The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer)

Journal of Antimicrobial Chemotherapy

Volumn 69, Issue 4, 2014, Pages 863-870

  Olliaro, Piero ^a,b   Delgado Romero, Petra ^c   Keiser, Jennifer ^d,e  

^a WORLD HEALTH ORGANIZATION   (Switzerland)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c PHARMALEX GMBH   (Germany)

^d SWISS TROPICAL AND PUBLIC HEALTH INSTITUTE   (Switzerland)

^e UNIVERSITY OF BASEL   (Switzerland)

Author keywords

Chemotherapy; Schistosoma spp.; Schistosomiasis

Indexed keywords

CARBAMAZEPINE; CYSTICIDE; GENERIC DRUG; PHENYTOIN; PRAZIQUANTEL; RIFAMPICIN; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; CLINICAL TRIAL (TOPIC); DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG ELIMINATION; DRUG MEGADOSE; DRUG MILK LEVEL; DRUG PENETRATION; DRUG SOLUBILITY; ENANTIOMER; FIRST PASS EFFECT; HUMAN; MAXIMUM PLASMA CONCENTRATION; META ANALYSIS (TOPIC); MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; RACEMIC MIXTURE; REVIEW; SCHISTOSOMIASIS; SINGLE DRUG DOSE; SYSTEMATIC REVIEW (TOPIC); TIME TO MAXIMUM PLASMA CONCENTRATION; UNSPECIFIED SIDE EFFECT;

CHEMOTHERAPY; SCHISTOSOMA SPP.; SCHISTOSOMIASIS;

ANTHELMINTICS; HUMANS; PRAZIQUANTEL; SCHISTOSOMIASIS; STEREOISOMERISM;

EID: 84896442621     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkt491     Document Type: Review

References (74)

