The drug "Clayra": reviews of doctors, pluses, minuses, instructions, side effects. Reviews of gynecologists about Claira tablets with endometriosis, with menopause

Recently, quite often modern doctors write out the drug "Clayra" for certain diseases. Reviews of doctors, pluses, minuses of this remedy - all this we will consider below.

How do they work?

This drug is a combined oral contraceptive, which is based on the interaction of a number of factors. The most important among them are the suppression of ovulation, as well as the adjustment of the properties of cervical mucus - this is the basis for the action of the drug "Clayra". Comments of doctors (pluses, minuses, experts always consider) often say that this means stands out among similar ones with its effect.

In addition to preventing unwanted pregnancy, this drug is also characterized by a number of additional useful properties, which, even taking into account any negative qualities, allow choosing the optimal variant of contraception. All contraindications describe to the drug "Claira" instruction. The doctor's comments also include information about who should not take this medication.

What does the reception give?

Reduction of intensity and painfulness of menstrual bleeding, which in the end leads to a significant decrease in the risk of iron deficiency anemia. This is the main effect that "Clayra" provides. The doctors' comments (pluses / minuses of this drug see below) indicate that all this is provided in full, and therefore the medication is recommended to be used so often. Among other things, it is often noted that the use of this drug provides a significant reduction in the possibility of developing endometrial cancer. Also taking the drug reduces the risk of ovarian cancer.

What do doctors say?

Regarding the drug "Clayra", doctors often comment on the fact that it has a very favorable effect on the endometrium, and therefore it is used in the treatment of prolonged or too severe menstrual bleeding without an organic pathology. These symptoms periodically refer to dysfunctional uterine bleeding. It is this fact that distinguishes the doctors' opinions about the "Claira" preparation. With endometriosis, its use can also be prescribed.

Research

The safety and effectiveness of the use of estradiol valerate / dienogest tablets in the treatment of various symptoms of uterine dysfunctional bleeding were identified in the course of two clinical trials.

Both studies used the same package design and analysis plan. In the end, 269 patients were selected to use Clayra. The doctors' comments (pluses / minuses are described in detail) participating in the study indicate that in addition to this, 152 patients were tested in the study, in which the placebo effect was tested . In these studies, it was determined that the drug was much more effective than placebo in the treatment of these symptoms, and it should be noted that the end point of the response to the Claira drug was more than 40% in each of the studies.

In addition, each of the studies clearly demonstrated statistically and clinically significant reduction in menstrual blood loss, and later it was accompanied by a statistically significant increase in the parameters of iron metabolism, which is currently often noted about the means of "Claira" reviews of doctors (the pros and cons of the drug we are considering) .

As an estrogen in this drug is estradiol varium, which is the precursor of human 17β-estradiol rights. The estrogen component used in this drug differs significantly from estrogens that are commonly used in combined oral contraceptives, which are standard synthetic estrogens such as mestranol or ethinylestradiol, each containing an ethynyl group in the 17α position. This group causes much greater metabolic stability, but at the same time, it has a more pronounced effect on the liver, which is also quite important.

In the description of the drug "Clayra", doctors' reviews are often mentioned and that his reception is characterized by a much less pronounced effect on the liver in comparison with other three-phase PDAs, which include levonorgestrel and ethinyl estradiol. During the research it was determined that the effect on the concentration of globulin intended for binding of sex hormones is less pronounced. In combination with dienogestradiol valerate shows a significant increase in HDL, while the total concentration of LDL cholesterol decreases.

Dienogest is a progestogen that works in the case of oral administration. It is characterized by additional antiandrogenic partial effects, while its anti-estrogenic, androgenic and estrogenic properties are insignificant. Due to the unique chemical structure, a whole spectrum of pharmacological action is achieved, which includes the most significant benefits of 19-nor-progestogens, as well as various progesterone derivatives, which are often noted for the Claira feedback (pluses / minuses will be discussed below).

