部份中文甲硝唑处方资料(仅供参考)
【药品名称】
通用名:甲硝唑注射液
英文名:Metronidazole Injection
商標名 ANAEMETRO Intravenous infusion
【成份】本品主要成份为甲硝唑。其化学名称为2-甲基-5-硝基咪唑-1-乙醇,化学结构式:
分子式:C6H9N3O3,分子量:171.16
辅料为氯化钠、注射用水。
【性状】
本品为无色或几乎无色的澄明液体。
【适应症】本品主要用于厌氧菌感染的治疗。
【用法用量】静脉滴注 。
1、成人常用量: 厌氧菌感染,静脉给药首次按体重15mg/kg(70kg成人为1g,即2瓶),维持量按体重7.5mg/kg,每6-8小时静脉滴注一次。
2、小儿常用量: 厌氧菌感染的注射剂量同成人。
【不良反应】
15-30%病例出现不良反应,以消化道反应最为常见,包括恶心、呕吐、食欲不振、腹部绞痛,一般不影响治疗;神经系统症状有头痛、眩晕,偶有感觉异常、肢体麻木、共济失调、多发性神经炎等,大剂量可致抽搐。少数病例发生荨麻疹、潮红、瘙痒、膀胱炎、排尿困难、口中金属味及白细胞减少等,均属可逆性,停药后自行恢复。
【注意事项】
(1)对诊断的干扰:本品的代谢产物可使尿液呈深红
(2)原有肝脏疾病患者,剂量应减少。出现运动失调或其他中枢神经系统症状时应停药。重复一个疗程之前,应做白细胞计数。厌氧菌感染合并肾功能衰竭者,给药间隔时间应由8小时延长至12小时。
(3)本品可抑制酒精代谢,用药期间应戒酒,饮酒后可能出现腹痛、呕吐、头痛等症状。
(4)若遇药液混浊、异物、瓶身破裂、轧口松动等,请勿使用。一次使用不完,禁止再用。
【孕妇及哺乳期妇女用药】
孕妇及哺乳期妇女禁用。
【儿童用药】
尚不明确。
【老年用药】
由于老年人肝功能减退,应用本品时药动学有所改变,应严密监测本品血药浓度。
【药物相互作用】
(1)本品能抑制华法林和其他口服抗凝药的代谢,加强它们的作用,引起凝血酶原时间延长。
(2)同时应用苯妥英钠、苯巴比妥等诱导肝微粒体酶的药物,可加强本品代谢,使血药浓度下降,而苯妥英钠排泄减慢。
(3)同时应用西咪替丁等抑制肝微粒体酶活性的药物,可减缓本品在肝内的代谢及其排泄,延长本品的血清半衰期,应根据血药浓度测定的结果调整剂量。
(4)本品干扰双硫仑代谢,两者合用患者饮酒后可出现精神症状,故2周内应用双硫仑者不宜再用本品。
(5)本品可干扰氨基转移酶和LDH测定结果,可使胆固醇、甘油三酯水平下降。
【药物过量】
大剂量可致抽搐。
【药理毒理】
甲硝唑对大多数厌氧菌具有强大的抗菌作用,但对需氧菌和兼性厌氧菌无作用,抗菌谱包括脆弱拟杆菌和其他拟杆菌属,梭形杆菌、产气梭状芽胞杆菌、真杆菌、韦容球菌、消化球菌和消化链球菌等,放线菌属、乳酸杆菌属、丙酸杆菌属对本品耐药。其杀菌浓度稍高于抑菌浓度。本品尚可抑制阿米巴原虫氧化还原反应,使原虫氮链发生断裂。体外试验证明,药物浓度为1-2mg/L时,溶组织阿米巴于6-20小时即可发生形态改变,24小时内全部被杀灭,浓度为0.2mg/L时,72小时内可杀死溶组织阿米巴。本品有强大的杀灭滴虫的作用,其机理未明。对某些动物有致癌作用。
【药代动力学】
静脉给药后迅速达峰值。蛋白结合率<5%,吸收后广泛分布于各组织和体液中,且能通过血脑屏障,药物有效浓度能够出现在唾液、胎盘、胆汁、乳汁、羊水、精液、尿液、脓液和脑脊液中。有报道,药物在胎盘、乳汁、胆汁的浓度与血药浓度相似。健康人脑脊液中血药浓度为同期血药浓度的43%。有效浓度能维持12小时。本品经肾排出60%-80%,约20%的原形药从尿中排出,其余以代谢产物(25%为葡萄糖醛酸结合物,14%为其他代谢结合物)形式由尿排出。10%随粪便排出。14%从皮肤排泄。
【贮藏】
遮光,密闭保存。
Name: Metronidazole Injection
Structural formula: C6H9N3O3
Description the product is colorless or almost colorless pellucid liquid.
