Products
Neostigmine is now commercially available in many countries only as a solution for injection (Robinul Neostigmine Injektionslsg). Prostigmine 15 mg tablets are no longer available in many countries.
Structure and properties
Neostigmine bromide (C12H19BrN2O2, 303.20 g/mol)
Effects
Neostigmine (ATC N07AA01 , ATC S01EB06) is indirectly parasympathomimetic by inhibiting acetylcholinesterase. It competitively competes with acetylcholine. However, because the neostigmine-acetylcholinesterase complex is hydrolyzed more slowly than the acetylcholine-acetylcholinesterase complex, the released acetylcholine accumulates at choline receptors. As a result, the action of acetylcholine at all cholinergic receptors is enhanced. The interaction of neostigmine with acetylcholinesterase is reversible. Once the complex between neostigmine and cholinesterase is dissolved, the enzyme is reactivated and can hydrolyze acetylcholine, terminating its action. The range of action of neostigmine is not limited to parasympathomimetic effects, but also includes other cholinomimetic effects distributed throughout the body: Tonus increase of intestinal and skeletal muscles, stimulation of sweat and salivary glands, miosis and bradycardia, etc.
Indications
- Atonic constipation, meteorism (for example, before radiographs).
- Postoperative intestinal atony and urine retention.
- Myasthenia gravis pseudoparalytica
- Curare antagonist (to abolish the effects of curare and curare-like nondepolarizing muscle relaxants).
