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Active ingredients
Estriol
Release form
Cream
Composition
In 1 g of cream: Estriol (estriol) 1 mg. Excipients: octyldodecanol, cetyl palmitate, glycerol, cetyl alcohol, stearyl alcohol, polysorbate, sorbitan stearate, lactic acid, chlorhexidine dihydrochloride, sodium hydroxide, purified water.
Pharmacological effect
Estrogenic drug. Analogue of the natural female hormone. Restores estrogen deficiency in postmenopausal women and reduces postmenopausal symptoms. Most effective in treating urogenital disorders. With atrophy of the mucous membrane of the lower urinary tract, estriol contributes to the normalization of the urinary tract epithelium and contributes to the restoration of normal microflora and physiological pH in the vagina. Increases the resistance of the urinary tract epithelial cells to infections and inflammation, reducing complaints such as pain during intercourse, dryness, itching in the vagina, reduces the likelihood of vaginal infections and urinary tract infections, helps normalize urination, prevents urinary incontinence. In contrast to other estrogens estriol has a short period of action, since it is retained in the nuclei of the cells of the endometrium for a short period of time. It is assumed that a single daily dose does not cause endometrial proliferation. Therefore, cyclic administration of progestogen is not required and withdrawal bleeding does not occur. In addition, it is shown that estriol does not increase mammographic density.
Pharmacokinetics
Absorption When administered orally as well as topically, estriol is rapidly and almost completely absorbed. C max estriol in plasma is achieved 1-2 h after intravaginal use. Distribution In plasma, almost all (90%) estriol is bound to albumin and, unlike other estrogens, is almost not bound with the sex hormone-binding globulin (SHBG). Excretion Estriol (in the bound form) is eliminated mainly by the kidneys; about 2% is excreted unchanged through the intestines. Excretion of metabolites with urine begins within a few hours after the use of the drug and lasts 18 hours.
Indications
Hormone replacement therapy (HRT) for the treatment of atrophy of the mucous membrane of the lower urogenital tract associated with estrogen deficiency; pre- and postoperative treatment of women in the postmenopausal period with vaginal access operations; for diagnostic purposes with unclear results of cytological examination of the cervix (suspected tumor process) on the background of atrophic changes.
Contraindications
Established, history or suspected breast cancer; diagnosed or suspected estrogen-dependent tumors (for example, endometrial cancer); bleeding from the vagina of unknown etiology; untreated endometrial hyperplasia; the presence of venous thrombosis at the present time and in history; active or recent thromboembolic arterial disease (eg, angina pectoris, myocardial infarction); liver disease in the acute stage or a liver disease in history, after which the indicators of liver function did not return to normal; porphyria; established hypersensitivity to the active substance or to any of the excipients of the drug.
Precautionary measures
With care If any of the following conditions are present or such a condition has been noted previously and / or worsened during previous pregnancies or previous hormone treatments, then such a patient should be under the direct supervision of a physician. It must be borne in mind that these conditions may recur or worsen during treatment with Ovestin; especially if they are present: leiomyoma (uterine fibroids) or endometriosis; previous thromboembolic disorders or existing risk factors for such disorders; risk factors for estrogen-dependent tumors, for example, 1st degree of heredity for breast cancer; arterial hypertension; benign liver tumors (for example, liver adenoma); diabetes mellitus with the presence or absence of a vascular component; cholelithiasis; jaundice (including a history of a previous pregnancy); liver failure; migraine or severe headache; systemic lupus erythematosus; endometrial hyperplasia in history; epilepsy; asthma; otosclerosis; familial hyperlipoproteinemia; pancreatitis.
Use during pregnancy and lactation
Drug Ovestin; contraindicated in pregnancy. In case of pregnancy during treatment with Ovestin ;, treatment must be immediately canceled. The results of most epidemiological studies conducted to date regarding the unintended effects of estrogen on the fetus, indicate the absence of teratogenic or fetotoxic effects. Ovestin; It is not recommended to appoint during breastfeeding. Estriol is excreted in breast milk and may reduce the formation of milk.
