普瑞巴林的部分中文处方资料（仅供参考）
药品英文名
Pregabalin
药品别名 
普瑞巴林、LYRICA
药物剂型
胶囊：25mg；50mg；75mg；100mg；150mg；200mg；300mg。
药理作用
本药为γ-氨基丁酸(GABA)类似物，结构和作用与加巴喷丁相似，具有抗癫痫、镇痛和抗焦虑活性。本药的抗癫痫作用机制尚不明确。在实验室研究中，本药对各种癫痫模型均有抗惊厥活性；动物模型的活性谱与加巴喷丁的活性谱相似，但本药的活性为加巴喷丁的3～10倍。
药动学
本药口服后，用于急性牙痛时30min内起效，持续时间约5h，用于糖尿病性神经病变时1周起效。达峰时间约1h，生物利用度为90%。较少在肝脏代谢，92%～99%以原形经肾排泄，低于口服量的0.1%随粪便排泄，半衰期为5～6.5h。
适应证
1.神经元性疼痛：糖尿病周围神经病变的神经痛和疱疹后遗神经痛。
2.癫痫部分发作的辅助治疗(国外资料)。
3.还可用于焦虑症、社交恐怖症、关节炎。
禁忌证
对本药过敏者(国外资料)。
注意事项
1.停药时，建议至少在1周的时间内逐渐减量。动物试验中，本药可引起雄性动物不育。
2.慎用：
(1)充血性心力衰竭患者(国外资料)。
(2)眼科疾病患者(国外资料)。
(3)糖尿病患者。
3.药物对儿童的影响：用药的安全性和有效性尚未确定。
4.药物对妊娠的影响：尚不明确。
5.药物对哺乳的影响：尚不明确。
6.用药前后及用药时应当检查或监测：定期进行血生化检测。
不良反应
1.心血管系统：可见周围性水肿、PR间期延长。
2.中枢神经系统：可出现头晕(21%～32%)、嗜睡(12%～22%)、共济失调(3%～15%)、头痛(7%)、衰弱(5%)、语言障碍(5%)、震颤(1%～8%)、健忘(1%～5%)、神经错乱(3%～4%)、思维紊乱(2%～8%)。
3.代谢/内分泌系统：可引起体重增加，发生率4%～12%。
4.肌肉骨骼系统：可见肌酸激酶水平升高(2%)、肌阵挛(2%)，另有发生横纹肌溶解的个案报道。5.肝脏：大剂量(一日900mg)用药偶见肝脏酶学水平轻度和一过性升高。
6.胃肠道：可引起唾液缺乏(4%～8%)、便秘(4%～5%)等。
7.血液：可见血小板减少(3%)。
8.眼：可出现视力模糊(4%～10%)、复视(2%～9%)、弱视等，但与本药的因果关系未确定。
9.其他：
(1)可见感染性疾病(7%)。
(2)己观察到大鼠用药后肿瘤发生率增加。
用法用量
成人常规剂量：口服给药：
1.癫痫部分发作的辅助治疗：
(1)一次75mg，一日2次或一次50mg，一日3次。根据个体反应和耐受性，可增至最大量一日600mg，分2～3次服用。
(2)其他抗癫痫药无效的顽固性癫痫患者，加用本药一日150～600mg，分2～3次服用。
2.糖尿病周围神经病变的神经痛：初始剂量一次50mg，一日3次；根据疗效和耐受性可在1周内增至一次100mg，一日3次。
3.疱疹后遗神经痛：初始剂量一次75mg，一日2次或一次50mg，一日3次；根据治疗效果和耐受性可在一周内增至一日300mg。维持量为一次75～150mg，一日2次或一次50～100mg，一日3次。
4.广泛性焦虑障碍：一日300～600mg。5.社交恐怖症：一次200mg，一日3次。
6.术后牙痛：单次300mg，可根据麻醉持续时间，每6小时重复给药1次。透析时剂量：血液透析后应立即给予补充剂量。
药物相应作用
1.合用噻唑烷二酮类抗糖尿病药，发生体重增加和周围性水肿的风险增加，合用时应慎重。
2.本药可增强中枢神经系统抑制药的镇静作用。
3.本药可增强酒精的镇静作用。
4.食物可降低本药的生物利用度。
[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。
[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300mg、600mg pregabalin8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。

LYRICA

Generic Name and Formulations:
Pregabalin 25mg, 50mg, 75mg, 100mg, 150mg, 200mg, 225mg, 300mg; caps.

Company:
Pfizer Inc.

Indications for LYRICA:
Fibromyalgia.

Adult Dose for LYRICA:
≥18yrs: initially 75mg twice daily, may increase to 150mg twice daily within 1 week as tolerated; max 450mg/day. Renal impairment (CrCl <60mL/min): reduce dose (see literature); hemodialysis: give supplemental dose after session.

Children's Dose for LYRICA:
<18yrs: not recommended.

See Also:
LYRICA ORAL SOLUTION

Pharmacological Class:
alpha2-delta ligand.

Warnings/Precautions:
Avoid abrupt cessation (taper over ≥1 week). Discontinue if angioedema, hypersensitivity reactions, myopathy or markedly elevated creatine kinase levels occur. CHF. Ocular conditions. Diabetes (monitor skin integrity). Suicidal tendencies (monitor). Labor & delivery. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions:
Potentiates CNS depression with alcohol, other CNS depressants. Additive edema, weight gain with thiazolidinediones.

Adverse Reactions:
Dizziness, somnolence, other CNS effects, dry mouth, edema, ocular/visual effects (eg, blurring), weight gain, thinking abnormal (primarily difficulty with concentration/attention), infection, asthenia, paresthesias, elevated creatine kinase, decreased platelets, arrhythmias (PR prolongation); male-mediated teratogenicity; may be tumorigenic.

