【作用与用途】本品主要作用于大脑皮质，能促进脑细胞的氧化还原代谢，调节神经细胞的代谢，增加对糖类的利用，对中枢抑制患者有兴奋作用。
　　适用于：多种原因如脑血管疾病、脑卒中、脑创伤、脑瘤、脑动脉硬化、新生儿缺氧症、手术后的复苏等所致昏迷及意识障碍。也可用于因缺氧、脑功能失调所致的记忆力障碍、儿童智力迟钝、小儿遗尿症、神经精神性尿频、严重疲乏症、倦怠、脑外伤后综合征等。
　　精神障碍如抑郁症、癔病。

【剂量与用法】
　　口服，成人一次0.1g-0.2g，3-4次/日，至少服1周。儿童0.01g/次，3次/日。
　　静脉注射或静脉滴注
　　成人一次0.1-0.25g，一日3次，临用前用注射用水或5%葡萄糖注射液稀释成5-10%溶液使用。
　　儿童一次60-100mg，一日2次，可注入脐静脉。
　　肌内注射
　　成人昏迷状态一次于0.25g，每2小时一次。
　　新生儿缺氧症一次60mg，每2小时一次。

【不良反应】
　　兴奋、激动、失眠、疲乏无力、胃部不适、血压变动、血管痛、头痛。
　　药物过量：中毒症状：焦虑不安、活动增多、共济失调、惊厥、可引起心悸、心率加快、血压升高。

【注意事项】
　　对本品过敏者禁用。
　　精神过度兴奋，锥体外系症状患者禁用。
　　高血压患者慎用。
　　本品易水解，配成溶液后立即使用。根据适应症可适当增加疗程。
　　药物中毒处理：洗胃、5%葡萄糖氯化钠注射液静脉滴注，并给予相应的对症治疗及支持疗法。

【制剂】胶囊剂：每胶囊0.1g；注射用盐酸甲氯芬酯：每支0.1g；0.25g。

【贮存】遮光，密闭保存

包装规格: 250毫克/瓶 10瓶/盒

生产厂家:Kyowa

Lucidril * (centrophenoxine).
Centrophenoxine is an antiaging drug widely used by humans to increase brain energy, since it stimulates the chemical activity of the brain. In particular, uptake of the sugar glucose is increased. Glucose is essential for energy production. Oxygen consumption and carbon dioxide production also increase significantly when centrophenoxine is taken regularly, providing further evidence of its effectiveness. Centrophenoxine has been found to be very effective in the treatment of various human disorders such as brain damage due to old age, stroke, brain injury caused by chemicals or drugs including excessive alcohol consumption . Centrophenoxine has the ability to protect against the damage caused by toxic environmental chemicals.

PROVIDES REAL PROTECTION AGAINST AGING DAMAGE
It also has been found that prolonged administration of centrophenoxine to healthy old animals causes a large reduction of the lipofuscin present in heart and brain cells . Lipofuscin is a waste product that builds up in old cells. The lifespan of centrophenoxine weaned animals is much longer than that of animals that do not receive the drug. The learning ability of treated animals is greatly improved compared to old untreated animals.

Centrophenoxine is able to REVERSE the age-dependent accumulation of the mineral potassium in brain cells, and a number of other damaging changes that occur as the brain ages. Centrophenoxine causes an increase in the production of chemicals that are essential for the proper functioning of the brain such as RNA and protein. Glucose uptake into the brain also is increased. In spite of the positive benefits obtained by taking centrophenoxine, the way it works is not quite clear. Some of its biological effects are possibly due to the DMAE (dimethylaminoethanol) that centrophenoxine contains. DMAE is able to stay in the brain in the membranes of nerve cells for a long time. Since DMAE is a very efficient free radical scavenger, centrophenoxine is able to protect the brain against free radical damage.

Free radicals occur in biological systems and are responsible for some aging damage. The drug centrophenoxine has played a central role in many antiaging experiments. Scientific experiments have proven the free radical scavenging properties of DMAE. It should be stressed that this part of centrophenoxine is actually incorporated into the brain cell membrane. The presence of DMAE in the brain cell membrane provides increased protection against damaging free radical attacks. The present findings offer strong evidence supporting the observation that vital membranes are protected during continuous treatment with centrophenoxine.

The other compound in centrophenoxine also is a powerful free radical scavenger, although probably not as important as the DMAE portion. The combined effect of both parts of the drug prevents free radical induced aging damage and improves the body's defense against free radical attack.

Many scientific experiments have revealed a considerable age-dependent drop in levels of the chemical RNA in the brain. RNA is essential for the body to make protein. Treatment with centrophenoxine is able to REVERSE this decrease in production of RNA.

Since the increased rate of RNA production allows the cell to carry out protein synthesis at a higher rate, the effects of centrophenoxine may also involve an increased rate of protein tumover. This increased rate of protein turnover is important because it is related to all the beneficial antiaging effects of centrophenoxine.

Combats Memory Loss
Various drugs have been developed to treat senile dementia and centrophenoxine has been found to be useful. Regular use of centrophenoxine offers you the chance to prevent mental deterioration. Memory performance is improved in both the normal elderly and those with dementia following treatment with centrophenoxine .

The most obvious change in the nerve cells of elderly individuals is the appearance and increase in the amount of lipofuscin pigment. Experimental studies have shown that centrophenoxine treatment can reduce the amount of lipofuscin in nerve cells. This suggests that the beneficial effects on mental function in demented patients is partly due to removal of age pigment from nerve cells. Many scientists believe that benefits also are produced by the improvements in cell metabolism that centrophenoxine produces.

