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甲吡唑注射液|FOMEPIZOLE(ANTIZOL GENERIC)

2011-08-28 17:19:32  作者:新特药房  来源:互联网  浏览次数:646  文字大小:【】【】【
简介: ANTIZOL® (fomepizole) Injection 注射劑 注射用甲吡唑(fomepizole)1998年初美国FDA批准了注射用甲吡唑(商品名为Antizol,由Orphan Medical公司生产)上市。甲吡唑(4-methylpyrazole,4-甲基吡唑)是一 ...
ANTIZOL® (fomepizole) Injection 注射劑 
注射用甲吡唑(fomepizole)
1998年初美国FDA批准了注射用甲吡唑(商品名为Antizol,由Orphan Medical公司生产)上市。甲吡唑(4-methylpyrazole,4-甲基吡唑)是一种乙醇脱氢酶抑制剂,可以口服或静注,主要用于乙二醇中毒的解救。

1 药理作用
甲吡唑用于乙二醇中毒的解救主要是通过抑制乙醇脱氢酶来实现的。乙二醇是抗冻剂和冷却剂中的主要成分,在体内乙醇脱氢酶的作用下会产生有毒的乙二醇代谢物(可能是乙二醛)。乙二醇急性中毒的临床表现有:中枢神经系统抑制、严重的代谢性酸中毒、肾功能衰竭和昏迷等。甲吡唑能够抑制乙醇脱氢酶的活性,从而有效地抑制了乙二醇代谢物的产生,最终达到治疗目的。

2 药动学特性
甲吡唑可供静注,蛋白结合率低,表观分布容积为0.8l.kg-1,半衰期为5h。其主要经肝脏代谢,可能与细胞色素P-450系统有关,消除过程与剂量大小有关,为非线性消除,无法用米氏方程来描述。本品主要经肾脏排泄,尿中的原型药物很少,主要是代谢产物4-carboxypyrazole,肾清除率为0.016ml.min-1.kg-1。
乙二醇中毒的早期患者,每12h静注400~1200mg,血药浓度可达到17~31μg.ml-1。中毒晚期进行透析的患者,给予负荷剂量20mg.kg-1,并持续静注(透析的同时)甲吡唑1.5mg.kg-1.h-1其血药浓度将高于14μg.ml-1。有研究表明治疗时的血药浓度应为8~15μg.ml-1或更高。

3 临床应用
3.1 乙二醇中毒 对于肾功能尚可的患者单独应用甲吡唑即有效,与乙醇治疗乙二醇中毒相比较,甲吡唑应用起来更方便、更安全。临床应用表明,及早应用甲吡唑(摄入乙二醇3~16h内),1日2次(静注或口服)即可消除酸中毒而不需进行血液透析。对于伴随肾功能衰竭的患者应用甲吡唑的同时还应进行透析[1,3]。
3.2 乙醇过敏 通过抑制乙醇脱氢酶来减少乙醛的积累达到治疗目的。如果提前1h预防性的口服甲吡唑10mg.kg-1则能阻止过敏症状的出现[4]。
3.3 甲醇中毒 动物实验表明甲吡唑对甲醇中毒有效。

4 用法用量
本品供静脉注射,用生理盐水稀释。中毒早期肾功能良好者,首次静注800或1200mg,然后每12h静注减少用量如600mg,300mg或400mg,100mg或200mg,50mg或100mg,直到血中检测不到乙二醇或其浓度低于0.1g.L-1。肾功能衰竭的患者不必调整剂量。中毒晚期,出现无尿性肾功能衰竭的患者,应进行血液透析。血液透析对甲吡唑有明显的清除作用,故需要提高剂量。一般首次负荷剂量为10~20mg.kg-1,透析期间的组持剂量为1~1.5mg.kg-1vh-1。

5 不良反应及禁忌
最常见的不良反应是转氨酶的升高,其它的有眩晕、头疼、高甘油三酯血症、嗜酸性粒细胞增多、皮疹、恶心(口服时)等。对甲吡唑过敏者禁用。

6 注意事项
据研究表明,甲吡唑可以抑制乙醇脱氢酶,而反过来乙醇有可抑制甲吡唑代谢,因而甲吡唑和乙醇可以相互抑制对方的消除,从而加强各自的作用。故临床上应注意乙醇和甲吡唑之间的这种相互作用。

【原产地英文商品名】FOMEPIZOLE(ANTIZOL GENERIC) 1GM/ML 1.5ML/VIAL
【原产地英文药品名】FOMEPIZOLE
【原产地英文化合物名称】4-methylpyrazole
【中文参考商品译名】甲吡唑(ANTIZOL仿制药) 1克/毫升 1.5毫升/瓶
【中文参考药品译名】甲吡唑
【中文参考化合物名称】4-甲基吡唑

Fomepizole injection

What is fomepizole?

FOMEPIZOLE (Antizol(TM)) is used to treat ethylene glycol or methanol poisoning. Ethylene glycol is found in antifreeze and coolants. Methanol may be found in windshield wiper fluid and many cleaning solutions. Generic fomepizole is not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• kidney disease
• an unusual or allergic reaction to fomepizole, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I receive this medicine?

Fomepizole is for infusion into a vein. It is given by a health-care professional in a hospital or clinic setting.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

This does not apply.

What drug(s) may interact with fomepizole?

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking fomepizole?

Your condition will be closely monitored while you receive fomepizole.

What side effects may I notice from receiving fomepizole?

Side effects that you should report to your prescriber or health care professional as soon as possible:
Rare or Less common:
• decrease in blood pressure
• pain or tenderness over area where the drug was given
• seizures
• skin rash
• slow or fast heartbeat
• uncontrolled back-and-forth and/or rolling eye movements
• severe vomiting

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
More common:
• dizziness
• headache
• nausea

Less common:
• abdominal pain
• blurred vision
• change in sense of smell
• diarrhea
• drowsiness
• feeling of drunkenness
• fever
• heartburn
• hiccups
• lightheadedness
• loss of appetite
• metallic or unpleasant taste
• sensation of spinning
• sore throat

Where can I keep my medicine?

Store at controlled room temperature [20 degrees to 25 degrees C (68 degrees to 77 degrees F)].


Last updated: 7/1/2002

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