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59 Cards in this Set

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___________ is the neurotrasmitter for the entire parasympathetic nervous system (ganglion and effector) and is the neurotrasmitter at the ganglion of the sympathetic nervous system, the adrenal medulla and sweat glands also some nuerons in CNS and somatic nerves in skeletal muscle
ACH
____________ is the NT at the effector in the sympathetic nervous system
norepi
__________ amines can be absorbed in the stomach, ________ amines cannot.
tertiary

quaternary
Parasympathetic Effects (Rest and Digest) of ach?
Eye: Contraction to give miosis and near vision
Salivary Glands: Secretion
Heart: Decreased HR, conduction velocity, contraction
Lungs: Bronchoconstriction
Pancreas: Increased insulin secretion
Intestine: Increased Motility and tone
Bladder: Sphincter relaxation and Detrosor contraction
_____________ are blocked by the nueromuscular blockers/muscle relaxants
Nicotinic Receptors
_____________ are blocked by the anticholigergic drugs
Muscarinic receptors
NMB's increase _________ neurotransmission but not change the __________ neurotransmission
nicotinic

muscarinic
For Alzheimer's use _________. why?
Physostigmine

lipophylic and can cross BBB
___________ is the only anticholinesterase not charged in the free base form.
Physostigmine
All anticholinesterases have carbamates except ____________.
Edrophonium
____________ binds within the active site because of it’s charge.
Edrophonium
2 insecticides?
malathion (organophosphate)

sevin
Catalytic triad?
Serine
Histadine
Glutamic acid
The __________ does the chemistry on the ester bond on the carbamate.

The chemistry happens on the _______.
catalytic triad

serine
_________ has a ring structure and is more lipophyllic …..helps orientation
Histadine
the _______ is negative, and our compounds are positive
triad
____________ binding is what places ester in correct site to form covalent bond with serine
Quaternary amine
__________ attacks ach and creates a covalent bond between the ________ of the serine and the _______ of the ester.
Acetylcholinesterase

oxygen

carbon
__________ forms strong electrostatic and hydrogen bonds with the enzyme.
Edrophonium
_______ AND _______ form covalent bond to the carbamate carbon of the enzyme
Neostigmine/Pyridostigmine
Organophosphate derivatives go through process called _______ and form irreversible bonds. (covalent bonds)
aging
there is no chemistry with?
edrophonium
Used to treat Myasthnia gravis – auto immune (destroys receptors)?
neostigmine
anti-Ach reversible mech's?
2 hydrolysis steps(ester first, amide second-takes longer….can’t interact w/ ach, this is what causes the reversal) for the reversibles
Losing an R group is ________. You could reverse after one aging, but not after two. (suicide inhibition)
aging
_________ only has one OR group so, it’s dead after one aging
Sarin
_________ can reverse complete block
no dosage
if too soon, will make the condition worse. why?
This may be that excess Ach causes desensitization like that observed for depolarizing muscle relaxants
Plasma concentrations quickly peak followed by a rapid decrease in concentration.

which ones?
all
absorption-
Poor from gut and across membranes since most are not lipophylic (exception is ________.)
physostigmine and organophosphates
Vd is?
more than would be expected

.7-1.4
metabolism?
50% neostigmine/30%edrophonium/25%pyridostigmine
Physostigmine hydrolyzed by plasma esterases
Elimination
T1/2 ~ 1-2 hr
Clearance greater than _______
glomular filtration rate
This volume of distribution is ________. Compare to 0.2 to 0.4 for the muscle relaxants. Suggested than must be stored in liver and kidneys but not peripheral tissues
large
Hepatic metabolism is _______.
minor
Fastest Onset is _________?
Edrophonium
Since kinetics nearly equivalent, shows potency difference in affinity for ________.
enzyme
Duration of Action
Parallel with disappearance from plasma
Nearly the same for all compounds
25-50% due to hepatic metabolism
50-75% due to renal clearance
Physostigmine metabolized by plasma esterases
Can be adjusted by dosage
0.043 mg/Kg neostigmine~0.21 mg/Kg pyridostigmine~0.5 mg/Kg edrophonium
Can potentiate a Neuromuscular blockade
__________ can prolong duration
Liver or renal disease
To increase duration of action, can __________ but must be careful
give a larger dose
Succinylcholine activity prolongs because?
So much acetylcholine that increase the initially depolarization and also inhibit psuedocholinesterase activity which is somewhat responsible for elimination of some the neuromuscular blockers (neostigmine and somewhat pyridostigmine can do this and edrophonium has very little anti-psuedocholinesterase activity). Example- mivacurium is metabolised by the psuedocholinesterase. If give neostigmine, the metabolism of mivacuirium is slowed a bit but the reversal still proceeds.
factors affecting time to recovery?
Choice/dosage of the inhibitor
The muscle relaxant being reversed
Extent of blockade at time of reversal
Side Effects, Cholinesterase Inhibitors also effect:
Cardiovascular Muscarinic Receptors
Vagal-like bradychardia to sinus arrest
Pulmonary Muscarinic Receptors
Bronchospasm and increased secreations
Cerebral Muscarinic and Nicotinic Receptors
Physostigmine
Diffuse Activation
Gastrointestinal Muscarinic Receptors
Increase paristaltic and gladular secretions
Perioperative bowel anastomotic leakage
Nausea and Vomiting
Can be used to antagonize the parasympathomimetic effects (muscarinic)?
Atropine/Glycopyrrolate

myesthenia gravis
When we increase ________ we are increasing duration
dosage
Atropine/glycopyrolate=?
antimuscarinic
Atropine has a _______ onset than glycopyrolate, hence they are paired with other agents based on onset.
faster
Neostigmine structure?
Carbamate*
Quat. amine
Pyridostigmin structure
Carbamate
Quat. amine
Edrophonium structure
Quat. amine
Physostigmine structure
Carbamate
Tert. amine
1 non carbamate?
Edrophonium
can cross BBB?
Physostigmine
anticholinergic for Pyridostigmine
0.05 mg glycopyrrolate**
anticholinergic with neostigmine
0.2 mg glycopyrrolate
Pregnancy: atropine for fetal bradycardia
anticholinergic for Edrophonium
0.014 mg atropine**
0.007 mg
(must be given early)
anticholinergic for Physostigmine
Infrequently needed but should have avail.
other uses for neostigmine?
Myasthenia Gravis
Urinary Bladder Atony
Paralytic ileus
Intrathecal anesthesia
other uses for Physostigmine
Central Anticholin. Toxicity
(atropine/scopolamine)
Reverse CNS depression
(benzo’s/volatiles)
Prevent postop. Shivering