Proginova drajee 2mg #21

Proginova instruction for use

Reed more and buy Proginova on this page

See also - Cyclo-Proginova

Composition

1 tablet (tablet) of Proginova contains 2 mg of estradiol valerate.
Additionally: 46.25 mg of lactose monohydrate; 3 mg of povidone 25,000; 26.2 mg of corn starch; 2,4 mg of talc; 33.54 mg of crystalline sucrose; 0.15 mg magnesium stearate; 3,719 mg of macrogol 6000; 0.323 mg of povidone 700,000; 14.572 mg precipitated calcium carbonate; 0.205 mg 85% glycerol; 7,104 mg of talc, 0.411 mg of titanium dioxide; 0.075 mg of montangicolic wax; 0.051 mg of indigocarmine.

Form of issue

Therapeutic Proginova is produced in the form of pills (tablets) No. 21 in a pack.

pharmachologic effect

Filling shortage of endogenous estrogen (estrogenic).

Pharmacodynamics and pharmacokinetics

Estradiol valerate, which is an active ingredient in Proginova, is estrogen (a female sex hormone), which when taken orally (inward) is converted into the human body in its natural 17β-estradiol. When taking this medication, the hormonal synthesis in the body itself is not actually registered and there is no suppression of the process of exit from the ovary of the ovum, so the use of Proginova and ovulation are compatible.
The function of the exogenous estradiol obtained from outside is to compensate for the shortage of female estrogens observed after the formation of menopause and to provide effective therapy for autonomic and psycho-emotional climacteric symptoms (including hot flashes, muscle and joint pain, hyperhidrosis, decreased libido, sleep disturbance, cardialgia, high nervous excitability, headaches, irritability, dizziness, palpitations). Also, the drug helps to reduce the manifestations of involution of the skin and mucous membranes, especially with regard to the genitourinary system (including irritation and dryness in the vagina, urinary incontinence, painful sexual intercourse).
Replacement hormone therapy (HRT) with an appropriately selected dosage of estrogen, which is found in Proginova's medication, during the postmenopause is favorable for reducing bone resorption, and also inhibits or completely eliminates the loss of bone tissue. The positive effect of prolonged HRT has been proven with respect to the risk of peripheral bone fractures in postmenopausal women. In the case of discontinuation of HRT, the rates of reduction in bone mass of patients were observed, comparable to those characteristic of the period immediately after menopause. However, complete restoration of bone tissue to pre-menopausal values ​​during HRT was not proven.
The beneficial effects of HRT have also been observed with respect to skin density, collagen concentration in the skin, and even in terms of slowing down the formation of wrinkles. Conducting such therapy leads to a decrease in LDL and total cholesterol levels and an increase in the content of HDL and triglycerides. Adherence to the treatment of gestagens to a certain extent can interfere with the effect of estradiol on metabolic processes. In general, metabolic effects of HRT are regarded as positive and contribute to reducing the risk of cardiovascular pathology in women during the postmenopause.
When passing therapy with Proginova using women with a non-removed uterus, in order to reduce their possible hyperplasia of the endometrium and the appearance of adenocarcinoma, a parallel reception of the progestogen (a restraining factor for endometrial growth) is shown for at least 10 days in each cycle.

