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Local + Opioids > Important facts > Flashcards

Important facts Flashcards

1
Q

What factors increase respiratory depression with a PCA?

A

-Basal infusion rate
-Administration of other sedative medications
-Old age
-OSA and pulmonary disease

Respiratory depression is NOT higher when compared to other opioid routes

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2
Q

What opioid is not recommended with PCA pumps?

A

-Meperidine

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3
Q

What meds
target perception ?

A

General Anesthetics, opioids, and Alpha-2

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4
Q

What drugs target modulation ? Where is the most important site?

A

Neuraxial
NMDA
Alpha 2
AchE
SSRI
SNRI

Substantia Gelatinosa

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5
Q

What is the order of block onset for fiber types?

A

B
C
A (gamma and delta)
A (Alpha and Beta

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6
Q

What concept is analogous to ED50?

A

Minimum effective concentration.

Lower are more easily blocked
Higher are harder to block

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7
Q

Do local anesthetics affect the RMP or TP?

A

NO

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8
Q

Where do local anesthetics bind to?

A

Alpha subunit INSIDE the sodium channel.

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9
Q

What are the three building blocks of a local anesthetic ?

A

benzene ring - lipophilic
Intermediate chain - determines class
Tertiary amine- hydrophilic

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10
Q

What is the primary determinant of potency ?

A

Lipid solubility

Intrinsic vasodilating effect is a secondary effect of potency

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11
Q

What determines the duration of action of a local anesthetic?

A
  1. Protein binding
  2. Lipid solubility and intrinsic vasodilating activity
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12
Q

Which local has a high intrinsic vasodilating effect?

A

Lidocaine

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13
Q

Which locals have low protein binding

A
  1. Chloroprocaine - 0
  2. Procaine - 6
  3. Prilocaine - 55
  4. Lidocaine - 65
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14
Q

What factors influence vascular uptake into the blood?

A
  1. Site of injection
  2. Tissue blood flow
  3. Properties of local
  4. Metabolism
  5. Adding a vasoconstrictor
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15
Q

Rank the injection sites from most vascular to least

A

IV
Tracheal
Interpleural
Intercostal
Caudal
Epidural
Brachial Plexus
Femoral
Sciatic
Subq

***Femoral is low

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16
Q

What is the most common sign of LAST?

A

Seizure

Except cardiotoxicity with Bupivacaine

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17
Q

What conditions increase the risk of CNS toxicity with LAST?

A

Hypercarbia - Increases blood flow to brain and increases the free fraction to enter the brain

Hyperkalemia - Raises RMP

Metabolic acidosis - Decreases the convulsion threshold

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18
Q

What drug has the highest cardiotoxicity ? Why?

A

Bupivacaine, Levobupivacaine, Ropivacaine, Lidocaine

Affinity for the voltage gated channel

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19
Q

What’s the drug of choice for resuscitation from LAST? What to avoid ?

A

Amiodarone

Avoid vaso, lido, and procainamide

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20
Q

Treatment for LAST?

A

Lipid emulsion therapy

Bolus 100mL over 2-3 minutes
Infusion of 250mL over 20 minutes
Repeat and/or double

If under 70kg
1.5mL/kg of LBW
0.25mL/kg/min
Repeat

MAX DOSE 12mL/kg

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21
Q

Max dose age for tumescent anesthesia ?

A
  • 50mg/kg
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22
Q

What two locals produce a leftward shift in the oxyhemoglobin curve?

A

Prilocaine and benzocaine which creates anemia

ALSO

EMLA and cetacaine

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23
Q

Treatment for methemoglobinemia ?

A

Methylene blue 1-2mg/kg over 5 minutes

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24
Q

What patients are at risk for methemoglobinemia ?

A

Glucose-6 phosphate reductase deficiency

and

Fetal hgb

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25
Q

Max dose for EMLA cream?

