Itraconazole Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R36/38:Reizt die Augen und die Haut.
R22:Gesundheitsschädlich beim Verschlucken.
S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Chemische Eigenschaften
Off-White Crystalline Solid
Verwenden
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..
Indications
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.
Antimicrobial activity
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.).
Acquired resistance
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.
Allgemeine Beschreibung
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.
Pharmazeutische Anwendungen
A synthetic dioxolane triazole available for oral or parenteral
administration.
Clinical Use
Aspergillosis
Systemic mycoses with dimorphic fungi (blastomycosis,
coccidioidomycosis, histoplasmosis, paracoccidioidomycosis, penicilliosis)
Subcutaneous mycoses (chromoblastomycosis, sporotrichosis)
Mucosal and cutaneous candidosis.
Dermatophytosis
Phaeohyphomycosis
Pityriasis versicolor
Nebenwirkungen
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.
Itraconazole Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
