Pharm 10: Cholinergic Pharm Flashcards
Muscarinic acetylcholine receptor type and location
G-protein
All parasympathetics, few sympathetics, CNS
Nicotinic Acetylcholine receptor type and location
Ligand gated
Post synaptic in excitatory ANS
Presynaptic in CNS
Acetylcholine synthesis _____+______= acetylcholine
what enzyme?
Acetyl CoA+ Choline
Choline acetyltransferase
How does choline get into neuron
NA+/Choline co-transporter
How does choline get into vesicle
AcH/H+ cotransporter
Hemicholinium-3 mechanism
Stops choline from entering the neuron (inhibits Na+/Choline transporter)
AcH can’t be synthesised
Anticholinergic
Vesamicol mechanism
Inhibits H+/ACh antiporter meaning AcH can’t get into vesicle
Anticholinergic
Muscarinic receptor type
G-protein coupled
Nicotinic receptor type
Ligand-gated ion channel
Muscarinic M1 Receptor location and response
Autonomic ganglia/CNS
Arousal, analgesia, late excitatory postsynaptic potential
Muscarinic M2 receptor location and response
Heart
Decreased conductivity, conduction velocity and contractility
Muscarinic M3 receptor location and response
Smooth muscle, contraction
Muscarinic M4 location and response
CNS
Presynaptic autoreceptor. Feedback inhibittion to suppress ACh release
Nicotinic Nm receptor location and response
Skeletal muscle neuromuscular junction
Depolarization and muscle contraction
Nicotinc Nn receptor location response
Autonomic ganglia, adrenal medulla, CNS
Depolarization of postganglionic neuron, catecholamine secretion, arousal/attention/analgesia
Ach is degraded by
AChE acetylcholinestarese
BuChE psyedocholinesterase
Hexamethonium MOA
antagonizes AcH causing rapid tetanic fade
Atropine MOA
antimuscarinic agent resulting in vagal blockade and subsequent tachycardia
Methacholine MOA and use
Muscarinic receptor agonist… used to diagnose asthma and as a vagomemetic
Reticular activating system
Cholinergic neurons that keep you awake
Benadryl make u sleeypy
Pirenzipine use
Muscarinic M2/M3 blockade
Decreased GI motility for some reason
Physostigmine MOA and use
AChE inhibitor
Used for anticholinergic overdoses
Neostigmine MOA and use
AChE inhibitor
Used for GI motility, glaucoma
Edrophonium MOA and use
Rapid and reversible AChE blocker
Used to diagnose myasthenia gravis
Pralidoxime MOA
Binds to organophosphate deactivated AChE
antidote
Chronic myasthenia gravis treatments
long acting AChE inhibitors
pyirdostigmine, neostigmine
Why is physostigmine used for anticholinergic poisoning
CNS penetrance
Drugs used for alzheimers
Donepezil, rivastigmine, galantamine
Which alzeheimers drugs can also treat parkinsons
Rivastigmine
Carbachol MOA and use
Muscarinic agonist
used for glaucoma
Bethanechol MOA and used
Muscarinic agonist. Used to promote GI/urinary motility
Pilocarpine MOA and use
Miotic and saliva producing agent
Cevilimine MOA and use
M1/M3 agonist for xerostomia in Sjörgen syndrome
Succynicholine
THE S U C C
depolarizing blockade of nicotinic receptors
Scopalamine use and MOA
Muscarinic antagonist
used for motion sickness
Methscopolamine and glycopyrrolate
Quaternary amine antimuscarinics used to decrease GI spasms and oral secretions
Glycoporrolate also prevents bradycardia (atropine pre medication style)
Ipatropium MOA
Muscarinic antagonist
Non depolarizing agents
Veccoronium
Pancoronium
Roccoronium
Non depolarizing antidote MOA
Sugammadex
forms complexes with vecc/rocc
Benzotropine and Trihexyphenidyl MOA and use
M1 receptor antagonists. Balances dopamine with ACh
Good for parkinsons
Ipatroprium receptor
M3
