What is estradiol medicine? Side effects and uses of Estradiol drug

Estradiol is a female sex hormone produced in the ovaries. This hormone plays an important role in women’s sexual growth and development, menstrual cycle and pregnancy. By binding to the estrogen receptor in the cytoplasm, estradiol increases the production of RNA, DNA and various proteins in the target tissues. This hormone is produced in small amounts in men, which plays an important role in sperm production and their sexual performance. This drug is produced and marketed in pharmaceutical forms such as transdermal gel, injection solution, tablet, topical emulsion, etc.

Pharmaceutical forms of estradiol

1. Transdermal gel: 0.6% (Elsterin; Estrogel), 0.1% (Davigel; generic)
2. Injection solution: 5 mg/ml, 10 mg/ml, 20 mg/ml, 40 mg/ml
3. Tablets: 45 mg (as acetate), 0.5 mg, 0.9 mg (as acetate), 1 mg, 1.5 mg, 2 mg
4. Transdermal patch: 025 mg, 0.0375 mg, 0.05 mg, 0.06 mg, 0.075 mg, 0.1 mg
5. Topical emulsion: 35 mg / 1.74 g (0.25%)

Uses of estradiol medicine

Estradiol is a hormone (estrogen) that is absorbed through the skin and enters the bloodstream. Women use it to help reduce certain symptoms of menopause (hot flashes). Certain brands may also help reduce vaginal menopause symptoms (such as vaginal dryness, burning, and itching) that result from less estrogen production in the body. If you are using this drug to treat symptoms only in and around the vagina, you should consider drugs that are used directly inside the vagina first before drugs that are taken by mouth, skin, or injection.

Uses of estradiol in adults

1. Vulvar and vaginal atrophy in menopause
2. Hypoestrogenism due to castration, hypogonadism or ovarian failure
3. Metastatic breast cancer
4. Hypoestrogenism
5. Osteoporosis
6. Vasomotor symptoms associated with menopause
7. Prostate Cancer
8. Estrogen replacement in Turner syndrome (orphan)

Pharmacological effects and mechanism of action of estradiol drug

endogenous estrogen; Decreased secretion of gonadotropin-releasing hormone and luteinizing hormone-releasing hormone from the hypothalamus, which reduces the secretion of gonadotropin from the pituitary gland. This drug increases the synthesis of DNA, RNA and various proteins in the target tissues. Estradiol is easily absorbed through the digestive system, skin and mucous membrane. This drug is mainly excreted through urine (conjugated with a small amount of unchanged drug) and most estrogens are also excreted through bile and undergo hepatic intestinal recycling.

Estradiol dosage

Estradiol medicine is available in the market in different pharmaceutical forms, the amount and time of use of each one is different. Apply this medicine once a day on clean and dry skin on the upper arm or shoulder. Some brands of this drug may be applied to the arm from the wrist to the shoulder. Avoid using this medicine on broken and irritated skin. After use, wash your hands thoroughly with soap and water to reduce the risk of accidentally spreading it from your hands to others. Wait about 5 minutes for the application area to dry completely before applying the dressing. Cover the application site with clothing (such as a long-sleeved shirt) to prevent others from contacting the application site and being exposed to the drug.

Time to take estradiol

If using topical forms, you should wait at least 1-2 hours (depending on your brand) and do not allow others to touch the skin where the medication is applied. If someone accidentally touches the gel (or the application site within 1-2 hours), have them wash the contact area thoroughly with soap and water. To get the best effect, wait at least 2 hours before showering or swimming for the medicine to be absorbed through the skin. Use this medicine regularly to get the most benefit.

