Cholinergic Agonist Flashcards
Bethanechol
Urecholine. Lax nicotinic action and directly stimulates muscarinic receptors causing increased intestinal motility and tone stimulates the detrusor muscle bladder relaxes trigone and sphincter produces urination.
Acetylcholine
Miochol-E. Decrease in heart rate and cardiac output. Decrease in blood pressure by vasodilation. Acetylcholine activate M3 receptors found in endothelial cells lining blood vessels. Increases salivary secretions stimulates intestinal secretions and motility and answers bronchiolar secretion involved and stimulation of ciliary muscle contraction for near vision and constriction of pupillae sphincter muscle.
Carbachol
Miostat/isopto carbochol. Both muscarinic and nicotinic actions. First stimulates cardiovascular and G.I. system then depresses them. Can cause release of norepinephrine and epinephrine from adrenal Medulla by its nicotinic action. Used in the eye as a miotic agent to treat glaucoma by decreasing intraocular pressure
Pilocarpine
Salagen/isopto carpine. Similar to acetylcholine but is stable to hydrolysis by acetylcholinesterase. far less potent than acetylcholine but can penetrate the CNS. Produces rapid miosis. Potent stimulator of sweat tears and saliva. Used to treat glaucoma.
Indirect acting cholinergic agonist: anticholinesterase agents (reversible)
Prevent degradation of acetylcholine by inhibiting acetylcholinesterase
Edrophonium
Enlon. Short acting acetylcholine esterase inhibitor. Find reversibly to the active center of acetylcholine esterase preventing hydrolysis of acetylcholine. Works for 10 to 20 minutes
Physostigmine
Antilirium. Forms carbamolated intermediate with the enzyme becomes reversibly inactivated. Stimulates not only muscarinic and nicotinic sides of ANS but also nicotinic receptors of the NMJ. Can stimulate cholinergic sites in the CNS. Increases intestinal bladder motility and used in the treatment of overdoses of drugs with anti-cholinergic actions such as atropine.
Nestigmine
Prostigmin. Similar to physostigmine but is more polar and poorly absorbed in G.I. tract and does not enter the CNS. Stimulates bladder and G.I. tract also used as an antidote for competitive neuromuscular blocking agents used to manage symptoms of myasthenia Gravis.
Pyridiostigmine and ambenonium.
Mestinon,mytelase. Cholinesterase inhibitor’s that are used for chronic management of myasthenia gravis
Tarcine,donepezil,rivastigmine, galantamine
No name, aricept, exelon, razadyne. Patients with Alzheimer’s deficiency of cholinergic neurons in the CNS. Highly polar anti-cholinesterase is are used as remedies for loss of cognitive function.
Indirect acting cholinergic agonist. anti-cholinesterase agents (irreversible).
By covalently to acetylcholinesterase. Results and long-lasting increase of acetylcholine at sites were released. Extremely toxic. Used as insecticides
Echothiophate.
Phospholine iodide. organo phosphate Covalently binds to phosphate group at active site of acetylcholinesterase. Once this occurs enzyme is permanently and activated and restoration of acetylcholine esterase require synthesis of new enzyme molecules. Cause paralysis of motor function breathing difficulties and convulsions atropine and I dose is going reverse many of effects. Topical solution can be used for glaucoma
Pralidoxime
Protopam. Reactivates acetylcholinesterase however is unable to penetrate into CNS
cevimeline
evoxac
