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Quiz 5 Flashcards

1
Q

What are the 3 layers of peripheral nerves?

A

endoneurium (inside), perineurium (middle), epineurium (outside)

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2
Q

Where are the Na gated channels located on peripheral nerves?

A

on the Nodes of Ranvier (break points between successive bands of myelin)

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3
Q

What do the Schwann cells do?

A

cell support and insulation- make myelin

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4
Q

What is saltatory conduction and where does it NOT occur?

A

AP jump from node to node- does not happen in C fibers because no myelination

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5
Q

What is the normal RMP?

A

-70 to -90 mV

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6
Q

What is the MoA for LA?

A

drug reversibly binds to sodium channel in the nerve in the INACTIVATED state and prevents them from opening

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7
Q

How many successive nodes of Ranvier must the LA bind to for it to be effective?

A

3

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8
Q

The ? form has to diffuse into the nerve axon first, and once inside, the new equilibrium forms between ionized and nonionized forms. The ? form binds to receptors

A

non-ionized, ionized

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9
Q

Do LA have an effect on RMP or threshold?

A

no

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10
Q

Describe A alpha fibers

A

motor efferent, proprioception; 12-30 mm diameter, 70-120 m/s conduction, heavily myelinated

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11
Q

Describe A beta fibers

A

touch and pressure, 5-12 mm diameter, 30-70 m/s conduction, myelinated

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12
Q

Describe A gamma fibers

A

motor efferent, 3-6 mm diameter, 30-70 m/s conduction, myelinated

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13
Q

Describe A delta fibers

A

pain, temp and touch; 2-5 mm diameter, 12-30 m/s conduction, myelinated

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14
Q

Describe B fibers

A

preganglionic autonomic fibers; <3 mm diameter, 3-14 m/s conduction, some myelination

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15
Q

Describe C dorsal root fibers

A

pain and temperature, 0.4-1.2 mm diameter, 0.5-2 m/s conduction, not myelinated

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16
Q

Describe C sympathetic fibers

A

postganglionic sympathetic fibers, 0.3-1.3 mm diameter, 0.7-2.3 m/s conduction, not myelinated

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17
Q

What fibers make up motor and muscle control?

A

A alpha fibers

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18
Q

What fibers make up sensory fibers and control touch, vibration, position, perception?

A

A alpha and beta

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19
Q

What fibers make up sensory fibers and control cold perception, and pain?

A

A delta fibers

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20
Q

What is the order in which nerves are blocked?

A

1) autonomic 2) sensory 3) motor

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21
Q

What is the minimum blocking concentration (Cm)?

A

lowest concentration of drug that is needed for blocking impulse propagation

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22
Q

The Cm of motor fibers is about ? that of sensory fibers

A

twice

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23
Q

What factors can affect the Cm of LA?

A

temp, pH, calcium concentration of bathing solution

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24
Q

Almost all LA are ?, which exist in both ? and ? forms when injected into physiological pH (there is an exception)

A

tertiary amines; ionized and nonionized (benzocaine is an exception- secondary amine, permanently non-ionized)