Pharmacology and toxicity
Potent Anaerobicidal Nitro -imidazole derivative. The exact mechanism of action of metronidazole is unknown. At physiologic pH, metronidazole is un-ionized and taken up readily by anaerobic organisms. The drug then undergoes intracellular chemical reduction via mechanisms unique to anaerobes. Reduced metronidazole interacts with DNA and inhibits nucleic acid synthesis, leading to cell death. Metronidazole is equally effective against dividing and nondividing cells.
Pharmacokinetics
The peak value is observed 20mins after administering by intravenous drip and binding rate with protein <5%. After absorption Metronidazole distributes widely in all kinds of tissues and body liquids, and pass easily blood brain barrier to the tissues such as saliva, placenta, bile, latex, ammiotic fluid, semen, urine, purulence, cerebrospinal fluid and etc. It is reported that the concentration in placenta, latex, bile is similar with that in plasma.
For the healthy people the concentration of Metronidazole in the cerebrospinal fluid is about 43% of that in the plasma, and the effective concentration can remain 12hours. 60~80% of the preparation is excreted via kidney, about 20% of Metronidazole is excreted unchanged in the urine, the other is excreted in the urine as the products of metabolism (25%- glucuronicacid combo, 14%-other kinds of products of metabolism). 10% of Metronidazole is excreted in the dejection, and 14% is excreted from skin.
Disease treated Metronidazole is mainly used in the treatment of anaerobe bacterial infection.
Administration and dosage By drip phleboclysis.
1. Doses for the adult In the treatment of anaerobic bacteria infections, administer by intravenous drip according to 1g/70kg for the first time, and calculate the does according to 7.5mg/kg during the course of treatment, and interval time is 6~8hours.
2. Doses for the children In the treatment of anaerobic bacteria infection, the doses are similar with that of the adult.
Side-effect 15~30% of the cases were reported side-effect, and adverse reactions frequently associated with Metronidazole include: Digestive tract reaction such as nausea, vomiting, and diarrhea stomach pain or cramps, anorexia; Symptoms of nerve system include headache and swirl; Abnormal sensation, numb limbs and tense tendons, ataxia, and multiple neuritis occasionally happen; Over high dose can cause convulsion. Few cases have the symptoms such as urticaria, moisst, pruritus, cystitis, dysuresia, change in taste sensation and decreased white cell. But the abovementioned symptoms are all reversible and recover after the administration.
Contraindication
Forbid to use the medicine for the patients with the diseases in central nervous system and flood.
Indication for women in pregnant and suckle
Forbid to use this medicine for women in pregnant and suckle.
Substance interactions
Metronidazole may increase the effects of Warfarin anticoagulants.
Overdose High dose may cause convulsion.
完整处方资料附件:http://www.info.pmda.go.jp/go/pack/6419401A1027_1_01/6419401A1027_1_01?view=body
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产地国家:日本
原产地英文商品名:
ANAEMETRO Intravenous infusion(アネメトロ点滴静注液)500mg/vials 5vials
原产地英文药品名:
Metronidazole
中文参考商品译名:
ANAEMETRO注射剂(アネメトロ点滴静注液) 500毫克/瓶 5瓶/盒
中文参考药品译名:
甲硝唑
生产厂家英文名:
Pfizer