Mercilon tablets 21 pcs. (tar, Ethinyl estradiol)
Special Price
$53.46
Regular Price
$54.00
In stock
SKU
florida494404
Release form
Tablets. Buy Mercilon tablets 21 pcs. (tar, Ethinyl estradiol) in florida free shipping. Fast international shipping USA, AU, EU, UK and others.
Tablets. Buy Mercilon tablets 21 pcs. (tar, Ethinyl estradiol) in florida free shipping. Fast international shipping USA, AU, EU, UK and others.
Release form
Tablets.
Packaging
21 pcs
Pharmacological action of
Pharmacodynamics of
The contraceptive effect of the drug Mercilon®, like other combined oral contraceptives (COCs), is based on the interaction of various factors, the most important of which are suppression of ovulation and changes in cervical secretion.
A progestogen (desogestrel) reduces the secretion of gonadotropic hormones, more luteinizing hormone (LH), and thus prevents follicle maturation (blocks ovulation). Ethinyl estradiol, a synthetic analogue of the natural hormone estradiol, reduces the likelihood of acyclic spotting when using COCs.
Along with the indicated central and peripheral mechanisms that prevent the fertilization of a fertile egg, the contraceptive effect is due to an increase in the viscosity of the mucus located in the cervix, which makes it relatively impassable for sperm.
In addition to contraceptive properties, 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 accompanied by less severe bleeding. The latter circumstance leads to a decrease in the frequency of concomitant iron deficiency anemia. When using COCs, a decrease in the risk of developing ovarian and endometrial cancer has been shown.
Pharmacokinetics
Desogestrel
Absorption
Oral desogestrel is rapidly and completely absorbed and then converted to etonogestrel. Its maximum concentration in blood serum is reached after 1.5 hours. Bioavailability is 62-81%.
Distribution of
Etonogestrel binds to serum albumin and sex hormone binding globulin (SHBG). Only 2-4% of the total concentration of etonogestrel in serum is present as a free steroid, 40-70% specifically bind to SHBG. An increase in the concentration of SHBG caused by ethinyl estradiol has an effect on the distribution between blood proteins, leading to an increase in the SHBG-related fraction and a decrease in the albumin-bound fraction. The apparent volume of distribution of desogestrel is 1.5 l / kg.
Metabolism
Etonogestrel is completely metabolized by known metabolic pathways of steroid hormones. The metabolic excretion rate from serum is 2 ml / min / kg. No interaction of etonogestrel with ethylene estradiol taken simultaneously.
Excretion of
The concentration of etonogestrel in serum decreases in 2 stages. The final stage is characterized by a half-life (T1 / 2) of about 30 hours. Desogestrel and its metabolites are excreted by the kidneys and through the intestines in a ratio of approximately 6: 4.
Equilibrium conditions
The pharmacokinetics of etonogestrel are influenced by SHBG, the concentration of which increases by 3 times under the influence of ethinyl estradiol. With daily use, the concentration of etonogestrel in blood serum increases by 2-3 times, reaching a constant value in the second half of the cycle.
Ethinyl estradiol
Absorption
Ethinyl estradiol after oral administration is rapidly and completely absorbed. Its maximum plasma concentration is achieved within 1-2 hours after administration. Absolute bioavailability (the result of presystemic metabolism) is about 60%.
Distribution of
Ethinyl estradiol non-specifically binds to serum albumin almost completely (98.5%), contributes to an increase in the concentration of SHBG. The apparent volume of distribution of ethinyl estradiol is 5 l / kg.
Metabolism
Ethinyl estradiol undergoes a presystemic metabolism, both in the mucous membrane of the small intestine and in the liver. Ethinyl estradiol is initially metabolized during aromatic hydroxylation to form a variety of hydroxylated and methylated metabolites, which are present both in the free state and in the form of conjugates with glucuronides and sulfates. The metabolic excretion rate of ethinyl estradiol from blood plasma is about 5 ml / min / kg.
Excretion of
The concentration of ethinyl estradiol in serum decreases in 2 stages. The final stage is characterized by T1 / 2 for about 24 hours. Unchanged, the drug is not excreted, ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6. T1 / 2 of metabolites is about a day.
Equilibrium conditions
Equilibrium concentration is reached after 3-4 days of administration, when the concentration in serum is 30-40% higher than the concentration after taking one dose.
Indications
Contraception.
Contraindications
The drug MercilonВ®, like other combined oral contraceptives, should not be taken in the presence of any of the diseases (conditions) listed below. If any of them occurs while taking the drug, you should immediately stop taking it.
Hypersensitivity to active substances or to any excipient of the drug MercilonВ®.
The presence at present or in the history of venous thrombosis (including deep vein thrombosis of the leg, thromboembolism of the pulmonary artery).
The presence at the moment or in the history of arterial thrombosis (including myocardial infarction, stroke) or precursors of thrombosis (incl. transient ischemic attack, angina pectoris).
Identified predisposition to venous or arterial thrombosis, including resistance to activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).
Migraine with focal neurological symptoms in history.
Diabetes mellitus with vascular disease.
The presence of severe or multiple risk factors for venous or arterial thrombosis (including arterial hypertension with a blood pressure of 160/100 mmHg or higher).
Pancreatitis (including a history), accompanied by severe hypertriglyceridemia
Severe liver disease (before normalization of liver function indicators), incl. in the anamnesis.
Tumors of the liver (benign and malignant), incl. in the anamnesis.
