neuromuscular pharmacology Flashcards

1
Q

what is pharmacology

A

how drugs interact with living organisms to produce a change in function

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2
Q

what is pharmacodynamics

A

what the drug does to the body
- what does it target
- what is the response

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3
Q

what is parmacokinetics

A

what the body does to the drug
- movement of the drug within the body
- where does the drug go
- therapeutic plasma concentration (concentration in blood effective but not toxic)

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4
Q

what is pharmacy

A

storing, prescribing and dispensing drugs

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5
Q

what are the different considerations when selecting, prescribing, and dispensing different drugs

A
  • correct indication with no contraindications
  • efficacy
  • route of administration
  • legalisation
  • pathophysiological status of the animal (young, old, pregnant, other disorders)
  • short (acute) vs. long term (chronic) therapy
  • cost
  • owner education
  • farm animal (meat/milk withdrawal, individual vs. group therapy)
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6
Q

what is efficacy

A

the effectiveness of the drug to treat the condition
- evidence based
- underlying science is important
- NOT the same as potency (how strong the drug is)

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7
Q

what is the regulatory body for veterinary medicines

A

Veterinary Medicines Directorate

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8
Q

what is absorption and reuptale of drugs influenced by

A
  • route of administration
  • physiochemical properties of the drug
  • status of gastro-intestinal tract (acidity of stomach, motility)
  • taken with food
  • formulation (fast acting vs. slow release
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9
Q

how are drugs distributed

A
  • transported in the plasma
  • most drugs temporarily bind to a plasma protein
  • will unbind (become active) and leave the blood to target different body fluids
  • different drugs will distribute to a lesser or greater extent
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10
Q

what are the 4 main targets that the drug interacts with to exert its effects within the body

A
  • receptors
  • ion channels
  • enzymes
  • carrier
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11
Q

what is an agonist

A

drugs that bind receptor and activate them (sgtimulate a particular function)

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12
Q

what is an antagonist

A

drugs that bond receptors but do not activate them (block the effects of agonsists)

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13
Q

what is an example of a drug that acts on an ion channel

A

lidocaine
- blocks sodium channels to prevent depolarisation and firing of the nerve synapse

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14
Q

how do drugs interact with enzymes

A

typically, a drug is an enzyme inhibitor and thus decrease their activity
- penicillin blocks cell wall synthesis in E. Coli

most drugs target enzymes

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15
Q

how are drugs eliminated by metabolism

A
  • can be metabolised by liver and inactivated
  • drug metabolite (metabolised product) often excreted by the kidney
  • the goal of metabolism is to make the drug more easily soluble by water (make it more polar and hydrophilic) so that it can be excreted by the kidney
  • some drugs are directly excreted by through the urine by the kidney (often polar)
  • renal diseases can impact the ability to excrete drugs properly, leading to a build up in the body
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16
Q

what are the events, in chronological order, that a drug will take through the body

A
  1. absorption
  2. distribution
  3. metabolism
  4. excretion
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17
Q

what are the unwanted side effects of a drug

A
  • adverse events (predicted vs idiopathic (not predicted))
  • drug has no effect (not even intended effect)
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18
Q

true or false: a free, unbound drug is active

A

True

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19
Q

do most drugs bind temporarily to albumin?

A

yes

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20
Q

rank the following mechanisms from fastest to slowest
- secondary messengers
- nuclear receptors
- ligand gated ion channels

A
  1. ligand gated ion channels
  2. secondary messengers
  3. nuclear receptors
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21
Q

The Veterinary Medicine Directorate (VMD) runs a scheme to monitor unwanted effects of drugs - what ois it called

A

SARSS

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22
Q

The VMD scheme to report adverse medicines includes what groups

A
  • animals
  • humans
23
Q

name the main components of the autonomic nervous system

A
  • the sympathetic system
  • the parasympathetic system
  • the enteric system
24
Q

what is a precursor for acetylcholine

A

choline

25
Q

what are the 2 receptors that acetylcholine binds to

A
  • muscarinic
  • nicotinic
26
Q

what effects would IV atropine have on a cat?