When taking estradiol valerate orally (inside), its rapid and almost complete absorption is observed. During the absorption and first passage of the steroid ester through the liver, it splits into valeric acid and estradiol, which in turn undergoes further significant transformations to estrone of sulfate, estriol, estrone, etc. The bioavailability of estradiol in internal administration is only 3%, in independence from the food taken in parallel.
Serum Cmax estradiol is approximately 30 pg / ml and is fixed already 4-9 hours after its oral administration, then decreases and after 24 hours it is half as much (15 pg / ml).
Estradiol mainly binds to proteins albumin and globulin, which bind sex steroids (GSPC). The serum free estradiol free fraction is approximately 1-1.5%, in contrast to the fraction of the HSH-bound substance, equal to 30-40%. With a single intravenous administration of estradiol, its apparent Vd is at a level of 1 L / kg.
After completion of the hydrolysis of estradiol valerate, its further metabolic transformations are identical to endogenous estradiol. The main organ that takes part in its metabolism is the liver, additional biotransformation takes place in the kidneys, intestines, target organs and skeletal muscles. These processes lead to the release of estriol, estrone, catecholestrogens and their glucuronide and sulfate conjugates, which have significantly lower estrogenic efficacy or none at all.
The serum clearance of estradiol, with its single-valued intravenous administration, is quite variable and is in the range of 10-30 ml / min / kg. A certain amount of estradiol is excreted with bile and passes through intestinal hepatic recirculation. The products of estradiol metabolism are mainly excreted by the kidneys in the form of glucuronides and sulfates.
The serum concentration of estradiol with multiple parenteral application is twice that of its plasma level, observed with its single administration. The minimum serum level of estradiol is 30 pg / l, and the maximum level is 60 pg / l. The concentrations of estradiol metabolism products exceed the concentration of the main drug (estrone approximately 8 times, estrone sulfate approximately 150 times). When Proginova discontinues therapy, the levels of estrone and estradiol return to the primary values ​​during 2-3 days.

Indications for use

The use of the therapeutic agent Proginova is shown:
    for HRT in the case of a diagnosed deficiency of estrogens that occurred due to the onset of sterilization or natural menopause;
    with observed involuntary changes in the genitourinary system and skin, menopausal disorders and depressive states associated with menopause;
    with the goal of preventing the progression of osteoporosis in postmenopausal women.

Contraindications

Prescribing HRT using Proginova is prohibited when:
    vaginal bleeding of an unexplained origin;
    thromboembolism or arterial thrombosis (including manifestations of stroke and myocardial infarction);
    pregnancy;
    breast cancer (including suspicions of its formation);
    deep vein thrombosis, which is in the stage of exacerbation;
    breastfeeding;
    observed thromboembolism (including indication of it in the anamnesis);
    hormone-dependent malignant education or hormone-dependent precancerous pathologies (including suspicions of the possibility of developing these disease states);
    severe hypertriglyceridemia;
    any tumors of the liver (malignant, benign), diagnosed at present or observed in the anamnesis;
    increased personal sensitivity to any of the ingredients of the tablets;
    severe hepatic pathologies;
    high probability of vein thrombosis;
    intolerance to sugars;
    up to 18 years.
In the event that any of the above conditions occur, it is necessary to immediately stop treatment during HRT.

With special care, they assign Proginova to:

    manifestations of cholestatic jaundice;
    arterial hypertension;
    endometriosis;
    diabetes mellitus;
    uterine myoma;
    congenital hyperbilirubinemia (including the syndromes of Rotor, Dubin-Johnson, Gilbert).

Side effects

    change in weight (in one direction or another);
    hypersensitivity phenomena;
    bloating;
    decreased mood;
    muscle spasms;
    nausea, vomiting;
    sense of anxiety;
    rash / itching;
    change in libido (in one direction or another);
    dyspepsia;
    acne;
    headache;
    hirsutism;
    dizziness;
    erythema nodosum;
    vaginal discharge;
    migraine;
    edema;
    impaired vision;
    dysmenorrhea;
    intolerance of used contact lenses;
    weakness;
    palpitation;
    hives;
    stomach ache;
    vaginal, uterine bleeding (including spotting);
    increased sensitivity or tenderness of the mammary glands;
    symptomatic complex of PMS.
When taking Proginova tablets, there were occasional side effects, manifested by thromboembolism and deep vein thrombosis.
With prolonged monotherapy with estrogen preparations, the risk of developing endometrial cancer or hyperplasia increases.
Based on the results of the observational and clinical studies, an increase in the relative risk of developing breast tumors against women undergoing HRT (including Proginova's treatment) was detected over several years.
Reception of sex hormones (including estradiol) in rare cases promoted the development of benign neoplasms, even less often the formation of malignant liver tumors. In isolated cases, these neoplasms led to intra-abdominal bleeding, which could pose a threat to the life of the patient.

