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Drugs used in uterine fibroids

Suspected uterine fibroids should not be a reason to panic. If during the examination there were reasons for concern – not worry, wait until your next period and try to get an ultrasound again. It is desirable that the study was conducted using the vaginal sensor. And even when the diagnosis is confirmed, it is necessary to exactly check it from another gynecologist.

Uterine fibroids – a benign tumorarising in the muscular layer and the wall of the body or cervix. Represents a collection of nodules of proliferating smooth muscle cells. Often, cell proliferation appears in several places and reaches a size from a couple millimeters to ten or twenty centimeters. The size of the fibroids gynecologists not measured in the metric system, and by analogy, increasing the uterus during pregnancy, in weeks.

In the early stages (before 12 weeks), when slow growth and lack of symptoms, possible conservative treatment of fibroids. Especially this contributes to the status premenopausal approximation menopause the early signs of menopause. At this time, due to the inhibition of the natural hormonal processes of tumor growth is strongly slowed down to a complete stop. Non-surgical treatment of leiomyomas is in the medication of various types, which will be discussed in the next sections of this article.

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COC (combined oral contraceptives)

Drugs in this group represent the means of different dosage forms on the basis of hormones. To reduce the size of the tumor therapy, the following combinations of hormones:

Ethinyl estradiol with desogestrel

This combination is present in the formulations:

  • Mercilon;
  • Novinet;
  • Marvelon.

Ethinyl estradiol and norgestrel

Together, these hormones are found in such medications as:

  • Evidon;
  • Rigevidon.

Ethinyl estradiol with gestodene

This combination is used in the formulations:

  • LOGEST;
  • Lindinet.

By taking these pharmaceuticals may lead to the termination of such symptoms of uterine fibroids as bleeding and abdominal pain. However, to achieve reduce the swelling can, in most cases, only if the size of the fibroids did not exceed in diameter half an inch. Because of this, combined oral contraceptives are not a priority in the treatment of fibroids.


Agonists gonadotropin-releasing hormone

Mechanism of action: agonist of gonadotropin-releasing hormone pharmacological trigger temporary menopause by suppressing the synthesis of gonadotropins. This is due to the binding and GnRH receptors GnRH in the anterior pituitary. With continuous introduction they cause the complete disappearance of these receptors from the cell membranes of the pituitary gland, which causes a blockade in the secretion of gonadotropin, which is temporary and reversible, though it is accompanied by amenorrhea.

This group includes funds on the basis of such hormones:

  • Triptorelin. Present in medication Decapeptyl, Diphereline and Decapeptyl depot. In the usual form required to be administered subcutaneously once a day or 0.5 mg in the first week and 0.1 mg for the next three weeks. Triptorelin acetate in depot form is introduced in day 3 of the menstrual cycle with a dose of 3.75 mg, then every 28 days for six months.

  • Goserelin. Presented in the drug Zoladex capsules depo dosage of 3.6 mg and similar capsules of the prolonged action of 10.8 mg. Introduction deep intramuscular or subcutaneous in the shoulder area, buttocks or abdomen. The course begins with 2-4 days of menstrual cycle at 3.6 mg every 28 days. Course duration – 4 to 6 months.

  • Nafarelin. Used in composition by endonasal spray has Synarel dosage of 400 to 800 mcg per day. Daily insufflation at 200 µg acetate nafarelin.

  • Buserelin. Pharmaceutical form is a nasal metered-dose spray Buserelin, containing 2100 mg of buserelin acetate, which corresponds to 2 g buserelina. One full press of the pump provides 150 mcg buserelina, a daily dose of 900 micrograms.

  • Leuprorelin. The drugLucrin-depo is available in powder form in vials or dual-chamber syringes for the preparation of suspension. Introduction intramuscular or subcutaneous dosage 3.75 mg leuprorelin acetate in each injection.

The treatment with agonists of gonadotropin-releasing hormone observed average volume reduction of fibroids is 52.6 %. However, in 5-18 % of cases the therapy and GnRH does not give visible results. In case of multiple fibroids, the degree of regression of several tumors in one patient are often different. Different researchers call the reasons for such variability as the age of the patients and uneven distribution of fibrous and smooth muscle components in the fibroids, as well as degenerative changes of the tumor and the loss of sensitivity to anti-estrogen effects.

