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1 dragee (tablet) of drug of Proginov includes 2 mg of oestradiol of valerate.
In addition: 46,25 mg of monohydrate of lactose; 3 mg of povidone 25000; 26,2 mg of corn starch; 2,4 mg of talc; 33,54 mg of crystal sucrose; 0,15 mg of magnesium stearate; 3,719 mg of a macrogoal 6000; 0,323 mg of povidone 700000; 14,572 mg of the besieged calcium carbonate; 0,205 mg of 85% of a glitserol; 7,104 mg of talc, 0,411 mg of titanium dioxide; 0,075 mg of montanglikolevy wax; 0,051 mg of indigo carmine.
Medical Proginova is made in the form of a dragee (tablets) No. 21 in a pack.
(Oestrogenic) compensating for the deficiency of endogenous estrogen.
Pharmacodynamics and pharmacokinetics
Oestradiol the valerate which is active ingredient of drug of Proginov represents estrogen (female sex hormone) which at reception orally will (inside) be transformed in a human body in natural to it 17β-эстрадиол. At reception of this drug change of hormonal synthesis in the organism actually is not registered and suppression of process of an exit of an ovum ovary in this connection use of drug of Proginov and an ovulation are compatible is not observed.
Function exogenous (received from the outside) oestradiol consists in completion of the lack of women's estrogen noted later formations of a menopause and in ensuring effective therapy of vegetative and psychoemotional climacteric symptomatology (including inflow, muscular and joint pains, a hyperhidrosis, decrease a libido, a sleep disorder, cardialgias, high nervous irritability, headaches, irritability, dizziness, heartbeat). Also drug promotes decrease in manifestations of involution of integuments and mucous membranes, in particular, as for urinogenital system (including irritation and dryness in a vagina, an urine incontience, morbidity of sexual intercourse).
The Replacement Hormonal Therapy (RHT) with adequately picked up estrogen dosage which just is present at medicine of Proginov in the period of a postmenopause favors to decrease in a bone resorption, and also brakes or completely levels loss of a bone tissue. Positive impact of long ZGT in relation to risk of emergence at women in a postmenopause of fractures of bones of the periphery was proved. In case of the termination of ZGT observed the rates of reduction of bone mass of patients comparable to the indicators inherent in the span coming right after a menopause. However and a complete recovery of a bone tissue to premenopausal values when carrying out ZGT it was not proved.
Beneficial influence of ZGT was also observed in relation to density of skin, concentration of collagen in integuments and even regarding delay of processes of formation of wrinkles. Carrying out such therapy leads to reduction of the LPNP levels and the general cholesterol and to increase in maintenance of LPVP and triglycerides. Accession to treatment of a gestagen to some extent can interfere with influence of oestradiol on processes of a metabolism. In total metabolic effects of the carried-out ZGT are regarded as the positive and promoting decrease in risk formations of cardiovascular pathologies at women in the period of a postmenopause.
When passing therapy using Proginova by women with not a remote uterus, for the purpose of decrease at them a possible hyperplasia of an endometria and emergence of an adenocarcinoma, showed parallel reception of a gestagen (a restraining factor for growth of an endometria) for not less than 10 days in each cycle.
At valerate oestradiol reception its fast and almost full absorption orally is (inside) observed. In the course of absorption and the first passing of steroid ether through a liver there is its splitting on valerianic acid and oestradiol which, in turn, is exposed to further considerable transformations to estrone of sulfate, estriol, estrone and so forth. Bioavailability of oestradiol at internal reception equals only 3%, in independence of food eaten in parallel.
Serumal Cmax of oestradiol approximately makes 30 pg/ml and is fixed in 4-9 hours after its oral administration, then decreases and in 24 hours becomes twice less (15 pg/ml).
Oestradiol generally contacts proteins albumine and globulin which connect sexual steroids (GSPS). The serumal estradiolovy free fraction makes about 1-1,5%, unlike the fraction of the connected GSPS of substance equaling 30-40%. At one-time its seeming Vd is in administration of oestradiol at the level of 1 l/kg.
After completion of process of hydrolysis of valerate of oestradiol its further metabolic transformations are identical to endogenous oestradiol. The main body which is taking part in its metabolism is the liver, additional biotransformation occurs in kidneys, intestines, target organs and muscles of a skeleton. These processes lead to release of estriol, estrone, the katekholestrogen and their glyukuronidny and sulphatic conjugates possessing considerably smaller oestrogenic efficiency or in general without that.
