アグレプリストン
Aglepristone
RU-534
別名: Alizine · RU-534 · RU46534 · RU-46534
VetSheet 獣医チームが監修更新日 2026年4月5日エビデンスに基づく獣医学リファレンス
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
動物種別用量
🌎 NA — North America🌍 EU — Europe
犬
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
用量は獣医専門家向けの臨床参考資料です。必ず最新の医薬品情報および個別症例に基づいて確認してください。
概要
アグレプリストンは、プロゲステロン受容体拮抗薬として作用する合成ステロイドです。主に獣医療において、犬や猫の妊娠中絶、および子宮蓄膿症や猫の線維腺腫性乳腺過形成の内科的治療に使用されます。
油・アルコールベースの製剤であるため、局所的な注射部位反応がよく見られます。
臨床のポイント: 競合的拮抗薬であるため、血中の内因性プロゲステロン濃度を低下させるのではなく、受容体レベルで直接その生物学的作用を阻害します。
作用機序
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・警告
禁忌
- 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
有害事象
- 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.
医薬品相互作用
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)
監視
- 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)
薬物動態
半減期
吸収
In dogs, after injecting two doses of 10 mg/kg 24 hours apart, peak serum levels occur about 2.5 days later.
分布
Highly lipophilic, distributes widely into tissues.
代謝
Hepatic metabolism is likely, given potential interactions with CYP450 inhibitors like ketoconazole.
消失
The majority (90%) of the drug is excreted via the feces.
過剰投与
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.
製品
製剤
- Injectable solution (30 mg/mL)
動物用医薬品
- Aglepristone 30 mg/mL in 5 mL & 10 mL vials (Alizine® or Alizin®)
規制ステータス
Authorized in multiple EU member states.
POM-V classification.
規制データなし: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
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.
飼主向け情報
- 獣医師による投与のみ: 誤って人体に注射した場合の重大なリスクがあるため、本製品の取り扱いおよび投与は獣医療従事者のみが行う必要があります。
- 妊娠中絶: 母犬の妊娠中絶に使用する場合、交配後26〜45日の使用での有効性は約95%であることをご理解ください。
- 膣分泌物: 胎児排出の約24時間前に、茶色の粘液性膣分泌物が見られることがあります。
- 副作用: 治療後、ペットに食欲不振、興奮、落ち着きのなさ、沈鬱、嘔吐、下痢などの症状が現れることがあります。
- 獣医師への連絡の目安: 治療後に化膿性または出血性の分泌物が見られる場合、または膣分泌物が3週間以上続く場合は、獣医師にご連絡ください。
- 子宮蓄膿症の治療: 子宮蓄膿症の治療に使用する場合、治療が失敗するリスクが十分にあり、最終的に外科手術（卵巣子宮摘出術）が必要になる可能性があります。
VetSheet医薬品リファレンスは獣医専門家の臨床意思決定支援を目的としており、専門的判断または製造業者の最新医薬品情報の代替にはなりません。