Neostigmine
3 - ( dimethylcarbamoyloxy ) - N, N, N- trimethylbenzenaminium
- 59-99-4
- 114-80-7 ( bromide)
- 51-60-5 ( Metilsulfat )
N07AA01, S01EB06
White solid ( bromide)
Parasympathomimetic
Acetylcholinesterase inhibitor
175-177 ° C ( bromide)
Risk
12.34 mg · kg -1 ( LD50, mouse, oral)
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Neostigmine inhibits the enzyme acetylcholinesterase. This enzyme cleaves both at various cholinergic synapses ( muscarinic, nicotinic ) and neuromuscular junctions the chemical transmitter acetylcholine. Thus, this is inactivated after distribution in the synaptic cleft and limited its effect. When the enzyme is inhibited by agents such as neostigmine, the concentration of acetylcholine in the synaptic cleft rises rapidly. This stimulates the parasympathetic nervous system, for example, and caused an increase in tone of skeletal muscles a. Similarly, physostigmine act, the insecticide E605 or some chemical warfare agents (eg, soman ).
Application
Neostigmine is used in cases of poisoning with competitive acetylcholine receptor antagonists (eg, curare, Procuron ). It is also found in the antagonizing of non- depolarizing muscle relaxants use, for example in the detoxification of anesthesia. To avoid undesired ( side) effects, which are mediated by muscarinic acetylcholine receptors and lead to an increase in parasympathetic tone ( bradycardia, bronchoconstriction, etc. ), in addition atropine is administered, the muscarinic acetylcholine receptors blocked, but the nicotinic acetylcholine receptors ( at the motor end plate ) not occupied.
In myasthenia neostigmine may be used to counteract muscle weakness. If there is an isolated paralytic ileus may be attempted with neostigmine to stimulate the motility and peristalsis of the intestines again.
In combination with pilocarpine neostigmine bromide is used in eye drops for the treatment of glaucoma.
Pharmacokinetics
As a quaternary ammonium compound neostigmine is poorly absorbed from the gastrointestinal tract and overcomes - in contrast to the tertiary amine physostigmine - not the blood- brain barrier, so is not CNS consistently.
Pharmaceutical information
Neostigmine is administered intravenously. Can be used medicinally, the highly water-soluble salts neostigmine bromide and Neostigminmetilsulfat.