The serumal clearance of oestradiol, at its single in introduction, quite variable also is in range of 10-30 ml/min. A quantity of oestradiol is excreted with bile and passes through enterohepatic recirculation. Products of a metabolism of oestradiol are generally removed by kidneys in the form of glucuronides and sulfates.
Serumal concentration of oestradiol at repeated parenteral use twice exceeds its plasma level observed at its single introduction. The minimum serumal level of oestradiol equals 30 pg/l, and maximum — 60 pg/l. Concentration of products of a metabolism of oestradiol exceed concentration of the main drug (estrone approximately by 8 times, estrone sulfate approximately by 150 times). At the termination of therapy of Proginova levels of estrone and oestradiol return to primary values for 2-3 days.
Indications to use
Use of a remedy of Proginov is shown:
- for carrying out ZGT in case of the diagnosed lack of estrogen which occurred owing to approach of sterilization or a natural menopause;
- at the observed involute changes of urinogenital system and integuments, climacteric frustration and depressions connected with a menopause;
- for the purpose of prevention of progressing of osteoporosis in a postmenopause.
It is forbidden to appoint ZGT using Proginov's drug at:
- vulval bleedings of the obscure nature of emergence;
- thrombembolia or arterial thrombosis (including displays of a stroke and myocardial infarction);
- breast cancer (including suspicions on its forming);
- the deep vein thrombosis which is in an aggravation stage;
- feeding by a breast;
- observed thromboembolism (including instructions on it in the anamnesis);
- hormonedependent malignancy or hormonedependent precancerous pathologies (including suspicions on a possibility of development of these painful states);
- the expressed gipertriglitseridemiya;
- any tumors of a liver (malignant, high-quality) diagnosed now or observed in the anamnesis;
- the increased personal sensitivity to any of ingredients of tablets;
- heavy hepatic pathologies;
- high probability of vein thromboses;
- intolerance of sugars;
- till 18 years.
In case of emergence any of above-mentioned painful states during ZGT it is necessary to stop treatment immediately.
With extra care appoint Proginova at:
- displays of cholestatic jaundice;
- arterial hypertension;
- diabetes mellitus;
- to hysteromyoma;
- inborn hyperbilirubinemias (including Rotor syndromes, the Cudgel Johnson, Gilbert).
- change of weight (in this or that party);
- hypersensitivity phenomena;
- abdominal distention;
- decrease in mood;
- muscular spasms;
- feeling of alarm;
- change of a libido (in this or that party);
- knotty erythema;
- vaginal allocations;
- vision disorder;
- intolerance of the used contact lenses;
- small tortoiseshell;
- abdominal pains;
- vulval, uterine bleedings (including the smearing allocations);
- increase of sensitivity or morbidity of mammary glands;
- PMS symptom complex.
At reception of tablets of Proginov sometimes noted the side effects which are shown emergence of thromboembolisms and deep vein thrombosis.
At long monotherapy by drugs of estrogen the risk of forming of cancer of an endometria or a hyperplasia increases.
By results of carrying out the observation and clinical trials increase of relative risk of developing of tumors of a mammary gland concerning the women passing ZGT (including Proginova's reception) for several years was revealed.
Reception of sex hormones (including oestradiol) in rare instances promoted development of high-quality new growths, is even more rare to forming of malignant tumors of a liver. In isolated cases these new growths led to the intra belly bleeding able to pose threat for the patient's life.
At some women predisposed to it at reception of estrogen noted developing of cholelithiasis.
There are limited data on probable increase in risk of dementia at patients after 65 years beginning ZGT.
Sometimes observed manifestations of a hloazma, in particular at women with this pathology in the anamnesis at the previous pregnancy.
At patients with genetic predisposition to Quincke's diseases the Quincke's edema symptomatology can arise or worsen.
Proginova, application instruction
The application instruction of Proginova recommends oral administration of a dragee (tablets) of drug in the whole look, washing down with the small volume of water.