In most cases, the full effect of the treatment and GnRH is observed at 3-4 months of therapy with slow fading by the sixth month. Sometimes after 50-68 % tumor regression in 4 month with the standard prolongation of therapy up to six months starting secondary increase of fibroids, leading to the return of 80-100 % of the original size. Negative point of using agonists are also side effects associated with hypoestrogenia: depression, lability, decreased libido, hot flashes and bone loss.

To combat the side effects of offers different strategies:

  • the add-back mode implies the addition to treatment by agonists of low-dose estrogens, which raise the level of estradiol to the threshold at which the growth of fibroids has not yet resumed, but the side effects of hypoestrogenia not observed or greatly reduced.

  • on-off mode means the discontinuous course of GnRH agonist – 3/3 month. During the 3 month interruption of therapy completely restored the endogenous production of estrogen, but the increase of the uterus in most cases is minimal.

  • interval mode allows to maintain an adequate rate of regression of fibroids with virtually no symptoms of hypoestrogenia by gradually increasing the standard interval and GnRH-28 to 70 and 84 days (10-12 weeks).

  • drow-back mode invented by researchers who with the help of a sharp decrease in the dose of agonist with 100 mg/day up to 5-20 mg/day after reaching the limit, which is manifested severe hypoestrogenia (approximately 2 months of therapy), achieved maintain the effect of reducing fibroids with a partial recovery of the synthesis of estrogens within the next 18 weeks.

Thus, agonists of GnRH are pretty effective for a non-surgical treatment of fibroids of the uterus in premenopausal before, if you useinnovative methods of their application. The larger size of the tumor, they significantly help to facilitate the surgical intervention, allowing to apply modern technologies of sparing reconstructive surgeries.

It should also be noted the useful properties of agonists in the treatment of fibroids in patients with anemia and metrorrhagia to reduce the risk of surgery to restore the blood to create a blood Bank with the aim of autodonation.

On topic: Surgery to remove fibroids of the uterus – whether it is necessary? Complications and consequences


Antiprogestogen

Mifepristone – blocks the effect of progesterone by binding gestagenov receptors. Is available tablets of 200 mg 3-6 pieces per pack. The drug is a tool for medical abortion (to 9 weeks), auxiliary cure for the extension of the cervix in abortion up to 12 weeks and potentiating the work of prostaglandins for abortion from 13 to 22 weeks. In uterine fibroids promotes short-term regression of the nodes of the tumor and eliminate the symptoms, is therefore used for preoperative therapy.


Antigonadotropin

Used only when other pharmacological agents were powerless. Group of drugs include such active ingredients as:

  • The danazol. Contains the drugs Danazol, Vero-danazol, Danol, Danoval, Danogen.

  • Gestrinone. The basis of drugs Nemectron.

Antigonadotropin are rarely used, as only able to reverse the symptoms of fibroids, but do not affect the size of the tumor. In addition, drugs of this class provoke acne and hypertrichosis (excessive hair growth) with changes of the voice.

Progestins

Relatively efficient and not expensive tools, making are still used in gynecology, although in many cases this efficiency has not been proven.

Mechanism of action: Accepted with the goal of blocking the synthesis of estrogen by the ovaries. Compared to a GnRH-there is a lack of inhibition of estrogen production. To enhance the action of strong excess blood levels of progesterone in the luteal phase of the cycle, which blocks the process of hyperplasia with hypertrophy of nutrients fibroids that stimulatesdegeneration of cells in the Central part of nodes tumors.

  • Monitor tablet 5 mg norethisterone. The dose should be calculated to the doctor based on tolerability and observed effectiveness of the drug. The standard course consists of daily taking 1 tablet of the drug at 5-25 days cycle for six months.
  • The main tablets with 10 mg of dydrogesterone. Are assigned to one tablet 2-3 times a day or from the 5th to 25th day of cycle or continuously. The course lasts from 3 months to half a year – at the end should be pronounced therapeutic effect is regression of the tumor and absence of symptoms of fibroids.
  • 17-DIC – medicine-based 17-oxyprogesterone caproate. Available in ampoules of 1 ml in the composition of the oil solution concentrations of 12.5 and 25% (0.125 and 0.25 g respectively). For the development of atrophy of the endometrium with subsequent regression of fibroids applies deep intramuscular injection of 500 mg of the drug in the two approaches in a week for a period of 3 to 6 months.

Unfortunately, hopes for a full or even a significant reduction in the leiomyoma nodes during therapy with analogues of progesterone are not met in full. In some cases, was even the worsening condition of patients. Scientifically established that progestins are due to the increase in mitotic index in the luteal phase of the cycle may even promote the growth of fibroids.


