11．脑活素

出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第44页（8683字）

【中文释文】：

治疗脑功能紊乱新药

〔成分〕

脑活素是用生物技术标准化的酶降解纯化的猪脑蛋白制成的一种肽制剂。应用于注射或滴注的溶液中不含蛋白，脂肪及其它抗原性物质。每毫升脑活素溶液中含有215．2mg浓缩脑活素(猪脑提取的肽制剂)。

〔功效与特性〕

脑活素疗效已经被大量临床、动物实验所证实。该药能加快小鸡大脑发育，推论脑活素对神经细胞的蛋白质合成及其呼吸链有良好的作用，并同时刺激有关激素产生。实验亦表明脑活素能有效地保护中枢神经系统免受有毒物质的侵害。事先注射脑活素可提高大鼠的抗缺氧能力。用药后，用电-光学方法证明，几日龄大鼠的大脑成熟显着加快，而成鼠在迷路试验时的识别能力亦增强。与对照组相比．使用脑活素组大鼠的葡萄糖在血脑屏障中转运速度显着加快。

已有丰富的文献阐述了脑活素的治疗经验。其中具特别意义的是一份关于在9个不同病种中大量受试者的研究，用11种心理试验对脑活素的效能进行各种分析。在几个临床对照试验中，脑活素治疗能改善记忆，认知能力，以及Alzheimer病以及血管性痴呆病人的自我评价，在中风和颅脑损伤后用脑活素治疗可以加速恢复。对有治疗性低血糖昏迷的病人，脑活素有明显的催醒作用，EEG(脑电图)也相应地恢复正常化。脑活素亦可作为电休克治疗的辅助用药，可使病人更迅速地从健忘的困扰中恢复。

〔适应证〕

尤以注意力及记忆障碍的器质性脑性综合征。

·原发性退行性痴呆(如早老性痴呆型的老年性痴呆)

·血管性痴呆(如多发梗塞性痴呆)

·混合型痴呆

·中风、卒中、颅脑手术后脑功能障碍

·脑挫伤或脑震荡后遗症

·脑血管代偿机能障碍

·神经衰弱及衰竭症状

〔副作用〕

脑活素，人对其一般耐受良好，几乎无任何毒性且安全性很高，脑活素在体内或体外毒性试验中没有任何致畸，致敏或致癌性。注射过快会有轻度热感，极少数病例会表现为寒颤，轻度发热的过敏反应，且多与病人体质反应有关。迄今尚未发现用药后发生持久的不良反应或危及生命的病例。高剂量后和注射太快有少数病例出现发热。

〔禁忌证〕

对本药任一成分过敏。

癫痫状态。

癫痫大发作：此时用药可能增加发作频率。

严重肾功能障碍。

〔剂量与用法〕

本药规格有1ml，2ml，5ml，10ml安瓿。

每一疗程最好连续注射，参考病人年龄、体重、病情以决定疗程长短及剂量。皮下注射不超过2ml，肌肉注射不超过5ml，静脉推注不超过10ml。

推荐用10～30ml脑活素稀释于250ml5%葡萄糖或生理盐水中缓慢滴注，60～120min滴完。

每疗程应依病情包括10～20次输注。

严重病例，尤其是伴有脑血管代偿不足者，可用10～30ml脑活素稀释于250ml5%葡萄糖或生理盐水中滴注。倘若每天给药，则每疗程用10～20次药物滴注。本药可与葡萄糖、维生素及任何需用的心血管药合用。对轻微病例或经大剂量用药后为保持疗效者，可用肌肉注射(或皮下，静脉注射)，开始每日1次，每次5ml，连用10～20次，以后每周2～3次，可重复几个疗程，直至临床表现不再改善为止。

〔包装·规格〕

1ml×10安瓿／盒

2ml×10安瓿／盒

5ml×5安瓿／盒

10ml×5安瓿／盒

〔保存〕

置不超过25℃安全、阴凉、干燥处，避光，勿让小孩接触。

〔生产厂家〕

奥地利依比威药厂

(附本品别名：脑蛋白水解物，Brain Protein Hydrolysate)

【外文释文】：

For the modern，safe and effective treatment of disturbed cerebral functions

Composition

Cerebrolysin is a peptide preparation produced by biotechnological standardised enzymatic breakdown of purified porcine brain protein．The solution，ready for injection or infusion，is free of proteins，lipids，as well as of antigenic properties．One ml of Cerebrolysin contains 215．2 mg of Cerebrolysin concentrate(porcine brain derived peptide preparation)in aqueous solution．

