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Cholinergic
Chapter 9 Pharm
27
Bartending
Undergraduate 4
11/13/2011

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Term
Hemicholinium-3

Vesamicol
Definition
Blocks the Choline/Na+ transporter into the cell and stops ACh synthesis

Blocks the ACh/H+ pump into the vessicles and prevents storage

Both only used in lab
Term
Muscarinic receptors
Definition
G- Proteins located within all Para-symp, CNS, and some sympath

Since these G proteins need to be activated they take time to respond
Term
M2, M4
Definition
Presynaptic- blocks calcium channels and prevents binding of ACh to the presnatic terminal

Postsynaptic- inhibitory and will inhibit adenylyl cyclase which increases intracellular K+ and hyperpolarizes the cell
Term
M1, M3, M5
Definition
Coupled to G proteins which stimulate Phospholipase C, and are excitatory neurons

1/5-CNS (Arousal attention,EPSP)
3-SM (Contractions)
Term
Nicotinic Receptors
Definition
Ligand based, need 2 molecules of ACh to bind to ellict a comformational change.

Allows K and Na ion flow. (Mostly Na into cell)

ACh binds onto Alpha subunits to elicit changes
Term
Desensitied Nicotinic Receptors
Definition
When a nicotinic receptor undergoes contiuned and extended exposure to ACh there will be a "locking of the channel" and ACh will remain bound to the receptor
Term
What are the two types of cholinesterases that break down ACh
Definition
AChE and butyrylcholinesterase BuChE

BuChE may be seen in Alzhemers pathology
Term
What do presynaptic Nm do to upregulate themselves
Definition
They stimulate ACh mobilization of synaptic vessels from the reserve pool to the depot pool
Term
Tetanic Fade
Definition
When over 50% of the nicotinic recepoters are desenitized

Hexamethonium- can cause this by blocking presynape Nm receptors and not allowing facilitation
Term
Slow ESP
Definition
Mediated by M1 receptors
Term
The heart is influenced most by which system when at rest
Definition
Parasympathetic
Term
Atropine
Definition
Blockage of vagal slowing of SA node---> increased heart rate

Muscarinic Antagonist
Term
Botulinum-A (BOTOX)
Definition
degrades SNAP-5 and prevents ACh release by stopping vesicle binding

Used to stop muscle contractions (Torticollis, wrinkles, headaches, pain)
Term
Edrophonium
Definition
ACE inhibitor--- fast and rapid reversable block
Term
Edrophonium
Definition
ACE inhibitor--- fast and rapid reversable block
Term
Physiotigmine
Ambenonium
Endophonium
Pyridostigmine
Neostigmine
Definition
ACE INHIBITORS

Endophonium- used for diagnosis
Neostigmine- used for GI distention
Physostigmine- can cross BBB
Ambenonium/Pyridostigmine/Neostigmine- used for Myasthenia gravis treatment
Term
Tacrine, Doneepezil, Rivastigmine, Galatamine
Definition
AD Treatment

GI Issues
Term
Methacholine
Definition
Asthma diagnosis- muscarinic receptors
Term
Carbachol
Definition
Glaucoma-- constricts pupils, lowers pressure

M agonist
Term
Bethanechol
Definition
GI and Urinary issues

Mus. Agonist
Term
Pilocarpine and Cevimeline
Definition
Treat dry mouth due to Sjorgrens syndrome by increasing salvation
Term
Succinylcholine
Definition
Produces neuromuscuar blockade for surgery
Term
Scopolamine
Definition
prevention of motion sickness, mild sedation, and decrease oral secretions
Term
Pirenzepine, Methscopolamine, Glycopyrrolate
Definition
Peptic Ulcer disease

Prevent bradycardia during surgery--- Glycopyrrolate
Term
Ipratropium, Tiotropium
Definition
COPD treatment, brochiodilator
Term
Oxybutynin, Propantheline, Terodiline, tolterodine, trospium, darifenacin, Solifenacin
Definition
Overactive bladder

Oxy, Pro, Tolt, Tros are nonspecific muscarinic

Darifenacin, Solifenacin are Selective M3 antagonists (cause less dry mouth and constipation)
Term
Mecamylamine and Trimethaphan
Definition
Treat aortic dissection to lower BP and blunt sympathetic reflexes that would normall cause a tear
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