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fundamental neuroscience > fundamental neuropharmacology > Flashcards

fundamental neuropharmacology Flashcards

1
Q

what is neuropharmacology?

A

the study of drugs that affect the NS and how they affect the NS.

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2
Q

what aspects of the NS do drugs effect?

A

sensory perception,
motor function,
seizure activity,
mood,
higher cognitive function,

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3
Q

what is picrotoxin?

A

a non-competitive GABA-A receptor antagonist.

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4
Q

what is tetratoxin (TTX)?

A

a potent neurotoxin that is poisonous to humans.

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5
Q

what can TTX be treated with?

A

a neostigmine

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6
Q

what are symptoms of TTX poisoning?

A

paralysis,
muscle weakness,
bradycardia,
cardiac arrest.

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7
Q

what is d-tubocurarine?

A

an alkaloid,

and an antagonist of acetylcholine.

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8
Q

which type of plant, often used to make spears, contains d-tubocurarine?

A

curare vine - liana.

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9
Q

what is novichok, what does it affect, and what does it cause?

A

a nerve agent.

inhibits acetylcholinesterase.

causes spasms, prevents relaxation of muscles (cardiac and respiratory).

very fast acting.

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10
Q

what did the leech test find?

A

that

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11
Q

NT criteria:
NT’s must be …

A

synthesised and released from neurons.

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12
Q

NT criteria:
NT should be released from nerve terminals in a …

A

… chemically or pharmacologically identifiable form.

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13
Q

NT criteria:
A NT should reproduce …

A

… at the postsynaptic cell the specific events that are seen after stimulation at the presynaptic neuron.

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14
Q

NT criteria:
Effects of NT should be blocked …

A

… by competitive antagonists of the receptor for that transmitter in a dose-dependent manner.

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15
Q

what are the 2 classes of receptors?

A
  1. ionotropic.
  2. metabotropic or G-protein coupled.
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16
Q

what is a ligand?

A

any chemical that binds/combines with a receptor.

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17
Q

what is a receptor?

A

a cellular macromol/mols that is concerned in chemical signalling between and within cells.

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18
Q

what type of process is the binding of ligands and receptors?

A

an active process.

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19
Q

what are endogenous ligands?

A

ligands that are naturally produced by the body.

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20
Q

what are exogenous ligands?

A

endogenous ligands that are modified or designed by chemists.

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21
Q

what were radioligands binding assays used for?

A

they were used to quantify the amount of ligand bound to receptors.

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22
Q

what is non-specific binding?

A

binding in a place other than the binding site that it under investigation.

it is unsaturable.

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23
Q

how can specific binding be calculated?

A

by calculating the difference between total and nonspecific binding.

24
Q

what does specific binding in a radioligand assay reflect?

A

it reflects the amount of radioligand bound to specific binding site.

25
Q

what is total binding?

A

the total binding observed - specific and non-specific.

26
Q

what shape would non-specific binding be on a graph? why?

A

linear - because its constantly happening.

27
Q

what shape would specific binding be on a graph? why?

A

curve then levels out - happens as max is eventually reached.

28
Q

Bmax

A

maximum saturated binding which is achievable.

29
Q

kd

A

dissociation constant = the affinity of binding that results in 50% of maximal binding (Bmax).

30
Q

what are the 2 types of ligands?

A

agonist,
antagonist.

31
Q

what does an agonist do?

A

produces effects in bio tissues

32
Q

what are the 3 types of agonists and what effects do they have?

A

full = produce max effect.

partial = effect but not maximal.

inverse = produces effects that are opposite from the original. can be partial or full.

33
Q

what do antagonists do?

A

they prevent the effect of an agonist but have no effect themselves.

34
Q

what are the 2 types of antagonists?

A

competitive and non-competitive.

35
Q

what do competitive antagonists do?

A

compete with the agonist for the same binding site on the receptor.

36
Q

do competitive antagonists effect the efficacy of the agonist? why?

A

no, they do not as the same number of receptors are available to both.

37
Q

what do non-competitive antagonists do?

A

they bind to a different binding site and alter the configuration of the receptors for agonists so they can’t bind.

38
Q

do non-competitive antagonists effect the efficacy of agonists?

A

yes they do as they reduce the number of receptors available for agonists to bind to.

39
Q

what happens when agonists are repeatedly used?

A

desensitisation.

40
Q

what can partial agonists act as? how do they do this?

A

as a functional antagonist because when they are in the presence of a full agonist, it reduces the ability of the full agonist to produce maximal effects.

41
Q

what does efficacy mean?

A

the ability of a drug to produce a max response of effect when binding.

42
Q

what does potency mean?

A

the amount of drug needed to produce a certain effect.

43
Q

Emax

A

maximal response that drugs produce.

44
Q

EC50

A

effective concentration in vivo.

45
Q

ED50

A

the does needed to produce 50% max response.

46
Q

what do psychotropic drugs do?

A

they influence behaviour

47
Q

what is pharmacodynamics?

A

the study of drugs that looks at what the drug does to the body - the time course of its effects the intensity of them.

48
Q

what is pharmacokinetics?

A

the study of what the body does to a drug - how it is absorbed, metabolised, etc.

movements of drugs in the body.

49
Q

what is bioavailability?

A

the ability of a drug to produce an effect of an organism is dependent on many properties

50
Q

what are the 6 stages of pharmocokinetics?

A
  1. route of administration.
  2. release/liberation.
  3. absorption.
  4. distribution (dosing regiments).
  5. metabolism (metabolite kinetics, clearance).
  6. excretion (clearance).
51
Q

what are the 3 most popular routes of administration?

A

oral, intravenous, subcutaneous.

52
Q

what is the bioavailability of a drug affected by?

A

by the absorption of a drug.

by metabolism and excretion.

53
Q

Cmax

A

peak plasma conc of drug after administration.

54
Q

tmax = time to reach Cmax.

A
55
Q

what are the 3 fundamentals of clearance?

A
  1. vol of distribution.
  2. clearance.
  3. elimination half-life.

fundamental neuroscience (13 decks)

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