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One tablet includes 20 mkg of ethinylestradiol and 150 mkg of a dezogestrel.
In addition: colloid silicon dioxide, lactose, α-tocopherol, magnesium stearate, potato starch, stearic acid, povidone.
Mersilon is made in the form of tablets on 21 pieces in the blister. Secondary packaging may contain 1, 3 or 6 blisters.
Contraceptive (contraceptive), it is oestrogenic-progestogennoye.
Pharmacodynamics and pharmacokinetics
Mersilon is the combined contraceptive (contraceptive) drug including estrogen and gestagen. Contraceptive efficiency of Mersilon, as well as the other the combined oral contraceptives (COC), first of all, is based on his ability to oppression of an ovulation and increase in release of cervical slime.
Effects of a gestagen – a dezogestrel are directed to synthesis braking by a hypophysis of LG and FSG that leads to prevention of maturing of a follicle, thereby blocking an ovulation.
Except the specified peripheral and central mechanisms of effect of drug interfering maturing of an ovum ready to fertilization the contraceptive effect caused by increase in viscosity of the slime enveloping a neck of uterus thereby is noted creating conditions to relative impassability of spermatozoa through it.
In addition to contraceptive effects Mersilon shows a number of properties which can be considered at the choice of a contraceptive method. At administration of drug the menstrualnopodobny phenomena are characterized by the bigger regularity, smaller morbidity and weaker bleedings reducing the frequency of manifestations of an iron deficiency anemia. Also at reception the COOK noted decrease in risk of forming of cancer of an endometria and an ovary.
At oral administration there is a fast and full absorption of ethinylestradiol in a gastrointestinal tract. Achievement of peak of plasma concentration of drug, a component about 80 pkg/ml, happens in 60-120 minutes. Absolute bioavailability, thanks to presistemny conjugation of ethinylestradiol and the first stage of its metabolism, equals about 60%.
In a blood plasma ethinylestradiol not specifically, but rather strongly communicates albumine (on average for 98,5%) that leads to increase of the plasma SHBG level. The seeming Vd of drug is equal to about 5 l/kg.
Ethinylestradiol passes stages of presistemny conjugation in a human body, is initial in mucous a small intestine, and further in a liver. Primary metabolism of ethinylestradiol happens to the help of an aromatic hydroxylation at which a large number of the various metilirovanny and hydroxylated metabolites which are present at a form of free products of a metabolism and conjugates with sulfates and glucuronides is allocated. The metabolic clearance proceeds with a speed about 5 ml/min.
Decrease in plasma level of ethinylestradiol passes two phases. In a final phase distribution of drug is characterized by T1/2 lasting about 24 hours. Not changed ethinylestradiol is not excreted. Products of a metabolism of drug are removed with bile and urine in the ratio 6:4. T1/2 of metabolites is equal to about 24 hours.
Equilibrium concentration of ethinylestradiol are observed in plasma after 3-4 days when its plasma concentration for 30-40% exceeds the similar indicator noted at a single dose.
Orally accepted dezogestret quickly enough and is in full soaked up in a gastrointestinal tract then there is its transformation etonogestret. The plasma peak of concentration is equal to about 2 mg/ml and is observed approximately after 90 minutes after one-time administration of drug. Bioavailability is at the level of 62-81%.
Formed etonogestret connects to plasma proteins albumine and globulin (SHBG) which connects sex hormones. Thus, 40-70% of an etonogestrel are specific are connected with SHBG and only 2-4% of the general plasma fraction of drug are present at a form of a free steroid. The increase of the SHBG level provoked by ethinylestradiol influences distribution between plasma proteins, leading to reduction albumine - the connected part of drug and increase in its SHBG related fraction. Vd of a dezogestrel reaches about 1,5 l/kg.
Full metabolic transformations of an etonogestrel happen in the specific way of a steroid metabolism. Speed of metabolic plasma clearance is equal to about 2 ml/min. Interaction with the ethinylestradiol accepted in parallel is not revealed.
Decrease in plasma level of an etonogestrel happens in two phases. In a final phase distribution of drug is characterized by T1/2, components are about 30 hours old. Dezogestrel, as well as products of his metabolism, are excreted with bile and urine in an approximate ratio 4:6.
