Buy Ovestin pills 2 mg, 30 pcs
  • Buy Ovestin pills 2 mg, 30 pcs

Estriol

N.V.Organon
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2019-09-19
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Clinical Pharmacology

Pharmacotherapeutic group: Estrogens.

ATC code: G03CA04

Pharmacological properties

Pharmacodynamics

Ovestin® contains the natural female sex hormone estriol. In the period preceding menopause and in postmenopausal (natural or surgical), estriol is used to treat symptoms caused by estrogen deficiency.

Estriol has a selective effect mainly on the cervix, vagina, vulva and is particularly effective for the treatment of urogenital symptoms caused by estrogen deficiency. In cases of atrophy of the vaginal mucosa, estriol causes increased proliferation of the epithelium of the vagina and cervix, stimulates its blood supply, helps restore epithelium, normal microflora and physiological pH of the vaginal environment, affects the quality and quantity of cervical mucus. As a result, the resistance of epithelial cells to infection and inflammation increases. Unlike other estrogens, estriol has a short-term effect, since it lingers for a short time in the nuclei of endometrial cells and, subject to the recommended dosing regimen, one should not expect endometrial proliferation. In this regard, the cyclic use of progestogens is not necessary, postmenopausal withdrawal bleeding does not occur.

Pharmacokinetics

After ingestion, estriol is rapidly and almost completely absorbed in the gastrointestinal tract. The maximum concentration of unconjugated estriol in plasma is achieved within 1 hour after administration. About 90% of estriol binds to plasma albumin, and, unlike other estrogens, estriol hardly binds to sex hormone-binding globulin (GSPG). The metabolism of estriol consists mainly of conjugation and deconjugation during the enterohepatic circulation. Estriol, the end product of metabolism, is mainly excreted in the urine in conjugated form. Only a small part (? 2%) is excreted in the feces, mainly in the form of unconjugated estriol.

Indications

  • Atrophy of the lower end of the urogenital tract due to estrogen deficiency, in particular, to treat symptoms such as dyspareunia, vaginal dryness and itching, to prevent recurrent infections of the vagina and lower urinary tract; for the treatment of urinary disorders (eg, increased frequency, dysuria) and moderate urinary incontinence;
  • Pre- and postoperative treatment for postmenopausal vaginal surgery;
  • Climacteric disorders, such as hot flashes and night sweats;
  • As an auxiliary diagnostic tool when receiving an atrophic picture of a cervical smear;
  • Infertility due to cervical factors.

Composition

Active ingredient: Estriol 2.0 mg;

Excipients: colloidal silicon dioxide 0.75 mg, potato starch 10.0 mg, magnesium stearate 0.50 mg, povidone 1.0 mg, lactose monohydrate to

100.0 mg (about 87.75 mg), q.s. * distilled water

* - removed during production.

Estriol is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Ovestin N.V.Organon Netherlands pills
Ovestin N.V.Organon Netherlands cream
Ornion Vertex Russia cream
Ovipol Clio Pharmaprim Moldova suppositories
Estrocard Ferring Germany suppositories

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Estriol

Dosage and Administration

The drug is administered orally.

The daily dose for oral administration should not exceed 8 mg. With atrophy of the lower parts of the urogenital tract due to estrogen deficiency: 4-8 mg per day for the first 4 weeks, followed by gradual reduction of the dose in accordance with the symptoms until a maintenance dose of 1-2 mg per day is reached. The smallest effective dose should be used. In the case of long-term treatment in women with an intact uterus, it is necessary to control the state of the endometrium or additionally use progestogens in therapy (see the section "Special Instructions").

Pre- and postoperative treatment for vaginal operations in the postmenopausal period: 4-8 mg per day for 2 weeks before surgery, 1-2 mg per day for 2 weeks after surgery.

Treatment of menopausal disorders (hot flashes, night sweats): 4-8 mg per week with a gradual decrease in dose. For maintenance therapy, the minimum effective dose should be used for the least prolonged period of time (see section "Special Instructions").

For infertility due to cervical factor: as a rule, 1-2 mg is administered per day from day 6 to day 15 of the menstrual cycle. However, in different patients, the daily dose may vary from 1 to 8 mg. The dose should be increased every month to achieve the optimal effect on the mucous membrane of the cervix. Differential diagnosis in case of doubtful cervical smear of atrophic type: 2-4 mg per day for 7 days before taking the next smear. If a woman missed taking the next dose and the delay was no more than 12 hours, you need to take it as soon as possible.

If the delay is more than 12 hours, you should skip one dose and then take the drug at regular times.

pills are taken with a glass of water, preferably at the same time of day, every day. The daily dose should be taken in one step (see "Special instructions"). In women who have not previously received HRT or have taken HRT in a continuous combination regimen, treatment with Ovestin® can be started at any time. In women who have taken HRT on an intermittent basis, Ovestin® should be administered one week after the completion of the cycle.

Adverse reactions

According to the monitoring of security studies there are the following adverse reactions:

On the part of the digestive system: - Nausea.

From the water and electrolyte exchange: - fluid retention.

On the part of the reproductive system: - tenderness and tension of the mammary glands; - intermenstrual bloody spotting from the vagina; - cervical hypersecretion.

Adverse reactions are usually transient and may also indicate an overdose of the drug. It is reported about other adverse reactions that have arisen on the background of estrogen monotherapy or combination therapy with estrogens and progestogens:

Reproductive system: - estrogen-dependent benign and malignant tumors, incl. endometrial cancer (for details, see the “Contraindications” and “Special Instructions” sections).

On the part of the digestive system: - Gall bladder disease.

On the part of the skin: - Chloasma, erythema multiforme, erythema nodosum, vascular purpura.

