Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-06-09
1999-08-24
Jarvis, William R. A.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
A61K 3155
Patent
active
059425032
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP96/04957, filed Nov. 13, 1996.
The present invention relates to a new use of epinastine for the treatment and prophylaxis of pain, especially chronic or inflammation-induced pain and in particular migraine. (1988): 1446-1453!. The active principle can be used in the form of a racemate or in the form of pure enantiomers or as a mixture of different proportions of both enantiomers. Therapeutically, epinastine is used as the hydrochloride. The invention described herein, however, is not limited to the hydrochloride but relates to any addition salt with a pharmacologically acceptable acid as well as the free base.
The use of epinastine and its salts for the treatment of asthma is known. European patent EP-B-0 035 749 discloses that this substance is also suitable for therapy of allergic diseases such as allergic rhinitis, allergic conjunctivitis and allergic bronchitis.
Headache is a commonly occurring symptom. In most cases the headache is of short duration and can readily be controlled by weak analgesics such as aspirin, paracetamol or ibuprofen. Such headache is bothersome but does not lead to any significant impairment of health. By contrast, chronic recurring headaches such as migraine can lead to such serious adverse affects that a doctor has to be consulted. These serious types of headaches often cannot be treated satisfactorily with a weak analgesic.
On the other hand, there is no universally accepted system of classifying headache; chronic recurring pain in the sense of this invention refers predominantly to migraine and Bing-Horton syndrome. Migraine itself 44 (1994) p6-p10 for a classification!. Although migraine and tension headaches are two different forms, several scientists see them as a clinical continuum with migraine at one end and tension headache at the in "Medical Clinics of North America" Vol. 79 No. 2 (1995) p.261 to 286!. Therefore it seems reasonable to suppose that many patients with tension headache will also respond to a therapy for migraine. Several other diseases which are associated with chronic pain, such as neuralgia, muscle pains and inflammation pain (as for example after sunburn or in osteoarthritis or after sports injuries) have common features with chronic Pharmacological Sciences 15 (1994): 190-197!.
Existing therapy for migraine includes the use of ergot alkaloids such as ergotamine and 5HT.sub.1D agonists such as sumatriptan. Although many patients profit from these medicaments, by no means all patients respond. Further, there are numerous side effects such as dizziness and nausea. Drugs for prophylactic management of migraine include methysergide and pizotifen, beta-blockers such as propanolol, and calcium channel blockers such as flunarizine. Chronic administration of these drugs can have side effects that impair the patients' quality of life and the drugs usually H. C. Diener, Eur. Neurol. 34(Suppl 2) (1994): 18-25.!
There therefore remains a need to provide a drug for the treatment of migraine which is not only effective but also free of significant side effects. There is also a need to provide a medicament with a high degree of safety for particular patient groups such as children, and patients with reduced liver or kidney function, or cardiovascular disease.
It has now been found that, surprisingly, epinastine fulfils these requirements to an exceptional degree. This is shown by the following research results:
In laboratory animals, it is possible to induce inflammation in the dura mater by electrical stimulation of the trigeminal ganglion, which causes the release of neuropeptides such as substance P from sensory nerve endings. Plasma extravasation can be monitored by markers such as Evans blue. This animal model is widely used for testing for drugs useful in migraine. Surprisingly, epinastine shows exceptionally good activity in this model. For chronic inflammatory pain, a widely used animal model is that first described in principle by Randall and Selitto (L. O. Randall, and J. J. Selitto, Arch. Int. Pharmacodyn. 111 (1957): 4
REFERENCES:
Jackson et al, Clin. Exp. Pharmacol. Physiol., vol. 19, No. 1, pp. 17-23, 1992.
Jung Birgit
Meade Christopher John Montague
Pairet Michel
Boehringer Indelheim KG
Devlin M-E. M.
Jarvis William R. A.
Raymond R. P.
Stempel A. R.
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