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autonomics and cholergenics Flashcards

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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
* CEVIMILINE (EVOXAC®) selective for? tx of?
* SELECTIVE FOR M3 * MORE SELECTIVE FOR EXOCRINE GLANDS * RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
26
INDIRECT ACTING CHOLINERGICS | types?
* ACETYLCHOLINESTERASE INHIBITORS * REVERSIBLE: ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®), GALANTAMINE (RAZADYNE®) * IRREVERSIBLE: ORGANOPHOSHPATES
27
INDIRECT ACTING CHOLINERGICS * USED FOR TREATMENT OF:
* MYASTHENIA GRAVIS * GLAUCOMA * GI MOTILITY * REVERSAL OF NEUROMUSCULAR BLOCKADE * ANTICHOLINERGIC TOXICITY * ALZHEIMER
28
REVERSIBLE ACHE INHIBITORS names
29
Pyridostigmine (Regonol®) indications? 1st line for? duration?
indications: *Myasthenia gravis *Nerve agent prophylaxis notes: 1st line for MG 4-6h duration
30
Neostigmine (Prostigmin®) indications? does not?
indications: *Myasthenia gravis *Post-op ileus / urinary retention *Neuromuscular blockade reversal Doesn’t enter CNS (quaternary amine)
31
Physostigmine (Antilirium®) indication? enters? why not routinely used?
*Anticholinergic toxicity Enters CNS (tertiary amine): Not routinely used due to CNS activity, ADRs
32
Edrophonium (Tensilon®) used for? why?
*Diagnosis of myasthenia gravis Doesn’t enter CNS (quaternary amine) Not routinely used for treatment, short t ½ (5 min)
33
Galantamine, rivastigmine, donepezil indication? why?
*Mild-to-moderate Alzheimer’s disease More selective AChE for management of cognitive dysfunction. Modest clinical benefits
34
ORGANOPHOSPHATES bind? Insecticides? nerve agents?
Irreversible AChE Long lasting Insecticides: Parathion (more dangerous), malathion (safer) Nerve agents: Sarin, soman, tabun, VX Novichok Agents (binary, req mixture)
35
NORMAL PROCESS - ACHE
cleavage to inactivate Ach
36
ORGANOPHOSPHATE MECHANISM
Phosphorous (+) attracted to serine (-) OP attaches to AChE, prevents ACh binding= excess Ach
37
outcomes of AchE with OP
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)
38
aged bond of AchE
39
cholergenic toxicity signs progression
usually muscarinic signs followed by nicotinic
40
Muscarinic S/S of Chol toxicity
SLUDGE: salivation lacrimation urination Diarrhea GI discomfort Emesis OR DUMBBELLS : Diarrhea Urination Miosis/muscles weak Bronchorrhea Bradycardia Emesis Lacrimation Salivation/sweating
41
nicotinic S/S of toxicity
M T W T F Muscle cramps Tachycardia Weakness Twitching Fasciculations
42
how much time do we have with these agents at play? | possible abbreviations
43
* PRALIDOXIME (2-PAM)
* REGENERATES ACHE must use before bond ages to prevent AchE inhibitors from binding
44
* ATROPINE with Ach toxicity, issues with this?
REQUIRES HUGE AMOUNTS * MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT NICOTINIC SX (PARALYSIS)
45
* PYRIDOSTIGMINE for Ach toxicity?
* PROPHYLAXIS ONLY, when exposure possible, acts as a cholergenic agent but binds AchE to prevent binidng of others
46
possible otpions for Ach toxicity tx
* PRALIDOXIME (2-PAM) * ATROPINE * PYRIDOSTIGMINE
47
ANTICHOLINERGICS/ MUSCARINIC ANTAGONISTS
* BINDS MUSCARINIC RECEPTORS, BLOCKS ACH
48
classes of M antagonists and anticholergenics | dif of the classes
* TERTIARY AMINES HAVE CENTRAL EFFECTS * QUATERNARY AMINES – PERIPHERAL EFFECTS
49
* TERTIARY AMINES anticholergenics names?
* TERTIARY AMINES HAVE CENTRAL EFFECTS * ATROPINE, SCOPOLAMINE, BENZTROPINE , DICYCLOMINE
50
* QUATERNARY AMINES anticholergenics
* QUATERNARY AMINES – PERIPHERAL EFFECTS * GLYCOPYRROLATE, TIOTROPIUM
51
ATROPINE * PROTOTYPICAL? * SELECTIVITY? * NO EFFECT in pts with hx of? * INDICATIONS? * DON’T USE what dose in adults. why?
