己烯雌酚
Diethylstilbestrol
別名: Apstil · Destilbenol · Distilbene · diethylstilbestrolum · diethylstilboestrol · NSC-3070
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 |
|---|---|---|---|---|---|
| Primary sphincter mechanism incompetence (Option A) | 0.1-1 mg (total dose) per dog PO for 5 days followed by maintenance of 1 mg/week or a maximum of 0.1 mg/kg/week. Minimum effective dose should be used for maintenance. Do NOT give more than recommended. | PO | Once daily for 5 days, then weekly | Long-term maintenance | 🌎 NA |
| Primary sphincter mechanism incompetence (Option B - females) | 0.1-1 mg (total dose) PO once daily for 5 days, then 1 mg once a week | PO | Once daily for 5 days, then weekly | Long-term maintenance | 🌎 NA |
| Primary sphincter mechanism incompetence (Option C) | 0.5-1 mg (0.02 mg/kg; maximum dose of 1 mg) for 3-5 days as an induction dose and then periodically decreased to every other day and then to the lowest dose that will maintain continence. | PO | Daily initially, then tapered | Long-term maintenance | 🌎 NA |
| Estrus induction | DES at 5 mg/day for a tentative 7 days. The first day of vulvar swelling is designated as Day 1. Continue DES on DAY 1 and Day 2. If no effect is seen in 7 days, give DES at 10 mg/day for another tentative 7 days. If vulvar swelling and bleeding detected, DES is continued on Day 1 and Day 2. If no effect seen in these 14 days, discontinue and restart in 30 days. Once proestrus initiated, on Day 5 give 5 mg of Luteinizing hormone (LH) if obtainable. If LH unavailable, give GnRH 3.3 micrograms/kg IM and FSH 10 mg IM in its place. Bitch is bred on Day 13. | PO | Daily | 7-14 days | 🌎 NA |
| Benign prostatic hypertrophy | 0.2-1 mg total dose PO for 5 days | PO | Daily | 5 days | 🌎 NA |
- Primary sphincter mechanism incompetence (Option A): As an alternative to phenylpropanolamine.
- Primary sphincter mechanism incompetence (Option C): In difficult cases, may be used with phenylpropanolamine. Note: Conjugated estrogens (e.g., Premarin) are sometimes used as a substitute (e.g., 20 mcg/kg PO every 4 days).
- Estrus induction: Adjust dosages of LH and FSH for animal size-the above dosages are for a dog weighing 50-60 lbs.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Estrogen-responsive incontinence (females) | 0.1-1 mg (total dose) PO once daily for 5 days, then 1 mg once a week | PO | Once daily for 5 days, then weekly | Long-term maintenance | 🌎 NA |
- Estrogen-responsive incontinence (females): Doses of 2.2 mg/kg per day have caused death in cats secondary to bone marrow toxicity.
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
己烯雌酚 (DES) 是一種合成的非類固醇雌激素，在獸醫學中主要用於治療已結紮母犬的雌激素反應性尿失禁。它也曾被用於公犬的良性前列腺肥大和誘導發情。
臨床要點： 由於具有嚴重的骨髓毒性（致命性再生不良性貧血）風險，且被歸類為潛在的致癌物和致畸胎物，DES 嚴禁使用於經濟動物。
基於人類健康考量和市場撤出，DES 目前在美國已無 FDA 核准的市售成藥，必須透過獸醫調劑藥局取得。在現代臨床實務中，通常更傾向使用較安全的替代藥物，如雌三醇 (Incurin) 或苯丙醇胺 (PPA) 作為括約肌機能不全的第一線治療。
作用機制
DES acts as a potent agonist at estrogen receptors (ER-α and ER-β). Upon binding, the receptor-ligand complex translocates to the cell nucleus, where it binds to estrogen response elements (EREs) on DNA, altering mRNA transcription and subsequent protein synthesis.
- Urinary Incontinence: Estrogens upregulate the expression and sensitivity of α-adrenergic receptors in the internal urethral sphincter. This increases the sphincter's responsiveness to endogenous norepinephrine, thereby increasing resting urethral closure pressure and preventing urine leakage.
