Active substanceEstradiol valerateEstradiol valerate
Similar drugsTo uncover
  • Proginova®
    pills inwards 
    Bayer Pharma AG     Germany
  • Dosage form: & nbsppills
    Composition:

    1 dragee contains:

    active components: estradiol valerate - 2.0 mg;

    auxiliary components: lactose monohydrate 46.25 mg, corn starch 26.2 mg, povidone 25,000 3 mg, talc 2.4 mg, magnesium stearate 0.15 mg, sucrose crystalline 33.54 mg, povidone 700,000 0.323 mg macrogol 6000 - 3.719 mg, calcium carbonate precipitated - 14.572 mg, talc - 7.104 mg, glycerol 85% - 0.205 mg, titanium dioxide - 0.411 mg, indigocarmine - 0.051 mg, wax montaglycol - 0.075 mg.

    Description:

    21 dragees of blue color.

    Pharmacotherapeutic group:estrogen
    ATX: & nbsp

    G.03.C.A.03   Estradiol

    Pharmacodynamics:

    Proginova® contains estrogen- estradiol valerate, which in the human body turns into a natural 17β-estradiol. Against the background of taking Proginova®, there is no suppression of ovulation, and the production of hormones in the body practically does not change.

    Estradiol replenishes the estrogen deficiency in the female body after the onset of menopause and provides effective treatment for psychoemotional and vegetative climacteric symptoms (such as "hot flashes", increased sweating, sleep disturbances, increased nervous excitability, irritability, palpitations, cardialgia, dizziness, headache, decreased libido,muscular and joint pain); involution of the skin and mucous membranes, especially the mucosal genitourinary system (urinary incontinence, dryness and irritation of the vaginal mucosa, tenderness in sexual intercourse).

    HRT with an adequate dose of estrogen, such as occurs in Proginove®, reduces bone resorption and delays or stops the loss of bone mass in postmenopausal women. Long-term use of hormone replacement therapy (HRT) has been shown to reduce the risk of fracture of peripheral bones in women after menopause. With the abolition of HRT, the rate of bone mass reduction is comparable to that characteristic for the period immediately after menopause. It is not proven that using HRT, it is possible to achieve bone mass recovery to the pre-menopausal level.

    HRT also has a beneficial effect on the content of collagen in the skin, as well as on its density, and can also slow the process of wrinkle formation.

    HRT leads to a reduction in total cholesterol, low-density lipoprotein (LDL) cholesterol, and high-density lipoprotein (HDL) cholesterol, and an increase in triglyceride levels.The addition of a progestogen can to a certain extent inhibit the effect of estradiol on metabolism. In general, the metabolic effects of HRT are considered positive and are believed to be involved in reducing the risk of cardiovascular disease in postmenopausal women.

    For women with a non-removed uterus, when Proginova® is used, an additional gestagen should be taken for at least 10 days in each cycle. This reduces the risk of developing endometrial hyperplasia and the concomitant risk of adenocarcinoma in women in this group.

    Pharmacokinetics:

    Absorption

    After ingestion estradiol valerate quickly and completely absorbed. During the absorption and the first passage through the liver, the steroid ester is split into estradiol and valeric acid. In the same time, estradiol is largely subjected to further metabolization, for example, to estrone, estriol and estrone sulfate. After oral administration, only about 3% of estradiol becomes bioavailable. The intake of food on the bioavailability of estradiol has no effect.

    Distribution

    The maximum concentration of estradiol in the serum, about 30 pg / ml, is usually achieved 4-9 hours after taking the pills.After 24 hours after administration, the serum estradiol level is reduced to a concentration of approximately 15 pg / ml.

    Estradiol binds to albumin and to globulin that binds to sex steroids (GSH). The free fraction of estradiol in the serum is about 1-1.5%, and the fraction of the substance bound to the GSPC is in the range of 30-40%.

    The apparent volume of distribution of estradiol after a single intravenous administration is about 1 l / kg.

    Metabolism

    After hydrolysis of estradiol valerate, the substance passes through the same biotransformation pathways as the endogenous estradiol. Estradiol it is metabolized mainly in the liver, and also partially in the intestines, kidneys, skeletal muscles and target organs. These processes are accompanied by the formation of estrone, estriol, catecholestrogens, as well as sulfate and glucuronide conjugates of these compounds, all of which have significantly less estrogenic activity or none have estrogenic activity.

