達卡巴仁 / 達卡巴肼
Dacarbazine
Dimethyl triazeno imidazole carboxamide
別名: DTIC-Dome · Asercit · Dacarbaziba · Dacatic · Deticene · Detilem · Detimedac · Fauldetic · Ifadac · Oncocarbil · Dacarbazine medac · dacarbazinum · DIC · imidazole carboxamide · diemthyl triazeno imadazol carboxamide · NSC-45388 · WR139007
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
這是按體表面積（mg/m²）計算的劑量；給藥前須先把體重換算為體表面積。
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Relapsed lymphoma, soft tissue sarcomas, melanoma | 800-1000 mg/m2 | IV | every 2-3 weeks | over 5-8 hours | 🌎 NA |
| Relapsed Lymphoma (Rescue Protocol) | 800-1000 mg/m2 | IV | every 3 weeks | as determined by oncologist | 🌍 EU |
| Relapsed Lymphoma (Alternative schedule) | 200 mg/m2 | IV | sid | for 5 consecutive days | 🌍 EU |
- Relapsed lymphoma, soft tissue sarcomas, melanoma: NOT mg/kg. Depending on the protocol used.
- Relapsed Lymphoma (Rescue Protocol): Administer as a slow IV infusion (over several hours) to minimize adverse effects. Pre-medicate with antiemetics.
- Relapsed Lymphoma (Alternative schedule): Repeat cycle every 3 weeks.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
達卡巴仁（常被稱為 DTIC）是一種注射用抗腫瘤藥物，在獸醫腫瘤學中主要用於治療犬隻復發性淋巴瘤、軟組織肉瘤和黑色素瘤。
臨床要點：
- 達卡巴仁是一種前驅藥（prodrug），需要經過肝臟活化才能發揮其細胞毒性作用。
- 不建議用於貓，因為目前尚不清楚貓的肝臟是否能充分將其代謝為活性形式，這使得該藥物在貓體內的療效和安全性極難預測。
- 它是一種強烈的發泡劑（vesicant）；藥物外滲會導致嚴重的組織壞死。必須透過放置完美的靜脈留置針給藥，通常建議以稀釋後的慢速輸注方式進行。
作用機制
Dacarbazine is a prodrug that undergoes hepatic N-demethylation (likely via cytochrome P450 enzymes) to form an active intermediate, which then degrades to form reactive carbonium ions.
- Alkylating Activity: These carbonium ions act as alkylating agents → cross-link DNA strands → interfere with DNA transcription and replication.
- Antimetabolite Activity: It also inhibits the incorporation of purine nucleosides into DNA.
- It possesses minimal immunosuppressant activity and is generally considered cell cycle-phase nonspecific.
安全性與警告
禁忌症
- Cats (due to unknown hepatic metabolism capabilities)
- Patients with known hypersensitivity to the drug
- Pregnancy (teratogenic)
- Pre-existing severe myelosuppression
- Severe hepatic dysfunction
- Pregnancy and lactation
不良反應
- Severe gastrointestinal toxicity (vomiting, anorexia, diarrhea) - often dose-limiting
- Bone marrow suppression (leukopenia, thrombocytopenia) - nadir occurs several weeks post-treatment
- Severe tissue damage and pain (if extravasated)
- Venous spasm and phlebitis during IV administration
- Alopecia (rare)
- Hepatotoxicity (rare)
- Renal impairment (rare)
- Photosensitivity (rare)
- Severe nausea and vomiting
- Myelosuppression (neutropenia, thrombocytopenia)
- Tissue necrosis if extravasated
- Lethargy
注意事項
WARNING: VESICANT. Dacarbazine can cause extensive pain and severe tissue damage if extravasated. Dilution and administration by IV infusion is strongly recommended.
- Use with extreme caution in patients with preexisting bone marrow depression, hepatic or renal dysfunction, or active infections.
- Pretreatment with antiemetics (e.g., ondansetron, dolasetron) is highly recommended due to severe GI toxicity.
- Pretreatment with dexamethasone and/or butorphanol may reduce vasospasm, phlebitis, and pain during infusion.
- Human Safety: Chronic exposure increases mutagenic, teratogenic, and carcinogenic risks. Proper hazardous drug handling precautions are mandatory.
藥物相互作用
May cause additive myelosuppression when used concurrently with DTIC.
May increase the hepatic metabolism of DTIC.
May increase the hepatic metabolism of DTIC.
May increase the hepatic metabolism of DTIC.
Additive bone marrow suppression
監測
- Efficacy (tumor response)
- CBC with differential and platelets (monitor for myelosuppression)
- Renal function tests
- Hepatic function tests
- IV catheter site for signs of extravasation during infusion
- Complete Blood Count (CBC) prior to each dose and at nadir (typically 7-14 days post-treatment)
- Liver function tests (ALT, AST, Bilirubin)
- Gastrointestinal signs (vomiting, diarrhea)
藥物動力學
半衰期
吸收
Poorly absorbed from the GI tract; must be administered intravenously.
分佈
Slightly bound to plasma proteins and probably concentrates in the liver. Only limited amounts cross the blood-brain barrier. It crosses the placenta.
代謝
Extensively metabolized in the liver to its active form.
排除
Excreted in the urine via tubular secretion.
過量
Because of the severe toxic potential of this agent, iatrogenic overdoses must be strictly avoided. Recheck all dosage calculations carefully (ensure dosing is based on body surface area in mg/m2, not mg/kg). Overdose will likely result in profound, life-threatening bone marrow suppression and severe gastrointestinal toxicity. Treatment is supportive.
可用產品
劑型
- Powder for injection
- 100 mg powder for reconstitution
- 200 mg powder for reconstitution
- 500 mg powder for reconstitution
人用標示
- Dacarbazine Powder for Injection: 100 mg & 200 mg vials (may contain mannitol)
- Dacarbazine 100mg, 200mg, 500mg, 1000mg powder for solution for injection/infusion
各地核准狀態
Human approved drug used off-label under the cascade.
POM. Human approved drug used off-label under the cascade.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Protect powder from light and keep refrigerated. If exposed to heat, the powder may change color from ivory to pink, indicating decomposition. After reconstituting with sterile water, the solution is stable for up to 72 hours refrigerated, or 8 hours at room temperature. If further diluted (up to 500 mL) with D5W or normal saline, it is stable for at least 24 hours refrigerated, or 8 hours at room temperature under normal lighting.
飼主須知
您的寵物已被處方一種化學治療藥物。請遵守以下指引：
- 腸胃不適： 嘔吐、腹瀉和食慾不振是常見的副作用。您的獸醫可能會開立止吐藥物，讓您在治療前後給予寵物。如果嘔吐或腹瀉嚴重，或排泄物中帶血，請立即聯繫您的獸醫。
- 感染風險： 此藥物會降低寵物的白血球數量，使其更容易受到感染。請密切注意寵物是否有嗜睡、發燒或精神沉鬱的跡象。
- 出血風險： 請注意是否有異常出血、瘀傷，或尿液/糞便中帶血的情況，因為此藥物會降低血小板數量。
- 安全預防措施： 化療藥物具有危險性。在治療後的幾天內，請遵循獸醫的指示安全處理寵物的排泄物（尿液、糞便、嘔吐物）。孕婦、哺乳期婦女及免疫力低下者應避免接觸寵物的排泄物。
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