Cholinoceptors Flashcards
DUMBBELLSS
Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Emesis,
Lacrimation, Lethargy, Salivation, Sweating
Mimic the effects of Acetylcholine (ACh)
Cholinomimetics
Bind to and activate nicotinic and/or muscarinic receptors
DIRECT-ACTING CHOLINOMIMETICS
DIRECT-ACTING CHOLINOMIMETICS: CLASSIFICATION
Choline Esters
Cholinomimetic Alkaloids
Cevimeline
Most susceptible to Acetylcholinesterase (AChE)
Acetylcholine
Less susceptible to Acetylcholinesterase (AChE)
Metacholine
Not susceptible to Acetylcholinesterase because of esterification to carbamic acid
Carbachol and Bethanechol
Topical: induction of miosis during ophthalmic surgery as ophthalmic solution
Acetylcholine
Inhalational: diagnosis of bronchial airway hyperactivity in patients who do
not have clinically apparent asthma
Metacholine
Oral: treatment of urinary retention (atonic bladder), prokinetic
Betanechol
Topical: treatment of glaucoma, induction of miosis during surgery as
ophthalmic solution
Carbachol
CHOLINOMIMETIC
ALKALOIDS: SOURCES
• Muscarine: Amanita muscaria
• Pilocarpine: Pilocarpus sp.
• Arecoline: Areca catechu
• Nicotine: Nicotiana tabacum
Agonist
Muscarine
Partial agonist
Pilocarpine
Nicotinic Activity
Nicotine
Muscarinic and Nicotinic Activity:
Arecoline
• Topical: treatment of glaucoma and miotic agent as ophthalmic solution
• Oral: treatment of xerostomia (that follows head and neck radiation
treatments or that is associated with Sjögren syndrome)
Pilocarpine
A quinuclidine derivative of acetylcholine
CEVIMELINE
Bind to and inactivate acetylcholinesterase (and butyrylcholinesterase) and thereby increase ACh
INDIRECT-ACTING CHOLINOMIMETICS
INDIRECT-ACTING CHOLINOMIMETICS: CLASSIFICATION
Covalent Inhibitors
Noncovalent Inhibitors
Noncovalent Inhibitors
Alcohols
Other Noncovalent Inhibitors
Covalent Inhibitors
Organophosphates
Carbamates
Derivatives of phosphoric acid
ORGANOPHOSPHATES
A nucleophile that can break the phosphorus-enzyme bond
PRALIDOXIME
Produce effects opposite to those of ACh
Cholinolytics