Mercilon
Mercilon: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in the elderly
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Mercilon
ATX code: G03AA09
Active ingredient: desogestrel + ethinylestradiol (desogestrel + ethinylestradiol)
Manufacturer: Organon (Netherlands)
Description and photo update: 2019-16-08
Prices in pharmacies: from 1200 rubles.
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Mercilon is a monophasic PDA (combined oral contraceptive) that suppresses ovulation and increases the secretion of cervical mucus.
Release form and composition
Dosage form Mersilon - tablets: biconvex, round, white, on one side there is an engraving "TR" above the number "4", on the other side there is an image of a five-pointed star and the inscription "ORGANON" (21 pcs. In a PVC / aluminum blister, each blister is hermetically sealed in a sachet made of aluminum laminated foil; 1, 3 or 6 sachets (respectively 21, 63 or 126 tablets) in a cardboard box).
1 tablet contains:
- Active ingredients: desogestrel - 0.15 mg, ethinylestradiol - 0.02 mg;
- Auxiliary components: povidone, potato starch, stearic acid, α-tocopherol, colloidal silicon dioxide, lactose monohydrate.
Pharmacological properties
Pharmacodynamics
Mercilon is a combined contraceptive drug that contains progestogen and estrogen. The contraceptive effect of the drug is based on its ability to suppress ovulation and increase the secretion of cervical mucus.
Ethinyl estradiol is a synthetic analogue of estradiol, the action of which is expressed in the regulation of the menstrual cycle simultaneously with the level of the corpus luteum hormone.
Desogestrel belongs to gestagens and is an inhibitor of the synthesis of FSH (follicle-stimulating hormone) and LH (luteinizing hormone), which are produced in the pituitary gland. This interferes with the maturation of the follicle and prevents ovulation.
Mercilon not only avoids the maturation of an egg ready for fertilization, but also has a contraceptive effect associated with an increase in the viscosity of mucus that envelops the cervix, which leads to difficulties in the movement of sperm in it. Also, taking the drug helps to regulate the menstrual cycle, provides less bleeding and minimizes pain during menstruation, reducing the risk of developing iron deficiency anemia. The incidence of endometrial and ovarian cancer in women taking Mercilon is also low.
Pharmacokinetics
Desogestrel
When taken orally, desogestrel is rapidly and almost 100% absorbed, turning into etonogestrel. The maximum concentration of the substance in the blood plasma is recorded after 1.5 hours. Bioavailability ranges from 62 to 81%.
Etonogestrel binds to sex hormone binding globulin (SHBG) and to albumin in blood plasma. Only 2–4% of the total content of etonogestrel in the body is present in free form in blood plasma, while 40–70% of the substance is characterized by specific binding to SHBG. An increase in the concentration of SHBG caused by ethinyl estradiol changes the distribution between blood proteins and leads to a decrease in the albumin-bound fraction and an increase in the SHBG-bound fraction. For desogestrel, the apparent volume of distribution is 1.5 l / kg.
Etonogestrel is completely metabolized by known methods of sex hormone metabolism. The rate of metabolic clearance of the compound from blood plasma is 2 ml / min / kg. There is no evidence of an interaction of etonogestrel with ethinyl estradiol, which is taken concomitantly with it.
The plasma level of etonogestrel decreases in 2 stages. At the final stage, the half-life is approximately 30 hours. Desogestrel and its metabolites are excreted through the kidneys and intestines in approximately a 6: 4 ratio.
The pharmacokinetic characteristics of etonogestrel are influenced by SHBG, the content of which increases by 3 times under the action of ethinyl estradiol. With daily intake, the level of etonogestrel in the blood plasma increases by 2–3 times, reaching a stable value in the second half of the cycle.
Ethinylestradiol
When taken orally, ethinyl estradiol is absorbed almost completely and at a high rate. Its maximum concentration in blood plasma is observed for 1-2 hours after administration. The absolute bioavailability, which is the result of presystemic metabolism, reaches 60%.
