Pharm: Anesthetics Flashcards

1
Q

inhalation anesthetics

A

make patient unconscious

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2
Q

IV anesthetics

A

make patient unconscious
highly lipid soluble: need pH adjustment or surfactant (can lead to toxicity)
INSTANTANEOUS compared to inhaled
rate limiting step of elimination: release from adipose
LONG T1/2, SHORT duration of action due to redistribution

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3
Q

nitrous oxide

A
gas
inhalation anesthetic
potentiate 2 pore K channel
inhibit NMDA, nicotinic ACh, serotonin, kainate
RAPID onset
maintains protective reflexes (resp. and CV)
can us less volatile agent
PAIN RELIEF 
teratogen in animals
inhibits vit. B12 synthetase
2ND GAS EFFECT, DIFFUSIONAL HYPOXIA, INCREASE PRESSURE
AE: N/V (important in anesthesia)
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4
Q

volatile liquids

A
-urane
inhalation anesthetic
potentiate GABA(A)
explosive: add FLUORINE (can cause renal damage)
NO pain relief
LOSS of REFLEXES
AE: MALIGNANT HYPERTHERMIA
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5
Q

halothane

A
volatile liquid
SLOW onset and recovery
most POTENT
hepatic metabolism
AE: ARRHYTHMIA, HEPATIC
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6
Q

enflurane

A

volatile liquid
MUSCLE RELAXATION
AE: SMELL, SEIZURE

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7
Q

isoflurane

A

volatile liquid
potentiate 2 pore K channel, glycine, serotonin, kainate
inhibit inward rectifying K channel, AMPA
MUSCLE RELAXATION
AE: SMELL

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8
Q

desflurane

A
volatile liquid
inhibit: NMDA, voltage gated K channel, kainate
most RAPID onset and recovery
least potent
AE: SMELL
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9
Q

sevoflurane

A

volatile liquid
potentiate: glycine
inhibit: NMDA, serotonin, AMPA
RAPID onset and recovery

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10
Q

thiopental

A

IV anesthetic: induction agent
barbiturate
CYP induction
AE: PORPHYRIA

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11
Q

propofol

A

IV anesthetic: induction agent
potentiate GABA(A) and glycine
minor NMDA inhibition: blocks glutamate from binding receptor
high concentration: acts like GABA
ANTIEMETIC
AE: INFUSION SYNDROME, CV/ organ failure when used for long time

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12
Q

etomidate

A
IV anesthetic: induction agent
potentiate GABA(A) and 2 pore K channel
NO CV effects
AE: inhibit STEROIDS
do NOT use in ICU
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13
Q

ketamine

A

IV anesthetic, IM
inhibit NMDA: PHYSICALLY occludes channel
inhibit muscarinic ACh
increase: cerebral blood flow, ICP, CV (HR, MAP, CO)
NO effects on respiratory rate
other: ANALGESIC, intact PHARYNGEAL/ LARYNGEAL REFLEX, BRONCHODILATOR
AE: emergence HALLUCINATION, EYES OPEN when unconscious (dissociative)

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14
Q

diazepam

A

IV anesthetic
benzodiazepine
perioperative drug: sedation
LONG duration

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15
Q

lorazepam

A

IV anesthetic
benzodiazepine
perioperative drug: sedation

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16
Q

midazolam

A

IV anesthetic
benzodiazepine
SHORT duration

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17
Q

morphine

A
IV anesthetic
opioid
LONG LASTING
SLOW onset
peri-operative analgesia
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18
Q

meperidine

A

IV anesthetic

opioid

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19
Q

fentanyl

A
IV anesthetic
peri-operative analgesia and RSI
neruolept-analgesia agent
opioid
FAST ONSET
SHORT acting
decrease sympathetic response during intubation
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20
Q

remifentanil

A

IV anesthetic
opioid
ULTRA SHORT ACTING
no accumulation: RAPID LOSS OF ANALGESIA

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21
Q

benzodiazepine

A

potentiate GABA(A): allosteric change (shift dose response and increase POTENCY)
CEILING EFFECT: safe
ANTICONVULSANT, AMNESIA, ANXIOLYTIC
minimal CV and respiratory depression
longer onset compared to other IV anesthetics
NO ANALGESIA

