Progestogen-anti-progestogen regimens

Abstract

An estrogen-free contraceptive is disclosed which does not have the bleeding-related drawbacks of conventional progestogen-only pills. The invention includes a contraceptive kit comprising a combined means for the simultaneous daily administration of a progestogen and an anti-progestogen. The combined means may be in the form of tablets having a normal contraceptive dose of the progestogen and a low dose of the anti-progestogen.

What is claimed is:  
     
         1 . A contraceptive kit comprising: 
 a pharmaceutical product including dosage units, the dosage units comprising a progestogen and an anti-progestogen in daily dosage amounts; and    wherein the pharmaceutical product is configured for the simultaneous, continuous daily administration of both the progestogen and the anti-progestogen;    wherein the daily dosage amount of the anti-progestogen comprises from about 0.05 mg to about 5 mg of (11β, 17β)-11-[4-dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.    
     
     
         2 . The contraceptive kit of  claim 1 , wherein: 
 the daily dosage amount of the progestogen is sufficient to inhibit ovulation; and    the daily dosage amount of the anti-progestogen does not affect ovulation.    
     
     
         3 . The contraceptive kit of  claim 1 , wherein the daily dosage amount of anti-progestogen comprises from about 0.1 mg to about 2.0 mg of (11β,17β)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.  
     
     
         4 . The contraceptive kit of  claim 1 , wherein said kit comprises 28 dosage units.  
     
     
         5 . The contraceptive kit according to  claim 1 , wherein the dosage units are tablets.  
     
     
         6 . The contraceptive kit of  claim 5 , wherein: 
 the tablets are configured for oral administration; and    the tablets form a continuous, monophasic combination of the progestogen and the anti-progestogen.    
     
     
         7 . The contraceptive kit of  claim 1 , wherein: 
 the progestogen is selected from the group consisting of desogestrel, gestodene, and (17α)-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one; and    the anti-progestogen is selected from the group consisting of (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one, (6α, 11β, 17β)-11-(4-dimethylaminophenyl)-6-methyl-4′,5′-dihydrospiro-[estra-4,9-diene-17,2′-(3′H)-furan]-3-one, and (11β,17α)-11-(4-acetylphenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one.    
     
     
         8 . The contraceptive kit of  claim 3 , wherein the daily dosage units further comprise a means for releasing the anti-progestogen in a sustained manner.  
     
     
         9 . A contraceptive kit comprising: 
 a pharmaceutical product including tablets, the tablets comprising a progestogen and an anti-progestogen in daily dosage amounts;    wherein the tablets include an ovulation-inhibiting amount of the progestogen;    wherein the tablets include an amount of the anti-progestogen sufficient to inhibit in vivo anti-progestational activity; and    the contraceptive kit is configured to provide the daily administration of the progestogen and the daily administration of the anti-progestogen.    
     
     
         10 . The contraceptive kit of  claim 9  wherein: 
 the anti-progestogen is (11β,17β)-11-[4-Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one or (11β,17α)-11-(4-acetylphenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one;  
 each tablet includes the progestogen and the anti-progestogen; and  
 the tablets are for daily administration.  
 
     
     
         11 . A method for treating bleeding induced by a progestogen-only contraceptive regimen comprising: 
 administering an anti-progestogen daily and continuously at a dose comprising from about 0.05 mg to about 5 mg (11β,17β)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.    
     
     
         12 . The method according to  claim 11 , wherein the daily dose of anti-progestogen comprises from about 0.1 mg to about 2 mg of (11β,17β)-11-[4-(dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.  
     
     
         13 . A method of contraception comprising: 
 administering dosage units to a female, the dosage units comprising a progestogen and an anti-progestogen for the simultaneous, continuous daily administration of the progestogen and the anti-progestogen;    wherein the daily dosage amount of the anti-progestogen comprises from about 0.05 mg to about 5 mg of (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.    
     
     
         14 . The method according to  claim 13 , wherein the daily dose of anti-progestogen is from about 0.1 mg to about 2 mg of (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one.  
     
     
         15 . The method according to  claim 13 , wherein: 
 the progestogen is selected from the group consisting of desogestrel, gestodene, and (17α)-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one; and    the anti-progestogen is selected from the group consisting of (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)estra-4,9-dien-3-one, (6α,11β,17β)-11-(4-dimethylaminophenyl)-6-methyl-4′, 5′-dihydrospiro-[estra-4,9-diene-17,2′-(3′H)-furan]-3-one and (11β,17α)-11-(4-acetylphenyl)-17,23-epoxy-19,24-dinorchola-4,9,20-trien-3-one.