Local Anesthetics Part 1 Flashcards
(139 cards)
1
Q
________ is the first local anesthetic.
A
cocaine
2
Q
1st synthetic Ester: _________ (1905)
A
Procaine
3
Q
1st synthetic Amide:____________ (1943)
A
Lidocaine
4
Q
__________ is the standard to which all local anesthetics are compared.
A
lidocaine
5
Q
Local Anesthetics are used for _________, acute and chronic pain and ___________.
A
- dysrhythmias
- anesthesia
6
Q
Local Anesthetics are used in anesthesia for ________ Blockade, _______ anesthesia and ____________ muscle paralysis.
A
- ANS
- Sensory
- Skeletal
7
Q
All Local Anesthetics are what type of Antiarrythmic classification?
A
- Class 1:Sodium Channel Blockers
8
Q
Antiarrhythmic Classes:
* Class 1: _______________
* Class 2: ______________
* Class 3: ______________
* Class 4: _____________
A
- sodium-channel blockers
- Beta-Blockers
- Potassium-channel blockers
- Calcium-channel blockers
9
Q
Miscellaneous Antiarrhythmic Drugs can include _____________, electrolytes supplements ( ______ and potassium) and ____________ compounds.
A
- adenosine
- magnesium
- digitalis
10
Q
Pre-Op Tylenol dose is ________ mg PO.
Pre-Op Gabapentin dose is _______ mg PO.
A
- 1000
- 300
11
Q
Pre-op dose of Ofiremev is ____ gram, if patient has OSA.
A
1 gram
12
Q
Intra-Op: Induce GA w/ __________, use lidocaine to blunt the burn, ketamine and __________. Maintain GA with _______________ anesthetic.
A
- propofol
- paralytic
- volatile
13
Q
Intra-Op Magnesium dose is ____ - ____ mg/kg (max ___ G) infusion over 1 hour.
A
- 30-60 mg/kg
- 6 grams
14
Q
Intra-Op Lidocaine infusion dose is ___mg/kg infusion ___ hour.
A
- 1 mg/kg
- 1 hour
15
Q
Intra-Op: Ondesetron, Decadron and _________ can be given as permitted by the surgeon.
A
- Ketoralac.
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
17
Q
Post-Op Tylenol dose is ______ mg TID
A
1000 mg
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
19
Q
Post Op Gabapentin dose is ______ mg ______.
A
- 300 mg
- TID
20
Q
Post-Op Dose:
Celebrex or Advil ____ as permitted byt the surgeon.
A
TID
21
Q
Lidocaine
* Intial Bolus: __ - __ mg/kg IV
* over ___ - __ mins
A
- 1-2 mg/kg over 2-4 mins
22
Q
Lidocaine is an ______ LA.
A
Amide
23
Q
Lidocaine:
* Drip: __ - __ mg/kg/hour:
* Terminate gtt within ___ - ___ hours.
A
- 1-2 mg/kg/hour
- terminate 12-72 hours
24
Q
Lidocaine require careful monitoring of _______, hepatic and ________ dysfunciton.
A
- Cardiac
- Renal
25
Plasma Lidocaine Concentration of 1-5 mcg/ml causes
Analgesia
26
Plasma Lidocaine Concentration of 5-10 mcg/ml causes:
* Circum- oral numbness,
* __________
* ______ muscle twitching
* systemic ________
* ___________ depression.
* tinnitus
* skeletal
* hypotension
* Myocardial
27
Plasma Lidocaine Concentration of 10-15 mcg/mL causes _________ and _________.
* Seizures
* Unconsciousness
28
Plasma Lidocaine Concentration of 15- 25 causes _______ and _________.
* Apnea
* Coma
29
Plasma Lidocaine Concentration of >25 mcg/ml causes ____________ depression.
Cardiovascular Depression
30
Local Anesthetic Molecular Structure has a (1) _________ portion connected by a (2) ___________chain to the (3) _____________ portion.
