Cholinoceptor antagonists Flashcards

1
Q

Where can nicotinic receptors have its effect?

A
  • they are always present on autonomic ganglia

- therefore they have the ability to interfere with the whole ANS

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2
Q

Where can drugs targeting muscarinic receptors have their effect?

A
  • they are present within the effector organs of the PNS and sweat glands innervated by the SNS
  • drugs effecting muscarinic receptors will be much more specific
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3
Q

What else are nicotinic receptor antagonists called and why?

A
  • ganglion blocking drug

- they block the action of nicotinic receptors that lie at the ganglion

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4
Q

WHat 2 ways can you interfere with an ion-channel linked receptor?

A
  • blocking the receptor

- blocking the ion channel

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5
Q

What are 2 clinical examples of nicotinic receptor antagonists?

A
  • hexamethonium (better at blocking the channel pore)

- trimetaphan (better at blocking the channel receptor)

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6
Q

What determines the effect of the drug on the body?

A
  • they are tissue specific, it depends which branch of the ANS predominates in a particular tissue
    e. g if sympathetic predominates those effects will be lost and vise versa
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7
Q

Which tissues are sympathetically dominated?

A
  • kidneys

- blood vessels

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8
Q

Which tissues are parasympathetically dominated?

A
  • eyes
  • lungs
  • bladder, ureter, GI tract
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9
Q

What types of secretions will cholinoceptor blockade also stop?

A

-exocrine (cannot sweat and issues producing saliva)

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10
Q

what was hexamethonium used for?

A

-anti-hypertensive

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11
Q

why was hexamethonium suspended?

A
  • wide side effect profile

e. .g loss of bladder control, pupil dilation, loss of GI motility

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12
Q

What is trimetaphan used for?

A
  • surgery when controlled hypotension is needed

- very short acting

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13
Q

Where are receptor blockade antagonists mostly found?

A
  • toxins and venoms

- irreversible they lead to a total loss of autonomic function

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14
Q

Why are muscarinic receptor antagonists more useful?

A
  • more specific

- target parasympathetic effector organs and sweat glands vs everything

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15
Q

List 3 different muscarinic receptor antagonists

A
  • atropine
  • hyoscine
  • tropicamide
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16
Q

What is tropicamide used for?

A
  • paralyses smooth muscle of the eye responsible for contraction
  • pupil can then fully dilate for examination
17
Q

How are muscarinic receptor antagonists used in anaesthetic premedication?

A
  • dilates the airway

- production of copious watery secretions is blocked

18
Q

How does a hyosciene patch work for motion sickness?

A
  • blocks muscarinic receptors at the vomiting centre preventing nausea
19
Q

How do muscarinic receptor antagonists treat Parkinsons disease?

A
  • block the M4 receptor so the inhibitory effect to dopamine is blocked
  • creating a bigger response to dopamine and decreasing parkinson’s
20
Q

How is asthma treated?

A

-ipratropium bromide or atropine are used to block the constriction pathway

21
Q

How is IBS treated?

A

M3 receptor antagonists reduce side effects, block parasympathetic activity of a hyperactive gut

22
Q

What are the unwanted side effects of muscarinic receptor antagonists?

A
  • hot as hell (decreased sweating, lack of thermoregulation)
  • dry as a bone (lack of secretions)
  • blind as a bat (cyclopegia)
  • mad as a hatter (CNS disturbance)
23
Q

How do you teat atropine poisoning?

A
  • bethanechol (stable version of acetylcholine and will outcompete atropine)
  • physostigmine (blocks acetylcholinesterase enzyme , it allows acetylcholine to build up in the synapse and out compete atropine)
24
Q

How is the botulinum toxin toxic?

A
  • blocked SNARE protein complex involved with exocytosis of acetylcholine- cannot have an effect on the muscle and is therefore paralysed
  • used in botox- paralyses skeletal muscle in the skin but has to be tightly regulated as it is extremely toxic