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Active ingredients
Desogestrel + Ethinyl Estradiol
Release form
Pills
Composition
In 1 tablet: ethinylestradiol 20 mcg, desogestrel 150 mcg. Adjuvants: potato starch - 8 mg, povidone - 2.4 mg, stearic acid - 800 mcg, silicon colloid oxide - 800 mcg, α-tocopherol - 80 mcg, lactose monohydrate - to 80 mg.
Pharmacological effect
Combined contraceptive drug containing estrogen and gestagen. The contraceptive effect of Marvelon, as well as other combined oral contraceptives (CCP), is based primarily on the ability to suppress ovulation and increase the secretion of cervical mucus. The progestogen (desogestrel) inhibits the synthesis of LH and FSH by the pituitary gland and thus prevents follicle maturation (blocks ovulation). Ethinyl estradiol is a synthetic analogue of the follicular hormone estradiol, together with the hormone of the corpus luteum regulates the menstrual cycle. Along with these central and peripheral mechanisms, in case of the maturation of an oocyte capable of fertilization, the contraceptive effect is due to an increase in the viscosity of the mucus in the cervix, which makes it relatively impassable for spermatozoa. In addition to the contraceptive properties of Mercilon; has a number of effects that can be considered when choosing a method of contraception. Menstrual-like reactions become more regular, less painful, and less bleeding. The latter circumstance leads to a decrease in the frequency of concomitant iron deficiency anemia. When using PDA, a reduction in the risk of developing ovarian and endometrial cancer
Pharmacokinetics
Desogestrel. Absorption. Orally administered desogestrel is rapidly and completely absorbed and becomes etonogestrel. The peak serum concentration is about 2 mg / ml and is reached in about 1.5 hours after a single dose. Bioavailability is 62-81%. Distribution. Etonogestrel is associated with serum albumin and sex hormone-binding globulin (SHBG). Only 2-4% of the total concentration of the drug in the serum is present in the form of a free steroid, and 40-70% is specifically associated with SHBG. The increase in SHBG induced by these nilestradiol affects the distribution between serum proteins, causing an increase in the SHBG-bound fraction and a decrease in the albumin-bound fraction.The estimated amount of distribution of desogestrel is 1.5 l / kg. Metabolism. Etonogestrel is completely metabolized by known pathways of steroid metabolism. The rate of metabolic clearance of serum is about 2 ml / min / kg. No interaction was detected with ethinyl estradiol administered simultaneously. Withdrawal The level of serogestrel in serum is reduced in two phases. The distribution in the final phase is characterized by a half-life of about 30 hours. Desogestrel and its metabolites are excreted in the urine and bile in a ratio of about 6: 4. Equilibrium. Etonogestrel pharmacokinetics are affected by SHBG levels, which increase threefold under the action of ethinyl estradiol. After daily intake, the level of medication in serum increases by about 2-3 times, reaching a state of equilibrium in the second half of the course of treatment. Ethynyl estradiol. Absorption. When orally administered, ethinyl estradiol is rapidly and completely absorbed. The peak of the serum concentration of about 80 pg / ml is reached within 1 to 2 hours. Absolute bioavailability as a result of presystemic conjugation and the first stage of metabolism is approximately 60%. Distribution. Ethinyl estradiol is strongly but not specifically associated with serum albumin (approximately 98.5%) and causes an increase in the serum concentration of SHBG. It is determined that the apparent volume of distribution is about 5 l / kg. Metabolism. This is estiyl estradiol is an object of presystemic conjugation in the mucosa of the small intestine and in the liver. Ethinyl estradiol is first metabolized by aromatic hydroxylation, but it produces a wide variety of hydroxylated and methylated metabolites, and they are present as free metabolites and as conjugates with glucuronides and sulfates. The metabolic clearance rate is about 5 ml / min / kg. Excretion. The level of ethinyl estradiol in serum decreases in two phases, the distribution in the final phase is characterized by a half-life of about 24 hours. Unchanged drug is not excreted, ethinyl estradiol metabolites are excreted in urine and bile in the ratio 4: 6. The half-life of the metabolite is about 1 day. The equilibrium state. Equilibrium concentrations are reached in 3-4 days,when the level of the drug in serum is 30-40% higher compared to a single dose. Preclinical safety data. To assess the risk to humans, animal toxicity studies were conducted for both components of the drug, ethinyl estradiol and desogestrel, and for their combination. A systematic study of tolerability with repeated administration of drugs revealed no effects that could indicate an unexpected risk to humans. In long-term toxicity studies with repeated doses, no oncogenic potential was detected. However, it should be borne in mind that sex steroids can accelerate the growth of certain hormone-dependent tissues and tumors. Studies of embryotoxicity and teratogenicity and assessment of the effect of both components on fertility of producing animals, fetal development, lactation and the ability to reproduce in their descendants did not give indications of the possibility the risk of undesirable effects in humans after using the recommended doses of drugs.
