Title:  Method for treatment of multiple sclerosis and related disease states

United States Patent:  6,277,402

Appl. No.:  340277

A method for treatment of multiple sclerosis and related disease states. A histamine H2 mimicking agent is administered in an amount which is effective to stimulate production of a cyclic AMP in the body. A phosphodiesterase inhibitor is administered in conjunction with the histamine H2 mimicking agent to conserve the cyclic AMP which is thus produced. It is believed that the increased cyclic AMP levels serve to maintain the patient's myelin against self degeneration. The histamine H2 mimicking agent may be histamine phosphate and the phosphodiesterase inhibitor may be caffeine. The histamine H2 mimicking agent and the phosphodiesterase inhibitor may be mixed in a gel and administered using a transdermal patch.

SUMMARY OF THE INVENTION

The present invention has solved the problems cited above, and is a method for treatment of multiple sclerosis and related disease states.

Broadly, the method comprises administering a composition comprising a histamine H2 mimicking agent, in an amount effective to stimulate production of cyclic AMP at a level which is adequate to maintain the patient's myelin against self degeneration. The treatment composition may further comprise a phosphodiesterase inhibitor, administered in an amount effective for conservation of the increased levels of cyclic AMP in the patient's body.

The histamine H2 mimicking agent may comprise histamine phosphate, or may comprise a selected beta adrenergic agent which mimics histamine H2. The phosphodiesterase inhibitor may comprise a methylxanthine agent; the methylxanthine agent may comprise caffeine, or may comprise theophylline or a theophylline derivative.

The method may comprise administering histamine phosphate transdermally at a rate in the range of about 0.06 mg/hr to about 0.50 mg/hr, and administering caffeine transdermally at a rate in the range from about 2 mg/hr to about 25 mg/hr.

The present invention also provides a treatment method which comprises administering histamine phosphate and caffeine simultaneously using a transdermal patch. In a preferred embodiment, the histamine phosphate is administered transdermally at a rate in the range from about 0.1 mg/hr to about 0.3 mg/hr, and the caffeine is administered transdermally at a rate of about 12.5 mg/hr.

The histamine phosphate may also be administered by subcutaneous injection or intravenously, and the caffeine may also be administered by oral ingestion or subcutaneous injection.

The invention further provides a composition for treatment of multiple sclerosis and related disease states. The composition may comprise a histamine H2 mimicking agent, a phosphodiesterase inhibitor, and a fluid medium in which the histamine H2 mimicking agent and phosphodiesterase inhibitor are mixed for simultaneous administration to a patient. The histamine H2 mimicking agent may be histamine phosphate and the phosphodiesterase inhibitor may be caffeine, and the fluid medium may comprise a transdermal gel or injectable solution.

Still further, the invention provides an apparatus for treatment of multiple sclerosis and related disease states. The apparatus comprises a transdermal patch and a treatment composition which is deposited thereon for administration to a patient, the treatment composition comprising, in predetermined amounts, a histamine H2 mimicking agent, a phosphodiesterase inhibitor, and a fluid medium in which the histamine H2 mimicking agent and phosphodiesterase inhibitor are mixed for simultaneous transdermal administration to the patient. Again, in a preferred embodiment the histamine H2 mimicking agent may be histamine phosphate and the phosphodiesterase inhibitor may be caffeine.

For an 8 hour transdermal dose, the histamine phosphate may be present in an amount from about 1.1 mg to about 2.2 mg, and the caffeine may be present in an amount from about 100 mg to about 200 mg.

Claim 1 of 29 Claims

What is claimed is:

1. A method for treatment of multiple sclerosis, said method comprising the steps of:

administering to a patient transdermally and on a continuing basis and substantially without the presence of an immunogen a composition comprising:

a histamine H2 agonist, in an amount effective to stimulate and sustain production of cyclic AMP at a level which is adequate to maintain myelin against self-degeneration; and

a phosphodiesterase inhibitor, in an amount effective for conservation of said level of cyclic AMP which is produced in response to administration of said histamine H2 agonist.

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