Bulk Itraconazole Raw Materials Powder

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Itraconazole Powder Usage and Synthesis.

Itraconazole is a synthetic triazole derivative, is a synthetic broad-spectrum antifungal drug, its antimicrobial spectrum and antimicrobial mechanism is similar to that of clotrimazole, but it has a stronger inhibitory activity against Aspergillus, it exerts antimicrobial activity by changing the permeability of the fungal cell membranes and has antimicrobial activity against the pathogens of superficial and deep fungal infections, and its antimicrobial spectrum is broader and stronger than that of ketoconazole, and it can suppress the synthesis of ergosterol in the cell membranes of the fungal cells, so as to It can inhibit the synthesis of ergosterol in the cell membrane of fungi, thus exerting antifungal effect.

This product has antibacterial activity against dermatophytes (Trichophyton, Microsporum, Sclerotinia floccosum), yeasts [Cryptococcus neoformans, Cryptosporidium glycosporium, Candida (including Candida albicans, Candida smooth and Candida crematorium)], Aspergillus spp., Histoplasma capsulatum, Paracoccus sp. Brazil, Schenk sporotrichum, Staphylococcus sp., Branchiomyces sp., Dermatophytes, and a variety of other yeast and fungus. Inhibitory effect. However, itraconazole does not inhibit the growth of Rhizoctonia solani and Trichoderma reesei.

Uses and functions of Itraconazole.

An imidazole antifungal with a triazole ring. By preventing the activation of cytochrome P-450 including oxidase and peroxidase, 14,α-methylsterol can not be dehydrogenated, can not be converted to ergosterol, so that the growth and proliferation of fungi is inhibited, has a strong lipophilicity, can be across the biological membrane, inhibit the membrane and the binding of fungi.

Its antibacterial spectrum is similar to that of ketoconazole. It is effective against superficial fungal diseases such as vaginal and oral candidiasis and cutaneous mycoses, and is expected to be a highly effective and safe drug for deep fungal infections such as cryptococcal encephalitis (in AIDS patients). It is used for vulvovaginal candidiasis, florid chaff rash and cutaneous fungal diseases caused by sensitive fungi.

Synthetic azole broad-spectrum antifungal for systemic infections caused by deep-seated fungi, also used for candidiasis and treponematosis.

Pharmacological Effects of Itraconazole.

1. Enzyme-inducing drugs: e.g. rifampicin and phenytoin can significantly reduce the oral bioavailability of the product; therefore, plasma concentrations of the product should be monitored when co-administered with enzyme-inducing drugs.

2. In vitro studies have shown no interaction in plasma protein binding between itraconazole and promethazine, cardioplegia, valium, cimetidine, anti-inflammatory pains, meglumine and sulphadoxine dimethylpyrimethamine.

3. Interactions with cyclosporine A, astemizole and terfenadine have been reported when this product is used above the recommended dose. The dose of these drugs should be reduced if taken with this product.

4. Interactions with warfarin and digoxin have been reported. Therefore, the dose of these drugs should be reduced if taken with this product.

5. No interaction has been observed between this product and AZT (Zidovudine).

6. Induction of metabolism of ethinylestradiol and norethindrone by itraconazole has not been observed.

Production method of Itraconazole Powder

From m-dichlorobenzene, compound (I) is obtained by a reaction exactly similar to that of ketoconazole. Compound (I) is then condensed with 1-acetyl-4-(4-hydroxyphenyl)piperazine, followed by hydrolysis to remove the acetyl group, condensation with p-nitrochlorobenzene, reduction by hydrogenation, chloroformate acylation, and then reaction with hydrazine hydrate followed by cyclization and alkylation to obtain itraconazole. Its intermediate 1-acetyl-4-(4-hydroxyphenyl)piperazine can be piperazine as raw material, prepared by the following reaction.

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