Livial

Livial is a medication used in the development of climacteric syndrome in women.

The drug helps to stabilize the function of the hypothalamus-pituitary structure during menopause in women. This occurs by providing estrogenic (female-type gonadosteroids), progestogenic (hormones whose effect is similar to the activity of the corpus luteum), and weak androgenic (male-type gonadosteroids) therapeutic activity. [ 1 ]

Indications Livial

It is used to treat signs of surgical or natural menopause (absence of menstruation due to natural age-related factors or due to appropriate surgery).

Release form

The medicinal element is released in tablets with a volume of 2.5 mg - 28 pieces per pack.

Pharmacodynamics

During postmenopause, a daily dose of 2.5 mg of the drug inhibits the secretion of gonadotropins (pituitary hormones that stimulate the activity of the glands) and does not stimulate endometrial proliferation processes (an increase in the number of cells in the inner uterine layer associated with reproduction). At the same time, the drug prevents bone loss during postmenopause, reduces the severity of vasomotor disorders (sweating and hot flashes) and has a positive effect on libido and mood. In addition, it has a stimulating effect on the vaginal mucosa. [ 2 ]

In women during the fertile period, the drug slows ovulation (inhibits the process of a mature egg leaving the ovary). [ 3 ]

Pharmacokinetics

After oral administration, tibolone is absorbed at a high rate. Due to the high rate of metabolic processes, the plasma level of tibolone is extremely low. Plasma values of the tibolone Δ4-isomer are also low. Because of this, individual pharmacokinetic properties cannot be identified. The plasma level of Cmax of 3α-OH- and 3β-OH-metabolic components is quite high, but accumulation of the substance does not occur.

Excretion of the substance is mainly realized in the form of conjugated (mostly with the help of sulfates) metabolic elements. Some part of the drug is excreted in urine, but it is mainly excreted in feces.

Food intake does not significantly affect the absorption of the drug.

The pharmacokinetics of tibolone with its metabolic components is not linked to renal activity.

Dosing and administration

The introduction of the drug begins after a year has passed since the last natural menstruation. In case of earlier initiation of drug use, irregular bleeding may occur.

The medication is taken 1 tablet per day (2.5 mg). It is recommended to take them at the same time.

The condition usually improves after a few weeks, but the maximum effect is observed when therapy is continued for at least 3 months. Treatment can be continued in the recommended doses for longer periods.

The tablets are taken starting from the top row, which is outlined in a frame. The first tablet should be the one marked with the required day of the week. Then they are taken one at a time per day in the order indicated by the arrow on the plate, until the entire package is used.

Exceeding the prescribed dosage may cause vaginal bleeding. If it is necessary to administer increased doses, a gestagen (a substance that contains hormones of the corpus luteum or their artificial analogues) should be additionally used - for example, in 10-day cycles every 3 months.

In case of transferring a patient to Livial from another hormone replacement drug, it is necessary to first induce withdrawal bleeding by prescribing a progestogen (a drug containing substances that precede the hormones of the corpus luteum or their artificial analogues). This will help eliminate any endometrial hyperplasia that may already exist.

During therapy, the patient needs to undergo periodic medical examinations.

• Application for children

There is no information regarding the use of drugs in pediatrics.

Use Livial during pregnancy

It is prohibited to use Livial during pregnancy.

Contraindications

Main contraindications:

• diagnosed presence of a neoplasm of hormonal nature or suspicion of it;
• disorders of cerebrovascular or cardiovascular etiology (disorders of intracerebral blood flow) - also their presence in the anamnesis;
• uterine bleeding of unknown origin.

The use of the drug should be discontinued in the event of development of symptoms of thromboembolism, changes in the results of functional liver tests, or the appearance of cholestatic jaundice.

Caution is required when administering the drug in cases of epilepsy, renal dysfunction, or migraine (also if present in the anamnesis). If the drug is used in women suffering from hypercholesterolemia, it is necessary to monitor plasma lipid levels during therapy.

Side effects Livial

Occasionally, taking the drug leads to dizziness, weight changes, vaginal bleeding, seborrheic dermatosis, pretibial edema, headaches, diarrhea, increased facial hair volume, and changes in liver function tests.

In diabetics, the use of Livial may cause a decrease in glucose tolerance and an increase in insulin requirements (or the need for other antidiabetic agents).

Overdose

Acute intoxication can cause vomiting with nausea, as well as vaginal bleeding.

There is no antidote; symptomatic measures are taken if disorders develop.

Interactions with other drugs

Due to the ability of the drug to enhance the fibrinolytic properties of blood, potentiation of the activity of anticoagulants may occur. Such an effect was noted in the case of warfarin. It is necessary to combine the drug with anticoagulants extremely carefully, especially during the periods of the beginning of therapy and after its completion. If necessary, the dosage of warfarin is adjusted.

There are limited data on drug-drug interactions with tibolone. In vivo testing revealed that administration with tibolone modestly alters the pharmacokinetic parameters of the hemoprotein P450 3A4 substrate midazolam. This suggests that the drug may interact with other Cyp3a4 substrates.

Medicines that have a stimulating effect on CYP3A4, including carbamazepine with rifampicin, hydantoin and barbiturates, can potentiate the processes of tibolone metabolism and thereby change its medicinal activity.

Plant substances, which contain St. John's wort, promote stimulation of metabolic processes of progestogens with estrogens via CYP3A4. Increased progestogen and estrogen metabolism may provoke a weakening of the effectiveness of the drug and a change in the profile of uterine bleeding.

Storage conditions

Livial should be stored in a place closed to small children. Temperature level – no more than 25°C.

Shelf life

Livial is approved for use within 24 months from the date of sale of the therapeutic product.

Analogues

An analogue of the drug is the medication Tibolone.