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CPR Exam 1 > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Direct-acting cholinomimetics

A
  • Ach
  • Bethanechol
  • Carbachol
  • Cevimeline
  • Methacholine
  • Pilocarpine
  • Varenicline (Chantix)
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2
Q

Cholinesterase inhibitors

A
  • Ambenonium
  • Donepezil
  • Echothiophate
  • Edrophonium
  • Galantamine
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Rivastigmine
  • Tacrine
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3
Q

Cholinesterase regenerator

A

Pralidoxime

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4
Q

Drugs used for respiratory disorders (asthma, COPD)

A
  • ipratropium

- tiotropium

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5
Q

Drugs used for urinary disorders

A
  • Darifenacin
  • fesoterodine
  • Oxybutynin
  • Solifenacin
  • Tolterodine
  • Trospium
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6
Q

What drugs are used for cholinergic poisoning?

A

Atropine (+ pralidoxime)

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7
Q

What drugs are used for movement disorders?

A
  • Benztropine
  • Biperiden
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl
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8
Q

What is the example given of a ganglion blocker?

A

Mecamylamine

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9
Q

What drug is used for motion sickness?

A

Scopolamine

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10
Q

What drugs are used for GI disorders?

A
  • Atropine
  • Dicyclomine
  • Glycopyrrolate
  • Hyoscyamine
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11
Q

What drugs are used in ophthalmology?

A
  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
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12
Q

M1 receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • nerves
  • Gq
  • IP3, DAG
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13
Q

M2 receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • heart, nerves, smooth muscle
  • Gi
  • inhibition of cAMP, K+ channel activation
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14
Q

M3 receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • glands, smooth muscle, endothelium
  • G1
  • IP3, DAG
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15
Q

M4 receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • CNS
  • Gi
  • inhibition of cAMP
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16
Q

M5 receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • CNS
  • Gq
  • IP3, DAG
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17
Q

NN receptor

  • location:
  • GPCR pathway:
  • mechanism:
A
  • postganglionic cell body, dendrites, CNS
  • alpha and beta only
  • Na+, K+ depolarizing ion channel
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18
Q

What is the predominant receptor in most organs?

A

M3

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19
Q

Which receptor predominates in the heart?

A

M2

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20
Q

Which receptor predominates in smooth muscle?

A

M2, M3

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21
Q

Which receptor types are found in the eye, lungs, and GI/GU?

A

M3, M2

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22
Q

What is the MOA of choline esters?

A

cholinergic agonist

  • choline esters permanently charged = poor absorption and CNS distribution
  • metabolized by acetylcholinesterase
23
Q

What is the MOA of alkaloids?

A

cholinergic agonist

  • uncharged tertiary structure = well absorbed
  • muscarine is charged, but can still cross BBB
24
Q

What are the 3 groups of AChE inhibitors?

A
  1. alcohols (reversible)
  2. carbamic acid esters (reversible)
  3. organophosphates (irreversible**)
25
Q

Which AChE inhibitors are insoluble in lipids?

A

charged AChE inhibitors

  • do not cross BBB
  • quaternary agents (edrophonium, physostigmine, neostigmine, echothiophate, ambenonium)
26
Q

Which AChE inhibitors are lipid-soluble?

A

neutral AChE inhibitors

  • can cross BBB
  • most organophosphates, teriary agents (physostigmine, doneppezil, galantamine, rivastigmine, tacrine)
27
Q

What is the parasympathetic response of the sphincter muscle of the iris?

A

contraction (miosis)

28
Q

What is the parasympathetic response of the ciliary muscle of the eye?

A

contraction for near vision

29
Q

What is the parasympathetic response of the SA node?

A

negative chronotropy (decreases HR)

30
Q

What is the parasympathetic response of the atria?

A

negative inotropy (decreases contractility)

31
Q

What is the parasympathetic response of blood vessels?

