Posaconazole
CLINICAL USE
Triazole antifungal agent
DOSE IN NORMAL RENAL FUNCTION
400 mg twice daily with food or 240 mL of a nutritional supplementOr 200 mg 4 times a day without food Oropharyngeal candidiasis severe infection or in immunocompromised patients: Loading dose of 200 mg once a day on the first day, then 100 mg once a day for 13 daysProphylaxis of invasive fungal infections: 200 mg 3 times a day
PHARMACOKINETICS
Molecular weight :700.8 %Protein binding :>98 %Excreted unchanged in urine : <0.2 Volume of distribution (L/kg) :1774 litreshalf-life – normal/ESRD (hrs) :20–66 (average 35)/Unchanged DOSE IN RENAL IMPAIRMENT
GFR (mL/MIN)
20 to 50 : Dose as in normal renal function 10 to 20 : Dose as in normal renal function <10 : Dose as in normal renal function DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES
CAPD :Not dialysed. Dose as in normal renal function HD :Not dialysed. Dose as in normal renal functionHDF/high flux :Unknown dialysability. Dose as in normal renal functionCAV/VVHD :Not dialysed. Dose as in normal renal function IMPORTANT DRUG INTERACTIONS
Potentially hazardous interactions with other drugsAntidepressants: avoid concomitant use with reboxetineAntibacterials: rifamycins may reduce posaconazole concentration; avoid concomitant administration unless benefit outweighs risk; rifabutin concentration increasedAnti-epileptics: phenytoin, carbamazepine, phenobarbital and primidone may reduce posaconazole concentration – avoid concomitant administration unless benefit outweighs riskAntimalarials: avoid concomitant administration with artemether/lumefantrineAntipsychotics: increased risk of ventricular arrhythmias with pimozide and sertindole – avoid concomitant use; possibly increase quetiapine levels – reduce dose of quetiapineAntivirals: possibly increases saquinavir levelsAnxiolytics and hypnotics: increases midazolam levelsCiclosporin: increases posaconazole concentration. Posaconazole can increase ciclosporin concentration, – dose reduction may be required Ergot alkaloids: may increase ergot alkaloid concentration leading to ergotism – avoid concomitant administrationLipid-lowering drugs: possibly increased risk of myopathy with atorvastatin or simvastatinSirolimus: may increase concentration of sirolimus – adjust sirolimus dose as required according to levelsSulphonylureas: posaconazole can decrease glucose concentrations, monitor glucose levels in diabetic patients Tacrolimus: concentration of tacrolimus increased – reduce dose of tacrolimus Ulcer-healing drugs: cimetidine may reduce posaconazole concentration by 39% – avoid concomitant administration unless benefit outweighs risk; drugs which reduce gastric acidity may reduce bioavailability of posaconazoleVinca alkaloids: may increase vinca alkaloid concentration leading to neurotoxicity – avoid concomitant administration unless benefit outweighs risk. It is advised to reduce the dose of the vinca alkaloid Tacrolimus: increases C max and AUC by 121% and 358% respectively of tacrolimus – reduce tacrolimus dose to about a third of current dose and adjust as required.594 PosAConAZoLE ADMINISTRATION
Reconstition
– Route
Oral Rate of Administration
–Comments
– OTHER INFORMATION
Use with caution in people with arrhythmias, electrolyte disturbances QT prolongation, sinus bradycardia and cardiomyopathyContains 7 g of glucose per 800 mg daily dose. Measure liver function tests as moderate increases have been noted.
See how to identify renal failure stages according to GFR calculation
See how to diagnose irreversible renal disease
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