イトラート 化學(xué)特性,用途語(yǔ),生産方法
外観
白色～わずかにうすい褐色, 結(jié)晶性粉末～粉末
溶解性
ジクロロメタンに溶けやすく、エタノールに極めて溶けにくく、水にほとんど溶けない
用途
トリアゾール系抗真菌剤です。
真菌細(xì)胞において、膜成分のエルゴステロー
ル生合成の抑制作用を示します。
用途
トリアゾール系抗真菌剤です。
真菌細(xì)胞において、膜成分のエルゴステロー
ル生合成抑制作用を示します。
効能
抗真菌薬, エルゴステロール合成阻害薬
商品名
イトリゾール (ヤンセンファーマ); イトリゾール (ヤンセンファーマ); イトリゾール (ヤンセンファーマ)
説明
Itraconazole is an orally-active triazole antifungal indicated for use in the treatment of
dermal, vaginal and systemic mycoses. In immunocompromised and AIDS patients,
itraconazole has been shown to significantly reduce the incidence of relapses of
cryptococcal meningitis.
化學(xué)的特性
Off-White Crystalline Solid
使用
Itraconazole is a triazole antifungal agent. It is used to inhibit cytochrome P-450-dependent enzymes and ergosterol synthesis. It has been used against histoplasmosis, blastomycosis, cryptococcal meningitis, and aspergillosis. It?s different formulations are used to study Candida strains in murine invasive infections. It has been used to study proliferative changes of the forestomach mucosa in alloxan-induced diabetic rats..
適応癥
Itraconazole (Sporanox) is effective in the treatment of histoplasmosis, blastomycosis,
candidiasis, and dermatophyte infection. Its efficacy in the treatment
of tinea capitis in children is equal to griseofulvin, and it is usually better
tolerated (21). It is metabolized by the cytochrome P-450 system and may
increase the levels ofwarfarin, cyclosporine, and digoxin among others. Its use
is contraindicated with certain medications.
Itraconazole (Sporanox) is a triazole antifungal that is related to the imidazole
ketoconazole. Similar to ketoconazole, it interferes with ergosterol
synthesis and cell membrane integrity. It is clinically active against dimorphic
fungi, yeast, dermatophytes, Blastomycetes, histoplasmosis, sporotrichosis,
and Aspergillus.
Itraconazole is a potent inhibitor of the cytochrome P450 3A enzyme
system, which may elevate blood levels of other drugs metabolized by this system
if taken concomitantly. Itraconazole levels may decrease in patients who
are concurrently taking rifampin, phenobarbital, or phenytoin. Cyclosporine,
felodipine, digoxin, warfarin, and oral hypoglycemic levels may increase when
given in conjunction with itraconazole.
Itraconazole, like ketoconazole, is contraindicated in patients taking cisapride.
Itraconazole may induce torsades de pointes, ventricular arrhythmias,
and congestive heart failure.
抗菌性
The spectrum includes dermatophytes, dimorphic fungi
(Blast. dermatitidis, Coccidioides spp., Hist. capsulatum, Paracocc.
brasiliensis,
Penicillium marneffei and Spor. schenckii), molds
(including Aspergillus spp.), dematiaceous fungi and yeasts
(Candida spp. and Cryptococcus spp.).
獲得抵抗性
This is uncommon, but fluconazole-resistant C. albicans and
C. glabrata are often cross-resistant to itraconazole. There are
reports of itraconazole-resistant strains of A. fumigatus.
一般的な説明
Itraconazole is an antifungal drug prescribed for oral or intravenous treatment of fungal infections. The drug is sold under trade names such as Sporanoxor Onmel
?. This Certified Spiking Solution
? is suitable as starting material for calibrators, controls, or linearity standards for clinical and diagnostic testing or therapeutic drug monitoring of itraconazole in patient blood, serum, or plasma samples by LC-MS/MS or HPLC.
応用例（製薬）
A synthetic dioxolane triazole available for oral or parenteral
administration.
臨床応用
Aspergillosis
Systemic mycoses with dimorphic fungi (blastomycosis,
coccidioidomycosis, histoplasmosis, paracoccidioidomycosis, penicilliosis)
Subcutaneous mycoses (chromoblastomycosis, sporotrichosis)
Mucosal and cutaneous candidosis.
Dermatophytosis
Phaeohyphomycosis
Pityriasis versicolor
副作用
Unwanted effects are more common with oral solution than
with capsules, and are more severe. They include nausea,
abdominal discomfort, dyspepsia, diarrhea, headache, pruritus
and skin rash. Rare side effects include Stevens–Johnson
syndrome, transient abnormalities of liver enzymes, reversible
idiosyncratic hepatitis and hypokalemia.
Intravenous itraconazole has been associated with congestive
heart failure. Neither intravenous nor oral itraconazole should
be used to treat infections in patients with evidence of ventricular
dysfunction unless the expected benefit clearly exceeds
the risk. Patients with risk factors for congestive heart failure
should be treated with caution and their condition monitored.
イトラート 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品