8．拔怒风

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28页（6911字）

【中文释文】：

(抗风湿剂)

本品系非甾体抗风湿剂，具有高度的镇痛、抗炎和解热效能，用于治疗风湿病。它是普施研究所独家研制的化合物，化学结构同其他应用的抗风湿药物不同。经临床对比，现已发现本品的抗风湿特性可同消炎痛相匹敌，不亚于甚至超过保泰松。不仅如此，本品还具有副作用发生率极为低微的特大优点。临床实验表明多数病人对此药均有极其良好的耐受性，许多服用其他抗风湿药长期胃肠功能障碍病人改服本品后无任何不良反应。业已证明本品胃肠耐受性良好，甚至患有消化性溃疡的病人也是如此。服用本品治疗后，胃部症状减轻，血红蛋白增高。

在整个初期一系列临床研究中，定期观察的结果显示本品在血液、生化或尿等方面没有引起显着的不良改变，以后的临床实践证明长期服用本品其副作用发生率极低。采用计算机分析，此项目持续研究将近4年之久，病人达900多例，所得数据证实本品为一高效抗风湿药物，其治疗价值不会因具有常见的副作用而受到影响。因此，对需要使用抗炎药物治疗的病人，本品是供他们选择的一种药物。

本品口服之后，吸收良好而且迅速，空腹服下一次剂量后约45min血药浓度便可达到高峰。而饭后服药则要在1．5～3h内可抵达较低然而较持久的高峰。现已证明连续服用此药不会出现此化合物或其代谢产物的明显蓄积，并且在停止给药后24h内它们可全部排出。在治疗关节炎时，本品可缓解疼痛和强直，减轻肿胀，改善握力和关节伸屈能力，并使病人在无痛状态下远距离行走。许多用本品治疗过的类风湿性关节炎病人，其红细胞沉降率的降低便表明此药物对疾病活动期有直接的作用。

按推荐用量给药，本品可使大多数关节炎病人的关节功能逐渐得到改善。

〔适应证〕

本品适用于治疗类风湿性关节炎，骨关节炎，强直性脊椎炎和同源的疾病。对斯提尔病(即儿童类风湿性关节炎)、非关节风湿病(包括肌风湿痛病)、慢性背痛及由于急性骨盘脱出引起的下部背痛，本品均有较好疗效。本品的强镇痛作用通常可用于控制疼痛，特别是伴有炎症的疼痛。作为解热药，本品对临床上因发炎或感染引起的发热亦有疗效。

〔剂量(成人)〕

于治疗初期，特别是当由另一种药物改服此药时，为了迅速获得药效，需日服1200mg(6片)。长期试用此药的报告表明，按此剂量长期服用本品并不增加副作用。

用于维持治疗时，该剂量可逐渐减少。多数病人对日服600～800mg的维持剂量(日服3～4次，每次1片)显示满意的效果。

〔用法〕

多数病人空腹吞服本品不致引起胃肠不适，此系本品在治疗清晨关节强直上的一大特点。这些病人可在早晨醒来就用早茶或其他饮料送服每天的第一个剂量，因腹中空无食物，故可迅速吸收药物，使强直很快得到缓解。以后的剂量应于饭后服用，以期较缓慢吸收而获得持久的疗效。

〔副作用〕

本品之所以得到广泛使用与其副作用极为轻微有关，但也偶有消化不良的报告。在某些敏感的病人中，个别病例曾有胃肠出血的记录。皮疹症状极少见。

〔组成与包装〕

本品在英国药典中称为异丁苯丙酸(Ibuprofen)，化学名为2-(4—异丁基苯)丙酸。本品以糖衣片包装出售，每片含200mg异丁苯丙酸(英国药典)。本品呈浅红色，每片印有黑色的“Brufen”字样。

〔生产厂家〕

英国普施制药公司

(附本品别名：异丁苯丙酸，布洛芬，Emodin Motrin)

