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Active ingredients
Dienogest + Ethinyl Estradiol
Release form
Dragee
Composition
In 1 tablet; ethinyl estradiol 30 mcg; dienogest 2 mg. Adjuvants: lactose monohydrate - 27.97 mg, potato starch - 15 mg, gelatin - 1.5 mg, talc - 1.5 mg, magnesium stearate - 0.5 mg.
Pharmacological effect
Low-dose monophasic oral combined estrogen-progestin contraceptive drug. Zhanin's contraceptive effect is accomplished through complementary mechanisms, the most important of which include suppression of ovulation and changes in the viscosity of cervical mucus, as a result of which it becomes impermeable to spermatozoa. the number of pregnancies in 100 women taking a contraceptive during the year) is less than 1. When skipping a pill or incorrect application Pearl index can vozrastat.Gestagenny component Jeanine - dienogest - possesses antiandrogenic activity, which is confirmed by the results of clinical studies. In addition, dienogest improves blood lipid profile (increases the number of high-density lipoproteins). In women taking combined oral contraceptives, the menstrual cycle becomes more regular, painful menstruation is less common, the intensity and duration of bleeding decreases, resulting in a reduced risk of iron deficiency anemia. In addition, there is evidence of a reduction in the risk of endometrial cancer and ovarian cancer.
Pharmacokinetics
Dienogest AbsorptionAfter oral administration, dienogest is rapidly and completely absorbed from the gastrointestinal tract. Cmax is reached in 2.5 hours and is 51 ng / ml. Bioavailability is approximately 96%. Distribution: Dienogest binds to serum albumin and does not bind to sex steroids (GLPS) and corticoid-binding globulin (GLA). In free form is about 10% of the total serum concentration; about 90% are non-specifically associated with serum albumin. Induction by ethinylestradiol of the synthesis of SHGS does not affect the binding of dienogest to serum protein. Dynegest's pharmacokinetics are not affected by the level of SHGS in serum.As a result of daily intake of the drug, the level of dienogest in serum increases about 1.5 times. MetabolismDenogest is almost completely metabolized. Serum clearance after a single dose is approximately 3.6 l / h. Excretion of T1 / 2 is approximately 8.5-10.8 h. A small part of the dienogest is excreted by the kidneys in an unchanged state. Metabolites are excreted in the urine and bile in a ratio of about 3: 1 with a T1 / 2 of 14.4 hours. Ethinyl estradiol Absorption After ingestion, ethinyl estradiol is rapidly and completely absorbed. Cmax in serum is reached in 1.5-4 hours and is 67 pg / ml. During suction and first passage through the liver, ethinyl estradiol is metabolized, resulting in its bioavailability when administered orally averages about 44%. The distribution of ethynyl estradiol is almost completely (approximately 98%), although not specifically, bound to albumin. Ethinyl estradiol induces the synthesis of SHBG. The apparent Vd of ethinyl estradiol is 2.8–8.6 l / kg. Css is achieved during the second half of the treatment cycle. Metabolism Ethinyl estradiol undergoes systemic conjugation, both in the mucous membrane of the small intestine and in the liver. The main metabolic pathway is aromatic hydroxylation. The rate of clearance from blood plasma is 2.3-7 ml / min / kg. ExcretionThe reduction of the concentration of ethinyl estradiol in the blood serum is biphasic; The first phase is characterized by T1 / 2 of the first phase - about 1 hour, T1 / 2 of the second phase - 10-20 hours. It is not excreted from the body in unchanged form. Ethinyl estradiol metabolites are excreted in urine and bile in a ratio of 4: 6 with a T1 / 2 of about 24 hours.
Indications
Contraception.
