Depolarizing skeletal muscle relaxants
OwnerMerouane Bencherif, Patrick M. Lippiello +1inventors
InventorsMerouane Bencherif, Patrick M. Lippiello, William S. Caldwell
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Abstract
Compounds such as 5-chloronicotine, 5-fluoronornicotine, anabaseine, 5-fluoroanabaseine, 2-acetoxymethylquinuclidine or!2-(3-pyridyl)-quinuclidine are useful as locally acting and highly selective muscle relaxants. Each compound, when administered intravenously, acts to bind to musculoskeletal nicotinic receptor sites in a reversible manner causing transient depolarization, and hence provides for reversible muscle relaxation to a patient during anesthesia.
Claims14
A method for providing musculoskeletal relaxation in a patient undergoing a surgical procedure requiring anesthesia, the method comprising administering to the patient an effective amount of a compound having the formula:
- ##STR5## where R' and R" individually represent alkyl containing 1 to 7 carbon atoms;
- X represents alkyl containing 1 to 7 carbon atoms, halo, primary amino, secondary amino or tertiary amino;
- j is an integer which ranges from 0-12;
- p is an integer which is 0 or 1;
- and n is an integer which ranges from 0-3.
A pharmaceutical composition having the form of a neuromuscular depolarizing muscle relaxant, the composition including as an active ingredient an effective amount of a compound having the formula:
- ##STR6## where R' and R" individually represent alkyl containing 1 to 7 carbon atoms;
- X represents alkyl containing 1 to 7 carbon atoms, halo, primary amino, secondary amino or tertiary amino;
- j is an integer which ranges from 0-12;
- p is an integer which is 0 or 1;
- and n is an integer which ranges from 0-3.
Dependencies are inferred from the claim text.