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Pharmacological properties

Estradiol Valeriate

The active substance, a synthetic 17β-estradiol valeriate, is converted in the body to 17β-estradiol. 17β-estradiol is identical in its chemical and biological properties to endogenous estradiol. It compensates for the lack of estrogen production in women during menopause and minimizes the symptoms characteristic of menopause.


Estrogens promote endometrial growth; estrogen monotherapy increases the risk of developing endometrial hyperplasia and cancer. The inclusion of levonorgestrel progestogen in the preparation significantly reduces the risk of developing endometrial hyperplasia caused by estrogens in women with an unexplained uterus.

Estradiol Valeriate

After oral administration of estradiol, valerate is completely adsorbed in the gastrointestinal tract, the maximum level of serum estradiol is reached in 2–4 hours. After taking an oral dose of estradiol of 2 mg, the maximum level of estradiol exceeds 100 mg / ml. The average plasma half-life is about 1 hour. Estradiol partially binds to plasma proteins.

Orally administered estradiol during the first passage through the liver is metabolized by 90%, mainly to estrone, estrone sulfate and estriol, as well as to free or methylated catecholesterogens. The metabolism process mainly occurs in the liver, as well as in other tissues.

Estradiol and its metabolites (estrone and estriol) are excreted in the urine for 48 hours in the form of conjugates with sulfuric and glucuronic acid, as well as in a small amount - unchanged. Estradiol is partially excreted in the feces.


After oral administration, levonorgestrel is rapidly and completely adsorbed in the digestive tract.

After oral administration of the drug, the maximum level in blood serum is reached after 1-2 hours. The half-life is 2 hours in the distribution phase and 10-24 hours in the elimination phase.

In blood plasma, 93–95% of levonorgestrel binds to albumin and more specifically to sex steroid-binding globulins.

The effect of the first passage has not been identified.

The plasma clearance rate is 106 ml / h / kg. Levonorgestrel is excreted in the form of reduced and / or hydroxylated metabolites, mainly conjugated to sulfuric and glucuronic acid. Excretion from the body occurs in equal parts with urine and feces.

A small amount of levonorgestrel is excreted in breast milk.


Climonorm is used for hormone replacement therapy (HRT) in women with symptoms of estrogen deficiency and menopause (for example, hot flashes, attacks of excessive sweating, sleep disturbances, depressive mood changes, nervousness, etc.) due to natural or surgical (complete or partial removal of the ovaries ) menopause.


Climonorm is taken 1 tablet a day (preferably in the evening) for 21 days.

Reception begins with a dragee, indicated by the number 1 on the blister and then continues in the direction of the arrow. After taking 9 yellow tablets, take 12 tablets of brown color. After all dragees have been taken for 3 weeks, a 7-day break occurs without taking the drug. During this period, one should expect the appearance of another menstrual bleeding.

After a 7-day break, they start taking dragees from the next package, regardless of whether the bleeding has ended or is still ongoing.

If preparations for HRT have not been used in the previous period: if the patient still has menstrual bleeding (premenopausal period), the first Klimonorm dragee is taken on the 5th day of the menstrual cycle.

In the menopausal period or with long periods of time between spontaneous menstrual bleeding, the drug can be started at any time. Before starting therapy, pregnancy should be excluded.

The use of the drug Klimonorm, if previously the patient used another drug for HRT

When switching to Klimonorm after the previous use of the combined preparation for continuous HRT, the patient may start taking Klimonorm tablets after completion of the cycle of the previous therapy.

If the patient switches to Klimonorm after a cyclic combined preparation for HRT, taking the Klimonorm dragee should begin after the end of the break, free from taking the tablets.

Dragees are taken without chewing. To avoid gastrointestinal disturbances, it is recommended to take dragees in the evening after a meal.

The duration of the course of treatment is determined by the doctor individually.

It is advisable to take dragees at the same time daily. If you miss the next dragee in the reception, you must take it within the next 12 hours. If the delay in taking the dragee is 12 hours, the missed dragee should be left in the package. With gaps in taking dragees, the likelihood of sudden bleeding or spotting increases.


