長春花鹼
Vinblastine
Vinblastine sulfate
別名: Velban · Alkaban · Blastovin · Cellblastin · Cytoblastin · Ifabla · Lemblastine · Periblastine · Serovin · Solblastin · Velbe · Velsar · Xintoprost · 29060-LE · NSC-49842 · sulfato de vimblastina · vinblastini sulfas · vincaleukoblastine sulphate · VBL · Vinblastine sulfate · VLB
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 neoplasms (e.g., mast cell tumors, lymphoma) | 2-2.2 mg/m2 | IV | every 1-2 weeks | — | 🌎 NA |
| Mast cell tumors (specific protocol) | Given on four subsequent days | IV | every 3 weeks | — | 🌎 NA |
- Susceptible neoplasms (e.g., mast cell tumors, lymphoma): Often used in combination with other chemo drugs (e.g., cyclophosphamide and prednisolone).
- Mast cell tumors (specific protocol): Consult specialized oncology references for exact protocol details.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Susceptible neoplasms | 2-2.2 mg/m2 | IV | every 1-2 weeks | — | 🌎 NA |
- Susceptible neoplasms: Often used in combination with other chemo drugs.
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
長春花鹼是一種源自長春花植物的長春花生物鹼類抗腫瘤藥物。在獸醫腫瘤學中，主要用於治療小動物的多種惡性腫瘤，包括淋巴瘤、癌、肥大細胞瘤和脾臟腫瘤。
臨床要點：
- 在治療犬肥大細胞瘤方面，長春花鹼的療效顯著優於其同類藥物長春新鹼（vincristine）。
- 它是一種強烈的發泡劑（vesicant）；若藥物外滲至血管外，會引起嚴重的組織壞死和蜂窩組織炎。
- 與長春新鹼相比，它通常具有更強的骨髓抑制作用，但在標準劑量下，其周邊神經毒性較輕。
- 帶有MDR1 (ABCB1) 基因突變的牧羊犬品種需高度謹慎使用，因為牠們發生嚴重骨髓抑制和胃腸道毒性的風險顯著增加。
作用機轉
Vinblastine is a cell-cycle specific agent that halts cell division.
- Microtubule Inhibition: It binds specifically to microtubular proteins (tubulin) in the mitotic spindle.
- Mitotic Arrest: By preventing microtubule assembly, it arrests cell division during metaphase.
- Metabolic Interference: It also interferes with amino acid metabolism by inhibiting glutamic acid utilization and preventing purine synthesis, the citric acid cycle, and urea formation.
安全性與警告
禁忌症
- Preexisting leukopenia or granulocytopenia (unless caused by the disease being treated)
- Active bacterial infection
- Pre-existing severe myelosuppression or active infection
- Pre-existing severe myelosuppression (Neutrophil count < 3 x 10^9/L or Platelet count < 100 x 10^9/L)
不良反應
- Gastroenterocolitis (nausea, vomiting, anorexia)
- Myelosuppression (neutropenia, thrombocytopenia, anemia; nadir at 4-9 days)
- Neurotoxicity (constipation, paralytic ileus, jaw and muscle pain, loss of deep tendon reflexes)
- Alopecia
- Stomatitis
- Syndrome of inappropriate ADH secretion (SIADH)
- Severe tissue irritation and cellulitis (if extravasated)
- Cats: Reversible axon swelling and paranodal demyelination
- Myelosuppression (primarily neutropenia)
- Gastrointestinal toxicity (vomiting, diarrhea, anorexia)
- Severe tissue necrosis (if extravasated)
注意事項
Vesicant Warning: Vinblastine is a severe tissue irritant. Strict IV administration is required. Avoid extravasation. Use a different needle for injection than the one used to draw up the drug. If extravasation occurs, stop immediately, apply moderate heat, and consider hyaluronidase injections to disperse the drug.
- MDR1 Mutation: Dogs with the ABCB1 (MDR1) mutation (e.g., Collies, Australian Shepherds) are highly susceptible to toxicity. Reduce dose by 25-30% in mutant/normal or mutant/mutant dogs.
