塞替派
Thiotepa
Triethylenethiophosphoramide
別名: Thioplex · Ledertepa · Onco Tiotepa · Tespamin · NSC-6396 · thiophosphamide · triethylenethiophosphoramide · TSPA · WR-45312
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 |
|---|---|---|---|---|---|
| Intracavitary use for neoplastic effusions or systemically for adjunctive therapy of carcinomas | 0.2-0.5 mg/m 2 | intracavitary; IV | Not specified | Not specified | 🌎 NA |
- Intracavitary use for neoplastic effusions or systemically for adjunctive therapy of carcinomas: Consultation with a veterinary oncologist and referral to current veterinary oncology references are strongly recommended.
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
塞替派（Thiotepa）是一種強效、非細胞週期特異性的烷化劑類抗腫瘤藥物。
在獸醫學中，主要用於：
- 體腔內灌注以控制惡性腫瘤積液（如胸腔或腹腔積液）。
- 膀胱內灌注治療膀胱移行細胞癌（儘管研究指出其療效明顯低於全身性阿黴素/環磷醯胺療程）。
- 作為多種癌瘤的全身性輔助治療。
臨床要點： 塞替派的治療指數非常狹窄。由於其為危險的細胞毒性藥物，必須嚴格遵守安全操作規範（例如使用生物安全櫃、封閉式傳輸系統及適當的個人防護裝備），以保護獸醫人員免受致突變和致畸胎風險。
作用機制
Thiotepa acts as a polyfunctional alkylating agent.
- Mechanism: It undergoes conversion to its active metabolite, TEPA, which directly cross-links DNA strands by binding to guanine bases.
- Pathway: DNA cross-linking → interference with DNA replication and RNA transcription → cell cycle arrest and apoptosis.
- Specificity: It is cell-cycle non-specific, meaning it exerts cytotoxic effects on both resting and actively dividing cells.
- When administered via the intracavitary route, it is believed to control malignant effusions through a direct, localized antineoplastic effect on the serosal surfaces.
安全性與警告
禁忌症
- Hypersensitivity to thiotepa
- Pregnancy (teratogenic and mutagenic - FDA Category D)
不良反應
- Leukopenia (most common)
- Thrombocytopenia
- Anemia
- Pancytopenia
- Vomiting
- Diarrhea
- Stomatitis
- Intestinal ulceration
- Dizziness (reported in humans)
- Headache (reported in humans)
注意事項
WARNING: Thiotepa has a very low therapeutic index and should only be administered by clinicians experienced with cytotoxic agents.
- Organ Dysfunction: Use with extreme caution in patients with hepatic dysfunction or renal function impairment (dosage adjustment may be necessary).
- Bone Marrow: Weigh risks vs. benefits in patients with pre-existing bone marrow depression, active infections, or tumor cell infiltration of the bone marrow.
- Urolithiasis: Use cautiously in patients with a history of urate urinary stones, as thiotepa may increase serum uric acid levels.
- Nursing: It is unknown if thiotepa enters maternal milk; use of a milk replacer is strongly recommended for nursing bitches or queens.
藥物相互作用
May increase the risk of severe infections due to additive immunosuppression.
Extreme caution required; bone marrow depression may be additive and lead to severe pancytopenia.
Increased risk of vaccine-induced infection or reduced vaccine efficacy; use with extreme caution, if at all.
監測
- Clinical efficacy (tumor response or reduction in effusion)
- CBC with platelets (monitor closely for myelosuppression)
- Serum uric acid levels
藥物動力學
吸收
Poorly absorbed from the GI tract. Systemic absorption is variable from the pleural cavity, bladder, and after IM injection. Absorption from bladder mucosa ranges from 10-100% of an administered dose.
分佈
Distribution characteristics are not well described; it is unknown if the drug enters maternal milk.
代謝
Extensively metabolized in the liver (primarily to its active metabolite, TEPA).
排除
Excreted primarily in the urine.
過量
There is no specific antidote for a thiotepa overdose.
Treatment is primarily supportive and symptomatic. If severe hematologic toxicity (profound myelosuppression) occurs, aggressive supportive therapy is required, which may include transfusions of appropriate blood products, broad-spectrum prophylactic antibiotics, and isolation to prevent secondary infections.
可用產品
劑型
- Lyophilized Powder for Injection: 15 mg, 30 mg
人用標示
- Thiotepa Lyophilized Powder for Injection: 15 mg & 30 mg in vials (Thioplex, generic)
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 both the powder and the reconstituted solution refrigerated (2-8°C) and protected from light. Do not use solution that is grossly opaque (slightly opaque is OK) or if a precipitate is present. If refrigerated, reconstituted solutions are stable for up to 5 days.
飼主須知
您的寵物已被處方一種強效的化療藥物。請仔細閱讀以下資訊：
- 毒性風險： 此藥物可能引起嚴重的副作用，包括白血球下降（增加感染風險）、紅血球下降（貧血）和血小板下降（出血風險）。在罕見情況下，化療可能引發繼發性腫瘤或危及生命。
- 何時應聯繫獸醫： 如果您的寵物出現異常出血、瘀傷、食慾不振、嘔吐、眼睛/皮膚發黃（黃疸）或感染跡象（如發燒或極度嗜睡），請立即聯繫您的獸醫。
- 居家安全操作： 由於這是一種危險藥物，治療後幾天內，您寵物的體液（尿液、糞便、嘔吐物）中可能含有微量藥物。清理排泄物時請戴上一次性手套，事後徹底洗手。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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