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Pharmacology > Pharm 7 - Cholinoceptor Antagonists > Flashcards

Pharm 7 - Cholinoceptor Antagonists Flashcards

1
Q

Define affinity.

A

the strength with which an agonist binds to a receptor

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2
Q

Define efficacy.

A

once the drug has bound to a receptor, the ability of the drug to produce a response and activate intracellular signalling pathways

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3
Q

Agonists have…

A

affinity and efficacy

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4
Q

Antagonist have…

A

affinity but no efficacy

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5
Q

Where are nicotinic receptors found?

A

all autonomic ganglia

at neuromuscular junctions

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6
Q

Where are muscarinic receptors found?

A

at parasympathetic effector organs and sweat glands

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7
Q

What are nicotinic receptor antagonists called?

A

Ganglion blockers

block the ion channel itself so prevent ions going through

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8
Q

Give 2 examples of ganglion blocking drugs.

A

Hexamethonium

Triemethaphan

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9
Q

What does use dependent block mean?

A

drugs work more effectively when the ion channels are open

e.g. if agonist there to open the channel, antagonist will work more effectively

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10
Q

What dominates the effect of ganglion blockade in a tissue?

A

Which limb of ANS dominates in the tissue

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11
Q

Which tissues are sympathetic dominated?

A

Vasculature

Kidneys

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12
Q

What is the overall effect of ganglion blockade in terms of loss of sympathetic dominance?

A

hypotension

as takes away the ability of kidneys to produce renin

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13
Q

Which tissues are parasympathetically dominated?

A

Eyes - maintains partial pupillary constriction at rest
Lungs - causes bronchoconstriction
Bladder, ureters and GI tract
Exocrine functions

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14
Q

What would the effect of ganglion blockage be on these tissues?

A 
Bronchodilation
Pupil dilation
Bladder dysfunction
Loss of GI motility and secretions
Decrease in exocrine secretion
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15
Q

What is hexamethonium?

A

ganglion blocker that was used as anti-hypertensive

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16
Q

What is trimethaphan?

A

only ganglion blocking drug still in clinical use

causes hypotension - needed for surgery

17
Q

In what types of chemicals are nicotinic receptor blockade antagonists found?

A

Toxins and venoms

18
Q

How do receptor blockade antagonists have their effect?

A

irreversible

19
Q

Give an example of nicotinic receptor blockade antagonist.

A

Alpha bungarotoxin

20
Q

What are the targets of muscarinic receptor antagonists?

A

Parasympathetic effector organs and sweat glands

21
Q

Give 4 examples of muscarinic receptor antagonists?

A

Atropine
Hyoscine
Tropicamide
Ipratropium Bromide

22
Q

What effect do muscarinic receptor antagonists have on the CNS?

A

atropine = low dose = restlessness

hyoscine = sedation

high dose = CNS agitation

23
Q

What is tropicamide used for?

A

used to dilate the pupil to observe the retina

24
Q

What is an important use of muscarinic receptor antagonists with regard to surgery?

A

Anaesthetic premedication

causes dilation of airways so easier to intubate patient
reduces secretion so less risk of aspiration
knocks out parasympathetic nervous system in decreasing heart rate and contractility

25
Q

What can hyoscine be used to treat?

A

Motion sickness
muscarinic receptors relay information from labyrinth in the inner ear to vomitting centre

so blocking these will reduce nausea

26
Q

What degenerative disorder can be treated using muscarinic receptor antagonists?

A

Parkinson’s disease

Muscarinic receptors have inhibitory impact on the dopamine neurones in the nigro-striatal

27
Q

Explain the use of muscarinic antagonists in treating asthma and COPD?

A

Ipratropium bromide
removes parasympathetic mediated bronchoconstriction

so used to treat COPD and asthma

28
Q

Explain the role of muscarinic antagonists in treating IBS?

A

reducing smooth muscle contraction, gut motility and gut secretions

29
Q

State some general unwanted side effects f

A

Hot as hell
Dry as a bone
Blind as a bat
Mad as a hatter

30
Q

How would you treat muscarinic receptor antagonist poisonin?

A

anticholinesterase e.g. physostigmine

31
Q

Describe botulinum toxin causes paralysis.

A

binds to SNARE complex and prevents fusion of vesicles containing acetylcholine

so prevents acetylcholine release into nerve terminal

muscle paralysis

32
Q

State the overall effects of ganglion blocking drugs on a subject at rest?

A 
Hypotension
Pupil dilation
Bronchodilation
Bladder dysfunction
Decreased GI tone
Decreased GI secretions

Pharmacology (10 decks)

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