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United States Patent 19 11) Patent Number: 4,565,689 Revici 45 Date of Patent: Jan

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United States Patent 19 11) Patent Number: 4,565,689 Revici 45 Date of Patent: Jan United States Patent 19 11) Patent Number: 4,565,689 Revici 45 Date of Patent: Jan. 21, 1986 54 METHOD FORTREATING THE EFFECTS 56 References Cited OF ALCOHOL U.S. PATENT DOCUMENTS 75 Inventor: Emanuel Revici, New York, N.Y. 4,346,082 8/1982 Revici................................. 424/162 (73) Assignee: Wirth Maschinen-und Primary Examiner-Stanley J. Friedman Bohrgerate-Fabrik GmbH, New Attorney, Agent, or Firm-Pennie & Edmonds York, N.Y. 57 ABSTRACT Appl. No.: 722,870 A method for treating or aiding in the treatment of the (21) manifestations of alcoholism or alcohol intoxication by 22 Filed: Apr. 12, 1985 aiding in the control of the craving for alcohol or by aiding in the control of alcohol withdrawal symptoms, 51 Int. Cl.' ................... A61K 31/21; A61K 31/095; or by aiding in the control of alcohol intoxication in a A61K 31/105; A61K 31/265; A61K 31/045; human which comprises internally administering to said A61K 33/04 human an effective amount of a compound having an (52) U.S. C. ...................................... 424/10; 424/162; active ingredient containing at least one bivalent nega 514/512; 514/513; 514/706; 514/707; 514/724; tive sulfur to control said craving, symptoms, or intoxi 514/738; 514/811 cation so as to counteract the effects of alcohol. 58 Field of Search .................. 424/10, 162; 514/512, 514/513, 706, 707, 724, 738, 810, 812, 813 13 Claims, No Drawings 4,565,689 & 1. 2 U.S. Pat. No. 2,799,619 to Seifter et al. discloses com METHOD FORTREATING THE EFFECTS OF positions comprising certain phenothiazines as effective ALCOHOL for treatment of alcoholics while British Pat. No. 1,399,992 (Revici) discloses that compositions compris TECHNICAL FIELD ing certain organic ethers are useful for the treatment of The invention relates to a method for eliminating or alcoholism. reducing the noxious effects of alcohol through the U.S. Pat. No. 4,346,082, granted to the applicant on administration of catabolic sulfur-containing com Aug. 24, 1982 discloses a method of treating alcoholism pounds. and for eliminating, reducing or preventing alcohol 10 intoxication in humans by internally administering a DESCRIPTION OF THE PRIOR ART therapeutic composition comprising an ammonium compound or compounds having a pH greater than 5.0 There has been much recent interest in the study of when placed in aqueous solution at a concentration of 5 alcoholism involving biological, psychological, and grams per 100 grams of solution, and particularly, am sociological investigations. Publications such as the 15 monium salt compounds comprising ammonium cations various "Proceedings of the . Annual Alcoholism and sulfur anions. Conference' and "Recent advances in Studies of Alco Further U.S. Pat. No. 4,368,206, issued to applicant holism', obtainable from the Superintendent of Docu on Jan. 11, 1983 discloses an alternate method of treat ments, U.S. Government Printing Office, Washington, ing alcoholism and for aiding in controlling alcohol D.C. 20402, indicate the rather intensive scientific in 20 intoxication in humans by the internal administration of vestigations in this area. a composition produced by heating certain allylically An article by E. B. Truitt and M. J. Walsh appearing unsaturated compounds sufficient to substantially in at p. 100 et sequa of "Proceedings of the First Annual crease the peroxide titer. The incorporation of sulfur Alcoholism Conference of the National Institute on into these compositions during the heating process was Alcohol Abuse and Alcoholism', DHEW Publication 25 found to be particularly advantageous. No. (NIH) 74-675 (1973) discloses a number of chemi Applicant has now discovered that a number of addi cals and drugs which have been reported to have anti tional compounds are effective for treating the effects of alcohol effects. Included in this list are disulfuram (tet alcohol. raethylthiuram disulfide-see also U.S. Pat. No. 2,567,814 Jacobsen et al), calcium carbimide (see also 30 SUMMARY OF THE INVENTION U.S. Pat. No. 2,998,350 de Grunigen et al), and thiocya The invention relates to a method for treating or nates which are used specifically for their anti-alcohol aiding in the treatment of the manifestations of alcohol properties. ism or alcohol addiction by aiding in the control of the U.S. Pat. No. 3,860,719 to Marshall discloses the use craving for alcohol or by aiding in the control of alco of 2-3,4-dichlorophenoxy)methyl)-2-imidazoline hy 35 hol withdrawal symptoms or by aiding in the control of drochlorine (fenmetozole HC1) for combatting ethanol alcohol intoxification in a human by internally adminis intoxication in mammals. tering a compound with an active ingredient containing However, an article by H. B. McNamee et al "Fen at least one bivalent negative sulfur in an amount suffi metozole in Acute Alcohol Intoxication in Man', Clini cient to control the craving for alcohol or the symptoms cal Pharmacology