Utrogestan capsules 100mg N28
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Active ingredients
Progesterone
Release form
Capsules
Composition
1 capsule contains: Active substance: natural progesterone micronized 100 mg. Auxiliary substances: sunflower oil - 149 mg, soy lecithin - 1 mg. Capsule shell composition: gelatin - 76.88 mg, glycerol - 31.45 mg, titanium dioxide - 1.67 mg.
Pharmacological effect
Progestin drug. Progesterone, the active ingredient of the drug Utrozestan ;, is a hormone of the corpus luteum. By binding to receptors on the surface of target cells, it penetrates into the nucleus, where by activating DNA, it stimulates the synthesis of RNA. Promotes the transition of the uterine mucosa from the proliferation phase caused by follicular hormone to the secretory phase. After fertilization promotes the transition to the state necessary for the development of a fertilized egg. Reduces the excitability and contractility of the muscles of the uterus and fallopian tubes, stimulates the development of the terminal elements of the mammary gland. Stimulating protein lipase, increases fat stores, increases glucose utilization. Increasing the concentration of basal and stimulated insulin, contributes to the accumulation of glycogen in the liver, increases the production of gonadotropic hormones of the pituitary gland; reduces azotemia, increases the excretion of nitrogen in the urine. It activates the growth of the secretory section of the acini of the mammary glands, induces lactation. Promotes the formation of normal endometrium.
Pharmacokinetics
When ingestion Absorption Micronized progesterone is absorbed from the gastrointestinal tract. The concentration of progesterone in the blood plasma gradually increases during the first hour, Cmax is noted 1-3 h after administration. The concentration of progesterone in the blood plasma increases from 0.13 ng / ml to 4.25 ng / ml after 1 h, to 11.75 ng / ml - after 2 h and amounts to 8.37 ng / ml after 3 hours, 2 ng / ml after 6 hours and 1.64 ng / ml after 8 hours after administration. Metabolism The main metabolites that are determined in blood plasma are 20-alpha-hydroxy-delta-4 alpha pregnanolone and 5 alpha dihydroprogesterone. Injection Excreted in the urine as metabolites, 95% of them are glucuron onyugirovannyh metabolites, mainly 3-alpha, 5-beta-pregnanediol (pregnandion). These metabolites, which are determined in blood plasma and urine, are similar to substances formed during the physiological secretion of the corpus luteum. . A high level of progesterone is observed after 1 h after administration.Cmax of progesterone in plasma is reached 2-6 hours after administration. With the introduction of the drug in 100 mg 2 times / day, the average concentration remains at 9.7 ng / ml for 24 hours. When given in doses of more than 200 mg / day, the concentration of progesterone corresponds to the first trimester of pregnancy. Metabolism Metabolizes to form predominantly 3-alpha, 5 beta pregnanediol. Plasma level of 5-beta-pregnanolone does not increase. Excretion Excreted in the urine as metabolites, the main part is 3-alpha, 5-beta-pregnanediol (pregnandion). This is confirmed by a constant increase in its concentration (Cmax 142 ng / ml after 6 h).
Indications
Progesterone-deficient states in women: oral route of administration: - infertility due to luteal insufficiency; - premenstrual tension syndrome; - menstrual cycle disorders due to impaired ovulation or anovulation; - fibrocystic mastopathy; - premenopause; - peritoneal hormone therapy (HRT) in postmenopausal (in combination with estrogen-containing drugs). Vaginal route of administration: - threatening abortion or preventing habitual abortion due to progesterone deficiency; - warning (prevention) of preterm labor in women at risk (with shortening of the cervix and / or the history of preterm labor and / or early rupture of the fetal membranes) - support of the luteal phase during preparation for extracorporal fertilization; - support of the luteal phase in a spontaneous or induced menstrual cycle; - premature menopause; - HRT (in combination with estrogen-containing drugs); - infertility due to luteal insufficiency; - HRT with progesterone deficiency in nonfunctioning niruyuschih (absent) ovaries (egg donation).
Contraindications
- Hypersensitivity to the drug. hypersensitivity to the components of the drug; - deep vein thrombosis, thrombophlebitis, thromboembolic disorders (pulmonary artery thromboembolism, myocardial infarction, stroke), intracranial hemorrhage or the presence of these conditions / diseases in the anamnesis; - established or suspected malignant neoplasms of the mammary glands and genitals. For oral administration: - severe liver disease (including cholestatic jaundice, hepatitis, D syndromes Ubina-Johnson, Rotor, Malignant Liver Tumors) currently or in history.
