Big medical encyclopedia. Estrogens Solution of estradiol in ampoules Latin
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Oestradioli dipropionas Analogs
(generics, synonyms)
Estradiol propionate, Dimenformone dipropionate, Diogin DP, Diovocycline, Estradiol dipropionate, Ovocycline dipropionate, Progynon DP, Sinformon
Recipe (international)
Rp. Sol. Oestradioli dipropionici oleosae 0 1% 1 ml
D.t. d. N; 3 in amp.
S. 1 ml into the muscles 2 times a week.
pharmachologic effect
It has a strong and long-lasting estrogenic effect (similar to the action of female sex hormones - estrogens). Estrogens are female sex hormones produced by the ovaries and the adrenal cortex, causing the development of female genital organs, secondary sexual characteristics, and also promote the proliferation (growth) of endometrial cells (the inner layer of the uterus).
Mode of application For adults:
Intramuscularly in the form of a 0.1% oil solution, 1 ml 1-2 times a week (1 time every 3-5 days). The treatment regimen and duration are selected strictly individually.
Indications
Diseases accompanied by insufficient ovarian function
- with underdevelopment or withering of the ovaries and mammary glands
- absence or irregularities of menstruation
- painful conditions associated with menopause or castration
- for infertility
- to stimulate labor
- to induce labor during post-term pregnancy.
Skin diseases: acne, virile hypertrichosis, etc.
Contraindications
Neoplasms of the genital organs, mammary glands and other organs (in women under 60 years of age), mastopathy (focal compaction in the mammary gland), endrometritis (inflammation of the inner lining of the uterus), tendency to uterine bleeding, hyperestrogenic phase of menopause (menopause period that occurs with increased release of female sex hormones).
Side effects
With prolonged use, uterine bleeding.
Release form
In ampoules of 1 ml of 0.1% oil solution in a package of 3 pieces.
The information on the page you are viewing is created for informational purposes only and does not in any way promote self-medication. The resource is intended to provide healthcare workers with additional information about certain medications, thereby increasing their level of professionalism. The use of the drug "" necessarily requires consultation with a specialist, as well as his recommendations on the method of use and dosage of the medicine you have chosen.
Gross formula
C18H24O2Pharmacological group of the substance Estradiol
Nosological classification (ICD-10)
CAS code
50-28-2Characteristics of the substance Estradiol
Estradiol is a hormonal estrogenic agent (17β-estradiol), identical to endogenous estradiol produced by the ovaries (formed in the body of women, starting from the first menstruation and ending with menopause). Synthetic estradiol is a white crystalline powder. Practically insoluble in water; easily soluble in alcohol; soluble in acetone, dioxane and other organic solvents; difficult to dissolve in vegetable oils. Molecular weight 272.37.
In medical practice, it is used in the form of estradiol hemihydrate and esters (benzoate, dipropionate).
Estradiol benzoate is stable in air; soluble in alcohol, acetone, dioxane, slightly soluble in ether, vegetable oils; molecular weight 376.49.
Estradiol dipropionate is a white crystalline powder, practically insoluble in water, slightly soluble in alcohol and vegetable oils. Molecular weight 384.51.
Estradiol is used in different dosage forms: transdermal gel, oily solution for intramuscular administration, nasal spray, film-coated tablets, transdermal therapeutic system (TDTS).
Pharmacology
pharmachologic effect- estrogenic.Penetrates the target cell by diffusion, is transported to the cell nucleus, where it binds to specific estrogen receptors and forms a receptor-ligand complex. Estrogen receptors have been identified in various tissues, most of them are found in the female genital organs, especially in the uterus, vagina and ovaries, as well as in the mammary glands, pituitary gland, hypothalamus, liver, and bones. The ligand-receptor complex interacts with estrogen effector elements of the genome and specific intracellular proteins, initiates the synthesis of mRNA, protein and the release of cytokines and growth factors.
It has a feminizing effect on the body, stimulates the development of the vagina, uterus, fallopian tubes, stroma and ducts of the mammary glands, pigmentation in the area of the nipples and genitals, the formation of secondary sexual characteristics of the female type (redistribution of adipose tissue, etc.), growth and closure of the epiphyses of the long tubular bones. Promotes timely endometrial rejection and regular bleeding, in high concentrations it causes endometrial hyperplasia, suppresses bone resorption, induces the synthesis of a number of transport proteins (transcortin, thyroxine-binding globulin, sex hormone-binding protein, transferrin), fibrinogen. Increases blood concentrations of thyroxine, iron, copper, etc.; has a procoagulant effect, increases the synthesis of vitamin K-dependent coagulation factors (II, VII, IX, X) in the liver, reduces the amount of antithrombin III. It has anti-atherosclerotic activity, increases HDL content, reduces LDL and cholesterol (triglyceride levels increase); modulates progesterone receptors and sympathetic regulation of smooth muscle tone, causes the transition of intravascular fluid into tissues and compensatory retention of sodium and water; in large doses it prevents the degradation of endogenous catecholamines (competes for active catechol-O-methyltransferase receptors). It has the ability to accelerate the recovery of the number of leukocytes (neutrophils) in myelodepression associated with radiation damage.
