1 - Autonomic Pharmacology Flashcards
Oxybutynin
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
For:
Urinary Urge Incontinence / Post-op Spasms
↓ detrusor bladder muscle smooth muscle tone, spasms
Also:
trospium = less cns effect
Darifenacin / solifenacin / tolteridone –> M3 Receptor selective
Classification & Action
Neostigmine / Physostigmine
Carbaryl / Edrophonium
CholinEsterase INHIBITORS
INDIRECT-Acting CholinoMimetics (Agonists)
BLOCK degradation of ACh –> ↑ACh
Endrophonium = MG / Ileus / Arrhythmias
Neostigmine = MG / Ileus
Pyridostigmine = MG
PhysoStigmine = for AC poisoning
Autonomic System Nerves
ParaSympathetic
Long Neuron
ACh
Ganglion –> Short Neuron
ACh
Muscarinic Receptors
on
smooth muscle / cardiac tissue / secretory Gland
Effects of:
ANTICHOLINERGIC POISONING
“Bloody Mary”
HyperThermia = HOT as a hare
Blurred Vision = BLIND as a bat
Dry Mouth/Skin = DRY as a boe
FLUSHED skin = RED as a beet
Confusion = MAD as a hatter
Urinary Retention = FULL as a flask
Classification
Hexamethonium / Mecamylamine / Tetraethylammonium / Decamethonium
NICOTINIC Receptor Antagonists
Ganglion & NM Junction Blockers
Synthetic Amines
rarely used
because more selective autonomic blocking agents are available
Dicyclomine
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
for:
GI DISORDERS = IBS / Diarrhea
↓ smooth muscle & secretory gut activity
Atropine
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
- *MANDATORY ANTIDOTE** for
- *severe CHOLINESTERASE INHIBITOR POISONING**
blocks muscarinic excess @:
exocrine glands / heart / smooth muscle
Atropine
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
for:
Retinal Exam / Prevention of Synechiae after eye surgery
Causes:
- *MYDRIASIS** = pupil dilation
- *Cyclopegia** = paralysis of ciliary muscle + accomodation loss
Pralidoxime
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
- *Usual Antidote** for
- *early stage (48h) cholinesterase inhibitor poisoning**
regenerates active AChE
can relieve skeletal muscle end plate block
Classification
Muscarine / Pilocarpine
Nicotine / Lobeline
CHolinoMimetic Alkaloids
DIRECT-ACTING CholinoReceptor Agonists
Direct-Acting Choloreceptor AGONISTS
Choline Esters & Cholinomimetic Alkaloids
Target Organs
More “Rest & Digest”
EYE
Contraction
Heart
↓ Rate ↓ contractile strength; ↓ ref period
Blood Vessels
Dilation, contraction @ high dose
Lung
bronchoconstriction
GI Tract
↑motility / relaxation / secretion
Urinary Bladder
relaxation
Glands
secretion
Classification
Atropine / Belladonna Alkaloid / Scopolamine
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
Autonomic System Nerves
SYMPATHETIC
SHORT NEURONS FIRST
VV
Adrenal MEDULLA for EPI/NE
or
Long Neurons (Ganglionic)
NE
a/b - Adrenergic Receptors
smooth muscle / cardiac tissue / secretory glands
Nicotinic Receptor Locations
SKELETAL Muscle
Neuromuscular END plate
Autonomic GANGLION Cells
Central Nervous System
Classification
ACh / Methacoline / Carbachol / Bethanechol
CHOLINE ESTERS
DIRECT-ACTING CholinoReceptor Agonists
Classification
Echothiophate
Sarin
Parathion / Malathion
ORGANOPHOSPHATE
CholinEsterase INHIBITORS
INDIRECT-Acting CholinoMimetics (Agonists)
BLOCK degradation of ACh –> ↑ACh
Echothiophate = Glaucoma
Parathion / Malathion = Insecticides
Scopolamine
Classification / Uses
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
For:
MOTION SICKNESS
↓ vertigo, post‐op N&V
Function of:
ChAT
- *Ch**oline Acetyl Transferase
- *ChAT**
Choline –> AcetylCholine (ACh)
@
Neuron
Muscarinic Receptor Locations
Nerves
Heart** & **Smooth Muscles
Glands** & **Endothelium
Somatic System Nerves
Direct Motor Neuron
ACh
Nicotinic Receptors
on
Skeletal Muscles
Classification
Dicyclomine / Ipratropium / Oxybutynin
Pralidoxime
Muscarinic Receptor ANTAGONIST
Cholinoreceptor Antagonist