Contraindications
Janine; Should not be applied in the presence of any of the conditions / diseases listed below. If any of these conditions develop for the first time against the background of its administration, the drug should be immediately canceled. - The presence of thrombosis (venous and arterial) now or in history (for example, deep vein thrombosis, pulmonary thromboembolism, myocardial infarction, cerebrovascular disorders ); - Present or past history of conditions preceding thrombosis (eg, transient ischemic attacks, angina); - Diabetes mellitus with vascular complications; - Present or presenting a history of migraine with och beef neurological symptoms - the presence of severe or multiple risk factors for venous or arterial thrombosis (includingcomplicated valvular lesions of the heart, atrial fibrillation, vascular diseases of the brain or coronary arteries of the heart, uncontrolled arterial hypertension, serious surgical intervention with prolonged immobilization, smoking after the age of 35); liver failure and severe liver disease (before normalization of liver tests) - present or past pancreatitis with severe hypertriglyceridemia; present or past benign or evil quality liver tumors; - identified hormone-dependent malignant diseases of the genital organs or mammary glands or suspicion of them; - vaginal bleeding of unknown origin; - pregnancy or suspicion of it; - breastfeeding period; - hypersensitivity to the components of the drug.
Precautionary measures
The potential risk and expected benefit of using combined oral contraceptives in each individual case should be carefully weighed with the following diseases / conditions and risk factors: - risk factors for thrombosis and thromboembolism (smoking, obesity, dyslipoproteinemia, hypertension, migraine, valvular heart disease, long-term immobilization, serious surgical intervention, extensive trauma, hereditary predisposition to thrombosis / thrombosis, myocardial infarction or impaired m other diseases in which peripheral circulation disorders may occur (diabetes, systemic lupus erythematosus, hemolytic uremic syndrome, Crohn's disease, UC, sickle cell anemia, superficial phlebitis veins); - hereditary angioedema; - hypertriglyceridemia; - liver disease; - diseases that first arose or worsened during pregnancy or against the background of previous intake of sex hormone new (e.g., jaundice, cholestasis, gallbladder disease, otosclerosis with hearing impairment, porphyria, herpes gestationis, Sydenham chorea); - puerperal period.Pri occurrence of liver function may require temporary cancellation Jeanine to normalization of laboratory parameters.With the development of cholestatic jaundice or cholestatic pruritus (first appeared during pregnancy or previous intake of sex hormones) Jeanine; should cancel.
Use during pregnancy and lactation
Janine; It is not prescribed during pregnancy and during breastfeeding. If pregnancy is detected while taking Zanin, the drug should be immediately canceled. However, extensive epidemiological studies have not revealed an increased risk of developmental defects in children born to women who received sex hormones before pregnancy, or teratogenic effects, when sex hormones were taken by negligence in the early stages of pregnancy. therefore, their use is contraindicated during lactation. A small amount of sex steroids and / or their metabolites can be excreted in milk.
Dosage and administration
Drops should be taken orally in the order indicated on the packaging, every day at about the same time, with a little water. Jeanine; should take 1 tablet / day continuously for 21 days. Reception of each next package begins after a 7-day break, during which withdrawal bleeding is observed (menstrual-like bleeding). It usually starts on the 2-3rd day after taking the last dragee and may not end before the start of taking a new package. Start of taking Zanin If you have not taken any hormonal contraceptives in the previous month, Zanin starts on the 1st day of the menstrual cycle (t. e. on the 1st day of menstrual bleeding). It is allowed to start taking on the 2-5th day of the menstrual cycle, but in this case it is recommended to use a barrier method of contraception during the first 7 days of taking pills from the first package. the next day after taking the last active dragee from the previous package, but in no case, no later than the next day after the usual 7-day break in the intake (for preparations containing 21 pills) or le receipt of the last inactive dragees (for formulations containing 28 pellets in the package).When switching from the vaginal ring or transdermal patch, it is preferable to start taking Zanin on the day the ring or patch is removed, but no later than the day when a new patch is to be inserted or a new patch is pasted. When switching from contraceptives containing only gestagens (mini-pili, injectable forms) , implant) or from a progestogen-releasing intrauterine contraceptive (Mirena), a woman can switch from taking mini-drank to Jeanine; on any day (without a break), from the implant or intrauterine contraceptive with the progestogen - on the day of its removal, from the injection contraceptive - on the day when the next injection should be made. In all cases, it is necessary to use an additional barrier method of contraception during the first 7 days of taking pills. After an abortion in