* 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
atropine mechanism
binds M2 to prevent Ach binding increased HR with no effect on sympathetics or BP, improves AV conduction
53
SCOPOLAMINE * FOUND IN? * AMINE? * PRIMARY USE? results of use?
* 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
GLYCOPYRROLATE * AMINE structure? * USED TO? * ADJUNCT FOR REVERSAL OF?
anticholergenic * QUATERNARY AMINE, FEWER CENTRAL EFFECTS * USED TO DRY SECRETIONS: * SURGERY * KETAMINE TREATMENT * ADJUNCT FOR REVERSAL OF NEUROMUSCULAR BLOCKERS
55
ANTICHOLINERGIC USES * OPHTHALMOLOGY
* INDUCE MYDRIASIS, INDUCE CYCLOPLEGIA, REDUCE IOP
56
ANTICHOLINERGIC USES GI
* ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
57
ANTICHOLINERGIC USEs CV
* VAGOLYTIC (INCREASES HEART RATE)
58
ANTICHOLINERGIC USES secretions
DECREASES ALL; SURGERY AND DENTAL USES
59
ANTICHOLINERGIC USES as ANTIDOTE
REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)
60
ANTICHOLINERGIC USES PULMONARY
* COPD / ASTHMA TREATMENT (BRONCHODILATION)
61
ANTICHOLINERGIC TOXICITY EFFECTS CNS: Eye: CV: Respiratory: GI:
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
amt liquid nic to be fatal? signs?
40MG (1 DROP PURE LIQUID) = FATAL signs: Seizure, Respiratory arrest, Coma, Paralysis
63
*VARENICLINE (CHANTIX®) * mechanism * T½ AND AFFINITY * INHIBITS: common side effect
* 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
NEUROMUSCULAR BLOCKERS classes/ names
* DEPOLARIZING: SUCCINYLCHOLINE * NONDEPOLARIZING: ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM
65
NEUROMUSCULAR BLOCKERS main action | general action of both classes
* INHIBIT BINDING OF ACH AT NMJ
66
SUCCINYLCHOLINE * mechanism * ONSET * DURATION * higher dose if pt is? * CAUTION FOR?
depolarizing NM blocker * OPENS SODIUM CHANNELS * ONSET ~ 60 SECONDS * DURATION ~ 5 MINUTES * MORE IF HYPOTENSIVE * CAUTION: HYPERKALEMIA! due to DENERVATION SUPERSENSITIVITY
67
denervation supersensitivity, implication with succinylcholine
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
ROCURONIUM * ONSET? * DURATION? * ADR? * REVERSAL?
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
Vecuronium onset/duration ADR?
2 min / 45 min Few ADRs
70
Pancuronium onset/duration causes?
3 min / > 2 hrs Causes tachycardia
71
Cisatracurium onset/duration? used as?
2 min / 1 hr Few ADRs, used as continuous infusion in therapeutic temperature management
72
Rocuronium onset/duration? excellent for?
1 min / 45 min Excellent intubating conditions, no sig. ADRs
73
* PILOCARPINE (SALAGEN) * BETHANECHOL (URECHOLINE) * CEVIMILINE (EVOXAC)
DIRECT ACTING CHOLINERGICS names
74
* GLAUCOMA TX * CAUSES MIOSIS, LOWERS IOP * DENTAL USE – RADIATION-INDUCED XEROSTOMIA TX
* PILOCARPINE (SALAGEN®) tx of? causes? dental use?
75
* POST-OPERATIVE URINARY RETENTION TX * MOST RESISTANT TO CHOLINESTERASE
* BETHANECHOL (URECHOLINE®) tx of? most resistant of?
76
* SELECTIVE FOR M3 * MORE SELECTIVE FOR EXOCRINE GLANDS * RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
* CEVIMILINE (EVOXAC®) selective for? tx of?
77
* REVERSIBLE: ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®), GALANTAMINE (RAZADYNE®) * IRREVERSIBLE: ORGANOPHOSHPATES
INDIRECT ACTING CHOLINERGICS * ACETYLCHOLINESTERASE INHIBITORS | types?
78
* MYASTHENIA GRAVIS * GLAUCOMA * GI MOTILITY * REVERSAL OF NEUROMUSCULAR BLOCKADE * ANTICHOLINERGIC TOXICITY * ALZHEIMER
INDIRECT ACTING CHOLINERGICS * USED FOR TREATMENT OF:
79
REVERSIBLE ACHE INHIBITORS names
80
indications: *Myasthenia gravis *Nerve agent prophylaxis notes: 1st line for MG 4-6h duration
Pyridostigmine (Regonol®) indications? 1st line for? duration?
