Orniona, vaginal cream 0.1% 15 g

The Orniona® cream contains oestriol, an analog of the natural female hormone. Estriol is used to correct estrogen deficiency in pre- and postmenopausal women.

Effective in the treatment of urogenital disorders. In case of epithelium atrophy it stops these disorders, promotes restoration of normal microflora and physiological pH of the vagina thus increasing resistance of the vaginal epithelium to infectious and inflammatory processes. </Unlike other estrogens, estriol interacts with endometrial cell nuclei for a short period of time, so that when using the recommended daily dose (once a day) there is no proliferation of the endometrium. Thus, there is no need for cyclic supplemental progestagen administration, and there are no withdrawal bleeding in the postmenopausal period.

Pharmacokinetics

The introduction of estriol into the vagina provides optimal local bioavailability of the drug. Estriol is also absorbed into the blood, which is manifested by a rapid increase in the concentration of unconjugated estriol in plasma, with a maximum value 1-2 hours after administration. Unlike other estrogens, up to 90% of plasma estriol is bound to albumin rather than to hGH.

The metabolism of estriol in the body is reduced to its conjugation and deconjugation during enterohepatic circulation. Because estriol is the end product of metabolism, it is mainly excreted by the kidneys in conjugated form. Only a small proportion (2%) is excreted through the intestine, mostly in the unconjugated form.

Indications

atrophy of the mucous membrane of the lower genitourinary tract caused by estrogen deficiency (which is manifested by unpleasant sensations in the vagina: pain during sexual intercourse, vaginal dryness, itching; urinary disturbances (increased frequency of urination and dysuria) and mild urinary incontinence) as hormone replacement therapy (HRT);
pre- and postoperative therapy in postmenopausal women who are about to undergo or have already undergone surgery via vaginal access;
for diagnostic purposes in case of unclear results of cytological examination of the cervical epithelium against the background of atrophic changes.

Pharmacological effect

Orniona® cream contains estriol, an analogue of the natural female hormone. Estriol is used to correct estrogen deficiency in pre- and postmenopausal women.

Effective in the treatment of urogenital disorders. In the case of epithelial atrophy, it stops these disorders, helps restore normal microflora and the physiological pH of the vagina, thereby increasing the resistance of the vaginal epithelium to infectious and inflammatory processes.

Unlike other estrogens, estriol interacts with the nuclei of endometrial cells for a short period of time, due to which endometrial proliferation does not occur when using the recommended daily dose (once a day). Thus, there is no need for cyclic additional administration of progestogens, and withdrawal bleeding is not observed in the postmenopausal period.

Pharmacokinetics

The introduction of estriol into the vagina ensures optimal local bioavailability of the drug. Estriol is also absorbed into the blood, which is manifested by a rapid increase in the concentration of unconjugated estriol in plasma with a maximum value 1–2 hours after administration. Unlike other estrogens, up to 90% of estriol in blood plasma is bound to albumin rather than SHBG.

The metabolism of estriol in the body is reduced to its conjugation and deconjugation during enterohepatic circulation. Since estriol is the end product of metabolism, it is mainly excreted by the kidneys in conjugated form. Only a small proportion (2%) is excreted through the intestines, mainly in unconjugated form.

Special instructions

To treat postmenopausal symptoms, HRT should only be started for symptoms that adversely affect quality of life. In all cases, a thorough assessment of the risks and benefits of treatment should be carried out at least once a year. HRT should only be continued for a period of time when the benefit outweighs the risk.

Medical examination/observation:

Before starting or resuming HRT, a detailed individual and family history should be obtained. Based on the medical history, contraindications and warnings for the use of the drug, it is necessary to conduct a clinical examination, including examination of the pelvic organs and mammary glands;
During treatment, it is recommended to conduct a general medical and gynecological examination, including examination of the mammary glands. The frequency and nature of examinations are individual, but at least once every 6 months. Women should be informed about the need to report changes in the mammary glands to their doctor. Tests, including mammography, must be performed in accordance with generally accepted screening standards.

Therapy should be discontinued if a contraindication is identified and/or if the following conditions/diseases occur:

jaundice and/or deterioration of liver function;
significant increase in blood pressure;
the occurrence or recurrence of migraine-type headaches;
pregnancy;
endometrial hyperplasia.

