Back to results
US 5,703,101 AGranted
Agonist-antagonist combination to reduce the use of nicotine and other drugs
AssigneeRobert J. Schaap
InventorsJed E. Rose, Edward D. Levin
Life of this patent
Estimating the term…
Loading patent…
Loading patent…
AssigneeRobert J. Schaap
InventorsJed E. Rose, Edward D. Levin
Estimating the term…
A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic effects of the drug or its other agonist. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist. In another embodiment, the drug or its other agonist is first administered and the antagonist is self-administered by a subject in a manner which mimics the use of the drug thereby counter-conditioning the drug user to the stimuli associated with the normal administration of the drug. The invention further provides a method of therapeutically treating psychophysiologic diseases and disorders involving neuronal dysregulation. The method additionally provides a pharmacologic composition for the treatment and reduction of drug dependence and which relied upon a combination of an agonist and an antagonist.
A pharmacologic composition for the treatment and reduction of dependency on an abused stimulating drug selected from the class consisting of cocaine and amphetamines where the addictive effects of this drug causes activation of receptors which are actuated by the drug, said composition comprising:
A pharmacologic composition for the treatment and reduction of dependency on an abused stimulating drug selected from the class consisting of cocaine and amphetamines where the addictive effects of the drug causes activation of receptors for the drug, said composition comprising:
A pharmacologic composition for the treatment and reduction of dependency on an abused stimulating opiate drug where the addictive effects of this drug causes activation of receptors for the drug, said composition comprising:
A pharmacologic composition for the treatment of physiological dysfunction of a subject in which brain receptors of the subject are subject to under-activity and over-activity and where the composition reduces this under-activity and over-activity, said composition comprising a bromocriptine agonist in the composition in an amount to provide a daily dosage rate of 40 to 100 milligrams per day which prevents under-activity of the brain receptors causing this physiological dysfunction and an antagonist to the agonist present in the composition and being selected from the class consisting of fluphenazine, fluphenazine hydrochloride and fluphenazine decanoate, said fluphenazine antagonist or fluphenazine hydrochloride antagonist being present in the composition to provide a daily dosage rate of 20 to 60 milligrams per day and the fluphenazine decanoate if used present in an amount to provide a daily dosage ratio of 20-75 milligrams per day, and where the amounts of the antagonist are sufficient to prevent over-activity of the receptors and at least partially block the pharmacologic effects of the agonist, said amounts of agonist and antagonist being such that there is always a substantial systemic amount of the antagonist present when there is a substantial systemic amount of the agonist present in the subject using the composition and the receptor amounts also being sufficient to preclude intoxication and to also prevent under-activity of the receptors such that the agonist is complemented by the antagonist to occupy a number of receptors of the subject which is greater than the number of receptors which would be occupied by the agonist alone.
A pharmacologic composition for the treatment of physiological dysfunction of a subject in which brain receptors of the subject are subject to under-activity or over-activity and where the composition reduces the over-activity and under-activity, said composition comprising a bromocriptine agonist in the composition in an amount to provide a dosage rate of 10-25 milligrams per day by a transdermal patch which prevents under-activity of the brain receptors causing this physiological dysfunction and an antagonist to the agonist present in the composition and being selected from the class consisting of a fluphenazine, fluphenazine hydrochloride and fluphenazine decanoate, said fluphenazine antagonist or fluphenazine hydrochloride antagonist being present in the composition to provide a daily dosage rate of 20 to 60 milligrams per day and the fluphenazine decanoate if used present in an amount to provide a daily dosage rate of 20-75 milligrams per day and where the amounts of the antagonist are sufficient to prevent over-activity of the receptors and at least partially block the pharmacologic effects of the agonist, said amounts of agonist and antagonist being such that there is always a substantial systemic level of the antagonist present in the subject using the composition and the respective amounts also being sufficient so that the drug or agonist precludes intoxication and the combination of the agonist and antagonist also prevents under-activity of the receptors such that the agonist is complemented by the antagonist to occupy a number of receptors of the subject which is greater than the number of receptors which would be occupied by the agonist alone.
A pharmacologic composition for the treatment and reduction of dependency on an abused stimulating drug selected from the class consisting of cocaine and amphetamines where the addictive effects of this drug causes activation of receptors which are actuated by the drug, said composition comprising:
A pharmacologic composition for the treatment and reduction of dependency on an abused stimulating drug selected from the class consisting of cocaine and amphetamine where the addictive effects of the drug causes activation of receptors for the drug, said composition comprising:
A pharmacologic composition for the treatment of physiological dysfunction of a subject in which brain receptors of the subject are subject to under-activity and over-activity and where the composition reduces this under-activity and over-activity, said composition comprising an agonist selected from the class consisting of amphetamines and cocaine and bromocriptine in the composition in an amount to provide a daily dosage rate of 40 to 100 milligrams per day which prevents under-activity of the brain receptors causing this physiological dysfunction and an antagonist to the agonist present in the composition and being selected from the class consisting of fluphenazine, fluphenazine hydrochloride and fluphenazine decanoate, said fluphenazine antagonist or fluphenazine hydrochloride antagonist being present in the composition to provide a daily dosage rate of 20 to 60 milligrams per day and the fluphenazine decanoate if used present in an amount to provide a daily dosage ratio of 20-75 milligrams per day, and where the amounts of the antagonist are sufficient to prevent over-activity of the receptors and at least partially block the pharmacologic effects of the agonist, said amounts of agonist and antagonist being such that there is always a substantial systemic amount of the antagonist present when there is a substantial systemic amount of the agonist present in the subject using the composition and the receptor amounts also being sufficient to preclude intoxication and to also prevent under-activity of the receptors such that the agonist is complemented by the antagonist to occupy a number of receptors of the subject which is greater than the number of receptors which would be occupied by the agonist alone.
A pharmacologic composition for the treatment of physiological dysfunction of a subject in which brain receptors of the subject are subject to under-activity or over-activity and where the composition reduces the over-activity and under-activity, said composition comprising an agonist selected from the class consisting of amphetamines and cocaine and bromocriptine in the composition in an amount to provide a dosage rate of 10-25 milligrams per day by a transdermal patch which prevents under-activity of the brain receptors causing this physiological dysfunction and an antagonist to the agonist present in the composition and being selected from the class consisting of a fluphenazine, fluphenazine hydrochloride and fluphenazine decanoate, said fluphenazine antagonist or fluphenazine hydrochloride antagonist being present in the composition to provide a daily dosage rate of 20 to 60 milligrams per day and the fluphenazine decanoate if used present in an amount to provide a daily dosage rate of 20-75 milligrams per day and where the amounts of the antagonist are sufficient to prevent over-activity of the receptors and at least partially block the pharmacologic effects of the agonist, said amounts of agonist and antagonist being such that there is always a substantial systemic level of the antagonist present in the subject using the composition and the respective amounts also being the composition and the respective amounts also being sufficient so that the drug or agonist precludes intoxication and the combination of the agonist and antagonist also prevents under-activity of the receptors such that the agonist is complemented by the antagonist to occupy a number of receptors of the subject which is greater than the number of receptors which would be occupied by the agonist alone.
Dependencies are inferred from the claim text.