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Clotrimazole / G01AF02
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Off-label Usage
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Related FDA Approved Drug
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FDA : Bµî±Þ
(clotrimazole vaginal use )
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Pharmacokinetics
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Mechanism of Action
Clotrimazole¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Clotrimazole interacts with yeast 14-¥á 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.
Pharmacology
Clotrimazole¿¡ ´ëÇÑ Pharmacology Á¤º¸ 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.
Metabolism
Clotrimazole¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 11A1 (CYP11A1)Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2D6 (CYP2D6)
Protein Binding
Clotrimazole¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 90%
Half-life
Clotrimazole¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2 hours
Absorption
Clotrimazole¿¡ ´ëÇÑ Absorption Á¤º¸ Poorly and erratically absorbed orally, minimal vaginal or topical absorption.
Pharmacokinetics
ClotrimazoleÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
Èí¼ö : ¿Ü¿ë : Á¤»ó ÇǺθ¦ ÅëÇØ¼´Â °ÅÀÇ Èí¼öµÇÁö ¾Ê´Â´Ù.
Ç÷ÁßÃÖ°í³óµµ µµ´Þ½Ã°£ :
Troches : Ÿ¾× ³óµµ : 3½Ã°£ À̳»
Áú Å©¸² : Áú³» ³óµµ : 8-24 ½Ã°£ À̳»
ÁúÁ¤ : Áú³» ³óµµ : 1-2 ÀÏ À̳»
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Biotransformation
Clotrimazole¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic (metabolized to inactive metabolites)
Toxicity
Clotrimazole¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include erythema, stinging, blistering, peeling, edema, pruritus, urticaria, burning, and general irritation of the skin, and cramps.
Drug Interactions
Clotrimazole¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
CYP450 Drug Interaction
[CYP450 TableÁ÷Á¢Á¶È¸]
Food Interaction
Clotrimazole¿¡ ´ëÇÑ Food Interaction Á¤º¸ Not Available
Drug Target
[Drug Target]
Description
Clotrimazole¿¡ ´ëÇÑ Description Á¤º¸ An imidazole derivative with a broad spectrum of antimycotic activity. It 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. [PubChem]
Dosage Form
Clotrimazole¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Cream IntravaginalCream Topical
Drug Category
Clotrimazole¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-Infective Agents, LocalAntifungal AgentsGrowth Inhibitors
Smiles String Canonical
Clotrimazole¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ ClC1=CC=CC=C1C(N1C=CN=C1)(C1=CC=CC=C1)C1=CC=CC=C1
Smiles String Isomeric
Clotrimazole¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ ClC1=CC=CC=C1C(N1C=CN=C1)(C1=CC=CC=C1)C1=CC=CC=C1
InChI Identifier
Clotrimazole¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C22H17ClN2/c23-21-14-8-7-13-20(21)22(25-16-15-24-17-25,18-9-3-1-4-10-18)19-11-5-2-6-12-19/h1-17H
Chemical IUPAC Name
Clotrimazole¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ 1-[(2-chlorophenyl)-di(phenyl)methyl]imidazole
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