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ICS - LOCAL ANAESTHESIA > LA - Pharmacology > Flashcards

LA - Pharmacology Flashcards

1
Q

what are the 3 trade names of the anaesthetic lidocaine (+adrenaline)?

A

utilycaine
lignospan special
xylocaine

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2
Q

mepivacaine - trade name?

A

scandonest

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3
Q

prilocaine (+felypressin) - trade name?

A

citanest

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4
Q

prilocaine (plain)?

A

citanest plain

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5
Q

articaine (+adrenaline) - 2 trade names?

A

bartinest

septanest

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6
Q

i. what are the components inside a cartridge of LA? x4

ii. how much liquid is there in total?

A

i. anaesthetic agent, vasoconstrictor, stabilizer/preservative, isotonic carrier medium
ii. usually 2.2ml or 1.8ml

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7
Q

LA structure: 3 components?

A

lipophilic head
intermediate chain
hydrophilic end

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8
Q

what are the two different classifications of LA?

A

esters or amides

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9
Q

name 2 examples of ester LAs

A

procaine

benzocaine

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10
Q

name 5 examples of amide LAs

A 
lidocaine
prilocaine
mepivacaine
bupivacaine
articaine
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11
Q

how does LA work?

A

blocks action potentials
- opening of NA channels followed by depolarization
LA blocks NA channels, works by the specific receptor theory

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12
Q

what implications does the specific receptor theory have on local anaesthesia?

A

LA would have to be:

  • lipid soluble (non-charged) to pass through axon membrane
  • charged: to bind to receptor in Na channel
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13
Q

what are the properties of LA? x4

A

dissociation
lipid solubility
protein binding
vasodilator ability

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14
Q

dissociation properties:

proportion of charged vs non-charged depends on? elaborate

A

depends on pH and pKa:
low pH: less non charged, slower onset
low pKa: more non-charged, rapid onset

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15
Q

lipid solubility properties:

high LS means?

A

rapid onset as it passes through membrane easily

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16
Q

protein binding properties:
what happens to LA bound to protein?
high protein binding capability?

A
  • LA bound to protein creates pool of available drug

- high PB capability increases duration of effect

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17
Q

vasodilator ability properties:

results in?

A
  • vasodilators increase blood flow
  • bring about a more rapid removal of LA
  • all LAs are vasodilators
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18
Q

which drug is the gold standard of LA?

A

lidocaine

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19
Q

which drug is the main alternative? what is another less vasodilatory drug?

A
  • prilocaine (no adrenaline)

- mepivacaine

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20
Q

what is a high protein binding i.e. long lasting drug?

A

bupivacaine

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21
Q

what is a relatively new, high diffusability drug?

A

articaine

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22
Q

nerve fibres: sequence of onset?

sequence of offset?

A

onset: C, Ad, Ab, Aa
offset: Aa, Ab, Ad, C

23
Q

define absorption

what does it lead to?

A

refers to uptake from site of deposition into the bloodstream
- leads to the loss of LA activity

24
Q

what affects rate of absorption? x4

A
  • dose
  • vasoactivity of drug
  • vascularity of tissue
  • vasodilator effects/use of vasoconstrictors
25
Q

distribution of LA: what are the highly perfused organs it can enter?

A

brain, kidney, liver, placenta

26
Q

what are the effects of LA on the myocardium?

A

reduces excitability and conductivity

- hence use in acute cardiac care

27
Q

what are the effects of LA on peripheral vasculature?

A

vasodilation - if OD -> hypotension

28
Q

what are the effects of LA on CNS? (initial vs increased dose)

A

initial: stimulation of CNS

increased dose: depression of CNS

29
Q

primary site of LA metabolism? what type of enzyme?

what kind of disease does this give significance to?

A
  • liver
  • amidases
  • liver diseases: in pts with liver disease, give less LA as they break it down slower
30
Q

other sites of LA metabolism? + example of drug it breaks down?

A

plasma: articaine

lungs & liver: prilocaine

31
Q

why are vasoconstrictors used in LA? x6

A
  • increase speed of onset
  • counteract vasodilatory effects of LA agent
  • extend duration of LA
  • improve depth of LA
  • lower blood levels of LA
  • reduce haemorrhage
32
Q

vasoconstrictors:

adrenaline is a type of ______ amine?

A

sympathomimetic

33
Q

vasoconstrictors:

example of a synthetic polypeptide?

A

felypressin (octapressin)

34
Q

adrenaline works on which receptors to produce vasoconstriction?

A

a1 receptors

35
Q

systemic effects of adrenaline? x3

A
  • vasoconstrictive
  • raises rate and force of contraction and hence cardiac output
  • increase blood pressure
36
Q

name 3 types of adrenoreceptors

A

alpha 1
beta 1
beta 2

37
Q

action, agonist, antagonist of alpha 1 receptors?

A

action: smooth muscle contraction, vasoconstriction
agonist: adrenaline
antagonist: phentolamine

38
Q

action, agonist, antagonist of beta 1 receptors?

A

action: heart muscle contraction
agonist: adrenaline
antagonist: atenolol, beta blocker

39
Q

action, agonist, antagonist of beta 2 receptors?

A

action: smooth muscle relaxation (bronchioles)
agonist: adrenaline, salbutamol
antagonist: propranolol

40
Q

felypressin:
works on venous or arterial side?
vasoconstrictive potency?
haemostatic properties?

A
  • venous
  • half of that of adrenaline
  • poor haemostasis compared to adrenaline
41
Q

significance of felypressin in pregnancy?

theoretical risk of?

A
  • felypressin has a mild oxytocic effect
  • risk of interfering with placental circulation and uterine tone
  • low risk but should still avoid in pregnancy
42
Q

what is the maximum recommended dose for a healthy adult?

Lidocaine 2% + Adrenaline?

A

500mg

43
Q

what is the maximum recommended dose for a healthy adult?

Lidocaine 2% plain?

A

300mg

44
Q

why does the use of vasoconstrictor allow a higher maximum dose?

A
  • vasoconstriction slows down systemic uptake of drug

* effect can be variable - best to lower maximum dosage for the plain drug

45
Q

how much lidocaine is contained in a 2% cartridge with 2.2ml?

A 
2% = 20mg/ml
2.2ml = 44mg lidocaine
46
Q

2 examples of preservative used in lidocaine&adrenaline?

A

sodium OR potassium metabisulphite

47
Q

mepivacaine:
anaesthetic?
vasoconstrictor?
preservative?

A
  • mepivacaine hydrochloride
  • none
  • none
48
Q

prilocaine & felypressin:
anaesthetic?
vasoconstrictor?
preservative?

A
  • prilocaine hydrochloride
  • felypressin
  • not required
49
Q

articaine & adrenaline:
anaesthetic?
vasoconstrictor?
preservative?

A
  • articaine hydrochloride?
  • adrenaline
  • sodium metabisulphite
50
Q

when to refrain from use of lidocaine & adrenaline? x3

A

when pt has:

  • unstable angina
  • severe cardiac dysrhythmia
  • allergy to any components
  • caution with other cardiac conditions - avoid/reduce dose
51
Q 
in the event of: 
avoiding adrenaline
latex allergy
preservative allergy 
which drug should be used??
A

prilocaine
OR
mepivacaine (alternative)

52
Q

for greater diffusability or inferior alveolar nerve blocks, which drug can be used?

A

articaine

53
Q

when should dose of LA be reduced? x4

what should be used instead?

A
  • liver disease, beta blockers, calcium channel blockers, drug abuse
  • tricyclic antidepressants, mono-amine oxidase inhibitors

ICS - LOCAL ANAESTHESIA (8 decks)

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