鏈脲佐菌素
Streptozocin
Streptozotocin (2-Deoxy-2-(3-methyl-3-nitrosoureido)-D-glucopyranose)
別名: Zanosar · NSC-85998 · streptozotocin · U-9889
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
這是依速率計算的持續輸注（CRI）劑量；須計算輸注速率，不能只依體重換算。
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 |
|---|---|---|---|---|---|
| Recurrent insulinoma after surgery (investigational) | Begin saline diuresis: Give normal saline at 18-20 mL/kg/hour for 7-8 hours. Over the 4th-5th hour, give streptozocin in the saline solution at a dose of 500 mg/m 2 IV. Give an antiemetic (e.g., butorphanol) at the end of the 7-hour period. | IV | Once | 7-8 hours total | 🌎 NA |
| Pancreatic islet cell tumors | Normal saline is given IV at 18.3 mL/kg/hr for 3 hours, then streptozocin is administered at 500 mg/m 2 over two hours with the saline diuresis continuing. After streptozocin infusion completed, continue saline diuresis for another 2 hours. Butorphanol is administered as an antiemetic immediately after streptozocin. | IV | May repeat at 3 week intervals | Until evidence of tumor progression, recurrence of hypoglycemia, or drug toxicity | 🌎 NA |
- Recurrent insulinoma after surgery (investigational): Requires aggressive fluid therapy.
- Pancreatic islet cell tumors: Monitor for myelosuppression and nephrotoxicity.
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
鏈脲佐菌素是一種最初源自Streptomyces achromogenes的抗腫瘤抗生素，儘管市售產品為人工合成。在獸醫學中，它主要利用其對胰腺β細胞的靶向毒性，成為治療犬隻復發性、無法手術切除或轉移性胰島素瘤的關鍵藥物。
- 臨床要點：胰島素瘤是分泌過量胰島素的胰腺功能性腫瘤，會導致危及生命的低血糖。鏈脲佐菌素能選擇性破壞這些腫瘤細胞，有助於控制低血糖並減緩腫瘤進展。
- 由於其嚴重的毒性特徵，通常僅保留用於手術切除不完全或無法手術的難治性病例。
作用機轉
Streptozocin acts primarily as an alkylating agent.
- DNA Damage: It cross-links DNA strands → inhibits DNA synthesis and prevents precursor incorporation into DNA.
- Beta-Cell Toxicity: The drug enters cells via the GLUT2 transporter, which is highly expressed on pancreatic beta cells. Once inside, it causes a species-specific diabetogenic effect in dogs by reducing nicotinamide adenine dinucleotide (NAD) and ATP concentrations → irreversible beta cell necrosis.
- While it possesses antibacterial activity against gram-positive and gram-negative bacteria, its severe cytotoxicity precludes its use as an antibiotic.
安全性與警告
禁忌症
- Patients without a confirmed histologic diagnosis of insulinoma
- Patients with completely resectable tumors
- Pregnancy (unless benefits outweigh risks; FDA Category C)
不良反應
- Serious, permanent renal toxicity
- Severe and protracted vomiting and nausea
- Mild myelosuppression
- Elevated liver enzymes
- Severe tissue necrosis if extravasated (vesicant)
注意事項
CRITICAL WARNING: Streptozocin is highly nephrotoxic. Aggressive IV saline diuresis is absolutely mandatory before, during, and after administration to prevent permanent renal failure.
- Must be used with extreme caution in patients with decreased renal, bone marrow, or hepatic function.
- Vesicant: Severe tissue necrosis will occur if the drug extravasates outside the vein. Ensure a perfectly placed, patent IV catheter.
- Nursing Safety: It is unknown if it is excreted in milk. Consider using milk replacer due to the potential for serious adverse reactions in nursing offspring.
藥物交互作用
Streptozocin may prolong the half-life of doxorubicin; dosage adjustment may be required.
Additive or synergistic myelosuppression may occur.
May cause additive nephrotoxicity when used concurrently.
Can block the diabetogenic effects of streptozocin without altering its antineoplastic activity; this may be beneficial or detrimental depending on the clinical goal.
監測
- Blood glucose (to assess efficacy)
- Baseline and post-treatment renal function tests (including urinalysis)
- CBC (for myelosuppression)
- Baseline and pre-retreatment liver function tests
- Hydration status (especially for the first few days after treatment or if vomiting is a problem)
藥物動力學
吸收
Must be administered IV. Cytotoxic nature precludes other routes.
分佈
Distributes to most tissues; concentrations in the pancreas are higher than those found in plasma.
代謝
Metabolized, probably in the liver.
排除
Both unchanged and metabolized drug are excreted in the urine.
過量
Severe toxicity may result if acutely overdosed, primarily manifesting as acute renal failure, severe gastrointestinal distress, and myelosuppression. Dosages must be calculated carefully based on body surface area (m^2). Treatment is supportive, focusing on aggressive fluid diuresis and management of uremia and cytopenias.
可用產品
劑型
- Powder for injection
人用標示
- Streptozocin Powder for Injection: 1 gram (100 mg/mL) in vials; Zanosar® (Genesia Sicor); (Rx)
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 lyophilized powder in the refrigerator and protect from light. Stable for at least 3 years after manufacture (1 year if stored at room temperature). Reconstitute with Dextrose 5% or 0.9% sodium chloride. The reconstituted solution is stable for 48 hours at room temperature and 96 hours if refrigerated, but as no preservative is added, the manufacturer recommends using the drug within 12 hours of mixing.
飼主須知
- 治療目的：您的狗狗被處方鏈脲佐菌素來治療胰島素瘤（一種會導致危險低血糖的胰腺腫瘤）。
- 需要住院：因為這種藥物對腎臟的負擔非常大，您的狗狗需要住院，在治療前、中、後接受持續的靜脈輸液，以沖洗腎臟並保護其免受損傷。
- 副作用：噁心和嘔吐非常常見。您的獸醫會給予強效的止吐藥物，讓您的狗狗盡可能保持舒適。
- 實驗性質：在獸醫學中，這被認為是一種「研究性」或標示外治療。嚴格的後續監測（包括血糖、腎功能指數和血球計數）是絕對必要的。
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