diethylstilbestrol

Action and Spectrum

Actions and Spectrum: 

Actions: 

Synthetic nonsteroidal estrogens like diethylstilbestrol have effects akin to those of natural estrogens. It prevents the pituitary from secreting luteinizing hormone, which in turn prevents the pituitary from secreting testosterone. 

Spectrum: 

It was also used to treat vulvar dystrophy, senile (atrophic) vaginitis, symptoms of menopause, and symptoms following ovariectomy. Diethylstilbestrol, sometimes referred to as the “morning-after pill,” was used as a postcoital emergency contraception. It was also useful in treating female hypogonadism, controlling irregular menstrual cycles, and preventing postpartum breast engorgement. 

Drug Interaction

Adverse Reaction

Frequency not defined 

• Allergic reactions:  Rash; peeling skin with or without fever; hives; swollen, red, blistered, or wheezing; itching; swallowing, trouble breathing, or talking; unusual hoarseness; tightness in the chest or throat; or swelling of the face, mouth, tongue, lips, or throat 
• Signs of high blood pressure include dizziness or very bad headaches, change in eyesight, and passing out 
• Signs of liver problems include feeling tired, dark urine, upset stomach or stomach pain, not being hungry, throwing up, light-colored stools, or yellow eyes or skin 
• Gallstone symptoms include sudden pain in the right shoulder area, upper right belly area, or between the shoulder blades; yellow eyes or skin; or fever with chills 
• Indications of elevated calcium levels include constipation, lassitude, fatigue, disorientation,  nausea, headache, or bone pain 
• Abnormal vaginal bleeding  
• A lump in the breast, soreness, 
• Breast pain or nipple discharge 
• Enlarged breasts 
• Breast pain 
• Not able to get or keep an erection 
• Mood changes 
• Change in how contact lenses feel in the eyes 
• Bulging eyes 
• Very upset stomach or throwing up 
• Low mood (depression) 
• One side weakness is difficulty speaking or thinking, imbalance, slumping on blurred vision or either side of the face 
• Feminization, gynacomastia, and impotence in men 
• Amenorrhea and irregular menses in females 
• Uncontrolled Diabetes 

Black Box Warning

Because of its propensity for cancer, diethylstilbestrol shouldn’t be administered to children or young people.

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Breast cancer (with exceptions) 
• Pregnancy 
• Porphyria 
• Thromboembolic disease 

Cautions 

• Renal impairment 
• Cardiovascular disorders 
• Hepatic impairment 
• Drug interactions 
• Geriatrics 
• Pediatrics 
• Breastfeeding

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology: 

Oral diethylstilbestrol, often known as Stilbestrol, is a non-steroidal female hormone that can affect both menopausal and postmenopausal conditions. Spermatogonial stem cells can experience apoptosis and DNA oxidation when exposed to diethylstilbestrol. Autophagy of thymocytes can be induced by diethylstilbestrol. Diethylstilbestrol is an inhibitor of 11β-hydroxysteroid dehydrogenase 2 (HSD11B2). 

Pharmacodynamics: 

Target cells are penetrated by estrogens, which then bind with the estrogen receptor, a protein receptor. The female reproductive system,  the hypothalamus, the mammary gland, and the pituitary are among the target cells. Follicle-stimulating hormone (FSH) from the anterior pituitary is suppressed when estrogen binds its receptors, which in turn induces downstream increases in the hepatic production of thyroid-binding globulin (TBG), sex hormone binding globulin (SHBG), and other blood proteins. Combining estrogen and progestin inhibits the hypothalamic-pituitary system, which lowers gonadotropin-releasing hormone (GnRH) output. 

Pharmacokinetics: 

Absorption 

The GI tract readily absorbs it.  

Metabolism 

The liver breaks down substances slowly. 

Elimination and Excretion 

Mostly as glucuronide, excreted in the urine and stool. 

Adminstartion

Administration: 

Diethylstilbestrol (DES) is usually administered orally, with the medication taken in the form of tablets or capsules. The prescribed dosage and frequency of administration are determined by the specific medical condition being addressed and the recommendations of the healthcare provider. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: diethylstilbestrol 

Pronounced: dye-ETH-uhl-still-BES-trawl 

Why do we use diethylstilbestrol? 

Diethylstilbestrol (DES) is a synthetic estrogen, a hormone pivotal in the development and upkeep of female reproductive tissues. DES was first created and given to expectant mothers between the 1940s and the 1970s in an effort to reduce miscarriages and other pregnancy-related issues. At the time, it was thought to provide hormonal support. 

But in the early 1970s, worries surfaced when it was discovered that daughters of pregnant women using DES had a higher chance of developing cervix and vaginal clear cell adenocarcinoma. Additionally, these individuals were more prone to reproductive tract abnormalities and other health issues. 

Due to these severe health concerns, the use of DES in pregnancy was halted, and its adverse effects became a cautionary tale in medical history. DES is no longer employed for pregnancy-related purposes, and alternative, safer treatments now exist for managing pregnancy complications. 

Despite its historical use and subsequent discontinuation, DES continues to impact the health of those exposed during pregnancy, underscoring the necessity of ongoing medical research and vigilance in monitoring the long-term effects of pharmaceutical interventions.