* lipophillic
* hydrocarbon
* hydrophillic
31
Local Anesthetic Molecular Structure:
Bond Between _________ portion and ___________ chain classifies it as an amide or ester
* lipophillic portion
* hydrocarbon
32
Local Anesthetic Compostion constists of:
* ph __ (___ salt)
* Epinephrine
* __________ bisulfite.
* 6 (HCL salt)
* weak base
* Sodium
33
General role for differentiating Amide from Ester LA?
* Amides have 2 i's
* Esters have 1 i.
34
______ ______ is the main determinant of DOA, but not the sole determinant.
Protein Binding
35
______ _____ is the main determinant of Potency.
Lipid Solubility
36
Name (3) Ester Local anesthetics
* Procaine
* Chloroprocaine
* Tetracaine
37
Name (6) Amide Local Anesthetics
* Lidocaine
* Prilocaine
* Mepivacaine
* Buprivacaine
* Levobupivacaine
* Ropivacaine
38
Procaine
potency/onset/Duration
* 1
* Slow
* 45-60 mins
39
Chloroprocaine
potency/onset/Duration
* 4
* Rapid
* 30-45 mins
40
Tetracaine
Potency/Onset/Duration
* 16
* Slow
* 60-180 mins
41
Lidocaine
potency/onset/duration
* 1
* rapid
* 60-120 mins
42
Prilocaine
potency/onset/duration
* 1
* slow
* 60-120 mins
43
Mepivacaine
potency/onset/duration
* 1
* slow
* 90-180 mins
44
Bupivacaine
potency/onset/duration
* 4
* slow
* 240-480 mins
45
Levobupivacaine
potency/onset/duration
* 4
* slow
* 240-480 mins
46
Ropivacaine
potency/onset/duration
* 4
* slow
* 240-480 mins
47
Name the (1) Amide Local Anesthetic that has a rapid onset
* Lidocaine
48
Name the (1) Ester Local Anesthetic that is rapid acting?
Chloroprocaine
49
What Ester Local Anesthetic has the longest duration?
* Tetracaine
50
Procaine pK
8.9
51
Chloroprocaine pK
8.7
52
Tetracaine pK
8.5
53
Lidocaine pK
7.9
54
Prilocaine pK
7.9
55
Mepivacaine pK
7.6
56
Bupivacaine pK
8.1
57
levobupivacaine pK
8.1
58
Ropivacaine pK
8.1
59
______ has the lowest pK of the base local anesthetics. (pK= __)
* mepivacaine
* 7.6
60
________ has the highest pK of all the local anesthetics. (pK = ___)
* Procaine
* 8.9
61
E 1/2 of Procaine
9 mins
62
E 1/2 of Chloroprocaine
7 mins
63
E 1/2 of Lidocaine
96 mins
64
E 1/2 of Prilocaine
96 mins
65
E 1/2 of Mepivacaine
114 mins
66
E 1/2 of Bupivacaine
210 mins
67
E 1/2 of Levobupivacaine
156 mins
68
E 1/2 of Ropivacaine
108
69
(3) Liposome Local Anesthetics are:
* Lidocaine
* Tetracaine
* bupivacaine
70
Liposome LA upload a ______ amount of LA into molecole and have a _______ release of LA in the _______.
* higher
* consistent
* tissue
71
Liposome LA have a ______ duration of action and ______ toxicity.
* prolonged
* decreased
72
FDA released: Bupivacaine ER (______) which can last up to ____ hours.
* Exparel
* 96 hours
73
LA bind to _____-gated ____ channels. They block/inhibit Na passage in _______ membranes.
* voltage- gated Sodium Channels
* nerve
74
Local Anesthetics:
* bind to Voltage-gated ___ channels.
* _____ Na+ passage in nerve membranes.
* Slows rate of __________.
* Does not reach _______.
* No action potential
* Na Channels
* Inhibits/blocks
* depolarization
* threshold
75
Some factors of LA that affect blockade:
* _____ solubility or _____ -ionized/unionized form.
* Repetively _______ nerve.
* _______ of the nerve.
* Lipid
* non-ionized
* stimulated
* Diameter
76
Other Sites of Action targets for LA are ______ channels, ______ Ion Channels and ____ protein- coupled receptors.
