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Pharmacology > Cholinergic agonists And AChe Inhibitors > Flashcards

Cholinergic agonists And AChe Inhibitors Flashcards

1
Q

What are the muscarinic agonists?

BCAP

A

Bethanechol ( Uricholine)

Cevimeline ( Evoxac)

Acetylcholine ( Michol - E)

Pilocarpine (Salagen)

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2
Q

What are Organophosphates?

A

Malathion

Sarin

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3
Q

What are reversible AchE inhibitors?

PEND

A

Pyridostigmine ( Mestinon)
Edrophonium ( Tensilon)
Neostigmine ( prostigmin)
Donepezil ( Aricept)

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4
Q

What are Cholinesterase reactivators

A

Pralidoxime (protopam)

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5
Q

What are the main drug strategies to intensify ACh neurotransmission?

A

Direct activation of ACh receptors

  1. nicotinic cholinergic receptor agonists
    - increase cognition in dementia
    - Smoking cessation
  2. Muscarinic cholinergic receptor agonists
    - enhance parasympathetic function to treat urinary retention, glaucoma and xerostomia
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6
Q

What are the main drug strategies to intensify ACh neurotransmission.

A

(2) AchE inhibitors increase the lifespan of ACh in the synapse.

  • Myasthenia gravis, dimentia
  • Chemical warfare insecticides
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7
Q

Nicotinic receptor facts

A

Excitatory ligand gated ion channels

Nn
Nm

Activated by nicotine

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8
Q

Muscarinic receptor facts

A

Mushroom

M1- M5

Glycoprotein- Coupled Receptors

Excite or Inhibit

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9
Q

Why does exogenous ACh not have widespread cholinergic activation?

A

Rapid plasma breakdown

Does not reach peripheral synapse

Does not penetrate BBB

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10
Q

How does peripheral mAchR agonist affect the heart?

A

It lowers BP and Heart workload

Decreased heart rate (M2)

Decreased conduction velocity

Vasodilation ( M3)

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11
Q

How does increased mAchR agonist affect the lungs

A

Respiratory tract - Bronchoconstriction

Smooth muscle

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12
Q

How does increase mAchR agonism affect the bladder

A

Bladder voiding

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13
Q

How does mAchR affect the GI

A

Increased GI motility and secretion

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14
Q

How does maAchR agonist affect the salivary and sweat glands?

A

Stimulate secretion of salivary, nasalpharyngeal, lacrimal and sweat glands

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15
Q

How does mAchR agonism affect the eyes?

A

Pupillary contraction accommodation of lens for near vision.

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16
Q

How is peripheral muscarinic agonism used?

A

Stimulate salivary and ocular secretions: cevilemine and pilocarpine

Urinary retention: bethanechol

Glaucoma pilocarpine

Diagnosis of sub-clinical asthma: methacholine

17
Q

What is Sjögrens Syndrome?

A

Progressive loss of exocrine glands

Dry eyes dry mouth difficulty swallowing
And speaking

18
Q

How is Sjögren’s syndrome treated symptomatically?

A

activation of remaining M3 receptors

19
Q

What is a muscarinic agonist and how does it promote aqueous humor flow?

A

Pilocarpine:

M3 activation on ciliary muscle and pupillary constrictor leads to contraction

Beta blocker and prostaglandins reduce aqueous humor

20
Q

How do muscarinic agonist promote bladder voiding?

A

Once we are sure retention is not due to physical obstruction

Give bethanechol
M3 causes contraction in upper bladder muscle

21
Q

How can cholinergic agonist be used to diagnose asthma?

A

Bronchoprovocation with methacholine by nebulizer activates M3 receptors and cause bronchospasm in people with latent asthma.

22
Q

What are adverse effects of Muscarinic agonists?

A

Diaphoresis bronchoconstriction diarrhea cramping nausea vomiting blurred vision hypotension

23
Q

What affect doe AChe inhibition have at Cholinergic synapses?

A

Increase ACh activity at all cholinergic synapses

24
Q

Why does therapeutic AchE inhibition resemble muscarinic agonism?

A

Because all M2 and 3 receptors are activated by ACh

25
Q

What is Myasthenia Gravis

A

A skeletal muscle weakness disease.

Selective or progressive destruction of motor end plate

26
Q

How is it treated

A

Using a reversible anti AChE agents that do not cross BBB

Excessive muscarinic affects treated with atropine

27
Q

What is used in diagnosing MG

A

Edrophonium is used in Tensilon test

28
Q

What AchE inhibitors are used for lethality?

A

Irreversible inhibitors

Organophosphate synthetics (sarin- nerve gas)
(Malathion- pesticide)

Carbamate- insecticides

29
Q

What is the cholinergic crisis produced by toxic AchE inhibition?

A

SLUDGE

Salvation 
Lacrimation  
urination 
defecation 
GI Distress 
Emesis

Bradycardia and hypotension

30
Q

What is an organophosphate Antidote?

A

Pralidoxime

Prior to aging pralidoxime can bind to organophosphate and pull it off

Does not cross BBB

31
Q

What is an antidote for all anti AchE?

A

Atropine a muscarinic agonist that penetrates CNS

Main effects in the lungs
To stop vasoconstriction and clear resporatory secretions.

32
Q

Which lipid-soluable anti-CHE agents and nicotonic agonists enhance cognition in Alzheimer’s?

A 
Physostigmine
Tacrine hepatotoxic
Donepezil
Rivastigmine
Galantamine

Pharmacology (4 decks)

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