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22
Q

barbiturates

A

potentiate GABA(A): PROLONG binding (increase EFFICACY)
high concentrations: open GABA channel in absence of GABA: COMA, DEATH
inhibit muscarinic ACh, AMPA, kainate
CYP inducer

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23
Q

opioid: reasons for/against use

A

For

  1. no effect on heart
  2. decrease airway reflex: intubation
  3. pain relief
  4. no malignant hyperthermia
  5. maintain regional blood flow

Against

  1. incomplete amnesia
  2. histamine reaction
  3. increase blood req.
  4. respiratory depression
  5. CV instability
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24
Q

opioid

A

OP1-3 receptors in spinal cord and CNS
AE: bradycardia, hypotension,, HTN, RESPIRATORY DEPRESSION, loss of response to PaCO2, WOODEN CHEST, increase CBF and ICP; CONSTIPATION, MIOSIS, N/V

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25
Q

amide type local anesthetic

A

prefix contains i
injection or infiltration
metabolized in liver

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26
Q

ester type local anesthetic

A

NO i in prefix
injection or infiltration
metabolized in any tissue by esterases: SHORTER DURATION
genomic changes in enzyme effect accumulation

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27
Q

topical only anesthetics

A

poor aqueous solubility and/or undesirable toxicity

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28
Q

EMLA (eutectic mixture of local anesthetics) cream

A

lidocaine and prilocaine

apple to skin with occlusive dressing before painful procedure

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29
Q

LET (lidocaine-epinephrine-tetracaine)

A

use in pediatric ED
liquid application to lacerations req. stitches
analgesia and vasoconstriction

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30
Q

vasoconstrictors: use with local anesthetics

A
  1. improve intensity of local anesthetic

2. increase duration of blockade

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31
Q

local anesthetics

A

-caine
bind INNER surface of voltage gated Na channel and inhibit AP in active or inactive state (does not bind in resting state)
act on nerve AXON
unconsciousness ONLY with incorrect administration
lipophilicity: benzene ring
AE: allergy (give other type of local anesthetic); allergy to preservative (sulphites)

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32
Q

lidocaine

A

amide type local anesthetic
peri-operative RSI
RAPID ONSET
decrease ICP and bronchospasm in intubation

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33
Q

mepivacaine

A

amide type local anesthetic
LEAST POTENT
SLOW ONSET

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34
Q

prilocaine

A

amide type local anesthetic
RAPID ONSET
AE: METHEMOGLOBINEMIA

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35
Q

bupivacaine

A
amide type local anesthetic
POTENT
LONG ACTING
SLOW ONSET
AE: CARDIOTOXIC if systemized
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36
Q

ropivacaine

A
amide type local anesthetic
POTENT
LONG ACTING
SLOW ONSET
reduced cardiotoxicity (reason produced)
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37
Q

articaine

A
amide type local anesthetic
ester link cleavage: inactivation
lipophilicity: thiophene ring
RAPID ONSET
BONE PENETRATION: dental block
AE: PARESTHESIA
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38
Q

procaine

A

ester type local anesthetic
LEAST POTENT
SHORT ACTING, SLOW ONSET

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39
Q

chloroprocaine

A

ester type local anesthetic

SHORT ACTING, FAST ONSET

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40
Q

tetracaine

A

ester type local anesthetic
POTENT
LONG ACTING
SLOW ONSET

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41
Q

cocaine

A

ester type local anesthetic

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42
Q

benzocaine

A

topical only local anesthetic: mucous membranes and skin

AE: METHEMOGLOBINEMIA

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43
Q

dyclonine

A

topical only local anesthetic: mucous membranes and skin

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44
Q

dibucaine

A

topical only local anesthetic: SKIN ONLY

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45
Q

pramoxine

A

topical only local anesthetic: SKIN ONLY

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46
Q

epinephrine

A

vasoconstrictor
peri-operative anaphylaxis
DI: B blocker, TCA, halothane, HTN, heart block, cerebral vascular insufficiency
CI: close angle glaucoma, HF, CAD, HTN, arrhythmia, cerebrovascular disorder, DM, hyperthyroid