Other states:

Estrogens can cause fluid retention, and therefore patients with impaired renal function and cardiovascular insufficiency should be under close medical supervision;
estriol is a weak gonadotropin inhibitor and does not have other significant effects on the endocrine system;
there is no convincing evidence of improvement in cognitive function;
in the presence of vaginal infections, concomitant specific treatment is recommended.

To prevent endometrial stimulation, the dose of Ornion® cream should not exceed 1 administration (0.5 mg estriol) per day, and this dose should not be administered daily for more than 3 weeks in a row.

Impact on the ability to drive vehicles and operate machinery

Estriol does not affect coordination of movements, concentration and the ability to drive vehicles and other mechanisms.

Active ingredient

Estriol

Composition

Composition (100 g):

active substance: estriol 0.1 g;
excipients:
cetyl palmitate – 1.5 g;
glycerol (glycerin) – 12 g;
cetyl alcohol – 3.67 g;
stearyl alcohol (crodacol) – 8.84 g;
sorbitan stearate – 0.76 g;
macrogol 25 cetostearate (macrogol 25 cetostearyl ether, Cremophor A25) – 3.24 g;
ethanol 95% (ethyl alcohol 95%) – 5 g;
lactic acid – 0.4 g;
chlorhexidine dihydrochloride – 0.01 g;
sodium hydroxide – 0.12 g;
purified water – up to 100 g.

Contraindications

established hypersensitivity to the active substance or any of the excipients of the drug;
untreated endometrial hyperplasia;
known, known or suspected breast cancer;
diagnosed or suspected estrogen-dependent tumors (for example, endometrial cancer);
bleeding from the vagina of unknown etiology;
the presence of venous thrombosis currently and/or in history;
active or recent thromboembolic arterial disease (eg, angina, myocardial infarction);
acute liver disease or a history of liver disease after which liver function tests have not returned to normal;
porphyria;
pregnancy;
lactation period.

With caution: the current presence of any of the following conditions/diseases, or in cases where such a condition/disease has been noted previously and/or worsened during previous pregnancies or previous hormonal treatment, the patient should be under the direct supervision of a physician. It must be taken into account that these conditions/diseases may recur or worsen during treatment with Orniona®, especially if they are present:

leiomyoma (uterine fibroids) or endometriosis;
history of 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 or without angiopathy;
cholelithiasis;
jaundice, itching, herpes (including a history of previous pregnancy);
liver failure;
migraine or headache (severe);
systemic lupus erythematosus;
history of endometrial hyperplasia;
epilepsy;
bronchial asthma;
otosclerosis;
familial hyperlipoproteinemia;
pancreatitis.

Side Effects

Orniona® Cream may cause local irritation or itching.

Acyclic spotting, breakthrough bleeding, and metrorrhagia are possible.

In rare cases, breast tenderness or tenderness may occur.

As a rule, these side effects disappear after the first weeks of treatment, in addition, they may indicate that the dose of the drug was prescribed too high.

Interaction

In clinical practice, no interaction has been observed between topical estriol preparations and other drugs.

The metabolism of estrogens may be enhanced when used in combination with compounds that induce enzymes involved in drug metabolism (especially cytochrome P450 enzymes), such as anticonvulsants (e.g. phenobarbital, phenytoin, carbamazepine), antimicrobials (e.g. rifampicin, rifabutin, nevirapine, efavirenz, ritonavir, nelfinavir), barbiturates.

Herbal preparations containing St. John’s wort (Hypericum perforatum) may induce estrogen metabolism.

Increased metabolism of estrogens may lead to a decrease in their clinical effect.

Estriol enhances the effect of lipid-lowering drugs; weakens the effects of male sex hormones, anticoagulants, antidepressants, diuretic, antihypertensive, hypoglycemic drugs.

Drugs for general anesthesia, narcotic analgesics, anxiolytics, some antihypertensive drugs, ethanol reduce the effectiveness of the drug.

Folic acid and thyroid medications enhance the estrogenic effect of estriol.

There is evidence that estrogens, incl. estriol, can enhance the pharmacological effect of corticosteroids and increase the activity of suxamethonium, theophylline and oleandomycin.

Overdose

When administered intravaginally, the likelihood of an overdose of Ornion® cream is low.

Symptoms: in case of accidental ingestion – nausea, vomiting, withdrawal bleeding.

Treatment: there is no specific antidote. If necessary, symptomatic therapy should be carried out.

Manufacturer

Vertex, Russia