After oral administration, it is quickly and completely absorbed (bioavailability is about 100%). During the “first pass” through the liver, it is metabolized to less active products - estrone and estriol. In the blood it is almost completely bound to proteins. Metabolites are excreted by bile into the lumen of the small intestine and reabsorbed (enterohepatic circulation). The final loss of activity occurs as a result of oxidation in the liver. Biodegradation products are excreted mainly by the kidneys in the form of sulfates and glucuronides; Small amounts of estradiol, estrone and estriol are also found in the urine.
After application of TDTS, estradiol is released from the patch and enters the bloodstream transdermally at a constant rate, maintaining a given level of the hormone in the blood. When used in the form of a gel and patch, estradiol is not subject to the “first pass” effect through the liver, as a result of which fluctuations in plasma estrogen levels are significantly less pronounced than when taking estrogens orally. With weekly application of TDTS, it is possible to achieve serum estradiol levels similar to those created during the early follicular phase of reproductive life, with a serum estradiol/estrone ratio of approximately 1. The absolute value of serum estradiol levels is directly proportional to the surface area of the patch. The average steady-state concentration of estradiol in serum is about 40 pg/ml (12.5 cm2 patch) and about 80 pg/ml (25 cm2 patch). 24 hours after removal of TDTS, the concentrations of estradiol and estrone in the serum decrease to the initial value. When applying the patch, the concentrations of estradiol conjugates in the urine increase 5-10 times and return to the initial level within 2 days after removal of the system.
When applied in the form of a gel, estradiol penetrates the skin, with most of it entering the systemic circulation immediately, and a certain amount is retained in the subcutaneous fat and is released into the bloodstream gradually. Tmax - 3-4 hours, bioavailability - 82%.
When using the TDTS patch and gel, the metabolism and excretion correspond to the metabolism and excretion of natural estrogens. Does not accumulate.
Use of the substance Estradiol
Estrogen deficiency during menopause and surgical menopause, incl.
Skin diseases: acne, virile hypertrichosis, etc.
Hypersensitivity, estrogen-dependent neoplastic processes or suspicion of them, liver tumors (including a history), sickle cell anemia, herpes, otosclerosis (including exacerbation during pregnancy), retinopathy or angiopathy, cholestatic jaundice or permanent pruritus (including worsening during a previous pregnancy or while taking steroid medications), history of gallbladder disease (especially cholelithiasis), unusual or undiagnosed genital or uterine bleeding (estrogens may interfere with diagnosis), thrombophlebitis or thromboembolic conditions in the active phase (except for treatment of breast or prostate cancer); thrombophlebitis, thrombosis or thromboembolic conditions associated with estrogen use (history); inflammatory diseases of the female genital organs (salpingoophoritis, endometritis); hypercalcemia associated with bone metastases of breast cancer.
Only for the treatment of breast and prostate cancer (additionally): diseases of the coronary or cerebral vessels, active thrombophlebitis or thromboembolic diseases (high doses of estrogens used for treatment increase the risk of myocardial infarction, pulmonary embolism, thrombophlebitis).
Restrictions on use
Bronchial asthma, diabetes mellitus, migraine, epilepsy, arterial hypertension, heart failure, coronary artery disease; renal failure; acute or chronic liver diseases (including a history) with changes in liver function tests, hyperlipoproteinemia, edema syndrome, endometriosis, fibrocystic mastopathy, porphyria, pituitary tumors, diffuse connective tissue diseases, Dubin-Johnson or Rotor syndrome.
Use during pregnancy and breastfeeding
Contraindicated during pregnancy, incl.
suspected (estrogens can have embryotoxic effects). Studies have shown an association between congenital malformations and the use of certain estrogens during pregnancy.
During treatment, it is necessary to stop breastfeeding (estrogens pass into breast milk).
