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Test 2 Pharm and Physiology for Anesthesia
Acetylcholinesterase Inhibitors
51
Pharmacology
Graduate
10/18/2014

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Cards

Term
give an example of the difference between the direct and indirect cholinergic?
Definition
a indirect cholinergic will cause AcH to be made or released while a direct cholinergic will be AcH or act like AcH.
Term
If you stimulate the PNS what will it do to the lungs? 2x thigns
Definition
bronchoconstriction and increase secretions
Term
does the PNS increase or decrease sweat glands?
Definition
increase sweat
Term
What does the PNS do to the pancreas
Definition
increase insulin (PNS IS EATING/POOPING/PEEING so you need insulin to help with digestion).
Term
What does the PNS do to the endothelium? Via what molecule?
Definition
causes smooth muscle dilation via NO release
Term
How many domains does a G protein have?
Definition
seven domains
Term
Which M receptors use phospholipase C and that stimulation results in?
Definition
M1,3,5 stimulates phospholipase C which results in increase Ca movement.
Term
M2 and M4 receptors do what?
Definition
inhibit adenylcyclase, K loss, and decrease in cAMP.
Term
What type of enzyme is acetylcholinesterase?
Definition
a type b carboxylesterase enzyme
Term
Describe the anatomy of an acetylcholinesterase enzyme and how is does its job of hydrolyzing AcH
Definition
Acetylcholinesterase enzyme is made up of two subunits one is known as anionic site and the other esteric site. The anionic site binds cations such as the amine part of AcH. At the esteric site the enzyme binds to the ester part of AcH and does the work to hydrolyze it.
Term
what part of the acetylcholinesterase enzyme does our anticholinesterases bind to to inhibit?
Definition
they bind to the esteric spot b/c it binds to the ester part of AcH and does the hydrolyzing.
Term
To treat glaucoma do we want more AcH or less?
Definition
We want more! So we treat with anticholinergics
Term
where are true acetylcholinesterase found?? 3x
Definition
1. RBCs
2. NMJ
3. Neuronal synapses
Term
Does pseudocholinesterase or true cholinesterase deactivate M and N Receptors?
Definition
TRUE!! Plasma (pseudo) cholinesterase does even hang out near the junction.
Term
What is sjogren's syndrome? How do we treat it?
Definition
an auto immune disease that attacks your exocrine glands so you can sweat or produce tears. We treat with parasympathometic drugs which act on muscarnic receptors to help produce tears and saliva.
Term
Which acetylcholinesterase inhibitor is reversible and acts on anionic and esteric site
Definition
edrophonium acts on the anionic and esteric site and is reversible.
Term
what acetylcholinesterase inhibitor is not reversible?
Definition
echothiophate
Term
max dose of neostigmine is
Definition
5 mg
Term
cholinergic stimulation results in the following sx
Definition
1. diarrhea, 2. urination 3. miosis 4. bradycardia 5. bronchospasms 6. emesis 7. lacrimation 8. emesis 9. salivartion/secretion/sweating
Term
why at large doses does an AcHe inhibitor cause a neuromuscular block?>
Definition
at high doses it causes excess AcH buildup which desensitizes the receptors on the motor end plate and can cause a block in itself or contribute to a channel block
Term
which AcHe Inibitor crosses the blood borne barrier? Where is its primary metabolism?
Definition
physostigmine, 90% metabolized by liver. can help with postop shivering and angalgeia similar to demerol.
Term
Describe neostigmine.
peak, DOA, contraindications, clearance, metabolized, what anticholinergic do you give with?
Definition
does not cross BBB, peaks in 5-10 minutes, 80% cleared by kidneys, metabolized in liver, helps with post op shivering, contraindicted for pts with mechanical intestinal or urinary obstructions and peritonitis. Couples with glycopyrrolate. treats true cholinesterase
Term
Describe Pyridostigmine
peak, DOA, contraindications, clearance, metabolized, what anticholinergic do you give with?
Definition
does not cross BBB, 75% renal clearance, depresses True cholinesterase, contraindicated with pts who have intestinal or urinary obstruction,
Term
describe edrophonium
peak, DOA, contraindications, clearance, metabolized, what anticholinergic do you give with?
