SYSTEN ® - Estradiol

SYSTEN ® is a drug based on Estradiol

THERAPEUTIC GROUP: Natural estrogens

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

Indications SYSTEN ® - Estradiol

SYSTEN ® is used in the treatment of symptoms associated with estrogen deficiency typical of menopause or surgically induced.

The use of SYSTEN ® has also proved effective in preventing post-climacteric pathological complications such as osteoporosis.

Mechanism of action SYSTEN ® - Estradiol

SYSTEN ® is a drug able to guarantee the transdermal intake of estradiol, thus making up for the endogenous deficiency of this hormone.

The particular form of administration, useful for eliminating the first pass phase, is able to guarantee constant hormonal concentrations for about 3-4 days thus allowing estradiol to perform its biological functions.

Linked to specific transport globulins, estradiol reaches target cells by interacting with specific nuclear receptors capable of reprogramming gene expression, and therefore its biosynthetic and functional characteristics.

In macroscopic terms this results in a reduction of the annoying symptomatology characterized by vasomotor disturbances and hot flushes, neurological symptoms such as insomnia, depression and behavioral alterations, and above all in a significant increase in bone density, thus reducing the risk of osteoporosis and pathological fractures .

Transdermal administration and the absence of a first-pass metabolism make therapy safer, reducing both potential drug interactions and related side effects.

Studies carried out and clinical efficacy

1. TRANSDERMIC EXTRADIOL AND INFLAMMATORY RISK

The contradictory effects of estradiol therapy on cardiovascular health are known. In this study, it is shown that the intake of estradiol by transdermal route can significantly limit the increase in concentrations of reactive protein C compared to oral therapy, reducing the cardiovascular risk.

2. SYSTEN AND BODY COMPOSITION

Side effects of estrogen replacement therapy include weight gain due to an increase in fat mass. In this study it was observed that the intake of estradiol through transdermal patches can keep the fat mass unchanged, without altering the oxidizing capacity of the organism and saving the lean mass from the deterioration observed following the oral administration of estradiol

3. SYSTEN AFTER BILATERAL OVARIETY

SYSTEN has been used successfully in the treatment of menopause surgically induced following bilateral oophorectomy for benign genital tumors. Most of the patients treated reported an improvement in symptoms.

Method of use and dosage

SYSTEN ®:

Estradiol 1.6 mg transdermal patch capable of releasing 25mcg of the hormone in 24 hours;
3.2 mg estradiol transdermal patch capable of releasing 50mcg of hormone in 24 hours;
4.8 mg estradiol transdermal patch capable of releasing 75mcg of hormone in 24 hours;
Estradiol 6.4 mg transdermal patch capable of releasing 100mcg of hormone over 24 hours;

the patches should guarantee a controlled release of the hormone for about 3-4 days, at the end of which replacement is necessary.

The therapeutic scheme could follow a continuous or cyclical assumption protocol according to the therapeutic needs of the patient.

The formulation of the aforementioned scheme should be carried out by the doctor after a careful evaluation of the patient's state of health and his clinical picture.

Warnings SYSTEN ® - Estradiol

The biological complexity of a hormone replacement therapy and the presence of potentially dangerous side effects require a careful and scrupulous check-up, useful to ascertain the absence of predisposing factors such as endometriosis, risk for thromboembolic or estrogen dependent diseases, hypertension, liver diseases, diabetes, migraine, autoimmune disorders before starting therapy with SYSTEN ®

Given the seriousness of the potential long-term side effects, the patient must be adequately informed about the real cost / benefit ratio deriving from the estradiol intake, in order to be able to distinguish and recognize the first signs.

PREGNANCY AND BREASTFEEDING

The intake of estradiol in any form during pregnancy and the subsequent period of breastfeeding is strongly contraindicated, despite the presence in the literature of studies showing the absence of direct side effects on fetuses accidentally exposed to estradiol or estrogens.

Interactions

The absence of a first-pass metabolism, given the transdermal intake of estradiol, allows to significantly reduce the risk of clinically relevant drug interactions.

However, the scientific literature shows how the concomitant intake of active ingredients such as barbiturates, hydantoin, carbamazepine, rifampicin, ritonavir etc, capable of inducing or inhibiting cytochromial enzymes could determine pharmacologically relevant alterations of estradiol, varying their biological efficacy.

Contraindications SYSTEN ® - Estradiol

SYSTEN ® is 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

Although transdermal administration of estradiol eliminates the first-pass phase, significantly reducing some of the side effects related to hepatic metabolism of the hormone, estradiol-based therapeutic treatment could be accompanied by acute but time-limited side effects such as 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.

Long-term therapy, on the other hand, could increase the risk of developing breast and endometrial cancer, especially in predisposed women.