Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
  • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Definitions

• the present invention relates to the use of acetyl ⁇ carnitine for the preparation of a medicament for the treatment of fibromyalgic syndrome.
• Fibromyalgic syndrome or fibromyalgia is a chronic pain syndrome characterised by diffuse arthromyalgias accompanied to varying extents by sleep disorders, muscle-tension headache, irritable bowel syndrome, and asthenia.
• the condition is distinctly more prevalent in subjects of female gender and is more frequent in patients aged from 25 to 55 years.
• fibromyalgia The cause of fibromyalgia is still unknown and various pathogenetic mechanisms are currently postulated, such as psychic disturbances, alteration of normal sleep activity and of the pain perception threshold, and functional disorders affecting skeletal muscle with the presence of morphological alterations of the muscle fibre cells (Scand. J. Rheumatol. 1986; 15: 1-6) or various metabolic deficits (Bull Rheum Dis 1978; 26: 928- 931; J. Rheumatol 1992; 19:90-94).
• fibromyalgia The diagnosis of fibromyalgia is obtained on a purely clinical basis (medical history and physical examination) since laboratory tests (haematology and blood chemistry) and instrumental investigations (radiology, electrophysiology) yield no diagnostically useful indications in this clinical picture.
• Tender points differ from trigger points, in that they do not cause referred and irradiated pain, but prove tender only in the site stimulated.
• the simplest technique for detecting tender points is simple digital pressure (approximately 4 kg with the digital pulp) or by pinching the skin at points corresponding to definite joints and tendon insertions. Pressure on these points is accompanied by an exaggerated reaction of withdrawal from the examiner, jump sign, and neurovegetative phenomena such as dermographia, horripilation, and cold sweats.
• the tender points most commonly used for diagnostic purposes are nine in number (bilaterally), and to exemplify the diagnostic and classificatory approach criteria have been defined for locating and evaluating the tender points present in the patient (Arthritis Rheum 1990; 33(2): 160-172).
• US 5192805 relates to the use of acetyl L-carnitine in the therapeutic treatment of coma.
• US 6,037,3721128 relates to the use of acetyl L-carnitine, isovaleryl L-carnitine and propionyl L-carnitine to increase IGF-I levels, for the treatment of lateral amyotrophic sclerosis, neuropathies of the optic and olfactory nerves, trigeminal nerve neuralgia and other pathologies.
• US 6,037,372 relates to the use of an L-carnitine alkanoyl, including acetyl L-carnitine, for the treatment of pathologies mediated by glutamate such as epilepsy, schizophrenia, chronic fatigue syndrome, lateral amyotrophic sclerosis and others.
• Acetyl L-carnitine a commercially available product, can be prepared with the process described by R. Krinmberg, and W. Wittandt, in Biochem. Z. 251, 229 (1932).
• Fibromyalgia despite being a clinical condition with a benign course, is difficult to treat (Rheum Dis Clin N Am 1989; 15:61-71).
• Muscle relaxants and antidepressant drugs have also been used for the treatment of this disease, but only improve the quality of sleep (Arthritis Rheum 1986; 29: 1371-7; Arthritis Rheum 1994, 37: 3240).
• acetyl L-carnitine or one of its pharmaceutically acceptable salts is a useful compound for the treatment of fibromyalgia.
• salt of acetyl L- carnitine is any salt prepared by addition of an acid to acetyl L-carnitine inner salt, and which does not give rise to unwanted toxic or side effects.
• the formation of salts by addition of an acid is well known in pharmaceutical technology.
• Non-limitative examples of such salts are chloride, bromide, orotate, aspartate, acid aspartate, citrate, acid citrate, magnesium citrate, phosphate, acid phosphate, fumarate, acid fumarate, magnesium fumarate, glycerophosphate, lactate, maleate and acid maleate, mucate, oxalate, acid oxalate, pamoate, acid pamoate, sulphate, acid sulphate, glucose phosphate, tartrate, acid tartrate, magnesium tartrate, 2-amino ethanesulphonate, magnesium 2-amino ethanesulphonate, methane- sulphonate, choline tartrate, trichloroacetate, and trifluoroacetate.
• the subject of the present invention is therefore the use of acetyl L- carnitine or of one of its pharmaceutically acceptable salts for the preparation of a medicament and/ or dietetic product for the treatment of fibromyalgia.
• the acetyl L-carnitine can be in any form suitable for oral or parenteral administration. It can be administered in the form of a unit dose or in divided doses, in amounts ranging from 40 mg to 4 g/day.
• the preferred dose according to the present invention is 1.5 g per day, administered at the start of treatment and for the first 2 weeks at the dose of 500 mg intramuscularly (i.m.) and 500 mg (twice daily) orally (os), the treatment thereafter being continued with oral doses of 500 mg three times daily.
• the daily dose will depend, according to the judgement of the primary care physician, on the patient's weight, age and condition. Larger doses of acetyl L-carnitine can be administered thanks to the extremely low toxicity of said active ingredient.
• the patients included in the trial were patients of either gender aged from 25 to 65 years, who matched up to the above-mentioned American College of Rheumatology diagnostic criteria for fibromyalgia syndrome.
• Acetyl L-carnitine was administered for a period of 10 consecutive weeks at a dose of 1,500 mg/day. During the first two weeks it was administered at the dose of 500 mg by the intramuscular route (i.m.) and 500 mg (twice daily) by the oral route
• acetyl L-carnitine was administered orally at doses of 500 mg three times daily.

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• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Neurology (AREA)
• Pain & Pain Management (AREA)
• Rheumatology (AREA)
• Biomedical Technology (AREA)
• Neurosurgery (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Physical Education & Sports Medicine (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
• Saccharide Compounds (AREA)

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• 2004
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