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Active ingredients
Desogestrel + Ethinyl Estradiol
Release form
Pills
Composition
In 1 tablet: ethinyl estradiol 30 mcg; desogestrel 150 mcg. Auxiliary substances: α-tocopherol, magnesium stearate, colloidal silicon dioxide, stearic acid, povidone, potato starch, lactose monohydrate.
Pharmacological effect
Monophasic oral contraceptive. The main contraceptive effect is to inhibit the synthesis of gonadotropins and suppress ovulation. In addition, by increasing the viscosity of the cervical mucus, the movement of spermatozoa through the cervical canal slows down, and the change in the state of the endometrium prevents implantation of a fertilized egg. Ethinyl estradiol is a synthetic analogue of endogenous estradiol. Regulon has a beneficial effect on lipid metabolism: it increases the concentration of HDL in the plasma blood, without affecting the content of LDL. When taking the drug, menstrual blood loss is significantly reduced (with initial menorrhagia), the menstrual cycle is normalized, there is a beneficial effect on the skin, especially in the presence of acne vulgaris.
Pharmacokinetics
Desogestrel. Absorption: Desogestrel is rapidly and almost completely absorbed from the gastrointestinal tract and immediately metabolized to 3-keto-desogestrel, which is the biologically active metabolite of deogestrel. Cmax is reached in 1.5 hours and is 2 ng / ml. Bioavailability - 62-81%. Distribution: 3-keto-desogestrel binds to plasma proteins, mainly albumin and sex hormone-binding globulin (SHBG). Vd is 1.5 l / kg. Css is set to the second half of the menstrual cycle. The level of 3-keto-desogestrel increases by 2-3 times. Metabolism: In addition to 3-keto-desogestrel (which is formed in the liver and in the intestinal wall), other metabolites are formed: 3α-OH-desogestrel, 3β-OH-desogestrel, 3α-OH -5α-H-desogestrel (metabolites of the first phase). These metabolites do not possess pharmacological activity and partially, by conjugation (the second phase of metabolism), are converted into polar metabolites, sulfates and glucuronates.Plasma clearance is about 2 ml / min / kg body weight. Output: T1 / 2 3-keto-desogestrel is 30 hours. Metabolites are excreted with urine and with feces (4: 6 ratio). Ethinyl estradiol. Absorption: Ethinyl estradiol is fast and completely absorbed from the digestive tract. Cmax is achieved within 1-2 hours after taking the drug and is 80 pg / ml. The bioavailability of the drug due to presystemic conjugation and the effect of the first passage through the liver is about 60%. Distribution: Ethinyl estradiol is completely associated with plasma proteins, mainly albumin. Vd is 5 l / kg. Css is set to 3-4 days of administration, with serum levels of ethinyl estradiol 30-40% higher than after a single dose. Metabolism: Presystemic conjugation of ethinyl estradiol is significant. Passing through the intestinal wall (first phase of metabolism), it undergoes conjugation in the liver (second phase of metabolism). Ethinyl estradiol and its conjugates of the first phase of metabolism (sulfates and glucuronides) are released into the bile and enter into the enterohepatic circulation. The plasma clearance is about 5 ml / min / kg of body weight. Excretion: Ethinyl estradiol T1 / 2 averages about 24 hours. About 40% is excreted in the urine and about 60% in the feces.
Indications
Contraception.
Contraindications
The presence of severe and / or multiple risk factors for venous or arterial thrombosis (including severe or moderate arterial hypertension with BP ≥ 160/100 mm Hg) - presence or indication in history of thrombosis precursors (in . transient ischemic attack, angina) - migraine with focal neurological symptoms, including in history - venous or arterial thrombosis / thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower leg, pulmonary embolism) now or in history; - the presence of venous thromboembolism in anamnesis; ); - pancreatitis (including history), accompanied by severe hypertriglyceridemia; - dyslipidemia; - severe liver disease, cholestatic jaundice (including during pregnancy), hepatitis, including in history (before normalization of functional and laboratory parameters and within 3 months after their normalization); jaundice when taking GCS; cholelithiasis now or in history; Gilbert syndrome, Dubin-Johnson syndrome, Rotor syndrome; liver cancer (includingin history); - severe itching, otosclerosis or its progression during a previous pregnancy or taking GCS; - hormone-dependent malignant neoplasms of the genitals and mammary glands (including those suspected of them); - vaginal bleeding of unknown etiology; - smoking at age over 35 years old (more than 15 cigarettes per day); - pregnancy or suspicion of it; - lactation period; - hypersensitivity to the drug components.