- Reproductive/Systemic Effects: Promotes growth and development of female sex organs, increases cervical/vaginal mucosal thickness, and causes endometrial proliferation. It also accelerates epiphyseal closure, increases calcium deposition in bone, and inhibits pituitary gonadotropin release via negative feedback.
安全性與警告
禁忌症
- Food-producing animals (FDA prohibited)
- Pregnancy (teratogenic; causes fetal genitourinary malformations)
- Patients with preexisting anemias or leukopenias
- Females with estrogen-sensitive neoplasms
不良反應
- Bone marrow suppression (thrombocytopenia, leukopenia, fatal aplastic anemia)
- Cystic endometrial hyperplasia
- Pyometra (in intact females)
- Mammary neoplasia
- Feminization (in males)
- Signs of estrus (in females)
- Pancreatic, hepatic, and cardiac lesions (reported in cats)
- Malignant ovarian adenocarcinomas (experimental)
注意事項
WARNING: DES is strictly prohibited by the FDA for use in food animals due to carcinogenic potential.
- Bone Marrow Toxicity: Estrogens are toxic to the bone marrow in dogs and cats. Use with extreme caution in patients with preexisting hematologic abnormalities. Toxicity is dose-dependent and more common in older animals.
- Pyometra Risk: Can induce cystic endometrial hyperplasia and open-cervix pyometra in intact females 1-6 weeks after initiating therapy.
- Carcinogenicity: May induce mammary neoplasias and has been linked to malignant ovarian adenocarcinomas in experimental settings.
藥物相互作用
May increase estrogen levels
May decrease metabolism of estrogens
Enhanced glucocorticoid effects may result; estrogens may alter protein binding or decrease metabolism of corticosteroids
May decrease the metabolism of estrogens
Oral anticoagulant activity may be decreased; increases in anticoagulant dosage may be necessary
May decrease estrogen concentrations
May decrease estrogen concentrations
May induce hepatic microsomal enzymes and decrease estrogen levels
監測
- Packed Cell Volumes (PCV)
- White blood cell counts
- Platelet counts
- Liver function tests (at baseline, one month after therapy begins, and repeat 2 months after cessation if abnormal)
藥物動力學
吸收
Well absorbed from the GI tract of monogastric animals.
代謝
Slowly metabolized by the liver, primarily to a glucuronide form.
排除
Excreted in the urine and feces.
過量
Acute overdosage in humans with estrogens has resulted in nausea, vomiting, and withdrawal bleeding in females.
In veterinary patients, acute overdose information is limited, but chronic overdosage or high doses are well-documented to cause severe, potentially fatal bone marrow suppression (aplastic anemia, thrombocytopenia, neutropenia). Doses of 2.2 mg/kg per day have caused death in cats. Treatment of overdose should involve immediate discontinuation of the drug and aggressive supportive care (e.g., blood transfusions, broad-spectrum antibiotics for neutropenia).
可用產品
劑型
- Compounded oral capsules
- Compounded oral tablets
- Compounded oral suspensions
人用標示
- No commercially available regular oral DES products are available in the USA. Compounded preparations may be available from compounding pharmacies.
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
All commercially available DES tablets (plain tablets, enteric-coated tablets) should be stored at room temperature (15-30°C) in well-closed containers.
飼主須知
己烯雌酚 (DES) 是一種主要用於治療已結紮母犬尿失禁（漏尿）的荷爾蒙藥物。
- 嚴格遵照劑量： 務必完全按照獸醫師的處方給藥。給予超過建議的劑量可能會導致致命的骨髓疾病。
- 注意出血/感染跡象： 如果您發現寵物牙齦蒼白、不明原因的瘀傷、嗜睡、虛弱或發燒，請立即聯繫您的獸醫師。
- 注意子宮蓄膿跡象： 如果您的寵物是未結紮的母犬，請注意是否有過度飲水、頻尿或外陰部異常分泌物，這可能表示嚴重的子宮感染。
- 其他需報告的症狀： 腹瀉、嘔吐或出現「發情」跡象（外陰腫脹、出血）。
- 安全處理： 處理藥物後請洗手，並將藥物嚴格放置在兒童和其他寵物接觸不到的地方。
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