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Drug Action > Cholinergic pharmacology > Flashcards

Cholinergic pharmacology Flashcards

1
Q

What are cholinergic nerves?

A

Those that release acetylcholine

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2
Q

Where are cholinergic nerves found?

A

In all divisions of the nervous system

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3
Q

What are the 6 stages to cholinergic nerve function?

A 
Supply
Synthesis
Storage
Release
Inactivation
Feedback
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4
Q

How is choline supplied?

A

Nerves cannot make enough choline
Choline is taken up from the blood
Choline comes from diet and liver
Na+ dependent process

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5
Q

What is hemicholinium?

A

Competitive inhibitor of choline carrier

Causes activity-dependent block of cholinergic transmission

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6
Q

How is acetylcholine synthesised?

A

In the nerve cytoplasm
Enzyme choline acetyltransferase
Choline + acetyl coA

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7
Q

How is acetylcholine stored?

A

Energy dependent pump
Synaptic vesicle
inhibition of pump by Vesamicol leads to depletion of stores

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8
Q

How is acetylcholine released?

A

Entry of Ca2+ into nerve ending

Occurs by exocytosis

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9
Q

What drugs block acetylcholine release?

A

Botulinum toxin

alpha latrotoxin

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10
Q

How is acetylcholine removed from the synaptic cleft?

A

Hydrolysis by acetylcholinesterase

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11
Q

What is sarin?

A

Acetylcholinesterase inhibitor

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12
Q

How is feedback relayed to the presynaptic nerve?

A

Ach receptors inhibit release of Ach
ATP is converted to adenosine which inhibits release
Morphine inhibits release
Noradrenaline inhibits release

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13
Q

How are receptors classified?

A

Anatomical
Chemical/pharmacological
Molecular

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14
Q

What is the most potent agonist of nicotinic cholinoceptors?

A

Nicotine

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15
Q

Describe the action of nicotine receptor agonists

A

Transiently stimulate ganglia and motor end plate if given briefly at high concentrations
Receptors rapidly desensitise

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16
Q

What is an antagonist of nicotinic receptors?

A

Hexamethonium and decamethonium

17
Q

What is the mechanism of action of hexamethonium?

A

Blocks the ion channel

18
Q

What is galantamine?

A

Increases activity of nicotinic receptors
Anticholinesterase activity
Treatment of alzheimers

19
Q

What is the most potent agonist for muscarinic cholinoceptors?

A

Metacholine and muscarine

20
Q

What is the structure of a muscarinic receptor?

A

7 transmembrane segments

21
Q

What are the clinical uses of antimuscarinic drugs?

A 
Asthma
Treat bradycardia
Decrease gut motility
Dilate pupils
Incontinence
Motion sickness
22
Q

What are the effects of parasympathomimetics?

A

Cardiovascular: decreased heart rate and cardiac output
Smooth muscle: contracts, vascular dilates
Exocrine glands secrete

23
Q

What is a use of parasympathomimetics?

A

Glaucoma

Drug Action (19 decks)

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