Even the preclinical data that were obtained during routine toxicity studies after numerous doses, as well as the carcinogenic potential and genotoxicity of this agent, did not show that there is any significant specific risk to a person. However, when describing the drug "Clayra" reviews of gynecologists often say that we should not forget about the possibility of stimulating a number of tumors and hormone-dependent tissues with sex hormones. In case of correct use, the so-called Perl index (the indicator determining the frequency of pregnancy in a hundred women during the year of application of a given drug) is less than 1, but in case of missing tablets or misuse, it can increase.

Next, the pharmacokinetics of the drug "Clayra" will be considered. Reviews of gynecologists almost completely confirm the information specified by the manufacturer, in connection with which this tool is prescribed for many patients.

Dienogest

• Absorption . After oral administration, this element is quickly and almost completely absorbed. C _max in serum reaches 90.5 ng / ml about an hour after the tablet is taken (it contains 3 mg of dienogest and 2 mg of estradiol of Variat). Bioavailability in this case reaches a rate of 91%. It should be noted that the pharmacokinetics of dienogest in the dosage range of 1 to 8 mg is characterized by a direct dose dependence. If the drug is used concomitantly with food intake, this does not cause any clinically significant effect on the degree or rate of absorption of this element.

• Distribution . A large part of the circulating dienogest (10%) is unbound, while the rest of it has a non-specific association with albumin. Dienogest itself does not directly bind to either corticosteroid-binding globulin or GSBG. It is for this reason that the risk of replacing testosterone from this bond with GSB or cortisol from the bond of this element to the CRS is completely excluded. This or that effect on the various physiological processes of the movement of endogenous steroids, respectively, is practically impossible. At an equilibrium concentration, V _d is 46 L as a result of intravenous administration of 85 μg of dienogest labeled with tritium.

• Metabolism . Dienogest element is almost completely metabolized in full accordance with the known ways of metabolism of steroid hormones, as well as with the formation of metabolites, which in the majority of cases are hormonally inactive. These metabolites are excreted extremely quickly, therefore the predominant fraction in the blood plasma is the constant dienogest. The total clearance after intravenous administration of tritiated dienogest is 5.1 l / h.

• Elimination . As a result of taking this element inside at a dose of 0.1 mg / kg, the dienogest completely exits as metabolites, excreted by the kidneys and intestines in an approximate ratio of 3: 1. After oral administration, approximately 42% of the dose is completely eliminated during the first 24 hours, while 63% is over 6 days through renal excretion. In addition, after 6 days, approximately 86% of the dose is discharged through the intestine and kidneys.

• Equilibrium concentration. In this case, the pharmacokinetics of the dienogest does not depend on the concentration of SHBG. The C _ss index is reached approximately three days after using the same dose, which is 3 mg of dienogest in combination with 2 mg of estradiol valerate.

Estradiol valerate

• Absorption . Due to the use of the drug estradiol, Varian is quickly and completely absorbed. Splitting into valeric acid and directly the estradiol itself is carried out during the absorption of this element in the mucosa of the gastrointestinal tract or during the first passage through the liver, resulting in the appearance of estradiol and its metabolites. If the drug is taken at the same time as food, it has no clinically significant effect on the degree or rate of absorption of this element.

• Metabolism . Valerian acid is characterized by extremely fast metabolism. After ingesting approximately 3% of the dose, it becomes absolutely bioavailable in the form of pure estradiol, which undergoes an intensive effect of the initial passage through the liver, as a result of which a significant part of the administered dose begins to be metabolized already in the mucosa of the gastrointestinal tract. In combination with presystemic metabolism directly in the liver, approximately 95% of the total oral dose is eventually metabolized before it enters the systemic circulation. As the main metabolites here are estrone sulfate, estrone and estrone glucuronide.