Ethinyl estradiol is characterized by nonspecific binding to blood plasma albumin, and it is quite complete (98.5%). This active component of Mersilon helps to increase the concentration of SHBG. The apparent volume of distribution is 5 l / kg.
Ethinylestradiol is involved in the processes of presystemic metabolism both in the liver and in the mucous membrane of the small intestine. At the initial stage, it is metabolized through aromatic hydroxylation, during which various methylated and hydroxylated metabolites are formed, which are determined both in the free state and in the form of conjugates with sulfates and glucuronides. The rate of metabolic elimination of ethinyl estradiol from blood plasma averages 5 ml / min / kg.
The content of ethinyl estradiol in blood plasma decreases in 2 stages. At the final stage, the half-life is approximately 24 hours. There is no excretion of the substance in unchanged form, and its metabolites are excreted in the urine and feces in a ratio of approximately 4: 6. The half-life of metabolites is about 1 day.
The equilibrium concentration of ethinyl estradiol is reached 3-4 days after the start of administration, when its content in the blood plasma is 30–40% higher than that after taking 1 dose.
Indications for use
According to the instructions, Mercilon is taken for contraception (in order to protect against unwanted pregnancy).
Contraindications
Absolute:
- Venous thrombosis, including pulmonary embolism and deep vein thrombosis of the leg (currently diagnosed or with a history);
- Arterial thrombosis (including stroke, myocardial infarction) or precursors of thrombosis (angina pectoris, transient ischemic attack) (currently diagnosed or a history of data);
- Predisposition to arterial or venous thrombosis: hyperhomocysteinemia, resistance to activated protein C, protein C deficiency, antithrombin III deficiency, protein S deficiency, antiphospholipid antibodies (lupus anticoagulant, antibodies to cardiolipin);
- Migraine (in the presence of data on focal neurological symptoms in the anamnesis);
- Diabetes mellitus with microangiopathy (vascular lesions);
- Multiple or severe risk factors for arterial or venous thrombosis, including hypertension with arterial pressure (BP) 160/100 mm Hg. Art. and more;
- Pancreatitis, accompanied by severe hypertriglyceridemia (hypertriglyceridemia), including data in the anamnesis;
- Severe liver damage, including a history of data (before normalization and restoration of liver function);
- Liver tumors (malignant and benign), including history;
- Malignant hormone-dependent tumors of the mammary glands or genitals (including suspected ones);
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- Vaginal bleeding of unexplained etiology;
- Smoking after 35 years in the amount of 15 cigarettes per day or more;
- Pregnancy period (including anticipated);
- Lactation (breastfeeding period);
- Hypersensitivity to active substances or to any auxiliary component of the PDA.
In the event of any of the diseases / conditions occurring during therapy with Mercilon, it is required to stop using it immediately.
Relative (for any of the following conditions / diseases, the use of Mersilon is allowed with caution, after a careful assessment of the ratio of potential risk and expected benefit):
- Hypertension;
- Hyperlipidemia;
- Sickle cell anemia;
- Migraine;
- Valvular (acquired) heart defects;
- Atrial fibrillation;
- Diabetes;
- SLE (systemic lupus erythematosus);
- Gasser's disease (hemolytic uremic syndrome);
- Superficial thrombophlebitis, varicose veins;
- Family history of thromboembolic diseases (arterial or venous thrombosis / thromboembolism in parents, sisters, brothers at a relatively early age);
- Changes in biochemical parameters, such as resistance to activated protein C, antithrombin III deficiency, hyperhomocysteinemia, protein C and S deficiency, antiphospholipid antibodies (lupus anticoagulant, antibodies to cardiolipin), indicating a congenital or acquired predisposition to arterial or venous thrombosis;
- Chronic inflammatory bowel disease (Crohn's disease and ulcerative colitis);
- Hypertriglyceridemia (including family history);
- Chronic liver diseases, including congenital hyperbilirubinemia - Dubin-Johnson, Gilbert, Rotor syndromes;
- Obesity (body mass index over 30 kg / m 2);
- Smoking;
- Postpartum period;
- Age over 35.
