Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-04-19
1998-02-24
Jarvis, William R. A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3144
Patent
active
057212589
DESCRIPTION:
BRIEF SUMMARY
This application claims benefit of international application PCT/EP94/02649, filed Aug. 10, 1994.
BACKGROUND OF THE INVENTION
FIELD OF THE INVENTION
The invention relates to the use of flupirtine in medicaments for the treatment of cerebral ischemia, neurodegenerative disorders, traumatic brain and bone marrow damage, epileptic attacks and other illnesses.
BACKGROUND INFORMATION
Flupirtine (Katadolon.RTM.) is a new, centrally acting, non-opiate analgesic. (Jakovlev, V. Sofia, R. D., Achterrath-Tuckermann, U., von Schlichtegroll, A., Thiemer, K., Arzneim.-Forsch./Drug Res. 35 (I), 30 (1985); Nickel, B., Herz, A., Jakovlev, V., Tibes, U., Arzneim.-Forsch/Drug Res. 35 (II), 1402 (1985). Flupirtine develops its central analgesic effects via mechanisms of action that differ from those of the opiate/opioid analgesics. (Nickel, B., Postgrad. med. J. 63 (Suppl. 3), 19 (1987); Szelenyi, I., Nickel, B., Borbe, H. O., Brune K., Br. J. Pharmacol. 143, 89 (1989)). Electrophysiological investigations have shown that flupirtine is able to intervene in the nociceptive process both at the supraspinal and at the spinal level. (Carlsson, K. H. Jurna, I., Eur. J. pharmacol. 143, 89 (1987); Bleyer, H., Carlsson K. H., Erkel H. J., Jurna, I., Eur. J. Pharmacol 151, 259 (1988); Nikel, B. Aledter, A., Postgrad Med. J. 63 (Suppl. 3) 41 (1987)).
Flupirtine has hitherto been used in the treatment of acute states of pain caused by diseases of the locomotor apparatus. Flupirtine has also been successfully used in patients with nerve pains, cancer pain, vasomotor and migraine headaches, post-operative pain, after injuries, burns, erosions, in dysmenorrhea and toothache. These indications and the dosages to be used are given in the professional information (Katadolon.RTM., monoanalgesic, scientific leaflet, second revised edition April 1992, published by ASTA Medica AG). Combination medicaments of flupirtine with non-steroidal anti-inflammatory agents are described in EP 189 788. In these indications it is of advantage that flupirtine has not only analgesic, but also a muscle-relaxant properties, as described in German published specification 41 22 166 4.
Chemically speaking, flupirtine is the maleate of synthesis of flupirtine and its pharmaceutically acceptable salts is described in EP 160 865 and 199 951. Flupirtine maleate has a chemical structure that cannot be assigned to hitherto known analgesically acting pharmaceuticals. Flupirtine is a colourless, crystalline, almost odourless powder with slightly bitter-sweet taste. It is only moderately soluble in water. The analgesic effect of flupirtine has been demonstrated in various animal experiments on pain models after mechanical (Haffner test), thermic (hotplate test), electrical (electropain test, dental pulp irritation), chemical (writhing test) and chemical-mechanical irritation (Randall-Selito test) in mouse, rat and dog. More information on the effect and side effects of the monoanalgesic flupirtine are given in the scientific leaflet (Katadolon.RTM., monoanalgesic, scientific leaflet, second revised edition April 1992, published by ASTA Medica AG).
Pharmacological examinations show that flupirtine has both a spinal and a supraspinal point of attack. Blockade experiments with antagonists have shown that neither the serotoninergic nor the opioid system can be involved in mediating the antinociceptic effect of flupirtine. The most probable explanation for the flupirtine-induced analgesia is the involvement of descending noradrenergic pain-modulating paths (I. Szelenyi, B. Nickel, H. O. Borbe, K. Brune Br. J. Pharmacol. (1989), 97, 835-842), although flupirtine has no binding affinity for .alpha..sub.1 - or .alpha..sub.2 -adrenergic receptors (B. Nickel et al., Br. J. Pharmacol. (1989) 97, 835).
In addition, the absence of affinity for the opiate receptors of rat brain also speaks against an opiate-like mechanism of action of flupirtine. According to these results, a mechanism of action of flupirtine corresponding to the opiates can be excluded. Tolerance and dependence h
REFERENCES:
patent: 5162346 (1992-11-01), Lobisch et al.
Schwarz et al: "N-Methyl-D-Aspartate (NMDA)-Mediated Muscle Relaxant Action of Flupirtine in Rat", Neuroreport, vol. 5, No. 15, Oct. 1994, pp. 1981-1984.
Friedel, et al: "Flupirtine", Drugs, vol. 45, NO. 4, Apr. 1993, pp. 548-569.
Seaman, et al: "Flupirtine", Curr. Probl. Epilepsy, vol. 4, 1986, pp. 135-145.
Sheridan, et al: "Pilot Stody of Flupirtine in Refractory Seizures," Neurology, vol. 36, 1986, p. 85.
Engel Jurgen
Nickel Bernd
Pergande Gabriela
Schwarz Michael
Szelenyi Stefan
Asta Medica Aktiengesellschaft
Jarvis William R. A.
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