吉西他濱
Gemcitabine
2,2'-difluorodeoxycytidine hydrochloride
別名: Gemzar · Abine · Antoril · Gemcite · Gemtrol · dFdC · LY-288022 · 2,2'-diflurodeoxycytidine · Gemcitabina · Gemcitabinum
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Carcinomas (in combination with carboplatin) | 2 mg/kg IV over 20-30 minutes | IV | no more than once every 7 days | — | 🌎 NA |
| Bladder urothelial carcinoma, lymphoma, and various carcinomas (High dose) | 800-900 mg/m2 | IV | every 7-14 days | for 4 doses | 🌍 EU |
| Bladder urothelial carcinoma, lymphoma, and various carcinomas (Low dose) | 25-50 mg/m2 | IV | once or twice a week | — | 🌍 EU |
| Carcinomas (Combination therapy) | 2 mg/kg | IV | every 7 days | — | 🌍 EU |
| Advanced solid tumors | Escalating doses per protocol | IV | single administration or per protocol | — | 🌍 EU |
- Carcinomas (in combination with carboplatin): Doses have ranged widely from 45 mg/m2-800 mg/m2 depending on the study.
- Bladder urothelial carcinoma, lymphoma, and various carcinomas (High dose): Administer over 20-60 minutes.
- Bladder urothelial carcinoma, lymphoma, and various carcinomas (Low dose): Administer over 20-60 minutes as per protocols.
- Carcinomas (Combination therapy): Administer over 20-30 minutes (in 0.9% NaCl) combined with carboplatin.
- Advanced solid tumors: Phase 1 dose-escalation trial.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Carcinomas (in combination with carboplatin) | 2 mg/kg IV over 20-30 minutes | IV | no more than once every 7 days | — | 🌎 NA |
| Exocrine pancreatic carcinoma (Low dose) | 20-25 mg/m2 or 2 mg/kg | IV | every 7 days | — | 🌍 EU |
- Carcinomas (in combination with carboplatin): Doses have ranged widely from 45 mg/m2-800 mg/m2 depending on the study.
- Exocrine pancreatic carcinoma (Low dose): Administer as a 20 minute IV infusion.
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
吉西他濱 (Gemcitabine) 是一種合成的嘧啶核苷類似物，作為抗腫瘤藥物使用。
- 獸醫用途：目前被視為試驗性療法，臨床數據有限。它具有作為無法切除腫瘤的放射增敏劑的潛力，或作為聯合化療方案（例如與卡鉑合用）的一部分。
- 人類用途：對治療胰腺癌、小細胞肺癌、膀胱癌、軟組織癌以及淋巴瘤具有療效。
臨床提示：由於其成本高昂且具有顯著的骨髓抑制潛力，在獸醫學中的應用通常僅限於專業的腫瘤科門診。
作用機轉
Gemcitabine is a cell-cycle phase-specific antimetabolite that acts primarily during the S phase (DNA synthesis) and blocks progression through the G1/S-phase boundary.
- It is transported intracellularly and phosphorylated to dFdCMP, then to active diphosphate (dFdCDP) and triphosphate (dFdCTP) metabolites.
- dFdCDP inhibits ribonucleotide reductase, depleting the cellular pool of deoxynucleotides required for DNA synthesis.
- dFdCTP competes with endogenous deoxycytidine triphosphate (dCTP) for incorporation into the elongating DNA strand. Once incorporated, it causes DNA chain termination and subsequent apoptosis.
安全性與警告
禁忌症
- Known hypersensitivity to gemcitabine
- Pre-existing bone marrow suppression
不良反應
- Myelosuppression (neutropenia and thrombocytopenia; nadir at 3-7 days)
- Mild to moderate gastrointestinal toxicity
- Retinal hemorrhage
- Myelosuppression (neutropenia, thrombocytopenia, anemia)
- Gastrointestinal toxicity (vomiting, diarrhea, anorexia)
- Retinal haemorrhage
- Treatment-related mortality (due to severe complications)
注意事項
Use with caution in patients with diminished renal or hepatic function. FDA Category D for pregnancy (evidence of fetal risk). Handle with standard cytotoxic safety precautions.
藥物交互作用
Additive toxic effects (myelosuppression, GI toxicity)
監測
- CBC before each treatment
- Fundic exam weekly while on therapy
- Baseline renal and hepatic function prior to therapy, and periodically thereafter
- Complete Blood Count (CBC) prior to each dose (monitor for myelosuppression)
- Hepatic function panel
- Renal function panel
- Gastrointestinal signs (vomiting, diarrhea, anorexia)
- Ophthalmic exam (monitor for retinal haemorrhage)
藥物動力學
半衰期
吸收
Administered intravenously.
分佈
Volume of distribution (steady-state) in dogs is around 1 L/kg. In humans, protein binding is negligible.
代謝
Metabolized intracellularly to active diphosphate and triphosphate forms. The primary inactive metabolite is uracil.
排除
Exhibits first-order elimination. Approximately 80% of the drug is excreted in the urine within 24 hours of dosing, primarily as the uracil metabolite.
過量
There is no known antidote to gemcitabine in an overdose situation. Severe myelosuppression should be expected. Treatment is supportive.
可用產品
劑型
- Lyophilized powder for injection
- Injectable: Lyophilized powder for reconstitution (200 mg in 10 ml vials)
- Injectable: Lyophilized powder for reconstitution (1 g in 50 ml vials)
人用標示
- Gemcitabine HCl lyophilized Powder for Injection: 200 mg (in 10 mL single-use vials) and 1 g (in 50 mL single-use vials) (Gemzar)
- Gemzar 200 mg lyophilized powder for injection
- Gemzar 1 g lyophilized powder for injection
各地核准狀態
Human authorized product used off-label under the cascade (POM).
Human authorized product used off-label under the cascade (POM).
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store unreconstituted vials at controlled room temperature (20-25°C). Reconstitute with preservative-free 0.9% sodium chloride. Reconstituted solution is stable for 24 hours at room temperature, or 7 days when frozen at -20°C. Do not refrigerate as crystallization may occur. Maximum concentration should not exceed 40 mg/mL.
飼主須知
- 試驗性療法：請理解獸醫界對此藥物的經驗有限，通常在標準療法無效時才會使用。
- 安全預防措施：吉西他濱是一種危險的化療藥物。治療後長達7天內，寵物的尿液中仍可檢測到藥物殘留。
- 清理尿液、糞便或嘔吐物時，請務必戴上拋棄式手套。
- 監測：您的寵物需要頻繁進行血液檢查 (CBC) 以監測白血球和血小板數量，因為此藥物會抑制骨髓。請密切觀察寵物是否有嗜睡、瘀傷或腸胃不適的跡象。
VetSheet 藥物參考供合格獸醫專業人員作臨床決策輔助之用，不能取代專業判斷或廠商最新仿單。