Estradiol

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Estradiol Information

Brand Name: Estrace

Generic Names: Estradiol, Generic Estrace

Other Common Names: Primogyn

Estradiol Indications:

Estradiol tablets are indicated in the:

Treatment of moderate to severe vasomotor symptoms associated with the menopause. There is no adequate evidence that estrogens such as contained in Estradiol are effective for nervous symptoms or depression which might occur during menopause and they should not be used to treat these conditions.

Treatment of vulval and vaginal atrophy.
Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.
Treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease.
Treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).
Prevention of osteoporosis.

Estradiol Ingredients and Composition

How Does Estradiol Work?

Estrogen drug products such as Estradil act by regulating the transcription of a limited number of genes. Estrogens diffuse through cell membranes, distribute themselves throughout the cell, and bind to and activate the nuclear estrogen receptor, a DNA-binding protein which is found in estrogen-responsive tissues. The activated estrogen receptor binds to specific DNA sequences, or hormone-response elements, which enhance the transcription of adjacent genes and in turn lead to the observed effects. Estrogen receptors have been identified in tissues of the reproductive tract, breast, pituitary, hypothalamus, liver, and bone of women.

Estrogens such as are contained in Estradil are important in the development and maintenance of the female reproductive system and secondary sex characteristics. By a direct action, they cause growth and development of the uterus, fallopian tubes, and vagina. With other hormones, such as pituitary hormones and progesterone, they cause enlargement of the breasts through promotion of ductal growth, stromal development, and the accretion of fat. Estrogens are intricately involved with other hormones, especially progesterone, in the processes of the ovulatory menstrual cycle and pregnancy, and affect the release of pituitary gonadotropins. They also contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones that allow for the pubertal growth spurt and its termination, and pigmentation of the nipples and genitals.

Estrogens occur naturally in several forms. The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. This is converted primarily to estrone, which circulates in roughly equal proportion to estradiol, and to small amounts of estriol. After menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone especially in its sulfate ester form is the most abundant circulating estrogen in postmenopausal women. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than estrone or estriol at the receptor.

Estrogens used in Estradil, and therapy in general are well absorbed through the skin, mucous membranes, and gastrointestinal tract. When applied for a local action, absorption is usually sufficient to cause systemic effects. When conjugated with aryl and alkyl groups for parenteral administration, the rate of absorption of oily preparations is slowed with a prolonged duration of action, such that a single intramuscular injection of estradiol valerate or estradiol cypionate is absorbed over several weeks.

Administered estrogens and their esters are handled within the body essentially the same as endogenous hormones. Metabolic conversion of estrogens occurs primarily in the liver (first pass effect), but also at local target tissue sites. Complex metabolic processes result in a dynamic equilibrium of circulating conjugated and unconjugated estrogenic forms which are continually interconverted, especially between estrone and estradiol and between esterified and unesterified forms. Although naturally-occurring estrogens circulate in the blood largely bound to sex hormone-binding globulin and albumin, only unbound estrogens enter target tissue cells. A significant proportion of the circulating estrogen exists as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogenic species. A certain proportion of the estrogen is excreted into the bile and then reabsorbed from the intestine. During this enterohepatic recirculation, estrogens are desulfated and resulfated and undergo degradation through conversion to less active estrogens (estriol and other estrogens), oxidation to nonestrogenic substances (catecholestrogens, which interact with catecholamine metabolism, especially in the central nervous system), and conjugation with glucuronic acids (which are then rapidly excreted in the urine).

When given orally, as is the case with Estradil, naturally-occurring estrogens and their esters are extensively metabolized (first pass effect) and circulate primarily as estrone sulfate, with smaller amounts of other conjugated and unconjugated estrogenic species. This results in limited oral potency. By contrast, synthetic estrogens, such as ethinyl estradiol and the nonsteroidal estrogens, are degraded very slowly in the liver and other tissues, which results in their high intrinsic potency. Estrogen drug products administered by non-oral routes are not subject to first-pass metabolism, but also undergo significant hepatic uptake, metabolism, and enterohepatic recycling.

How To Take Estradiol and Estradiol Dosage and Administration

For treatment of moderate to severe vasomotor symptoms, vulval and vaginal atrophy associated with the menopause, the lowest Estradiol dose and regimen that will control symptoms should be chosen and medication should be discontinued as promptly as possible: Attempts to discontinue or taper Estradiol should be made at 3-month to 6-month intervals.

The usual initial Estradiol dosage range is 1 to 2 mg daily of estradiol adjusted as necessary to control presenting symptoms. The minimal effective Estradiol dose for maintenance therapy should be determined by titration. Administration should be cyclic (e.g., 3 weeks on and 1 week off).

For treatment of female hypoestrogenism due to hypogonadism, castration, or primary ovarian failure: Treatment is usually initiated with an Estradiol dose of 1 to 2 mg daily, adjusted as necessary to control presenting symptoms; the minimal effective Estradiol dose for maintenance therapy should be determined by titration.

For treatment of breast cancer, for palliation only, in appropriately selected women and men with metastatic disease: Suggested dosage is 10 mg three times daily for a period of at least three months.