* Potassium
* calcium
* G
77
_____ or ___ (LAs) = MAC (Volatiles).
1 MAC should block ___ cm
* Minimum Effective Concentration (MEC)
* Cm
* 1
78
Mimimum Effect Concentration:
_____ fibers need _____ concentrations of LAs.
* Larger
* Higher
79
T/F: Sensory nerves have a higher Minimum Effective Concentration than Motor nerves 2x in diameter.
* False
80
Minimum Effective Concentration requires 2, preferably 3 Nodes of ______ (__ cm) blocked.
* Ranvier
* 1 cm
81
Minimum Effective Concentration:
* Preganglionic __ fibers (_____) are in charge of (SNS) are ________.
## Footnote
20
* B
* fastest
* sensory
82
Minimum Effective Concentration:
Myelinated ___ (medium) and ___ fibers (fastest) > Unmyelinated ___ fibers (small)
* A
* B
* C
83
Minimum Effective Concentration:
Pain and Temperature (touch/pressure, proprioception and motor) are Myelinated _______ and Unmyelinated ___ fibers.
## Footnote
20
* A-δ
* C
84
Minimum Effective Concentration:
Pregnancy ________ sensitivity.
## Footnote
20
* increased
85
Name the safe level to block in the throracic region? And why?
* T1-T4
* Lower and you will block diaphram and cardiac accelerators
86
Pharmacokinetics LA:
* Weak _______ with pKa values above physiologic _______.
* Only _____ in lipid-soluble ________ form .
* bases
* pH
* 50%
* nonionized
87
LA: pKa ______ to physiologic pH = most ______ OOA.
* closest
* rapid
88
LA:
* Intrinsic __________ activity = increases potency and DOA
* ________ = greater systemic absorption
* vasodilator
* lidocaine
89
LA:Factors that influence absorption:
* _________ of injection
* Dosage
* Use of ___________.
* Pharmacologic _______________ of the drug
* site
* Epinephrine
* Characteristics
90
Subcutaneous LA result in the _______ blood concentration.
lowest
91
Intravenous LA result in the _______ Blood Concentration.
* highest
92
LA: Pharmacologic characteristics of the drug is determine by the
_________ of _______ distribution.
* rate
* tissue
93
______ solubility is the primary determinant of ________.
* Lipid
* potency
94
Pharmacologic characteristics of the drug is determine by:
* rate of ________
* Cardiac ________
* ________ binding
* rate of clearance
* Cardiac Output
* Protein Binding
95
Protein binding of a LA:
% bound is _______ relatated to % plasma.
* inversely
96
Protein binding % of Lidocaine
70
97
Protein Binding % of Mepivacaine
77
98
Protein binding % of Bupivacaine
* 95
99
Metabolism of Amide LA is due to microsomal ______ in the _____.
* enzymes
* liver
100
Most Rapidly metabolized Amide LA.
Prilocaine
101
Intermediate metabolized Amide LA. (2)
* Lidocaine
* Mepivacaine
102
Slowest Metabolized Amide LA. (3)
* Etidocaine
* Bupivacaine
* Ropivacaine
103
Metabolism of Ester LA are Hydolysis by _______ enzymes in _______ > liver.
* cholinesterase
* plasma
104
Name the (1) Esters LA that is metabolized in the liver.
Cocaine
105
______ -______ acid in Ester LA is the main cause of allergic reactions
para-aminobenzoic acid
106
Amides are metabolized ____ than esters.
slower
107
LA that are First-Pass Pulmonary Extraction
* lidocaine
* bupivacaine (dose-dependent)
* prilocaine
108
Renal Eliminatation and Clearance of LA:
* poor water ____
* Unchanged drug in urine = __%
* Cocaine is ___ - __ %
* PABA through _______.
* solubility
* 5%
* 10 to 12%
* urine
109
Pregnancy causes _____ levels of plasma cholinesterase
lower
110
Pregnancy: Significant Transplacental transfer:
* _______, but not significant with _______/
* Ion ________
* Protein binding = rate and degree of _______.