Hormone-dependent malignant neoplasms of the genitals or mammary glands (including suspects).
Vaginal bleeding of unknown etiology.
Smoking older than 35 years (more than 15 cigarettes per day).
Pregnancy (including implied).
Lactation.
Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Caution:
If any of the conditions / risk factors listed below are present, you should carefully consider the potential risk and expected benefits of using MercilonВ® in each individual case:
Age over 35 years old
Smoking
The presence of thromboembolic diseases in the family history (venous or arterial thrombosis / thromboembolism in siblings or in parents at a relatively young age)
Obesity (body mass index> 30 kg / m)
emia
Migraine
Valvular heart defects
Atrial fibrillation
Prolonged immobilization, extensive surgery, surgery on the lower extremities, severe trauma (with prolonged immobilization and the aforementioned surgical procedures recommended to stop drug use, not later than 4 weeks during elective surgery to surgery and do not resume taking it within 2 weeks after complete remobilization)
Varicose veins, superficial thrombophlebitis (at the moment there is no unequivocal opinion on 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 an acquired predisposition to venous or arterial thrombosis, including resistance to activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant)
Diabetes mellitus
Systemic lupus erythematosus
Hemolytic-uremic syndrome
Chronic inflammatory bowel disease (Crohn’s disease or ulcerative colitis)
Sickle-cell anemia including congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson syndrome, Rotor).
Use during pregnancy and lactation
Use of the drug Mercilon® during pregnancy is contraindicated. In case of pregnancy when using the drug Mercilon®, you should stop taking the drug. It should be noted that extensive epidemiological studies did not reveal an increased risk of giving birth to children with birth defects in women who took COCs before pregnancy, or teratogenic effects in case of inadvertent use of COCs at the beginning of pregnancy.
Mercilon® can affect lactation, since COCs reduce the amount and alter the composition of breast milk. Therefore, the use of the drug Mercilon® is not recommended until the nursing mother has completely stopped breast-feeding.
A small amount of contraceptive steroids and / or their metabolic products may be excreted in milk.
Special instructions
If you have any of the following conditions or risk factors, you should carefully weigh the benefits and possible harm of taking MercilonВ®. This question should be discussed with the patient before starting the drug. In the case of exacerbation of disease, worsening of the condition or the appearance of the first symptoms of the above conditions or risk factors, the patient should immediately consult a doctor. The doctor should decide whether to discontinue the drug.
Vascular disease
An epidemiological study found that there may be a link between COC use 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 COC is associated with an increased risk of venous thromboembolism (VTE), manifested as deep vein thrombosis and / or pulmonary embolism. The risk is higher in the first year of admission than in women taking COCs for more than 1 year.
Some epidemiological studies show that women who took low-dose COCs containing the third generation of gestagens, including desogestrel, have an increased risk of VTE compared to women who took low-dose COCs containing levonorgestrel gestagen.
Very rarely, thrombosis occurs in other blood vessels (for example, in the veins and arteries of the liver, mesentery, kidney, brain or retina). There is no single point of view whether this thrombosis is a consequence of the use of COCs.
An increase in the frequency and intensity of migraines when taking the drug MercilonВ® (which may be a sign of cerebrovascular disorders) may serve as the basis for immediate discontinuation of the drug. Tumors
The most important risk factor for cervical cancer is the persistence of the human papillomavirus (HPV infection). Epidemiological studies have shown an increase in the risk of cervical cancer in women who have been using COCs for a long time, however, there is still uncertainty about the degree of influence of various factors on this data, such as an increase in screening examinations of the cervix and differences in sexual behavior, including the use of barrier methods contraception, or their relationship.
There is evidence that there is a slight increase in relative risk (1, 24) the development of breast cancer in women using COCs. The increased risk gradually decreases within 10 years after the withdrawal of COCs. Since breast cancer in women under 40 years of age is quite rare, the increase in the likelihood of developing breast cancer in women who are currently using COCs or have 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 increased risk of breast cancer can be explained both by the fact that in women taking COCs, the diagnosis of breast cancer is established earlier, and by the biological effects of COCs, or a combination of both of these factors. There is a tendency that in women who have ever taken COCs, breast cancer is clinically less advanced than in women never taking COCs.
Very rarely, with the use of the drug MercilonВ®, there have been cases of the development 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 taking MercilonВ® if the symptoms include acute pain in the upper abdomen, enlarged liver, or signs of intra-abdominal bleeding.
Other diseases
If a woman or her family is diagnosed with hypertriglyceridemia, then the risk of pancreatitis may be increased when taking MercilonВ®.
If a woman using the drug Mercilon® persistent clinically significant arterial hypertension develops, the doctor should discontinue the drug Mercilon® and prescribe treatment for arterial hypertension. In cases where it is possible to achieve normal blood pressure values ​​with antihypertensive therapy, the doctor may consider it possible for the patient to resume taking the drug.
There are reports that jaundice and / or pruritus caused by cholestasis are gallstones, porphyria, systemic lupus erythematosus, hemolytic uremic syndrome, Sydenham chorea (small chorea), pregnant herpes, hearing loss due to otosclerosis, (hereditary) angioedema develop or are aggravated both during pregnancy and when taking the drug MercilonВ®, however, evidence of this in part regarding the administration of the drug MercilonВ® is inconclusive.
