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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
what are the primary excretory organ for local anesthesia
kidneys
26
what does procaine appear in the urine as
PABA 90%
27
what percentage of cocaine is found in urine
10%
28
what is found more in the liver amides or esters
amides
29
what is the systemic action of local anesthesia on the CNS
- 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
skeletal muscle is more sensitive to ______
local irritant properties
30
describe the systemic action of local anesthesia of the cardiovascular system
- direct action on myocardium - produces myocardial depression - therapeutic advantage - management of hyper excitable myocardium - premature ventricular contraction - ventricular tachycardia
30
what are the initial clinical signs/symptoms of CNS toxicity
-numbness of tonuge and circumoral region - symptom - slurred speech, shivering, A/V disturbances, disorientation, tremor- signs - lidocaine only causes mild sedation or drowsiness
30
what is the direct action of local anesthesia on peripheral vasculature
- cocaine and ropivacaine are vasocontrictors - all other local anesthetics are vasodilators - local anesthetics cause hypotension
31
respiratory is generally _____ unless ______
unaffected; overdose
32
do amide anesthetics trigger malignant hyperthermia
no
33
what is the importance of vasoconstrictors
- 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
what are the natural catecholamines
-epinephrine - norepinephrine - dopamine
35
what are the synthetic catecholamines
- isoproterenol - levonordefrin
36
what are the non catecholamines
- amphetamine - ephedrine - methamphetamine
37
what are the 3 modes of action
- direct acting - indirect acting - mixed acting
38
all catecholamines work on ______ with _____-
adrenergic receptors; direct acting
39
what do alpha 1 receptors do
vasocontriction
40
what do alpha 2 receptors do
post synaptic inhibitory
41
where are beta 1 receptors
located at heart and intenstine
42
what do beta 2 receptors do and where are they found
vasodilation - in bronchi and vascular beds
43
what is the most used vasoconstrictor
epinephrine
44
what is added to epinephrine to delay deterioration
sodium bisulfite - an antioxidant
45
where does epi come from
can be synthetic or from the adrenal medulla
46
what is the mode of action of epinephrine
- 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
what makes epinephrine a good treater of acute asthma
potent bronchiole smooth muscle dilator
48
how is epinpehrine action terminated
reuptake or inactivated by COMT and MAO
49
what happens to epinephrine level after usual intra oral injection
increase
50
how does epi intra oral injection affect the heart
- increase CO and SV - minimum change in BP and HR
51
what explains why patient feels palpitation after injection
-no change in BP or HR but increase in CO and SV
52
how does intravascular injection of epi affect HR and systolic BP
- heart rate: increase from 25 bpm to 75 bpm - BP: increase from 20mmHg to 70mmHg
53
what receptors does norepinephrine act on
- lacks B2 actions - intense vasoconstriction - dramatic elevation of BP- 9x higher than epi
54
what does levonordefrin closely resembly
norepinephrine
55
how long do vasocontrictors without epi last? with epi?
-without: about 10 mins - with: about 60 mins
56
epinephrine produces _____
rebound vasodilatory effect
57
norepinephrine produces _____ and _____
tissue necrosis and slough
58
what are the ASA classifications 1-6
-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
what are the contraindications to vasoconstrictors
- 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
what are the contraindications of severe cardiovascular disease
- 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
what patients are considered ASA 4 from the contraindications list and are not considered candidates for elective or emergnecy dental treatment in office
-BP higher than 200 systolic or 115 diastolic - uncontrolled hyerthryoidism - severe cardiovascular disease ( except post CABG)
62
so what should you do with local anesthetics
- multiple aspirations - slow administration - minimum concentration of vasoconstrictor and local anesthetic
63

Intro to OS and Pain Management (9 decks)

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