2',3'-ジデオキシシチジン 化学特性,用途語,生産方法
外観
白色~淡黄色、結晶性粉末~粉末
解説
ジデオキシシチジン,ヌクレオシド系の抗エイズ薬。 RNAから DNAを合成する逆転写酵素の働きを阻害することによって HIVの増殖を抑える働きをする。新たに日本でも承認され,すでに承認され使用されている AZT (アジドチミジン) や ddI (ジデオキシイノシン) では十分な効果が得られなくなった場合に併用薬として投与される。
用途
核酸アナログ逆転写酵素阻害
剤です。ウィルス DNA ポリメラーゼによる
基質の取り込みを競合的に阻害し、DNA 鎖の
伸長を停止することにより、ウィルスの増殖
阻害作用を示します。
用途
核酸アナログ逆転写酵素阻害
剤です。ウイルス DNA ポリメラーゼによる
基質の取り込みを競合的に阻害し、DNA 鎖の
伸長を停止することにより、ウイルス増殖阻
害作用を示します。
用途
抗菌剤及び抗癌剤研究用。
用途
ヒト免疫不全ウイルス(HIV)感染症に使用するため承認された最初の薬(1990年代初期に)の一つだったが、工業化され一般的に使用されるようになった。
効能
抗ウイルス薬, 逆転写酵素阻害薬
説明
Zalcitabine is an orally active dideoxynucleoside andog for combination use with
zidovudine in advanced HIV infection and also as monotherapy for AIDS patients who
cannot tolerate or have not responded to zidovudine. It has a similar mechanism of
action (inhibition of reverse transcriptase) to didanosine. Like didanosine, its side effect profile includes peripheral neuropathy. Unlike
zidovudine, zalcitabine does not cause bone marrow suppression.
化学的特性
White to Off-White Cyrstalline Powder
定義
ChEBI: A pyrimidine 2',3'-dideoxyribonucleoside compound having cytosine as the nucleobase.
適応症
Zalcitabine (ddC, Hivid) is a cytidine analogue active
against HIV-1, HIV-2, and hepatitis B virus. It is used
for the treatment of HIV infection in adults and asymptomatic
children as part of a multidrug regimen. It may
be less effective than the other nucleoside inhibitors
and is used less frequently.
一般的な説明
Zalcitabine, 2',3'-dideoxycytidine or ddCyd, is an analog ofcytosine that demonstrates activity against HIV-1 and HIV-2,including strains resistant to AZT. The potency (in peripheralblood mononuclear cells) is similar to that of AZT, but thedrug is more active in populations of monocytes andmacrophages as well as in resting cells.
The oral bioavailability of zalcitabine is over 80% in adultsand less in children.The major dose-limiting side effect isperipheral neuropathy, characterized by pain, paresthesias,and hypesthesia, beginning in the distal lower extremities.These side effects are typically evident after several months oftherapy with zalcitabine. A potentially fatal pancreatitis is anothertoxic effect of treatment with ddC. The drug has beenapproved for the treatment of HIV infection in adults with advanceddisease who are intolerant to AZT or who have diseaseprogression while receiving AZT. ddC is combined with AZTfor the treatment of advanced HIV infection.
空気と水の反応
Water soluble.
反応プロフィール
Zalcitabine may be sensitive to prolonged exposure to light.
火災危険
Flash point data for Zalcitabine are not available; however, Zalcitabine is probably combustible.
薬物動態学
Zalcitabine (ddC) is a useful alternate drug to ZDV and is given in combination with ZDV when CD4 cell counts fall to less than 300 cells/mm3 . Monotherapy with ddC is more active than ZDV. Its oral bioavailability is 87%, and its plasma half-life is approximately 1 hour.
In low doses (0.005 mg/kg every 4 hours), ddC produces sustained decrease in p24 antigen level and increase in CD4 cell counts. The CSF fluid/plasma ratio of ddC is 0.2. Following oral administration, bioavailability of ddC is less than 80%, which is further reduced when taken with food. The mean maximum plasma concentration of the drug also is reduced from 25.2 to 15.5 ng/mL when the drug was taken with food.
薬理学
Peripheral neuropathy occurs in up to 50% of patients
taking zalcitabine. Stomatitis, esophageal ulceration,
hepatotoxicity, rash, and pancreatitis may occur.
Zalcitabine should be used with caution in individuals
with a history of pancreatitis, liver disease, or alcohol
abuse. Dosage adjustment is necessary for individuals
with renal impairment. Zalcitabine should not be used in
combination with didanosine, lamivudine, or stavudine.
副作用
It has side effects, such as stomatitis, rash, fever, malaise, arthritis, and arthralgia.
代謝
Dideoxyuridine is the major metabolite in urine and feces. The drug penetrates the blood-brain barrier. The major toxicity of ddC is peripheral neuropathy, in which case it should be discontinued. In some cases, pancreatitis occurs when given alone or in combination with ZDV."
2',3'-ジデオキシシチジン 上流と下流の製品情報
原材料
準備製品