the first trimester of pregnancy, a woman can start taking the drug immediately. In this case, the woman does not need additional methods of contraception. After childbirth or abortion in the second trimester of pregnancy, it is recommended to start taking the drug on the 21-28th day after delivery or abortion in the second trimester of pregnancy. If reception is started later, it is necessary to use an additional barrier method of contraception during the first 7 days of taking pills. However, if a woman has already lived sexually, before pregnancy Zanin is started, pregnancy should be excluded or it is necessary to wait for the first menstruation. Reception of missed pills. If a delay in taking pills is less than 12 hours, the contraceptive protection is not reduced. The woman should take the missed dragee as soon as possible, the following dragee is taken at the usual time. If the delay in taking the dragee is more than 12 hours, the contraceptive protection can be reduced. At the same time, the following two basic rules can be used: - the drug should never be interrupted more than than 7 days; - to achieve adequate suppression of the hypothalamic-pituitary-ovarian system, 7 days of continuous ingestion of pills are required. Accordingly, if the delay in taking active pills was more than 12 hours (int Since the last active dragee has been taken more than 36 hours, the following can be recommended: The first week of taking the drug. It is necessary to take the last missed pill as soon as possible as soon as the woman remembers it (even if you need to take two pills at the same time). The following pills are taken at the usual time. Additionally, a barrier method of contraception (for example, a condom) should be used within the next 7 days.If sexual intercourse took place within a week before skipping dragees, it is necessary to take into account the probability of pregnancy. The more pills are missed, and the closer they are to a break in taking active substances, the greater the likelihood of pregnancy. The second week of taking the drug. You need to take the last missed pill as soon as possible as soon as the woman remembers this (even if you need to take two dragee at the same time). The following pills are taken at the usual time. Provided that the woman took the pills correctly for 7 days preceding the first missed pills, there is no need to use additional contraceptive measures. Otherwise, as well as skipping two or more pills, it is necessary to additionally use barrier methods of contraception (for example, a condom) for 7 days. The third week of taking the drug. The risk of pregnancy increases due to the upcoming break in taking pills. A woman should strictly adhere to one of the following two options. Moreover, if during the 7 days preceding the first missed pills, all the pills were taken correctly, there is no need to use additional contraceptive methods. You need to take the last missed dragee as soon as possible, as soon as the woman remembers this (even if you need to take two dragees at the same time). The next dragee is taken at the usual time until the dragee from the current package is finished. The next package should start immediately without a break. Withdrawal bleeding is unlikely until the second package is completed, but there may be spotting and breakthrough bleeding while taking pills. A woman can also interrupt the taking of pills from the current package. Then she should take a break for 7 days, including the day of skipping pills, and then start taking new packaging. If a woman misses taking pills, and then during a break in reception she has no withdrawal bleeding, pregnancy should be excluded. Recommendations in case of vomiting and diarrhea. If a woman has vomiting or diarrhea within up to 4 hours after taking active dragees, absorption may not be complete and additional contraceptive measures should be taken. In these cases, you should be guided by the recommendations when skipping pills. Changing the day of the beginning of the menstrual cycle. To delay the onset of menstruation, a woman should continue taking pills from the new Zhanin package immediately after taking all the pills from the previous one, without interruption in reception.Drops from this new package can be taken as long as the woman wants (until the package ends). While taking the drug from the second package, a woman may have spotting or breakthrough uterine bleeding. To resume taking Zhanin from a new package should be after the usual 7-day break. In order to postpone the start of menstruation to another day of the week, a woman should shorten the next break in taking pills for as many days as she wants. The shorter the interval, the higher the risk that she will not have withdrawal bleeding and in the future there will be spotting and breakthrough bleeding while taking the second package (just as she would like to delay the onset of menstruation). Additional information for Special categories of patients. Children and adolescents drug Jeanine; shown only after menarche. After menopause, the drug Jeanine; not shown. The drug Jeanine; contraindicated in women with severe liver disease, as long as the indicators of liver function do not normalize. The drug Jeanine; not specifically studied in patients with impaired renal function. The available data do not imply a change in treatment in these patients.
