menopause

LIVIAL® - Tibolone

LIVIAL ® is a drug based on Tibolone

THERAPEUTIC GROUP: Synthetic estrogens

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

Indications LIVIAL ® - Tibolone

LIVIAL ® is indicated in the treatment of post-menopausal symptoms and in the prevention of female osteoporosis due to estrogen deficiency.

Mechanism of action LIVIAL ® - Tibolone

The tibolone contained in LIVIAL ® is a synthetic steroid with estrogenic, progestin and androgenic properties, belonging to the STEAR family, ie selective regulators of tissue estrogenic activity

Taken orally it is rapidly absorbed at the intestinal level and metabolized through hydroxylation processes into three different active ingredients, responsible for the aforementioned biological properties.

Among these the metabolite endowed with estrogenic activity seems to be the one responsible for the therapeutic capacities interacting selectively with the estrogenic receptors present at the tissue level and mimicking the action of endogenous hormones, lacking during menopause.

Experimental studies show that the therapeutic effects of tibolone on vasomotor disorders and vaginal dryness can be comparable to those of replacement estrogen therapy in the face of a better endometrial safety profile and adequate control over sexual disorders, guaranteed by androgenic activity of some of its metabolites.

Different studies conducted both in the clinical phase and on experimental models have also shown a control action on some mechanisms involved in the development of breast cancer such as the enzymatic inhibition of metabolic pathways falling within the estrogenic synthesis and the activation of apoptotic processes of mammary carcinomatous cells .

Studies carried out and clinical efficacy

1. TIBOLONE AND MAMMARY CARCINOMA

A very interesting study that shows that although tibolone can reduce the incidence of breast cancer compared to classical estrogen therapy, the risk of developing breast cancer in patients exposed to tibolone remains about 1.5 times higher than in the control (no drug)

2. CLINICAL EFFECTIVENESS OF THE TIBOLONE

An important study that has shown that in post-menopausal women suffering from osteoporosis, the daily intake of tibolone has significantly reduced the risk of developing new vertebral fractures.

3. TIBOLONE AND ENDOMETRIC HEALTH

Despite numerous studies seem to agree on the absence of side effects at the endometrial level, guaranteed by the presence of metabolites with progestin activity, quite recent evidences have shown how tibolone therapy can increase the risk of developing endometrial carcinomas compared to estrogen-progestin therapy .

Method of use and dosage

LIVIAL ® tibolone 2.5 mg tablets:

therapy for the treatment of symptoms related to menopause should be started with the lowest possible dose useful to ensure improvement of symptoms.

Generally the administration of one tablet a day should be sufficient to produce the expected therapeutic effect.

All treatment must necessarily be supervised by medical personnel.

The presence of tibolone metabolites endowed with progestational activity make it possible to avoid the simultaneous intake of a progestin.

Warnings LIVIAL ® - Tibolone

Tibolone therapy should be preceded by a careful medical examination to assess the presence of predisposing conditions incompatible with the intake of LIVIAL ®

Endometriosis, thromboembolic or estrogen-dependent diseases of leiomyoma, hypertension, liver disease, diabetes, migraine, cardiovascular disease, liver and kidney disease, bronchial asthma and allergic diseases are just some of the conditions for which particular care should be taken.

The patient must be informed of the potential risks, especially cardiovascular, related to the administration of LIVIAL ® and decide with her doctor to undertake this therapeutic process only after having carefully evaluated the cost / benefit ratio.

PREGNANCY AND BREASTFEEDING

The presence in the literature of experimental studies conducted on laboratory animals in which a reproductive toxicity of the tibolone was observed led the various international agencies to contraindicate the intake of LIVIAL ® both during the entire pregnancy and in the subsequent period of breastfeeding.

Interactions

The hepatic metabolism of tibolone, supported by the enzymatic family of p450 cyto-hormones, makes this active principle particularly subject to pharmacokinetic changes induced by the concomitant intake of inhibitors and inducers of the aforementioned enzymes.

In addition, the fibrinolytic activity of tibolone may potentiate the anticoagulant effects of warfarin, thereby increasing the risk of bleeding.

Contraindications LIVIAL ® - Tibolone

LIVIAL ® is contraindicated in cases of untreated endometrial hyperplasia, venous thromboembolism, hepatopathy, porphyria, estrogen-dependent tumors, vaginal bleeding, breast cancer and related predisposing conditions, pregnancy and lactation and hypersensitivity to the active substance or to one of its excipients.

Undesirable effects - Side effects

Tibolone therapy is decidedly more tolerated than that with natural estrogens and characterized by a significantly lower overall risk of neoplastic development.

Among the most common reactions, which tend to occur more frequently in patients predisposed or following prolonged therapies, we observed:

  • Gastrointestinal disorders: nausea, vomiting, diarrhea and abdominal cramps;
  • Skin disorders due to hypersensitivity to the active ingredient;
  • Reproductive system disorders: bleeding, itching, viral and bacterial infections, pain etc;
  • Nervous disorders: headache, migraine, depression and behavioral alterations.

Among the most important and dangerous side effects, there is the increased cardiovascular risk characterized by stroke, venous thromboembolism and myocardial infarction.

Note

LIVIAL ® is salable only under medical prescription.

The use of LIVIAL ® without any medical needs before and during the competition is doping practice.