In some women predisposed to this, the appearance of cholelithiasis was noted when taking estrogens.
Limited data are available on the likely increase in the risk of dementia in patients after 65 years of age starting HRT.
Occasionally, manifestations of chloasma were observed, especially in women with a history of previous pathology.
Patients with a hereditary predisposition to angioedema may develop or worsen the symptoms of Quincke's edema.

Proginova, instructions for use

Instructions for use Proginova recommends oral ingestion of tablets in whole form, with a small amount of water.
In case of taking the drug by women with unattached uterus and continuing menstruation, it is necessary to start therapy in conjunction with some gestagen at the beginning of the menstrual cycle, namely in the first 5 days. Patients with fairly rare menstruation, as well as women in postmenopausal women, can be treated at any time, previously excluding a possible pregnancy.
Each blister (primary packaging) includes 21 pills and is accordingly designed for a 21-day course of therapy with a daily intake of the 1st pill. After each such therapeutic course (21 days), it is possible to interrupt the treatment, which takes an average of 1 week (for cyclic HRT), or continue to receive daily pills (for continuous HRT). In this case, the first dragee of the new blister should be taken the day after the Proginova tablets in the previous blister have run out.
Women who have not been removed from the uterus before starting treatment with Proginova are recommended to take an adequate gestagenic drug in parallel. For cyclic combined HRT, gestagen is taken for 10-14 days after every 28 days of therapy, and for continuous combined HRT - together with each subsequent pellet of estrogen.
The intake of Proginova tablets can be performed at any time convenient for a woman, however with the preservation of the specific daily time of taking each subsequent pellet. In case of an accidental miss of taking another tablet, it should be taken within the next 12-24 hours. With a longer break in therapy, bleeding may develop.

Overdose

When taking Proginova doses, many times exceeding the therapeutic daily dosage, there were no serious negative manifestations. The symptomatology of such an overdose is usually limited to nausea with possible vomiting and the occurrence of vaginal bleeding.
There is no specific antidote to estradiol. The treatment for such conditions should correspond to the observed negative manifestations.

Interaction

In the case of the appointment of HRT with Proginova, a woman should stop using hormonal contraceptives (with their previous intake). If necessary, non-hormonal contraceptives or methods may be recommended to the patient.
Long-term therapy with drugs that are inducers of liver enzymes (including some antimicrobial and anticonvulsant medications) can increase the clearance of sex hormones and reduce their clinical effectiveness. Drugs with similar liver enzyme inducing properties include: carbamazepine, barbiturates, hydantoins, primidon and rifampicin, and also presumably: Felbamate, Oxcarbazepine, Griseofulvin and Topiramate. The most pronounced induction of hepatic enzymes is usually observed 2-3 weeks after the initiation of treatment and can persist for 4 weeks after the abolition of therapy.
In some rare cases, concurrent antibiotic therapy (for example, tetracycline and penicillin drugs) can lead to a decrease in the concentration of estradiol.
Medications significantly exposed to the conjugation process (Paracetamol and the like) may increase the bioavailability of estradiol due to competitive inhibition of conjugation during the absorption of the drug.
Due to the impact of HRT on the tolerance of the human body to glucose, in some cases there may be a change in the patient's need for insulin and / or oral antidiabetic drugs.