The drug climonorm can not be used in any of the following conditions. if any of these conditions occurs during therapy, the drug should be stopped immediately;

diagnosed or suspected breast cancer or history of the disease;

diagnosed or suspected estrogen-dependent tumors (e.g. endometrial cancer);

vaginal bleeding of unknown etiology;

untreated endometrial hyperplasia;

history of venous thromboembolism (VTE) of unknown etiology or existing VTE (deep vein thrombosis, pulmonary embolism);

acute arterial thromboembolism or recent arterial thromboembolism (e.g. angina pectoris, myocardial infarction);

severe liver disease at this time or in history, until normalization of laboratory parameters of the functional state of the liver;

known hypersensitivity to active substances or any of the auxiliary components of the drug;


hereditary fructose intolerance, galactose intolerance, lactose deficiency, glucose-galactase malabsorption or sucrose-isomaltase deficiency.

Side effects

In clinical studies, side effects associated with taking the drug were recorded, and which in some cases were probably manifestations of menopause.

Frequency: Common (1/100, 1/10)

From the nervous system: headache.

From the cardiovascular system: hypertension.

From the reproductive system and mammary glands: benign mastopathy.

Common disorders: hot flashes.

Frequency: not common (1/1000, 1/100)

From the side of the nervous system: migraine, weak memory, depressed mood, dizziness.

From the cardiovascular system: tachycardia, varicose veins.

From the gastrointestinal system: nausea, flatulence, abdominal pain, constipation, dyspepsia.

Skin: acne, itching.

From the reproductive system and mammary glands: intermenstrual bleeding, a feeling of tension or pain in the mammary glands, mastitis, vaginitis, vaginal discharge, thickening of the endometrial layer, glandular-cystic endometrial hyperplasia.

From the side of the respiratory system: infectious diseases of the respiratory tract.

Eyes: impaired vision.

Liver and gall bladder: cholangitis, cholecystitis, increased activity of liver enzymes, bilirubinemia.

General disorders: hypersensitivity reactions, weakness.

Other disorders: increased blood sugar, changes in blood lipids, edema, changes in body weight, anemia, pelvic pain, nodules in the thyroid gland.

The following adverse reactions have also been reported in connection with therapy with other estrogen / progestogen combinations:

benign and malignant estrogen-dependent neoplasms, for example endometrial cancer;

VTE, that is, deep vein thrombosis or pulmonary embolism, is more common in women using HRT than among women not using HRT;

myocardial infarction or stroke;

gall bladder disease;

violation of the skin or subcutaneous tissue: chloasma, erythema nodosum, exudative erythema multiforme, vascular purpura;

possible development of dementia;

possible development of a liver tumor.

special instructions

It is recommended to start HRT for the treatment of symptoms characteristic of the postmenopausal period only in cases where such symptoms seriously affect the quality of life. in any case, it is necessary to conduct a thorough annual analysis of the relationship between the benefit and the risk of using the drug and continue HRT only when the benefit prevails over the risk.

Endometrial hyperplasia

The risk of endometrial hyperplasia and cancer increases with prolonged estrogen monotherapy. This risk increases with the duration of treatment. Based on the results of epidemiological studies, the risk assessment for women who do not use HRT is about 5 cases of endometrial cancer, detected at the age of 50–65 years per 1000 women. Depending on the duration of treatment and the dose of estrogen, a 2–12-fold increase in the development of endometrial cancer in women with estrogen monotherapy is noted compared with women not using HRT. The inclusion of progestogen in the treatment regimen for women with an unexplained uterus for at least 12 days / cycle significantly reduces this risk.

During the first months of treatment, breakthrough bleeding or spotting may occur. If these phenomena are noted during therapy or continue after treatment is discontinued, an examination should be conducted to determine the etiology of bleeding, which includes an endometrial biopsy to exclude a malignant tumor of the endometrium.