A

0-3 , 1g - 10cm

3-12 months , 2g - 20cm

1-6 years ,10g - 100cm

7-12 years , 20g - 200cm

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26
Q

How does bicarbonate affect local ?

A

Shortens the onset time and reduces pain

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27
Q

WHAT DRUG REDUCES THE EFFECTIVNESS OF OPIOIDS?

A

Chloroprocaine

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28
Q

What drugs offer supplemental analgesia to locals?

A

Clonidine, Epi, Opioids

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29
Q

What can improve the diffusion through tissue?

A

Hyaluronidase, used in eye blocks frequently

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30
Q

What conditions allow extrajunctional receptors to populate in the myocyte?

A

Motor neuron injury
Spinal cord injury
Burns
Cerebrovascular accident
Chemical denervation
Tetanus
Sepsis
Muscular dystrophy

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31
Q

How are extra junctional receptors affected by sux and nondepolarizers ?

A

Sux - remain open longer so have an increased in Potassium

Nondepolarizers - Need an increase dosage

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32
Q

Is there fade with Succ? When do you see fade?

A

No unless high dose or continuous IV infusion

7-10mg/kg

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33
Q

What TOF ratio correlates with full recovery from a NMB?

A

> 0.9 at the adductor pollicis

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34
Q

Best location to measure the onset and recovery for NMB?

A

Onset - Orbicularis Oculi

Recovery - Adductor pollicis

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35
Q

What is the best test to assess recovery from NMB?

A

Tongue blade. Max 50% of receptors are occupied

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36
Q

What other tests are used to assess NMB recovery?

A

No fade (60% of receptors)

Sustained head lift and hand grip (50% of receptors)

Tidal volume >5mL/kg (80)

Vital Capacity>20mL (70)

Ins force better than negative 40 (50)

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37
Q

How does succ affect HR, IOP, Renal failure, intragastric pressure?

A

Tachy and Bradycardia

Increase IOP

Okay to give in renal failure if K is normal, however caution with elevated K

Increases intragastric but is canceled out by esophageal sphincter tone

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38
Q

What are the three variants of pseudocholinesterase ?

A

Homo (Dibucaine of 80) 8 min duration of succ

Hetero (Dibucaine of 50) 25 min duration of succ

Atypical Homo (dibucaine of 25) 5 hour duration of succ

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39
Q

What is the treatment for hyperkalemia cardic arrest ?

A

Calcium to raise the Threshold Potential

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40
Q

How is hyperkalemia treated when from Succ?

A

Calcium

Hyperventilation, glucose and insulin, sodium bicarb, albuterol

Diuretics, dialysis, volume

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41
Q

Who is at the highest risk for myalgia?

A

Young adults, women more than men, those who do not exercise

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42
Q

How can myalgia be reduced?

A

HIGH dose of succ
Lidocaine
NSAIDS

NOT opioids

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43
Q

What populations are at increased risk with succ?

A

Charcot - Marie - Tooth
Hyperkalemic paralysis
Duchenne’s
Guillain Barre
Upregulation of extra junctional
Amyotrophic lateral sclerosis
MS

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44
Q

Rank the NMB smallest to largest ED95 ( dose which there is a 95% decrease in twitch height )

A

Cis
Vec
Miv and Panc
Atra
Roc

Need 3x for intubating dose

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45
Q

What NBM are metabolized through Hoffman?

A

-Atracurium 33% (66% by non specific plasma esterase (different that Pseudo))

-Cisatracurium 100%

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46
Q

Which NMB is metabolized by pseudocholinesterase? what other paralytic is ?

A

Mivacurium and Succ

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47
Q

What does Hoffman rely on ? how does it change the reaction?

A

Normal blood pH

Faster with alkalosis and hyperthermia

Slower with acidosis and hypothermia

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48
Q

What is the active metabolite of cis and atracurium ?

A

Laudanosine - CNS stimulant

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49
Q

How is roc metabolized and eliminated? Any metabolite?

