Neostigmine☆

Add time:08/23/2019    Source:sciencedirect.com

Neostigmine is a carbamate inhibitor of acetylcholinesterase, the enzyme responsible for hydrolyzing acetylcholine at synapses to terminate cholinergic signaling. It is mainly used postoperatively under the brand name “Bloxiverz” to reverse shallow levels of neuromuscular blockade induced by non-depolarizing muscle relaxants such as rocuronium, vecuronium. It can also be used to treat myasthenia gravis, intestinal pseudo-obstruction and glaucoma. Neostigmine does not readily cross the blood–brain barrier due to its quaternary nitrogen structure. It increases acetylcholine levels in both neuromuscular junctions and synapses of the autonomic nervous system, resulting in undesirable muscarinic side effects such as bradycardia. Muscarinic antagonists (atropine or glycopyrrolate) are, therefore, often used in combination with neostigmine in reversal of neuromuscular blockade.

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