    Excretion from the body

    The clearance of estradiol from serum after a single intravenous administration is characterized by a high degree of variability in the range of 10 to 30 ml / min / kg. A certain part of estradiol is excreted with bile and is subjected to intestinal-hepatic recirculation.Metabolites of estradiol are mainly excreted in the urine in the form of sulfates and glucuronides.

    The equilibrium concentration

    The concentration of estradiol in serum after repeated administration is approximately twice as high as after the administration of a single dose. On average, the concentration of estradiol in the serum ranges from 30 pg / l (minimum level) to 60 pg / l (maximum level). The concentration of estrone (the weaker estrogen) is about 8 times, and the concentration of estrone sulfate is about 150 times higher than the concentration of estradiol. After stopping Proginova®, the concentrations of estradiol and estrone return to their initial values ​​within 2-3 days.

    Indications:

    - Replacement hormone therapy (HRT) in menopausal disorders, involuntary changes in the skin and genitourinary tract, depressive conditions in the climacteric period, as well as symptoms of estrogen deficiency due to natural menopause or sterilization.

    - Prevention of postmenopausal osteoporosis.

    Contraindications:

    It is not recommended to start hormone replacement therapy (HRT), in the presence of any of the diseases / conditions listed below.If any of these circumstances occur during HRT, then immediately stop using the drug.

    - Pregnancy and lactemia

    - Bleeding from the vagina of unknown origin

    - Proven or suspected breast cancer

    - Proven or presumed hormone-dependent precancerous diseases or hormone-dependent malignant tumors

    - Tumors of the liver at present or in the anamnesis (benign or malignant)

    - Severe liver disease

    - Acute arterial thrombosis or thromboembolism (such as myocardial infarction, stroke)

    - Deep vein thrombosis in the acute stage, thromboembolism now or in the anamnesis

    - The presence of a high risk of venous and arterial thrombosis

    - Severe hypertriglyceridemia

    - Hypersensitivity to any component of Proginova ®

    - Congenital deficiency of lactase, sucrose / isomaltase, lactose intolerance, glucose galactose malabsorption

    - Children and adolescence under 18 years.

    Carefully:

    Preparation Proginova® should be administered with caution in the following diseases: hypertension,congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson and Rotor syndrome), cholestatic jaundice or cholestatic pruritus during pregnancy, endometriosis, uterine myoma, diabetes mellitus (see "Special instructions").

    Pregnancy and lactation:

    HRT is not prescribed during pregnancy or lactation. If pregnancy is detected during the administration of Proginova ®, the drug should be discontinued. Large-scale epidemiological studies of steroid hormones used for contraception or HRT did not reveal an increased risk of developing birth defects in children born in women who took such hormones before pregnancy, as well as teratogenic effects of hormones when they were accidentally taken in the early stages of pregnancy. A small amount of sex hormones can be excreted in the mother's milk.

    Dosing and Administration:

    Dragee is taken whole, washed down with a small amount of liquid.

    If the patient retains the uterus and the menstruation is still on, take Proginova® in combination with some gestagen in the first 5 days of the menstrual cycle.However, patients with very rare menstruation, as well as postmenopausal women, can start taking the drug at any time, provided that pregnancy is excluded.

    Each package is designed for a 21-day reception. Every day take one dragee.

    When prescribing Proginova ® in the premenopause, a cyclic regimen is used. In this case, after each 21-day course, take a break in taking the drug, usually 7 days or less (cyclic HRT).

    At appointment in a postmenopause continue to accept dragees daily (continuous HRT). In the latter case, the dragees from the new package are taken as soon as the dragees have run out in the previous package.

    Combined treatment regimen

    Women with a preserved uterus are advised to take an additional progestin for 10-14 days every 4 weeks (cyclic combined HRT) or together with each estrogen pellet (continuous combined HRT). The physician must prescribe the necessary progestational drug to achieve the recommended combination therapy.

    The time of day when a woman takes the drug does not matter, however, if she starts taking the pills at any particular time, then you should stick to this time and continue.If the woman forgot to take the pills, she should take it as soon as possible. If treatment is interrupted for more than 24 hours, bleeding may occur.

