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Pharmacology Exam 4 > Local Anesthetics Part 1 > Flashcards

Local Anesthetics Part 1 Flashcards

1
Q

________ is the first local anesthetic.

A

cocaine

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2
Q

1st synthetic Ester: _________ (1905)

A

Procaine

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3
Q

1st synthetic Amide:____________ (1943)

A

Lidocaine

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4
Q

__________ is the standard to which all local anesthetics are compared.

A

lidocaine

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5
Q

Local Anesthetics are used for _________, acute and chronic pain and ___________.

A
  • dysrhythmias
  • anesthesia
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6
Q

Local Anesthetics are used in anesthesia for ________ Blockade, _______ anesthesia and ____________ muscle paralysis.

A
  • ANS
  • Sensory
  • Skeletal
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7
Q

All Local Anesthetics are what type of Antiarrythmic classification?

A
  • Class 1:Sodium Channel Blockers
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8
Q

Antiarrhythmic Classes:
* Class 1: _______________
* Class 2: ______________
* Class 3: ______________
* Class 4: _____________

A
  • sodium-channel blockers
  • Beta-Blockers
  • Potassium-channel blockers
  • Calcium-channel blockers
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9
Q

Miscellaneous Antiarrhythmic Drugs can include _____________, electrolytes supplements ( ______ and potassium) and ____________ compounds.

A
  • adenosine
  • magnesium
  • digitalis
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10
Q

Pre-Op Tylenol dose is ________ mg PO.
Pre-Op Gabapentin dose is _______ mg PO.

A
  • 1000
  • 300
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11
Q

Pre-op dose of Ofiremev is ____ gram, if patient has OSA.

A

1 gram

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12
Q

Intra-Op: Induce GA w/ __________, use lidocaine to blunt the burn, ketamine and __________. Maintain GA with _______________ anesthetic.

A
  • propofol
  • paralytic
  • volatile
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13
Q

Intra-Op Magnesium dose is ____ - ____ mg/kg (max ___ G) infusion over 1 hour.

A
  • 30-60 mg/kg
  • 6 grams
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14
Q

Intra-Op Lidocaine infusion dose is ___mg/kg infusion ___ hour.

A
  • 1 mg/kg
  • 1 hour
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15
Q

Intra-Op: Ondesetron, Decadron and _________ can be given as permitted by the surgeon.

A
  • Ketoralac.
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16
Q

Intra-Op Ibuprofen dose is ____ to ____ mg IV over ____ mins; or PO Q__H PRN.

MAX dose is _______ mg/day.

A
  • 200-800 mg
  • 6 hours
  • 3200 mg/day
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17
Q

Post-Op Tylenol dose is ______ mg TID

A

1000 mg

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18
Q

Post-Op: Super Mag dose is _____ mg BID or Magnesium Aspartate _______ mg TID
or Magnesium Oxide ______ mg BID

A
  • 400 mg
  • 615 mg
  • 500 mg
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19
Q

Post Op Gabapentin dose is ______ mg ______.

A
  • 300 mg
  • TID
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20
Q

Post-Op Dose:
Celebrex or Advil ____ as permitted byt the surgeon.

A

TID

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21
Q

Lidocaine
* Intial Bolus: __ - __ mg/kg IV
* over ___ - __ mins

A
  • 1-2 mg/kg over 2-4 mins
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22
Q

Lidocaine is an ______ LA.

A

Amide

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23
Q

Lidocaine:
* Drip: __ - __ mg/kg/hour:
* Terminate gtt within ___ - ___ hours.

A
  • 1-2 mg/kg/hour
  • terminate 12-72 hours
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24
Q

Lidocaine require careful monitoring of _______, hepatic and ________ dysfunciton.

A
  • Cardiac
  • Renal
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25
Q

Plasma Lidocaine Concentration of 1-5 mcg/ml causes

A

Analgesia

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26
Q

Plasma Lidocaine Concentration of 5-10 mcg/ml causes:
* Circum- oral numbness,
* __________
* ______ muscle twitching
* systemic ________
* ___________ depression.

A
  • tinnitus
  • skeletal
  • hypotension
  • Myocardial
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27
Q

Plasma Lidocaine Concentration of 10-15 mcg/mL causes _________ and _________.

A
  • Seizures
  • Unconsciousness
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28
Q

Plasma Lidocaine Concentration of 15- 25 causes _______ and _________.

A
  • Apnea
  • Coma
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29
Q

Plasma Lidocaine Concentration of >25 mcg/ml causes ____________ depression.

A

Cardiovascular Depression

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30
Q

Local Anesthetic Molecular Structure has a (1) _________ portion connected by a (2) ___________chain to the (3) _____________ portion.