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25
What parts of the LA molecule make them lipophilic and hydrophilic?
aromatic ring- lipophilic | amine- hydrophilic
26
Which type of LA have a higher allergic potential?
esters- broken down to PABA
27
What will increase LA potency, and how can this become a problem?
a higher lipid solubility- also correlated with higher protein binding, longer DoA, and higher tendency for cardiotoxicity
28
What is the most lipid soluble ester of commonly used LA?
tetracaine
29
What is the most lipid soluble amide?
bupivacaine
30
What is more important in terms of DoA, protein binding or lipid solubility?
protein binding
31
What is the most important factor for onset?
ionization (lipid solubility)
32
LA are weak ? and prefer to bind to ?
bases; alpha 1 acid glycoprotein
33
Do esters or amides have shorter DoA?
esters
34
List the LA from most to least in terms of protein binding
bupivicaine (95%) > etidocaine, ropivicaine, tetracaine (94%) > mepivicaine (77%) > lidocaine (64%) > procaine (6%) > chloroprocaine (0%)
35
What does the addition of sodium bicarb to LA do?
increases pH of the LA, and therefore increases the amount of drug in the nonionized form
36
What LA are considered low potency and short DoA (60-90 min)?
procaine and chloroprocaine
37
What LA are considered inermediate potency and duration (90-240 min)?
mepivacaine, prilocaine, lidocaine
38
What LA are considered high potency, long DoA (180-600 min)
tetracaine, bupivacaine, etidocaine, ropivacaine, levobupivacaine
39
What is the max single dose for infiltation of procaine?
500-600 mg or 7 mg/kg
40
What is the max single dose for infiltration of chloroprocaine?
600-800 mg or 11 mg/kg
41
What is the max single dose for infiltration of tetracaine?
100 mg (topical)
42
What is the max single dose for lidocaine?
300 mg 4.5 mg/kg
43
What is the max single dose for prilocaine?
400-600 mg or 8 mg/kg
44
What is the max single dose for mepivacaine
300-400 mg or 7 mg/kg
45
What is the max single dose for bupivacaine and levobupivacaine?
175 mg or 2.5 mg/kg
46
What is the max single dose for ropivacaine
200-250 mg or 3 mg/kg
47
What is the pKa of procaine?
8.9
48
What is the pKa of chloroprocaine?
8.7
49
What is the pKa of tetracaine?
8.5
50
What is the pKa of lidocaine and prilocaine?
7.9
51
What is the pKa of mepivacaine?
7.6
52
What is the pKa of bupivacaine, levobupivacaine, and ropivacaine?
8.1
53
List from most absorbent to least absorbent injection sites
IV> tracheal > intercostal > caudal > paracervical > epidural > brachial plexus > subarachnoid, sciatic, fem > subcutaneous
54
What is the mnemonic for injection sites?
In Time I Can Please Everyone But Susie & Sally
55
What does the addition of epi do for LA?
decreases rate of absorption, facilitates neuronal uptake, enhances analgesic quality, prolongs DoA, limits toxic SE
56
What is the max dose of epi you can administer to prolong LA?
200-250 mcg or 3-5 mcg/kg
57
What concentration of epi should you use for LA?
1:200,000 (5 mcg/mL)
58
What are some contraindications to epinephrine?
unstable angina, cardiac dysrhythmias, uncontrolled HTN, uteroplacental insufficiency, areas that block collateral BF (digits)
59
What has the most significant vasoconstrictive property?
cocaine
60
What topical LA do we use, what is it made with, and how long does it last?
EMLA cream; 1:1 lidocaine and prilocaine, lasts 1-2 hours
61
When is EMLA cream contraindicated?
open skin, mucous membranes, amide LA allergy
62
How are amides metabolized?
P450 enzymes in the liver
63
What can the metabolites of prilocaine and benzocaine do?
can accumulate after large doses and convert hemoglobin to methemoglobin- treat with methylene blue
64
How are esters metabolized?
plasma cholinesterases- rapid hydrolysis
65
What are the 4 conditions that increase duration of esters because they decrease cholinesterase activity?
pregnancy, liver disease, 1st 6 months of life, atypical plasma cholinesterase
66
What are 4 drugs that prolong ester activity by decreasing plasma cholinesterase activity?
echthiophate, neostigmine, pyridostigmine, edrophonium
67
What is the least toxic amide?
prilocaine
68
Which amide has the slowest hepatic metabolism?
bupivacaine
69
What are the 3 least potent amides?
lidocaine, mepivicaine, prilocaine
70
What is LAST?
local anesthetic systemic toxicity
71
What can LAST cause?
seizures, coma, blockade of cardiac ion channels, respiratory and cardiac arrest, muscle twitching
72
What are the most common anesthetics that can lead to LAST?
epidural, axilary, interscalene
73
What is the most common drug that causes LAST?
bupivicaine, due to its high affinity for Na channels
74
What are predisposing risk factors for LAST?
pregnancy, hypoxemia, respiratory acidosis
75
What are some early signs of LAST?
perioral numbness, facial tingling, tinnitis, metallic taste, slurred speech, vertigo
76
What is a safe plasma concentration of lidocaine
1-5 mcg/mL
77
What plasma level of lidocaine leads to cardiovascular collapse?
>25 mcg/mL
78
What is the treatment for LAST?
airway support, mechanical compressions, 20% lipid solution, cardiac bypass
79
What is the least toxic ester?
chloroprocaine
80
What is the most toxic ester?
tetracaine
81
Who should you avoid esters in?
patients with atypical or depressed cholinesterase activity
82
Never administer a LA into a neuraxial compartment if...
it contains a preservative
83
What drugs decrease hepatic BF and decrease lidocaine clearance?
propranolol (BB) and cimetidine (H2 blockers)
84
What is the max dose of bupivicaine with epi?
225 mg
85
What is the max dose of lidocaine with epi?
7 mg/kg or 500 mg
86
What is the max dose of mepivacaine with epi?
500 mg
87
What is the max dose of benzocaine, with or without epi?
200 mg
88
What is the max dose of chloroprocaine with epi?
1000 mg or 14 mg/kg
89
What is the max dose of cocaine?
3 mg/kg or 150 mg
90
LA's typically work by binding to the receptor in the Na channel within the neuron while in their charged form. Which LA is an exception to this rule?
benzocaine (weak acid)
91
LA with which pKa value would you expect to have the quickest onset of action?
7.4
92
LA produce a differential blockade in which different modes of nerve transmission are interrupted in an equal fashion. Which is the correct order?
temp sensation, sharp pain, light touch
93
The concept of Cm is most similar to?
MAC

Pharm 2 (7 decks)

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