多拉司瓊
Dolasetron
Dolasetron mesylate
別名: Anzemet · Anemet · Zamanon · Dolasetron mesylate · Hydrodolasetron · Reduced dolasetron
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 |
|---|---|---|---|---|---|
| Anti-emetic, particularly for patients receiving chemotherapeutics | 0.6 mg/kg IV once daily | IV | q24h | — | 🌎 NA |
| General anti-emetic | 0.6 mg/kg IV q24h or 0.5 mg/kg PO, SC or IV q24h | IV/PO/SC | q24h | — | 🌎 NA |
| Vomiting disorders | 0.6-1 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Prevent vomiting | 0.6 mg/kg IV or PO once daily | IV/PO | q24h | — | 🌎 NA |
| Treat vomiting | 1 mg/kg PO or IV once daily | PO/IV | q24h | — | 🌎 NA |
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Anti-emetic, particularly for patients receiving chemotherapeutics | 0.6 mg/kg IV once daily | IV | q24h | — | 🌎 NA |
| Vomiting disorders | 0.6-1 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Prevent vomiting | 0.6 mg/kg IV or PO once daily | IV/PO | q24h | — | 🌎 NA |
| Treat vomiting | 1 mg/kg PO or IV once daily | PO/IV | q24h | — | 🌎 NA |
| General anti-emetic | 0.6 mg/kg IV q12h or 0.6-1 mg/kg PO q12h | IV/PO | q12h | — | 🌎 NA |
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
多拉司瓊是一種強效的 5-HT3 受體拮抗劑，在獸醫學中主要作為止吐藥使用。它對於控制犬貓因癌症化療引起的嚴重噁心和嘔吐特別有效。
- 給藥便利性：與通常需要每日多次給藥的昂丹司瓊 (ondansetron) 不同，多拉司瓊通常只需每日一次給藥。
- 劑型挑戰：雖然注射劑型在醫院內使用非常方便，但市售的人用口服錠劑（50 毫克和 100 毫克）對於大多數小動物來說太大，無法直接投藥。因此，口服使用通常需要經過藥物調劑 (compounding)。
臨床要點：由於成本和劑型的限制，常規門診通常更傾向於使用馬羅匹坦 (maropitant) 或昂丹司瓊等其他止吐藥，而將多拉司瓊保留用於難治性病例或特定的化療療程。
作用機制
Dolasetron exerts its anti-nausea and antiemetic effects by selectively antagonizing 5-hydroxytryptamine 3 (5-HT3) receptors.
- Peripheral Pathway: Chemotherapy and severe GI insults cause the release of serotonin from mucosal enterochromaffin cells in the small intestine. Serotonin binds to 5-HT3 receptors on vagal afferent nerve terminals, sending emetogenic signals to the brain. Dolasetron blocks this interaction.
- Central Pathway: Dolasetron also blocks 5-HT3 receptors located directly within the Chemoreceptor Trigger Zone (CRTZ) in the central nervous system.
Once administered, dolasetron is rapidly converted by carbonyl reductase into its active metabolite, hydrodolasetron, which is primarily responsible for the pharmacological effects.
安全性與警告
禁忌症
- Known hypersensitivity to dolasetron
- Atrioventricular (AV) block II to III
- Markedly prolonged QTc interval
不良反應
- Dose-related ECG interval prolongation (PR, QTc, JT prolongation, and QRS widening)
- Headache (reported in humans)
- Dizziness (reported in humans)
注意事項
Use with extreme caution in patients susceptible to cardiac conduction interval prolongation. This includes patients with hypokalemia, hypomagnesemia, congenital QT syndrome, those receiving anti-arrhythmic drugs or diuretics that induce electrolyte abnormalities, or those who have received a cumulative high dose of anthracycline chemotherapy. Note that 5-HT3 antagonists are generally ineffective for vomiting associated with feline hepatic lipidosis or mechanical GI obstruction.
藥物相互作用
May reduce the clearance and increase blood levels of hydrodolasetron
May reduce the clearance and increase blood levels of hydrodolasetron
May reduce the clearance and increase blood levels of hydrodolasetron
Can reduce hydrodolasetron blood levels
Can reduce hydrodolasetron blood levels
監測
- Efficacy (resolution of nausea and vomiting)
- Heart rhythm (ECG) in at-risk patients (e.g., those with electrolyte imbalances or on arrhythmogenic drugs)
藥物動力學
半衰期
吸收
Rapidly absorbed after oral administration. In humans, oral bioavailability is approximately 75%.
分佈
In dogs, the volume of distribution for the active metabolite (hydrodolasetron) is 8.5 L/kg.
代謝
Rapidly reduced via carbonyl reductase to hydrodolasetron (reduced dolasetron), which is the primary active compound. Partially metabolized in the liver.
排除
In dogs, total body clearance is 25 mL/min/kg. In humans, 50-60% is excreted unchanged into the urine. Clearance may be reduced in severe renal or hepatic impairment.
過量
Data on overdosage is very limited.
- Clinical Signs: In humans, a massive overdose (13 mg/kg) resulted in severe hypotension and dizziness.
- Treatment: Manage overdoses with supportive therapy, including IV fluids and pressors if hypotension occurs.
- Toxicity: Lethal intravenous doses in mice and rats were 160 mg/kg and 140 mg/kg, respectively.
可用產品
劑型
- Tablets
- Injection
人用標示
- Dolasetron Tablets: 50 mg & 100 mg (Anzemet)
- Dolasetron Injection: 20 mg/mL in ampules and vials (Anzemet)
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
Tablets should be stored at room temperature 20-25°C (68-77°F) and protected from light. Injection should be stored at room temperature 20-25°C (68-77°F) with excursions permitted to 15-30°C (59-86°F); protect from light. After dilution in compatible IV fluids, the injectable is stable under normal lighting at room temperature for 24 hours, or 48 hours if refrigerated.
飼主須知
什麼是多拉司瓊？ 多拉司瓊是一種強效的止吐藥物，最常用於預防或治療寵物因化療引起的嚴重嘔吐。
- 給藥方式：注射劑型通常由獸醫師在診所內施打。如果您需要在家中給予口服藥物，通常會由藥局進行特殊調劑（重新製成較小的藥丸或藥水），因為標準的人用藥錠對犬貓來說太大了。
- 副作用：寵物通常對此藥物耐受性良好。
- 何時應聯繫獸醫師：如果您的寵物在服藥後仍然持續嘔吐，或者您發現寵物出現極度嗜睡、虛弱或倒下的情況，請立即聯繫您的獸醫師。
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