Cholinergic Pharmacology Flashcards
Used for the treatment of bladder and bowel atony (post-surgery or spinal cord injury)
Betanechol
M3 receptor agonist
Direct-acting muscarinic agonists
Bethanechol
Pilocarpine
Muscarine
MOA of Bethanechol
Activates muscarinic receptors; increases IP3 and DAG
Used for Sjogren’s syndrome (increases salivation); was used in glaucoma (causes ciliary muscle contraction, opening or trabecular meshwork, increased outflow)
Pilocarpine
M3 receptor agonist
Triad of Sjogren Syndrome
Xerostomia
Xerophthalmia
Rheumatoid arthritis
Alkaloid found in mushrooms; causes mushroom poisoning of fast-onset type
Muscarine
Used for smoking cessation
Nicotine
Varenicline
Indirect-acting cholinomimetic (alcohol)
Edrophonium
Shortest-acting cholinesterase inhibitor
Direct-acting nicotinic agonists
Nicotine
Varenicline
Succinylcholine
MOA of edrophonium
Inhibitor of cholinesterase; amplifier of endogenously released ACh
Indications of edrophonium
Reversal of Nm block by nondepolarizing drugs; diagnosis of myasthenia gravis (Tensilon test)
Indirect-acting cholinomimetic (organophosphates)
Insecticides:
Parathion
Malathion
Sarin
Tabun
Indirect acting cholinomimetic (carbamates)
Neostigmime
Pyridostigmine
Physostigmine
Indirect-acting cholinomimetic (for Alzheimer’s)
Rivastigmine
Galantamine
Donepezil
Tacrine (obsolete)
Indirect-acting cholinomimetics
Edrophonium Neostigmine Pyridostigmine Physostigmine Rivastigmine Galantamine Donepezil Tacrine
Used for the treatment of myasthenia gravis
Neostigmine
(Indirect-acting cholinomimetic)
Others:
Pyridostigmine
Physostigmine
Indirect-acting cholinomimetic used for the treatment of glaucoma
Physostigmine
Indirect-acting cholinomimetic
Used for the reversal of severe atropine poisoning (IV)
Physostigmine
How is Tensilon test performed?
Edrophonium 2mg is injected via IV after baseline muscle strength has been measured. If no rxn occurs after 45s, an additional 8mg may be injected. If the patient has MG, an improvement that lasts about 5min can usually be observed.
Indirect-acting cholinomimetic used for the treatment of Alzheimer’s disease
Rivastigmine
(Indirect-acting cholinomimetic)
Others:
Galantamine
Donepezil
Tacrine (obsolete)
Antidote for organophosphate poisoning (1st choice)
Atropine
Nonselective muscarinic antagonist
Signs and symptoms of organophosphate poisoning
DUMBBELSS Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation Lacrimation Sweating Salivation
Toxicities of atropine
All parasympatholytic effects plus sedation, delirium, hyperthermia, flushing
MOA of Indirect-acting cholinomimetics
Inhibits acetylcholinesterase; amplifies endogenously released Ach
Antidote for organophosphate poisoning and nerve gas poisoning
Pralidoxime
Cholinesterase regenerator
Muscarinic antagonist used for asthma and COPD
Ipatropium
Tiotropium
Muscarinic antagonist used for Parkinson’s disease
Benztropine
Biperiden
Trihexyphenidyl
Preferred bronchodilator in patients with comorbid COPD and heart disease
Ipatropium
Muscarinic antagonist used for motion sickness
Scopolamine
Contraindications to muscarinic blockers
Infants
Hyperthermia due to decreased sweating
Acute angle-closure glaucoma
BPH
Nondepolarizing neuromuscular blockers
Tubocurarine
Pancuronium
Atracurium
Vecuronium
Depolarizing neuromuscular blockers
Succinylcholine
Chemical antagonist of organophosphates; used for organophosphate poisoning
Pralidoxime
MOA of pralidoxime
Cholinesterase regenerator:
Binds phosphorus of organophosphate; breaks organophosphate bond with cholinesterase
How is pralidoxime given?
Must be administered before 6-8 hours of organophosphate bond with cholinesterase occurs
M1-selective antimuscarinic drugs
Pirenzepine
Telenzepine
Indications of M1-selective antimuscarinic drugs (Pirenzepine, Telenzepine)
Peptic disease
Antinicotinic ganglion blocker; blocks all autonomic effects
Hexamethonium
M3 selective antimuscarinics
Darifenacin
Fesoterodine
Solifenacin
Tolterodine
The most dangerous effect of the antimuscarinic drugs in children and is potentially lethal in infants
Atropine fever
A drug which causes vasodilation that can be blocked by atropine
Bethanechol
Indications of M3-selective antimuscarinics
Urinary urgency; incontinence