This class of drug inhibits the acetylcholinesterase enzyme, which normally acts to break down acetylcholine. This leads to increased levels and duration of action of the neurotransmitter acetylcholine.
Edrophonium is a reversible acetylcholinesterase inhibitor, which prevents the breakdown of acetylcholine. It works by competitively inhibiting the enzyme, acetylcholinesterase, at the neuromuscular junction. This drug is used to diagnose myasthenia gravis.
Also known as the "tensilon-test," myasthenia gravis can be diagnosed with edrophonium, as patients immediately show decreased muscle weakness.
These medications are cholinomimetics, or parasympathomimetics, which work to reversibly inhibit acetylcholinesterases and do not cross the blood brain barrier (BBB). These drugs work to treat mysasthenia gravis, while neostigmine is also used to reverse neuromuscular blocking agensts in anesthesia.
These are used for long term treatment of myasthenia gravis because acetylcholinesterase inhibitors such as pyridostigmine and neostigmine can improve muscle function by slowing the natural enzyme cholinesterase that degrades acetylcholine in the motor end plate; the neurotransmitter is therefore around longer to stimulate its receptor.
Neostigmine is indicated in the treatment of post-operative and neurogenic ileus as well as in treating urinary retention.
Physostigmine is more hydrophobic than other indirect cholinomimetics, and crosses the blood brain barrier. It is used to treat atropine and anticholinergic drug overdoses.
Physostigmine is used to counter the CNS effects of atropine overdose.
Physostigmine is helpful in inducing miosis, and leading to decreased intraocular pressure in glaucoma.
Donepezil is an acetylcholinesterase inhibitor which is used for treating Alzheimer's disease.
In Alzheimer's disease, patients have relatively decreased acetylcholine levels. Thus, centrally acting acetylcholinesterase inhibitors help increase the available amount of relative acetylcholine.
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