In case of administration of drug by women with not a remote uterus and the proceeding periods, in a complex with any gestagen it is necessary to start therapy at the beginning of a menstrual cycle, namely in the first 5 days. To patients with rather rare periods, as well as to women in a postmenopause, it is possible to appoint treatment at any time, previously having excluded possible pregnancy.
Each blister (primary packaging) includes 21 dragees and is respectively counted on carrying out a 21-day course of therapy with daily reception of the 1st tablet. After each such therapeutic course (21 days) allow a possibility of a break in treatment which on average takes 1 week (for cyclic ZGT), or continue daily reception of a dragee (for continuous ZGT). In this case the first dragee from the new blister needs to be accepted next day after Proginov's tablets in the previous blister ended.
To women at whom before an initiation of treatment using Proginova the uterus was not removed, recommend to accept adequate gestagenny drug in parallel. For the cyclic combined ZGT gestagen accept for 10-14 days every 28 days therapy, and for the continuous combined ZGT – together with each subsequent dragee of estrogen.
Reception of tablets of Proginov can be carried out in any time of day convenient to the woman, however with preservation of specific daily time of reception of each subsequent dragee. In case of the accidental admission of reception of the next tablet it should be accepted for the next few 12-24 hours. At more long break in therapy development of bleeding is possible.
At reception of the doses of Proginova which are repeatedly exceeding a therapeutic daily dosage, serious negative manifestations it was not revealed. The symptomatology of such overdose is usually limited to nausea with possible vomiting and developing of vaginal bleeding.
The specific antidote to oestradiol does not exist. Carried out treatments of similar states has to correspond to observed negative manifestations.
In case of purpose of ZGT using Proginova, the woman needs to stop using hormonal contraceptives (at their previous reception). If necessary it is possible to recommend to the patient non-hormonal contraceptive drugs or methods.
Long therapy by the drugs which are inductors of liver enzymes (including some antimicrobic and anticonvulsant remedies) can increase clearance of sex hormones and reduce their clinical performance. With the similar properties inducing liver enzymes carry to drugs: Carbamazepine, barbiturates, hydantoins, Primidonum and Rifampicin, and also allegedly: Felbamat, Okskarbazepin, Griseofulvin and Topiramat. The most expressed induction of liver enzymes, as a rule, is observed in 2-3 weeks after an initiation of treatment and can remain for 4 weeks after therapy cancellation.
The remedies which considerably are exposed to conjugation process (Paracetamol and to it similar drugs), can increase bioavailability of oestradiol because of competitive inhibition of processes of conjugation during drug absorption.
Owing to impact of ZGT on tolerance of a human body to glucose, change of need of the patient in insulin and/or in oral anti-diabetic means in certain cases can be observed.
Terms of sale
The remedy of Proginov is on sale only at presentation of the recipe.
The most admissible temperature indicator of storage of drug is temperature of 30 °C.
Period of validity
From the moment of production of tablets – 5 years.
In a case purpose of ZGT patients in whose anamnesis the expressed risk factor of developing of thrombosis or the sum of less powerful risk factors of a thrombogenesis is traced need to consider probability of mutual strengthening of effects of these factors and the carried-out treatment in relation to forming of thromboses. In such cases the general meaning of observed risk factors increases. In the presence at the patient of high risk of a possibility of development of thromboses Proginova's appointment is contraindicated.
Before ZGT and in the subsequent at all stage of carrying out treatment, through approximately equal periods (at least 1 time in half a year), the patient should appoint gynecologic survey and research of mammary glands, and also to measure the ABP and in case of need to carry out other tests.
The women suffering prolaktinomy and accepting Proginova at all stage ZGT have to pass periodic medical examination with determination of level of prolactin.
In need of carrying out ZGT in relation to patients with one or several painful states which are listed below continuous and attentive medical supervision can be required. In this regard in case of detection at herself, at least, one of these states, the woman is obliged to report about it to the doctor prior to Proginova's reception.
The painful states demanding extra care of carrying out ZGT:
- uterus fibromyoma;
- hysterical chorea;
- endometriosis (attendees or postponed in the past);
- system lupus erythematosus;
- pathologies of a gall bladder and/or liver (after the previous hepatitis Proginova's appointment is possible only after 6 months, at full normalization of all hepatic functions);
- the jaundice (observed at the past pregnancy or the previous therapy by sex hormones);
- diabetes mellitus;
- the increased level of serumal triglycerides;
- arterial hypertension;
- the hloazma (which is present or postponed in the past);
- bronchial asthma;
- high probability of a vein thrombosis.