A
  • lipophillic
  • hydrocarbon
  • hydrophillic
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31
Q

Local Anesthetic Molecular Structure:
Bond Between _________ portion and ___________ chain classifies it as an amide or ester

A
  • lipophillic portion
  • hydrocarbon
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32
Q

Local Anesthetic Compostion constists of:
* ph __ (___ salt)
* Epinephrine
* __________ bisulfite.

A
  • 6 (HCL salt)
  • weak base
  • Sodium
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33
Q

General role for differentiating Amide from Ester LA?

A
  • Amides have 2 i’s
  • Esters have 1 i.
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34
Q

______ ______ is the main determinant of DOA, but not the sole determinant.

A

Protein Binding

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35
Q

______ _____ is the main determinant of Potency.

A

Lipid Solubility

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36
Q

Name (3) Ester Local anesthetics

A
  • Procaine
  • Chloroprocaine
  • Tetracaine
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37
Q

Name (6) Amide Local Anesthetics

A
  • Lidocaine
  • Prilocaine
  • Mepivacaine
  • Buprivacaine
  • Levobupivacaine
  • Ropivacaine
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38
Q

Procaine
potency/onset/Duration

A
  • 1
  • Slow
  • 45-60 mins
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39
Q

Chloroprocaine
potency/onset/Duration

A
  • 4
  • Rapid
  • 30-45 mins
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40
Q

Tetracaine
Potency/Onset/Duration

A
  • 16
  • Slow
  • 60-180 mins
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41
Q

Lidocaine
potency/onset/duration

A
  • 1
  • rapid
  • 60-120 mins
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42
Q

Prilocaine
potency/onset/duration

A
  • 1
  • slow
  • 60-120 mins
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43
Q

Mepivacaine
potency/onset/duration

A
  • 1
  • slow
  • 90-180 mins
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44
Q

Bupivacaine
potency/onset/duration

A
  • 4
  • slow
  • 240-480 mins
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45
Q

Levobupivacaine
potency/onset/duration

A
  • 4
  • slow
  • 240-480 mins
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46
Q

Ropivacaine
potency/onset/duration

A
  • 4
  • slow
  • 240-480 mins
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47
Q

Name the (1) Amide Local Anesthetic that has a rapid onset

A
  • Lidocaine
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48
Q

Name the (1) Ester Local Anesthetic that is rapid acting?

A

Chloroprocaine

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49
Q

What Ester Local Anesthetic has the longest duration?

A
  • Tetracaine
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50
Q

Procaine pK

A

8.9

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51
Q

Chloroprocaine pK

A

8.7

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52
Q

Tetracaine pK

A

8.5

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53
Q

Lidocaine pK

A

7.9

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54
Q

Prilocaine pK

A

7.9

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55
Q

Mepivacaine pK

A

7.6

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56
Q

Bupivacaine pK

A

8.1

57
Q

levobupivacaine pK

A

8.1

58
Q

Ropivacaine pK

A

8.1

59
Q

______ has the lowest pK of the base local anesthetics. (pK= __)

A
  • mepivacaine
  • 7.6
60
Q

________ has the highest pK of all the local anesthetics. (pK = ___)

A
  • Procaine
  • 8.9
61
Q

E 1/2 of Procaine

A

9 mins

62
Q

E 1/2 of Chloroprocaine

A

7 mins

63
Q

E 1/2 of Lidocaine

A

96 mins

64
Q

E 1/2 of Prilocaine

A

96 mins

65
Q

E 1/2 of Mepivacaine

A

114 mins

66
Q

E 1/2 of Bupivacaine

A

210 mins

67
Q

E 1/2 of Levobupivacaine

A

156 mins

68
Q

E 1/2 of Ropivacaine

A

108

69
Q

(3) Liposome Local Anesthetics are:

A
  • Lidocaine
  • Tetracaine
  • bupivacaine
70
Q

Liposome LA upload a ______ amount of LA into molecole and have a _______ release of LA in the _______.

A
  • higher
  • consistent
  • tissue
71
Q

Liposome LA have a ______ duration of action and ______ toxicity.

A
  • prolonged
  • decreased
72
Q

FDA released: Bupivacaine ER (______) which can last up to ____ hours.

A
  • Exparel
  • 96 hours
73
Q

LA bind to _____-gated ____ channels. They block/inhibit Na passage in _______ membranes.

A
  • voltage- gated Sodium Channels
  • nerve
74
Q

Local Anesthetics:
* bind to Voltage-gated ___ channels.
* _____ Na+ passage in nerve membranes.
* Slows rate of __________.
* Does not reach _______.
* No action potential

A
  • Na Channels
  • Inhibits/blocks
  • depolarization
  • threshold
75
Q

Some factors of LA that affect blockade:
* _____ solubility or _____ -ionized/unionized form.
* Repetively _______ nerve.
* _______ of the nerve.

