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Climen® [Cyproterone, Estradiol]

Bayer Pharma AG
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Clinical Pharmacology

Climen contains estrogen - estradiol valerate, which in the human body turns into natural 17β-estradiol. Also in the preparation Climen is a derivative of progesterone - cyproterone acetate, which has a gestagenic, antigonadotropic and antiandrogenic effect.

Due to the composition and cyclic regimen of Climen®e, (taking estrogen only for 11 days, then a combination of estrogen and progestogen for 10 days, and finally, a 7-day break), women with an unreduced uterus with a regular intake of the drug set the menstrual cycle .

On the background of Climen®e's reception, there is no suppression of ovulation, and hormone production in the body remains almost unchanged. Climen can be used by women of reproductive age for the regulation of the menstrual cycle, as well as women in perimenopause for the treatment of irregular uterine bleeding.

Estradiol compensates for the lack of estrogen in the female body after menopause and provides effective treatment of psycho-emotional and autonomic menopausal symptoms (such as hot flashes, increased sweating, sleep disturbances, increased nervous irritability, irritability, palpitations, cardialgia, dizziness, headache, depression, cardiac irritation, irritability, palpitations, cardialgia, dizziness, headache. libido, muscle and joint pain); involutions of the skin and mucous membranes, especially the mucous membranes of the urogenital system (urinary incontinence, dryness and irritation of the vaginal mucosa, pain during sexual intercourse).

Estradiol prevents bone loss caused by estrogen deficiency. This is mainly due to the suppression of osteoclast function and the shift of the bone remodeling process towards bone formation. It has been proven that prolonged use of hormone replacement therapy (HRT) reduces the risk of peripheral bone fractures in women after menopause. With the abolition of HRT, the rate of decrease in bone mass is comparable to the indicators characteristic of the period immediately after menopause. It is not proved that, using HRT, it is possible to achieve recovery of bone mass to the premenopausal level.

HRT also has a beneficial effect on the collagen content in the skin, as well as on its density, and can also slow down the formation of wrinkles.

In addition, due to the antiandrogenic properties of cyproterone acetate, Climen has a therapeutic effect on androgen-dependent diseases such as acne, seborrhea, androgenetic alopecia.

Taking Climen®e leads to a decrease in total cholesterol, low-density lipoprotein (LDL) and an increase in high-density lipoprotein (HDL), which significantly increases the ratio of HDL / LDL, as well as increased triglycerides. Due to the lack of androgenic properties of cyproterone acetate, it practically does not interfere with the effect of estradiol on lipid metabolism. The effect of Climen®e is especially noticeable in women with pronounced atherogenic changes in the lipid profile.

The addition of cyproterone acetate for 10 days each cycle prevents the development of hyperplasia and endometrial cancer.

Observational studies suggest that among postmenopausal women, the incidence of colon cancer is reduced when using HRT. The mechanism of action is still unclear.


Estradiol Valerate


After oral ingestion of estradiol, valerate is rapidly and completely absorbed. During absorption and first passage through the liver, the hormone ester is broken down into estradiol and valeric acid. At the same time, estradiol is largely subjected to further metabolization, for example, to estrone, estriol, and estrone sulfate. After oral administration, the bioavailability of estradiol is about 3%. Eating does not affect the bioavailability of estradiol.


The maximum serum estradiol concentration of approximately 30 pg / ml is usually reached 4–9 hours after taking the pills. 24 hours after administration, serum estradiol concentration decreases to a concentration of approximately 15 pg / ml.

Estradiol binds to albumin and sex hormone-binding globulin (SHBG). The free fraction of estradiol in serum is about 1-1.5%, and the fraction of the SHBH-bound substance is in the range of 30-40%.

The apparent volume of distribution of estradiol after a single intravenous injection is about 1 l / kg.


After hydrolysis of exogenous estradiol valerate, the substance passes through the same pathways of biotransformation as endogenous estradiol. Estradiol is metabolized mainly in the liver, and also partially in the intestine, kidneys, skeletal muscles and target organs. These processes are accompanied by the formation of estrone, estriol, catechol estrogen, as well as sulfate and glucuronide conjugates of these compounds, all of which have significantly less estrogenic activity or no estrogenic activity at all.


Serum estradiol clearance after a single intravenous administration is characterized by a high degree of variability in the range from 10 to 30 ml / min / kg. A certain part of estradiol is excreted in the bile and undergoes enterohepatic recycling. Estradiol metabolites are excreted mainly in the urine in the form of sulfates and glucuronides.

Equilibrium concentration

The concentration of estradiol in the serum after repeated administration is approximately two times higher than after the administration of a single dose. On average, serum estradiol concentration ranges from 40 pg / l (minimum level) to 90 pg / l (maximum level). The concentration of estrone (weaker estrogen) is about 8 times, and the concentration of estrone sulfate is about 150 times higher than the concentration of estradiol. After discontinuation of Climen, estradiol and estrone levels return to their original values ​​within two to three days.

Cyproteronea acetate


After ingestion, a wide range of doses of cyproteran acetate is quickly and completely absorbed. Absolute bioavailability after oral administration is 88%.


The maximum concentration of cyproterone acetate in serum, which is about 30 ng / ml, is achieved 1–2 hours after a single dose of 1 mg of cyproterone acetate. After that, there is a two-phase decrease in serum concentration of cyproterone acetate with a half-life of 0.8 hours and 2.3 days, respectively.

Cyproterone acetate binds almost exclusively to serum albumin. About 3.5-4% of the total serum concentration of cyproterone acetate is not associated with protein. Because plasma protein binding is not specific, changes in HSPG levels do not affect the pharmacokinetics of cyproterone acetate.


Cyproterone acetate is metabolized in various ways, including hydroxylation and conjugation. The main metabolite in human serum is the 15β-hydroxyl derivative.