Indications
Contraception.
Contraindications
Presence or history of venous thrombosis (including deep vein thrombosis of the lower leg, pulmonary artery thromboembolism) - the presence of arterial thrombosis (including myocardial infarction, stroke) or thrombosis precursors at the moment ( including transient attack of coronary artery disease, angina pectoris .– identified susceptibility to venous or arterial thrombosis, including resistance to activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (anti bodies to cardiolipin, lupus anticoagulant); - migraine with focal neurological symptoms in history; - diabetes mellitus with vascular lesion; - presence of severe or multiple risk factors for venous or arterial thrombosis (including arterial hypertension with AD 160/100 mm Hg Art. and above); - pancreatitis (including a history of), accompanied by severe hypertriglyceridemia; - severe liver disease (until normalization of liver function indicators), including in history - liver tumors (benign and malignant), incl. in history; hormone-dependent malignant neoplasms of the genital organs or mammary glands (includingsuspected); - bleeding from the vagina of unknown etiology; - smoking over the age of 35 years (more than 15 cigarettes per day); - pregnancy (including suspected); - lactation period; - lactose intolerance, lactase deficiency, glucose-galactose malabsorption; - hypersensitivity to the drug components. If while using the drug Mercilon; (like other PDA) any of the above diseases (conditions) occurs, you should immediately stop taking the drug. The drug is contraindicated in severe liver diseases, liver tumors (benign and malignant), including in the anamnesis.
Precautionary measures
With caution: If any of the conditions / risk factors listed below are presently present, then the potential risk and the expected benefits of using the drug Mercilon should be carefully weighed; in each individual case: age over 35 years; smoking; family history of thromboembolic diseases (venous or arterial thrombosis / thromboembolism in siblings or parents at a relatively early age); obesity (body mass index> 30 kg / m2); dyslipoproteinemia; arterial hypertension; migraine; valvular heart disease; atrial fibrillation; prolonged immobilization, extensive surgery, surgery on the lower limbs, severe trauma (with prolonged immobilization and the above surgical interventions, it is recommended to stop using the drug, with planned surgical interventions no later than 4 weeks before surgery, and not to resume reception for 2 weeks after complete remobilization); varicose veins, superficial thrombophlebitis (at the moment there is no unequivocal opinion about the possible role of these conditions in the etiology of venous thromboembolism); postpartum period; changes in biochemical parameters that may be markers of congenital or acquired susceptibility to venous or arterial thrombosis (including resistance to activated protein C, hyperhomocysteinemia, deficiency of antithrombin III, deficiency of protein C, deficiency of protein S, antiphospholipid antibodies, includingantibodies to cardiolipin, lupus anticoagulant); diabetes; systemic lupus erythematosus; hemolytic uremic syndrome; chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis); sickle cell anemia; hypertriglyceridemia (including a family history); acute and chronic liver diseases, including congenital hyperbilirubinemia (Gilbert, Dubin-Johnson syndrome, Rotor).
