Vizan

Visanne belongs to the category of hormonal substances (progestogens), as well as drugs used for diseases affecting the genital area. The drug is based on the active element dienogest.

Dienogest is a derivative of the substance nortestosterone, which exhibits a strong antiandrogenic effect. In general, this element accounts for 1/3 of the total activity of the cyproterone acetate component. Dienogest is able to influence endometriosis by decreasing the internal production of estradiol. As a result, the trophic effect of estradiol on the endometrium is inhibited. [1]

Indications Vizan

It is used in the treatment of endometriosis .

Release form

The drug is produced in tablets - 14 pieces inside the cell plate. There are 2 such records inside the box.

Pharmacodynamics

With the continuous introduction of dienogest, it creates a hypergestogenic and hypoestrogenic environment, in which decidualization of endometrial tissues is first realized, and later atrophy of the areas affected by endometriosis occurs.

Dienogest is able to synthesize with progesterone endings located inside the uterus, but it has only 10% relative affinity. Although the active element of the drug has a weak affinity for the endings of progesterone, it has a powerful progestogenic effect in vivo. [2]

The drug has no significant mineralocorticoid, androgenic or GCS effects in vivo. Other effects, including anti-angiogenic and immunological, help slow down dienogest on cell proliferation. [3]

Pharmacokinetics

Absorption.

When administered orally, dienogest is fully absorbed and at high speed. Serum Cmax values are noted with a single use after 90 minutes and are equal to 47 ng / ml. The bioavailability values of the drug are approximately 91%. The pharmacokinetic characteristics of dienogest are tied to serving size in a dosage range of 1-8 mg.

Distribution processes.

Dienogest is synthesized with albumin, but not with globulin, which synthesizes SHBG, or with globulin, which synthesizes GCS (GOK). Only 10% of the total indicators of dienogest inside the blood serum are in the form of free steroids, and 90% of the substance is nonspecifically synthesized with albumin. The level of the apparent distribution volume of the drug is 40 liters.

Exchange processes.

Dienogest fully participates in metabolic processes - through steroid metabolism with the formation of metabolic elements that generally do not have endocrinological activity. When tested in vitro, as well as in vivo, CYP3A4 is the main enzyme involved in the metabolic processes of dienogest. Such metabolic elements are excreted from the plasma at a very high rate, leaving the unchanged dienogest as the dominant intraplasmic metabolite.

The rate of intra-serum clearance is 64 ml per minute.

Excretion.

Intra-serum dienogest values decrease in 2 steps, with a half-life of 9-10 hours. Dienogest is excreted in the form of metabolic components along with urine and feces (in proportions 3k1), after administration of a portion of 0.1 mg / kg.

The term for the half-life of metabolic components in the urine is approximately 14 hours. After using the drug, 86% of the portion is excreted over a period of 6 days, and most of it is excreted during the first 24 hours, mainly in the urine.

Dosing and administration

The medication must be taken 1 time per day, at the same time of the day. It is allowed to start use on any day of a woman's menstrual cycle. There is no need to take a break between new packs of drugs, use is continued without any intervals, and also without reference to the menstrual cycle.

If you skip the use of the pill or if the patient has diarrhea or vomiting, there may be a weakening of the effectiveness of the medication.

In case of skipping the use, this pill should be taken as quickly as possible, and the new one should be used at its usual time. You cannot increase the portion, it is left unchanged. The same scheme is followed in case of skipping the application due to diarrhea or vomiting.

• Application for children

The medication is not used for prescribing girls who have not started their first menstruation.

Use Vizan during pregnancy

Visanne is not used during pregnancy, because during this period, endometriosis therapy is not required. In this case, it is necessary to exclude the presence of pregnancy before the start of the treatment course.

If you need to take medication during hepatitis B, breastfeeding should be abandoned during therapy.

