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  药店国别: 美国药房
产地国家: 美国
所属类别: 神经系统药物->抗癫痫药物
处方药:处方药
包装规格: 10毫克/片 30片/盒
计价单位:
   
生产厂家中文参考译名:
卫材
生产厂家英文名:
EISAI INC
该药品相关信息网址1:
https://www.rxlist.com/fycompa-drug.htm
原产地英文商品名:
FYCOMPA 10 MG TABLET 30 Tablets
原产地英文药品名:
PERAMPANEL
中文参考商品译名:
FYCOMPA 10毫克/片 30片/盒
中文参考药品译名:
吡仑帕奈
原产地国家批准上市年份:
2012/10/22
英文适应病症1:
epilepsy
临床试验期:
完成
中文适应病症参考翻译1:
癫痫
药品信息:
FYCOMPA (perampanel)片,为口服使用 美国初次批准:2012 适应症和用途 FYCOMPA,一个非竞争性AMPA谷氨酸盐受体拮抗剂,适用于在有癫痫年龄12岁和以上患者中作为辅助治疗为有或无继发性全身性癫痫部分性癫痫发作的治疗(1) 剂量和给药方法 ● 在不对酶-诱导抗癫痫药物患者中,开始剂量为睡前2 mg每天1次和对酶-诱导抗癫痫药物患者4 mg (2.1) ● 根据临床反应和耐受性通过在睡前最大2 mg每天1次每周增量可增加至睡前剂量4 mg至12 mg每天1次。发生剂量增加不应频繁高于每周间隔。(2.1) ● 每天最大推荐剂量为睡前12 mg每天1次。(2.1) ● 老年患者:对剂量增加最高频数是每两周。 ● 轻度和中度肝受损患者:对轻度和中度肝受损患者每天最大推荐剂量分别为睡前6 mg和4 mg每天1次,. 剂量增加最高频数是每2周。(2.2) ● 严重肝受损患者:无建议。 (2.2) ● 严重肾受损或进行血液透析患者:无建议。(2.3) 剂型和规格 片:2 mg,4 mg,6 mg,8 mg,10 mg,和12 mg。(3) 禁忌症 无。(4) 警告和注意事项 ● 自杀行为和意念:监视自杀的想法或行为(5.2) ● 神经系统的影响:监视头晕,步态不稳,睡意,和疲乏(5.3) 当驾驶或操作机械时患者应谨慎(5.3) ● 跌交:监视跌交和损伤(5.4) ● 撤销抗癫痫药物:在癫痫患者中,有可能增加癫痫发作频数 (5.5) 不良反应 最常见不良反应(较高于安慰剂≥4%和≥1%)包括头晕,睡意,疲乏,易怒,跌交,恶心,体重增加,眩晕,共济失调,步态不稳,和平衡障碍。(6.1) 药物相互作用 ● 避孕药:12 mg每天1次剂量可能会减低含左炔诺孕酮激素避孕药的有效性。(7.1) ● 细胞色素P450诱导剂:卡马西平[Carbamazepine],奥卡西平[oxcarbazepine]和苯妥英[phenytoin]增加 perampanel的清除率和减低perampanel血浆浓度和减低FYCOMPA的有效性。对此没有充分信息描述可完全纠正的剂量调整。苯巴比妥 [Phenobarbital]和普里米酮[primidone]也可能减低perampanel浓度。当这些酶-诱导抗癫痫药物被引入或撤销时,应严密 监视患者。可能需要调整FYCOMPA剂量。(7.2) ● 强CYP3A诱导剂除了抗癫痫药物:应避免(如,利福平[rifampin],圣约翰草[St. John's wort])。(7.2) 为报告怀疑不良反应,联系 Eisai电话1-888-274-2378或联系FDA电话1-800-FDA-1088或www.fda.gov/medwatch. 特殊人群中使用 妊娠:根据动物数据,可能引起胎儿危害。(8.1) 完整处方资料 第二部分 12.3 药代动力学 健康受试者和有部分性癫痫发作患者Perampanel的药代动力学相似。Perampanel的半衰期约105小时,使约在2-3周达到稳态。单次给予0.2–12 mg的Perampanel后和每天1次多次给予1-12 mg后,AUC以剂量-正比例方式增加。 吸收 口服给药后Perampanel被迅速和完全吸收与可忽略的首过代谢。在空腹条件下中位Tmax范围从0.5至2.5小时。食物不影响吸收的程度 (AUC),但减慢吸收的速率。在进食条件下,perampanel的Cmax与空腹条件比较减低28-40%和Tmax延迟2-3小时。 分布 来自体外 研究数据表明,在浓度范围20至2000 ng/mL,perampanel约95-96%结合至血浆蛋白,主要结合至白蛋白和α1-酸性糖蛋白。Perampanel的血液与血浆比值为0.55-0.59。 代谢 Perampanel通过原发氧化和相继葡萄糖醛酸化被广泛地代谢。根据体外 研究用重组人CYPs和人肝微粒体的结果氧化代谢是通过CYP3A4和/或CYP3A5介导的。也可能涉及其他CYP 酶。 给予放射性标记 perampanel后,在全身循环中未变化perampanel占总放射性74-80%,而在血浆中检测到只有痕量个体perampanel代谢物。 消除 放射性标记perampanel给予8例健康老年受试者后,在尿中回收22%给予放射性和在粪中48%。在尿和粪中,回收的放射性主要是氧化和结合代谢物 的混合物组成。来自19项报道的1期研究合并数据的群体药代动力学分析perampanel的t1/2平均为105小时。健康受试者和患者的 Perampanel表观清除率约为12 mL/min。 特殊人群 肝受损 在12例有轻度和中度肝受损(分别Child-Pugh A和B)受试者与12例人口统计指标匹配的健康受试者比较,在单次1 mg剂量后评价Perampanel的药代动力学。与其健康对照比较有轻度肝受损受试者中总体(游离和蛋白结合)perampanel的暴露(AUC0- inf)是较大50%和有中度肝受损受试者中高于两倍(2.55-倍)。有轻度和中度肝受损受试者的游离perampanel的AUC0-inf分别为匹 配健康对照的1.8-倍和3.3-倍。轻度受损受试者T1/2延长(306相比125小时)和中度受损(295相比139小时)。未曾在有严重肝受损受试 者中研究Perampanel[见剂量和给药方法(2.2),特殊人群中使用(8.6)]。 肾受损 在有肾受损患者中尚未进行专门研究评价Perampanel的药代动力学。用来自在安慰剂-对照临床试验有部分性癫痫发作和接受FYCOMPA直至12 mg/day患者的合并数据进行群体药代动力学分析。结果显示在有轻度肾受损患者(肌酐清除率50-80 mL/min)与有正常肾功能患者(肌酐清除率 > 80 mL/min)比较perampanel表观清除率减低27%,与AUC相应增加37%。考虑到正常和轻度受损患者间暴露的重大重叠,对有轻度肾受损患者 无需剂量调整。尚未在有严重肾受损患者和进行血液透析患者中进行Perampanel研究[见剂量和给药方法(2.3),特殊人群中使用(8.7)]。 