Classically, anticholinesterase drugs, such as neostigmine, are given to reverse neuromuscular block. These agents inhibit the enzyme cholinesterase at the neuromuscular junction. They enable more acetylcholine molecules to find their way onto vacant receptors, and help to restore neuromuscular transmission.

Anticholinesterases are usually mixed with drugs that block muscarinic receptors, such as atropine or glycopyrrolate. Muscarinic stimulation would create many unwanted side effects e.g. excessive salivation, bronchospasm and bradycardia.

A novel method of reversal will soon be available, in the form of a drug called sugammadex (formerly Org 25969). This is a modified cyclodextrin, and is the first selective relaxant binding agent (SRBA). It binds to aminosteroid muscle relaxants, especially rocuronium, and rapidly reverses neuromuscular block.