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外観
白色～ほとんど白色粉末～結晶
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用途
抗悪性腫瘍薬。神経膠腫の治療
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効能
抗悪性腫瘍薬, アルキル化剤
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商品名
ギリアデル (エーザイ)
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説明
Carmustine is a nitrogen mustard β-chloro-nitrosourea compound that is used as an alkylating agent. It forms interstrand crosslinks in DNA, which prevents DNA replication and transcription leading to apoptosis. Carmustine is also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase. Carmustine has been tested in clinical trials as a cytostatic agent for Hodgkin’s and non-Hodgkin’s lymphoma, myeloma, malignant melanoma, glioblastoma, and other brain tumors.
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化学的特性
Carmustine is an orange-yellow crystalline
solid or powder.
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使用
Carmustine is a nitrogen mustard β-chloro-nitrosourea compound that is used as an alkylating agent. It forms interstrand crosslinks in DNA, which prevents DNA replication and transcription leading to apoptosis. Carmustine is also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase. Carmustine has been tested in clinical trials as a cytostatic agent for Hodgkin’s and non-Hodgkin’s lymphoma, myeloma, malignant melanoma, glioblastoma, and other brain tumors.
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定義
ChEBI: A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.
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一般的な説明
Orange-yellow solid.
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空気と水の反応
Insoluble in water.
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反応プロフィール
Carmustin decomposes rapidly in acid and in solutions above pH 7; most stable in petroleum ether or aqueous solution at pH 4.
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危険性
Extremely toxic, central nervous system
depression, pulmonary fibrosis, renal and hepatic
damage, cytotoxic, immunosuppressive, carcino-
gen.
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火災危険
Flash point data for Carmustin are not available. Carmustin is probably combustible.
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安全性プロファイル
Confirmed carcinogen withexperimental carcinogenic and tumorigenic data. A humanpoison by parenteral route. An experimental poison byingestion, intravenous, intraperitoneal, parenteral, andsubcutaneous routes. Human systemic effects byparenteral, int
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職業ばく露
BCNU has been used since 1971 as an
antineoplastic agent in the treatment of Hodgkin’slymphoma; multiple meyloma; and primary or metastatic
brain tumors. It also has been reported to have antiviral,
antibacterial, and antifungal activity, but no evidence was
found that it is used in these ways. BCNU is not known to
be naturally occurring. Health professionals who handle
this drug (for example, pharmacists, nurses, and physicians)
may possibly be exposed to BCNU during drug preparation, administration, or cleanup; however, the risks can be
avoided through use of containment equipment and proper
work practices
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発がん性
Bis(chloroethyl) nitrosourea (BCNU) is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.
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環境運命予測
It is generally assumed that BCNU exerts its cytotoxicity
through the liberation of alkylating and carbamoylating
moieties. An alkylating entity, particularly chloroethyl carbonium
ion, is strongly electrophilic and can alkylate a variety
of biomolecules, including the purine and pyrimidine bases of
DNA. BCNU causes DNA interstrand cross-linking, which is
associated with cytotoxicity. The carbamoylation of lysine
residues of protein can inactivate certain enzymes, thus interfering
with DNA and RNA synthesis and repair processes. The
inhibition of glutathione reductase by this carbamoylation
further contributes to cytotoxicity.
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輸送方法
UN3249 Medicine, solid, toxic, n.o.s., Hazard
Class: 6.1; Labels: 6.1-Poisonous materials. UN2811 Toxic
solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-
Poisonous materials, Technical Name Required.
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不和合性
Acids and acid solutions above pH 7
cause rapid decomposition. Most stable at pH 4 in aqueous
solution or petroleum ether.
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廃棄物の処理
It is inappropriate and possibly dangerous to the environment to dispose of expired or
waste pharmaceuticals by flushing them down the toilet or
discarding them to the trash. Household quantities of
expired or waste pharmaceuticals may be mixed with wet
cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consideration applicable DEA, EPA, and FDA regulations. If
possible return the pharmaceutical to the manufacturer for
proper disposal being careful to properly label and securely
package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a
state licensed medical waste contractor to dispose by burial
in a licensed hazardous or toxic waste landfill or
incinerator.