【外文释文】：

Antirheumatic agent

Brufen(Ibuprofen B．P．)is a non-steroidal anti-rheumatic agent which provides the high level of analgesic，antiinflammatory and anti-pyretic activity required for the effective treatment of rheumatic diseases．It is an original compound evolved in the Boots Research Laboratories and is chemically unrelated to the other anti-rheumatic agents in use．The antirheumatic properties of Brufen have been found，in controlled clinical assessments，to be comparable to those of indomethacin and comparable or superior to phenylbutazone．However，Brufen offers the considerable extra advantage of a singularly low incidence of side-effects．Clinical experience has shown that Brufen is extremely well tolerated by most patients，and that many who have suffered persistent gastrointestinal disturbance with other antirheumatic agents can take Brufen without trouble．Brufen has been shown to have good gastro intestinal toleration even in patients with peptic ulceration；indeed，gastric symptoms have been seen to decrease and haemoglobin levels to rise when therapy with Brufen was undertaken．

Regular observations throughout the initial series of clinical studies indicated that Brufen caused no adverse haematological，biochemical or urinary changes of significance，and subsequent clinical experience has confirmed a remarkably low incidence of side-effects during prolonged administration of the drug．A continuous study，which is subjected to computer analysis，has now been in progress for almost four years and now covers more than 900 patients．The results have established that Brufen is a highly effective anti-rheumatic agent whose therapeutic value is not limited by frequent side-effects．It is therefore，seen as the drug of choice for patients requiring anti-inflammatory therapies．

Brufen is well and rapidly absorbed after oral administration，peak serum levels being achieved about 45 minutes after a single dose given on an empty stomach．When given after food，a lower and more sustained peak level is achieved within 1．5-3 hours．It has beendemonstrated that there is no appreciable bulid-up of the compound or its metabolites during repeated dosing and that，after dosing ceases，excretion is virtually complete within 24 hours．In the treatment of arthritic conditions，Brufen relieves pain and stiffeness，reduces swelling，improves gripstrength and joint flexion，and extends pain-free walking distance．The lowered erythrocyte sedimentation rate observed in many rheumatoid arthritic patients receiving Brufen therapy may indicate a direct effect upon disease activity．

At the recommended dosage，Brufen produces a progressive improvement in the functional capacity of most arthritic patients．

Indications

Brufen is indicated in the treatment of rheumatoid arthritis，osteoarthritis，ankylosing spondylitis and allied conditions．Favourable results have been achieved in Still’s disease(juvenile rheumatoid arthritis)，non-articular rheumatism including fibrositis，in chronic backaches and in low back pain due to acute disc prolapse．The powerful analgesic action．of Brufen is useful for control of pain generally and particularly where pain is associated with inflammation．As an anti-pyretic，Brufen has been shown to be clinically effective in reducing fever associated with inflammation or infection．

Dosage(Adult)

To obtain a rapid response at the start of therapy，particularly when transferring from another drug，a daily dosage of 1 200 mg(6 tablets)，may be used．Reports of long-term trials indicate that even prolonged therapy at this dosage level-does not cause an increased incidence of side effects．For maintenance therapy，the dosage may be gradually reduced．Most patients continue to show a satisfactory response to a maintenance dosage of 600-800 mg(one tablet 3 or 4 times a day)．

Administration

Most patients can take Brufen on an empty stomach without gastric discomfort．It is an important feature in dealing with the problem of early morning stiffness．These patients can take the first dose of each day with morning tea or other drink，as soon as they are awake and，since the stomach contains no food，absorption of the drug is rapid and stiffness quickly relieved．Subsequent doses should be given after meals so that absorption is more gradual and a more prolonged effect achieved．

Side-effects

The widespread use of Brufen has been associated with a singularly low incidence of sideeffect，but occasional reports of dyspepsia have been received．In some susceptible patients，isolated cases of gastro-intestinal haemorrhage have been recorded．Rarely，a rash has been observed．

Composition and presentation

Brufen is Ibuprofen B．P．，described chemically as 2-(4-iso-butylphenyl)propionic acid．

Brufen is available as sugar-coated tablets，each containing 200 mg of Ibuprofen B．P．The tablets are coloured light magenta，each bearing the overprint of‘Brufen’in black．

Manufacturer

Boots Co．Ltd．，England．