Comparative Bioavailability Of Two Oral Formulations Of Clozapine In Steady State Administered In Schizophrenic Volunteers Under Individualized Dose Regime

dc.creatorBorges N.C.C.
dc.creatorAstigarraga R.B.
dc.creatorSverdloff C.E.
dc.creatorGalvinas P.R.
dc.creatorBorges B.C.
dc.creatorMoreno R.A.
dc.date2012
dc.date2015-06-25T20:23:47Z
dc.date2015-11-26T15:19:30Z
dc.date2015-06-25T20:23:47Z
dc.date2015-11-26T15:19:30Z
dc.date.accessioned2018-03-28T22:29:01Z
dc.date.available2018-03-28T22:29:01Z
dc.identifier
dc.identifierCurrent Clinical Pharmacology. , v. 7, n. 4, p. 241 - 253, 2012.
dc.identifier15748847
dc.identifier10.2174/157488412803305849
dc.identifierhttp://www.scopus.com/inward/record.url?eid=2-s2.0-84867765180&partnerID=40&md5=c7941f6641b233a32a74ba8d6a6ce4f6
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/90089
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/90089
dc.identifier2-s2.0-84867765180
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1259757
dc.descriptionIn the present study, a novel, fast, sensitive and robust method to quantify clozapine in human plasma using quetiapine as the internal standard (IS) is described. The analyte and the IS were extracted from plasma using a single protein precipitation extraction technique with methanol and analyzed by high performance liquid chromatography coupled to the electrospray ionization tandem mass spectrometric (HPLC-ESI-MS/MS). The method was linear over the range 20 to 1500 ng.mL-1. The intra-assay precisions ranged from 3.8 to 5.9%, while inter-assay precisions ranged from 4.2 to 6.0%. The intra-assay accuracies ranged from 99.3 to 107.5%, while the inter-assay accuracies ranged from 98.9 to 101.7%. This method agrees with the requirements proposed by the US Food and Drug Administration of high sensitivity, specificity and high sample throughput and was used to evaluate the pharmacokinetic profiles and bioequivalence of the two clozapine formulations in twenty six schizophrenic patients affected by refractory schizophrenia under steady-state conditions. During the hospitalization period the patients received the 100 mg clozapine formulation tablets corresponding to the same dose they were using 14 days before hospitalization. The clozapine pharmacokinetic did not differ significantly after administration of both test and the reference formulations. The Tmax and T1/2 for the test formulation were 2.26 and 10.92 h, respectively. In addition, the Tmax and T1/2 for the reference formulation were 2.44 and 11.08 h, respectively. The 90% confidence interval of the mean ratio of lnAUC0-t was within 0.80-1.25 range which indicates that the test formulation was bioequivalent to the reference formulation when orally administered to schizophrenic patients regarding both the rate and extent of absorption. © 2012 Bentham Science Publishers.
