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Cholinergic system (agonists and antagonists) - Coggle Diagram
Cholinergic system (agonists and antagonists)
Cholinolytics (Antagonists)
Nicotinic Antagonists
Gangilonic blocking agents ( block nicotonic receptors on synapse of both sympathetic and parasympathetic ganglia)
Snake Toxin
Irreversible blocking of cholinergic transmission = death.
Skeletal neromuscular blocking agents (Block nicotinic receptors on skeletal muscle)
First found Curare but it causes paralysis *block Ach signals to muscles
First drugs
Decamethonium
Long lasting, side effect heart
Suxamethonium
esters incorporated so short acting. side effect autonomic ganglia > not selective to neromuscular junction
Second drug
Atracurium
Lacks caradic side effects
Muscarinic Antagonists
First drugs (not charged, can cross BBB affect CNS)
Atropine
(decrease GIT Motility) (Antidote for anticholinesterase by blocking receptor sites for the antis on the esterse)
Hyoscine (Scopolamine
Tiotropium bromide (derivative)
Long acting 24 hours bronchodilator hydrophilic have no central effect
Second drugs (charged)
Atropinemethonitrate (lower GIT motility)
Ipratropium (bronchodilator) anti asthma
Cholinomimetics (Agonists)
Indirect: Anticholinestrases ( AChEs)
Irreversible long acting organophosphorus compounds
Reversible Short acting Carbamates
Better drugs
Neostigmine
Pyridostigmine
Physostigmine for glaucoma
Dangerous can cross BBB effect CNS
Nicotinic agonist
Modification of choline ester
Carbachol
Nicotine
Muscarinic agonists
Direct acting alkaloids
Muscarine
Pilocarpine for glaucoma
Modification of choline ester (analouges)
Carbachol
(Long acting, resistant to hydrolysis because CH3 of ester will be replaced by NH2
Methacholine
Increased stability but decreased activity
Beethanechol
very Stable and oraaly active + Selective to muscaniric