Angelique Tab n / a film about 28 pc

Description

Composition
Active substance:
Drospirenone 2 mg, 1 mg of estradiol hemihydrate [based on estradiol].
Product form:
Coated tablets (blisters).
Contraindications
Hypersensitivity, vaginal bleeding of unknown origin, or suspected breast cancer, or suspected premalignant disease or hormone-hormone dependent cancers, benign or malignant liver tumors (including history), severe liver disease, severe kidney disease, in m .ch. a history (before normalization of the renal function), acute arterial thrombosis or thromboembolism (including myocardial infarction, stroke), deep vein thrombosis in the art. acute venous thromboembolism (including history) expressed hypertriglyceridemia, pregnancy, lactation.
Dosage
1 mg + 2mg
Indications
HRT at climacteric disorders in postmenopausal women with a uterus unremoved. Prevention of postmenopausal osteoporosis.
Interaction with other drugs
Prolonged treatment with drugs that induce liver enzymes (including derivatives of hydantoin, barbiturates, primidone, carbamazepine, rifampicin, oxcarbazepine, topiramate, felbamate, griseofulvin) may increase the clearance of hormones and reduce their clinical efficacy. Maximal induction of enzyme is usually observed after 2-3 weeks after initiation of treatment and can be stored for 4 weeks after stopping treatment. In rare cases, the background concomitant ingestion of certain antibiotics (including penicillin and tetracycline groups) there was a decrease estradiol concentrations. PM largely exposed conjugation (including paracetamol) may increase the bioavailability of estradiol due to competitive inhibition of conjugation in the process of absorption. Ethanol can increase the concentration of circulating estradiol.
Overdose
Acute toxicity studies showed no risk of acute adverse effects in case of accidental taking the drug in an amount several times greater than the daily therapeutic dose. Symptoms of (alleged) nausea, vomiting, vaginal bleeding. Treat symptomatically, no specific antidote.
pharmachologic effect
Pharmacological group:
Protivoklimaktericheskoe combination means (+ estrogen-progestogen).
Pharmacological properties:
Antiandrogens protivoklimaktericheskoe, oestrogenic, gestagenic ,.
Pharmacodynamics:
Combined estrogen-progestogen preparation. Estradiol in the human body turns into a natural 17 beta-estradiol. Drospirenone – a derivative of spironolactone having progestational, antigonadotropnym and antiandrogenic and antimineralocorticoid activity. Estradiol restores estrogen deficiency in the body after menopause and provides effective treatment of psycho-emotional and autonomic menopausal symptoms (such as “hot flashes”, sweating, insomnia, irritability, irritation, palpitation, cardialgia, dizziness, headache, decreased libido, myalgia , arthralgia), involution of the skin and mucous membranes, especially the mucous membranes of the urogenital system (urinary incontinence, and dryness of mucous membrane irritation puts conductive, dyspareunia). Prevents bone loss caused by estrogen deficiency, mainly due to the suppression of bone remodeling process osteoclast function and a shift toward bone formation. It is proved that long-term use of HRT reduces the risk of peripheral bone fractures in women after menopause. When canceling HRT rates of decrease in bone mass comparable to those typical for the period immediately following menopause. Is no evidence that using HRT, it is possible to achieve restoration of bone mass to premenopausal levels. HRT also has a positive influence on the content of collagen in the skin, skin firmness, slows the formation of wrinkles. Due antiandrogenic properties drospirenone preparation has a therapeutic effect on androgen diseases such as acne, seborrhea, androgenic alopecia. Drospirenone has antimineralocorticoid activity, increases the excretion of Na + and water, which can prevent the increase in blood pressure, body weight, swelling, breast tenderness and others. Symptoms associated with fluid retention. After 12 weeks of drug application has been a slight decrease in blood pressure (systolic – on average 2-4 mm Hg diastolic -.. At 1-3 mm Hg..). Effect on blood pressure was more pronounced in women with borderline hypertension. After 12 months of preparation the average body weight remains unchanged or is reduced to 1.1-1.2 kg. Drospirenone deprived of androgen, estrogen, and glucocorticosteroid antiglyukokortikosteroidnoy activity has no effect on glucose tolerance and insulin resistance, which in combination with antimineralocorticoid and antiandrogenic action, drospirenone provides biochemical and pharmacological profile similar to natural progesterone. Taking the drug leads to a decrease in total cholesterol concentration and LDL, and also a slight increase in the concentration of triglycerides. Drospirenone attenuates growth triglyceride concentration vyzyvamy estradiol. The addition of drospirenone prevents development of hyperplasia and endometrial cancer. Observational studies suggest that among postmenopausal women using HRT reduced incidence of colon cancer. The mechanism of action is unclear so far.
