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Week 2 CA1 > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Types of cholinergic receptors and where they are found

A 
Nicotinic 
1. N1 = skeletal muscle
2. N2 = ganglia and CNS
Muscuranic
M1 = Stomach and CNS
M2 = Heart, CNS, Gall bladder, Genitals (remember using HCG)
M3 = Lungs, glands, GIT, cilliary body, iris, CNS
M4, M5 = CNS
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2
Q

Post synaptic receptor stimulation of eccrine sweat glands and receptor involved

A

M3 receptor

Acetylcholine is the neurotransmitter used

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3
Q

What does any cholinergic drug that crosses the BBB do

A

Binds to M1 receptor in the brain and causes Nausea and Vomitting

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4
Q

Common adverse effects of cholinergic agonist and contraindications

A

Adverse effects

  1. Nausea
  2. Miosis
  3. Urinary urgency
  4. Diarrhoea
  5. Sweating

Contraindications

  1. Asthma
  2. Peptic ulcer
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5
Q

Names of direct cholinergic agonists

A
  1. Pilocarpine (muscuranic agonist, alkaloid)
  2. Bethanachol (muscuranic agonist, carbamate choline ester)
  3. Carbachol (muscuranic agonist, carbamate choline ester)
  4. Nicotine (nicotinic agonist, alkaloid)
  5. Vareniciline (nicotinic agonist, alkaloid)
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6
Q

What type of ammonium is ACh and does it cross BBB

A

It is a quatenary ammonium

Does not cross BBB

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7
Q

What is the benefit of Carbamate choline esters

A

Carbamate choline esters are not broken down by endogenous choline esterases but are broken down by other enzymes as such their half life is longer

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8
Q

What is Pilocarpine and what is it used for and its adverse effects

A

Alkaloid non-selective muscuranic receptor agonist
Used in treatment of glaucoma and dry mouth
Side effects : Nausea, blurred vision, urinary urgency, diarrhoea, sweating
Contraindicated in patients with ASTHMA and COPD

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9
Q

Bathenachol

Receptor, function, used to treat what, side effects and contraindications

A

Quaternary choline ester
Does not cross BBB
Increases detrusor tone and decrease outlet resistance of internal sphincter
Used to treat : Gastric atony and urinary retention
Side effects : Nausea, blurred vision, urinary urgency, diarrhoea, sweating
Contraindications: Asthma and COPD

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10
Q

Nicotine

Receptor, Function, what its used to treat, adverse effects

A

Binds to both neuromuscular receptor and neuronal nicotinic receptor

Low dose :
Causes skeletal muscle fasiculations, low dose causes ganglionis activation causing adrenaline release which causes increase in heart rate and contractility. Nicotine also causes increase in GI motility and secretion

High dose:
Causes depolarising blockade, medullary depression, bradycardia

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11
Q

Variniciline

Receptor and use

A

Partial nicotinic agonist, highly effective in smoking cessation

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12
Q

Indirect cholinergic drugs

A

Reversable and irreversible category

Reversible category :

  1. Physostigmine/donapazil
  2. Neostigmine
  3. Pyridostigmine

Irreversible category:

  1. Sarin
  2. Parathion
  3. Malathion
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13
Q

Donepazil/Physostigmine

A
  • crosses BBB
  • used to treat alzheimer’s disease
  • Side effects : Nausea, vomiting, blurred vision, urinary urgency, diarrhoea, sweating
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14
Q

Neostigmine

A
  • Does not cross BBB
  • Used to reverse non-depolarising blockade (i.e. coming out of anaesthesia) and myasthenia gravis
  • Side effects : Nausea, blurred vision, urinary urgency, diarrhoea, sweating
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15
Q

Irreversible choline esterase inhibitors

A

Sarin, Parathion, Malathion

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16
Q

Sarin, parathion, malathion

A

Organophosphate agent
Suicide inhibitor of acetylcholine esterase
Clinical presentation : Salivation, Lacrimation, Urination, Defecation (SLUD), miosis, bradycardia, hypotension
Antidote = Pralidoxime (acetyl choline esterase regenerator) and Atropine (muscuramic antagonist)

17
Q

Pralidoxime

A

Acetylcholine esterase regenerator
Higher affinity for phosphate than acetylcholine
Used to treat organophosphate poisoning

Only effective in inhibition of AChE via organophosphate not if it is inhibited in other mechanisms such as carbamylation via neostigmine

18
Q

Direct anticholinergic drugs

A
  1. Atropine
  2. Benzatropine
  3. Scopolamine
  4. Ipratropium
  5. Oxybutynin
  6. NonDepolarising NeuroMuscular Blocking Agent (NMBA)
    - Pancuronium
    - Rocuronium
    - Atracurium
    - Tubocurarine
19
Q

Benzatropine

A

Non-selective muscuranic acetylcholine receptor antagonist
Crosses BBB
Used to treat Parkinson’s disease
Side effects : Dry mouth, Blur vision, Urinary retention, Glaucoma, Sedation (use D-BUGS to remember)
Contraindicated in : Narrow angle glaucoma

20
Q

Atropine

A

Non-selective muscuranic acetylcholine receptor antagonist
Increases heart rate
Used to treat : 1. Overdose of AChE inhibitor and organophosphate poisoning
Side effects : Superficial vasodilation, Blur vision, decreased secretion, hyperthermia, delerium and hallucinations
Contraindications : Narrow angle glaucoma

Use red as a beet, blind as a bat, dry as a bone, hot as a hare, mad as a hatter to remember

21
Q

Scopolamine

A

Non-selective muscuranic acetylcholine receptor antagonist
Used to treat motion sickness
Side effects : Dry mouth, Blur vision, Urinary retention, Glaucoma, Sedation (use D-BUGS to remember)
Contraindicated in narrow angle glaucoma

22
Q

Ipratropium

A
  • Non-selective muscuranic acetylcholine receptor antagonist
  • reduce bronchoconstriction
  • used to treat Asthma and COPD
  • Side effects : Dry mouth, Blur vision, Urinary retention, Glaucoma, Sedation (use D-BUGS to remember)
23
Q

Oxybutynin

A

Relax smooth muscle walls, increase sphincter tone
Used to treat Urinary incontinance
Contraindicated in : pyloric obstruction and bladder retention

24
Q

Non depolarising NeuroMuscular Blocking Agents

A

Pancuronium
Rocuronium
Atrocurorium
Tubocurarine

Competitively block nicotinic acetylcholine receptor
Causes paralysis of skeletal muscle
Side effects : Histamine release at higher doses causeing flushing, edema and hypotension

25
Q

Indirect anticholinergic drugs

A
  1. High dose nicotine
  2. Succinylcholine
  3. Botulinium Toxin
26
Q

Clinical uses and side effects of BOTOX

A

Clinical uses

  1. Blepharospasm (excessive blinking)
  2. Strabismus (excessive squinting)
  3. Cervical dystonia
  4. Migraine
  5. Upper limb spasticity
  6. Cosmetic

Side effects : paralysis of wrong muscle group and allergic reaction

Week 2 CA1 (9 decks)

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