estradiol dienanthate

Action and Spectrum

Actions and spectrum: 

Estrogenic Action: 

• Tissue Effects: Like natural estrogens, estradiol dienanthate exerts its effects on various tissues in the body, including the reproductive organs, breasts, bones, and the cardiovascular system. 
• Uterine Effects: It can stimulate the growth of the uterine lining (endometrium), influencing the menstrual cycle. 
• Breast Development: estradiol dienanthate plays a role in breast development and maintenance. 
• Bone Health: Estrogens contribute to bone health by helping to maintain bone density. 
• Cardiovascular Effects: Estrogens have been associated with cardiovascular benefits, including effects on cholesterol levels and blood vessel function. 

Hormone Replacement Therapy (HRT): estradiol dienanthate may be used as part of hormone replacement therapy in postmenopausal women to alleviate symptoms of estrogen deficiency, like hot flashes, vaginal dryness, and mood changes. 

Contraception: estradiol dienanthate, when combined with a progestin, may be used as a component of hormonal contraceptives, such as combined oral contraceptives. 

Hormone Regulation: In certain medical conditions, estradiol dienanthate may be used to regulate hormonal balance in individuals with estrogen deficiency. 

Spectrum: The spectrum of estradiol dienanthate’s action is primarily related to estrogen receptor-mediated effects. It is specific to tissues that express estrogen receptors, including reproductive tissues, mammary glands, bone cells, and others. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Malignant Neoplasms 

Cardiovascular Disorders 

Black Box Warning

Black Box Warning: 

There were no specific black box warnings for estradiol dienanthate. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity or Allergy: Contraindicated in known hypersensitivity or allergy to estradiol or any of the components in the formulation. 
• Estrogen-Dependent Neoplasms: Contraindicated in known or suspected estrogen-dependent neoplasms, such as breast cancer or endometrial cancer. 
• Undiagnosed Vaginal Bleeding: Contraindicated in individuals with undiagnosed abnormal vaginal bleeding. Abnormal vaginal bleeding should be evaluated to determine the cause before initiating hormonal therapy. 
• Pregnancy: Contraindicated during pregnancy. If pregnancy is detected during treatment, the medication should be discontinued. 
• Hypercalcemia: Contraindicated in individuals with hypercalcemia associated with metastatic bone disease.

Caution: 

• Breast Cancer: Estrogen therapy has an increased risk of breast cancer. Caution is advised, and the benefits and risks should be carefully evaluated, especially in individuals with a family history of breast cancer. 
• Endometrial Cancer: Estrogen-alone therapy in postmenopausal women with an intact uterus has an increased risk of endometrial cancer. Adding a progestin may reduce this risk. Caution is needed in individuals with a history of endometrial hyperplasia or cancer. 
• Liver Function: Estrogens are metabolized in the liver, and caution is advised in individuals with impaired liver function. Liver function should be monitored during treatment. 
• Hypertension: Estrogen therapy may be associated with an increase in blood pressure. Blood pressure should be monitored, and caution is advised in individuals with hypertension. 
• Fluid Retention: Estrogen therapy may cause fluid retention. Caution is advised in individuals with conditions influenced by fluid balance, such as cardiac or renal dysfunction. 
• Gallbladder Disease: Estrogen therapy may increase the risk of gallbladder disease. Caution is needed in individuals with a history of gallbladder disease. 

Comorbidities: 

• Thromboembolic Disorders: Individuals with a history of venous or arterial thromboembolic events, including deep vein thrombosis (DVT) or pulmonary embolism (PE), may be at an increased risk. Estrogen therapy, including estradiol dienanthate, may further elevate this risk. 
• Endometrial Cancer or Hyperplasia: Individuals with a history of endometrial cancer or hyperplasia may require caution when using estrogen therapy. Adding a progestin may be recommended to reduce the risk of endometrial cancer. 
• Diabetes: Estrogen therapy may affect glucose tolerance. Individuals with diabetes may need careful monitoring and management of their blood glucose levels. 
• Migraines: Individuals with a history of migraines may experience exacerbation or changes in migraine patterns with estrogen therapy. 
• Bone Health: While estrogen therapy is often beneficial for bone health, individuals with specific bone conditions or diseases may require individualized consideration. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

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: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

estradiol dienanthate is a synthetic form of the endogenous estrogen hormone estradiol. As a prodrug, it undergoes metabolic conversion to estradiol in the body, exerting its pharmacological effects. estradiol, a primary female sex hormone, binds to estrogen receptors in target tissues, influencing gene expression and modulating various physiological processes. In reproductive tissues, it promotes the development and maintenance of the female reproductive system, including the uterus and breasts.