1. Steinmann P, Keiser J, Bos R et al. Schistosomiasis and water resources development: systematic review, meta-analysis, and estimates of people at risk. Lancet Infect Dis 2006; 6: 411-25.
2. Murray CJ, Vos T, Lozano R et al. Disability-adjusted life years (DALYs) for 291 diseases and injuries in 21 regions, 1990-2010: a systematic analysis for the Global Burden of Disease Study 2010. Lancet 2012; 380: 2197-223.
3. Utzinger J, Keiser J. Schistosomiasis and soil-transmitted helminthiasis: common drugs for treatment and control. Expert Opin Pharmacother 2004; 5: 263-85.
4. Utzinger J, N'Goran EK, Caffrey CR et al. From innovation to application: social-ecological context, diagnostics, drugs and integrated control of schistosomiasis. Acta Trop 2011; 120 Suppl 1: S121-37.
5. Gryseels B. Schistosomiasis. Infect Dis Clin North Am 2012; 26: 383-97.
6. WHO. Sustaining the Drive to Overcome the Global Impact of Neglected Tropical Diseases. Second WHO Report on Neglected Tropical Diseases. Crompton DWT, ed. Geneva: WHO, 2013.
7. Stothard JR, Sousa-Figueiredo JC, Navaratnam AM. Advocacy, policies and practicalities of preventive chemotherapy campaigns for African children with schistosomiasis. Expert Rev Anti Infect Ther 2013;11: 733-52.
8. Stothard JR, Sousa-Figueiredo JC, Betson M et al. Schistosomiasis in African infants and preschool children: let them now be treated! Trends Parasitol 2013; 29: 197-205.
9. Meyer T, Sekljic H, Fuchs S et al. Taste, a new incentive to switch to (R)-praziquantel in schistosomiasis treatment. PLoS Negl Trop Dis 2009; 3: e357.
10. Woelfle M, Seerden JP, de Gooijer J et al. Resolution of praziquantel. PLoS Negl Trop Dis 2011; 5: e1260.
11. Woelfle M, Olliaro P, Todd MH. Openscience is a research accelerator. Nat Chem 2011; 3: 745-8.
12. Keiser J, Ingram K, Utzinger J. Antiparasitic drugs for paediatrics: systematic review, formulations, pharmacokinetics, safety, efficacy and implications for control. Parasitology 2011; 138: 1620-32.
13. Montresor A, Stoltzfus RJ, Albonico M et al. Is the exclusion of children under 24 months from anthelmintic treatment justifiable? Trans R Soc Trop Med Hyg 2002; 96: 197-9.
14. Montresor A, Awasthi S, Crompton DWT. Use of benzimidazoles in children younger than 24 months for the treatment of soil-transmitted helminthiasis. Acta Trop 2003; 86: 223-32.
15. Andrews P, Thomas H, Pohlke R et al. Praziquantel. Med Res Rev 1983; 3: 147-200.
16. King CH, Mahmoud AA. Drugs five years later: praziquantel. Ann Intern Med 1989; 110: 290-6.
17. Cioli D, Pica-Mattoccia L. Praziquantel. Parasitol Res 2003; 90: S3-9.
18. Dayan AD. Albendazole, mebendazole and praziquantel. Review of non-clinical toxicity and pharmacokinetics. Acta Trop 2003; 86: 141-59.
19. Ali BH. A short review of some pharmacological, therapeutic and toxicological properties of praziquantel in man and animals. Pak J Pharm Sci 2006; 19: 170-5.
20. Lindenberg M, Kopp S, Dressman JB. Classification of orallyadministered drugs on the World Health Organization Model list of Essential Medicines according to the biopharmaceutics classification system. Eur J Pharm Biopharm 2004; 58: 265-78.
21. Benet LZ, Broccatelli F, Oprea TI. BDDCS applied to over 900 drugs. AAPSJ 2011; 13: 519-47.
22. Mandour ME, el Turabi H, Homeida MM et al. Pharmacokinetics of praziquantel in healthy volunteers and patients with schistosomiasis. Trans R Soc Trop Med Hyg 1990; 84: 389-93.
23. el Guiniady MA, el Touny MA, Abdel-Bary MA et al. Clinical and pharmacokinetic study of praziquantel in Egyptian schistosomiasis patients with and without liver cell failure. Am J Trop Med Hyg 1994; 51: 809-18.
24. Ofori-Adjei D, Adjepon-Yamoah KK, Lindstrom B. Oral praziquantel kinetics in normal and Schistosoma haematobium-infected subjects. Ther Drug Monit 1988; 10: 45-9.
25. Valencia CI, Catto BA,Webster LT Jr et al. Concentration time course of praziquantel in Filipinos with mild Schistosoma japonicum infection. Southeast Asian J Trop Med Public Health 1994; 25: 409-14.
26. Watt G, White NJ, Padre L et al. Praziquantel pharmacokinetics and side effects in Schistosoma japonicum-infected patients with liver disease. J Infect Dis 1988; 157: 530-5.
