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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
distribution of LA: what are the highly perfused organs it can enter?
brain, kidney, liver, placenta
26
what are the effects of LA on the myocardium?
reduces excitability and conductivity | - hence use in acute cardiac care
27
what are the effects of LA on peripheral vasculature?
vasodilation - if OD -> hypotension
28
what are the effects of LA on CNS? (initial vs increased dose)
initial: stimulation of CNS | increased dose: depression of CNS
29
primary site of LA metabolism? what type of enzyme? | what kind of disease does this give significance to?
- liver - amidases - liver diseases: in pts with liver disease, give less LA as they break it down slower
30
other sites of LA metabolism? + example of drug it breaks down?
plasma: articaine | lungs & liver: prilocaine
31
why are vasoconstrictors used in LA? x6
- 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
vasoconstrictors: | adrenaline is a type of ______ amine?
sympathomimetic
33
vasoconstrictors: | example of a synthetic polypeptide?
felypressin (octapressin)
34
adrenaline works on which receptors to produce vasoconstriction?
a1 receptors
35
systemic effects of adrenaline? x3
- vasoconstrictive - raises rate and force of contraction and hence cardiac output - increase blood pressure
36
name 3 types of adrenoreceptors
alpha 1 beta 1 beta 2
37
action, agonist, antagonist of alpha 1 receptors?
action: smooth muscle contraction, vasoconstriction agonist: adrenaline antagonist: phentolamine
38
action, agonist, antagonist of beta 1 receptors?
action: heart muscle contraction agonist: adrenaline antagonist: atenolol, beta blocker
39
action, agonist, antagonist of beta 2 receptors?
action: smooth muscle relaxation (bronchioles) agonist: adrenaline, salbutamol antagonist: propranolol
40
felypressin: works on venous or arterial side? vasoconstrictive potency? haemostatic properties?
- venous - half of that of adrenaline - poor haemostasis compared to adrenaline
41
significance of felypressin in pregnancy? | theoretical risk of?
- felypressin has a mild oxytocic effect - risk of interfering with placental circulation and uterine tone - low risk but should still avoid in pregnancy
42
what is the maximum recommended dose for a healthy adult? | Lidocaine 2% + Adrenaline?
500mg
43
what is the maximum recommended dose for a healthy adult? | Lidocaine 2% plain?
300mg
44
why does the use of vasoconstrictor allow a higher maximum dose?
- vasoconstriction slows down systemic uptake of drug | * effect can be variable - best to lower maximum dosage for the plain drug
45
how much lidocaine is contained in a 2% cartridge with 2.2ml?
``` 2% = 20mg/ml 2.2ml = 44mg lidocaine ```
46
2 examples of preservative used in lidocaine&adrenaline?
sodium OR potassium metabisulphite
47
mepivacaine: anaesthetic? vasoconstrictor? preservative?
- mepivacaine hydrochloride - none - none
48
prilocaine & felypressin: anaesthetic? vasoconstrictor? preservative?
- prilocaine hydrochloride - felypressin - not required
49
articaine & adrenaline: anaesthetic? vasoconstrictor? preservative?
- articaine hydrochloride? - adrenaline - sodium metabisulphite
50
when to refrain from use of lidocaine & adrenaline? x3
when pt has: - unstable angina - severe cardiac dysrhythmia - allergy to any components * caution with other cardiac conditions - avoid/reduce dose
51
``` in the event of: avoiding adrenaline latex allergy preservative allergy which drug should be used?? ```
prilocaine OR mepivacaine (alternative)
52
for greater diffusability or inferior alveolar nerve blocks, which drug can be used?
articaine
53
when should dose of LA be reduced? x4 | what should be used instead?
- liver disease, beta blockers, calcium channel blockers, drug abuse - tricyclic antidepressants, mono-amine oxidase inhibitors

ICS - LOCAL ANAESTHESIA (8 decks)

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