autonomics and cholergenics Flashcards

1
Q

NS divisions

A
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2
Q

ANS

A
  • INVOLUNTARY
  • SYMPATHETIC (SANS) ANDPARASYMPATHETIC (PANS)
  • HANDLES VISCERAL FUNCTIONS
  • 2 NEURONS IN SERIES
  • PRE- AND POST-GANGLIONIC
  • ALL PREGANGLIONIC FIBERS RELEASE ACH
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3
Q

SYMPATHETIC (SANS)

A
  • FIGHT OR FLIGHT
  • RUNS ON NOREPINEPHRINE
  • INCREASES CO, BP, RR, BLOOD FLOW, BG
  • DECREASES RBF, DIGESTIVE PROCESSES
  • FIRES AT ONCE
  • SHORT PRE-, LONG POST
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4
Q

PARASYMPATHETIC (PANS)

A
  • NORMAL MAINTENANCE AND ANABOLIC METABOLISM
  • INCREMENTAL ACTIVATION
  • VAGAL STIMULATION
  • LONG PRE-, SHORT POST
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5
Q

SOMATIC NERVOUS SYSTEM

A
  • VOLUNTARY
  • CONTROLS MOVEMENT, RESPIRATION, POSTURE
  • ALWAYS EXCITATORY
  • NO GANGLIA
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6
Q

CHOLINERGIC FIBERS

A
  • SYNTHESIZE AND RELEASE ACH
  • ALL PREGANGLIONIC EFFERENT AND SOMATIC MOTOR FIBERS TO SKELETAL MUSCLE
  • MOST PARASYMPATHETIC POSTGANGLIONIC FIBERS
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7
Q

ADRENERGIC FIBERS

A
  • RELEASE NOREPINEPHRINE
  • MOST SYMPATHETIC POSTGANGLIONIC FIBERS
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8
Q

somatic NS fiber diagram

A
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9
Q

SNS fiber diagram

A
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10
Q

SNS function at adrenal medulla diagram

A
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11
Q

parasym nn diagram

A
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12
Q

CHOLINERGIC
TRANSMISSION mechanism

A
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13
Q

andregenic transmission mechanism

A

same as cholergenic except Tyr converted to Dopamine then to NE
NE stored and released via Ca
NO NE BREAKDOWN in synapse (NET reuptake)

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14
Q

AUTONOMIC RECEPTORS classes

A
  • CHOLINERGIC RECEPTORS:
    NICOTINIC (GANGLIONIC)
    MUSCARINIC
  • ADRENERGIC RECEPTORS:
    ALPHA
    BETA
    DOPAMINE
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15
Q

NICOTINIC RECEPTORS
classes?
excitatory or inhibitory?

A
  • 3 MAIN CLASSES:
    1. MUSCLE
    2. GANGLIONIC
    3. CNS
  • EXCITATORY: Ach binds for Na influx
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16
Q

MUSCARINIC RECEPTORS classes

A

M1-5

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17
Q

M1

A
  • M1 – NEURAL; CNS EXCITATION, GASTRIC SECRETION
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18
Q

M2

A

M2 – ATRIAL; CARDIAC AND NEURAL
INHIBITION
decreases HR and CO

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19
Q

M3

A
  • M3 – GLANDULAR/SMOOTH MUSCLE; GASTRIC ACID, SALIVARY SECRETION, GI CONTRACTION, OCULAR ACCOMMODATION, VASODILATION
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20
Q

ADRENERGIC RECEPTORS

where/types?

A
  • POST-GANGLIONIC SYMPATHETIC SYSTEM ONLY
  • Α1, Α2
  • Β1, Β2, Β3
  • DOPAMINE
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21
Q

CHOLINERGIC DRUGS

types?

A

muscarinic agonists
* PARASYMPATHOMIMETIC

  • DIRECT ACTING: BINDS DIRECTLY TO NACH(OS) AND MACH(OS)
  • INDIRECT ACTING: INHIBITS ACETYLCHOLINESTERASE, AMPLIFIERS OF ENDOGENOUS ACH
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22
Q

DIRECT ACTING CHOLINERGICS names

A
  • PILOCARPINE
  • BETHANECHOL
  • CEVIMILINE
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23
Q
  • PILOCARPINE (SALAGEN®)
    tx of what usually? how does it help this?
    dental use?
A
  • GLAUCOMA TX
  • CAUSES MIOSIS, LOWERS IOP
  • DENTAL USE – RADIATION-INDUCED XEROSTOMIA TX
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24
Q
  • BETHANECHOL (URECHOLINE®)
    tx of?
    most resistant of?
A
  • POST-OPERATIVE URINARY RETENTION TX
  • MOST RESISTANT TO CHOLINESTERASE
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25
Q
  • CEVIMILINE (EVOXAC®)
    selective for?
    tx of?
A
  • SELECTIVE FOR M3
  • MORE SELECTIVE FOR EXOCRINE GLANDS
  • RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
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26
Q

INDIRECT ACTING CHOLINERGICS

types?

