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首页> 外文期刊>CNS drug reviews >Clinical data on the CGRP antagonist BIBN4096BS for treatment of migraine attacks.
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Clinical data on the CGRP antagonist BIBN4096BS for treatment of migraine attacks.

机译：CGRP拮抗剂BIBN4096BS用于治疗偏头痛的临床数据。

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Basal studies have shown that calcitonin gene-related peptide (CGRP) is a major sensory neuronal messenger in the trigeminovascular system, the pathway conveying intracranial pain. In migraine and cluster headache attacks, CGRP is released in parallel with the pain and successful treatment of the attacks abort both the associated pain and the CGRP release. The search for a potent small molecule CGRP antagonist has been successful and such an agent has been tested in preclinical and clinical studies. The aim of the present study was to examine current knowledge on the clinical pharmacology of systemic BIBN4096BS, which has been shown in man to abort acute migraine attacks as well or better than oral sumatriptan. BIBN4096BS is a specific and potent CGRP receptor antagonist in humans. In safety and tolerability studies the substance is well tolerated with no or only mild side effects. In acute migraine attacks the overall response was 66% with the drug and 27% with placebo. A difference as compared to placebo was seen at 30 min; the response was still rising at 4 h suggesting a long duration of action. At 24 h the pain-free rate was better than that with triptans, suggesting a lower grade of rebound and perhaps even a prophylactic possibility.
机译：基础研究表明，降钙素基因相关肽（CGRP）是三叉神经血管系统（传递颅内疼痛的途径）中主要的感觉神经元信使。在偏头痛和丛集性头痛发作中，CGRP与疼痛同时释放，成功治疗发作中止了相关的疼痛和CGRP释放。寻找有效的小分子CGRP拮抗剂的研究已经成功，并且已经在临床前和临床研究中测试了这种药物。本研究的目的是检查有关全身性BIBN4096BS临床药理学的最新知识，该知识已被证明可以使人中止急性偏头痛发作，甚至优于口服舒马曲坦。 BIBN4096BS是人类中一种有效的特异性CGRP受体拮抗剂。在安全性和耐受性研究中，该物质具有良好的耐受性，没有或仅有轻微的副作用。在急性偏头痛发作中，该药的总缓解率为66％，而安慰剂为27％。在30分钟时发现与安慰剂相比有差异。 4 h时反应仍在上升，表明作用时间长。在24小时时，无痛率比曲坦类药物更好，表明反弹的程度较低，甚至可能是预防性的可能性。

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