CANESTEN

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Canesten® (Canesten®)

Composition:

Active substance: clotrimazole;

One vaginal tablet contains 100 mg or 200 mg or 500 mg of clotrimazole;

Excipients: calcium lactate pentahydrate; microcrystalline cellulose; crospovidone; hypromellose; lactic acid; lactose monohydrate; magnesium stearate; corn starch; colloidal anhydrous silicon dioxide.

Pharmaceutical form. Vaginal tablets.

Main physicochemical properties:

For the 100 mg dose: white or yellowish vaginal tablet with the imprint «P3» on one side and «BAYER» on the other.

For the 200 mg dose: white or yellowish vaginal tablet with the imprint «NR» on one side and «BAYER» on the other.

For the 500 mg dose: white or yellowish vaginal tablet with the imprint «MU» on one side and «BAYER» on the other.

Pharmacotherapeutic group.

Antibacterial and antiseptic agents used in gynecology, excluding combinations with corticosteroids. Clotrimazole.

ATC code G01AF02.

Pharmacological properties.

Pharmacodynamics.

The antifungal mechanism of action of clotrimazole is associated with inhibition of ergosterol synthesis, resulting in structural and functional damage to the cytoplasmic membrane.

Clotrimazole has a broad spectrum of antifungal activity in vitro and in vivo and acts against dermatophytes, yeasts, molds, and dimorphic fungi.

Under appropriate testing conditions, minimal inhibitory concentrations for these types of fungi are approximately less than 0.062–8.0 µg/mL of substrate.

The mechanism of action of clotrimazole is related to primary fungistatic or fungicidal activity, depending on the concentration of clotrimazole at the site of infection.

In vitro, activity is limited to proliferating fungal elements; fungal spores exhibit only minimal sensitivity.

In addition to its antifungal activity, clotrimazole also acts against gram-positive microorganisms (streptococci, staphylococci, Gardnerella vaginalis) and gram-negative microorganisms (Bacteroides).

In vitro, clotrimazole inhibits the growth of Corynebacteria and gram-positive cocci (except Enterococci) at concentrations of 0.5–10 µg/mL of substrate. Primary resistant strains of susceptible fungal species are rarely encountered. Development of secondary resistance during treatment in susceptible fungi has so far been observed very rarely. Preclinical studies conducted in volunteers using single and repeated toxic doses did not reveal any damaging toxic, genotoxic, or reproductive effects.

Pharmacokinetics.

Pharmacokinetic studies following vaginal administration have shown that only a small amount of clotrimazole (3–10%) is absorbed. Absorbed clotrimazole is rapidly metabolized in the liver to inactive metabolites. Therefore, the peak plasma concentration of clotrimazole after vaginal administration of a 500 mg dose was less than 10 ng/mL. This indicates that measurable systemic effects or adverse reactions following intravaginal administration of clotrimazole are unlikely.

Clinical characteristics.

Indications.

Genital area infections (vaginitis) caused by fungi (usually of the genus Candida), and superinfections caused by bacteria sensitive to clotrimazole.

Contraindications.

Hypersensitivity to clotrimazole or to any of the other components of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

Concomitant treatment with vaginally administered clotrimazole and orally administered tacrolimus (FK-506; immunosuppressant) or sirolimus may lead to increased plasma levels of tacrolimus/sirolimus. Therefore, patients should be carefully monitored for symptoms of tacrolimus or sirolimus overdose, and plasma levels of these drugs should be checked when necessary.

Special precautions for use.

Avoid contact with the eyes. Do not swallow.

The patient should consult a physician:

at the first signs of the disease;

if symptoms persist for more than 7 days;

if symptoms recur within 2 months or occur more than 4 times within the last 12 months;

if hypersensitivity to any antifungal agents or imidazole derivatives has been diagnosed;

if there is a history of sexually transmitted infections or if the partner has a complicated history of sexually transmitted infections;

if the patient has had more than two episodes of candidal vaginitis within the last 6 months;

if the patient develops high body temperature (38 °C or higher), lower abdominal pain, dysuria, back pain, purulent vaginal discharge with unpleasant odor, vulvar ulcers or vaginal ulcers, redness, diarrhea, nausea, vomiting, vaginal bleeding accompanied by shoulder pain.