Precautionary measures
The drug should be prescribed with caution in conditions that increase the risk of developing venous or arterial thrombosis / thromboembolism: age over 35, smoking, family history, obesity (body mass index more than 30 kg / m2), dyslipoproteinemia, arterial hypertension, migraine, epilepsy, valve heart defects, atrial fibrillation, prolonged immobilization, extensive surgery, surgery on the lower limbs, severe trauma, varicose veins and superficial thrombophlebitis, postpartum the new period, the presence of severe depression (including history), changes in biochemical parameters (resistance of activated protein C, hyperhomocysteinemia, deficiency of antithrombin III, deficiency of protein C or S, antiphospholipid antibodies, including antibodies to cardiolipin, including lupus anticoagulant), diabetes mellitus, not complicated by vascular disorders, SLE, Crohn's disease, ulcerative colitis, sickle cell anemia, hypertriglyceridemia (including family history), acute and chronic liver disease.
Use during pregnancy and lactation
The use of the drug during pregnancy and during breastfeeding is contraindicated. During breastfeeding, it is necessary to resolve the issue of either discontinuing the drug or stopping breastfeeding.
Dosage and administration
The drug is prescribed inside. Taking pills start from the 1st day of the menstrual cycle. Assign 1 tab. / Day for 21 days, if possible at the same time of day. After taking the last tablet out of the package, a 7-day break is taken during which menstrual-like bleeding occurs as a result of discontinuation of the drug. The next day after a 7-day break (4 weeks after taking the first pill, on the same day of the week), taking the drug from the next package, which also contains 21 pills, is resumed, even if the bleeding has not stopped. This pill regimen is followed as long as there is a need for contraception.If the rules of administration are observed, the contraceptive effect is maintained for the duration of the 7-day break. The first dose of the drug: The first pill should be taken from the first day of the menstrual cycle. In this case, you do not need to use additional methods of contraception. Taking the pills can be started from 2-5 days of menstruation, but in this case, in the first cycle of using the drug, additional methods of contraception should be used in the first 7 days of taking the pills. If more than 5 days have passed after the start of menstruation, you should postpone the start of taking the drug until the next menstruation . Taking the drug after childbirth: Non-breastfeeding women can start taking the pills no earlier than 21 days after delivery, after consulting a doctor. In this case, there is no need to use other methods of contraception. If after childbirth there was already sexual contact, then pills should be postponed until the first menstruation. If you decide to take the drug later than 21 days after delivery, then in the first 7 days you need to use additional methods of contraception. Taking the drug after an abortion: After an abortion, in the absence of contraindications, you should start taking the pills from the first day after the operation, and In this case, there is no need to use additional methods of contraception. Transfer from another oral contraceptive: When switching from another oral medication (21 or 28 days): the first tablet of Regulon is recommended to take s the day after the completion of a 28-day drug packaging. After completing the 21-day course, you need to take a normal 7-day break and then begin to take Regulon. There is no need to use additional methods of contraception. Transition to Regulon after using oral hormonal preparations containing only progestogen (mini-drank) The first tablet Regulon should be taken on the 1st day of the cycle. There is no need to use additional methods of contraception. If menstruation does not occur while taking a mini-drink, then you can start taking Regulon on any day of the cycle, but in this case, additional methods of contraception should be used in the first 7 days (using a cervical cap with spermicidal gel, condom, or abstaining from sexual intercourse).The use of the calendar method in these cases is not recommended. Postponing the menstrual cycle: If there is a need to postpone menstruation, you should continue taking the pills from the new package, without a 7-day break, in the usual way. With the postponement of menstruation, breakthrough or spot bleeding may occur, but this does not reduce the contraceptive effect of the drug. Regulon's regular intake can be restored after the usual 7-day break. Missed pills: If a woman forgot to take a pill in a timely manner, and no more than 12 hours passed after skipping, you need to take a forgotten pill, and then continue taking it at your usual time. If more than 12 hours have passed between taking the pills, this is considered to be skipping the pill, contraceptive reliability in this cycle is not guaranteed and the use of additional contraceptive methods is recommended. If you skip one pill in the first or second week of the cycle, you need to take 2 tabs. the next day and then continue regular intake, using additional methods of contraception until the end of the cycle. When you miss a pill in the third week of the cycle, you must take a forgotten pill, continue regular intake and not take a 7-day break. It is important to remember that due to the minimal dose of estrogen, the risk of ovulation and / or bleeding increases when you skip a pill and therefore additional contraceptive methods are recommended. Vomiting / diarrhea: If vomiting or diarrhea occurs after taking the drug, then the absorption of the drug may be defective. If the symptoms stopped within 12 hours, then you need to take another pill extra. After that, you should continue taking the pills in the usual way. If vomiting or diarrhea continues for more than 12 hours, it is necessary to use additional methods of contraception during vomiting or diarrhea and for the next 7 days.