Acute or chronic dysfunction of the liver may serve as a basis for discontinuation of the drug MercilonВ® until the indicators of liver function are normalized. Relapse of cholestatic jaundice, observed earlier during pregnancy or when using sex steroid preparations, requires the discontinuation of the drug MercilonВ®.
Although MercilonВ® may affect peripheral tissue tolerance to insulin and glucose, there is no evidence that patients with diabetes need to change the therapeutic regimen for low-dose COCs (containing less than 0.05 mg of ethinyl estradiol). In any case, women with diabetes should be carefully monitored by a doctor while taking MercilonВ®.
There is evidence that there is a connection between COC administration and Crohn's disease and ulcerative colitis.
Sometimes when taking the drug MercilonВ® pigmentation of the skin of the face (chloasma) can be observed, especially if it was previously during pregnancy. Women with a predisposition to chloasma should avoid direct sunlight and ultraviolet radiation from other sources when taking the drug MercilonВ®.
Medical examinations / consultations
Before you start or resume using MercilonВ® in a woman, you need to collect a detailed medical history (including family history) and conduct a thorough examination. It is necessary to measure blood pressure and in the case of the detection of clinically significant signs, it is necessary to conduct a physical examination, guided by contraindications and warnings. You should instruct the woman about the need to carefully read these instructions for use and adhere to the recommendations. The frequency and list of examinations should be based on generally accepted practice and selected individually for each woman (but at least 1 time in 6 months).
A woman should be advised that oral contraceptives do not protect against HIV (AIDS) and other sexually transmitted infections.
Decreased efficacy of
The effectiveness of MercilonВ® may decrease if you skip the drug, have a gastrointestinal upset, or take certain medications concomitantly (see Interaction with Other Medicines).
Irregular spotting
When taking MercilonВ®, especially in the first months of use, irregular spotting or heavy spotting may occur. Therefore, the assessment of irregular bleeding should be carried out only after the end of the adaptation period, lasting three months.
If irregular bleeding persists or appears after previous regular cycles, you should consider the possible non-hormonal causes of the cycle disorder and conduct appropriate studies to exclude malignant neoplasms or pregnancy. These measures may include diagnostic curettage.
Some women may not have menstrual bleeding between meals. If the drug MercilonВ® was taken according to the recommendations given above, the probability that the woman is pregnant is small. Otherwise, or if there are no bleeding twice in a row, the possibility of pregnancy should be excluded and consult a doctor.
Laboratory studies
Oral contraceptives may affect the results of several laboratory studies, including biochemical parameters of liver, thyroid, adrenal and kidney function, plasma transport protein content, for example, corticosteroid-binding globulin and lipid / lipoprotein fractions, carbohydrate metabolism parameters, parameters coagulation and fibrinolysis. Typically, these changes are within normal laboratory values.
Lactose
Each tablet of MercilonВ® 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, must take into account the lactose content in the drug MercilonВ®.
Influence on the ability to drive a car and other mechanisms
No effect of the drug MercilonВ® on the ability to drive a car and work with mechanisms was noted.
Composition
Active ingredients:
Desogestrel 0.150 mg
Ethinyl estradiol 0.020 mg.
Excipients:
Potato starch 8.0 mg
povidone 2.4 mg
stearic acid 0.8 mg
colloidal silicon dioxide 0.8 mg
alpha tocopherol 0.08 mg
lactose monohydrate up to 80 mg.
Dosage and administration of
Tablets should be taken orally in the order indicated on the package, every day at approximately the same time, with a little water if necessary. Take 1 tablet daily for 21 days. Taking tablets from the next package should begin 7 days after the previous one. During these 7 days, menstrual bleeding occurs. Usually it begins 2-3 days after taking the last pill and may not stop until the next package is taken.
How to start taking Mercilon®
- If hormonal contraceptives have not been used within the last month
Tablets should be taken on the 1st day of the menstrual cycle (i.e. on the first day of menstrual bleeding). You can start taking the drug on the 2nd-5th day of the 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 tablets in the first cycle.
- Transition from combined hormonal contraceptives (combined oral contraceptive, vaginal ring or transdermal patch)
It is advisable to start taking Mercilon® the day after taking the last active tablet of the previously used drug (last tablet containing active substances), but no later than the day after the end of the usual break in taking pills or the day after taking the last hormone-free pill. In case of using a vaginal ring or transdermal patch, it is advisable to start taking Mercilon® on the day of their removal, but no later than the day when a new ring was to be introduced or the next patch application was made.
If a woman used 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 Mercilon® on any day of the cycle.
It should be noted that the usual interval in the application of the previous method of contraception should not exceed its recommended duration.
- Switching from drugs containing only gestagen (mini-pill, injection, implant) or from the gestagen-releasing intrauterine system (IUD)
A woman taking a mini-pill can switch to Mercilon® any day using an implant or IUD - on the day of their removal using the drug in the form of injections - per day, when the next injection should be, 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 in the first trimester
A woman can start taking the drug immediately. There is no need to use any additional methods of contraception.
- After giving birth or having a second trimester abortion
For nursing mothers, see the section “Use during Pregnancy and Breastfeeding”.
It is recommended to start taking the drug no earlier than 21-28 days after childbirth or abortion in the second trimester of pregnancy. At the beginning of taking the drug at a later date, it is recommended to use barrier methods of contraception during the first 7 days of taking the drug Mercilon®. Anyway, if a woman after childbirth or abortion prior to taking the drug Mercilon® already had sexual intercourse, pregnancy should be excluded before taking the drug or wait until the first menstruation.
