門冬醯胺酶
Asparaginase
L-Asparaginase / L-asparagine amidohydrolase
別名: Elspar · Crasnitine · Erwinase · Kidrolase · Laspar · Leucogen · Leunase · Paronal · Serasa · coloaspase · A-ase · ASN-ase · L-asparaginase · L-asparagine amidohydrolase · MK-965 · NSC-109229 · L-Asparginase · Crisantaspase
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
這是按體表面積（mg/m²）計算的劑量；給藥前須先把體重換算為體表面積。
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Lymphoid malignancies / Leukemia | 400 Units/kg or 10,000 Units/m2 IM or SC, with a maximum dose of 10,000 Units per patient | IM/SC | Protocol dependent | Protocol dependent | 🌎 NA |
| Treatment of lymphoid malignancies | 10,000 IU/m2 or 400 IU/kg | IM/SC | q7d or less frequently | As per chemotherapy protocol | 🌍 EU |
- Lymphoid malignancies / Leukemia: Many oncologists recommend administering diphenhydramine at 2 mg/kg SC 30 minutes prior to administration.
- Treatment of lymphoid malignancies: See specialist texts for chemotherapy protocols and conversion of body weight to body surface area.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Lymphoid malignancies / Leukemia | 400 Units/kg or 10,000 Units/m2 IM or SC, with a maximum dose of 10,000 Units per patient | IM/SC | Protocol dependent | Protocol dependent | 🌎 NA |
| Treatment of lymphoid malignancies | 10,000 IU/m2 or 400 IU/kg | IM/SC | q7d or less frequently | As per chemotherapy protocol | 🌍 EU |
- Lymphoid malignancies / Leukemia: Many oncologists recommend administering diphenhydramine at 1 mg/kg SC 30 minutes prior to administration.
- Treatment of lymphoid malignancies: See specialist texts for chemotherapy protocols and conversion of body weight to body surface area.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
門冬醯胺酶是一種獨特的酵素類抗腫瘤藥物，主要用於獸醫腫瘤學中治療犬貓的淋巴系統惡性腫瘤（如淋巴瘤）和白血病（特別是急性淋巴細胞白血病 ALL）。
與直接破壞 DNA 的傳統化療藥物不同，它透過剝奪癌細胞的重要營養物質來發揮作用。因為它對骨髓（極少引起骨髓抑制）和胃腸道黏膜的毒性較小，所以當病患骨髓功能已經受損時，它是誘導方案或「救援」治療的絕佳選擇。
臨床重點： 由於它是一種大型外來蛋白質（源自大腸桿菌），過敏反應/過敏性休克是一個主要的臨床問題，且其療效會因病患免疫系統產生中和抗體而隨時間下降。
作用機制
Normal cells can synthesize their own asparagine using the enzyme asparagine synthetase. However, many lymphoid malignant cells lack this enzyme and rely entirely on exogenous asparagine from the bloodstream for protein and DNA synthesis.
Asparaginase is an enzyme that circulates in the intravascular space and catalyzes the breakdown of circulating asparagine: L-asparagine + H2O → (via L-asparaginase) → Aspartic acid + Ammonia
By rapidly depleting circulating asparagine, the drug halts protein synthesis in the tumor cells, leading to apoptosis. The antineoplastic activity is greatest during the post-mitotic (G1) phase of the cell cycle.
安全性與警告
禁忌症
- Patients with a history of anaphylaxis to asparaginase
- Patients with pancreatitis or a history of pancreatitis
不良反應
- Hypersensitivity reactions (vomiting, diarrhea, urticaria, pruritus, dyspnea, hypotension, collapse)
- Hemorrhagic pancreatitis
- Hepatotoxicity
- Coagulation defects
- Hyperglycemia (secondary to altered insulin synthesis)
- Leukopenia (rare)
注意事項
Use with caution in patients with preexisting hepatic, renal, hematologic, gastrointestinal, or CNS dysfunction. Intravenous (IV) administration is generally avoided as it significantly increases the risk of anaphylaxis. Premedication with an antihistamine (e.g., diphenhydramine) is strongly recommended. Asparaginase can be a contact irritant; wash off any inadvertent skin contact. May alter thyroid function tests by decreasing thyroxine-binding globulin (TBG).
藥物相互作用
Asparaginase may reduce methotrexate effectiveness against tumor cells until serum asparagine levels return to normal.
Concurrent use may increase the risk for hyperglycemia.
Increased toxicity (neuropathy and erythropoiesis disruption) and myelosuppression may occur. Some oncologists recommend separating the dosing by a few days to a week.
監測
- Hepatic function
- Renal function (BUN may be increased by drug action)
- Pancreatic function (blood glucose, amylase)
- Hematopoietic function
- Patient observation for hypersensitivity during and immediately after administration
- Serum ammonia (may be increased)
藥物動力學
吸收
Not absorbed from the GI tract. After IM injection, serum levels are approximately 50% of those achieved after IV injection.
分佈
Due to its high molecular weight, it does not diffuse readily out of capillaries; about 80% of the drug remains within the intravascular space.
代謝
The metabolic fate of asparaginase is not known.
排除
Unknown.
過量
In dogs, the maximally tolerated dose is 10,000 IU/kg and the lethal dose is 50,000 IU/kg. Overdosage is expected to cause severe toxicity secondary to protein synthesis alteration (pancreatitis, hepatotoxicity, coagulopathy). Treatment is supportive.
可用產品
劑型
- Powder for Injection (lyophilized)
人用標示
- Asparaginase Powder for Injection, lyophilized: 10,000 Units in 10 mL vials (with 80 mg mannitol, preservative-free) (Elspar)
各地核准狀態
POM (Prescription Only Medicine)
POM-V
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store powder for injection at < 8°C; stable for at least 48 hours at room temperature. After reconstitution, the manufacturer states it is stable refrigerated for up to 8 hours (other sources state up to 14 days). Solutions should be clear; discard if turbid. Do not shake vigorously during reconstitution to avoid foaming and loss of potency.
飼主須知
重要提示： 門冬醯胺酶是一種化療藥物，但其作用方式與大多數化療藥物不同，通常不會導致白血球數量嚴重下降。
- 過敏反應： 因為這種藥物是源自細菌的蛋白質，注射後可能會立即發生過敏反應（喘氣、面部腫脹、嘔吐、焦躁不安、虛脫）。我們通常會預先給予抗組織胺來幫助預防。
- 胰臟與肝臟： 它偶爾會引起胰臟發炎（胰臟炎）或肝臟問題。請密切注意是否有嚴重的嘔吐、腹瀉、腹痛或眼睛/牙齦發黃。
- 出血： 如果您發現寵物有不明原因的瘀傷、牙齦出血或血便，請立即聯絡您的獸醫師。
- 安全處理： 您寵物的排泄物中可能在幾天內含有微量藥物。請遵循腫瘤科獸醫師的指示，安全處理尿液和糞便。
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