性别 在安慰剂-对照临床试验中有部分性癫痫发作接受FYCOMPA患者的群体药代动力学分析,在女性中perampanel表观清除率(0.605 L/hr)是低于男性(0.730 L/hr)17%。无需根据性别调整剂量。 儿童患者 尚未在<12岁患儿中研究FYCOMPA,在有部分性癫痫发作患者年龄范围从12至74岁接受FYCOMPA的安慰剂对照试验,在一项群体药代动力学分析,在青少年(0.787 L/hr)中perampanel的表观清除率是略微,但不显著,较高于成年。儿童患者高于12岁可相似于成年给药。 老年人 在安慰剂-对照试验,有部分性癫痫发作患者的群体药代动力学分析年龄范围从12至74岁接受FYCOMPA 未发现年龄对perampanel表观清除率的明显影响[见剂量和给药方法(2.1),特殊人群中使用(8.5)]。 种族 在安慰剂对照试验中,有部分性癫痫发作患者的群体药代动力学分析包括576例高加索人,14例黑人,97例非-中国亚裔,和62例中国人接受FYCOMPA,未发现种族对perampanel表观清除率明显影响。无需剂量调整。 药物相互作用研究 体外药物相互作用的评估 药物代谢酶 在人肝微粒体中,perampanel浓度30 μmol/L,大约在12 mg剂量稳态Cmax的10倍,对CYP2C8,CYP3A4,UGT1A9和UGT2B7有弱抑制作用。Perampanel在浓度30 μmol/L不抑制CYP1A2,CYP2A6,CYP2C9,CYP2C19,CYP2D6,CYP2E1,UGT1A1,UGT1A4和UGT1A6。 在培养人肝细胞中,与阳性对照比较(包括苯巴比妥和利福平),发现perampanel弱诱导CYP2B6(30μmol/L)和CYP3A4/5(≥ 3μmol/L)。Perampanel还诱导UGT1A1(≥ 3μmol/L)和UGT1A4 (30μmol/L)。在浓度直至30 μmol/L时Perampanel不诱导CYP1A2。 转运蛋白 体外研究显示perampanel不是以下的底物或显著抑制剂:有机阴离子转运多肽1B1和1B3;有机阴离子转运蛋白1,2,3,和4:有机阳离子转运蛋白1,2,和3;流出转运蛋白P-糖蛋白和乳腺癌耐药蛋白。 体外药物相互作用的评估 与抗癫痫药物药物相互作用 同时抗癫痫药物对FYCOMPA的影响: 卡马西平 . 作为一种CYP酶诱导剂,卡马西平增加perampanel清除率。给予卡马西平在300 mg BID健康受试者稳态时分别减低单次2 mg剂量perampanel的Cmax和AUC0-inf为26%和67%。Perampanel的t1/2从56.8小时被缩短至25小时。在临床研 究检查部分性癫痫发作,一项群体药代动力学分析显示用卡马西平患者perampanel的AUC与不用酶-诱导抗癫痫药物患者AUC比较被减低67%[见 剂量和给药方法(2.1),药物相互作用(7.2)]。 奥卡西平 . 在临床研究检查部分性癫痫发作,一项群体药代动力学分析显示用奥卡西平患者与不用酶-诱导抗癫痫药物患者比较perampanel的AUC减低一半[见剂量和给药方法(2.1),药物相互作用(7.2)]。 苯妥英 . 在临床研究检查部分性癫痫发作,一项群体药代动力学分析显示用苯妥英患者与不用酶-诱导抗癫痫药物患者比较perampanel AUC减低一半[见剂量和给药方法(2.1),药物相互作用(7.2)]。 苯巴比妥和普里米酮 :在一项有部分性发作癫痫患者群体药代动力学分析,在临床试验(37例患者与苯巴比妥共同给药和9例患者与普里米酮共同给药)未发现对perampanel AUC显著影响。不能除外苯巴比妥和普里米酮对perampanel 浓度轻微影响。 托吡酯[Topiramate] :在有部分性癫痫发作临床试验患者的群体药代动力学分析显示用托吡酯患者与不用酶-诱导抗癫痫药物患者比较perampanel AUC减低约20%。 其他抗癫痫药物 :在临床试验有部分性癫痫发作患 者的群体药代动力学分析显示氯巴占[clobazam],氯硝西泮[clonazepam],拉莫三嗪[lamotrigine],左乙拉西坦 [levetiracetam],丙戊酸钠[valproate],和唑尼沙胺[zonisamide]对perampanel的清除率没有影响。 其他强CYP3A诱导剂 (如,利福平,圣约翰草)也可能大大增加perampanel的清除率和减低perampanel血浆浓度[见药物相互作用(7.2)]。 FYCOMPA对同时抗癫痫药物的影响: 根据在有部分性癫痫发作患者临床试验的一项群体药代动力学分析,FYCOMPA直至12 mg/day不显著影响氯硝西泮,左乙拉西坦, 苯巴比妥,苯妥英,托吡酯,或唑尼沙胺的清除率。FYCOMPA对卡马西平,氯巴占,拉莫三嗪,和拉莫三嗪的清除率有统计意义的影响,但在最高perampanel剂量评价(12 mg/day)时这些药物清除率中的增加各小于10%。 FYCOMPA共同给药导致奥卡西平清除率减低26%和增加其浓度。未测定奥卡西平的活性代谢物10-单羟基代谢物(MHD)浓度。 与其他药物-药物相互作用研究 其他药物对FYCOMPA的影响 酮康唑[Ketoconazole] . 健康受试者of 单次1-mg剂量perampanel与酮康唑剂量400 mg每天1次,一种强 CYP3A4抑制剂共同给药共8天延长perampanel t1/2为15%(67.8相比58.4小时)和增加AUC0-inf 为20%。 口服避孕药 .当单次6-mg剂量perampanel被给予健康女性受试者含炔雌醇 30 μg和左炔诺孕酮150 μg口服避孕药21-天疗程后,Perampanel Cmax和AUC0-72h 没有改变。 FYCOMPA对其他药物的影响 咪达唑仑[Midazolam] . 在健康受试者中Perampanel给予6 mg每天1次doses共20天分别减低咪达唑仑(一种 CYP3A4底物)的AUC0-inf和Cmax为13%和15%。 口服避孕药 . 在健康女性受试者中Perampanel 4 mg每天1次与一种含炔雌醇 30 μg和左炔诺孕酮150 μg口服避孕药共同给药共21天不改变或炔雌醇或左炔诺孕酮的Cmax或AUC0-24h。在另一研究中,在健康女性中FYCOMPA 12 mg或8 mg每天1次给药后21-天给予单剂量口服避孕药。FYCOMPA在12 mg不改变炔雌醇的AUC0-24h但减低其Cmax为18%,和也减低左炔诺孕酮的Cmax和AUC0-24h分别为42%和40%。FYCOMPA 在8 mg对或炔雌醇或左炔诺孕酮的Cmax或AUC0-24h没有显著影响,对左炔诺孕酮AUC0-24h有小(9%)减低[见药物相互作用(7.1)]。 左旋多巴Levodopa . 健康受试者给予Perampanel 4 mg每天1次剂量共19天对左旋多巴的Cmax和AUC0-inf 无影响。 