The pharmacokinetics of an etonogestrel directly depends on concentration of SHBG which is tripled under the influence of ethinylestradiol. At daily reception of Mersilon the plasma level of an etonogestrel increases approximately by 2-3 times and in the second half of course reception reaches an equilibrium state.
Preclinical information on safety
For the purpose of an assessment of possible risks for the person conducted researches of toxic influence of ethinylestradiol and a dezogestrel, and also their combination, on animals. During systematic testing of portability of these drugs at their repeated use the phenomena indicating unexpected toxic risk for a human body were not revealed. In the analysis of the remote toxicity of reception of repeated doses of drugs their oncogenous potential is noted. Nevertheless, it is necessary to take ability of sexual steroids to accelerate growth of tumors and some hormone - dependent internal body tissues into account.
Researches of possible teratogenecity and embriotoxity and the assessment of impact of both drugs on a lactation of animals, fertility, forming and fetation, ability of their descendants to a reproduction did not give a reason to suspicion of a possibility of such negative phenomena at the person at use of the recommended dosages of drugs. The carried-out in vitro and in vivo of research did not reveal their any mutagen potential.
Indications to use
Monthly course reception of tablets of Mersilon is shown for the purpose of contraception.
Mersilon is absolutely contraindicated at:
- heavy pathologies of a liver, including instructions on them in the anamnesis (up to absolute normalization of indicators of hepatic function);
- the venous thrombosis observed in the present or which is present at the past including a thromboembolism of a pulmonary artery (TELA) and the deep vein thrombosis (DVT);
- hepatic tumors of any etiology (high-quality or malignant), including instructions on their development in the past;
- the arterial thrombosis observed in the present or which is present at the past (including a stroke and a myocardial infarction) or the painful states which are risk factors of forming of thrombosis (I include stenocardia and a tranzitorny attack of an ischemic heart disease);
- pregnancies (including cases of expected pregnancy);
- vulval bleedings of not clear etiology;
- feeding by a breast;
- tendencies to arterial or venous thrombosis, inclusive with cases of insufficiency of a protein of C or S, resistance to the activated protein With, deficit of antithrombin III, a gipergomotsisteinemiya, presence of anti-phospholipidic antibodies (cardiolipin antibodies and lupoid anticoagulant);
- intolerance of sugars;
- the migraine in the anamnesis proceeding with neurologic focal symptomatology;
- personal hypersensitivity;
- the diabetes mellitus which is followed by vascular defeat;
- nicotine addiction aged after 35 years (when smoking a day more than 15 cigarettes);
- presence of multiple or heavy risk factors of forming of thrombosis (including an arterial hypertension with fixation of arterial pressure at the level of 160/100 mm hg and more);
- the malignant hormonedependent educations found in mammary glands or in generative organs (including suspicions on them);
- the pancreatitis observed in the present or which is present at the past proceeding with the expressed gipertriglitseridemiya.
In case of any of above-mentioned painful states at Mersilon's use, the woman it is necessary to interrupt immediately reception of tablets and to ask for medical care.
At identification now of risk, any of following factors / states, the doctor is obliged to weigh carefully expected advantage of reception of tablets Mersilon and potential risk of negative effects of their use for the woman and to appoint drug with extra care at:
- fibrillations of auricles;
- gemolitiko-uraemic syndrome;
- nicotine addiction;
- tracking in the family anamnesis of serious thromboembolic pathologies (a thromboembolism / venous or arterial thrombosis, observed at parents, brothers or sisters at rather young age);
- hereditary sickemia;
- obesity (at a weight more than 30 kg/sq.m index);
- gipertriglitseridemiya (including the instruction on it in the family anamnesis);
- chronic and acute hepatic diseases, inclusive with inborn hyperbilirubinemias (a syndrome the Cudgel Johnson, Gilbert, the Rotor);
- arterial hypertension;
- inflammatory chronic pathologies of intestines (including ulcer colitis and an illness Krone);
- displays of migraine;
- to system lupus erythematosus;
- valve cordial defects;
- diabetes mellitus;
- changes in the biochemical indicators able to represent markers of the acquired or inborn tendency to thrombosis (inclusive with cases of insufficiency of a protein of C or S, resistance to the activated protein With, deficit of antithrombin III, a gipergomotsisteinemiya, presence of anti-phospholipidic antibodies (cardiolipin antibodies and lupoid anticoagulant);
- superficial thrombophlebitis, varicosity (because of the obscure role of these painful states on forming of a venous thromboembolism);
- long forced immobilization, carrying out surgeries on the lower extremities or extensive body parts, severe injuries (in case of emergence at Mersilon's reception of the states demanding the above-stated surgeries or a long immobilization it is necessary to interrupt drug use, and when carrying out planned surgeries to suspend its reception in 4 weeks prior to intervention and for 2 weeks after a remobilization);
- in a puerperal period and aged after 35 years.
