ジエチルスチルベストロール
Diethylstilbestrol
別名: Apstil · Destilbenol · Distilbene · diethylstilbestrolum · diethylstilboestrol · NSC-3070
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 |
|---|---|---|---|---|---|
| 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.
猫
| 適応 | 用量 | 経路 | 頻度 | 期間 | 地域 |
|---|---|---|---|---|---|
| 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.
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
ジエチルスチルベストロール（DES）は合成非ステロイド性エストロゲンであり、獣医療では主に避妊済み雌犬のエストロゲン反応性尿失禁の管理に使用されます。また、雄犬の良性前立腺肥大症や発情誘起にも使用されてきました。
臨床のポイント： 重篤な骨髄毒性（致命的な再生不良性貧血）のリスクがあり、潜在的な発がん性および催奇形性物質に分類されているため、産業動物への使用は厳格に禁止されています。
人間の健康への懸念と市場からの撤退により、DESはFDA承認の市販製品としては入手できなくなり、獣医用調剤薬局を通じて入手する必要があります。現代の臨床では、括約筋機能不全の第一選択薬として、エストリオール（Incurin）やフェニルプロパノールアミン（PPA）などのより安全な代替薬が好まれることが多くなっています。
作用機序
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・警告
禁忌
- Food-producing animals (FDA prohibited)
- Pregnancy (teratogenic; causes fetal genitourinary malformations)
- Patients with preexisting anemias or leukopenias
- Females with estrogen-sensitive neoplasms
有害事象
- 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.
医薬品相互作用
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
監視
- 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)
薬物動態
吸収
Well absorbed from the GI tract of monogastric animals.
代謝
Slowly metabolized by the liver, primarily to a glucuronide form.
消失
Excreted in the urine and feces.
過剰投与
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).
製品
製剤
- Compounded oral capsules
- Compounded oral tablets
- Compounded oral suspensions
ヒト用医薬品
- No commercially available regular oral DES products are available in the USA. Compounded preparations may be available from compounding pharmacies.
規制ステータス
規制データなし: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
保管・安定性
All commercially available DES tablets (plain tablets, enteric-coated tablets) should be stored at room temperature (15-30°C) in well-closed containers.
飼主向け情報
ジエチルスチルベストロール（DES）は、主に避妊済み雌犬の尿失禁（尿漏れ）を治療するために使用されるホルモン剤です。
- 厳格な用量遵守： 処方された通りに正確に投薬することが極めて重要です。推奨量を超えて与えると、致命的な骨髄疾患を引き起こす可能性があります。
- 出血/感染の兆候に注意： 歯茎の蒼白、原因不明のあざ、無気力、衰弱、または発熱に気づいた場合は、直ちに獣医師に連絡してください。
- 子宮蓄膿症の兆候に注意： ペットが避妊していない雌の場合、過剰な飲水、頻尿、または外陰部からの異常な分泌物に注意してください。これらは重篤な子宮感染症を示す可能性があります。
- その他の報告すべき症状： 下痢、嘔吐、または「発情」の兆候（外陰部の腫れ、出血）。
- 取り扱い： 薬を取り扱った後は手を洗い、子供や他のペットの手の届かない場所に厳重に保管してください。
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。