Hogg Rosemary M G, Mirakhur Rajinder K
Department of Anaesthetics and ICM, Queen's University, Belfast, UK.
Expert Rev Neurother. 2009 May;9(5):599-608. doi: 10.1586/ern.09.22.
Neostigmine, the currently used agent for reversal of neuromuscular block, has several drawbacks, such as a slow onset of peak effect, inability to reverse deep block and the occurrence of widespread muscarinic effects. Sugammadex is a new class of reversal agent that acts by encapsulating the molecules of the relaxants rocuronium and vecuronium, for which it is a specific antagonist. Clinical trials in over 2000 subjects have shown it to be effective for reversal of block by these two relaxants even from deep levels, in doses of 2.0-4.0 mg/kg. Sugammadex can also reverse an intense (profound) high-dose rocuronium block, but the dose required in this situation is 16.0 mg/kg. The agent has been found to be safe so far, with few side effects.
新斯的明是目前用于逆转神经肌肉阻滞的药物,有几个缺点,如达到峰值效应起效缓慢、无法逆转深度阻滞以及出现广泛的毒蕈碱样效应。舒更葡糖钠是一类新型的逆转剂,其作用机制是包裹罗库溴铵和维库溴铵等松弛剂分子,是这两种药物的特异性拮抗剂。超过2000名受试者的临床试验表明,即使对于深度阻滞,舒更葡糖钠以2.0 - 4.0 mg/kg的剂量也能有效逆转这两种松弛剂引起的阻滞。舒更葡糖钠还能逆转强烈(深度)的高剂量罗库溴铵阻滞,但在这种情况下所需剂量为16.0 mg/kg。到目前为止,该药物已被证明是安全的,副作用很少。