FYCOMPA (perampanel) tablets for oral use Initial U.S. Approval: 2012    Indications and Usage FYCOMPA, a non-competitive AMPA glutamate receptor antagonist for epilepsy in patients over age 12 years old and was used as adjuvant therapy with or without secondary generalized partial seizures in epilepsy treatment ( 1 ) Dosage and Administration ● In the right enzyme - inducing antiepileptic drugs in patients , a starting dose of 2 mg 1 times and bedtime enzyme daily - inducing antiepileptic drugs in patients with 4 mg (2.1) ● based on clinical response and tolerability by 2 mg daily at bedtime biggest weekly increments can be increased to 4 mg bedtime dose to 12 mg 1 time per day. Dose increases should not occur frequently higher than weekly intervals. ( 2.1 ) ● The maximum daily recommended dose is 12 mg 1 time a day at bedtime . ( 2.1 ) ● Elderly patients : The dose was increased every two weeks, the number of the highest frequency . ● Patients with mild and moderate hepatic impairment : For patients with mild and moderate hepatic impairment , respectively, the maximum recommended daily dose of 6 mg at bedtime and 4 mg 1 per day, the highest frequency to increase the number of doses every two weeks . ( 2.2 ) ● Patients with severe hepatic impairment : No recommendation. ( 2.2 ) ● severe renal impairment or in patients undergoing hemodialysis : no recommendations. ( 2.3 ) Formulations and specifications Sheet : 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, and 12 mg. ( 3 ) Contraindications None. ( 4 ) Warnings and Precautions ● suicidal behavior and ideation : Monitor suicidal thoughts or behavior ( 5.2 ) ● affect the nervous system : monitoring dizziness, ataxia, drowsiness , and fatigue ( 5.3 ) When driving or operating machinery patients should be cautious ( 5.3 ) ● fall off : Monitoring of falls and injuries ( 5.4 ) ● revocation of antiepileptic drugs : In patients with epilepsy , it is possible to increase the frequency of seizures (5.5 ) Adverse reactions The most common adverse reactions ( ≥ 4% higher in the placebo and ≥ 1%) include dizziness , drowsiness , fatigue, irritability , fall off , nausea , weight gain, dizziness , ataxia, unsteady gait and balance disorders . ( 6.1 ) Drug Interactions ● contraceptives : 12 mg daily dose may reduce the effectiveness of hormonal contraceptives containing levonorgestrel . ( 7.1 ) ● cytochrome P450 inducers : carbamazepine [Carbamazepine], oxcarbazepine [oxcarbazepine] and phenytoin [phenytoin] increase perampanel clearance and reduce perampanel plasma concentrations and reduce the effectiveness of FYCOMPA . No description for this full dose adjustments can be completely corrected. Phenobarbital [Phenobarbital] and primidone [primidone] may also reduce perampanel concentrations. When these enzyme - inducing antiepileptic drugs are introduced or withdrawn , the patient should be closely monitored . FYCOMPA may need to adjust the dose . ( 7.2 ) ● In addition to the strong