Contraindications

The main contraindications:

• severe intolerance associated with the elements of the drug;
• thromboembolism of a venous nature;
• diseases of a cardiovascular or arterial nature (among them cardiac ischemia, myocardial infarction and cerebrovascular pathologies);
• diabetes mellitus, in which vascular diseases are noted;
• severe stages of liver disease (this includes neoplasms of any etiology);
• neoplasms, the development of which is associated with gonadosteroids;
• having an unknown nature of vaginal bleeding;
• lactose intolerance.

When using the medication, you must use barrier-type contraception, because during this period it is forbidden to take hormonal contraceptives.

Side effects Vizan

With the introduction of the drug, some side signs may be observed (especially during the first months of the course). During therapy, these disorders disappear. Among the manifestations noted: discomfort in the area of the mammary glands, acne, headaches and depression.

If other negative symptoms develop during the use of Visanne, you need to consult with your doctor about a possible change in the treatment regimen.

Interactions with other drugs

The impact of other drugs in relation to Visan.

Progestogens, including dienogest, are involved in metabolic processes mainly through the structure of the hemoprotein P450 ZA4 (CYP3A4), which is located inside the liver and intestinal mucosa. Because of this, agents that induce or slow down the action of CYP3A4 are able to affect the metabolic processes of the progestogen. An increase in the level of clearance of gonadosteroids due to the induction of enzymes can weaken the therapeutic activity of Visanne and cause the appearance of negative symptoms (for example, a change in the nature of menstrual bleeding).

A decrease in the clearance of gonadosteroids due to inhibition of the enzyme can reduce the therapeutic effect of drugs and cause the appearance of side signs.

Elements that increase the clearance of gonadosteroids (weakening the effect through the induction of enzymes).

These include barbiturates with carbamazepine, phenytoin, rifampicin and primidone, and in addition, possibly felbamate and oxcarbazepine with griseofulvin and topiramate, as well as substances that contain St. John's wort.

Enzyme induction can be noted after several days of treatment. The maximum enzyme induction develops after several weeks. Enzyme induction can last up to 1 month after the end of treatment.

The effect of rifamipicin (an inducer of CYP 3A4 action) has been studied in healthy, post-menopausal women. The use of rifampicin together with dienogest / estradiol valerate tablets caused a significant decrease in the equilibrium values and the systemic effect of estradiol with dienogest. The overall effect shown by estradiol and dienogest (at equilibrium values calculated by the level of AUC (in the range of 0-24 hours)) weakened by 44% and 83%.

Medicines that have a different effect on the level of clearance of gonadosteroids.

The combined use of gonadosteroids and a large number of combinations of HIV protease inhibitors, as well as inhibitors (nonccleoside type) of reverse transcriptase activity, together with combinations of hepatovirus type C inhibitors, can reduce or increase the plasma progestin level. The combined effect of these changes may be clinically significant in some situations.

Drugs that reduce the level of clearance of gonadosteroids (enzyme inhibitors).

Dienogest is a substrate for hemoprotein P450 (CYP) 3A4. The introduction together with powerful inhibitors of the CYP3A4 component can increase the plasma level of the substance.

The use in combination with ketoconazole, a potent inhibitor of the CYP3A4 enzyme, causes an increase in the AUC values of dienogest (range 0-24 hours) by 2.9 times at equilibrium values.

The combination with erythromycin (a moderate inhibitor) caused an increase in the AUC of dienogest (within 0-24 hours) by 1.6 times at equilibrium values.

Lab tests.

The use of progestogens can change the readings of certain laboratory tests, including the biochemical characteristics of the liver or thyroid gland, renal and adrenal functions, indicators of plasma proteins (which are carriers) (among them, for example, GOK and lipoprotein / lipid fractions), values of fibrinolysis and coagulation, and also the properties of the carbohydrate metabolic process. Such changes are often kept within laboratory limits.

Storage conditions

Visanne must be kept out of the reach of small children. Temperature indicators - no more than 30 ° C.

Shelf life

Visanne can be used for a 5-year term from the date of manufacture of the pharmaceutical product.

Analogs

Analogs of drugs are Sofiti, Justinda with Denovel 30, Yulidora and Klimodien with Dinoret, and in addition to this Luvina, Janine, Silhouette with Klayra and Naadin.