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1, for systemic fungal infections such as aspergillosis, candidiasis, cryptococcosis (including cryptococcal meningitis), histiocytosis, sporotrichosis, Brazilian paraccidioidosis, blastomycosis and a variety of other rare systemic or tropical fungal diseases.
2, for oral, pharyngeal (foreign data), esophageal (foreign data), vulvovaginal candida infection, as well as fungal conjunctivitis, fungal keratitis.
3, for superficial fungal infections, such as tinea pedis, tinea corporis, tinea corporis, tinea versicolor, etc.
4. For onychomycosis caused by dermatophyton and (or) yeast.
Uses of Itraconazole.
Imidazole antifungal agents of triazole ring. By preventing the activation of cytochrome P-450 including oxidase and peroxidase, so that 14, α-methylsterol can not dehydrogenate, can not be converted into ergosterol, so that the growth and proliferation of fungi is inhibited, has a strong lipophilic, can pass through the biofilm, inhibit the membrane and fungal binding. Its antibacterial profile is similar to ketoconazole. It is effective for superficial fungal diseases such as vaginal and oral candidiasis and dermatomycosis, and is expected to become an efficient and safe drug for deep fungal infections such as cryptococcal encephalitis (AIDS). It is used for vulvovaginal candidiasis, pityriasis variegata and cutaneous mycosis caused by sensitive fungi.
Drug interaction of Itraconazole.
1. Enzyme-inducing drugs: such as rifampicin and phenytoin can significantly reduce the oral bioavailability of this product, so the plasma concentration of this product should be monitored when taken together with enzyme-inducing drugs.
2. In vitro studies have shown no interaction between itraconazole and imipramine, propranolol, diazepam, cimetidine, indomethacin, metanine, and sulfadimethymidine in plasma protein binding.
3. Interactions with cyclosporin A, astimizole, and terphenadine have been reported when used in excess of recommended doses. If these drugs are taken with this product, the dosage should be reduced.
4. Interactions with warfarin and digoxin have been reported. Therefore, if these drugs are taken with this product, the dose should be reduced.
5. No interaction between Zidovudine and AZT has been observed.
6. The induced effects of itraconazole on the metabolism of ethinylestradiol and norethisterone have not been observed.
Product Method of Bulk Itraconazole Powder.
Starting from m-dichlorobenzene, compound (I) can be obtained by a reaction exactly similar to ketoconazole. Compound (I) is then condensed with 1-acetyl -4-(4-hydroxyphenyl) piperazine, followed by water deacetylation, condensation with p-nitrochlorobenzene, hydroreduction, chlorocarbonate acylation, and then reaction with hydrazine hydrate and recyclization, alkylated to itraconazole. The intermediate 1-acetyl-4 -(4-hydroxyphenyl) piperazine can be prepared from piperazine by the following reaction.
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