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Anesthesia Pharm II > Local Anesthetics > Flashcards

Local Anesthetics Flashcards

1
Q

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

A

Esters and Amides

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2
Q

List 4 esters

A

Chloroprocaine, Procaine, cocaine, tetracaine

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3
Q

List 5 Amides

A

Lidocaine, Mepivicaine, Bupivicaine, Prilocaine, Ropivicaine

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4
Q

Name 4 short acting Locals

A

Procaine, Chloroprocaine, Lidocaine, Tetracaine

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5
Q

Name 3 longer acting Locals

A

Mepivacaine, Bupivicaine, Ropivicaine

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6
Q

Local anesthetics MOA

A

Na+ inhibition the the Na+ Ion channels

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7
Q

Which portion of the drug crosses the membrane?

A

Non-ionized

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8
Q

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

A

Onset

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9
Q

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

A

Potency

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10
Q

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

A

Duration

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11
Q

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

A

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

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12
Q

Max dose of Bupivacaine or Ropivacaine with and without epi?

A

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

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13
Q

Max toxic dose for Lidocaine and Mepivacaine without epi

A

300 mg

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14
Q

Max toxic dose for Lidocaine and Mepivacaine with epi

A

500 mg

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15
Q

Max dose of Bupivacaine and Ropivacaine without epi

A

175 mg

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16
Q

Max dose of Bupivacaine and Ropivacaine with epi

A

225 mg

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17
Q

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

A

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

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18
Q

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

A

Procaine pKa 8.9 Tetracaine pKa 8.6

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19
Q

Which Locals have a moderate onset?

A

Bupivacaine pKa 8.1 Ropivacaine pKa 8.1

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20
Q

Know this Chem formula

A
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21
Q

Absorption is influenced by?

A

Dosage, site of injuection, Vasoconstriction, and Pharmacologic properties

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22
Q

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

A

Increased

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23
Q

Cocaine causes vasocontstiction by affecting ?

A

Dopaimine and norepinephrine decreasing reuptake

24
Q

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

A

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
Q

Amides have a wider distribution because

A

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
Q

Esters have a shorter duration because

A

They are broken down by plasma esterase

27
Q

Which Locals are best for stat C Sections?

A

Chloroprocaine and procaine

Because they are ESTERS it get hydrolized in < 1 min

28
Q

LA are excreated in what form Ionized or Nonionized

A

Nonioinzed - the renal tubules do not reabsorb charged metabolites

29
Q

MOA of LA

A

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
  2. Penetration of the cation into and attachment to a receptor site within the sodium channel.
  3. Blockade of the sodium channel
  4. Inhibition of sodium conduction
  5. Decrease in the rate and degree of the depolarization phase of the action potential
  6. Failure to achieve the threshold potential
  7. Lack of development of a propagated action potential
  8. Blockade of impulse conduction
30
Q

La block conduction in the following order?

A

Small myelinated axons

non myelinated axons

Large myelinated axons

31
Q

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

__________ and ________ transmission are blocked first?

A

Nociceptive and sympathetic transmission

32
Q

LA have use dependence meaning

A

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
Q

Which of the following elevated extracellularly electrolyte partially antagonizes LA?

Potassium

Sodium

Calcium

Magnesium

A

Calcium

34
Q

Which of the following elevated extracellular electrolyte partially enhances LAs?

Potassium

Sodium

Calcium

Magnesium

A

Potassium

35
Q

INCREASED Lipophlicity equals???

A

INCREASED POTENCY

36
Q

INCREASED Protein Binding equals

A

INCREASED DURATION

37
Q

INCREASED Diffusability equals

A

DECREASED ONSET

38
Q

INCREASED vasodilation equals

A

DECREASED POTENCY AND DURATION

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

39
Q

CNS Toxicity Symptoms

A

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

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

40
Q

Cardiovascular Toxicity symptoms

A

abnormal automaticity

excitability

arteriolar dilation (except cocaine)

41
Q

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

A

100cc of 10% Intralipids

42
Q

Lidocaine toxicity effects respiratory drive by?

A

Supressing Hypoxic drive

43
Q

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

A

1.5 mg/kg

44
Q

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

A

Amide

45
Q

Allergic reaction treatment would include?

A

100% O2

Epi 0.01 to 0.5 IV or IM

Intubate ??????

Benadryl 25-75 mg IV

Hydrocortisone 100-200 mg IV

46
Q

Prilocaine greater the 10 mg/kg can cause what?

A

Methemoglobin

3-5 mg/dl causes cyanosis

47
Q

Damage to neuronal tissue is caused by

A

high doses

48
Q

Bupivacaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

A

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
Q

Ropivacaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

A

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
Q

Lidocaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

A

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

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

51
Q

Mepivacaine

Max dose without EPI_______ mg/kg_______

Max dose with EPI_________ mg/kg_______

A

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

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

52
Q

Prilocaine

Max dose without EPI_______ mg/kg_______

A

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

53
Q

Chloroprocaine

Max dose without EPI_______ mg/kg_______

A

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

54
Q

Procaine

Max dose without EPI_______ mg/kg_______

A

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

55
Q

Tetracaine

Max dose without EPI_______ mg/kg_______

A

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

Anesthesia Pharm II (19 decks)

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