Precautionary measures
The drug should be used with caution in diseases of the cardiovascular system, arterial hypertension, chronic renal failure, diabetes mellitus, bronchial asthma, epilepsy, migraine, depression, hyperlipoproteinemia.
Use during pregnancy and lactation
In pregnancy, the drug can only be used intravaginally. The drug should be used with caution in the II and III trimesters of pregnancy because of the risk of cholestasis. Progesterone penetrates into breast milk, therefore, the use of the drug is contraindicated during breastfeeding.
Dosage and administration
The duration of treatment is determined by the nature and characteristics of the disease. The oral route of administration. The drug should be taken orally with water. In most cases with progesterone deficiency, the daily dose of the drug is Utrozhestan; 200-300 mg divided into 2 doses (morning and evening). When the luteal phase is inadequate (premenstrual tension syndrome, fibrocystic mastopathy, dysmenorrhea, premenopause), the daily dose of the drug is 200 or 400 mg for 10 days (usually with 17 on the 26th day of the cycle). In case of HRT in perimenopause along with estrogen, the drug Utrozestan; 200 mg / day are applied for 12 days. In post-menopausal HRT, the drug Utrogestan is continuous; used in a dose of 100-200 mg from the first day of estrogen. Dose selection is carried out individually. Vaginal route of administration. Capsules are inserted deep into the vagina. Prevention (prevention) of preterm birth in women at risk (with shortening of the cervix and / or the presence of anamnestic data of preterm delivery and / or premature rupture of the fetal membranes): the usual dose is 200 mg at bedtime, from the 22nd to the 34th week of pregnancy. The complete absence of progesterone in women with non-functioning (missing) ovaries (egg donation): during therapy with estrogen at 200 mg / s tons on the 13th and 14th days of the cycle, then - 100 mg 2 times / day from the 15th to the 25th day of the cycle, from the 26th day and in the case of pregnancy determination, the dose increases by 100 mg / day each week, reaching a maximum of 600 mg / day, divided into 3 doses. This dose is usually applied for 60 days. Supports the luteal phase during the in vitro fertilization cycle: it is recommended to use from 200 to 600 mg / day,starting from the day of injection of chorionic gonadotropin during the I and II trimesters of pregnancy. Supporting the luteal phase in a spontaneous or induced menstrual cycle for infertility associated with impaired function of the corpus luteum: it is recommended to use 200-300 mg / day starting from the 17th day of the cycle for 10 days, in case of delayed menstruation and diagnosis of pregnancy, treatment should be continued. In cases of threatening abortion or in order to prevent habitual abortion, occurring against the background of progesterone deficiency: 200-400 mg / day 2 doses daily in the first and second trimester of pregnancy.
Side effects
The adverse events listed below, noted during oral administration of the drug, are distributed by frequency of occurrence. Drowsiness, transient dizziness are possible, as a rule, 1-3 h after taking the drug. These side effects can be reduced by reducing the dose, using the drug at bedtime or switching to the vaginal route. These unwanted effects are usually the first signs of overdose. Drowsiness and / or transient dizziness are observed, in particular, in the case of concomitant hypoestrogenism. Reduction of the dose or recovery higher estrogenisation immediately eliminates these phenomena, without reducing the therapeutic effect of progesterone. If the treatment begins too early (in the first half of the shortening of the menstrual cycle or acyclic bleeding are possible. Recorded changes in the menstrual cycle, amenorrhea or acyclic bleeding are characteristic of all progestogens. Clinical practice In the post-marketing application, the following undesirable effects were noted in oral progesterone: insomnia, premenstrual syndrome, tension in the mammary glands, vaginal discharge, joint pain, hyperthermia, increased sweating in night hours, fluid retention, changes in body weight, acute pancreatitis, alopecia, hirsutism, changes in libido, thrombosis and thromboembolic complications (when performing HRT in combination with estrogen-containing drugs), increased blood pressure. The drug contains soy lecithin,which can cause hypersensitivity reactions (urticaria and anaphylactic shock). In case of vaginal application, individual cases of local intolerance to the components of the drug (in particular, soy lecithin) in the form of vaginal mucosa hyperemia, burning, itching, oily secretions were reported. intravaginal use of the drug in recommended doses, in particular, drowsiness or dizziness (observed with oral administration of the drug), were not observed.