Definition
Fastest onset with 1-2 minutes, couple with atropine, 75% renal clearance, DOES NOT DEPRESS plasma cholinesterase, does not cross BBB, does not treat anticholinergic syndrome, most commond to be associated with arrythmias
Term
which AcHe inhibitor is most often associated with arrhythmias
Definition
edrophonium
Term
which AcHe Inhibitor is used to differenitiate between MG and anticholinesterase OD
Definition
edrophonium
Term
By giving Edrophonium what will happen to the following patients:
1. MG
2. AcH crisis patient
3. Lambert Eaton Myasthenic syndrome
Definition
1. MG: Will make their Sx better. Less muscle weakness
2. AcH crisis: Makes it worse by adding more AcH and causing desensitization and possible depolariztion / block.
3. Lambert Eaton: No change.
Term
Which AcHe inhibitor is an organophosphate
Definition
echothiophate
Term
Which AcHe Inhibtor causes severe plasma cholinesterase inhibition
Definition
echothiophate
Term
what is the dose of edrophonium
Definition
1mg / kg
Term
what is recurarization
Definition
When the inhibotor is cleared faster than the NDMB then a reblock occurs.
Term
What structure of AcHe inhibitors contributes to their ability to cross the BBB
Definition
tertiary amines.
Term
for renal failure patients which drug is the wrose because it is least cleared by the liver?
Definition
pyridostigmine.
Term
what is the dose of glycopyrrolate?
Definition
0.2 mg/
Term
generally contraindications for AcHe Inhibitors is? 4x
Definition
1. gastric obstruction
2. urinary tract obstruction
3. asthma
4. peptic ulcers.
Term
what muscle is responsible for enlarging the airway..it is greatly weakened by blockers.
Definition
genioglossus muscle
Term
list in order which muscle recovers first from a block..
adductor policis, diagphram and facial muscle
Definition
Facial muscle first, then diagphram then adductor policis.
Term
cholinergic crisis results from? Describe Sx,
Definition
from large amounts of AcH, results in ANS control, weakness to paralysis at muscles b/c of desensitziation from excess AcH, also CNS effects of dysphoria, confusion, ataxia, coma
Term
Treatment for cholinergic crisis
Definition
atropine b/c you need to give something that can cross the BBB, diazpam for seizures related to excess AcH in brain, and pralidoxime which reactivates acetylcholinesterase.
Term
which Muscle relaxant is not as effective with myasthenia gravis. Why
Definition
Sux, b/c there are less receptors due to T-cells killing nicotinic receptors.
Term
what is the drug used to diagnose Myastehnia gravis
Definition
endrophonium
Term
name the drug used to deferentiate myasthenia gravis from cholinergic crisis
Definition
endrophonium
Term
name two drugs to treat myastehnia gravis
Definition
neostigmine and pyridostimgine. neither cross BBB. Both are anti-cholinesterase. means more AcH and more parasympathetic.
Term
"Fixo-stigmine" is another nick name for? used for?
Definition
name for physostigmine, used to treat atropine overdose. Crosses BBB.
Term
echoth I ophate treats? What kind of drug is it?
Definition
glaucoma!! STRESS THE "I" = eye. Its a anticholinesterase
Term
Drug for alzheimers b/c I DONT remember anything..what kind of drug is it?
Definition
Don-epezil. An anticholinesterase. I "DONT" remember anhything
Term
Which M receptor is primary brain
Definition
M1. #1 most important organ = brain. so 1. Also M1 does enteric nervous system.
Term
which m receptor is heart
Definition
M2. B/c after your brain the #2 most important organ = heart = 2.
Term
What M receptor for bladder constriction exocrine, gut motility accommodation and bronchoconstriction?
Definition
M3. M3 is everything else in the body. M4 and M5 aren't that important.
Term
you treat parkinsons disease with what class of drug
Definition
anti-cholinergic. PARK YOUR "BENZ". Benztropine.
Term
i pray i breath... what drug does this pertain to? what type of drug?
Definition
ipratropium. I-PRA-Tropium. An anticholinergic. Safe to give to a asthmatic and COPD pt to bronchodilate without a lot of secretions.
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