Clinical pharmacodynamics and pharmacokinetics of the antifungal extended-spectrum triazole posaconazole: an overview.

@article{Lipp2010ClinicalPA,
  title={Clinical pharmacodynamics and pharmacokinetics of the antifungal extended-spectrum triazole posaconazole: an overview.},
  author={H. -P. Lipp},
  journal={British journal of clinical pharmacology},
  year={2010},
  volume={70 4},
  pages={
          471-80
        }
}
  • H. Lipp
  • Published 2010
  • Chemistry, Medicine
  • British journal of clinical pharmacology
In recent years, the antifungal triazole posaconazole has become increasingly important for the prophylaxis and treatment of systemic mycoses. Although oral bioavailability of posaconazole can be enhanced by concomitant food intake and administration in divided daily doses, increased gastric pH or gut motility, as well as enzyme-inducing drugs, can result in lower plasma concentrations than expected. Whether therapeutic drug monitoring can reduce the risk of treatment failures by avoiding sub… Expand
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References

SHOWING 1-10 OF 61 REFERENCES
Clinical relevance of the pharmacokinetic interactions of azole antifungal drugs with other coadministered agents.
TLDR
An overview of all published drug-drug interactions in humans (either healthy volunteers or patients) is provided, and on the basis of these findings, recommendations for managing the specific interactions are developed. Expand
Antifungal agents – clinical pharmacokinetics and drug interactions
  • H. Lipp
  • Biology, Medicine
  • Mycoses
  • 2008
TLDR
Echinocandins reveal a more comfortable class of antifungal agents in this regard with no obvious incidence of nephrotoxic side effects compared to amphotericin B and its lipid formulations. Expand
Drug interaction assessment following concomitant administration of posaconazole and phenytoin in healthy men
TLDR
Because co-administration of phenytoin and posaconazole significantly reduces posaconzole exposure and increases pheny toin levels in some subjects, concomitant use of these agents should be avoided unless the benefit outweighs the risk. Expand
Oral Bioavailability of Posaconazole in Fasted Healthy Subjects
TLDR
It is suggested that divided daily dose administration (every 12 or 6 hours) significantly increases posaconazole exposure under fasted conditions and significantly increases the bioavailability fraction among regimens. Expand
Posaconazole: an extended-spectrum triazole antifungal agent.
TLDR
Posaconazole suspension administered at up to 800 mg/d is a reasonable alternative to conventional antifungal agents for the prevention and treatment of IFIs in high-risk populations. Expand
Disposition of Posaconazole following Single-Dose Oral Administration in Healthy Subjects
TLDR
Observations suggest that oxidative (phase 1) metabolism by cytochrome P450 isoforms represents only a minor route of elimination for posaconazole, and therefore cyto Chrome P450-mediated drug interactions should have a limited potential to impact posaconzole pharmacokinetics. Expand
Effects of oral posaconazole on the pharmacokinetics of sirolimus
TLDR
Because posaconazole has a clinically relevant effect on sirolimus exposure, the agents should probably not be coadministered. Expand
Evaluation of the pharmacokinetics of posaconazole and rifabutin following co-administration to healthy men
TLDR
Based on the reduced exposure to posaconazole observed in the limited number of subjects in this study and the increased risk for adverse events associated with elevated rifabutin concentrations, concomitant use of rifAButin and posaconzole should be avoided unless the benefit outweighs the risk. Expand
Posaconazole Plasma Concentrations in Juvenile Patients with Invasive Fungal Infection
TLDR
Posaconazole concentrations in plasma were similar for juvenile and adult patients, suggesting that clinical outcomes are expected to be similar in adults and children with refractory invasive fungal infection. Expand
Effects of oral posaconazole on the pharmacokinetic properties of oral and intravenous midazolam: a phase I, randomized, open-label, crossover study in healthy volunteers.
TLDR
Based on point estimates of logarithm-transformed data, posaconazole 200 and 400 mg BID were associated with significant increases in midazolam C(max) and AUC(tf) values, and drug interactions were evaluated using analysis of variance. Expand
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