Side effects
When taking combined oral contraceptives, irregular bleeding (spotting or breakthrough bleeding) may occur, especially during the first months of use. Against the background of the drug Jeanine; women also had other undesirable effects indicated in the table below. Within each group, allocated depending on the frequency of the undesirable effect, unwanted effects are presented in order of decreasing severity. The frequency of adverse reactions: often (≥1 / 100 and <1/10), infrequently (≥1 / 1000 and <1/100 ), rarely (≥1 / 10 000 and <1/1000). For additional adverse reactions identified only in the process of post-marketing observations and for which it is not possible to conduct a frequency assessment, it is indicated that the frequency is unknown. Often (≥1 / 100 and <1/10) Infrequently (≥1 / 1000 and <1/100) Rarely (≥1 / 10,000 and <1/1000) Frequently not knownInfections and infectionsVaginitis / vulvovaginitisVaginal candidiasis or other vulvovaginal infections Salpingoophoritis (adnexitis) Urinary tract infections Cystitis Mastitis Calvitis fungal infections Candidosis ерп рон рон рон ерп ерп ерп рон рон рон н н ин н н н н н н н н н н н н н н н н н ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ек ii puteyVirusnye upper respiratory infections are benign,and unspecified malignant tumors (including cysts and polyps) Fibroids matkiLipoma breast Blood and lymphatic sistemaAnemiya Endocrine sistemaVirilizatsiya MetabolizmUsilenie appetite Anorexia Psychiatric narusheniyaSnizhenie DepressiyaPsihicheskie narusheniyaBessonnitsaNarusheniya snaAgressiya mood changes nastroeniyaSnizhenie libidoPovyshenie libidoNervnaya sistemaGolovnaya GolovokruzhenieMigren Ischemic pain insultTserebrovaskulyarnye rasstroystvaDistoniya Agencies mucosa chuvstvSuhost glazRazdrazh ix mucosa glazOstsillopsiyaVnezapnaya loss in sluhaShum ushahGolovokruzhenieNarushenie sluhaNeperenosimost contact lens (the unpleasant feeling of wearing them) Cardiovascular sistemaArterialnaya gipertenziyaArterialnaya hypotension Cardiovascular rasstroystvaTahikardiya including increased ChSSTromboz / pulmonary circulatory arteriiTromboflebitDiastolicheskaya gipertenziyaOrtostaticheskaya distoniyaPrilivyVarikoznoe extension venPatologiya venBol in venDyhatelnaya sistemaBronhialnaya ast maGiperventilyatsiya Digestive sistemaBoli abdominal pain, including pain in the upper and lower abdominal discomfort / vzdutieToshnotaRvotaDiareya GastritEnteritDispepsiya Dermatological reaktsiiAkneAlopetsiyaSyp, including macular sypZud including generalized pruritus Atopic dermatitis / neyrodermitEkzemaPsoriazGipergidrozHloazmaNarushenie pigmentation / giperpigmentatsiyaSeboreyaPerhotGirsutizmPatologicheskie change kozhiApelsinovaya korkaSosudistye zvezdochkiMnogoformnaya eritemaAllergicheskie reaktsiiProyavleniya allergic x reactions, allergies vaginal bleeding and metrorrhagia Increase in breast size, swelling and a feeling of swelling in the mammary glands lactic zhelezyDismenoreyaVydeleniya from the genital tract / isolation of vlagalischaKisty yaichnikaBoli pelvic cervical dysplasia matkiKistymatkiBol adnexal appendages in matkiKisty zhelezFibrozno mammary cystic mastopatiyaDipareuniyaGalaktoreyaNarusheniya menstrual discharge from dairy zhelezObschie simptomyUtomlyaemostAsteniyaPlohoe feel pain grudiPerifericheskie otekiGrippopodobnye simptomyVospaleniePovyshenie temperaturyRazdrazhitelnost delay zhidkostiRezultaty obsledovaniyIzmeneniya body weight (increased, decreased, and fluctuations in body weight) Increased TG levels and kroviGiperholesterinemiya Congenital genetic narusheniyaObnar angling more breast / polimastiya In women receiving combined oral contraceptives reported on the development of the following adverse effects: venous thromboembolism, arterial thromboembolism, cerebrovascular complications, hypertension, hypertriglyceridemia, a change in glucose tolerance or effect on insulin resistance of peripheral tissues and liver tumors ( benign or malignant), abnormal liver functions, chloasma. In women with nasal exogenous estrogens may cause exacerbation of symptoms. Anginaedema and aggravation of conditions for which the relationship with the use of combined oral contraceptives has not been clearly proven: jaundice and / or itching associated with cholestasis, gallbladder stones, porphyria, systemic lupus erythematosus; hemolytic-uremic syndrome, Sydengham's chorea, pregnant herpes, otosclerosis with impairment of hearing, Crohn's disease, ulcerative colitis, cervical cancer. Women who use combined oral contraceptives have a very small increase in the rate of breast cancer detection. Since breast cancer rarely occurs in women under 40 years of age, given the overall risk of developing breast cancer, the additional number of cases is very small. The relationship with the use of combined oral contraceptives is not known.
