Esmiya

Description overdue on 11/26/2014

• Latin name: Esmya
• ATC code: G03XB02
• Active substance: Ulipristal (Ulipristal)
• Manufacturer: Gedeon Richter (Hungary)

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Esmiya, instructions for use
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Babies
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

One tablet formulation comprises 5 mg Esmiya ulipristal acetate   - The active ingredient.

As auxiliary substances medicine contains: 43 mg 5 - mannitol; 93, 5 mg - microcrystalline cellulose; 4 mg - Talc; 1, 5 mg - magnesium stearate; 2, 5 mg - sodium croscarmellose.

Product form

The drug Esmiya (Esmya) comes in the form of tablets, one side of which there is engraved «ES5". One package may contain 28 or 84 tablets.

Pharmacological action

Antigestagens.

Pharmacodynamics and pharmacokinetics

The drug Esmiya (Esmya) contains a substance -   ulipristal   synthetic origin, are selective progesterone receptor modulator   and different tissue-specific selective antiprogesteronovym action.

Ulipristal is characterized by a direct effect on endometrium . For most women, the application of 5 mg daily for menstrual cycle , Including sufferers myoma , Does not occur subsequent to this cycle menstrual bleeding . Upon termination of the pills, menstrual cycle Usually recovered within a month.

The direct effect of the drug on endometrium due to some of its specific changes characteristic for this class of drugs and provoked antagonistic action progesterone receptors . In 60% of women taking ulipristal over 3 months, histological changes are weak proliferating inactive epithelium   with related asymmetry of growth and growth stroma , and cystic expansion   glands progestagenic and estrogenic impacts on epithelium . These changes are reversible with the disappearance at the end of treatment, and are not related to endometrial hyperplasia .

In 10-15% of women held therapy with ulipristala It was observed growth of the endometrium Which reached a thickening 16 mm. This thickening also independently disappears at the end of treatment and return to normal menstrual bleeding . If within 3 months after discontinuation of the drug,   thickening of the endometrium   does not come to the state standards, it is necessary to pass an additional examination in order to exclude or confirm other pathologies.

Ulipristal induces apoptosis   and oppresses cell proliferation Thereby providing a direct effect on leiomyoma Leading to their reduction.

The daily intake of 5 mg ulipristala It leads to the guaranteed inhibition of ovulation   the majority of women receiving it, confirming the maintenance of the level of progesterone   at 0, 3 ng / ml. Also, a daily intake of a given dose of the drug is partially reduced the concentration of FSH While leaving the content in the blood plasma Estradiol at the secondary level the follicular phase .

During the 3-month treatment ulipristal It has no effect on the amount of plasma ACTH . prolactin . thyroxine binding globulin .

In preclinical animal studies, while taking multiple doses, there was no threat Toxicity and genotoxicity Products for Human Use. It was noted that the death of fetuses animals when receiving doses greater than 1 mg / kg, and therefore, is not installed Safety ulipristala   towards human embryos . In small doses, which allows you to keep a pregnancy in animals, teratogenic   action was not observed. Also, according to the findings of these studies, there is no direct evidence of the effect of the drug on reproductive ability   animals and their offspring.

Clinical studies of safety and efficacy Esmii at daily doses of 5 and 10 mg, were conducted on volunteers with a female menstrual bleeding   severe, provoked uterine myoma . Compared with the group placebo It was noted clinically significant decrease in the volume of blood loss   Related menstruation , In patients receiving ulipristal , Which allows for faster effective correction of anemia Than when applied alone iron supplementation . Patients receiving group ulipristala , Lowering the amount of blood loss was comparable with the group of patients treated with Leuprorelin (GnRH agonist). In most cases resulted in a reception Esmii cessation of bleeding   during the first week of treatment (developing amenorrhea ). MRI studies in this group showed a significant a decrease uterine fibroids As compared with the group placebo . Carrying US control   at the end of treatment (Week 13), in order to establish reduce the size of uterine fibroids It showed preservation of its parameters in a group ulipristala for 25 weeks, compared with some increase in its dimensions in the group Leuprolide .

Upon receiving ulipristala in a single dose of 5 mg, a rapid absorption of the drug from reaching Cmax after 60 minutes at - 23 ± 5 14, 2 ng / ml plasma concentrations of 61, 3 31 ± 7 ng / ml. Ulipristal undergoes rapid transformation with the release pharmacologically active metabolite While after 60 minutes reached Cmax 4 9 ± 4 ng / ml and a plasma concentration of 26 ± 12 ng / ml.

