Climen, dragee, 21pcs

Composition

1 white dragee contains:

Active ingredient:

estradiol valerate 2 mg;

Auxiliary substances:

lactose monohydrate;

corn starch;

povidone 25000;

talc;

magnesium stearate;

sucrose;

povidone 700000 (K700);

macrogol 6000;

calcium carbonate;

wax.

1 pink dragee contains:

Active ingredients:

estradiol valerate 2 mg;

ciproterone acetate 1 mg;

Auxiliary substances:

lactose monohydrate,

corn starch,

povidone 25000 (K25),

talc,

magnesium stearate,

sucrose,

povidone 700000 (K700),

macrogol 6000,

calcium carbonate,

glycerol 85%,

titanium dioxide,

iron oxide red,

iron oxide yellow,

wax.

Pharmacological action

Climen is a combined product containing estrogen (female sex hormones — – estradiol valerate and antiandrogen (a substance that has the opposite effect to the effects of male sex hormones) – ciproterone acetate, which has progestogenic (similar to the action of ovarian corpus luteum hormones) properties.

It is a means of hormone replacement therapy, which makes up for the lack of sex hormones in a woman’s body. It reduces or eliminates the symptoms of menopausal disorders, has a preventive effect against the development of osteoporosis (bone nutrition disorders, accompanied by an increase in its fragility associated with changes in the hormonal background) and cardiovascular diseases.

Estradiol valerate eliminates or reduces symptoms associated with a decrease in premenopausal estrogen levels, such as hot flashes, sweating, sleep disorders, irritability, depressive (depressed) states, memory disorders, vascular crises (a sharp rise in blood pressure), atrophic degenerative changes in the skin and mucous membranes (high fragility of nails, thinning of the skin and formation of wrinkles, dryness of the mucous membranes of the genitourinary tract), osteoporosis and high blood pressure. bone fragility, changes in lipid metabolism, expressed in an increase in the level of LDL (low-density lipoproteins), which cause atherosclerotic changes in blood vessels.

Unlike synthetic estrogens of non-steroidal structure, estradiol valerate has a lesser effect on the protein-synthesizing function of the liver and weakly stimulates the formation of renin.

Ciproterone acetate is an antiandrogenic product; due to its progestogenic properties, it promotes secretory changes in the proliferating epithelium of the uterus and other target organs, which stops the further development of proliferative processes leading to the development of hyperplasia (overgrowth), in particular, the growth of hormonal tumors of a progesterone-deficient (associated with a reduced progesterone content in the body) nature.

Being an active antiandrogen, ciproterone acetate reduces the phenomena of androgenization (the appearance of masculine features in women — voice coarsening, male-type hair loss, etc. ) in patients receiving estrogen replacement therapy due to estrogen deficiency, including against the background of ovariectomy (surgical removal of the ovaries). It has virtually no effect on lipid metabolism, which contributes to a more complete implementation of the preventive effect of estradiol against cardiovascular diseases in the postmenopausal period.

Indications

• menopause in women
• prevention of osteoporosis
• menstrual cycle disorders.

Contraindications

• thrombophlebitis
• acute and chronic liver diseases liver
• tumor
• arterial hypertension.

Side effects

From the side of the reproductive system and mammary glands:  changes in the frequency and intensity of uterine bleeding, breakthrough bleeding, intermenstrual spotting (usually relieved during therapy), dysmenorrhea, changes in vaginal discharge, a condition similar to premenstrual syndrome; soreness, tension, and/or enlargement of the mammary glands.

From the gastrointestinal tract:  dyspepsia, bloating, nausea, vomiting, abdominal pain, recurrent cholestatic jaundice

Skin and subcutaneous tissue disorders:  skin rash, pruritus, chloasma, erythema nodosum

From the central nervous system:  headache, migraine, dizziness, anxiety or depressive symptoms, increased fatigue

Other services:  rapid heartbeat, edema, increased blood pressure, venous thrombosis and thromboembolism, muscle cramps, changes in body weight, changes in libido, visual disturbances, contact lens intolerance, allergic reactions

Interaction

When starting HRT, it is necessary to stop using hormonal contraceptives. If necessary, the patient should be recommended non-hormonal contraceptives.

