Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-05-30
1998-11-10
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
058344977
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 PCT/SE96/00601, filed May 8, 1996.
FIELD OF THE INVENTION
The present invention is related to the use of 2,6-dimethyl-4-(2,3-dichlorophenyl-1,4-dihydropyridine-3,5-dicarboxylic acid-3-methyl-5-ethyl ester, generic name felodipine, in the form of the racemate or an optical isomer as well as pharmaceutically acceptable salts thereof, for the treatment of cerebral dysfunction due to solvent exposure and in the manufacture of pharmaceutical preparations with effect on cerebral dysfunction due to solvent exposure.
BACKGROUND OF THE INVENTION
Felodipine, which is described in the European patent EP 7293, is a dihydropyridine calcium antagonist which has been shown in hypertensive patients to lower blood pressure through a direct effect on the resistance vessels (small arteries). However, no effect on cerebral dysfunction due to solvent exposure has been reported earlier.
By dysfunction due to solvent exposure is in this context meant altered cognative functioning, in particular impaired memory ability, psychomotor capacity and reaction times.
PRIOR ART
No specific treatment of cerebral dysfunction due to solvent exposure is available today.
OUTLINE OF THE INVENTION
It has now been found that felodipine is effective in the treatment of cerebral dysfunction due to solvent exposure, which produces a dementia like disease. Various solvents may produce a dementia like disease. Examples of such solvents are organic solvents both chlorinated and non-chlorinated. Improvement of cerebral dysfunction can also be expected when caused by agents other than a solvent
The compound 2,6-dimethyl-4-(2,3-dichlorophenyl1,4-dihydropyridine-3,5-dicarboxylic acid-3-methyl-5-ethyl ester and pharmaceutically acceptable salts thereof, can be prepared by processes known in the art, see e.g. EP 7293.
Felodipine may be in the form of its optical antipodes or the racemate; the effect of this compound on cerebral dysfunction due to solvent exposure and dementia is obtained with the racemic mixture as well as the separate isomeric forms.
Pharmaceutically acceptable salts of felodipine can be prepared from inorganic and organic acids including for example acetic, benzene-sulfonic, benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethonic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric, and p-toluenesulfonic acids.
Conventional pharmaceutical preparations can be used.
The pharmaceutical preparations are preferably in the form of tablets or capsules, but it is also possible to use other kinds of preparations, such as oral solutions or suspensions or injection solutions. Extended release formulations can also be used.
Unit dose pharmaceutical preparations usually contain 5 to 20 mg of felodipine, preferably 10 to 15 mg. By using an oral liquid formulation it is possible to administer 1 mg/ml.
The daily dosage of felodipine for use in cerebral dysfunction due to solvent exposure and dementia is 5 to 20 mg per day.
EXPERIMENTAL DATA
Three male patients with solvent induced chronic toxic encephalopathy were treated with felodipine during a period of 3 to 5 months.
The patients were examined with semi-structured interviews, Target Complaints, neuropsychological tests and cerebral blood flow examinations (Cortexplorer and SPECT) on 2 or 3 occasions. The baseline examinations were conducted twelve weeks before and again immediately before the felodipine treatment revealed servere symptoms such as sleep disturbance and headache, impaired performance in the neuropsychological testing and pathological cerebral blood flow.
At the examination after the treatment the patients' symptoms were considerably reduced. The neuropsychological testing revealed improved (at least 10 per cent) functioning in tests assessing visuo-spatial memory ability.
An increase of at least 10 per cent in the cerebral blood flow was also found in both the Cortexplorer and the SPECT examinations.
CONCLUSION
REFERENCES:
G. Zupan, et al., Arch. Int. Pharmacodyn, vol. 325, pp. 61-69, (1993) Effects of Nicardipine, Felodipine and Nifedipine on Passive Avoidance Behavior of Intact and Hypoxia-Exposed Rats.
Elmfeldt Dag
Fagher Birger
Jonsson Lars
Lindgren May
Partridge Stephen
Astra Aktiebolag
Jarvis William R. A.
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