阿糖胞苷
Cytarabine
Cytosine arabinoside
別名: Cytosar-U · DepoCyt · Tarabine PFS · Ara-C · 1-beta-D-arabinofuranosylcytosine · arabinosylcytosine · cytarabine liposome · cytarabinum · NSC-63878 · U-19920
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
這是依體表面積（mg/m²）計算的劑量；給藥前須先將體重換算為體表面積。
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible neoplastic diseases | 100 mg/m2 | IV/SC | continuous infusion over 2-3 days or divided and given IV or SC for 2-4 days | 2-4 days | 🌎 NA |
- Susceptible neoplastic diseases: Dosed in mg/m2 (NOT mg/kg). Use only as a general guide.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible neoplastic diseases | 100 mg/m2 | IV/SC | continuous infusion over 2-3 days or divided and given IV or SC for 2-4 days | 2-4 days | 🌎 NA |
- Susceptible neoplastic diseases: Dosed in mg/m2 (NOT mg/kg). Cats are generally dosed similarly to dogs.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Neoplastic diseases | 200-300 mg/m2 (usually 1-1.5 grams per horse per dose) | SC/IM/IV | every 1-2 weeks | — | 🌎 NA |
- Neoplastic diseases: Consultation with a veterinary oncologist is encouraged before use.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
阿糖胞苷（通常稱為 Ara-C）是一種合成的嘧啶核苷抗代謝物，在獸醫學中主要用於治療犬貓的淋巴網狀內皮腫瘤、骨髓增生性疾病（白血病）和中樞神經系統淋巴瘤。
臨床重點： 除了傳統的腫瘤學應用外，阿糖胞苷在獸醫神經學中被廣泛用作治療犬隻不明原因腦膜腦炎 (MUE) 和肉芽腫性腦膜腦炎 (GME) 的核心免疫抑制療法。由於其在連續靜脈輸注 (CRI) 或高劑量皮下注射方案下能夠穿透血腦屏障，因此對中樞神經系統發炎性疾病非常有效。
作用機轉
Cytarabine is a cell-cycle phase-specific antimetabolite that acts principally during the S-phase (active DNA synthesis).
- Intracellular Conversion: Cytarabine enters the cell and is phosphorylated into its active form, cytarabine triphosphate.
- Enzyme Inhibition: This active metabolite competes with deoxycytidine triphosphate → incorporates into DNA → potently inhibits DNA polymerase.
- Result: Inhibition of DNA synthesis and repair, leading to cell death in rapidly dividing cells. Under certain conditions, it may also block cells from transitioning from the G1 phase to the S phase.
安全性與警告
禁忌症
- Hypersensitivity to cytarabine
- Pregnancy (potentially teratogenic and embryotoxic)
不良反應
- Myelosuppression (leukopenia, anemia, thrombocytopenia)
- Anorexia
- Nausea
- Vomiting
- Diarrhea
- Conjunctivitis
- Oral ulceration
- Neurotoxicity
- Hepatotoxicity
- Fever
- Anaphylaxis (rare)
注意事項
Cytarabine is a mutagenic and potentially carcinogenic agent. It should only be used in patients who can be adequately and regularly monitored. Personnel preparing or administering the drug must wear gloves and follow hazardous drug handling protocols. Wash skin or mucous membranes thoroughly if contamination occurs.
藥物交互作用
Cytarabine may decrease the amount of digoxin (tablets only) absorbed after oral dosing due to intestinal mucosa alterations; effect may persist for several days after cytarabine discontinuation.
Cytarabine may antagonize the anti-infective activity of flucytosine; monitor for decreased efficacy.
Cytarabine may antagonize the anti-infective activity of gentamicin; monitor for decreased efficacy.
監測
- Efficacy (tumor response or resolution of neurologic signs)
- Hemograms (mandatory; monitor for myelosuppression, nadir typically at 5-7 days)
- Liver function tests (periodic)
- Kidney function tests (periodic)
藥物動力學
吸收
Very poor systemic availability after oral administration. Following IM or SC injections, peaks in plasma within 20-60 minutes, but levels are much lower than equivalent IV doses.
分佈
Widely distributed throughout the body. Crosses into the CNS in a limited manner with bolus injection, but continuous IV infusion achieves CSF levels 20-60% of plasma levels. About 13% bound to plasma proteins in humans. Crosses the placenta.
代謝
Rapidly metabolized by the enzyme cytidine deaminase (principally in the liver, but also kidneys, intestinal mucosa, and granulocytes) to the inactive metabolite ara-U (uracil arabinoside).
排除
About 80% of a dose is excreted in the urine within 24 hours as both ara-U (≈90%) and unchanged cytarabine (≈10%). Elimination half-life in the CSF is significantly longer than in serum.
過量
Efficacy and toxicity are dependent on both the dose and the rate of administration. In dogs, the IV LD50 is 384 mg/kg when given over 12 hours, but drops to 48 mg/kg when infused IV over 120 hours. In the event of an inadvertent overdose, aggressive supportive therapy should be instituted.
可用產品
劑型
- Powder for injection
- Injection solution
- Liposomal injection
人用標示
- Cytarabine Powder for Injection: 100 mg, 500 mg, 1 g & 2 g in vials
- Cytarabine Injection: 10 mg/mL (liposomal) preservative free in 5 mL vials
- Cytarabine Injection: 20 mg/mL in 5 mL vials & 50 mL bulk package vials
- Cytarabine Injection: 100 mg/mL in 20 mL single-dose vials
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store sterile powder at room temperature (15-30°C). After reconstitution with bacteriostatic water, solutions are stable for at least 48 hours at room temperature (some studies show 90% potency retention up to 17 days). Discard if the solution develops a slight haze.
飼主須知
阿糖胞苷是一種強效的化療藥物。
- 毒性風險： 請注意此藥物可能引發嚴重的毒性反應，包括危及生命的併發症或藥物相關的死亡風險。
- 何時聯繫獸醫： 如果您的寵物出現嚴重的精神沉鬱、嗜睡、異常出血（例如牙齦出血、流鼻血）、瘀斑、發燒或嚴重的腸胃不適，請立即聯繫您的獸醫。
- 安全操作： 由於這是一種危險藥物（化療藥），在治療後的幾天內，請務必遵循獸醫的指示，安全處理寵物的排泄物（尿液/糞便）。
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