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Med Chem modules > Neuropharmacy II > Flashcards

Neuropharmacy II Flashcards

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1
Q

What is an allosteric modulator?

A

Binds to receptor but to different site to agonist
Causes an allosteric change in the receptor which alters the affinity for the agonist
This accordingly alters the receptor occupancy for the agonist, altering the extent of agonist action

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2
Q

How does benzodiazepines alter GABAergic transmission?

A

Benzodiazepines are positive allosteric modulators, so increase GABAergic transmission

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3
Q

How does dosage of benzodiazepine affect pharmacological outcome?

A

Large dose

Anaesthesia 
Muscle relaxation
Hypnosis 
Sedation 
Ataxia
Anticonvulsant 
Anxiolytics

Small dose

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4
Q

What is the name and time span of a short term benzodiazepine?

A

Triazolam

8-16h

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5
Q

What is the name and time span of a medium acting benzodiazepine?

A

Diazepam

32h

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6
Q

What is the name and time span of a long acting benzodiazepine?

A

Clonazepam

55 h

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7
Q

What is the cellular effect of GABA(A)-R activation?

A

Cl pore opens
Cl ions flow into cell
Cell is hyperpolarised

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8
Q

Which benzodiazepine would you use for hypnosis?

A

Triazolam

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9
Q

Which benzodiazepine would you use as an anxiolytic?

A

Diazepam

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10
Q

Which benzodiazepine would you use as an anticonvulsant?

A

Clonazepam

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11
Q

What effects are seen from barbiturates at low doses?

A

Anxiolytic and sedative

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12
Q

What effects are seen from barbiturates at high doses?

A

Fatality due to respiratory depression and cardiovascular collapse

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13
Q

Why are barbiturates no longer used as anxiolytics?

A

Anxiolytic effects are only seen at sedative doses
Induction of P(450) in the liver causes drug tolerance
Dangerous in overdose (problem in suicide prone patients)
They have additive effects with other CNS depressants (e.g. Alcohol)

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14
Q

How is serotinergic transmission targeted in anxiolysis

A

Busiprone:

Agonist to 5HT(1A) presynaptic autoreceptors to reduce 5HT exocytosis

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15
Q

How is noradrenergic transmission targeted in anxiolysis?

A

Clonidine:

Agonist to alpha 2 autoreceptors to reduce NA exocytosis

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16
Q

what are the two major categories of epilepsy?

A

Partial

Generalised

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17
Q

How do the two different types of epilepsy differ?

A

For partial:
Seizures begin in a particular area of the brain involving only one side

For general:
Seizures begin with an electrical discharge involving both sides of the brain

18
Q

What ion channels can be targeted to reduce neuronal excitability?

A

Na-VGIC

T-type Ca-VGIC

19
Q

Give examples of sodium channel blockers

A

Phenytoin
Carbamazepine
Valproate

20
Q

Give an example of a T-type Ca- channel blocker

A

Ethosuximide

21
Q

What does valproate do?

A

Blocks Na channel

Inhibits GABA transaminase (increases brain GABA)

22
Q

What role does diazepam have as an anticonvulsant

A

Increases efficacy of Postsynaptic GABA transmission by allosteric modulation

23
Q

What role does Phenobarbitone have in anti-epileptics?

A

Increases efficacy for GABA transmission

Directly increases Cl influx

24
Q

How can the NMDA receptor be targeted for epilepsy?

A

Felbamate:
Blocks NMDA
Binds to glycine site

25
Q

How can the AMPA receptor be targeted for epilepsy?

A

Parampanel:

Non-competitive antagonist of AMPA

26
Q

Name 3 currently used volatile anaesthetics

A

Halothane
Isoflurane
Nitrous oxide

27
Q

How do you increase anaesthetic potency?

A

Unsaturation
Halogenation
Ether groups

28
Q

What is a MAC?

A

Minimum alveolar concentration

The concentration of anaesthesia in the air air inspired giving a safe level of anaesthesia in 50% of patients

29
Q

Does a potent anaesthetic have a low MAC?

A

Yes,

Potency is inversely proportional to the MAC

30
Q

Name 4 intravenous anaesthetics

A

Thiopentone
Propofol
Etomidate
Ketamine

31
Q

Which general anaesthetics work through potentiation of GABA(A) receptor transmission

A 
Halothan
Isoflurane
Thiopentone
Propofol
Eromidate
Nitrous oxide
32
Q

Which general anaesthetics work through inhibition of excitatory transmission

A 
Halothane
Isoflurane
Nitrous oxide
Thiopentone
Propofol
Ketamine
33
Q

Which nerve fibres transmit the perception of pain?

A

C fibres

34
Q

Which types of tissue damage produces pain?

A

Inflammation

Neuropathy

35
Q

How might hypersensitivity be produced at spinal level?

A

Repetitive painful stimulation on the c-fibres can cause them to enter a high state of excitability
Different pain states then converge on common pathways to the spine

36
Q

What voltage channels can be blocked to alleviate pain?

A

NMDA

AMPA

37
Q

What drugs block the NMDA channel?

A

Ketamine

Gabapentin

38
Q

What drugs block the AMPA channel

A

Carbamazepine

Lignocaine

39
Q

How might pain be reduced by suppression of excitatory NT release?

A

Inhibition of presynaptic Ca channels would prevent NT vesicle exocytosis

K channels may be open hyperpolarising the cell so Ca channels won’t open

40
Q

What are the endogenous opioids and receptors?

A

Mu- endorphin
Delta- enkaphalin
Kappa- dynorphin
Orl-1- nociceptin

41
Q

Name some exogenous opiates used for analgesia

A

Morphine

Codeine

42
Q

Which transmitters are involved in the descending pathways that regulate nociception?

A

Substance P
CGRP
glutamate
Aspartate

Med Chem modules (8 decks)

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