Physiology and pharmacology 1 Flashcards

1
Q

what is the safety plus system?

A
  • syringe barrel with needle STERILE, single use
  • LA cartridges STERILE,single use
  • Plunger/handle STERILE and REUSE (black) or SINGLE USE (white)
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2
Q

what is in a cartridge?

A
  • usually 2.2ml or 1.8ml
  • anaesthetic agent
  • vasoconstrictor
  • stabilizer / preservative
  • isotonic carrier medium
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3
Q

Name the drug names of LA preparations and their UK trade name.

A

-Lidocaine
and adrenaline:
UtilycaineTM
Lignospan SpecialTM XylocaineTM

-Mepivacaine:
ScandonestTM

-Prilocaine
and Felypressin:
CitanestTM

-Prilocaine Plain:
Citanest PlainTM

-Articaine
and adrenaline:
BartinestTM
SeptanestTM

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4
Q

what is the basic local anaesthetic?

A

Has a lipophilic end and a hydrophilic end with an intermediate chain in the middle

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5
Q

what are the two types of intermediate chain in local anaesthetic?

A
  • Ester- O=C-O-R1

- Amide- NH-C=O

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6
Q

Are more drugs amide or ester and why?

A

More drugs are amide as they have a lower level of allergic potential than esters

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7
Q

Name ester types of local anaesthetic.

A
  • Procaine

- Benzocaine

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8
Q

Name amide types of local anaesthetic.

A
  • Lidocaine
  • prilocaine
  • mepivacaine
  • bupivacaine
  • articaine
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9
Q

How do local anaesthetics work?

A

Local anaesthetic reversibly blocks Na+ channels to block action potentials as it prevents depolarisation by an influx of Na+ into the cell (keeping inside the cell negative)

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10
Q

what are the theories of local anaesthetic action?

A
  • Membrane expansion- makes membrane expand so it physically blocks Na+ channels
  • Specific receptor theory - anaesthetic agent gets inside cell and causes Na+ channel to close
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11
Q

what does local anaesthetic need to be?

A
  • Lipid soluble (non-charged): to pass through the axon membrane
  • Charged: to bind to receptor in the Na+ channel
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12
Q

How does pH affect the effectiveness of local anaesthetic?

A

-Equilibrium varies with pH
-more acidic environemnt- the less ions pass into the cell
- LA into an area with absess is less likely to work
LA doesnt work as well in infected tisue (acidic)

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13
Q

Describe the lipid solubility of LA.

A

-High lipid solubility (partition coefficient)

– Rapid onset as passed though membrane easily

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14
Q

Describe the protein binding of LA.

A

-LA bound to protein provides a pool of available drug

– High protein binding capability – increases duration

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15
Q

Describe the vasodilator ability of LA.

A

-most LA have vasodilators effects
-vasodilation results in increase in­ blood flow
– more rapid removal of LA
– all LAs are vasodilators
so there is an importance of vasoconstrictors

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16
Q

what are the standards of LA?

A
  • Lidocaine -gold standard
  • Prilocaine - alternative
  • Mepivacaine-alternatuve /least vasodilatory
  • Bupivacaine - high protein binding so long lasting
  • Articaine- New, USP:diffusability
17
Q

what is the sequence of onset/offset in LA?

A
  • C fibres - (nonciception so pain is treated first)
  • Ad fibres
  • Ab fibres
  • Aa fibres (offsets first)
18
Q

Describe the absorption of LA.

A
  • uptake from site of deposition into bloodstream

- loss of LA activity

19
Q

what does absorption depend on?

A

-dose
– vasoactivity of the drug
– vascularity of the tissue
– vasodilator effect vs use of vasoconstrictors

20
Q

How is LA distributed?

A

-unbound LA may enter any organ
-in particular highly perfused organs:
– brain
– liver
– Kidneys
– Placenta

21
Q

what is LA’s effect on myocardium?

A

– reduces excitability and conductivity

– hence use in acute cardiac care

22
Q

what is LA’s effect on peripheral vasculature?

A

– vasodilation

– if overdose - hypotension

23
Q

what is LA’s effect on CNS?

A

– initial stimulation

– then, with increased doses, depression

24
Q

where is LA metabolised?

A

Primarily in the liver :
–amidases
– importance of liver disease

The plasma:
– articaine

Lungs (and liver):
– Prilocaine – methaemaglobinaemia – interferes with O2 carrying ability