What to do if you miss the next dose of
If the next pill is delayed by less than 12 hours, the reliability of contraception does not decrease. A woman should take a pill as soon as she remembers this, and take the next pill at the usual time.
If taking the next pill is delayed for more than 12 hours, the reliability of contraception may be reduced. In this case, you should be guided by the following two rules:
1. taking tablets should never be interrupted for more than 7 days.
2. for adequate suppression of the hypothalamic-pituitary-ovarian system, tablets must be taken 7 days in a row.
Cycling of the drug involves 3 weeks of use. Accordingly, you can give the following recommendations:
Week 1
A woman should take a missed pill as soon as she remembers this, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. Additionally, the method of barrier contraception should be used over the next 7 days. If a woman has had sexual intercourse in the previous 7 days, the possibility of pregnancy should be considered. The more tablets missed, and the closer the interruption in taking the drug to the time of sexual intercourse, the higher the risk of pregnancy.
Week 2
A woman should take a missed pill, as soon as she remembered it, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. Provided that the woman took the tablets on time for 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 over the next 7 days.
Week 3
Reliability of contraception may be reduced due to a subsequent interruption in taking the drug. This can be avoided by adapting the drug regimen. If you use either of the following two schemes, there is no need to use additional contraceptive measures, provided that a woman took the pill on time for 7 days preceding the first missed dose. Otherwise, it is recommended to use one of the following two schemes and also use additional contraceptive measures over the next 7 days.
1. A woman should take a missed pill as soon as she remembers this, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. A new package should be started as soon as the current package ends, i.e., there should be no break between packages. The likelihood of “withdrawal bleeding” before the end of the second package is small, but some may have spotting or heavy spotting while taking the drug.
2. A woman can be advised 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 pills, and then start a new package.
If you skip taking the drug and the subsequent absence of “withdrawal bleeding” in the next break in taking the pills, you should consider the possibility of pregnancy.
Recommendations for gastrointestinal upsets
If severe gastrointestinal upsets are present, absorption may not be complete 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. If a woman does not want to change her usual regimen, she needs to take additional (s) tablet (s) from another package (the number of additional tablets is determined by a specialist obstetrician-gynecologist at a face-to-face consultation).
How to change the period of onset of menstrual bleeding
In order to delay menstrual bleeding, you should continue to take tablets from another package of the drug Mercilon® without the usual interruption. You can delay menstrual bleeding for any period until the end of the tablets from the second package. During this period, a woman may experience spotting or heavy spotting. Taking the drug according to the usual schedule should be resumed after a 7-day interval in admission.
In order to shift the day of the onset of menstrual bleeding to another day, You can shorten your regular pill break by as many days as necessary. The shorter the break, the higher the risk of no menstrual bleeding during the break and the occurrence of heavy or spotting spotting while taking the tablets from the second package.
Side effects
Thrombosis or thromboembolism (including myocardial infarction, stroke, deep vein thrombosis, pulmonary embolism), hepatic, mesenteric, renal arteries and veins, retinal arteries.
Increased blood pressure.
Hormone-dependent tumors (liver tumors, breast cancer).
Chloasma (especially in the case of a history of chloasma during pregnancy).
Acyclic spotting is more common in the first months of administration.
Allergic reactions.
Drug Interactions
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: interactions can occur with drugs that induce microsomal enzymes, which can lead to increased clearance of sex hormones (e.g. phenytoin, barbiturates, primidone, carbamazepine, rifampicin, rifabutin, and possibly also oxcarbazepine, topiramate, felvirfam, felvirfam preparations containing St. John's wort perforated). 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 break in taking the drug.
A contraceptive effect has also been reported while taking Mercilon® with antibiotics such as ampicillin and tetracyclines. The mechanism of this influence is not clear.
Women who take any of the above drugs should temporarily use the additional method of barrier contraception or choose another method of contraception. With the simultaneous use of inducers of microsomal enzymes, the barrier method of contraception should be used throughout the course of treatment and within 28 days after cessation of treatment. In the case of long-term treatment with the use of inducers of microsomal enzymes, another method of contraception must be used. Women who use antibiotics (excluding rifampicin and griseofulvin, which possess the properties of inducers of microsomal enzymes) should use the barrier method of contraception throughout the course of treatment and within 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 tablets in the COC package, then the next package of the drug must be started without the usual interval in admission.
Oral contraceptives may affect the metabolism of other medicines.
Accordingly, they can change their concentration in plasma and tissues: increase (for example, cyclosporine) or decrease (lamotrigine).
When treating with other drugs, to determine possible interactions, you should read the instructions for medical use of these drugs.
Overdose
No serious complications were observed with an overdose of Mersilon®. Symptoms that can occur with overdose: nausea, vomiting, young girls - bloody discharge from the vagina. There are no antidotes and further treatment should be symptomatic.
Storage Conditions
Store at 2 to 30 ° C in a dry, dark place.
Keep out of the reach and sight of children.
Shelf life
3 years.
Deystvuyushtee substance
Desogestrel, Эtinilэstradiol
Terms and conditions vacation vacation srdlk holiday recipe holiday vacation prescription
dosage form
tablets
At
value Prescription
For women, Adults as prescribed by a doctor, For women of childbearing age
N.V. Organon, the Netherlands
Mercilon tablets 21 pcs. (tar, Ethinyl estradiol) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Mercilon tablets 21 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.
Tablets.
