CLOTRIMAZOLE TOPICAL equipment USP, 1% includes 10 mg clotrimazole USP, a synthetic antifungal agent having actually the chemical name 1-(o-Chloro-α,α-diphenylbenzyl) imidazole v the complying with structural formula:
MOLECULAR FORMULA C22H17CIN2MOLECULAR weight 344.85
Clotrimazole is one odorless, white crystalline substance. It is virtually insoluble in water, sparingly dissolve in ether and an extremely soluble in polyethylene glycol 400, ethanol, and also chloroform.
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Each mL that CLOTRIMAZOLE TOPICAL solution USP, 1% consists of 10 mg clotrimazole USP in a nonaqueous vehicle of polyethylene glycol 400.
Clotrimazole is a broad-spectrum antifungal agent the is supplied for the treatment of dermal infections brought about by various species of pathogenic dermatophytes, yeasts, and also Malassezia furfur. The primary action of clotrimazole is versus dividing and also growing organisms.
In vitro, clotrimazole exhibits fungistatic and also fungicidal task against isolates that Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, Microsporum canis, and Candida types including Candida albicans. In general, the in vitro task of clotrimazole corresponds to that of tolnaftate and also griseofulvin against the mycelia of dermatophytes (Trichophyton, Microsporum, and also Epidermophyton), and to that of the polyenes (amphotericin B and also nystatin) versus budding fungi (Candida). Making use of an in vivo (mouse) and an in vitro (mouse kidney homogenate) trial and error system, clotrimazole and also miconazole to be equally effective in avoiding the development of the pseudomycelia and mycelia the Candida albicans.
Strains the fungi having actually a herbal resistance to clotrimazole space rare. Only a solitary isolate of Candida guilliermondi has actually been reported to have actually primary resistance come clotrimazole.
No single-step or multiple-step resistance come clotrimazole has developed during successive passages the Candida albicans and Trichophyton mentagrophytes. No appreciable adjust in sensitivity to be detected after successive passages the isolates of C. Albicans, C. Krusei, or C. Pseudotropicalis in liquid or solid media comprise clotrimazole. Also, resistance can not be emerged in chemically induced mutant strains that polyene-resistant isolates the C. Albicans.
Slight, reversible resistance was detailed in 3 isolates of C. Albicans tested by one investigator. There is a single report that records the clinical appearance of a C. Albicans stress, overload with significant resistance come flucytosine and also miconazole, and also with cross-resistance come clotrimazole; the strain stayed sensitive to nystatin and also amphotericin B.
In research studies of the mechanism of action, the minimum fungicidal concentration that clotrimazole led to leakage the intracellular phosphorus compounds right into the ambient medium with concomitant breakdown of cellular main point acids and sped up potassium efflux. Both this events started rapidly and also extensively after enhancement of the drug.
Clotrimazole shows up to it is in well absorbed in humans adhering to oral administration and is got rid of mainly as inactive metabolites. Following topical and vaginal administration, however, clotrimazole shows up to it is in minimally absorbed.
Six hrs after the applications of radiation clotrimazole 1% cream and 1% equipment onto intact and also acutely inflamed skin, the concentration of clotrimazole varied from 100 mcg/cm3, in the stratum corneum to 0.5 come 1 mcg/cm3 in the stratum reticulare, and also 0.1 mcg/cm3 in the subcutis.
No measurable lot of radiation (≤0.001 mcg/mL) was uncovered in the serum within 48 hrs after application under occlusive dressing of 0.5 mL that the equipment or 0.8 g that the cream.
Only 0.5% or much less of the applied radioactivity to be excreted in the urine.
Following intravaginal administration of 100 mg 14C-clotrimazole vaginal tablet computers to ripe adult females, an typical peak serum level, corresponding to just 0.03 µg equivalents/mL the clotrimazole, was got to 1 come 2 work after application. ~ intravaginal administration of 5 g that 1% 14C-clotrimazole vaginal cream include 50 mg energetic drug, to 5 subjects (one through candidal colpitis), serum levels matching to about 0.01 µg equivalents/mL were reached in between 8 and 24 hrs after application.
INDICATIONS and also USAGE
Prescription CLOTRIMAZOLE TOPICAL equipment product is indicated for the topical therapy of candidiasis due to Candida albicans and also tinea versicolor as result of Malassezia furfur.
This formulation is also accessible as a nonprescription product which is suggested for the topical treatment of the adhering to dermal infections: tinea pedis, tinea cruris, and tinea corporis because of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton fluoccosum, and also Microsporum canis.