Side effects of the substance Estradiol From the nervous system and sensory organs:
dizziness, headache, migraine, depression, chorea, visual impairment (change in corneal curvature), discomfort when wearing contact lenses. increased blood pressure, thromboembolism.
From the gastrointestinal 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 genitourinary system: in women - breakthrough bleeding, uterine bleeding of unknown etiology, changes in the nature of uterine bleeding and spotting, metrorrhagia (a sign of estradiol overdose), premenstrual syndrome, amenorrhea, dysmenorrhea, an increase in the size of fibroids or uterine leiomyomas, changes in cervical secretion, changes in the nature of vaginal discharge , vaginal candidiasis, endometrial hyperplasia (when prescribed without progestogen), endometrial carcinoma (in menopausal women with an intact uterus), symptoms of cystitis (without bacterial infection); with long-term use - ovarian sclerosis; soreness, sensitivity and enlargement of the mammary glands, increased libido; in men - pain and sensitivity of the mammary glands, gynecomastia, decreased libido.
From the skin: chloasma or melasma, contact dermatitis, hemorrhagic rash, erythema nodosum, erythema multiforme, alopecia, hirsutism, itching and hyperemia of the skin (at the site of application of the TDTS patch).
Other: changes in body weight, decreased tolerance to carbohydrates, worsening of porphyria, spasms of the calf muscles; with long-term use - disruption of the metabolism of sodium, calcium and water with the formation of peripheral edema.
Interaction
Estradiol reduces the activity of diuretics, anticoagulants, antihypertensive and hypoglycemic agents. Reduces glucose tolerance (adjustment of the dosage regimen of hypoglycemic drugs may be required). Estradiol increases the effectiveness of lipid-lowering drugs.
Inducers of microsomal liver enzymes, such as 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 effect of estradiol. Significant alcohol consumption during treatment may result in increased circulating estradiol levels.
Overdose
Symptoms: nausea, vomiting, and in some cases metrorrhagia.
Treatment: maintenance of vital functions (during drug withdrawal), symptomatic therapy.
Routes of administration
Inside, locally, intranasally, intramuscularly.
Precautions for the substance Estradiol
Before starting use, it is necessary to conduct a complete general medical and gynecological examination, including examination of the abdominal and pelvic organs, mammary glands, blood pressure measurement, and cytological analysis of the endometrium. Pregnancy must be excluded. During long-term therapy, such examinations should be carried out every 6-12 months.
4-6 weeks before the planned surgical intervention and during a period of prolonged immobilization, it is recommended to interrupt treatment to avoid thrombosis.
The drug should be stopped immediately in the following cases: deep vein thrombosis, thromboembolic diseases, significant increase in blood pressure, the appearance of jaundice, the appearance of a migraine-like headache, sudden blurred vision.
During hormone replacement therapy in patients with hypertension, blood pressure should be regularly monitored.
In the initial period of treatment, patients with diabetes mellitus require careful monitoring due to a possible decrease in glucose tolerance.
Changes in estrogen levels in the blood may affect some endocrine and liver function tests.
Estrogens can cause fluid retention in the body, so patients with impaired cardiac or renal function require careful monitoring.
It is necessary to inform your doctor about the simultaneous use of barbiturates, phenylbutazone, hydantoins, rifampicin, the appearance of irregular bleeding or unusually heavy bleeding in the period between the use of the drug, discomfort in the epigastric region.
If irregular uterine bleeding occurs while taking the drug, a cytological analysis of the endometrium should be performed.
During treatment, it should be taken into account that long-term use of estrogen alone during menopause can lead to endometrial hyperplasia and increases the risk of developing endometrial cancer. To reduce the risk of developing endometrial cancer, additional intake of progestogen is necessary (usually for 10-12 days a month), which leads to the transition of the uterine mucosa into the secretory phase with its rejection and subsequent menstrual-like bleeding after stopping the administration of progestogen. If irregular menstrual flow appears (in women with an intact uterus) during treatment with estradiol, a diagnostic curettage is necessary to exclude a malignant neoplasm of the uterus.
Postmenopausal women on long-term hormone replacement therapy have an increased risk of breast cancer. When treatment lasts more than 5 years, the positive effects of treatment must be carefully weighed against the adverse effects.
In patients undergoing long-term treatment, regular examination of the mammary glands is necessary, incl.
They should be taught to do regular self-examination. Particular caution should be exercised when prescribing estrogens to women who have or have had in the past nodular or fibrocystic changes in the mammary glands. In such cases, careful monitoring and regular mammography are necessary.
Women taking estrogen drugs during menopause have an increased risk of cholelithiasis (estrogens increase the lithogenicity of bile).