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47
Q

phenylephrine

A

vasoconstrictor

peri-operative CV support for hypotension

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48
Q

oxymetazoline

A

vasoconstrictor

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49
Q

phentolamine

A

alpha adrenergic blocker
reversal agent for local anesthetics
increases blood flow to anesthetized area

50
Q

perioperative drugs: sedation and reduced anxiety

A

benzodiazepine
phenothiazines
antihistamine

51
Q

preoperative drugs: analgesia

A

opioids

NSAID

52
Q

preoperative drugs: antimicrobial

A

aimed at most likely agents

cefazolin, cefotetan, cefoxitin, vancomycin

53
Q

preoperative drugs: RSI

A

intubation

  1. lidocaine: decrease ICP and bronchospasm
  2. fentanyl: decrease sympathetic response
  3. atropine: mitigate bradycardia response of SCh
  4. vecuronium: mitigates ICP response of SCh
  5. succinylcholine: NMB
  6. sedative
54
Q

preoperative drugs: anaphylaxis

A

stop drug, give O2 and epinephrine, volume expansion

prophylaxis: cimetidine, diphenhydramine
other: aminophylline, steroids, Na bicarbonate

55
Q

preoperative drugs: aspiration pneumonitis

A
H2 blocker
antacids
Bicitra, Polycitra
metoclopramide
water: facilitates emptying
56
Q

preoperative drugs: N/V

A

antihistamines
phenothiazines
also drugs that act on: DA, muscarinic and opiate receptors

57
Q

preoperative drugs: anticholinergic

A

reduce secretions, mitigate reflex bradycardia
antihistamines
phenothiazines
atropine, scopolamine, glycopyrrolate

58
Q

preoperative drugs: CV support

A

for hypotension: DA, phenylephrine, ephedrine

HTN: nitroprusside, trimethaphan

59
Q

promethazine

A
preoperative sedation
phenothiazine
sedative, antiemetic
inhibit: DA, ACh, Histamine
AE: lowers threshold for seizures
60
Q

hydroxyzine

A

preoperative sedation
phenothiazine
sedative, anti-emetic
inhibit: DA, ACh, Histamine

61
Q

diphenhydramine

A

preoperative sedation
antihistamine, anticholinergic, anti-emetic
bronchodilator, analgesic
Tx: allergic rxn to local anesthetics

62
Q

codeine

A

peri-operative analgesia

opioid

63
Q

ketorolac

A

peri-operative analgesia
NSAID: PG inhibition (COX inhibition)
AE: bleeding, reduced fracture healing

64
Q

ibuprofen

A

peri-operative analgesia
NSAID: PG inhibition (COX inhibition)
AE: bleeding, reduced fracture healing

65
Q

cefazolin

A

peri-operative antimicrobial

effective against: staph, strep

66
Q

cefotetan

A

peri-operative antimicrobial

effective agains: bowel anaerobes

67
Q

cefoxitin

A

peri-operative antimicrobial

effective agains: bowel anaerobes

68
Q

vancomycin

A

peri-operative antimicrobial
use: MRSA
do NOT use routinely

69
Q

veuronium

A

peri-operative RSI

mitigates ICP response of SCh during intubation

70
Q

atropine

A

peri-operative RSI and anticholinergic
most potent vagolytic
mitigate bradycardia response of SCh in intubation

71
Q

aminophylline

A

peri-operative anaphylaxis

72
Q

hydrocortisone

A

peri-operative anaphylaxis

73
Q

methylprednisolone

A

peri-operative anaphylaxis

74
Q

cimetidine

A

peri-operative aspiration pneumonitis

H2 blocker

75
Q

ranitidine

A

peri-operative aspiration pneumonitis

H2 blocker

76
Q

bicitra

A

peri-operative aspiration pneumonitis

antacid

77
Q

polycitra

A

peri-operative aspiration pneumonitis

antacid

78
Q

metoclopramide

A

peri-operative aspiration pneumonitis and N/V
gastrokinetic agent: accelerates gastric emptying
AE: sedation, lower seizure threshold, potentiation of EXTRA-PYRAMIDAL effects
antagonized by: anticholinergics, narcotics (reduces usefulness)