    Side effects:

    System of organs /

    Class of disorders

    Often

    (>1/100)

    Infrequently

    (> 1/1000 and <1/100 )

    Rarely

    (<1/1000)

    Immune

    system

    Reactions

    hypersensitivity

    Metabolism

    Changes in body weight (decrease or increase)

    Mental

    disorders

    Decrease

    moods

    Anxiety,

    change of libido

    (increase or

    decrease)

    Nervous system

    Head

    pain

    Dizziness

    Migraine

    Body of sight

    Visual disturbances

    Intolerance

    contact lenses

    (unpleasant

    sensations when wearing them)

    Cardiovascular

    system

    Palpitation

    Gastrointestinal tract

    Abdominal pain, nausea

    Dyspepsia

    Bloating,

    vomiting

    Skin and subcutaneous tissue

    Rash,

    pruritus

    Nodular erythema,

    hives

    Hirsutism,

    acne

    The musculoskeletal system,

    connecting

    the cloth

    Muscle spasms

    Reproductive

    system,

    dairy

    gland

    Uterine, vaginal

    bleeding, incl. bleeding bleeding

    Pain in the mammary glands, increasing the sensitivity of the mammary glands

    Dysmenorrhea,

    highlighting

    of

    vagina,

    symptom complex

    premenstrual

    syndrome (PMS),

    enlargement

    mammary glands

    General and local disorders

    Edema

    Weaknesses

    When taking the drug in rare cases, it is possible to develop deep vein thrombosis and thromboembolism (see also "Special instructions").

    With prolonged monotherapy with estrogen, the risk of developing hyperplasia or endometrial cancer increases.

    According to clinical and observational studies, an increase in the relative risk of breast cancer in women taking HRT, which includes Proginova®, has been detected for several years.

    Against the background of the use of sex hormones, which include and means for HRT, in rare cases, there were benign, and even less often, malignant liver tumors. In some cases, these tumors led to a life-threatening intra-abdominal bleeding.

    Some women are predisposed to the development of cholelithiasis in treatment with estrogen.

    There are limited data showing an increased likelihood of dementia risk in women starting hormone replacement therapy at the age of 65 and older.

    In some cases, there may be a chloasma, especially in women with a history of pregnant women with chloasma.

    In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen symptoms of angioedema.

    Overdose:

    There was no risk of a serious risk of acute side effects when the drug was taken inadvertently in quantities many times greater than the daily therapeutic dose.

    Symptoms, which can occur during an overdose: nausea, vomiting, vaginal bleeding.

    There is no specific antidote, treatment symptomatic.

    Interaction:

    At the beginning of HRT, it is necessary to stop the use of hormonal contraceptives. If necessary, the patient should recommend non-hormonal contraceptives.

    Long-term treatment with drugs that induce liver enzymes (for example, some anticonvulsant and antimicrobial drugs) can increase the clearance of sex hormones and reduce their clinical effectiveness. A similar property of inducing liver enzymes was found in hydantoids, barbiturates, primidon, carbamazepine and rifampicin, the presence of this feature is also assumed in oxcarbazepine, topiramate, felbamate and griseofulvin.The maximum induction of enzymes is usually observed not earlier than 2-3 weeks, but then it can persist for at least 4 weeks after discontinuation of the drug.

    In rare cases, along with the concomitant use of certain types of antibiotics (for example, penicillin and tetracycline groups), a decrease in the level of estradiol was observed.

    Substances that are highly conjugated (for example, paracetamol), can increase the bioavailability of estradiol due to competitive inhibition of the conjugation system in the absorption process.

    Due to the effect of HRT on glucose tolerance, in some cases, the need for oral antidiabetics or insulin may change.

    - Interaction with alcohol

    Excessive consumption of alcohol during HRT may lead to an increase in the level of circulating estradiol.

    Special instructions:

    Proginova® is not used for contraception. If it is necessary to use contraception, non-hormonal methods should be used (with the exception of calendar and temperature methods).

    If you suspect a pregnancy, you should stop taking the pills until the pregnancy is excluded (see "Pregnancy and lactation").

    In the presence or deterioration of any of the following conditions or risk factors, before starting or continuing with Proginova®, the relationship between individual benefit and the risk of treatment should be assessed.

    When prescribing Proginova® to women who have several risk factors for thrombosis or a high degree of severity of one of the risk factors, the possibility of mutual strengthening of the effect of risk factors and the drug on the development of thrombosis should be taken into account. In such cases, the total value of the available risk factors is increased. In the presence of high Proginova ® preparation is contraindicated.

