Antifungal Clotrimazole Raw materials powder

CAS:23593-75-1

MF:C22H17ClN2

MW:344.84

EINECS:245-764-8

Specification: 99% min Clotrimazole powder

Sample:Clotrimazolepowder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:white

Storage: Store at -20°C

Shelf Life: 2 Years

Test Method: HPLC

Clotrimazole powder of Usage and Synthesis.

(1) By reducing the activity of cytochrome P450, thereby inhibiting the biosynthesis of sterols such as ergosterol in fungal cell membranes, damaging fungal cell membranes and changing their permeability, so that important substances in the cells are lost.

(2) Clotrimazole can also inhibit the biosynthesis of triacylglycerol and phospholipids in fungi. 

(3) It can still inhibit the activity of oxidase and peroxidase, resulting in excessive accumulation of hydrogen peroxide in cells, causing degeneration of fungal subcellular structure and cell necrosis. 

(4) Candida albicans can inhibit the process of transforming from spore to invasive hyphae.

Drug interactions of Clotrimazole.

Clotrimazole can inhibit the metabolism of sirolimus, dofetilide and other drugs mediated by cytochrome P450 3A4, so that the blood concentration of these drugs increases; Combined with tacrolimus, trimetrexate, etc. it can slow down the metabolism of these drugs and increase their toxic reactions; The combination of clotrimazole and betamethasone can make the skin susceptible to infection or increase the chance of microbial multiplication, and the possible mechanism is that the local inflammatory response is inhibited; Combined with nystatin, amphotericin B and flucytosine, it has no synergistic antibacterial effect on Candida albicans; And when combined with amphotericin B, it has an antagonistic effect on pharmacodynamics.

Pharmacological action of Clotrimazole.

In vivo and in vitro clotrimazole has good antibacterial effect on Candida, cryptococcus, aspergillus, algae, dermatophytes, etc., the efficacy of superficial skin mycosis is similar to that of griseofulvin, the efficacy of deep fungal disease is similar to amphotericin B, and it has a good effect on visceral pathogenic fungi such as Candida albicans, Cryptococcus neoformans, coccidioides and histoplasma, etc., and the effect on Candida albicans is stronger than nystatin. Fungi are not easy to develop resistance to this product. This product is easy to absorb and can be taken internally to treat systemic and deep fungal infections, such as aspergillosis fumigatus, candidiasis albicans, cryptococcosis, coccidioidomycosis, histoplasmosis (dogs, cats) and fungal sepsis. For severe deep fungal infections, it is advisable to combine with amphotericin B. Topical use can also be used to treat superficial fungal infections, such as cockscomb ringworm and ringworm of domestic animals. Not effective for tinea capitis. Clotrimazole is also effective against certain gram-positive bacteria and Trichomonas vaginalis.

Product Methods of Bulk Clotrimazole powder.

It is obtained by esterification, addition, hydrolysis, chlorination and condensation of o-chlorobenzoic acid. It can also be chlorinated from o-chlorotoluene to obtain o-chlorotrichlorotoluene, and then condensed with benzene in the presence of aluminum trichloride to form diphenyl-(2-chlorophenyl)chloromethane, and finally condensed with imidazole to obtain clotrimazole.