Mammary cancer

The results of randomized, placebo-controlled studies and epidemiological studies indicate an increased risk of breast cancer in women taking estrogens, estrogen-progestogen combinations, or tibolone for HRT over the course of several years. For all types of HRT, this increased risk becomes apparent during several years of therapy and increases with the duration of treatment, but returns to its initial level several (mainly 5) years after its termination.

In studies, the relative risk of developing breast cancer with conjugated equine estrogens or estradiol (E2) was higher with the cyclic or continuous inclusion of progestogen in the treatment regimen, regardless of the type of progestogen. It is not known whether there are differences in risk indicators for different routes of administration.

In the studies, the use of a drug containing conjugated equin estrogen and medroxyprogesterone acetate for continuous combination therapy was associated with the development of breast cancer, which was more invasive and more often metastasized to regional lymph nodes compared with placebo.

HRT, in particular combined estrogen-progestogen therapy, increases the density of images during mammography studies, which may lead to an incorrect assessment of the results of a radiological study for breast cancer.


The use of HRT is associated with an increase in the relative risk of developing VTE, that is, deep vein thrombosis or pulmonary embolism.

The generally recognized risk factors for the development of VTE include: personal and family history, severe obesity (BMI 30 kg / m2) and systemic lupus erythematosus. The question of the possible role of varicose veins in the development of VTE remains controversial.

Patients with VTE have a history of an increased risk of developing VTE. HRT may slightly increase this risk. Therefore, the appointment of HRT should be preceded by a thorough study of the patient’s personal and family history, attention should be paid to the presence of repeated involuntary abortions in the history. The use of HRT in such patients is contraindicated until a complete assessment of the risk factors for thromboembolism and the need for anticoagulant therapy. Women receiving anticoagulant therapy need to carefully assess the expected benefits and potential risks of HRT.

The risk of VTE may temporarily increase with prolonged immobilization, after a major operation, especially abdominal surgery or surgery on the lower extremities or a serious injury. In this regard, consideration should be given to terminating HRT 4–6 weeks before surgery, if possible. Treatment is not recommended to be resumed until complete recovery. If VTE develops after the start of HRT, treatment should be stopped immediately.

Ischemic heart disease

The results of randomized controlled trials indicate a negative effect on the cardiovascular system when using continuous combination therapy with conjugated estrogens and medroxyprogesterone acetate (MPA). Based on clinical studies, a possible increase in the risk of developing diseases of the cardiovascular system during 1 year of use is shown, which persisted with the further use of drugs.


Another negative consequence is the increased risk of ischemic stroke in healthy women with the use of continuous combination therapy with conjugated estrogens and MPA.

Ovarian cancer

According to the results of the studies, long-term (at least 5–10 years) estrogen monotherapy in women with a removed uterus was associated with an increased risk of ovarian cancer. It was not revealed whether there are differences regarding this risk with prolonged combination therapy with conjugated estrogens and MPA compared with estrogen monotherapy.

Liver tumors

After the use of hormonal substances, the components of which are contained in the Klimonorm preparation, in isolated cases the development of benign, and even less often, malignant liver tumors was noted. In some cases, tumor growth was complicated by intraperitoneal bleeding, which posed a threat to life. If there is pain in the upper abdomen, an increase in the size of the liver, or signs of intra-abdominal bleeding during differential diagnosis, the likelihood of a liver tumor should be considered.

Other conditions

The use of estrogen can lead to fluid retention. Given this, patients with functional impairment of cardiac or renal activity should be closely monitored. It is necessary to closely monitor the condition of patients with terminal renal failure, since in these cases an increase in the level of circulating active substances of Klimonorm can be expected.

Women with a history of hypertriglyceridemia need special monitoring during estrogen monotherapy or HRT using the estrogen / progestogen combination, as frequent cases of significant increase in plasma TG levels have been reported with estrogen monotherapy. In some cases, this led to the development of pancreatitis.

No data are available on improving cognitive function.Some results of the study indicate an increased risk of the possible development of dementia in women who use continuous combined HRT with conjugated estrogens and MPA over the age of 65 years.

Effect on laboratory results

Estrogens increase the level of globulin that binds thyroid hormones, which leads to an increase in circulating total thyroid hormone, which is determined by the level of T4 or T3 (using immunological studies).