    - Venous thromboembolism

    In a number of controlled randomized clinical, as well as epidemiological studies, an increased relative risk of venous thromboembolism (VTE) in the background of HRT, i.e. thrombosis of deep veins or thromboembolism of the pulmonary artery.

    Therefore, when prescribing Proginova® to women with risk factors for VTE, the risk-benefit ratio should be carefully weighed and discussed with the patient.

    Risk factors for VTE development include individual and family history (the presence of VTE in close relatives in a relatively youngage may indicate a genetic predisposition) and severe obesity. The risk of VTE also increases with age. The question of the possible role of varicose veins in the development of VTE remains controversial.

    The risk of VTE may temporarily increase with prolonged immobilization, "large" planned and traumatological operations or massive trauma. Depending on the cause or duration of immobilization, the expediency of temporarily discontinuing Proginova® should be decided. Immediately discontinue treatment if there is or suspected thrombosis symptoms.

    - Arterial thromboembolism

    In two large clinical trials, a possible increase in the risk of coronary artery disease during the first year of admission and the absence of a positive effect on this risk during follow-up are sketched in women with a combination of conjugated estrogens and medroxyprogesterone acetate in a constant mode. In one major clinical study, using only EFE, a potential reduction in the incidence of coronary artery disease among women aged 50-59 years was found in the absence of a general positive effect among the population of the study.As a secondary result, in two large-scale clinical studies with the use of EFS as monotherapy or in combination with MPA, a 30-40% increase in the risk of developing ischemic stroke was found. Therefore, it is not known whether this increased risk extends to HRT preparations containing other types of estrogens and progestogens or to non-oral methods of use.

    - Endometrial cancer

    With prolonged monotherapy with estrogen, the risk of developing hyperplasia or endometrial cancer increases. Studies have confirmed that with the addition of gestagens, this risk is reduced.

    - Mammary cancer

    According to clinical and observational studies, an increase in the relative risk of breast cancer in women using HRT for several years has been found. This may be due to earlier diagnosis, the acceleration of growth of an already existing tumor in the background of HRT, or a combination of both.

    The relative risk increases with the duration of estrogen monotherapy, but may be absent or decreased. This increase is comparable to the increased risk of breast cancer in women with a later onset of natural menopause, as well as obesity and alcohol abuse.The increased risk gradually decreases to the usual level during the first few years after discontinuation of HRT.

    Assumptions regarding the increased risk of developing breast cancer are based on the results of more than 50 epidemiological studies.

    Data on the prevalence of breast cancer beyond the breast are controversial.

    In two large-scale, randomized trials with EFS in monotherapy or in combination with MPA, after approximately 6 years of HRT use, estimated risk values ​​of 0.77 (95% confidence interval: 0.59-1.01) or 1.24 (95 % confidence interval: 1.01-1.54), respectively. It is not known whether this increased risk also extends to other products for HRT, which include the Proginova® preparation.

    HRT increases the mammographic density of the mammary glands, which in some cases may have a negative impact on the radiographic detection of breast cancer.

    - Ovarian Cancer

    During the epidemiological study, there was a slight increase in the risk of ovarian cancer in women who use estrogen replacement therapy (EST) for a long time (more than 10 years). At the same time, a meta-analysis of 15 studies did not reveal an increased risk in the use of EST.However, these data are currently controversial.

    - Liver tumors

    Against the background of the use of sex hormones, which include and means for HRT, in rare cases, there were benign, and even less often, malignant liver tumors. In some cases, these tumors led to a life-threatening intra-abdominal bleeding. With pain in the upper abdomen, enlarged liver, or signs of intra-abdominal bleeding in differential diagnosis, the probability of a liver tumor should be taken into account.

    - Cholelithiasis

    It is known that estrogens increase the lithogenicity of bile. Some women in the treatment with estrogen are predisposed to the development of cholelithiasis.

    - Dementia

    There are limited data showing an increased likelihood of dementia risk in women starting hormone replacement therapy at the age of 65 and older. The risk can be reduced if the use of HRT is started in early menopause, as observed in studies. It is not known whether this applies to other preparations of HRT, which include Proginova®.