With prolonged immobilization, extensive surgical interventions (especially on the lower extremities), severe injuries, it is recommended to stop using Mercilon, in case of planned operations no later than 4 weeks, and not resume taking it for 2 weeks after remobilization.
Instructions for the use of Mersilon: method and dosage
Mersilon tablets are taken orally, following the order indicated on the package, every day at about the same time, if necessary with a small amount of water.
Dosage regimen: 1 tablet per day for 3 weeks.
The tablets from the next package begin to be taken after 1 week of a break, during which menstrual bleeding passes, usually starting 1-2 days after taking the last tablet; bleeding may continue until the next pack is taken.
Start taking Mercilon tablets, depending on the previous methods of contraception or the woman's condition:
- Hormonal contraceptives have not been used for the last month or more: tablets are taken on the 1st day of the menstrual cycle; it is allowed to take the first pill 2-5 days from the beginning of the menstrual cycle, but during the first week of taking pills in the first cycle, you should additionally use a non-hormonal method of protection;
- CHC (combined hormonal contraceptives): oral dosage forms - it is advisable to start using Mersilon the next day after taking the last active tablet of the previous drug, but no later than the next day after the end of the usual break in taking pills (the day after taking the last tablet, not containing hormones); transdermal patch or vaginal ring - it is advisable to start taking pills on the day the patch or ring is removed, but no later than the day when the next application of the patch should be made or a new ring inserted;
- Monopreparations containing only a gestagenic component - "mini-pills", injections, an implant, a progestogen-releasing intrauterine system (IUD): you can switch from a "mini-pill" to Mersilon any day; from an implant or IUD - on the day of their removal; from injections - on the day of the next injection. In all cases, during the first week of admission, additional methods of protection must be used;
- Abortion performed in the first trimester: it is recommended to start taking the PDA immediately, you do not need to use additional methods of contraception;
- Abortion made in the II trimester or childbirth: start taking the drug 3-4 weeks after the abortion or childbirth; if you start taking it at a later date, during the first week it is necessary to use additional barrier methods of contraception; if, before using Mercilon, a woman has already had sexual intercourse after an abortion or childbirth, it is required to exclude the presence of pregnancy before the start of admission, or wait for the first menstrual bleeding.
The reliability of contraception does not decrease if the next pill is delayed by less than 12 hours. In such a situation, a woman needs to take Mercilon as soon as the opportunity arises, and take subsequent pills at the usual time. If reception is delayed for more than 12 hours, contraception reliability may decrease.
You can not interrupt taking the pills for more than 1 week. Adequate suppression of the hypothalamic-pituitary-ovarian system occurs after taking the tablets for 1 week without interruption.
The cycle includes 3 weeks of use, for each week there are special recommendations in case of missing the next Mercilon tablet.
1st week. The missed pill must be taken as soon as the woman remembered about the pass, even if she needs to drink 2 pills at the same time. Then the reception continues according to the standard scheme. During the next week, it is additionally required to use the method of barrier contraception, and in the presence of sexual contacts in the previous week, the possibility of pregnancy must be taken into account. The risk of pregnancy is higher, the closer the interruption in taking Mercilon to the time of sexual intercourse and the more tablets are missed.
II week. The missed pill must be taken as soon as the woman remembered about the pass, even if she needs to drink 2 pills at the same time. Then the reception continues according to the standard scheme. If during the week preceding the first missed dose, the pills were taken on time, there is no need to use additional non-hormonal methods of contraception. With the previous irregular intake or missing more than 1 tablet during the next week, additional measures of protection against pregnancy are used.
