Agonist-antagonist combination to reduce the use of nicotine and other drugs

A method of pharmacologically treating and reducing drug dependency where the drug causes activation of receptors responsive to that drug, without causing over-activity or under-activity in receptors mediating the drug dependency, said method comprising:

• a) administering to a subject a drug or an agonist of the drug which acts upon receptors that mediate addiction and are responsive to that drug to which the subject is dependent and which causes those receptors which are responsive to that drug to become activated, said drug being administered in an amount which satisfies a demand for the drug, and
• b) simultaneously administering to said same subject an antagonist to the drug which blocks effects of the agonist that causes activation of these same receptors and which receptors are also sensitive to the antagonist, and said antagonist being present in an amount sufficient to attenuate the pharmacologic effects of the drug or an agonist thereof, said antagonist in combination with said drug or an agonist being present in an amount wherein more of the receptors responsive to that drug or agonist are being occupied by the drug and the antagonist than would be occupied by the same amount of the drug alone or the antagonist alone, and that a lesser number of the receptors are left available to respond to additional doses of the drug thereby insulating the subject from further reinforcing addictive effects of the drug, and without said agonist and said antagonist causing over-activity or under-activity of the receptors caused by administration of a drug or agonist or withdrawal from the drug or agonist, said drug or agonist and said antagonist both being present in an amount such that any toxic effects of the amount of the drug or agonist and the toxic effects of the amount of the antagonist are attenuated by each other, and with said drug or agonist causing the receptors for the drug or agonist to be activated and said antagonist causing additional receptors for the drug or agonist to be blocked, the drug or agonist being administered by a technique other than that to which the subject was accustomed to.

A method of treating and reducing drug dependency without causing over-activity and under-activity of receptors for an addictive drug of abuse to thereby mediate the drug dependency, said method comprising:

• a) administering to a subject a drug or agonist of the drug which causes receptors which are responsive to a systemic introduction of that drug to become activated, said drug being administered in an amount which, in the absence of a co-administered antagonist, achieves a pharmacologic action comparable to the action achieved by the drug of abuse to which the subject was previously accustomed to receiving,
• b) administering to the subject an antagonist to the drug or agonist in a manner to which the subject was previously accustomed to administration of said drug and this antagonist blocks effects of the agonist that causes activation of these same receptors and which receptors are also sensitive to the antagonist, and said antagonist being present in an amount to increase the saturation of the receptors for said drug or agonist and also causing a reduced systemic effect of the drug or agonist, thereby reducing the satisfaction of said subject to the drug or agonist and inversely conditioning the subject to the desire for the drug, and the administration of said drug or agonist being complemented by said antagonist by occupying a number of receptors of said subject using the drug or agonist which is greater than the number of receptors that would be occupied by the drug or agonist alone, said drug or agonist and said antagonist having opposing effects with regard to receptor stimulation and leaving a lesser number of receptors to respond to the drug or agonist due to receptor occupancy without causing over-activity or under-activity of the receptors responsive to the drug or agonists and which over-activity or under-activity is caused by administration of said drug or agonist or withdrawal from said drug or agonist, such that said drug or agonist is administered in an amount that causes receptors of the drug or agonist to be activated, and which thereby satiates the need for the drug or agonist by said subject, said drug or agonist also being present in a sustained amount in the bloodstream of a subject and in such amount which results in a reduced satisfaction from additional doses of the drug, and said antagonist also causing additional receptors of the drug or agonist to be blocked, at least the drug or agonist being administered by a technique other than that to which the subject was previously accustomed to.

A method of therapeutically treating psychophysiological diseases and disorders resulting from neuronal dysregulation and which causes an over-activity or an under-activity in the amount of activation of receptors of a subject, said method comprising simultaneously administering to said subject a first component comprised of a drug or an agonist of the drug which causes receptors which are responsive to a systemic introduction of that drug or agonist to become activated, said drug or agonist being administered in addition to a second component comprised of an antagonist to the drug or agonist which blocks effects of said drug or agonist that causes activation of these same receptors and which receptors are also sensitive to the antagonist, said first component being administered in an amount which would reduce the effects of the psychophysiological disease or disorder resulting from under-activity of the receptors, said second component being administered in an amount which reduces the effects of the psychophysiological disease or disorder resulting from over-activity of said receptors, both being co-administered in an amount to reduce the systemic effects of the components individually and which in combination counters the effect of the psychophysiological disease or disorder without causing over-activity or under-activity in receptor activation caused by a neurotransmitter of said subject, said second component being present in a substantial systemic amount sufficient to block such activation.

A pharmacologic composition for the treatment of drug dependency and psychophysiologic disorders and diseases in a subject without causing over-activity or under-activity in receptors mediating a drug dependency and the psychophysiologic diseases and disorders, said composition comprising:

• a) a drug or an agonist of that drug present in the composition in an amount which causes receptors which are responsive to a systemic introduction of that drug to become activated, said drug being present in amounts to provide some satisfaction of the demand for the drug by the subject using the composition, and
• b) an antagonist to said drug or an agonist of the drug which blocks effects of the drug or the agonist that causes activation of these same receptors and wherein these receptors are sensitive to the antagonist, said antagonist being present in the composition in an amount sufficient to block a substantial amount of the effects of the drug or agonist on the over-activity or under-activity of the receptors, the amount of said drug or agonist and the amount of said antagonist being present in the composition so that there is always a substantial systemic amount of the antagonist present in an amount sufficient to partially block the effects of the drug or agonist when there is a substantial systemic amount of the drug or agonist present in the blood of said subject using the composition, said drug or agonist and said antagonist being administered in amounts to reduce reinforcing effects of the drug and to reduce a derivation of enjoyable effects on a subject to whom administered and to also prevent a state of withdrawal from the drug or agonist in the subject, without causing a over-activity or an under-activity of the receptors responsive to the drug or agonist and which over-activity or under-activity is caused by administration of a drug or agonist or withdrawal from the drug or agonist, and with said drug or agonist causing the receptors for the drug or agonist to be activated and said antagonist causing the receptors for that drug or agonist to be blocked, the amounts of said drug or agonist and said antagonist also being established so that the drug or agonist is complemented by the antagonist to occupy a number of receptors of the subject using the drug or agonist greater than the number of receptors which would be occupied by the drug or agonist alone, and with said drug or agonist and said antagonist having opposing effects with regard to receptor stimulation and leaving a lesser number of receptors to respond to the drug or agonist due to receptor occupancy, the drug or agonist being provided in a form so as to be administered by a technique other than that to which the user was accustomed to.

A method of treating and reducing drug dependency without causing over-activity or under-activity in receptors for an addictive drug to thereby mediate the drug dependency and where the drug causes activation of receptors responsive to that drug, said method comprising:

• a) administering to a subject a drug or an agonist of the drug which acts upon receptors that mediate addiction and wherein these receptors are responsive to a systemic introduction of the drug, causing said receptors to become activated, said drug or an agonist being administered in an amount which would in the absence of a co-administered antagonist provide effects achieved by the drug or agonist alone and at least partially saturate the receptors of said subject, said drug or agonist also at least partially saturating the receptors of the subject and in an amount sufficient to reduce the need for the abused drug, and resulting in reduced satisfaction caused by additional doses of the drug or agonist.
• b) administering to said subject an antagonist to the drug or agonist which blocks effects of the agonist that causes activation of said receptors which are also sensitive to the antagonist, said antagonist being present in an amount sufficient to at least partially block the effects of said drug or agonist on the receptors and also reduce the reinforcing effects of the drug of abuse while there is a sustained amount of the drug or agonist present, such that the administration of the drug or agonist is thus complemented by the antagonist by occupying a number of receptors of the subject responsive to that drug or agonist and which is greater than the number of receptors which would be occupied by the drug or agonist alone without causing under-activity or over-activity of the receptors responsive to said drug or agonist and where any such over-ctivity or under-activity of the receptors is caused by administration of said drug or agonist or withdrawal from the drug or agonist and with the drug or agonist and the antagonist having opposing effects with regard to receptor stimulation and leaving a lesser number of receptors to respond to the drug or agonist due to receptor occupancy,
• c) said receptor activating drug or agonist and said antagonist being administered in amounts and in a ratio to preclude intoxication and thereby reduce a derivation of rewarding effects from the drug by said subject to whom administered and to also prevent a state of withdrawal from the drug or agonist in said subject, and
• d) said drug or agonist being administered by technique other than that to which the subject was accustomed to.

A method of treating and reducing drug dependency without causing over-activity or under-activity in receptors responsive to the drug to thereby mediate the drug dependency where addictive effects of an abused drug causing the dependency results in part from activation of the receptors responsive to that abused drug, said method comprising:

• a) administering to a subject a drug or an agonist of the drug which causes receptors which are responsive to an introduction of that drug to become activated, said drug being administered in an amount which would thereby saturate a substantial amount of the receptors of said subject for said drug or an agonist if administered in the absence of an antagonist to the drug or agonist, and thereby provide substantially the same pharmacologic effects to which the subject is accustomed, said drug or agonist being administered in an amount which satiates the need for the drug or agonist by said subject and resulting in a reduced satisfaction caused by additional doses of the drug or agonist upon self-administration of the drug or agonist,
• b) administering to said subject an antagonist to the drug or agonist that blocks effects of the drug or agonist causing activation of the receptors, said receptors also being sensitive to the antagonist, the antagonist being present in an amount sufficient to at least partially block a substantial amount of the pharmacologic effects of said drug or agonist and thereby reduce the satisfaction to said subject obtained from additional doses of the drug or agonist while a substantial number of the receptors are occupied without causing over-activity or under-activity in the receptors when administration of the abused drug is no longer satisfying, the drug or agonist and the antagonist also being administered in respective amounts to reduce receptor over-activity or under-activity which is caused by administration of said drug or agonist or withdrawal from said drug or agonist and in an amount and a ratio to preclude intoxication, and thereby reduce a derivation of rewarding effects from said drug or agonist by said subject to whom administered and to also prevent a state of withdrawal from the drug or agonist in said subject, such that the administration of said drug or agonist is complemented by said antagonist by occupying a number of receptors of said subject using the drug or agonist which is greater than the number of receptors which would be occupied by the drug or agonist alone, the drug or agonist causing the receptors for the drug or agonist to be activated and the antagonist causing additional receptors for the drug or agonist to be blocked, and where said drug or agonist and said antagonist have opposite effects with regard to receptor stimulation and leaving a lesser number of receptors to respond to the drug or agonist due to receptor occupancy and with said antagonist causing attenuation of response to the drug or agonist, said drug or agonist and said antagonist both being present in an amount such that toxic effects of the amount of the drug or agonist and the toxic effects of the amount of the antagonist are attenuated by each other, and
• c) said drug or agonist being administered by a technique other than that to which the subject was accustomed to.