* Amides
* esters
* ion trapping
* diffusion
111
Ion trapping in Fetus:
* Fetus has a _____ pH and a ___ CO2
* non-ionized turns ______ can gets trapped
* causes fetal ________.
* lower
* higher
* ionized
* bradycardia
112
Bupivacaine:
Protein bound/Arterial Concentration
* 95%
* 0.32
113
Lidocaine:
Protein bound/Arterial Concentration
* 70%
* 0.73
114
Prilocaine:
Protein Bound/Arterial Concentration
* 55%
* 0.85
115
Lidocaine is metabolized through _______ dealkylation in _____, then hydrolysis.
* Oxidative
* liver
116
Metabolite of Lidocaine
Xylidide
117
______ disease will affect metabolism and elimination of Lidocaine.
Hepatic
118
_______ is an LA that is also an anti-dysrhythmic.
Lidocaine
119
maximum infiltration dose of lidocaine is _____ mgs plain and _____ mgs w/ EPI.
* 300
* 500
120
_______ induced Hypertension can prolong clearance of Lidocaine.
Pregnancy
121
________ is the metabolite of Prilocaine that converts Hemoglobin to methemoglobin causing ______________.
* Orthotoluidine
* Methemoglobinemia
122
Orthotoluidine:
* converts Hgb --> Met HGB
* Prilocaine Dose: > _____ mgs
* Cause _____ d/t decreased O2 carrying capacity
* Tx: __________ Blue
* >600 mgs
* Cyanosis
* methylene blue
123
Methylene Blue:
* ___ - ___ mgs/kg IV over 5 mins
* Total dose does not exceed ___ to___ mgs/kg
* 1 to 2 mgs/kgs IV
* 7 to 8 mgs/kg
124
Mepivacaine is similiar to Lidocaine except:
* ____ DOA
* lacks ______ activity
* ______ elimination in fetus & newborns; No OB.
* longer
* vasodilator
* prolonged
125
Bupivacaine:
* Metabolism: _______ hydroxylation, N-dealkylation, _____ hydrolysis and conjugation
* Protein (95%) binding site: ________ - Acid glycoprotein
* aromatic
* amide
* α1-Acid
126
Dibucaine
* Metabolism: ______
* MOA: inhibits the activity of normal butyrylcholinesterase (_________ ___________) by more than ___%.
* liver
* plasma cholinesterase
* 70%
127
Procaine
* Metabolite: _______, excreted unchanged in _______.
* PABA
* urine
128
Chloroprocaine
* Metabolism: ________ ____________ (3.5x faster)
* Pregnancy __________ plasma cholinesterase by ____%
* plasma cholinesterase
* decreases
* 19%
129
Tetracaine
Metabolism: _________ than procaine
slower
130
Hydrolysis: chloroprocaine > ________ > tetracaine
procaine
131
Benzocaine is unique because it is a weak ______ with a pKa of ____.
* acid
* 3.5
132
Benzocaine is used for ________ anesthesia of ______ membranes:
* _______ intubations, Endoscopy, TEE and __________.
* Topical
* mucous
* Tracheal Intubation
* Bronchoscopy
133
Benzocaine
* Onset: _______
* Duration: ____ to ____ mins
* Dose: Brief Spray (20%) = ___ to ___ mgs
* rapid
* 30 to 60 mins
* 20%
* 200-300 mgs
134
A critical S/E of Benzocaine is ____________.
methemoglobinemia.
135
Cocaine is metabolized by _______ and _____ Cholinesterase.
* Liver
* plasma
136
Plasma Cholinesterase is decreased in Parturient, ________, Elderly and ______ Hepatic Disease.
* Neonates
* Severe
137
Cocaine:
* Peak: ___ to ___ mins
* Duration: ___ minutes after peak
* Elimination by _____ (24 to 36 hours)
* 30 to 45 mins
* 60 minutes
* urine
138
Cocaine cautions:
* Coronary _______
* _______ dysrhythmias
* HTN
* Tachycardia
* CAD
* vasospasms
* ventricular dysrhythmias
139
Name the (1) LA that is a weak acid and not a weak base.
* Benzocaine