Properties and effectiveness

The effectiveness of cerebrolysin is proven in numerous animal experiments and clinical trials．Cerebrolysin favorably influences protein synthesis and the respiratory chain of neurons while simultaneously stimulating the complex production of hormones．This can be inferred from the rapid cerebral development of chicks．This is also demonstrated by experimental studies in which cerebrolysin protects the central nervous system from noxious substances．Prior treatment of rats with cerebrolysin induces enhanced resistance to anoxia．In these experiments a dosage-dependent effect on the nucleinic acid concentration in the brain occurs．A pronounced acceleration in maturation in the brain of several days-old rats was demonstrated by electro-optical means，and adult rats exhibited enhanced learning ability in labyrinth tests，both after administration of cerebrolysin．Glucose transport processes at the blood brain barrier improve at a markedly faster rate in cerebrolysin treated subjects as compared to a control group．

Cerebrolysin is a brain-specific peptidergic nootropic and neurotrophic drug able to effect the central nervous system in a multimodal way like regulation and improvement of neuronal metabolism，modulation of the synaptic plasticity and induction of neuronal differentiation and further protection against different types of ischaemic and neurotoxic lesions．Abundant literature exists on therapeutic experience with cerebrolysin．Of particular significance is a study involving an extensive number of subjects distributed among 9 different disease groups in which the effectiveness of cerebrolysin could be established through the use of 11 psychological tests subjected to variance analysis．In several controlled clinical trials cerebrolysin treatment leads to an improvement of memory，cognitive performance and patients self-assessed well-being in Alzheimer’s Disease as well as in vascular dementia．After stroke and craniocerebral trauma treatment with cerebrolysin leads to an accelerated recovery．In patients experincing therapeutic hypoglycaemic coma a pronounced arousal effect was observed after administration of cerebrolysin with a correlative normalization of the EEG．Cerebrolysin is also suitable as an adjuvant in electroshock therapy，as it has been shown to ensure more rapid recovery from amnesic disturbances．Literature on Cerebrolysin is documented and available on demand．

Indications

Organic brain syndrome particularly disturbances of concentration and memory：

·primary degenerative dementia(e．g senile dementia of Alzheimer’s type)

·vascular dementia(e．g．multiinfarct dementia)

·mixed forms of dementia

·disturbed cerebral functions after stroke，apoplexia，cranial surgery

·complaints following cerebral contusion or concussion

·cerebrovascular decompensation

·nervous exhaustion and failure symptoms

Side effects

Cerebrolysin is generally well tolerated．Cerebrolysin possesses almost no toxicity and shows an extremely high level of drug safety．Cerebrolysin does no show any mutagenic potential，sensitising effects or carcinogenicity in toxicological tests，neither in vitro nor in vivo．If injected too rapidly，it can cause a moderate heat sensation．In extremely rare cases ahypersensitivity reaction manifested in chills or a slight increase in body temperature has occured，the cause of which is most probably to be found in the responsiveness of the patient．In no case to date has the undesirable effect persisted or proved threatening for the patient．After high dosage and if too rapidly injected，in rare cases fever has been observed．

Contraindications

·hypersensitivity to one of the components of the drug

·status epilepticus

·grand mal fits；in these cases an increase of the fit frequency can appear

Dosage and administration

Cerebrolysin is available in 1 ml，2 ml，5 ml and 10 ml ampoules．It is recommended to carry out the series of injections in accordance with a course of treatment，the length of therapy and the individual doses being dependent on the age of the patient and the severity of the disease．Up to 2 ml of Cerebrolysin can be injected subcutaneously，up to 5 ml intramuscularly and up to 10 ml intravenously．In addition，an infusion containing 10 ml to maximum 30 ml diluted in approx．250 ml of physiologic saline is recommended，which should be given slowly enough so that the length of the infusion is approx．60-120 minutes．A serial course of treatment should comprise 10 to 20 injections of infusions，depending on the severity of the case．In severe cases，especially those involving cerebrovascular decompensation，10-30 ml diluted in 250 ml of physiologic saline is administered as an infusion．In the case of daily administration a series consists of 10-20 infusions．Cerebrolysin can also be combined with dextrans(e．g．Rheomacrodex)，vitamins，and any required cardiac or circulatory drugs．In mild cases or to ensure success following high-dosage Cerebrolysin therapy series of 10 to 20 injections iv(im also possible)of about 5 ml are given initially daily and later 2 to 3 times weekly．Cerebrolysin injection series can be repeated several times in accordance with the clinical condition until further improvement is not longer achieved．

Presentation and packs

Original packs with 10 ampoules of 1 ml

10 ampoules of 2 ml

5 ampoules of 5 ml

5 ampoules of 10 ml

Keep in a safe place out of the reach of children．Store in a cool dry place not over 25℃，away from light．

Manufacturer

Ebewe Arzneimittel Ges．m．b．H．，Austria