Clotrimazole, vaginal cream 2% 20 g

Pharmacotherapeutic group:

antifungal agent.

ATX code: G01AF02

Pharmacological properties

Pharmacodynamics

Clotrimazole is a broad spectrum antifungal agent for local use. Antimycotic effect of the active active substance clotrimazole (imidazole derivative) is associated with disruption of ergosterol synthesis, a component of the cell membrane of fungi, which changes membrane permeability and causes subsequent cell lysis.

In low concentrations it is fungistatic and in high concentrations it is fungicidal, and not only on proliferating cells. In fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in hydrogen peroxide concentration to toxic levels, which also helps destroy fungal cells.

It is effective against dermatophytes, yeasts, molds and protozoa. It has antimicrobial action against Gram-positive (Streptococcus spp., Staphylococcus spp.) and anaerobes (Bacteroides spp., Gardnerella vaginalis).

Clotrimazole has no effect on lactobacilli. In vitro at a concentration of 0.5-10 µg/ml clotrimazole inhibits the reproduction of bacteria of the family Corinebacteria and Gram-positive cocci (except enterococci); it has a trichomonacid effect at a concentration of 100 µg/ml.

Pharmacokinetics

When using clotrimazole intravaginally, absorption is 3 to 10% of the administered dose. High concentrations in vaginal secretion and low concentrations in blood persist for 48 to 72 hours. It is metabolized in the liver to inactive metabolites, which are excreted by the kidneys and through the intestine.

Indications

Genital infections caused by Candida yeast-like fungi (candida vulvovaginitis).

Active ingredient

Composition

100 g of the cream contain:

The active ingredient:

Excipients:

sorbitan stearate – 2.0 g,

cetyl palmitate – 3.0 g,

cetostearyl alcohol [60% cetyl alcohol and 40% stearyl alcohol] – 10.0 g,

Polysorbate-60 – 1.5 g,

Octyldodecanol – 13.5 g,

How to take, the dosage

Topically. For intravaginal use only.

For 6 consecutive days, once daily in the evening before going to bed, insert the contents of the filled applicator (approximately 5 g) as deeply as possible into the vagina, in a supine position, with the legs slightly bent.

Applying the vaginal cream with the disposable applicator:

1. Open the tube and screw on the disposable applicator.

2. While gently squeezing the tube, fill the disposable applicator until the piston is completely out.

3. Unscrew the applicator from the tube. Insert the applicator as far into the vagina as possible (preferably in the supine position) and squeeze the contents of the applicator by pressing the piston.

4. Remove the disposable applicator after use and discard.

Please only use the product according to the route of administration and the dosage listed in the directions for use.

Renewed treatment is possible after checking with your doctor.

If there is no improvement or new symptoms after treatment, consult a physician.

Interaction

In vaginal administration clotrimazole reduces the activity of amphotericin B and other polyene antibiotics.

Concomitant use with natamycin and nystatin may decrease the activity of clotrimazole.

Simultaneous use of clotrimazole intravaginally and oral tacrolimus, sirolimus may lead to increased plasma concentrations of the latter, so patients should be monitored for the development of symptoms of overdose, with measurement of plasma concentrations if necessary.

Special Instructions

Read the instructions for use carefully before using this product. Keep the instructions; you may need them again. If you have any questions, ask your doctor.

The medicine you are taking is for you, and should not be given to others, because it can cause them harm, even if they have the same symptoms as you do.

If you have any allergic reactions or irritation where the medicine was given, stop the treatment.

The drug should not be used during menstruation; it is advisable to start treatment after menstruation.

In case of simultaneous infection of the labia and adjacent areas (candidal vulvitis), clotrimazole should be additionally treated topically.

In pregnancy, treatment with vaginal cream is carried out without an applicator.

The simultaneous treatment of sexual partners is necessary to prevent infection.

At the time of treatment, it is recommended to refrain from sexual intercourse.

The use of contraception is recommended during treatment. The risk of condom or diaphragm rupture increases if they are used at the same time as the drug. Reliable contraceptive methods should be used.

Hygiene practices should be followed to prevent reinfection.

If clinical signs of infection persist after treatment has been completed, repeat microbiological testing to confirm the diagnosis.

Impact on driving and operating ability

The drug does not affect the ability to drive vehicles and to perform other potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Contraindications

Hypersensitivity to clotrimazole or other ingredients of the drug, especially to cetostearyl alcohol;

menstrual period;

I trimester of pregnancy.

With caution

The period of breastfeeding.

Side effects

According to the World Health Organization (WHO), adverse effects are classified according to their frequency of occurrence as follows: Very common (≥1/10), common (≥1/100, ˂1/10), infrequent (≥1/1000, ˂1/100), rare (≥1/10000, ˂1/1000), and very rare (˂ 1/10000); frequency unknown (frequency of the events cannot be determined from available data).

Disorders of the immune system:

frequency unknown: allergic reactions with symptoms such as urticaria, syncope, arterial hypotension, shortness of breath.

Gastrointestinal tract disorders:

frequency unknown: abdominal pain.

Skin and subcutaneous tissue disorders:

frequency unknown: allergic reactions may occur in case of hypersensitivity to the active substance or another component of the drug, such as cetostearyl alcohol.

Renal and urinary tract disorders:

incidence unknown: rapid urination, intercurrent cystitis.

Genital disorders:

frequency unknown: itching, burning, hyperemia and swelling of the vaginal mucosa, ulceration of the vaginal mucosa, rash, pain in the pelvic area.

Other:

frequency unknown: headache, gastralgia.

If any of the side effects listed in the instructions worsen, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose

In case of overdose the following symptoms are possible: dizziness, nausea, vomiting.

Pregnancy use

The use in the first trimester of pregnancy is contraindicated. The question on the appropriateness of using the drug in the II-III trimesters of pregnancy should be decided individually after physician’s consultation.

The use of the drug during breast-feeding is allowed only if, in the opinion of the doctor, the potential benefit of using the cream for the mother is greater than the possible risk to the baby.

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