A

No metabolite

70% through liver

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50
Q

How is vec metabolized and eliminated? Any metabolite?

A

Liver

50% Liver and 50% kidney

3-OH vec

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51
Q

How is panc metabolized and eliminated? Any metabolite?

A

Liver

15% Liver and 85% kidney

3-OH panc

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52
Q

What drugs potentiate (increase the effect) NMB

A

Antibiotics, antidysrhythmics, locals, diuretics, dantrolene, cyclosporine

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53
Q

How do electrolytes potentiate NMB?

A

Increased Lithium and Mag

Decreased Ca and K

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54
Q

Which NMB have a histamine release

A

Succ, atra, mivacurium

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55
Q

What NMB can block the heart?

A

Panc and a little roc

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56
Q

What NMB has a vagolytic effect?

A

Panc - Increases HR while no effect on SVR

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57
Q

What NMB should be avoided with hypertrophic cardiomyopathy

A

Panc
Atra
Miva

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58
Q

What NMB is most likely to cause anaphylaxis?

A

Succ

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59
Q

3 examples ways to inhibit acetylcholinesterase ?

A

Competitive through electrostatic attachment - Edrophonium

Formation of carbamyl esters (competitive) - neostigmine, pyridostigmine

Phosphorylation - noncompetitive inhibition - organophosphates and echothiopate

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60
Q

How does renal failure affect the dosing of acetylcholinesterase?

A

Prolongs the duration

Also prolongs the duration of NMB

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61
Q

Is neostigmine faster or slower in children or adults?

A

Faster in children

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62
Q

What acetylcholinesterase inhibitor passes through the BBB.

A

Physostigmine

The rest do NOT

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63
Q

Common side effects of acetylcholinesterase inhibitors includes

A

DUMBBELLS - Increases parasympathetic nervous system

Diarrhea
Urination
Miosis
Bradycardia
Bronchoconstriction
Emesis
Lacrimation
Laxation
Salvation

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64
Q

Which anticholinergic does not pass through the BBB?

A

Glyco

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65
Q

When can atropine cause paradoxical bradycardia?

A

small IV dose.

<0.5 mg in adult

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66
Q

What are two ways AchE inhibitors increase Ach?

A

-Enzyme inhibition
-Presynaptic effects

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67
Q

What AchE inhibitor is mainly presynaptic ? What is it also used for ?

A

Edrophonium

Tensilon test, symptoms get better with MG and will get worse if in cholinergic crisis

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68
Q

Which AchE inhibitors inhibit pseudocholinesterase?

A

Neostigmine and pyridostigmine

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69
Q

How is edrophonium metabolized and eliminated? Neostigmine?

A

75% renal

50/50

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70
Q

Onset of AchE inhibitors is directly related to?

A

Depth of block

They also have an additive effect and more isn’t always better

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71
Q

Which AchE inhibitor passes the BBB?

A

Physostigmine because it goes through more physiologic membranes

72
Q

What can small doses of atropine cause? Why?

A

Paradoxical bradycardia through the blockage of M1 receptor on vagal nerve endings which normal reduce Ach

73
Q

Roc dosage for reintubation after 4mg/kg or less of roc in the last 4 hours? more than 4 hours?

A

5 min to 4 hours - 1.2mg/kg

4+ hours. 0.6mg/kg or vec 0.1mg/kg

74
Q

After an injection of an LA, it rapidly dissociates into a …

A

Uncharged base and an ionized conjugate acid

75
Q

What form of the LA binds to the LA binding site?

A

ionized conjugate acid

76
Q

What are the two common reasons for LA allergies ?

A

esters - Para aminobenzoic Acid

Amides - Methylparaben

77
Q

What is the primary variable contributing to LA onset of action? Secondary variables?

A

pKa

-Dose and concentration

78
Q

What is the primary variable contributing to LA potency? Secondary variables?

A

Lipid solubility

Intrinsic vasodilating effect

79
Q

What is the primary variable contributing to LA duration of action? Secondary variables?

