Sertaconazole

When ATH:
D01AC14

Pharmacological action.

The antifungal agent for external and topical use. Sertaconazole is imidazole derivatives and benzothiophene derivatives with a broad spectrum of activity against pathogenic fungi Candida spp. (incl. Candida albicans, Candida tropicalis), other pathogenic fungi (Orbicular Pityrospores, Malassezia spp.), dermatofitov (Trichophyton and Microsporum), Gram-positive bacteria (Streptococcus spp., Staphylococcus spp.), and Gardnerella vaginalis, Enterococcus faecalis, Bacteroides spp., Trichomonas vaginalis.

Sertaconazole not suppress the viability of Lactobacillus spp. in vitro.

At therapeutic doses, it has a fungicidal and fungistatic. The mechanism of action of sertaconazole is to suppress the synthesis of ergosterol, main component of fungal cell membranes, and in a competitive antagonism with another component of the cell wall - tryptophan. This leads to disorganization and increased permeability of the cell membrane, degradation and destruction of the pathogen.

Pharmacokinetics

Therapeutic concentrations of sertaconazole in the cornified layer of the skin after application to the skin is achieved during 30 min and stored more 48 no. In daily use for 14 day increasing amounts sertaconazole is not detected in blood and urine.

After intravaginal application of high concentrations of sertaconazole in the lumen of the vagina stored for a long time and is significantly higher than both the minimum inhibitory concentrations, and fungicidal concentration against C.albicans, C.glabrata and other fungi, not belonging to genus Candida. Systemic absorption after intravaginal application offline. Unmodified sertaconazole not detected in any serum, audio in urine.

Testimony

Superficial fungal infections of the skin: dermatofitozы; mycosis shins, feet and hands; mycosis body; beard mycosis; candidiasis; variegated (pityriasis) lichen; seborrheic dermatitis.

Infections of the mucous membrane of the vagina, caused by fungi of the genus Candida (vulvovaginal candidiasis).

Dosage regimen

External used 1-2 during 2-4 weeks.

Intravaginal – 1 time / within 7 days.

Side effect

When applied topically: quickly passing local erythematous reactions.

In intravaginal application,: rarely – burning sensation, itching of the vagina, which are themselves.

Contraindications

Hypersensitivity to sertaconazole, imidazole derivatives.

Pregnancy and breast-feeding

Teratogenic effects. Reproduction studies after oral administration in rats and rabbits showed no toxicity for females, embryotoxicity and teratogenicity at doses sertaconazole nitrate 160 mg / kg / day (exceed MRDC based on surface area 40 times in rats and in 80 times in rabbits). In peri- and postnatal study in rats after oral administration, a decrease of live birth index and increase in the number of stillborn pups at doses 80 and 160 mg / kg / day.

There are no adequate and well-controlled trials of sertaconazole nitrate in pregnant women is not carried out. Given the lack of systemic absorption after intravaginal application and cutaneous, use of sertaconazole nitrate during pregnancy is possible in the case, if the potential benefit to the mother outweighs the potential risk to the fetus and child.

Category actions result in FDA - C.

Sufficient data on the use of sertaconazole nitrate lactation No. Unknown, Do penetrates sertaconazole in human breast milk. During lactation cream should not be applied to the breast. If necessary, use sertaconazole lactation should consider the issue of termination of breastfeeding.

Cautions

Not used in ophthalmic practice. After applying the cream is not recommended the use of acid detergents (in an acidic medium amplified reproduction Candida spp.).

The cream should be used with caution in patients with established hypersensitivity to imidazoles (possible cross-sensitivity).

With the development of irritation or manifestation of hypersensitivity reactions should stop use of the cream.

In the absence of characteristic clinical symptoms alone detection of Candida in the vaginal mucosa can be an indication for prescribing. If candidiasis confirmed, it is recommended to identify and try to eliminate factors, conducive to the emergence and development of fungi. When simultaneous infection of the labia and surrounding areas (Candida vulvitis) It should be further carried out by local treatment with a cream.

In applying the drug to abstain from sex. To prevent reinfection urogenital encouraged to consider the simultaneous treatment of sexual partners. The risk of condom breakage or diaphragm increases when used simultaneously with the use of the drug.

The treatment can be carried out during menstruation.

Drug Interactions

Not recommended simultaneous use of intravaginal sertaconazole and local spermicidal contraceptive drugs, tk. spermicidal effect may weaken.