III week. Due to the subsequent interruption in the use of Mercilon, the reliability of contraception may be reduced. If the pills were taken on time during the week preceding the first missed dose, there is no need to use additional non-hormonal methods of contraception. Otherwise, one of the following two schemes should be applied, and additional contraceptive measures should be used for a week:
- The missed pill must be taken as soon as the woman remembered about the pass, even if she needs to drink 2 pills at the same time. Then the reception continues according to the standard scheme. It is necessary to start a new package immediately after the end of the current one, without taking a break between them. The chance of withdrawal bleeding before the end of the second pack is small, but some women may have spotting or profuse bleeding while taking the pills;
- You should stop taking the drug from the current package and take a break for no more than 1 week, including days when the woman forgot to take the pills, and then start a new package.
If there was a pass when taking Mercilon, and there was no withdrawal bleeding in the next break in taking the pills, the likelihood of pregnancy must be taken into account.
In the case of severe gastrointestinal disorders, the absorption of Mercilon may be incomplete, therefore additional contraceptive measures must be taken. If vomiting occurs within 3-4 hours after taking the drug, you need to use the recommendations for skipping the next pill intake. If the woman does not want to change the usual dosage regimen, then the additional pill (s) should be taken from the other package in the amount determined by the obstetrician-gynecologist.
To delay the onset of menstruation, you must continue taking pills from a different package without a standard break. The duration of the delay can be any, up to the end of the tablets from the second package, at this time spotting spotting or heavy bleeding may occur. After a week's break, Mercilon should be resumed as usual.
To shift your period to a different day of the week than expected while following the standard dosing regimen, it is recommended to shorten the interval in admission to the number of days required for the shift. It should be borne in mind that the shorter the break, the greater the likelihood of the absence during this period of menstruation and the occurrence of smearing or profuse bleeding when taking pills from the second package.
Side effects
- Cardiovascular system: thrombosis or thromboembolism (including stroke, myocardial infarction, pulmonary embolism, deep vein thrombosis) thromboembolism of retinal arteries, mesenteric, hepatic, renal veins and arteries, increased blood pressure;
- Hormone-dependent tumors: breast cancer, liver tumors;
- Skin: chloasma (especially if there is a history of chloasma during pregnancy);
- Reproductive system: acyclic spotting mainly in the initial months of admission;
- Other: allergic reactions.
Side effects observed when taking Mercilon, the connection of which with taking the drug has not been proven:
- Immune system: rarely - hypersensitivity;
- Metabolism and nutrition: often - weight gain; infrequently - fluid retention; rarely - weight loss;
- Nervous system: often - mood swings, depression, headache; infrequently - decreased libido, migraine; rarely - increased libido;
- Organ of vision: rarely - intolerance to contact lenses;
- Digestive system: often - abdominal pain, nausea; infrequently - vomiting;
- Skin and subcutaneous tissues: infrequently - urticaria, skin rash; rarely - erythema multiforme, erythema nodosum;
- Reproductive system: often - breast tenderness; infrequently - breast augmentation; rarely - discharge from the breast and from the vagina.
Overdose
An overdose of Mercilon usually does not lead to the development of any serious complications. Nausea and vomiting are considered probable signs of this condition; in young girls, bleeding from the vagina may appear. Antidotes to desogestrel and ethinyl estradiol are unknown, therefore symptomatic therapy is prescribed.
special instructions
The presence of any of the following conditions / factors requires a careful assessment of the benefits and possible risks of taking Mercilon. This should be discussed with your doctor before starting a contraceptive course. In case of exacerbation of diseases, worsening of the condition, or in the event of the appearance of their first symptoms, it is necessary to immediately consult a doctor who will decide whether to continue using the drug.
Vascular diseases
In epidemiological studies, the possibility of a link between the use of Mersilon and an increased risk of thrombotic, thromboembolic arterial and venous diseases such as stroke, myocardial infarction, pulmonary embolism and deep vein thrombosis has been established; these diseases are observed extremely rarely.
The use of any PDA increases the risk of venous thromboembolism (VTE), which manifests itself as pulmonary embolism and / or deep vein thrombosis (in some cases with fatal consequences). The likelihood of illness is higher in the first year of admission than in the case when Mercilon has been used for more than 1 year.
As a result of some epidemiological studies, it was found that when taking low-dose PDAs containing third-generation progestogens, including desogestrel, the risk of VTE is increased compared to taking low-dose PDAs containing the progestogen levonorgestrel.
