Generic Medication guide:
What is Esterase and when is its use appointed?
Estrace is one of the brands for artificial Estradiol which is a hormonal medication. It has the same physiological effect as natural hormone estradiol that is synthesized by the ovaries from the first menstruation and till menopause. If you need to buy Estrace according to your healthcare provider recommendations, you should know that it is manufactured by different companies and can be bought cheaper than the branded Estrace if sold under a less known name.
Short drug info
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Trade names |
Estradiol, Estrace, Evalon, Prognova, Progynova, Aerodiol |
Pregnancy use |
Contraindicated |
Routes of administration |
Oral, sublingual, intranasal, topical/transdermal, vaginal, intramuscular or subcutaneous (as an ester), subdermal implant |
Bioavailability |
Oral: <5% |
Protein binding |
~98%:
Albumin: 60%
SHBG: 38%
Free: 2%
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Metabolism |
Liver (via hydroxylation, sulfation, glucuronidation) |
Biological half-life |
Oral: 13–20 hours
Sublingual: 8–18 hours
Topical (gel): 36.5 hours
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Excretion |
Urine: 54%
Feces: 6%
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The medication causes changes (proliferative) in the endometrium, stimulates the development of genital organs, increases the excitability of the uterus, and inhibits lactation. In addition, estradiol regulates nitrogen metabolism, has a weak anabolic effect, and lowers blood lipids and cholesterol. It helps maintain a balance between osteoclasts and osteoblasts, reduces bone resorption, and promotes its formation.
The benefits of Estrace or its generic use are:
- Improved and timely endometrial rejection and regular period;
- Elevation of thyroxine, iron, copper, etc. in the blood;
- Increased synthesis in the liver of vitamin K-dependent coagulation factors;
- Anti-atherosclerotic effect;
- Lowering of bad cholesterol;
- Modeling of the receptors for to progesterone and normalization of smooth muscle tone;
- Transmission of intravascular fluid in the tissue and compensatory retention of sodium and water;
- Acceleration of leukocytes restoration in myelosuppression associated with radiation damage.
What are the indications for Estrace use?
You can buy generic Estrace for:
- Estrogen deficit in menopause including artificially induced;
- Lack of menstruation, short period, and other menstrual disorders;
- Alopecia with hyperandrogenism;
- Increased body hair growth in polycystic ovary syndrome;
- Vaginitis (in girls and seniors);
- Underdeveloped genitals;
- Infertility;
- Weak labor;
- Prolonged pregnancy;
- To inhibit lactation;
- Hypertrichosis;
- Prevention of osteoporosis;
- Breast cancer in men and women with metastases;
- Prostate carcinoma;
- Urogenital disorders (dyspareunia, vulvovaginitis);
- As a means of stimulating hematopoiesis in men with acute radiation damage.
When the use of Estrace is contraindicated?
- Hypersensitivity,
- Estrogen-dependent cancer or suspected,
- Liver tumors (including history),
- Sickle cell anemia,
- Herpes,
- Otosclerosis (including exacerbation during pregnancy),
- Retinopathy or angiopathy,
- Cholestatic jaundice or persistent itching (including during a previous pregnancy or while taking steroid medictions),
- History of gallbladder disease,
- Unusual genital or uterine bleeding of the unidentified cause,
- Thrombophlebitis or thromboembolic conditions in the active phase (except for breast or prostate cancer);
- Inflammatory diseases of the female genital organs (endometritis);
- Hypercalcemia associated with bone metastases of breast cancer.
If the medication is prescribed for cancer, doctor should assess the risks in case of diseases of the coronary or cerebral vessels, active thrombophlebitis or thromboembolic diseases as the medication can cause aggravation of these conditions.
Application restrictions
- Asthma,
- Diabetes,
- Migraine,
- Seizures,
- Elevated arterial tension,
- Heart failure,
- Coronary heart disease,
- Renal failure,
- Acute or chronic liver diseases (including a history) with a change in the performance of liver function tests,
- Hyperlipoproteinemia,
- Edematous syndrome,
- Endometriosis,
- Fibrocystic mastopathy,
- Porphyria,
- Pituitary tumors,
- Diffuse connective tissue diseases,
- Johnson or Rotor syndrome.
The medication use is prohibited during pregnancy, including presumed (estrogens may have an embryotoxic effect). Studies have shown the association of congenital malformations with the use of certain estrogens during pregnancy.
How to take estradiol?
Inside, without chewing, drinking a small amount of liquid, 2 mg/day, for 21 days, followed by a break of 7 days, after which treatment is continued. The duration of treatment is up to 28 weeks, after which an examination is carried out to decide on the continuation or cessation of the therapy.
In removed uterus or in menopause, treatment can be started any day. With the menstrual cycle preserved, the first pill is taken from the 5th day of the cycle (1 day of the cycle = 1 day of menstruation).
What adverse effects can Estrace cause?
When you buy Estradiol, you should know that its use can cause the following negative effects:
- Lightheadedness, headache, migraine, depression, visual impairment (change in the curvature of the cornea), discomfort when wearing contact lenses.
- From the cardiovascular system and blood (blood formation, hemostasis): elevated arterial tension, thromboembolism.
- From the digestive tract: nausea, vomiting (mainly of central origin when using high doses), pain in the epigastric region, flatulence, diarrhea, anorexia, cholestatic jaundice, cholelithiasis, hepatitis, pancreatitis, intestinal and biliary colic.