A
  • Lipid
  • non-ionized
  • stimulated
  • Diameter
76
Q

Other Sites of Action targets for LA are ______ channels, ______ Ion Channels and ____ protein- coupled receptors.

A
  • Potassium
  • calcium
  • G
77
Q

_____ or ___ (LAs) = MAC (Volatiles).

1 MAC should block ___ cm

A
  • Minimum Effective Concentration (MEC)
  • Cm
  • 1
78
Q

Mimimum Effect Concentration:
_____ fibers need _____ concentrations of LAs.

A
  • Larger
  • Higher
79
Q

T/F: Sensory nerves have a higher Minimum Effective Concentration than Motor nerves 2x in diameter.

A
  • False
80
Q

Minimum Effective Concentration requires 2, preferably 3 Nodes of ______ (__ cm) blocked.

A
  • Ranvier
  • 1 cm
81
Q

Minimum Effective Concentration:
* Preganglionic __ fibers (_____) are in charge of (SNS) are ________.

20

A
  • B
  • fastest
  • sensory
82
Q

Minimum Effective Concentration:
Myelinated ___ (medium) and ___ fibers (fastest) > Unmyelinated ___ fibers (small)

A
  • A
  • B
  • C
83
Q

Minimum Effective Concentration:

Pain and Temperature (touch/pressure, proprioception and motor) are Myelinated _______ and Unmyelinated ___ fibers.

20

A
  • A-δ
  • C
84
Q

Minimum Effective Concentration:
Pregnancy ________ sensitivity.

20

A
  • increased
85
Q

Name the safe level to block in the throracic region? And why?

A
  • T1-T4
  • Lower and you will block diaphram and cardiac accelerators
86
Q

Pharmacokinetics LA:
* Weak _______ with pKa values above physiologic _______.
* Only _____ in lipid-soluble ________ form .

A
  • bases
  • pH
  • 50%
  • nonionized
87
Q

LA: pKa ______ to physiologic pH = most ______ OOA.

A
  • closest
  • rapid
88
Q

LA:
* Intrinsic __________ activity = increases potency and DOA
* ________ = greater systemic absorption

A
  • vasodilator
  • lidocaine
89
Q

LA:Factors that influence absorption:
* _________ of injection
* Dosage
* Use of ___________.
* Pharmacologic _______________ of the drug

A
  • site
  • Epinephrine
  • Characteristics
90
Q

Subcutaneous LA result in the _______ blood concentration.

A

lowest

91
Q

Intravenous LA result in the _______ Blood Concentration.

A
  • highest
92
Q

LA: Pharmacologic characteristics of the drug is determine by the
_________ of _______ distribution.

A
  • rate
  • tissue
93
Q

______ solubility is the primary determinant of ________.

A
  • Lipid
  • potency
94
Q

Pharmacologic characteristics of the drug is determine by:
* rate of ________
* Cardiac ________
* ________ binding

A
  • rate of clearance
  • Cardiac Output
  • Protein Binding
95
Q

Protein binding of a LA:
% bound is _______ relatated to % plasma.

A
  • inversely
96
Q

Protein binding % of Lidocaine

A

70

97
Q

Protein Binding % of Mepivacaine

A

77

98
Q

Protein binding % of Bupivacaine

A
  • 95
99
Q

Metabolism of Amide LA is due to microsomal ______ in the _____.

A
  • enzymes
  • liver
100
Q

Most Rapidly metabolized Amide LA.

A

Prilocaine

101
Q

Intermediate metabolized Amide LA. (2)

A
  • Lidocaine
  • Mepivacaine
102
Q

Slowest Metabolized Amide LA. (3)

A
  • Etidocaine
  • Bupivacaine
  • Ropivacaine
103
Q

Metabolism of Ester LA are Hydolysis by _______ enzymes in _______ > liver.

A
  • cholinesterase
  • plasma
104
Q

Name the (1) Esters LA that is metabolized in the liver.

A

Cocaine

105
Q

______ -______ acid in Ester LA is the main cause of allergic reactions

A

para-aminobenzoic acid

106
Q

Amides are metabolized ____ than esters.

A

slower

107
Q

LA that are First-Pass Pulmonary Extraction

A
  • lidocaine
  • bupivacaine (dose-dependent)
  • prilocaine
108
Q

Renal Eliminatation and Clearance of LA:
* poor water ____
* Unchanged drug in urine = __%
* Cocaine is ___ - __ %
* PABA through _______.

A
  • solubility
  • 5%
  • 10 to 12%
  • urine
109
Q

Pregnancy causes _____ levels of plasma cholinesterase

A

lower

110
Q

Pregnancy: Significant Transplacental transfer:
* _______, but not significant with _______/
* Ion ________
* Protein binding = rate and degree of _______.