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dc.descriptionLieberman, J.A., Safferman, A.Z., Clinical profile of clozapine: Adverse reactions and agranulocytosis (1992) Psychiatr Q, 63, pp. 51-70
dc.descriptionSenn, H.J., Jungi, W.F., Kunz, H., Poldinger, W., Clozapine and agranulocytosis (1977) Lancet, 1, p. 547
dc.descriptionKane, J., Honigfeld, G., Singer, J., Meltzer, H., Clozapine for the treatment-resistant schizophrenic. A double-blind comparison with chlorpromazine (1988) Arch Gen Psychiatry, 45, pp. 789-796
dc.descriptionMeltzer, H.Y., Treatment-resistant schizophrenia--the role of clozapine (1997) Curr Med Res Opin, 14, pp. 1-20
dc.descriptionJann, M.W., Grimsley, S.R., Gray, E.C., Chang, W.H., Pharmacokinetics and pharmacodynamics of clozapine (1993) Clin Pharmacokinet, 24, pp. 161-176
dc.descriptionMauri, M.C., Volonteri, L.S., Colasanti, A., Fiorentini, A., de Gaspari, I.F., Bareggi, S.R., Clinical pharmacokinetics of atypical antipsychotics: A critical review of the relationship between plasma concentrations and clinical response (2007) Clin Pharmacokinet, 46, pp. 359-388
dc.descriptionRaedler, T.J., Hinkelmann, K., Wiedemann, K., Variability of the in vivo metabolism of clozapine (2008) Clin Neuropharmacol, 31, pp. 347-352
dc.descriptionBaldessarini, R.J., Frankenburg, F.R., Clozapine. A novel antipsychotic agent (1991) N Engl J Med, 324, pp. 746-754
dc.descriptionCentorrino, F., Baldessarini, R.J., Kando, J.C., Frankenburg, F.R., Volpicelli, S.A., Flood, J.G., Clozapine and metabolites: Concentrations in serum and clinical findings during treatment of chronically psychotic patients (1994) J Clin Psychopharmacol, 14, pp. 119-125
dc.descriptionKurz, M., Hummer, M., Kurzthaler, I., Oberbauer, H., Fleischhacker, W.W., Efficacy of medium-dose clozapine for treatment-resistant schizophrenia (1995) Am J Psychiatry, 152, pp. 1690-1691
dc.descriptionLin, S.K., Chang, W.H., Chung, M.C., Lam, Y.W., Jann, M.W., Disposition of clozapine and desmethylclozapine in schizophrenic patients (1994) J Clin Pharmacol, 34, pp. 318-324
dc.descriptionGuitton, C., Abbar, M., Kinowski, J.M., Chabrand, P., Bressolle, F., Multiple-dose pharmacokinetics of clozapine in patients with chronic schizophrenia (1998) J Clin Psychopharmacol, 18, pp. 470-476
dc.descriptionHaring, C., Barnas, C., Saria, A., Humpel, C., Fleischhacker, W.W., Doserelated plasma levels of clozapine (1989) J Clin Psychopharmacol, 9, pp. 71-72
dc.descriptionHaring, C., Fleischhacker, W.W., Schett, P., Humpel, C., Barnas, C., Saria, A., Influence of patient-related variables on clozapine plasma levels (1990) Am J Psychiatry, 147, pp. 1471-1475
dc.descriptionPerry, P.J., Bever, K.A., Arndt, S., Combs, M.D., Relationship between patient variables and plasma clozapine concentrations: A dosing nomogram (1998) Biol Psychiatry, 44, pp. 733-738
dc.descriptionCheng, Y.F., Lundberg, T., Bondesson, U., Lindstrom, L., Gabrielsson, J., Clinical pharmacokinetics of clozapine in chronic schizophrenic patients (1988) Eur J Clin Pharmacol, 34, pp. 445-449
dc.descriptionChoc, M.G., Hsuan, F., Honigfeld, G., Single-vs multiple-dose pharmacokinetics of clozapine in psychiatric patients (1990) Pharm Res, 7, pp. 347-351
dc.descriptionByerly, M.J., DeVane, C.L., Pharmacokinetics of clozapine and risperidone: A review of recent literature (1996) J Clin Psychopharmacol, 16, pp. 177-187
dc.descriptionFang, J., Coutts, R.T., McKenna, K.F., Baker, G.B., Elucidation of individual cytochrome P450 enzymes involved in the metabolism of clozapine (1998) Naunyn Schmiedebergs Arch Pharmacol, 358, pp. 592-599
