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Intro to OS and Pain Management > Pharmacology of Local Anesthesia > Flashcards

Pharmacology of Local Anesthesia Flashcards

1
Q

what type of effect do most local anesthetics have

A

vasodilation

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2
Q

what is the most potent vasodilator

A

procaine

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3
Q

what does procaine treat

A

accidental intra- arterial injection of thiopental

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4
Q

what is the clinical undesirable effect of vasodilation

A

increases rate of absorption into the blood -> potential systemic overdose

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5
Q

what is the only local anesthetic with constrictor effect

A

cocaine

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6
Q

what does cocaine do

A

inhibits catecholamine re uptake

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7
Q

how well is local anesthesia orally absorbed

A

poorly except cocaine

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8
Q

describe the topical route of local anesthesia uptake

A
  • rapid absorption to mucous membrane
  • tracheal> pharyngeal > esophageal
  • non intact skin- sunburn remedy
  • EMLA cream for intact skin
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9
Q

what is injection of local anesthesia uptake for

A

management of ventricular dysrhythmias (PVC)

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10
Q

highly perfused organ will initially have _____ blood level of anesthetics

A

higher

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11
Q

which muscle has the highest % of anesthetics and why

A
  • skeletal muscle
  • because largest tissue mass in the body
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12
Q

how are drugs eliminated from the body

A
  • metabolic pathways
  • excretory pathways
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13
Q

what are the 1-4 half lives

A

1st: 50%
2nd: 75%
3rd: 87.5%
4th: 97%

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14
Q

what do all local anesthetics cross

A

blood brain barrier and placenta

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15
Q

what are ester local anesthetics hydrolyzed by and where

A
  • hydrolyzed in plasma by pseudocholinesterase into paraminobenzoic acid (PABA)
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16
Q

what is the allergic reaction with ester local anesthesia related to

A

PABA

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17
Q

what might lead to a potential for toxicity with ester local anesthesia and what is the prevalence

A

atypical pesudocholinesterase
- 1/2800 persons

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18
Q

where is the primary biotransformation site of amide local anesthetics

A

liver

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19
Q

what influences the biotransformation of amide local anesthetics

A

liver function and hepatic perfusion

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20
Q

what persons is amide local anesthetics contraindicated for

A

ASA IV to V patients with liver dysfunction, heart failure

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21
Q

what is the sedative effect of amide local anesthetics

A

lidocaine active metabolite

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22
Q

what is another name for methemoglobinemia and describe it

A
  • blue baby syndrome
  • inherited blood disorder
  • atypical hemoglobin that is unable to deliver oxygen efficiently
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23
Q

what can be the cause of methemoglobinemia

A

primary metabolite of prilocaine

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24
Q

what are the signs and symptoms of methemoglobinemia

A

-easily tired
- bluish tint on lips or skin

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25
Q

what are the primary excretory organ for local anesthesia

A

kidneys

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26
Q

what does procaine appear in the urine as

A

PABA 90%

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27
Q

what percentage of cocaine is found in urine

A

10%

28
Q

what is found more in the liver amides or esters

A

amides

29
Q

what is the systemic action of local anesthesia on the CNS

A
  • local anesthesia readily crosses blood brain barrier
  • pharmacological action is CNS depression
  • initial clinical signs/symptoms of CNS toxicity are excitatory
  • higher level of CNS toxicity -> tonic clonic convulsion
  • further increase of cessation of seizure activity -> respiratory depression -> reparatory arrest
30
Q

skeletal muscle is more sensitive to ______

A

local irritant properties

30
Q

describe the systemic action of local anesthesia of the cardiovascular system

A
  • direct action on myocardium
  • produces myocardial depression
  • therapeutic advantage
  • management of hyper excitable myocardium
  • premature ventricular contraction
  • ventricular tachycardia
30
Q

what are the initial clinical signs/symptoms of CNS toxicity

A

-numbness of tonuge and circumoral region - symptom
- slurred speech, shivering, A/V disturbances, disorientation, tremor- signs
- lidocaine only causes mild sedation or drowsiness

