Title: Composition for controlling mood disorders in
United States Patent: 6,335,021
Inventors: Cavazza; Claudio (Rome, IT)
Assignee: Sigma-Tau HealthScience S.p.A. (Pomezia, IT)
Appl. No.: 446358
Filed: December 20, 1999
PCT Filed: June 12, 1998
PCT NO: PCT/IT98/00157
371 Date: December 20, 1999
102(e) Date: December 20, 1999
PCT PUB.NO.: WO98/57629
PCT PUB. Date: December 23, 1998
Foreign Application Priority Data: Jun 18, 1997[IT]
The use of acetyl L-carnitine and its pharmacologically acceptable
salts is disclosed for producing a composition suitable for controlling
mood disorders mainly in young individuals who are not affected by
permanent pathological CNS disturbances.
Description of the Invention
The present invention relates to the use of acetyl L-carnitine
and its pharmacologically accetable salts for producing a composition
suitable for controlling mood disorders in individuals not presenting
permanent pathological alterations of the central nervous system (CNS) by
restoring the normal balance of neurotransmitter levels.
For the purposes of the present invention what is meant by "mood
disorders" are those disorders which present as behavioural
alterations of a depressive or manic type and, in particular, those
disorders that present as oscillations between depressive and manic states
alternating in the same individual. According to the present invention,
these disorders also include the so-called premenstrual syndrome and
states of bulimia.
Normal variations in mood (melancholy, mildly depressed states, anguish or
joy and moderate excitement) constitute habitual aspects of daily life and
must be distinguished from the pathological fluctuations of affective
Nevertheless, increasingly wide oscillations in affective attitudes and in
that complex series of behavioural reactions and expressions, whether
towards the self or towards external reality, which we define
synthetically as "mood", would appear to affect an increasingly
large population, consisting mainly of young individuals. Though the
extent of such oscillations fails to reach the threshold of pathological
relevance, this phenomenon is beginning to have substantial repercussions
on important aspects of family life and on social and personal relations
with profound consequences even of a socio-economic nature.
The main cause of this phenomenon probably has to do with the profound
changes in lifestyle which have occurred, particularly with regard to
young individuals, over a relatively short space of time.
Whereas, on the one hand, the opportunities for socialising (from travel
and holidays even in far-off locations to attending public events and
frequenting public meeting places, such as discotheques, aimed mainly at
attracting a youthful population) have increased enormously compared to
the past, amongst other things as a by-product of the boom in affluence,
this phenomenon also presents worrying negative aspects such as the
increased use of beverages with a strong alcohol content and the ever
wider diffusion of psycho-active substances and of soft and hard drugs.
Set against the liberalisation of sexual habits and the increasingly
widespread use and greater safety of contraceptive methods is the fear of
sexually transmitted diseases, the most notable, of course, being AIDS,
with its deterrent burden of anxiety which can have adverse repercussions
on the normal expression of libido in both male and female subjects.
It is therefore hardly surprising that increasingly large numbers of the
younger population are suffering from mood disorders.
These disorders which have a tendency to become chronic, but which exclude
the precipitation of major or decidedly bipolar, cyclothymic depression
disorders, are currently classified as dysthymias (DSM IV, 300.40)
according to the definition provided by the authoritative Diagnostic and
Statistical Manual of Mental Disorders (DSM IV) published by the American
In these dysthymic individuals, who present a reduced social functional
capability due to the chronic nature of their disorders, and certainly not
as a result of the severity of their depressive or manic disturbances,
there are often associated disorders of eating habits, with lack of
appetite or bulimia, insomnia or hypersomnia, asthenia and fatigue, and
reduced self-esteem, concentration and decision-making ability.
The attempts made to date to treat the mood disorders described above with
well-known tricyclic antidepressants such as imipramine, nortriptyline,
desipramine, amitriptyline etc., have failed to yield satisfactory
results, whereas, in younger subjects particularly, their troublesome side
effects such as sedation, dry mouth, tremors, postural vertigo, blurred
vision, sweating and constipation are poorly tolerated.
It has now been found that acetyl L-carnitine and its pharmacologically
acceptable salts constitute an effective means of treating the
above-described mood disorders essentially without presenting any of the
side effects typical of tricyclic antidepressants.
The object of the present invention thus consists in the use of acetyl L-carnitine
or of one of its pharmacologically acceptable salts to produce a
composition suitable for controlling mood disorders in individuals not
presenting permanent pathological alterations of the central nervous
system (CNS) by restoring the normal balance of neurotransmitter levels.
It is important to note that, since the subjects who are to receive the
compositions of the present invention are essentially healthy and do not
present fluctuations of pathological significance in their affective or
mood disorders, the compositions of the invention may present themselves
not only as pharmaceutical compositions, but also as health foods, medical
foods or nutraceuticals, or as components of such products, containing
other active ingredients, dietary supplements, vitamins, co-enzymes,
mineral substances and the like in combination with acetyl L-carnitine.
The compositions of the invention are formulated, as regards their
presentation form, nature of the unit dose form, weight and so on, in such
a way as to favour administration of 500-3000 mg/day of acetyl L-carnitine
or a molar equivalent amount of one of its pharmacologically acceptable
salts to subjects who need it, either in a single dose or according to a
multidose administration regimen.
In cases in which the subject suffering from a mood disorder, as defined
in the context of the invention described herein, is also a bulimic or
overweight subject (bulimia and depression often being associated
manifestations in the same subject), the compositions may also
advantageously include an effective amount of 5-hydroxy-tryptophane
(5-HTP) in addition to acetyl L-carnitine or one of its pharmacologically
Compositions suitable for such subjects are those which, as a result of
their presentation form, type of unit dose form, weight and so on, favour
the administration to the subject of 500-1500 mg/day of acetyl L-carnitine
or a molar equivalent amount of one of its pharmacologically acceptable
salts and 300-700 mg/day of 5-hydroxy-tryptophane.
Claim 1 of 27 Claims
What is claimed is:
1. A composition, comprising:
acetyl L-carnitine or its pharmacologically acceptable salt;
an excipient; and 5hydroxy-tryptophane.
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