Esmya tabs 5mg #28

Instruction for Esmya

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Composition

One tablet of the Esmya preparation contains 5 mg of viperacet acetate - the active ingredient.
As auxiliary substances, the drug contains: 43.5 mg of mannitol; 93.5 mg of microcrystalline cellulose; 4 mg - talc; 1.5 mg magnesium stearate; 2.5 mg - croscarmellose sodium.

Form of issue

The medicine Esmya is available in the form of tablets, on one side of which there is an engraving "ES5". One package can hold 28 or 84 tablets.

pharmachologic effect

Antigestagenic.

Pharmacodynamics and pharmacokinetics

The preparation Esmya contains a substance - ulcurette of synthetic origin, which is a selective modulator of progesterone receptors and is characterized by a tissue-specific selective antiprogestronic action.
Ulipristal is characterized by direct action on the endometrium. In most women, with the use of 5 mg of the drug every day during the menstrual cycle, including those suffering from fibroids, menstrual bleeding following this cycle does not occur. At the termination of reception of tablets, the menstrual cycle, as a rule, is restored during a month.
The direct effect of the drug on the endometrium is associated with some specific changes in it, characteristic for this class of drugs and provoked antagonistic action on progesterone receptors. In 60% of women taking ulpospistal for 3 months, histological changes are manifested by weakly proliferating inactive epithelium with concomitant asymmetry of its growth and stromal growth, as well as cystic enlargement of glands with progestagenic and estrogenic effects on the epithelium. These changes are reversible with disappearance at the end of the course of treatment and are not related to endometrial hyperplasia.
In 10-15% of women who underwent abdominal therapy, endometrial growth was observed, which reached a thickening of more than 16 mm. This thickening also disappears by itself at the end of treatment and the return of normal menstrual bleeding. If within 3 months after drug discontinuation, the thickening of the endometrium does not come to normal, additional tests should be performed to exclude or confirm other pathologies.
Ulipristal induces apoptosis and inhibits cell proliferation, thereby directly affecting leiomyomas, leading to their reduction.
Daily intake of 5 mg of vaginal results in guaranteed suppression of ovulation in the majority of women who receive it, which confirms the maintenance of the level of progesterone at 0.3 ng / ml. Also, the daily intake of this dose partially reduces the concentration of FSH, while leaving the content in the plasma of estradiol at the level of the middle follicular phase.
During a 3-month therapy, vulture does not affect the amount of ACTH, prolactin, thyroxine-binding globulin in the blood plasma.
In pre-clinical studies in animals, when taking multiple doses, there was no threat of toxicity and genotoxicity of the drug to humans. The death of the fetuses of animals with the intake of doses of more than 1 mg / kg was noted, therefore, the safety of the vandalism in relation to the human embryo has not been established. In small doses, which allowed to preserve pregnancy in animals, there was no teratogenic effect. Also, according to the findings of these studies, there is no direct evidence of the effect of the drug on the reproductive capacity of animals and their offspring.

Clinical studies of the safety and efficacy of Esme in daily doses of 5 and 10 mg have been conducted on female volunteers with menstrual bleeding of a severe nature, provoked by uterine myoma. Compared with the placebo group, there was a clinically significant decrease in the amount of blood loss associated with menstruation, in patients receiving ulcers, which allowed for faster effective correction of anemia than with the use of certain iron preparations. In the patients of the admission group, the loss of blood loss was comparable with the group of patients taking Leiprorelin (GnRH agonist). In most cases, taking Esmya led to an end to bleeding during the first week of treatment (amenorrhea was developing). MRI studies in this group showed a significant decrease in uterine fibroids, compared to the placebo group. Carrying out ultrasound at the end of the course of treatment (week 13), in order to establish a decrease in the size of uterine fibroids, showed the preservation of its parameters in the group of ulcers for 25 weeks, compared with some increase in its size in the Leiprorelin group.
After receiving vigil in a single dose of 5 mg, there is a rapid absorption of the drug, reaching Cmax after 60 minutes at a level of 23.5 ± 14.2 ng / ml and a plasma concentration of 61.3 ± 31.7 ng / ml. Ulipristal undergoes a rapid transformation with the release of a pharmacologically active metabolite, after 60 minutes Cmax is reached at 9 ± 4.4 ng / ml and a plasma concentration of 26 ± 12 ng / ml.
When taking 30 mg of Esmya during breakfast with a lot of fats, a 45% decrease in Cmax was observed, up to 3 hours, an increase in Tmax and a 25% increase in plasma concentration, both the most vandalized and its metabolite, in contrast to fasting. With daily administration of tablets, this effect is not considered significant.
Plasma proteins are associated with 98% and even more.
Metabolism occurs with the participation of cytochrome P450 with the release of the final di-N-demethylated metabolite.
Mostly excreted by the intestine, in less (about 10%) kidneys. T1 / 2 at a dose of 5 mg, about 38 hours, with an average clearance of about 100 l / h.