79
Q

ondansetron

A

peri-operative N/V

80
Q

scopolamine

A

peri-operative N/V and anticholinergic

most potent at sedation and amnesia

81
Q

glycopyrrolate

A

peri-operative anticholinergic

most potent at decreasing secretions

82
Q

dopamine

A

peri-operative CV support for hypotension

B effect and renal preservation

83
Q

nitroprusside

A

peri-operative CV support for hypertension

vasodilator

84
Q

trimethaphan

A

peri-operative CV support for HTN

ganglionic blocker

85
Q

anxiolysis

A

decrease apprehension

86
Q

conscious sedation

A

protective reflexes maintained
independent maintenance of airway
response to physical/ verbal stimulation

87
Q

deep or unconscious sedation

A

profound effect with loss of 1 or more of the following: protective relaxes, independent airway maintenance, or response to physical/ verbal stimulation

does NOT mean they are unconsciousness
transition into unconsciousness with additional drug application

88
Q

general anesthesia

A

sensory, mental, reflex, motor blockade

loss of ALL protective reflexes

89
Q

general anesthesia

A

IV or inhalation: most control

req. mechanical airway

90
Q

Meyer-Overton Hypothesis

A

potency of anesthesia is proportional to lipid solubility

larger oil gas partition coefficient: more lipid soluble

91
Q

minimum alveolar concentration (MAC)

A

concentrate non inspired gas required to render half of patients unconsciousness

lower MAC: more potent

92
Q

Patient stages of inhalation anesthetic administration: BP, muscle tone, respiration, pupils

  1. initial (due to?)
  2. after unconsciousness
A
  1. increased BP and muscle tone, pupil dilation, exaggerated respiration (removal of inhibitory neural pathways)
  2. decreased respiratory function, CV function (decrease BP), loss of protective reflexes and muscle tone, pupil dilation
93
Q

What generally precedes loss of pain in anesthesia?

What is important to do when giving anesthesia related to this?

A

memory loss and perception loss (autonomics go after pain)

give ANALGESICS

94
Q

2nd gas effect

A

NITROUS OXIDE

causes 2nd gas to accumulate more quickly than it does on its own

95
Q

diffusional hypoxia

A

NITROUS OXIDE
turn off anesthetic and large amount exits in exhale
must apply OXYGEN MASK

96
Q

NMDA receptor

A

for stimulatory glutamate system

97
Q
Effects of induction IV anesthetics 
(thiopental, etomidate, ketamine, propofol)
1. CBF and ICP
2. respiratory function
3. CV
A
  1. depress cerebral blood flow and ICP (exception: ketamine)
  2. inhibitory (exception: ketamine)

CV

  1. thiopental, propofol: increase HR, decrease CO and MAP
  2. etomidate: no effects
  3. ketamine: cardio stimulatory
98
Q

flumazenil

A

benzodiazepine antagonist

99
Q

neurolept-analgesia

A

pain relief and state of indifference (decrease anxiety)
can respond to command

add nitrous oxide to induce anesthesia

100
Q

droperidol

A

neurolept-analgesia

state of indifference, anti-emetic, anti-convulsant

101
Q

atropine + morphine or meperidine

A

neurolept-analgesia

prep for surgery: dry secretions and analgesia

102
Q

malignant hyperthermia

A

MoA: intracellular Ca release for SR
HEAT, RIGIDITY, TACHYCARDIA/PNEA, ACIDOSIS, unexpected CARDIAC ARREST, increase end tidal CO2
SUCCINYLCHOLINE, VOLATILE anesthetics
genetic predisposition: RYANODINE receptor (RYR1)
Tx: DANTROLENE