Packaging
21 pcs
Pharmacological action of
Pharmacodynamics of
The contraceptive effect of the drug Mercilon®, like other combined oral contraceptives (COCs), is based on the interaction of various factors, the most important of which are suppression of ovulation and changes in cervical secretion.
A progestogen (desogestrel) reduces the secretion of gonadotropic hormones, more luteinizing hormone (LH), and thus prevents follicle maturation (blocks ovulation). Ethinyl estradiol, a synthetic analogue of the natural hormone estradiol, reduces the likelihood of acyclic spotting when using COCs.
Along with the indicated central and peripheral mechanisms that prevent the fertilization of a fertile egg, the contraceptive effect is due to an increase in the viscosity of the mucus located in the cervix, which makes it relatively impassable for sperm.
In addition to contraceptive properties, 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 accompanied by less severe bleeding. The latter circumstance leads to a decrease in the frequency of concomitant iron deficiency anemia. When using COCs, a decrease in the risk of developing ovarian and endometrial cancer has been shown.
Pharmacokinetics
Desogestrel
Absorption
Oral desogestrel is rapidly and completely absorbed and then converted to etonogestrel. Its maximum concentration in blood serum is reached after 1.5 hours. Bioavailability is 62-81%.
Distribution of
Etonogestrel binds to serum albumin and sex hormone binding globulin (SHBG). Only 2-4% of the total concentration of etonogestrel in serum is present as a free steroid, 40-70% specifically bind to SHBG. An increase in the concentration of SHBG caused by ethinyl estradiol has an effect on the distribution between blood proteins, leading to an increase in the SHBG-related fraction and a decrease in the albumin-bound fraction. The apparent volume of distribution of desogestrel is 1.5 l / kg.
Metabolism
Etonogestrel is completely metabolized by known metabolic pathways of steroid hormones. The metabolic excretion rate from serum is 2 ml / min / kg. No interaction of etonogestrel with ethylene estradiol taken simultaneously.
Excretion of
The concentration of etonogestrel in serum decreases in 2 stages. The final stage is characterized by a half-life (T1 / 2) of about 30 hours. Desogestrel and its metabolites are excreted by the kidneys and through the intestines in a ratio of approximately 6: 4.
Equilibrium conditions
The pharmacokinetics of etonogestrel are influenced by SHBG, the concentration of which increases by 3 times under the influence of ethinyl estradiol. With daily use, the concentration of etonogestrel in blood serum increases by 2-3 times, reaching a constant value in the second half of the cycle.
Ethinyl estradiol
Absorption
Ethinyl estradiol after oral administration is rapidly and completely absorbed. Its maximum plasma concentration is achieved within 1-2 hours after administration. Absolute bioavailability (the result of presystemic metabolism) is about 60%.
Distribution of
Ethinyl estradiol non-specifically binds to serum albumin almost completely (98.5%), contributes to an increase in the concentration of SHBG. The apparent volume of distribution of ethinyl estradiol is 5 l / kg.
Metabolism
Ethinyl estradiol undergoes a presystemic metabolism, both in the mucous membrane of the small intestine and in the liver. Ethinyl estradiol is initially metabolized during aromatic hydroxylation to form a variety of hydroxylated and methylated metabolites, which are present both in the free state and in the form of conjugates with glucuronides and sulfates. The metabolic excretion rate of ethinyl estradiol from blood plasma is about 5 ml / min / kg.
Excretion of
The concentration of ethinyl estradiol in serum decreases in 2 stages. The final stage is characterized by T1 / 2 for about 24 hours. Unchanged, the drug is not excreted, ethinyl estradiol metabolites are excreted by the kidneys and through the intestines in a ratio of 4: 6. T1 / 2 of metabolites is about a day.
Equilibrium conditions
Equilibrium concentration is reached after 3-4 days of administration, when the concentration in serum is 30-40% higher than the concentration after taking one dose.
Indications
Contraception.
Contraindications
The drug MercilonВ®, like other combined oral contraceptives, should not be taken in the presence of any of the diseases (conditions) listed below. If any of them occurs while taking the drug, you should immediately stop taking it.
Hypersensitivity to active substances or to any excipient of the drug MercilonВ®.
The presence at present or in the history of venous thrombosis (including deep vein thrombosis of the leg, thromboembolism of the pulmonary artery).
The presence at the moment or in the history of arterial thrombosis (including myocardial infarction, stroke) or precursors of thrombosis (incl. transient ischemic attack, angina pectoris).
Identified predisposition to venous or arterial thrombosis, including resistance to activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant).
Migraine with focal neurological symptoms in history.
Diabetes mellitus with vascular disease.
The presence of severe or multiple risk factors for venous or arterial thrombosis (including arterial hypertension with a blood pressure of 160/100 mmHg or higher).
Pancreatitis (including a history), accompanied by severe hypertriglyceridemia
Severe liver disease (before normalization of liver function indicators), incl. in the anamnesis.
Tumors of the liver (benign and malignant), incl. in the anamnesis.
Hormone-dependent malignant neoplasms of the genitals or mammary glands (including suspects).
Vaginal bleeding of unknown etiology.
Smoking older than 35 years (more than 15 cigarettes per day).
Pregnancy (including implied).
Lactation.
Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Caution:
If any of the conditions / risk factors listed below are present, you should carefully consider the potential risk and expected benefits of using MercilonВ® in each individual case:
Age over 35 years old
Smoking
The presence of thromboembolic diseases in the family history (venous or arterial thrombosis / thromboembolism in siblings or in parents at a relatively young age)
Obesity (body mass index> 30 kg / m)
emia
Migraine
Valvular heart defects
Atrial fibrillation
Prolonged immobilization, extensive surgery, surgery on the lower extremities, severe trauma (with prolonged immobilization and the aforementioned surgical procedures recommended to stop drug use, not later than 4 weeks during elective surgery to surgery and do not resume taking it within 2 weeks after complete remobilization)
Varicose veins, superficial thrombophlebitis (at the moment there is no unequivocal opinion on 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 an acquired predisposition to venous or arterial thrombosis, including resistance to activated protein C, hyperhomocysteinemia, antithrombin III deficiency, protein C deficiency, protein S deficiency, antiphospholipid antibodies (antibodies to cardiolipin, lupus anticoagulant)
Diabetes mellitus
Systemic lupus erythematosus
Hemolytic-uremic syndrome
Chronic inflammatory bowel disease (Crohn’s disease or ulcerative colitis)
Sickle-cell anemia including congenital hyperbilirubinemia (Gilbert syndrome, Dubin-Johnson syndrome, Rotor).
Use during pregnancy and lactation
Use of the drug Mercilon® during pregnancy is contraindicated. In case of pregnancy when using the drug Mercilon®, you should stop taking the drug. It should be noted that extensive epidemiological studies did not reveal an increased risk of giving birth to children with birth defects in women who took COCs before pregnancy, or teratogenic effects in case of inadvertent use of COCs at the beginning of pregnancy.
Mercilon® can affect lactation, since COCs reduce the amount and alter the composition of breast milk. Therefore, the use of the drug Mercilon® is not recommended until the nursing mother has completely stopped breast-feeding.
A small amount of contraceptive steroids and / or their metabolic products may be excreted in milk.
Special instructions
If you have any of the following conditions or risk factors, you should carefully weigh the benefits and possible harm of taking MercilonВ®. This question should be discussed with the patient before starting the drug. In the case of exacerbation of disease, worsening of the condition or the appearance of the first symptoms of the above conditions or risk factors, the patient should immediately consult a doctor. The doctor should decide whether to discontinue the drug.
Vascular disease
An epidemiological study found that there may be a link between COC use 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 COC is associated with an increased risk of venous thromboembolism (VTE), manifested as deep vein thrombosis and / or pulmonary embolism. The risk is higher in the first year of admission than in women taking COCs for more than 1 year.
Some epidemiological studies show that women who took low-dose COCs containing the third generation of gestagens, including desogestrel, have an increased risk of VTE compared to women who took low-dose COCs containing levonorgestrel gestagen.
Very rarely, thrombosis occurs in other blood vessels (for example, in the veins and arteries of the liver, mesentery, kidney, brain or retina). There is no single point of view whether this thrombosis is a consequence of the use of COCs.
An increase in the frequency and intensity of migraines when taking the drug MercilonВ® (which may be a sign of cerebrovascular disorders) may serve as the basis for immediate discontinuation of the drug. Tumors
The most important risk factor for cervical cancer is the persistence of the human papillomavirus (HPV infection). Epidemiological studies have shown an increase in the risk of cervical cancer in women who have been using COCs for a long time, however, there is still uncertainty about the degree of influence of various factors on this data, such as an increase in screening examinations of the cervix and differences in sexual behavior, including the use of barrier methods contraception, or their relationship.
There is evidence that there is a slight increase in relative risk (1, 24) the development of breast cancer in women using COCs. The increased risk gradually decreases within 10 years after the withdrawal of COCs. Since breast cancer in women under 40 years of age is quite rare, the increase in the likelihood of developing breast cancer in women who are currently using COCs or have 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 increased risk of breast cancer can be explained both by the fact that in women taking COCs, the diagnosis of breast cancer is established earlier, and by the biological effects of COCs, or a combination of both of these factors. There is a tendency that in women who have ever taken COCs, breast cancer is clinically less advanced than in women never taking COCs.
Very rarely, with the use of the drug MercilonВ®, there have been cases of the development 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 taking MercilonВ® if the symptoms include acute pain in the upper abdomen, enlarged liver, or signs of intra-abdominal bleeding.
Other diseases
If a woman or her family is diagnosed with hypertriglyceridemia, then the risk of pancreatitis may be increased when taking MercilonВ®.
If a woman using the drug Mercilon® persistent clinically significant arterial hypertension develops, the doctor should discontinue the drug Mercilon® and prescribe treatment for arterial hypertension. In cases where it is possible to achieve normal blood pressure values ​​with antihypertensive therapy, the doctor may consider it possible for the patient to resume taking the drug.
There are reports that jaundice and / or pruritus caused by cholestasis are gallstones, porphyria, systemic lupus erythematosus, hemolytic uremic syndrome, Sydenham chorea (small chorea), pregnant herpes, hearing loss due to otosclerosis, (hereditary) angioedema develop or are aggravated both during pregnancy and when taking the drug MercilonВ®, however, evidence of this in part regarding the administration of the drug MercilonВ® is inconclusive.
Acute or chronic dysfunction of the liver may serve as a basis for discontinuation of the drug MercilonВ® until the indicators of liver function are normalized. Relapse of cholestatic jaundice, observed earlier during pregnancy or when using sex steroid preparations, requires the discontinuation of the drug MercilonВ®.
