Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-06-29
1995-06-20
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514557, 514810, 514811, 514812, 514813, 514909, 514910, A61K 3119, A61K 3134, A61K 31045
Patent
active
054261201
DESCRIPTION:
BRIEF SUMMARY
This application is the National stage of PCT/EP92/01409, filed 23 Jun. 1992.
The present invention relates to pharmaceutical compositions having therapeutic effects on abstinence, on craving (the intense and compulsive desire for a substance), and on dependence on drugs, drugs of abuse, psychotropics, stupefacient and/or psychoactive substances, nicotine and also on nutritional disorders (in particular bulimia, obesity and anorexia) , such compositions being characterised in that they contain, as the active principle, .gamma.-hydroxybutyric acid (GHB), or salts thereof with pharmaceutically acceptable cations, or the corresponding lactone.
The invention further relates to the use of .gamma.-hydroxybutyric acid or of its physiologically equivalent forms for the preparation of a medicament which is useful in the treatment of the withdrawal syndrome induced by drugs, drugs of abuse, psychotropics, stupefacient and/or psychoactive substances and nicotine.
The relevant salts of GHB include, for example, alkali metal (e.g. sodium or potassium) salts, alkaline earth metal (e.g. calcium or magnesium) salts, ammonium salts, salts of pharmaceutically acceptable bases (ethanolamine, diethanolamine, piperidine, piperazine and the like) , salts of basic amino acids (lysine, ornithine, citrulline) etc.
GHB, various salts thereof and its lactone have been known for decades. The acid is a normal constituent of the central nervous system (CNS) of mammals, with the highest concentration in the hypothalamus and in the basal ganglia (c % 1.78 nM/g and 4.1 nM/g in rats and in guinea pigs, respectively).
The almost universal prevalence of binding sites for GHB in the CNS makes it probable that such a compound acts as a neurotransmitter and as neuro-modulator, rather than as incidental metabolite of .gamma.-aminobutyric acid (GABA). The use of GHB in clinical practice has been known for many years for general anaesthetic and narcoleptic purposes, with prevailing utilisation by way of intravenous administration (see Anesth. Analg. (Cleve), 41, 721-726, 1962; Science 143, 1045-1047, 1964; Electroencephalogr. Clin. Neurophysiol., 22, 558-562, 1967; Sleep, 9, 285-289, 1986). More recently, the clinical use of GHB for ethyl alcohol anti-abstinence purposes has been described (see The Lancet, 2,787-789, 1989).
It has now surprisingly been found that .gamma.-hydroxybutyric acid and physiologically equivalent forms can advantageously be utilised for the treatment of the so-called withdrawal syndrome from drugs, drugs of abuse, psychotropics, stupefacient and/or psychoactive substances and from nicotine; in particular, drugs such as narcotics, opiates, cocaine, cannabinoids or psychoactive substances such as benzodiazepines, psychostimulants, amphetamines, nicotine and their derivatives or the like. The use of .gamma.-hydroxybutyric acid has also proved to be effective in the treatment of nutritional disorders such as bulimia, obesity and anorexia.
The withdrawal syndromes, dependences on drugs, drugs of abuse, psychotropics, stupefacient and/or psychoactive substances and nutritional disorders have as their common denominator the manifestation of so-called "craving" which can be defined as an intense and compulsive desire for a given substance or a given food.
.gamma.-Hydroxybutyric acid has proved to be particularly active in inhibiting the onset of such-symptoms, as it has been possible to demonstrate on the basis of clinical experiments on 23 subjects meeting the diagnostic criteria of opiate dependence and on 3 patients affected by nutritional disorders (one case of anorexia, one of bulimia and one of obesity).
Table 1 shows the characteristics of the groups of subjects employed, in accordance with a "double blind" scheme, for the study of the activity of GHB in the treatment of the opiate withdrawal syndrome.
Eleven subjects were treated with GHB, including six who had used heroin in the last 24 hours (5 M, 1 F) and 5 undergoing methadone treatment (4 M, 1 F).
The control group consisted of 12 patients, 7 who used heroin (6 M, 1 F
Crepaldi Gaetano
Ferrara Santo
Gallimberti Luigi
Gessa Gian L.
Hydorn Michael B.
Richter Johann
LandOfFree
Pharmaceutical composition containing .gamma.-hydroxybutyric aci does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical composition containing .gamma.-hydroxybutyric aci, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical composition containing .gamma.-hydroxybutyric aci will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1844343