In other blood vessels (arteries and veins of the mesentery, liver, kidneys, retina or brain), thrombosis occurs extremely rarely, and there is no consensus on whether the use of COCs is the cause of its formation.
In case of an increase in the intensity and frequency of migraines while taking the drug, it is recommended to immediately cancel Mersilon, since this condition may be a sign of cerebrovascular disorders.
Neoplasms (tumors)
The most significant risk factor for cervical cancer is persistent human papillomavirus infection. In the results of some epidemiological studies, it was noted that women who receive COC for a long time increase the risk of cervical cancer. However, there is no reliable data on the extent to which these indicators were influenced by the confusion of various factors (such as a woman's sexual behavior (including the use of barrier methods of contraception) and cervical screening examinations) or their relationship.
With the use of COCs, the RR increases slightly (up to 1.24) - the relative risk of developing breast cancer, and after the abolition of COCs, it gradually decreases over 10 years. Since breast cancer is quite rare in women under 40, the increase in the likelihood of its development against the background of taking COCs, current or recently stopped, is insignificant relative to the baseline probability of developing cancer. Data on the etiology of cancer in the materials of these studies are not provided. The increased risk of breast cancer due to the use of COCs can be explained both by the fact that breast cancer is diagnosed at an earlier stage, and by the biological influence of COCs, or a combination of these factors.
Breast cancer in women who have ever used COCs is clinically less advanced than in women who have never used them.
The development of benign liver neoplasms with the use of the drug Mercilon was observed extremely rarely, malignant tumors were diagnosed even less often, but as a result of this, in some cases, life-threatening intra-abdominal bleeding was noted. When carrying out the differential diagnosis of diseases in women receiving COCs, it is necessary to take into account the possibility of liver neoplasms, the symptoms of which may be its enlargement, acute pain in the upper abdomen or signs of intra-abdominal bleeding.
Other diseases
With the development of persistent, clinically significant arterial hypertension (AH) while taking Mercilon, it should be canceled and therapy for AH should be started. After using antihypertensive drugs it is possible to reduce the pressure to normal, it is possible to resume taking Mercilon.
There is a possibility of an increased risk of pancreatitis due to the use of Mercilon if the woman or her family members are diagnosed with hypertriglyceridemia.
There are reports that cholelithiasis, porphyria, Gasser's disease, systemic lupus erythematosus, Sydenham's chorea, herpes during pregnancy, hearing loss due to otosclerosis, hereditary angioedema (HAE), pruritus and / or jaundice caused by cholestasis may develop or worsen as in pregnancy, and when taking Mercilon, but the evidence for the connection of these effects with the use of the drug is inconclusive.
In case of acute or chronic violations of liver function, the drug must be discontinued until the liver function indicators normalize. The previously observed (with the use of sex steroids or pregnancy) recurrence of cholestatic jaundice is the basis for discontinuing the use of Mercilon.
Despite the fact that Mersilon is capable of affecting peripheral glucose and insulin tolerance, it has not been proven that in diabetes mellitus, a change in the therapeutic regimen of low-dose (containing less than 50 μg ethinyl estradiol) PDAs is required, but such patients should be under close medical supervision.
There is evidence of a connection between the use of PDAs with ulcerative colitis and Crohn's disease.
Sometimes, due to the use of Mercilon, chloasma can be observed, especially if there is pigmentation of the facial skin earlier during pregnancy. If you are prone to chloasma, it is recommended to avoid UV radiation and direct sunlight.
Before starting or resuming the use of Mercilon, the doctor should take a complete medical history, including family history, and conduct a thorough medical examination of the patient. It is required to measure blood pressure and, if clinically significant signs of hypertension are detected, conduct a physical examination taking into account contraindications and warnings. A woman should carefully read the instructions for use of Mercilon and follow all recommendations. The list of necessary examinations and the frequency of their conduct should be based on generally accepted practice, selected individually and carried out at least once every six months.