The concentration of free T4 and T3 remain unchanged. Levels of other serum proteins can increase, for example, corticoid-binding globulin, sex hormone-binding globulin, resulting in increased concentrations of circulating corticosteroids and sex steroids, respectively. Concentrations of free or biologically active hormones remain unchanged. Levels of other plasma proteins (substrate of renin / angiotensinogen, alpha-1-antitrypsin, ceruloplasmin) may increase.

Careful Monitoring Conditions

If a patient is diagnosed, suspected, or transferred to any of the following conditions or diseases and / or aggravates during pregnancy or previous hormonal therapy, careful medical monitoring of the patient should be carried out. You should consider the possibility of relapse or exacerbation of the following conditions when using the drug Klimonorm: leiomyoma (uterine fibroma) or endometriosis; a risk of thromboembolic disorders or a history of such disorders; the risk of developing estrogen-dependent tumors, such as breast cancer in a relative of the first knee; Hypertension; liver disease (e.g., hepatoadenoma); diabetes with or without vascular complications; cholelithiasis; migraine or severe headache; systemic lupus erythematosus; history of endometrial hyperplasia; epilepsy; BA otosclerosis.

Medical examination / consultation

Before starting or resuming HRT, you need to study the patient’s family history in detail and conduct a full physical examination (including examination of the pelvic organs and mammary glands), taking into account contraindications and warnings when using HRT. Such examinations are recommended to be repeated periodically: to conduct an examination of the mammary glands, including mammography, according to the existing standards of medical practice, taking into account the individual characteristics of each patient.

Use during pregnancy and lactation. Climonorm should not be prescribed during pregnancy and lactation. In the event of pregnancy during the administration of Kliamonorm should immediately stop treatment.

Clinical data based on a limited number of cases of the drug during pregnancy do not indicate a negative effect of levonorgestrel on the fetus. According to the results of most epidemiological studies, no teratogenic or fetotoxic effects of estrogen / progestogen combinations were detected during their accidental administration during pregnancy.

Influences on the ability to drive vehicles and work with complex mechanisms have not been identified.


Simultaneous administration of drugs that stimulate enzymes that metabolize active substances, in particular enzymes of the cytochrome p450-dependent system, such as anticonvulsants (e.g. phenobarbital, phenytoin, carbamazepine) and drugs for the treatment of certain infectious diseases (e.g. rifampicin, rifabutin, nevirapine, efavirez) enhances the metabolism of estrogens and paragestogens.

Although ritonavir and nelfinavir are known as potent inhibitors, when used with steroid hormones, they exhibit inducing properties.

Herbal medicines containing Hypericum perforatum can induce the metabolism of estrogen and progestogen.

An enhanced metabolism of estrogens and progestogens can lead to a decrease in the clinical effectiveness of therapy and a change in the nature of uterine bleeding.

The levels of Klimonorms active substances in blood plasma may increase due to the use of drugs that inhibit enzymes that metabolize active substances (for example, ketoconazole).

Estrogens may enhance the effects and side effects of imipramine.

A change in the intestinal flora due to the use of antibiotics, such as ampicillin or tetracyclines, can cause a decrease in the level of active substances and, as a result, the effectiveness of the Klimonorm drug. In this regard, an increase in the number of out-of-cycle bleeding was reported.

With concomitant use of cyclosporine, levels of cyclosporin, creatinine and hepatic transaminases may increase due to a decrease in hepatic clearance of cyclosporin.

Due to the effect of estrogen on glucose tolerance (decrease) and the response to insulin, the need for oral antidiabetic agents or insulin dosage may change.

Estrogens may affect the results of certain laboratory tests, such as thyroid function parameters or glucose tolerance.


An overdose is manifested by nausea and vomiting. in case of a serious overdose detected within 2-3 hours, it is recommended to induce vomiting. special antidotes do not exist; symptomatic overdose treatment.

Storage conditions

At a temperature not exceeding 25 ° C.

Tags: Klimonorm