药品详细
Carmustine(卡莫司汀)
化学结构式图
中文名
卡莫司汀
英文名
Carmustine
分子式
C5H9Cl2N3O2
化学名
1,3-bis(2-chloroethyl)-1-nitrosourea
分子量
Average: 214.05
Monoisotopic: 213.007181961
Monoisotopic: 213.007181961
CAS号
154-93-8
ATC分类
L01A 烷化剂
药物类型
small molecule
阶段
approved
商品名
Becenun;Bi CNU;BiCNU;Carmubris;Gliadel;Gliadel Wafer;Nitrumon;
同义名
BCNU;Bischlorethylnitrosourea;Bischlorethylnitrosurea;Carmustin;
基本介绍
A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed)
生产厂家
- Bristol laboratories inc div bristol myers co
- Eisai inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
Cancer 癌症;
药理
| Indication | For the treatment of brain tumors, multiple myeloma, Hodgkin's disease and Non-Hodgkin's lymphomas. |
| Pharmacodynamics | Carmustine is one of the nitrosoureas indicated as palliative therapy as a single agent or in established combination therapy with other approved chemotherapeutic agents in treatment of brain tumors, multiple myeloma, Hodgkin's disease, and non-Hodgkin's lymphomas. Although it is generally agreed that carmustine alkylates DNA and RNA, it is not cross resistant with other alkylators. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins. |
| Mechanism of action | Carmustine causes cross-links in DNA and RNA, leading to the inhibition of DNA synthesis, RNA production and RNA translation (protein synthesis). Carmustine also binds to and modifies (carbamoylates) glutathione reductase. This leads to cell death. |
| Absorption | 5 to 28% bioavailability |
| Volume of distribution | Not Available |
| Protein binding | 80% |
| Metabolism |
Hepatic and rapid with active metabolites. Metabolites may persist in the plasma for several days.
|
| Route of elimination | Approximately 60% to 70% of a total dose is excreted in the urine in 96 hours and about 10% as respiratory CO2. |
| Half life | 15-30 minutes |
| Clearance | Not Available |
| Toxicity | The oral LD50s in rat and mouse are 20 mg/kg and 45 mg/kg, respectively. Side effects include leukopenia, thrombocytopenia, nausea. Toxic effects include pulmonary fibrosis (20-0%) and bone marrow toxicity. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Bendamustine | Increases toxicity through pharmacodynamic synergism. Additive myelosuppression. |
| Cimetidine | Increases myelosuppression caused by carmustine |
| Digoxin | The antineoplasic agent decreases the effect of digoxin |
| Fosphenytoin | The antineoplasic agent decreases the effect of hydantoin |
| Leflunomide | Immunosuppressants such as carmustine may enhance the adverse/toxic effect of leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Consider eliminating the use of a leflunomide loading dose in patients who are receiving other immunosuppressants in order to reduce the risk for serious adverse events such as hematologic toxicity. Also, patients receiving both leflunomide and another immunosuppressive medication should be monitored for bone marrow suppression at least monthly throughout the duration of concurrent therapy. |
| Natalizumab | Immunosuppressants such as carmustine may enhance the adverse/toxic effect of natalizumab. Specifically, the risk of concurrent infection may be increased. Patients receiving natalizumab should not use concurrent immunosuppressants. |
| Phenytoin | The antineoplasic agent decreases the effect of hydantoin |
| Pimecrolimus | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants such as carmustine. Avoid use of pimecrolimus cream in patients receiving immunosuppressants. |
| Roflumilast | Roflumilast may enhance the immunosuppressive effect of immunosuppressants such as carmustine. The Canadian roflumilast product monograph recommends avoiding concurrent use of roflumilast with any immunosuppressant medications due to the antiinflammatory/immune altering effects of roflumilast and the lack of relevant clinical experience with such use. Of note, this recommendation to avoid concurrent use does not apply to either inhaled corticosteroids (which have much more limited systemic immune-suppressing actions) or short-term systemic corticosteroid use. U.S. prescribing information does not contain this warning; but it appears prudent to avoid this combination when possible. |
| Tacrolimus | Tacrolimus (Topical) may enhance the adverse/toxic effect of immunosuppressants such as carmustine. Avoid use of tacrolimus ointment in patients receiving immunosuppressants. |
| Trastuzumab | Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events. |
食物相互作用
- Echinacea
收藏