Contraceptive tablets Mersilon sometimes lead to the following by-effects:
- thrombembolia or thrombosis (inclusive with thromboembolisms of arteries of a retina, mesenteric, hepatic, renal veins and arteries, a myocardial infarction, TELA, a stroke, TGV);
- knotty erythema;
- increase of the ABP;
- allocations from chest glands / vaginas;
- liver tumors;
- abdominal pains;
- breast cancer;
- mnogoformny erythema;
- bloody acyclic vulval allocations (mostly in the first months of use);
- hloazma (in particular at its existence during the previous pregnancy);
- allergic reactions;
- decrease/increase of a libido;
- small tortoiseshell;
- increase/reduction of weight;
- skin rash;
- liquid delay;
- intolerance of contact lenses;
- change of mood;
- increase/morbidity of chest glands.
Contraceptive tablets Mersilon, application instruction
Tablets Mersilon are shown to oral everyday administration in the order specified on the blister. The application instruction of Mersilon orders to women daily reception of one tablet for 21 days, it is desirable in a certain time of day, washing down, at the existing need, with the small volume of water. The beginning of reception of tablets from the subsequent blister should be carried out after the 7 a day interval over which there has to be menstrualnopodobny bleeding. Developing of menstrualnopodobny bleeding is, as a rule, observed for 2-3 days of the termination of tablets in the used blister and can continue at reception of tablets from the subsequent blister.
Beginning of reception of Mersilon
If the woman did not accept hormonal contraceptives for the last 30 days, it is better to start Mersilon's reception in the first days of periods. Also allow a possibility of the beginning of reception of these contraceptive tablets for the 2-5th days of periods, but at the same time for 7 days of the first cycle recommend to use auxiliary barrier (caps, condoms) a contraception method.
Upon transition to Mersilon from the other hormonal combined contraceptive means (transdermalny plasters, vaginal rings, others the COOK) it is reasonable to start reception of tablets of Mersilon in the next days after the last use of the previous contraceptive method / means, but not later than the next day following the usual break which is followed by menstrualnopodobny bleeding.
In case of the correct and consecutive use by the woman of the previous contraceptive method / means and at reliable information about lack of pregnancy it is possible to pass to Mersilon in any convenient day of a cycle. It is necessary to consider that the obligatory interval when using the previous method / contraceptive should not be more recommended.
It is possible to pass to Mersilon with "mini-saw" in any convenient day; from Naval Forces or an implant – in day of their removal; from contraceptive injections – at the time of carrying out the following injection. In all above described cases for the first 7 days of use of Mersilon it is necessary to use barrier contraceptives.
After the abortion which is carried out in the I trimester it is possible to begin to accept Mersilon immediately, without additional use of any contraceptives.
After the abortion which is carried out in the II trimester or childbirth recommend to start Mersilon's reception after 21-28 days. In case of need later beginning of use of Mersilon, for the first 7 days it is necessary to use barrier contraceptives. At implementation by the woman of sexual contacts during non-use of contraceptives, before Mersilon's reception it is necessary to be convinced of lack at it of pregnancy or to wait for periods.
Algorithm of actions at the admission of the next reception of a tablet
At 12 to an hour delay of reception of the next tablet reliability of contraceptive effect of Mersilon does not decrease. The required pill needs to be taken during 12 hour period and further to follow the standard scheme of reception.
At a delay of reception of the next tablet more than for 12 hours lowering of contraceptive effect of Mersilon is possible. In this case the woman has to be guided by two rules below:
- never to interrupt reception of tablets it is more than for 7 days;
- to remember that adequate oppression gipotalamo - pituitary and ovarian system demands continuous tablets 7 day reception.