Use during pregnancy and lactation
Use of the drug Mercilon; during pregnancy is contraindicated. In the event of pregnancy with the use of Mercilon should stop taking the drug. It should be noted that extensive epidemiological studies did not reveal an increase in the risk of having children with birth defects in women who took COCs before pregnancy, or a teratogenic effect if they inadvertently receive COCs in early pregnancy Mercilon; may affect lactation, because PDAs reduce the amount and change the composition of breast milk. Therefore Mercilon; It is not recommended to apply until the nursing mother completely stops breastfeeding. A small amount of contraceptive steroids and / or their metabolic products may be excreted in breast milk.
Dosage and administration
Tablets should be taken orally in the order indicated on the packaging, every day at about the same time, with a small amount of water, if necessary. Take 1 tablet / day for 21 days. Acceptance of pills from the next package should be started 7 days after the end of the previous one. During these 7 days, menstrual bleeding occurs. It usually starts 2-3 days after taking the last pill and may not stop before the next pack is started. How to start taking Mercilon ;. If hormonal contraceptives have not been used during the last month, then take the drug on the 1st day of the menstrual period. cycle. You can start taking the drug at 2-5 days after the start of the menstrual cycle, but in this case it is recommended to use an additional (non-hormonal) method of contraception during the first 7 days of taking the pills in the first cycle. The transition from combined hormonal contraceptives (CPC,vaginal ring or transdermal patch): it is advisable to start taking the drug Mercilon; the next day after taking the last active tablet of a previously used drug (the last tablet containing the active substances), but no later than the next day after the end of the usual interruption in taking the pills or the next day after taking the last pill that does not contain hormones. In case of using the vaginal ring or transdermal patch, it is advisable to start taking the drug Mercilon; on the day of their removal, but not later than the day when the new ring should have been inserted or the next patch applied. If the woman applied the previous method of contraception consistently and correctly and if it is reliably known that the woman is not pregnant, in this case the woman can switch to taking the drug Mercilon; on any day of the cycle. It should be borne in mind that the usual interval in applying the previous method of contraception should not exceed its recommended duration. Transfer from drugs containing only progestogen (mini-drank, injection, implant) or from the progestogen-releasing intrauterine system (IUD). A woman taking a mini-drink can go on a drug Marvelon any day; using an implant or IUD - on the day of their removal; using the drug in the form of injections - on the day when there should be the next injection, in all cases during the first 7 days of taking the drug Mercilon; It is recommended to use additional methods of contraception. After an abortion made in the first trimester: a woman can start taking the drug immediately. There is no need to use any additional methods of contraception. After a birth or abortion made in the II trimester, it is recommended to start taking the drug no earlier than 21-28 days after the birth or abortion made in the II trimester of pregnancy. At the beginning of taking the drug at a later date, it is recommended during the first 7 days of taking the drug Mercilon; use barrier methods of contraception. In any case, if a woman has a child after childbirth or an abortion before the start of taking Mercilon; There were already sexual contacts, you should exclude pregnancy before taking the drug or wait until the first menstruation. If you miss the next drug intake. If the next pill is delayed for less than 12 hours, the contraceptive reliability does not decrease.A woman should take a pill as soon as she remembered it, and take the next pill at the usual time. If the reception of a regular pill is delayed for more than 12 hours, the reliability of contraception can be reduced. In this case, the following rules should be followed: 1. pill intake should never be interrupted for more than 7 days; 2. for adequate suppression of the hypothalamic-pituitary-ovarian system, you must take the pill 7 days in a row. The cyclical use of the drug involves 3 weeks of use. Therefore, the following recommendations can be given. Week 1. A woman should take a missed pill as soon as she remembers, even if it means taking 2 pills at the same time. Then you should continue to receive the usual pattern. Additionally, use the barrier contraceptive method for the next 7 days. If a woman has had sexual intercourse within the previous 7 