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Pharmacy Year 2 Semester 1 > Patient: Cholinergic drugs > Flashcards

Patient: Cholinergic drugs Flashcards

1
Q

Difference between muscarinic and nicotinic acetylcholine receptors

A

Muscarinic: G-protein coupled, slow

Nicotinic: ligand-gated ion channel, fast transmission

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2
Q

Name 3 sites of action for nicotinic acetylcholine receptors

A

CNS, NMJ, autonomic ganglia

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3
Q

Name 3 sites of action for muscarinic acetylcholine receptors

A

CNS, Parasympathetic nervous system, sympathetic nervous system

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4
Q

Describe nicotinic acetylcholine receptors using this:

1) -meric
2) number of subunits and receptor subtypes
3) built in/g protein
4) number of Ach sites
5) speed of response

A

1) Pentameric
2) 18 subunits of multiple types
3) built in ion channel
4) 2 Ach sites
5) microseconds to milliseconds

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5
Q

Describe muscarinic acetylcholine receptors using this:

1) -meric
2) number of subunits and receptor subtypes
3) built in/g protein
4) number of Ach sites
5) speed of response

A

1) Monomeric
2) M1-5 subtypes, 5 receptor sites
3) Binding site for G protein
4) 1 Ach site
5) milliseconds to seconds

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6
Q

Agonists of nicotinic acetylcholine receptors

A

nicotine, suxamethonium

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7
Q

Antagonists of nicotinic acetylcholine receptors

A

atracurium, tubocurarine, alpha-bugarotoxin

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8
Q

Agonists of muscarinic acetylcholine receptors

A

pilocarpine, muscarine

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9
Q

Antagonists of muscarinic acetylcholine receptors

A

atropine, hyoscine

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10
Q

Drugs acting at ACh

A 
Paralyzing agents used in surgery*
Drugs to treat nicotine addiction*
Anti-emetic drugs*
Anti-asthma drugs*
Drugs used in eye exams
Drugs used to treat glaucoma
?Alzheimer’s disease drugs*
?Parkinson’s disease drugs
?Anti-schizophrenia drugs
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11
Q

Drugs acting on ACh metabolism/release

A 
ACh esterase (AChE)
Drugs to treat myasthenia gravis*
Drugs to treat Alzheimer’s disease*
Drugs to treat glaucoma
Nerve gases, insecticides*
ACh release
Botox*
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12
Q

Name two type of blockers to neuromuscular transmission

mechanism-wise

A

Competitive antagonists at nAChR (flaccid paralysis)

Depolarising blockers agonists at nAChR

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13
Q

How to reverse the effect of a competitive antagonist at the nAChR

A

Can be reversed by AChE inhibitors

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14
Q

Can depolarising blockers (agonists at nAChR) be reversed with AChE inhibitors?

A

No

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15
Q

Name a use of a neuromuscular transmission blocker

A

muscle relaxation in surgery

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16
Q

Muscle relaxation doing surgery.. name some drugs which use the competitive antagonist of nAChR route

A 
Atracurium
Pancuronium
Vecruonium
Gallamine
Tubocurarine
17
Q

Muscle relaxation doing surgery.. name some drugs which use the depolarising blocker agonists at nAChR route

A

Suxamethonium

Decamethonium

18
Q

What is Suxamethonium hydrolysed by? How long does it work for?

A

serum ChE

fast recovery - 3 minutes

19
Q

How does Atracurium break down?

A

Spontaneously breaks down

20
Q

Duration of action for Pancuronium? Uses?

A

100-200 minutes

Used for euthanasia and executions

21
Q

Tell me about a receptor involved in nicotine addiction/smoking cessation

A

Receptor containing α4 and β2 subunits may be important in nicotine addiction
Varenicline (Champix) = partial agonist at α4β2 receptor.
NICE concludes it is cheaper long term than NRT or bupropion

22
Q

Are agonists used with muscarinic drugs? Name two

A 
Agonists not widely used
apart from
Pilocarpine in glaucoma 
and
bethanechol in bladder disorders
23
Q

Name 3 general effects of muscarinic antagonists

A
  • tachycardia
  • inhibits secretions (saliva, gastric acid)
  • relaxes smooth muscle (GI tract, bronchi)
24
Q

Name some therapeutic effects of muscarinic antagonists

A

Anti-emetic
Anti-parkinsonian
(Amnesia, sedation)

25
Q

Name some muscarinic antagonists

A

Atropine
Tiotropium, ipratropium
Hyoscine
Darifenacin, solifenacin

26
Q

Use of Atropine

A

Prevent bronchial secretions during surgery

27
Q

Use of Tiotropium and ipratropium

A

Inhaled bronchodilators in asthma

quaternary ammonium salts so not absorbed systemically

28
Q

Use of Hyoscine

A

treat motion sickness

29
Q

Use of Darifenacin and Solifenacin

A

Treat M3 selective bladder hyperactivity

30
Q

How does botulinum toxin work?

A

Blocks release of ACh by breaking down SNARE proteins

31
Q

Effects of botulinum

A

Paralysis of skeletal muscle, autonomic block

systemic effects can cause death

32
Q

Use of botulinum

A

Can be used to paralyse muscles on a local basis

muscle spasm treatment and cosmetic wrinkle removal

33
Q

List some irreversible acetylcholinesterase inhibitors

A

Sarin, VX

34
Q

What are sarin and VX used for?

A

irreversible acetylcholinesterase inhibitors
nerve gases and insecticides
causes muscle paralysis and over-activation of the autonomic nervous system (especially the parasympathetic route)

35
Q

How to counteract the effects of sarin and VX

A

Atropine can counter some symptoms via mAChR

Pralidoxime regenerates enzyme if administered within five hours.

36
Q

Name some competitive reversible AChEsterase inhibitors

A

Edrophonium
Physostigmine
Neostigmine
Rivastigmine

37
Q

Name some non-competitive reversible AChEsterase inhibitors

A

Tacrine

Donepezil

38
Q

When are reversible AChEsterase inhibitors used?

A

In situations where there needs to be a boost cholinergic transmission

39
Q

Clinical uses of reversible AChEsterase inhibitors

A

Reversal of non-depolarizing NMJ blocker e.g. pancuronium
Autoimmune myasthenia gravis
immune attack on nAChR in NMJ. Increasing ACh boosts transmission via remaining receptors
increases muscle strength
edrophonium (test); pyridostigmine, neostigmine, physostigmine
Alzheimer’s disease
loss of cholinergic neurons
tacrine, donepezil

Pharmacy Year 2 Semester 1 (32 decks)

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