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長春新鹼

Vincristine

Vincristine sulfate

抗腫瘤藥 - 長春花生物鹼IV

別名: Oncovin · Vincasar PFS · leurocristine sulfate · VCR · LCR compound 37231 · NSC-67574 · 22oxovincaleukoblastine sulphate · sulfato de vincristina · vincristini sulfas · Vincristine sulfate

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

0.02 mg/kgIV· once
🐕

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

適應症劑量途徑頻次療程地區
Neoplastic diseases (usually in combination protocols)0.5-0.75 mg/m2IVevery 1-2 weeks🌎 NA
Transmissible venereal tumor (TVT)0.5 mg/m2 (maximum dose 1 mg)IVonce weeklyfor 4-6 weeks🌎 NA
Adjunctive treatment of immune-mediated thrombocytopenia (IMT)0.5 mg/m2IVonce🌎 NA
Adjunctive treatment of immune-mediated thrombocytopenia (IMT) refractory to prednisone0.5-0.7 mg/m2IVonce🌎 NA
Adjunctive treatment of immune-mediated thrombocytopenia (IMT)0.02 mg/kgIVonce🌎 NA
Neoplastic diseases (particularly lymphoproliferative disorders), immune-mediated thrombocytopenia, transmissible venereal tumourSee Appendix for chemotherapy protocols and conversion of body weight to body surface area.IVNot specifiedNot specified🌍 EU
  • Neoplastic diseases (usually in combination protocols): Dosed in mg/m2, NOT mg/kg. Consultation with an oncologist recommended.
  • Transmissible venereal tumor (TVT): Used as sole therapy.
  • Adjunctive treatment of immune-mediated thrombocytopenia (IMT): If platelet count <10-20,000 cells/mcL or bleeding; consider bone marrow aspiration to document megakaryocytes.
  • Adjunctive treatment of immune-mediated thrombocytopenia (IMT) refractory to prednisone: Given as an IV bolus or as an infusion over 4-6 hours.
  • Adjunctive treatment of immune-mediated thrombocytopenia (IMT): Generally single use.
  • Neoplastic diseases (particularly lymphoproliferative disorders), immune-mediated thrombocytopenia, transmissible venereal tumour: Must be administered i.v. through a carefully pre-placed catheter.

適應症劑量途徑頻次療程地區
Neoplastic diseases0.5-0.75 mg/m2IVevery 1-3 weeks🌎 NA
Neoplastic diseases (particularly lymphoproliferative disorders)See Appendix for chemotherapy protocols and conversion of body weight to body surface area.IVNot specifiedNot specified🌍 EU
  • Neoplastic diseases: Dosed in mg/m2, NOT mg/kg. Consultation with an oncologist recommended.
  • Neoplastic diseases (particularly lymphoproliferative disorders): Must be administered i.v. through a carefully pre-placed catheter.

適應症劑量途徑頻次療程地區
Neoplastic diseases0.5 mg/m2 (usually 2.5-3 mg total dose per horse)IVweekly🌎 NA
  • Neoplastic diseases: Often used in CAP protocol with cytarabine and cyclophosphamide.

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。

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概覽

長春新鹼是一種源自長春花(Catharanthus roseus)的細胞週期特異性(M期)抗腫瘤藥物。它是獸醫腫瘤學中的基石,主要用於淋巴和造血系統腫瘤(如淋巴瘤)的聯合化療方案(如CHOP)。

主要臨床重點:

  • ​骨髓保護性​:與許多其他化療藥物(如其類似物長春花鹼)不同,長春新鹼在標準劑量下對骨髓的抑制作用較小,這使其在聯合方案中極具價值。
  • ​傳染性性病腫瘤 (TVT)​:作為單一藥物治療犬隻TVT具有極高的療效。
  • ​免疫介導性血小板減少症 (IMT)​:長春新鹼獨特地用於治療難治性IMT。它能促進巨核細胞的碎裂,導致血小板快速釋放到血液循環中。
  • ​發泡劑​:它是一種嚴重的組織發泡劑;必須透過完美放置的導管嚴格進行靜脈注射,以防止毀滅性的藥物外滲損傷。

作用機轉

Vincristine is a cell-cycle specific agent that acts during the M-phase (mitosis).

  • Antineoplastic Action: It binds specifically to tubulin dimers → inhibits microtubule polymerization → prevents the formation of the mitotic spindle → arrests cell division in metaphase, ultimately leading to apoptosis.
  • Metabolic Effects: It interferes with amino acid metabolism by inhibiting glutamic acid utilization and preventing purine synthesis, citric acid cycle, and urea formation.
  • Thrombocytosis: The exact mechanism is unknown, but it is believed to stimulate megakaryocyte fragmentation, accelerating the release of platelets into the peripheral blood.
  • Immunosuppression: Exhibits mild immunosuppressive activity, which may contribute to its efficacy in immune-mediated conditions.

安全性與警告

禁忌症

  • Preexisting neuromuscular disease
  • Severe leukopenia
  • Uncontrolled infection
  • No specific absolute contraindications listed, but requires extreme caution in specific disease states

不良反應

  • Peripheral neuropathy (proprioceptive deficits, spinal hyporeflexia)
  • Paralytic ileus and severe constipation
  • Mild leukopenia
  • Tissue necrosis and sloughing (if extravasated)
  • Anorexia, vomiting, diarrhea
  • Impaired platelet aggregation
  • Increased liver enzymes
  • Syndrome of inappropriate ADH secretion (SIADH)
  • Jaw pain
  • Alopecia
  • Stomatitis
  • Seizures
  • Pulmonary edema (rare, reported in cats)
  • GI tract toxicity
  • Severe local irritation/tissue necrosis (if administered perivascularly)
  • Myelosuppression (potential)

注意事項

Extravasation Warning: Vincristine is a potent vesicant. It must be given strictly IV. Use a different needle for injection than the one used to draw the drug from the vial. If extravasation occurs, stop immediately, apply moderate heat (or ice, depending on protocol), and consider topical DMSO or hyaluronidase injections.