CYP3A inducers of antiepileptic drugs : should be avoided ( eg , rifampicin [rifampin], St. John's wort [St John's wort.]). ( 7.2 ) To report suspected adverse reactions, contact Eisai telephone 1-888-274-2378 or contact FDA at 1-800-FDA-1088 or www.fda.gov / medwatch. Use in Specific Populations Pregnancy: Based on animal data , may cause fetal harm. ( 8.1 ) Full prescribing information The second part 12.3 Pharmacokinetics drug Healthy subjects and patients with partial seizures Perampanel pharmacokinetics similar. Perampanel half-life of about 105 hours to reach steady state in about 2-3 weeks . After a single dose of 0.2-12 mg once a day for several Perampanel and give 1-12 mg, AUC dose - increase proportional manner . Absorb Perampanel after oral administration is rapid and complete absorption and negligible first-pass metabolism. Under fasting conditions median Tmax ranging from 0.5 to 2.5 hours . Food does not affect the extent (AUC) uptake , but at a slower rate of absorption . Under fed conditions , perampanel the Cmax and fasting conditions are 28-40 % and to reduce the delay Tmax of 2-3 hours . Distributed Data from in vitro studies showed that the concentration range of 20 to 2000 ng / mL, perampanel approximately 95-96 % bound to plasma proteins, mainly bound to albumin and α1- acid glycoprotein . Perampanel blood and plasma ratio was 0.55-0.59 . Metabolize Perampanel is extensively metabolized by the primary oxidation and sequential glucuronidation . According to the results of in vitro studies using recombinant human CYPs and oxidative metabolism in human liver microsomes by CYP3A4 and / or CYP3A5 -mediated . It may also involve other CYP enzymes. After administration of radiolabeled perampanel, no change in systemic circulation perampanel 74-80 % of the total radioactivity , and only trace amounts of the detected individual perampanel metabolites in plasma. Eliminate After giving radiolabeled perampanel 8 healthy elderly subjects , 22% of recovered radioactivity in the urine and the feces give 48%. The urine and feces , the recovered radioactivity oxide and combinations mixtures mainly composed of metabolites . From 19 reported in a population pharmacokinetic study combined data of kinetic analysis perampanel t1 / 2 with an average of 105 hours . Perampanel healthy subjects and patients with apparent clearance rate of approximately 12 mL / min. Special Populations Liver damage In 12 cases with mild and moderate hepatic impairment ( Child-Pugh A , respectively, and B) subjects and 12 cases of demographic indicators matched healthy comparison subjects , after a single 1 mg dose pharmacokinetic evaluation Perampanel school . Its healthy comparison subjects with mild hepatic impairment overall ( free and protein-bound ) perampanel exposure (AUC0-inf) is larger by 50% and in subjects with moderate hepatic impairment than twice ( 2.55 - X) . With mild and moderate hepatic impairment subjects free