• Indication
  • Mode of Action
  • Pharmacokinetics
  • Dosage
  • Packing

Antifungals Itraconazole belongs to the class of triazole derivatives.It is used indicated for the treatment of the following fungal infections in immunocompromised and non-immunocompromised adult patients (1): • Blastomycosis, pulmonary and extrapulmonary • Histoplasmosis, including chronic cavitary pulmonary disease and disseminated, non-meningeal histoplasmosis, and • Aspergillosis, pulmonary and extrapulmonary, in patients who are intolerant of or who are refractory to amphotericin B therapy.

Itraconazole acts by inhibiting the fungal cytochrome P-450 dependent enzyme lanosterol 14-α-demethylase. When this enzyme is inhibited it blocks the conversion of lanosterol to ergosterol, which disrupts fungal cell membrane synthesis.

Peak plasma concentrations of itraconazole are reached within 2 to 5 hours following oral administration. As a consequence of non-linear pharmacokinetics, itraconazole accumulates in plasma during multiple dosing. Steady-state concentrations are generally reached within about 15 days, with Cmax values of 0.5 μg/mL, 1.1 μg/mL and 2.0 μg/mL after oral administration of 100 mg once daily, 200 mg once daily and 200 mg b.i.d., respectively. The terminal half-life of itraconazole generally ranges from 16 to 28 hours after single dose and increases to 34 to 42 hours with repeated dosing.

The usual dosing of Itraconazole is 100mg BD or 200mg OD. Under fasted conditions, itraconazole absorption was decreased in the presence of decreased gastric acidity. The absorption of itraconazole may be decreased with the concomitant administration of antacids or gastric acid secretion suppressors. Rare cases of serious hepatotoxicity have been observed with SPORANOX® treatment, including some cases within the first week. It is recommended that liver function monitoring be considered in all patients receiving

It is available in capsule in packaging of 10*10s

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