Pharmacokinetics:
Estradiol after ingestion rapidly and completely absorbed. During the absorption and the “first pass” through the liver estradiol largely metabolized (including estrone, estriol and estrone sulfate). Bioavailability – about 5%. Food intake has no effect on the bioavailability of estradiol. Cmax – 22 pg / ml, TSmax – Css estradiol 6-8 hours after repeated administration of about 2 times higher than after a single dose.. The average concentration of estradiol in the serum is in the range 20-43 pg / ml. After discontinuation of estrone and estradiol concentrations returned to baseline values ​​within 5 days. Estradiol binds to albumin and globulin, sex hormone binding (SHBG). Free fraction in the serum estradiol is about 1-12%, and the fraction substance associated SHBG – 40-45%. The apparent volume of distribution – about 1 liter / kg. Is metabolized primarily in the liver, and partly in the intestine, kidney, skeletal muscle and target organs to form estrone, estriol, kateholestrogenov, as well as sulfate and glucuronide conjugates of these compounds having substantially less estrogenic activity, or a pharmacologically inactive. Clearance of the estradiol – 30 ml / min / kg. Estradiol metabolites are excreted in the urine and bile with T1 / 2 – 24 hours. Drospirenone after ingestion rapidly and completely absorbed. Bioavailability – 76-85%. Eating does not affect the bioavailability. Cmax – 22 ng / ml, TSmax – 1 h after single and multiple administration of 2 mg drospirenone. Thereafter observed biphasic reduction in serum concentration with a finite T1 / 2 of about 35-39 hours. Css attained after about 10 days of daily dosing. Because of the long T1 / 2 drospirenone Css 2-3 times higher than the concentration after a single dose. Drospirenone is bound to serum albumin and does not bind to SHBG and corticoid binding globulin. About 3-5% of drospirenone is not bound to proteins. The major metabolites are the acid form of drospirenone and 4.5 digidrodrospirenon-W-sulfate, which are formed without involvement of cytochrome P450 system. Clearance drospirenone – 1.2-1.5 ml / min / kg. Write mainly as metabolites in the urine and feces in a ratio of 1.2 1.4 with a T1 / 2 of about 40 h, a small part is displayed in unchanged form.
side effects
With the reproductive system side “breakthrough” uterine bleeding and spotting (usually terminated in the course of therapy), the changing nature of vaginal discharge, an increase of fibroids size, condition similar to premenstrual syndrome, pain, tension, and / or breast enlargement, benign breast . From the digestive system indigestion, bloating, nausea, vomiting, abdominal pain, recurrent cholestatic jaundice. For the skin skin rash, itchy skin, chloasma, erythema nodosum, erythema multiforme. From the central nervous headache, migraine, dizziness, emotional lability, anxiety, irritability, fatigue, insomnia. Other rarely – palpitations, edema, increased blood pressure, varicose veins, superficial thrombophlebitis, venous thrombosis and thromboembolism, muscle cramps, changes in body weight, changes in libido, visual disturbances, intolerance to contact lenses, allergic reactions.
special instructions
Not applicable for the purpose of contraception. If necessary, contraception, hormonal methods should be used (except the calendar and temperature methods). If you suspect a pregnancy should stop taking the drug for as long as the pregnancy will not be excluded. A number of controlled randomized and epidemiological studies found an increased relative risk of developing venous thromboembolism (including deep vein thrombosis or pulmonary embolism) due to HRT. Therefore, the appointment with risk factors for venous thromboembolism HRT to women is necessary to correlate the risks and benefits, and discuss with the patient. venous thromboembolism risk factors include a personal and family history (presence of venous thromboembolism in the immediate family at a relatively young age may indicate genetic disposition) and severe obesity. The risk of venous thromboembolism also increases with age. The possible role of varicose veins in the development of venous thromboembolism is controversial. The risk of venous thromboembolism may temporarily increase during prolonged immobilization, extensive planning, operations, trauma or massive trauma. Depending on the cause or duration of immobilization should decide whether a temporary discontinuation of HRT. treatment should be discontinued immediately if symptoms of thrombotic disorders or suspected their appearance. In randomized controlled trials with prolonged use of combined conjugated estrogens and medroxyprogesterone there is no evidence of the positive effect on the cardiovascular system. Also, the increased risk of stroke was found. So far, not been long-term randomized controlled trials of others. Drugs for HRT to detect a positive effect on morbidity and mortality related to CAS. Therefore unknown whether the increased risk of drugs for HRT, containing other. Types of estrogen and progestogen. During prolonged estrogen alone increases the risk of endometrial hyperplasia or carcinoma. Studies have confirmed that the combination of a progestin reduces the risk of endometrial hyperplasia and cancer. According to clinical studies and the results of observational studies have found an increased risk of developing breast cancer in women who use HRT for several years. This may be due to an earlier diagnosis, the biological effects of HRT, or a combination of both factors. The relative risk increases with duration of treatment (by 2.3% at 1 year of use). This compares with an increase risk of cancer of breast in women with delayed onset of natural menopause each year (by 2.8% in the 1 year delay). The increased risk gradually decreases to normal levels during the first 5 years after stopping HRT. Breast cancer detected