環戊丙酸雌二醇
Estradiol Cypionate
Estradiol cyclopentanepropionate
別名: Delestrogen · DepoEstradiol · Depogen · Dura-Estrin · ECP · E-Cypionate · Estra-D · Estrace · Estro-Cyp · Estroject · depGynogen · Femtrace · Gynodiol · beta-oestradiol · dihydrofolliculin · dihydrotheelin · dihydroxyoestrin · estradiolum · NSC-9895 · NSC-20293 · oestradiol cyclopentylpropionate · oestradiol cypionate
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 |
|---|---|---|---|---|---|
| Pregnancy avoidance after mismating | 44 micrograms/kg (0.044 mg/kg) IM once; during day 4 estrus to day 2 of diestrus | IM | once | — | 🌎 NA |
- Pregnancy avoidance after mismating: Rarely used for this indication today as there are safer, more effective treatments. Toxic at >=100 micrograms/kg.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Pregnancy avoidance after mismating | 250 micrograms/kg (0.25 mg/kg) IM once 6 days after coitus; or 0.25 mg/cat IM at 40 hours after coitus | IM | once | — | 🌎 NA |
- Pregnancy avoidance after mismating: Rarely used for this indication today as there are safer, more effective treatments.
馬
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| To enhance estrus behavior and receptivity in ovariectomized mares | 5-10 mg (total dose) IM once | IM | once | — | 🌎 NA |
| Treatment of mares with estrogen-responsive incontinence | 4-10 micrograms/kg estradiol cypionate IM daily for three days and then every other day | IM | daily then q48h | 3 days then ongoing | 🌎 NA |
- Treatment of mares with estrogen-responsive incontinence: Some mares will improve, but does not 'cure'.
牛
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Any | Illegal | — | — | — | 🌎 NA |
- Any: The FDA has stated that the use of ECP in food-producing animals is illegal.
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
環戊丙酸雌二醇（Estradiol Cypionate）是一種長效的天然雌激素酯類衍生物。過去常被用作小動物的墮胎藥（錯配後的避孕），但由於其具有引發致命性骨髓抑制（再生不良性貧血）及子宮蓄膿的高風險，目前多數獸醫繁殖學專家已不再推薦使用，臨床上多偏好更安全有效的替代方案。
臨床重點：美國FDA已明令禁止將此藥物用於產食動物，任何針對此類動物的給藥或調劑皆屬違法。
作用機制
Estradiol is the most active endogenous estrogen. It diffuses across the cell membrane and binds to specific intracellular estrogen receptors (ERα and ERβ).
The receptor-hormone complex translocates to the nucleus → binds to estrogen response elements (EREs) on DNA → modulates gene transcription.
Key systemic effects include:
- Reproductive: Stimulates normal growth and development of female sex organs, increases cervical mucosal secretions, thickens vaginal mucosa, and induces endometrial proliferation and uterine tone.
- Skeletal: Increases calcium deposition, accelerates epiphyseal closure, and promotes bone formation.
- Endocrine: Modulates pituitary gonadotropin release, which can inhibit lactation, ovulation, and androgen secretion.
安全性與警告
禁忌症
- Pregnancy (teratogenic and causes fetal bone marrow depression)
- Food-producing animals (illegal per FDA)
- Ferrets (highly susceptible to severe bone marrow toxicity)
- Estrogen-responsive incontinence in small animals (safer alternatives like DES or estriol should be used)
不良反應
- Bone marrow toxicity (thrombocytopenia, leukopenia, fatal aplastic anemia)
- Cystic endometrial hyperplasia
- Pyometra
- Mammary neoplasia
- Feminization (in males)
- Prolonged estrus (in females)
- Genital irritation (cattle)
- Decreased milk flow (cattle)
- Follicular cysts (cattle)
注意事項
Use with extreme caution in small animals due to the high risk of blood dyscrasias (bone marrow depression), which are more prevalent in older animals and at higher dosages. Toxicity can progress to fatal aplastic anemia.
In cows with a prolonged corpus luteum, rule out endometritis or pregnancy before use.
Do not use in ferrets due to extreme sensitivity to estrogen-induced bone marrow toxicity.
藥物相互作用
May increase estrogen levels due to CYP450 enzyme inhibition.
Enhanced glucocorticoid effects; estrogens may alter protein binding or decrease metabolism of corticosteroids.
May increase estrogen levels.
May decrease estrogen activity via hepatic enzyme induction.
May decrease estrogen activity via hepatic enzyme induction.
May decrease estrogen activity.
Oral anticoagulant activity may be decreased; dosage adjustments may be necessary.
監測
- Packed Cell Volumes (PCV)
- White blood cell counts (CBC)
- Platelet counts (Baseline, one month after therapy, and repeated two months after cessation if abnormal)
- Liver function tests
藥物動力學
吸收
Esterified estrogens (like estradiol cypionate) have delayed, prolonged absorption after IM administration in oil solutions.
分佈
Distributed throughout the body and accumulates in adipose tissue.
代謝
Principally metabolized by the liver.
排除
Primarily excreted in the urine, but also excreted into the bile where most is reabsorbed from the GI tract (enterohepatic recirculation).
過量
Acute overdosage reports in veterinary patients are rare, but chronic or high-dose exposure leads to severe adverse effects.
Overdose manifestations:
- Small Animals: Severe bone marrow depression (thrombocytopenia, leukopenia, aplastic anemia), cystic endometrial hyperplasia, and pyometra.
- Cattle: Prolonged estrus, genital irritation, decreased milk flow, precocious development, and follicular cysts.
Treatment is largely supportive. If bone marrow suppression occurs, aggressive supportive care (transfusions, broad-spectrum antibiotics) is required, though prognosis for aplastic anemia is poor.
可用產品
劑型
- Injection (oil solution)
- Tablets
- Implants (veterinary beef cattle)
獸醫用
- Estradiol-containing implants for use in beef cattle
人用標示
- Estradiol Cypionate in Oil for Injection: 5 mg/mL
- Estradiol Valerate in Oil for Injection: 10 mg/mL, 20 mg/mL & 40 mg/mL
- Estradiol Tablets: 0.45 mg, 0.5 mg, 0.9 mg, 1 mg, 1.5 mg, 1.8 mg & 2 mg micronized estradiol
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 in light-resistant containers at temperatures of less than 40°C, preferably at room temperature (15-30°C); avoid freezing. Do not mix with other medications.
飼主須知
- 極度危險警告：此藥物可能對貓狗的骨髓造成嚴重且有時是致命的損害，因此現今已極少使用。
- 如果您的寵物出現貧血或出血跡象，例如牙齦蒼白、異常瘀斑、皮膚出現紅色出血點或極度疲倦，請立即聯繫獸醫。
- 密切觀察是否有嚴重的子宮感染（子宮蓄膿）跡象，包括：飲水量異常增加、頻尿、精神沉鬱或陰道分泌物。這可能在治療後 1 到 6 週內發生。
- 絕對不可用於懷孕動物，會導致嚴重的胎兒畸形。
- 產食動物禁用：此藥物絕不能用於供人類食用的動物。
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