Topical antifungal agents room contraindicated in those patients with a background of hypersensitivity to any type of of the components of the preparation.
If irritation or sensitivity develops with the usage of clotrimazole, treatment have to be discontinued and appropriate treatment instituted.
Information for Patients
This information is to plan to help in the safe and effective use of this medication. It is not a disclosure of all possible adverse or to plan effects.
The patient should be advised to:Use the medication for the complete treatment time also though the symptoms may have improved. Notify the physician if there is no innovation after 4 mainly of treatment.Inform the doctor if the area of applications shows signs of enhanced irritation (redness, itching, burning, blistering, swelling, oozing) indicative of feasible sensitization.Avoid resources of infection or reinfection.
If over there is absence of response to clotrimazole, appropriate microbiological studies have to be repeated to check the diagnosis and rule out various other pathogens before instituting an additional course of antimycotic therapy.
Synergism or antagonism in between clotrimazole and also nystatin, or amphotericin B, or flucytosine versus strains that C. Albicans has actually not been reported.
Carcinogenesis, Mutagenesis, and Impairment of Fertility
An 18-month dental dosing study with clotrimazole in rats has actually not revealed any kind of carcinogenic effect.
In tests for mutagenesis, chromosomes that the spermatophores that Chinese hamsters which had actually been exposed come clotrimazole to be examined because that structural changes during the metaphase.
Prior to testing, the hamsters had received five oral clotrimazole sheep of 100 mg/kg human body weight. The results of this study showed that clotrimazole had no mutagenic effect.
Pregnancy category B
The disposition of 14C-clotrimazole has actually been studied in humans and animals. Clotrimazole is an extremely poorly took in following dermal applications or intravaginal administration to humans. (See CLINICAL PHARMACOLOGY.)
In clinical trials, usage of vaginally used clotrimazole in pregnant ladies in their 2nd and 3rd trimesters has actually not been connected with ill effects.
There are, however, no adequate and well-controlled studies in pregnant women during the very first trimester the pregnancy.
Studies in pregnant rats v intravaginal doses as much as 100 mg/kg have actually revealed no proof of damage to the fetus as result of clotrimazole.
High oral doses of clotrimazole in rats and also mice ranging from 50 come 120 mg/kg caused embryotoxicity (possibly an additional to maternal toxicity), disability of mating, diminished litter size and number of viable young and decreased pup survive to weaning. However, clotrimazole was not teratogenic in mice, rabbits and also rats at dental doses as much as 200, 180 and 100 mg/kg, respectively. Dental absorption in the rat quantities to approximately 90% the the administered dose.
Because animal reproduction studies are not always predictive of human being response, this drug should be offered only if clearly indicated during the very first trimester the pregnancy.
It is not well-known whether this medicine is excreted in human milk. Because many drugs are excreted in human being milk, caution should be worked out when clotrimazole is offered by a education woman.
Safety and effectiveness in pediatric patients have been created for clotrimazole when supplied as indicated and also in the recommended dosage.
The complying with adverse reactions have actually been report in connection with the use of clotrimazole: erythema, stinging, blistering, peeling, edema, pruritius, urticaria, burning, and also general irritation of the skin.
Acute overdosage v topical applications of clotrimazole is unlikely and would not be intended to cause a life-threatening situation.
DOSAGE and also ADMINISTRATION
Gently massage enough CLOTRIMAZOLE TOPICAL equipment USP, 1% right into the impacted and neighboring skin locations twice a day, in the morning and also evening.
Clinical improvement, through relief that pruritus, typically occurs in ~ the an initial week the treatment with CLOTRIMAZOLE TOPICAL systems USP, 1%. If the patient reflects no clinical development after 4 weeks of treatment v CLOTRIMAZOLE TOPICAL solution USP, 1%, the diagnosis must be reviewed.
CLOTRIMAZOLE TOPICAL solution USP, 1% is gave in 30 mL plastic bottles (NDC 51672-1260-3); boxes of one.
Mfd. By: Taro Pharmaceuticals Inc., Brampton, Ontario, CANADA L6T 1C1Dist by: Taro Pharmaceuticals U.S.A., Inc. Hawthorne, NY 10532
Revised: December, 2012
PRINCIPAL display PANEL - 30 mL bottle Carton
ClotrimazoleTopical SolutionUSP, 1%
FOR EXTERNALUSE ONLY.NOT FOROPHTHALMIC USE.
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