Cholinomimetics Flashcards
M1 receptor organs
Nerve, CNS
M2 receptor organs
Heart and smooth muscle
M3 receptor organs
Endothelium, bladder GI, eye
M1 receptor and 2nd messenger
Gq
IP3 DAG
M2 receptor and 2nd messenger
Gi
dec cAMP
M3 receptor and 2nd messenger
Gq IP3 DAG
Nicotinic receptor organs
NMJ, Skeletal ms, adrenal glands, autonomic ganglia
Direct acting acetylcholine receptor agonists (2)
Esters
Alkaloids
Indirect acting binding to acetylcholinesterase (2)
Reversible
Irreversible
Muscarinic agonist, negligible nicotinic effect
Bethanecol
Muscarinic agonist for all receptors for post op ileus and urinary retention
Bethanecol
Muscarinic and nicotinic agonist for glaucoma
Carbachol
Bethanecol and carbachol SE
bronchospasm
mydriasis
Partial muscarinic agonist for Glaucoma and Sjogrens
Pilocarpine
Direct acting muscarinic agonist For asthma testing
Methacoline
Methacoline SE
PUD, bronchospasm
Agonist at Nn & Nm receptors activating sympathetic and parasympathetic effects
Nicotine
Selective nicotinic partial agonist for smoking
Varenicline
Acetylcholinesterase inhibitor with short duration of action for DX of myesthenic and cholinergic crisis
Endrophonium
Other name endrophonium
Tensilon test
Covalently bonds to acetylcholinesterase to hydrolyze and release Ach but with longer acting effect for myesthenia gravis
Neostigmine
Acetylcholinesterase inhibitor also used for post operative neurogenic ileus, urinary retention and antagonist for NM blockade drugs
Neostigmine
Longer acting 4-6h anticholinesterase for MG
Pyridostigmine
Alkaloid anticholinesterase that can cross BBB
Physostigmine
Why can physostigmine cross BBB and the 3 others can’t
It is a tertiary amine while
others are quarternary
Anticholinesterase inhibitors that can enter CNS but also treats glaucoma
Echothiophate
Causes excessive muscarinic and nicotinic sx
Organophosphates (malathione, parathion, sarin)
Regenerates acetylcholineste at NMJ relieves peripheral sx of organophosphate tox but cannot cross BBB
Pralidoxime
Organophosphate poisoning antidote that crosses BBB
Atropine
Organophosphate toxicity (sx)
DUMBBELS
Acetylcholinesterase inhibitors used for Alzheimer (3)
Donapezil
Rivastigmine
Galantamine
Acetylcholinesterase given as patch for Alzheimers
Rivastigmine
