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24 Cards in this Set

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  • Back
where is acetylcholine synthesized and by which enzyme?
in the nerve terminals, by choline acetyltransferase ( joins acetylcoenzyme A and choline)
How is acetylcholine metabolized?
hydrolysis by acetylcholinesterase into acetate and choline
where are the acetylcholine receptors found?
entire paracsympathetic nervous system, parts of the sympathetic nervous system ( sympathetic ganglions, and adrenal medulla and some sweat glands), some CNS, skeletal muscle
what are the two types of cholinergic receptors?
Muscarinic and nicotinic
where are the muscarinic receptors found?
endo organ effector cells in bronchial smooth muscle, salivary glands, and the SA node, some CNS
where are the nicotinic receptors found?
skeletal muscle and the autonomic ganglia
what is the goal of reversal of neuromuscular blockade?
Maximize nicotinic transmission and minimize muscarinic side effects
what is the function of cholinesterase inhibitors?
inactivate acetylcholinesterase by reversibly binding to the enzyme and indirectly increasing the amount of acetylcholine to compete w/ nondepolarizers.
What are organophosphates?
cholinesterase inhibitors that for stable, irreversible bonds w/ the enzyme
Effect of acetylcholinesterase blockers on succinylcholine?
Potentiation of block, due to and increase of acetylcholine and inhibition of pseydocholinesterase activity .
what is the effect of cholinesterase inhibitors at sites other than skeletal muscle?
CV- bradycardia
Pulmonary - bronchospasm, increased secretions
GI - diarrhea, increased peristalsis
CNS - diffuse excitation
GU - increased bladder tone
Ophto - pupillary constriction
How many min after a palpable post0tetanic twitch does the first TOF appear for vec? for panc?
about 10 min for vec and about 40 for panc
Neostigmine, structure
carbamate moiety and a quaternary ammonium group, enables covalent bonding
Does Neostigmine pass through the blood brain barrier?
No
Neostigmine dosage?
0.08 mg/ kg ( up to 5 mg in adults)
When does the effect of neostigmine peak?
at 10 - 15 min
Does neostigmine cross the placenta?
Yes, can cause fetal bradycardia. For this reason it's better to reverse w/ atropine if using neo
How potent is pyridostimine vs. neostigmine?
Pyridostigmine is about 20% as potent as neostigmine
dosage for pyridostimine?
0.4 mg/kg (a total of 20 mg in adults)
Onset of action for pyridostimine
slower than neostigmine, about 10-20 min.
Edrophonium, how does it bind to acetylcholinesterase?
Non-covalent bonding, shorter acting
Edrophonium dosage
0.5-1 mg/kg , it's less than 10 % as potent as neostigmine
Edrophonium onset of action
rapid, 1-2 min
what is physostigmine commonly used for?
treatment of central anticholinergic toxicity, because it freely passes the blood brain barrier
prevention of post-op shivering
reversal of benzo-induced delirium