Although MercilonВ® may affect peripheral tissue tolerance to insulin and glucose, there is no evidence that patients with diabetes need to change the therapeutic regimen for low-dose COCs (containing less than 0.05 mg of ethinyl estradiol). In any case, women with diabetes should be carefully monitored by a doctor while taking MercilonВ®.
There is evidence that there is a connection between COC administration and Crohn's disease and ulcerative colitis.
Sometimes when taking the drug MercilonВ® pigmentation of the skin of the face (chloasma) can be observed, especially if it was previously during pregnancy. Women with a predisposition to chloasma should avoid direct sunlight and ultraviolet radiation from other sources when taking the drug MercilonВ®.
Medical examinations / consultations
Before you start or resume using MercilonВ® in a woman, you need to collect a detailed medical history (including family history) and conduct a thorough examination. It is necessary to measure blood pressure and in the case of the detection of clinically significant signs, it is necessary to conduct a physical examination, guided by contraindications and warnings. You should instruct the woman about the need to carefully read these instructions for use and adhere to the recommendations. The frequency and list of examinations should be based on generally accepted practice and selected individually for each woman (but at least 1 time in 6 months).
A woman should be advised that oral contraceptives do not protect against HIV (AIDS) and other sexually transmitted infections.
Decreased efficacy of
The effectiveness of MercilonВ® may decrease if you skip the drug, have a gastrointestinal upset, or take certain medications concomitantly (see Interaction with Other Medicines).
Irregular spotting
When taking MercilonВ®, especially in the first months of use, irregular spotting or heavy spotting may occur. Therefore, the assessment of irregular bleeding should be carried out only after the end of the adaptation period, lasting three months.
If irregular bleeding persists or appears after previous regular cycles, you should consider the possible non-hormonal causes of the cycle disorder and conduct appropriate studies to exclude malignant neoplasms or pregnancy. These measures may include diagnostic curettage.
Some women may not have menstrual bleeding between meals. If the drug MercilonВ® was taken according to the recommendations given above, the probability that the woman is pregnant is small. Otherwise, or if there are no bleeding twice in a row, the possibility of pregnancy should be excluded and consult a doctor.
Laboratory studies
Oral contraceptives may affect the results of several laboratory studies, including biochemical parameters of liver, thyroid, adrenal and kidney function, plasma transport protein content, for example, corticosteroid-binding globulin and lipid / lipoprotein fractions, carbohydrate metabolism parameters, parameters coagulation and fibrinolysis. Typically, these changes are within normal laboratory values.
Lactose
Each tablet of MercilonВ® 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, must take into account the lactose content in the drug MercilonВ®.
Influence on the ability to drive a car and other mechanisms
No effect of the drug MercilonВ® on the ability to drive a car and work with mechanisms was noted.
Composition
Active ingredients:
Desogestrel 0.150 mg
Ethinyl estradiol 0.020 mg.
Excipients:
Potato starch 8.0 mg
povidone 2.4 mg
stearic acid 0.8 mg
colloidal silicon dioxide 0.8 mg
alpha tocopherol 0.08 mg
lactose monohydrate up to 80 mg.
Dosage and administration of
Tablets should be taken orally in the order indicated on the package, every day at approximately the same time, with a little water if necessary. Take 1 tablet daily for 21 days. Taking tablets from the next package should begin 7 days after the previous one. During these 7 days, menstrual bleeding occurs. Usually it begins 2-3 days after taking the last pill and may not stop until the next package is taken.
How to start taking Mercilon®
- If hormonal contraceptives have not been used within the last month
Tablets should be taken on the 1st day of the menstrual cycle (i.e. on the first day of menstrual bleeding). You can start taking the drug on the 2nd-5th day of the 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 tablets in the first cycle.
- Transition from combined hormonal contraceptives (combined oral contraceptive, vaginal ring or transdermal patch)
It is advisable to start taking Mercilon® the day after taking the last active tablet of the previously used drug (last tablet containing active substances), but no later than the day after the end of the usual break in taking pills or the day after taking the last hormone-free pill. In case of using a vaginal ring or transdermal patch, it is advisable to start taking Mercilon® on the day of their removal, but no later than the day when a new ring was to be introduced or the next patch application was made.
If a woman used 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 Mercilon® on any day of the cycle.
It should be noted that the usual interval in the application of the previous method of contraception should not exceed its recommended duration.
- Switching from drugs containing only gestagen (mini-pill, injection, implant) or from the gestagen-releasing intrauterine system (IUD)
A woman taking a mini-pill can switch to Mercilon® any day using an implant or IUD - on the day of their removal using the drug in the form of injections - per day, when the next injection should be, 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 in the first trimester
A woman can start taking the drug immediately. There is no need to use any additional methods of contraception.
- After giving birth or having a second trimester abortion
For nursing mothers, see the section “Use during Pregnancy and Breastfeeding”.
It is recommended to start taking the drug no earlier than 21-28 days after childbirth or abortion in the second trimester of pregnancy. At the beginning of taking the drug at a later date, it is recommended to use barrier methods of contraception during the first 7 days of taking the drug Mercilon®. Anyway, if a woman after childbirth or abortion prior to taking the drug Mercilon® already had sexual intercourse, pregnancy should be excluded before taking the drug or wait until the first menstruation.
What to do if you miss the next dose of
If the next pill is delayed by less than 12 hours, the reliability of contraception does not decrease. A woman should take a pill as soon as she remembers this, and take the next pill at the usual time.