Dosage and administration
The cream should be inserted into the vagina using a calibrated applicator at night (before bedtime) .1 application (applicator filled to the ring mark) contains 500 mg of cream, which corresponds to 500 μg of estriol. When treating atrophy of the mucous membrane of the lower urinary tract - 1 application / during the first weeks (maximum 4 weeks), followed by a gradual decrease in dose, based on the relief of symptoms, until a maintenance dose is reached (ie, 1 application 2 times a week). In the pre- and postoperative therapy of postmenopausal women auznom period during surgery vaginal access - 1 application / day for 2 weeks prior to surgery; 1 application 2 times a week for 2 weeks after surgery. For diagnostic purposes, with unclear results of cervical cytology, 1 application every other day for a week before taking the next smear. When skipping a dose, you should enter the missed dose on the same day the patient will remember this (the dose should not be administered 2 times / day). In the future, applications are carried out in accordance with the usual dosing regimen. At the beginning or during the continuation of treatment of postmenopausal symptoms, the smallest effective dose must be applied for the shortest period of time. Women who do not receive HRT or women who are transferred from continuous oral administration of the combined drug for HRT, treatment with Ovestin can be started any day. Women who are switching from a cyclic regimen of drugs for hormone therapy should begin treatment with Ovestin cream; 1 week after discontinuation of HRT drugs. Instructions for use for patients1.The cream is introduced into the vagina at night (at bedtime) .2. 3. Remove the cap from the tube, turn the cap over and use a sharp rod to open the tube. Roll up the applicator on the tube. Squeeze the tube to fill the applicator with cream until the piston stops. Unscrew the applicator from the tube and close the tube with a cap. In the prone position, the end of the applicator is inserted deep into the vagina and slowly pushes the piston until it stops, introducing the cream. After the drug is injected, remove the piston from the cylinder and wash the cylinder and piston with warm water and soap. Do not use detergents. After that, the cylinder and piston are rinsed abundantly with clean water. Do not immerse the applicator in hot or boiling water.
Side effects
As in the case of the use of any other drug that is applied to the surface of the mucous membranes, Ovestin cream; may sometimes cause local irritation or itching. Sometimes there may be sensitivity, tension, soreness, an increase in the size of the mammary glands. These undesirable reactions are usually short and passing, but at the same time may indicate the use of too high a dose. Also acyclic bleeding, breakthrough bleeding, metrorrhagia are also observed. At HRT using estrogen-progestogen-containing drugs, the following side effects were also observed, communication which with the use of Ovestin has not been proven: benign and malignant estrogen-dependent neoplasias (endometrial cancer and mammary glands); venous thromboembolism (deep vein thrombosis of the legs or pelvis, pulmonary embolism) occurs more often with HRT than with no therapy; myocardial infarction, stroke; cholelithiasis; skin and subcutaneous diseases (chloasma, erythema multiforme, erythema nodosum, hemorrhagic purpura); dementia; increased libido.
Overdose
The acute toxicity of estriol in animals is very low. An overdose of the drug Ovestin; with vaginal administration is unlikely. However, in the case of ingestion of large quantities of the drug in the gastrointestinal tract, nausea, vomiting and cessation of bleeding in women may develop. Treatment: There is no specific antidote. If necessary, symptomatic treatment should be carried out.
Interaction with other drugs
In clinical practice, no interaction between the drug Ovestin; and other drugs. Estrogen metabolism can be enhanced when they are used in combination with compounds that induce enzymes involved in drug metabolism, especially cytochrome P450 isoenzymes, such as anticonvulsants (for example, phenobarbital, phenytoin, carbamazepine) and antimicrobial agents (for example, rifampicin, rifabutin, nevirapine, efavirenz). Ritonavir and nelfinavir exhibit inducing properties when used in combination with steroid hormones. nye preparations containing St. John's wort (Hypericum perforatum), may induce estrogen metabolism estrogenov.Povyshenny metabolism may lead to a decrease in their clinical effekta.Estriol enhances the effect of hypolipidemic drugs sredstv.Oslablyaet effects of male sex hormones, anticoagulants, antidepressants, diuretics, hypotensive, hypoglycemic drugs Drugs for general anesthesia, opioid analgesics, anxiolytics, some antihypertensive drugs, ethanol t effectiveness preparata.Folievaya acid and thyroid drugs increase the action of estriol.
special instructions
Therapy should be discontinued if a contraindication is detected and / or when the following conditions occur: jaundice and / or impairment of liver function; a significant increase in blood pressure; the resumption of headaches for the type of migraine; pregnancy. In the presence of vaginal infections, concomitant specific treatment is recommended.