Storage conditions

The maximum permissible temperature of storage of the preparation is 30 ° C.
Shelf life - 5 years.

special instructions

In the case of HRT, patients who have a history of a significant risk of thrombosis or a smaller amount of risk factors for thrombosis should consider the likelihood of a reciprocal enhancement of the effects of these factors and treatment compared to the formation of thromboses. In such cases, the overall significance of the observed risk factors increases. If the patient has a high risk of developing thrombosis, the appointment of Proginova is contraindicated.
Before the onset of HRT and afterwards at the entire stage of treatment, at approximately equal intervals (at least once every six months), the patient should be prescribed a gynecological examination and examination of the mammary glands, as well as to measure blood pressure and, if necessary, conduct other tests.
Women suffering from prolactinoma and taking Proginova should undergo a periodic medical examination at the entire stage of HRT with a determination of the level of prolactin.
If HRT is necessary in relation to patients with one or more of the disease states listed below, continuous and close medical attention may be required. In this regard, in the event that at least one of these conditions is detected in her, the woman is obliged to inform her doctor about this before the start of Proginova's reception.

Painful conditions requiring special care for HRT:

    uterine fibroids;
    epilepsy;
    chorea;
    endometriosis (present or transferred in the past);
    systemic lupus erythematosus;
    pathology of the gallbladder and / or liver (after the previous hepatitis, Proginova's appointment is possible only after a lapse of 6 months, with the complete normalization of all hepatic functions);
    otosclerosis;
    jaundice (observed with past pregnancy or previous therapy with sex hormones);
    porphyria;
    diabetes;
    elevated serum triglycerides;
    arterial hypertension;
    migraine;
    Chloasma (present or transferred in the past);
    bronchial asthma;
    mastopathy;
    high probability of vein thrombosis.
The risk of possible formation of vein thrombosis increases with age, as well as with excess weight, varicose veins and indications for it in a family history.
Temporary increase in the risk of deep vein thrombosis is observed in patients who have suffered serious injuries, surgical interventions, or in a state of prolonged immobility. In case of planning any operations against the background of HRT, the patient must inform the doctor in advance about it (for 4-6 weeks).
Carry out HRT for the prevention of stroke or heart attack is not recommended.
The following warnings apply to all drugs used in HRT, including Proginova's drug.

In the case of monotherapy with estrogens, especially with their continued use, the likelihood of developing a cancer of the uterine mucosa (endometrial cancer) increases. If the uterus is kept in the patient, HRT should be taken in conjunction with drugs that reduce this risk, for which purpose Proginova is prescribed with a parallel administration of progestational drugs.
A woman who watches herself in the background of using Proginova, frequent breakthrough or irregular bleeding, should inform her doctor about this.
Based on the results of several studies, a certain increase in the incidence of breast cancer in women undergoing HRT has been demonstrated in comparison with their peers who do not take hormonal drugs. The relative risk of this pathology increases with the time of estrogen alone, but may be reduced or absent completely. The tendency to increase the risk of formation of breast tumors is almost identical to that of women with alcoholism, obesity or a later development of natural menopause. The increased likelihood of such a cancer is gradually reduced to the average figure during the first years after refusal of HRT.
Carrying out HRT also contributes to the increase in mammographic density of female mammary glands, which can adversely affect the radiographic definition of breast cancer and sometimes requires the use of alternative methods for detecting cancer.
During the epidemiological study, there was a slight increase in the risk of ovarian cancer in patients on estrogen replacement therapy for a fairly long time (more than 10 years). At the same time, analysis of 15 other studies did not demonstrate an increase in this risk. At this time, these data are controversial.
In isolated cases with the intake of drugs that include sex hormones, the occurrence of benign liver tumors was noted, malignant tumors of this organ were even less common. Sometimes bleeding from such tumor formations into the abdominal cavity threatened the life of the patient. The association of such adverse events with HRT has not been proven. Despite the fact that the occurrence of such episodes is unlikely, in case of finding unusual negative feelings at the top of the abdomen, continuing for a fairly long period of time, the patient should inform them about it to her doctor.
Also the patient is obliged to inform the attending physician about any revealing of the following painful conditions:
    sudden auditory and visual disturbances;
    phlebitis (inflammation of veins);
    unusually severe and / or frequent headaches;
    the first developed migraine attack (with manifestations of nausea and pulsating pain and with a previous impairment of vision function);
    worsening of attacks of already existing migraines.
In the case of the formation of thrombosis on the background of the use of Proginova or even suspicion of the possibility of its occurrence, it is necessary to immediately stop the treatment and undergo a medical examination.
An alarming manifestation of the possible formation of thromboses are:
    sudden shortage of air;
    cough accompanied by blood;
    loss of consciousness;
    unexplained pain in the extremities and / or their rapid puffiness.
Immediate discontinuation of taking Proginova tablets requires the development of jaundice and the detection of pregnancy.
With therapy with the use of sex hormones, errors in the results of some laboratory tests can occur. If it is necessary to conduct any clinical study, you need to inform the doctor about taking Proginova.
The medicine Proginova can not be considered as a contraceptive. If it is necessary to use contraception, a woman needs to use nonhormonal methods or means (excluding the temperature and calendar method). At the first suspicion of a possible pregnancy, dragee Proginova is suspended until exclusion or confirmation of pregnancy.