The risk of possible forming of a vein thrombosis increases with age, and also at the excess weight, varicosity and instructions by it in the family anamnesis.
Temporary increase of risk of formation of a deep vein thrombosis is observed at the patients who had serious injuries, operative measures, or being in a condition of a long immovability. In case of planning of any operations against carrying out ZGT, the patient is obliged to report about it to the attending physician in advance (in 4-6 weeks).
The preventions below belong to all drugs used in ZGT, including also medicine of Proginov.
In case of monotherapy by estrogen, in particular at their long use, the probability of forming of cancer of uterine mucous membrane (endometria cancer) increases. At the uterus kept at the patient it is necessary to carry out ZGT in a complex with the drugs reducing such risk for what appoint Proginova with parallel reception of gestagenny drugs.
The woman observing at herself against Proginova's use, frequent breakthrough or irregular bleedings has to inform of it the attending physician.
By results of several conducted researches some increase of episodes of forming of a breast cancer at the women passing ZGT in comparison with their coevals who are not accepting hormonal drugs was proved. The relative risk of developing of this pathology increases with increase in time of carrying out monotherapy by estrogen, however can be reduced or be absent completely. The tendency to increase in risk of forming of tumors of mammary glands is almost identical concerning women with alcoholism, obesity or later development of a natural climax. The increased probability of developing of such cancer gradually decreases to an average indicator for the first years after refusal of ZGT.
Carrying out ZGT also promotes increase of mammography density of female mammary glands that can negatively be reflected in radiological definition of a cancer tumor of a mammary gland and sometimes demands use of alternative methods of detection of oncological diseases.
In the course of carrying out epidemiological research observed slight increase of risk of forming of cancer of ovaries at the patients who are on replacement oestrogenic therapy on quite long period (more than 10 years). At the same time the analysis of 15 other researches did not show increase of such risk. For this time these data are disputable.
In the isolated cases at administration of drugs including sex hormones noted emergence of high-quality new growths of a liver, malignant tumors of this body met even less often. Sometimes bleedings from such tumoral educations in an abdominal cavity bore in themselves threat for the patient's life. Communication of such negative phenomena with the carried-out ZGT was not proved. In spite of the fact that emergence of such episodes is improbable, in case of detection at itself the unusual negative feelings at the top of a stomach proceeding throughout quite long period, the patient has to report about them to the doctor.
Also the patient is obliged to inform the attending physician on any identification at herself the following painful states:
- sudden acoustical and visual disturbances;
- phlebitis (inflammation of veins);
- unusually heavy and/or frequent headaches;
- for the first time the developed migraine attack (with displays of nausea and a throbbing pain and with the previous sight dysfunction);
- deterioration in attacks of already available migraine.
In case of forming of thrombosis against Proginova's use or even suspicion on a possibility of its emergence it is necessary to interrupt immediately treatment and to pass medical examination.
The guarding manifestations of possible formation of thromboses are:
- unexpected shortage of air;
- the cough which is followed by blood;
- loss of consciousness;
- inexplicable extremity pains and/or their fast puffiness.
The immediate termination of reception of tablets of Proginov is demanded by development of jaundice and identification of pregnancy.
At therapy to use of sex hormones there can be mistakes in results of some conducted laboratory researches. In case of need carrying out any clinical trial it is necessary to inform the doctor on administration of drug of Proginov.
The remedy of Proginov cannot be considered as a contraceptive. In need of contraception use the woman needs to use non-hormonal ways or means (excepting a temperature and calendar method). At the first suspicion on possible pregnancy reception of a dragee of Proginova is stopped up to an exception or confirmation of pregnancy.
Data on need of correction of the dosing regime of Proginova at therapy of elderly patients (after 65 years) are absent. Women of 65 years have limited references to a possibility of increase in risk of display of dementia and are more senior, the beginning ZGT. In case of need Proginova's appointments to patients are more senior than 65 years to the doctor it is necessary to show care.
Use of medicine of Proginov for patients with pathologies of livers/kidneys was not studied. According to some information there is no need of correction of dosages of Proginova at these pathologies.
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