A
  • ACETYLCHOLINESTERASE INHIBITORS
  • REVERSIBLE: ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®), GALANTAMINE (RAZADYNE®)
  • IRREVERSIBLE: ORGANOPHOSHPATES
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27
Q

INDIRECT ACTING CHOLINERGICS
* USED FOR TREATMENT OF:

A
  • MYASTHENIA GRAVIS
  • GLAUCOMA
  • GI MOTILITY
  • REVERSAL OF NEUROMUSCULAR BLOCKADE
  • ANTICHOLINERGIC TOXICITY
  • ALZHEIMER
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28
Q

REVERSIBLE ACHE INHIBITORS names

A
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29
Q

Pyridostigmine (Regonol®)
indications?
1st line for?
duration?

A

indications:
*Myasthenia gravis
*Nerve agent prophylaxis
notes:
1st line for MG
4-6h duration

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30
Q

Neostigmine (Prostigmin®)
indications?
does not?

A

indications:
*Myasthenia gravis
*Post-op ileus / urinary retention
*Neuromuscular blockade reversal

Doesn’t enter CNS (quaternary amine)

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31
Q

Physostigmine (Antilirium®)
indication?
enters? why not routinely used?

A

*Anticholinergic toxicity
Enters CNS (tertiary amine): Not routinely used due to CNS activity, ADRs

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32
Q

Edrophonium (Tensilon®)
used for? why?

A

*Diagnosis of myasthenia gravis

Doesn’t enter CNS (quaternary amine)
Not routinely used for treatment, short t ½ (5 min)

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33
Q

Galantamine, rivastigmine, donepezil
indication?
why?

A

*Mild-to-moderate Alzheimer’s disease

More selective AChE for management of cognitive dysfunction.
Modest clinical benefits

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34
Q

ORGANOPHOSPHATES
bind?
Insecticides?
nerve agents?

A

Irreversible AChE
Long lasting
Insecticides: Parathion (more dangerous), malathion (safer)
Nerve agents: Sarin, soman, tabun, VX
Novichok Agents (binary, req mixture)

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35
Q

NORMAL PROCESS - ACHE

A

cleavage to inactivate Ach

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36
Q

ORGANOPHOSPHATE
MECHANISM

A

Phosphorous (+) attracted to serine (-)
OP attaches to AChE, prevents ACh binding= excess Ach

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37
Q

outcomes of AchE with OP

A

Cholinesterase is now blocked, 1 of 3 things can happen
1. Hydrolyze to original state (slow)
2. Regenerate with an oxime (fast)
3. Age (cannot regenerate)

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38
Q

aged bond of AchE

A
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39
Q

cholergenic toxicity signs progression

A

usually muscarinic signs followed by nicotinic

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40
Q

Muscarinic S/S of Chol toxicity

A

SLUDGE:
salivation
lacrimation
urination
Diarrhea
GI discomfort
Emesis

OR
DUMBBELLS :
Diarrhea
Urination
Miosis/muscles weak
Bronchorrhea
Bradycardia
Emesis
Lacrimation
Salivation/sweating

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41
Q

nicotinic S/S of toxicity

A

M T W T F
Muscle cramps
Tachycardia
Weakness
Twitching
Fasciculations

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42
Q

how much time do we have with these agents at play?

possible abbreviations

A
43
Q
  • PRALIDOXIME (2-PAM)
A
  • REGENERATES ACHE
    must use before bond ages to prevent AchE inhibitors from binding
44
Q
  • ATROPINE with Ach toxicity, issues with this?
A

REQUIRES HUGE AMOUNTS
* MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT NICOTINIC SX (PARALYSIS)

