A

stimulation - twitch / hyperactivity of skeletal muscle

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6
Q

what is the mechanism of direct acting cholinomimetics?

A

bind directly to and activate mucarinic or nicotinic cholinoceptors

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7
Q

what is the mechanism of indirect acting cholinomimetics?

A

produce their effects by inhibiting the action of AchE thus preventing destruction of endogenous Ach

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8
Q

what are the direct acting cholinoceptor agonists that act on M receptors (choline esters)?

A
  1. Ach
  2. methacholine
  3. carbachol
  4. bethanechol
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9
Q

how does the cationic quaternary ammonium group affect the choline ester metabolism?

A
  1. poor GI absorption

2. poor CNS distribution

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10
Q

how does the presence of methacholine’s methyl group affect its half life?

A

increase

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11
Q

how does the presence of carbachol’s and bethanechol’s amine group affect its metabolism?

A

insusceptible to cholinesterase

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12
Q

what is the clinical use for methacholine?

A

Dx - bronchial hyperactivity

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13
Q

what is the clinical use for carbachol?

A

Rx - glaucoma

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14
Q

what is the clinical use for bethanechol?

A

Rx - ileus, urinary retention

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15
Q

what are the muscarinic effects of Ach on the heart?

A
  1. vasodilation - reflex tachcardia (low doses)

2. bradycardia, decreased AV conduction, inotropy (high doses)

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16
Q

what are the muscarinic effects of Ach on the lungs?

A
  1. bronchial constriction

2. increased bronchial secretion

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17
Q

what are the muscarinic effects of Ach on glands?

A

salivary excretion, tears, sweat

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18
Q

what are the muscarinic effects of Ach on the bladder?

A

contraction

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19
Q

what are the muscarinic effects of Ach on the eye?

A

short lasting miosis

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20
Q

what are the nicotinic effects of Ach?

A

not normally seen - cannot penetrate fat surrounding skeletal muscle and autonomic ganglia

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21
Q

what are the clinical uses of Ach?

A
  1. eye surgery (short lasting miosis)

2. provocation testing in coronary angiography (Dx coronary vasospasm)

22
Q

what are the clinical uses for methacholine?

A

diagnosis of bronchiolar hypersensitivity - excessive bronchoconstriction via M3 receptors in asthmatic patients

23
Q

what are the effects of therapeutic doses of carbachol?

A

activate both nicotinic and muscarinic cholinoceptors

nicotinic effects on autonomic ganglia, adrenal medulla, skeletal muscle

24
Q

what are the effects of high doses of carbachol?

A

cardiac arrest

25
Q

what are the clinical uses of carbachol?

A

glaucoma

  1. contracts ciliary muscle
  2. enlarges Canal of Schlemm
  3. increases drainage of aqeuous humor
  4. decreases intraocular pressure
26
Q

bethanechol acts primarily on what type of receptor?

A

M3

27
Q

what is the effect of bethanechol on the GU system?

A
  1. increase detrusor tone

2. decrease outlet resistance of internal sphincter

28
Q

what is the effect of bethanechol on the GI system?

A

increase motility and secretion

29
Q

what are the effects of bethanechol on the heart (M2 receptors)?

A

weak / minimal effect

30
Q

what are the indications for bethanechol use?

A
  1. gastric atony
  2. gastric emptying abnormalities
  3. urinary retention (in absence of obstruction)
31
Q

what are the direct acting cholinoceptor agonists that act on M receptors (alkaloids)?

A
  1. muscarine

2. pilocarpine

32
Q

what are the symptoms of muscarine poisoning?

A
  1. salivation, swear, lacrimation
  2. abdominal pain, nausea, diarrhea, blurred vision, dyspnea
  3. symptoms generally subside within 2 hours
  4. severe cases - cardiac and respiratory failure may lead to death
33
Q

what are the primary effects of pilocarpine?

A

opthalmic

  1. contracts sphincter pupillae - miosis
  2. opens Canal of Schlemm
  3. enhances tone of trabecular network
  4. contracts ciliary muscle - accommodation
34
Q

what are the clinical uses for pilocarpine?

A
  1. glaucoma Rx of choice

2. test on autonomic state

35
Q

what are contraindications for direct acting cholinoceptor agonists?

A
  1. peptic ulcers
  2. GI tract disorders
  3. asthma
36
Q

what are the main drug interactions with direct acting cholinoceptor agonists?

A
  1. quinidine - antiarrhythmics
  2. procainamide - antiarrhthmics
  3. tricyclic antidepressants
37
Q

what are the direct acting cholinoceptor agonists that act on nicotinic receptors (alkaloids)?

A
  1. nicotine

2. succinylcholine

38
Q

what are the effects of nicotine on Nm receptors?

A
  1. skeletal muscle contraction
  2. fasciculations, spasm
  3. depoloarizing blockade
39
Q

what are the nicotinic effects of Nm receptor activation on the heart?

A

increased HR (mostly SNS)

40
Q

what are the nicotinic effects of Nn receptor activation on the vasculature?

A

peripheral vasoconstriction (mostly PNS)

41
Q

what are the nicotinic effects of Nn receptor activation on the GI system?

A

increased gut motility and secretion

42
Q

what are the nicotinic effects of Nn receptor activation on the carotid bodies?

A

increased respiratory rate

43
Q

what are the nicotinic effects of Nn receptor activation on the medullary emetic chemoreceptors?

A

nausea and vomiting

44
Q

what are the clinical uses for edrophonium?

A

Dx - myasthenia gravis

45
Q

what are the clinical uses for neostigmine and pyridostigmine?

A

Rx - ileus, urinary retention, myasthenia, reversal of non-depolarizing NM blockers

46
Q

what are the clinical uses for physostigmine?

A

Rx - glaucoma, antidote in atropine overdose

47
Q

what are the clinical uses for donepezil tacrine?

A

Rx - Alzheimer disease

48
Q

what are the clinical uses for organophosphates?

A

Rx - glaucoma, insecticides, nerve gas

49
Q

what are the symptoms of cholinesterase inhibitor toxicity?

A

DUMBBELSS

  1. Diarrhea
  2. Urination
  3. Miosis
  4. Bronchiolar constriction
  5. Bradycardia
  6. Excitement
  7. Lacrimation
  8. Sweating
  9. Salivation
50
Q

what is the antidote for cholinesterase inhibitor toxicity?

A

atropine - muscarinic receptor antagonist

51
Q

what is the function of pralidoxim?

A

regeneration of AchE following cholinesterase intoxication

Year 2 Pharmacology (70 decks)

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