perampanel the AUC0-inf matched healthy controls were 1.8 - fold and 3.3 - fold. Mildly impaired subjects T1 / 2 to extend ( 306 compared to 125 hours ) and moderately impaired ( 295 compared to 139 hours ) . Perampanel not been studied in subjects with severe hepatic impairment [ see Dosage and Administration ( 2.2 ) , Use in Specific Populations ( 8.6 ) ] . Kidney damage Specializing in the evaluation of renal damage Perampanel pharmacokinetics has not been conducted in patients . Used from the placebo - controlled clinical trials have partial seizures and acceptance FYCOMPA until 12 mg / day patients were consolidated data population pharmacokinetic analysis . The results showed that in patients with mild renal impairment ( creatinine clearance 50-80 mL / min) and in patients with normal renal function ( creatinine clearance > 80 mL / min) Compare perampanel apparent clearance reduce by 27% , with a corresponding AUC an increase of 37 %. Taking into account the normal and mildly impaired patients with significant overlap between the exposure of patients with mild renal impairment without dose adjustment . Yet in patients with severe renal impairment and in patients undergoing hemodialysis performed Perampanel study [ see Dosage and Administration ( 2.3 ) , Use in Specific Populations ( 8.7 ) ] . Sex In the placebo - controlled clinical trials have accepted FYCOMPA partial seizures in patients with population pharmacokinetic analysis in women perampanel apparent clearance (0.605 L / hr) was lower than men (0.730 L / hr) 17% . No need to adjust the dose based on gender . Pediatric patients Yet at < 12 years of age in children study FYCOMPA, have partial seizures in patients ranging in age from 12-74 years of age to receive FYCOMPA placebo-controlled trial in a population pharmacokinetic analysis in adolescents (0.787 L / hr ) in perampanel apparent clearance was slightly , but not significantly , higher in adulthood. Pediatric patients above 12 years of age may be similar to the adult dose . Old people In placebo - controlled trials , patients have a population pharmacokinetic analysis of partial seizures ranging in age from 12-74 years old are not accepted FYCOMPA obvious effect of age on perampanel apparent clearance [see Dosage and Administration ( 2.1 found ) , use in Specific Populations ( 8.5 ) ] . Race In placebo-controlled trials, patients with partial seizures population pharmacokinetic analysis included 576 cases of Caucasians , 14 blacks, 97 cases of non - Chinese Asians , and 62 cases of Chinese people to accept FYCOMPA, race was not found on perampanel apparent clearance rate was significantly affected. Without dose adjustment . Drug interaction studies In vitro assessment of drug interactions Drug metabolizing enzymes In human liver microsomes , perampanel concentrations of 30 μmol / L, about 12 mg dose of 10 times the steady state Cmax of CYP2C8, CYP3A4, UGT1A9 and UGT2B7 weak inhibition. Perampanel