days, consider the possibility of pregnancy. The more pills are missed, and the closer the break in taking the drug at the time of sexual intercourse, the higher the risk of pregnancy. Week 2. The woman should take the missed pill as soon as she remembered, even if it means taking two pills at the same time. Then you should continue to receive the usual pattern. Provided that the woman took the tab. on time within 7 days preceding the first missed dose, there is no need to use additional (non-hormonal) methods of contraception. Otherwise, or if the woman missed more than 1 tablet, it is recommended to use additional methods of contraception for the next 7 days. Week 3. Reliability of contraception may be reduced, due to the subsequent interruption in the administration of the drug. This can be avoided by adapting the regimen. If you use either of the following two schemes, there is no need to use additional contraceptive measures, provided that the woman took the pills on time within 7 days preceding the first missed dose. Otherwise, it is recommended to use one of the two following schemes and also to use additional contraceptive measures over the next 7 days.A woman should take the missed pill as soon as she remembered about it, even if it means taking 2 pills at the same time. Then you should continue to receive the usual pattern. New packaging should start as soon as the current packaging ends, i.e. do not break between packs. The likelihood of withdrawal bleeding before the end of the second package is small, but some may experience a spotting or heavy bleeding even while taking the drug. It may be recommended to stop taking the drug from the current package. A woman should take a break in taking the drug Mercilon; lasting no more than 7 days, including the days when she forgot to take the pills, and then start a new package. When skipping the drug and following no withdrawal bleeding in the near interruption in the pill, consider the possibility of pregnancy. Recommendations in case of gastrointestinal disorders. In severe gastrointestinal disorders, absorption may be incomplete and additional contraceptive measures should be taken. If vomiting occurs within 3-4 hours after taking the drug, you should use the recommendations regarding skipping the next dose of the drug. If a woman does not want to change her usual regimen, she needs to take an extra pill (s) from another package (the number of additional pills is determined when visiting the obstetrician-gynecologist. How to change the period of menstruation. To delay the menstruation, you should continue taking pills from another package of the drug Mercilon; without the usual interruption in reception. You can postpone menstruation for any period until the end of the table from the second package. During this period, a woman may have spotting or heavy blood Discharge of the drug. The usual pattern should be resumed after a 7-day interval in reception. In order to shift menstruation on a day of the week different from that expected if the usual regimen is observed, it is possible to reduce the usual interruption in reception for so many days, as needed. The shorter the break, the higher the risk of the absence of menstruation during the break and the occurrence of heavy or spotting bleeding while taking the drug from the second package.
Side effects
Since the cardiovascular system: thrombosis or thromboembolism (includingmyocardial infarction, stroke, deep vein thrombosis, pulmonary thromboembolism (hepatic thromboembolism, mesenteric, renal arteries and veins, retinal arteries); increase in blood pressure hormones: liver tumors, breast cancer. On the skin: chloasma (especially if there is a history of chloasma during pregnancy). On the part of the reproductive system: acyclic bloody discharge more often in the first months of admission. Other: allergic reactions. The side effects that have been noted while taking the drug Mercilon; but which have not been shown to take the drug. Frequently: (≥ 1/100) Infrequently (≥1 / 1000- <1/100) Rarely (<1/1000). Со side of the immune system; hypersensitivity.For metabolism and nutrition; weight gain; fluid retention; weight loss. From the nervous system; depression; mood swings; migraine headache; decreased libido; increased libido. For the organ of vision; contact lenses intolerance. From the side of the digestive system; nausea; abdominal pain vomiting. On the side of the skin and subcutaneous tissue; skin rash, urticaria, erythema nodosum; erythema multiforme. For the reproductive system; breast tenderness; increase in mammary glands discharge from the vagina; discharge from the mammary glands.
Overdose
Symptoms: possible nausea, vomiting, in young girls - bleeding from the vagina. Any serious complications of an overdose of the drug Mercilon; not observed. Treatment: symptomatic therapy. There are no antidotes.
