CLIMARA ® - Estradiol

CLIMARA ® is a drug based on Estradiol

THERAPEUTIC GROUP: Natural estrogens

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

Indications CLIMARA ® - Estradiol

CLIMARA ® commonly used as a replacement estrogen therapy in menopausal women for a period longer than a year and as a therapeutic and preventive tool for post-menopausal osteoporosis.

Mechanism of action CLIMARA ® - Estradiol

CLIMARA ® a drug based on 17-Beta Estradiol, a hormone that, although synthetically obtained, is structurally and functionally identical to the endogenous one.

The formulation in plasters allows a transdermal absorption of estradiol, which results in a greater systemic bioavailability, given the absence of a first pass metabolism.

Once its action is over, this hormone is metabolized into inactive or totally inactive metabolites from multiple organs, including the liver naturally, and subsequently eliminated via the bile duct.

This hormone, normally produced by the ovaries and released into the circulation tied to proteins known as sex hormon binding protein, acts on target organs and tissues thanks to nuclear receptors for steroid hormones allowing:

Maturation and maintenance of secondary female sexual characteristics;
Endometrial regeneration and proliferation with the related cellular components;
Maintenance of bone health, modulating the processes of re-employment / osteodeposition.

The normal "cyclic" production of this hormone that accompanies women throughout their fertile period, fails with the advent of menopause, leading to the appearance of a complex symptomatology, characterized by neurological symptoms such as depression, sleep disorders, flushes of heat, urological syndrome with vaginal atrophy, long-term pathological manifestations such as osteoporosis and cardiological affections.

It is therefore evident how substitution therapy can significantly affect the improvement of the described symptomatology and the prevention of strongly invalidating pathologies.

Studies carried out and clinical efficacy

1. CLIMARA AND PLASMA LIPID LEVELS

The dermal administration of estradiol has proven to be useful in preventing some cardiovascular accidents in post-menopausal women, increasing both HDL and nitric oxide concentrations.

2. CLIMARA AND QUALITY OF LIFE

Despite the numerous side effects observed for estrogen replacement therapy, which greatly limit its clinical use, the transdermal administration of estradiol in addition to being particularly effective, improving the quality of life of women undergoing therapy, appears to have a lower profile of risk compared to oral therapy.

3. TRANSDERMIC PATCHES AND APPLICATION POINTS

Study evaluating the absorption and bioavailability of estradiol following transdermal intake. From the study it emerges that the most appropriate area for the application of the patch is that of the buttocks, given the bioavailability of the active ingredient, decidedly greater than that observed on the abdomen.

Method of use and dosage

CLIMARA ® estradiol transdermal patch of 3.8 mg (CLIMARA 50) or 25 mg estradiol (CLIMARA 100):

replacement therapy should always be started with the application of lower dose patches and, only after assessing the efficacy and tolerability of the therapy, provide for a possible adjustment of the dosage.

The application of the patch, which has a weekly duration, could follow continuous or cyclical regimes depending on the patient's needs and medical evaluation, always varying the point of application, sparing the skin region at the breast.

Dosages, methods and regimes of use must necessarily be formulated by the doctor after a careful evaluation of the state of health and the clinical picture of the patient.

Warnings CLIMARA ® - Estradiol

The numerous and serious side effects of estrogen replacement therapy impose a very high scrupulousness in the evaluation of the relationship between cost and benefits, recommending the therapy exclusively in those cases in which the climacteric symptomatology significantly affects the quality of life of the patient.

The beginning of the therapeutic procedure should be preceded by a careful medical examination useful for evaluating all risky conditions such as endometriosis, risk for thromboembolic or dependent estrogen diseases, hypertension, liver disease, diabetes, migraine, autoimmune diseases that could increase the danger of therapy.

In the same way the entire treatment period must necessarily be supervised by medical personnel and marked by periodic checks.

It is also useful to remember that estrogen therapy increases the risk of developing breast cancer, endometrial cancer, breast cancer, coronary heart disease and stroke.

PREGNANCY AND BREASTFEEDING

Although from epidemiological studies there are no particular teratogenic and mutagenic effects on the fetus, when accidentally exposed to estrogen, the intake of CLIMARA ® is contraindicated both during pregnancy and in the subsequent period of breastfeeding.

Interactions

Despite the possibility that clinically significant interactions with low dose hormone therapy are achieved, especially when conducted through the use of patches, which minimize the first pass effect, it is necessary to remember how liver enzymes (cytochrome p450 class) deputies to the metabolism of estradiol can be easily induced or inhibited by numerous active ingredients.

The alteration of the normal activity of these enzymes could have repercussions on the efficacy of hormonal therapy, accentuating or reducing the potential therapeutic and collateral effects.

Among the most important inductors it is possible to remember the anticonvulsants and anti-infectives, while among the inhibitors ritonavir and nelfinavir which however seem to increase their activity when taken together with steroids.

Contraindications CLIMARA ® - Estradiol

CLIMARA ® contraindicated during pregnancy and lactation, in patients with estorgeno-dependent carcinomas, breast carcinoma, acute thrombophlebitis, recent embolic thrombus disease,

history of thrombus embolism, liver disease, porphyria, untreated endometrial hyperplasia, undiagnosed vaginal discharge and of course in case of hypersensitivity to the active substance or to one of its excipients.

Undesirable effects - Side effects

The initial phase of treatment with CLIMARA ® is often accompanied by numerous manifestations affecting different organs and systems, which fortunately tend to regress easily with time or with the suspension of therapy.

Among the adverse reactions the most common are: weight changes, increased size and breast tenderness, changes in liver function, impaired glucose tolerance, migraine, palpitations, general malaise, dizziness, depression, libido changes, endometrial hyperplasia, urinary incontinence, cystitis, hypercholesterolemia, dyspnea and rhinitis.

On the other hand, the side effects of long-term hormone replacement therapy, characterized by a slight increase in the risk of developing breast cancer, as highlighted by the Women's Health Initiative study, of the risk of developing endometrial carcinoma in non-hysterectomised women and pathologies vascular.