HRT – hormone replacement therapy

Hormone replacement therapy helps relieve symptoms of menopause, reduce the risk of heart disease, prevents destruction of bone and atrophy of the vagina. Therapy hormonal therapy reduces overall mortality in women in menopause and corrects disorders of the climacteric syndrome.

Controversial is the question of the use of drugs hormonal therapy in women in menopause: during menopause the growth of benign tumors is stopped and the fibroids are not progressing, but the body's response to hormones is unpredictable.

According to clinical observations the authorship of A. Senez, the diameter of myomatous nodes in the treatment of conjugated oestrogen (0,625 mg) and medroxyprogesterone (2.5 mg) during the year did not change. However, with increasing doses of progestogen twice the size of the nodes became larger. Thus, treatment with progesterone affect the growth of benign tumors to a greater extent than preparations of estrogen. Other authors have noted that growth miomatoznyh nodes, as well as changes in the size and volume of the uterus, while application of cyclic modes is not detected.

The differences in the impactcyclic progestins in hormone replacement therapy depend on the pharmacological characteristics of the drugs. Recommended as ZMG (hormone replacement therapy) to women in menopause to prescribe a progestogen with anti-proliferative effects. These include drugs such as Trisequens and Kliogest.


Homeopathic medicines

Mamasan – sugar dragees on the basis of leaf Arnica, Sepia (cuttlefish ink) and asterios (starfish). Apply 5-7 drops thrice a day half hour before or one hour after eating. First, the required trial period of one week during which it is taken 1-2 tablets 3 to 4 times a day. If no effect is the transition to the standard dosage.

Epigallo is a dietary Supplement, non-hormonal remedy for the treatment and prevention of women's diseases, provoked by the uncontrolled proliferation of cells. Active substance – epigallocathechin-3-gallate, 45 mg per softgel. Available in blister packs of 30 pieces in the package and in a plastic pot (120 pieces). The standard dosage is 2 capsules 2 times a day. On the recommendation of the manufacturer, the best effect is observed while admission to the Indinol Forte.

Indinol – BAD, promises proliferazione correction of pathological processes in the organs of the female reproductive system. Produced in capsules, the active ingredient is indole-3-carbinol, 300 mg per capsule. Packaging – blister packs of 10 and 20 capsules and plastic jars by 60, 80, 100 and 120 capsules. The recommended dose is 1 capsule three times a day during meals.

Topic: upland uterus and red brush with uterine fibroids


The intrauterine device Mirena if the fibroids

IUDs are mostly not used to treat any disease. But one of them, the hormonal Mirena spiral, it was discovered the properties that help to cope with a number of symptoms characteristic of uterine fibroids.

Mirena acts locally, gradually releasing levonorgestrel low doses only within the uterus. Daily intake of this hormone reduces the amount released during menstruation blood and pain in the abdomen. Due to the fact that he almost misses, overall health does not change over the 5 years that it is possible to wear this spiral.

Intrauterine therapeuticsystem Mirena, moreover, prevents unwanted pregnancy, without disturbing the fertility. A year after the removal of the helix in 80% of women who wanted to have children get pregnant.


Recent studies of medical treatment

The solution to the problem of treatment of uterine fibroids have significantly advanced scientists from Belgium. They were interested in research data indicating that rapid growth and development of uterine fibroids is not only estrogen, but also progesterone. This prompted scientists to study the properties of drugs that can block the effect of progestins. The Brussels team of scientists on the basis of the hospital of St. Luke was particularly attracted by the pill-emergency contraception containing has ulipristal acetate.

It is the active ingredient is a modulator of progesterone receptors. On its base was created the esmya.

In the first clinical trial (randomized double placebo) was attended by 550 women preparing for surgery to remove uterine fibroids. After three months in the group taking pills Esme, there was a significant reduction in the size of the tumor and relief from the symptoms of fibroids.

In conclusion, the researchers published these results:

  • 90% of women who decreased the intensity of bleeding and volume of leiomyoma.
  • 50 % of the patients had the opportunity to refuse surgical intervention.
  • The results obtained according to the principle of comparable treatment with hormone blockers, but, unlike them, Esme causes of tides and degeneration of bone tissue.
  • After a 6-month course of blockers, the tumor is usually completely or partially returns to its size, which was not observed even after six months after taking Asmee.

The Belgian scientists conducted studies have a real opportunity to address the issue of treatment of uterine fibroids to one tool, no side effects and complex procedures.