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Pharmacology > S3 Cholinergic Drugs & Muscarinic/Nicotinic Receptors > Flashcards

S3 Cholinergic Drugs & Muscarinic/Nicotinic Receptors Flashcards

1
Q

Acetylcholine

A

Choline ester drug

Activity at BOTH muscarinic and nicotinic receptors

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2
Q

Pilocarpine

A 
Muscarinic AChR agonist only
Alkaloid drug
Uses (optical)
1. Glaucoma 
a. Promotes drainage of aqueous humor 
2. Dry eye = stim. lacrimation
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3
Q

Carbamylcholine

A

Choline ester drug

Activity at BOTH muscarinic and nicotinic receptors

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4
Q

Bethanechol

A 
Muscarinic AChR agonist only
Choline ester drug
Target = smooth muscle
Effects
1. Stimulates urinary bladder motility
2. Stimulates GI motility
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5
Q

Edrophonium

A 
AChE inhibitor
Reversible 
Quaternary ammonium compound 
Short duration (few minutes)
Diagnose/treat myasthenia gravis
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6
Q

Pyridostigmine

A 
AChE inhibitor
Reversible
Carbamate (insecticide)
Intermediate duration (15-30 min)
Diagnose/treat myasthenia gravis
Similar to Neostigmine
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7
Q

Neostigmine

A 
AChE inhibitor
Reversible
Carbamate
Intermediate duration (15-30 min)
Diagnose/treat myasthenia gravis
Similar to Pyridostigmine
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8
Q

Organophosphates

A 
AChE inhibitor
Irreversible 
Insecticides
Long duration (days)
Lipid soluble = dangerous!
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9
Q

Acetylcholine (as drug)

A 
Muscarinic AChR agonist at low doses
Also binds nicotinic AChRs at high doses
High doses = loss of specificity 
Effects
1. Low dose = dec. BP &dec. HR
2 High dose = inc. BP & inc. HR
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10
Q

Atropine

A

Muscarinic AChR antagonist
Vasorelaxation
Similar to Scopolamine

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11
Q

Carbachol

A

Muscarinic AChR agonist only
Target = smooth muscle
Effect = stimulate rumen or colonic motility
Can be dangerous!

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12
Q

Scopolamine

A 
Muscarinic AChR antagonist 
Optical use
Effects = smooth muscle paralysis
1. Mydraisis (pupil dilation)
2. Cycloplegia (paralysis; lens cannot focus)
Similar to atropine
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13
Q

Atropa belladonna (Deadly nightshade)

A

Muscarinic AChR antagonist
Dilates pupils = mydriasis
Fixes lens = cycloplegia
Similar to atropine & scopolamine

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14
Q

Trimethaphan

A 
Ganglionic blocker
Nicotinic (Nn) AChR
Blocks both parasympathetic & sympathetic
No effect on skeletal muscle
Many side effects- not routinely used
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15
Q

Pancuronium

A 
Skeletal muscle relaxant
Nicotinic (Nm) AChR competitive antagonist
Curariform blocker = GOOD
Non-depolarizing
Acts as a neuromuscular blocker
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16
Q

Succinylcholine

A 
Skeletal muscle relaxant
Nicotinic AChR depolarizing agonist
Causes desensitization of the receptor
Persistent 
No reversing agents but short acting
17
Q

Nicotine (toxicology)

A

Ganglionic stimulant –> desensitization
Nicotinic AChR agonist
Skeletal muscle relaxant
Death from respiratory paralysis

18
Q

Acetylcholine (high dose)

A

Nicotinic AChR agonist
Loses specificity at high concentrations
This occurs with cholinesterase inhibitor as well

19
Q

Levamisole

A

Nicotinic AChR antagonist
Depolarizing neuromuscular blocker
Causes muscle paralysis in nematodes

20
Q

Vecuronium

A

Skeletal muscle relaxant
Nicotinic AChR competative antagonist
Curariform blocker = BETTER

21
Q

Atracurium

A

Skeletal muscle relaxant
Nicotinic AChR competative antagonist
Curariform blocker = BEST
Spontaneously decomposed in plasma = Hoffmann elimination

22
Q

Gammamine

A

Skeletal muscle relaxant

Nicotinic AChR competative antagonist

23
Q

D-Turbocurarine

A

Skeletal muscle relaxant
Nicotinic AChR competative antagonist
Dart arrow poison

24
Q

Cholinergic drugs bind what receptors?

A

Muscarinic receptors

Nicotinic receptors

25
Q

Muscarinic receptor mechanism & effects

A

Sensitive to low concentrations of ACh
G-protein coupled
Blocked by atropine

Effects
1. Smooth muscle contraction
2. Increased exocrine secretion
3. Action at cardiac nodes --> 
decrease HR
4. Vasodilation from NO release 
(low doses)
26
Q

Nicotinic receptor mechanism & effects

A 
Require high concentrations of ACh
Multi-subunit cation channel
Blocked by
Nn receptors = Trimethaphan (ganglia)
Nm receptors = Pancuronium (sk. muscle)

Effects

  1. Skeletal muscle contraction
  2. Ganglionic transmission
27
Q

Ach inhibitors

A

Indirect acting drugs
Raise levels of ACh by inhibiting breakdown
More ACh is available to bind receptors

28
Q

Muscarinic receptors and locations

A 
M1
a. Peripheral neurons
b. CNS neurons
M2
a. Heart
b. Neurons
c. Smooth muscle
M3
a. Exocrine glands
b. Blood vessels
c. Eye
M4
a. CNS neurons
M5
a. CNS neurons
Odd = coupled to calcium
Even = coupled to decrease in cAMP
29
Q

SLUD sydrome

A 
Results from AChE inhibitors overdose
= Increased ACh concentrations 
1. Salivation
2. Lacrimation
3. Urination
4. Defeccation
Can lead to cardiac and respiratory arrest
30
Q

Skeletal muscle relaxants

A 
Nicotinic competitive antagonists 
Pancuronium = Good
Vecuronium = Better
Atracurium = Best
Levamisole
Gammamine
D-Turbocurarine

Desensitizing agonists
Succinylcholine
Nicotine

Pharmacology (9 decks)

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