Dosage of estradiol in adults

1. Vulvar and vaginal atrophy in menopause (stress), 1-2 mg orally once daily for 3 weeks followed by 1 week rest, Valerate 10-20 mg intramuscularly, Estrogel 25 mg daily for 3 weeks and 1 week off are used.
2. For the treatment of castration-induced hypoestrogenism and hypogonadonism or ovarian failure (Estrace), titrate to 1 to 2 mg orally daily to use the minimum effective dose. Also Valerate 10 to 20 mg is used as intramuscular injection in 4 weeks.
3. For the treatment of metastatic breast cancer, 10 mg orally 3 times a day is used.
4. Hypoestrogenism, 1.5 to 2 mg intramuscular injection every 4 weeks.
5. Osteoporosis (Estrace), 0.5 mg/day is prescribed for 23 days of the 28-day cycle used in clinical studies.
6. Vasomotor symptoms associated with menopause (stress), 1-2 mg/day for 3 weeks followed by a week off, Valerate 10-20 mg IM every 3-4 weeks, Cypionate 1-5 mg IM In 3 to 4 weeks, Elsterin 87 g/day gel is used at the same time every day.

Precautions

Before taking estradiol, if you are allergic to it or other ingredients in the medicine, avoid using it. This medicine may contain inactive ingredients that can cause allergic reactions or other problems. In case of medical history including vaginal bleeding of unknown cause, certain cancers (such as breast cancer, uterine or ovarian cancer), blood clots, stroke, heart disease (such as heart attack), liver disease, kidney disease, family medical history ( especially breast masses, cancer, blood clots), family or personal history of a certain swelling disorder (angioedema), high blood pressure, diabetes, high cholesterol and triglyceride levels, obesity, lupus, hypothyroidism, etc. Consult your doctor .

1. Severe anaphylactic reactions including urticaria, itching, swelling of the lips, respiratory abnormalities, abdominal pain, vomiting have been reported during skin treatment.
2. An increased risk of stroke and DVT has been reported with estrogen alone and estrogen plus progestin therapy. If any of these occur or are suspected, discontinue estrogen with or without progestin immediately.
3. Discontinue treatment if jaundice, vision problems (may cause intolerance to contact lenses), any signs of venous thromboembolism, migraine of unusual severity, significant increase in blood pressure, severe depression, increased risk of thromboembolic complications after surgery.
4. Patients taking warfarin or other oral anticoagulants (increased anticoagulant dose may be necessary).
5. Some studies have linked OC use to an increased risk of breast cancer, while other studies have shown no change in risk. This risk depends on conditions in which normal high hormone levels persist for long periods, including early onset of menstruation (less than 12 years), late menopause (over 55 years), first child after age 30. did
6. An increased risk of ovarian cancer has been reported in women who used hormone therapy for menopausal symptoms.
7. An increased risk of cervical cancer with the use of OC has been reported in some patients. However, human papillomavirus (HPV) remains the main risk factor for this cancer. Evidence suggests that long-term (>5 years) use of OCs may be associated with increased risk.
8. Hypercalcemia occurs in some patients with breast cancer or bone metastases. If hypercalcemia occurs, discontinue treatment and take appropriate measures to reduce serum calcium levels.
9. Angioedema involving the eyes or eyelids, face, larynx, pharynx, tongue, and extremities (hands, feet, ankles, and fingers) with or without urticaria has been reported. If angioedema occurs, discontinue treatment permanently.

Estradiol increases the risk of endometrial cancer

1. Close clinical monitoring of all women taking estrogen is essential. The risk of endometrial cancer increases with the use of unopposed estrogens. Adding a progestin to estrogen therapy may reduce the risk of endometrial hyperplasia, a precursor to endometrial cancer.
2. Adequate diagnostic procedures, including endometrial sampling if indicated, should be performed to rule out malignancy in all cases of persistent or recurrent abnormal vaginal bleeding.

Contraindications to the use of estradiol

1. Documented hypersensitivity
2. Known anaphylactic reaction or angioedema with topical emulsion
3. Known protein C, protein S or antithrombin deficiency or other known thrombophilic disorders
4. Active or previous breast cancer
5. Arterial thromboembolic disease (stroke, myocardial infarction [MI]), thrombophlebitis, DVT/PE, thrombogenic valvular disease
6. Estrogen-dependent neoplasia
7. Uncontrolled blood pressure, diabetes with vascular involvement, jaundice with previous use of oral contraceptives (OC).
8. Undiagnosed abnormal vaginal bleeding
9. Liver diseases and liver tumors

