Pharmacology :
Mode of action ; Invitro studies have demonstrated that itraconazole inhibits the cytochrome P-450 dependent synthesis ergosterol, which is a vital component off fugal cell membranes. Impairment of its synthesis ultimately result in an anti fungal effect.
Pharmacokinetics :
Itraconazole is absorbed from the gastrointestinal tract with maximal level of 1,5 - 4 hours after it has been given orally. ninety five percent is bound in plasma protein and distributed in the whole body. In several tissues of the body, Itraconazole level may be 10 times grater than plasma. The half life of itraconazole is 20 hours at a single dose and may be longer ( 30 hours ) when repeated. Itraconazole id metabolized in the liver and excreted in bile and urine.
Indication :
1. Candidiasis Vulvovaginal
2. Pityriasis versicolor
3. Tinea corporis/cruris
3. Tinea Pedis/manuum
4. Nail infections
5. Oropharingeal candidiasis
6. Crytococcal Meningitis.
Contraindications:
- Itraconazole is contraindicated in patients who have shown hypersensitivity to the drug or its excipients and other triazoles
- Itraconalzole should not be administered to pregnant patients or to women contemplating pregnancy.
Interaction :
- The use of Rifamicin and Phenytoin together with itraconazole can cause a decrease of itraconazole level in plasma
- Use with antasid, Adsorbent of Histamine H2 - antagonist can decrease itraconazole absorption
- The metabolism of itraconazole can be accelerated by Rifampicin
- Itraconazole could have interaction with cyclosporin A warfarin and Digoxin.
Mode of action ; Invitro studies have demonstrated that itraconazole inhibits the cytochrome P-450 dependent synthesis ergosterol, which is a vital component off fugal cell membranes. Impairment of its synthesis ultimately result in an anti fungal effect.
Pharmacokinetics :
Itraconazole is absorbed from the gastrointestinal tract with maximal level of 1,5 - 4 hours after it has been given orally. ninety five percent is bound in plasma protein and distributed in the whole body. In several tissues of the body, Itraconazole level may be 10 times grater than plasma. The half life of itraconazole is 20 hours at a single dose and may be longer ( 30 hours ) when repeated. Itraconazole id metabolized in the liver and excreted in bile and urine.
Indication :
1. Candidiasis Vulvovaginal
2. Pityriasis versicolor
3. Tinea corporis/cruris
3. Tinea Pedis/manuum
4. Nail infections
5. Oropharingeal candidiasis
6. Crytococcal Meningitis.
Contraindications:
- Itraconazole is contraindicated in patients who have shown hypersensitivity to the drug or its excipients and other triazoles
- Itraconalzole should not be administered to pregnant patients or to women contemplating pregnancy.
Interaction :
- The use of Rifamicin and Phenytoin together with itraconazole can cause a decrease of itraconazole level in plasma
- Use with antasid, Adsorbent of Histamine H2 - antagonist can decrease itraconazole absorption
- The metabolism of itraconazole can be accelerated by Rifampicin
- Itraconazole could have interaction with cyclosporin A warfarin and Digoxin.
Itraconazole chemical name is (2R,4S)-rel-1-(butan-2-yl)-4-{4-[4-(4-{[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazin-1-yl]phenyl}-4,5-dihydro-1H-1,2,4-triazol-5-one
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