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Drug Evaluations

Asenapine review, part I: chemistry, receptor affinity profile, pharmacokinetics and metabolism

, MD MPH (Clinical Professor of Psychiatry & Behavioral Sciences)

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Vishwa Kotak, Nisha Tanna, Mrunali Patel & Rashmin Patel. (2022) Determination of Asenapine Maleate in Pharmaceutical and Biological Matrices: A Critical Review of Analytical Techniques over the Past Decade. Critical Reviews in Analytical Chemistry 52:8, pages 1755-1771.
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Sharon Taub, Amir Krivoy, Eromona Whiskey & Sukhi S. Shergill. (2022) New approaches to antipsychotic medication adherence – safety, tolerability and acceptability. Expert Opinion on Drug Safety 21:4, pages 517-524.
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Haruna Matsuzaki, Masakazu Hatano, Miko Iwata & Shigeki Yamada. (2021) Treatment Continuation of Asenapine or Olanzapine in Japanese Schizophrenia Patients: A Propensity Score Matched Study. Neuropsychiatric Disease and Treatment 17, pages 3655-3661.
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Brennan Carrithers & Rif S El-Mallakh. (2020) Transdermal Asenapine in Schizophrenia: A Systematic Review. Patient Preference and Adherence 14, pages 1541-1551.
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Akhil Suresh, Reema Narayan & Usha Y Nayak. (2020) Recent advances in the development of asenapine formulations. Expert Opinion on Drug Delivery 17:10, pages 1377-1393.
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Donatella Marazziti, Federico Mucci, Valentina Falaschi & Liliana Dell’Osso. (2019) Asenapine for the treatment of bipolar disorder. Expert Opinion on Pharmacotherapy 20:11, pages 1321-1330.
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Peter Dogterom, Robert Riesenberg, Rik de Greef, Justin Dennie, Martin Johnson, Venkatesh Pilla Reddy, André MM Miltenburg, Robert L Findling, Abhijeet Jakate, Timothy J Carrothers & Matthew D Troyer. (2018) Asenapine pharmacokinetics and tolerability in a pediatric population. Drug Design, Development and Therapy 12, pages 2677-2693.
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Gina Stassinos & Wendy Klein-Schwartz. (2018) Asenapine, iloperidone and lurasidone exposures in young children reported to U.S. poison centers. Clinical Toxicology 56:5, pages 355-359.
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Leslie Citrome, Ronald Landbloom, Cheng-Tao Chang & Willie Earley. (2017) Effects of asenapine on agitation and hostility in adults with acute manic or mixed episodes associated with bipolar I disorder. Neuropsychiatric Disease and Treatment 13, pages 2955-2963.
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Juilee A. Kulkarni & Amelia M. Avachat. (2017) Pharmacodynamic and pharmacokinetic investigation of cyclodextrin-mediated asenapine maleate in situ nasal gel for improved bioavailability. Drug Development and Industrial Pharmacy 43:2, pages 234-245.
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Leslie Citrome. (2014) Asenapine review, part II: clinical efficacy, safety and tolerability. Expert Opinion on Drug Safety 13:6, pages 803-830.
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Articles from other publishers (35)

Shuhei Wada, Kunihiro Iwamoto, Hiroki Okumura, Hirotake Hida, Shuichi Hiraoka, Aya Kamei, Daisuke Mori, Kiyofumi Yamada & Norio Ozaki. (2023) Sensory evaluation of the bitterness of asenapine using D-sorbitol pretreatment: single-blind, placebo-controlled, crossover trial. BMC Psychiatry 23:1.
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George T. Kannarkat, Stanley N. Caroff & James F. Morley. (2022) Risk of Drug-induced Movement Disorders with Newer Antipsychotic Agents. Tremor and Other Hyperkinetic Movements 12:1.
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Frank M. Schmidt. 2020. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1 8 .
Peter Schönknecht. 2020. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1 10 .
Frank M. Schmidt. 2022. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1575 1582 .
