Cholinergic Drugs Flashcards
A direct acting agonist belonging to choline esters that is a prototype. It is used as eye drops to constrict the pupil. Use of this drug leads to negative chronotropy and decreased blood pressure
Acetylcholine
A direct acting agonist belonging to choline esters that is used for increasing intestinal motility and for benign prostatic hyperplasia. It is not hydrolyzed by AChE
Bethanechol
A direct acting agonist belonging to choline esters that is used for glaucoma. It is not hydrolyzed by AChE
Carbachol
A direct acting agonist belonging to choline esters that is used to diagnose asthma in the past
Methacholine
A direct acting agonist belonging to alkaloids that is from Pilocarpus jaborandi. It is a prodrug used as the drug of choice for emergency lowering of intraocular pressure or opthalmologic emergency and for glaucoma. Being a tertiary amine, it is stable to hydrolysis of AChE
Pilocarpine
A direct acting agonist belonging to alkaloids that is from Areca catechu (betel nut)
Arecoline
A direct acting agonist belonging to alkaloids that is from Amanita muscaria
Muscarine
An indirect and short acting agonist belonging to quaternary amines that is used to diagnose myasthenia gravis. it is the prototype for short acting AChE inhibitors. It binds reversibly to the active center of AChE, preventing its hydrolysis. It is also usually given IV or IM
Edrophonium (Tensilon)
An indirect acting agonist from carbamates with intermediate duration of action. This is also known as eserine, from the Calabar or ordeal bean (Physostigma venenosum), and is used for intestinal and bowel atony, glaucoma, and as an antidote for organophosphate poisoning like atropine, phenothiazine, and TCAs
Physostigmine
An indirect acting agonist from carbamates with intermediate duration of action. It is used for the treatment for myasthenia gravis and as an antidote for tubocurarine poisoning
Neostigmine
An indirect acting agonist from carbamates with intermediate duration of action. It is used for the treatment for myasthenia gravis
Pyridostigmine
They are indirect acting agonists from carbamates with intermediate duration of action. They are known as carbamate insecticides
Carbaryl
Methylcarbamate
They are indirect and long acting agonists that are organophosphates used for glaucoma
Isofluorophate
Echothiopate
They are indirect and long acting agonists that are organophosphates used as pesticides
Malathion
Parathion
They are indirect and long acting agonists that are organophosphates used for chemical warfare
Tabun
Sarin
Soman
The prototype muscarinic blocker, which has an active isomer of L-hyoscyamine, responsible for GI antispasmodic activity. This is extracted in alkaloids like the deadly nightshade (Atropa belladonna) and jimsonweed (Datura stramonium). It is used for ophthalmoscopic examination, as organophosphate poisoning antidote, and for bradycardia.
Atropine
This is a muscarinic blocker also known as hyoscine, an alkaloid from henbane (Hyoscyamus niger). It is used to prevent motion sickness, administered via transdermal patches
Scopolamine
These are muscarinic blockers that are atropine analogs used in ophthalmoscopic examination with less systemic effects than atropine
Homatropine, Cyclopentolate, Tropicamide
These are muscarinic blockers, specifically of M3 receptors for bronchodilation. They are quaternary derivative of atropine and has a more peripheral effect on the lungs and is thereby used for asthma
Ipratropium and tiotropium
This is a muscarinic blocker used as a treatment for peptic ulcer
Pirenzepine
These are muscarinic blockers used for Parkinson’s disease
Benztropine, Trihexyphenidyl, Biperiden
These are muscarinic blockers used for overactive bladder, wherein the patient frequently urinates
Darifenacin, Fesoterodine, Oxybutynin (specifically), Solifenacin, Tolterodine, Trospium Chloride
These are other drugs used that block muscarinic receptors
Antihistamines
Antipsychotics
TCAs (imipramine and clomipramine)
A ganglionic blocker from Nicotiana tabacum that initially stimulates then blocks ganglia
Nicotine
Ganglionic blockers that block the ganglia without prior stimulation. These are used to treat hypertension before, but is no longer used due to lack of selectivity
Hexamethoium, Mecamylamine, Trimethaphan
A ganglionic blocker from Indian tobacco (Lobelia inflata) that initially stimulates then blocks ganglia
Lobeline
These are non-depolorazing, competitive, and reversible neuromuscular blockers that have isoquinoline in their structure. At a low dose, they competitively block ACh at the receptor without stimulating it. At high doses, they block the ion channels, which are no longer reversed by AChE inhibitors
Atracurium
Tubocurarine
These are non-depolorazing, competitive, and reversible neuromuscular blockers that have steroids in their structure. At a low dose, they competitively block ACh at the receptor without stimulating it. At high doses, they block the ion channels, which are no longer reversed by AChE inhibitors
Pancuronium
Rocuronium
It is a depolorazing, non-competitive, and irreversible neuromuscular blocker that depolarizes (seen as transient fasciculations) then repolarizes (seen as flaccid paralysis) and is more resistant AChE. It facilitates intubation for mechanical ventilation and as a muscle relaxant during surgery. It is very notorious for causing malignant hyperthermia (Type B ADR) with anesthetic agents
Succinylcholine/ Suxamethonium
This is a drug used to inhibit the storage of ACh
Vesamicol
This drug is used to inhibit the release of ACh
Botulinum toxin
This causes the excessive release of ACh
Spider venom
This drug is used to inhibit the uptake of choline in the cell
Hemicholinium