- From the genitals system: in women - “breakthrough” bleeding, uterine bleeding of unknown etiology, a change in the nature of uterine bleeding and spotting, metrorrhagia (a sign of an overdose of estradiol), premenstrual syndrome, amenorrhea, dysmenorrhea, an increase in the size of uterine fibroids or leiomyoma, changes in cervical secretion , changes in the nature of vaginal discharge, vaginal candidiasis, endometrial hyperplasia (if prescribed without a progestogen), uterus carcinoma (in menopause with an intact uterus), symptoms of cystitis; sclerosis of the ovaries; soreness, sensitivity and growth of mammary glands, increased libido; in men - soreness and sensitivity of the mammary glands, gynecomastia, decreased libido.
- From the skin: chloasma or melasma, contact dermatitis, hemorrhagic rash, acne, alopecia, hirsutism, pruritus.
- Other: changes in body weight, decreased tolerance to carbohydrates, aggravation of porphyria, spasms of the calf muscles; a violation of the exchange of sodium, calcium and water and as a result, peripheral edema.
Relative and absolute risk seen in the estradiol use vs placebo
Event
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Relative Risk CE/MPA vs placebo at 5.2 Years (95% CI*) (%)
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Absolute Risk per 10,000 Women-years
Number of patients: Estrace – 8506 Placebo - 8102 Placebo vs Estradiol (%)
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Coronary heart disease (Non-fatal)
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1.29 (1.02-1.63)
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30 (37)
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Coronary heart disease death
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1.32 (1.02-1.72)
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6 (7)
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Invasive breast cancer
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1.26 (1.001.59)
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30 (38)
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Stroke
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1.41 (1.07- 1.85)
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21 (29)
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Pulmonary embolism
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2.13 (1.39-3.25)
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8 (16)
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Colorectal cancer
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0.63 (0.430.92)
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16 (10)
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Endometrial cancer
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0.83 (0.471.47)
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6 (5)
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Hip fracture
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0.66 (0.450.98)
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15 (10)
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Death due to causes other than the events above
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0.92 (0.741.14)
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40 (37)
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Deep vein thrombosis
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2.07 (1.492.87)
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13 (26)
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Vertebral fractures
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0.66 (0.440.98)
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15 (9)
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Other osteoporotic fractures
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0.77 (0.690.86)
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170 (131)
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Interactions of Estrace
Before you buy generic Estradiol, consult your doctor if you take any other medicines. Estradiol reduces the activity of diuretics, anticoagulants, blood tension-lowering medications, and hypoglycemic agents. Reduces glucose tolerance (may require adjustment of the dosage regimen of antidiabetic medications). Estradiol enhances the effectiveness of lipid-lowering medicines.
- Inducers of microsomal liver enzymes, for example, some anticonvulsants and antimicrobials (including hydantoins, barbiturates, primidone, carbamazepine, rifampicin), can accelerate the metabolism of estradiol, increase the clearance of sex hormones and reduce clinical effectiveness.
- Folic acid and thyroid medications enhance the effects of estradiol. Significant alcohol consumption during treatment can lead to increased levels of circulating estradiol.
Overdose
Symptoms: nausea, vomiting. Treatment: maintenance of vital functions (against the background of medication withdrawal), symptomatic therapy.
Precautions for the substance Estradiol
- Before starting use, it is necessary to conduct a complete general medical and gynecological examination, including an examination of the abdominal and pelvic organs, mammary glands, blood pressure measurement, cytological analysis of the endometrium. It is necessary to exclude pregnancy. With prolonged therapy, such an examination should be carried out every 6-12 months.
- A month or a month and a half before the planned surgical intervention and/or extended bed rest, the treatment should be interrupted to avoid thrombosis.
- The course must be discontinued without any delay in the following cases: deep vein thrombosis, thromboembolic diseases, a significant rise in the arterial tension, the appearance of jaundice, the appearance of a migraine-like headache, and sudden visual impairment.
- In the use of the medication in hypertension, blood tension should be regularly monitored.
- In the initial period of treatment, individuals with diabetes need careful monitoring due to a possible drop in glucose tolerance.
- Changes in estrogen levels in the blood may affect the performance of certain endocrine and liver functions.
- Estrogens can cause fluid retention and swelling. Thus, individuals with impaired cardiac or renal function need close monitoring. - Inform your doctor about the simultaneous use of barbiturates, phenylbutazone, hydantoins, rifampicin, the appearance of irregular bleeding or unusually heavy bleeding in the breaks between the medication use and discomfort in the abdomen.
- In the event of irregular uterine bleeding, cytological analysis of the endometrium should be performed.
- During treatment, it should be borne in mind that the extended use of estrogen alone in the menopause can lead to endometrial hyperplasia and elevates the risk of uterine cancer. To lower the risks, an additional progestogen is necessary (usually within 10-12 days per month), which leads to the transition of the uterine mucosa to the secretory phase with its rejection and subsequent menstrual bleeding after cessation of progestogen administration. With the appearance of irregular menstrual flow (in women without a removed uterus), diagnostic curettage is necessary to exclude cancer of the uterus.
- Postmenopausal women who use the medication for a long time have raised risk of mammary gland cancer. A regular checkout of the mammary glands is necessary, including they should be taught regular self-examination. Particular caution should be exercised when prescribing the medication to women who have or have had nodular or fibrocystic changes in the mammary glands in the past. In such cases, careful monitoring and regular mammograms are necessary. - In women taking estrogenic drugs during menopause, there is a higher risk of gallstone disease.
- The drug is not a contraceptive and does not restore the ability to fertilize.
Free prescription
Our doctor prescribes online for free, and there is no doctor’s consultation fee.
Discrete packaging
All orders arrive in discrete unmarked parcels. We leave the shipment description blank.
For more answers see the FAQ section
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