GB2510374A - Formulation comprising N-acetylcarnitine and D-ribose - Google Patents

Abstract

 A formulation for the treatment of chronic fatigue syndrome, fibromyalgia and some depressions comprises a combination of N-acetylcarnitine and D-ribose. The formulation may also comprise: dl-phenylalanine, green tea extract, GABA, ginseng, caffeine, vitamin D3, fish oils, and multi vitamins.

Description

Description A Formulation for the treatment of chronic fatigue syndrome, chronic fatigue, fibromyalgia and depression Many patients afflicted with chronic fatigue or fibromyalgia or depression, fail to respond to conventional treatments.

A formulation comprised of N-acetylcarnitine (500 mg), D-ribose (750 mg) with further ingredients for increased therapeutic benefit including dI-phenylalanine (500mg), green tea extract (300mg standardised extract at 15% polyphenols), Korean ginseng (500mg panax ginseng at 2% ginsenosides), omega-3 fish oils (8000mg comprising 2400mg total EPA/DMA omega-3), vitamin D3 (25 micro grammes), multi-vitamins (international standard daily dose formulation) -This formulation was found very therapeutic to chronic fatigue with depression and anxiety.

This formulation was administered either as a single morning dose, or divided as a morning dose of N-acetylcarnitine, Korean ginseng and D-ribose, vitamin D3, multi vitamins (international standard formulation) and fish oils, followed by an afternoon dose of dI-phenylalanine and green tea extract.

Doses were as described above.

Alternatively for a simpler dosing regime, a complete formulation dose may be given once a day in mornings, or a complete formulation dose at half strength once in morning and once in the afternoon should afternoon fatigue be particularly problematic.

Higher total daily doses of d-ribose (up to 3g maximum) have been administered; however maximum doses of dI-phenylalanine are 500mg daily, maximum ginseng daily dose of 3g and N-acetylcarnitine maximum daily dose of 1g. To achieve these higher doses of particular ingredients without exceeding the maximum dose of other ingredients, in a single formulation, would not be possible, however the synergistic effects observed are such that the inventor finds the formulation as described above in paragraph 2, very successful. Occasional 2nd doses a day at the above doses were carried out with increased effects however the likelihood of diminished effect with long term use, cautions such continuous high dosing although this was not investigated for long periods.

A synergistic effect between N-acetylcarnitine and D-ribose was observed enabling increased physical activity, decreased fatigue, effective restoration of diminished concentration spans and effective restoration of diminished learning ability. Ginseng enhances this effect and greatly reduced fatigue especially the morning exhaustion that exacerbated late awakening. Green tea extract was also observed to reduce anxiety to some degree and dI-phenylalanine also increase concentration ability and sense of well being and reduced morning depression and intolerance to even very low levels of alcohol. VitaminD3 (25 micro grammes) was included to reduce susceptibility to infections, nerve and muscle aches and pains. Multi vitamin supplementation that included all vitamins at an international standard dose, ensured no vitamin, in particular B deficiency, was contributing to the fatigue and depression.

DI-phenylalanine is the amino-acid precursor to the important neurotransmitters dopamine, nor epinephrine and epinephrine, which may be implicated in some depressions, in particular morning depression, and inability to concentrate. Its use is contraindicated for phenyl ketonuria, Parkinson's disease, psychosis and schizophrenia.

N-acetylcarnitine is important in the biosynthesis of acetyl-CoA and the release of energy and also the biosynthesis of acetylcholine which is a neurotransmitter important in memory and learning which may become deficient in chronic fatigue patients contributing to symptoms observed.

D-ribose is an important sugar that is important for ATP synthesis, the central energy molecule in physiology which may have become depleted.

GABA has been used successively in this formulation at 500mg however should the patient be receiving anxiety medication or sleeping pills targeting GABA receptors, long term use would not be recommended in such a formulation, hence its omission in the specific formulation given in paragraph 2. Separate occasional dosing 1/7 days does enhance effects.

Low doses of caffeine (20mg) have also been used successfully in this formulation, however high doses may trigger anxiety and therefore this ingredient has been omitted from the formulation.

This formulation does not specifically address serotonin biosynthesis or deficiency which is the main target of conventional therapies for depression and which may in fact have little therapeutic impact in chronic fatigue and some depressions, when other neurotransmitters are implicated. Such serotonin intervention therapy was observed to worsen the health of the inventor.

