阿格列酮
Aglepristone
RU-534
別名: Alizine · RU-534 · RU46534 · RU-46534
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 |
|---|---|---|---|---|---|
| To terminate pregnancy (up to day 45) | 10 mg/kg (0.33 mL/kg) subcutaneous injection only. Repeat one time, 24 hours after the first injection. | SC | q24h | 2 doses | 🌎 NA |
| To induce parturition | At day 60 (post-estimated LH surge): 15 mg/kg SC and another dose 24 hours later. Subsequently, give oxytocin 0.15 Units/kg SC at hourly intervals until last pup is delivered. | SC | q24h | 2 doses | 🌎 NA |
| To induce parturition | On or after day 58 of pregnancy: 15 mg/kg subcutaneously; repeat in 9 hours. | SC | Repeat in 9 hours | 2 doses | 🌎 NA |
| As an adjunct to treating pyometra/metritis (preserve fertility) | Treatment begun at week 2-4 of diestrus with a single SC injection of aglepristone at 10 mg/kg. Doses are repeated at days 2, 7, and 14. | SC | Days 1, 2, 7, 14 | 14 days | 🌎 NA |
| For closed cervix pyometra | 6 mg/kg twice daily on the first day followed by the same dose once daily on days 2, 3, and 4. Some prefer using larger doses (10mg/kg) once daily on days 1, 3, and 8, then follow up also on days 15 and 28 depending on the bitch's condition. | SC | Variable | Variable | 🌎 NA |
| For metritis | 10 mg/kg subcutaneously once daily on days 1, 2 and 8. | SC | Days 1, 2, 8 | 8 days | 🌎 NA |
| For open or closed pyometra | aglepristone 10 mg/kg subcutaneously once daily on days 1, 2 and 8 and cloprostenol 1 microgram/kg subcutaneously on days 3 to 7. | SC | Days 1, 2, 8 | 8 days | 🌎 NA |
| For pyometra | 10 mg/kg SC on days 1, 2, 8, 15, & 29. Give misoprostol 10 micrograms/kg PO twice daily on days 3 through 12. | SC | Days 1, 2, 8, 15, 29 | 29 days | 🌎 NA |
| Pregnancy termination | 10 mg/kg | SC | q24h | 2 doses | 🌍 EU |
| Progesterone-induced acromegaly | 10 mg/kg | SC | q24h for 2 doses, then q7d | 5 doses total | 🌍 EU |
| Pyometra | 10 mg/kg | SC | Days 1, 2, and 7 | 3 doses (up to 5) | 🌍 EU |
- To terminate pregnancy (up to day 45): A maximum of 5 mL should be injected at any one site. Light massage of the injection site is recommended.
- To induce parturition: Additional studies confirming efficacy and safety are warranted before routine clinical application.
- To induce parturition: Expulsion of first pup occurred between 32 and 56 hours after treatment. Use standard protocols to assist with birth.
- As an adjunct to treating pyometra/metritis (preserve fertility): During first 7 days, daily injections of amoxicillin/clavulanic acid were also given.
- For open or closed pyometra: Bitches with closed pyometra or with elevated temperature/dehydration should also receive IV fluids and antibiotics. If unresolved, additional doses on days 14 and 28.
- For pyometra: Approximately 75% of cases show significant clinical improvement without developing adverse effects associated with prostaglandins.
- Pregnancy termination: Maximum of 5 ml injected at any one site.
- Progesterone-induced acromegaly: Maximum of 5 ml injected at any one site.
- Pyometra: Maximum of 5 ml injected at any one site. Additional doses may be given on days 14 and 21 if there is an inadequate response.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| For treating mammary fibroadenomatous hyperplasia | 20 mg/kg aglepristone subcutaneously once weekly until resolution of signs. | SC | q7d | Until resolution | 🌎 NA |
| For treating mammary fibroadenomatous hyperplasia | 10 mg/kg SC on two consecutive days, once weekly. | SC | Two consecutive days weekly | 3-5 weeks | 🌎 NA |
| To terminate pregnancy (up to day 45) | 15 mg/kg SC twice 24 hours apart. | SC | q24h | 2 doses | 🌎 NA |
| Pregnancy termination | 15 mg/kg | SC | q24h | 2 doses | 🌍 EU |
| Fibroadenomatous hyperplasia | 20 mg/kg | SC | q7d | Until resolution | 🌍 EU |
| Pyometra | 15 mg/kg | SC | Days 1, 2, and 7 | 3 doses (up to 5) | 🌍 EU |
- For treating mammary fibroadenomatous hyperplasia: Cats with HR > 200 BPM should receive atenolol at 6.25 mg (total dose) until HR < 200 BPM with regression in mammary gland size.
- For treating mammary fibroadenomatous hyperplasia: Complete regression occurs on average 3-4 weeks. Relapses can occur, particularly if treated with long-acting progestins; these cats should be treated for 5 weeks.
- To terminate pregnancy (up to day 45): Efficacy is 95% if administered before implantation, 85% if after implantation. Termination occurs within 3 days in 50% of queens.
- Pregnancy termination: Maximum of 5 ml injected at any one site.
