Following oral administration, in micronized form is its rapid absorption in the gastrointestinal tract. The drug is subject to primary metabolism in liver and intestine. Maximum plasma concentration of approximately 44 pg / ml (30-53 pg / ml) reached after 6 hours after administration of 2 mg. The npp cycle is about 18 hours. It circulates in the blood as a complex with binding globulin hormones , and albumin (61%), and only 1-2% remains unbound form. Occurs mainly in the liver and intestine, as well as the target organs and involves the formation of less active and inactive metabolites including estrone, and various kateholestrogeny estrogen sulfates and glucuronides. Estrogens are displayed along with the bile, where they are partially hydrolyzed and again comes methyltrienolone in enteric hepatic blood flow (recycle), and the majority of estrogen excreted in urine in biologically inactive form. After oral administration, norethisterone is rapidly absorbed and transformed to norethisterone . The maximum plasma concentration of about 9 ng / ml (6.11 ng / ml) reached after 1 hour after taking 1 mg. The is about 10 hours. and albumin (61%). It undergoes first-pass metabolism in the liver and intestine. The most important metabolites are isomersT, which are derived mainly in the urine as sulfate or glucuronide conjugates. The elderly Pharmacokinetic studies have not been conducted
Indications for use:
Hormone replacement therapy npp cycle in women with symptoms of estrogen deficiency. Prevention of osteoporosis in postmenopausal women when there is a high risk of fractures in those patients who can not tolerate or are contraindicated other medicines intended for the prevention of osteoporosis. The experience of treating women older than 65 is limited.
- Breast cancer (set, a history, and it is also suspected)
- Known or suspected estrogen-dependent tumors (including endometrial cancer)
- Abnormal bleeding from the genital organs of unknown etiology.
- Untreated endometrial hyperplasia
- Recently transferred or in the active phase of venous thromboembolic disease (deep vein thrombosis, pulmonary embolism)
- Newly migrated in the active phase or arterial thromboembolic disease (including angina, myocardial infarction)
- Acute liver disease or a history of liver disease in which liver function tests are not normalized
- Congenital lactase deficiency, lactose intolerance, glucose-galactose malabsorption
- Hypersensitivity to the active agent or other components within the drug
- porphyriaPrecautions (a disease in which the need to follow-up) – If the patient of the following diseases and / or if the disease has occurred previously and / or is aggravated during pregnancy or previous hormone treatment metribolone, the patient must be such under close medical supervision. It will be appreciated that these diseases may recur or worsen during treatment with npp cycle , in particular, this applies to the following diseases:
- Leiomyoma (fibroadenoma of the uterus) or endometriosis (see. Below)
- Risk factors for thromboembolism, or a history of thromboembolism (see. below)
- Risk factors for estrogen-dependent tumors (eg, the presence of suffering from breast cancer family first-degree relatives)
- Arterial hypertension
- Liver disease (including liver adenoma)
- Diabetes mellitus with or without vascular lesions
- Migraines or severe headaches
- Systemic lupus erythematosus
- Endometrial hyperplasia in history (see. Below)
- Bronchial asthma
- otosclerosisPregnancy and lactation reception is not shown during pregnancy. If pregnancy occurs during treatment with the drug npp cycle, treatment should be discontinued immediately. The data, based on a limited number of pregnancies, during which the patients received hormonal preparations, indicate of adverse effects of norethisterone on the fetus. At doses in excess of those normally used in HRT, there was masculinization of female fetuses. The results of most conducted dimethylnandrolone to date epidemiological studies related to the unintended effects on the fetus of combined formulations of estrogen and progestogen, indicate the absence of teratogenic and foetotoxic action.