A
  • tachycardia (increased HR)
  • Dries secretions
  • pupil dilation
27
Q

what is an example of a nicotinic agonist that is used therapeutically

A

suxamethonium

28
Q

how does botulinum toxin work

A

binds pre-synaptically to prevent acetylcholine release

29
Q

what is the precursor of noradrenaline

A

tyrosine

30
Q

which enzymes degrade noradrenaline

A
  • monoamine oxidase
  • catechol-O-methyltranferase
31
Q

dexmedetomdine is commonly used sedative and alagesic drugs used in dogs and cats. which receptors does it target

A

presynaptic alpha 2 receptors

32
Q

anitpamezole is an alpha 2 receptor antagonist. what will happen if you give it after an alpha 2 agonist

A

antagonism of the agonist

33
Q

which types of drugs improve cognitive function in elderly dogs

A

mono amine oxidase inhibitors

34
Q

what is the effect of activation of an alpha 1 receptor

A

vasoconstriction

35
Q

what are neurotransmitters and what are the major ones of interest

A

a chemical substance which is release at the end of a nerve fibre by the arrival of a nerve impulse and by diffusing across the synapse or junction which effects the transfer of the impulse to another fibre
- acetylcholine
- dopamine
- GABA
- glutamate
- noradrenaline
- histamine
- etc…

36
Q

what is the stepwise process involved in synthesis, storage and release of amine and amino acid transmitters

A
  1. uptake of precursors
  2. synthesis of transmitter
  3. uptake/transport of transmitter into vesicles
  4. degradation of surplus transmitter
  5. depolarisation by propagated action potential
  6. influx of calcium ions in response to depolarisation
  7. release of transmitter by exocytosis
  8. diffusion to postsynaptic membrane
  9. interaction with postsynpatic receptors
  10. inactivation of transmitter
  11. reuptake of transmitter or degradation products by nerve terminals
  12. uptake and release of transmitter by non-neuronal cells
  13. interaction with presynaptic receptors
37
Q

what type of transmitters fo cholinergic nerves have

A

acetylcholine transmitters

38
Q

what are the 2 receptors that noradrenaline bind to

A
  1. alpha
  2. beta
39
Q

give an example of a muscarinic agonist and what is it used for

A

pilocarpine: used in neurogenic “dry eye” to stimulate tear production

40
Q

give an example of a muscarinic antagonist and what is it used for

A

atropine: used to speed up heart rate and dry secretions (when there is too much)
or
scopolamine: used for abdominal pain

41
Q

give an example of a nicotinic agonist and what is it used for

A

suxamethonium: overstimulates neuromuscular junction to stop muscles from spasm

42
Q

give an example of a nicotinic antagonist and what is it used for

A

alpha bungarotoxin/vecronium: neuromuscular blocking agent

43
Q

what drugs inhibit acetylcholineesterase

A

carbamate insecticides, organophosphates, neostigmine

44
Q

what is the pathway of noradrenaline

A
  1. produced from tyrosine (tryosine enters cell, tyrosine hydroxylase turns it into dihydroxyphenylalanine, which turns into dopamine via decaboxylation, dopamine beta hydroxylase turns dopamine into noradrenaline)
  2. action potential causes vesicle to bind to membrane and release noradrenaline into synaptic cleft
  3. noradrenaline binds to either pre or post synaptic adrenoreceptors OR action is terminated by monoamine oxidase (MAO) and reuptake
45
Q

give an example of an alpha 1 agonist and what is it used for

A

adrenaline: for cardiac arrest

46
Q

give an example of an alpha 2 agonist and what is it used for

A

medetomidine/romifidine/xylazine for sedation/analgesia

47
Q

give an example of a beta 1 agonist and what is it used for

A

Dobutamine: increasing blood pressure

48
Q

give an exmaple of a beta 2 agonist and what is it used for

A

salbutamol: for asthma (causes bronchodilation)

49
Q

give an example of an alpha 2 antagonist and what is it used for

A

antipamezole: reversal of sedation/analgesia

50
Q

give an example of a beta antagonsit (beta blocker) and what is it used for

A

propranolol: slows down HR

51
Q

in terms of noradrenaline receptors, what do each of them act on generakly

A

alpha 1 receptor: blood vessels (vasoconstriction)
alpha 2 receptor: blood vessels, nerve terminals (autoreceptors) - inhibition of transmitter release
beta 1 receptor: heart (tachycardia), increased force
beta 2 receptors: blood vessels (vasodilation), bronchi (bronchodilator), liver (glycogenolysis)

52
Q

what drugs influence MOA inhibitors and increase noradrenaline availibility

A

MOA-A inhibitors not used in animals
MOA-B inhiibitors: treat canine cognitive dysfunction by increasing dopamine

53
Q

what drugs affect the synthesis or stimulating synthesis of noradrenaline and what are they used for

A

carbidopa/levodopa used for Parkinsons disease

54
Q

what drugs affect re-uptake and what do they get used for

A
  • tricyclic antidepressants used as analgesics for chronic pain
  • fluoxetine, clomipramine for behavioural issues