Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-03-19
2000-08-22
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...
514343, A61K 3140, A61K 3144
Patent
active
06107330&
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to a medicament for inhibiting developments of dependency and tolerance to analgesic action which are induced by the administration of a narcotic analgesic agent.
BACKGROUND ART
Narcotic analgesic agents, e.g., morphine, have excellent analgesic action against visceral pains or other, and are clinically used for alleviation of pain for terminal cancer patients. However, the narcotic analgesic agents are typical drugs that affect on mental functions and develop psychic and physical dependency. In addition, tolerance to analgesic action, as being their primary efficacy, is rapidly developed by repeated administrations. Accordingly, carefully controlled frequency of administration and dose are required to achieve a desired analgesic action, while maintaining minimized development of dependency.
Therefore, when a narcotic analgesic agent such as morphine is used, it is necessary to inhibit the development of tolerance to analgesic activity without reducing analgesic activity to meet the purpose of the use. It is also important to inhibit the development of dependency.
An object of the present invention is to provide a medicament having inhibitory activity against the development of dependency induced by the administration of the narcotic analgesic agent such as morphine. Another object of the present invention is to provide a medicament having inhibitory activity against the development of tolerance to analgesic action induced by the administration of the narcotic analgesic agent such as morphine. A further object of the present invention is to provide a medicament having both of the aforementioned pharmacological activities.
DISCLOSURE OF THE INVENTION
The inventors of the present invention conducted various studies to achieve the foregoing objects, and as a result, they found that 2-(1-pyrrolidinyl)acetamide derivatives, which are useful as medicaments for improving cerebral functions, have the aforementioned pharmacological activities. They also found that the derivatives are useful as active ingredients of medicaments which inhibit the developments of dependency and/or the developments of tolerance to analgesic actions induced by narcotic analgesic drugs. The present invention was achieved on the basis of these findings.
The present invention thus provides a medicament which comprises as an active ingredient a compound represented by the following formula: R.sup.2 -CH.sub.2 CONH-R.sup.1 wherein R.sup.1 represents a pyridyl group, a substituted pyridyl group, phenyl group, or a substituted phenyl group; and R.sup.2 represents 2-oxo-1-pyrrolidinyl group which may optionally be substituted, and inhibits the development of dependency induced by a narcotic analgesic agent and/or inhibits the development of tolerance to analgesic action induced by a narcotic analgesic agent.
According to preferred embodiments of the present invention, the following inventions are provided: the aforementioned medicament which inhibits the development of dependency induced by a narcotic analgesic agent, and also inhibits the development of tolerance to analgesic action induced by a narcotic analgesic agent; the aforementioned medicament which inhibits the development of dependency induced by a narcotic analgesic agent; the aforementioned medicament which inhibits the development of tolerance to analgesic action induced by a narcotic analgesic agent; the aforementioned medicament used in combination with a narcotic analgesic agent; the aforementioned medicament having a prophylactic effect to reduce or prevent the development of dependency induced by a narcotic analgesic agent and/or the development of tolerance to analgesic action induced by a narcotic analgesic agent; the aforementioned medicament having a therapeutic effect to reduce or eliminate dependency already developed by a narcotic analgesic agent and/or tolerance to analgesic action already developed by a narcotic analgesic agent; the aforementioned medicament wherein said active ingredient is N-(2,6-dimethylphenyl)-2-
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Nabeshima Toshitaka
Shiotani Tadashi
Yoshii Mitsunobu
Daiichi Pharmaceutical Co. Ltd.
Jarvis William R. A.
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