Autonomic and Cholinergic Rc Flashcards
1
Q
• INVOLUNTARY • SYMPATHETIC (SANS) AND PARASYMPATHETIC (PANS) • HANDLES VISCERAL FUNCTIONS • 2 NEURONS IN SERIES • PRE- AND POST- GANGLIONIC • ALL PREGANGLIONIC release Ach
A
AUTONOMIC
NERVOUS SYSTEM
2
Q
All pregang fibers release ____ in the ANS
A
Ach
3
Q
• FIGHT OR FLIGHT • RUNS ON NOREPINEPHRINE • INCREASES CO, BP, RR, BLOOD FLOW, BG • DECREASES RBF, DIGESTIVE PROCESSES • FIRES AT ONCE • SHORT PRE-, LONG POST-
A
Sympathetic nervous system
4
Q
• NORMAL MAINTENANCE AND ANABOLIC METABOLISM • INCREMENTAL ACTIVATION • VAGAL STIMULATION • LONG PRE-, SHORT POST-
A
Parasympathetic nervous system
5
Q
- VOLUNTARY
- CONTROLS MOVEMENT, RESPIRATION, POSTURE
- ALWAYS EXCITATORY
- NO GANGLIA
A
SOMATIC NERVOUS SYSTEM
6
Q
• SYNTHESIZE AND RELEASE ACH • ALL PREGANGLIONIC EFFERENT AND SOMATIC MOTOR FIBERS TO SKELETAL MUSCLE • MOST PARASYMPATHETIC POSTGANGLIONIC FIBERS
A
CHOLINERGIC
FIBERS
7
Q
- RELEASE NOREPINEPHRINE
* MOST SYMPATHETIC POSTGANGLIONIC FIBERS
A
ADRENERGIC
FIBERS
8
Q
A ____ is a molecule that induces a response by binding to receptor at site of relase
-Short duration, quick acting
A
Neurotransmitter
9
Q
A ____ is a molecule released in bloodstream that travels to target to induce effect;
Long lasting, long time before it can take action
A
neurohormone
10
Q
______RECEPTORS
NICOTINIC (GANGLIONIC)
MUSCARINIC
A
CHOLINERGIC
11
Q
______ RECEPTORS
ALPHA
BETA
DOPAMINE
A
ADRENERGIC
12
Q
Is a nicotinic receptor used to excite or inhibit?
A
Excite
13
Q
______ muscarinic receptors: CNS EXCITATION,
GASTRIC SECRETION
A
M1 – NEURAL;
14
Q
______ muscarinic receptors:CARDIAC AND NEURAL
INHIBITION
A
M2 – ATRIAL;
15
Q
______ muscarinic receptors:
GASTRIC ACID, SALIVARY
SECRETION, GI CONTRACTION,
OCULAR ACCOMMODATION, VASODILATION
A
M3 – GLANDULAR/SMOOTH MUSCLE;
16
Q
Para or symp NS?
- Mydriasis
- Reduced saliva flow
- Increased SV and HR
- Vasoconstriction
- Reduced peristalsis and secretion
- Glycogen to glucose
- Inhibition of bladder contraction
- Epinephrine release
A
Sympathetic NS
17
Q
Para or symp NS?
- Miosis
- Stimulated salivary flow
- Decreased HR
- Bronchoconstriction
- Stimulates peristalsis and secretion
- Stimulates bile release
- Bladder constriction
A
Parasmyp
18
Q
\_\_\_\_\_\_ drugs • PARASYMPATHOMIMETIC • DIRECT ACTING • BINDS DIRECTLY TO NACH(OS) AND MACH(OS) • INDIRECT ACTING • INHIBITS ACETYLCHOLINESTERASE • AMPLIFIERS OF ENDOGENOUS ACH
A
Cholinergic drugs
19
Q
DIRECT ACTING
- GLAUCOMA TX
- CAUSES MIOSIS, LOWERS IOP
- DENTAL USE – RADIATION-INDUCED XEROSTOMIA
A
CHOLINERGICS• PILOCARPINE (SALAGEN®)
20
Q
DIRECT ACTING
CHOLINERGICS
- POST-OPERATIVE URINARY RETENTION
- MOST RESISTANT TO CHOLINESTERASE
A
• BETHANECHOL (URECHOLINE®)
21
Q
DIRECT ACTING
CHOLINERGICS
- SELECTIVE FOR M3
- MORE SELECTIVE FOR EXOCRINE GLANDS
- RADIATION-INDUCED XEROSTOMIA; SJOGREN’S SYN
A
• CEVIMILINE (EVOXAC®)
22
Q
- USED FOR TREATMENT OF
- MYASTHENIA GRAVIS
- GLAUCOMA
- GI MOTILITY
- REVERSAL OF NEUROMUSCULAR BLOCKADE
- ANTICHOLINERGIC TOXICITY
- ALZHEIMERS
A
INDIRECT ACTING
CHOLINERGICS
23
Q
•Used for Diagnosis of myasthenia gravis Doesn’t enter CNS (quaternary
amine)
Not routinely used for treatment, short t ½ (5 min)
A
Edrophonium (Tensilon®
24
Q
What 3 drugs? •Mild-to-moderate Alzheimer’s disease More selective AChE for management of cognitive dysfunction.
