Naphthyne

It has antifungal, antibacterial and anti-inflammatory effects.

Antifungal action

Naftifin is highly active against various fungi (dermatophytes, molds and yeasts in vitro ). Naphthyphine has a predominantly fungicidal effect on dermatophytes and molds; naphthyphine has a fungistatic or fungicidal effect on yeast, depending on the strain of fungi. In addition, it was found that the effect of naphthyne depends on pH; the greatest activity of the drug is observed at a neutral pH range.

Naftifin inhibits squalene epoxidase, which inhibits the biosynthesis of ergosterol, an essential component of fungal cell membranes. As a result, ergosterol deficiency occurs and fungal cell growth stops. Thus, the fungistatic effect of naftifin is possibly due to a lack of ergosterol. On the other hand, the accumulation of squalene associated with the inhibition of squalene epoxidase leads to some dystrophic intracellular processes, for example, the deposition of lipid droplets. Such an accumulation of squalene occurs not only in the cell membrane, but also in other membranes, for example, in the endoplasmic reticulum. Violation of the properties of membranes and all intracellular processes associated with lipid membranes can lead to damage to the cell wall. This explains the fungicidal effect of naftifine ^[2] .

Antibacterial action

Naftifin has a local bactericidal effect against gram-positive and gram-negative bacteria. The minimum bactericidal concentrations (MBC) established for various bacteria were in the range from 0.04 to 1.25% of the active substance. In a clinical study, the antibacterial effect of naftifin was compared with the action of gentamicin with the same indication for use - pyoderma. The effectiveness of naftifin in stopping the symptoms of pyoderma, as well as in terms of inhibiting bacterial growth, was similar to gentamicin ^[2] .

Anti-inflammatory action

Dermatomycosis can be accompanied by dermatitis associated with irritation and toxic skin reactions. In some cases, with dermatomycosis in combination with inflammatory skin lesions, combination therapy with an antifungal drug and a local corticosteroid is performed. Corticosteroids inhibit early as well as late inflammatory reactions, preserve the integrity of cells and plasma membranes, and also stabilize lysosome membranes, as a result of which the release of lysosomal enzymes is inhibited. In the case of naftifin, confirmation of the direct vasoconstrictor and anti-inflammatory effect of the drug could be obtained when conducting new experimental and clinical studies:

1. The efficacy of naftifine was compared with the efficacy of the combination of econazole and triamcinolone in patients with inflammatory dermatomycoses. It was found that naftifin has the same anti-inflammatory effect as azole in combination with class I corticosteroids.
2. The anti-inflammatory effect of naftifin was studied by evaluating the erythematous response to ultraviolet radiation. In a double-blind study in which 20 healthy volunteers participated, the anti-inflammatory effects of naphthyne on the right and left sides of the body were compared based on the assessment of erythema resulting from exposure to ultraviolet radiation. After local application of naftifine, an anti-inflammatory effect was observed, which was mainly due to the direct effect on the mediators of the early phases of inflammation - prostaglandins. This suggests that naftifin acts in the same way as anti-inflammatory drugs that inhibit the formation, release and action of prostaglandins. However, the mechanism of the anti-inflammatory effect of naftifine has not been fully studied and is currently being investigated.
3. In a multicenter, double-blind, randomized trial in which 269 patients with clinically diagnosed fungal infections of the skin participated in parallel groups, naftifin was used for treatment, and the combination of clotrimazole 1% and hydrocortisone 1% (Canesten HC®) twice in day for 4 weeks. Clinical results in all 265 patients showed no difference between the two drugs in terms of treatment of the disease, which indicates that naphthyne has anti-inflammatory activity equal to the activity of the combination of clotrimazole and hydrocortisone. This study shows that in the treatment of patients with a clinically diagnosed fungal infection of the skin, there is no clinical advantage of using a combination of antimycotics and corticosteroids compared with the use of naftifine in monotherapy.

A large number of double-blind, randomized clinical trials have been carried out to determine the clinical and microbiological efficacy, as well as the tolerance of naftifin when used for various indications. In these studies, the clinical and microbiological response rate was studied with naphthyne.

