Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-05-24
1996-03-05
Jordan, Kimberly R.
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
054968291
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP94/01601 filed Dec. 8, 1992.
TECHNICAL FIELD
The present invention relates to an agent for relieving disturbance of consciousness and a narcotic antagonist which contain 2-nitroxyethyl (+)apovincaminate (hereinafter referred to as VA-045) as an active ingredient.
BACKGROUND ART
In general, a central nervous mechanism which maintains and controls consciousness is composed of two systems, i.e., ascending midbrain reticular formation activating system and hypothalamus activating system. That is, brainstem reticular body and hypothalamus, as well as hemicerebrum and thalamus which are affected by them, are related to consciousness. Disturbance of consciousness occurs when the functions of these organs are impaired by an impact on head (neurotrauma) or cerebral ischemia. Agents for relieving disturbance of consciousness act on central nervous systems concerned with consciousness, to exhibit a relieving effect. As such agents for relieving disturbance of consciousness, there have been known thyrotropin releasing hormone tartrate (hereinafter referred to as TRH), meclofenoxate hydrochloride, CDP-choline, etc.
The ascending midbrain reticular formation activating system participates greatly in a central nervous mechanism which controls sleep. Anesthesia by use of pentobarbital or the like is induction of sleep by inhibition of the aforesaid activating system. Narcotic antagonists act on the inhibited ascending midbrain reticular formation activating system to recover the function of the system. As the narcotic antagonists, there have been known methamphetamine hydrochloride, doxapram hydrochloride, TRH, etc. The above-mentioned conventional agents for relieving disturbance of consciousness and narcotic antagonists, however, are all different from apovincaminic acid skeleton.
On the other hand, VA-045 is a compound disclosed in Japanese Patent KOKAI No. 2-167279, and it has an excellent curative effect on cerebral ischemia, hypertension and the like because of its cerebro-vasodilation effect. However, of apovincaminic acid derivatives including this compound, none is known to have relieving effect on disturbance of consciousness or antagonistic effect on narcotism.
By the way, cerebro-vasodilators improve cerebral circulation by relaxation of cerebral smooth muscle, and drugs heretofore known as cerebro-vasodilators (e.g. vinpocetine, nifedipine, nicardipine verapamil) do not have relieving effect on disturbance of consciousness or antagonistic effect on narcotism.
An object of the present invention is to provide an agent for relieving disturbance of consciousness and a narcotic antagonist which are novel.
DISCLOSURE OF THE INVENTION
The present invention is an agent for relieving disturbance of consciousness which contains VA-045 as an active ingredient, and the present invention is a narcotic antagonist containing VA-045 as an active ingredient.
An administration route of VA-045 as an agent for relieving disturbance of consciousness includes, for example, parenteral and oral administrations. An administration route of VA-045 as narcotic antagonist is parenteral administration. The dosage form of VA-045 is an injection in the case of parenteral administration, and a form selected from tablets, granules, powders, capsules, syrups and suspensions in the case of oral administration. When VA-045 is used as an agent for relieving disturbance of consciousness, these dosage forms may be properly chosen depending on the condition and age of a patient and the purpose of treatment, though the most preferable pharmaceutical form is an injection. Preparations of various pharmaceutical forms can be prepared by conventional preparation methods (for example, the methods prescribed in the No. 12 revised Japanese Pharmacopoeia) by using conventional excipients (e.g. crystalline cellulose, starch, lactose or mannitol), binders [e.g. hydroxypropyl cellulose or polyvinyl pyrrolidone], lubricants (e.g. magnesium stearate or talc), disintegrators (e.g. calcium carboxymethyl cellulose), etc.
A
REFERENCES:
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Hatayama Katsuo
Kawashima Yutaka
Okuyama Shigeru
Otomo Susumu
Jordan Kimberly R.
Taisho Pharmaceutical Co. Ltd.
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