Long-term treatment with drugs that induce liver enzymes (for example, some anticonvulsants and antimicrobials) can increase the clearance of sex hormones and reduce their clinical effectiveness. A similar property of inducing liver enzymes was found in hydantoins, barbiturates, primidone, carbamazepine, and rifampicin; this feature is also suggested in oxcarbazepine, topiramate, felbamate, and griseofulvin. The maximum induction of enzymes is usually observed no earlier than 2-3 weeks, but then it can persist for at least another 4 weeks after discontinuation of the drug.

In rare cases, concomitant use of certain antibiotics (for example, penicillin and tetracycline groups) resulted in a decrease in estradiol levels.

Substances that are highly conjugated (for example, paracetamol) can increase the bioavailability of estradiol due to competitive inhibition of the conjugation system during absorption.

Due to the effect of HRT on glucose tolerance, the need for oral antidiabetic agents or insulin may change in some cases.

Alcohol interaction

Excessive alcohol consumption during HRT can lead to increased levels of circulating estradiol.

How to take, course of use and dosage

Inside, without chewing, with a small amount of liquid, approximately at the same time,1 tablet per day, starting from the 5th day of the cycle.

After the end of taking the drug from 1 calendar package, make a 7-day break, during which 2-4 days after taking the last dragee, menstrual-like bleeding begins.

If the doctor does not prescribe another therapy, after a 7-day break, start taking the drug from the next calendar package. If there is no bleeding during the 7-day break, treatment is continued only after excluding pregnancy.

Overdose

Symptoms that may occur with an overdose:  nausea, vomiting, and vaginal bleeding.

Treatment:  there is no specific antidote, and the treatment is symptomatic.

Special instructions

Climen is not used for the purpose of contraception.

If contraception is necessary, non-hormonal methods should be used (with the exception of calendar and temperature methods). If pregnancy is suspected, you should stop taking pills until pregnancy is ruled out.

If any of the following conditions or risk factors are present or worsen, the individual risk-benefit ratio should be evaluated before starting or continuing HRT.

Venous thromboembolism

A number of controlled, ranomized, and epidemiological studies have identified an increased relative risk of developing venous thromboembolism (VTE) with HRT, i. e. deep vein thrombosis or pulmonary embolism. Therefore, when prescribing HRT to women with VTE risk factors, the risk-benefit ratio should be carefully weighed and discussed with the patient.

Risk factors for VTE include an individual and family history (the presence of VTE in close relatives at a relatively young age may indicate a genetic predisposition) and severe obesity. The risk of VTE also increases with age. The question of the possible role of varicose veins in the development of VTE remains controversial.

The risk of VTE may temporarily increase with prolonged immobilization, “large” elective and traumatic surgeries, or massive trauma. Depending on the cause or duration of immobilization, the question of whether to temporarily stop HRT should be decided

Treatment should be stopped immediately if symptoms of thrombotic disorders appear or if they are suspected to occur.

Arterial thromboembolism

In randomized controlled trials, long-term use of combined conjugated estrogens and medroxyprogestron acetate did not provide evidence of a positive effect on the cardiovascular system. In large-scale clinical trials of this compound, a possible increase in the risk of coronary disease in the first year of use was identified. An increased risk of stroke was also found. To date, no long-term randomized controlled trials have been conducted with other HRT drugs to identify a positive effect on morbidity and mortality rates related to the cardiovascular system. Therefore, it is not known whether this increased risk extends to HRT medications containing other types of estrogens and progestogens.

Endometrial cancer

Long-term estrogen monotherapy increases the risk of developing endometrial hyperplasia or carcinoma.Studies have confirmed that the addition of progestogens reduces the risk of endometrial hyperplasia and cancer.

Breast cancer

Clinical trials and observational studies have shown an increase in the relative risk of developing breast cancer in women who have been using HRT for several years. This may be due to an earlier diagnosis, the biological effect of HRT, or a combination of both. The relative risk increases with increasing duration of treatment and may increase even more with the combination of estrogens and progestogens. This increase is comparable to the increase in the risk of breast cancer in women with each year of delay in the onset of natural menopause, as well as with obesity and alcohol abuse. The increased risk gradually decreases to normal levels during the first few years after stopping HRT.

