USE OF PSYCHOACTIVE DRUGS AS VAGINAL CONTRACEPTIVES

Abstract: The present invention relates to prevention of conception. The use of psychoactive drugs as vaginal contraceptives is disclosed. The following classes of psychoactive drugs have been shown to be effective in preventing conception by inhibiting the function of the regulatory protein calmodulin phenothiazines, thioxanthenes, butyrophenones, diphenylbutylamines, dibenzodiazepines, benzodiazepines, dibenzazepines. The invention may be implemented by incorporating a psychoactive drag in a known application method such as jelly, foam, or suppository introduction means prior to intercourse. Furthermore, the use of psychoactive drugs after intercourse using the above methods is disclosed.

Description: Description USE OF PSYCHOACTIVE DRUGS AS VAGINAL CONTRACEPTIVES Technical Field The present invention relates to a method of preventing conception. More specifically, the present invention relates to the use of psycho- active drugs as vaginal contraceptives. Presently, many forms of contraception are available, including oral contraceptives, me¬ chanical contraceptives, and vaginal contracep¬ tive solutions generally comprising spermato- cides. Each form of contraception suffers from undesirable characteristics such as varying ef- fectiveness , discomfort, or physical side ef¬ fects. Background Art Vaginal contraceptives comprising spermato- cidal agents are well known in the prior art in many methods of usage, including jellies and creams (hereinafter referred to as jelly), foams from tablets or aerosols, and suppositories. However, these methods are among the least ef¬ fective in terms of preventing conception and are basically unsatisfactory as a sole method of contraception. Psychoactive drugs are . currently used clin¬ ically to treat certain types of mental disord¬ ers and stress. Chemical classes of psychoac- tive drugs and examples of drugs in each class are as follows: Chemical Class Examples Phenothiazines Trifluoperazine Fluphenazine -2- Thior idaz ine Chlorpromaz ine Pro ethaz ine Thioxanth enes Chlorprothixene Butyrophenones Penf lur idol Benperidol Haloperidol Diphenylbutylamines Pimozide Dibenzodiaz epines Clozapine 10 Benzod iazepines Medazepam Chlordiazepoxide Dibenzazepines Imipra ine A triptyline Protriptyline 15 Desipramine The use of psychoactive drugs as medications to affect mental processes has become widespread since the early 1950's. Such use typically en¬ tails taking such drugs internally at dosages 20 ranging from 10 to 120 milligrams daily. For a detailed background of such use and description of such drugs see Chapter 12 of The Pharmacolog¬ ical Basis of Theraputics, 5th Ed. , edited by L. S. Goodman and A. Gilman (1975). 25 Disclosure of Invention The present invention comprises the use of psychoactive drugs as vaginal contraceptives. The introduction of such drugs into the vagina can be accomplished by any of the many commonly 30 available methods currently used in conjunction with spermatocides, such as jelly, foam or sup¬ pository means. By substitution of the appro¬ priate amount or concentration of a psychoactive drug in place of, or in addition to, the sperma- 35 tocidal agent in any of these means, a form of OM /., W WII contraceptive embodying the invention, to be ap¬ plied in the same manner prior to sexual inter¬ course, is accomplished. The present invention also comprises the use of a psychoactive drug shortly after intercourse to prevent concep¬ tion. This may be accomplished by use of a sup¬ pository, jelly or other suitable vehicle con¬ taining the appropriate amount of a psychoactive drug. As stated previously, current forms of vagi¬ nal contraceptives are based on the use of sper- atocides , which are intended to kill the sperm. Generally, the use of such contracep¬ tives by themselves have not proven to be a sat- isfactorily effective contraceptive method. The present invention does not involve the killing of the sperm, but instead directly and . specific- ally blocks the physiological process of concep¬ tion and results in greatly improved effective- ness of contraception. It has been shown in the past few years that there is a regulatory protein known as calmodu¬ lin, found in all cells of higher organisms and which is the key to the control of a wide vari- ety of physiological processes. Calmodulin is involved in triggering the activation of mamma¬ lian spermatozoa, a prerequisite to the fertili¬ zation process. Calmodulin is a calcium binding protein, which means that when calcium is bound to the protein the resulting calcium-protein complex turns on a variety of cellular processes including spermatozoan activation. It is known that psychoactive drugs will bind tightly to calmodulin only in the presence of calcium. The binding of these drugs to cal¬ modulin results in the inhibition of calmoduli function. Of the many thousands of proteins found in a cell, calmodulin is the only detect¬ able target of psychoactive drugs. Thus, psy¬ choactive drugs are specific in their binding to 5 calmodulin and will specifically inhibit calmod¬ ulin function. The use of a psychoactive drug as a vaginal contraceptive has a number of advantages. First, it is extremely effective since the spe- 10 cific binding of the drug to calmodulin would turn off spermatozoan activation and thus pre¬ vent fertilization. Experimental evidence has demonstrated that the phenothiazine drugs pene¬ trate the spermatozoan membranes within seconds 15 and concentrate in the region of the cell occu¬ pied by calmodulin. Second, there will be no expected side effects since, the drug would not be used internally and since low concentrations will be very effective as a vaginal contracep- 20 tive. Third, the effectiveness of an applica¬ tion may last for hours due to the stability of these drugs. Additionally, evidence has indicated that calmodulin is also the target protein during 25 ovum activation since this is also a calcium de¬ pendent process. Thus if the drug comes into contact with the ovum, fertilization will not occur. It is seen, therefore, that the present invention may be doubly effective by preventing 30 activation of both the sperm and the egg. Best Mode for Carrying Out the Invention The most effective drugs for contraceptive purposes can be predicted based on their effec¬ tiveness in binding to calmodulin. Therefore, 35 the most promising specific drugs, in order of OMPI effectiveness, are: penfluridol, pimozide, tri¬ fluoperazine, f luphenazine, chlorprothixene, thioridazine, chlorpromazine , benperidol, ha- loperidol, and clozapine. While a concentration of 0.5% (5 milligrams per milliliter of jelly) will be effective in the most effective drugs such as penfluridol or trifluoperazine, less ef¬ fective drugs will require a higher concentra¬ tion to achieve similar effectiveness. A preferred embodiment of the present inven¬ tion comprises a one-half percent concentration of trifluoperazine in a jelly, introduced into the vagina in sufficient quantity and under known methods prior to sexual intercourse and allowed to remain therein for a period of time, preferably more than a few hours, after inter¬ course.

