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Pharma 1st semester > B. 3- Cholinomimetics > Flashcards

B. 3- Cholinomimetics Flashcards

1
Q

classify the direct-acting cholinomimetics (cholinergic agonists) and give examples

A 
1. choline esters: 
Acetylcholine 
Carbachol
2. Alkaloids: 
pilocarpine
3. synthetic: 
Varenicline
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2
Q

list choline esters

A

Acetylcholine
Methacholine
Bethanechol
Carbachol

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3
Q

which choline ester is only M agonist (selective)?

A

bethanechol

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4
Q

does Acetycholine have clinical use?

A

no

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5
Q

which choline esters are resistant to acetylcholinesterase?

A

bethanechol

carbachol

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6
Q

are choline esters lipid soluble?

A

they are poorly lipid-soluble

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7
Q

how is Carbachol given?

A

topically

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8
Q

for what is Carbachol given?

A

glaucoma

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9
Q

indications for Bethanechol

A

non obstructive ileus (post-operative/neurogenic)
urinary retention

“B” think -Bowls and Bladder

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10
Q

what is methacholine used for?

A

methacholine provocation test (DD of bronchial hyperactivity)

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11
Q

list the Alkaloids type cholinomimetics

A

Muscarine
Nicotinic
Pilocarpine

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12
Q

are alkaloids lipid soluble?

A

yes

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13
Q

how is pilocarpine given?

A

oral, parenteral

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14
Q

duration of action of bethanechol and pilocarpine

A

30min-2 hours

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15
Q

indications for pilocarpine

A
  1. Glaucoma
  2. Xerostomia- dry mouth (Sjögren syndrome, radiation, drug-induced)
    * pilocarpine ↑ fluid production
  3. pilocarpine-induced sweat test (cystic fibrosis diagnosis)
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16
Q

where is muscarine found?

A

mushroom poison

can result in poisoning effects- nausea, vomiting, diarrha

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17
Q

is Vareniciline N or M agonist ?

A

N (partial agonist)

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18
Q

why do we give varenicline?

A

for smoking cessation (inhibits the reward effect of nicotine in the limbic system)

19
Q

classify the indirect-acting cholinomimetics (acetylcholinesterase inhibitors)

A
  1. Carbamates (non-competitive, reversible inhibition)
  2. Organophosphates (irreversible inhibition)
  3. Alcohol (non-competitive, reversible inhibition)
20
Q

signs for AchE inhibitor poisoning

A 
"DUMBBELS"
Diarrhea 
Urination
Miosis
Bradycardia
Bronchoconstriction
Excitation (CNS, muscles)
Lacrimation 
Secretion (sweating, salivation)

*atropin helps reverse most effects

21
Q

what is the difference between a tertiary amine to a Quaternary amine?

A

Tertiary amine freely crosses the BBB and has CNS effects

Quaternary doesn’t

22
Q

list Carbamates

A

Neostigmine
Pyridostigmine
Physostigmine

Rivastigmine
Galantamine
Donepezil

23
Q

mechanism of Carbamates

A

bind to AchE and undergo hydrolysis, preventing binding and hydrolysis of endogenous Ach

24
Q

give the carbamates that are Quaternery amines

A

Neostigmine

pyridostigmine

25
Q

indications for Neostigmine

A

Myasthenia gravis–> muscle weakness
non-obstructive ileus (post-operative/neurogenic)
Urinary retention
Reversal of Nm Block (curare- like overdose)

26
Q

indication for pyridostigmine

A

myasthenia gravis

27
Q

indications for Physostgimine

A

antidote in atropin overdose (IV)

glaucoma (topical)

28
Q

duration of neostigmine and physostigmine

A

2-4 hours

29
Q

duration of pyridostigmine

A

4-8 hours

30
Q

half life of Rivastigmine, Donepazil

A

1.5- 70 hours

31
Q

what Carbamates are Tertiary amines?

A

Physostigmine
Rivastigmine
Galantamine
Donepezil

32
Q

what are the indications for Rivastigmine, Galantamine, donepazil?

A

Alzheimer disease (transdermal patch)

33
Q

list the OPS

A

Malathion
Parathion
Sarin

34
Q

where is Sarin found?

A

nerve gas (lethal, rapid acting)

35
Q

mechanism of OPS

A

binds to AchE and undergo hydrolysis–> phosphorylation of serine residue–> preventing binding and hydrolysis of endogenous Ach

36
Q

where is malathion found?

A

in insecticides (highly toxic)

37
Q

what is the duration of action of Malathion and Parathion?

A

days-weeks

38
Q

is Malathion/Parathion lipid soluble?

A

HIGHLY lipid-soluble

39
Q

what is the half-life of Edrophonium?

A

short (5-10min)

40
Q

what is Edrophonium?

A

Alcohol type Ach inhibitor (non competitive, reversible inhibition)

41
Q

what are the indications for Edrophonium?

A

Diagnosis of myasthenia gravis
(improved muscle tone–>positive diagnosis)
DD (‘Tensilon test’) : cholinergic crisis vs. myasthenia crisis

42
Q

what drug is given with AchE inhibitors to control muscarinic side effects?

A

selective muscarinic antagonist (e.g glycopyrrolate)

43
Q

Mechanism of AchE inhibitors

A

inhibits AchE–> ↑ in the concentration, half-life and activity of Ach in synapses–> induce both muscarinic and nicotic effects

Pharma 1st semester (19 decks)

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