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.

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

Menopause, Urinary incontinence, Night sweats, Itching and dryness in the genital area

• Atrophy of the mucous membrane of the lower parts of the genitourinary tract caused by estrogen deficiency (which is manifested by discomfort in the vagina: pain during intercourse, vaginal dryness, itching; impaired urination (increased frequency of urination and dysuria) and mild urinary incontinence) as hormone replacement therapy (HRT);
• Pre- and postoperative therapy in post-menopausal women undergoing or who have undergone vaginal surgery;
• For diagnostic purposes, with unclear results of cervical cytology and atrophic changes.

.

Active ingredient

Estriol

Composition

Composition (100 g):

• active ingredient: estriol 0.1 g;
• excipients:
• cetylpalmitate – 1.5 g;
• glycerol (glycerin) – 12 g;
• cetyl alcohol – 3.67 g;
• stearyl alcohol (crodacol) – 8,84 g;
• sorbitan stearate – 0,76 g;
• macrohaole 25 cetoasterate (macrohaole 25 cetoasteryl ether, Cremophor A25) – 3,24 g;
• ethanol 95% (ethyl alcohol 95%) – 5 g;
• lactic acid – 0,4 g;
• Sodium hydroxide – 0,12 g;
• cleared water – up to 100 g.

.

How to take, the dosage

Intravaginally.

The Ornion® cream should be inserted into the vagina before bedtime using a calibrated applicator. One dose (when the applicator is filled to the ring mark) contains 0.5 g of Ornion® cream, which corresponds to 0.5 mg of estriol.

Lower urinary tract mucosal atrophy caused by estrogen deficiency: one intravaginal injection of the cream daily for not more than 2 weeks, until relief of symptoms. Thereafter, the dose is gradually reduced to a maintenance dose, depending on the clinical picture (e.g. one injection twice a week).

Pre- and postoperative therapy in postmenopausal women who are about to undergo or have undergone vaginal surgery: 1 intravaginal injection of the cream daily for 2 weeks before surgery; 1 injection 2 times a week for 2 weeks after surgery.

For diagnostic purposes if the results of cervical cytology are unclear with atrophic changes of epithelium: we administer 1 intravaginal injection of the cream every other day for a week before the next smear.

If the next dose of the drug was missed, the drug should be continued according to the usual schedule without making up for the missed dose earlier. Do not give two doses of the drug in the same day.

When starting or continuing treatment for postmenopausal symptoms, the lowest effective dose should be used for the shortest time possible.

In women who are not receiving OST medications or who are transitioning from continuous oral combination OST medications, treatment with Ornion® can be started on any day.

Women who are changing from a cyclic regimen of oral combination oral hypertension drugs should begin treatment with Ornion® one week after withdrawal of these drugs.

The administration technique:

• unscrew the cap from the tube, turn it over, and use a sharp tip to open the tube;
• screw the applicator onto the tube;
• press the tube so that the applicator fills with cream until the piston stops;
• unscrew the applicator from the tube and close the tube with the cap;
• Lying on your back, insert the applicator deep into your vagina and gently push out the entire contents of the applicator with the piston;
• After using the applicator, remove the piston from the body and wash the piston and applicator body in warm water and soap. Do not use washing powder for this purpose. After washing, rinse the applicator with clean water. Do not put the applicator in hot water or boiling water.

.

Interaction

In clinical practice, no interactions between topical estriol preparations and other drugs have been noted.

. Estrogen metabolism may be increased 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.

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

Elevated estrogen metabolism may decrease their clinical effect.

Estriol increases the effect of hypolipidemic drugs, reduces the effects of male sex hormones, anticoagulants, antidepressants, diuretics, hypotensive, hypoglycemic drugs.

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

There is evidence that estrogens, including estriol, may increase the pharmacological effects of corticosteroids and increase the activity of suxamethonium, theophylline and oleandomycin.

Special Instructions

To treat postmenopausal symptoms, ZGT should be started only for symptoms that adversely affect quality of life. In all cases, a thorough risk-benefit assessment should be performed at least once a year. ZGT should be continued only for a period of time when the benefits outweigh the risks.

Medical examination/surveillance:

• before starting or restarting on MHT, a detailed individual and family history should be taken. Based on the history, contraindications, and warnings for use of the drug, a clinical examination should be performed, including pelvic and breast examinations;
• Gynecological and general medical examinations, including breast examinations, are recommended during treatment. 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 the doctor. Examinations, including mammography, should be performed in accordance with generally accepted standards of examination.

Therapy should be discontinued if contraindications are identified and/or if the following conditions/diseases occur:

• jaundice and/or worsening of liver function;
• significant increase in BP;
• appearance or recurrence of migraine-type headache;
• pregnancy;
• endometrial hyperplasia.

Other conditions:

• estrogens can cause fluid retention, and therefore patients with impaired renal function and cardiovascular failure should be closely monitored by a physician;
• there is no conclusive evidence of improved cognitive function;
• with vaginal infections, concomitant specific treatment is recommended.

In order to prevent endometrial stimulation, the dose of Ornion® cream should not exceed 1 injection (0.5 mg estriol) per day, and this dose should not be administered daily for more than 3 consecutive weeks.

The effect on the ability to drive and operate machinery

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

Contraindications

• identified hypersensitivity to the active ingredient or any of the excipients of the drug;
• untreated endometrial hyperplasia;
• diagnosed or suspected oestrogen-dependent tumors (e.g., endometrial cancer);
• blooding from the vagina of unknown etiology;
• present and/or history of venous thrombosis;
• active or recent arterial thromboembolic disease (e.g., angina, myocardial infarction);
acute liver disease or a history of liver disease after which liver function has not returned to normal;
• porphyria;
• pregnancy;
• lactation period.

With caution: the presence of any of the following conditions/diseases currently present or in cases where such a condition/disease has previously been noted and/or worsened during previous pregnancies or previous hormonal treatments – the patient should be under the direct supervision of a physician. It should be considered that these conditions/diseases may recur or worsen during treatment with Ornion®, especially if present:

• leiomyoma (uterine fibroma) or endometriosis;
• a history of thromboembolic disorders or existing risk factors for such disorders;
• risk factors for estrogen-dependent tumors, such as 1st degree of heredity for breast cancer;
• arterial hypertension;
• denignant liver tumors (e.g., hepatic adenoma);
diabetes mellitus with or without angiopathy;
• biliary stone disease;
• jaundice, pruritus, herpes (incl.ч. history of prior pregnancy;
• hepatic insufficiency;
• migraine or headache (severe);
• systemic lupus erythematosus;
• hyperplasia of the endometrium in history;
• Epilepsy;
• bronchial asthma;
• otosclerosis;
• family hyperlipoproteinemia;
• pancreatitis.

.

Side effects

Orniona® cream may cause local irritation or itching.

Acyclic bleeding, breakthrough bleeding, and metrorrhagia may occur.

In rare cases, tightness or soreness of the mammary glands may occur.

In general, these side effects usually disappear after the first weeks of treatment, except that they may be an indication that too high a dose of the drug has been prescribed.

Overdose

In intravaginal administration, the likelihood of overdose of Ornion® cream is small.

Symptoms: Inadvertent ingestion – nausea, vomiting, bleeding withdrawal.

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

.

Similarities

Ovestin, Estrocade, Ovipol Clio