Indications for use

Preoperative treatment of manifestations of uterine fibroids of moderate and severe severity, in women of reproductive age who have attained 18 years of age, lasting no more than 3 months.

Contraindications

Carrying out of therapy by a drug Esmya it is counter-indicative:
    when the patient is hypersensitive to ulcers or other components of the tablets;
    with vaginal bleeding of undiagnosed nature or for reasons not related to uterine myoma;
    with malignant tumors of cervix, ovaries, uterus, mammary glands;
    with severe bronchial asthma, which is not amenable to treatment with oral GCS;
    when not reaching the age of 18;
    during periods of breastfeeding and pregnancy;
    in the case of a presumptive course of therapy exceeding 3 months (due to the lack of reliable data on the influence of vandalizing on the body, for more than this period).

Carefully:

    pathology of the kidney and / or liver;
    bronchial asthma.

Side effects

CNS:

    emotional disorders;
    headache;
    feeling of anxiety;
    dizziness.

Gastrointestinal organs:

    nausea;
    abdominal pain;
    dyspepsia;
    flatulence;
    dryness in the oral cavity;
    constipation.

Hearing organs:

    Vertigo.

Respiratory system:

    nasal bleeding.

Skin and subcutaneous tissues:

    increased sweating;
    the appearance of acne;
    lesions of skin.

Musculoskeletal system:

    soreness of muscles and bones;
    pain in the back.

Genitourinary system and mammary glands:

    amenorrhea;
    urinary incontinence;
    thickening of the endometrium;
    metrorrhagia;
    tides;
    formation of ovarian cysts;
    pelvic pain;
    tenderness, increase, tension of mammary glands;
    vaginal discharge;
    rupture of the ovarian cyst.

Others:

    increase in body weight;
    increased fatigue;
    edema;
    asthenia.

Laboratory indications:

    increase in blood cholesterol and triglycerides.
In the course of clinical studies, the most frequent adverse events were observed, of which 10-15% was occupied by a thickening of the endometrium, in most cases self-passing after the withdrawal of treatment; 12-13% - high tides; 6.4% - headaches of mild or moderate severity; 1.5% - ovarian cysts, disappearing spontaneously for several weeks; uterine bleeding, which in some cases requires surgical intervention.

Esmya, instructions for use

Instruction for Esmya recommends a one-time daily intake of the 1st pill orally (inside), regardless of food.
The start time of therapy is limited to the first week of the menstrual cycle. In this period, you should start taking Esmya tablets, preferably at the same time of day.
If you miss the time of taking the next pill, you must take it as soon as possible, for 12 hours. If this time limit is exceeded, this method is skipped and the course of treatment continues with the subsequent tablet in due time.
Due to the lack of experience with the use of Esmya for more than 3 months, this is the only time-limit for therapy.

Overdose

Complete data on the possibility of an overdose of the drug Esmya and subsequent negative manifestations, at this time does not exist. It is well known that the administration of a single 200 mg dose of the drug and a daily dose of 50 mg for 10 days did not lead to serious or severe conditions of the patient.