The cyclic scheme of use of Mersilon means use of tablets for 3 weeks in this connection, the recommendations below about resuming of reception of tablets after their admission will be reasonable.
The woman needs to take a required pill during the next time period, even in case of a concomitant use of 2 tablets then to follow the standard scheme of reception. In addition in the first 7 days it is necessary to use barrier contraceptives. At implementation by the woman of sexual contacts for the previous 7 days it is necessary to exclude probable pregnancy. The risk of pregnancy increases with number of the passed tablets and with approach of time of an interval in their reception.
The woman needs to take a required pill during the next time period, even in case of a concomitant use of 2 tablets then to follow the standard scheme of reception. At timely reception of all previous tablets for the previous 7 days to the passed dose, it is possible not to resort to additional use of other contraceptive means / methods. Otherwise, or in case of the admission more than one tablet, for the next 7 days it is necessary to use barrier contraceptives.
Decrease in reliability of contraceptive effect because of approach of an interval in reception of tablets is possible. This situation can be avoided by adaptation of the scheme of reception of contraceptive means. At use of any of two following schemes it is possible not to resort to additional use of other contraceptives, at timely reception of all previous tablets for the previous 7 days to the passed dose. In case of disturbance of the standard reception of tablets, recommend to use the first scheme below, at the same time for the next 7 days it is necessary to use barrier contraceptives.
The recommended schemes of correction of reception of tablets at their admission on the third week
- The woman needs to take a required pill during the next time period, even in case of a concomitant use of 2 tablets then to follow the standard scheme of reception. Tablets from the new blister need to begin to be drunk right after their termination in the previous blister, without 7 a day interval. In this case the possibility of development of menstrualnopodobny bleedings is extremely small, however at some women bloody allocations can be observed (plentiful or smearing).
- It is possible to recommend to the woman complete cessation of reception of tablets from the used blister for a span about 7 days (including interval time) then to start reception of tablets from the new blister.
In case of absence of menstrualnopodobny bleedings in the period of the next interval in reception of tablets at their previous admission, it is necessary to consider probability of pregnancy.
Precautionary measures at disorders of a gastrointestinal tract
In case of development in the woman of heavy disorders of a gastrointestinal tract, absorption of active ingredients of Mersilon can occur in incomplete volume that demands additional use of barrier contraceptives. At the vomiting which arose within 3-4 hours after reception of a tablet it is necessary to follow the algorithm of actions recommended at the admission of the next reception of a tablet or in addition to take the corresponding pill from other blister.
Change of time of the beginning of a menstrual cycle
Continuous reception of tablets from two blisters, without 7 a day interval is necessary for a delay of periods. It allows to delay periods for any necessary term up to full use of the second blister. During this period at some women can be observed bloody allocations (plentiful or smearing). Resuming of the normal standard administration of drug perhaps later obligatory the 7th day interval.
For periods shift on a desirable day of the week, it is necessary to reduce usual the 7th a daily interval by the required number of days (from the 1st to 6). The interval is less, the risk of absence in it is more than menstrualnopodobny bleedings and emergence of bloody allocations (plentiful or smearing) at reception of tablets from the subsequent blister.
At single-step reception of a large number of tablets of Mersilon developing of the nausea sometimes passing into vomiting and also bloody vulval allocations at young girls is possible. Any serious negative consequences of reception of excessive dosages of drug Mersilon were not noted. Treatment – symptomatic.
It is necessary to remember that against continuous reception of oral contraceptives, use of other medical drugs can lead to decrease in efficiency of contraceptives, and also to developing of acyclic bleedings.
During course reception the COOK, parallel use of inductors of microsomal liver enzymes (St. John's Wort drugs, Griseofulvin, Phenytoinum, felbamat, barbiturates, ritonavir, Primidonum, Topiramat, Carbamazepine, Rifabutin, Rifampicin, okskarbazepin and so forth) can increase clearance of sex hormones. On 2-3 week of reception of Mersilon the peak induction of liver enzymes can not be observed, and be shown only after an interval in reception of tablets of drug by the end of the 4th week.
Also there are messages on decrease in contraceptive efficiency of Mersilon at the combined reception of the antibiotics belonging to groups of Tetracyclines and Ampitsillinov with the obscure mechanism of interaction.
