Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach

Clozapine is the first-line medication for treatment-resistant schizophrenia. However, it has complex metabolism, an unclear exposure-response relationship, and potential adverse drug reactions (ADRs). The present study aimed to develop an analytical method and pharmacometrics-based models for cloza...

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Main Author: Orwa, Albitar
Format: Thesis
Language:English
Published: 2022
Subjects:
Online Access:http://eprints.usm.my/59662/
http://eprints.usm.my/59662/1/24%20Pages%20from%20ALBITAR%20ORWA%20-%20TESIS.pdf
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author Orwa, Albitar
author_facet Orwa, Albitar
author_sort Orwa, Albitar
building USM Institutional Repository
collection Online Access
description Clozapine is the first-line medication for treatment-resistant schizophrenia. However, it has complex metabolism, an unclear exposure-response relationship, and potential adverse drug reactions (ADRs). The present study aimed to develop an analytical method and pharmacometrics-based models for clozapine and norclozapine pharmacokinetics and pharmacodynamics in healthy volunteers and schizophrenia spectrum disorder (SSD) patients. A surfactant-assisted dispersive liquid-liquid microextraction coupled with HPLC-UV was used for clozapine and norclozapine determination after optimizing experimental factors. 270 data points obtained from 33 healthy volunteers after receiving a single dose of 12.5 mg clozapine were utilized in the semi-physiological pharmacokinetic model development incorporating the pre-systemic clozapine metabolism. To assess clozapine interaction with pantoprazole, a randomized, crossover, open-label study design was implemented. 12 volunteers were given clozapine alone; then clozapine after five days of 40 mg pantoprazole or vice versa, separated by a washout period. Meanwhile, clinical data were extracted from 116 SSD patients’ medical records in Penang General Hospital, with a mean retrospective follow-up of 306 weeks.
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spelling usm-596622023-12-13T01:21:21Z http://eprints.usm.my/59662/ Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach Orwa, Albitar RS1-441 Pharmacy and materia medica Clozapine is the first-line medication for treatment-resistant schizophrenia. However, it has complex metabolism, an unclear exposure-response relationship, and potential adverse drug reactions (ADRs). The present study aimed to develop an analytical method and pharmacometrics-based models for clozapine and norclozapine pharmacokinetics and pharmacodynamics in healthy volunteers and schizophrenia spectrum disorder (SSD) patients. A surfactant-assisted dispersive liquid-liquid microextraction coupled with HPLC-UV was used for clozapine and norclozapine determination after optimizing experimental factors. 270 data points obtained from 33 healthy volunteers after receiving a single dose of 12.5 mg clozapine were utilized in the semi-physiological pharmacokinetic model development incorporating the pre-systemic clozapine metabolism. To assess clozapine interaction with pantoprazole, a randomized, crossover, open-label study design was implemented. 12 volunteers were given clozapine alone; then clozapine after five days of 40 mg pantoprazole or vice versa, separated by a washout period. Meanwhile, clinical data were extracted from 116 SSD patients’ medical records in Penang General Hospital, with a mean retrospective follow-up of 306 weeks. 2022-09 Thesis NonPeerReviewed application/pdf en http://eprints.usm.my/59662/1/24%20Pages%20from%20ALBITAR%20ORWA%20-%20TESIS.pdf Orwa, Albitar (2022) Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach. PhD thesis, Perpustakaan Hamzah Sendut.
spellingShingle RS1-441 Pharmacy and materia medica
Orwa, Albitar
Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title_full Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title_fullStr Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title_full_unstemmed Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title_short Pharmacokinetics And Pharmacodynamics Modeling Of Clozapine In Healthy Volunteers And Patients With Schizophrenia Spectrum Disorders Using Pharmacometrics Approach
title_sort pharmacokinetics and pharmacodynamics modeling of clozapine in healthy volunteers and patients with schizophrenia spectrum disorders using pharmacometrics approach
topic RS1-441 Pharmacy and materia medica
url http://eprints.usm.my/59662/
http://eprints.usm.my/59662/1/24%20Pages%20from%20ALBITAR%20ORWA%20-%20TESIS.pdf