Data on the need to adjust the dosage regimen Proginova in the treatment of elderly patients (after 65 years) are absent. There are limited references to the possibility of increasing the risk of developing dementia in women 65 years of age and older starting HRT. If it is necessary to assign Proginova to patients over 65, the doctor should be cautious.
The use of Proginova in patients with liver / kidney pathologies has not been studied. According to some data there is no need to adjust the dosages of Proginova in these pathologies.

Divigel or Proginova - which is better?

Comparison of these two drugs in principle reduces to their dosage form, since the active ingredient and the main effect of these medications are identical. Dragee (tablets) Proginova and Divigel gel contain estradiol, are prescribed for the same painful conditions and differ only in the way they are applied (the gel is applied externally and the tablets are taken orally). Often the scheme of HRT involves the sequential use of both drugs with the initial intake of tablets and a smooth transition to the use of the gel. In this case, the appointment of one of these drugs or their consistent application should be based on the individual characteristics of the female body and its response to the method of administration of the drug.

Children

The medicine Proginova is not prescribed until 18 years.

With alcohol

By and large, Proginova and alcohol are incompatible. During the course of HRT, excessive drinking of alcoholic beverages can lead to an increase in the level of the circulating active ingredient of the drug, estradiol.

During pregnancy (and lactation)

The official instruction to the drug prohibits the appointment of Proginova to pregnant and lactating women, and in case of pregnancy, when taking medication, it is recommended to interrupt the therapy, from which it can be concluded that Proginova and pregnancy are incompatible.
Quite the opposite situation can be traced with the use of Proginova in the planning of pregnancy, where this drug has been used for a long time and quite successfully, as with the usual preparation of a woman for conception and pregnancy after IVF (in vitro fertilization). The fact that the active substance of tablets - estradiol - actively replenishes the deficiency of this endogenous hormone in the female body, promotes thickening of the uterine endometrium, prepares the general hormonal background for conception and bearing. It has been clinically proven that Proginova and ovulation are fully compatible. Therapeutic dosages of estradiol do not interfere, but more often on the contrary help the normal maturation, the release of the egg and its fixation in the endometrium of the uterus, which in many cases leads to the long-awaited conception and full-fetal bearing of the fetus.

Reviews about Proginova

The drug Proginova, doctors' reviews about which in relation to her key action is mostly positive, is one of the most prescribed hormonal drugs for women in the postmenopausal period. In most cases HRT with its use has a beneficial effect on all aspects of women's health after menopause and helps to overcome many negative phenomena associated with the cessation of menstruation and changes in the hormonal background.
Reviews about Proginova in planning pregnancy are not so unambiguous and include both positive and negative aspects of such therapy, depending on the personal response of the female body to the intake of estradiol from the outside. In this case, the effectiveness, as well as the manifestations of side effects of Proginova, are purely individual and can only be elucidated during the course of treatment.