Claims: Claims 1. A method for preventing conception in a female which comprises: introducing a psy¬ choactive drug into the vagina of the female. 5 2. The method as described in claim 1 wherein the introduction of said pschoactive drug comprises the steps of: introducing said psychoactive drug into the vagina of the female prior to sexual intercourse; and 10 allowing said psychoactive drug to remain in the vagina during and after sexual inter¬ course. 3. The method as described in claim 2, wherein the step of introducing said psycho- 15 active drug comprises the steps of: mixing said psychoactive drug with a foam carrier; and introducing said mixture into the vagina of the female prior to sexual intercourse by foam injection means. 20 4. The method as described in claim 2, wherein the step of introducing said psycho¬ active drug comprises the steps of: mixing said psychoactive drug with a jelly carrier; and introducing said mixture into the vagina 25 of the female prior to sexual intercourse by jelly insertion means. 5. The method as described in claim 2, wherein said psychoactive drug is introduced into the vagina of the female by suppository 30 means. 6. The method as descr ibed in claim 1 wherein the introducti on of said psychoac¬ tive drug compris es : introducing said psy¬ choactive drug into the vagina after sexual 35 intercour se. 7. The method as described in claim 6, wherein the step of introducing said. psycho¬ active drug comprises the steps of: mixing said psychoactive drug with a suitable car- 5 rier; and introducing the mixture into the vagina. 8. The method as described by claims 1, 2, 3, 4, 5, 6, or 7, wherein said psychoactive drug is selected from the group consisting 10 of the phenothiazines, thioxanthenes , buty- rophenones, diphenylbutylamines, dibenzodi- azepines, benzodiazepines, and dibenzaze- pines. 9. The method as described by claims 1, 2, 15 3, 4, 5, 6, or 7 wherein said psychoactive drug is selected from the group consisting of penfluridol, pimozide, trifluoperazine, fluphenazine, chlorprothixene, thioridazine, chlorpro azine, benperidol, haloperidol, and 20 clozapine. 10. The method as described by claim 9 wherein the amount of the psychoactive drug introduced into the vagina is about 10 mil¬ ligrams or greater.

Inventors: CORMIER M
Applicants: UNIV GEORGIA, UNIV GEORGIA RES FOUND INC
Application year: 1980
Main classification: A61K31
IPC codes: A61K9, A61K31