Substance with sedative effect

Abstract

A substance with sedative effect comprises a therapeutically effective amount of a gamma-pyrone such as comenic acid, meconic acid, 5-methoxy-gamma-pyrone-2-carboxylic acid, and alike in a pharmaceutically acceptable carrier. When administered at a daily dosage of between 0.05 mg to about 10,000 mg of active ingredient per unit dose of a patient, the substance can be used to treat various disorders of a nervous system such as pain, insomnia, anxiety, neurosis, depression, as well as withdrawal symptoms experienced by drug addiction patients, especially for patients addicted to opiate-based drugs. The substance can be delivered in a number of ways of systemic administration of a pharmaceutical agent including oral, parenteral, transdermal, and transmucosal administration. For drug addicted patients, the preferred method of administration involves a subcutaneous implant providing a continuous release of an active ingredient at an effective daily rate over the entire treatment period ranging from 5 to 30 days, and preferably from 13 to 20 days.

1 . A substance for treating a disorder of a nervous system comprising a gamma-pyrone compound and a pharmaceutically acceptable carrier in a unit dosage form, said unit dosage containing from about 0.05 mg to about 10,000 mg of said gamma-pyrone, said substance prepared in a form suitable for systemic administration, said gamma-pyrone molecule having a carboxy group in position 2 of the pyranone ring, said gamma-pyrone molecule also having a carbonyl group in position 4 of the pyranone ring, said gamma-pyrone molecule further having a substituent in position 5 capable of participating in Ca 2+  chelation.  
   
   
       2 . The substance as in  claim 1 , wherein said gamma-pyrone compound is 5-methoxy-gamma-pyrone-2-carboxylic acid.  
   
   
       3 . The substance as in  claim 1  prepared in a form suitable for parenteral administration.  
   
   
       4 . The substance as in  claim 1  prepared in a form suitable for transdermal administration.  
   
   
       5 . The substance as in  claim 1  prepared in a form suitable for transmucosal administration.  
   
   
       6 . The substance as in  claim 1  prepared in a form suitable for inhalation administration.  
   
   
       7 . The substance as in  claim 1  prepared in a form suitable for oral administration.  
   
   
       8 . The substance as in  claim 1 , wherein said pharmaceutically acceptable carrier includes disassociated ions of calcium.  
   
   
       9 . The substance as in  claim 1 , wherein said pharmaceutically acceptable carrier includes disassociated ions of sodium.  
   
   
       10 . The substance as in  claim 1 , wherein said unit dosage containing from about 1 mg to about 100 mg of said gamma-pyrone compound.  
   
   
       11 . The substance as in  claim 1  prepared to be capable of providing sustained systemic release of the gamma-pyrone over a time period of between 5 and 30 days, said substance prepared in a form suitable for injection or subcutaneous implantation.  
   
   
       12 . The substance as in  claim 11 , wherein said time period is between 13 and 20 days.  
   
   
       13 . The substance as in  claim 11 , wherein the release rate of said gamma-pyrone is between about 2 mg to about 200 mg per day.  
   
   
       14 . A method for treatment of a subject with a disorder of a nervous system, said method including systemic administration of a therapeutically effective amount of a substance comprising a pharmaceutically acceptable carrier with a gamma-pyrone molecule, said gamma-pyrone molecule having a carboxy group in position 2 of the pyranone ring, said gamma-pyrone molecule also having a carbonyl group in position 4 of the pyranone ring, said gamma-pyrone molecule further having a substituent in position 5 capable of participating in Ca 2+  chelation.  
   
   
       15 . The method as in  claim 14 , wherein said gamma-pyrone compound is 5-methoxy-gamma-pyrone-2-carboxylic acid.  
   
   
       16 . The method as in  claim 14 , wherein said therapeutically effective amount defined as a daily dosage ranging from about 0.001 mg to about 40 mg of said gamma-pyrone per kilogram of body weight of said subject.  
   
   
       17 . The method as in  claim 14 , wherein said daily dosage ranging from about 3 to about 100 mg per subject.  
   
   
       18 . The method as in  claim 14 , wherein said disorder of a nervous system is pain.  
   
   
       19 . The method as in  claim 14 , wherein said disorder of a nervous system is anxiety.  
   
   
       20 . The method as in  claim 14 , wherein said disorder of a nervous system is insomnia.  
   
   
       21 . The method as in  claim 14 , wherein said disorder of a nervous system is depression.  
   
   
       22 . The method as in  claim 14 , wherein said disorder of a nervous system is neurosis.  
   
   
       23 . The method as in  claim 14 , wherein said disorder of a nervous system is pain and other symptoms associated with withdrawal syndrome in drug abuse treatment.  
   
   
       24 . The method as in  claim 23 , wherein said drug is based on opioid and its alkaloids.  
   
   
       25 . The method as in  claim 14 , wherein the duration of said treatment is from about 5 to about 30 days.  
   
   
       26 . The method as in  claim 25 , wherein said duration is from about 13 to about 20 days.  
   
   
       27 . The method as in  claim 14 , wherein said substance is in a form suitable for parenteral administration.  
   
   
       28 . The method as in  claim 14 , wherein said substance is in a form suitable for transmucosal administration.  
   
   
       29 . The method as in  claim 14 , wherein said substance is in a form suitable for transdermal administration.  
   
   
       30 . The method as in  claim 14 , wherein said substance is in a form suitable for continuous release administration via an injection or a subcutaneous implant.  
   
   
       31 . The method as in  claim 30 , wherein said substance is in a form for continuous release administration for the entire treatment duration.  
   
   
       32 . The method as in  claim 31 , wherein said duration is between about 13 and about 30 days.  
   
   
       33 . The substance as in  claim 14 , wherein said pharmaceutically acceptable carrier includes disassociated ions of calcium.  
   
   
       34 . The substance as in  claim 14 , wherein said pharmaceutically acceptable carrier includes disassociated ions of sodium.  
   
   
       35 . A method for treatment of a subject with a disorder of a nervous system of a type being effected by modulation of a slow sodium channel signaling pathway involving ligand-receptor binding in the opioid receptor site area and a tetrodotoxin-resistant slow sodium channel known as Na v 1.8, said method including administration of a therapeutically effective amount of a substance with sedative effect comprising a gamma-pyrone compound and a pharmaceutically acceptable carrier, whereby said substance effects modulation of said sodium channels without causing physical dependency typically associated with opiates.  
   
   
       36 . The method as in  claim 35 , wherein said gamma-pyrone compound having a carboxy group in position 2 of the pyranone ring, said gamma-pyrone molecule also having a carbonyl group in position 4 of the pyranone ring, said gamma-pyrone molecule further having a substituent in position 5 capable of participating in Ca 2+  chelation.