Abstract��The wide fluctuation on blood concentration of triazole antifungal extended-spectrum drug posaconazole was exposed due to the pharmacokinetic differences and drug interaction. Based on the literatures in recent years, the pharmacological mechanism, pharmacokinetic characteristics,drug interactions and drug dosage forms were reviewed and introduced, prospects for the therapeutic drug monitoring were analyzed. And then try to provide a reference for the personalized medicine of posaconazole.
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MA Xiao,ZHAO Li,WANG Xiao-xing,DU Wen-wen,LIU Xiao. Advances in Research on Pharmacokinetic Characteristics and Therapeutic Drug Monitoring for the Antifungal Extended-Spectrum Posaconazole. Chinese Pharmaceutical Journal, 2016, 51(6): 433-436.
WANG X J,WAN Z,LI R Y,et al. Antifungal susceptibility testing of clinical isolates of fluconazole-resistant Candida spp. and itraconazoleresistant Aspergillus funmigates to posaconazole[J]. Chin J Mycol(�й����ѧ��־),2014,9(2):75-78.
[2]
ZHENG J M,ZHANG Y X. Posaconazole,a new antifungal drug[J]. World Clin Drugs(�����ٴ�ҩ��),2007,28(9):546-549.
[3]
BAXTER C G,MARSHALL A,ROBERTS M,et al. Peripheral neuropathy in patients on long-term triazole antifungal therapy[J]. J Antimicrob Chemother,2011,66(9):2136-2139.
[4]
KRISHNA G,MOTON A,MA L,et al. Pharmacokinetics and absorption of posaconazole oral suspension under various gastric conditions in healthy volunteers[J]. Antimicrob Agents Chemother,2009,53(3):958-966.
[5]
VAN BURIK J A,HARE R S,SOLOMON H F,et al. Posaconazole is effective as salvage therapy in zygomycosis: A retrospective summary of 91 cases [J]. Clin Infect Dis,2006,42(7):61-65.
[6]
FDA. Highlights of prescribing information[EB/OL]. 2010,09:1-23 [2014-09-23]. http://www. accessdata. fda. gov/drugsatfda_docs/label/2010/02 2003s008,022027s001lbl. pdf
[7]
Martindale-The Complete Drug Reference [M]. 36th ed. UK: The Pharmaceutical Press,2009:544-545.
[8]
SABATELLI F,PATEL R,MANN P A,et al. In vitro activities of posaconazole,fluconazole,itraconazole,voriconazole,and amphotericin B against a large collection of clinically important molds and yeasts [J]. Antimicrob Agents Chemother,2006,50(6):2009-2015.
[9]
WALSH T J,RAAD I,PATTERSON T F,et al. Treatment of invasive aspergillosis with posaconazole in patients who are refractory to or intolerant of conventional therapy: An externally controlled trial[J]. Clin Infect Dis,2007,44(1):2-12.
[10]
RESTREPO A,TOB�VN A,CLARK B,et al. Salvage treatment of histoplasmosis with posaconazole[J]. J Infect,2007,54(4):319-327.
[11]
WARRILOW A G,MELO N,MARTEL C M,et al. Expression,purification,and characterization of Aspergillus fumigatus sterol 14-alpha demethylase (CYP51) isoenzymes A and B[J]. Antimicrob Agents Chemother,2010,54(10):4225-4234.
[12]
NAGAPPAN V,DERESINSKI S. Reviews of anti-infective agents: Posaconazole: A broad-spectrum triazole antifungal agent[J]. Clin Infect Dis,2007,45(12):1610-1617.
[13]
ULLMANN A J,CORNELY O A,BURCHARDT A,et al. Pharmacokinetics,safety,and efficacy of posaconazole in patients with persistent febrile neutropenia or refractory invasive fungal infection[J]. Antimicrob Agents Chemother,2006,50(2):658-666.
[14]
EZZEF F,WEXLER D,COURTNEY R,et al.Oral bioavailability of posaconazole in fasted healthy subjects: Comparison between three regimens and basis for clinical dosage recommendations[J]. Clin Pharmacokinet,2005,44(2):211-220.
[15]
CONTE J E J R,GOLDEN J A,KRISHNA G,et al. Intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole at steady state in healthy subjects[J]. Antimicrob Agents Chemother,2009,53(2):703-707.
[16]
KRIETER P,FLANNERY B,MUSICK T,et al. Disposition of posaconazole following single-dose oral administration in healthy subjects[J]. Antimicrob Agents Chemother,2004,48(9):3543-3551.
[17]
WANG C J,XIE D D. Posaconazole,antifungal agent[J]. World Clin Drugs(�����ٴ�ҩ��),2007,28(8):509.
