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ビンクリスチン

Vincristine

Vincristine sulfate

抗悪性腫瘍薬 - ビンカアルカロイドIV犬猫馬

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

VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス

0.02 mg/kgIV· once
— 🐕

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

動物種別用量

🌎 NA — North America🌍 EU — Europe

犬

適応用量経路頻度期間地域
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.

猫

適応用量経路頻度期間地域
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.

馬

適応用量経路頻度期間地域
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.

用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。

診察中ですか？VetSheet の AI が薬剤・用量・投与期間を構造化された診察記録に直接記入します。VetSheet の仕組みを見る

概要

ビンクリスチンは、ニチニチソウ（Catharanthus roseus）由来の細胞周期特異的（M期）抗悪性腫瘍薬です。獣医腫瘍学における重要な薬剤であり、主にリンパ腫などのリンパ系および造血系腫瘍に対する多剤併用化学療法（CHOP療法など）で使用されます。

主な臨床的特徴：

  • ​骨髄抑制が軽度​：他の多くの抗がん剤（類似薬のビンブラスチンなど）とは異なり、標準用量では骨髄抑制が軽度であるため、併用療法において非常に有用です。
  • ​可移植性性器腫瘍（TVT）​：犬のTVTに対しては単剤で極めて高い有効性を示します。
  • ​免疫介在性血小板減少症（IMT）​：難治性のIMTの治療にも独自に使用されます。巨核球の断片化を促進し、血小板の血中への放出を早めます。
  • ​壊死性物質（起泡薬）​：重度の組織障害を引き起こす起泡薬です。壊滅的な血管外漏出による損傷を防ぐため、適切に留置されたカテーテルからの厳密な静脈内投与が必須です。

作用機序

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・警告

禁忌

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

有害事象

  • 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).

医薬品相互作用

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)

監視

  • 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)

薬物動態

半減期

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

吸収

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

分布

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.

消失

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

過剰投与

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.

製品

製剤

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

ヒト用医薬品

  • 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

規制ステータス

European Union✓ 承認済み処方箋医薬品EMA
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

United Kingdom✓ 承認済み処方箋医薬品VMD
🐕 Dogs🐈 Cats

POM (Prescription Only Medicine)

規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

保管・安定性

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

飼主向け情報

ビンクリスチンは、がんや特定の免疫系疾患の治療に使用される強力な化学療法薬です。

  • ​毒性のリスク​：一般的に忍容性は良好ですが、重篤な副作用が起こる可能性があります。ペットに極度の元気消失、異常な出血やあざ、血便、重度の便秘、歩行困難（神経障害）が見られた場合は、直ちに獣医師に連絡してください。
  • ​家庭での安全対策​：薬剤およびその分解物はペットの体液中に排泄されます。​治療後最大7日間は、ペットの尿、唾液、便に直接触れないようにしてください。​ 排泄物を片付ける際は手袋を着用し、その後は石鹸で手をよく洗ってください。
  • ​投与忘れ​：化学療法のスケジュールは非常に厳密です。予約を逃した場合は、すぐに獣医師に連絡してスケジュールを再調整してください。

VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。