ビンブラスチン
ビンブラスチンは、ニチニチソウ由来の**ビンカアルカロイド系抗悪性腫瘍薬**です。獣医腫瘍学において、リンパ腫、癌腫、肥満細胞腫、脾臓腫瘍など、小動物の様々な悪性腫瘍の治療に主に使用されます。 **臨床上のポイント:** * **犬の肥満細胞腫**の治療において、同効薬のビンクリスチンよりも著効を示します。 * 強力な**発泡性物質(壊死起因物質)**であり、血管外に漏出すると重篤な組織壊死や蜂窩織炎を引き起こします。 * ビンクリスチンと比較して骨髄抑制作用が強い傾向がありますが、標準用量での末梢神経毒性は比較的軽度です。 * **MDR1 (ABCB1) 遺伝子変異**を持つ牧羊犬種では、重篤な骨髄抑制および消化管毒性のリスクが著しく高まるため、細心の注意が必要です。
作用機序: 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.
動物種別の用量
- Susceptible neoplasms · 2-2.2 mg/m2 · IV · every 1-2 weeks · Often used in combination with other chemo drugs.
- Susceptible neoplasms (e.g., mast cell tumors, lymphoma) · 2-2.2 mg/m2 · IV · every 1-2 weeks · Often used in combination with other chemo drugs (e.g., cyclophosphamide and prednisolone).
- Mast cell tumors (specific protocol) · Given on four subsequent days · IV · every 3 weeks · Consult specialized oncology references for exact protocol details.
用量は獣医療従事者向けの臨床リファレンスです。必ず最新の添付文書と個々の患者で確認してください。
投与経路
禁忌
- Preexisting leukopenia or granulocytopenia (unless caused by the disease being treated)
- Active bacterial infection
- Neutrophil count < 3 x 10^9/L
- Platelet count < 100 x 10^9/L
- 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)
有害事象
- 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)
- Myelosuppression (neutropenia, thrombocytopenia)
- Gastrointestinal toxicity
薬物相互作用
- Cisplatin · May cause additive risk for ototoxicity.
- Carboplatin · May cause additive risk for ototoxicity.
- P-glycoprotein inhibitors (e.g., Amiodarone, Ketoconazole, Cyclosporine, Diltiazem, Erythromycin, Spironolactone, Verapamil) · Can inhibit P-glycoprotein clearance of vinblastine, increasing the risk of severe toxicity, particularly in dogs with the MDR1 (ABCB1) mutation.
- Cimetidine · Inhibits hepatic cytochrome P450 enzymes, potentially decreasing vinblastine metabolism and increasing toxicity. · major
- Other myelosuppressive agents · Additive bone marrow suppression. · major
モニタリング
- 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
過量投与
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).
VetSheet の薬剤リファレンスは、獣医療従事者向けの臨床意思決定支援を目的としており、専門的判断やメーカーの最新添付文書に代わるものではありません。