Overdose
Symptoms: drowsiness, transient dizziness, euphoria, shortening of the menstrual cycle, dysmenorrhea. In some patients, the average therapeutic dose may be excessive due to the existing or unstable endogenous progesterone secretion, a special sensitivity to the drug or too low estradiol concentration. the occurrence of drowsiness or dizziness, you must reduce the daily dose or prescribe the drug before going to bed during the 10 days of the menstrual cycle; - in the case of a shorter It is recommended to transfer the menstrual cycle or bloody discharge to the later day of the cycle (for example, on the 19th instead of the 17th); - in perimenopause and in postmenopausal HRT, make sure that the concentration of estradiol is optimal. Overdose symptomatic treatment if necessary.
Interaction with other drugs
In the case of oral progesterone, progesterone acceleration of progesterone metabolism in the liver. Simultaneous administration of progesterone with certain antibiotics (penicillins, those ratsikliny) may reduce its effectiveness due to violation of enterohepatic recirculation of sex hormones due to changes in intestinal mikroflory.Stepen severity of these interactions can be varied in different patients,therefore, the prediction of the clinical effects of these interactions is difficult. Ketoconazole can increase the bioavailability of progesterone. Progesterone can increase the concentration of ketoconazole and cyclosporine. Progesterone can reduce the effectiveness of bromocriptine. diabetes mellitus. The bioavailability of progesterone can be reduced in smoking patients and with excessive use of Alcohol. In intravaginal administration. The interaction of progesterone with other drugs in intravaginal administration has not been evaluated. The simultaneous use of other drugs used intravaginally should be avoided to avoid impairing the release and absorption of progesterone.
special instructions
The drug Utrozhestan can not be used for contraception. The drug can not be taken with food, because food intake increases the bioavailability of progesterone. The drug Utrozhestan should be taken with caution in patients with diseases and conditions that can be aggravated by fluid retention (arterial hypertension, cardiovascular diseases, chronic renal failure, epilepsy, migraine, bronchial asthma); in patients with diabetes; impaired liver function mild and moderate severity; photosensitivity. Patients with a history of depression should be monitored, and if severe depression develops, the drug should be discontinued. Patients with concomitant cardiovascular diseases or their history should also be periodically observed by a physician. Use of Utrogestan after the first trimester of pregnancy may also cause development of cholestasis. During prolonged treatment with progesterone, it is necessary to regularly conduct medical examinations (including liver function tests); treatment should be canceled in case of deviations from normal liver function tests or cholestatic jaundice. When using progesterone, glucose tolerance may decrease and the need for insulin and other hypoglycemic drugs in diabetic patients may increase. If amenorrhea appears during treatment, it is necessary to exclude the presence of pregnancy. If the treatment starts too early at the beginning of the menstrual cycle, especially before the 15th day of the cycle,cycle shortening and / or acyclic bleedings are possible. In the case of acyclic bleeding, the drug should not be used until their cause has been determined, including a histological examination of the endometrium. If there is a history of chloasma or a tendency to develop it, patients are advised to avoid UV irradiation. In addition, the cause of spontaneous abortions in early pregnancy can be infectious processes and mechanical damage. The use of the drug Utrozhestan in these cases can only lead to a delay in rejection and evacuation of the nonviable fetal egg. The use of the drug Utrogestan to prevent threatening abortion is justified only in cases of progesterone deficiency. shock). When conducting hormone replacement therapy with estrogens during the perimenopause, the use of the drug Utrogestan is recommended for at least 12 days during the continuous mode of HRT in postmenopausal use of the drug is recommended from the first day of estrogen administration. When conducting HRT increases the risk of venous thromboembolism (deep vein thrombosis or pulmonary embolism), the risk of ischemic stroke IBS. the drug should be discontinued in case of: - visual impairment, such as loss of vision, exophthalmos, double vision, vascular lesions of the retina; migraine; - venous thromboembolism or thrombotic complications, regardless of their location. If there is a history of thrombophlebitis, the patient should be carefully monitored. Health Initiative Study (WHI) indicate a slight increase in the risk of breast cancer with a long, more than 5 years, the joint use of estrogen obsessive drugs with synthetic gestagens.It is not known whether there is an increase in the risk of breast cancer in postmenopausal women during HRT with estrogen-containing drugs in combination with progesterone. a woman should be examined to identify contraindications to her. In the presence of clinical indications, an examination of the mammary glands and gynecological examination should be carried out. The use of progesterone can influence the results of some laboratory tests, including indicators of the function of the liver, thyroid gland; coagulation parameters; concentration of pregnandiol. Effect on the ability to drive vehicles and control mechanisms When using the drug orally, care should be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.