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CNS > [PHARMA] LOCAL ANESTHETICS > Flashcards

[PHARMA] LOCAL ANESTHETICS Flashcards

1
Q

Local anesthetic definition

A

a drug that induces reversible loss of sensation without inducing loss consciousness or sleep

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2
Q

esters example

A

procaine

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3
Q

short acting LA

A

procaine (0.5-1h)

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4
Q

intermediate acting LA

A

lidocaine (2h)

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5
Q

long acting LA

A

bupivacaine (3h)

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6
Q

esters are hydrolyzed by

A

plasma pseudocholine esterases

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7
Q

amide are metabolized by

A

liver

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8
Q

PABA derivatives & liable to allergy

A

ester LA

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9
Q

liable to induce systemic toxicity

A

amide LA

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10
Q

amides duration of action is prolonged in case of

A

liver disease
reduced hepatic BF as in heart disease

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11
Q

esters duration of action

A

short

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12
Q

amides duration of action

A

long

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13
Q

duration of action is prolonged in esters by

A

genetic plasma pseudo choline esterase deficiency

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14
Q

LA mechanism of action

A

bind to receptors on inner surface of Na channel & block them=>block action potential

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15
Q

neurons sensitive to LA

A

Small neurons (pain,temp, autonomic nerves)
rapid firing nerves (sensory nerves)

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16
Q

motor neurons are only affected by LA in case of

A

higher LA concentration

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17
Q

pKA of LA

A

7.7-9

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18
Q

pH of LA is

A

basic, they’re weak bases

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19
Q

LA solubility can be increased by

A

preparing them as acid salts

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20
Q

forms of LA

A

ionized
unionized

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21
Q

which form of LA can cross nerve membrane

A

unionized

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22
Q

relation between PPB and LA

A

proportional

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23
Q

LA with highest percentage of PPB and therefore longer duration of action

A

Bupivacaine (95%)

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24
Q

relationship between lipid solubility and potency

A

proportional

25
Q

lipid solubility affects

A

potency

26
Q

the more the lipid content the ____the potency

A

potency

27
Q

pKa affects

A

speed of onset

28
Q

the lower the pKA the ____the onset of action

A

faster

29
Q

affect of pKa

A

the lower the pKa the more unionized forms there is= faster onset

30
Q

lidocaine pKa

A

7.9

31
Q

bupivacaine pKa

A

8.1

32
Q

which drug has a higher percentage of unionized forms: Lidocaine or Bupivacaine

A

Lidocaine

33
Q

affect of extracellular pH

A

the more acidic the ECF pH, the less the unionized forms available= less crossing=less anesthesia

34
Q

factors increasing extracellular acidity

A

infections or lidocaine Hcl repeated injection

35
Q

how can extracellular acidity be decreased

A

adding NaHCO3

36
Q

affect of vasoconstrictors

A

prolong action of LA
decrease absorption–>
↑duration & ↓systemic toxicity

37
Q

LAs affect on BV

A

induce VD–>↑ absorption–> termination of effect–>↑risk of toxicity

38
Q

adverse effects & toxicity

A

~CNS=
-sleepiness, numbness, metallic taste (low)
-tremors, convulsions, resp depression, coma,death (high conc)

~Neurotoxicity
~CVS: HypoTN, Bradycardia
~allergy (esters)
~↑BP & arrhythmias with VC added to LA

39
Q

neurotoxicity can happen due to

A

high conc of LA injected close to nerve trunk/spinal cord

40
Q

side effect of high dose Bupivacaine

A

extremely cardiotoxic

41
Q

drug interaction b/w LA x propanolol

A

↓hepatic BF= impairs lidocaine clearance= toxicity

42
Q

drug interaction b/w
LA x adrenaline x Propanolol

A

dangerous rise in BP
due to unopposed alpha action

43
Q

drug interaction b/w
LA x adrenaline x TCAs

A

hypertensive crisis

44
Q

DOC in surface anesthesia

A

lidocaine

45
Q

surface anesthesia is used in

A

minor surgery

46
Q

infiltration anesthesia is used in

A

minor surgery

47
Q

nerve block anesthesia is used in

A

dentistry & surgery

48
Q

spinal anesthesia site of injection

A

subarachnoid space below L2

49
Q

spinal anesthesia is used in

A

abdomen surgery
pelvis, leg surgery when GA is CI

50
Q

anesthesia injected close to nerve trunks

A

nerve trunk

51
Q

anesthesia applied to skin, mucous membranes of nose, mouth, cornea as solution/jelly/cream

A

surface anesthesia

52
Q

anesthesia injected SC & submucosal to reach nerve branches

A

infiltration

53
Q

IV regional anesthesia procedure

A

double cuff is applied & inflated above arterial BP
LA is injected after elevation to drain venous the system

54
Q

side effects of spinal aesthesia

A

headache
hypoTN
spinal root injury
infection

55
Q

hypoTN as a result of spinal anesthesia is due to

A

sympathetic nerve block

56
Q

headache as a result of spinal anesthesia is due to

A

CSF leakage & traction

57
Q

CSF leakage & traction in spinal anesthesia can be avoided by

A

pencil point needles

58
Q

anesthesia injected outside the dura to block the spinal roots

A

epidural anesthesia

59
Q

epidural anesthesia is used in

A

painless labor

CNS (29 decks)

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