When receiving 30 mg Esmii during breakfast high in fat, 45% reduction was observed Cmax, up to 3 hours and an increase in Tmax 25% increase in plasma concentrations, both the ulipristala And its metabolite Unlike fasting. With daily pill, this effect is not regarded as significant.

The plasma protein ulipristal It binds to 98% or even more.

Metabolism takes place with the participation of cytochrome P450 with the final selection di-N-demethylated metabolite .

In more output intestines less (about 10%) by the kidneys. T1 / 2 at a dose of 5 mg, about 38 hours, with an average clearance of about 100 l / h.

Indications

Pre-treatment   manifestations uterine fibroids   moderate to severe in women of reproductive age who have attained 18 years of age, duration of not more than 3 months.

Contraindications

Conducting drug therapy is contraindicated Esmiya:

• at hypersensitivity ulipristalu to the patient or other components of the tablet;
• at Vaginal bleeding   undiagnosed nature or for reasons unrelated to the uterine cancer ;
• at malignancies   cervix, ovaries, uterus, mammary glands;
• at severe bronchial asthma That is not treatable oral corticosteroids ;
• when not reaching the age of 18 years;
• during periods breast-feeding   and pregnancy ;
• in the case of alleged course of therapy than 3 months (because of the lack of reliable data on the impact of ulipristala on the body, for over this period).

Carefully:

• renal disease and / or liver disease;
• bronchial asthma .

Side effects

CNS:

• emotional disturbances;
• headache ;
• anxiety;
• dizziness .

Bodies of the digestive tract:

• nausea ;
• abdominal pain;
• dyspepsia ;
• flatulence ;
• dryness of the mouth;
• constipation .

The organs of hearing:

• vertigo .

Respiratory system:

• nosebleeds .

Skin and subcutaneous tissue disorders:

• increase sweating ;
• appearance acne ;
• lesions of the skin.

Musculoskeletal system:

• soreness   muscles and bones;
• pain in the back.

Genito-urinary system and mammary glands:

• amenorrhea ;
• urinary incontinence;
• thickening of the endometrium ;
• metrorrhagia ;
• tides ;
• education ovarian cysts ;
• pelvic pain;
• soreness . increase , Tension Breast ;
• vaginal discharge ;
• cyst rupture   ovary.

Others:

• weight gain;
• fatigue;
• swelling ;
• asthenia .

Laboratory evidence:

• increase of blood cholesterol and triglycerides .

In clinical trials, the most frequent adverse events, of which 10-15% occupied thickening of the endometrium In most cases their own passing after discontinuation of treatment; 12-13% - tides ; 6, 4% - headache   mild or moderate in severity; 15% - ovarian cysts , Disappear spontaneously over several weeks; uterine bleeding Which in some cases require surgery.

Esmiya, instructions for use

Instructions on Esmiyu recommends daily intake of one-time first tablet orally (inside), regardless of the meal.

Time of the first week of therapy is limited menstrual cycle . This period should start taking pills Esmiya, preferably at the same time of day.

At the time pass reception the next tablet should be taken as soon as possible, within 12 hours. If you exceed this time limit, passed the acceptance and continue the course of treatment followed by tablets at one time.

Due to the lack of experience with Esmii over time exceeding 3 months, this term is only valid for the treatment.

Overdose

Full information on the possibility of overdose Esmiya and the consequent negative manifestations, for the time being does not exist. Thoroughly aware that receiving a single 200 mg dose and 50 mg daily doses for 10 days did not result in serious or grave condition of the patient.

Cooperation

Hormonal birth control pills As well as affect Esmiya progesterone receptors   and may reduce the effects of each other, and therefore, not recommended for combined use.

Combines the reception and Esmii inhibitors of CYP3A4   moderate ( Erythromycin ) And powerful ( Nefazodone . Ritonavir . Ketoconazole ) Steps could trigger a significant increase in plasma concentration ulipristala . For this reason it is recommended to use them together. Receiving inhibitors of CYP3A4   benign not significantly affect the pharmacokinetics Esmii, and therefore does not require adjusting the dose of the latter.

