Estriol - instructions for use, dose, side effects, contraindications

Estrogen, an analog of the natural female hormone. It replenishes the estrogen deficiency in postmenopausal women and weakens postmenopausal symptoms. The most effective in treating genitourinary disorders. With atrophy of the mucous membrane of the lower sections of the urogenital tract estriol helps normalize the epithelium of the genito-urinary tract and helps restore normal microflora and physiological pH in the vagina. Increases the resistance of the epithelial cells of the urinary tract to infections and inflammation, reducing complaints such as soreness in intercourse, dryness, itching in the vagina, reduces the likelihood of vaginal infections and urinary infectionsways, promotes the normalization of urination, prevents incontinence.

Unlike other estrogens, estriol has a short period of action, since in the nuclei of endometrial cells it is retained for a short period of time. It is assumed that a single dose of a daily dose does not cause endometrial proliferation. Therefore, cyclic progestogen administration is not required and no withdrawal bleeding occurs. In addition, it is shown that estriol does not increase mammographic density.

Pharmacokinetics:

When using the drug inside, as well as locally estriol quickly and almost completely absorbed.

The maximum concentration of estriol in the plasma is achieved 1-2 hours after intravaginal application.

In plasma, almost the whole (90%) estriol is associated with albumin and unlike other estrogens is practically not associated with globulin, binding sex hormones.

The excretion of estriol (in a bound form) is mainly carried out by the kidneys; about 2% is excreted through the intestine in an unchanged form. Excretion of metabolites with urine begins a few hours after application and lasts for 18 hours.

Indications:

Replacement hormone therapy for the treatment of atrophy of the mucous membrane of the lower parts of the urinary and genital tract associated with estrogen deficiency; pre- and post-operative treatment of women in the postmenopausal period during vaginal operations; with a diagnostic purpose for unclear results of cervical cervical examination (suspicion of a tumor process) against the background of atrophic changes.

ICD-10

XIV.N80-N98.N95.3 Conditions associated with artificially induced menopause

XIV.N80-N98.N95.1 Menopause and menopause in women

XIV.N80-N98.N97 Female infertility

XIV.N80-N98.N95.2 Postmenopausal atrophic vaginitis

XII.L20-L30.L29.3 Anogenital itching, unspecified

Contraindications:

Established, history of or suspected breast cancer; diagnosed or suspected estrogen-dependent tumors (eg, endometrial cancer); bleeding from the vagina of an unclear etiology; untreated endometrial hyperplasia; presence of venous thrombosis at the present time and in the anamnesis; active or recent thromboembolic disease of the arteries (eg, angina pectoris, myocardial infarction); liver disease in the acute stage or a history of liver disease,after which the liver function indicators did not return to normal; porphyria; established hypersensitivity to the active substance or to any of the excipients of the drug.

Carefully:

During treatment with estriol, relapse or worsening of the following diseases and conditions is possible: leiomyoma (uterine fibroids) or endometriosis; transferred thromboembolic disorders or existing risk factors for such disorders; risk factors for estrogen-dependent tumors, for example, the 1st degree of heredity for breast cancer; arterial hypertension; Benign tumors of the liver (eg, liver adenoma); diabetes mellitus with the presence or absence of a vascular component; cholelithiasis; jaundice (including anamnesis during previous pregnancy); liver failure; migraine or severe headache; systemic lupus erythematosus; endometrial hyperplasia in the anamnesis; epilepsy; asthma; otosclerosis; familial hyperlipoproteinemia; pancreatitis.

Pregnancy and lactation:

Use during pregnancy is contraindicated. In case of pregnancy during estriol therapy, treatment should be immediately canceled.

The results of most epidemiological studies conducted so far on the unintended impact of estrogen on the fetus indicate the absence of teratogenic or fetotoxic effects.

It is not recommended to use during lactation (breastfeeding). Estriol is excreted in breast milk and can reduce the formation of milk.

Dosing and Administration:

Inside: the initial daily dose is 4-8 mg once a day for 2-3 weeks, then the dose is gradually reduced to 1-2 mg per day.

Vaginal Candles and Cream: intravaginally 500 micrograms per day daily in the first 2-3 weeks, then twice a week.

Side effects:

Tension or pain in the mammary glands, fluid retention, nausea, hypersecretion of cervical mucus, arterial hypertension, gastrocnemius muscle cramps, headache, visual impairment, pigmentation spots on the skin; local irritation or itching (cream).

Overdose:

Symptoms: nausea, vomiting, spotting from the vagina.

Treatment: symptomatic therapy.

Interaction:

Metabolism of estrogens can be enhanced by their use in combination with compounds,which induce enzymes involved in the metabolism of drugs, in particular cytochrome P450 isoenzymes, for example, such as anticonvulsants (phenobarbital, phenytoin, carbamazepine) and antimicrobial agents (rifampicin, rifabutin, nevirapine, efavirenz).

Ritonavir and nelfinavir exhibit inducing properties when used in combination with steroid hormones.

Herbal preparations containing St. John's wort (Hypericum perforatum) can induce estrogen metabolism.

Elevated estrogen metabolism can lead to a decrease in their clinical effect.

Estriol enhances the action of lipid-lowering agents.

Weakens the effects of male sex hormones, anticoagulants, antidepressants, diuretic, hypotensive, hypoglycemic agents.

Means for general anesthesia, opioid analgesics, anxiolytics, some antihypertensives, ethanol reduce the effectiveness of the drug.

Folic acid and thyroid medications enhance the effects of estriol.

Special instructions:

For the treatment of postmenopause, hormone replacement therapy should be started only with regard to symptoms that adversely affect the quality of life.In all cases, a careful assessment of the risks and benefits of treatment should be carried out at least once a year. Hormone replacement therapy should only be continued for a period of time when the benefit exceeds the risk.

Therapy should be discontinued if there is a contraindication and / or if the following conditions occur: jaundice and / or impaired liver function; significant increase in blood pressure; relapse of a migraine headache; pregnancy.

With intravaginal application of estriol, the risk of breast cancer is not known. It was shown that the use of estriol, unlike other estrogens, was not associated with an increased risk of developing breast cancer.

If estriol it is necessary to provide preventive treatment for thrombosis prevention according to the indication "pre- and post-operative treatment of women in the postmenopausal period with operations with vaginal access".

If the venous thrombosis and embolism develop after the application of estriol, the treatment should be stopped.

Estriol is a weak inhibitor of gonadotropin and has no other significant effects on the endocrine system.

Instructions

Estriol (Estriolum)