A

Protein binding

Lipid solubility, intrinsic vasodilating effect, vasoconstrictors

80
Q

Lipid solubility of an LA is increased with?

A

Alkyl group substitution

81
Q

How does stereoselectivity play a role in LA?

A

Potency

82
Q

Which LA has the highest degree of protein binding?

A

Levo bupivacaine 98&
Bupivacaine 96%

82
Q

What determines the final plasma concentration of an LA?

A

TOTAL DOSE

not

concentration or speed of injection

83
Q

What else acts as a reservoir and limits plasma concentration of LAs?

A

Lungs which remove LA from circulation

84
Q

Which block does dexamethasone extend?

A

Brachial plexus

85
Q

How does hypercapnia affect LAST?

A

Increases the free fraction

Decreases protein binding

Increases cerebral blood flow

86
Q

How does metabolic acidosis affect LAST?

A

Favors Ion trapping and decreases the convulsion threshold

87
Q

How do LA effect the myocardium?

A

Depresses it by altering the calcium regulation

88
Q

How do LAs disrupt hemodynamics?

A

Alter the cardiac action potential, decrease automaticity, conduction velocity, AP duration, and vascular resistance

89
Q

How do LAs affect vascular smooth muscle?

A

Low doses causes constriction

Normal and higher doses produce vasodilation

90
Q

What determines the extent of cardiotoxicity?

A

Affinity for the receptor

Rate of dissociation from receptor

91
Q

With cocaine toxicity, what should be given?

A

Nitro

Best beta blocker choice would be a selective

92
Q

What can be given if seizure can not be broken?

A

Succ

but won’t stop seizures in the brain

Do NOT use propofol

93
Q

What is the max dose for lipid emulsion ? When should it be stopped?

A

Stopped ten minutes after hemodynamic stability

Max dose -10mL/kg in the first 30 min

94
Q

Most common cause of death with liposuction? What is contained in tumescent anesthesia?

A

PE

Lidocaine, epi, bicarb

95
Q

Max dosage for tumescent? When does it peak? When is it out?

A

50mg/kg

12 hours

36 hours

96
Q

How is methemoglobin formed? how is it diagnosed?

A

Iron becomes oxidized to ferric acid - fe3+

Co oximeter

97
Q

LAs that can cause methemoglobinemia?

A

Prilocaine
Benzocaine
Cetacaine
EMLA (prilocaine and lidocaine)

98
Q

What is prilocaine metabolized to?

A

o-toluidine which oxidizes Hgb to Mhgb

99
Q

Drugs that may prolong the duration of action of LAs?

A

epi, dexamethasone, dextran

100
Q

Drugs that provide supplemental analgesia with LAs?

A

Epi, Clonidine, and opioids

101
Q

Drugs that shorten onset time with LAs?

A

Sodium bicarb

102
Q

Drugs that improve diffusion through tissue with LAs?

A

Hyaluronidase - has allergic potential

103
Q

What LA reduces the effectiveness of analgesia opioids?

A

Chloroprocaine

104
Q

What are the two extra junctional receptors? What depolarizes them?

A

Gamma subunit - succ

7 alpha subunits - stimulated by succ and choline

105
Q

When and how long should succ be avoided?

A

24 hours after the injury and for one year

EXCEPT BURNS - several years

106
Q

What happens when presynaptic Nn receptors are stimulated by acetylcholine?

A

More Ach is mobilized inside the presynaptic nerve

107
Q

What does succ do to prejunctional receptors ?

A

Stimulates them like Ach

108
Q

In adults why does succ produce more tachycardia?

A

mimics Ach at the sympathetic ganglia

Succ causes brady in children

109
Q

What can be seen before MH caused from succ?

A

Masseter muscle spasms

Do not need to cancel if Trismus is seen, can open the mouth

110
Q

Where is pseudocholinesterase produced?