• Distribution . In the blood serum, about 38% of estradiol has a direct relationship with SHBG, while 60% - with albumin, and only 2-3% constantly circulates in an unbound state. It should be noted that estradiol can significantly increase the total concentration of SHBG in blood serum, and this effect directly depends on the dose received. On the 21st day of taking this drug, the total concentration of SHBG reached approximately 146% of the initial concentration, while by the 28th day, which was the completion of the phase of inactive tablets, it had already been reduced to 141%.

• Elimination . Because of the rather large circulating pool of glucuronides and sulfates, and also due to hepatic intestinal recirculation, T _{1/2 of} estradiol after oral use in the terminal phase is a complex characteristic directly dependent on all these processes.

• Equilibrium concentration. The pharmacokinetics of estradiol directly depends on the concentration of SHBG. In women, the concentration of estradiol in the blood plasma is a complex of endogenous estradiol, as well as the estradiol that enters the process of taking this drug. During the phase of taking the tablets, which contain 3 mg of dienogest and 2 mg of estradiol valerate, the average concentration of estradiol in blood serum when equilibrated is 51.6 pg / ml.

When is this drug used?

First of all, "Clayra" is administered with menopause. The doctors say that this is the optimal choice for the treatment of women suffering from profuse or prolonged menstrual bleeding in the absence of any organic pathology.

This drug is also used for oral contraception.

Contraindications

About the drug "Claira" reviews of doctors (side effects - to blame) are not always positive. So, there are some contraindications. We note several conditions in which this agent should not be used, and the reception should be completely canceled in the event that one of them begins to develop against the background of therapy:

• Excessive sensitivity to any active substances or to a certain auxiliary component;
• Thromboembolism or thrombosis at the present time or in the anamnesis;
• Conditions that are previous thrombosis, both in the history and at the present time;
• Expressed hereditary or acquired predisposition to the appearance of arterial or venous thrombosis, including also a deficiency of antithrombin III, deficiency of protein S and C, antibodies to phospholipids and hyperhomocystsinemia;
• The presence of an increased risk of arterial or venous thrombosis;
• The presence of migraine with any neurologic focal symptoms both at the moment and in the anamnesis;
• Diabetes mellitus, characterized by various vascular complications;
• Pancreatitis, with severe hypertriglyceridemia at the moment or in the anamnesis;
• Severe liver disease or liver failure;
• Manifested hormone-dependent malignant tumors or suspected of their occurrence;
• Liver tumors;
• Pregnancy or suspected of it;
• Bleeding from the vagina of unknown origin;
• The presence of lactose intolerance, glucose-galactose malabsorption or a deficiency of lactase.

Among other things, it is worth noting one more case in which the contraceptive pill "Claira" can not be used. The doctors say that they should not be taken during breastfeeding.

Special caveats

If certain diseases, conditions or risk factors, indicated below, are present in a person at present, it will be necessary to think very carefully about the potential risk and benefits of taking this drug in each individual case. In particular, this applies to the following situations:

• Risk factors for the subsequent development of thromboembolism and thrombosis;
• Other diseases in which various violations of the peripheral circulation can be seen;
• Hypertriglyceridemia;
• Presence of hereditary angioedema;
• Various diseases that first appeared or worsened during pregnancy or during the previous use of sex hormones.

In all these cases, you can not take "Clayra" tablets. Comments of doctors in this situation will help to maintain health.

Pregnancy and the period of breastfeeding

Use of this drug is contraindicated during pregnancy. In this case, there are situations when conception occurs against the background of the reception, which also mentions the "Clayra" preparation instruction for use. The doctors say that in this case you need to immediately stop the next appointment. However, in the process of conducting large-scale studies, there was no increased risk of developing any birth defects in children born to women who had taken the CCP both before conception and when they were randomly admitted at the beginning of pregnancy.

CCPs sometimes have an effect on lactation, as they can adversely affect the amount of milk produced or even change its composition, which often refers to the drug "Clayra" reviews of doctors. After 40 years for this reason, its use is not particularly recommended.