shevyatiwari's version from 2015-04-23 03:10


Question Answer
An allylamineF, triazole
BA of 40%F, 55%
Extensive hepatic metabolismT
Should be given with colaT, esp in those fasting, relative/absolute achlorhydria (h2 inhibitors/PPI's)
Liver failure -> increase in elimination half life by a factor of 2T
Re: tablets, Should be given either with a full meal or fasted with a cola beverageT
Re; suspension, should be taken fastedT
Metabolised by numerous CYP isoformsF, only CYP3A4
Converted to an inactive metabolite hydroxyl-itraconazoleF, active metabolite
Half life of 21 hours for tabletsT, 37-40 for suspension
Peak levels at 2 hoursF, 3-5 hours
Low protein bindingF, 99.8%
Excretion in sweat is a significant modality of excretionF, cf griseofulvin, ketoconazole, fluconazole. It is extensively excreted in the sebum
Extensive excretion in sebumT
Lasts in skin for many months post completionF, 2-3 weeks
Detected in toenails up to 11 months laterT
Plasma levels drop to negligible in 7-14 days after completionT
Pulse regimen for hair -> detection in hair up to 9 months laterT
Inhibits squalene epoxidaseF, inhibits lanoseterol 14 a demethylase, prevents conversion of lansoterol to ergosterl
FungicidalF, static
FDA approved for systemic mycoses onlyF, also for dermatophyte onychomycosis
If approved for toenails, pulse regime usedF, daily regime for 12 weeks. If fingernails - pulse 200mg BD for 1/52 per month, for 2 cycles
Effective against candida onychomycosisT
For the oral solution, higher doses/kg are required cf tabletsF, lower
Effective in pityriasisT
Can be used for prophylaxis for tineaT, use 400mg once monthly for 6 months
Used for deep and invasive fungal infectionsT
CCF is not a C/I to treatmentF, can cause decreased cardiac contractility in normal patients
Proarrhythmic conditions are not C/I for azolesF,
Serious cardiac events are associated with fluconazole and itraconazoleT - QT prolongation, torsades, VT, cardiac arrest, sudden death
Cisapride, pimozide and quinidine impair excretion of itraconazoleF - can prolong QT interval, so are C/I with azoles
C/I with dofetilide, leavacetylmethydol, lovastatin, simvastatin, midazolam, triazolam, nisoldipine, dihydroergotamine, ergometrineT
Liver disease, abnormal liver enzymes is a C/IT
Past sensitivity to another azole requires cautionT, there is cross reactivity
Headache, GI and cutaneous problems are the most common S/ET
Cat BF C
Affects androgen levelsF, that's ketoconazole
IF given with cyclosporin, requires careful monitorignT
LFT's should be done prior in all patientsT
Weak inhibitor of CYP3A4F, potent inhibitor
Enters breast milkT

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