dc.descriptionPirmohamed, M., Williams, D., Madden, S., Templeton, E., Park, B.K., Metabolism and bioactivation of clozapine by human liver in vitro (1995) J Pharmacol Exp Ther, 272, pp. 984-990
dc.descriptionDahl, M.L., Llerena, A., Bondesson, U., Lindstrom, L., Bertilsson, L., Disposition of clozapine in man: Lack of association with debrisoquine and S-mephenytoin hydroxylation polymorphisms (1994) Br J Clin Pharmacol, 37, pp. 71-74
dc.descriptionGaray, G.L., Forfar-Bares, I., Pehourcq, F., Jarry, C., Simultaneous determination of four antipsychotic drugs in plasma by highperformance liquid chromatography. Application to management of acute intoxications (2003) J Chromatogr B Analyt Technol Biomed Life Sci, 795, pp. 257-264
dc.descriptionGuitton, C., Kinowski, J.M., Aznar, R., Bressolle, F., Determination of clozapine and its major metabolites in human plasma and red blood cells by high-performance liquid chromatography with ultraviolet absorbance detection (1997) J Chromatogr B Biomed Sci Appl, 690, pp. 211-222
dc.descriptionJaniszewski, J.S., Fouda, H.G., Cole, R.O., Development and validation of a high-sensitivity assay for an antipsychotic agent, CP-88,059, with solid-phase extraction and narrow-bore high-performance liquid chromatography (1995) J Chromatogr B Biomed Appl, 668, pp. 133-139
dc.descriptionLiu, Y.Y., van Troostwijk, L.J., Guchelaar, H.J., Simultaneous determination of clozapine, norclozapine and clozapine-N-oxide in human plasma by high-performance liquid chromatography with ultraviolet detection (2001) Biomed Chromatogr, 15, pp. 280-286
dc.descriptionLlerena, A., Berecz, R., Norberto, M.J., de la Rubia, A., Determination of clozapine and its N-desmethyl metabolite by high-performance liquid chromatography with ultraviolet detection (2001) J Chromatogr B Biomed Sci Appl, 755, pp. 349-354
dc.descriptionMosier, K.E., Song, J., McKay, G., Hubbard, J.W., Fang, J., Determination of clozapine, and its metabolites, N-desmethylclozapine and clozapine N-oxide in dog plasma using high-performance liquid chromatography (2003) J Chromatogr B Analyt Technol Biomed Life Sci, 783, pp. 377-382
dc.descriptionSachse, J., Koller, J., Hartter, S., Hiemke, C., Automated analysis of quetiapine and other antipsychotic drugs in human blood by high performance-liquid chromatography with column-switching and spectrophotometric detection (2006) J Chromatogr B Analyt Technol Biomed Life Sci, 830, pp. 342-348
dc.descriptionWeigmann, H., Bierbrauer, J., Hartter, S., Hiemke, C., Automated determination of clozapine and major metabolites in serum and urine (1997) Ther Drug Monit, 19, pp. 480-488
dc.descriptionWeigmann, H., Hiemke, C., Determination of clozapine and its major metabolites in human serum using automated solid-phase extraction and subsequent isocratic high-performance liquid chromatography with ultraviolet detection (1992) J Chromatogr, 583, pp. 209-216
dc.descriptionRaggi, M.A., Bugamelli, F., Mandrioli, R., Sabbioni, C., Volterra, V., Fanali, S., Rapid capillary electrophoretic method for the determination of clozapine and desmethylclozapine in human plasma (2001) J Chromatogr A, 916, pp. 289-296
dc.descriptionMaresova, V., Chadt, J., Novakova, E., Screening and semiquantitative analysis of drugs and drugs of abuse in human serum samples using gas chromatography-mass spectrometry (2008) Neuro Endocrinol Lett, 29, pp. 749-754
dc.descriptionMaurer, H.H., Advances in analytical toxicology: The current role of liquid chromatography-mass spectrometry in drug quantification in blood and oral fluid (2005) Anal Bioanal Chem, 381, pp. 110-118