27. Metwally A, Bennett J, Botros S et al. Impact of drug dosage and brand on bioavailability and efficacy of praziquantel. Pharmacol Res 1995; 31: 53-9.
28. Kaojarern S, Nathakarnkikool S, Suvanakoot U. Comparative bioavailability of praziquantel tablets. Dicp 1989; 23: 29-32.
29. Leopold G, Ungethum W, Groll E et al. Clinical pharmacology in normal volunteers of praziquantel, a newdrug against schistosomes and cestodes. An example of a complex study covering both tolerance and pharmacokinetics. Eur J Clin Pharmacol 1978; 14: 281-91.
30. Undevia SD, Gomez-Abuin G, Ratain MJ. Pharmacokinetic variability of anticancer agents. Nat Rev Cancer 2005; 5: 447-58.
31. Castro N, Medina R, Sotelo J et al. Bioavailability of praziquantel increases with concomitant administration of food. Antimicrob Agents Chemother 2000; 44: 2903-4.
32. Homeida M, Leahy W, Copeland S et al. Pharmacokinetic interaction between praziquantel and albendazole in Sudanese men. Ann Trop Med Parasitol 1994; 88: 551-9.
33. Lopez-Gomez M, Castro N, Jung H et al. Optimization of the single-day praziquantel therapy for neurocysticercosis. Neurology 2001; 57: 1929-30.
34. Wilkinson GR. The effects of diet, aging and disease-states on presystemic elimination and oral drug bioavailability in humans. Adv Drug Deliv Rev 1997; 27: 129-59.
35. Murray M. Altered CYP expression and function in response to dietary factors: potential roles in disease pathogenesis. Curr Drug Metab 2006; 7: 67-81.
36. Kearns GL, Abdel-Rahman SM, Alander SW et al. Developmental pharmacology-drug disposition, action, and therapy in infants and children. N Engl J Med 2003; 349: 1157-67.
37. Jung-Cook H. Pharmacokinetic variability of anthelmintics: implications for the treatment of neurocysticercosis. Expert Rev Clin Pharmacol 2012; 5: 21-30.
38. Putter J, Held F. Quantitative studies on the occurrence of praziquantel in milk and plasma of lactating women. Eur J Drug Metab Pharmacokinet 1979; 4: 193-8.
39. Dollery CT. Praziquantel. In: Therapeutic Drugs. Edinburgh, UK: Churchill Livingstone, 1999; 184-8.
40. Gonzalez-Esquivel D, Rivera J, Castro N et al. In vitro characterization of some biopharmaceutical properties of praziquantel. Int J Pharm 2005; 295: 93-9.
41. Bohnert T, Gan LS. Plasma protein binding: from discovery to development. J Pharm Sci 2013; 102: 2953-94.
42. Castro N, Jung H, Medina R et al. Interaction between grapefruit juice and praziquantel in humans. Antimicrob Agents Chemother 2002; 46: 1614-6.
43. Bittencourt PR, Gracia CM, Martins R et al. Phenytoin and carbamazepine decreased oral bioavailability of praziquantel. Neurology 1992; 42: 492-6.
44. Ridtitid W, Wongnawa M, Mahatthanatrakul W et al. Rifampin markedly decreasesplasmaconcentrations of praziquantel in healthy volunteers. Clin Pharmacol Ther 2002; 72: 505-13.
45. Meier H, Blaschke G. Investigation of praziquantel metabolism in isolated rat hepatocytes. J Pharm Biomed Anal 2001; 26: 409-15.
46. Huang J, Bathena SP, Alnouti Y. Metabolite profiling of praziquantel and its analogs during the analysis of in vitro metabolic stability using information-dependent acquisition on a hybrid triple quadrupole linear ion trap mass spectrometer. Drug Metab Pharmacokinet 2010; 25: 487-99.
47. Lima RM, Ferreira MA, Ponte TM et al. Enantioselective analysis of praziquantel and trans-4-hydroxypraziquantel in human plasma by chiral LC-MS/MS: application to pharmacokinetics. J Chromatogr B Analyt Technol Biomed Life Sci 2009; 877: 3083-8.
48. Westhoff F, Blaschke G. High-performance liquid chromatographic determination of the stereoselective biotransformation of the chiral drug praziquantel. J Chromatogr 1992; 578: 265-71.
49. Staudt U, Schmahl G, Blaschke G et al. Light and scanning electron microscopy studies on the effects of the enantiomers of praziquantel and its main metabolite on Schistosoma mansoni in vitro. Parasitol Res 1992; 78: 392-7.
50. Xiao SH, You JQ, Guo HF et al. Uptake and effect of praziquantel and the major human oxidativemetabolite, 4-hydroxypraziquantel, by Schistosoma japonicum. J Parasitol 1991; 77: 241-5.
51. Koren G. Therapeutic drug monitoring principles in the neonate. Clin Chem 1997; 43: 222-7.