81
AchE inhibitor indicated for: *Myasthenia gravis *Post-op ileus / urinary retention *Neuromuscular blockade reversal Doesn’t enter CNS (quaternary amine)
Neostigmine (Prostigmin®) indications? does not?
82
indication: *Anticholinergic toxicity tx via AchE inhibition Enters CNS (tertiary amine) Not routinely used due to CNS activity, ADRs
Physostigmine (Antilirium®) indication? enters? why not routinely used?
83
indication: *Diagnosis of myasthenia gravis Doesn’t enter CNS (quaternary amine) Not routinely used for treatment, short t ½ (5 min)
Edrophonium (Tensilon®) used for? why?
84
*Mild-to-moderate Alzheimer’s disease More selective AChE for management of cognitive dysfunction with Modest clinical benefits
Galantamine, rivastigmine, donepezil all 3amine AchE inhibitors
85
Irreversible AChE Long lasting Insecticides: Parathion (more dangerous), malathion (safer) Nerve agents: Sarin, soman, tabun, VX Novichok Agents (binary, req mixture)
ORGANOPHOSPHATES bind? Insecticides? nerve agents?
86
* REGENERATES ACHE must use before bond ages to prevent AchE inhibitors from binding
* PRALIDOXIME (2-PAM)
87
REQUIRES HUGE AMOUNTS * MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT NICOTINIC SX (PARALYSIS)
* ATROPINE with Ach toxicity
88
* PROPHYLAXIS ONLY, when exposure possible, acts as a cholergenic agent but binds AchE to prevent binidng of others
* PYRIDOSTIGMINE for Ach toxicity?
89
* 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
ATROPINE * PROTOTYPICAL? * SELECTIVITY? * NO EFFECT in? * INDICATIONS? * DON’T USE what dose in adults. why?
90
* FOUND IN HYOSCYAMUS NIGER (HENBANE) * TERTIARY AMINE can be used to prevent short term mem formation/ increase suggestability * PRIMARY USE: * MOTION SICKNESS * VOODOO ZOMBIFICATION
SCOPOLAMINE * FOUND IN? * AMINE? * PRIMARY USE? results of use?
91
* QUATERNARY AMINE, FEWER CENTRAL EFFECTS * USED TO DRY SECRETIONS: * SURGERY * KETAMINE TREATMENT * ADJUNCT FOR REVERSAL OF NEUROMUSCULAR BLOCKERS
GLYCOPYRROLATE * AMINE structure? * USED TO? * ADJUNCT FOR REVERSAL OF?
92
* 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
*VARENICLINE (CHANTIX®) * mechanism * T½ AND AFFINITY * INHIBITS: common side effect
93
depolarizing NM blocker * OPENS SODIUM CHANNELS * ONSET ~ 60 SECONDS * DURATION ~ 5 MINUTES * MORE IF HYPOTENSIVE * CAUTION: HYPERKALEMIA! due to DENERVATION SUPERSENSITIVITY
SUCCINYLCHOLINE * mechanism * ONSET * DURATION * higher dose if pt is? * CAUTION FOR?
94
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
ROCURONIUM * ONSET? * DURATION? * ADR? * REVERSAL?
95
2 min / 45 min Few ADRs
Vecuronium onset/duration ADR?
96
3 min / > 2 hrs Causes tachycardia
Pancuronium onset/duration causes?
97
2 min / 1 hr Few ADRs, used as continuous infusion in therapeutic temperature management
Cisatracurium onset/duration? used as?
98
1 min / 45 min Excellent intubating conditions, no sig. ADRs
Rocuronium onset/duration? excellent for?
99
* ATROPINE, SCOPOLAMINE (SCOPACE®), BENZTROPINE (COGENTIN®), DICYCLOMINE (BENTYL®
* TERTIARY AMINES anticholergenics * * TERTIARY AMINES HAVE CENTRAL EFFECTS
100
* GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM (SPIRIVA®)
* QUATERNARY AMINES anticholergenics * * QUATERNARY AMINES – PERIPHERAL EFFECTS
101
depolarizing NM blockers
succinylcholine
102
nondepolarizing NM blockers
ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM
103
ROCURONIUM, VECURONIUM, PANCURONIUM, CISATRICURIUM
nondepolarizing NM blockers

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