Oral contraceptives do not protect against the human immunodeficiency virus (HIV-AIDS) and other sexually transmitted infections.
The effectiveness of contraception may decrease if you skip taking Mercilon, in case of gastrointestinal disorders, or while taking a PDA with some drugs.
Evaluation of irregular bleeding should be carried out at the end of the adaptation period, which lasts 3 months, since in the first months of using Mercilon there is a high probability of profuse bloody or irregular spotting.
When irregular bleeding continues or appears after previous established cycles, it is necessary to take into account the possibility of non-hormonal causes of cycle disturbances and, in order to exclude pregnancy or malignant neoplasms, conduct adequate studies (including diagnostic curettage).
In the absence of menstrual bleeding in the interval between taking the pills, if all the recommendations given are followed, the likelihood of pregnancy is negligible. If there is no bleeding for the second time in a row, or the recommendations for taking the drug have been violated, it is required to exclude the possibility of pregnancy.
CPC affect the results of the following laboratory studies: the content of transport proteins in the plasma (for example, lipid / lipoprotein fractions and corticosteroid-binding globulin), parameters of coagulation, fibrinolysis and carbohydrate metabolism, biochemical parameters of the function of the thyroid gland, kidneys, adrenal glands and liver. Typically, the magnitude of the change is within the normal laboratory range.
One tablet of Mersilon contains less than 80 mg of lactose, but in the case of rare hereditary disorders, such as lactase deficiency, lactose intolerance, glucose-galactose malabsorption, the presence of lactose in the preparation should be taken into account.
Influence on the ability to drive vehicles and complex mechanisms
At the moment, the effect of Mersilon on the ability to drive vehicles and perform complex types of work that require increased concentration of attention and quick reactions has not been studied.
Application during pregnancy and lactation
Reception of Mercilon during pregnancy is contraindicated. If pregnancy is diagnosed while taking the drug, it should be canceled immediately. The results of most epidemiological studies have not confirmed an increased risk of congenital malformations in children whose mothers took Mercilon before pregnancy. Also, with the accidental use of such combined oral contraceptives (CPC) in early pregnancy, teratogenic effects were not observed.
Mercilon can affect lactation as it changes the composition and decreases the amount of breast milk. Therefore, the use of the drug is not recommended until breastfeeding is complete. Desogestrel, ethinyl estradiol and / or their metabolites in small amounts can be excreted in breast milk, but there is no information about their negative impact on the health of the newborn.
Use in the elderly
Mersilon is not used in elderly patients.
Drug interactions
To take into account the possible interaction of Mersilon with other medicinal substances / agents, if necessary, their joint use, you should seek the advice of your doctor.
Analogs
Mercilon's analogues are: Belara, Logest, Dailla, Bonade, Jess, Artisia, Janine, Yarina, Lindinet, Rigevidon, Logest, Zoely, Midiana, Egestrenol, Marvelon, Regulon, Munali, Novinet, Tri-Mercy.
Terms and conditions of storage
Store in a dry, dark place at a temperature not exceeding 2-30 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Mercilon
Basically, doctors leave positive reviews about Mersilon, since they consider it a very effective drug, subject to regular admission and compliance with all the recommendations of a specialist. The patients also confirm the good contraceptive properties of this PDA. However, a contraceptive is not suitable for every woman due to the individual characteristics of the body and the presence of possible concomitant diseases. There are also frequent reports of adverse reactions while taking Mercilon (chloasma, decreased libido, skin rashes, headaches, depression) or increased symptoms of pre-existing pathological conditions (migraine, thrombosis, pancreatitis), which prompts some women to stop taking the drug.
The price of Mercilon in pharmacies
The approximate price for Mersilon is about 1,360-1870 rubles (the package contains 21 tablets).
Mercilon: prices in online pharmacies
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Drug name Price Pharmacy |
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Mersilon 150 mcg + 20 mcg tablets 21 pcs. 1200 RUB Buy |
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Mersilon tablets 21 pcs. 1569 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
