디에틸스틸베스트롤
Diethylstilbestrol
다른 이름: Apstil · Destilbenol · Distilbene · diethylstilbestrolum · diethylstilboestrol · NSC-3070
VetSheet 수의사 팀 검수업데이트 2026년 4월 5일근거 기반 수의학 참고자료
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
동물 종별 용량
🌎 NA — North America🌍 EU — Europe
개
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
고양이
| 적응증 | 용량 | 경로 | 빈도 | 기간 | 지역 |
|---|---|---|---|---|---|
| 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.
용량은 수의사 전문가를 위한 임상 참고자료입니다. 반드시 최신 약물 정보 및 개별 환자에 따라 확인하시기 바랍니다.
개요
디에틸스틸베스트롤(DES)은 합성 비스테로이드성 에스트로겐으로, 수의학에서는 주로 중성화된 암컷 반려견의 에스트로겐 반응성 요실금 관리에 사용됩니다. 수컷 반려견의 양성 전립선 비대증 및 발정 유도에도 사용된 바 있습니다.
임상 요점: 심각한 골수 독성(치명적인 재생불량성 빈혈) 위험이 있으며 잠재적인 발암 물질 및 기형 유발 물질로 분류되어 있으므로 식용 동물에 대한 사용이 엄격히 금지됩니다.
인체 건강에 대한 우려와 시장 철수로 인해 DES는 더 이상 FDA 승인을 받은 시판 제품으로 제공되지 않으며 수의 조제 약국을 통해서만 구해야 합니다. 현대 임상에서는 괄약근 기능 부전의 1차 치료제로 에스트리올(Incurin)이나 페닐프로판올아민(PPA)과 같은 더 안전한 대안이 선호되는 경우가 많습니다.
작용 기전
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.
안전성·주의사항
금기사항
- Food-producing animals (FDA prohibited)
- Pregnancy (teratogenic; causes fetal genitourinary malformations)
- Patients with preexisting anemias or leukopenias
- Females with estrogen-sensitive neoplasms
부작용
- 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)
주의
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.
약물 상호작용
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
모니터링
- 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)
약동학
흡수
Well absorbed from the GI tract of monogastric animals.
대사
Slowly metabolized by the liver, primarily to a glucuronide form.
배설
Excreted in the urine and feces.
과다투여
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).
제품
제형
- Compounded oral capsules
- Compounded oral tablets
- Compounded oral suspensions
인용의약품
- No commercially available regular oral DES products are available in the USA. Compounded preparations may be available from compounding pharmacies.
규제 현황
규제 데이터 없음: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
보관·안정성
All commercially available DES tablets (plain tablets, enteric-coated tablets) should be stored at room temperature (15-30°C) in well-closed containers.
보호자 정보
디에틸스틸베스트롤(DES)은 주로 중성화된 암컷 반려견의 요실금(소변 새는 증상)을 치료하는 데 사용되는 호르몬제입니다.
- 엄격한 용량 준수: 처방된 대로 정확하게 약을 투여하는 것이 매우 중요합니다. 권장 용량보다 많이 투여하면 치명적인 골수 질환을 유발할 수 있습니다.
- 출혈/감염 징후 주의: 잇몸 창백, 원인 불명의 멍, 무기력, 쇠약 또는 발열이 관찰되면 즉시 수의사에게 연락하십시오.
- 자궁축농증 징후 주의: 반려동물이 중성화되지 않은 암컷인 경우, 과도한 물 섭취, 잦은 배뇨 또는 외음부의 비정상적인 분비물이 있는지 관찰하십시오. 이는 심각한 자궁 감염을 의미할 수 있습니다.
- 기타 보고해야 할 증상: 설사, 구토 또는 "발정" 징후(외음부 부종, 출혈).
- 취급 주의: 약물을 만진 후에는 손을 씻고, 어린이와 다른 반려동물의 손이 닿지 않는 곳에 엄격히 보관하십시오.
VetSheet 의약품 참고자료는 수의사 전문가의 임상 의사결정 지원을 위한 것이며, 전문적 판단이나 제조사의 최신 약물 정보를 대체할 수 없습니다.