Overdose
No serious violations in overdose have been reported. Symptoms: nausea, vomiting, spotting or metrorrhagia. Treatment: symptomatic therapy is carried out. There is no specific antidote.
Interaction with other drugs
The interaction of oral contraceptives with other drugs can lead to breakthrough bleeding and / or a decrease in contraceptive reliability. The following types of interaction have been reported in the literature. Effects on hepatic metabolism The use of drugs that induce liver microsomal enzymes can increase the clearance of sex hormones. Such drugs include phenytoin, barbiturates, primidone, carbamazepine, rifampicin; There are also suggestions for oxcarbazepine, topiramate, felbamate, griseofulvin, and drugs that contain St. John's wort. HIV protease inhibitors (such as ritonavir) and non-nucleoside reverse transcriptase inhibitors (such as nevirapine) and their combinations can also potentially affect hepatic metabolism. enterohepatic circulation. According to individual studies, some antibiotics (for example, penicillins and tetracycline) can reduce the enterohepatic circulation of estrogen, thereby lowering the concentration Yu ethinyl estradiol. When taking any of the above medicines, a woman should additionally use a barrier method of contraception (for example, a condom). Substances that affect the metabolism of combined hormonal contraceptives (enzyme inhibitors) Dienogest is a substrate of cytochrome P450 (CYP) 3A4. Known inhibitors of CYP3A4, such as azole antifungals (for example, ketoconazole), cimetidine, verapamil, macrolides (for example, erythromycin), diltiazem, antidepressants and grapefruit juice, can increase plasma levels of the diogenogest. The barrier method of contraception should be additionally used within 28 days after their cancellation. While taking antibiotics (with the exception of rifampicin and griseofulvin), an additional dose should be taken within 7 days after their cancellation. but use a barrier method of contraception. If the period of use of the barrier method of protection ends later than the pills in the package, you need to proceed to the next package of Zhanin without the usual interruption in taking pills. Oral combination contraceptives can affect the metabolism of other drugs, which leads to an increase (for example, cyclosporine) or decrease (for example , lamotrigine) their concentrations in plasma and tissues.
special instructions
Before starting or resuming the use of the drug Jeanine; It is necessary to familiarize with the history of life, family history of women, conduct a thorough general medical (including measurement of blood pressure, heart rate, determination of body mass index) and gynecological examination, including the study of the mammary glands and cytological examination of cervical scraping (Pap test), to exclude pregnancy. The amount of additional research and the frequency of control examinations is determined individually. Usually, control tests should be carried out at least 1 time per year. A woman should be informed that Jeanine; It does not protect against HIV infection (AIDS) and other sexually transmitted diseases. If any of the conditions, diseases, and risk factors listed below are present, then the potential risk and the expected benefits of using combined oral contraceptives should be carefully weighed. in each individual case and discuss it with a woman before she decides to start taking the drug. When weighting, amplification or the first manifestation of risk factors may require the abolition of the drug. Cardiovascular diseases Epidemiological studies indicate a relationship between the use of combined oral contraceptives and increased incidence of venous and arterial thrombosis and thromboembolism such as deep vein thromboembolism and thromboembolism. , myocardial infarction, cerebrovascular diseases) when taking combined oral contraceptives. These diseases are rare. The risk of venous thromboembolism (VTE) is maximum in the first year of taking such drugs. Increased risk is present after the initial use of oral contraceptives or the resumption of the use of the same or different combined oral contraceptives (after a break between taking the drug in 4 weeks or more). Data from a large prospective study involving 3 groups of patients show that this increased risk is predominantly present during the first 3 months. The overall risk of VTE in patients taking low-dose combined oral contraceptives (<50 μg of ethinyl estradiol) is 2-3 times higher than in non-pregnant patients who do not take combined oral contraceptives, however, this risk remains lower compared to the risk of VTE during pregnancy and childbirth.VTE can be fatal (1-2% of cases). Venous thromboembolism (VTE), manifested as deep vein thrombosis, or pulmonary embolism, can