in women taking HRT, usually more localized than in women who did not take it. HRT increases mammographic breast density, which in some cases may adversely affect the radiological detection of breast cancer. Against the background of sex hormones in rare cases benign, and even more rarely – malignant tumors of the liver, and in some cases life-threatening intra-abdominal hemorrhage. When the pain in the upper abdomen, liver enlargement or signs of intraabdominal bleeding in the differential diagnosis should take into account the probability of the presence of liver tumor. It was established that estrogen increases the lithogenic bile, which increases the risk of cholelithiasis in predisposed patients. Treatment should be discontinued immediately at the first appearance of migraine or frequent and unusually severe headaches, as well as the appearance of other symptoms -. Possible precursors of thrombotic stroke brain. The relationship between HRT and the development of clinically significant hypertension has not been established. In women taking HRT, described a slight increase in blood pressure, a clinically significant increase is rare. However, in some cases, the development of the intake of HRT reception clinically significant hypertension should consider the abolition of HRT. In renal insufficiency may reduce the excretion capacity of K +. Receiving drospirenone has no effect on the concentration of K + in serum in patients with mild to moderate renal insufficiency. The risk of hyperkalemia is theoretically can not be excluded in the group of patients in whom the concentration of K + in serum before treatment was determined by the upper limit of normal and which in addition taking potassium sparing drugs. When non-severe hepatic dysfunction, including various forms of hyperbilirubinemia (Dubin-Johnson syndrome, Rotor), requires medical supervision and periodic liver function tests. If deterioration in liver function HRT should be abolished. When relapse cholestatic jaundice or cholestatic pruritus, observed for the first time during pregnancy or previous treatment sex hormones, you should immediately discontinue HRT. The need for special monitoring of women with moderate hypertriglyceridemia. In such cases, the use of HRT may cause a further increase in the concentration of triglycerides in the blood, which increases the risk of acute pancreatitis. Although HRT can influence on peripheral insulin resistance and glucose tolerance, necessary to change the treatment regimen of patients with diabetes during HRT is not usually arise. However, women with diabetes during HRT should be monitored. Some patients under the influence of HRT may develop undesirable manifestations of estrogen stimulation, including abnormal uterine bleeding. Frequent or persistent abnormal uterine bleeding during treatment is an indication for the study of the endometrium. If the treatment of irregular menstrual cycles do not produce results, it is necessary to conduct a survey to exclude organic nature of the disease. Under the influence of estrogen uterine fibroids may increase in size. In this case, the treatment should be discontinued. It is recommended to discontinue treatment with the development of recurrence of endometriosis on the background of HRT. Suspicion of prolactinomas before treatment to exclude the disease. In some cases, chloasma may occur, especially in women with a history of chloasma pregnant. During the HRT women with a tendency to the appearance of chloasma should avoid prolonged exposure to sunlight or UV-radiation. The following conditions may occur or worsen amid HRT (HRT relationship with unproven), epilepsy, benign mammary tumors, asthma, migraine, porphyria, otosclerosis, SLE, chorea. Before starting or resuming HRT woman should undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), exclude pregnancy. Furthermore, it should eliminate blood coagulation disorders. Periodic follow-up examinations should be carried out. Receiving sex hormones may affect liver function, thyroid, adrenals and kidneys, to the content in the plasma transport proteins such as SHBG and lipid / lipoprotein fractions, carbohydrate metabolism, coagulation and fibrinolysis. The drug has no negative effect on glucose tolerance. HRT is not appointed during pregnancy or breastfeeding. Large-scale epidemiological studies of sex hormones used for contraception or HRT, showed no increased risk of birth defects in children born to women who took t
Carefully
Артериальная гипертензия, врожденные гипербилирубинемии (синдром Жильбера, Дубина-Джонсона и Ротора), холестатическая желтуха или холестатический зуд во время беременности, эндометриоз, миома матки, сахарный диабет.
Storage conditions
При комнатной температуре не выше 25 °C 5 лет.
Dosing and Administration
Внутрь, по 1 таблетке ежедневно. Таблетку проглатывают целиком, запивая небольшим количеством жидкости. Если женщина не принимает эстрогенов или переходит с др. комбинированного гормонального препарата для непрерывного приема, то она может начинать лечение в любое время. Пациентки, которые переходят с комбинированного препарата для циклической ГЗТ, должны начинать прием препарата после окончания кровотечения “отмены”. После окончания приема 28 таблеток из текущей упаковки, на следующий день начинают новую упаковку, принимая первую таблетку в тот же день недели, что и первую таблетку из предыдущей упаковки. Время суток, когда женщина принимает препарат, не имеет значения, однако, если она начала принимать таблетки в какое-либо конкретное время, она должна придерживаться этого времени и дальше. Забытую таблетку необходимо выпить как можно скорее. Если же после обычного времени приема прошло более 24 ч, дополнительную таблетку принимать не следует. При пропуске нескольких таблеток возможно развитие вагинального кровотечения.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist