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CM - Pharm: Cholinesterase Inhibitors

Terms in this set (10)

cholinesterase
-aka ACh-esterase
-an enzyme that breaks ACh down into acetate + choline to be taken back up by the presynaptic nerve
cholinesterase inhibitors
-aka anti-cholinesterase
-prevent the breakdown of ACh
-increase levels of ACh left in the synaptic cleft
cholinesterase inhibitor toxicity
-ACh is NOT broken down by cholinesterase because it has been inhibited
-this leaves more ACh in the synaptic cleft
-leads to cholinergic syndrome
-characterized by SLUDGE:
*salivation
*lacrimation (over production of tears)
*urination
*defecation
*gastrointestinal upset
*emesis
examples of cholinesterase inhibitor toxicity
chemicals irreversibly bind to cholinesterase and prevent it from working
-organophosphate insecticides
-Novichok
-Sarin gas
Novichok
-placed in Alexi Navalny's underwear
-can be toxic and fatal
-permeates through the skin
symptoms of Novichok / Sarin Gas toxicity
-profuse watering of the eyes
-frothing at the mouth
-profound bradycardia
-diarrhea
-loss of urine control
-death due to build-up of ACh
-continuous firing of motor neurons with seizures and muscle tetany
-diaphragm constantly contracted on inhalation cycle, which thus inhibits exhalation
treatment for cholinesterase inhibition
treat with an anticholinergic that blocks muscarinic receptors
-ex. Atropine
examples of cholinesterase inhibitor benefit
-myasthenia gravis
-Alzheimer's disease
myasthenia gravis
-a chronic autoimmune disease that affects the neuromuscular junction and produces serious weakness of voluntary muscles
-an antibody blocks the nicotinic motor neuron receptors
-neurons can't fire and leads to muscle weakness
-cholinesterase inhibitors will prevent cholinesterase from breaking down ACh, which will leave more ACh in the synaptic cleft in the hopes that this will cause more motor neuron firing
Alzheimer's disease
-an irreversible, progressive brain disorder characterized by the deterioration of memory, language, and, eventually, physical functioning
-cholinesterase inhibitors can get into the CNS and thus raise ACh levels, which is thought to be low and contributory in the pathogenesis of this disease
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