dc.descriptionNiessen, W.M., Progress in liquid chromatography-mass spectrometry instrumentation and its impact on high-throughput screening (2003) J Chromatogr A, 1000, pp. 413-436
dc.descriptionAravagiri, M., Marder, S.R., Simultaneous determination of clozapine and its N-desmethyl and N-oxide metabolites in plasma by liquid chromatography/electrospray tandem mass spectrometry and its application to plasma level monitoring in schizophrenic patients (2001) J Pharm Biomed Anal, 26, pp. 301-311
dc.descriptionKirchherr, H., Kuhn-Velten, W.N., Quantitative determination of forty-eight antidepressants and antipsychotics in human serum by HPLC tandem mass spectrometry: A multi-level, single-sample approach (2006) J Chromatogr B Analyt Technol Biomed Life Sci, 843, pp. 100-113
dc.descriptionMing, D.S., Heathcote, J., Therapeutic drug monitoring of clozapine and norclozapine in human serum using ultra-performance liquid chromatography-tandem mass spectrometry (2009) J Anal Toxicol, 33, pp. 198-203
dc.descriptionWang, X.Q., Pan, X.J., Lin, G.Y., Simultaneous determination of clozapine, olanzapine and mirtazapine in human plasma by LCMS/ MS (2009) Fa Yi Xue Za Zhi, 25, pp. 123-126
dc.descriptionZhang, G., Terry Jr., A.V., Bartlett, M.G., Liquid chromatography/ tandem mass spectrometry method for the simultaneous determination of olanzapine, risperidone, 9-hydroxyrisperidone, clozapine, haloperidol and ziprasidone in rat plasma (2007) Rapid Commun Mass Spectrom, 21, pp. 920-928
dc.descriptionZhang, G., Terry Jr., A.V., Bartlett, M.G., Sensitive liquid chromatography/tandem mass spectrometry method for the simultaneous determination of olanzapine, risperidone, 9-hydroxyrisperidone, clozapine, haloperidol and ziprasidone in rat brain tissue (2007) J Chromatogr B Analyt Technol Biomed Life Sci, 858, pp. 276-281
dc.descriptionZhou, Z., Li, X., Li, K., Simultaneous determination of clozapine, olanzapine, risperidone and quetiapine in plasma by highperformance liquid chromatography-electrospray ionization mass spectrometry (2004) J Chromatogr B Analyt Technol Biomed Life Sci, 802, pp. 257-262
dc.descriptionSaint-Marcoux, F., Sauvage, F.L., Marquet, P., Current role of LC-MS in therapeutic drug monitoring (2007) Anal Bioanal Chem, 388, pp. 1327-1349
dc.descriptionMoreno, R.A., Oliveira Costa, I., Brum Junior, L., Cimetidine Quantification in Human Plasma by High-performance Liquid Chromatography Coupled to Electrospray Ionization Tandem Mass Spectrometry. Application to a Comparative Pharmacokinetics Study (2009) J Bioanal & Biomed, 1, p. 9
dc.descriptionChoong, E., Rudaz, S., Kottelat, A., Guillarme, D., Veuthey, J.L., Eap, C.B., Therapeutic drug monitoring of seven psychotropic drugs and four metabolites in human plasma by HPLC-MS (2009) J Pharm Biomed Anal, 50, pp. 1000-1008
dc.descriptionNiederlander, H.A., Koster, E.H., Hilhorst, M.J., High throughput therapeutic drug monitoring of clozapine and metabolites in serum by on-line coupling of solid phase extraction with liquid chromatography-mass spectrometry (2006) J Chromatogr B Analyt Technol Biomed Life Sci, 834, pp. 98-107
dc.descriptionSong, M., Yu, X., Zhao, H., Hang, T., Yang, L., Wei Xu, W., LC-MS-MS Determination and Pharmacokinetic Study of Clozapine in Human Plasma (2009) Chromatographia, 69, pp. 1049-1054
dc.descriptionKollroser, M., Schober, C., Direct-injection high performance liquid chromatography ion trap mass spectrometry for the quantitative determination of olanzapine, clozapine and Ndesmethylclozapine in human plasma (2002) Rapid Commun Mass Spectrom, 16, pp. 1266-1272
