Ovestin cream vag. 1mg / g 15g No. 1

Dosage form

A homogeneous mass of creamy consistency from white to almost white with a specific odor.

Release form

Vaginal cream 1 mg / 1 g. 15 g of cream are placed in an aluminum tube, closed with a screwed polyethylene cap.

A tube with an applicator consisting of a styrene-acrylonitrile cylinder and a polyethylene piston, and instructions for use are placed in a cardboard box.

Structure

Active substance:

Estriol 1 mg / g

Excipients:

Octyldodecanol 50.0 mg, cetyl palmitate 15.0 mg, glycerol 120.0 mg, cetyl alcohol 36.7 mg, stearyl alcohol 88.4 mg, polysorbate 60 32.4 mg, sorbitan stearate 7.6 mg, lactic acid 4, 0 mg, chlorhexidine dihydrochloride 0.1 mg, sodium hydroxide to pH 4.0, purified water to 1000.0 mg.

pharmachologic effect

Ovestin® contains estriol, an analogue of the natural female hormone. It compensates for estrogen deficiency in postmenopausal women and relieves postmenopausal symptoms. The most effective estriol in the treatment of genitourinary disorders. In the case of atrophy of the mucous membrane of the lower parts of the genitourinary tract, estriol helps to normalize the epithelium of the genitourinary tract and helps restore normal microflora and physiological pH in the vagina. As a result, it increases the resistance of epithelial cells of the genitourinary tract to infection and inflammation, reducing complaints such as soreness during intercourse, dryness, itching in the vagina, reduces the likelihood of vaginal and urinary tract infections, helps to normalize urination and prevents urinary incontinence.

Unlike other estrogens, estriol has a short duration of action, since it is retained in the nuclei of endometrial cells for a short period of time.

It is assumed that a single administration of a daily dose does not cause endometrial proliferation.

Therefore, cyclic administration of progestogen is not required and withdrawal bleeding does not occur.

In addition, estriol has been shown to not increase mammographic density.

Pharmacokinetics

Intravaginal administration of estriol provides optimal bioavailability at the site of action.

Estriol is also absorbed and enters the general bloodstream, which is manifested by a rapid increase in the concentration of unbound estriol in plasma.

The maximum concentration in plasma is observed 1-2 hours after administration.

In plasma, almost all (90%) of estriol is bound to albumin and, unlike other estrogens, is practically not bound to globulin, which binds sex hormones.

Estriol metabolism consists mainly in the transition to a conjugated and unconjugated state during intestinal-hepatic circulation.

Estriol, being the end product of metabolism, is mainly excreted in the urine in bound form.

Only a small part (? 2%) is excreted in the feces, mainly in the form of unbound estriol.

The half-life is approximately 6-9 hours.

After vaginal administration of 0.5 mg of estriol, the maximum Cmax concentration is approximately 100 pg / ml, the minimum Cmin concentration is approximately 25 pg / ml, and the average Cav concentration is approximately 70 pg / ml.

After 3 weeks of daily application of 0.5 mg of vaginal estriol, the Cav value decreased to 40 pg / ml.

Side effects

As with any other drug that is applied to the surface of the mucous membranes, Ovestin® cream can sometimes cause local irritation or itching.

Sometimes there may be tension, soreness, tenderness and enlargement of the mammary glands.

These adverse reactions are usually short-lived and transient, but at the same time, they may indicate the use of too high a dose.

Also found: acyclic spotting, breakthrough bleeding, metrorrhagia.

Other adverse reactions have been reported with estrogen monotherapy or combination therapy with estrogens and proges

Name ENG

OVESTIN

Clinical and pharmacological group

Estrogen drug

ATX code

Estriol

Dosage

1mg / g x 15g

Structure

Active substance: Estriol 1 mg / g.

Excipients: Octyldodecanol 50.0 mg, cetyl palmitate 15.0 mg, glycerol 120.0 mg, cetyl alcohol 36.7 mg, stearyl alcohol 88.4 mg, polysorbate 60 32.4 mg, sorbitan stearate 7.6 mg, milk acid 4.0 mg, chlorhexidine dihydrochloride 0.1 mg, sodium hydroxide to pH 4.0, purified water to 1000.0 mg.

Indications

Hormone replacement therapy (HRT) for the treatment of atrophy of the mucous membrane of the lower urinary tract associated with estrogen deficiency in postmenopausal women.

Pre- and postoperative therapy of women in the postmenopausal period with surgical interventions with vaginal access.

As an auxiliary diagnostic tool when obtaining an atrophic picture of a cervical smear.

Contraindications

Established, history, or suspected breast cancer.

Diagnosed or suspected estrogen-dependent tumors (eg, endometrial cancer).

Vaginal bleeding of unknown etiology.

