Bi-Est Cream (Estriol/Estradiol 50/50) (30 mL) / (Estriol/Estradiol 80/20) (30 mL)

At the cellular level, estradiol is the main intracellular human estrogen and is much more active than its metabolites, estrone and estriol. Estradiol can either be produced synthetically or derived from natural sources. There is no proof that “natural” estrogens are more or less effective or safe than “synthetic” estrogens. Estradiol must be provided in a micronized oral dosage form to guarantee therapeutic impact because nearly total first-pass metabolism exists. Mainly used to avoid osteoporosis and ease vasomotor and genitourinary symptoms linked with menopause (natural or surgical), estradiol is also used for prevention of postmenopausal osteoporosis, is Additionally used to treat abnormalities of female gonadotropin dysfunction and female hypogonadism. Several estrogen formulations have been sold in the United States since 1938. Postmenopausal women with only genitourinary symptoms prefer vaginal treatments because most of these dosage forms have lesser systemic absorption/exposure. Many estradiol items have FDA approval since the 1990s following the FDA’s instructions to offer effective low-dose estrogen treatments in alternative drug delivery methods.

Estrogens boost the rate of synthesis of DNA, RNA, and certain proteins once they enter the cells of sensitive tissues (e.g., female organs, breasts, hypothalamus, pituitary). Estrogen administration decreases the hypothalamus’s secretion of gonadotropin-releasing hormone, therefore lowering follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary. The growth and development of female sex organs as well as the preservation of sex traits including axial and pubic hair fall under estrogens’ responsibility. also molding of skeletal and body curves. At the cellular level, estrogens raise uterine tone, stimulate the endometrium to proliferate, and boost cervical secretions. Prolonged estrogen therapy ironically shrinks the endometrium. Withdrawal of estrogen starts menstruation during the preovulatory or nonovulatory phase of the menstrual cycle; in the ovulatory phase, progesterone production declines. Is the major driver behind monthly flow? Amenorrhea manifests itself in most women within a few months of oral estrogen use in postmenopausal practice.

Although they can quicken epiphysial closure and influence bone calcium deposition, estrogens’ anabolic effect is slight. Estrogens seem to stop the osteoporosis that accompanies the start of menopause. By 15% on average, estrogens usually favorably affect blood lipids by lowering LDL and boosting HDLcholesterol levels. Estrogen administration raises serum triglycerides. Estrogens accelerate the production of a number of proteins including thyroid binding globulin and various clotting agents. Estrogens raise platelet aggregation and lower antithrombin III levels. Estrogens also promote sodium and fluid retention.

In women experiencing menopause with an intact uterus, unopposed estrogen has been linked to greater endometrial cancer risk; concomitant progestin therapy decreases but not eliminate this risk. But the HERS studies, the Women’s Health Initiative study, and other research reveal that for some women, combination hormone replacement therapy (HRT) could add further health risks.

Estradiol is a form of estrogen, a hormone that plays a key role in women’s health, especially during menopause or in hormone replacement therapy. However, it’s not suitable for everyone and can cause serious complications if used in certain situations.

Studies show that using estradiol during pregnancy can harm the baby, affecting the development of organs like the heart, limbs, and reproductive system. Even though accidental use in early pregnancy doesn’t seem to greatly increase birth defects, treatment should be stopped immediately if pregnancy is suspected.

Estradiol is also unsafe in breastfeeding mothers. Estrogens can reduce the quantity and quality of breast milk, and trace amounts of the hormone can pass into the baby’s system. While not approved for postpartum use, some doctors may consider low-dose vaginal forms after discussing risks and benefits.

Women with certain cancers should avoid estradiol. If a person has or suspects breast, ovarian, cervical, uterine, or other estrogen-sensitive tumors, the hormone can worsen their condition. Regular screenings like mammograms, pelvic exams, and blood tests are essential for women on estrogen therapy.

Estradiol should be avoided by women with a history of blood clots, strokes, or heart disease, as it increases the risk of thrombosis (clots), strokes, and heart attacks. Even women with risk factors like high blood pressure, smoking, diabetes, or obesity need close monitoring. Estradiol can also worsen conditions like lupus, where immune and clotting problems are already present.

Liver diseases, including cancer or severe liver problems, are another reason to avoid estradiol. Estrogens are processed by the liver, and impaired function can cause harmful effects. Similarly, women with a history of gallbladder issues, porphyria, or thyroid disease should consult their doctors before starting treatment.

Mood disorders, including depression, can worsen with estradiol, so women with a history of mental health issues need extra care. Conditions like asthma, seizures, and kidney or heart problems may also be aggravated by fluid retention caused by the hormone.

