Livial

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

The medicine helps to stabilize the function of the hypothalamus-pituitary gland structure during the onset of menopause in a woman. This happens by providing estrogenic (female-type gonadosteroids), progestogenic (hormones whose effect is similar to the activity of the corpus luteum), as well as 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 factors or due to the corresponding operation).

Release form

The release of the drug element is realized in tablets with a volume of 2.5 mg - 28 pieces inside the pack.

Pharmacodynamics

During postmenopausal women, a daily dosage of 2.5 mg of the drug inhibits the secretion of gonadotropins (pituitary hormones that stimulate the activity of the glands) and at the same time does not stimulate the processes of endometrial proliferation (an increase in the number of cells of the inner uterine layer associated with reproduction). At the same time, the drug prevents bone loss in postmenopausal women, 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 fertility, the medication slows down ovulation (inhibits the process of leaving the mature egg from the ovary). [3]

Pharmacokinetics

After oral administration, tibolone is absorbed at high speed. Due to the high rate of metabolic processes, the plasma index of tibolone is extremely low. The plasma values of the tibolone Δ4 isomer are also low. Because of this, individual pharmacokinetic properties cannot be identified. The plasma level of Cmax 3α-OH-, as well as 3β-OH-metabolic components, is quite high, but the 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 of the drug is excreted in the urine, but most of it is excreted in the faeces.

Eating food does not significantly affect the absorption of the medication.

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

Dosing and administration

The introduction of the drug begins after a year has passed since the last natural menstruation took place. In the case of an earlier start of the use of drugs, an irregular appearance of bloody discharge is possible.

The medication is taken in 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 noted with continued therapy for at least 3 months. You can continue treatment in the recommended portions for longer periods.

The use of tablets starts from the top row, which is surrounded by a frame. The first should be the tablet labeled with the required day of the week. Then they are consumed in 1 piece per day in the sequence indicated by the arrow on the plate, until the entire package is used up.

Exceeding the prescribed dosage may cause vaginal bleeding. If the introduction of increased portions is required, progestogen (a substance that contains hormones of the corpus luteum or their artificial analogues) should be additionally applied - for example, in 10-day cycles every 3 months.

In the case of transferring the patient to the use of Livial from another hormone replacement drug, you must first provoke the development of withdrawal bleeding - by prescribing a progestogen (a medication that contains substances preceding the hormones of the corpus luteum, or their artificial analogs). This will help eliminate any existing endometrial hyperplasia.

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

• Application for children

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

Use Livial during pregnancy

It is forbidden to use Livial during pregnancy.

Contraindications

The main contraindications:

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

It is necessary to cancel the use of drugs in the event of the development of symptoms of thromboembolism, changes in the indications of functional liver tests, or the appearance of cholestatic jaundice.

Caution when administering the medication is required in case of epilepsy, renal dysfunction or migraine (also if they have a history). If the drug is used in women suffering from hypercholesterolemia, it is required to monitor plasma lipid levels during therapy.

Side effects Livial

At times, taking the drug leads to dizziness, weight change, vaginal bleeding, seborrheic dermatosis, pretibial swelling, headaches, diarrhea, increased facial hair and changes in liver function values.

In diabetics, the use of Livial can provoke a weakening of glucose tolerance and an increase in insulin demand (or the need for other antidiabetic substances).

Overdose

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

There is no antidote; with the development of disorders, symptomatic actions are performed.

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. Similar effects have been reported with warfarin. It is required to very carefully combine the drug with anticoagulants, especially during the periods of initiation of therapy and after its termination. If necessary, the dosage of warfarin is adjusted.

There is limited information regarding drug pharmacokinetics interactions with tibolone. In vivo tests have shown that administration with tibolone moderately alters the pharmacokinetic parameters of the hemoprotein P450 of the 3A4 substrate midazolam. This allows us to conclude that the drug is capable of interacting with other Cyp3a4 substrates.

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

Herbal substances, which contain St. John's wort, stimulate the metabolic processes of progestogens with estrogens through CYP3A4. An increase in progestogenic and estrogenic metabolism can provoke a weakening of the effectiveness of drugs and a change in the profile of bleeding from the uterus.

Storage conditions

Livial must be kept in a place closed from the penetration of small children. Temperature level - no more than 25 ° С.

Shelf life

Livial is allowed to be used within a 24-month period from the date of sale of the therapeutic product.

Analogs

An analogue of the drug is the drug Tibolon.