shevyatiwari's version from 2015-04-22 11:06


Question Answer
A triazoleT
BA of 55%F, > 90% (55% is itraconazole)
Undergoes extensive hepatic metabolismF, unlike terbinafine and itraconazole
Steady state concentrations can be achieved rapidly by doubling the initial doseT
Steady state concentrations are reached in 48 hoursF, 5-10 days
Elimination from stratum corner is 2-3 times slower than plasmT
Accumulates in SC by sweat and direct diffusionT
Inhibits squalene epoxidaseF, inhibits 14 a lansoterol
FungicidalF, fungistatic
Approved for candidiasis, cryptococcal meningitisT, also as prophylaxis for candidiasis
Can be effective in tinea capitis and onychomycosis not caused by dermatophyte fungiT
Not effective in pit versicolorF, highly effective
Broad spectrum of actionF, narrow
Caution is advised for pro arrhythmic conditionsT
QT interval prolongation, torsades, VT, tachycardia, arrest and sudden death are noted as S/ET
Can safely be administered with cisapride, pimozide, quinidineF, C/I
C/I with erythromycin, cisapride, asetimizole, pimozide, quinidine, terfenaidne at all dosesF, only for doses > 400
Inhibitor of CYP3A4 onlyF, also CYP 2C9
Caution in liver diseaseT
Sensitivity to one azole -> increased risk for another azoleT
Headache, nausea, vomiting, abdominal pain, diarrhoea are common S/ET
Rare cases of skin disorders such as TEN, SJS, angioedema, EMT
Serious hepatotoxicity is commonF, rare
Self limiting hepatic and biliary abnormalities are reported in 0.5% T, up to 10% in chronic therapy
Cat XF, D
No effect on testosterone levelsT
INR may increase if on warfarinT - excessive anticoagulation
Cyclosporine levels may increaseT
Phenytoin, carbamazepine and theophylline levels are decreasedF, increased
LFT's need close monitoringT

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