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Flashcards in Local Anesthetics Deck (55):
1

Local Anesthetics are classified by their linkage what are the 2 classes

Esters and Amides

2

List 4 esters

Chloroprocaine, Procaine, cocaine, tetracaine

3

List 5 Amides

Lidocaine, Mepivicaine, Bupivicaine, Prilocaine, Ropivicaine

4

Name 4 short acting Locals

Procaine, Chloroprocaine, Lidocaine, Tetracaine

5

Name 3 longer acting Locals

Mepivacaine, Bupivicaine, Ropivicaine

6

Local anesthetics MOA

Na+ inhibition the the Na+ Ion channels

7

Which portion of the drug crosses the membrane?

Non-ionized

8

pKa equated to what - potency, onset, or duration?

Onset

9

Lipid solubility equates to what- potency, onset, or duration?

Potency

10

Protein binding equates to what - potency, onset, or duration?

Duration

11

max dose of Lidocaine and Mepivacaine per Kg with and without Epi

4.5 mg/kg without and 7 mg/kg with epi

12

Max dose of Bupivacaine or Ropivacaine with and without epi?

2.8 mg/kg without and 3.2mg/kg with epi

13

Max toxic dose for Lidocaine and Mepivacaine without epi

300 mg

14

Max toxic dose for Lidocaine and Mepivacaine with epi

500 mg

15

Max dose of Bupivacaine and Ropivacaine without epi

175 mg

16

Max dose of Bupivacaine and Ropivacaine with epi

225 mg

17

Which Locals have a fast onset or closer to physiologic Ph? There is one exception to this?

Lidocaine pKa 7.7 Mepivacaine pKa 7.6 Chloroprocaine Pka 9.1 (THE EXCEPTION)

18

Which Locals have a slower onset or are further away from physiologic Ph?

Procaine pKa 8.9 Tetracaine pKa 8.6

19

Which Locals have a moderate onset?

Bupivacaine pKa 8.1 Ropivacaine pKa 8.1

20

Know this Chem formula

A image thumb
21


Absorption is influenced by?


Dosage, site of injuection, Vasoconstriction, and Pharmacologic properties

22


When the vessel is in the nerve bundle will you have ? Increased or Decreased uptake of the LA?


Increased

23


Cocaine causes vasocontstiction by affecting ?


Dopaimine  and norepinephrine decreasing reuptake

24


Will epi extend short acting or longer acting LA for a longer time period?


It will extend longer acting LA for a longer time period because Longer acting LA are more Lipophilic which is directly related to durration 

25


Amides have a wider distribution because


Increased storage in the tissues because of rapid uptake of highly perfused tissues like the  the brain, liver kidneys and heart and a slower uptake from the moderately perfused tissues lik the gut and muscles

LONG ANSWER IT SUCKS

26


Esters have a shorter duration because


They are broken down by plasma esterase

27


Which Locals are best for stat C Sections?


Chloroprocaine and procaine

Because they are ESTERS it get hydrolized in < 1 min

28


LA are excreated in what form Ionized or Nonionized


Nonioinzed -  the renal tubules do not reabsorb charged metabolites

29


MOA of LA

Mechanism of Action:
1. Diffusion of the base form across the across the nerve sheath and nerve membrane                                                             2. Re-equilibration  between the base and cationic forms in the axoplasm
3. Penetration of the cation into and attachment to a receptor site within the sodium channel.
4. Blockade of the sodium channel
5. Inhibition of sodium conduction
6. Decrease in the rate and degree of the depolarization phase of the action potential
7. Failure to achieve the threshold potential
8. Lack of development of a propagated action potential
9. Blockade of impulse conduction

30


La block conduction in the following order?


Small myelinated axons

non myelinated axons

Large myelinated axons

 

31


Because these axons are blocked in this order (Small myelinated axons, non myelinated axons, Large myelinated axons)

__________ and ________ transmission are blocked first?

Nociceptive and sympathetic transmission

32


LA have use dependence meaning

The increase in action potential frequency increases depth of block (The more u use it the faster it is blocked)

This is important in the use of LA as antiarrhythmics and anticonvulsants

33


Which of the following elevated extracellularly electrolyte partially antagonizes LA?

Potassium

Sodium

Calcium

Magnesium

Calcium

34


Which of the following elevated extracellular electrolyte partially enhances LAs?

Potassium

Sodium

Calcium

Magnesium

Potassium

35


INCREASED  Lipophlicity equals???


INCREASED POTENCY

36


INCREASED Protein Binding equals


INCREASED DURATION

37


INCREASED Diffusability equals


DECREASED ONSET

38


INCREASED vasodilation equals


DECREASED POTENCY AND DURATION

Its all moving into the vasculature from the site of infiltration decreasing less drug at the site to work

39


CNS Toxicity Symptoms


Early: Circumoral numbness, metalic taste, tinnitus, blurred vision and dizziness

Late: Agitation, restlessness, slurring of speach, unconciousness, Seizure, resp arrest and death

40


Cardiovascular Toxicity symptoms


abnormal automaticity

excitability

arteriolar dilation (except  cocaine)

41


Bupivacaine is the most cardio toxic what the antagonist for this drug?

100cc of 10% Intralipids

42


Lidocaine toxicity effects respiratory drive by?


Supressing Hypoxic drive

43


Lidocaine may block bronchospasm or reactive airway with bronchial smooth muscle relaxation at what dose?

1.5 mg/kg

44


Amide or ester is rare to have an allergic reaction to ??


Amide

45


Allergic reaction treatment would include?

100% O2

Epi 0.01 to 0.5 IV or IM

Intubate ??????

Benadryl 25-75 mg IV

Hydrocortisone 100-200 mg IV

 

46


Prilocaine greater the 10 mg/kg can cause what?


Methemoglobin

3-5 mg/dl causes cyanosis

47


Damage to neuronal tissue is caused by

high doses

48


Bupivacaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

 

Max dose without EPI --->175 mg,  Weight based ------> 2.8 mg/kg

Max dose with EPI----> 225 mg,   Weight based-----> 3.2 mg/kg

49


Ropivacaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

Max dose without EPI --->175 mg,  Weight based ------> 2.8 mg/kg

Max dose with EPI----> 225 mg,   Weight based-----> 3.2 mg/kg

50


Lidocaine


Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

Max dose without EPI --->300 mg,  Weight based ------> 4.5 mg/kg

Max dose with EPI----> 500 mg,   Weight based-----> 7 mg/kg

51

Mepivacaine


Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

Max dose without EPI --->300 mg,  Weight based ------> 4.5 mg/kg

Max dose with EPI----> 500 mg,   Weight based-----> 7 mg/kg

52


Prilocaine

Max dose without EPI_______ mg/kg_______


Max dose without EPI --->400 mg,  Weight based ------> 8 mg/kg

53


Chloroprocaine

Max dose without EPI_______ mg/kg_______


Max dose without EPI ---> 600mg,  Weight based ------> 12 mg/kg

54


Procaine

Max dose without EPI_______ mg/kg_______


Max dose without EPI ---> 500 mg,  Weight based ------> 12 mg/kg

55


Tetracaine

Max dose without EPI_______ mg/kg_______


Max dose without EPI ---> 100 mg,  Weight based ------> 3 mg/kg