Method and means for treating alcoholism by extinguishing the alcohol-drinking response using a transdermally administered opiate antagonist

• US 5,096,715 A
• Filed: 11/20/1989
• Issued: 03/17/1992
• Est. Priority Date: 11/20/1989
• Status: Expired due to Term

• Current Assignee: Contral Clinics Oy
• Original Assignee: Alko Ltd.
• Inventors: Sinclair, John D.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Spear, James M.
• Application Number:
  US07/439,050
• Time in Patent Office: 848 Days
• Field of Search: 424/449, 514/282, 514/811
• US Class Current: 424/449
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/48 Preparations in capsules, e.g. of gelatin, of chocolate A61K9/0004 takes precedence; bite capsules A61K9/0056

Abstract

A method for treating alcoholism by extinguishing the alcohol-drinking response in which an opiate antagonist is transdermally administered to a subject and a device for transdermally administering the antagonist. The device is a package containing a fixed dose of opiate antagonist, a vehicle and a permeation enhancer.

Claims

1. A method for treating alcoholism by extinguishing the alcohol-drinking response, comprising the steps of:

transdermally administering to a subject suffering from alcoholism, an opiate antagonist selected from the group consisting of naloxone, naltrexone, cyclazocine, diprenorphine, etazocine, levalorphan, metazocine, nalorphine, and salts thereof, in a daily dosage sufficient to block the stimulatory effect of alcohol, said opiate antagonist being administered by a transdermal delivery means containing a fixed dose of the antagonist, a vehicle and a permeation enhancer;

while the amount of antagonist in the subject'"'"'s body is sufficient to block the stimulatory effect of alcohol, having the subject drink an alcoholic beverage; and

continuing the steps of administration of the opiate antagonist and drinking of an alcoholic beverage until the alcohol-drinking response is extinguished.

2. The method of claim 1 further comprising, after the alcoholic beverage is consume, administering to the subject electric shock an emetic, or an alcohol sensitizing compound.

3. The method of claim 2 wherein the alcohol sensitizing compound is disulfiram or cyanamide.

4. The method of claim 1 further comprising continuing the administration of an opiate antagonist after the alcohol-drinking response is extinguished.

5. The method of claim 1 wherein the transdermal means is a capsule that is easily rupturable when pressed against the skin.

6. The method of claim 5 wherein the volume of the capsule is in the range of 0.001 to 2 ml.

7. The method of claim 1 wherein the transdermal means is a sachet or squeeze tube with a net volume ranging from 0.05 to 2 ml.

8. The method of claim 1 wherein the opiate antagonist is naloxone and the fixed dose is 0.2 to 40 mg.

9. The method of claim 1 wherein the opiate antagonist is naltrexone and the fixed dose is 20 to 300 mg.

10. The method of claim 1 wherein the vehicle is selected from the group consisting of propylene glycol, isopropanol, ethanol, oleic acid, N-methylpyrrolidone, sesame oil, olive oil, wood alcohol ointments, vaseline, and triglyceride gel.

11. The method of claim 1 wherein the permeation enhancer is selected from the group consisting of saturated and unsaturated fatty acids and their esters;

alcohols;

acetates;

monoglycerides, diethanolamides and N,N-dimethylamides.

12. The method of claim 11 wherein the permeation enhancer is selected from the group consisting of linolenic acid, linolenyl alcohol, oleic acid, oleyl alcohol, stearic acid, stearyl alcohol, palmitic acid, palmityl alcohol, myristic acid, myristyl alcohol, 1-dodecanol, 2-dodecanol, lauric acid, decanol, capric acid, octanol, caprylic acid, 1-dodecylazacycloheptan-2-one, ethyl caprylate, isopropyl myristate, hexamethylene lauramide, hexamethylene palmitate, capryl alcohol, decyl methyl sulfoxide, dimethyl sulfoxide, salicylic acid and derivatives, N,N-diethyl-m-toluamide, crotamiton, 1-substituted azacycloalkan-2-ones, and polyethylene glycol manolaurate.