देश: दक्षिण अफ़्रीका
भाषा: अंग्रेज़ी
स्रोत: South African Health Products Regulatory Authority (SAHPRA)
Janssen
SPORANOX™ capsules SCHEDULING STATUS Schedule 4. PROPRIETARY NAME (and dosage form) SPORANOX™ capsules COMPOSITION Each capsule contains 100 mg of itraconazole in a pellet formulation. PHARMACOLOGICAL CLASSIFICATION A.20.2.2 Antimicrobial (chemotherapeutic) agents. Fungicides. PHARMACOLOGICAL ACTION Itraconazole is a synthetic broad-spectrum triazole antifungal agent, active in vitro against strains of the following: dermatophytes (Trichophyton spp., Microsporum spp., Epidermophyton floccosum), yeasts (Cryptococcus neoformans, Candida spp.), Aspergillus spp., Histoplasma spp., Paracoccidioides brasiliensis, Sporothrix schenckii, Blastomyces dermatitidis. In vitro activity does not necessarily imply clinical efficacy. In vitro studies have demonstrated that itraconazole impairs the synthesis of ergosterol which is a vital cell membrane component in fungi. Impairment of its synthesis ultimately results in an antifungal effect. Correlation between in vitro minimum inhibitory concentration (MIC) results and clinical outcome, has yet to be established for itraconazole. The oral bioavailability of itraconazole is maximal when the capsules are given immediately after a full meal. Peak plasma levels are reached 3 to 4 hours following an oral dose. During chronic administration, steady-state is reached after 1-2 weeks. Steady-state plasma concentrations of itraconazole 3-4 hours after drug intake are 0,4 micrograms/mL (100 mg daily), 1,1 micrograms/mL (200 mg daily) and 2,0 micrograms/mL (200 mg twice daily). Elimination from plasma is biphasic with an elimination half-life of 1 to 1,5 days. The plasma protein binding of itraconazole is 99,8%. Concentrations of itraconazole in whole blood are 60% of those in plasma. Uptake in keratinous tissues especially the skin, is up to 5 times higher than in p पूरा दस्तावेज़ पढ़ें