The drug is not a contraceptive and does not restore the ability to fertilize.
The patch should not be placed on the breast or waist area. If the patch is applied correctly, you can take a bath or shower, but keep in mind that the patch may come off in hot water. Name:
Estradiol dipropionate (Oestradiolidipropionas)
Pharmacological effects:
It has a strong and long-lasting estrogenic effect (similar to the effect of female sex hormones - estrogens). Estrogens are female sex hormones produced by the ovaries and the adrenal cortex, causing the development of female genital organs, secondary sexual characteristics, and also promote the proliferation (growth) of endometrial cells (the inner layer of the uterus).
Estradiol dipropionate - indications for use:Used in the same cases as folliculin.
Estradiol dipropionate - method of application:Intramuscularly in the form of a 0.1% oil solution, 1 ml 1-2 times a week (1 time every 3-5 days). The treatment regimen and duration are selected strictly individually.
Estradiol dipropionate - side effects:With prolonged use, uterine bleeding.
ContraindicationsEstradiol dipropionate - contraindications:
Release formEstradiol dipropionate - release form:
Estradiol dipropionate - storage conditions:List B. In a place protected from light.
Estradiol dipropionate - synonyms:Estradiol propionate, Dimenformone dipropionate, Diogin DP, Diovocycline, Estradiol dipropionate, Ovocycline dipropionate, Progynon DP, Sinformon.
Important! Before using the medicine you should consult your doctor. This instruction is intended for informational purposes only.
Estradiol monobenzoate(Oestradiolum monobenzoicum). The ester of estradiol and monobenzoic acid is a long-acting drug.
Its pharmacological action is similar to folliculin.
Indications and contraindications for use are the same as for the use of folliculin.
Treatment carried out in combination with progestins, taking into account the menstrual cycle.
Estradiol dipropionate(Oestradiolum dipropionicum). Estradiol and propionic acid ester is a synthetic drug containing 20,000 units per 1 mg.
Indications and the contraindications are the same as for estradiol monobenzoate.
Recipe:
Rp. Sol. Oestradioli dipropionici oleosae 0.1% 1.0
D.t. d. N. 10 in ampul. S. 1 ml every 3 days intramuscularly
Sinestrol(Synoestrolum). Synthetic estrogen, the action is identical to folliculin.
Indications and contraindications are the same as for folliculin.
It is used in injections or tablets taking into account the menstrual cycle and subsequent administration of progesterone. For adenoma and prostate cancer, it is prescribed to men. As a side effect, feminization, enlargement of the mammary glands, loss of mustache and beard, and decreased potency are observed.
Diethylstilbestrol(Diaethylstilboestroluin). A synthetic drug whose action is similar to folliculin.
1 mg of the drug corresponds to 20,000 units. Indications and contraindications are the same as for folliculin.
Treatment must be carried out taking into account the menstrual cycle, followed by the introduction of progesterone.
In case of overdose, dyspepsia, vomiting, and sometimes occur. Other estrogenic drugs include microfollin, which is much more effective than estradiol. The composition of each tablet is 0.05 mg ethinyl estradiol.
Microfollin(Microfollinum). Ethinyl estradiol.
Indications: dysmenorrhea, hyper- and hypomeorrhea, bleeding at a young age, menopause and other painful conditions caused by folliculin deficiency. The contraindications are the same as for sinestrol.
The drug microfollip-forte contains 0.00005 g in 1 tablet.
Octestrol(Octoestrolum). The action of the drug is identical to sinestrol.
Indications and contraindications are the same as for sinestrol.
Dienestrol acetate(Dienoestrolum aceticum). A synthetic drug whose action is similar to diethylstilbestrol. Indications and contraindications for use are the same.
Dimestrol(Dimoeslrolum). Diethylstilbestrol dimethyl ether has a prolonged effect. It is used intramuscularly once a week. One 2 ml ampoule contains 24,000 units.
Akrofollin(Acrofollinum). Contains 1 - 5 mg of estradiol monopropionate per ml. Available in ampoules and tablets.
Phosfestrol(Phosphoestrolum). Diphosphoric ester of diethylstilbestrol. This drug is effective against prostate cancer. Blocks the enzymatic synthesis of ribonucleic acid and thereby complicates protein synthesis.
A drug phosphoestrol Available in tablets and ampoules of 5 ml of 5% or 10% solution of tetrasodium salt of fosfestrol. Used intravenously at 2.5-5 ml for 20 days.
Composition of the medicinal product Before using the medicine
Active ingredient: Estradiol.