52. Andrews P. A summary of the efficacy of praziquantel against schistosomes in animal experiments and notes on its mode of action. Arzneimittelforschung 1981; 31: 538-41.
53. 2+ channels and praziquantel: a view from the free world. Parasitol Int 2013; 62: 619-28.
54. Manneck T, Braissant O, Haggenmüller Y et al. Isothermal microcalorimetry to study drugs against Schistosoma mansoni. J Clin Microbiol 2011; 49: 1217-25.
55. IngramK, Yaremenko IA, Krylov IB et al. Identification of antischistosomal leadsbyevaluatingbridged 1,2,4,5-tetraoxanes, alphaperoxides, and tricyclic monoperoxides. J Med Chem 2012; 55: 8700-11.
56. Keiser J, Manneck T, Vargas M. Interactions of mefloquine with praziquantel in the Schistosoma mansoni mouse model and in vitro. J Antimicrob Chemother 2011; 66: 1791-7.
57. Brindley PJ, Sher A.Thechemotherapeutic effect of praziquantel against Schistosoma mansoni is dependent on host antibody response. J Immunol 1987; 139: 215-20.
58. Xiao SH, Catto BA. Comparative in vitro and in vivo activity of racemic praziquantel and its levorotated isomer on Schistosoma mansoni. J Infect Dis 1989; 159: 589-92.
59. Tanaka M, Ohmae H, Utsunomiya H et al. A comparison of the antischistosomal effect of levo-and dextro-praziquantel on Schistosoma japonicum and S.: mansoni in mice. Am J Trop Med Hyg 1989; 41: 198-203.
60. Irie Y, Utsunomiya H, Tanaka M et al. Schistosoma japonicum and S. mansoni: ultrastructural damage in the tegument and reproductive organs after treatment with levo-and dextro-praziquantel. Am J Trop Med Hyg 1989; 41: 204-11.
61. Liu YH, Qian MX, Wang XG et al. Comparative efficacy of praziquantel and its optic isomers in experimental therapy of schistosomiasis japonica in rabbits. Chin Med J (Engl) 1986; 99: 935-40.
62. WHO. Preventive Chemotherapy in Human Helminthiasis: Coordinated Use of Anthelminthic Drugs in Control Interventions: A Manual for Health Professionals and Programme Managers. Geneva: WHO, 2006.
63. Danso-Appiah A, Olliaro PL, Donegan S et al. Drugs for treating Schistosoma mansoni infection. Cochrane Database Syst Rev 2013; issue 2: CD000528.
64. Danso-Appiah A, Utzinger J, Liu J et al. Drugs for treating urinary schistosomiasis. Cochrane Database Syst Rev 2008; issue 3: CD000053.
65. Liu YH, Qian MX, Wang XG et al. Levo-praziquantel versus praziquantel in experimental and clinical treatment of schistosomiasis japonica. ChinMedJ (Engl) 1993; 106: 593-6.
66. Wu MH, Wei CC, Xu ZY et al. Comparison of the therapeutic efficacy and side effects of a single dose of levo-praziquantel with mixed isomer praziquantel in 278 cases of schistosomiasis japonica. Am J Trop Med Hyg 1991; 45: 345-9.
67. Botros SS, El-Din SH, El-Lakkany NM et al. Drug-metabolizing enzymes and praziquantel bioavailability in mice harboring Schistosoma mansoni isolates of different drug susceptibilities. J Parasitol 2006; 92: 1344-9.
68. Xiao SH, You JQ, Guo HF. Plasma pharmacokinetics and therapeutic efficacy of praziquantel and 4-hydroxypraziquantel in Schistosoma japonicum-infected rabbits after oral, rectal, and intramuscular administration. Am J Trop Med Hyg 1992; 46: 582-8.
69. Mutapi F, Gryseels B, Roddam A. On the calculation of intestinal schistosome infection intensity. Acta Trop 2003; 87: 225-33.
70. van Dam GJ, de Dood CJ, Lewis M et al. A robust dry reagent lateral flow assay for diagnosis of active schistosomiasis by detection of Schistosoma circulating anodic antigen. Exp Parasitol 2013; 135: 274-82.
71. Coulibaly JT, N'Gbesso YK, Knopp S et al. Accuracy of urine circulating cathodic antigen test for the diagnosis of Schistosoma mansoni in preschool-aged children before and after treatment. PLoS Negl Trop Dis 2013; 7: e2109.
72. Montresor A, Engels D, Chitsulo L et al. Development and validation of a 'tablet pole' for the administration of praziquantel in sub-Saharan Africa. Trans R Soc Trop Med Hyg 2001; 95: 542-4.
73. Sousa-Figueiredo JC, Betson M, Stothard JR. Treatment of schistosomiasis in African infants and preschool-aged children: downward extension and biometric optimization of the current praziquantel dose pole. Int Health 2012; 4: 95-102.
74. Olliaro PL, Vaillant M, Hayes DJ et al. Practical dosing of praziquantel for schistosomiasis in preschool-aged children. Trop Med Int Health 2013; 18: 1085-9.