Untreated endometrial hyperplasia.

Current and history of venous thrombosis (deep vein thrombosis, pulmonary thromboembolism).

Confirmed thrombophilia (for example, a deficiency of protein C, protein S or antithrombin (see section Special instructions")).

Thrombosis (venous and arterial) and thromboembolism at present or in history (including deep vein thrombosis, pulmonary embolism, myocardial infarction, stroke), cerebrovascular disorders

conditions preceding thrombosis (including transient ischemic attacks, angina pectoris) at present or in anamnesis.

Acute liver disease or a history of liver disease after which liver function tests have not returned to normal.

Established hypersensitivity to the active substance or to any of the excipients of the drug.

Porphyria.,

Carefully,

With caution (under the close supervision of a physician), Ovestin® should be used if any of the following diseases or conditions are present, or if these diseases or conditions have been noted earlier and / or worsened during previous pregnancies or previous hormonal treatment (since they can recur or worsen during treatment with Ovestin®):

Leiomyoma (uterine fibroids) or endometriosis

Risk factors for thromboembolism (see section "Special instructions").

Risk factors for estrogen-dependent tumors, for example, 1st degree of heredity for breast cancer.

Arterial hypertension.

Benign liver tumors (eg, liver adenoma).

Diabetes mellitus with or without diabetic angiopathy.

Cholelithiasis.

Jaundice (including a history of a previous pregnancy).

Liver failure.

Migraine or (severe) headache.

Systemic lupus erythematosus.

History of endometrial hyperplasia (see section "Special instructions").

Epilepsy.

Bronchial asthma.

Otosclerosis.

Familial hyperlipoproteinemia.

Pancreatitis

INN / Active ingredient

estriol

Storage conditions and periods

At a temperature of 2-25 degrees (do not freeze).

Expiration date: 3 years

Specifications

Category

Hormonal agents

Scope of the drug

Endocrine system

Release form

Cream

Manufacturer country

Germany

Package quantity, pcs

one

Way of introduction

Vaginally

Vacation conditions

Without recipe

Brand name

Aspen Pharma

Components

applicator

The amount of the dosage form in the primary package

15 g

Primary packaging type

Tuba

Type of consumer packaging

Pack of cardboard

Pharmaco-therapeutic group

Estrogen

Anatomical and therapeutic characteristics

G03CA04 Estriol

Dosage form

Vaginal cream

Expiration date in days

1095

Dosage (volume) of the substance in the preparation

estriol 1 mg

Package weight, g

twenty

Mode of application

:

Ovestin® Cream should be inserted into the vagina using a calibrated applicator at night before bed. < br> 1 application (applicator filled up to the annular mark) contains 0.5 g of cream, which corresponds to 0.5 mg of estriol. < br> In the treatment of atrophy of the mucous membrane of the lower urinary tract: < br> 1 application per day for the first weeks (maximum 4 weeks), followed by a gradual dose reduction, based on the dynamics of symptoms, until a maintenance dose is reached (i.e. 1 introduction twice a week). < br> Pre- and postoperative therapy for women in the postmenopausal period with surgical interventions by vaginal access: < br> 1 application per day for 2 weeks before the operation 1 application twice a week for 2 weeks after surgery. < br> For diagnostic purposes in case of unclear results of cytological examination of the cervix: < br> 1 application every other day for a week before taking the next smear. < br> < br> Instructions for use for patients < br> 1. The cream is injected into the vagina at night before bedtime. < br> 2. Remove the cap from the tube, turn the cap over and use a sharp rod to open the tube. < br> 3. Screw the applicator onto the tube. < br> 4. Squeeze the tube for filling the applicator with cream until the plunger stops. 5. Unscrew the applicator from the tube and close the tube with a cap. 6. In the "lying" position, the cream is introduced, the end of the applicator is inserted deep into the vagina and slowly pressed on the piston until it stops. < br> After injection of the drug, the piston is removed from the cylinder and the cylinder and piston are washed with warm water and soap.Do not use detergents. Then the cylinder and piston are rinsed abundantly with clean water. < br> DO NOT LET THE APPLICATOR INTO HOT OR BOILING WATER. < br> The missed dose must be entered on the same day, as soon as the patient remembers this (the dose should not be administered twice a day). Further applications are carried out in accordance with the usual dosage regimen. < br> When starting or continuing the treatment of climacteric symptoms, the lowest effective dose should be used for the shortest period of time. < br> In women who are not receiving HRT, or women who are switched from continuous oral administration of the combined HRT medication, treatment with Ovestin® cream can be started any day. Women who switch from a cyclic regimen of taking HRT drugs,should begin treatment with Ovestin® cream one week after discontinuation of HRT drugs.

Information on technical characteristics, delivery set, country of manufacture "