Composition
Active ingredient:
estriol 500 mcg;
Auxiliary substance:
semisynthetic glycerides (such as “Suppocir”) – 1999.5 mg
Pharmacological action
Estrogen synthesized in the human body. Once in the bloodstream, it forms a complex with specific receptors (in the uterus, vagina, urethra, breast, liver, hypothalamus, pituitary gland), stimulates the synthesis of DNA and proteins. It has a selective effect, mainly on the cervix, vagina, vulva, increases the proliferation of the epithelium of the vagina and cervix, stimulates its blood supply, helps restore the epithelium with its atrophic changes during premenopause and menopause, normalizes the pH of the vaginal environment, the vaginal microflora, increases the resistance of its epithelium to infectious and inflammatory processes, affects the quality and quantity of cervical mucus. The effect on the endometrium is insignificant (there is a slight risk of uterine bleeding).
It has a hypolipidemic effect, slightly increases the concentration of beta-lipoproteins in the blood, increases sensitivity to the action of insulin, improves glucose utilization, and stimulates the liver to produce globulins that bind sex hormones, renin, HDL, and blood clotting factors. Due to its participation in the implementation of positive and negative feedback in the hypothalamic-pituitary-ovarian system, estriol is able to cause moderate central effects; it stimulates parasympathicomimetic reactions.
Pharmacokinetics
Absorption is high. The time to reach Cmax in blood plasma with intravaginal application is 1-2 hours. Binding to plasma albumins is 90%.
Excretion is mainly carried out by the kidneys in the form of metabolites (a few hours after ingestion and lasts up to 18 hours),2% is excreted unchanged through the intestine.
Indications
- atrophy of the mucous membrane of the lower urinary tract, caused by estrogen deficiency, pre – and postoperative therapy in women in the postmenopausal period during surgical interventions vaginal access, menopause (hot flashes and increased sweating at night, etc. );
- the infertility caused by cervical factor;
- dyspareunia, vaginal dryness, itching, frequent urination, mild urinary incontinence;Â
- diagnosis with unclear results of a vaginal smear for cytology.
Contraindications
Hypersensitivity, thrombosis (venous and arterial), embolism, severe liver function disorders, hormone-dependent tumors of the uterus or mammary glands, uterine bleeding of unclear etiology, otosclerosis, severe itching or cholestatic jaundice, as well as increased manifestations during previous pregnancy or while taking steroid medications, pregnancy.
Side effects
Tightness or pain in the mammary glands, fluid retention, nausea, hypersecretion of cervical mucus, arterial hypertension, calf muscle cramps, headache, visual disturbances, pigmented spots on the skin; local irritation or itching (cream).
Interaction
Inducers of microsomal oxidation (phenobarbital, carbamazepine, phenytoin, rifampicin, rifabutin, nevirapine, efavirenz) enhance estrogen metabolism; powerful inhibitors (ritonavir, nelfinavir) significantly inhibit metabolism.
Preparations of St. John’s wort can induce estrogen metabolism.
Estriol enhances the effect of lipid-lowering agents.
Reduces the effects of male sex hormones, anticoagulants, antidepressants, diuretics, hypotensive, hypoglycemic agents.
How to take, course of use and dosage
Intravaginally, before going to bed.
In case of atrophy of the mucous membrane of the lower parts of the urogenital tract,1 suppository (0.5 mg) is prescribed daily for the first 2-3 weeks, then the dose is gradually reduced, based on the symptoms,1 suppository (0.5 mg) 2 times a week.
Pre-and postoperative therapy in postmenopausal women – 1 suppository (0.5 mg) for 2 weeks before or after surgery.
As a diagnostic tool – 1 suppository every other day for a week before taking the next smear.
If the next dose of the drug was missed, you should take it immediately. However, if this is detected only on the day of taking the next dose, you should continue taking the drug according to the usual scheme, without making up for the missed dose. Do not use 2 doses in one day.
Product form
vaginal suppositories
Storage conditions
Store in a dry place, protected from light, at a temperature of 2-25 °C
Shelf life
3 years
Active ingredient
Estriol
Dosage form
suppositories vaginal
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