30
Q

what is the direct action of local anesthesia on peripheral vasculature

A
  • cocaine and ropivacaine are vasocontrictors
  • all other local anesthetics are vasodilators
  • local anesthetics cause hypotension
31
Q

respiratory is generally _____ unless ______

A

unaffected; overdose

32
Q

do amide anesthetics trigger malignant hyperthermia

A

no

33
Q

what is the importance of vasoconstrictors

A
  • decreased perfusion to site of administration
  • slow the absorption of L.A into the cardiovascular system
  • minimize the risk of systemic toxicity
  • increase duration of action for L.A
  • decreased hemorrhage
34
Q

what are the natural catecholamines

A

-epinephrine
- norepinephrine
- dopamine

35
Q

what are the synthetic catecholamines

A
  • isoproterenol
  • levonordefrin
36
Q

what are the non catecholamines

A
  • amphetamine
  • ephedrine
  • methamphetamine
37
Q

what are the 3 modes of action

A
  • direct acting
  • indirect acting
  • mixed acting
38
Q

all catecholamines work on ______ with _____-

A

adrenergic receptors; direct acting

39
Q

what do alpha 1 receptors do

A

vasocontriction

40
Q

what do alpha 2 receptors do

A

post synaptic inhibitory

41
Q

where are beta 1 receptors

A

located at heart and intenstine

42
Q

what do beta 2 receptors do and where are they found

A

vasodilation
- in bronchi and vascular beds

43
Q

what is the most used vasoconstrictor

A

epinephrine

44
Q

what is added to epinephrine to delay deterioration

A

sodium bisulfite - an antioxidant

45
Q

where does epi come from

A

can be synthetic or from the adrenal medulla

46
Q

what is the mode of action of epinephrine

A
  • alpha and beta receptors
  • beta 2 is more sensitive to epi
  • alpha acts first, later dilation because of beta action- about 6 hours later
47
Q

what makes epinephrine a good treater of acute asthma

A

potent bronchiole smooth muscle dilator

48
Q

how is epinpehrine action terminated

A

reuptake or inactivated by COMT and MAO

49
Q

what happens to epinephrine level after usual intra oral injection

A

increase

50
Q

how does epi intra oral injection affect the heart

A
  • increase CO and SV
  • minimum change in BP and HR
51
Q

what explains why patient feels palpitation after injection

A

-no change in BP or HR but increase in CO and SV

52
Q

how does intravascular injection of epi affect HR and systolic BP

A
  • heart rate: increase from 25 bpm to 75 bpm
  • BP: increase from 20mmHg to 70mmHg
53
Q

what receptors does norepinephrine act on

A
  • lacks B2 actions
  • intense vasoconstriction
  • dramatic elevation of BP- 9x higher than epi
54
Q

what does levonordefrin closely resembly

A

norepinephrine

55
Q

how long do vasocontrictors without epi last? with epi?

A

-without: about 10 mins
- with: about 60 mins

56
Q

epinephrine produces _____

A

rebound vasodilatory effect

57
Q

norepinephrine produces _____ and _____

A

tissue necrosis and slough

58
Q

what are the ASA classifications 1-6

A

-ASA 1: normal healthy patient
- ASA2: mild systemic disease
- ASA 3: severe systemic disease that limits activity: mild DM, controlled HTN, obesity
- ASA 4: incapacitating disese that is a constant threat to life: CHF, renal failure
- ASA 5: moribound patient not expected to survive 24 hours: ruptured aneurysm
- ASA 6: brain dead patient whose organs are being harvested

59
Q

what are the contraindications to vasoconstrictors

A
  • BP higher than 200 systolic or 115 diastolic
  • uncontrolled hyerthryoidism
  • severe cardiovascular disease
  • undergoing general anesthesia with halogenated agents
  • patient receiving nonspecific B-blocker, MAOi, tricyclic antidepressants
60
Q

what are the contraindications of severe cardiovascular disease

A
  • less than 6 months after MI
  • less than 6 months after stroke
  • daily angina or unstable angina
  • cardiac dysrhythmias even with therapy
  • post CABG, less than 6 months
61
Q

what patients are considered ASA 4 from the contraindications list and are not considered candidates for elective or emergnecy dental treatment in office

A

-BP higher than 200 systolic or 115 diastolic
- uncontrolled hyerthryoidism
- severe cardiovascular disease ( except post CABG)

62
Q

so what should you do with local anesthetics

A
  • multiple aspirations
  • slow administration
  • minimum concentration of vasoconstrictor and local anesthetic
63
Q
A

Intro to OS and Pain Management (9 decks)

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