ニムスチン
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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2018/03/24 17:53:54」(JST)
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Nimustine
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Clinical data |
AHFS/Drugs.com |
International Drug Names |
Routes of
administration |
Intravenous |
ATC code |
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Legal status |
Legal status |
- In general: ℞ (Prescription only)
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Identifiers |
IUPAC name
- N'-[(4-amino-2-methylpyrimidin-5-yl)methyl]-N-(2-chloroethyl)-N-nitrosourea
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CAS Number |
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PubChem CID |
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ChemSpider |
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UNII |
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KEGG |
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ChEBI |
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ECHA InfoCard |
100.050.744 |
Chemical and physical data |
Formula |
C9H13ClN6O2 |
Molar mass |
272.69 g/mol |
3D model (JSmol) |
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SMILES
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CC1=NC=C(C(=N1)N)CNC(=O)N(CCCl)N=O
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InChI
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InChI=1S/C9H13ClN6O2/c1-6-12-4-7(8(11)14-6)5-13-9(17)16(15-18)3-2-10/h4H,2-3,5H2,1H3,(H,13,17)(H2,11,12,14) N
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Key:VFEDRRNHLBGPNN-UHFFFAOYSA-N N
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NY (what is this?) (verify) |
Nimustine (INN) is a nitrosourea alkylating agent.
References
UpToDate Contents
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English Journal
- Phase II Trial of Radiotherapy After Hyperbaric Oxygenation With Multiagent Chemotherapy (Procarbazine, Nimustine, and Vincristine) for High-Grade Gliomas: Long-Term Results.
- Ogawa K, Ishiuchi S, Inoue O, Yoshii Y, Saito A, Watanabe T, Iraha S, Toita T, Kakinohana Y, Ariga T, Kasuya G, Murayama S.SourceDepartment of Radiology, University of the Ryukyus, Okinawa, Japan.
- International journal of radiation oncology, biology, physics.Int J Radiat Oncol Biol Phys.2012 Feb 1;82(2):732-8. Epub 2011 Mar 21.
- PURPOSE: To analyze the long-term results of a Phase II trial of radiotherapy given immediately after hyperbaric oxygenation (HBO) with multiagent chemotherapy in adults with high-grade gliomas.METHODS AND MATERIALS: Patients with histologically confirmed high-grade gliomas were administered radioth
- PMID 21420247
- Complications of chemotherapy in neuro-oncology.
- Marosi C.AbstractThe persisting reservation against the use of chemotherapy in patients with malignant glioma was finally overcome by the breakthrough achieved with the use of the oral alkylating agent temozolomide (TMZ) as concomitant and adjuvant chemotherapy in patients with newly diagnosed glioblastoma multiforme (GBM). The basic condition for an effective systemic drug therapy against malignant glioma is that the drug be able to cross the blood-brain barrier (BBB) and the brain-tumor barrier. Drugs crossing the BBB have to be nonpolar, small molecules with a molecular weight of less than 500Da, to bear no electrical charge, or to be able to use active transport mechanisms, as the BBB is functional in the peripheral growing areas of GBM. The prerequisite of liposolubility is best achieved by a group of drugs termed alkylating agents; nitrosoureas were the agents used most historically, until the now most widely used drug, TMZ, became available. All alkylating agents share a common molecular mechanism of action, which is by nature cytotoxic, mutagenic, and carcinogenic. They differ greatly in their pharmacokinetic features and liposolubility, and thus also in the pattern of toxicities observed, such as myelosuppression, induction of secondary tumors, impact on fertility in both sexes, and induction of nausea and vomiting. The effectiveness of alkylating chemotherapy in tumors of glial origin depends on the DNA repair capacity of the individual tumor - most precisely on the intracellular presence of the DNA repair enzyme MGMT (O(6)-methylguanine-DNA methyltransferase). The promoter of the gene encoding for MGMT may be silenced by epigenetic methylation; in this case, the tumor responds to alkylating therapy. At the time of writing, it is not clear whether prolonged exposure to alkylating chemotherapy succeeds in depleting MGMT in tumor cells and might thus produce a response in patients whose tumor cells have an unmethylated MGMT promoter sequence. The most prominent clinically relevant side-effect is myelosuppression, most pronounced for white blood cells and platelets, less for red blood cells. ACNU (nimustine), BCNU (carmustine), and CCNU (lomustine) are nitrosourea drugs that have been used for the treatment of brain tumors for more than 40 years. Their most prominent side-effect is delayed myelosuppression, with the nadir occurring 5-6 weeks after drug administration. This long delay to the occurrence of the dose-limiting side-effects of leukocytopenia and thrombocytopenia demands special attention for controls and complicates the use of drug combinations. For TMZ, the risk of severe myelosuppression in the standard dosage is around 7% for thrombocytopenia and for leukocytopenia. With increasing duration of TMZ use, the rate of lymphopenia, selective for CD4 lymphocytes, increases, with up to 47% encountered in the 21/28 schedule. When the CD4 count drops below 200/mm(3) or the total lymphocytes decrease to less than 400/mm(3), there is a significant risk of opportunistic infection, such as Pneumocystis carinii pneumonia, herpes zoster, Kaposi sarcoma, or reactivation of herpes or hepatitis B infection. In analogy to patients with HIV/AIDS, P. carinii prophylaxis with trimethoprim or monthly pentamidine inhalations is strongly recommended during concomitant chemotherapy and/or for patients with lymphocyte counts below 400/mm(3). Other drugs used in neuro-oncology include the platinum compounds cisplatin and carboplatin, which act like alkylating agents and are sometimes used in low doses in combination with alkylating agents, the topoisomerase inhibitors derived from camptothecins, irinotecan and, for brain metastases, topotecan; and the podophyllum toxins etoposide and VM26, pegylated and/or liposomal anthracyclines, and, although it does not penetrate the BBB, the vinca alkaloid vincristine. The toxicity profiles of these drugs are reviewed briefly.
