Econazole (vaginal)

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[edit] BRAND NAMES

[edit] STRUCTURE

Econazole.jpg

[edit] MECHANISM OF ACTION

Econazole is an antifungal agent of the imidazole class. It inhibits lanosterol 14α-demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol.

Ergosterol is an essential component of the fungal cell membrane. The inhibition of its synthesis results in accumulation of toxic 14α-methylated sterols and the production of a defective cell membrane with altered permeability and leakage of cellular contents.

[edit] INDICATIONS

Local treatment of fungal infections of the vagina

[edit] DOSAGE

  • Ovules (50 mg): One ovule is inserted high into the vagina once daily at bedtime for not less than 14 consecutive days. The treatment should be continued for the full course even if the subjective symptoms (pruritus, leucorrhoea) disappear.
  • Ovules (150 mg): Adults: One ovule should be inserted high into the vagina once daily at bedtime for three consecutive days. In event of relapse, or if the culture examination one week after treatment is positive, a second round of treatment should be undertaken.
  • Depot Ovules 150 mg (Gyno-Pevaryl depot): One depot ovule is inserted high into the vagina in the morning and one in the evening.
  • Vaginal cream (1%): 1 applicator full (5cc) is administered into the vagina once daily at bedtime for not less than 14 consecutive days. The treatment should be continued for the full course, even if the subjective symptoms (pruritus, leucorrhoea) disappear.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to econazole

[edit] WARNINGS AND PRECAUTIONS

  • If marked irritation or sensitivity should occur the treatment should be discontinued.

[edit] INTERACTIONS

  • Clinically relevant interactions are unlikely to occur

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Econazole (vaginal) should not be used in the first trimester of pregnancy unless the physician considers it essential to the welfare of the patient. Econazole (vaginal) may be used during the second and third trimester if the potential benefit to the mother outweighs the possible risks to the fetus
  • Nursing Mothers: It is not known whether econazole is excreted in human milk. Caution should be exercised when using Econazole (vaginal) if the patient is breastfeeding.

[edit] SIDE EFFECTS

Intravaginal econazole is usually been well tolerated, side effects being limited to local irritation [1] such as burning and stinging sensations, pruritus, and erythema in about 1 to 4% of patients in most studies.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://www.ncbi.nlm.nih.gov/pubmed/98315
Antifungals
Ergosterol target : Cell membrane target Azoles (lanosterol 14 alpha-demethylase inhibitors) : Ergosterol inhibitors Imidazoles Topical: Bifonazole   Clotrimazole   Econazole   Fenticonazole   Ketoconazole   Isoconazole   Miconazole   Sertaconazole   Tioconazole
Triazoles Topical: Fluconazole   Terconazole
Systemic: Fluconazole   Itraconazole   Posaconazole   Voriconazole
Polyene antimycotics (ergosterol binding; they form pores in the membrane) Topical: Nystatin
Systemic: Amphotericin B
Allylamines (squalene epoxidase inhibitors) : Ergosterol inhibitors Topical: Amorolfine   Naftifine   Terbinafine
Systemic: Terbinafine
Echinocandins (β-glucan synthase inhibitors) : Cell wall target Anidulafungin   Caspofungin   Micafungin
Pyrimidine analogues / Thymidylate synthase inhibitors : Nucleic acid inhibitors Flucytosine
Mitotic inhibitors Griseofulvin
Others Ciclopirox