- Fibroadenomatous hyperplasia: Maximum of 5 ml injected at any one site. Consider atenolol if cat is tachycardic with heart rate >200 bpm.
- Pyometra: Maximum of 5 ml injected at any one site. Additional doses may be given on days 14 and 21 if there is an inadequate response.
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
阿格列酮是一種合成類固醇，作為黃體素受體拮抗劑。主要用於獸醫學中犬貓的終止妊娠，以及內科治療子宮蓄膿和貓的纖維腺瘤性乳腺增生。
由於其基質為油醇混合物，局部注射部位反應相當常見。
臨床要點：作為競爭性拮抗劑，阿格列酮不會降低體內循環的黃體素濃度，而是直接在受體層次阻斷黃體素的生物學作用。
作用機制
Aglepristone competitively binds to progesterone (P4) receptors in the uterus and other target tissues.
- In dogs, its affinity for uterine progesterone receptors is ~3x that of endogenous progesterone; in queens, it is ~9x greater.
- Pathway: Aglepristone binding → blockade of progesterone signaling → withdrawal of pregnancy support → cervical dilation and resumption of myometrial contractility → fetal resorption or abortion (usually within 7 days).
- It also binds to glucocorticoid receptors acting as an antagonist, which can block endogenous or exogenously administered glucocorticoids from acting at these sites.
安全性與警告
禁忌症
- Known hypersensitivity to aglepristone
- Pregnancy (unless used specifically for pregnancy termination or inducing parturition)
- Hypoadrenocorticism (Addison's disease) or genetic predisposition to it
- Peritonitis (must be ruled out before using for pyometra)
- Caution in patients with poor health, diabetes, or impaired hepatic/renal function
不良反應
- Injection site reactions (pain, edema, skin thickening, ulceration, localized lymph node enlargement)
- Anorexia (25%)
- Excitation (23%)
- Depression (21%)
- Diarrhea (13%)
- Uterine infections (3.4%)
- Vomiting (2%)
- Brown mucoid vaginal discharge (associated with pregnancy termination)
- Mammary gland congestion
注意事項
WARNING: Accidental injection of this product can induce abortion; it should not be administered or handled by pregnant women. Accidental injection can also cause severe pain, intense swelling, and ischemic necrosis that can lead to serious sequelae, including loss of a digit. Seek prompt medical attention if accidentally injected.
- Injection Site Care: Light massage of the injection site is recommended after administration. Larger dogs should not receive more than 5 mL at any one SC injection site. Administering into the scruff of the neck may help avoid severe injection reactions.
- Pyometra: When used for pyometra, there is a substantial risk of treatment failure, and ovariohysterectomy may ultimately be required.
藥物相互作用
Could reduce the efficacy of aglepristone
Aglepristone could reduce the efficacy of glucocorticoid treatment due to receptor antagonism
May interact with aglepristone (manufacturer warning, likely due to CYP450 enzyme inhibition)
May interact with aglepristone (manufacturer warning)
May interact with aglepristone (manufacturer warning)
監測
- Clinical efficacy
- For pregnancy termination: ultrasound 10 days after treatment and at least 30 days after mating
- Injection site reactions (pain, swelling, ulceration)
- Systemic adverse effects (anorexia, excitation, depression, diarrhea)
藥物動力學
半衰期
吸收
In dogs, after injecting two doses of 10 mg/kg 24 hours apart, peak serum levels occur about 2.5 days later.
分佈
Highly lipophilic, distributes widely into tissues.
代謝
Hepatic metabolism is likely, given potential interactions with CYP450 inhibitors like ketoconazole.
排除
The majority (90%) of the drug is excreted via the feces.
過量
When administered at 3X (30 mg/kg) recommended doses, bitches demonstrated no untoward systemic effects. Localized reactions were noted at the injection site, presumably due to the larger volumes injected.
可用產品
劑型
- Injectable solution (30 mg/mL)
獸醫用
- Aglepristone 30 mg/mL in 5 mL & 10 mL vials (Alizine® or Alizin®)
各地核准狀態
Authorized in multiple EU member states.
POM-V classification.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Aglepristone injection should be stored below 25°C and protected from light. The manufacturer recommends using the product within 28 days of withdrawing the first dose. Due to the product's oil/alcohol vehicle formulation, it should not be mixed with any other medication.
飼主須知
- 僅限獸醫施打：由於意外注射人體會帶來嚴重風險，本產品僅限由獸醫專業人員操作與施打。
- 終止妊娠：用於母犬終止妊娠時，請了解在交配後第26至45天使用，成功率約為95%。
- 陰道分泌物：在胎兒排出前約24小時，可能會觀察到棕色黏液性陰道分泌物。
- 副作用：治療後，您的寵物可能出現食慾不振、興奮、焦躁或抑鬱、嘔吐或腹瀉等症狀。
- 何時應聯繫獸醫：若治療後出現化膿或出血性分泌物，或陰道分泌物持續超過3週，請立即聯繫您的獸醫師。
- 子宮蓄膿治療：用於治療子宮蓄膿時，存在相當的治療失敗風險，最終可能仍需進行外科手術（卵巢子宮摘除術/結紮）。
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