  • ABCB1 (MDR1) Mutation: Herding breeds (e.g., Collies, Australian Shepherds) with this mutation are highly susceptible to severe bone marrow suppression and GI toxicity. Reduce dose by 25-30% in mutant/normal or mutant/mutant dogs.
  • Hepatic Impairment: Extensively metabolized by the liver. Consider a 50% dose reduction if serum bilirubin is > 2 mg/dL.
  • Neurotoxicity: Cats are particularly sensitive to neurotoxicity, which can manifest as paralytic ileus, severe constipation, and reversible axon swelling.
  • Handling: Wear gloves and protective clothing. Wash thoroughly with soap and water if skin exposure occurs.
  • Pregnancy: Potentially teratogenic and embryotoxic (FDA Category D).

藥物交互作用

Asparaginase

Additive neurotoxicity may occur; less common if asparaginase is administered after vincristine.

Mitomycin

Severe bronchospasm has occurred in humans receiving mitomycin-C with Vinca alkaloids.

Amiodarone

Inhibits P-glycoprotein; may increase vincristine toxicity, especially in MDR1/ABCB1 mutant dogs.

Azole Antifungals (e.g., ketoconazole)

Inhibits P-glycoprotein; may increase vincristine toxicity.

Carvedilol

Inhibits P-glycoprotein; may increase vincristine toxicity.

Cyclosporine

Inhibits P-glycoprotein; may increase vincristine toxicity.

Diltiazem

Inhibits P-glycoprotein; may increase vincristine toxicity.

Erythromycin

Inhibits P-glycoprotein; may increase vincristine toxicity.

Clarithromycin

Inhibits P-glycoprotein; may increase vincristine toxicity.

Quinidine

Inhibits P-glycoprotein; may increase vincristine toxicity.

Spironolactone

Inhibits P-glycoprotein; may increase vincristine toxicity.

Tamoxifen

Inhibits P-glycoprotein; may increase vincristine toxicity.

Verapamil

Inhibits P-glycoprotein; may increase vincristine toxicity.

CYP3A inhibitorsMajor

Decreased metabolism of vincristine and increased toxicity

L-asparaginaseMajor

Reduced clearance of vincristine and increased toxicity if given with or before vincristine (vincristine should be given 12-24 hours before L-asparaginase)

監測

  • Efficacy (tumor burden reduction or platelet count)
  • Peripheral neuropathic clinical signs (e.g., gait abnormalities, constipation)
  • Complete blood counts (CBC) with platelets
  • Liver function tests (prior to therapy and repeated as necessary)
  • Serum uric acid
  • Complete Blood Count (CBC) prior to each dose
  • IV catheter site for any signs of extravasation during administration
  • Gastrointestinal signs (monitoring for ileus or severe constipation)
  • Neurological exams (monitoring for peripheral neuropathy, e.g., dragging paws, loss of reflexes)

藥物動力學

半衰期

Biphasic: alpha half-life 13 minutes, beta half-life 75 minutes

吸收

Unpredictably absorbed from the GI tract; must be administered IV.

分佈

Rapidly distributed to tissues after injection. In humans, ~75% is bound to tissue proteins. Does not appreciably enter the CNS.

代謝

Extensively metabolized, presumably by the liver.

排除

Primarily excreted in the bile/feces; lesser amounts are eliminated in the urine.

過量

Vincristine has a narrow therapeutic index.

  • Dogs: The maximally tolerated dose is reported as 0.06 mg/kg every 7 days for 6 weeks. Toxicity signs include slight anemia, leukopenia, increased liver enzymes, and neuronal shrinkage in the peripheral and central nervous systems.
  • Cats: The lethal dose is reportedly 0.1 mg/kg. Toxic signs include weight loss, seizures, leukopenia, and general debilitation. A reported 10X overdose (5 mg/m2) resulted in death within 72 hours despite intensive care (including calcium folinate).
  • Treatment: Primarily supportive. Includes cardiovascular and hematologic monitoring, anticonvulsants for seizures, and prevention of ileus. Fluid restriction and loop diuretics may be needed to manage SIADH. Leucovorin calcium has been used in humans, but efficacy is unconfirmed.

可用產品

劑型

  • Injection
  • Injectable: 1 mg, 2 mg, 5 mg vials

人用標示

  • Vincristine Sulfate Injection: 1 mg/mL in 1 mL, 2 mL & 5 mL vials and flip-top vials (Vincasar PFS; generic)
  • Oncovin
  • Vincristine 1 mg, 2 mg, 5 mg vials

各地核准狀態

European Union✓ 已核准處方藥EMA
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Protect from light and store in the refrigerator (2-8°C).

飼主須知

長春新鹼是一種強效的化療藥物,用於治療癌症和某些免疫系統疾病。

  • ​毒性風險​:雖然通常耐受性良好,但可能會出現嚴重的副作用。如果您的寵物出現極度抑鬱、異常出血或瘀傷、血便、嚴重便秘或行走困難(神經病變),請立即聯繫您的獸醫。
  • ​居家安全預防措施​:藥物及其代謝產物會排泄在寵物的體液中。​治療後長達7天內,請避免直接接觸寵物的尿液、唾液或糞便。​ 清理排泄物時請戴上手套,事後徹底洗手。
  • ​錯過劑量​:化療時間表非常嚴格。如果您錯過了預約,請立即聯繫您的獸醫重新安排。

VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠商最新仿單。