Bloxiverz获准用于逆转手术中所用神经肌肉阻滞剂的效应

圣路易斯(MD Consult)——Flamel Technologies公司宣布，美国食品药品管理局(FDA)已批准Bloxiverz(甲硫酸新斯的明)用于手术后逆转非去极化型神经肌肉阻滞剂的效应。这种药物为静脉应用，将有0.5和1.0 mg/ml两种规格可供选择。

Bloxiverz是一种胆碱酯酶抑制剂，通过在胆碱能神经冲动传导部位与乙酰胆碱酯酶竞争性结合而抑制胆碱酯酶的水解。该药物通过促进神经肌肉接头处的冲动传导而提高胆碱能神经活性。新斯的明增高突触乙酰胆碱水平的能力是其有效逆转神经肌肉阻滞效应的基础。新斯的明不易穿透血脑屏障，因此不会对中枢神经系统的胆碱能神经活性产生显著影响。

治疗中最常见的不良反应包括心动过缓、恶心和呕吐。为了降低心动过缓风险，在使用Bloxiverz之前应使用阿托品或格隆溴铵。Bloxiverz应慎用于有心律失常、近期急性冠脉综合征、迷走神经紧张、甲状腺功能亢进、重症肌无力、癫痫或消化性溃疡患者。因为偶有患者发生过敏，故在使用时应备好阿托品和抗过敏药物。当神经肌肉阻滞很轻微时，使用大剂量Bloxiverz可能导致神经肌肉功能障碍。当接近完全从神经肌肉阻滞状况中恢复时，应减少Bloxiverz的剂量。

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ST LOUIS (MD Consult) - On June 3, 2013, Flamel Technologies announced that the US Food and Drug Administration (FDA) has approved Bloxiverz (neostigmine methylsulfate) for use in reversing the effects of nondepolarizing neuromuscular blocking agents after surgery. The drug is administered intravenously and will be available in 0.5- and 1.0-mg/mL strengths.

Bloxiverz is a cholinesterase inhibitor that inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission. It enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions. Neostigmine's ability to increase synaptic acetylcholine levels underlies its effectiveness in reversing neuromuscular blockade produced by neuromuscular blocking agents used during surgery. Neostigmine does not readily cross the blood-brain barrier and therefore does not significantly affect cholinergic function in the central nervous system.

The most common adverse reactions during treatment include bradycardia, nausea, and vomiting. Atropine or glycopyrrolate should be administered before Bloxiverz to minimize the risk of bradycardia. Bloxiverz should be used with caution in patients with arrhythmias, recent acute coronary syndrome, vagotonia, hyperthyroidism, myasthenia gravis, epilepsy, or peptic ulcer. Because of the possibility of hypersensitivity in an occasional patient, atropine and medications to treat anaphylaxis should always be readily available. Large doses of Bloxiverz administered when neuromuscular blockade is minimal can produce neuromuscular dysfunction. The dose of Bloxiverz should be reduced if recovery from neuromuscular blockade is nearly complete.