A

dilation via EDRF

NOTE: at high doses, direct effect causes constriction

32
Q

What is the parasympathetic response of bronchial muscle?

A

bronchoconstriction

33
Q

What is the parasympathetic response of GI motility?

A

increases motility

34
Q

What is the parasympathetic response of GI secretions?

A

stimulates secretion

35
Q

What is the parasympathetic response of GI sphincters?

A

relaxes sphincters

36
Q

What is the parasympathetic response of urinary detrusor muscle?

A

contraction (parasympathetic makes you pee)

37
Q

What is the parasympathetic response of urinary trigone and sphincter?

A

relaxation

38
Q

What is the parasympathetic response of sweat, salivary, lacrimal and nasopharyngeal glands?

A

increases secretion

39
Q

What is Bethanechol?

A

selective mAChR agonist that primarily affects urinary and GU tracks

  • used to treat urinary retention and heartburn
  • little CV stimulation
  • may produce UTI if sphincter fails to relax
40
Q

What is Carbachol?

A

nonspecific cholinergic agonist used to treat glaucome, or produce miosis during surgery

41
Q

What is Cevimeline?

A

oral tablet used to treat dry mouth (xerostomia) in patients with Sjogren syndrome

42
Q

What is Pilocarpine?

A

pure mAChR agonist

- approved for xerostomia in patients with Sjogren syndrome, head/neck cancer treatment, or during opthalmic procedures

43
Q

What is Varencline (Chantix)

A

FDA approved drug for smoking sessation
- partial agonist that binds with high affinity and selectivity for NN

NOTE: sustained release of dopamine thought to reduce craving and withdrawal symptoms of smoking

44
Q

What are the major uses of direct-acting cholinergic agonists in GI/GU disorders?

A
  • postoperative ileus
  • congenital megacolon
  • urinary retention
  • esophageal reflux
  • xerostomia, Sjogren syndrome
45
Q

What are the contraindications for direct-acting cholinergic agonists?

A

patients who have asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease

46
Q

What are the clinical uses of indirect-acting cholinergic agonists?

A
  • glaucoma
  • dementia
  • antidote to anticholinergic poisoning
  • reversal of neuromuscular paralysis
  • myasthenia gravis
  • AChE inhibitor toxicity
47
Q

What are the most clinically useful cholinergic antagonists?

A

antimuscarinic agents

48
Q

What anticholinergics are used for respiratory disorders?

A

Ipratropium and tiotropium

  • inhalation mAChR antagonists
  • Tiotropium has longer bronchodilator action, can be dosed once daily
49
Q

What anticholingergics are used for GI disorders?

A

mAChR antagonists can treat common travelers diarrheaand other mild conditions of hypermotility

NOTE: often combined with an opiod antidiarrheal drug

50
Q

What anticholinergics are used for GU disorders?

A

agents with selectivity to M3 subtype are beneficial due to presence in bladder wall and sphincter smooth muscle

  • Oxybutynin (but has side effects of dry mouth/eyes, dizziness, constipation)
  • Darifenacin, solifenacin and tolterodine are advantageous because of longer half-lives and reduced incidence of zerostomia and constipation
51
Q

What anticholinergics are used for cholinergic poisoning?

A

Atropine! given to reduce mAChR stimulation

  • no effective treatment at nAChR
  • useless in delayed-onset mushroom poisoning
52
Q

What are the adverse effects of anticholinergics?

A

good for one system, bad for another
- mydriasis (pupil dilation) and cycloplegia (ciliary muscle paralysis) may be adverse effects of antimuscarinic agents used to reduce GI secretion

53
Q

What do high systemic concentrations of anticholinergics lead to? How do you treat it?

A

will block parasympathetic function

- treat with AChE inhibitors

54
Q

What are the contraindications of anticholinergics?

A
  • glaucoma
  • prostatic hyperplasia
  • acid-peptic disease

CPR Exam 1 (18 decks)

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