• A comparison was made between naftifin and placebo, with azole derivatives, as well as with a combination of azoles and corticosteroids. In general, when compared with azole derivatives, the frequency of clinical recovery in patients with dermatomycoses treated with naphthyphine ranged from 70% to 92% ^[3] .
• The safety and efficacy of 1% naftifin cream were compared with the combined treatment of 1% clotrimatozole and 0.05% betamethasone dipropionate in the treatment of foot dermatophytosis. In this study, naftifine was found to have a significantly higher recovery rate compared to clotrimazole / betamethasone dipropionate in terms of mycological recovery, treatment effectiveness and overall improvement. Regarding the frequency of mycological recovery, the effectiveness of the treatment, and the overall improvement in this study, a significantly higher efficacy was found to be for 1% naftifin cream than for 1% clotrimazole / 0.05% betamethasone dipropionate ^[4] .
• The retention time in the skin after a single application of 1% cream of ³ H-labeled naphthyne to unaffected forearm skin was significant in several patients. When conducting this in vivo study, it was confirmed that even 5-10 days after the use of the drug, the concentrations of naftifin in the epidermis were 3-5 times higher than the minimum inhibitory concentration (MIC) for Trichophyfon menfagrophytes . This is the rationale for such a treatment regimen as applying the drug once a day.
• Naphthyphine penetrates the skin transdermally. This was confirmed in studies with labeled ¹⁴ C naphthyphine ^[5] . A number of concentrations of the drug were obtained in various layers of the skin - 1300 μg / ml in the stratum corneum, 38 μg / ml in other layers of the epidermis, 13.5 μg / ml in the dermis and only 0.5 μg / ml in the subcutaneous layer. In vitro penetration of naphthyphine into various layers of nails has also been studied. Naphthyne was determined in all layers of the nail plate.
• According to a new study by Verma A., naphthyne has a powerful fungicidal effect on the most common dermatophytes without the development of resistance during repeated exposure of strains. He demonstrated fungicidal activity against 83% of the studied Trichophyton strains. In this case, the development of resistance to naphthyphine with its repeated exposure was not observed in dermatophytes. This allows us to consider naftifine an effective tool in the fight against fungal infections ^[6] .

When applied externally, naftifin quickly penetrates the skin and nails by the transdermal route, creating stable antifungal concentrations in their various layers, which makes it possible to use it once a day. After application to the skin of the cream, systemic absorption is exposed to from 4.2% to 6% of the active substance ^[2] . In vitro penetration of naphthyphine into various layers of nails has also been studied. Naphthyne was determined in all layers of the nail plate.

In this case, the drug is well tolerated and does not cause significant side effects from the central nervous system and circulatory system. Naftifin is almost completely metabolized, with the formation of many metabolites. Metabolites do not have an antifungal effect and are excreted in urine and bile. The half-life of the drug is 2-3 days ^[7] .

Indications for use

• fungal infections of the skin and skin folds ( tinea corporis , tinea inguinalis ), including interdigital mycoses ( tinea manum , tinea pedum );
• fungal infections of the nails (onychomycosis);
• candidiasis of the skin;
• pityriasis versicolor;
• dermatomycosis (with or without itching).

The drug is effective in the treatment of mycoses affecting areas of the skin with hyperkeratosis, as well as in areas of hair growth ^[7] .

Contraindications

Hypersensitivity to naftifine, propylene glycol, benzyl alcohol (as part of a cream) and other components of the drug; pregnancy and lactation (safety and efficacy not determined). Application of the drug to the wound surface is contraindicated ^[7] .

Special instructions

Precautions for use

Naftifin is not intended for use in ophthalmology. Avoid contact with the eyes and open wounds ^[7] .

Impact on the ability to drive vehicles and other mechanisms

Naftifin does not adversely affect the ability to drive vehicles and perform other activities that require concentration and speed of psychomotor reactions ^[7] .

Ways to use

Cream and solution are applied externally. The solution is preferable to use for fungal infections of the nail plate, and cream - for fungal infections of the skin.

The drug is applied 1 time per day to the affected surface of the skin and adjacent areas (approximately 1 cm of a healthy area of ​​the skin along the edges of the affected area) after thorough cleaning and drying. The duration of therapy with dermatomycosis is 2-4 weeks (if necessary, up to 8 weeks), with candidiasis - 4 weeks. With nail damage, the drug is applied 2 times a day to the affected nail. Before the first use of the drug, the affected part of the nail is removed as much as possible with scissors or a nail file. The duration of therapy for onychomycosis is up to 6 months. To prevent relapse, treatment should be continued for at least 2 weeks after the disappearance of clinical symptoms ^{[7] [8] [9]} .

Side

In some cases, local reactions may occur: dry skin, flushing of the skin and burning sensation. Side effects are reversible and do not require discontinuation of treatment ^[7] .

Overdose

No cases of overdose have been reported ^[7] .

Interaction with other medicinal substances

No interaction with other drugs was noted ^[7] .

Holiday Terms

Over-the-counter ^[7] .

• Site of the Radar Drug Encyclopedia (rlsnet.ru). Naftifine (Naftifine): instruction, application and formula.