For treatment of advanced androgen-dependent carcinoma of the prostate, for palliation only: Suggested Estradiol dosage is 1 to 2 mg three times daily. The effectiveness of therapy can be judged by phosphatase determinations as well as by symptomatic improvement of the patient.

For the prevention of osteoporosis: Therapy with Estradiol tablets to prevent postmenopausal bone loss should be initiated as soon as possible after menopause. A daily dosage of 0.5 mg should be administered cyclically (i.e., 23 days on and 5 days off). The Estradiol dosage may be adjusted if necessary to control concurrent menopausal symptoms. Discontinuation of estrogen replacement therapy may re-establish the natural rate of bone loss.

If you suspect a Estradiol Overdose

Serious ill effects have not been reported following acute ingestion of large doses of estrogen-containing oral contraceptives by young children. Overdosage of Estradiol may cause nausea and vomiting, and withdrawal bleeding may occur in females.

Estradiol Side Effects

Estradiol Warnings

Taking Estradiol during Pregnancy or Breast-feeding

As a general principle, the administration of any drug to nursing mothers should be done only when clearly necessary since many drugs are excreted in human milk. In addition, Estradiol administration to nursing mothers has been shown to decrease the quantity and quality of the milk.

Estradiol Precautions and Contraindications

Addition of a Progestin: Studies of the addition of a progestin for 7 or more days of a cycle of estrogen administration (such as Estradil) have reported a lowered incidence of endometrial hyperplasia which would otherwise be induced by estrogen treatment. Morphological and biochemical studies of endometrium suggest that 10 to 14 days of progestin are needed to provide maximal maturation of the endometrium and to eliminate any hyperplastic changes. There are possible additional risks which may be associated with the inclusion of progestins in estrogen replacement regimens. These include: (1) adverse effects on lipoprotein metabolism (lowering HDL and raising LDL) which may diminish the possible cardioprotective effect of estrogen therapy (see Drug/Laboratory Test Interactions); (2) impairment of glucose tolerance; and (3) possible enhancement of mitotic activity in breast epithelial tissue (although few epidemiological data are available to address this point). The choice of progestin, its dose, and its regimen may be important in minimizing these adverse effects, but these issues will remain to be clarified.
Physical Examination: A complete medical and family history should be taken prior to the initiation of any estrogen therapy. The pretreatment and periodic physical examinations should include special reference to blood pressure, breasts, abdomen, and pelvic organs, and should include a Papanicolaou smear. As a general rule, estrogen should not be prescribed for longer than one year without reexamining the patient.
Hypercoagulability: Some studies have shown that women taking estrogen replacement therapy have hypercoagulability, primarily related to decreased antithrombin activity. This effect appears dose- and duration-dependent and is less pronounced than that associated with oral contraceptive use. Also, postmenopausal women tend to have increased coagulation parameters at baseline compared to premenopausal women. There is some suggestion that low dose postmenopausal mestranol may increase the risk of thromboembolism, although the majority of studies (of primarily conjugated estrogens users) report no such increase. There is insufficient information on hypercoagulability in women who have had previous thromboembolic disease.
Familial Hyperlipoproteinemia: Estrogen therapy may be associated with massive elevations of plasma triglycerides leading to pancreatitis and other complications in patients with familial defects of lipoprotein metabolism.
Fluid Retention: Because estrogens may cause some degree of fluid retention, conditions which might be exacerbated by this factor, such as asthma, epilepsy, migraine, and cardiac or renal dysfunction, require careful observation.
Uterine Bleeding and Mastodynia: During Estradiol therapy certain patients may develop undesirable manifestations of estrogenic stimulation, such as abnormal uterine bleeding and mastodynia.
Impaired Liver Function: Estrogens may be poorly metabolized in patients with impaired liver function and should be administered with caution.

Estradiol 2 mg tablets contain FD&C yellow no. 5 (tartrazine) which may cause allergic-type reactions (including bronchial asthma) in certain susceptible individuals. Although the overall incidence of FD&C yellow no. 5 (tartrazine) sensitivity in the general population is low, it is frequently seen in patients who also have aspirin hypersensitivity.

Contraindications to Estradiol

Estrogens such as is contained in Estradiol should not be used in individuals with any of the following conditions:

Known or suspected pregnancy. Estrogens may cause fetal harm when administered to a pregnant woman.

Undiagnosed abnormal genital bleeding.
Known or suspected cancer of the breast except in appropriately selected patients being treated for metastatic disease.
Known or suspected estrogen-dependent neoplasia.
Active thrombophlebitis or thromboembolic disorders

Storing Estradiol

Store Estrace at controlled room temperature 15-30°C (59-86°F).

Additional Patient Information for Estradiol

Your doctor has prescribed Estradiol for you and you alone. Do not give the drug to anyone else.

If you will be taking calcium supplements as party of the treatment to help prevent osteoporosis, check with your doctor about how much to take.

Keep this and all drugs out of the reach of children. In case of overdose, call your doctor, hospital or poison control center immediately.