Receiving inducers of CYP3A4 It leads to a decrease of the plasma content ulipristala . Therefore, concomitant use inducers of CYP3A4   powerful action ( Rifampicin . Phenytoin . Carbamazepine , Means including St. John's wort ) not recommended.

During absorption in the walls of the digestive tract ulipristal able inhibit P-gp Thereby increasing plasma concentrations of substrates of P-gp . In this regard, it is not recommended, and coadministration Esmii substrates of P-gp   ( Digoxin . Dabigatran ).

In the future clinical use Esmii may identify other drug interactions.

The patient preparing to undergo therapy with Esmii is obliged to inform your doctor about all the measures it funds as of prescription and OTC list.

Terms of sale

Pharmacies Russia to purchase the drug Esmiya required to present a doctor's prescription.

Storage conditions

Tablets Esmiya drug should be stored in the original packaging at an ambient temperature of 30 ° C.

Shelf life

When stored product shelf life is 2 years.

Cautions

The drug Esmiya may be appointed only after a thorough examination in order to confirm indications and contraindications exceptions pregnancy .

During therapy is recommended to use additional barrier methods of contraception As efficiency hormonal contraceptives   It can be reduced, as the action of the drug.

Although reliable data on the impact of renal failure   on elimination ulipristala No, I do not recommend its acceptance by patients with the disease, especially in severe form, without the supervision of a physician. These recommendations apply to patients with hepatic insufficiency   moderate to severe, as it is assumed the impact of this disease on elimination ulipristala .

Duration of therapy should not exceed 3 months.

Patients taking Esmiyu should be made aware that the effect of the drug is usually accompanied by significant reduction in menstrual blood loss   or leads to amenorrhea during 10 days of therapy. At the expiration of this period, in the case of continuing profuse bleeding , You need to see a doctor. In general, normal menstrual cycle   He returned one month after discontinuation of treatment.

The majority of patients treated with the drug Esmiya, observed anovulation . Nonetheless, fertility in therapy ulipristalom It has not been studied.

Analogs Esmii

Match code ATC 4th level:

• Zhenale
• Mifegin
• Miropriston
• Ginepriston
• Mifepristone
• Penkrofton

Analogs ulipristala belonging to one group of pharmacological and similar but not identical in the main action, represented by the following drugs:

• Agesta ;
• Ginepriston ;
• Zhenale ;
• Gynestril administration ;
• Miropriston ;
• Mifepreks ;
• Mifegin ;
• Mifepristone ;
• Penkrofton ;
• Mifolian .

Babies

Due to the lack of research, therapy with Esmii in patients under 18 years old are not carried out.

During pregnancy and lactation

At this time, the periods breast-feeding   and pregnancy are contraindications to therapy ulipristalom .

Reviews Esmii

Currently, treatment uterine fibroids   Esmiya with the drug has not yet reached the scale, after which it is possible to make an unambiguous conclusion about the advisability of the appointment of its mass. Reviews of doctors about the drug often cautious, although some experts say about Esmii, as a real "breakthrough" in the treatment of this disease, most doctors are positioning it as a cure for preoperative   patient in order to reducing the size of fibroids   and correction of anemia   by reducing or stopping uterine bleeding .
It is proved that, in many cases, the possibility to prepare a tablet Esmii uterus for surgery so that subsequently save reproductive function . Among the side effects, doctors usually say tides Especially at the beginning of treatment, discomfort . headache   and cyst formation That confirm the ratings of patients taking the drug.

Reviews Esmii in forums to negotiate ways and methods treatment of uterine Also mixed. Mostly women discuss failure, in their view, the effectiveness of Esmii and associated with its intake side of manifestation. Also not unimportant role in the discussion covers the cost of the drug, which today is quite high. The majority of patients treated with ulipristal They remained dissatisfied with its action and lots of side effects. In fairness it should be noted that few of them had a full course of treatment takes 3 months, and often stopped therapy at some point or another.

In summary, an unequivocal positive or negative conclusion about the drug Esmiya can be done. On the successful struggle against uterine fibroids   influenced by many factors, ranging from the time of its discovery, and the size and finishing skills and intuition of the attending physician. In any case, we hope that further experience with ulipristala It will allow him to take the appropriate niche treatment of uterine fibroids   and really show the positive results of therapy.

Price Esmii where to buy

Price Esmii pharmacies in Russia ranges from 7000 - 9000 rubles.

This drug you can buy in Moscow, about 7,500 rubles.

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