- Handbook of clinical neurology / edited by P.J. Vinken and G.W. Bruyn.Handb Clin Neurol.2012;105:873-85.
- The persisting reservation against the use of chemotherapy in patients with malignant glioma was finally overcome by the breakthrough achieved with the use of the oral alkylating agent temozolomide (TMZ) as concomitant and adjuvant chemotherapy in patients with newly diagnosed glioblastoma multiform
- PMID 22230539
- Effects of Chemotherapeutics on Organotypic Corticostriatal Slice Cultures Identified by A Panel of Fluorescent and Immunohistochemical Markers.
- Nørregaard A, Jensen SS, Kolenda J, Aaberg-Jessen C, Christensen KG, Jensen PH, Schrøder HD, Kristensen BW.SourceDepartment of Pathology, Odense University Hospital, Winsløwparken 15, 5000, Odense C, Denmark.
- Neurotoxicity research.Neurotox Res.2011 Dec 28. [Epub ahead of print]
- Effects of chemotherapeutics on glioma cell lines and spheroids are usually investigated without evaluating the effects of chemotherapeutics on normal brain tissue. To perform such investigations, the aim of this study was to establish a panel of markers for detection of general cell death and more
- PMID 22203610
Japanese Journal
- Therapy-related myelodysplastic syndrome developed by dacarbazine, nimustine hydrochloride and vincristine sulfate (DAV) therapy for patient with malignant melanoma
- NITTA Yukiko,IKEYA Toshihiko,SAKAKIBARA Akihiro,TOMITA Yasushi
- Journal of dermatology 38(2), 164-168, 2011-02-01
- NAID 10029330340
- シングルバルーン小腸内視鏡にて術前に病理診断し得た小腸原発悪性黒色腫の1例
- 川口 真矢,杉本 真也,山本 玲,山村 光弘,大山田 純,黒田 幹人,亀井 昭,佐藤 兵衛,福家 博史,奥田 善大,矢花 正
- 日本消化器病学会雑誌 108(4), 633-639, 2011
- 症例は72歳男性.下腹部痛および貧血にて近医を受診し,精査目的に当院を紹介受診された.腹部造影CTにて骨盤内小腸に腫瘤を指摘された.小腸X線検査にて腫瘤は空腸に指摘され,シングルバルーン小腸内視鏡検査では灰白色調から黒色調の弾性軟の腫瘤を認め,生検にて悪性黒色腫と診断された.全身検索にて他に原発巣を認めず,小腸原発悪性黒色腫と診断し,空腸部分切除術が施行された.リンパ節転移陽性(stage III …
- NAID 130000669407
- 吉井 貴彦,堀口 明男,城武 卓,戸邉 武蔵,田崎 新資,早川 正道,住友 誠,浅野 友彦
- 日本泌尿器科學會雜誌 101(6), 734-737, 2010-09-20
- 女性の尿道悪性黒色腫はまれな疾患であり,特に色素沈着の少ない無色素性悪性黒色腫の報告は本邦で4例を認めるに過ぎない.女性の尿道原発無色素性悪性黒色腫に対して拡大尿道摘除術を施行し,良好な治療経過を示した一例を経験したので報告する.症例は58歳女性.外尿道口腫瘤を自覚し,近医を受診した.尿道腫瘍の診断で,精査加療目的で当院を紹介受診した.外尿道口より突出する母指頭大の腫瘤を認め,生検にて悪性黒色腫と …
- NAID 110007730477
Related Links
- Nimustine is a medicine available in a number of countries worldwide. A list of US medications equivalent to Nimustine is available on the Drugs.com website. ... Drugs.com provides accurate and independent information on more than ...
- ニムスチン(ニドラン)は脳腫瘍に有効なニトロソウレア系の抗がん剤です。この系統の薬は分子量が小さいため、脳血管の特殊構造(血液脳関門)を通過して脳に入ることができます。
★リンクテーブル★
[★]
- 英
- nimustine
- 同
- 1-(4-amino-2-methyl-5-pyrimidinyl)methyl-3-(2-chloroethyl)-3-nitrosourea hydrochloride ACNU
- 化
- 塩酸ニムスチン nimustine hydrochloride
- 商
- ニドラン、サイメリン
- 関
- DAV・フェロン療法、悪性黒色腫
[★]
- 関
- nimustine