Neuromuscular blocking agents
DCFirst Claim
1. A physiologically acceptable 1R-cis,1'"'"'R-cis-2,2'"'"'-(3,11-dioxo-4,10-dioxatridecamethylene)-bis-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium salt being substantially free of other geometric or optical isomers thereof, the amount of said other geometric or optical isomers thereof being less than 8% w/w based on the combined weight of said physiologically acceptable salt and any of said geometric or optical isomers.
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Abstract
1R-cis,1'"'"'R-cis isomer of a 2'"'"',2'"'"'-(3,11-dioxo-4,10-dioxatridecylene)-bis(1,2,3,4-tetrahydro-6, 7-dimethoxy-2-methyl-1-veratrylisoquinolium) said, substantially free from other geometrical and optical isomers thereof. The 1R-cis,1'"'"'R-cis isomer has been found to have an advantageous combination of pharmacological properties, notably greater neuromuscular blocking potency, weaker histamine-releasing potency, and at equivalent levels of neuromuscular blockade, fewer potential adverse effects on the autonomic nervous system (sympathetic and parasympathetic blockage), in comparison with the known mixture of geometrical and optical isomers.
43 Citations
24 Claims
- 1. A physiologically acceptable 1R-cis,1'"'"'R-cis-2,2'"'"'-(3,11-dioxo-4,10-dioxatridecamethylene)-bis-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium salt being substantially free of other geometric or optical isomers thereof, the amount of said other geometric or optical isomers thereof being less than 8% w/w based on the combined weight of said physiologically acceptable salt and any of said geometric or optical isomers.
- 4. A physiologically acceptable 1R-cis,1'"'"'R-cis-2,2'"'"'-(3,11-dioxo-4,10-dioxatridecamethylene)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium besylate salt being substantially free of other geometric or optical isomers being less than 8% w/w based on the combined weight of said besylate salt and any of said geometric or optical isomers thereof.
- 7. A physiologically acceptable 1R-cis,1'"'"'-R-cis-2,2'"'"'-(3,11-dioxo-4,10-dioxatridecamethylene)-bis-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium mesylate salt being substantially free of other geometric or optical isomers thereof the amount of, said other geometric or optical isomers being less than 8% w/w based on the combined weight of said mesylate salt and any of said geometric or optical isomers thereof.
- 13. A method of producing neuromuscular blockage in an animal which comprises administering by injection or infusion to said animal an effective neuromuscular blockade amount of a pharmacologically acceptable liquid containing a physiologically acceptable 1R-cis,1'"'"'R-cis-2,2'"'"'-(3,11-dioxo-4,10-dioxatridecamethylene)-bis-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium salt being substantially free of other geometric or optical isomers thereof, the amount of said other geometric or optical isomers thereof being less than 8% w/w based on the combined weight of said physiologically acceptable salt and any of said geometric or optical isomers.
Specification