简介:
部份中文环磷酰胺处方资料(仅供参考)
商品名:ENDOXAN
英文名:Cyclophosphamide
中文名:环磷酰胺
藥理類別:抗癌藥物
孕婦用藥分級
D 級:
在對照的人體研究試驗中顯示該藥物對胚胎有不良影響,若此藥能帶來之效益遠超過其它藥物的使用,因此即使在其危險性的存在下,仍可接受此藥物用於懷孕婦女上。
結構式
Image:Cyclophosphamide structure.svg
N,N-bis(2-chloroethyl)-1,3,2-oxazaphosphinan-2-amine 2-oxide
UpToDate UpToDate 連結
藥理作用
Cyclophosphamide是由oxazaphosphamide基團衍生而出的細胞抑制劑,結構上和芥子氣相關。體外不活化,須經由肝臟內的微粒體酵素活化成4-hydroxycyclophosphamide,和aldophosphamide為立體異構物。其細胞毒性作用為烴基性代謝物和DNA起交互作用而來,使DNA雙股產生錯誤的交叉連結及蛋白質結構改變。細胞循環中,經由G2期的通道是退化的,細胞毒性作用對於細胞週期階段不具特異性,但對細胞週期則有。和其他烴基化物一樣,尤其是構造相關的細胞抑制劑,如Ifosfamide,交叉抗藥性不能被排除。
適應症
Hodgkin病,非Hodgkin淋巴瘤(Non-Hodgkin's lymphomas)濾泡淋巴瘤(Follicular lymphomas)網狀細胞肉瘤(reticulum cell carcoma)淋巴母細胞的淋巴肉瘤,Burkitt's淋巴瘤(首選用藥),多發性骨髓瘤白血病(Leukemias)。慢性淋巴性白血病(Chronic lmphocytic leukemia)慢性顆粒性白血病(Chronic leukemia)急性骨髓性和單核細胞白血病(Acute myelogenous and monocytic leukemia)。急性淋巴母細胞白血病(acute lymphoblastic leukemia)蕈狀肉芽腫(Mycosis fungoides)神經母細胞瘤(Neuroblastoma)卵巢腺癌(Adenocarcinoma of Ovary)網膜母細胞瘤(Retinoblastoma)(首選用藥),乳或肺癌(首選用藥)。
防治癌症
用法用量
口服:成人─1天1~5mg/kg;孩童─成人:2~8mg/kg或60~250mg/㎡,共6天或6天以上。維持量:2~5mg/kg,或50~150mg/㎡每週2次。
藥動力學
Absorption
Well absorbed orally. T max is 2 to 3 h for metabolites (IV dose).
Distribution
More than 75% bioavailable after oral administration. More than 60% of metabolites are bound to plasma proteins. Low protein binding for cyclophosphamide.
Metabolism
Converted to active alkylating metabolites in the liver.
Elimination
The t ½ is 3 to 12 h (unchanged drug). Eliminated primarily as metabolites. 5% to 25% is excreted in urine as unchanged drug.
Special Populations
Renal Function Impairment
Metabolites may be elevated but increased toxicity has not been seen.
副作用
接受Endoxan治療的病人,副作用的產生依劑量而定,在大多數的案例中市可逆的。最常見的副作用是噁心、嘔吐。
交互作用
Anticoagulants
Increased hypoprothrombinemic effect may occur.
Barbiturates, other enzyme inducers
May increase the rate of active cyclophosphamide metabolite formation and possibly increase neutropenic effects.
Chloramphenicol, other enzyme inhibitors
May inhibit cyclophosphamide's antineoplastic activity by decreasing rate of active metabolite formation.
Digoxin
May cause decreased serum levels of digoxin.
Oral quinolone antibiotics
May cause decreased GI absorption of quinolone antibiotics.
Succinylcholine and possibly mivacurium
Prolongation of neuromuscular blockade by cyclophosphamide's inhibition of pseudocholinesterase may occur.
禁忌
1.對cylcophosphamide過敏者。
2.骨髓功能嚴重受損者(尤其是曾以cytotoxic agent治療或接受放射性治療的病人)
3.膀胱炎。
4.尿道阻塞。
5.感染症(active infection)。
6.懷孕及授乳期。
注意事項
有下列情況之病人應用Endoxan時應注意:
1.白血球、血小板減少症。
2.骨髓之腫瘤細胞浸潤。
3.以前用X光治療過。
4.以前用其他的Cytatoxic agent治療過。
5.肝功能損害。
因為Endoxan有抑制免疫機轉之作用,病人如引起細菌、黴菌或病毒之感染應停藥或更改劑量,尤其是與類固醇藥物合併治療,有時會使病人死亡。在這些情況下,水痘-帶狀泡疹之感染尤其危險。
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,不可再食用。
Endoxan Tablets Details:
Brand Name: Endoxan
Contents: Cyclophosphamide
Form: Tablet
Strength: 50mg
Manufacturer: Zydus Biogen ( Baxter)
ENDOXAN 50MG TABLETS
Endoxan 50mg is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug. This medication is classified as an “alkylating agent.”
USES
Cyclophosphamide is used for treating certain types of the following cancers: lymphoma, multiple myeloma, leukemia, mycosis fungoides, neuroblastoma, ovarian cancer, eye cancer, and breast cancer. It is usually used in combination with other medicines. It may also be used to treat certain kidney problems (nephrotic syndrome) in children or for other conditions as determined by your doctor.
SIDE EFFECTS
Appetite loss; absence of menstrual periods; color change in skin; diarrhea; general unwell feeling; hair loss; nausea; skin rash; stomach discomfort or pain; texture change in nails; vomiting; weakness.
Seek medical attention right away if any of these SEVERE side effects occur:
Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blood in urine; bloody or black tarry stools; chest pain; chills; fever; hallucinations; increased or decreased urination; infection; lower back or abdominal pain; pain, swelling, or redness at the injection site; painful urination; persistent cough; pneumonia; red, swollen, or blistered skin; seizures; severe stomach pain; shortness of breath; sore throat; sores in the mouth; swelling of the hands or feet; unusual bruising or bleeding; unusual or severe tiredness or weakness; yellowing of the skin or eyes.
This is not a complete list of side effects and others may occur. |