dc.descriptionBaldessarini, R.J., Cohen, B.M., Teicher, M.H., Significance of neuroleptic dose and plasma level in the pharmacological treatment of psychoses (1988) Arch Gen Psychiatry, 45, pp. 79-91
dc.descriptionKluznik, J.C., Walbek, N.H., Farnsworth, M.G., Melstrom, K., Clinical effects of a randomized switch of patients from clozaril to generic clozapine (2001) J Clin Psychiatry, 62 (SUPPL. 5), pp. 14-17. , discussion 23-4
dc.descriptionLayton, S., Barbeau, M., Generic replacement of clozapine: A simple decision model from a Canadian perspective (2004) Curr Med Res Opin, 20, pp. 453-459
dc.descriptionMakela, E.H., Cutlip, W.D., Stevenson, J.M., Branded versus generic clozapine for treatment of schizophrenia (2003) Ann Pharmacother, 37, pp. 350-353
dc.descriptionMofsen, R., Balter, J., Case reports of the reemergence of psychotic symptoms after conversion from brand-name clozapine to a generic formulation (2001) Clin Ther, 23, pp. 1720-1731
dc.descriptionNuss, P., Taylor, D., de Hert, M., Hummer, M., The generic alternative in schizophrenia: Opportunity or threat? (2004) CNS Drugs, 18, pp. 769-775
dc.descriptionSajbel, T.A., Carter, G.W., Wiley, R.B., Converting patients from brandname clozapine to generic clozapine (2001) Ann Pharmacother, 35, pp. 281-284
dc.descriptionChoc, M.G., Lehr, R.G., Hsuan, F., Multiple-dose pharmacokinetics of clozapine in patients (1987) Pharm Res, 4, pp. 402-405
dc.descriptionJerling, M., Merle, Y., Mentre, F., Mallet, A., Population pharmacokinetics of clozapine evaluated with the nonparametric maximum likelihood method (1997) Br J Clin Pharmacol, 44, pp. 447-453
dc.descriptionGolden, G., Honigfeld, G., Bioequivalence of clozapine orally disintegrating 100-mg tablets compared with clozapine solid oral 100-mg tablets after multiple doses in patients with schizophrenia (2008) Clin Drug Investig, 28, pp. 231-239
dc.descriptionHaring, C., Meise, U., Humpel, C., Saria, A., Fleischhacker, W.W., Hinterhuber, H., Dose-related plasma levels of clozapine: Influence of smoking behaviour, sex and age (1989) Psychopharmacology (Berl), 99 (SUPPL.), pp. S38-S40
dc.descriptionPokorny, R., Finkel, M.J., Robinson, W.T., Normal volunteers should not be used for bioavailability or bioequivalence studies of clozapine (1994) Pharm Res, 11, p. 1221
dc.descriptionGuidance for Industry (2005) Clozapine Tablets: In Vivo Bioequivalence and In Vitro Dissolution Testing, , FDA
dc.descriptionTassaneeyakul, W., Kittiwattanagul, K., Vannaprasaht, S., Steady-state bioequivalence study of clozapine tablet in schizophrenic patients (2005) J Pharm Pharm Sci, 8, pp. 47-53
dc.descriptionGuitton, C., Kinowski, J.M., Abbar, M., Chabrand, P., Bressolle, F., Clozapine and metabolite concentrations during treatment of patients with chronic schizophrenia (1999) J Clin Pharmacol, 39, pp. 721-728
dc.descriptionOluboka, O., Stewart, S., Landry, S., Adams, S., Does therapeutic equivalence follow bioequivalence? A randomized trial to assess clinical effects after switching from clozaril to generic clozapine (gen-clozapine) (2010) J Clin Pharmacol, 50, pp. 531-535
dc.languageen
dc.publisher
dc.relationCurrent Clinical Pharmacology
dc.rightsfechado
dc.sourceScopus
dc.titleComparative Bioavailability Of Two Oral Formulations Of Clozapine In Steady State Administered In Schizophrenic Volunteers Under Individualized Dose Regime
dc.typeArtículos de revistas


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