Vaginal suppository during menopause: moisturizing, with estrogens

During menopause, a woman begins to experience such unpleasant symptoms as irritation, itching, dryness, burning in the vagina. In addition, the vulnerability of this area to infections is also increasing. In this case, the optimal solution will be to use special suppositories in menopause, which help to eliminate these manifestations.

Indications of the suppositories for menopause

Suppositories are prescribed to eliminate atrophic changes associated with age and lack of estrogen, affecting the vaginal mucosa (symptoms such as itching and dryness, discomfort in the vagina, pain during intercourse).

Release form

The medicine is issued in the form of vaginal suppositories.

Ovestin

Ovestin contains estriol and other components that allow normalizing the vaginal flora, as well as the hormonal balance in this area. The medicine helps maintain vaginal acidity at the required level, preventing the proliferation of pathogenic microorganisms.

[1], [2], [3]

Climaxan

Climaxan is a natural herbal remedy, which helps to eliminate the disturbances manifested by the onset of menopause. Due to this drug can reduce the severity of menopausal manifestations, while not affecting the balance of hormones.

Suppositories with estrogen in menopause

There are hormonal vaginal suppositories that contain estrogens. They are very effective in menopause. There are such drugs:

• Estrokad, an active component of which is estriol, which helps to restore the thickness of the vaginal mucosa, and also enhances its secretory function;
• Ovipol Clio, who also contains estriol. This active ingredient, supplemented by auxiliary elements, helps to remove burning sensation with itching, and besides it moisturizes the mucous membrane and promotes the production of natural mucus;
• Ortho-ginest with the help of estriol stimulates secretion production by the uterine neck, and not only by the vaginal walls. Thanks to moistening with this medication, the microflora of the mucosa is restored;
• Estriol contributes to the production of natural mucus, resulting in a woman's burning, dryness, and itching, which are prevented by the woman, disappear.

Non-hormonal suppository with menopause

Non-hormonal suppositories containing bioidentical estrogens are an effective alternative to hormone treatment. These drugs, in their chemical structure, are similar to beta-estradioles, which are of vegetable origin. Nowadays, pharmacists produce bioidentical vaginal suppositories containing 3 basic estrogens - estriol, as well as estrone with estradiol.

In case the patient is contraindicated in treatment with suppositories containing hormones, natural preparations such as Feminela, Vagikal, and Cicatridine should be used.

The properties of suppositories in menopause are examined using the example of Ovestin.

Pharmacodynamics

Ovestin is an estrogenic drug that acts identically to a natural hormone produced by a female body. Helps restore the level of estrogen at the onset of postmenopause, and also reduces the manifestation of symptoms of menopause.

It is very effective in eliminating diseases of the genitourinary system. With atrophic processes in the mucous lower part of the urogenital system, estriol helps to strengthen the epithelial layer of the urogenital tract, and restores a healthy microflora with a physiologically necessary pH level inside the vagina. Due to this drug, the epithelial cells in this area become more resistant to inflammatory processes and infections, thereby reducing the severity of such symptoms as vaginal pruritus along with dryness, as well as pain during intercourse. In addition, the risk of developing genito-urinary infections decreases, the function of urination normalizes, and incontinence is eliminated.

The difference between estriol and other estrogens is that it has a short duration of exposure, since in the nuclei of endometriod cells it is delayed only for a short time. It is believed that a single daily dose of estriol does not cause the reproduction of endometrial cells. As a consequence, cyclic application of the hormone progestogen will not be needed, and the abolition will not cause bleeding. It has also been established that estriol does not enhance mammographic density.

Pharmacokinetics

After intravaginal administration of the drug at the site of its effect, optimal bioavailability is observed. Estriol is absorbed into the systemic blood stream, manifesting itself under the guise of a rapid increase in blood plasma concentrations of so-called unbound estriol. After the administration of the drug reaches a peak after 1-2 hours.

Of plasma proteins at 90 binds to albumin, but with globulin (it synthesizes sex hormones) is almost unrelated, which distinguishes estriol from other estrogens.

When the active substance is metabolized in the process of intestinal-hepatic circulation, it is converted into a conjugate as well as an unconjugated state. As the final metabolite, estriol is excreted from the body together with urine, being bound. Only a small part (approximately 2%) is excreted along with the feces, as unbound estriol. Half-life lasts about 6-9 hours.

After insertion in the vagina of the drug at a dosage of 0.5 mg, the peak concentration is 100 pg / ml, and the minimum value is about 25 pg / ml. The average is about 70 pg / ml. After 21 days of daily administration of the drug at a dosage of 0.5 mg, the mean was reduced to 40 pg / ml.

[4], [5], [6], [7], [8]

Dosing and administration

Suppositories help to restore vaginal tissues, and it happens in a fairly short time. They should be entered vaginally in the evening (before bedtime). The procedure is required within 1-2 weeks, and after this course continue to put on the 1st suppository 2-3 times per week.

[13]

Contraindications

Ovestin is contraindicated:

• during pregnancy, and in addition, with intolerance of the components of the drug;
• also it can not be prescribed for breast cancer (if there is an anamnesis or if the woman is ill at the moment or if it is suspected);
• except for a malignant tumor of an estrogen dependent nature (often with endometrial cancer or suspected of it);
• with bleeding from the vagina having an unclear nature;
• in the presence of an anamnesis of acute blockage of a thrombus (venous or arterial type);
• with acute liver disease or changes in liver tests;
• with porphyrin disease.

Vagical is not allowed for use in cases of hypersensitivity to drug components.

[9], [10]

Side effects of the suppositories for menopause

Like any topical medication, the suppository with menopause may cause an allergic reaction due to intolerance to the elements of the drug such as itching and irritation in the vagina.

Ovestin can cause such side effects as pain and discomfort in the mammary glands, as well as nausea. In rare cases, headaches occur, and blood pressure also increases.

[11], [12]

Overdose

Among the manifestations of an overdose of Ovestin in case of ingestion of the suppository inside: vomiting with nausea; with vaginal application - bleeding from the vagina. It is required to carry out symptomatic therapy, since there is no specific antidote for treatment.

[14], [15], [16],

Interactions with other drugs

There were no cases of negative interaction of suppositories with other drugs.

Estrogen exchange processes can be accelerated by combining with substances that induce such enzymes that participate in the metabolism of drugs. Especially this concerns isoenzymes of cytochrome P450 - for example, antiepileptic (such as phenytoin, as well as phenobarbital with carbamazepine), as well as antimicrobial agents (such as nevirapine and rifampicin, as well as efavirenz with rifabutin).

When steroid hormones are combined with nelfinavir and ritonavir, the inducing effect of the latter is enhanced.

Medicines on a plant basis (which contain St. John's wort) are able to induce estrogen exchange processes.

The increased metabolism of estrogens can reduce their clinical effectiveness.

Estriol increases the properties of lipid-lowering drugs. In addition, it reduces the effects of anticoagulants, diuretics, antidiabetics, hypotensive drugs, and male sex hormones.

Preparations of general anesthesia, tranquilizers narcotic analgesics, individual antihypertensive drugs, and also ethanol reduce the medicinal effect of Ovestina.

Preparations of thyroid hormones, as well as folic acid increase the therapeutic properties of estriol.

Storage conditions

Vaginal suppository should be kept in a place protected from moisture and sunlight, and also closed from children. Temperature conditions are generally not more than 25 ° C. Suppositories Ovestin should be stored in conditions of 2-25 ° C.

[17], [18]

Shelf life

Suppositories in menopause should be used for 2-3 years from the date of manufacture.

[19], [20], [21]