Serum cyproterone acetate clearance is 3.6 ml / min / kg. Some of the dose received is excreted unchanged with the bile. Most of the dose is excreted in the form of metabolites with urine and bile in the ratio of 3: 7, with a half-life of 1.9 days. Metabolites are excreted from serum with a similar half-life of 1.7 days.

Equilibrium concentration

Due to the long serum half-life of cyproterone acetate from serum, it can be expected that the serum concentration of cyproterone acetate in the course of one drug administration cycle will increase 2-2.5 times.


  • hormone replacement therapy (HRT) for menopausal disorders, involutional changes of the skin and urinary tract, menopausal depressions, as well as estrogen deficiency symptoms due to natural menopause or hypogonadismsterilization or primary ovarian dysfunction in women with an unreduced uterus;
  • prevention of postmenopausal osteoporosis;
  • normalization of irregular menstrual cycles;
  • treatment of primary or secondary amenorrhea.


1 white bean contains:

Active substance: estradiol valerate 2 mg;

Excipients: lactose monohydrate; corn starch; Povidone 25,000; talc; magnesium stearate; sucrose; Povidone 700,000 (K700); macrogol 6000; calcium carbonate; wax.

1 pink bean contains:

Active substances: estradiol valerat2 mg; cyproterone acetate 1 mg;

Excipients: 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.

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Climen® [Cyproterone, Estradiol]

Dosage and Administration

At one dose - 5 pellets (keep in the mouth until completely dissolved - not during the meal), take 2 times a day, morning and evening.

Depending on the severity of the symptoms, it is possible to increase the drug intake up to 3-4 times a day. The recommended duration of use of the drug is 6 months. Perhaps repeated courses of treatment on the recommendation of a doctor.

Adverse reactions

Allergic reactions are possible.

Hypersensitivity to the drug.

Special instructions

During the course of treatment with a drug, it is recommended to consult with your doctor at least once every 2 months for the possible correction of therapy.

  • Brand name: Climax
  • Active ingredient: Homeopathic composition
  • Dosage form: Homeopathic granules.
  • Manufacturer: Materia Medica
  • Country of Origin: Russia

Studies and clinical trials of Cyproterone, Estradiol (Click to expand)

  1. Simultaneous spectrophotometric determination of cyproterone acetate and ethinyl estradiol in tablets using continuous wavelet and derivative transform
  2. Long-term sequential treatment with combined estradiol valerate and cyproterone acetate in early postmenopause
  3. Influence of cyproterone acetate and estradiol on cell kinetics in the sebaceous gland of the golden hamster ear
  4. Effect of cyproterone acetate-ethinyl estradiol treatment on the proportions of linoleic and sebaleic acids in various skin surface lipid classes
  5. Therapy of androgenetic symptomatology with cyproterone acetate and ethinyl estradiol
  6. The effect of ethinyl estradiol–cyproterone acetate treatment on homocysteine levels in women with polycystic ovary syndrome
  7. Alteration of cardiovascular risk parameters in women with polycystic ovary syndrome who were prescribed to ethinyl estradiol–cyproterone acetate
  8. The Local Effects of Topically Applied Estradiol, Cyproterone Acetate, and Ethanol on Sebaceous Secretion in Intact Male Rats.
  9. Proliferation of lamellar whorls in arcuate neurons of the hypothalamus of male rats treated with estradiol benzoate or cyproterone acetate
  10. Estrogen-induced sexual receptivity and localization of 3H-estradiol in brains of female mice: Effects of 5α-reduced androgens, progestins and cyproterone acetate
  11. Cyproterone acetate/ethinyl estradiol in the treatment of acne. A comparative dose-response study of the estrogen component
  12. Testosterone-estradiol binding globulin (TeBG) in hirsute patients treated with cyproterone acetate (CPA) and percutaneous estradiol
  13. Does vitamin D3 have negative effects on serum levels of lipids? A follow-up study with a sequential combination of estradiol valerate and cyproterone acetate and/or vitamin D3
  14. Combined use of metformin and ethinyl estradiol–cyproterone acetate in polycystic ovary syndrome
  15. Effects of metformin versus ethinyl-estradiol plus cyproterone acetate on ambulatory blood pressure monitoring and carotid intima media thickness in women with the polycystic ovary syndrome
  16. Comparison of effects of 3 mg drospirenone plus 20 μg ethinyl estradiol alone or combined with metformin or cyproterone acetate on classic metabolic cardiovascular risk factors in nonobese women with polycystic ovary syndrome
  17. Effect of estradiol valerate alone or in association with cyproterone acetate upon vascular function of postmenopausal women at increased risk for cardiovascular disease
  18. Hormone replacement therapy with estradiol valerate and cyproterone acetate:: effects on endothelium-dependent vasodilatation and arterial wall compliance
  19. Effects of estradiol, cyproterone acetate, tibolone and raloxifene on uterus and aorta atherosclerosis in oophorectomized cholesterol-fed rabbits
  20. Effects of estradiol alone or in combination with cyproterone acetate on carotid artery pulsatility index in postmenopausal women
  21. Changes in normal lipid profile of menopausal women with combined hormone replacement therapy: Comparative clinical trial of two hormonal combinations (conjugated estrogens/medroxyprogesterone acetate versus estradiol valerate/cyproterone acetate)
  22. Flutamide versus a cyproterone acetate-ethinyl estradiol combination in moderate acne: a pilot randomized clinical trial
  23. Effects of ethinyl estradiol combined with desogestrel and cyproterone acetate on glucose tolerance and insulin response to an oral glucose load: A one-year randomized, prospective, comparative trial
  24. Treatment of hirsutism by an association of oral cyproterone acetate and transdermal 17β-estradiol

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