45
Q
  • PYRIDOSTIGMINE for Ach toxicity?
A
  • PROPHYLAXIS ONLY, when exposure possible, acts as a cholergenic agent but binds AchE to prevent binidng of others
46
Q

possible otpions for Ach toxicity tx

A
  • PRALIDOXIME (2-PAM)
  • ATROPINE
  • PYRIDOSTIGMINE
47
Q

ANTICHOLINERGICS/ MUSCARINIC
ANTAGONISTS

A
  • BINDS MUSCARINIC RECEPTORS, BLOCKS ACH
48
Q

classes of M antagonists and anticholergenics

dif of the classes

A
  • TERTIARY AMINES HAVE CENTRAL EFFECTS
  • QUATERNARY AMINES – PERIPHERAL EFFECTS
49
Q
  • TERTIARY AMINES anticholergenics
    names?
A
  • TERTIARY AMINES HAVE CENTRAL EFFECTS
  • ATROPINE, SCOPOLAMINE, BENZTROPINE , DICYCLOMINE
50
Q
  • QUATERNARY AMINES anticholergenics
A
  • QUATERNARY AMINES – PERIPHERAL EFFECTS
  • GLYCOPYRROLATE, TIOTROPIUM
51
Q

ATROPINE
* PROTOTYPICAL?
* SELECTIVITY?
* NO EFFECT in pts with hx of?
* INDICATIONS?
* DON’T USE what dose in adults. why?

A
  • PROTOTYPICAL ANTICHOLINERGIC
  • MUSCARINIC SELECTIVITY
  • NO EFFECT S/P HEART TRANSPLANT (vagal transection)
  • INDICATIONS:
  • BRADYCARDIA
  • OP TOXICITY – HUGE AMOUNTS NEEDED
  • DON’T USE < 0.5MG IN ADULTS= PARADOXICAL BRADYCARDIA
52
Q

atropine mechanism

A

binds M2 to prevent Ach binding
increased HR with no effect on sympathetics or BP, improves AV conduction

53
Q

SCOPOLAMINE
* FOUND IN?
* AMINE?
* PRIMARY USE?
results of use?

A
  • FOUND IN HYOSCYAMUS NIGER (HENBANE)
  • TERTIARY AMINE
    can be used to prevent short term mem formation/ increase suggestability
  • PRIMARY USE:
  • MOTION SICKNESS
  • VOODOO ZOMBIFICATION
54
Q

GLYCOPYRROLATE
* AMINE structure?
* USED TO?
* ADJUNCT FOR REVERSAL OF?

A

anticholergenic
* QUATERNARY AMINE, FEWER CENTRAL EFFECTS

  • USED TO DRY SECRETIONS:
  • SURGERY
  • KETAMINE TREATMENT
  • ADJUNCT FOR REVERSAL OF NEUROMUSCULAR BLOCKERS
55
Q

ANTICHOLINERGIC USES
* OPHTHALMOLOGY

A
  • INDUCE MYDRIASIS, INDUCE CYCLOPLEGIA, REDUCE IOP
56
Q

ANTICHOLINERGIC USES GI

A
  • ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
57
Q

ANTICHOLINERGIC USEs CV

A
  • VAGOLYTIC (INCREASES HEART RATE)
58
Q

ANTICHOLINERGIC USES secretions

A

DECREASES ALL; SURGERY AND DENTAL USES

59
Q

ANTICHOLINERGIC USES as ANTIDOTE

A

REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)

60
Q

ANTICHOLINERGIC USES PULMONARY

A
  • COPD / ASTHMA TREATMENT (BRONCHODILATION)
61
Q

ANTICHOLINERGIC TOXICITY EFFECTS
CNS:
Eye:
CV:
Respiratory:
GI:

A

CNS: Drowsiness, amnesia, agitation, hallucinations, coma (scopolamine > atropine)
Eye: Mydriasis, cycloplegia, reduced lacrimal secretion
CV: Tachycardia (vagal inhibition)
Respiratory: Bronchodilation, reduced airway secretions
GI: Decreased motility, xerostomia

62
Q

amt liquid nic to be fatal?
signs?

A

40MG (1 DROP PURE LIQUID) = FATAL
signs: Seizure, Respiratory arrest, Coma, Paralysis

63
Q

*VARENICLINE (CHANTIX®)
* mechanism
* T½ AND AFFINITY
* INHIBITS:
common side effect

A
  • PARTIAL AGONIST/ ANTAGONIST of nicotine
  • LONG T½ AND HIGH AFFINITY FOR NACH(OS)
  • INHIBITS:
  • NICOTINE BINDING
  • WITHDRAWAL SYMPTOMS
  • DOPAMINE RELEASE

people cease due to vivid nightmares

64
Q

NEUROMUSCULAR
BLOCKERS classes/ names

A
  • DEPOLARIZING: SUCCINYLCHOLINE
  • NONDEPOLARIZING: ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM
65
Q

NEUROMUSCULAR
BLOCKERS main action

general action of both classes

A
  • INHIBIT BINDING OF ACH AT NMJ
66
Q

SUCCINYLCHOLINE
* mechanism
* ONSET
* DURATION
* higher dose if pt is?
* CAUTION FOR?