Additionally, estradiol plays a crucial role in bone health by aiding in the maintenance of bone density. In postmenopausal women, estradiol dienanthate may be used as hormone replacement therapy to alleviate menopausal symptoms and prevent associated complications such as osteoporosis. The pharmacological actions are tightly regulated, and its use requires careful consideration of individual health status, including factors like cardiovascular health and the presence of comorbidities.  

Pharmacodynamics: 

• Estrogen Receptor Binding: The primary pharmacodynamic action of estradiol dienanthate is mediated through binding to estrogen receptors (ER) in target tissues. estradiol has a high affinity for both estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ). 
• Gene Expression Regulation: Upon binding to estrogen receptors, estradiol modulates gene expression, influencing the synthesis of various proteins. This process is essential for the regulation of physiological functions in estrogen-responsive tissues. 
• Reproductive Tissues: In reproductive tissues, such as the uterus and breasts, estradiol promotes growth, development, and maintenance. It plays a role in menstrual cycle, endometrial proliferation, and breast development. 
• Bone Health: estradiol contributes to bone health by influencing bone density and mineralization. It helps maintain a balance between bone resorption and formation, which is crucial for preventing osteoporosis. 
• Cardiovascular Effects: Estrogen has been associated with cardiovascular effects, including favourable changes in lipid profiles and vascular function. However, the cardiovascular effects are complex and can be influenced by various factors, requiring careful consideration. 
• Menopausal Symptom Relief: In postmenopausal women, estradiol dienanthate may be used as hormone replacement therapy to alleviate menopausal symptoms like vaginal dryness, hot flashes, and mood changes. 

Pharmacokinetics: 

Absorption: 

• Route of Administration: estradiol dienanthate is typically administered via intramuscular injection. The drug gets slowly released into the bloodstream, providing a sustained effect. 
• Absorption Rate: The absorption rate is influenced by the injection site, formulation, and other factors. Intramuscular administration allows for gradual absorption over time. 

Distribution: 

• Plasma Protein Binding: Once in the bloodstream, estradiol dienanthate binds to plasma proteins, primarily albumin and sex hormone-binding globulin (SHBG). This binding influences the availability of estradiol to target tissues. 
• Tissue Distribution: estradiol has widespread distribution in tissues, with estrogen receptors present in various organs such as the reproductive organs, breasts, bones, and the central nervous system. 

Metabolism: 

• Conversion to estradiol: estradiol dienanthate undergoes enzymatic cleavage to release estradiol, its active metabolite. This process occurs in various tissues, including the liver. 
• Liver Metabolism: The liver plays a significant role in metabolizing estradiol, and the resulting metabolites are conjugated with glucuronic acid or sulfate before excretion. 

Excretion: 

• Renal Excretion: Metabolites of estradiol are excreted via the kidneys. The conjugated forms are often eliminated in urine. 
• Biliary Excretion: Some metabolites may undergo biliary excretion into the feces. 

Adminstartion

Administration: 

• Dosage: The dosage of estradiol dienanthate is prescribed by a healthcare provider and depends on the specific medical condition being treated. Dosages may vary for hormone replacement therapy, contraception, or other indications. 
• Route of Administration: Intramuscular Injection: estradiol dienanthate is commonly administered as an intramuscular injection. The injection is typically given deep into the muscle tissue. 
• Injection Sites: The injection is often given into the gluteal (buttock) muscle. Other potential sites may include the deltoid muscle in the upper arm. The choice of injection site is determined by the healthcare provider. 
• Frequency of Administration: The frequency of administration can vary. In some cases, injections may be given monthly, while in others, a different schedule may be recommended. 
• Professional Administration: In many cases, healthcare professionals administer estradiol dienanthate injections in a clinical setting. This ensures proper technique and reduces the risk of complications. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: estradiol dienanthate 

Pronounced: (ES-truh-dye-ol dy-en-AN-thate)  

Why do we use estradiol dienanthate? 

estradiol dienanthate is often used in hormone replacement therapy for women experiencing menopausal symptoms. It helps alleviate symptoms such as hot flashes, vaginal dryness, and mood changes associated with hormonal changes during menopause. In some formulations, estradiol dienanthate may be combined with a progestin to create a combination hormonal contraceptive.

This combination is used for birth control. Estrogen, including formulations containing estradiol dienanthate, is sometimes prescribed to postmenopausal women to help maintain bone density. estradiol dienanthate may be used in the management of certain cases of hypogonadism, particularly in women. In some cases, estradiol dienanthate may be prescribed to induce menstruation in women with amenorrhea.