CLIMEN ® - Estradiol + Ciproterone

CLIMEN ® a drug based on estradiol valerate + cyproterone acetate

THERAPEUTIC GROUP: Female sexual hormones - Progestin and estrogens

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications CLIMEN ® - Estradiol + Ciproterone

CLIMEN ® used in hormone replacement therapy during menopause and in the postmenopausal age.

This drug can also be used in the prevention of osteoporosis in high-risk postclimating age women.

Mechanism of action CLIMEN ® - Estradiol + Cyproterone

The combination of estrogens and progestins that we find in drugs dedicated to improving symptoms in the post-climacteric age such as CLIMEN ® is particularly important in contributing to the maintenance of a good quality of life even in this period.

The drastic decrease in estrogen that accompanies menopause in fact results in a series of vasomotor symptoms, such as hot flashes, and neurological symptoms such as insomnia, alterations in mood and depression that represent a biological and social problem.

Furthermore, the absence of these hormones induces a metabolic reshaping at the bone level, such as to significantly increase resorption in the face of a limited osteo-deposition process, which contributes to the onset of chronic and disabling diseases such as osteoporosis.

The exogenous intake of estrogens in this phase of life, can compensate for the endogenous deficiency, significantly improving the symptoms but at the same time leading to an uncontrolled growth of endometrial cells able to promote hyperplasia and neoplastic transformations.

In this regard, hormone replacement therapy also uses progestogens and active ingredients such as cyproterone, which with an antiandrogenic and progestin activity allow to control endometrial growth, reducing both the incidence of malignant transformations and the onset of side effects such as hirsutism or acne.

Studies carried out and clinical efficacy

1. STUDY ATTEMPTS

Study attempt on the cardiovascular effects of female sex hormones, carried out on women undergoing hormone replacement therapy. Unfortunately the study did not bring statically significant results given the numerous interruptions recorded following the appearance of side effects.

2. THE SUBSTITUTE HORMONAL THERAPY IN PROGRESS OF DIABETES

Study that demonstrates how hormone replacement therapy based on cyproterone and estradiol, can be particularly indicated in patients also suffering from type 1 diabetes, given the positive metabolic effects on glucose control

3. REPLACEMENT ORMONAL THERAPY AND ADIPOSITY

Hormone replacement therapy has been shown to be effective in reducing weight gain with predominantly central adipose distribution described following the arrival of the menopausal period.

Method of use and dosage

CLIMEN ®

white-coated tablets of 2 mg estradiol valerate;

pink coated tablets of 2 mg estradiol valerate and 1 mg of cyproterone acetate:

the dosing schedule involves taking a white tablet every day at the same time for the first 11 days, followed by a pink tablet for the next 10 days.

Recruitment cycles are interspersed with a period of weekly withdrawal, in which suspension bleeding similar to menstruation could occur.

Compliance with this scheme is simplified by the graphic constitution of the blister, which allows to minimize possible errors.

Warnings CLIMEN ® - Estradiol + Cyproterone

The assumption of sex hormones must necessarily be preceded by a careful medical-gynecological examination aimed at assessing the prescriptive appropriateness and the possible presence of conditions capable of increasing the incidence of side effects.

In this regard, women with a predisposition to the development of neoplastic and thromboembolic diseases, such as leiomyomas (uterine fibroids) or endometriosis, a history of thromboembolic disorders, risk factors for estrogen-dependent tumors, eg. hereditary predisposition (1st degree relatives with breast cancer), hypertension, liver disease, diabetes mellitus with or without vascular involvement, cholelithiasis, migraine or headache (severe), systemic lupus erythematosus, history of endometrial hyperplasia, epilepsy, and osteosclerosis, they should carefully evaluate with their doctor the cost / benefit ratio that would result from taking CLIMEN ® and opt for this type of therapy, only when the advantages are really significant and any side effects that can be easily diagnosed and managed.

CLIMEN ® contains lactose so that its intake in patients with lactase enzyme deficiency, glucose / galactose malabsorption or lactose intolerance, may be associated with severe gastrointestinal disorders.

PREGNANCY AND BREASTFEEDING

The intake of CLIMEN ® contraindicated during pregnancy, given the potential side effects of estrogen on the health of the fetus.

In addition, the ability of estradiol and cyproterone to permeate the breast filter and concentrate in breast milk, extends the aforementioned contraindication even to the subsequent breastfeeding period.

Interactions

The hepatic metabolism to which both estradiol and cyproterone are subjected exposes the patient in therapy with CLIMEN ® possible clinically relevant drug interactions.

More precisely, the concomitant intake of active ingredients capable of modulating the normal activity of cytochromial enzymes, such as primidone, phenytoin, barbiturates, carbamazepine (used to treat epilepsy), rifampicin (used to treat tuberculosis), ampicillin, tetracycline, griseofulvin (antibiotics used for the treatment of infectious diseases), ritonavir, modafinil and sometimes St. John's wort (hypericum perforatum) could induce an increased metabolism of the hormones contained in CLIMEN ® reducing its therapeutic efficacy.

It is useful to remember how the assumption of sex hormones could determine variations in some laboratory parameters related to thyroid, hepatic, renal and adrenal function.

Contraindications CLIMEN ® - Estradiol + Cyproterone

CLIMEN ® contraindicated in case of hypersensitivity to the active ingredient or to one of its excipients, in case of vaginal bleeding of unknown origin, breast cancer or estrogen-progestin dependent tumors, changes in liver and kidney function, existing or previous thromboembolic processes

Undesirable effects - Side effects

Hormone replacement therapy is often a source of numerous side effects from the different clinical course and from the different frequency of incidence.

Among the most frequent but fortunately clinically insignificant and readily regressive side effects it has been possible to observe weight gain, migraine and headache, abdominal pain, nausea, alterations in menstrual flow, dyspepsia, dizziness, increased breast tension and tenderness.

More rare were cases of anxiety, changes in mood, hirsutism, acne, asthenia, cholelithiasis and pancreatitis.

However, what is of most concern is the increased incidence of embolic, cardiovascular and tumor thrombus episodes, which has been correlated with long-term use of sex hormones.