Clotrimazole (Tablets, Solution, Ointment, Cream) Instructions for Use

ATC Code

G01AF02 (Clotrimazole)

Active Substance

Clotrimazole (Rec.INN registered by WHO)

Clinical-Pharmacological Group

A drug with antifungal action for topical use in gynecology

Pharmacotherapeutic Group

Antimicrobial agents and antiseptics used in gynecology; antimicrobial agents and antiseptics, except combinations with corticosteroids; imidazole derivatives

Pharmacological Action

Clotrimazole is a broad-spectrum antifungal agent for vaginal use. The action of clotrimazole is associated with the disruption of ergosterol synthesis, which is a component of the fungal cell membrane, thereby altering the permeability of the cytoplasmic membrane and causing subsequent cell lysis.

In low concentrations, it acts fungistatically; in high concentrations, it acts fungicidally, 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 a toxic level, which also contributes to the destruction of fungal cells.

Clotrimazole exhibits fungicidal and fungistatic activity against dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis), yeast-like and mold fungi (Candida spp., including Candida albicans; Torulopsis glabrata, genus Rhodotorula, Pityrosporum orbiculare).

It is active against the causative agent of tinea versicolor – Pityrosporum orbiculare (Malassezia furfur). It is effective against gram-positive bacteria – the causative agent of erythrasma Corynebacterium minutissimum, as well as Staphylococcus spp., Streptococcus spp., and gram-negative bacteria – Bacteroides, Gardnerella vaginalis. In high concentrations, it is active against Trichomonas vaginalis.

It does not affect lactobacilli. Primarily resistant variants of sensitive fungi are very rare; the development of secondary resistance in sensitive fungi is also noted in exceptional cases under therapeutic conditions.

Pharmacokinetics

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

Indications

Genital infections caused by yeast-like fungi of the genus Candida (candidal vulvovaginitis); sanitation of the birth canal before childbirth.

ICD codes

Dosage Regimen

Solution, Ointment, Cream

The dose, method, and regimen of administration are determined individually, depending on the indications, the patient’s age, and the dosage form used.

For external use, the duration of treatment depends on the severity of the disease, the localization of pathological changes, and the effectiveness of therapy.

It is necessary to strictly adhere to the correspondence between the indications and the dosage form used.

Tablets

The dose, method, and regimen of administration are determined individually, depending on the indications, the patient’s age, and the dosage form used.

For topical use, the recommended duration of therapy is 6 days.

It is necessary to strictly adhere to the correspondence between the indications and the dosage form used.

Adverse Reactions

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

Gastrointestinal disorders frequency unknown – abdominal pain.

Urinary system disorders frequency unknown – frequent urination, intercurrent cystitis.

Reproductive system and breast disorders frequency unknown – itching, burning, hyperemia and swelling of the vaginal mucosa, ulceration of the vaginal mucosa, rash, pelvic pain, burning sensation in the penis of the sexual partner, pain during sexual intercourse.

Other frequency unknown – headache.

Contraindications

Hypersensitivity to clotrimazole; first trimester of pregnancy, menstrual period.

Use in Pregnancy and Lactation

Contraindicated in the first trimester of pregnancy. Use in the second and third trimesters of pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

In patients with hepatic insufficiency, the functional state of the liver should be periodically monitored.

Pediatric Use

It can be used in children according to indications, in doses and dosage forms recommended for the respective age. It is necessary to strictly follow the instructions in the package inserts of clotrimazole preparations regarding the use of specific dosage forms of clotrimazole in children of different ages and regarding contraindications for specific age groups in this category of patients.

Special Precautions

If allergic reactions or irritation occur at the site of application, treatment should be discontinued.

To prevent reinfection, hygiene rules should be observed.

Application of clotrimazole to the skin in the eye area is not recommended.

If clinical signs of infection persist after completion of treatment, a repeat microbiological examination should be performed to confirm the diagnosis.

To prevent infection/reinfection with genital infections, simultaneous treatment of sexual partners is necessary. It is recommended to abstain from sexual intercourse during treatment.

When using dosage forms intended for topical intravaginal application, it is recommended to use reliable contraceptive methods. The risk of condom or diaphragm rupture increases with their simultaneous use with clotrimazole.

Drug Interactions

With simultaneous use with amphotericin B, nystatin, the activity of clotrimazole decreases.

Simultaneous intravaginal use of clotrimazole and oral administration of tacrolimus, sirolimus may lead to an increase in the plasma concentrations of the latter, so patients should be monitored for symptoms of overdose, with measurement of plasma concentrations if necessary.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.