Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-10-18
1994-11-08
Rose, Shep K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514315, 514317, 514449, 514452, 514461, 514467, A61K 3144, A61K 31505
Patent
active
053627318
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of compounds, for which other applications are known, in the manufacture of a medicinal product intended for the treatment of patients having unstable or hyperactive bladders ("hyper reflexic bladder").
Unstable or hyperactive bladders are bladders which, for various reasons, result in frequent and urgent micturitions which may extend to urinary incontinence which, from a psychological and social point of view, constitutes a serious handicap.
The causes of such an instability of the detrusor may be of numerous origins, particularly due to the side effects of diseases such as brain tumors or tumors of the spinal cord, traumatic impairment of the nervous system, cerebrovascular accidents, demyelinating or degenerative diseases such as multiple sclerosis, Parkinson's disease and dementias.
The treatments known for these hyperactive bladders consist either of a treatment using compositions having antispasmodic or anticholinergic effects, such as oxybutynin chloride, imipramine or propantheline bromide, or in a surgical operation to denervate the detrusor.
The use of anticholinergic compounds, although effective, is often accompanied by many side effects, including a very extensive dryness of the mouth, which often make them difficult to accept by the patients. There are certain cases where no really acceptable treatment of this type of pathology is possible.
Accordingly, it is particularly advantageous to have demonstrated the surprising activities of compounds otherwise known for the treatment of different pathologies.
Thus, the present invention relates to the use of a compound of general formula I: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, taken separately or together, may represent a hydrogen atom, a hydroxyl radical, an acetoxy group CH.sub.3 COO--, a C.sub.1 -C.sub.5 lower alkoxy group or an alkylenedioxy chain --O--(CH.sub.2).sub.n --O-- in which n may take the values 1 or 2, and R.sub.4 may represent a hydrogen atom, a C.sub.1 -C.sub.5 lower alkyl radical, or a phenyl nucleus optionally substituted by radicals or groups R.sub.1, R.sub.2, R.sub.3, of the same type as those mentioned above, and R' represents a hydrogen atom or a methyl radical, its physiologically acceptable derivatives and its active metabolites for the manufacture of a medicinal product intended for the treatment of hyperactive bladders.
Active metabolites mean the degradation products of the compound of formula I which is active in the treatment of hyperactive bladders.
Preferably, piribedil, known in particular for its vasodilating, anti-ischemic and anti-parkinsonian properties, will be used.
Among the deviated [sic] of these products which can be used, the salts, especially methanesulfonate for piribedil, should be mentioned.
Taking into account the pathology to be treated, the most suitable galenical forms are the oral forms, especially tablets, as well as the delayed-action galenical forms, especially the transdermal forms.
The tablets generally contain doses of between 15 and 60 mg of compound of general formula I.
The injectable forms are also preferred for an intravenous or parenteral administration.
The forms and the doses which can be used may vary between 1 to 15 mg/kg per day of active ingredient, it being possible for these doses to be adjusted according to the condition of the patient and the extent of the disorder, as well as the progression of his condition.
The examples below make it possible to demonstrate other characteristics and advantages of the present invention.
EXAMPLE 1
Procedure for Carrying Out the Piribedil Test
Piribedil is provided in the form of an injectable solution of 0.003 g/ml of piribedil methanesulfonate. On the eve of the test, the patient optionally stops taking antiparkinsonian drugs, and ingests three times 20 mg of domperidone, 20 mg dose repeated the next morning 2 hours before the test.
A perfusion is then fitted and a cystomanometry and a reference urethral profile are performed.
During the course of the entire test, the arterial constancy
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