Side effects
Side effects requiring discontinuation of the drug: From the side of the cardiovascular system: arterial hypertension; rarely, arterial and venous thromboembolism (including myocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary thromboembolism); very rarely - arterial or venous thromboembolism of the liver, mesenteric, renal,retinal arteries and veins. From the sensory organs: hearing loss due to otosclerosis. Others: hemolytic-uremic syndrome, porphyria; rarely, exacerbation of reactive systemic lupus erythematosus; very rarely - Sydenham chorea (passing after discontinuation of the drug). Other side effects that are more common, but less severe. The feasibility of continuing to use the drug is decided individually after consultation with the doctor, based on the benefit / risk ratio. On the part of the reproductive system: acyclic bleeding / bleeding from the vagina, amenorrhea after discontinuation of the drug, changes in the state of vaginal mucus, development of inflammatory processes of the vagina, candidiasis, stress, pain, breast augmentation, galactorrhea. On the digestive system: nausea, vomiting, Crohn's disease, ulcerative colitis, the occurrence or exacerbation of jaundice and / or teeth a, associated with cholestasis, cholelithiasis. Dermatological reactions: erythema nodosum, exudative erythema, rash, chloasma. On the side of the central nervous system: headache, migraine, mood lability, depression. On the part of the organ of vision: increased sensitivity of the cornea (when wearing contact lenses). On the part of metabolism: fluid retention in the body, a change (increase) in body weight, a decrease in tolerance to carbohydrates. Other: allergic reactions.
Overdose
Symptoms: nausea, vomiting, in girls - bloody discharge from the vagina. Treatment: in the first 2-3 hours after taking the drug in a high dose, it is recommended to carry out a gastric lavage. There is no specific antidote, the treatment is symptomatic.
Interaction with other drugs
Drugs that induce hepatic enzymes such as hydantoin, barbiturates, primidone, carbamazepine, rifampicin, oxcarbazepine, topiramate, felbamate, griseofulvin, Hypericum ordinary formulations, reduce the effectiveness of oral contraceptives and increase the risk of breakthrough bleeding. The maximum level of induction is usually achieved not earlier than 2-3 weeks, but can last up to 4 weeks after discontinuation of the drug. Ampicillin and tetracycline reduce the effectiveness of Regulon (the interaction mechanism has not been established). If necessary, joint use is recommended to use an additional barrier method of contraception during the entire course of treatment and for 7 days (for rifampicin - for 28 days) after discontinuation of the drug. Oral contraceptives can reduce the tolerance to carbohydrates,increase the need for insulin or oral antidiabetic drugs.
special instructions
Before using the drug, it is necessary to conduct general medical (detailed family and personal history, blood pressure measurement, laboratory tests) and gynecological examination (including examination of the mammary glands, pelvic organs, cytological analysis of cervical smear). A similar examination in the period of taking the drug is carried out regularly, every 6 months. The drug is a reliable contraceptive: Pearl index (an indicator of the number of pregnancies occurring during the use of the contraceptive method in 100 women within 1 year) with proper use is about 0.05. In each case The prescription of hormonal contraceptives individually assesses the benefits or possible negative effects of their use. This issue should be discussed with the patient, who after receiving the necessary information will make the final decision on the preference for hormonal or any other method of contraception. The health status of the woman should be carefully monitored. If any of the following conditions / diseases appear or worsen while taking the drug, you should stop taking the drug and switch to another, non-hormonal method of contraception: - hemostasis system diseases; - conditions / diseases predisposing to the development of cardiovascular, renal failure; epilepsy; - migraine; - risk of developing an estrogen-dependent tumor or estrogen-dependent gynecological diseases; - diabetes mellitus not complicated by vascular disorders; - severe depression (e if depression is associated with breach of the tryptophan metabolism, with the aim of correction can be applied vitamin B6), - sickle-cell anemia, as in some cases (eg, infections, hypoxia), estrogen-containing drugs in this pathology can provoke thromboembolism; - appearance of abnormalities in laboratory tests assessing liver function. Thromboembolic diseases: Epidemiological studies have shown that there is a link between oral hormonal contraceptive use and an increased risk of development arterial and venous thromboembolic diseases (includingmyocardial infarction, stroke, deep vein thrombosis of the lower extremities, pulmonary thromboembolism). Proved an increased risk of venous thromboembolic diseases, but it is significantly less than during pregnancy (60 cases per 100 thousand pregnancies). Some researchers suggest that the likelihood of venous thromboembolic diseases is greater when using drugs containing desogestrel and gestoden (third-generation drugs) than when using drugs containing levonorgestrel (second-generation drugs). The frequency of spontaneous emergence of new cases of venous thromboembolic disease in healthy non-pregnant women who do not take oral contraceptives, about 5 cases per 100 thousand women per year. With the use