How Supplied:
Caps—90; Soln—16oz

Important Safety Information
LYRICA is contraindicated in patients with known hypersensitivity to pregabalin or any of its other components. Angioedema and hypersensitivity reactions have occurred in patients receiving pregabalin therapy.
There have been postmarketing reports of hypersensitivity in patients shortly after initiation of treatment with LYRICA. Adverse reactions included skin redness, blisters, hives, rash, dyspnea, and wheezing. Discontinue LYRICA immediately in patients with these symptoms.
There have been postmarketing reports of angioedema in patients during initial and chronic treatment with LYRICA. Specific symptoms included swelling of the face, mouth (tongue, lips, and gums), and neck (throat and larynx). There were reports of life-threatening angioedema with respiratory compromise requiring emergency treatment. Discontinue LYRICA immediately in patients with these symptoms.
Antiepileptic drugs (AEDs) including LYRICA increase the risk of suicidal thoughts or behavior in patients taking AEDs for any indication. Monitor patients treated with any AED for any indication for the emergence or worsening of depression, suicidal thoughts or behavior, and/or any unusual changes in mood or behavior. Pooled analysis showed clinical trial patients taking an AED had approximately twice the risk of suicidal thoughts or behavior than placebo-treated patients. The estimated incidence rate of suicidal behavior or ideation among 27,683 AED-treated patients was 0.43%, compared to 0.24% among 16,029 placebo-treated patients, representing an increase of approximately one patient for every 530 patients treated with an AED.
The most common adverse reactions across all LYRICA clinical trials are dizziness, somnolence, dry mouth, edema, blurred vision, weight gain, constipation, euphoric mood, balance disorder, increased appetite, and thinking abnormal (primarily difficulty with concentration/attention).
Inform patients taking LYRICA that dizziness and somnolence may impair their ability to perform potentially hazardous tasks such as driving or operating complex machinery until they have sufficient experience with LYRICA to determine its effect on cognitive and motor function.
In controlled studies, a higher proportion of patients treated with LYRICA reported blurred vision (7%) than did patients treated with placebo (2%), which resolved in a majority of cases with continued dosing. Consider more frequent assessment for patients who are already routinely monitored for ocular conditions.
Higher frequency of weight gain and edema was observed in patients taking both LYRICA and thiazolidinedione antidiabetic drugs. Exercise caution when coadministering these drugs. Patients who are taking other drugs associated with angioedema such as angiotensin-converting enzyme inhibitors (ACE inhibitors) may be at increased risk of developing angioedema. Exercise caution when using LYRICA in patients who have had a previous episode of angioedema.
LYRICA may exacerbate the effects of oxycodone, lorazepam, or ethanol on cognitive and gross motor functioning.
Patients with a history of drug or alcohol abuse may have a higher chance of misuse or abuse of LYRICA.
As with all antiepileptic drugs (AEDs), withdraw LYRICA gradually over a minimum of 1 week to lessen the potential of increased seizure frequency in patients with seizure disorders.
Patients with a creatinine clearance of 30 to 60 mL/min had a greater incidence of discontinuation due to adverse reactions than patients with normal creatinine clearance. Adjust the daily dose of LYRICA for patients with reduced renal function (creatinine clearance ≤60 mL/min) and in those undergoing hemodialysis. Administer a supplemental dose of LYRICA immediately following every 4-hour hemodialysis treatment.
In standard, preclinical in vivo lifetime carcinogenicity studies of LYRICA, an unexpectedly high incidence of hemangiosarcoma was identified in 2 different strains of mice. The clinical significance of this finding is unknown. In clinical studies across various patient populations comprising 6396 patient-years of exposure in patients >12 years of age, new or worsening preexisting tumors were reported in 57 patients.
Indication
LYRICA® (pregabalin) capsules  is indicated for the management of:
Fibromyalgia
Neuropathic pain associated with Diabetic Peripheral Neuropathy (DPN)
Postherpetic neuralgia (PHN)
Neuropathic pain associated with Spinal Cord Injury (SCI)
LYRICA is also indicated as adjunctive therapy for adult patients with Partial Onset Seizures
附件:

200963023312624.pdf 

 
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注：以下产品不同规格和不同价格，购买以咨询为准！
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产地国家: 澳大利亚
原产地英文商品名:
LYRICA 25MG/CAP 56CAPS/BTL
原产地英文药品名:
PREGABALIN
中文参考商品译名:
LYRICA 25毫克/胶囊 56胶囊/瓶
中文参考药品译名:
普瑞巴林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer
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产地国家: 西班牙
原产地英文商品名:
LYRICA 150毫克x100胶囊/瓶
原产地英文药品名:
pregabalin
中文参考商品译名:
普瑞巴林
中文参考药品译名:
普瑞巴林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer Global Pharmaceuticals
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产地国家: 西班牙
原产地英文商品名:
LYRICA 75毫克x100胶囊/瓶
原产地英文药品名:
pregabalin
中文参考商品译名:
普瑞巴林
中文参考药品译名:
普瑞巴林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer Global Pharmaceuticals
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产地国家: 加拿大
原产地英文商品名:
LYRICA 75MG/CAP 60CAPS/BTL
原产地英文药品名:
PREGABALIN
中文参考商品译名:
LYRICA 75毫克/胶囊 60胶囊/瓶
中文参考药品译名:
普瑞巴林
生产厂家中文参考译名:
辉瑞公司
生产厂家英文名:
Pfizer