FILENA ® - Estradiol + Medroxyprogesterone

FILENA ® is a drug based on estradiol valerate + medroxyprogesterone acetate

THERAPEUTIC GROUP: Female sexual hormones - Progestin and estrogen, biphasic combination

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

Indications FILENA ® - Estradiol + Medroxyprogesterone

FILENA ® is a drug used as a hormone replacement therapy in ovariectomized women or in post-climacteric age, with vasomotor and neurological symptoms.

Mechanism of action FILENA ® - Estradiol + Medroxyprogesterone

FILENA ® owes its therapeutic action to the simultaneous presence of an estrogen such as estradiol and a progestogen such as medroxyprogesterone.

Successfully used in the treatment of post-climacteric symptomatology, it allows the control of vasomotor and neurological disorders due to the lack of estrogen that occurs in physiological conditions such as menopause or pathological conditions as a result of ovariectomy.

The presence of the progestin, as well as contributing to the maintenance of the correct hormonal pattern, reduces some of the most serious side effects associated with estrogen therapy such as the uncontrolled proliferation of endometrial cells and the consequent hyperplasia, often a forerunner of frank carcinomas.

The previously described therapeutic action is associated with a particularly important preventive approach to bone health, able to rebalance the relationship between resorption and neodeposition avoiding the onset of chronic and disabling conditions such as osteoporosis.

Studies carried out and clinical efficacy

1. ESTRADIOLO / MEDROSSIPROGESTERONE AND SOMATOTROPO AXIS

Work evaluating the influence of estradiol and medroxyprogesterone taken in combination on the somotatropo axis in post-menopausal women. Although there has been an increase in the bioavailability of IGF 1, this is within the physiological limits.

2. MEDROSSIPROGESTERONE AND HEALTH HEALTH

Experimental study demonstrating that taking high-dose medroxyprogesterone could aggravate the condition of oxidative stress and ventricular dysfunction in rats with previous myocardial infarction.

3. ESTRADIOLO / MEDROSSIPROGESTERONE AND LIPID PROFILE

The low dose cyclical intake of estradiol and medroxyprogesterone was found to be effective in improving the lipidemic profile of post-menopausal patients, reducing the risk of developing coronary heart disease.

Method of use and dosage

FILENA ®

white coated tablets of 2 mg estradiol valerate

light blue coated tablets of 2 mg estradiol valerate and 10 mg of medroxyprogesterone acetate:

the biphasic formulation of FILENA ® imposes a precise therapeutic scheme consisting in taking a white tablet for 11 days followed by taking a celestial tablet for the 10 consecutive days.

The intake cycles must necessarily be interspersed with a drug-free week in which suspension bleeding should occur similar to the physiological menstruation.

Given the half-life of the two active ingredients, estimated at around 24 hours, the tablets should be taken every day at the same time.

Warnings FILENA ® - Estradiol + Medroxyprogesterone

The biological and therapeutic importance of hormone replacement therapy, the numerous side effects, potentially dangerous and the need for specialized medical supervision require a careful medical-gynecological examination before taking FILENA ®

This visit should be directed towards ascertaining the absence of conditions predisposing to the development of thromboembolic, carcinomatous and hepatic diseases, whose incidence tends to increase during hormone replacement therapy.

More precisely, the presence of leiomyomas (uterine fibroids) or endometriosis, a history of thromboembolic disorders, risk factors for estrogen-dependent tumors, e.g. 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, it represents a potential risk factor for which it would be necessary to carefully evaluate the cost / benefit ratio, opting for the therapeutic option only when it can be easily managed and monitored through periodic checks.

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

PREGNANCY AND BREASTFEEDING

Although the scientific literature has not yet produced studies able to characterize the safety profile of estrogens when pregnant, the use of FILENA ® is contraindicated during pregnancy given some experimental work conducted on laboratory animals, in which a potential teratogenic effect of these hormones taken at high doses.

The aforementioned contraindication also extends to the subsequent breastfeeding period given the presence of pharmacokinetic studies that show that both estradiol and medroxyprogesterone can permeate the breast filter and concentrate in breast milk.

Interactions

The hepatic metabolism to which both estradiol and medroxyprogesterone are subjected, significantly increases the risk of possible pharmacologically relevant interactions.

Indeed, metabolic inducers of cytochromial enzymes such as primidone, phenytoin, barbiturates, carbamazepine (used to treat epilepsy), rifampicin (used to treat tuberculosis), ampicillin, tetracycline, griseofulvin (antibiotics used to treat infectious diseases), ritonavir, modafinil and sometimes St. John's wort (hypericum perforatum), could, if taken together with FILENA ® reduce blood concentrations of estradiol and medroxyprogesterone, significantly reducing the therapeutic efficacy of the drug.

It is also useful to remember that the use of sex hormones could cause variations in some laboratory values related to thyroid, hepatic, renal and adrenal function.

Contraindications FILENA ® - Estradiol + Medroxyprogesterone

FILENA ® is 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-progestogen dependent tumors, changes in liver and kidney function, current or previous thromboembolic processes

Undesirable effects - Side effects

Hormone replacement therapy is often associated with the appearance of side effects from the different clinical course.

In particular among the most frequent adverse reactions, but fortunately of low clinical relevance, it is possible to describe: nervousness and alterations of the state of the mood, migraine, palpitations, nausea, occasional bleeding spotting, edema and weight gain.

However, the various cases of breast cancer, endometrial carcinoma, cardiovascular and thromboembolic diseases, gallbladder lithiasis and pancreatitis most frequently observed in patients receiving female sex hormones are of particular concern.