Interaction

Hormonal contraceptives, as well as Esmya, act on progesterone receptors and can reduce the effects of each other, and therefore, their joint application is not recommended.
The combination of Esmya and inhibitors of the CYP3A4 isoenzyme moderate (Erythromycin) and potent (Nefazodone, Ritonavir, Ketoconazole) actions, can provoke a significant increase in plasma concentrations of vomit. For this reason, their joint application is not recommended. The intake of inhibitors of the CYP3A4 isoenzyme of weak action does not significantly affect the pharmacokinetics of Esmya, and therefore does not require adjustment of the dose of the latter.
Receiving the inducers of the isoenzyme CYP3A4, leads to a decrease in the plasma content of the vandal. Therefore, the parallel use of powerful CYP3A4 isoenzyme inducers (Rifampicin, Phenytoin, Carbamazepine, agents including St. John's wort) is not recommended.
During absorption in the walls of the gastrointestinal tract, it is able to inhibit P-gp, thereby increasing the plasma concentrations of P-gp substrates. In this regard, the joint assignment of Esmya and P-gp substrates (Digoxin, Dabigatran) is not recommended.
In the future, the clinical use of Esmya can reveal other drug interactions.
A patient preparing to undergo therapy with the use of Esmya must tell her doctor about all the drugs she receives, both from the prescription and over-the-counter drugs.

Storage conditions

Tablets of the preparation Esmya must be stored in the original packaging, at ambient temperatures up to 30 ° C.
Shelf life - 2 years.

special instructions

The drug Esmya can be administered only after a thorough examination, in order to confirm the indications, exclude contraindications and pregnancy.
During the therapy, additional barrier methods of contraception are recommended, since the effectiveness of hormonal contraceptives can be reduced, as is the effect of the drug itself.
Although there is no reliable information on the effect of renal failure on excretion, it is not recommended for patients with this disease, especially in severe form, without the supervision of a doctor. These recommendations are also applicable to patients with hepatic insufficiency of moderate and severe severity, since the influence of this pathology on excretion is assumed.
The duration of therapy should not exceed 3 months.
Patients taking Esmya should be advised that the effect of the drug is usually accompanied by a significant reduction in menstrual blood loss or leads to amenorrhea for 10 days of therapy. At the end of this period, in the case of continued heavy blood loss, you need to see a doctor. Basically, the normal menstrual cycle is returned a month after the withdrawal of treatment.
Anemia was observed in most patients treated with Esmya. Nevertheless, fertility in street school is not studied.

Children

In connection with the lack of research, therapy with the use of Esme in patients under 18 years of age is not carried out.

In pregnancy and lactation

At this time, the periods of breastfeeding and pregnancy are contraindications to the treatment of vandalism.

Reviews about Esmya

Currently, the treatment of uterine fibroids with the use of the drug Esmya has not yet reached the scale after which it is possible to make an unambiguous conclusion about the expediency of its mass use. The doctors' comments about the drug are often cautious, although some experts say about Esmya as a real "breakthrough" in the therapy of this pathology, most doctors position it as a medicine for preoperative preparation of the patient, in order to reduce the size of fibroids and correct anemia by lowering or stopping the uterine bleeding.
It has been proved that in many cases, the Esmya tablets allow the uterus to be prepared for surgical intervention in such a way that it will later preserve the reproductive function. Among adverse reactions, doctors tend to notice hot flashes, especially at the beginning of treatment, a feeling of discomfort, headaches and cyst formation, which is confirmed by the reviews of patients taking this drug.
Reviews about Esme in the forums that discuss the methods and methods of treatment of fibroids, are also ambiguous. Basically, women discuss the inadequate, in their opinion, effectiveness of Esmya and its associated side effects. Also, a not negligible role in the discussion is the cost of the drug, which today is quite high. Most of the patients who took the hives were dissatisfied with his actions and an abundance of side effects. It is fair to say that only a few of them have completed a full course of treatment, which takes 3 months, and more often stopped therapy at this or that stage.
Summarizing all of the above, an unambiguous positive or negative conclusion about the preparation of Esmya can not be done. Successful struggle with uterine fibroids is affected by many factors, from the time of its detection and size and ending with the qualification and intuition of the attending physician. In any case, let's hope that the further experience of using vandalism will allow it to occupy a corresponding niche in the treatment of uterine fibroids and show really positive results of therapy.