Interaction with other drugs
The interaction between oral contraceptives and other drugs can lead to acyclic bleeding and / or decrease the effectiveness of contraceptives. The following interactions are described in the literature. Hepatic metabolism: interaction may occur with inducers of microsomal liver enzymes, which may lead to an increase in the clearance of sex hormones (for example, phenytoin, barbiturates, primidone, carbamazepine, rifampicin, rifabutin; and possibly also oxcarbazepine, topiramate, felbampam, felbes. ritonavir, griseofulvin and preparations containing St. John's wort). The maximum induction of enzymes is not observed in the first 2-3 weeks of taking the drug Mercilon; but may occur at the end of 4 weeks after the usual interruption in taking the drug. A violation of the contraceptive effect when taking the drug Mercilon was also reported; with antibiotics such as ampicillin and tetracyclines.The mechanism of this effect is not clear. Women who are taking any of the above drugs should temporarily use an additional method of barrier contraception or choose another method of contraception. With the simultaneous use of microsomal enzyme inducers, a barrier method of contraception should be used throughout the entire course of treatment and for 28 days after stopping treatment. In the case of long-term treatment using inducers of microsomal enzymes, it is necessary to use another method of contraception. During antibiotics (with the exception of rifampicin and griseofulvin, which are inducers of microsomal enzymes), it is necessary to use a barrier method of contraception throughout the course of treatment and for 7 days after the end of therapy. If the period during which the barrier method of contraception is used continues even after the end of the pills in the CCP package, then the next package of the drug should be started without the usual interval intake. tissues: increase (for example, cyclosporine) or decrease (lamotrigine). With the concomitant use of other drugs, sex is necessary Call instructions for medical use of these medicines.
special instructions
If any of the conditions or risk factors listed below are present, you should carefully weigh the benefits and the possible risk of taking Mercilon; This question should be discussed with the patient before the start of the drug. In the case of exacerbation of diseases, deterioration of the condition or the appearance of the first symptoms of these conditions or risk factors, the patient should immediately consult a doctor. The doctor decides on canceling the drug individually. Vascular diseases: During epidemiological studies, it was established that there may be a link between the use of the drug Mercilon; and an increased risk of arterial and venous thrombotic and thromboembolic diseases, such as myocardial infarction, stroke, deep vein thrombosis, and pulmonary embolism.These diseases are extremely rare. The use of any PDA is associated with an increased risk of venous thromboembolism (VTE), manifested as deep vein thrombosis and / or pulmonary thromboembolism, sometimes with fatal consequences. The risk is higher in the first year of admission than in women taking CPC for more than 1 year. Some epidemiological studies show that women who have taken low-dose CPC that contain third-generation progestogens, including desogestrel, have an increased risk of VTE compared with those who took low-dose CPCs containing progestogen levonorgestrel. Thrombosis is extremely rare in other blood vessels (for example, in the veins and arteries of the liver, mesentery, kidneys, brain or retina). There is no single point of view whether this thrombosis is a consequence of the use of PDA. An increase in the frequency and intensity of migraines when taking the drug Mercilon; (which may be a sign of cerebrovascular disorders) may serve as a basis for immediate discontinuation of the drug. Tumors: The persistence of the human papillomavirus (HPV infection) is the most important risk factor for developing cervical cancer. Some epidemiological studies have noted an increase in the risk of cervical cancer in women who receive CPC for a long time, but so far there are controversies about the extent to which various factors influence such mixing data, such as cervical screening and sexual behavior, including their relationship. There is evidence that there is a slight increase in the relative risk (1.24) of breast cancer in women using PDA. The increased risk gradually decreases over 10 years after the abolition of COC. Since breast cancer in women under 40 years of age is quite rare, the increase in the likelihood of developing breast cancer in women receiving CCP currently or recently abandoned their use is small relative to the initial probability of developing cancer. These studies do not provide data on the etiology of cancer. The increase in the risk of breast cancer can be explained by the fact that in women receiving CPC, the