at concentrations 30 μmol / L did not inhibit CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, UGT1A1, UGT1A4 and UGT1A6. In cultured human hepatocytes , compared with the positive control ( including phenobarbital and rifampin ) , found perampanel weak induction CYP2B6 (30μmol / L) , and CYP3A4 / 5 (≥ 3μmol / L). Perampanel also induces UGT1A1 (≥ 3μmol / L) and the UGT1A4 (30μmol / L). Until the concentration of 30 μmol / L when Perampanel not induce CYP1A2. Transporters In vitro studies show that perampanel is not a substrate or less significant inhibitor : organic anion transporting polypeptide 1B1 and 1B3; organic anion transporter 2, 3 , and 4: organic cation transporter 1, 2 and 3 ; efflux transporter P - glycoprotein and breast cancer resistance protein . In vitro assessment of drug interactions Drug interactions with antiepileptic drugs Meanwhile antiepileptic drugs on FYCOMPA of : Carbamazepine . CYP enzyme as an inducer, carbamazepine increase perampanel clearance . When given carbamazepine 300 mg BID , respectively, to reduce the steady state in healthy subjects a single 2 mg dose of perampanel Cmax and AUC0-inf was 26 % and 67 %. Perampanel the t1 / 2 was shortened from 56.8 hours to 25 hours . In clinical studies, examination of partial seizures, a population pharmacokinetic analysis of patients perampanel display AUC of carbamazepine with no enzyme - inducing antiepileptic drugs in patients with AUC comparison is reduced 67% [ see Dosage and Administration ( 2.1 ) , Drug Interactions ( 7.2 ) ] . . Oxcarbazepine in the clinical study examined partial seizures , a population pharmacokinetic analysis of patients with oxcarbazepine display without enzyme - inducing antiepileptic drugs compared to patients perampanel the AUC was reduced by half [ see Dosage and Administration ( 2.1 ) , Drug Interactions ( 7.2 ) ] . . Phenytoin clinical study examined partial seizures , a population pharmacokinetic analysis display phenytoin patients with no enzyme - inducing antiepileptic drugs compared to patients perampanel AUC was reduced by half [ see Dosage and Administration ( 2.1 ) , drug interactions action ( 7.2 ) ] . Phenobarbital and primidone : there is a partial seizures in patients with epilepsy population pharmacokinetic analysis in clinical trials ( 37 patients with co-administration of phenobarbital and primidone 9 patients with co-administration ) found no significant effect on perampanel AUC . Not except phenobarbital and primidone minor impact on perampanel concentrations. Topiramate [Topiramate]: There are partial seizures in patients with a clinical trial population pharmacokinetic analysis showed that the use of topiramate in patients with no enzyme - inducing antiepileptic drugs compared to patients perampanel AUC by about 20%. Other antiepileptic drugs : In clinical trials of partial seizures in patients with kinetic analysis showed population pharmacokinetics clobazam [clobazam], clonazepam [clonazepam], lamotrigine [lamotrigine], levetiracetam [levetiracetam], valproate [valproate], and zonisamide [zonisamide] has no effect on perampanel clearance . Other strong CYP3A inducers ( eg , rifampin, St. John's wort ) may also greatly increase perampanel clearance and reduce perampanel plasma concentrations [ see Drug Interactions ( 7.2 ) ] . FYCOMPA impact while antiepileptic drugs : According to seizures in some patients in clinical trials of a population pharmacokinetic analysis , FYCOMPA up to 12 mg / day did not significantly affect clonazepam , levetiracetam , phenobarbital , phenytoin , topiramate , or clearance of zonisamide . FYCOMPA have a statistically significant impact on carbamazepine, clobazam , lamotrigine , and lamotrigine clearance rate , but at the highest perampanel dose evaluated (12 mg / day) when these drugs increase the clearance rate of each less than 10% . FYCOMPA co-administration resulted in clearance of oxcarbazepine reduce by 26% and increase its concentration. Not determined active metabolite of oxcarbazepine 10 - monohydroxy metabolite (MHD) concentrations. With other drugs - drug interaction studies Influence of other drugs on FYCOMPA Ketoconazole [Ketoconazole]. Healthy volunteers of a single 1-mg dose of perampanel with ketoconazole 400 mg 1 dose per day, co-administration of a potent CYP3A4 inhibitor, a total of eight days lengthen perampanel t1 / 2 was 15% ( 67.8 compared to 58.4 hours ) and increased AUC0-inf was 20% . Oral contraceptives when single 6-mg dose of perampanel was given a healthy female subjects containing 30 μg ethinyl estradiol and levonorgestrel 150 μg oral contraceptives 21 - After days of treatment , Perampanel Cmax and AUC0-72h did not change . The impact of other drugs FYCOMPA Midazolam [Midazolam]. Perampanel in healthy subjects given 6 mg daily doses of 20 days , respectively, to reduce midazolam (a kind of CYP3A4 substrate) AUC0-inf and Cmax of 13% and 15% . Oral contraceptives. Do not change or ethinyl estradiol , or in healthy female subjects Perampanel 4 mg 1 time a day with one containing 30 μg ethinyl estradiol and levonorgestrel 150 μg co-administration of oral contraceptives for 21 days levonorgestrel Cmax or AUC0-24h. In another study , FYCOMPA 12 mg or 8 mg daily after one dose in healthy women 21 - day administration of a single dose of oral contraceptives. FYCOMPA not change in 12 mg ethinyl estradiol AUC0-24h but reduce its Cmax was 18% , and also reduce the levonorgestrel Cmax and AUC0-24h , respectively, 42% and 40%. FYCOMPA at 8 mg significantly affect the Cmax or AUC0-24h or ethinyl estradiol or levonorgestrel no right, levonorgestrel AUC0-24h for a small ( 9% ) reduction [ see Drug Interactions ( 7.1 ) ] . Levodopa Levodopa. Perampanel 4 mg in healthy subjects given a daily dose of 19 days had no effect on levodopa Cmax and AUC0-inf.
更新日期: 2019-1-24
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