Posaconazole

General information:
Substance group: Antifungal ATC: J02AC04
Trade names: Noxafil®
available dosages: enteric coated tablets 100 mg, solution for oral 40 mg/ml
Reference ranges:
>0.7 mg/l
Toxic Plasma concentrations:
Sampling:
Material: Serum (Monovette brown) Minimum volume for analysis: 50µL
Recommendation: trough level (directly before the next intake)
Requirement (internal): about …. Requirement (external):
Determination method:
Test principle: liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS)
Protein precipitation with acetonitrile, chromatographic separation, mass spectrometry
Analysis according to mass charge ratio
Analysis system: triple stage Quadrupol mass spectrometer (LC-MS/MS)
Findings communication: on the day of submission, via LIMS

Pharmacokinetics:
T1⁄2 : 35 h (20 – 66 h)
Tmax : 3 h (median)
Bioavailability: 20% (with food or 4 times daily Dose: 40 – 80%) Protein binding: > 98%
Clearance:
Excretion: Fages: 77%; urine: 14%
Metabolism: hepatic
Therapeutic concentration range: >0.7mg/L
Toxic: ..
Distribution volume: 1,774 l/kg
Time to steady state: 7 – 10 days

Indication:
TDM is recommended, especially for the tablet formulation.
TDM at least every 3-6 months or more frequently in case of dose titration, suspected non-adherence, altered dosage, changes in comedic medication, adverse drug effects, insufficient clinical improvement.

DrugBank: https://go.drugbank.com/drugs/DB01263