Hubertus Himmerich & Amy Hamilton. 2022. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1447 1467 .
Peter Schönknecht. 2022. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1871 1879 .
Przemysław J. Danek & Władysława A. Daniel. (2021) Long-Term Treatment with Atypical Antipsychotic Iloperidone Modulates Cytochrome P450 2D (CYP2D) Expression and Activity in the Liver and Brain via Different Mechanisms. Cells 10:12, pages 3472.
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Przemysław J. Danek, Ewa Bromek, Anna Haduch & Władysława A. Daniel. (2021) Chronic treatment with asenapine affects cytochrome P450 2D (CYP2D) in rat brain and liver. Pharmacological aspects. Neurochemistry International 151, pages 105209.
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Mehak Pahwa, Ahmad Sleem, Omar H. Elsayed, Megan Elizabeth Good & Rif S. El-Mallakh. (2021) New Antipsychotic Medications in the Last Decade. Current Psychiatry Reports 23:12.
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Jonathan M. Meyer & Stephen M. Stahl. 2021. The Clinical Use of Antipsychotic Plasma Levels. The Clinical Use of Antipsychotic Plasma Levels 337 371 .
Ann Kathleen Sheehan, Christopher Richards-Bentley, Raed J. Hawa & Joseph J. Rasimas. (2021) Case report: asenapine and anticholinergic toxicity. International Clinical Psychopharmacology 36:4, pages 214-217.
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Meghan Musselman, Justin Faden & Leslie Citrome. (2021) Asenapine: an atypical antipsychotic with atypical formulations. Therapeutic Advances in Psychopharmacology 11, pages 204512532110352.
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Przemysław J. Danek, Jacek Wójcikowski & Władysława A. Daniel. (2020) Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy. Toxicology and Applied Pharmacology 406, pages 115239.
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Jyothsna Manikkath, Harendra S. Parekh & Srinivas Mutalik. (2020) Surface-engineered nanoliposomes with lipidated and non-lipidated peptide-dendrimeric scaffold for efficient transdermal delivery of a therapeutic agent: Development, characterization, toxicological and preclinical performance analyses. European Journal of Pharmaceutics and Biopharmaceutics 156, pages 97-113.
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Felice Iasevoli, Elisabetta Filomena Buonaguro, Camilla Avagliano, Annarita Barone, Anna Eramo, Licia Vellucci & Andrea de Bartolomeis. (2020) The Effects of Antipsychotics on the Synaptic Plasticity Gene Homer1a Depend on a Combination of Their Receptor Profile, Dose, Duration of Treatment, and Brain Regions Targeted. International Journal of Molecular Sciences 21:15, pages 5555.
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Santosh Ashok Kumbhar, Chandrakant R. Kokare, Birendra Shrivastava, Bapi Gorain & Hira Choudhury. (2020) Preparation, characterization, and optimization of asenapine maleate mucoadhesive nanoemulsion using Box-Behnken design: In vitro and in vivo studies for brain targeting. International Journal of Pharmaceutics 586, pages 119499.
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Jacek Wójcikowski, Przemysław J. Danek, Agnieszka Basińska-Ziobroń, Renata Pukło & Władysława A. Daniel. (2020) In vitro inhibition of human cytochrome P450 enzymes by the novel atypical antipsychotic drug asenapine: a prediction of possible drug–drug interactions. Pharmacological Reports 72:3, pages 612-621.
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Renuka S. Managuli, Julie Tzu-Wen Wang, Farid Muhammad Faruqu, Abhjieet Pandey, Sanyog Jain, Khuloud T. Al-Jamal & Srinivas Mutalik. (2020) Surface engineered nanoliposomal platform for selective lymphatic uptake of asenapine maleate: In vitro and in vivo studies. Materials Science and Engineering: C 109, pages 110620.
