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Claims for Patent: 4,952,586

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Claims for Patent: 4,952,586

Title: Edrophonium-atropine composition and therapeutic uses thereof
Abstract:A composition is provided which includes a balanced combination of an edrophonium component and an atropine component. A preferred embodiment has 0.5 mg of edrophonium chloride and 8 micrograms of atropine sulfate, with respect to patient weight. The inventive composition is useful to antagonize nondepolarizing blockade during medical treatment when muscle relaxation is no longer necessary, provides extremely rapid onset of action and results in minimal heart rate changes.
Inventor(s): Morris; Robert B. (Mill Valley, CA), Cronnelly; Roy (Pacifica, CA), Miller; Ronald Dean (Greenbrae, CA)
Assignee: The Regents of the University of California (Berkeley, CA)
Application Number:07/262,175
Patent Claims: 1. A composition useful for antagonizing nondepolarizing neuromuscular blockade in a patient of determined weight by rapid intravenous unit dosage administration consisting essentially of:

edrophonium in an amount of from about 21 to about 70 mg for each unit dosage of the composition, atropine in an amount of from about 0.42 to about 0.70 for mg each unit dosage of the composition, said edrophonium being in a weight ratio with respect to said atropine of about 50:1 to 100:1, said edrophonium and atropine being admixed.

2. The composition as in claim 1 wherein said edrophonium is substantially water soluble.

3. The composition as in claim 2 wherein said atropine is substantially water soluble.

4. The composition as in claim 3 wherein said composition is an aqueous solution, and said weight ratio is about 62.5:1 to 71.5:1.

5. The composition as in claim 1 or 4 herein said edrophonium is edrophonium chloride.

6. The composition as in claim 1 or 4 wherein said atropine is atropine sulfate.

7. The composition as in claim 1 wherein said edrophonium is edrophonium chloride in an amount of about 35 mg for each unit dosage, said atropine is atropine sulfate in an amount of about 0.49 to about 0.56 mg for each unit dosage, and said weight ratio is about 62.5:1 to 71.5:1.

8. The composition as in claim 7 wherein said edrophonium chloride and said atropine sulfate are solubilized in an aqueous solution.

9. A method for antagonizing nondepolarizing blockage in a patient of determined weight comprising the step of:

intravenously administering a dose consisting essentially of edrophonium sufficient to provide an amount from 0.3 to about 1 mg with respect to a kg of patient's weight, and

atropine in an amount sufficient to provide from about 6 to about 10 micrograms with respect to a kg of patient's weight, the edrophonium and atropine being admixed in said dose with edrophonium being in a weight ratio with respect to the atropine of not less than about 50:1 and not greater than about 100:1, the administering of said dose of edrophonium and atropine being by a single, rapid injection.
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