In case of use by the woman accepting the COOK, any of above-mentioned remedies recommend to use her in addition barrier contraceptives or to pass completely to other contraceptive method / means. At combined use of inductors of liver enzymes, barrier contraceptives need to be used throughout a therapeutic course, and also within the next 28 days. In need of long therapy by inductors of liver enzymes, it is better for woman to pass to other contraceptive means / method.
In case of use by the woman accepting the COOK, antibiotics (except for possessing properties of Griseofulvin and Rifampicin, similar to inductors of liver enzymes) it is necessary for her at all stage of therapy, and also for the next 7 days, to use barrier contraceptives. At continuation of a span of need of use of barrier contraceptives after reception of all tablets COOKS in the used blister, it is necessary to start reception of tablets from the subsequent blister without 7 a day interval.
Oral contraceptives are also capable to influence metabolic transformations of other medical drugs and to respectively change their plasma and fabric concentration, for example, to lower at Lamotridzhin and to raise at Cyclosporine.
In need of use by the woman accepting the COOK, other remedies it is necessary to be guided by the official instruction for their use.
Terms of sale
Mersilon is prescription medicine.
Tablets Mersilon should be stored in the factory blister, in the dark, dry room, with observance of temperature condition of 2-30 °C.
Period of validity
3 years from the moment of release.
In the presence at the woman of any of following risk factors or painful states it is necessary to weigh carefully advantages and probable risk of use of contraceptive tablets Mersilon. All possible negative effects of reception the COOK should be explained to the patient prior to drug use. At identification at herself exacerbations of the existing diseases or deterioration in risk factors or painful states, the woman is obliged to see immediately a doctor for the purpose of the solution of a question of the termination or further reception of Mersilon.
Women with any hereditary intolerance of sugars should consider 80 mg of lactose which are contained in one tablet of Mersilon.
Diseases of vascular system
When carrying out epidemiological researches there was a suspicion about possible existence of communication between Mersilon's reception and increase of risk of developing of trombotichesky and thromboembolic arterial and venous pathologies (including a myocardial infarction, TGV, a stroke, TELA).
Reception of any drug from COOK group increases risk of forming of a venous thromboembolism which can be shown both TELA, and TGV (sometimes with a lethal outcome). The increased risk of developing of these pathologies is observed in the first 12 months of use the COOK.
Some conducted epidemiological researches showed the increased risk of forming of a venous thromboembolism at the women accepting low-dosed the COOK, including the III generation of progestogens which treats and dezogestret, in comparison with the women accepting low-dosed the COOK, including progestogen levonorgestrel.
Occasionally thrombosis can arise in other blood vessels (including arteries and veins of a liver, a retina, a mesentery, a brain or kidneys). The consensus about use communication the COOK with developing of thrombosis does not exist.
Increase in intensity and frequency of attacks of migraine against Mersilon's reception which can be a symptom of cerebrovascular disturbances gives a reason for the immediate termination of reception of this contraceptive.
Carry a persistention of a human papillomavirus to the most essential risk factor of forming of cancer of neck of uterus (VPCh-infection). Separate epidemiological researches fixed increase of probability of forming of cancer of neck of uterus at long reception by women the COOK. Till today's time there is no consensus about extent of influence on these indicators of mixing of different minor factors, including increase of number of screening testings of a neck of uterus and specificity of sexual behavior, including use of barrier contraceptives, or their interrelations.
There are data on small increase of relative risk (approximately by 1,24 times) formations at women of a breast cancer at reception by them the COOK. This increased risk systematically decreases for 10 years after completion of use the COOK. In a type of the fact that at women till 40 flyings of a tumor of mammary glands are noted rather seldom increase in probability of forming of this pathology at the women who are accepting the COOK at the moment, or recently stopped their use it is small, in comparison with initial probability of developing of such cancer. Increase of risk of forming of cancer of chest glands at the women using the COOK can be explained with earlier diagnosing of similar cancer, biological influence the COOK, and also a combination of these factors.
The tendency according to which, at women ever using the COOK, cancer of chest glands to be in clinically less started state, than at the women using other contraceptive methods / means is observed.
