Cholinesterase Inhibitors
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| prevents degradation of acetycholine by acetylcholinesterase thereby enhancing | the activity of acetylcholine at cholinergic receptors
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| they can intensify ACh activity at all cholinergic junctions | muscarinic, ganglionic, nicotinic
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| reversible inhibitors: | ambenonium[Myletase], demecarium[Humorsol], donepezil[Aricept], galantamine{Reminyl], neostigmine[Prostigmin], pyridostigmine[Mestinon], physostigmine[Antilirium, rivastigmine[Exelon], tacrine[Cognex]
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| irreversible inhibitors: | organophosphate cholinesterase inhibitors, toxic and can be absorbed through the skin, only clinical indication is glaucoma tx
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| not a cholinesterase inhibitor but used to tx Alzheimer's, adhd, postherpetic neuralgia, prevention of migraine | memantine[Namenda], N-methyl-D-aspartate [NMDA] inhibitor
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| Possible contributers to Alzheimer's | profound cholinergic depletion so these drugs increase the availability of acetylcholine in the brain
persistent stimulation of the NMDA receptors by the excitatory amino acid glutamate
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| signs of toxicity: | GI stimulation, excessive salivation, miosis, fasciculations
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| used to treat myasthenia gravis and to reverse nonpolarizing neuromuscular blockade[not succ b/c it is a depolarizing neuromuscular blocker] | neostigmine[Prostigmin, oral; Bloxiverz, injectable]
pyridostigmine[Mestinon, Rebonol]
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| other NMDA receptor antagonists: | amantadine[Symmetrel], ketamine, dextromethorphan
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| Alzheimer's is associated with a significant deficiency in brain levels of choline acetyltransferase, | the enzyme responsible for the synthesis of acetylcholine
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| myasthenia gravis is an autoimmune disorder that produces antibodies directed against | nicotinic receptors on skeletal muscle reducing the number of receptors by 70-90% resulting in muscle weakness
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| s/s of increased acetylcholine | dizziness, miosis, lacrimation, excessive secretions in the respiratory and GI tract, bronchospasm, bradycardia, abdominal cramps, n/v/c, excessive salivation
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