Pharmacokinetics and Tolerability of Intramuscular, Oral and Intravenous Aripiprazole??in Healthy Subjects and in??Patients??with Schizophrenia

Boulton, David W.; Kollia, Georgia; Mallikaarjun, Suresh; Komoroski, Bernard J.; Sharma, Anjali; Kovalick, Lawrence J.; Reeves, Richard

doi:10.2165/00003088-200847070-00004

Cited by 29 publications

(25 citation statements)

References 18 publications

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“…Consequently, the times of sample collection were not optimal for a reliable calculation of pharmacokinetic parameters. The plasma concentrations observed in this study appeared to be consistent with published data for all evaluated drugs 25, 26, 27, 28, 29…”

Section: Discussionsupporting

confidence: 91%

Comparison of Capillary and Venous Drug Concentrations After Administration of a Single Dose of Risperidone, Paliperidone, Quetiapine, Olanzapine, or Aripiprazole

Remmerie

Meulder

Weiner

et al. 2016

Clinical Pharm in Drug Dev

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Risperidone, paliperidone, quetiapine, olanzapine, and aripiprazole are antipsychotic drugs approved for treating various psychiatric disorders, including schizophrenia. The objective of this randomized, parallel‐group, open‐label study was to compare finger‐stick‐based capillary with corresponding venous whole‐blood and plasma concentrations for these drugs after administration of a single dose to healthy volunteers. All whole‐blood and plasma drug concentrations were measured with validated liquid chromatography–tandem mass spectrometry methods. Capillary and venous concentrations (both in plasma and whole blood) were in close agreement, although a time‐dependent difference was observed, most obviously for olanzapine and paliperidone, with slightly higher capillary versus venous drug concentrations during the first hours after administering a single dose. The observed difference between capillary and venous plasma drug concentrations is expected not to be relevant in clinical practice, considering the wide window of therapeutic concentrations and the wide range of drug concentrations in the patient population for a given dose. Based on these results, finger‐stick‐based capillary drug concentrations have been shown to approximate venous drug concentrations.

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Section: Discussionsupporting

confidence: 91%

Comparison of Capillary and Venous Drug Concentrations After Administration of a Single Dose of Risperidone, Paliperidone, Quetiapine, Olanzapine, or Aripiprazole

Remmerie

Meulder

Weiner

et al. 2016

Clinical Pharm in Drug Dev

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“…Research suggests that second‐generation IM antipsychotics are effective and safe in various age ranges and populations diagnosed with various psychoses; they are typically able to reduce agitation within 2 hours and reduce psychotic symptoms within 24 hours …”

Section: Sociodemographic Variablesmentioning

confidence: 99%

Intramuscular Aripiprazole in the Acute Management of Psychomotor Agitation

et al. 2013

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“…The bioavailability of the psychopharmacons was predicted from in vitro pharmacokinetic parameters obtained in human hepatocytes, and the predicted values were compared with in vivo oral bioavailability determined in clinical studies (Table 4) [26][27][28][29][30][31][32].…”

Section: Prediction Of Human Clearance and Bioavailability Of Psychopmentioning

confidence: 99%

Utility of in vitro clearance in primary hepatocyte model for prediction of in vivo hepatic clearance of psychopharmacons

Tóth

Sirok

Kiss

et al. 2018

Microchemical Journal

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Katalin Tóth and Dávid Sirok equally contributed to this work. Highlights• Primary hepatocytes offer a simple in vitro model for pharmacokinetic studies.• The utility of hepatocytes for prediction of in vivo clearance of drugs or novel chemical entities may have some limitations.• In vitro pharmacokinetic behaviour of psychopharmacons in rat hepatocytes correlated with in vitro human pharmacokinetics.• Neither the elimination rates nor the intrinsic clearance in dog or rabbit cells resembled those parameters in human cells.• For prediction of in vivo hepatic clearance, rat hepatocyte model appeared to be the most relevant to human.• Human bioavailability values predicted from in vitro clearance were in good agreement with clinical bioavailability data. 3In conclusion, the predicted bioavailability obtained from human hepatocytes showed an excellent rank order with in vivo findings. Furthermore, rat was considered to be the most relevant animal model to human subjects.

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Pharmacokinetics and Tolerability of Intramuscular, Oral and Intravenous Aripiprazole??in Healthy Subjects and in??Patients??with Schizophrenia

Abstract: More rapid absorption was observed following intramuscular aripiprazole injection than following oral dosing. These results support the recently reported efficacy of intramuscular aripiprazole for managing agitation in patients with schizophrenia or bipolar I disorder.

Cited by 29 publications

References 18 publications

Comparison of Capillary and Venous Drug Concentrations After Administration of a Single Dose of Risperidone, Paliperidone, Quetiapine, Olanzapine, or Aripiprazole

Comparison of Capillary and Venous Drug Concentrations After Administration of a Single Dose of Risperidone, Paliperidone, Quetiapine, Olanzapine, or Aripiprazole

Intramuscular Aripiprazole in the Acute Management of Psychomotor Agitation

Utility of in vitro clearance in primary hepatocyte model for prediction of in vivo hepatic clearance of psychopharmacons

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