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Mycospor® [Bifonazole]

Bayer Pharma AG
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Clinical Pharmacology

Mycospor is a broad-spectrum antifungal drug derived from imidazole. The mechanism of action is associated with impaired biosynthesis of ergosterol, which is part of the cell membrane of the fungus, at two different levels, which distinguishes it from other antifungal drugs and other azole derivatives. This double action leads to structural and functional damage to the cytoplasmic membrane of fungi.

Active in relation to:

  • Dermatophytes.
  • Yeast and mold fungi.
  • Malassezia furfur.
  • Corynebacterium minutissimum.

The urea contained in the ointment performs keratoplastic function, softening the keratin of an infected nail and increasing the depth of penetration of bifonazole. This combination enhances the antimycotic effect of the drug.

The full fungicidal effect is achieved at a bifonazole concentration of 5 μg / ml and an exposure time of 6 hours.

With the defeat of yeast fungi (Candida species) at a concentration of 1-4 μg / ml, the fungistatic effect is predominantly observed; For the fungicidal effect, a bifonazole concentration of 20 mcg / ml is required. With the defeat of Corynebacterium, the concentration of bifonazole should be 0.5-2 μg / ml.

Resistant strains of fungi are very rare. Studies have not confirmed the development of secondary resistance in primary sensitive strains.

Indications

  • Dermatophytosis (including microsporia, trichophytia, rubrofitia);
  • candidiasis of the skin, nail rollers, nails, genitals;
  • pityriasis versicolor;
  • erythrasma;
  • interdigital diaper rash;
  • hyperhidrosis stop.

Composition

1 g ointment contains:

Active substances: bifonazole 10 mg; urea 400 mg;

Excipients: white beeswax, white petrolatum, lanolin.

Bifonazole is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Mycospor Bayer Pharma AG Germany ointment
Mycospor Bayer Pharma AG Germany cream
Mycospor Bayer Pharma AG Germany vials

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Mycospor® [Bifonazole]

Dosage and Administration

Ointment is applied to the infected nail 1 time per day in an amount sufficient to cover the entire surface of the nail with a thin layer. Then, the treated nail is sealed with a plaster and left under the dressing for 24 hours, after which the dressing is changed. After removing the patch, the finger (either an arm or a leg) is immersed in warm water for about 10 minutes and then the softened part of the infected nail is carefully removed with a scraper. The nails treated in this way are thoroughly dried, ointment is applied again and sealed with a plaster. To cover with ointment the skin areas adjacent to the nail should not be. If signs of irritation appear, the skin around the nail can be treated with zinc paste before applying the patch.

The treatment should be carried out carefully, changing the dressings every day, and continue until the softened nail plate infected with the fungus is no longer removed with a scraper and the nail bed becomes smooth. It usually takes 7-14 days, depending on the extent of the infection and the thickness of the nail.

Ointment Mycospor acts only on the infected nail plate, without affecting healthy areas. It is necessary to monitor the state of the nail in the process of therapy.

The patient should be informed that after removal of the affected nail plate (ie, after 7-14 days of therapy), it is necessary to consult a doctor.

For the final antifungal therapy, apply the cream Mycospor 1 time per day for 4 weeks.

Adverse reactions

Slight redness and irritation of the skin, burning; local reactions at the edges or on the nail bed (irritation, redness, maceration, desquamation, contact dermatitis); allergic reactions.

Contraindications

Hypersensitivity, infancy (use is possible only under the supervision of a physician).

Pregnancy and Lactation

The drug is contraindicated for use in the first trimester of pregnancy.

Special instructions

When using the drug, it should be borne in mind that the success of therapy largely depends on the thoroughness of the removal of the affected areas of the nail and the subsequent treatment of the nail bed with Microspor cream or one of the other forms of the drug.

In very rare cases, allergic reactions to the patch may occur, in which case it is possible to use another type of patch or rubber patch.