- Hepatic Impairment: Extensive hepatic metabolism requires a 50% dose reduction if serum bilirubin is > 2 mg/dL.
- Handling: Wear gloves and protective clothing during preparation and administration. Wash thoroughly with soap and water if skin exposure occurs.
- Pregnancy/Nursing: Potentially teratogenic and embryotoxic (FDA Category D). Avoid in pregnant animals and use milk replacer if nursing.
藥物交互作用
May cause additive risk for ototoxicity.
May cause additive risk for ototoxicity.
Can inhibit P-glycoprotein clearance of vinblastine, increasing the risk of severe toxicity, particularly in dogs with the MDR1 (ABCB1) mutation.
Inhibits hepatic cytochrome P450 enzymes, potentially decreasing vinblastine metabolism and increasing toxicity.
Additive bone marrow suppression.
監測
- Efficacy (tumor response)
- Complete blood counts (CBC) with platelets (monitor for nadir)
- Liver function tests (prior to therapy and repeated as necessary)
- Serum uric acid
- IV site for signs of extravasation during administration
- Haematology (CBC) prior to each treatment
- Biochemistry prior to first treatment
- Tumour restaging (lymph node palpation, cytology)
- Complete Blood Count (CBC) prior to every dose (specifically neutrophils and platelets)
- Tumor restaging at week 4 and week 12 (for high-risk tumors)
- IV catheter site for signs of extravasation during administration
藥物動力學
半衰期
吸收
Administered strictly IV.
分佈
Rapidly distributed to tissues after injection. In humans, approximately 75% is bound to tissue proteins. Does not appreciably enter the CNS.
代謝
Extensively metabolized by the liver.
排除
Primarily excreted in the bile and feces; lesser amounts are eliminated in the urine.
過量
The lethal dose in dogs is reported as 0.2 mg/kg.
Clinical Signs of Overdose: Exacerbation of adverse effects, including profound myelosuppression, severe gastrointestinal signs, and neurotoxicity (similar to vincristine).
- Feline Case Report (4X IV overdose): Depression, inability to jump, anorexia (days 1-11), neutropenia with fever, thrombocytopenia, anemia, vomiting, diarrhea, and syndrome of inappropriate ADH (SIADH).
Treatment: Aggressive supportive care is required. Monitor cardiovascular and hematologic status closely. Treatment may include anticonvulsants, prevention/management of ileus, and management of SIADH (fluid restriction and loop diuretics to maintain serum osmolality).
可用產品
劑型
- Injection solution (1 mg/mL)
- Powder for injection (10 mg)
- 1 mg/mL injectable solution
人用標示
- Vinblastine Sulfate Injection: 1 mg/mL in 10 mL & 25 mL vials
- Vinblastine Powder for Injection: 10 mg in vials (Velban)
- Velbe 10mg powder for solution for injection
- Vinblastine sulfate 1mg/ml solution for injection
- Vinblastine sulfate 1 mg/mL injection
各地核准狀態
Used under the cascade. Requires specialized handling and disposal as a cytotoxic agent.
Used under the cascade. Requires specialized handling and disposal as a cytotoxic agent.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Protect from light. Store powder for injection and injection solution in the refrigerator (2-8°C). Intact powder for injection is stable at room temperature for at least one month. After reconstituting with bacteriostatic saline, the powder for injection is stable for 30 days if refrigerated.
飼主須知
- 毒性風險： 這是一種強效的化療藥物。可能會出現嚴重的毒性反應，甚至包括與藥物相關的死亡風險。
- 何時聯繫獸醫： 如果您的寵物出現極度抑鬱、嗜睡、異常出血（包括血便）、瘀傷，或持續嘔吐/食慾不振，請立即聯繫您的獸醫。
- 排泄物處理： 在治療後的幾天內，請遵循獸醫的指示，安全處理寵物的尿液和糞便。
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