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Cholinergics
Cholinergic Agonists and Antagonists
36
Pharmacology
Professional
06/26/2009

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Term
MUSCARINIC SIGNS AND SYMPTOMS OF CHOLINESTERASE INHIBITORS
Definition
Diarrhea Urination (micturition)
Miosis (constricted pupils) Mucous
Bradycardia
Bronchorrhea/spasm/constriction
Emesis
Lacrimation
Salivation/Secretion/Sweating
Term
NICOTINIC SIGNS AND SYMPTOMS OF CHOLINESTERASE INHIBITORS
Definition
Weakness
Tachycardia
Fasciculation
Hypertension/Hyperglycemia
Mydriasis (less common
Term
SIGNS AND SYMPTOMS OF CHOLINESTERASE INHIBITORS in Central Nervous System
Definition
Confusion
Convulsions
Coma
Term
Parasympathetic Neuroeffector Junction
Definition
Muscarinic
M1-M5 Neurons
M1 Gastric Parietal Cells (Increase HCl Secretion)
M2 Cardiac & Smooth Muscle
M3 exocrine glands, smooth muscle
Term
Postganglionic Nerve of Sympathetic and Parasympathetic
Skeletal Muscle Motor End Plate
Definition
Cholinergic Receptor Locations (Nicotinic)
Term
Central Nervous System
Definition
Nicotinic and Muscarinic Receptors are both found here
Term
Cholinergic Agonists
Definition
Indirect (Reversible and Irreversible) and Direct (resemble acetylcholine) acting affect M receptors and N receptors
Term
Direct acting cholinergic agonists general toxic effects
Definition
Flushing, sweating, bradycardia, Bronchoconstriction, GI distress, belching, nausea and vomiting, diarrhea, salivation
Term
Bethanechol, Carbachol, Pilocarpine
Definition
Direct acting cholinergic agonists
Term
Bethanechol
Definition
Indication – Urinary retention after surgery or postpartum
Contraindications – Physical obstruction, asthma and Peptic ulcers
Term
Carbachol
Definition
Indication – Only used topically as a miotic to decrease IOP
Can stimulate BOTH Muscarinic and Nicotinic receptors at PNS/SNS
Term
Pilocarpine
Definition
Indications - Glaucoma: IOP decreases in 1 hour
Tertiary amine
Term
Open Angle Glaucoma
Definition
Increased intraocular pressure, degenerative process in the trabecular meshwork
Term
Angle-Closure Glaucoma
Definition
No abnormal resistance to aqueous humor outflow
Term
Anticholinesterases
Definition
Indirect Cholinergic agents
Prolongs duration of endogenous acetylcholine
Cause both Muscarinic and Nicotinic Stimulation
Term
Edrophonium, Physostigmine, Neostigmine, Pyridostigmine
Definition
Reversible anticholinesterases
Term
Edrophonium
Definition
Clinical indication – diagnosis of myasthenia gravis
Quaternary Ammonium
Term
Physostigmine
Definition
Tertiary Amine
Indications – Atony (Increases intestinal and bladder motility)
Treatment for anticholinergic overdose (atropine, tricyclics and phenothiazines); glaucoma
May cause convulsions in high doses
Term
Neostigmine
Definition
Quarternary ammonium
Clinical Indication – antidote for neuromuscular blockers and myasthenia gravis
Term
Pyridostigmine
Definition
Clinical Indication - Used for myasthenia gravis treatment
Term
Echothiophate
Definition
Irreversible Anticholinesterases
Clinical Indication - Irreversible anticholinesterase used to treat glaucoma
Term
Pralidoxime
Definition
Will reactivate cholinesterase, antidote to Cholinesterase Inhibitors
Term
Atropine
Definition
A M receptor antagonist, relieves the symptoms
Term
SLUDWARMF
Definition
Acronym for symptoms of a direct acting or indirect acting acetylcholinesterase inhibitors
Sweating, Lacrimation, Urination, Diarrhea, Wheezing, Accommodation, Rinorrhea, Miosis, Fasiculations
Term
Cholinergic Antagonists
Definition
Sub categories:
Antimuscarinic - interrupts parasympathetic signals
Ganglionic Blockers - (Nicotinic blockers)
Neuromuscular Blockers
Term
Antimuscarinic Agents
Definition
Block muscarinic receptors on the effector organs of the parasympathetic nervous system and on the sweat glands (exception from sympathetic system)
Symptoms are opposite those from acetylcholinesterase inhibitors
Contraindications - Narrow angle glaucoma, Tachycardia, GI or GU Obstructive disease, Myasthenia gravis , Asthma (Atropine only)
Term
Atropine Sulfate, Scopolamine, Oxybutynin, Tolterodine, Ipratropium
Definition
Antimuscarinic Agents
Term
Atropine Sulfate
Definition
GI - Antispasmodic agent for GI track and bladder - Reduces motility but not HCL secretion
Antidote for cholinergic agonists (organophosphate overdoses)
Term
Scopolamine
Definition
Motion Sickness - Topical patch used to treat motion sickness
Term
Oxybutynin
Definition
Exerts direct antispasmotic effect on smooth muscle
Indication - Bladder instability and overactive bladder
Term
Tolterodine
Definition
Indicated for overactive bladder
Term
Ipratropium
Definition
Indication – Bronchospasm associated with COPD and Rhinorrhea
Term
Ganglionic Blockers
Definition
No selectivity - block receptors on both the parasympathetic and sympathetic ganglia
Term
Neuromuscular Blocking Drugs
Definition
Indication – Surgery to produce complete muscle relaxation
Term
Tubocurarine, pancuronium, vecuronium
Definition
Nondepolarizing blockers
Competitive blocker - action can be reversed by increasing concentration of acetylcholine with cholinesterase inhibitors
Term
Succinylcholine
Definition
Depolarizing Agent
Attaches to nicotinic receptor and depolarizes the junction but remains on the receptor for a long time, noncompetitive
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