Ch. 10: Cholinergic Drugs Flashcards

1
Q

what do anticholinesterase agents do? How do they differ from antagonists?

A

block the degradation of Ach. Their action is similar to direct-acting agonists, just indirect. Differ from antagonists in that they do not interact with/block receptor

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2
Q

T/F: atropine comes from natural sources

A

T

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3
Q

Primary NT of parasympathetic side of ANS

A

Ach

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4
Q

2 broad classes of receptors that Ach works on

A

nicotinic and muscarinic

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5
Q

primary mech. of transmission between somatic motor neuron and target skeletal muscle

A

Ach action on nicotinic receptors

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6
Q

major sites where Ach actions are mediated via muscarinic receptors***

A

CNS and visceral organs. “recognize that agents that act on muscarinic receptors can also act on CNS”

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7
Q

what receptors does carbechol act on?

A

nicotinic and muscarinic

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8
Q

N-butylammonium come from natural source?

A

yes

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9
Q

bethanechol natural or synthetic?

A

synthetic

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10
Q

bethanechol acts on what receptor(s)?

A

muscarinic (selective)

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11
Q

carbechol acts on what receptor(s)?

A

muscarinic and nicotinic (nonselective)

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12
Q

Acetylcholine acts on what receptor(s)?

A

muscarinic and nicotinic (nonselective)

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13
Q

2 broad classifications of cholinergic receptors?**

A

muscarinic and nicotinic

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14
Q

T/F: all cholinergic receptors are stimulated by Ach?

A

T

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15
Q

muscle relaxants typically target what receptors?

A

nicotinic receptors in skeletal muscle

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16
Q

what are muscarinic receptors stimulated by?

A

natural alkaloid muscarine

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17
Q

what are nicotinic receptors stimulated by?

A

natural plant alkaloid nicotine

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18
Q

What does SLUD stand for? What causes it?

A

salivation, lacrimation, urination, defecation. Caused by excess parasympathetic nervous system stimulation

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19
Q

Ach is a physiological antagonist of what NT?***

A

NE and EP

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20
Q

A MAJOR consequence of PS activation or mAChR stimulation

A

GI stimulation (motility, secretions, relaxation of sphincters)

21
Q

T/F: horses are very susceptible to Anticholinergic drugs

A

T

22
Q

What are prokinetic agents? What are they used for?

A

cholinergic agonists. Good for tx of constipation, impaction

23
Q

What are spasmolytics/antispasmotics? What are they used for?

A

anticholinergics (cholinergic antagonist). Tx of GI spasms

24
Q

parasympathetic stimulation of mAChR receptors promotes/inhibits secretions from most secretory glands?

A

promotes

25
Q

What agents promote stimulation of secretory glands?

A

cholinergic agonists and AchE agents

26
Q

Do anticholinergic drugs promote or inhibit stim. of secretory glands? What is a clinical problem of this?

A

inhibit. Can interfere with normal sweating, leading to hyperthermia in warm environments

27
Q

What is a rationale for using anticholinergic agents during anesthesia?**

A

to counteract increased respiratory tract secretions, bronchoconstriction, and respiratory center inhibition from drugs that activate muscarinic receptors on parasympathetic side

28
Q

muscarinic activation –> respiratory system

A

bronchoconstriction

29
Q

muscarinic activation via agonist –> eye

A

-pupil constriction

30
Q

muscarinic activation via antagonist –> eye

A

pupil dilation

31
Q

mAChR activation causes 2 main mechanical changes in eye

A

contraction of sphincter muscle and ciliary muscle

32
Q

mAChR activation –> cardiac tissue

A

decreased HR, with reduced contractility and impulse conduction to a lesser extent. Due to increased K conductance in pacemaker cells

33
Q

mAChR activation –> blood vessels

A

vasodilation, decreased BP

34
Q

Where does most parasympathetic innervation to blood vessels lie?

A

on the endothelial cells surrounding vessels, NOT on the vascular smooth muscle of the vessel itself

35
Q

Carbachol

A
  • cholinergic agonist
  • mixed N/M agonist
  • not used anymore; very potent; GI stimulant and bladder contraction
  • resistant to cholinesterase degredation
36
Q

Bethanechol

A
  • cholinergic agonist
  • muscarinic agonist
  • less potent than carbachol
  • GI stimulant, contract bladder
  • resistant to AChE deg.
37
Q

contraindications of bethanechol

A

known urinary tract obstruction, GI obstruction, asthma, resp. disease, GI ulcers

38
Q

What is the purpose of combining bethanechol with an alpha-adrenergic blocking agent?

A

contraction of sphincter is inhibited while contraction of smooth muscle inside the bladder is stimulated; helps void the bladder

39
Q

pilocarpine

A

natural muscarinic agonist. Used to treat glaucoma and KCS

40
Q

3 natural muscarinic agonists

A

muscarine, pilocarpine, arecoline

41
Q

treat SLUD syndrome with:

A

atropine w/wo EP and support

42
Q

contraindications of cholinergic agonists**

A
asthma,COPD, pulm. dz
GI/urinary tract obstruction
GI ulcer
hyperthyroidism
coronary insufficiency
pregnancy
43
Q

atropine is a mild CNS depressant/stimulant

A

depressant. It is a cholinergic antagonist

44
Q

T/F: atropine crosses BBB

A

True!

45
Q

N-butylscopolammonium Bromide

A
  • cholinergic (competitive) antagonist
  • targets muscarinic receptors
  • antispasmotic agent, aid for rectal exam
  • no BBB cross
46
Q

Glycopyrrolate

A
  • cholinergic antagonist
  • targets muscarinic receptors
  • similar but less potent than atropine
47
Q

Summary of therapeutic uses for anti-cholinergic agents**

A
  • reduce smooth muscle spasms
  • antisecretory
  • ophthalmic exams: pupillary dilation
  • reduces cardiodepressant effects of other drugs
  • antidotes for mushroom poisoning and anticholinesterases
48
Q

Side effects of cholinergic antagonists**

A
  • dry mouth
  • tachycardia
  • mydriasis
  • hyperthermia
  • GI stasis
  • ataxia
  • delerium
  • convulsions
  • resp. depression
  • amnesia