Term
4 most important reasons why acetylcholinesterase inhibitors are important:
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Definition
Myasthemia gravis Alzheimer’s disease Insecticides Chemical weapons |
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Term
process by which acetylcholinesterase works
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Definition
1)Cleaves by acetylation. (choline biproduct)
2)Rapid hydrolysis- Binds covalently (acetate biproduct |
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Term
what does acetylcholine esterace produce from the inactivation of acetylcholine
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Definition
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Term
Edrophonium theraputic use
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Definition
diagnosis of myastheula gravis (not treatment) competative inhibitor so short duration of action
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Term
physostigmine theraputic use
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Definition
use: to treat overdose of drugs such as antidepressants MOA: inhibits acetylcholine esterase in muscarinic effector junctions in heart, brain, muscle. |
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Term
isoflurophate (diisoprpylflurophosphate) therapeutic use:
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Definition
Insectiside and nerve gas MOA:covalently binds Organophosphate so is irrversible and has a long duration of action
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Term
Echothiophate therapeutic use:
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Definition
use: glaucoma MOA: covalent binding class: organphosphate half life is 100 hours
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Term
organophosphate insecticides |
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Definition
Parathion- occupatuional suicide prodrugs (farming insecticides) (P is the human posion) Malathion - cleavage of these ester bonds by carboxylesterase will inactivate the drug. This makes it safe for humans. It has selective toxicity for insects only because they do not have carboxylesterases. It is also not safe for fish or birds Malathion is used to kill lice and eggs |
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Term
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Definition
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Term
AchE inhibitor effect on neuromuscular junctions
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Definition
low doses- increase force if contraction High doses- You will see neuromuscular blockade. (same effect as lots of Ach in synapse |
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Term
myasthenia Gravis symptoms
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Definition
muscle weakness starting in small muscles then progressing to larger muscles and respiratory muscles Episodic symptoms
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Term
Neostigmine pyridostigmine? Ambenonium ?
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Definition
use: treatment of myasthenia gravis duration of action 1-2hrs, 3-6hrs, 4-8 hrs(respectably)
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Term
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Definition
early: memory loss (anteriograde) no longterm new memories middle: disorientation, confusion late: bed ridden
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Term
Alzheimers effects on the brain
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Definition
Widespread degeneration of the brain (hippocampus, cortex) beta amyloid plaque- extracellular dying neurons due to abnormal protein prduction form a normal protein neurofibrillary tangles-intracellular proteins become hyperphosphorylated |
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Term
Donepezil therapeutic use
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Definition
Donepezil (aracept) - is a competative antagonist and has a half life of about 70 hours use: Alzheimer's disease |
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Term
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Definition
use: Alzheimer's disease
is a carbamate and has a half life of about 10 hrs |
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Term
efficacy of alzheimer's drugs
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Definition
1) -they have kept patients out of nursing homes for about 6 months on average 2) Do they delay progression of the disease- NO 3)Treat the family Peripheral side effects due to activation of muscarinic receptors |
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Term
most adverse effects of Alzheimers drugs
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Definition
nausea, diarrhea, vommiting -these are drugs that you will feel side effects on also salvation and sweating
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Term
toxicity of AChE inhibitors on eye
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Definition
causes pupillary constriction, accomadation
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Term
toxicity of AChE inhibitors on GI
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Definition
causes nausea, diarrhea, vommiting
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Term
toxicity of AChE inhibitors on respiratory system |
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Definition
bronchioconstriction and mucus secretion
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Term
toxicity of AChE inhibitors on skeletal muscle |
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Definition
causes fasiculatio- depolarizing blockade |
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Term
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Definition
1) atropine (used to inject in the thigh)
2) pralidoxime
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