According to most studies, breast cancer detected in women who take HRT is usually more differentiated than in women who do not take it.

HRT increases mammographic density of the mammary glands, which in some cases can have a negative impact on the X-ray detection of breast cancer.

Liver tumor

Against the background of the use of sex steroids, which also include HRT products, in rare cases benign, and even less often malignant liver tumors were observed. In some cases, these tumors have resulted in life-threatening intra-abdominal bleeding. If there is pain in the upper abdomen, an enlarged liver, or signs of intra-abdominal bleeding, the differential diagnosis should take into account the likelihood of a liver tumor.

Cholelithiasis

Estrogens are known to increase the lithogenicity of bile. Some women are predisposed to developing cholelithiasis when treated with estrogens.

Other states

Treatment should be stopped immediately if migraine-like or frequent and unusually severe headaches occur for the first time, as well as if other symptoms appear – possible harbingers of a thrombotic stroke of the brain.

The relationship between HRT and the development of clinically pronounced arterial hypertension has not been established. A slight increase in blood pressure has been reported in women taking HRT, but clinically significant increases are rare. However, in some cases, if persistent clinically significant arterial hypertension develops while taking HRT, discontinuation of HRT may be considered.

Patients with mild hepatic impairment, including various forms of hyperbilirubinemia, such as Dubin-Johnson syndrome or Rotor syndrome, should be monitored by a doctor, as well as periodic studies of liver function. If liver function indicators worsen, HRT should be discontinued.

If there is a recurrence of cholestatic jaundice or cholestatic pruritus observed for the first time during pregnancy or previous treatment with sex steroid hormones, HRT should be stopped immediately.

Special monitoring is necessary for women with moderately elevated triglyceride levels. In such cases, the use of HRT can cause a further increase in the level of triglycerides in the blood, which increases the risk of acute pancreatitis.

Although HRT can affect peripheral insulin resistance and glucose tolerance, there is usually no need to change the treatment regimen for patients with diabetes mellitus during HRT. However, women with diabetes should be monitored during HRT.

Some patients may develop undesirable manifestations of estrogen stimulation, such as abnormal uterine bleeding, under the influence of HRT. Frequent or persistent abnormal uterine bleeding during treatment is an indication for endometrial examination.

If treatment of irregular menstrual cycles does not give results, an examination should be performed to exclude organic diseases.

Under the influence of estrogens, uterine fibroids can increase in size. In this case, the treatment should be discontinued.

It is recommended to stop treatment if a relapse of endometriosis develops on the background of HRT. If the presence of prolactinoma is suspected, this disease should be excluded before starting treatment.

In some cases, chloasma may occur, especially in women with a history of pregnancy chloasma. During HRT, women with a tendency to develop chloasma should avoid prolonged exposure to the sun or ultraviolet radiation.

The following conditions may occur or worsen with HRT. Although their relationship to HRT has not been proven, women with these conditions should be under medical supervision when undergoing HRT: epilepsy; benign breast tumor; bronchial asthma; migraine; porphyria; otosclerosis; systemic lupus erythematosus, chorea minor.

Medical examination and counseling

Before starting or resuming HRT, a woman is recommended to undergo a thorough general medical and gynecological examination (including breast examination and cytological examination of cervical mucus), to exclude pregnancy. In addition, violations of the blood coagulation system should be excluded. Follow-up examinations should be carried out periodically.

Influence on the results of laboratory tests

The use of sex steroids can affect the biochemical parameters of liver, thyroid, adrenal and kidney function, the content of transport proteins in plasma, such as corticosteroid-binding globulin and lipid/lipoprotein fractions, indicators of carbohydrate metabolism, coagulation and fibrinolysis.

Influence on the ability to drive motor vehicles and manage mechanisms

It doesn’t affect you.

Form of production

Two types of dragees

Storage conditions

Keep out of reach of children. Under normal conditions.

Shelf life

5 years

Active ingredient

Ciproterone, Estradiol

Conditions of release from pharmacies

By prescription

Dosage form

dragees

Purpose

Adults as prescribed by a doctor, For postmenopausal women

Indications

Menstrual disorders, Menopause