diagnosis of breast cancer is established earlier,and the biological effects of CPC, or a combination of both of these factors. There is a tendency that women who have ever taken CPC have breast cancer that is less clinically advanced than women who have never taken CPC. It is extremely rare when using the drug Mercilon; there have been cases of benign, and even more rarely, malignant liver tumors. In some cases, these tumors led to life-threatening intra-abdominal bleeding. The doctor should consider the possibility of a liver tumor in the differential diagnosis of diseases in a woman receiving Mercilon; if the symptoms include acute pain in the upper abdomen, enlarged liver or signs of intra-abdominal bleeding. Other diseases: If hypertriglyceridemia is diagnosed in a woman or her family member, it may increase the risk of pancreatitis when taking the drug Mercilon ;.If a woman receiving Mercilon; develops persistent clinically conceivable arterial hypertension, the doctor should about to cancel Mercilon; and prescribe the treatment of hypertension. In cases where it is possible to achieve normal blood pressure with antihypertensive therapy, the doctor may consider it possible for the patient to resume taking the drug. There are reports that jaundice and / or itching caused by cholestasis; gallstones, porphyria, systemic lupus erythematosus, hemolytic-uremic syndrome, Sideyama chorea (minor chorea), pregnant herpes, hearing loss due to otosclerosis, (hereditary) angioedema develop or worsen during pregnancy and when taking the drug Mercilon ; however, the evidence regarding the administration of the drug Mercilon ;, is inconclusive. Acute or chronic liver dysfunction may serve as a basis for discontinuation of the drug Mercilon; until liver function normalizes. Relapse of cholestatic jaundice, observed earlier during pregnancy or when using sex steroids, requires discontinuation of the drug Mercilon;. Although Mercilon; can affect the tolerance of peripheral tissues to insulin and glucose, there is no evidence that patients with diabetes need to change the therapeutic regimen of low-dose PDA (containing less than 50 μg of ethinyl estradiol).In any case, while taking the drug Mercilon; Patients with diabetes mellitus need careful medical control. There is evidence of a link between taking CPC and Crohn's disease and ulcerative colitis. Sometimes, while taking the drug Mercilon; skin pigmentation (chloasma) may occur, especially if it was previously present during pregnancy. Women with a predisposition to chloasma should avoid direct sunlight and UV radiation from other sources when taking the drug Mercilon; .Medical examinations / consultations: Before starting or resuming taking the drug Mercilon; the doctor must collect a detailed medical history (including family history) and conduct a thorough examination. It is necessary to measure blood pressure and in the event of the detection of clinically significant signs, it is necessary to conduct a physical examination, guided by contraindications and warnings. A woman should be instructed to carefully read the instructions for use of the drug and adhere to the recommendations. The frequency and list of examinations should be based on common practice and selected individually for each woman (but not less than 1 time in 6 months). It should be reported to the woman that oral contraceptives do not protect against HIV (AIDS) and other sexually transmitted infections. Reduced efficacy: The effectiveness of the drug Mercilon; may decrease if you miss a drug intake, gastrointestinal disorders or with the concomitant use of certain medications. Irregular spotting: When you take the drug Mercilon; especially in the first months of use, there may be irregular spotting or copious bloody discharge. Therefore, assessment of irregular bleeding should be carried out only after the end of the adaptation period, lasting 3 months. If irregular bleeding persists or appears after previous regular cycles, consider possible non-hormonal causes of cycle disturbances and conduct appropriate studies to exclude malignant tumors or pregnancy. These measures may include diagnostic curettage. Some women may not have menstrual-like bleeding in between taking the drug. If taking the drug Mercilon; was carried out according to the above recommendations, the probability of pregnancy is small.Otherwise, or if there is no bleeding 2 times in a row, the possibility of pregnancy should be excluded. -binding globulin and lipid / lipoprotein fractions, carbohydrate metabolism parameters, coagulation and fibrinolysis parameters. Typically, these changes are within the normal values of laboratory parameters. Lactose: Each tablet of the drug Mercilon; contains less than 80 mg of lactose. Women with rare hereditary disorders, such as lactose intolerance, lactase deficiency, glucose-galactose malabsorption, who follow a lactose-free diet, should take into account the lactose content of Mercilon ;.