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SfM > Autonomic & NMJ Pharmacology > Flashcards

Autonomic & NMJ Pharmacology Flashcards

1
Q

What are the two types of cholinergic receptors?

A
  • Nicotinic (selectively activated by nicotine) - ionotropic (ligand gated) with an integral ion channel
  • Muscarinic (selectively activated by muscarine) - split into M1/2/3 based on what G protein they’re coupled to and therefore 2nd messenger signals they produce
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2
Q

What are the types of adrenergic receptors?

A

All metabotropic are are split into a1/2/3 and B1/2/3/4

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3
Q

Steps in synaptic transmission

A
  1. Transmitter synthesis and packaged into vesicles
  2. AP activates voltage gated Ca2+ channels
  3. Triggers Ca2+ dependent exocytosis of pre-packaged vesicles of transmitter
  4. Binds to iono/metaboltropic receptors of postsynaptic membrane
  5. Also binds to presynaptic autoreceptors which inhibit further transmitter release
  6. Transmitter inactivated and uptake into neurones and glia
  7. Transmitter metabolised with cells
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4
Q

What does hemicholinium do at the NMJ?

A

Inhibits choline transporter

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5
Q

What does Black widow spider venom do at the NMJ?

A

Block voltage gates Ca2+ channels

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6
Q

What does botulinum toxin at the NMJ?

A

Block vesicle fusion

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7
Q

What does d-tubacurarine do at the NMJ?

A

It is a non-depolarising nicotinic receptor blocker

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8
Q

What does succinylcholine do at the NMJ?

A

It is a depolarising nicotinic receptor blocker

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9
Q

What does eserine do at the NMJ?

A

Block acetylcholinesterase - inhibit ACh break down so it remains in the synaptic cleft

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10
Q

What are non-depolarising and depolarising blockers used for?

A

Paralysis during:

  • Surgery
  • Electroconvulsive therapy
  • Controlling spasms in tetanus
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11
Q

What is botox used for?

A

Treating muscle spasm and cosmetic procedures

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12
Q

What is anticholinesterase used for?

A
  • Treating myasthenic syndromes
  • Reversing action of non-depolarising blockers
  • Countering botulinum poisoning
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13
Q

Potential sites of action for drugs on the postganglionic parasympathetic transmission

A
  • Muscarinic receptor antagonists

- Muscarinic receptor agonists - mimic effects

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14
Q

Action on Atropine on postganglionic parasympathetic transmission

A

Muscarinic receptor antagonist

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15
Q

Pilocarpine

A

agonist of muscarinic receptors

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16
Q

What are muscarinic receptor antagonists used for?

A

Block effects of parasympathetic system

17
Q

What are muscarinic receptor agonists used for?

A

Mimic effects of parasympathetic system

18
Q

Problem associated with postganglionic parasympathetic transmission drugs

A

Not many specific agonist or antagonists available so the drug mimics or blocks all effect caused of para sympathetic NS unless you can deliver drug straight to site of action (inhalation to lungs, eyedrops)

19
Q

What can muscarinic agonists treat?

A

Glaucoma (raised intraoccqular pressure) - agonists contract ciliary muscle and contract the sphincter muscle of the pupil which opens trabecular network and increase drainage of the aqueous humour - MITOTIC DRUGS

20
Q

What is miosis?

A

Making pupil smaller

21
Q

What does carbidopa do in the postgang sympathetic transmission?

A

Blocks the enzymes that produce NA

22
Q

What does reserpine do in the postgang sympathetic transmission?

A

Block the transporter that fills the vesicles with NA

23
Q

What does methyldopa do in the postgang sympathetic transmission?

A

‘False’ transmitter - packaged and released as NA but cannot activate adrenergic receptors

24
Q

What does amphetamine do in the postgang sympathetic transmission?

A

Stimulate NA release - sympathomimetic amines

25
Q

What are sympathomimetics?

A

Drugs that potentiate the synapses and make them work better

26
Q

What do cocaine and tricyclic antidepressants do in the postgang sympathetic transmission?

A

Inhibit uptake into neurones

27
Q

What do phenylephrine and salbutamol do in the postgang sympathetic transmission?

A

Activate postsynaptic receptors

28
Q

What can a1 agonist be used for?

A

Decongestants and to dilate the pupil

29
Q

What can a2 agonists be used for?

A

Treatment of hypertension (high blood pressure)- inhibit transmitter release

30
Q

What can B2 agonists be used for?

A

Treating asthma

31
Q

What can B1 antagonists be used for?

A

Treating hypertension, angina, cardiac arrhythmias and glaucoma

32
Q

Action of hexamethoneum of the ANS?

A

Block ACh activated channel

SfM (12 decks)

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