103
Q

dantrolene

A

repackages Ca into SR
Tx: malignant hyperthermia
CI: Ca channel blocker

104
Q

ideal local anesthetic

A

lipophilic (pass membrane) and hydrophilic

short onset, reversible, low toxicity

105
Q

Order of sensitivity of nerves to nerve block

A

most: small myelinated and non-myelinated nerves
least: large myelinated

spontaneously active nerves: local anesthetics more effective

106
Q

local anesthetics: ionized vs nonionized

  1. pH of environment = pKa of drug
  2. pH is 1 > pKa
  3. pH is 2 > pKa
  4. pH is 1
A
  1. 50% of drug is nonionized
  2. 90% of drug is nonionized
  3. 99% of drug is nonionized
  4. 90% of drug is ionized
  5. 99% of drug is ionized

nonionized: can cross membrane
charged: can bind channel

inflammation: more acidic environment leads to inability of drug to cross membrane because it is ionized

107
Q

Direction of nerve block and recovery

A

proximal to distal

108
Q
  1. signs of systemic toxicity with local anesthetics

2. AE of toxicity

A
  1. ringing in ears, metallic taste, numb lip and tongue

2. CV depression, respiratory arrest, convulsions

109
Q

How many mg/mL

  1. 1% solution
  2. 2% solution
  3. 5% solution
  4. 5.5% solution
A

members mean 1g/ 100mL

(% solution x 1000mg) / 100mL

OR

add a zero to the % number

  1. 1000mg/ 100mL: 10mg/mL
  2. 2000mg/100mL: 20mg/mL
  3. 5000mg/100mL: 50mg/mL
  4. 5500mg/100mL: 55mg/mL
110
Q

How many mg/mL

  1. 1: 1,000
  2. 1: 10,000
  3. 1: 100,000
  4. 1: 200,000
A

numbers mean 1g/ (x)mL

(first number x 1,000mg) / (second number x 1mL)

  1. 1000mg/1000mL: 1mg/mL
  2. 1000mg/10,000mL: 0.1mg/mL
  3. 1000mg/100,000mL: 0.01mg/mL
  4. 1000mg/200,000mL: 0.005mg/mL
111
Q

What determines

  1. potency
  2. time of onset
  3. duration of action
  4. metabolism
A
  1. lipid solubility: increased means more potent
  2. dissociation constant/ pKa: low pKa hastens onset
  3. protein binding (increased affinity increases time bound to Na channel)
  4. amide vs. ester linkage
112
Q

methemoglobinemia

A

oxidized Fe causes reduced O2 carrying capacity
PRILOCAINE, BENZOCAINE
Sx: BLUE skin, SOB, lack of energy, headache
Tx: methylene blue or ascorbic acid

113
Q

lidocaine-oxymetazoline

A

reduce vascular engorgement and provide analgesia

use by otolaryngologist to aid in visualization of engorged nasal passage

114
Q

epidural/spinal anesthesia

A

block is on fibers exiting cord (not the cord itself)

distribution depends on baricity (density compared to CSF) and patient orientation
increase temperature: increase spread

115
Q

spinal anesthesia of

  1. isobaric solution
  2. hyperbaric solution
  3. hypobaric solution
A
  1. stays at level of injection
  2. travels down with gravity
  3. travels against gravity
    depends on patient position
116
Q

What should you keep in mind about injection technique of local anesthetics?

A

neutralize with Na Bicarb immediately before use to preserve drug stability

local anesthetics are acidic causing stinging so add base

117
Q

What drugs can be given in intubation?

A
  1. lidocaine: decrease ICP and bronchospasm
  2. fentanyl: decrease sympathetic response
  3. atropine: mitigate bradycardia response of SCh
  4. vecuronium: mitigates ICP response of SCh
  5. succinylcholine: NMB
  6. sedative
118
Q

ephedrine

A

peri-operative for CV support for hypotension

119
Q

What do you give to someone that won’t wake up from Sx?

A

reversal of most likely agent
1. narcotic of benzodiazepine antagonist
2. physostigmine to reverse Ach effects
other reasons: lidocaine, old age, NM agents (only if severe respiratory depression is this suspected)

120
Q

signs of anaphylaxis

A

respiratory: cyanosis, wheeze
CV: arrest, tachycardia
cutaneous: flushing, edema, urticaria