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FTCM Pharm > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Cholinergic drugs are split into…

A

agonists (direct and indirect) and antagonists

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2
Q

How do direct act?

A

bind and activate

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3
Q

How do indirect act?

A

inhibit acetylcholinesterase

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4
Q

Where are m receptors?

A

Parasym in cardiac and smooth muscle, only symp in sweat glands

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5
Q

What are the direct effects of ACh?

A

Vasodilation (M3)
Decrease cardiac output (M2)
Decrease conduction in SA and AV M2
Decrease force in conduction (M2)

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6
Q

Small dose of Ach?

A

reflex tachycardia

decrease PVR
decrease MAP
increase HR

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7
Q

Large dose of Ach?

A

bradycardia

decrease PVR
decrease MAP
decrease HR

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8
Q

Effects of Ach on various organs…

A

PARASYMPATHETIC

think of miosis, bronchial constrictions, decrease heart rate

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9
Q

What happens if M receptors are blocked by atropine and you add large doses of Ach?

A

Nicotinic effects:
increase in BP and vasoconstriction

stimulation of symp and release of epinephrine from medulla

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10
Q

Direct acting agonists

A
  1. Esters of Choline (ABC-M)
    - Ach
    - Bethanechol
    - Carbachol
    - Methacholine
  2. Alkaloids
    - Pilocarpine
    - Nicotine
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11
Q

Choline esters

A

quaternary ammoniums
poorly absorbed in CNS
Ach rapidly hydrolyzed

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12
Q

Acetylcholine

A
  • rapidly hydrolyzed

- rapid miosis in cataract surgery

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13
Q

Bethanechol

A
  • Muscarinic agonist

- Atony of urinary bladder

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14
Q

Carbachol

A
  • Muscarinic and Nicotinic agonist

- Cataract surgery/miosis

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15
Q

Methacholine

A
  • Muscarinic agonist

- bronchial airway hyperreactivity in ppl who maybe have asthma

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16
Q

Pliocarpine

A
  • partial M agonist

- open angle glaucoma and dry mouth

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17
Q

M agonist AE:

A
  • sweating, flushing, low BP, diarrhea, AB pain
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18
Q

Nicotine intersting fact:

A

depolarizes autonomic ganglia–> stimulation then paralysis

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19
Q

Nicotine actions

A

Para and Symp

Mainly Para except CV system–> increase in BP and HR

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20
Q

Nicotine poisoning

A

nausea, AB pain, cold swears, mental confusion

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21
Q

Nicotine use

A

smoking cessation therapy

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22
Q

Indirect Acting:

A
  1. Edrophonium- reversible binding
  2. Carbamates “stigmine”- covalent bond
    - Physostigmine
    - Neostigmine
    - Pyridostigmine
  3. Organophosphates- phosphorylation
    - Echothiophate
    - Malathion
    - Sarin
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23
Q

Organophosphates interesting fact:

A

phosphorylated enzyme goes through ageing to strengthen bond

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24
Q

ANTICHOLINESTERASES:

ORGAN SYSTEM EFFECTS

A

CNS:
low- activation
high- convulsions

Most systems: PARA

CV: both para and symp

  • in heart: mainly para
  • increase resistance and BP

TLDR: bradycardia, decrease CO, increase vascular resistance and BP

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25
Q

ANTICHOLINESTERASES interesting fact:

A

minimal effect in vascular smooth muscle

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26
Q

Edrophonium

A

does not enter CNS

diagnosis of Myasthenia gravis

27
Q

Physostigmine

A

enter CNS

overdose of anticholinergic drugs

28
Q

Neostigmine

A

does not enter CNS

treatment of myasthenia gravis

29
Q

Pyridostigmine

A

does not enter CNS

treatment of myasthenia gravis

30
Q

Echothiophate

A

glaucoma RARELY used

31
Q

Malathion

A

insecticides

32
Q

Sarin

A

nerve agent: poison gas

33
Q

Ach inhibitors in Alzheimer disease

A

Galantamine
Donepezil
Rivastigmine

34
Q

Pralidoxime

A

split phosphorous-enzyme bond

*used for organophosphate insecticide poisoning

35
Q

Cholinergic antagonists are split up to?

