Clotrimazole Information
Clotrimazole (0) Description
Clotrimazole (0) cream USP, 1% contains Clotrimazole (0) , a synthetic antifungal agent having the chemical name {1-(o-Chloro-α, α-diphenylbenzyl)imidazole}; the molecular formula CHClN; a molecular weight of 344.84; and the structural formula:
Clotrimazole (0) USP is an odorless, white crystalline substance. It is practically insoluble in water, sparingly soluble in ether and very soluble in polyethylene glycol 400, ethanol and chloroform.
Each gram of Clotrimazole (0) cream USP contains 10 mg Clotrimazole (0) USP, dispersed in a vanishing cream base of sorbitan monostearate, polysorbate 60, cetyl esters wax, cetostearyl alcohol, octyldodecanol, purified water, and benzyl alcohol (1%) as preservative.
Clotrimazole (0) Clinical Pharmacology
Clotrimazole (0) is a broad-spectrum antifungal agent that is used for the treatment of dermal infections caused by various species of pathogenic dermatophytes, yeasts, and . The primary action of Clotrimazole (0) is against dividing and growing organisms.
Strains of fungi having a natural resistance to Clotrimazole (0) are rare. Only a single isolate of has been reported to have primary resistance to Clotrimazole (0) .
No single-step or multiple-step resistance to Clotrimazole (0) has developed during successive passages of and . No appreciable change in sensitivity was detected after successive passage of isolates of , or in liquid or solid media containing Clotrimazole (0) . Also, resistance could not be developed in chemically induced mutant strains of polyene-resistant isolates of . Slight, reversible resistance was noted in three isolates of tested by one investigator. There is a single report that records the clinical emergence of strain with considerable resistance to flucytosine and micronazole, and with cross-resistance to Clotrimazole (0) , the strain remained sensitive to nystatin and amphotericin B.
In studies of the mechanism of action, the minimum fungicide concentration of Clotrimazole (0) caused leakage of intracellular phosphorus compounds into the ambient medium with concomitant breakdown of cellular nucleic acids and accelerated potassium efflux. Both these events began rapidly and extensively after addition of the drug.
Clotrimazole (0) appears to be well absorbed in humans following oral administration and is eliminated mainly as inactive metabolites. Following topical and vaginal administration, however, Clotrimazole (0) appears to be minimally absorbed.
Six hours after the application of radioactive Clotrimazole (0) 1% cream and 1% solution onto intact and acutely inflamed skin, the concentration of Clotrimazole (0) varied from 100 mcg/cm in the stratum corneum to 0.5 to 1 mcg/cm in the stratum reticulare, and 0.1 mcg/cm in the subcutis. No measurable amount of radioactivity (≤0.001 mcg/mL) was found in the serum within 48 hours after application under occlusive dressing of 0.5 mL of the solution or 0.8 g of the cream. Only 0.5% or less of the applied radioactivity was excreted in the urine.
Following intravaginal administration of 100 mg C-Clotrimazole (0) vaginal tablets to nine adult females, an average peak serum level, corresponding to only 0.03 μg equivalent/mL of Clotrimazole (0) , was reached one to two days after application. After intravaginal administration of 5 g of 1% C-Clotrimazole (0) vaginal cream containing 50 mg active drug, to five subjects (one with candidal colpitis), serum levels corresponding to approximately 0.01 μg equivalents/mL were reached between 8 and 24 hours after application.
Clotrimazole (0) Indications And Usage
Clotrimazole (0) cream USP is indicated for the topical treatment of candidiasis due to and tinea versicolor due to
Clotrimazole (0) is also available as a nonprescription item which is indicated for the topical treatment of the following dermal infections: tinea pedis, tinea cruris, and tinea corporis due to , , and
Clotrimazole (0) Contraindications
Clotrimazole (0) cream is contraindicated in individuals sensitive to its components.
Clotrimazole (0) Warnings
Clotrimazole (0) cream is not for ophthalmic use.
Clotrimazole (0) Precautions
An 18-month oral dosing study with Clotrimazole (0) in rats has not revealed any carcinogenic effect.
In tests for mutagenesis, chromosomes of the spermatophores of Chinese hamsters which had been exposed to Clotrimazole (0) were examined for structural changes during the metaphase. Prior to testing, the hamsters had received five oral Clotrimazole (0) doses of 100 mg/kg body weight. The results of this study showed that Clotrimazole (0) had no mutagenic effect.
The disposition of C-Clotrimazole (0) has been studied in humans and animals. Clotrimazole (0) is very poorly absorbed following dermal application or intravaginal administration to humans. (See )
In clinical trials, use of vaginally applied Clotrimazole (0) in pregnant women in their second and third trimesters has not been associated with ill effects. There are, however, no adequate and well-controlled studies in pregnant women during the first trimester of pregnancy.
Studies in pregnant rats with doses up to 100 mg/kg have revealed no evidence of harm to the fetus due to Clotrimazole (0) .
High doses of Clotrimazole (0) in rats and mice ranging from 50 to 120 mg/kg resulted in embroyotoxicity (possible secondary to maternal toxicity), impairment of mating, decreased litter size and number of viable young and decreased pup survival to weaning. However, Clotrimazole (0) was teratogenic in mice, rabbits and rats at oral doses up to 200, 180 and 100 mg/kg, respectively. Oral absorption in the rat amounts to approximately 90% of the administered dose.
Because animal reproduction studies are not always predictive of human response, this drug should be used only if clearly indicated during the first trimester of pregnancy.
Clotrimazole (0) Adverse Reactions
The following adverse reactions have been reported in connection with the use of this product: erythema, stinging, blistering, peeling, edema, pruritis, urticaria, burning, and general irritation of the skin.
Clotrimazole (0) Overdosage
Acute overdosage with topical application of Clotrimazole (0) is unlikely and would not be expected to lead to a life-threatening situation.
Clotrimazole (0) Dosage And Administration
Gently massage sufficient Clotrimazole (0) cream into the affected and surrounding skin areas twice a day, in the morning and evening.
Clinical improvement, with relief of pruritis, usually occurs within the first week of treatment with Clotrimazole (0) cream. If the patient shows no clinical improvement after four weeks of treatment with Clotrimazole (0) cream, the diagnosis should be reviewed.
Clotrimazole (0) How Supplied
Clotrimazole (0) cream USP, 1% is supplied in 15, 30, 45 and (2 x 45) gram tubes.
NDC 68462-181-17 (15 g) NDC 68462-181-35 (30 g)NDC 68462-181-47 (45 g)NDC 68462-181-48 (2 x 45 g)
Clotrimazole (0)
Clotrimazole (0)
Clotrimazole (0) Principal Display Panel