[18]
COURTNEY R,PAI S,LAUGHLIN M,et al. Pharmacokinetics,safety and tolerability of oral posaconazole administered in single and multiple doses in healthy adults[J]. Antimicrob Agents Chemother,2003,47(9):2788-2795.
[19]
WEXLER D,COURTNEY R,RICHARDS W,et al. Effect of posaconazole on cytochrome P450 enzymes: A randomized,open-label,two-way crossover study[J]. Eur J Pharm Sci,2004,21(5):645-653.
[20]
LI Y,THEURETZBACHER U,CLANCY C J,et al. Pharmacokinetic/pharmacodynamic profile of posaconazole[J]. Clin Pharmacokinet,2010,49(6):379-396.
[21]
FDA. Highlights of prescribing information[EB/OL]. 2014,03:1-38 [2014-09-23]. http://www. accessdata. fda. gov/drugsatfda_docs/label/2014/205596s000lbl. pdf
[22]
COURTNEY R,SANSONE A,SMITH W,et al. Posaconazole pharmacokinetics,safety,and tolerability in subjects with varying degrees of chronic renal disease[J]. J Clin Pharmacol,2005,45(2):185-192.
[23]
LUKE D R,TOMASZEWSKI K,DAMLE B,et al. Review of the basic and clinical pharmacology of sulfobutylether-beta-cyclodextrin (SBECD) [J]. J Pharm Sci,2010,99(8):3291-3301.
[24]
SANSONE-PARSONS A,KRISHNA G,SIMON J,et al. Effects of age,gender,and race/ethnicity on the pharmacokinetics of posaconazole in healthy volunteers[J]. Antimicrob Agents Chemother,2007,51(2):495-502.
[25]
GUBBINS P O,KRISHNA G,SANSONE-PARSONS A,et al. Pharmacokinetics and safety of oral posaconazole in neutropenic stem cell transplant recipients[J]. Antimicrob Agents Chemother,2006,50(6):1993-1999.
[26]
KONTOYIANNIS D P,LEWIS R E. How I treat mucormycosis [J]. Blood,2011,118(5):1216-1224.
[27]
JAIN R,POTTINGER P. The effect of gastric acid on the absorption of posaconazole[J]. Clin Infect Dis,2008,46(10):1627.
[28]
LEKAKIS L J,LAWSON A,PRANTE J,et al. Fatal rhizopus pneumonia in allogeneic stem cell transplant patients despite posaconazole prophylaxis:Two cases and review of the literature[J]. Biol Blood Marrow Transplant,2009,15(8):991-995.
[29]
ANDES D,PASCUAL A,MARCHETTI O. Antifungal therapeutic drug monitoring:Established and emerging indications[J]. Antimicrob Agents Chemother,2009,53(1):24-34.
[30]
EIDEN C,MENIANE J C,PEYRI�HRE H,et al. Therapeutic drug monitoring of posaconazole in hematology adults under posaconazole prophylaxis: Influence of food intake[J]. Eur J Clin Microbiol Infect Dis,2012,31(2):161-167.
[31]
JANG S H,COLANGELO P M,GOBBURU J V. Exposure-response of posaconazole used for prophylaxis against invasive fungal infections:Evaluating the need to adjust doses based on drug concentrations in plasma[J]. Clin Pharmacol Ther,2010,88(1):115-119.
[32]
SMITH J,ANDES D. Therapeutic drug monitoring of antifungals:Pharmacokinetics and pharmacodynamic considerations[J]. Ther Drug Monit,2008,30(2):167-172.
[33]
ALMYROUDIS N G,SUTTON D A,FOTHERGILL A W,et al. In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents[J]. Antimicrob Agents Chemother,2007,51(7):2587-2590.
[34]
CAMPOLI P,AL ABDALLAH Q,ROBITAILLE R,et al. Concentration of antifungal agents within host cell membranes: A new paradigm governing the efficacy of prophylaxis[J]. Antimicrob Agents Chemother,2011,55(12):5732-5739.
[35]
MOU L P,YAO Y U. Interpretation of clinical guide to histoplasmosis revised edition 2007 by Infectious Diseases Society of America[J]. World Notes on Antibiotics,2008,29(3):125-139.
[36]
KRISHNA G,MOTON A,MA L,et al. Effects of oral posaconazole on the pharmacokinetic properties of oral and intravenous midazolam: A phase I,randomized,open-label,crossover study in healthy volunteers[J]. Clin Ther,2009,31(2):286-298.
[37]
JAIN S,KAPOOR G. Severe life threatening neurotoxicity in a child with acute lymphoblastic leukemia receiving posaconazole and vincristine[J]. Pediatr Blood Cancer,2010,54(5):783.