Cholinergic Agonists - Drugs Flashcards

1
Q

Types of cholinergic drugs

A

Cholinergic agonist

Cholinergic antagonist

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2
Q

Types of cholinergic agonist

A

Direct acting and non-direct acting

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3
Q

What are direct acting cholinergic agents

A
  • muscarinic agonist

- nicotinic agonist

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4
Q

Example of muscarinic agonists are

A

Pilocarpine
Bethanechol
Carbachol
Methacholine

(Chol)

Acetylcholine - ABC-MP

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5
Q

What are the indirect acting cholinomimetics

A

-reversible and irreversible

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6
Q

Reversible AchE inhibitors

A

Stigmines
Edrophonium
Tacrine
Donepezil

DETS

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7
Q

Irreversible AchE inhibitors

A
  • OPC
  • Melathion
  • Parathion
  • Echothiophate

OPEM : cause anticholinesterase poisoning

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8
Q

Bethanechol?

A

A direct acting muscarinic agonist which work mainly on

  • increasing motility / contraction in GIT & UB respectively
  • Congenital megacolon
  • Xerostomia
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9
Q

Pilocarpine

A

A tertiary amine that binds to muscuranic agonist

Functions to reduce IOP for open and closed angle glaucoma (DOC) by constriction of the circular ciliary muscles and pupillary sphincter

It also stimulates sweat, tears and saliva

Xerostomia

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10
Q

S/e of pilocarpine

A

Apart of muscuranic effects it can lead to CNS effects of drowsiness and sedation

Because they cross bbb

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11
Q

Carbachol?

A

A direct acting cholmimetic which acts on both M and N receptors

Used for glaucoma via motic action

Can cause release of epinephrine from adrenal gland

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12
Q

Physostigmine

A

An indirect reversible cholinergic agonist

Act on GIT, UB and treat glaucoma

S/e: muscarinic effects and CNS effects (crosses bbb)

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13
Q

Does physostigmine cross bbb

A

Yes and cause CNS s/e

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14
Q

Neostgmine

A

Does not cross bbb

  • Act on GIT: postoperative and neurogenic ileus
  • UB retention
  • an antidote for tubocurarine and other competitive NMJ blocking agent -myasthenia gravis
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15
Q

Which cholomimetic cross CNS

A
Physostigmine
Pilocarpine 
OPC
Donepezil
Tacrine
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16
Q

Myasthenia gravis

A
  • Loss of muscle on exertion but improves after rest
  • affects mostly extraocular muscles, face muscles, swallowing muscles, chewing muscles.
  • fist symptom is ptosis or diplopia
17
Q

Mysthenia gravies tx

A

Pyridostigmine (doc for chronic cases)
Neostigmine
Edrophonium (for diagnosis)

Endrophonium has been replaced with anti-ACHr antibody

18
Q

Use of Donepezil, tacrine, rivastigmine, galantamine

A

Treat Alzheimer’s disease (1st line)

By inhibiting the enzyme that destroys ach

Don Riva forgot to dance at the Gala

19
Q

S\E of Donepezil

A

V/p/n/d

Liver damage =increased ALT

20
Q

Tx of glaucoma

A
  • Pilocarpine (DOC)
  • cabarchol
  • OPC : topical ointment
  • physostigmine
21
Q

Physostigmine overdose tx

A
  • atropine
  • phenothiazine
  • TCA

all are anti cholinergics

22
Q

What can you use to activate AchE

A

Pralidoxime via dephosphorylation if given early

Reversers the nicotinic effects of anticholinesterase poisoning

23
Q

Contraindications of cholinergic agonists

A
Diarrhea 
GI or UB obstruction 
Pudx
Bronchial asthma
Hypotension 
Bradycardia
24
Q

Symptoms of achE inhibitors toxicity

A

DUMBBELLS

Diarrhea 
Urination
Miosis
Bronchoconstriction 
Bradycardia 
Emesis 
Lacrimation 
Salivating 
Sweating

+ Nicotinic effects: NMJ blockage similar effects to succinylcholine

25
Q

Substances used for AchE inhibitors toxicity

A

Atropine: cross bbb for CNS symptoms

Pralidoxime: does not cross bbb

26
Q

Methacholine

A

It stimulates muscarinic receptors when inhaled.

A challenge test for the diagnosis of asthma

27
Q

Reversible indirect cholinergic agonist that does not cross bbb

A
  • neostigmine
  • pyridostigmine

Cuz that have positive charge as a quaternary amine

28
Q

What drugs do you give to Andre the s/e of pyridostigmine

A
  • glycopyrrolate
  • hyoscyamine
  • propantheline
29
Q

CNS effects of anticholinesterase poisoning

A

Lethargy, seizures, respiratory depression, coma