and Therapeutics Vol. 17, Number 6, 40 caused by abstaining from it. pp. 735-737 concludes that, within the scope of the The most clinically effective compounds for this subject study, fenmetozole does not antagonize or sig purpose are the hydropersulfides, alkyl sulfides, colloi nificantly modify acute effects of alcohol intoxification dal sulfur and organic thio compounds or their pharma in humans. ceutically acceptable salts. The most effective thio com Another publication entitled "Testing For a "Sober 45 pounds to date are the thioglycerols and ethylenetrithio ing Pill” DOT HS-801 288 (1974) available from Na carbonate or their pharmaceutically acceptable salts. tional Technical Information Service, Springfield, Va. These compounds are amenable to oral administra 22151 discloses that nikethamide, propranolol, L-dopa, tion into the human body by mixing it with suitable pipradrol, aminophylline, ephedrine, sted-eze, and am binders or bulking materials, and placing an amount of monium chloride were investigated to determine their 50 the active material which is equal to a therapeutic dos potential for blocking or neutralizing the effect of alco age level into a pharmaceutical capsule. hol on a human brain; the most effective amethystic The preferred therapeutic dosage level is about 100 agent found was L-dopa. milligrams of the active ingredient and the subject J. L. Mottin, in an article entitled "Drug-Induced should be instructed to ingest a sufficient number of Attenuation of Alcohol Consumption' Quart J. Stud. 55 capsules to reduce or eliminate the desire to drink or to Alc. 34: 444-472 (1973) discussed, inter alia, the use of reduce or eliminate the affects of alcohol. The active the following compounds re the subject title: disul ingredient may also be administered, however, by furam, citrated calcium cyanamide, and metronidazole. means of an injection, which allows the active ingredi Russian Inventor's Certificate 187250 discloses the ent to work more quickly, initially. The most clinically use of the "thiolic' preparations-“unitol' and "dicap effective active ingredient is ethylene trithio carbonate tol'-for use in treating alcoholism. The Merck Index and thioglycerols. (Eighth Edition) discloses that Dicaptol (BAL or Brit ish Anti-Lewisite) is 2,3-dimercaptopropanol and is DETAIILED DESCRIPTION OF THE marketed as a 10% solution in peanut oil with 20% PREFERRED EMBODIMENTS benzyl benzoate. It is further asserted that in the 65 It is desirable to have a method for treating or aiding U.S.S.R., a water soluble form is available under the in the treatment of alcoholism in a human by controlling name Unithiol and is 2,3-dimercapto-1-propanol sodium the craving for alcohol, by controlling withdrawal sulfonate. symptons, or by aiding in the control of alcohol intoxi 4,565,689 3 4. cation by humans. It is further desirable to have a subject's need for alcohol or to reduce or eliminate its method for aiding the control of alcohol intoxication of effects after consumption. a non-alcoholic person by reducing or eliminating the As an alternate embodiment of the present invention, effects alcohol intoxication upon him as well. the compounds disclosed hrein may also be mixed with A series of tests run on alcoholic compounds by the the compounds disclosed in U.S. Pat. No. 4,368,206. applicant has shown them to possess a manifest anabolic Therefore, the teachings of this patent are expressly action, due to the presence of a positively charged hy incorporated herein. droxyl (OH) group. This anabolic action is also due to While it is apparent that the invention herein dis the solubility of the alcohols in lipids, which are fatty closed is well calculated to fulfill the objects above substances found in the human body. Due to the small 10 stated, it will be appeciated that numerous modifica number of carbon atoms which form the organic struc tions and embodiments may be devised by those skilled ture of ethyl alcohol (CH3CH2OH) and of other alco in the art, and it is intended that the appended claims hols present in alcoholic beverages, the anabolic action cover all such modifications and embodiments as fall referred to hereinabove is manifested at the higher lev within the time spirit and scope of the present invention. els of the body's hierarchic organization, i.e., mainly the 15 I claim: organic and systemic levels. 1. A method for treating or aiding in the treating of Alcoholic compounds induce the typical anabolic the manifestations of alcoholism or alcohol intoxication manifestations, which include a preliminary excitation by adding in the control of the craving for alcohol or by stage followed by a relaxant stage. The applicant has aiding in the control of alcohol withdrawal symptoms, discovered that the adminstration of catabolic agent to 20 or by aiding in the control of alcoholic intoxication in a a human subject, which is antigonistic to the anobolic human having said manifestations, craving, symptoms effect of alcohol, is an extremely satisfactory technique or intoxication which comprises internally administer for counteracting the subject's desire to drink.
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