Cholinergic and Anticholinergic Flashcards
Gimme the NT involved and the Muscarinic stuffies
2 systems, 1 system, 5 systems
All pre G is Ach, Nicotinic
- Post G parasympathetic is all Muscarinic, including Sweat Glands; under sympathetic control
- NMJ, somatic is NICOTINIC
M1
- N&V, Vomiting Centre, Vestibular Nu
- CNS Confusion, Delirium also
- Note Vestibular & VC has H1 and mAch
- Stomach Acid secretion
M2
- Heart
M3
- Lung, Secretion
- Saliva, GI secretion
- GI motility
- GU, bladder contraction, erection
- EYE - near vision, iris sphincter, lens thickening, ciliary muscle - all improves drainage, decreases IOP, good for glaucoma
- SWEAT
Hence should Ach overdose what are the effects in general
Parasympathetic - diarrhoea, urine, near vision; Nausea Vomiting
Sympathetic - sweat
SOMATIC motor - fasciculation, spasms, falccid paralysis
Excitation of skeletal muscle and CNS!!!
What is contra-indicated for Ach agonists
Asthma; COPD
- M3 bronchoconstriction
Peptic ulcer disease
- M1 stomach secretion; recall Vagus, parietal
acute asthma, myocardial infarction, hyperthyroidism, paralytic ileus, benign prostatic hyperplasia, urinary retention, narrow-angle glaucoma, and myasthenia gravis.
In open-angle (WIDE) glaucoma, the iris is in the right position, and the uveoscleral drainage canals are clear. But the trabecular meshwork isn’t draining properly. In closed-angle (NARROW) glaucoma, the iris is squeezed against the cornea, blocking the uveoscleral drains and the trabecular meshwork.
Muscarinic Agonists 2 names and functions
- side effects?
Pilocarpine and Bethanechol
- both are non selective
Pilocarpine focus on SALIVA and eye functions
- miosis, accommodation, improve IOP - Glaucoma
- saliva for dry mouth
Bethanechol - think GI, GU
- GI motility for gastric atony after vagotomy
- GU for peeing for urinary incontinence
AE:
- Respi: COPD, Asthma
- Sweat
- GI,
- N&V
- Ophthalmic - miosis, near vision
Nicotine low dose function
USE
AE
Note nicotine receptors at Pre-G also for Sympathetic
++++ NMJ hence: activating
CVS: BP increase, RR increase; Vasoconstriction
GI: motility increase
NMJ: fasciculations
CNS: N&V
USE: Smoking cessation
AE: Dependence
Indirect cholinergics! what class and names only
AchE Inhibitors - just either reversible or irreversible
Reversible
- Neostigmine
- Physostigmine
- DONEpezil
Irreversible
- Sarin
Reversible AchE inhibitors clinical functions
AE
Donepezil - Azh Disease (Cholinergic neurons affected)
Neostigmine - NMJ for Myasthenia Gravis
- reversal of NM blockage after surgery;
- urinary retention treatment
AE
- Bradycardia, hypotension
- miosis, ab cramp
Whats sarin;
effects
antidote
Organophosphate; suicide AchE Inhibitor
- Bradycardia
- RR depressant;
- Sweat
- diarrhoea
- blurry vision
- N&V; Coma;
NOTE ACH is also universAL to nicotine to NMJ
- but sympathetic “dominance” is not here
- NMJ: Fasciculation, spasms, flaccid paralysis
Antidote
- Pralidoxime
- removes phosphate before ageing
- regenerates AchE
- Also Atropine
- block parasymp functions
- mAch blocker
Atropine
effects
use
contra I
Effects
- Confusion, Delirium (hence crosses BBB)
- M1: gastric secretion
- M2: CVS INCREASE
- M3: GI decrease GU decrease, sweating decrease; Eye dilated - mydriasis - careful increased IOP
- Blind, Mad, Hot, Red, Dry
- — red could be TC + CUTANEOUS Vasodilation
Use:
- bradycardia
- ophthalmic exams
- AchEI overdose
- Diphenoxylate opioid diarrhoe, prevent abuse;
contra I is Glaucoma;
note Benztropine for Parkinsonism
- cos DoR blocked
- Ach control
okie
Hyoscine, Scopolamine
functions
gimme a related drug
N&V
- block M1 in Vomiting centre, more impt in
- Vestibular Nu - for motion sickness
Diphenhydramine - first gen AH
- combined H1 blocker + M blocker
- both H1 and M1 are found at Vestibular Nu for motion sickness;
- but this one has sedation cos first gen AH
Ipratropium use
- SSSSAMA
Muscarinic antagonist
- Lung bronchoconstriction and secretions for COPD
- first line COPD second line Asthma
Note Scopolamine crosses BBB for N&V
- Atropine crosses BBB for delirium, confusion AE
- Ipratropium does not
okie
Nicotinic high dose
MOA
Effect
Depolarizing ganglionic block
Depolarizes cell, the VGNC inactivated
cell repolarizes but desensitized to action potential
Effect:
- block - respi block, BC, NM block
2 stages are depolarizing blockage and non-depolarizing blockage
NM blockages
- think of function why block NMJ
Non-depolarising NMBA, blocking agent
- pancuronium
- NMJ block
- used for surgery
- can be overcome w AchEI
DNMBA
- succinylcholine
- cannot be overcome w AchEI
- Phase 1: depolarises cell, fasciculations
- Phase 2: cell repolarizes but desensitized
- used for surgery
Botininum Toxin
- cleaves SNARE protein needed for exocytosis of Ach at NMJ
- AE: allergy, wrong paralysis
Pancuronium vs Succinylcholine vs Nicotine high does
Pancuronium is not depolarizing block
only at NMJ
Nicotine is global vs SCC is only at NMJ
Name drug classes which has anticholinergic functions
- also name anticholinergics
Anticholinergics
- Atropine
- Hyoscine, Scopolamine - N&V
Anti-Psychotics
- gen 1 gen 2 Haloperidol, Olanzapine, Clozapine;
Gen 1 Antihistamines eg Diphenhydramine!!!
- also M BLOCK and alpha BLOCK SE
- also 5HT3 block
TCA!!!
— w both M block and A1 block SE