A
Galantamine,
rivastigmine,
donepezil
25
```
Irreversible AChE
Long lasting
Insecticides
Parathion, malathion
Nerve agents
Sarin, soman
tabun, VX
Novichok Agents
```
ORGANOPHOSPHATES
26
Once a bond between an organophosphate and Serine site on acetylcholinesterase is ______, it is permanently out of commission/destroyed
Aged
27
What are the muscarinic symptoms of cholinergic toxicity?
| Sludge Dumbbels
```
Salivation
Lacrimation
Urination
Diarrhea
GI discomfort
Emesis
```
```
Diarrhea
Urination
Miosis/muscles weak
Bronchorrhea
Bradycardia
Emesis
Lacrimation
Salivation/sweating
```
28
What are the nicotinic symptoms of cholinergic toxicity?
| MTWTF
```
Muscle cramps
Tachycardia
Weakness
Twitching
Fasciculations
```
29
(Drug treating cholinergic toxicity)
| • REGENERATES ACHE; must be given before aging
PRALIDOXIME (2-PAM)
30
(Drug treating cholinergic toxicity)
– REQUIRES HUGE AMOUNTS
• MUSCARINIC ANTAGONISM ONLY, WON’T CORRECT
NICOTINIC SX (PARALYSIS)
ATROPINE
31
```
•BINDS MUSCARINIC RECEPTORS, BLOCKS
ACH
•TERTIARY AMINES HAVE CENTRAL EFFECTS
• ATROPINE, SCOPOLAMINE (SCOPACE®),
BENZTROPINE (COGENTIN®), DICYCLOMINE
(BENTYL®)
•QUATERNARY AMINES – PERIPHERAL
EFFECTS
• GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM
(SPIRIVA®)
37
```
ANTICHOLINERGICS
32
```
(anticholinergics)
_____ AMINES HAVE CENTRAL EFFECTS
• ATROPINE, SCOPOLAMINE (SCOPACE®),
BENZTROPINE (COGENTIN®), DICYCLOMINE
(BENTYL®)
```
TERTIARY Amines
33
```
(anticholinergics)
• ____ amines– PERIPHERAL
EFFECTS
• GLYCOPYRROLATE (ROBINUL®), TIOTROPIUM
(SPIRIVA®)
```
QUATERNARY AMINES
34
* 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
35
Where does atropine work as far as muscarinic receptor?
Blocks M2
36
```
•FOUND IN HYOSCYAMUS NIGER
(HENBANE)
•TERTIARY AMINE
•PRIMARY USE
• MOTION SICKNESS
• VOODOO ZOMBIFICATION
```
SCOPOLAMINE
37
```
• QUATERNARY AMINE, FEWER
CENTRAL EFFECTS
• USED TO DRY SECRETIONS
• SURGERY
• KETAMINE TREATMENT
• ADJUNCT FOR REVERSAL OF
NEUROMUSCULAR BLOCKERS
- Doesn't mess with HR
```
GLYCOPYRROLATE
38
______ uses
• OPHTHALMOLOGY
• MYDRIASIS, CYCLOPLEGIA, Decreases INTRAOCULAR PRESSURE (IOP)
• GI/GU
• ANTISPASMODIC, ANTIDIARRHEAL, URINARY INCONTINENCE
• CARDIOVASCULAR
• VAGOLYTIC (INCREASES HEART RATE)
• SECRETIONS
• DECREASES ALL; SURGERY AND DENTAL USES
• ANTIDOTE
• REVERSAL OF CHOLINERGIC TOXICITY (ORGANOPHOSPHATE POISONING)
• PULMONARY
• COPD / ASTHMA TREATMENT (BRONCHODILATION)
ANTICHOLINERGIC
| USES
39
_____ effectes
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
ANTICHOLINERGIC EFFECTS
40
How many mg of nicotine is fatal?
40 mg (1 drop of pure liquid)
41
(NICOTINIC DRUGS_
```
• PARTIAL
AGONIST/ANTAGONIST
• LONG T½ AND HIGH AFFINITY FOR NACH(OS)
• INHIBITS:
• NICOTINE BINDING
• WITHDRAWAL SYMPTOMS
• DOPAMINE RELEASE
```
•VARENICLINE (CHANTIX®)
42
```
The following drugs are used as _______
• DEPOLARIZING
SUCCINYLCHOLINE
• NONDEPOLARIZING
ROCURONIUM
```
Neuromuscular blockers
43
```
• OPENS SODIUM CHANNELS
• ONSET ~ 60 SECONDS
• DURATION ~ 5 MINUTES
• 1.5 MG/KG IV (ACTUAL BODY WEIGHT)
• MORE IF HYPOTENSIVE
• CAUTION: HYPERKALEMIA!
• DENERVATION SUPERSENSITIVITY
- 2 Ach molecules fused together and blocks Na channels
```
SUCCINYLCHOLINE
44
* NONDEPOLARIZING
* ONSET ~60 SECONDS
* DURATION ~ 45 MINUTES
* 0.6 – 1.2 MG/KG
* NO SIGNIFICANT ADR
* REVERSAL AGENT
ROCURONIUM
