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
2
Q
- 2 NEURONS IN SERIES
A
- PRE- AND POST-
GANGLIONIC
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
4
Q
PARASYMPATHETIC
(PANS)
(4)
A
- NORMAL MAINTENANCE
AND ANABOLIC
METABOLISM - INCREMENTAL
ACTIVATION - VAGAL STIMULATION
- LONG PRE-, SHORT
POST-
5
Q
SOMATIC NERVOUS
SYSTEM
(4)
A
- VOLUNTARY
- CONTROLS MOVEMENT, RESPIRATION, POSTURE
- ALWAYS EXCITATORY
- NO GANGLIA
6
Q
CHOLINERGIC
FIBERS
(3)
A
- SYNTHESIZE AND RELEASE ACH
- ALL PREGANGLIONIC EFFERENT AND SOMATIC
MOTOR FIBERS TO SKELETAL MUSCLE - MOST PARASYMPATHETIC POSTGANGLIONIC
FIBERS
7
Q
ADRENERGIC
FIBERS
(2)
A
- RELEASE NOREPINEPHRINE
- MOST SYMPATHETIC POSTGANGLIONIC FIBERS
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
9
Q
AUTONOMIC
RECEPTORS
(7)
A
CHOLINERGIC RECEPTORS
NICOTINIC (GANGLIONIC)
MUSCARINIC
ADRENERGIC RECEPTORS
ALPHA
BETA
DOPAMINE
10
Q
NICOTINIC RECEPTORS
* 3 MAIN CLASSES
Excitatory or Inhibitory?
A
- MUSCLE
- GANGLIONIC
- CNS
- EXCITATORY
11
Q
MUSCARINIC
RECEPTORS
* M1 –
* M2 –
* M3 –
* M4 AND M5 –
A
NEURAL
ATRIAL
GLANDULAR/SMOOTH MUSCLE
CNS
12
Q
- M1 – NEURAL;
A
CNS EXCITATION,
GASTRIC SECRETION
13
Q
- M2 – ATRIAL;
A
CARDIAC AND NEURAL
INHIBITION
14
Q
- M3 – GLANDULAR/SMOOTH MUSCLE;
A
GASTRIC ACID,
SALIVARY SECRETION,
GI CONTRACTION,
OCULAR ACCOMMODATION,
VASODILATION
15
Q
- M4 AND M5 – CNS;
A
NOT AS clinically relevant
16
Q
ADRENERGIC
RECEPTORS
* —-GANGLIONIC SYMPATHETIC SYSTEM ONLY
A
POST
17
Q
ADRENERGIC
RECEPTORS
* POST-GANGLIONIC SYMPATHETIC SYSTEM ONLY
(3)
A
- Α1, Α2
- Β1, Β2, Β3
- DOPAMINE
18
Q
PHARMACOLOGY OF
DRUGS AFFECTING
CHOLINERGIC
TRANSMISSION
(4)
A
MUSCARINIC AGONISTS
MUSCARINIC ANTAGONISTS
GANGLION STIMULATING DRUGS
NEUROMUSCULAR BLOCKERS
19
Q
MUSCARINIC
AGONISTS
AKA:
A
CHOLINERGICS
20
Q
Skipped
CHOLINERGIC
DRUGS
(3)
A
- PARASYMPATHOMIMETIC
- DIRECT ACTING
- INDIRECT ACTING
21
Q
- DIRECT ACTING
A
- BINDS DIRECTLY TO NACH(OS) AND MACH(OS)
22
Q
- INDIRECT ACTING
(2)
A
- INHIBITS ACETYLCHOLINESTERASE
- AMPLIFIERS OF ENDOGENOUS ACH
23
Q
DIRECT ACTING
CHOLINERGICS
(3)
A
PILOCARPINE (SALAGEN)
BETHANECHOL (URECHOLINE)
CEVIMILINE (EVOXAC)
24
Q
PILOCARPINE (SALAGEN®)
(3)
A
- GLAUCOMA TX
- CAUSES MIOSIS, LOWERS IOP
- DENTAL USE – RADIATION-INDUCED XEROSTOMIA
25
BETHANECHOL (URECHOLINE®)
(2)
* POST-OPERATIVE URINARY RETENTION
* MOST RESISTANT TO CHOLINESTERASE
26
CEVIMILINE (EVOXAC®)
(3)
* SELECTIVE FOR M3
* MORE SELECTIVE FOR EXOCRINE GLANDS
* RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYNDROME
27
INDIRECT ACTING
CHOLINERGICS
(3)
* ACETYLCHOLINESTERASE INHIBITORS
* REVERSIBLE
* IRREVERSIBLE
28
REVERSIBLE
* ‘-STIGMINE’ AGENTS, DONEPEZIL (ARICEPT®),
GALANTAMINE (RAZADYNE®)
29
IRREVERSIBLE
* ORGANOPHOSHPATES
30
INDIRECT ACTING
CHOLINERGICS
* USED FOR TREATMENT OF
(6)
* MYASTHENIA GRAVIS
* GLAUCOMA
* GI MOTILITY
* REVERSAL OF NEUROMUSCULAR BLOCKADE
* ANTICHOLINERGIC TOXICITY
* ALZHEIMERS
31
ORGANOPHOSPHATES
(5)
Irreversible AChE
Long lasting
Insecticides
Nerve agents
Novichok Agents
32
Insecticides
(2)
Parathion, malathion
33
Nerve agents
(4)
Sarin, soman
tabun, VX
34
ORGANOPHOSPHATE MECHANISM
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
CHOLINERGIC TOXICITY
Muscarinic Symptoms
Salvation
Lacrimation
Urination
diarrhea
GI discomfort
emesis
diarrhea
urinationmiosis/muscles weak
braadycardia
emesis
lacrimation
salivation/sweating
36
CHOLINERGIC TOXICITY
Nicotinic Symptoms
muscle cramps
tachycardia
weakness
twitching
fasciculations
37
WHAT DO YOU
DO?
