Dietilestilbestrol
Diethylstilbestrol
También conocido como: Apstil · Destilbenol · Distilbene · diethylstilbestrolum · diethylstilboestrol · NSC-3070
Revisado por el equipo veterinario de VetSheetActualizado 5 abr 2026Referencia veterinaria basada en la evidencia
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Dosis por especie
🌎 NA — North America🌍 EU — Europe
Perros
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Gatos
| Indicación | Dosis | Vía | Frecuencia | Duración | Región |
|---|---|---|---|---|---|
| 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.
Las dosis son una referencia clínica para profesionales veterinarios autorizados. Confirme siempre con el prospecto actual y cada paciente individual.
Resumen
El dietilestilbestrol (DES) es un estrógeno sintético no esteroideo utilizado principalmente en medicina veterinaria para el manejo de la incontinencia urinaria sensible a estrógenos en perras esterilizadas. También se ha utilizado para la hipertrofia prostática benigna en perros machos y para la inducción del estro.
Perla clínica: Debido al riesgo grave de toxicidad en la médula ósea (anemia aplásica mortal) y su clasificación como posible carcinógeno y teratógeno, el DES está estrictamente prohibido en animales destinados al consumo humano.
Debido a preocupaciones de salud pública y retiros del mercado, el DES ya no está disponible comercialmente como un producto fabricado aprobado por la FDA y debe obtenerse a través de farmacias de formulación magistral veterinaria. En la práctica moderna, a menudo se prefieren alternativas más seguras como el estriol (Incurin) o la fenilpropanolamina (PPA) como terapias de primera línea para la incompetencia del mecanismo del esfínter.
Mecanismo de acción
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.
Seguridad y advertencias
Contraindicaciones
- Food-producing animals (FDA prohibited)
- Pregnancy (teratogenic; causes fetal genitourinary malformations)
- Patients with preexisting anemias or leukopenias
- Females with estrogen-sensitive neoplasms
Efectos adversos
- 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)
Precauciones
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.
Interacciones farmacológicas
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
Monitorización
- 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)
Farmacocinética
Absorción
Well absorbed from the GI tract of monogastric animals.
Metabolismo
Slowly metabolized by the liver, primarily to a glucuronide form.
Eliminación
Excreted in the urine and feces.
Sobredosis
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).
Productos disponibles
Formulaciones
- Compounded oral capsules
- Compounded oral tablets
- Compounded oral suspensions
Etiquetado para humanos
- No commercially available regular oral DES products are available in the USA. Compounded preparations may be available from compounding pharmacies.
Estado regulador
Sin datos reguladores para: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
Almacenamiento y estabilidad
All commercially available DES tablets (plain tablets, enteric-coated tablets) should be stored at room temperature (15-30°C) in well-closed containers.
Información para el cliente
El dietilestilbestrol (DES) es una hormona utilizada principalmente para tratar la incontinencia urinaria (goteo de orina) en perras esterilizadas.
- Dosificación estricta: Es fundamental administrar este medicamento exactamente como se le ha recetado. Administrar más de la dosis recomendada puede provocar una enfermedad mortal de la médula ósea.
- Vigile signos de sangrado/infección: Contacte a su veterinario inmediatamente si nota encías pálidas, hematomas inexplicables, letargo, debilidad o fiebre.
- Vigile signos de piómetra: Si su mascota es una hembra no esterilizada, observe si hay un consumo excesivo de agua, micción frecuente o secreción anormal por la vulva, lo cual podría indicar una infección uterina grave.
- Otros signos a reportar: Diarrea, vómitos o signos de estar en "celo" (vulva inflamada, sangrado).
- Manipulación: Lávese las manos después de manipular el medicamento y manténgalo estrictamente fuera del alcance de niños y otras mascotas.
La referencia de medicamentos de VetSheet está destinada a profesionales veterinarios autorizados como ayuda para la toma de decisiones clínicas, no como sustituto del criterio profesional ni del prospecto actual del fabricante.