A

liver

NOT located in the CSF but everywhere else

111
Q

Max Percent of receptors occupied when tidal> 5ml/kg

A

80

112
Q

Max Percent of receptors occupied when head lift is greater than 5 seconds and hand grip is baseline?

A

50%

113
Q

Max Percent of receptors occupied when inspiratory force is better than NEGATIVE 40?

A

50%

114
Q

Why does Succ cause bradycardia?

A

Stimulation of M2 at the SA

Metabolite succinylmonocholine

115
Q

What drugs reduce pseudocholinesterase activity?

A

Reglan
Neostigmine
MAOI
Esmolol
Nitrogen mustard
Contraceptives
Cyclophosphamide
Echothiopate

116
Q

What conditions reduce pseudocholinesterase activity ?

A

Atypical PChE
Liver and kidney disease
Burns
Neoplasm
Late pregnancy
Organophosphate poisoning
Malnutrition
Advanced age

117
Q

What is treatment for atypical PChE?

A

Keep them on the vent

Whole blood, ffp, purified cholinesterase

118
Q

Most common skeletal muscle myopathy in children ? What happens?

A

Duchenne’s- absence of dystrophin protein

Causes hyperkalemic rhabdo NOT MH

119
Q

What is dystrophin

A

Structural component of cytoskeleton - helps anchor actin and myosin

120
Q

What lab values are elevated when the sarcolemma breaks down?

A

Creatine phosphokinase and myoglobin

121
Q

Dose of calcium to stabilize myocardium in the presence of hyperkalemia?

A

C chloride 20mg/kg (contains more Ca)

C gluconate 60mg/kg

122
Q

What shifts K into the cells?

A

Insulin/Glucose
Albuterol
Calcium
Hyperventilation
Bicarb

123
Q

Dose of glucose to drive potassium into the cells? How much insulin?

A

0.5g/kg 10% solution

1 unit per 5g of glucose

124
Q

How much bicarb to drive K into the cells?

A

1-2mmol/kg

125
Q

When using a defasciculating dose of a Non depolarizer, how do you adjust the dose of succ?

A

Give more
1.5-2mg/kg

126
Q

What disease is resistant to succ?

A

myasthenia gravis

127
Q

List the NMB potency from least to most

A

Cis
Vec
Miv
Pan
Atra
Succ
Roc

128
Q

How is mivacurium metabolized? Metabolite?

A

pseudocholinesterase

NO metabolite

129
Q

What drugs potentiate NMB?

A

Volatiles
Antibiotics
Antidysrhythmic
Locals
Lasix
Dantrolene

130
Q

What volatile potentiates NMBs the most?

A

Des
Sevo
Iso
N20
Propofol

131
Q

What test would show an allergic reaction to NMB?

A

Elevated tryptase peaking at 120 minutes after exposure

132
Q

How is pain inhibited?

A
  1. Spinal neurons release GABA and glycine
  2. Descending pathway release norepi, 5HT, and endorphins
133
Q

How is pain augmented?

A

Central sensitization

Wind up

134
Q

What type of receptors are opioid receptors?

A

G protein

turns off adenylate cyclase and decreases cAMP

Ca conductance in decrease (reduces neurotransmitter release)

K conductance is increased (hyperpolarizes the RMP)

135
Q

Where are opioid receptors in the brain?

A

Periaqueductal gray, locus coeruleus, and rostral ventral medulla

136
Q

What opioid receptors are responsible for pruritus?

A

Mu and Delta

137
Q

What opioid receptor is responsible for immune supression

A

Mu - subtype 3

138
Q

What opioid receptor is responsible for dependence and spinal analgesia and constipation ?

A

Mu 2

Cant go number 2

139
Q

How do opioids affect the Co2 response curve?

A

Down and to the right

140
Q

How do opioids affect heart contractility?

A

Doesn’t unless combined with nitrous

141
Q

What causes the pupil to constrict with opioids?

