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Pharmacology > Autonomic and Cholinergic > Flashcards

Autonomic and Cholinergic Flashcards

1
Q

AUTONOMIC
NERVOUS SYSTEM
(5)

A
  • INVOLUNTARY
  • SYMPATHETIC (SANS) AND PARASYMPATHETIC (PANS)
  • HANDLES VISCERAL FUNCTIONS
  • 2 NEURONS IN SERIES
  • ALL PREGANGLIONIC = Ach
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2
Q
  • 2 NEURONS IN SERIES
A
  • PRE- AND POST-
    GANGLIONIC
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3
Q

SYMPATHETIC
(SANS)
(6)

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)
(4)

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

SOMATIC NERVOUS
SYSTEM
(4)

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

CHOLINERGIC
FIBERS
(3)

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
(2)

A
  • RELEASE NOREPINEPHRINE
  • MOST SYMPATHETIC POSTGANGLIONIC FIBERS
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8
Q

CHOLINERGIC
TRANSMISSION

A

Acetyl CoA + choline = ACh
Transported to cytoplasm, prepped for release
Calcium triggers release
Binds to cholinergic receptor
Acetylcholinesterase breaks up the party:
choline + acetate

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9
Q

AUTONOMIC
RECEPTORS
(7)

A

CHOLINERGIC RECEPTORS
NICOTINIC (GANGLIONIC)
MUSCARINIC
ADRENERGIC RECEPTORS
ALPHA
BETA
DOPAMINE

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10
Q

NICOTINIC RECEPTORS
* 3 MAIN CLASSES

Excitatory or Inhibitory?

A
  • MUSCLE
  • GANGLIONIC
  • CNS
  • EXCITATORY
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11
Q

MUSCARINIC
RECEPTORS
* M1 –
* M2 –
* M3 –
* M4 AND M5 –

A

NEURAL
ATRIAL
GLANDULAR/SMOOTH MUSCLE
CNS

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12
Q
  • M1 – NEURAL;
A

CNS EXCITATION,
GASTRIC SECRETION

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13
Q
  • M2 – ATRIAL;
A

CARDIAC AND NEURAL
INHIBITION

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14
Q
  • M3 – GLANDULAR/SMOOTH MUSCLE;
A

GASTRIC ACID,
SALIVARY SECRETION,
GI CONTRACTION,
OCULAR ACCOMMODATION,
VASODILATION

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15
Q
  • M4 AND M5 – CNS;
A

NOT AS clinically relevant

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16
Q

ADRENERGIC
RECEPTORS
* —-GANGLIONIC SYMPATHETIC SYSTEM ONLY

A

POST

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17
Q

ADRENERGIC
RECEPTORS
* POST-GANGLIONIC SYMPATHETIC SYSTEM ONLY
(3)

A
  • Α1, Α2
  • Β1, Β2, Β3
  • DOPAMINE
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18
Q

PHARMACOLOGY OF
DRUGS AFFECTING
CHOLINERGIC
TRANSMISSION
(4)

A

MUSCARINIC AGONISTS
MUSCARINIC ANTAGONISTS
GANGLION STIMULATING DRUGS
NEUROMUSCULAR BLOCKERS

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19
Q

MUSCARINIC
AGONISTS
AKA:

A

CHOLINERGICS

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20
Q

Skipped
CHOLINERGIC
DRUGS
(3)

A
  • PARASYMPATHOMIMETIC
  • DIRECT ACTING
  • INDIRECT ACTING
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21
Q
  • DIRECT ACTING
A
  • BINDS DIRECTLY TO NACH(OS) AND MACH(OS)
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22
Q
  • INDIRECT ACTING
    (2)
A
  • INHIBITS ACETYLCHOLINESTERASE
  • AMPLIFIERS OF ENDOGENOUS ACH
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23
Q

DIRECT ACTING
CHOLINERGICS
(3)

A

PILOCARPINE (SALAGEN)
BETHANECHOL (URECHOLINE)
CEVIMILINE (EVOXAC)

