Clotrimazole

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Contents

[edit] BRAND NAMES

  • Canesten, Gyne-Lotrimin, Gynocanesten
  • Canada: Canesten, Canesten Cream 6, Canesten Cream 3, Canesten ComforTAB 3, Canesten Cream 1, Canesten ComforTAB 1, Canesten Combi-Paks PI
  • U.S.: Mycelex

[edit] STRUCTURE

Clotrimazole.jpg

[edit] MECHANISM OF ACTION

Clotrimazole 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

  • Treatment of a wide range of skin infections caused by fungi such as, ringworm (tinea corporis), athlete's foot (tinea pedis), and jock itch (tinea cruris)
  • Treatment for vaginal thrush (Candidiasis)

[edit] DOSAGE

  • Topical: apply to the affected area of skin two to three times daily. Treatment should be continued for at least one month.
  • Thrush:
    • vaginal cream: Apply clotrimazole vaginal cream, once daily, preferably in the evening for 1, 3, or 6 successive days (Depending on the cream), one applicator should be filled with cream and inserted as deeply as possible into the vagina with the patient lying on her back.
    • Vaginal Pessaries: The pessaries should be inserted as deeply as possible into the vagina once daily, preferably in the evening before going to bed. A course of treatment normally consists of either a single 500 mg pessary or of six 100 mg pessaries. The latter may be given either as two pessaries, inserted one after the other, daily for three days or as one pessary daily for six days. Clinical investigations have shown comparable efficacy from either dosage scheme. Where a first course proved unsuccessful, a second course produced success in 8 of 12 women treated.

[edit] CONTRAINDICATIONS

hypersensitivity to clotrimazole

[edit] PRECAUTIONS

  • Treatment for vaginal thrush (Candidiasis) during the menstrual period should not be performed. The treatment should be finished before the onset of menstruation.

[edit] INTERACTIONS

  • Tacrolimus: Concomitant medication with vaginal Clotrimazole and oral tacrolimus (immunosuppressant) might lead to increased tacrolimus plasma levels. Patients should thus be thoroughly monitored for symptoms of tacrolimus overdosage

[edit] PREGNANCY AND LACTATION

  • Vaginal Clotrimazole should not be used in the first trimester of pregnancy unless the physician considers it essential to the welfare of the patient. The use of applicators may be undesirable in some pregnant patients and digital insertion of the vaginal tablets may be considered. Sanitation of the birth canal should be ensured particularly during the last 4 – 6 weeks of pregnancy.

[edit] SIDE EFFECTS

Vaginal Clotrimazole: Vaginal Clotrimazole is well tolerated after topical application.
Erythema, stinging, blistering, genital peeling, edema, discomfort within the reproductive system and breasts, pruritus, allergic reaction (syncope, hypotension, dyspnea, urticaria), general irritation of the skin, pelvic pain and abdominal pain have been reported infrequently.

[edit] RELATED LINKS

Azoles mechanism of action

[edit] BIBLIOGRAPHY

[edit] REFERENCES

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