At Mersilon's use extremely seldom noted cases of emergence of high-quality, is even more rare than malignant, hepatic new growths. In some cases these tumors were the reason of the intra belly bleedings posing threat for life. The doctor needs to take into account probability of existence of a hepatic tumor at differential diagnosis of pathologies at the woman accepting Mersilon in case of identification of the symptomatology including: increase in a liver, an acute pain at the top of a stomach, symptoms of intra belly bleeding.
In case of diagnosing at the woman, or even members of her next family, gipertriglitseridemiya against Mersilon's reception, increase of risk of developing of pancreatitis can be observed.
When developing a persistent arterial hypertension at the woman accepting Mersilon it is necessary to suspend administration of drug and to begin therapy of an arterial hypertension. In case of full stabilization of the ABP owing to the carried-out anti-hypertensive therapy it is possible to consider a question of resuming of use of Mersilon.
There is an opinion that the itch and/or jaundice provoked by a cholestasia; forming of concrements in a gall bladder; system lupus erythematosus; herpes of pregnant women; porphyria; Sidengam's chorea; gemolitiko-uraemic syndrome; Quincke's disease (hereditary); the hearing loss caused by an otosclerosis form or aggravated both at pregnant women, and at the women accepting Mersilon. In the latter case the evidence of communication of the above described painful states using drug Mersilon is produced by unconvincing.
Emergence of any disturbances of hepatic function, observed during Mersilon's reception, can be considered as the basis for drug withdrawal, up to normalization of indicators of hepatic function. Developing of the cholestatic jaundice which was earlier observed at reception of sex hormones or pregnancy demands phase-out of Mersilon.
In spite of the fact that Mersilon's effects can break tolerance to insulin and glucose, there are no actual proofs of need of change for patients with a diabetes mellitus of the therapeutic scheme of use low-dosed the COOK (including up to 50 mkg of ethinylestradiol). However, the women with a diabetes mellitus accepting Mersilon demand careful medical supervision.
There are data connecting forming of ulcer colitis and diseases Krone with system use the COOK including Mersilon.
In certain cases against Mersilon's use observed emergence of a hloazma (pigmentation on face skin), in particular at its development during the previous pregnancy. In case of Mersilon's reception by the women predisposed to a hloazma they need to avoid any (natural or artificial) influence of an ultraviolet.
Medical consultations / surveys
Before Mersilon's appointment, or resuming of its use, the doctor needs to conduct full examination, the woman, to collect her exact medical anamnesis, and also the family anamnesis assuming to accept drug. The list of necessary inspections and frequency of their carrying out have to be selected individually both correspond to the standard practice and be carried out at least 1 time to half a year.
The woman is obliged to study attentively the official application instruction of Mersilon and to strictly implement the recommendations registered in it.
Decrease in efficiency
The woman should remember that efficiency of contraceptive action of Mersilon can decrease at the admission of the next tablet, emergence of disorders of a gastrointestinal tract and parallel reception of some remedies.
At Mersilon's use, in particular in the first months, emergence of irregular bloody allocations is possible (plentiful or smearing). In this regard, the assessment of irregular bleedings needs to be carried out after the adaptation period, as a rule, occupying 3 months.
In case of preservation of irregular bleedings or their emergence after former regular cycles, it is necessary to consider possible non-hormonal factors of disturbance of a usual cycle and to appoint the corresponding tests for the purpose of a pregnancy exception (perhaps diagnostic scraping) and malignant new growths.
At some women absence of menstrualnopodobny bleeding is noted during an obligatory interval between reception of tablets from different blisters. In case of conscientious execution by the woman of all recommendations about Mersilon's use, the probability of pregnancy at it is extremely small. Otherwise, and in the absence of bleedings throughout 2 consecutive cycles, it is necessary to exclude probable pregnancy.
Use of oral contraceptives can negatively influence indicators of separate laboratory tests, including biochemical indicators of functionality of kidneys/liver, adrenal glands, a thyroid gland; serumal level of transport proteins (in particular, a corticosteroid - the connecting globulin and fractions of lipids/lipoproteins); parameters of coagulation, carbohydrate metabolism and fibrinolysis. As a rule, such changes are not beyond standard deviations in results of laboratory indicators.
Coincidence on the ATH code of the 4th level:
- Egestrenol, etc.
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