of second-generation drugs - 15 cases per 100 thousand women per year, and with the use of third-generation drugs - 25 cases per 100 thousand women per year. When using oral contraceptive drugs, arterial or venous thromboembolism of the liver, mesenteric, renal vessels or retinal vessels. The risk of arterial or venous thromboembolic diseases increases: - with age; - when smoking (intensive smoking and over 35 years of age are risk factors); - pr and a family history of thromboembolic disease (for example, a parent, brother, or sister). If you suspect a genetic predisposition, you must consult a specialist before using the drug; - for obesity (body mass index more than 30 kg / m2); - for dyslipoproteinemia, - for hypertension, - for valvular heart disease complicated by hemodynamic disorders, - for fibrillation atria; - in case of diabetes mellitus complicated by vascular lesions; - during prolonged immobilization, after a large surgery, after surgery on the lower limbs, after a severe injury. In these cases, it is supposed to temporarily stop using the drug (no later than 4 weeks before surgery, and resume - no earlier than 2 weeks after remobilization). Women after childbirth increase the risk of venous thromboembolic diseases. take into account that diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, ulcerative colitis, sickle cell anemia,increase the risk of venous thromboembolic diseases. It should be noted that resistance to activated protein C, hyperhomocysteinemia, deficiency of proteins C and S, deficiency of antithrombin III, the presence of antiphospholipid antibodies, increase the risk of developing arterial or venous thromboembolic diseases. It should be borne in mind that the targeted treatment of this condition reduces the risk of thromboembolism. Symptoms of thromboembolism are: - sudden pain in the chest that radiates to the left hand; - sudden shortness of breath; - any unusually severe headache that lasts a long time or appears for the first time, especially when combined with sudden full or partial loss of vision or diplopia, aphasia, dizziness , collapse, focal epilepsy, weakness or severe numbness of the half of the body, motor impairment, severe unilateral pain in the gastrocnemius muscle, acute abdomen. Tumor diseases: In some studies niyah reported quickening of cervical cancer in women who took a long time, hormonal contraceptives, but research results are contradictory. Sexual behavior, infection with human papillomavirus and other factors play a significant role in the development of cervical cancer. A meta-analysis of 54 epidemiological studies has shown that there is a relative increase in the risk of breast cancer among women taking oral hormonal contraceptives, but the higher detection of breast cancer glands could be associated with more regular medical examinations. Breast cancer is rare among women younger than 40 years old, regardless of whether they take hormonal contraceptives or not, and increases with age. Taking pills can be considered as one of many risk factors. However, a woman should be made aware of the possibility of developing breast cancer risk, based on an evaluation of the benefit-risk ratio (protection against ovarian cancer and endometrial cancer). There are few reports about the development of a benign or malignant liver tumor in women who take hormone for a long time. contraceptives.This should be borne in mind when the differential diagnostic assessment of abdominal pain, which may be associated with an increase in liver size or intraperitoneal bleeding. Chloasma: Chloasma may develop in women with a history of pregnancy. Those women who are at risk of chloasma should avoid contact with sunlight or ultraviolet radiation while taking Regulone. Effectiveness Effectiveness of the drug may decrease in the following cases: missed pills, vomiting and diarrhea, the simultaneous use of other drugs that reduce the effectiveness of the pill. the patient simultaneously takes another drug that can reduce the effectiveness of birth control pills, additional contraceptive methods should be used ii.Effektivnost drug may be reduced if, after several months of their applications appear irregular, spotting or breakthrough bleeding, in such cases it is advisable to continue taking the pills before their next closure in the package. If at the end of the second cycle the menstrual-like bleeding does not start or the acyclic bleeding does not stop, stop taking the pills and resume it only after pregnancy is excluded. Changes in laboratory parameters: Under oral contraceptive pills - due to the estrogen component - some laboratory parameters may change ( functional parameters of the liver, kidneys, adrenal glands, thyroid gland, hemostasis indicators, levels of lipoproteins and transport of teins). Additional information: After suffering acute viral hepatitis, the drug should be taken after normalization of liver function (not earlier than after 6 months). In diarrhea or intestinal disorders, vomiting contraceptive effect may decrease. Without stopping the drug, it is necessary to use additional non-hormonal methods of contraception. Smoking women have an increased risk of developing vascular diseases with serious consequences (myocardial infarction, stroke). The risk depends on age (especially in women over 35) and on the number of cigarettes smoked. A woman should be warnedthat the drug does not protect against HIV infection (AIDS) and other sexually transmitted diseases. Influence on the ability to drive vehicles and control mechanisms The drug does not affect the ability to drive and work with mechanisms.