During treatment with this medicinal product, sexual intercourse should be avoided, as the infection may be transmitted to the partner. The effectiveness and safety of latex products (such as condoms and diaphragms) may be reduced.

Since both the vagina and external genital organs (labia and adjacent areas) are usually affected, combined treatment of both areas should be applied, including topical treatment with cream for external use.

During treatment with Canesten® vaginal tablets, it is recommended to treat both partners using the cream.

Treatment should not be carried out during menstruation. Treatment should be completed before the onset of menstruation.

Do not use tampons, intravaginal douches, spermicides, or other vaginal products during use of this medicinal product.

Use during pregnancy or breastfeeding.

Clinical studies on the effect of clotrimazole on female fertility have not been conducted; however, animal studies have not revealed any effect of clotrimazole on fertility.

Animal studies have not shown any direct or indirect adverse effects in terms of reproductive toxicity. The number of clinical studies using clotrimazole during pregnancy is limited; therefore, the use of Canesten® vaginal tablets is not recommended during the first trimester of pregnancy.

During pregnancy, vaginal tablets should be used without an applicator.

During treatment with Canesten® vaginal tablets, breastfeeding should be discontinued.

Ability to influence reaction speed when driving or operating machinery.
Canesten® vaginal tablets do not affect the ability to drive a vehicle or operate machinery, or have only a negligible effect.

Method of Administration and Dosage

One vaginal tablet should be administered in the evening. The treatment course for 100 mg vaginal tablets is 6 days; for 200 mg – 3 days; for 500 mg – 1 day.

Vaginal tablets should be inserted as deeply as possible into the vagina in the evening. The most convenient position for insertion is lying on the back with knees slightly bent.

Canesten® vaginal tablets must become moistened within the vagina to dissolve completely. Otherwise, undissolved fragments of the vaginal tablet may be expelled from the vagina. To prevent this, it is important to insert the medicinal product as deeply as possible into the vagina before going to bed. If the vaginal tablets do not dissolve completely overnight, consider switching to a vaginal cream.

Children. Do not use in children under 12 years of age. For children aged 12 years and older, use only after consultation with a physician; do not use the applicator.

Overdose.

There is no risk of acute intoxication, as overdose is unlikely following a single vaginal dose or topical application to the skin (application over large skin areas under conditions favoring increased absorption), as well as after accidental oral ingestion. No specific antidote exists.

After accidental oral ingestion, gastric lavage may rarely be necessary if a life-threatening dose has been ingested within the previous hour or if visible symptoms of overdose are present (e.g., dizziness, nausea, or vomiting). Gastric lavage should only be performed if adequate airway protection is ensured.

Side effects.

Immune system: allergic reactions, including fainting, hypotension, shortness of breath, urticaria.

Reproductive system and mammary glands: skin desquamation in the genital area, itching, rash, swelling, erythema, discomfort, burning sensation, irritation, pelvic pain, vaginal bleeding.

Gastrointestinal tract: abdominal pain.

Shelf life.

4 years.

Storage conditions.

Store at a temperature not exceeding 25 °C.

Keep out of reach of children.

Packaging.

Vaginal tablets 100 mg, pack of 6; 200 mg, pack of 3; or 500 mg, pack of 1 in aluminum foil blisters with an applicator in a cardboard box.

Dispensing category.

Over-the-counter.

Manufacturer.

Bayer AG

Manufacturer's address and place of business.

Kaiser-Wilhelm-Allee, 51368, Leverkusen, Germany / Kaiser-Wilhelm-Allee, 51368, Leverkusen, Germany.