A
  • M antagonists
  • N antagonists
  • Drugs that act presynaptically
36
Q

M antagonists –>

A
  1. Natural alkaloids
    - Atropine
    - Scopolamine
  2. Synthetic and semi synthetic drugs
37
Q

Atropine:

A 
Eye: mydriasis, cycloplegia
GI: reduces motility
Urinary: reduces motility
CV:
low- bradycardia 
high- tachycardia
38
Q

Atropine intersting fact:

A

atropine flush- cutaneous vasodilation

39
Q

Atropine uses:

A
  1. relax GI and bladder
  2. antidote for cholinergic agonists
  3. reduce respiratory secretions prior to surgery
40
Q

Atropine AE:

A

blurry vision, sandy eyes, constipation, tachycardia, urinary retention

confusion, hallucinations

41
Q

Scopolamine

A
  • similar to atropine but longer duration
  • can produce sedation
  • mydriasis and motion sickness**
42
Q

Synthetic and semi synthetic drugs:

A
  1. Quaternary ammonium MA “pium”
    - Ipratropium and Tiotropium
  2. Tertiary amine MA
    - Homatropine
    - Cyclopentolate
    - Tropicamide
  • Benztropine
  • Trihexyphenidyl
43
Q

Ipratropium and Tiotropium

A

COPD and asthma

44
Q
  • Homatropine
  • Cyclopentolate
  • Tropicamide
A

Mydriasis

45
Q
  • Benztropine

- Trihexyphenidyl

A

Parkinsons and effects of antipsychotic drugs

46
Q

Other M antagonists

A

Glycopyrolate
Oxybutynin
Tolterodine

47
Q

Glycopyrolate

A
  • COPD
  • Peptic ulcer
  • drooling
  • reduce secretions
48
Q

Oxybutynin

Tolterodine

A

Overactive bladder

49
Q

Contraindications of Anti-M agents:

A

angle-closure glaucoma, prostatic hypertrophy and elderly

50
Q

Nicotinic receptor antagonists:

A
  1. Ganglion blockers

2. NMJ blockers

51
Q

Ganglion blockers:

A

both symp and para
2 mechanisms:
1. Prolonged depolarization- nicotine
2. Antagonism- Hextamethonium and mecamylamine

52
Q

Hextamethonium and mecamylamine

A

used for hypertension

53
Q

Ganglion blockers interesting fact:

A

remove dominant control of various organs

a1- arterioles and veins
M3- sweat glands
will both become para (so dilation and no sweat)

the rest by M2 and M3 will be symp

54
Q

NMJ blockers:

A

block on skeletal muscle

  1. Competitive antagonists (non depolarizing)
  2. Agonists (depolarizing)
55
Q

Competitive antagonists (non depolarizing)

A

Tubocurarine

56
Q

Tubocurarine

A
  • reversible competitive
  • can be overcome by cholinesterase inhibitors like neostigmine or edrophonium
  • used for muscle relaxation during surgery in anaesthesia
57
Q

Agonists (depolarizing)

A

Succinylcholine

58
Q

Succinylcholine

A
  • receptor desensitizes

used for: Rapid endotracheal intubation and ECT

59
Q

Succinylcholine AE:

A
  • malignant hyperthermia dur to excess release of Ca+ from SR

treated with: dantrolene

60
Q

Drugs that act presynaptically

A
  1. inhibitors of synthesis
    - Hemicholinium-3
  2. inhibitors of storage
    - Vesamicol
  3. Inhibitors of release
    - Botox
61
Q

Hemicholinium-3

A

blocks CHT and prevents uptake of choline

62
Q

Vesamicol

A

blocks Ach-H antiporter (VAChT) needed for storage into vesicles

63
Q

Botox

A

inhibits Ach release

FTCM Pharm (4 decks)

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