From the side of the central nervous system: - headache; - dementia at the beginning of HRT in a continuous mode after 65 years (see the section "Special Instructions"). There is evidence of the development of the risk of breast cancer, ovarian cancer, the risk of venous thromboembolism, the risk of coronary heart disease, the risk of ischemic stroke (for more information, see the Special Guidelines section).

Contraindications

WITHcautionthe drug should be prescribed in the following conditions:

  • familial hyperlipoproteinemia;
  • increased risk of thromboembolic complications;
  • systemic lupus erythematosus;
  • long immobilization, serious surgical interventions;
  • severe liver disease;
  • a history of gallbladder disease (especially cholelithiasis);
  • hepatic porphyria;
  • severe itching or cholestatic jaundice (including a history of a previous pregnancy);
  • pancreatitis;
  • endometriosis;
  • leiomyoma;
  • bronchial asthma;
  • arterial hypertension;
  • hypercalcemia due to bone metastasis of breast cancer;
  • herpes pregnant;
  • epilepsy;
  • otosclerosis.

Drug interactions

There were no cases of drug interactions with Ovestin®. However, there are data on the enhancement of the pharmacological effect of glucocorticosteroids, lipid-lowering agents when used together with estrogens. If necessary, the dose of glucocorticosteroids can be reduced. Possible weakening of the effects of drugs of male sex hormones, anticoagulants, antidepressants, diuretic, hypotensive and hypoglycemic drugs. Barbiturates, anti-epileptic drugs (carbamazepine, phenytoin), nevirapine and efavirenz antiretroviral drugs, herbal preparations containing Hypericum Perforatum, which make them bruise, increase the metabolism of steroid hormones. Ritonavir and nelfinavir exhibit inducing properties when used simultaneously with steroid hormones. From a clinical point of view, an increase in estrogen metabolism may lead to a decrease in the effectiveness of Ovestin® 7 and a change in the nature of uterine bleeding. Antibiotics (griseofulvin, ampicillin, rifampicin), drugs for general anesthesia, narcotic analgesics, anxiolytics, antiepileptic drugs, some antihypertensive drugs, ethanol reduce the effectiveness of estrogens. Folic acid and thyroid hormone drugs enhance the effect of estriol. Estriol can change the effectiveness of oral anticoagulants, increase the pharmacological effect of succinylcholine, theophylline, foleandomycin.

Pregnancy and Lactation

Ovestin is contraindicated for use during pregnancy and lactation (breastfeeding).

Special instructions

For the treatment of menopausal symptoms of HRT, it is necessary to begin only in relation to symptoms that adversely affect the quality of life. In all cases, it is necessary to conduct a thorough assessment of the risks and benefits of treatment at least once a year and HRT should be continued only as long as the benefits outweigh the risks.

Overdosage

Overdose causes nausea, vomiting and vaginal bleeding. Symptomatic treatment.

Studies and clinical trials of Estriol (Click to expand)
  1. Involvement of genotoxic effects in the initiation of estrogen-induced cellular transformation: Studies using Syrian hamster embryo cells treated with 17β-estradiol and eight of its metabolites
  2. Combination of elevated maternal serum alpha-fetoprotein (MSAFP) and low estriol is highly predictive of anencephaly
  3. Levels of unconjugated estriol and other maternal serum markers in pregnancies with Smith-Lemli-Opitz (RSH) syndrome fetuses
  4. Antimammary carcinogenic activity of 17-alpha-ethinyl estriol
  5. Inhibition of radiogenic mammary carcinoma in rats by estriol or tamoxifen
  6. Unexplained elevated midtrimester maternal serum levels of alpha fetoprotein, human chorionic gonadotropin, or low unconjugated estriol: Recurrence risk and association with adverse perinatal outcome
  7. Elevated maternal serum alpha-fetoprotein with low unconjugated estriol and the risk for lethal perinatal outcome
  8. Isolated familial adrenocorticotropin deficiency: Prenatal diagnosis by maternal plasma estriol assay
  9. Prenatal diagnosis of P450 oxidoreductase deficiency (ORD): A disorder causing low pregnancy estriol, maternal and fetal virilization, and the Antley–Bixler syndrome phenotype
  10. Recognition of Smith–Lemli–Opitz syndrome (RSH) in the fetus: Utility of ultrasonography and biochemical analysis in pregnancies with low maternal serum estriol
  11. Treatment of multiple sclerosis with the pregnancy hormone estriol
  12. Determination of estriol and creatinine in urine by high performance liquid chromatography
  13. Direct determination of estriol 3- and 16-glucuronides in pregnancy urine by column-switching liquid chromatography with electrospray tandem mass spectrometry
  14. Studies on the mass fragmentographic determination of plasma estriol
  15. Maternal height, pregnancy estriol and birth weight in reference to breast cancer risk in Boston and Shanghai
  16. The contribution of hepatic steroid metabolism to serum estradiol and estriol concentrations in nonylphenol treated MMTVneu mice and its potential effects on breast cancer incidence and latency
  17. Measurement of serum unconjugated estriol and estradiol by high-performance liquid chromatography
  18. The adsorption of estriol by the plasma proteins
  19. Inhibition of imidazole-induced tyrosinase activity by estradiol and estriol in cultured B 16/C3 melanoma cells
  20. Development of an estriol-releasing intrauterine device
  21. Determination of estradiol and estriol by single-sweep polarography
  22. Direct chemiluminescence immuoassay of estriol and progresterone and their ratio during pregnancy
  23. Anomalous epimerization of estriol to 16-epiestriol
  24. Bioluminescent enzyme immunoassay for estriol. Use of reversibly inactivated bacterial luciferase as label

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