(3)
* PRALIDOXIME (2-PAM)
* ATROPINE – REQUIRES HUGE AMOUNTS
* PYRIDOSTIGMINE
38
* PRALIDOXIME (2-PAM)
* REGENERATES ACHE
39
* ATROPINE – REQUIRES HUGE AMOUNTS
* MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT
NICOTINIC SX (PARALYSIS)
40
* PYRIDOSTIGMINE
* PROPHYLAXIS ONLY
41
MUSCARINIC
ANTAGONISTS
AKA:
ANTICHOLINERGICS
42
ANTICHOLINERGI
CS
(3)
*BINDS MUSCARINIC RECEPTORS, BLOCKS
ACH
*TERTIARY AMINES HAVE CENTRAL EFFECTS
*QUATERNARY AMINES – PERIPHERAL
EFFECTS
43
Skipped
TERTIARY AMINES HAVE CENTRAL EFFECTS
* ATROPINE, SCOPOLAMINE (SCOPACE®),
BENZTROPINE (COGENTIN®), DICYCLOMINE
(BENTYL®)
44
Skipped
QUATERNARY AMINES – PERIPHERAL
EFFECTS
* GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM
45
ATROPINE
(3)
* PROTOTYPICAL ANTICHOLINERGIC
* MUSCARINIC SELECTIVITY
* NO EFFECT S/P HEART TRANSPLANT
46
ATROPINE
* INDICATIONS
(2)
* BRADYCARDIA
* OP TOXICITY – HUGE AMOUNTS NEEDED
47
ATROPINE
* DON’T USE --- IN ADULTS
< 0.5MG
* PARADOXICAL BRADYCARDIA
48
SCOPOLAMINE
(2)
*FOUND IN HYOSCYAMUS NIGER
(HENBANE)
*TERTIARY AMINE
49
SCOPOLAMINE
*PRIMARY USE
(2)
* MOTION SICKNESS
* VOODOO ZOMBIFICATION
50
GLYCOPYRROLATE
* Amine
* USED TO
* ADJUNCT FOR
QUATERNARY AMINE, FEWER
CENTRAL EFFECTS
DRY SECRETIONS
REVERSAL OF
NEUROMUSCULAR BLOCKERS
51
GLYCOPYRROLATE
* USED TO DRY SECRETIONS
(2)
* SURGERY
* KETAMINE TREATMENT
52
ANTICHOLINERGIC
USES
(6)
OPHTHALMOLOGY
GI/GU
CARDIOVASCULAR
SECRETIONS
ANTIDOTE
PULMONARY
53
* OPHTHALMOLOGY
* MYDRIASIS, CYCLOPLEGIA, INTRAOCULAR PRESSURE (IOP)
54
* GI/GU
* ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
55
* CARDIOVASCULAR
* VAGOLYTIC (INCREASES HEART RATE)
56
* SECRETIONS
* DECREASES ALL; SURGERY AND DENTAL USES
57
* ANTIDOTE
* REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)
58
* PULMONARY
* COPD / ASTHMA TREATMENT (BRONCHODILATION)
59
Skipped
ANTICHOLINERGI
C EFFECTS
CNS: (6)
Eye: (3)
CV: (1)
Respiratory: (1)
GI: (2)
Drowsiness, amnesia, agitation, hallucinations, coma
scopolamine > atropine
Mydriasis, cycloplegia, reduced lacrimal secretion
Tachycardia (vagal inhibition)
Bronchodilation, reduced airway secretions
Decreased motility, xerostomia
60
NICOTINIC DRUGS
*VARENICLINE
(CHANTIX®)
(3)
* PARTIAL
AGONIST/ANTAGONIS
T
* LONG T½ AND HIGH
AFFINITY FOR
NACH(OS)
* INHIBITS: NICOTINE BINDING
61
NEUROMUSCUL
AR BLOCKERS
* DEPOLARIZING (1)
* NONDEPOLARIZING (4)
SUCCINYLCHOLINE
ROCURONIUM
VECURONIUM
PANCURONIUM
CISATRICURIUM
62
NEUROMUSCULAR
BLOCKERS
* INHIBIT BINDING OF ACH AT NMJ
* DEPOLARIZING (1)
* NONDEPOLARIZING (4)
SUCCINYLCHOLINE
* ROCURONIUM
* VECURONIUM
* PANCURONIUM
* CISATRICURIUM
63
SUCCINYLCHOLINE
*
* ONSET ~
* DURATION ~
* --- MG/KG IV (ACTUAL BODY WEIGHT)
* MORE IF ---
* CAUTION:
OPENS SODIUM CHANNELS
60 SECONDS
5 MINUTES
1.5
HYPOTENSIVE
HYPERKALEMIA!
* DENERVATION SUPERSENSITIVITY
64
ROCURONIUM
*
* ONSET ~
* DURATION ~
* --- MG/KG
* ADR
* --- AGENT
NONDEPOLARIZING
60 SECONDS
45 MINUTES
0.6 – 1.2
NO SIGNIFICANT ADR
REVERSAL