Senile dementia is related to changes in the part of the brain known as the hippocampus. The nerve cells of the hippocampus are damaged as part of the aging process; however, in senile dementia these damaging changes are much worse. Similar changes also may occur in the rest of the central nervous system. This extra damage indicates a furthur decline in metabolic activity in affected nerve cells.

A very important effect of centrophenoxine is the stimulation of uptake of glucose by the brain. This can help to make up for the damage caused to the hippocampus by aging and senile dementia.

The beneficial effects on mental performance seen in older people following regular use of centrophenoxine are due to a real improvement in the efficiency of the workings of vital cells. Nerve cells in particular work much better under the influence of cetrophenoxine..

The exact way that centrophenoxine works to combat the aging process is unclear, however, an attempt to explain it has been made using the so-called "membrane theory of aging".

The "membrane theory of aging" attributes a primary role in aging to a decrease in the ability of the mineral potassium to get into and out of cells. This causes the level of potassium in the cell to rise leading to a reduction in essential protein production. the rise in potassium levels is due to free-radical induced cross-linking in the cell membrane. the "membrane theory of aging" as outlined above suggest that the cells of the body gradually lose their ability to eliminate damaged components ie. lipofuscin builds up within the cells. Centrophenoxine slows down the rate of accumulation of age deposits (lipofuscin) in brain cells and it also removes deposits that have already accumulated in aged brains, is incorporated into the membranes of brain cells, where it protects against the cross-linking effects of free-radicals.The drug is able to increase the storage of new information in long-term memory and increase mental alertness.

TOXICITY
There is virtually no toxicity associated with centrophenoxine in therapeutic doses.
Caution: People with the following medical conditions should not take centrophenoxine: severe high blood pressure, convulsive disorders including epilepsy, pregnant and lactating women.

注射用ルシドリール250mg

作成又は改訂年月

その他

（0.1％未満）

全身違和感

その他の副作用の注意

注2)このような症状があらわれた場合には、投与を中止するなど適切な処置を行うこと。

適用上の注意

1.

筋肉内注射時

筋肉内注射にあたっては組織・神経等への影響を避けるため、下記の点に注意すること。

(1)

筋肉内注射はやむを得ない場合にのみ、必要最小限に行うこと。なお、特に同一部位への反復注射は行わないこと。また、新生児、低出生体重児、乳児、幼児、小児には特に注意すること。

(2)

神経走行部位を避けるよう注意すること。

(3)

注射針を刺入したとき、激痛を訴えたり、血液の逆流をみた場合は直ちに針を抜き、部位を変えて注射すること。

2.

溶解後

溶解後はなるべく速やかに使用し、放置したものは投与しないこと。

薬物動態

1.

血中濃度

Cmax

データなし

T_1/2

データなし

2.

主な代謝産物及び代謝経路^1,2)(参考)

メクロフェノキサートは体内で加水分解され、パラクロルフェノキシ酢酸(活性あり)及びジメチルアミノエタノール(活性あり)になる。(マウス)

3.

排泄経路及び排泄率¹⁾(参考)

排泄経路

主として尿中(マウス)

排泄率

静脈内投与後24時間までに総排泄量の95％がその代謝物であるパラクロルフェノキシ酢酸として尿中排泄される。(マウス)

臨床成績

二重盲検比較試験(対照薬：プラセボ)を含む総計202例についての臨床成績は次のとおりである³⁾。

対象疾患：頭部外傷の急性期における意識障害

有効率：80％(142/177)

対象疾患：脳術後の意識障害

有効率：64％(16/25)

薬効薬理

1.

中枢神経賦活作用^4,5)

無麻酔家兎を用いた実験において、脳幹網様体の単位放電の増加、脳幹網様体刺激による覚醒反応閾値の下降及び知覚求心路・錐体路系の促進が、また、麻酔家兎を用いた実験において脳波の覚醒波への移行が認められている。

2.

脳代謝促進作用^6,7)

マウスを用いた実験で¹⁴C-グルコースの脳への移行の増加が、また、ウサギ脳切片を用いたin vitro実験で脳内のグルコース代謝の促進が認められている。

3.

脳血流増加作用⁸⁾

成人の脳血管障害患者について本剤投与後の局所脳血流の変化を¹³³Xe-クリアランス法で検討した実験において、脳血流量の増加が認められている。

4.

抗低酸素作用^6,9)

ラットを用いた実験で、脳の低酸素状態に対する抵抗性を増加させることが脳波上認められており、また、マウスを用いた実験で、低酸素ガス負荷による酸素欠乏及びシアン化カリウムによる組織低酸素状態における抗低酸素作用が認められている。

5.

その他の作用^10,11)

ラットの実験的脳浮腫による脳内グリコーゲン量の減少、乳酸量の増加に対する抑制作用や家兎後頭神経の冷却によって生じる病変を抑制する作用が認められている。

有効成分に関する理化学的知見

一般名

メクロフェノキサート塩酸塩(塩酸メクロフェノキサート)
(Meclofenoxate Hydrochloride)

化学式

C₁₂H₁₆ClNO₃・HCl＝294.17

構造式

化学名

2-(Dimethylamino)ethyl (4-chlorophenoxy)acetate monohydrochloride

性状

白色の結晶又は結晶性の粉末で、わずかに特異なにおいがあり、味は苦い。
水又はエタノール(95)に溶けやすく、無水酢酸にやや溶けにくく、ジエチルエーテルにほとんど溶けない。
1.0gを水20mLに溶かした液のpHは3.5～4.5である。

融点

139～143℃

1バイアル×10、1バイアル×50