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ICPP > ICPP 8 ANS Neurochemistry + Pharmacology > Flashcards

ICPP 8 ANS Neurochemistry + Pharmacology Flashcards

1
Q

Where do drugs work?

A

At points of chemical communication

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2
Q

Common locations for drug action

A
  • Degradation of transmitter
  • Interaction of transmitter with post-synaptic receptors
  • inactivation of transmitter
  • re-uptake of transmitter (neuronal)
  • interaction with pre-synaptic receptors
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3
Q

Describe acetylcholine synthesis

A

Acetyl CoA + choline > acetylcholine + coenzyme
choline acetyl transferase

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4
Q

Enzyme involved in ACh synthesis

A

Choline acetyl transferase

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5
Q

Describe acetylcholine degradation

A

Acetylcholine > acetate + choline
(acetyl)cholinesterase

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6
Q

Enzyme in ACh degradation

A

(Acetyl)cholinesterase

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7
Q

What does SLUDGE stand for?

A

Salivation
Lacrimation
Urination
Defecation
Gastrointestinal upset
Emesis

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8
Q

What is emesis

A

Vomiting

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9
Q

Cause of SLUDGE

A

Drug overdoes
Ingestion of magic mushroms
Exposure to organophosphorus insecticides
Exposure to nerve agent e.g. novichock

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10
Q

Effect of organophosphorus insecticides + nerve agents

A

Covalently modify cholinesterase
Irreversibly deactivate
Increase in ACh
Pronged over stimulation of Muscarinic receptors

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11
Q

Treatment of SLUDGE

A

Atropine
Pralidoxine
Anti-choleric agents

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12
Q

What does atropine do?

A

Reverse the modification of cholinesterase

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13
Q

What is SLUDGE a mnemonic for?

A

Pathological effects indicative of massive discharge of parasympathetic nervous system

Due to prolonged overstimulation of Muscarinic receptors

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14
Q

What drugs can be used to block nicotinic ACh receptors?

A

Ganglion blocking drugs
e.g. Trimethaphan

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15
Q

Nicotinic ACh receptors in ANS vs SNS
What does this mean for drugs?

A

Structure differs between autonomic + somatic
Drug only effects one, not both

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16
Q

What drugs can be used to decrease ACh degradation?

A

Cholinesterase inhibitors
e.g. pyridostigmine, donepezil

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17
Q

Why do drugs acting on Muscarinic ACh receptors often have side effects?

A

5 subtypes M1-5
Difficult to make drug for specific subtype

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18
Q

What drugs are muscarinic ACh receptor agonists?

A

pilocarpine
bethanechol

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19
Q

What type of drug is pilocarpine?

A

Muscarinic ACh receptor agonist

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20
Q

What type of drug is bethanechol?

A

Muscarinic ACh receptor agonsit

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21
Q

Clinical use of pilocarpine

A

Treat glaucoma

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22
Q

What is glaucoma?

A

Eye disease
Increased pressure
Damage to optic nerve

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23
Q

Clinical use of bethanechol

A

Stimulate bladder emptying

24
Q

What drugs are muscarinic ACh receptor antagonists?

A

ipratropium + tiotopium
tolterodine, darifenacin + oxybutynin
hyoscine (scopolamine)

25
Q

What type of drug is ipratropium?

A

Muscarinic ACh receptor antagonist

26
Q

What type of drug is tiotropium?

A

Muscarinic ACh receptor antagonist

27
Q

What type of drug is tolterodine?

A

Muscarinic ACh receptor antagonist

28
Q

What type of drug is darifenacin?

A

Muscarinic ACh receptor antagonist

29
Q

What type of drug is oxybutynin?

A

Muscarinic ACh receptor antagonist

30
Q

What type of drug is hyoscine?

A

Muscarinic ACh receptor antagonist

31
Q

Clinical use of ipratorpium

A

Treat asthma + COPD

32
Q

Clinical use of tiotropium

A

Treat asthma and COPD

33
Q

Clinical use of tolterodine

A

Treat overactive bladder

34
Q

Clinical use of darifenacin

A

Treat overactive bladder

35
Q

Clinical use of oxybutynin

A

Treat overactive bladder

36
Q

Clinical use of hyoscine

A

Treat IBS + post operative nausea

37
Q

Describe the process of noradrenaline synthesis

A

Tyrosine > DOPA > dopamine > noradrenaline

38
Q

What is the precursor for noradrenaline?

A

Tyrosine

39
Q

What enzyme converts noradrenaline into adrenaline?

A

Phenylethaloamine M-methyltransferase

40
Q

What does phenylethaloamine M-methyltransferase do?

A

Convert noradrenaline to adrenaline in adrenal medulla

41
Q

Describe transmission of noradrenaine

A

1- NA release by Ca2+ dependent exocytosis
2- diffuses across the synaptic cleft
3- acts on post synaptic adrenoreceptors
4- rapidly removed from synaptic cleft by NET

42
Q

How is noradrenaline released?

A

Ca+ dependent exocytosis

43
Q

What receptors does noradrenaline act on?

A

Adrenoreceptors

44
Q

What is NET?

A

Norepinephrine (noradrenaline) transporter

45
Q

What is NET dependent on?

A

Na+

46
Q

What is noradrenaline action terminated by?

A

Re-uptake using NET (uptake 1)

47
Q

Affinity of NET

A

High affinity

48
Q

What happens to noradrenaline not re-captured by uptake 1?

A

Taken up by non neuronal mechanism (uptake 2)
Lower affinity

49
Q

Affinity of uptake 2

A

Lower affinity than NET

50
Q

What happens to noradrenaline not in pre-synaptic vesicles?

A

Susceptible to metabolism by monoamine oxidase + catechol O methytransferase

51
Q

What enzymes metabolise noradrenaline not in vesicles?

A

Monoamine oxidase
Catechol O methyltransferase

52
Q

Clinical use of salbutamol

A

Treat asthma - reverse bronchoconstriction

53
Q

What drug is a B2-adrenoreceptors selective agonist?

A

Salbutamol

54
Q

What drug is an a1-adrenoreceptors selective agonist?

A

Doxazosin

55
Q

What drug is a B1-adrenoreceptors selective agonist?

A

atenolol

56
Q

Clinical use of doxazosin

A

Treat CVS disorders
e.g. hypertension

57
Q

Clinical use of atenolol

A

Treat CVS disorders
e.g. hypertension

ICPP (18 decks)

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