Cholinoceptor Antagonists Flashcards

1
Q

Where are nicotinic receptors found

A

All autonomic ganglia

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2
Q

What part of the ANS can nicotinic receptor ant/agonists interfere with

A

The whole ANS

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3
Q

What type of receptor is a nicotinic receptor

A

Type 1 ion channel

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4
Q

What 2 ways can a nicotinic receptor antagonist work

A

Can block the receptor or block the ion channel

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5
Q

what does use dependent blocking mean

A

drugs work most effectively when the ion channels are open. Thus, the more agonist that is present at the receptor, the more opportunity for the antagonist to block the channel, therefore, the more useful and effective these drugs can be

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6
Q

What makes a use dependent blocker more potent

A

If there is more agonist to open the ion channel

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7
Q

what is incomplete blocking

A

Ion channel blockers, they don’t completely block they slow it down considerably but not fully stop the functioning

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8
Q

Difference between normal receptor blockade and ion channel blockade regarding use dependency

A

When have a normal receptor blockade, then less agonist makes it more effective. Opposite is true for ion channel blockers

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9
Q

why do nicotinic receptor antagonists cause hypotension (2)

A

The SNS is dominant in blood vessels and the dominant effect is to constrict. This increases TPR and in turn, increases BP. The drugs take out the dominant sympathetic effect so the vessel will dilate. The TPR would decrease and so the BP would decrease.
Drugs might also interfere with the Renin secretion reduced aldosterone would be produced which means less water and Na is reabsorbed so less renin produced and thus, less ACE produced (see below).

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10
Q

Sympathetic dominated organ? (5)

A

Liver, kidney, adipose tissue, skin, blood vessels

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11
Q

PS dominated organ? (5)

A

Eyes, lungs, bladder/ureters/GIT

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12
Q

predominant method of action of trimetaphan

A

Receptor antagonism (but also ion channel blockade)

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13
Q

predominant method of action of hexamethonium

A

Ion channel blockade (but also receptor antagonism)

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14
Q

Use of trimetaphan?

A

IV for hypotension presurgery

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15
Q

other name for nicotinic receptor antagonist?

A

Ganglion blocking drugs

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16
Q

difference between receptor blockade antagonists and ganglion blocking drugs targets?

A

ganglion blocking drugs only target ANS nicotinic receptors, RBA can also target somatic NS

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17
Q

difference between receptor blockade antagonists and ganglion blocking drugs binding?

A

Ganglion blocking drugs are usually reversible RBA usually covalently bind and are irreversible

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18
Q

Another name for ganglion blocking drugs

A

Nicotinic receptor anatagonists

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19
Q

What part of the NS do muscarinic receptor antagonists target?

A

The PSNS

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20
Q

2 examples of muscarinic receptor antagonists?

A

Atropine, hyoscine

21
Q

Where are muscarinic receptors predominantly found? Exception is?

A

In the PSNS effector organs, exception is the sweat glands

22
Q

Atropine effects, normal and high dose?

A

Normal, does not do much.

High dose causes restlessness and CNS agitation

23
Q

Hyoscine effects, normal and high dose?

A

Sedative/amnesia at normal dose, high dose causes CNS depression and paradoxical CNS excitation

24
Q

Difference between hyoscine and atropine? What does this mean for its use

A

Hyoscine is more lipid soluble and so can penetrate the brain.

Other theory is that it is more M1 selective and so targets brain better.

25
Q

What is tropicamide used for? Its drug class? effect? Use?

A

Muscarinic receptor antagonist for the eye. Inhibits PS pupillary constriction and so causes dilation. used in eye exams

26
Q

What drugs are used as anaesthetic premeds?

A

Muscarinic receptor antagonists

27
Q

What is used for optical exams to dilate eyes

A

Tropicamide

28
Q

What effects do you want anaesthetic premeds to do? (3+1 for hyoscine)

A

Reduce secretions, reduce bronchoconstrictions, increase heart rate. Hyoscine also induces a little sedation

29
Q

What drug is used to stop motion sickness

A

Hyoscine patches

30
Q

How does hyoscine work to stop motion sickness?

A

Blocks muscarinic receptors in the vomiting centre

31
Q

Which neurons are important for fine control of movement

A

Nigrostriatal dopamine neurons

32
Q

What are nigrostriatal dopamine neurons important for

A

Fine movement

33
Q

What (name) neurons are lost in parkinsons

A

Nigrostriatal dopamine neurons

34
Q

Nigrostriatal dopamine neurons are lost in what disease

A

Parkinson’s

35
Q

What system is inhibitory to the dopaminergic system

A

Cholinergic

36
Q

How do muscarinic receptor antagonists help with parkinsons

A

Remove the inhibition caused by cholinergic (M4) neurons on the dopaminergic (D1) neurons

37
Q

What type of neurone is lost in parkinsons

A

D1 dopaminergic

38
Q

What drug is used to treat COPD and Asthma

A

Muscarinic receptor antagonist - ipratropium bromide

39
Q

How do muscarinic receptor antagonists help COPD and asthma

A

These block the PS constriction of the lungs so bronchodilation occurs.

40
Q

Why is ipratropium bromide especially good for asthma and COPD

A

Because it is a large polar molecule so cannot cross into the blood when inhaled and then cause muscarinic side effects

41
Q

How can muscarinic receptor antagonists help with irritable bowel syndrome

A

Block M3 mediated GI tone and motility, as well as secretions

42
Q

What are the main uses for muscarinic receptor antagonists (7)

A

Eye examination, anaesthetic premed, motion sickness, Parkinsons, COPD/asthma and irritable bowel syndrome

43
Q

4 sentences to help remember side effects of muscarinic receptor antagonists

A

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

44
Q

What are the side effects of muscarinic receptor antagonists (4)

A

Decreased sweating and thermoregulation, reduced secretions, ability to focus on nearby objects, CNS disturbance

45
Q

What is an inability to focus on nearby objects called

A

Cyclopegia

46
Q

What would be used for atropine/muscarinic receptor antagonists overdose? (3)

A

Bethanechol, ecothiopate or physostigmine

47
Q

How does botulinum toxin work

A

prevents the ACh from being exocytosed and getting to the synapse

48
Q

therapeutic use of botulinum toxin

A

Get rid of wrinkles or stop people sweating

49
Q

Effects of nicotinic receptor antagonists? (6)

A
Hypotension sympathetic causes vasoconstriction and increased renin secretion
Pupil dilation
Bronchodilation
Bladder Dysfunction
Decrease GI tone
Decrease in secretions