Cholinergic Agonists Flashcards
Parasympathomimetics actions (Cholinergic)
Decreases heart rate & CO
Bronchoconstriction , Miosis
Increases GI tract motility +lacrimation + urination
Nicotinic Receptors Types
Muscular/NMJ (Nm) / Ganglionic (Nn)
Muscarinic Receptors Types
M1- Gq (neural , gastric), M2- Gi (cardiac), M3-Gq (glandular/smooth muscle),
Bethanechol Type
Direct Acting Cholinergic Agonist (not hydrolyzed by acetylcholinesterase)
Bethanechol Uses
Urinary Retention
Bethanechol MOA
increases bladder smooth muscle tone
Bethanechol Side Effects
generalized cholinergic stimulation
Carbachol
Direct Acting Cholinergic Agonist (not hydrolyzed by acetylcholinesterase)
Carbachol Uses
Glaucoma
Carbachol MOA.
miosis (Muscarinic & Nicotinic)
Pilocarpine
Direct Acting Cholinergic Agonist (not hydrolyzed by acetylcholinesterase)
Pilocarpine Uses
Glaucoma , Xerostomia
Pilocarpine MOA
miosis , inc. sweat , tears , & saliva (M. effect)
Methacholine
Direct Acting Cholinergic Agonist (doesn’t Cross BBB)
Methacholine MOA
Bronchoconstriction
Methacholine Uses
diagnose bronchial hypersensitivity (Methacholine Challenge Test)
Physostigmine
Indirect acting cholinergic agonist (inhibits AchE)
Physostigmine Uses
Glaucoma (not v effective) , Atropine/tricyclic AD overdoses , used to increase intestinal & bladder motility
Physostigmine Side Effects
Convulsions , bradycardia , skeletal muscle paralysis (high doses)
Neostigmine
Indirect acting cholinergic agonist (inhibits AchE)
Neostigmine Uses
Treats Myasthenia Gravis (greater effect on Nm) , antidote for tubocurarine
Edrophonium
Indirect acting cholinergic agonist (inhibits AchE)
Edrophonium Uses
Diagnosis of MG
Donepezil, Rivastigmine, Galantamine Uses
delay progression of Alzheimer’s
Donepezil, Rivastigmine, Galantamine
Indirect acting cholinergic agonist (inhibit AchE)
Nerve Gaz (sarin)
Indirect Acting Cholinergic Agonists: Irreversible
Nerve Gaz Effects
Respiratory depression
Echothiophate
Indirect Acting Cholinergic Agonists: Irreversible
Echothiophate Uses
Glaucoma
Pralidoxime MOA
Reactivation of inhibited AChE
Pralidoxime Uses
treat organophosphate and pesticide poisoning
Ach Cardiovascular Actions
decreases HR : M2-R (inhibit AC & Ca entry) , Decreases BP : M3-R (nitric oxide= SM relaxation)
Ach GI + Eye actions
Increases salivary secretion & motility
Contraction: colicky pain / expulsion of urine (Tone of muscle is increased) / miosis
Ach Adverse Effects
Diarrhea , nausea , urinary urgency , miosis , diaphoresis
Nicotine Actions
Low doses: stimulation of ganglionic nicotinic receptors → enhancing S (BV) and PS (heart+GI)
High doses: depolarizing blockade of ganglia
Suxamethonium MOA
Depolarizing Nm blocker (agonist)