디에틸스틸베스트롤

호르몬제 - 합성 에스트로겐

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.

동물 종별 용량

Cats

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 · Doses of 2.2 mg/kg per day have caused death in cats secondary to bone marrow toxicity.

Dogs

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 · As an alternative to phenylpropanolamine.
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
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 · 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 · 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 · Adjust dosages of LH and FSH for animal size-the above dosages are for a dog weighing 50-60 lbs.

투여 경로

금기

Food-producing animals (FDA prohibited)
Pregnancy (teratogenic; causes fetal genitourinary malformations)
Patients with preexisting anemias or leukopenias
Females with estrogen-sensitive neoplasms

이상반응

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)

약물 상호작용

Azole Antifungals (itraconazole, ketoconazole, etc.) · May increase estrogen levels
Cimetidine · May decrease metabolism of estrogens
Corticosteroids · Enhanced glucocorticoid effects may result; estrogens may alter protein binding or decrease metabolism of corticosteroids
Erythromycin, Clarithromycin · May decrease the metabolism of estrogens
Warfarin · Oral anticoagulant activity may be decreased; increases in anticoagulant dosage may be necessary
Phenobarbital · May decrease estrogen concentrations
Phenytoin · May decrease estrogen concentrations
Rifampin · 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)

과용량

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).

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