Cardiovascular risks of estradiol drugs

1. Estrogen with and without progestin should not be used to prevent cardiovascular diseases.
2. Estrogen plus progestin: the Women’s Health Initiative (WHI) substudy of estrogen plus progestin increased the risk of myocardial infarction, stroke, invasive breast cancer, pulmonary embolism (PE), and deep vein thrombosis (DVT) in postmenopausal women (50–79 years). ) reported.
3. Estrogen alone: ​​A substudy of the WHI reported an increased risk of stroke and DVT in postmenopausal women (50–79 years) during 6.8 years of treatment with conjugated estrogen (625 mg orally per day) alone compared with placebo.
4. The relevance of the WHI findings on the effects of lower doses of conjugated estrogens, other routes of administration, or other estrogen-only products on cardiovascular adverse events is not known. Without such data, it is not possible to definitively exclude risks or quantify the risk for other drugs.

Side effects of estradiol

Depression, dry mouth, headache, blood pressure, impotence, flu, leucorrhoea, melasma, muscle cramps, nausea, etc. are some of the side effects of estradiol medicine. If any of these effects persist or worsen, tell your doctor or pharmacist right away. In case of serious side effects, including psychological and behavioral changes (such as depression and memory loss), unusual vaginal bleeding (such as spotting, sudden bleeding, prolonged or frequent bleeding), increased or new vaginal irritation, itching and discharge, Severe stomach and abdominal pain, yellowing of the eyes and skin, dark urine, swelling of the hands, ankles and feet, increased thirst, urination, etc., consult a doctor.

1. Abdominal cramps
2. flatulence
3. breakthrough bleeding
4. Breast enlargement
5. Breast tenderness
6. Delayed ejaculation
7. depression
8. dry mouth
9. Headache
10. blood pressure
11. impotence
12. Flu
13. muscle cramps
14. nausea

Estradiol drug interactions

1. Class X interactions (avoid): anastrazole, dihydroepiandrosterone, exemestane, hemin, indium 111 capromib pentide, lasmiditan, spamifen
2. Reduction of the effects of drugs by estradiol (systemic): antidiabetic drugs, chenodiol, cosinetropin, exemestane, Hemin, hyaluronidase, indium 111 capromib pentide, lamotrigine, spamifen, somatropin, thyroid preparations
3. Reduction of estradiol effects (systemic) by drugs: dabrafenib, deferasirox, enzalutamide, erdafitinib, ivocidanib, mitotane, P-gp/ABCB1 inhibitors, sarilumab, ciltuximab, tipranavir, tocilizumab
4. Enhancement of drug effects by estradiol (systemic): ajmaline, nigella immunoglobulin (human), C1 inhibitors, clozapine, corticosteroids (systemic), dantrolene, immunoglobulin, lenalidomide, mivacurium, spamifen, ropinirole, succinylcholine, thalidomide, theophylline derivatives, tipranavir, tizanidine

Estradiol consumption during pregnancy and breastfeeding

The use of estradiol is not recommended during pregnancy, as there is no information on its use in pregnant women. However, epidemiological studies and meta-analyses have shown an increased risk of genital or non-genital birth defects (including cardiac malformations and limb-reduction defects) following exposure to combined hormonal contraceptives (estrogen and progestin) before or during early pregnancy. They have not shown pregnancy. Also, the treatment is not recommended for use in women of reproductive potential. Estrogen in human milk can reduce milk production in lactating women.

Estradiol storage conditions

Estradiol medicine should be stored away from heat or ignition and at room temperature. All chemical and herbal medicines should be kept out of the reach of animals and children.

The last word of estradiol medicine

As we said in this article from Positive Green Pharmacy magazine, estradiol drug has different uses, including prevention of osteoporosis, prevention of breast cancer, infertility, menstrual problems, menopause, etc. However, in case of excessive and non-prescription use, we see side effects such as hot flashes, night sweats, vaginal dryness, headache, weight gain, swelling and dizziness in patients. For this reason, before taking any medicine, patients should consult their doctor about the side effects and risks of its use.

Site source: Medscape