define equipoise

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Due to the composition and cyclic regimen define equipoise (receiving estrogen alone for 11 days, then – a combination of estrogen and progestogen for 10 days, and finally, a 7-day rest period) in women with unremoved uterus when taken regularly the drug is established menstrual cycle .

While taking  not suppress ovulation, and the virtually unchanged production of hormones in the body. Define equipoisecan be used by women of childbearing age to regulate the menstrual cycle, as well as women in perimenopause to treat irregular uterine bleeding.

Estradiol restores deficit of estrogen in the female body after menopause and provide effective treatment for psycho-emotional and vegetative menopausal symptoms (such as “hot flashes”, sweating, insomnia, increased nervous excitability, irritability, palpitations, false angina, dizziness, headache, decreased libido, muscle and joint pain); involution of the skin and mucous membranes, especially the mucous membranes of the genitourinary system (urinary incontinence, dryness and irritation of the vagina, pain during sexual intercourse).

Estradiol prevents bone loss caused by estrogen deficiency. This is mainly due to the suppression of bone remodeling toward bone formation of osteoclast function and process shift. It has been proven that long-term use of hormone replacement therapy can reduce the risk of fractures of the peripheral bone in women after menopause. If you cancel  rate of decline in bone mass comparable to the characteristic of the period immediately after menopause. Do not proven that using it is possible to achieve the restoration of bone mass to premenopausal levels.

Also has a beneficial effect on the collagen content of the skin, as well as its density, and can also slow down the formation of wrinkles.

Define equipoise leads to lower total cholesterol, low density lipoprotein cholesterol and increasing high density lipoprotein cholesterol  and triglyceride levels increase. Progestogen contained in the  to some extent prevent the effects of oestradiol on lipid metabolism.

Observational studies suggest that among postmenopausal women using  reduced incidence of colon cancer. The mechanism of action is unclear to date.

Pharmacokinetics
After oral administration estradiol valerate is rapidly and completely absorbed from the gastrointestinal tract define equipoise. After entering the body, he quickly metaboliziretsya to form 17B-estradiol and estrone, which are subsequently subjected to a standard metabolic transformations. After oral bioavailability of estradiol of about 3%. Food does not affect the bioavailability of estradiol. The maximum concentration of estradiol in the serum of approximately 30 pg / ml, typically achieved through 4-9 hours after the pellets. Estradiol metabolites excreted as primarily in the urine as glucuronides and sulfates.

After oral administration, norgestrel is rapidly and almost completely absorbed from the gastrointestinal tract. The maximum concentration of levonorgestrel in serum of approximately 7-8 pg / ml, typically achieved after 1-1.5 hours of tablet. Levonorgestrel binds to albumin and globulin, sex hormone binding . About 1-1.5% of the total concentration levonorgestrel in serum is not associated with the protein. With the half-life of about 1 day, norgestrel metabolites are excreted in the urine and bile.

Indications

 

  • Hormone replacement therapy define equipoise for menopausal disorders, involutional changes of the skin and the urogenital tract, depression, menopause and symptoms of estrogen deficiency due to natural menopause or hypogonadism, sterilization or primary ovarian dysfunction in women with a uterus unremoved.
  • Prevention of postmenopausal osteoporosis.
  • Normalisation of irregular menstrual cycles.
  • Treatment of primary or secondary amenorrhea.