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24
Q

PILOCARPINE (SALAGEN®)
(3)

A
  • GLAUCOMA TX
  • CAUSES MIOSIS, LOWERS IOP
  • DENTAL USE – RADIATION-INDUCED XEROSTOMIA
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25
Q

BETHANECHOL (URECHOLINE®)
(2)

A
  • POST-OPERATIVE URINARY RETENTION
  • MOST RESISTANT TO CHOLINESTERASE
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26
Q

CEVIMILINE (EVOXAC®)
(3)

A
  • SELECTIVE FOR M3
  • MORE SELECTIVE FOR EXOCRINE GLANDS
  • RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
27
Q

INDIRECT ACTING
CHOLINERGICS
(3)

A
  • ACETYLCHOLINESTERASE INHIBITORS
  • REVERSIBLE
  • IRREVERSIBLE
28
Q

REVERSIBLE

A
  • ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®),
    GALANTAMINE (RAZADYNE®)
29
Q

IRREVERSIBLE

A
  • ORGANOPHOSHPATES
30
Q

INDIRECT ACTING
CHOLINERGICS
* USED FOR TREATMENT OF
(6)

A
  • MYASTHENIA GRAVIS
  • GLAUCOMA
  • GI MOTILITY
  • REVERSAL OF NEUROMUSCULAR BLOCKADE
  • ANTICHOLINERGIC TOXICITY
  • ALZHEIMERS
31
Q

ORGANOPHOSPHATES
(5)

A

Irreversible AChE
Long lasting
Insecticides
Nerve agents
Novichok Agents

32
Q

Insecticides
(2)

A

Parathion, malathion

33
Q

Nerve agents
(4)

A

Sarin, soman
tabun, VX

34
Q

ORGANOPHOSPHATE MECHANISM

A

Phosphorous (+) attracted to serine (-)
OP attaches to AChE, prevents ACh binding
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)
The aged bond. This AChE is now permanently
out of commission

35
Q

CHOLINERGIC TOXICITY
Muscarinic Symptoms

A

Salvation
Lacrimation
Urination
diarrhea
GI discomfort
emesis

diarrhea
urinationmiosis/muscles weak
braadycardia
emesis
lacrimation
salivation/sweating

36
Q

CHOLINERGIC TOXICITY
Nicotinic Symptoms

A

muscle cramps
tachycardia
weakness
twitching
fasciculations

37
Q

WHAT DO YOU
DO?
(3)

A
  • PRALIDOXIME (2-PAM)
  • ATROPINE – REQUIRES HUGE AMOUNTS
  • PYRIDOSTIGMINE
38
Q
  • PRALIDOXIME (2-PAM)
A
  • REGENERATES ACHE
39
Q
  • ATROPINE – REQUIRES HUGE AMOUNTS
A
  • MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT
    NICOTINIC SX (PARALYSIS)
40
Q
  • PYRIDOSTIGMINE
A
  • PROPHYLAXIS ONLY
41
Q

MUSCARINIC
ANTAGONISTS
AKA:

A

ANTICHOLINERGICS

42
Q

ANTICHOLINERGI
CS
(3)

A

*BINDS MUSCARINIC RECEPTORS, BLOCKS
ACH
*TERTIARY AMINES HAVE CENTRAL EFFECTS
*QUATERNARY AMINES – PERIPHERAL
EFFECTS

43
Q

Skipped
TERTIARY AMINES HAVE CENTRAL EFFECTS

A
  • ATROPINE, SCOPOLAMINE (SCOPACE®),
    BENZTROPINE (COGENTIN®), DICYCLOMINE
    (BENTYL®)
44
Q

Skipped
QUATERNARY AMINES – PERIPHERAL
EFFECTS

A
  • GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM
45
Q

ATROPINE
(3)

A
  • PROTOTYPICAL ANTICHOLINERGIC
  • MUSCARINIC SELECTIVITY
  • NO EFFECT S/P HEART TRANSPLANT
46
Q

ATROPINE
* INDICATIONS
(2)