A

Edinger Westphal
Cilia ganglion of oculomotor nerve

142
Q

Where is the CTZ?

A

Area postrema of medulla

143
Q

Which opioid causes the lowest increase in biliary pressure?

A

meperidine

144
Q

What are tolerance and physical dependence most likely due to ?

A

Desensitization and increased cAMP

NOT enzyme induction

145
Q

What are early signs of withdrawal ? late?

A

Early- diaphoresis, insomnia, restlessness

Late - abd cramping and N/V

146
Q

Withdrawal times of fentanyl and meperidine ?

A

onset 2- hours
peak 6 -12 hours
last 4-5 days

147
Q

Withdrawal times of morphine and heroin?

A

onset 6-18 hours
Peak at 36-72 hours
Last 7-10 days

148
Q

Which opioid has the greatest rostral spread when given intrathecal ?

A

Morphine

149
Q

Which opioids have metabolites? What is the active form ?

A

Morphine and meperidine

m6G

150
Q

Does m6G cross the BBB? S/S?

A

NO
Drowsiness, respiratory depression, N/V

151
Q

Which opioid should not be given in a epidural or intrathecal?

A

Remi - contains glycine and free base

152
Q

What can prevent hyperalgesia from remi?

A

Mag and Ketamine

153
Q

When should meperidine be avoided?

A

Elderly, PCA, Dialysis , MAOI

154
Q

What opioid acts like atropine?

A

Meperidine

155
Q

Which opioids stimulate kappa?

A

Meperidine

156
Q

Opioid with the largest Vd? Smallest?

A

Largest fentanyl
Smallest remi

157
Q

pka of opioids?

A

Alf - 6.5
Remi - 7.2
Morphine 7.9
Su - 8
Fent - 8.4
Meperidine - 8.5

158
Q

Opioids with the highest protein binding ? Lowest?

A

Remi and Su at 93%

Morphine at 35%

159
Q

Which opioid is sensitive to a low extraction ratio? Also may by inhibited erythromycin

A

Alf

160
Q

Racemic mixtures of opioids?

A

Methadone

161
Q

How does methadone reduce pain? What is the oral bioavailability?

A

MU
NMDA
MAOI

80%

162
Q

Facts about methadone

A

Good for chronic pain and abuse
Can increase QT
Inhibits K
No metabolite
3-6 hours

163
Q

What causes muscle rigidity with opioids?

A

Rapid administration

ALL the fentanil’s

164
Q

Complications from opioid induced muscle rigidity?

A

Increased thoracic pressure -
Increased CVP, PAP,PVR

Increased O2

Decreased ventilation, and mixed venous O2

165
Q

Opioid agonist - antagonist FACTS

A

Provides analgesia with reduced risk of resp depression

Ceiling effect
Decreases other opioids

Can cause acute opioid withdrawal

Lower risk of dependence

166
Q

Facts of buprenorphine

A

Partial Mu

HARD to reverse

Long duration

Can use patch

167
Q

Facts of nalbuphine

A

Kappa agonist and Mu antagonist

Revered with Narcan

Does not affect cardiac so good in heart disease

168
Q

Facts of butorphanol

A

Kappa agonist and weak Mu antagonist

Revered by Narcan

Good for post op shivering

169
Q

Which two agonist provide greater pain relief compared to morphine?

A

B’s

170
Q

Facts about Narcan

A

Short acting 30-40 minutes

Can causes Pulmonary edema from SNS activation

N/V

All opioid receptors

FIRST PASS LIVER

171
Q

Can Narcan cross the placenta?

A

Yes careful - can send baby into withdrawal

172
Q

Methylnaltrexone Facts?

A

Does not cross BBB (quaternary amine)

DOES NOT REVERSE RESP DEPRESSION

good for other effects

173
Q

Nalmefene facts

A

Long acting, good for abusers

174
Q

Naltrexone

A

Good for withdrawal and abusers

Local + Opioids (3 decks)

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