ESTROKAD®

Active material: Theelol
When ATH: G03CA04
CCF: Estrogen drugs
ICD-10 codes (testimony): N95.1, N95.2, N95.3
When CSF: 15.11.01
Manufacturer: Dr. KADE Pharmaceutical Factory GmbH (Germany)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

◊ Vaginal Suppositories white, Homogeneous, without smell.

Excipients: Witepsol S 51: tallow, macrogol cetostearyl ether, glyceryl monodiritsinoleat.

5 PC. – aluminum strips (2) – packs cardboard.

Pharmacological action

Theelol – estrogen, synthesized in humans. Once in the bloodstream, It forms a complex with specific receptors (in utero, vagina, urethra, mammary gland, liver, gipotalamuse, gipofize), It stimulates the synthesis of DNA and proteins.

It has a selective effect, preferably the cervix, vagina, vulva, causes increased proliferation of the epithelium of the vagina and cervix, It stimulates its blood supply, helps to restore the epithelium when atrophic changes in premenopausal and menopause, normalize the pH of the vaginal environment, vaginal microflora, it increases the resistance of the epithelium to infection and inflammation, It affects the quality and quantity of cervical mucus. Effects on the endometrium slightly (small risk of uterine bleeding).

It has a lipid-lowering effect, slightly increases the blood concentration of beta-lipoprotein, increases sensitivity to insulin action, improves glucose utilization, stimulates hepatic globulins, sex hormone binding, renin, HDL and blood clotting factors.

Through participation in the realization of positive and negative feedback in the hypothalamic-pituitary-ovarian system of estradiol can cause moderate pronounced central effects; It stimulates the parasympathetic reaction.

Pharmacokinetics

Absorption and distribution

C_max plasma in intravaginal application is achieved through the 1-2 no. Plasma protein binding – 90%.

Metabolism and excretion

Derivation is performed primarily in the urine as metabolites (a few hours after application and lasts until 18 no), 2% excreted in the feces as unchanged.

Testimony

- Atrophic changes in the mucosa of the vagina and vulva, accompanied by itching, burning and dryness;

- Pain during sexual intercourse;

- Inflammation of the vagina, vulʹvy or cervical canal;

- Vaginal discharge;

- Narrowing of the vagina;

- Ulcers of the vagina and cervix;

- Concomitant therapy in the treatment of vaginal infections;

- Atrophic cystitis;

- Prevention of recurrent infections of the lower urinary tract;

- Concomitant therapy for incontinence;

- Before- and postoperative therapy in post-menopausal vaginal surgical interventions access;

- Diagnosis in unclear Pap test results.

Dosage regimen

It should use the drug 1 soup. / day (the dose should not be exceeded). Suppository injected deep into the vagina at night before bedtime.

At atrophic changes of the vagina and vulva and vaginal infections concomitant therapy Treatment usually lasts about 3 weeks. Then, during the period, the duration of which the doctor sets, as a maintenance dose used for 1-2 vaginal soup. vagina weekly.

At atrophic changes of the lower urinary tract vaginal suppositories to be applied daily for 3 weeks.

To maximum effect It may require an extension of treatment to 2 months.

To subsequent treatment as a maintenance dose apply for 1-2 vaginal soup. weekly.

To before- and postoperative therapy in surgical vaginal access use of the drug is carried out daily for 2 weeks before the planned operation and 1-2 times a week after the surgery for a period of, doctor set.

At diagnostic tests paintings cell vaginal smear vaginal suppositories are used daily for 1-2 weeks before the scheduled sampling on analysis.

Depending on the degree of estrogen deficiency in post-menopausal patients vaginal suppositories may be applied over a longer period of time. In this case, to decide whether further treatment is necessary to at least, than every 6 months take a gynecological examination of vaginal smears for analysis.

To use the vaginal suppository of the upper edges of the film thus divide, so you can easily remove the suppository.

Side effect

On the part of the endocrine system: sometimes – early treatment can intermenstrual spotting vaginal discharge, soreness, sensitivity and increase the size of the breast, hypersecretion of cervical mucus, vaginal discharge, a temporary increase in body weight due to fluid retention.

From the digestive system: sometimes – kišečnaâ or how želčnaâ, jaundice, nausea, flatulence, anorexia, diarrhea.

Local reactions: sometimes – irritation of the vagina, itchy, burning, a feeling of heat and redness.

Other: rarely – migrenepodobnaya headache; rarely – a feeling of heaviness in the legs, leg cramps.

Side effects, associated with the endocrine system, may indicate an overdose of the drug and therefore, usually, disappear after dose reduction.

Contraindications

- Estrogen-dependent malignancies uterus or mammary glands or suspected them;

- Genital or uterine bleeding of unknown etiology;

- Thrombophlebitis or thromboembolic disease in active phase;

- Pregnancy;

- Lactation.

FROM caution use in patients with thrombophlebitis, thrombosis, thromboembolism during treatment with estrogens in history, family hyperlipoproteinemia, pancreato, эndometrioze, gallbladder disease in history (especially cholelithiasis), severe hepatic insufficiency, jaundice (incl. a history of previous pregnancy during), hepatic porphyria, LM, hypercalcemia, associated with bone metastases of breast cancer.

Pregnancy and lactation

Do not use this drug during pregnancy and breastfeeding.

Cautions

The use of vaginal suppositories Estrokad^® It should be carried out exclusively under regular medical supervision. Before the start of every reception 6 months of treatment is recommended a thorough general medical and gynecological examination, including the study of mammary glands. This is especially important during long and repeated vaginal bleeding.

Perhaps treatment of urinary tract infections during therapy Estrokadom^®.

The physician should decide about the continuation of therapy Estrokadom^® at:

- The debut of migraine headaches;

- Repeated unusually severe headaches;

- The first sign of phlebitis;

- Thromboembolic symptoms;

- The appearance of jaundice;

- High blood pressure;

- Severe visual impairment.

Overdose

Side effects, associated with the endocrine system, may indicate an overdose of the drug and therefore, usually, disappear after dose reduction.

Drug Interactions

In an application Estrokada^® barbiturates, antiepileptic drugs (incl. Carbamazepine, phenytoin) intensifies metabolism of steroid hormones, which can lead to inefficiency estriol.

In an application Estrokada^® with antibiotics (incl. ampicillin, rifampicin), drugs for general anesthesia, opioid analgesics, anxiolytics, some antihypertensive drugs, ethanol reduces the effectiveness of estriol.

With simultaneous use of estriol increases the effects of lipid-lowering drugs.

With simultaneous use of estriol reduces the effects of male hormones, antykoahulyantov, Antidepressants, diuretic, antihypertensive and hypoglycemic drugs.

With simultaneous use of folic acid and thyroid medications increase the effect of estriol.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life – 3 year.