    - Other states

    Immediately stop treatment when migraine-like or frequent and unusually severe headaches occur, as well as when other symptoms appear - possible precursors of ischemic stroke.

    The relationship between HRT and the development of clinically significant arterial hypertension has not been established. Women taking HRT have reported a slight increase in blood pressure, but a clinically significant increase is rare. However, in some cases, with the development of a clinically significant hypertension in the presence of HRT, the cancellation of Proginova® can be considered.

    In case of mild violations of the liver function, including various forms of hyperbilirubinemia, such as Dubin-Johnson syndrome or Rotor syndrome, it is necessary to observe the doctor, as well as periodic studies of liver function. With worsening of liver function, Proginova® should be discontinued.

    In case of recurrence of cholestatic jaundice or cholestatic pruritus observed for the first time during pregnancy or previous treatment with sex steroid hormones, it is necessary to immediately stop taking Proginova®.

    Special care is required for women with moderately elevated concentrations of triglycerides. In such cases, the use of HRT may cause a further increase in the concentration of triglycerides in the blood, which increases the risk of acute pancreatitis.

    Although HRT can affect glucose resistance and glucose tolerance in peripheral insulin, there is usually no need to change the treatment regimen for diabetic patients with HRT. However, women with diabetes mellitus should be monitored when using Proginova®.

    In some patients, HRT may cause unwanted estrogen stimulation, such as abnormal uterine bleeding. Frequent or persistent abnormal uterine bleeding against the background of treatment is an indication for endometrial research to eliminate organic disease.

    Under the influence of estrogens, the myomatous nodes of the uterus can increase in size. In this case, treatment should be discontinued.

    It is recommended to stop treatment with the development of recurrence of endometriosis with the use of Proginova ®.

    If you suspect a prolactinoma before starting treatment, you should exclude this disease. In case of detection of prolactinoma, the patient should be under close medical supervision (including periodic evaluation of prolactin concentration).

    In some cases, there may be a chloasma, especially in women with a history of pregnant women with chloasma. During HRT, women with a tendency to develop chloasma should avoid prolonged exposure to sunlight or ultraviolet radiation.

    The following conditions may occur or worsen in the background of HRT. Although their relationship with HRT is not proven, women with these conditions should be under the supervision of a doctor when using Proginova®: epilepsy; benign breast diseases; bronchial asthma; migraine; porphyria; otosclerosis; systemic lupus erythematosus; chorea.

    In women with hereditary forms of angioedema, exogenous estrogens can cause or worsen symptoms of angioedema.

    Additional Information

    There is no data on the need for dose adjustment in women under 65 years of age. When using Proginova ® in women over 65 years of age, you should take into account the information provided in the section "Special instructions".

    The use of Proginova ® in women with impaired hepatic function not studied.

    The use of Proginova ® in women with impaired renal function not studied. The available data indicate that there is no need for dose adjustment in such patients.

    Medical examination and counseling

    Before starting or resuming the use of Proginova®, you should familiarize yourself with the patient's medical history and perform a physical and gynecological examination. The frequency and nature of such surveys should be based on existing standards of medical practice, taking into account the individual characteristics of each patient (but not less than once in 6 months) and should include measurement of blood pressure, assessment of the mammary glands, abdominal organs and pelvic organs, including cytological examination of the epithelium of the cervix.

    Influence on the results of laboratory studies

    Admission of sex hormones can affect the biochemical parameters of the liver, thyroid, adrenal and kidney function,on the plasma content of transport proteins, such as corticosteroid-binding globulin, lipid / lipoprotein fractions, carbohydrate metabolism, coagulation and fibrinolysis.

    Effect on the ability to drive transp. cf. and fur:Not found.
    Form release / dosage:Dragee, 2 mg.
    Packaging:

    Cyclonic packages containing 21 tablets of blue color.

    21 dragees per blister.

    1 blister in a pack of cardboard.

    Storage conditions:

    Store at a temperature not higher than 30 ° C.

    Keep out of the reach of children.

    Shelf life:

    5 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N013529 / 01
    Date of registration:15.07.2009
    The owner of the registration certificate:Bayer Pharma AGBayer Pharma AG Germany
    Manufacturer: & nbsp
    Representation: & nbspBAYER, AOBAYER, AO
    Information update date: & nbsp02.10.2015
    Illustrated instructions
      Instructions
      Up