Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-06-27
2000-08-01
Criares, Theodore J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514213, 514646, A61K 3155, A61K 31135
Patent
active
060967374
DESCRIPTION:
BRIEF SUMMARY
This invention relates to the treatment of Multiple Sclerosis (MS) and other Demyelinating Conditions.
Multiple sclerosis is a common and well known neurological disorder. It is characterised by episodic patches of inflammation and demyelination which can occur anywhere in the central nervous system (CNS) almost always without any involvement of the peripheral nerves. The occurrence of the patches is disseminated in time and space, hence the older alternative name of disseminated sclerosis. It is believed that the pathogenesis involves local disruption of the blood brain barrier, a local immune and inflammatory response, with consequent damage to myelin and hence to neurons.
Clinically, MS can present in both sexes and at any age. However, its most common presentation is in relatively young adults, often with a single focal lesion such as damage to the optic nerve (optic neuritis), an area of anaesthesia or paraesthesia or muscular weakness. Vertigo, nystagmus double vision, pain, incontinence, cerebellar signs, L'Hermitte's sign (paraesthesia or pain in the arms and legs on flexing the neck) and a large variety of less common symptoms may occur. The initial attack is often transient and it may be weeks, months or years before a further attack occurs. Some fortunate individuals may have a stable condition, while other unfortunate ones may have an unrelenting downhill course ending in complete paralysis. More commonly there is a long series of remissions and relapses, each relapse leaving the patient somewhat worse than before. Relapses may be triggered by stressful events or viral infections. Elevated body temperature almost invariably makes the condition worse whereas a reduced temperature, for example induced by a cold bath, may make the condition better.
There are no satisfactory treatments for MS. Steroids may produce a temporary improvement but any beneficial effect invariably wears off. Recent clinical trials have shown that interferon may somewhat reduce the risk of relapse. However, the effect is modest and most patients still deteriorate.
I have now developed a new and highly effective treatment for compensating for the effects of nerve damage caused by MS and other demyelinating conditions.
My invention is based on the use of a combination of an antidepressant or a monoamine oxidase inhibitor in combination with an inducer or precursor of a neurotransmitter. The two compounds may be administered in the same dosage form, or may be in separate dosage forms but a combined pack may be in separate packs for administration at separate times but so as to be effective together in the body.
Lofepramine and related tricyclic and tetracyclic antidepressants work by interfering with the inactivation of substances called neurotransmitters which are required for the normal transmission of nerve impulses from one nerve cell to the next. Such neurotransmitters, among them substances called noradrenaline and serotonin, are released from one nerve cell and activate the next one. They are inactivated by various mechanisms including rapidly being taken up into nerve cells and also enzymic destruction by enzymes known as monoamine oxidase inhibitors (MAOI). Lofepramine is a drug which inhibits neurotransmitter uptake and which is in the class of tricyclic antidepressants and which also has some MAOI activity. Newer drugs to treat depression are more active against serotonin and are known as selective serotonin reuptake inhibitors (SSRIs).
I have discovered that the use of L-phenylalanine (LPA), the precursor of noradrenaline, contributes to the therapeutic effect. In some individuals, however, an alternative may be L-tryptophan which is a precursor of the neurotransmitter, serotonin. Several different antidepressants including tricyclic antidepressants, SSRIs and MAOIs have beneficial effects but have consistently obtained the best results with lofepramine. Detailed information on lofepramine is given in the Merck Index. I have also noted that when the patient receives regular injections of vitamin B.sub.12 the treat
REFERENCES:
patent: 4409243 (1983-10-01), Lieb
patent: 4650789 (1987-03-01), Pollack
Abstract of Charles F. Scott, Jr., et al., "Experimental Allergic Encephalitis; Treatment with Drugs Which Alter CNS Serotonin Levels", Journal of Immunopharmacology, pp. 153-162, 1982.
D. Chadwick, et al., "5-Hydroxytryptophan-Induced Myoclonus in Guinea Pigs" Journal of the Neurological Sciences, pp. 157-165, 1976.
Karin N. Westlund, et al., "Serotonin is found in myelinated axons of the dorsolateral funiculus in monkeys" Neuroscience Letters, pp. 35-38, 1992.
E.H. Reynolds, "Multiple sclerosis and vitamin B12 metabolism", Journal of Neuroimmunology, pp. 225-230, 1992.
Guy M. Goodwin, "Tricyclic and newer antidepressants", Handbook of Affective Disorders, pp. 327-343, 1992.
Abdulla A.-B. Badawy, et al., "The Effects of Lofepramine and Desmethylimipramine on Tryptophan Metabolism and Disposition in the Rat", pp. 921-929, 1991.
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