Estradiol may increase triglycerides in some women, possibly leading to pancreatitis, and can cause vision problems like retinal thrombosis or migraines with neurological symptoms.

For older women, especially those over 65, estradiol is generally not recommended. It does not prevent memory loss and may increase dementia risk. Experts advise against using it to improve cognitive function or manage urinary incontinence.

Finally, certain forms of estradiol, like topical sprays and gels, can be dangerous if accidentally transferred to children or pets. Fire safety is also a concern, as alcohol-based gels are flammable.

What you need to know about estradiol and its side effects

Estradiol is a type of estrogen hormone that’s often used to help with symptoms like menopause. While it can be beneficial, it may also cause a range of side effects, especially if not used correctly or in certain health conditions.

Some women notice changes in their sexual health, like an increase or decrease in libido. Improvements may happen because estradiol helps with dryness and discomfort in the vagina after menopause. However, it can also lead to irritation, unusual discharge, or infections like yeast infections.

Estradiol may cause breast tenderness, pain, or enlargement. Some women experience discharge, while others may develop lumps or changes in breast tissue. It’s important to have regular breast exams and screenings like mammograms.

Digestive issues are also common. You may feel bloated, nauseous, or have cramps, especially when starting therapy. Rarely, more serious problems like gallbladder disease, liver issues, or pancreatitis may occur.

Estradiol can increase the risk of blood clots, stroke, and heart problems, particularly in older women or those with existing heart issues. Monitoring blood pressure during treatment is advised, as estradiol can raise it in some cases.

Headaches are another possible side effect, and severe headaches with vision changes could signal a serious problem, like a stroke. Mood changes such as anxiety, depression, or irritability have also been reported.

Skin and hair reactions may occur, including acne, dark patches on the face, or hair loss. Some women may develop allergic reactions, rashes, or irritation where creams or patches are applied.

Vision changes, like retinal problems or discomfort from contact lenses, have been seen in a few cases. Estradiol may also affect blood sugar control, so people with diabetes should use it with caution.

More serious risks include an increased chance of developing cancers like breast, endometrial (lining of the uterus), or ovarian cancer, especially with long-term use. The risk grows the longer estradiol is used and depends on the dose.

Estradiol should never be used during pregnancy because it may cause serious harm to the developing baby, including birth defects or reproductive problems later in life. It should also be avoided by breastfeeding mothers since small amounts can pass into breast milk.

Important Information About Estradiol Use in Pregnancy, Breastfeeding, and With Other Medications

Pregnancy:

Estradiol and other estrogens should never be used during pregnancy, as they can cross the placenta and harm the developing baby.

Prolonged use during pregnancy may lead to birth defects, such as abnormal development of sexual organs, heart issues, or limb problems.

In some cases, estradiol is used briefly to support fertility treatments, but it is stopped once pregnancy is confirmed.

Breastfeeding:

Estradiol is generally avoided while nursing because it can reduce both the amount and quality of breast milk.

Small amounts of estrogen can pass into breast milk and affect the baby’s health.

It is not recommended for treating breastfeeding issues like engorgement.

Drug Interactions:

Estradiol is processed in the liver and interacts with many other medications.

Certain drugs, such as CYP3A4 inhibitors or inducers, can affect how estradiol is broken down in the body.

Medications like bromocriptine, cyclosporine, corticosteroids, dantrolene, and certain antidepressants may have interactions, leading to increased side effects or altered hormone levels.

Warfarin (a blood thinner) should be used with caution, as estradiol can increase clotting risks.

Estradiol may reduce the effectiveness of some anticonvulsants, antibiotics, antifungals, and herbal supplements like St. John’s wort.

Contraceptive failure may occur when estradiol is combined with drugs like bosentan or modafinil.

Soy supplements might interact with estradiol because of their estrogen-like effects.

Certain sunscreens can increase estradiol absorption if applied too close to treatment time.

Estradiol may interfere with medications like aromatase inhibitors or ursodeoxycholic acid, reducing their effectiveness.

Monitoring and Caution:

Patients should be regularly monitored if taking estradiol with other medications.

Additional or alternative forms of contraception may be needed when estradiol is used with certain drugs.

Any unusual symptoms, side effects, or signs of drug interactions should be reported to a healthcare provider immediately.

Store this medication at 68°F to 77°F (20°C to 25°C) and away from heat, moisture and light. Keep all medicine out of the reach of children. Throw away any unused medicine after the beyond use date. Do not flush unused medications or pour down a sink or drain.

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