Directory → Hormones and their antagonists → Estrogens, gestagena; Their homologues and antagonists → Lindinet 20
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Lindinet 20See also ExemestaneRoman nameLindynette 20CharacteristicsMonofazny gestagen-estrogenny combined contraceptive product.PharmacokineticsGestoden.bystro and virtually 100% of the skin glands (bioavailability about 99%). After 1 hour after a single concentration of 2-4 ng / J Associated with albuminami and globulinom linking sex hormones (GSPG). 1-2% is in the form of a free steroida, 50-75% specifically binds to GSPG. Improved GSPG in the blood caused by etinilestradiolom affects the gestodena : growing faction associated with GSPG and declining fraction associated with albuminami. Average distribution gestodena 0,7-1,4 l / kg Treated biotransformation like other Steroids. Averages ground : 0.8-1.0 ml / min / kg The level in the serum decreased dwuhfazno. The final stage T_1/2 - 12-20 hours Provided only in the form of metabolites : 60% from urine, 40% from faeces. T_1/2 metabolites about 1 дня.Этинилэстрадиол.Б ыстро and almost completely absorbed from the digestive tract. Mean C_max in the serum - 30-80 pg / ml achieved in 1-2 h after administration. Bioavailability because presistemna conjugation and primary metabolism of about 60%. Completely, but nespecificski contact albuminami (about 98.5%), and produces the GSPG level in the serum. Average distribution-18 l / kg Most are aromatic gidrauxilirovaniu education and gidrauxilirovannah metilirovannah metabolites, which are present in the form of free or metabolites in the form of kongugatov (glukuronidov and sulphate). Metabolic klirens from blood plasma about 13 ml / min / kg The concentration in the serum decreased dwuhfazno. T_1/2 the second phase is about 16 to 24 hours Estrogens is only in the form of metabolites in urine and jelchew ratio of 2:3. T_1/2 metabolites about 1 Dna.stabilnaya concentration (20% higher than after a single dose) for a 3-4 day.Clinical pharmacologyOral contraceptives, in addition to preventing pregnancy, had a positive impact on the menstrual cycle (in the event of violation) : monthly cycle is regular reduce krovopoteri during menstruation and the frequency of iron deficiency, the frequency decreases dismenorei, the emergence of functional ovarian cyst, ectopic pregnancy, a fibroadenom fibrokist and in the milk glands, inflammatory diseases of small pelvis and education endometrium cancer; improving the skin in acne skin.IndicationsContraception.Pregnancy and lactationThe drug is contraindicated in pregnancy. If necessary, the appointment of the drug during lactation to determine whether or not a breast-feeding (active drug substance in small quantities available in breast milk).ContraindicationsHypersensitivity to the drug component; Sexually violent expressed human liver; Liver tumors (including in history); Thrombosis and embolism (incl. history); Myocardial infarction (incl. history); Heart failure; Cerebrovascular disorders (including in history); Of the preceding car (including tranzitorne heart attack Drinking); Koagulopatia; sickle cell anemia; estrogenozawisimae tumours, including tumours breast or endometrium (incl. history); diabetes mellitus, oslojnenny mikroangiopatiami; breeding bleeding unknown etiology; idiopathic jaundice and itching of the skin during pregnancy; that the disease virus; otoscleros deteriorating during the previous pregnancy; Beremennosti.s caution is breast cancer, trochaic pregnant (prior appointment could aggravate the horei pregnant), diabetes, epilepsy, disease gall bladder, especially jelchekamennaya disease (incl. disease), liver failure, arterial hypertension, immobilization, big surgery, holetsatical jaundice (including pregnant women in history), depression (incl. disorder), migraines.Patient interactionRifampicin (klirens increases), as well as barbiturates, carbamazepine, fenilbutazon, phenytoin, griseofulvin, topiramat, felbamat, okscarbasepin could lead to prorave bleeding of the uterus or reduced control действия.Контрацепти��ная reliability with reduced hospital admission, tetracycline (mechanism of this action is not clear). During concomitant admission to the above-mentioned products, as well as for a period of 7 days after the completion of their reception, it is necessary to apply different negormonale (condoms, spermicidal gels) methods of contraception. Using rifampitina additional methods of contraception should be used within four weeks after the completion of his reception. Any property that increase motoriku tract, reduces preparation in Krovi.ls (eg ascorbic acid), which are sulfatirovaniu wall in the intestines, preventing competitive sulfatirovnie etinilestradiola and reinforce its biological availability. Inhibitors liver enzymes (eg Itraconazole, flukonazol) to the concentration of etinilestradiola plasma крови.Этинилэстрадио�� by inhibition of liver enzymes or accelerate conjugation (primarily glukuronirovania) may affect the metabolism of other drugs, increasing or reducing their concentration in the blood (eg ciclosporin, theofillin). The common drugs (including tea) reduces the concentration of the drug in the blood, which can lead to prorave bleeding, pregnancy (reason is the inducyrutee John enzymes in the liver, which continued for a further two weeks after the course reception St.). Ritonavir reduces etinilestradiola AUC by 41%. In this regard, during the ritonavira should use product with a greater dose etinilestradiola (Lindinet 30), or apply negormonale methods.Storage conditionsAt temperatures below 30 ° CShelf life2The registration015122/01-2003 |
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