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Nicolo Milani, NaHong Qiu, Birgit Molitor, Justine Badée, Gabriele Cruciani & Stephen Fowler. (2020) Use of Phenotypically Poor Metabolizer Individual Donor Human Liver Microsomes To Identify Selective Substrates of UGT2B10. Drug Metabolism and Disposition 48:3, pages 176-186.
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P. Danek & W.A. Daniel. (2020) P.103 The effect of chronic treatment with the asenapine on the cytochrome P450 2D (CYP2D) activity in different brain areas. European Neuropsychopharmacology 31, pages S2-S3.
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Hubertus Himmerich & Amy Hamilton. 2020. NeuroPsychopharmacotherapy. NeuroPsychopharmacotherapy 1 21 .
Leslie Citrome & Jan Volavka. 2020. Violence and Mental Disorders. Violence and Mental Disorders 253 268 .
Jyothsna Manikkath, Gautham G. Shenoy, Sureshwar Pandey & Srinivas Mutalik. (2019) Response Surface Methodology for Optimization of Ultrasound-Assisted Transdermal Delivery and Skin Retention of Asenapine Maleate. Journal of Pharmaceutical Innovation 14:4, pages 391-399.
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Kohei Takahashi, Osamu Nakagawasai, Wakana Sakuma, Wataru Nemoto, Takayo Odaira, Jia-Rong Lin, Hiroshi Onogi, Lalit K. Srivastava & Koichi Tan-No. (2019) Prenatal treatment with methylazoxymethanol acetate as a neurodevelopmental disruption model of schizophrenia in mice. Neuropharmacology 150, pages 1-14.
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Massimo Carlo Mauri, Silvia Paletta, Chiara Di Pace, Alessandra Reggiori, Giovanna Cirnigliaro, Isabel Valli & Alfredo Carlo Altamura. (2018) Clinical Pharmacokinetics of Atypical Antipsychotics: An Update. Clinical Pharmacokinetics 57:12, pages 1493-1528.
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Ekaterina Stepanova, Bradley Grant & Robert L. Findling. (2017) Asenapine Treatment in Pediatric Patients with Bipolar I Disorder or Schizophrenia: A Review. Pediatric Drugs 20:2, pages 121-134.
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Sanjay Kumar Singh, Mahendra Kumar Hidau, Shrikant Gautam, Kiran Gupta, Krishna Pal Singh, Shio Kumar Singh & Sanjay Singh. (2018) Glycol chitosan functionalized asenapine nanostructured lipid carriers for targeted brain delivery: Pharmacokinetic and teratogenic assessment. International Journal of Biological Macromolecules 108, pages 1092-1100.
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Eduard Vieta & José Manuel Montes. (2017) A Review of Asenapine in the Treatment of Bipolar Disorder. Clinical Drug Investigation 38:2, pages 87-99.
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Peter SturmeyLeslie Citrome & Jan Volavka. 2017. The Wiley Handbook of Violence and Aggression. The Wiley Handbook of Violence and Aggression 1 15 .
Leslie Citrome. 2017. The Diagnosis and Management of Agitation. The Diagnosis and Management of Agitation 200 218 .
Greg L. Plosker & Emma D. Deeks. (2016) Asenapine: A Review in Schizophrenia. CNS Drugs 30:7, pages 655-666.
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Toshihiko Kinoshita, Ya-Mei Bai, Jong-Hoon Kim, Mutsuo Miyake & Nobuyuki Oshima. (2016) Efficacy and safety of asenapine in Asian patients with an acute exacerbation of schizophrenia: a multicentre, randomized, double-blind, 6-week, placebo-controlled study. Psychopharmacology 233:14, pages 2663-2674.
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Leslie Citrome & Jan Volavka. (2015) Preventing Violence in Patients with Schizophrenia. Current Treatment Options in Psychiatry 2:2, pages 182-191.
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Xinhui Lim, Prashant Tibrewal, Rohan Dhillon, Tarun Bastiampillai, Linda Chen & Andrew Lin. (2015) Can asenapine cause myocarditis?. Asian Journal of Psychiatry 14, pages 78-79.
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