A
  • Amides
  • esters
  • ion trapping
  • diffusion
111
Q

Ion trapping in Fetus:
* Fetus has a _____ pH and a ___ CO2
* non-ionized turns ______ can gets trapped
* causes fetal ________.

A
  • lower
  • higher
  • ionized
  • bradycardia
112
Q

Bupivacaine:
Protein bound/Arterial Concentration

A
  • 95%
  • 0.32
113
Q

Lidocaine:
Protein bound/Arterial Concentration

A
  • 70%
  • 0.73
114
Q

Prilocaine:
Protein Bound/Arterial Concentration

A
  • 55%
  • 0.85
115
Q

Lidocaine is metabolized through _______ dealkylation in _____, then hydrolysis.

A
  • Oxidative
  • liver
116
Q

Metabolite of Lidocaine

A

Xylidide

117
Q

______ disease will affect metabolism and elimination of Lidocaine.

A

Hepatic

118
Q

_______ is an LA that is also an anti-dysrhythmic.

A

Lidocaine

119
Q

maximum infiltration dose of lidocaine is _____ mgs plain and _____ mgs w/ EPI.

A
  • 300
  • 500
120
Q

_______ induced Hypertension can prolong clearance of Lidocaine.

A

Pregnancy

121
Q

________ is the metabolite of Prilocaine that converts Hemoglobin to methemoglobin causing ______________.

A
  • Orthotoluidine
  • Methemoglobinemia
122
Q

Orthotoluidine:
* converts Hgb –> Met HGB
* Prilocaine Dose: > _____ mgs
* Cause _____ d/t decreased O2 carrying capacity
* Tx: __________ Blue

A
  • > 600 mgs
  • Cyanosis
  • methylene blue
123
Q

Methylene Blue:
* ___ - ___ mgs/kg IV over 5 mins
* Total dose does not exceed ___ to___ mgs/kg

A
  • 1 to 2 mgs/kgs IV
  • 7 to 8 mgs/kg
124
Q

Mepivacaine is similiar to Lidocaine except:
* ____ DOA
* lacks ______ activity
* ______ elimination in fetus & newborns; No OB.

A
  • longer
  • vasodilator
  • prolonged
125
Q

Bupivacaine:
* Metabolism: _______ hydroxylation, N-dealkylation, _____ hydrolysis and conjugation
* Protein (95%) binding site: ________ - Acid glycoprotein

A
  • aromatic
  • amide
  • α1-Acid
126
Q

Dibucaine
* Metabolism: ______
* MOA: inhibits the activity of normal butyrylcholinesterase (_________ ___________) by more than ___%.

A
  • liver
  • plasma cholinesterase
  • 70%
127
Q

Procaine
* Metabolite: _______, excreted unchanged in _______.

A
  • PABA
  • urine
128
Q

Chloroprocaine
* Metabolism: ________ ____________ (3.5x faster)
* Pregnancy __________ plasma cholinesterase by ____%

A
  • plasma cholinesterase
  • decreases
  • 19%
129
Q

Tetracaine
Metabolism: _________ than procaine

A

slower

130
Q

Hydrolysis: chloroprocaine > ________ > tetracaine

A

procaine

131
Q

Benzocaine is unique because it is a weak ______ with a pKa of ____.

A
  • acid
  • 3.5
132
Q

Benzocaine is used for ________ anesthesia of ______ membranes:
* _______ intubations, Endoscopy, TEE and __________.

A
  • Topical
  • mucous
  • Tracheal Intubation
  • Bronchoscopy
133
Q

Benzocaine
* Onset: _______
* Duration: ____ to ____ mins
* Dose: Brief Spray (20%) = ___ to ___ mgs

A
  • rapid
  • 30 to 60 mins
  • 20%
  • 200-300 mgs
134
Q

A critical S/E of Benzocaine is ____________.

A

methemoglobinemia.

135
Q

Cocaine is metabolized by _______ and _____ Cholinesterase.

A
  • Liver
  • plasma
136
Q

Plasma Cholinesterase is decreased in Parturient, ________, Elderly and ______ Hepatic Disease.

A
  • Neonates
  • Severe
137
Q

Cocaine:
* Peak: ___ to ___ mins
* Duration: ___ minutes after peak
* Elimination by _____ (24 to 36 hours)

A
  • 30 to 45 mins
  • 60 minutes
  • urine
138
Q

Cocaine cautions:
* Coronary _______
* _______ dysrhythmias
* HTN
* Tachycardia
* CAD

A
  • vasospasms
  • ventricular dysrhythmias
139
Q

Name the (1) LA that is a weak acid and not a weak base.

A
  • Benzocaine

Pharmacology Exam 4 (4 decks)

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