A

depolarizing NM blocker
* OPENS SODIUM CHANNELS
* ONSET ~ 60 SECONDS
* DURATION ~ 5 MINUTES
* MORE IF HYPOTENSIVE
* CAUTION: HYPERKALEMIA! due to DENERVATION SUPERSENSITIVITY

67
Q

denervation supersensitivity, implication with succinylcholine

A

occurs with injury, can allow a denervated mm fiber to increase AchR over days post injury
when suc administered the K outflux would be much greater (Potassium Increase 5 – 10 mEq/L)

68
Q

ROCURONIUM
* ONSET?
* DURATION?
* ADR?
* REVERSAL?

A

NONDEPOLARIZING
* ONSET ~60 SECONDS
* DURATION ~ 45 MINUTES, not broken down by AchE like Succ
* NO SIGNIFICANT ADR
* REVERSAL AGENT can be given to ensure proper sedation

69
Q

Vecuronium
onset/duration
ADR?

A

2 min / 45 min
Few ADRs

70
Q

Pancuronium
onset/duration
causes?

A

3 min / > 2 hrs
Causes tachycardia

71
Q

Cisatracurium
onset/duration?
used as?

A

2 min / 1 hr
Few ADRs, used as continuous infusion in therapeutic temperature management

72
Q

Rocuronium
onset/duration?
excellent for?

A

1 min / 45 min
Excellent intubating conditions, no sig. ADRs

73
Q
  • PILOCARPINE (SALAGEN)
  • BETHANECHOL (URECHOLINE)
  • CEVIMILINE (EVOXAC)
A

DIRECT ACTING CHOLINERGICS names

74
Q
  • GLAUCOMA TX
  • CAUSES MIOSIS, LOWERS IOP
  • DENTAL USE – RADIATION-INDUCED XEROSTOMIA TX
A
  • PILOCARPINE (SALAGEN®)
    tx of?
    causes?
    dental use?
75
Q
  • POST-OPERATIVE URINARY RETENTION TX
  • MOST RESISTANT TO CHOLINESTERASE
A
  • BETHANECHOL (URECHOLINE®)
    tx of?
    most resistant of?
76
Q
  • SELECTIVE FOR M3
  • MORE SELECTIVE FOR EXOCRINE GLANDS
  • RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
A
  • CEVIMILINE (EVOXAC®)
    selective for?
    tx of?
77
Q
  • REVERSIBLE: ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®), GALANTAMINE (RAZADYNE®)
  • IRREVERSIBLE: ORGANOPHOSHPATES
A

INDIRECT ACTING CHOLINERGICS
* ACETYLCHOLINESTERASE INHIBITORS

types?

78
Q
  • MYASTHENIA GRAVIS
  • GLAUCOMA
  • GI MOTILITY
  • REVERSAL OF NEUROMUSCULAR BLOCKADE
  • ANTICHOLINERGIC TOXICITY
  • ALZHEIMER
A

INDIRECT ACTING CHOLINERGICS
* USED FOR TREATMENT OF:

79
Q
A

REVERSIBLE ACHE INHIBITORS names

80
Q

indications:
*Myasthenia gravis
*Nerve agent prophylaxis
notes:
1st line for MG
4-6h duration

A

Pyridostigmine (Regonol®)
indications?
1st line for?
duration?

81
Q

AchE inhibitor indicated for:
*Myasthenia gravis
*Post-op ileus / urinary retention
*Neuromuscular blockade reversal

Doesn’t enter CNS (quaternary amine)

A

Neostigmine (Prostigmin®)
indications?
does not?

82
Q

indication:
*Anticholinergic toxicity tx via AchE inhibition
Enters CNS (tertiary amine)
Not routinely used due to CNS activity, ADRs

A

Physostigmine (Antilirium®)
indication?
enters? why not routinely used?

83
Q

indication:
*Diagnosis of myasthenia gravis

Doesn’t enter CNS (quaternary amine)
Not routinely used for treatment,
short t ½ (5 min)

A

Edrophonium (Tensilon®)
used for? why?

84
Q

*Mild-to-moderate Alzheimer’s disease

More selective AChE for management of cognitive dysfunction with Modest clinical benefits

A

Galantamine, rivastigmine, donepezil
all 3amine AchE inhibitors

85
Q

Irreversible AChE
Long lasting
Insecticides: Parathion (more dangerous), malathion (safer)
Nerve agents: Sarin, soman, tabun, VX
Novichok Agents (binary, req mixture)

A

ORGANOPHOSPHATES
bind?
Insecticides?
nerve agents?

