丙卡巴肼
Procarbazine
Procarbazine hydrochloride
別名: Matulane · Natulanar · Ibenzemethyzin · NSC-77213 · Ro-46467/1 · MIH · N-Methylhydrazine
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 |
|---|---|---|---|---|---|
| Lymphoma rescue (MOPP protocol) | 50 mg/m2 | PO | once daily for the first 14 days of the treatment cycle | 14 days | 🌎 NA |
| Granulomatous meningoencephalitis (GME) | 25-50 mg/m2 | PO | once daily initially, then every other day | — | 🌎 NA |
- Lymphoma rescue (MOPP protocol): Used as part of a protocol in combination with other antineoplastic agents.
- Granulomatous meningoencephalitis (GME): Initially given with prednisone treatment. After the first month, attempt to reduce to every other day. Monitor CBC weekly for the first month.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| MOPP lymphoma rescue | 50 mg/m2 or 10 mg (total dose per cat) | PO | once daily for the first 14 days of the treatment cycle | 14 days | 🌎 NA |
- MOPP lymphoma rescue: Used as part of a protocol in combination with other antineoplastic agents.
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
丙卡巴肼 (Procarbazine) 是一種非典型的烷化抗腫瘤藥物，在獸醫學中主要作為 MOPP 或 LOPP 化療方案的一部分，用於治療犬貓的復發性或抗藥性淋巴瘤。
臨床要點：與許多其他化療藥物不同，丙卡巴肼具有高度脂溶性，能輕易穿透血腦屏障 (BBB)。這項獨特屬性使其在治療中樞神經系統 (CNS) 腫瘤和發炎性疾病（尤其是犬的肉芽腫性腦膜腦炎, GME）方面具有極高的療效。
此外，丙卡巴肼具有微弱的單胺氧化酶抑制劑 (MAOI) 活性，因此在與其他藥物（如三環類抗憂鬱藥、擬交感神經藥）或特定飲食（富含酪胺的食物）併用時必須嚴格謹慎，以防止引發高血壓危象。
作用機制
Procarbazine is a prodrug that requires hepatic and renal metabolism to become active. Its exact mechanism is complex and multifaceted:
- Hepatic Metabolism → Procarbazine is oxidized to azo-procarbazine and further metabolized to yield methyl radicals and hydrogen peroxide.
- DNA Alkylation → The methyl radicals directly methylate nucleic acids, causing DNA strand breakage and inhibiting the synthesis of DNA, RNA, and proteins.
- Oxidative Stress → The auto-oxidation process generates hydrogen peroxide, which directly induces oxidative damage to DNA.
- MAO Inhibition → As an off-target effect, it inhibits the enzyme monoamine oxidase (MAO), preventing the breakdown of monoamines like serotonin, norepinephrine, and dopamine.
安全性與警告
禁忌症
- Known hypersensitivity to procarbazine
- Inadequate bone marrow reserve
不良反應
- Nausea and vomiting
- Hepatotoxicity
- Myelosuppression (thrombocytopenia, leukopenia)
- Hemorrhagic gastritis
- CNS effects (sedation, agitation)
- Peripheral neuropathy (loss of tendon reflexes, paresthesias, myalgia)
注意事項
Hazardous Drug: Procarbazine is a cytotoxic agent and a known teratogen (FDA Category D). Strict safe handling protocols must be followed by both veterinary staff and pet owners.
- Use with extreme caution in patients with impaired renal or hepatic function.
- Use with extreme caution when co-administering with other CNS depressant drugs.
- Because it is often used in combination protocols (e.g., MOPP), myelosuppression and GI effects may be significantly enhanced.
藥物相互作用
May cause severe nausea and vomiting (disulfiram-like reaction).
Procarbazine can cause CNS depression; concurrent use can lead to severe depression. Coma and death have been reported with opiates.
Serious hypertension may result due to procarbazine's MAOI activity.
Serious hypertension may result due to procarbazine's MAOI activity.
Do not use concurrently due to MAOI activity; risk of serotonin syndrome or hypertensive crisis.
監測
- Baseline: CBC, hepatic and renal function, urinalysis
- Repeat CBC at least once weekly for the first month of treatment, and then monthly thereafter
- Monitor for signs of neurotoxicity or severe GI distress
藥物動力學
吸收
Well absorbed after oral administration.
分佈
Rapidly equilibrates between the CSF and plasma. Peak levels in plasma occur in about 1 hour; in the CSF, about 30-90 minutes after dosing.
代謝
Almost entirely metabolized in the liver and kidney into cytotoxic products.
排除
Metabolic products are excreted in the urine.
過量
The LD50 for laboratory animals ranges from 150 mg/kg (rabbits) to 1.3 grams/kg (mice).
- Treatment: Treat overdoses aggressively to remove the drug from the gut if the overdose occurred within an hour or two (e.g., induction of emesis, activated charcoal).
- Anticipated Effects: Extensions of the drug's adverse effect profile, including severe GI distress, profound bone marrow suppression, and CNS effects.
- Management: Monitor closely and provide supportive care as necessary. Contact an animal poison control center for further guidance.
可用產品
劑型
- Capsules: 50 mg
- Compounded oral suspension (oil-based)
人用標示
- Procarbazine HCl Capsules: 50 mg (Matulane)
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store capsules in airtight containers, protected from light at temperatures less than 40°C (preferably between 15-30°C / 59-86°F). Compounded oil-based solutions (e.g., using sesame oil and silica gel) are typically assigned an expiration date of 30 days.
飼主須知
重要的安全警告：丙卡巴肼是一種化療藥物。在家中必須採取嚴格的安全措施，以保護人類家庭成員的健康。
- 安全處理：處理此藥物時請務必戴上拋棄式手套。給藥後請徹底洗手。
- 廢棄物管理：給藥後的數天內，請避免直接接觸寵物的唾液、嘔吐物、尿液或糞便。清理排泄物時請戴上手套，並將廢棄物密封於塑膠袋中丟棄。
- 何時聯繫獸醫：如果您的寵物出現中毒跡象，包括嘔吐、食慾不振、腹瀉、異常出血或瘀傷、嚴重抑鬱、焦躁不安、口腔潰瘍或跛行，請立即聯繫您的獸醫。
- 懷孕警告：孕婦、哺乳期婦女及準備懷孕的人士應避免接觸此藥物。
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