If taking the next pill is delayed for more than 12 hours, the reliability of contraception may be reduced. In this case, you should be guided by the following two rules:
1. taking tablets should never be interrupted for more than 7 days.
2. for adequate suppression of the hypothalamic-pituitary-ovarian system, tablets must be taken 7 days in a row.
Cycling of the drug involves 3 weeks of use. Accordingly, you can give the following recommendations:
Week 1
A woman should take a missed pill as soon as she remembers this, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. Additionally, the method of barrier contraception should be used over the next 7 days. If a woman has had sexual intercourse in the previous 7 days, the possibility of pregnancy should be considered. The more tablets missed, and the closer the interruption in taking the drug to the time of sexual intercourse, the higher the risk of pregnancy.
Week 2
A woman should take a missed pill, as soon as she remembered it, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. Provided that the woman took the tablets on time for 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 over the next 7 days.
Week 3
Reliability of contraception may be reduced due to a subsequent interruption in taking the drug. This can be avoided by adapting the drug regimen. If you use either of the following two schemes, there is no need to use additional contraceptive measures, provided that a woman took the pill on time for 7 days preceding the first missed dose. Otherwise, it is recommended to use one of the following two schemes and also use additional contraceptive measures over the next 7 days.
1. A woman should take a missed pill as soon as she remembers this, even if it means taking two tablets at the same time. Then you should continue the reception in the usual way. A new package should be started as soon as the current package ends, i.e., there should be no break between packages. The likelihood of “withdrawal bleeding” before the end of the second package is small, but some may have spotting or heavy spotting while taking the drug.
2. A woman can be advised 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 pills, and then start a new package.
If you skip taking the drug and the subsequent absence of “withdrawal bleeding” in the next break in taking the pills, you should consider the possibility of pregnancy.
Recommendations for gastrointestinal upsets
If severe gastrointestinal upsets are present, absorption may not be complete 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. If a woman does not want to change her usual regimen, she needs to take additional (s) tablet (s) from another package (the number of additional tablets is determined by a specialist obstetrician-gynecologist at a face-to-face consultation).
How to change the period of onset of menstrual bleeding
In order to delay menstrual bleeding, you should continue to take tablets from another package of the drug Mercilon® without the usual interruption. You can delay menstrual bleeding for any period until the end of the tablets from the second package. During this period, a woman may experience spotting or heavy spotting. Taking the drug according to the usual schedule should be resumed after a 7-day interval in admission.
In order to shift the day of the onset of menstrual bleeding to another day, You can shorten your regular pill break by as many days as necessary. The shorter the break, the higher the risk of no menstrual bleeding during the break and the occurrence of heavy or spotting spotting while taking the tablets from the second package.
Side effects
Thrombosis or thromboembolism (including myocardial infarction, stroke, deep vein thrombosis, pulmonary embolism), hepatic, mesenteric, renal arteries and veins, retinal arteries.
Increased blood pressure.
Hormone-dependent tumors (liver tumors, breast cancer).
Chloasma (especially in the case of a history of chloasma during pregnancy).
Acyclic spotting is more common in the first months of administration.
Allergic reactions.
Drug Interactions
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: interactions can occur with drugs that induce microsomal enzymes, which can lead to increased clearance of sex hormones (e.g. phenytoin, barbiturates, primidone, carbamazepine, rifampicin, rifabutin, and possibly also oxcarbazepine, topiramate, felvirfam, felvirfam preparations containing St. John's wort perforated). 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 break in taking the drug.
A contraceptive effect has also been reported while taking Mercilon® with antibiotics such as ampicillin and tetracyclines. The mechanism of this influence is not clear.
Women who take any of the above drugs should temporarily use the additional method of barrier contraception or choose another method of contraception. With the simultaneous use of inducers of microsomal enzymes, the barrier method of contraception should be used throughout the course of treatment and within 28 days after cessation of treatment. In the case of long-term treatment with the use of inducers of microsomal enzymes, another method of contraception must be used. Women who use antibiotics (excluding rifampicin and griseofulvin, which possess the properties of inducers of microsomal enzymes) should use the barrier method of contraception throughout the course of treatment and within 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 tablets in the COC package, then the next package of the drug must be started without the usual interval in admission.
Oral contraceptives may affect the metabolism of other medicines.
Accordingly, they can change their concentration in plasma and tissues: increase (for example, cyclosporine) or decrease (lamotrigine).
When treating with other drugs, to determine possible interactions, you should read the instructions for medical use of these drugs.
Overdose
No serious complications were observed with an overdose of Mersilon®. Symptoms that can occur with overdose: nausea, vomiting, young girls - bloody discharge from the vagina. There are no antidotes and further treatment should be symptomatic.
Storage Conditions
Store at 2 to 30 ° C in a dry, dark place.
Keep out of the reach and sight of children.
Shelf life
3 years.
Deystvuyushtee substance
Desogestrel, Эtinilэstradiol
Terms and conditions vacation vacation srdlk holiday recipe holiday vacation prescription
dosage form
tablets
At
value Prescription
For women, Adults as prescribed by a doctor, For women of childbearing age
N.V. Organon, the Netherlands
Mercilon tablets 21 pcs. (tar, Ethinyl estradiol) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Mercilon tablets 21 pcs. - Sale. PayPal accept. Free shipping florida. Fast international shipping.
Submit your review to Earn 10 Reward Points click here to login
Write Your Own Review