Novel Intermediate-Duration Neruomuscular Blockers
- *Abstract
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Neuromuscular blockade is an integral part of most anesthetic procedures. This invention relates to the discovery of novel nondepolarizing neuromuscular blocking agents of intermediate duration that have minimal circulatory effects. After administration, the activity of these neuromuscular blocking agents can easily be reversed by the amino acid cysteine. Their reversal by cysteine is the basis for their intermediate duration in vivo, where endogenous cysteine is available in the bloodstream. When exogenous cysteine is given i.v. in doses from 10 to 50 mg/kg, neuromuscular blockade caused by the compounds of the present invention is abolished typically within 2-3 minutes after injection of cysteine, given as little as 1-2 minutes after inducing paralysis.
The unique properties and advantages of these compounds are:
- they are potent nondepolarizing neuromuscular blocking drugs
- they cause little or no circulatory effect
- they are degraded by endogenous cysteine at a rate which results in an intermediate duration of action
- they react immediately with exogenous cysteine given i.v. so that neuromuscular blockade is abolished within minutes. This is a major potential advantage to clinical practice. Neuromuscular blockade is abolished because the active material is converted rapidly in a chemical reaction, to an inactive derivative.
- *Licensing
- Brian J. Kellybjk44@cornell.edu212-746-6186
- 其他
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None
- 国家/地区
- 美国
