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METHOTREXATE PF(甲氨喋呤注射剂)

2014-03-25 12:28:29  作者:新特药房  来源:互联网  浏览次数:151  文字大小:【】【】【
简介: 部分中文甲氨喋呤信息资料(仅供参考)【适应症】 1、各型急性白血病,特别是急性淋巴细胞白血病、恶性淋巴瘤、非何杰金氏淋巴瘤和蕈样肉芽肿、多发性骨髓病; 2、头颈部癌、肺癌、各种软组织肉瘤、银屑病 ...
部分中文甲氨喋呤信息资料(仅供参考)
【适应症】
1、各型急性白血病,特别是急性淋巴细胞白血病、恶性淋巴瘤、非何杰金氏淋巴瘤和蕈样肉芽肿、多发性骨髓病;
2、头颈部癌、肺癌、各种软组织肉瘤、银屑病;
3、乳腺癌、卵巢癌、宫颈癌、恶性葡萄胎、绒毛膜上皮癌、睾丸癌。
藥理作用 
methotrexate為一種葉酸拮抗劑,主要是抑制DNA合成也會直接作用於RNA,蛋白質合成。methotrexate對細胞分裂中之s期有專一性的抑制作用,所以對快速增殖的癌細胞有相當大的毒性。
用法用量 
1. 肌注,靜注:1週1次10~25mg至最大量,1週50mg。
2. 大劑量的methotrexate─靜脈滴注:100mg/㎡~10g/㎡, 6~24小時以下,每1~3週1次,接著用Calcium leucovorin。
藥動力學 
Absorption
Oral absorption is dose dependent. T max is 1 to 2 h (oral) and 30 to 60 min (IM). The mean bioavailability is 60%. Absorption of doses more than 80 mg/m 2 is significantly less, possibly because of a saturation effect. Food delays absorption and reduces peak concentration.
Distribution
Initial Vd is 0.18 L/kg (18% of body weight); steady state Vd is approximately 0.4 to 0.8 L/kg (40% to 80% of body weight). Approximately 50% is protein bound. Methotrexate does not penetrate the blood-cerebrospinal fluid barrier in therapeutic amounts when given orally or parenterally, but it has been detected in breast milk.
Metabolism
Methotrexate undergoes hepatic and intracellular metabolism to active polyglutamated forms and is partially metabolized by intestinal flora after oral administration. Major metabolite is 7-hydroxymethotrexate.
Elimination
Renal excretion is the primary route of elimination and is dependent upon dosage and route of administration. With IV administration, 80% to 90% is excreted unchanged in urine within 24 h and less than 10% through biliary excretion. The t½ for doses less than 30 mg/m 2 is approximately 3 to 10 h; 8 to 15 h for high doses.
Special Populations
Renal Function Impairment
An increase in serum levels occurs because of decreased elimination in patients with renal function impairment.
副作用 
1.常見-潰瘍性口腔炎、舌炎、齒齦炎、頭痛、白血球減少、血小板減少。
2.嚴重者-肝毒性、肝硬化、骨髓抑制、肺炎、猝死。
交互作用 
Acitretin, etretinate, NSAIDs, penicillins, probenecid, salicylates, sulfonamides, tetracyclines
May increase methotrexate blood levels and toxicity.
Antibiotics (oral) such as chloramphenicol, nonabsorbable broad spectrum antibiotics (eg, neomycin), and tetracycline
May decrease intestinal absorption of methotrexate or interfere with enterohepatic circulation.
Charcoal
May reduce methotrexate efficacy.
Digoxin
May reduce serum digoxin levels and actions.
Folic acid
May decrease responses to systemically administered methotrexate.
Hydantoins
May reduce plasma levels.
Mercaptopurine
Plasma concentrations may be increased by methotrexate.
Theophylline
Methotrexate decreases Cl of theophylline.
Trimethoprim
May increase risk of methotrexate-induced bone marrow suppression and megaloblastic anemia.
禁忌 
凡孕婦,營養不良,嚴重肝腎不良,骨隨成形不全,白血球減少,及貧血之乾癬患者,禁用本劑。
注意事項 
1. 當投與Cytarabine或methotreate後,注意病人是否發生心跳過快、低血壓、和呼吸短促;還會發生類無防禦性過反應(anaphylactoid reactions),此需要支持療法。
2. Calcium leucovorin為methotrexate過量的解毒劑,在投與大劑量methotrexate後12小時內,IV灌注75mg calcium leucovoorin,然後每6小時IM 12mg,連續4次投與較小劑量methotrexate後,可每6小時IM 12小時,連續4次。一般而言,Calcium leucovorin劑量應該等於或高於methotrexate的劑量,而且要在1小時內投與。
3. 服用本品會降低抗菌力,病人應該避免與傳染病的患者接觸。
4. 本品可能會產生光敏感反應,病人應避免日曬或照射日光燈太久。
藥品保存方式 
藥品應置於攝氏 15 ~ 25 度乾燥處所;如發生變質或過期,不可再使用。
----------------------------------------------
产地国家: 美国
原产地英文商品名:
METHOTREXATE PF(Rheumatrex generic) 250mg/10ml/vial 1 vial
原产地英文药品名:
METHOTREXATE SODIUM
原产地英文化合物名称:
METHOTREXATE SODIUM
中文参考商品译名:
甲氨喋呤(Rheumatrex generic)250毫克/10毫升/瓶
中文参考药品译名:
甲氨喋呤
中文参考化合物名称:
甲氨喋呤
生产厂家中文参考译名:
辉瑞制药
生产厂家英文名:
Pifzer
----------------------------------------------
产地国家: 美国
原产地英文商品名:
METHOTREXATE PF(Rheumatrex generic) 50mg/2ml/vial 10vials
原产地英文药品名:
METHOTREXATE SODIUM
原产地英文化合物名称:
METHOTREXATE SODIUM
中文参考商品译名:
甲氨喋呤(Rheumatrex generic)50毫克/2毫升/瓶 10瓶/盒
中文参考药品译名:
甲氨喋呤
中文参考化合物名称:
甲氨喋呤
生产厂家中文参考译名:
梯瓦
生产厂家英文名:
Teva

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