药品详细
Cyclophosphamide (环磷酰胺 )
化学结构式图
中文名
环磷酰胺
英文名
Cyclophosphamide
分子式
Not Available
化学名
2-[bis(2-chloroethyl)amino]-1,3,2$l^{5}-oxazaphosphinan-2-one
分子量
Average: 261.086
Monoisotopic: 260.024819660
Monoisotopic: 260.024819660
CAS号
6055-19-2
ATC分类
L01A 烷化剂;L01D 细胞毒素抗生素及相关物质
药物类型
small molecule
阶段
商品名
ASTA;Asta B 518;Clafen;Claphene;CP;CPA;CTX;CY;Cyclophosphamid;Cyclophosphamide Monohydrate;Cyclophosphamide Sterile;Cyclophosphamidum;Cyclophosphan;Cyclophosphane;Cyclophosphoramide;Cyclostin;Cyklofosfamid;Cytophosphan;Cytoxan;Cytoxan Lyoph;Endoxan;Endoxan R;Endoxan-Asta;Endoxana;Endoxanal;Endoxane;Enduxan;Genoxal;Hexadrin;Lyophilized Cytoxan;Mitoxan;Neosar;Procytox;Rcra Waste Number U058;Revimmune;Semdoxan;Sendoxan;Senduxan;Zyklophosphamid;
同义名
cyclophosphamide;
基本介绍
Precursor of an alkylating nitrogen mustard antineoplastic and immunosuppressive agent that must be activated in the liver to form the active aldophosphamide. It has been used in the treatment of lymphoma and leukemia. Its side effect, alopecia, has been used for defleecing sheep. Cyclophosphamide may also cause sterility, birth defects, mutations, and cancer. [PubChem]
生产厂家
- Baxter healthcare corp
- Baxter healthcare corp anesthesia and critical care
- Roxane laboratories inc
- Teva parenteral medicines inc
封装厂家
参考
剂型
Form | Route | Strength |
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Powder, for solution | Intravenous | |
Solution | Intravenous | |
Tablet | Oral |
规格
Unit description | Cost | Unit |
---|---|---|
Cyclophosphamide 500 mg vial | 37.76 USD | vial |
Cyclophosphamide 100% powder | 33.66 USD | g |
Cytoxan 500 mg vial | 15.25 USD | vial |
Cytoxan 50 mg tablet | 4.14 USD | tablet |
Cyclophosphamide 50 mg tablet | 3.92 USD | tablet |
Cytoxan 25 mg tablet | 2.26 USD | tablet |
Cyclophosphamide 25 mg tablet | 2.09 USD | tablet |
化合物类型
Type | small molecule |
Classes |
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Substructures |
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适应症
Cancer 癌症;
药理
Indication | For management of malignant lymphomas, multiple myeloma,leukemias, mycosis fungoides (advanced disease), neuroblastoma (disseminated disease), adenocarcinoma of the ovary, retinoblastoma and carcinoma of the breast | ||||||||||||||||||||||||||||||
Pharmacodynamics | Cyclophosphamide is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death. | ||||||||||||||||||||||||||||||
Mechanism of action | Alkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations. | ||||||||||||||||||||||||||||||
Absorption | 90-100% | ||||||||||||||||||||||||||||||
Volume of distribution | Not Available | ||||||||||||||||||||||||||||||
Protein binding | >60% | ||||||||||||||||||||||||||||||
Metabolism |
hepatic
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Route of elimination | It is eliminated primarily in the form of metabolites, but from 5% to 25% of the dose is excreted in urine as unchanged drug. | ||||||||||||||||||||||||||||||
Half life | 3-12 hours | ||||||||||||||||||||||||||||||
Clearance | Not Available | ||||||||||||||||||||||||||||||
Toxicity | infection, myelosuppression, and cardiac toxicity | ||||||||||||||||||||||||||||||
Affected organisms |
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Pathways |
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理化性质
Properties | |||||||||||||||||||||||||||||||||||||
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State | solid | ||||||||||||||||||||||||||||||||||||
Melting point | 41-45 oC | ||||||||||||||||||||||||||||||||||||
Experimental Properties |
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Predicted Properties |
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药物相互作用
Drug | Interaction |
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Acenocoumarol | The antineoplastic agent, cyclophosphamide may alter the anticoagulant effect of acenocoumarol. |
Anisindione | The antineoplastic agent, cyclophosphamide may alter the anticoagulant effect of anisindione. |
Dicumarol | The antineoplastic agent, cyclophosphamide may alter the anticoagulant effect of dicumarol. |
Digoxin | The antineoplasic agent decreases the effect of digoxin |
Fluconazole | Fluconazole reduces metabolism and clearance of cyclophosphamide. |
Pentostatin | Increased toxicity of cyclophosphamide |
Succinylcholine | Cyclophosphamide may increase the effect of succinylcholine. |
Thiotepa | Thiotepa, a strong CYP2B6 inhibitor, may decrease the metabolism and clearance of Cyclophosphamide, a CYP2B6 substrate. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Cyclophosphamide if Thiotepa is initiated, discontinued or dose changed. |
Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
Warfarin | The antineoplastic agent, cyclophosphamide may alter the anticoagulant effect of warfarin. |
食物相互作用
- Drink liberally- 2 to 3 liters/day.
- Take with food to reduce irritation.