Pharmacological properties

Pharmacodynamics. the mechanism of anti-mycotic effect of Clotrimazolum is connected with ergosterol synthesis suppression that leads to structural and functional damage of a cytoplasmic membrane.

Clotrimazolum renders to

a wide range of anti-mycotic activity of in vitro and in vivo, affects dermatophytes, barmy, mold and dimorphous mushrooms.

Under the corresponding test conditions the minimum inhibiting concentration for these types of mushrooms make about 0.062-8.0 mkg/ml of substrate.

Mechanism of effect of Clotrimazolum is connected by

with primary fungistatic or fungicide activity depending on concentration of Clotrimazolum in the place of an infection.

In vitro the activity is limited to proliferating elements of a mushroom; spores of a mushroom have only insignificant sensitivity.

Clotrimazolum also affects with

In addition to anti-mycotic activity gram-positive microorganisms (streptococci, staphylococcus, Gardnerella vaginalis) and gram-negative microorganisms (Bacteroids)).

In vitro Clotrimazolum suppresses reproduction of Corynebacteria and gram-positive cocci (except for Enterococci) in concentration of 0.5-10 mkg/ml of substrate. Originally resistant strains of sensitive species of mushrooms meet seldom. Development of secondary resistance at treatment at sensitive mushrooms was still observed very seldom.

Preclinical trials conducted with participation of volunteers using a single and repeated toxic dose did not reveal the damaging toxic, genotoksichesky influence and influence on a reproduction.

Pharmacokinetics. Pharmacokinetics researches after vaginal application showed that only the insignificant amount of Clotrimazolum (3–10%) is soaked up. The absorbed Clotrimazolum quickly is metabolized in a liver to inactive metabolites. Therefore plasma C _max Clotrimazolum after vaginal application in a dose of 500 mg made 10 ng/ml. It means that emergence of measurable system effects or side effect after intravaginalny use of Clotrimazolum is improbable.

Indication

Infection in genitals (vaginitis), caused by mushrooms (usually the sorts candida), and the superinfections caused by the bacteria sensitive to Clotrimazolum.

Use

Suppository of vaginal 100 mg

Suppository vaginal should be entered into a vagina as it is possible more deeply as far as it is possible, before going to bed. It is more convenient to enter a suppository lying on a back with slightly bent legs.

One course of therapy on 2 suppositories within three days or on 1 candle within six days.

Second year of therapy can be appointed by

if it is necessary.

treatment should not be carried out by

During periods. Treatment should be finished prior to the beginning of periods.

do not use tampons, intravaginalny irrigations, spermitsida or other vaginal products at use of this medicine.

At use of this medicine should avoid sexual contacts as the infection can be transmitted to the partner.

Suppository of vaginal 500 mg

One suppository vaginal to apply

for the night.

Suppository vaginal should be entered into a vagina as it is possible more deeply as far as it is possible, before going to bed. It is more convenient to enter a suppository lying on a back with slightly bent legs.

Second year of therapy can be appointed by

if it is necessary.

treatment should not be carried out by

During periods. Treatment should be finished prior to the beginning of periods.

do not use tampons, intravaginalny irrigations, spermitsida or other vaginal products at use of this medicine.

At use of this medicine should avoid sexual contacts as the infection can be transmitted to the partner.

Contraindication

Hypersensitivity to Clotrimazolum or other components of medicine.

Side effects

from the immune system: allergic reactions, including faints, arterial hypotension, an asthma, a small tortoiseshell, the naggers.

from a reproductive system and mammary glands: peeling of skin in genitals, an itch, rash, hypostasis, an erythema, discomfort, burning, irritation, pelvic pain, vaginal bleeding.

from a GIT: abdominal pain.

Special instructions

Should avoid contact with eyes. not to swallow.

to the Patient is recommended to consult with the doctor:

• at the first manifestations of a disease;
• if symptoms remain 7 days;
• if symptoms appear within 2 months or more than 4 times again within the last 12 months;
• at the established hypersensitivity to any antifungal means or derivatives of an imidazole;
• in the presence of venereal diseases in the anamnesis or the burdened anamnesis of rather venereal diseases at the partner;
• in the presence of more than two episodes of a mycotic vulvovaginitis within the last 6 months;
• if the patient has a high temperature of a body (≥38 °C), pain in the lower part of a stomach, a dysuria, a dorsodynia, purulent vaginal discharges with an unpleasant smell, ulcers of a vulva and vaginal ulcers, reddening, diarrhea, nausea, vomiting, the vaginal bleeding which is followed by shoulder pain.

during use of medicine should avoid sexual contacts as the infection can be transmitted to the partner. The efficiency and safety of latex products (such as condoms and diaphragms) can decrease (see INTERACTIONS).

As usually are surprised both a vagina, and external genitals (vulvar lips and adjacent sites), it is necessary to perform the combined treatment of both sites, including topical treatment by external use cream.

during the Klofan medicament treatment, suppositories vaginal, treatment of both partners using cream is recommended to

.

treatment should not be carried out by

During periods. Treatment should be finished prior to the beginning of periods.

not to use tampons, intravaginalny irrigations, spermitsida or other vaginal products at use of this medicine.

Use during pregnancy and feeding by a breast. Clinical trials of influence of Clotrimazolum on fertility at women were not conducted, however researches on animals did not reveal influence of Clotrimazolum on fertility.

Research on animals did not reveal direct or indirect harmful effects in terms of reproductive toxicity. The number of researches using Clotrimazolum during pregnancy is limited therefore it is recommended to avoid medicine Klofan use, suppositories vaginal, during the I trimester of pregnancy.

during the Klofan medicament treatment, suppositories vaginal, it is necessary to stop feeding by a breast.

Children. Not to apply at children aged up to 12 years. At children 12 years are aged more senior to apply after consultation with the doctor.

Ability to influence speed of response at control of vehicles or work with other mechanisms.

Drug does not influence or has insignificant impact on ability to steer the vehicle or to work with other mechanisms.

Interaction

Simultaneous treatment by Clotrimazolum applied vaginalno, and takrolimusy orally (fk-506; the immunosuppressant) or sirolimusy can lead to increase in level of a takrolimusa/sirolimus in blood plasma. thus, it is necessary to control carefully a condition of the patient for identification of symptoms of overdose of a takrolimus or a sirolimus, if necessary — by check of their levels in blood plasma.

Simultaneous application of suppositories vaginal with latex contraceptives (such as condom and diaphragm) can lead

to damage of the last therefore the efficiency of these contraceptives can decrease. The specified effect temporary can also arise only during treatment. Patients are recommended to use alternative methods of contraception, at least within 5 days after use of this medicine.

Overdose

is present

No risk of sharp intoxication as it is improbable that the overdose is possible after a single vaginal dose or drawing on skin (application on big sites of skin under the conditions promoting the increased absorption) and also after accidental oral administration. there is no specific antidote.

However in case of accidental oral administration and only at manifestation of clinical symptoms of overdose (such as dizziness, nausea or vomiting) should apply such preventive actions as gastric lavage. Gastric lavage should be carried out only in cases when there is an appropriate protection of airways.

Storage conditions

In original packing at a temperature not above 25 °C.