- Use in pediatrics At present, there is insufficient clinical data on the use of Micospor ointment in children. Despite the fact that there is no clinical evidence of the negative impact of Mycospor in this category of patients, the treatment of onychomycosis in children should be carried out only according to strict indications and under medical supervision.

  • Brand name: Mycospor
  • Active ingredient: Bifonazole
  • Dosage form: Ointment + dispenser + plaster + srebok
  • Manufacturer: Bayer Pharma AG
  • Country of Origin: Germany

Studies and clinical trials of Bifonazole (Click to expand)

  1. Researches on Antibacterial and Antifungal Agents, XII1): Analogues of Bifonazole with Two Imidazole Moieties and Related Azoles
  2. Antibacterial and Antifungal Agents, XV: Synthesis and Antifungal Activity of Structural Analogues of Bifonazole and Ketoconazole
  3. Synthesis, Antibacterial and Antifungal Activities of Bifonazole Derivatives
  4. Association of high-dose bifonazole administration during early pregnancy and severe limb reduction defects in the newborn
  5. ChemInform Abstract: Chiral Azole Derivatives. Part 4. Enantiomers of Bifonazole and Related Antifungal Agents: Synthesis, Configuration Assignment, and Biological Evaluation.
  6. ChemInform Abstract: Synthesis and Biological Evaluation of Azole Derivatives, Analogues of Bifonazole, with a Phenylisoxazolyl or Phenylpyrimidinyl Moiety.
  7. Copper Carbenoid Mediated N-Alkylation of Imidazoles and Its Use in a Novel Synthesis of Bifonazole.
  8. Enantiomeric resolution of bifonazole by supercritical fluid chromatography
  9. Effects of the newer antifungal agents (bifonazole, ICI 195, 739 and amorolfin) on in vitro phagocytic, lymphocytic and natural-killer cell responses
  10. Gas chromatographic—mass spectrometric determination of two new antimycotic agents, 1-[(5-chloro-2-benzofuranyl)(2-chlorophenyl)methyl]-1H-imidazole and 1-[(5-bromo-2-benzofuranyl)phenylmethyl]-1H-imidazole, in rabbit plasma following topical administration: a preliminary comparison with bifonazole
  11. Chromatographic approach to study β-cyclodextrin as a promoter of the penetration of bifonazole into keratinic tissue
  12. Determination of bifonazole in creams containing methyl- and propyl p-hydroxybenzoate by derivative spectrophotometric method
  13. Treatment of pityriasis versicolor with a shampoo containing 1% bifonazole (AgisporR shampoo) in children
  14. Treatment of onychomycosis: a randomized, double-blind comparison study with topical bifonazole-urea ointment alone and in combination with short-duration oral griseofulvin
  15. Bifonazole (Mycospor® cream) in the treatment of moccasin-type tinea pedis. Comparison between combination therapy of bifonazole cream +10% urea ointment (Urepearl®) and occlusive dressing therapy with the same agents
  16. Onychomycosis in Children: Treatment with Bifonazole-Urea
  17. Molecular design of two sterol 14α-demethylase homology models and their interactions with the azole antifungals ketoconazole and bifonazole
  18. Bifonazole, but not the structurally-related clotrimazole, induces both peroxisome proliferation and members of the cytochrome P4504A sub-family in rat liver
  19. Copper carbenoid mediated N-alkylation of imidazoles and its use in a novel synthesis of bifonazole
  20. Short course bifonazole therapy in pityriasis versicolor
  21. A single application of bifonazole 1% location in pityriasis versicolor
  22. A clinical double-blind trial comparing amorolfine cream 0·5% (RO-14-4767) with bifonazole cream 1% in the treatment of dermatomycoses
  23. Double-blind comparison of amorolfine and bifonazole in the treatment of dermatomycoses
  24. Ultra-short topical treatment of pityriasis versicolor with 2.5% bifonazole cream

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