药品名称: 普瑞巴林
药理药效：普瑞巴林是一种新型γ-氨基丁酸(GABA)受体激动剂,能阻断电压依赖性钙通道,减少神经递质的释放,临床主要用于治疗外周神经痛以及辅助性治疗局限性部分癫痫发作。
别名: C1-1008
化学名称: (3S)-3-氨甲基-5-甲基己酸
美国化学文摘登录号: [ 148553-50-8 ]
分子式: C8H17NO2
分子量: 159.23
物化性质： 白色结晶性粉末
[简介]：辉瑞公司开发的pregabalin [CI 1008]是一种γ氨基丁酸结构类似物，是一种具有抗痉挛作用的化合物。该化合物正在美国进行治疗癫痫的III期临床试验。该化合物的其他适应症包括神经病理性疼痛、泛发性焦虑症和社交恐怖症。辉瑞公司暂时停止了在美国进行的pregabalin治疗神经病理性疼痛的III期临床试验，因为动物实验发现该化合物有可能引起小鼠肿瘤，实际上之前的研究没有发现pregabalin有任何潜在的致瘤性。辉瑞公司称正与FDA协商以解决这一问题，但向FDA提交新药申请的计划不受影响。治疗癫痫和焦虑症的临床试验仍继续进行。Pregabalin的抗痉挛作用机理还不完全明了，实验发现Pregabalin可以和细胞的加巴喷丁结合位点结合，但是否是和加巴喷丁类似的作用机理和不得而知。临床前研究发现Pregabalin的抗痉挛特性和加巴喷丁类似，但活性更强。一项II期临床试验发现pregabalin对顽固性局灶性癫痫仍有抗痉挛作用。

[药代动力学]：在随机、安慰剂对照交叉临床试验中，29名健康志愿者接受pregabalin 1-300mg单次口服。Pregabalin吸收迅速，tmax在1.3小时内达到。Cmax和AUC 0-∞和给药剂量成正比，两者的范围分别为0.0383-9.46μg/ml和0.223-66.3μg x h-1xml-1。清除半衰期的范围为4.6-6.8h，和剂量无关。89.8%的给药剂量以原型形式从尿中排出[1]。

[不良反应]：一项双盲、安慰剂对照试验发现，165名局部发作型癫痫病人在原有治疗基础上加上pregabalin治疗（剂量为50、100、150、300和600 mg/day，每日两次）。最大剂量时大部分患者的耐受性良好。头晕和嗜睡是最常出现的不良反应，600mg/day剂量组的发生率最高，头晕发生率为42%，嗜睡的发生率为29%。而安慰剂组这两种不良反应的发生率均为11%。大部分不良反应为轻到中度。8名患者因不良反应退出了试验，这些患者均是300mg/day 和600mg/day剂量组的患者[2]。泛发型焦虑症和社交恐怖症患者所进行的临床试验也发现头晕和嗜睡是最常出现的不良反应[3] [4]。

[临床试验]：在2003年6月美国神经病学会议上，辉瑞公司公布的pregabalin试验数据表明，该药可以快速有效的治疗广泛性焦虑障碍(GAD)的各种症状。数据综合自5个安慰剂对照试验，包括II期临床试验和III期临床先导试验。数据表明pregabalin对GAD急性治疗的效果广泛、快速。Pregabalin在使用第一周就缓解了每个参加试验患者的精神和身体焦虑症状。在其中一个先导试验中，抗抑郁药文拉法新（venlafaxine）作为对照药物。与之相比pregabalin改善精神和躯体焦虑症状显著快，文拉法新没能在第一周就改善患者焦虑症状。在另一个先导试验中，以苯并二氮卓类药物阿普唑仑(alprazolam)为对照药品，数据再次显示pregabalin显著快速的改善精神和躯体焦虑症状，在第一周就有所改善，而阿普唑仑在第一周只改善了精神症状。2002年的一项双盲试验考察疱疹感染后神经痛患者服用300 mg、600mg pregabalin 8周后与安慰剂的差别，评价方式为平均疼痛得分和SF-McGill疼痛调查表（SF-MPQ）。治疗后第一周疗效就很明显，并且效果持续到研究结束。而另一个研究表明该药效果与剂量相关。在健康志愿者和肾功能不好的慢性疼痛患者中的药代动力学考察表明药物释放呈线性，两者的药物消除率与肌酐清除率有关，在同时服用口服胰岛素、利尿剂和抗糖尿病药物时不必调整该药剂量。

Monograph Number: 7813
Title: Pregabalin
CAS Registry Number: 148553-50-8
CAS Name: (3S)-3-(Aminomethyl)-5-methylhexanoic acid
Additional Names: (S)-(+)-4-amino-3-(2-methylpropyl)butanoic acid; (S)-(+)-3-isobutyl-g-aminobutyric acid
Manufacturers' Codes: CI-1008; PD-144723
Molecular Formula: C8H17NO2
Molecular Weight: 159.23.
Percent Composition: C 60.34%, H 10.76%, N 8.80%, O 20.10%
Literature References: GABA analog. Prepn of racemate: R. Andruszkiewicz, R. B. Silverman, Synthesis 1989, 953. Enantioselective synthesis: P. Yuen et al., Bioorg. Med. Chem. Lett. 4, 823 (1994). Manufacturing process: M. S. Hoekstra et al., Org. Process Res. Dev. 1, 26 (1997). HPLC determn in biological fluids: B. L. Windsor, L. L. Radulovic, J. Chromatog. B 674, 143 (1995). Anticonvulsive activity: C. P. Taylor et al., Epilepsy Res. 14, 11 (1993). Activity in models of neuropathic pain: M. J. Field et al., Pain 80, 391 (1999).
Properties: White crystalline solid, mp 186-188? [a]D23 +10.52?(c = 1.06 in water).
Melting point: mp 186-188°
Optical Rotation: [a]D23 +10.52?(c = 1.06 in water)
Therap-Cat: Anticonvulsant.
LYRICA is indicated for the management of fibromyalgia. It is also used to help people with diabetes manage nerve pain and for pain after shingles. LYRICA is also used together with other seizure medicines to help adults with partial seizures.

LYRICA is not for everyone. LYRICA may cause serious allergic reactions. Tell your doctor right away about any serious allergic reaction such as swelling of the face, mouth, lips, gums, tongue or neck or if you have any trouble breathing. Other allergic reactions may include rash, hives and blisters. Tell your doctor about any changes in your eyesight, including blurry vision, muscle pain along with a fever or tired feeling, or skin sores due to diabetes.

Some of the most common side effects of LYRICA are dizziness, sleepiness, weight gain, blurred vision, dry mouth, feeling "high", swelling of hands and feet, and trouble concentrating. You may have a higher chance for swelling and hives if you are also taking angiotensin converting enzyme (ACE) inhibitors so you should let your doctor know if you are taking these medications. You may have a higher chance of swelling or gaining weight if you are also taking certain diabetes medicines.

You should not drive a car or operate machinery until you know how LYRICA affects you. Do not drink alcohol while on LYRICA. Be especially careful about medicines that make you sleepy. Also tell your doctor if you are planning to father a child. Tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you have had a drug or alcohol problem, you may be more likely to misuse LYRICA. You should talk with your doctor before you stop taking LYRICA, or any other prescription medication. LYRICA is one of several treatment options for you and your doctor to consider.
包装规格: 75毫克x60胶囊/瓶

单价(人民币 RMB): 1,868 元
生产厂家：Pfizer Global Pharmaceuticals （辉瑞公司）
药品相关信息网址：http://www.lyrica.com/