A
  • BRADYCARDIA
  • OP TOXICITY – HUGE AMOUNTS NEEDED
47
Q

ATROPINE
* DON’T USE — IN ADULTS

A

< 0.5MG
* PARADOXICAL BRADYCARDIA

48
Q

SCOPOLAMINE
(2)

A

*FOUND IN HYOSCYAMUS NIGER
(HENBANE)
*TERTIARY AMINE

49
Q

SCOPOLAMINE
*PRIMARY USE
(2)

A
  • MOTION SICKNESS
  • VOODOO ZOMBIFICATION
50
Q

GLYCOPYRROLATE
* Amine
* USED TO
* ADJUNCT FOR

A

QUATERNARY AMINE, FEWER
CENTRAL EFFECTS
DRY SECRETIONS
REVERSAL OF
NEUROMUSCULAR BLOCKERS

51
Q

GLYCOPYRROLATE
* USED TO DRY SECRETIONS
(2)

A
  • SURGERY
  • KETAMINE TREATMENT
52
Q

ANTICHOLINERGIC
USES
(6)

A

OPHTHALMOLOGY
GI/GU
CARDIOVASCULAR
SECRETIONS
ANTIDOTE
PULMONARY

53
Q
  • OPHTHALMOLOGY
A
  • MYDRIASIS, CYCLOPLEGIA, INTRAOCULAR PRESSURE (IOP)
54
Q
  • GI/GU
A
  • ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
55
Q
  • CARDIOVASCULAR
A
  • VAGOLYTIC (INCREASES HEART RATE)
56
Q
  • SECRETIONS
A
  • DECREASES ALL; SURGERY AND DENTAL USES
57
Q
  • ANTIDOTE
A
  • REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)
58
Q
  • PULMONARY
A
  • COPD / ASTHMA TREATMENT (BRONCHODILATION)
59
Q

Skipped
ANTICHOLINERGI
C EFFECTS
CNS: (6)
Eye: (3)
CV: (1)
Respiratory: (1)
GI: (2)

A

Drowsiness, amnesia, agitation, hallucinations, coma
scopolamine > atropine

Mydriasis, cycloplegia, reduced lacrimal secretion

Tachycardia (vagal inhibition)

Bronchodilation, reduced airway secretions

Decreased motility, xerostomia

60
Q

NICOTINIC DRUGS
*VARENICLINE
(CHANTIX®)
(3)

A
  • PARTIAL
    AGONIST/ANTAGONIS
    T
  • LONG T½ AND HIGH
    AFFINITY FOR
    NACH(OS)
  • INHIBITS: NICOTINE BINDING
61
Q

NEUROMUSCUL
AR BLOCKERS
* DEPOLARIZING (1)
* NONDEPOLARIZING (4)

A

SUCCINYLCHOLINE

ROCURONIUM
VECURONIUM
PANCURONIUM
CISATRICURIUM

62
Q

NEUROMUSCULAR
BLOCKERS
* INHIBIT BINDING OF ACH AT NMJ
* DEPOLARIZING (1)
* NONDEPOLARIZING (4)

A

SUCCINYLCHOLINE

  • ROCURONIUM
  • VECURONIUM
  • PANCURONIUM
  • CISATRICURIUM
63
Q

SUCCINYLCHOLINE
*
* ONSET ~
* DURATION ~
* — MG/KG IV (ACTUAL BODY WEIGHT)
* MORE IF —
* CAUTION:

A

OPENS SODIUM CHANNELS
60 SECONDS
5 MINUTES
1.5
HYPOTENSIVE
HYPERKALEMIA!
* DENERVATION SUPERSENSITIVITY

64
Q

ROCURONIUM
*
* ONSET ~
* DURATION ~
* — MG/KG
* ADR
* — AGENT

A

NONDEPOLARIZING
60 SECONDS
45 MINUTES
0.6 – 1.2
NO SIGNIFICANT ADR
REVERSAL

Pharmacology (13 decks)

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