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Active ingredient: Clotrimazole - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-Infective Agents, Local
  • Antifungal Agents
  • Growth Inhibitors

Dosage Forms

  • Cream
  • Liquid
  • Solution
  • Suppository
  • Ointment
  • Lozenge

Brands / Synonyms

Canesten; Canesten 1-Day Cream Combi-Pak; Canesten 1-Day Therapy; Canesten 3-Day Therapy; Canesten 6-Day Therapy; Canesten Combi-Pak 1-Day Therapy; Canesten Combi-Pak 3-Day Therapy; Canesten Cream; Canesten Solution; Canestine; Canifug; Chlotrimazole; Cimetidine; Cimetidine (Type A); Cimetidine (Type AB); Cimitidine; Clotrimaderm; Clotrimaderm Cream; Clotrimazol; Clotrimazole (USAN); Clotrimazole and Betamethasone; Clotrimazole ZnSO4 complex; Crystalline Clotrimazole; Empecid; FemCare; Gyne lotrimin; Gyne-lotrimin; Gyne-Lotrimin 3; Gyne-Lotrimin 3 Combination Pack; Gyne-Lotrimin Combination Pack; Gynix; Lotrimin; Lotrimin Af; Lotrimin AF Cream; Lotrimin AF Cream (OTC); Lotrimin AF Jock-Itch Cream; Lotrimin AF Lotion; Lotrimin AF Lotion (OTC); Lotrimin AF Solution; Lotrimin AF Solution (OTC); Lotrimin Cream; Lotrimin Cream (Rx); Lotrimin Lotion; Lotrimin Lotion (Rx); Lotrimin Solution; Lotrimin Solution (Rx); Lotrisone; Mono-baycuten; Mycelax; Mycelex; Mycelex 7; Mycelex Cream; Mycelex Cream (OTC); Mycelex G; Mycelex OTC; Mycelex Solution; Mycelex Solution (OTC); Mycelex Troches; Mycelex Twin Pack; Mycelex-7; Mycelex-7 Combination Pack; Mycelex-G; Myclo Cream; Myclo Solution; Myclo Spray Solution; Myclo-Gyne; Mycosporin; Mykosporin; Neo-Zol Cream; Trimysten; Trivagizole 3; Veltrim

Indications

For the local treatment of oropharyngeal candidiasis and vaginal yeast infections, also used in fungal infections of the skin such as ringworm, athlete's foot, and jock itch.

Pharmacology

Clotrimazole, an imidazole derivative with a broad spectrum of antimycotic activity, inhibits biosynthesis of the sterol ergostol, an important component of fungal cell membranes. Its action leads to increased membrane permeability and apparent disruption of enzyme systems bound to the membrane. Betamethasone and clotrimazole are used together to treat cutaneous tinea infections. In studies in fungal cultures, the minimum fungicidal concentration of clotrimazole caused leakage of intracellular phosphorous compounds into the ambient medium with concomitant breakdown of cellular nucleic acids, and accelerated potassium etflux. Both of these events began rapidly and extensively after addition of the drug to the cultures. The primary action of clotrimazole is against dividing and growing organisms.

Mechanism of Action

Clotrimazole interacts with yeast 14-α demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the membrane. In this way, clotrimazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Clotrimazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.

Absorption

Poorly and erratically absorbed orally, minimal vaginal or topical absorption.

Toxicity

Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps.

Biotrnasformation / Drug Metabolism

Hepatic (metabolized to inactive metabolites)

Contraindications

MycelexÒ Troches are contraindicated in patients who are hypersensitive to any of its components.

Drug Interactions

No information provided.

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