occur with any combination of oral contraceptives. Thrombosis is extremely rare when using combined oral contraceptives other blood vessels, such as the hepatic, mesenteric, renal, cerebral veins, and arteries or retinal vessels. There is no consensus regarding the relationship between the occurrence of these events and the use of combined oral contraceptives. Symptoms of deep vein thrombosis (DVT) include: one-sided swelling of the lower limb or along the vein on the leg, pain or discomfort in the leg only in the upright position or when walking, local temperature increase in the affected leg, redness or discoloration of the skin on the leg. Symptoms of thromboembolism pulmonary artery (pulmonary embolism) are as follows: difficulty breathing or rapid breathing; sudden cough, incl. with hemoptysis; acute pain in the chest, which may increase with a deep breath; sense of anxiety; severe dizziness; rapid or irregular heartbeat. Some of these symptoms (eg, shortness of breath, cough) are nonspecific and can be interpreted incorrectly as symptoms of other more or less severe events (eg, respiratory tract infection). Arterial thromboembolism can lead to stroke, vascular occlusion or myocardial infarction. Symptoms of a stroke: sudden weakness or loss of sensitivity of the face, arm or leg, especially on one side of the body, sudden confusion, problems with speech and understanding; sudden one or two-sided vision loss; sudden gait disturbance, dizziness, loss of balance or coordination of movements; sudden, severe or prolonged headache for no apparent reason; loss of consciousness or fainting with or without epileptic seizures. Other signs of vascular occlusion are: sudden pain, swelling and weakness of the limbs, acute abdomen. Symptoms of myocardial infarction include: pain, discomfort, pressure, heaviness, a feeling of constriction or distention in the chest, arm, or behind the sternum; discomfort radiating to the back, cheekbone, larynx, arm, stomach; cold sweat, nausea,vomiting or dizziness, severe weakness, anxiety, or shortness of breath; rapid or irregular heartbeat. Arterial thromboembolism can be fatal. The risk of thrombosis (venous and / or arterial) and thromboembolism increases: - with age; - in smokers (with an increase in the number of cigarettes or increasing age, the risk increases, especially in women over 35 years); - for obesity (body mass index of more than 30 kg / m2); - if there is a family history (for example, venous or arterial thromboembolism has ever been with close relatives or parents at a relatively young age). In the case of a hereditary or acquired predisposition, the woman should be examined by an appropriate specialist to decide on the possibility of taking combined oral contraceptives - during prolonged immobilization, serious surgery, any surgery on the legs or extensive trauma. In these situations, it is desirable to stop the use of combined oral contraceptives (in the case of the planned operation, at least four weeks before it) and not to resume reception for two weeks after the end of immobilization; - for dyslipoproteinemia; - for hypertension; - for migraine; - in diseases of the heart valves; - in atrial fibrillation. The question of the possible role of varicose veins and surface thrombophlebitis in the development of venous thromboembolism remains controversial. The increased risk of developing thromboembolism in the postpartum period should be considered. Disorders of the peripheral circulation can also be observed in diabetes mellitus, systemic lupus erythematosus, hemolytic uremic syndrome, chronic inflammatory bowel disease (Crohn's disease or ulcerative colitis) and sickle cell anemia. migraine during the use of combined oral contraceptives (which may precede cerebrovascular disorders) may be Considerations for the immediate cessation of these preparatov.K biochemical parameters indicating hereditary or acquired predisposition for venous or arterial thrombosis include resistance to activated protein C, hyperhomocysteinemia,lack of antithrombin III, deficiency of protein C, deficiency of protein S, antiphospholipid antibodies (anticardiolipin antibodies, lupus anticoagulant). When assessing the risk / benefit ratio, it should be noted that adequate treatment of the corresponding condition can reduce the associated risk of thrombosis. It should also be borne in mind that the risk of thrombosis and thromboembolism during pregnancy is higher than when taking low-dose oral contraceptives (<50 µg ethinyl estradiol). Tumors The most significant risk factor for cervical cancer is persistent papilloma viral infection. There are reports of some increase in the risk of cervical cancer with prolonged use of combined oral contraceptives. However, the association with the intake of combined oral