The use of combined omega-3 supplementation may have a long term therapeutic benefit, possibly by acting to increase levels of neurotransmitter storage vesicles in the brain, enabling the depleted neurotransmitters to possibly accumulate once more and therapeutic benefit to enhance and possibly become more long term.

Long term use (3 years of treatment using the regimes described) provides continuing very effective therapy to the inventor, with a return to substantially improved mental health, restoration of cognitive abilities that include great enhancement for prolonged concentration that had severely diminished, ability to learn returned, computer programming ability restored, short term-memory greatly improved, sense of well being substantially restored, physical well being restored and greatly reduced pain observed. This was observed after 4 years of failed conventional antidepressant SSRI therapy in which the inventor was afflicted with complete loss of computer programming ability, complete inability to learn new information, severe insomnia, impotence, sterility, agitation, pain, inability to concentrate or focus, severe short -term memory problems, immense fatigue that was overwhelming, depression and many periods in which the inventor could not function at more than 5% of normal levels. Such severe side effects indicated that serotonin was not the neurotransmitter to be targeted, and by increasing this system, other neurotransmitter symptoms had become depleted. Chronic mental ill-health had thus been inadvertently established, which was successfully treated and alleviated by this formulation.

Therapeutic effects of the formulation as described occur within days and accumulate over months with careful pacing of physical and mental exertions to avoid over exertions and possible collapse in to severer fatigue and depression. Regular breaks, of 2 days in each week, from mental concentration by pursuing other relaxing physical (but not too demanding) activities where prolonged mental concentration was avoided, enabling continuous and progressively improving mental and physical health.

The inventor does not recommended discontinuations of existing pharmacological medications if they are successful, unsuccessful medications that worsen patient health could be replaced by this formulation by a graduated but reasonably swift reduction over a few days and replacement (before any collapse in health can occur) under supervision of GPs or psychiatrists or clinical psychologists, alternatively it could be used as an early short term treatment and assessed for efficacy prior to deciding the direction of medication to take.

However, long term daily and continuous use of this formulation (ie 7 days per week) is to be cautioned against simply because of the possibility of reduced efficacy from prolonged continuous use, and also dependency, although no such dependency was observed, and a recommended regime is 4/7 days per week or possibly 5/7 days dosing followed by 2 days alternative treatments that may include NADH with energy drinks. NADH can quickly lose effects after a short period of prolonged use, however short term intermittent use shows some benefit, but substantially less than the formulation. By such a regime, long term efficacy and successful treatment was observed by the inventor for 3 years with no side-effects observed.

Occasional extra doses of this formulation when severe fatigue was triggered by stress and continued mental or physical exertion was beneficial. Doses as stated at 3 times a day during early stages of treatment in severe cases, with a reduction to doses above may be required in severe cases. Continuous use of more than 5/7 days per week is advised against. The preferred dosing regime would be Monday and Tuesday, Thursday and Friday, only two consecutive days of use thereby greatly reducing any physiological adaptations which may occur to reduce efficacy with time, thereby also reducing possible side effects. Although a more complex regime, the 4/7 regime for this formulation proves successful. Some existing pharmaceuticals with daily continuous administration and many side effects could well benefit from such discontinuous dosing.

As would be standard practice, a complete list of contra-indications and possible side-effects to any of these ingredients should be sought by any patient or manufacturer and all recommendations on use adhered to. All individual ingredients have been in widespread use and studies are prevalent should further information be sought. Medical advice and supervision should be sought as considered necessary. The inventor bases his findings from remarkable improvements observed from self experimentation over three years with little if any side effects observed; however the inventor accepts no responsibility or liability what so ever for any side effects or adverse effects that may occur.

Claims (2)

1. Claims 1) A formulation comprising a combination of N-acetylcarnitine and D-ribose for the treatment of chronic fatigue syndrome, chronic fatigue (where CFS criteria are not fully met), fibromyalgia, depression, depression where the patient is intolerant to conventional medications or suffers significant side-effects, depression where the patient wishes for alternative medication, and non responsive depression (where conventional anti depressants have failed to achieve remission of symptoms).
2. 2) A formulation according to claim 1, in which the following eight ingredients, in any combination (none to all eight) ingredients may also be added -dI-phenylalanine, green tea extract, GABA, ginseng, fish oils, caffeine, vitamin D3 and multi vitamins.