86
Q
  • REGENERATES ACHE
    must use before bond ages to prevent AchE inhibitors from binding
A
  • PRALIDOXIME (2-PAM)
87
Q

REQUIRES HUGE AMOUNTS
* MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT NICOTINIC SX (PARALYSIS)

A
  • ATROPINE with Ach toxicity
88
Q
  • PROPHYLAXIS ONLY, when exposure possible, acts as a cholergenic agent but binds AchE to prevent binidng of others
A
  • PYRIDOSTIGMINE for Ach toxicity?
89
Q
  • PROTOTYPICAL ANTICHOLINERGIC
  • MUSCARINIC SELECTIVITY
  • NO EFFECT S/P HEART TRANSPLANT
  • INDICATIONS:
  • BRADYCARDIA
  • OP TOXICITY – HUGE AMOUNTS NEEDED
  • DON’T USE < 0.5MG IN ADULTS= PARADOXICAL BRADYCARDIA
A

ATROPINE
* PROTOTYPICAL?
* SELECTIVITY?
* NO EFFECT in?
* INDICATIONS?
* DON’T USE what dose in adults. why?

90
Q
  • FOUND IN HYOSCYAMUS NIGER (HENBANE)
  • TERTIARY AMINE
    can be used to prevent short term mem formation/ increase suggestability
  • PRIMARY USE:
  • MOTION SICKNESS
  • VOODOO ZOMBIFICATION
A

SCOPOLAMINE
* FOUND IN?
* AMINE?
* PRIMARY USE?
results of use?

91
Q
  • QUATERNARY AMINE, FEWER CENTRAL EFFECTS
  • USED TO DRY SECRETIONS:
  • SURGERY
  • KETAMINE TREATMENT
  • ADJUNCT FOR REVERSAL OF NEUROMUSCULAR BLOCKERS
A

GLYCOPYRROLATE
* AMINE structure?
* USED TO?
* ADJUNCT FOR REVERSAL OF?

92
Q
  • PARTIAL AGONIST/ ANTAGONIST of nicotine
  • LONG T½ AND HIGH AFFINITY FOR NACH(OS)
  • INHIBITS:
  • NICOTINE BINDING
  • WITHDRAWAL SYMPTOMS
  • DOPAMINE RELEASE

people cease due to vivid nightmares

A

*VARENICLINE (CHANTIX®)
* mechanism
* T½ AND AFFINITY
* INHIBITS:
common side effect

93
Q

depolarizing NM blocker
* OPENS SODIUM CHANNELS
* ONSET ~ 60 SECONDS
* DURATION ~ 5 MINUTES
* MORE IF HYPOTENSIVE
* CAUTION: HYPERKALEMIA! due to DENERVATION SUPERSENSITIVITY

A

SUCCINYLCHOLINE
* mechanism
* ONSET
* DURATION
* higher dose if pt is?
* CAUTION FOR?

94
Q

NONDEPOLARIZING
* ONSET ~60 SECONDS
* DURATION ~ 45 MINUTES, not broken down by AchE like Succ
* NO SIGNIFICANT ADR
* REVERSAL AGENT can be given to ensure proper sedation

A

ROCURONIUM
* ONSET?
* DURATION?
* ADR?
* REVERSAL?

95
Q

2 min / 45 min
Few ADRs

A

Vecuronium
onset/duration
ADR?

96
Q

3 min / > 2 hrs
Causes tachycardia

A

Pancuronium
onset/duration
causes?

97
Q

2 min / 1 hr
Few ADRs, used as continuous infusion in therapeutic temperature management

A

Cisatracurium
onset/duration?
used as?

98
Q

1 min / 45 min
Excellent intubating conditions, no sig. ADRs

A

Rocuronium
onset/duration?
excellent for?

99
Q
  • ATROPINE, SCOPOLAMINE (SCOPACE®), BENZTROPINE (COGENTIN®), DICYCLOMINE (BENTYL®
A
  • TERTIARY AMINES anticholergenics
    • TERTIARY AMINES HAVE CENTRAL EFFECTS
100
Q
  • GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM (SPIRIVA®)
A
  • QUATERNARY AMINES anticholergenics
    • QUATERNARY AMINES – PERIPHERAL EFFECTS
101
Q

depolarizing NM blockers

A

succinylcholine

102
Q

nondepolarizing NM blockers

A

ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM

103
Q

ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM

A

nondepolarizing NM blockers