Application of physiologically‐based pharmacokinetic model approach to predict pharmacokinetics and <scp>drug–drug</scp> interaction of rivaroxaban: A case study of rivaroxaban and carbamazepine

Ngo, Lien Thi; Yang, Sung-Yoon; Shin, Sug Kyun; Tuan, Cao Duc; Hung, Nguyen Van; Jung, Sangkeun; Lee, Jae-Young; Lee, Jong-Hwa; Yun, Hwi-yeol; Chae, Jung-Woo

doi:10.1002/psp4.12844

Cited by 5 publications

(8 citation statements)

References 38 publications

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“…In a previous study, our team developed a PBPK model for RIV in humans. In that model, the metabolic degradation by CYP3A4, CYP2J2, and non-CYP enzymes, and the active transportation by Pgp/BCRP, were implemented [ 17 ]. To perform the simulation for the DDI profile of RIV and CBZ, the PBPK model for RIV was paired with a previously developed PBPK model for CBZ extracted from the OSP Library [ 26 , 27 ].…”

Section: Resultsmentioning

confidence: 99%

“…DDI profiles of RIV and CBZ predicted from the PopPK model were then compared with those observed from the PBPK model-based approach [ 17 ]. The comparison showed agreement in predicting CBZ effects on the PK of RIV.…”

Section: Discussionmentioning

confidence: 99%

“… Data are presented as mean (5th percentile–95th percentile), except t 1/2 . ¥ Results from the PBPK model-based approach were extracted from our previous study [ 17 ]. The subscriptions “first” and “SS” stand for “first dose” and “steady state”, respectively; AUC , area under the concentration–time curve calculated during one dosing interval; C max , maximum concentration; t 1 / 2 , elimination half-life.…”

Section: Figurementioning

confidence: 99%

“…Our group recently developed and published a PBPK model for RIV [ 17 ]. In that study, DDI profiles between RIV and carbamazepine (CBZ), one of the recommended first-line options for the treatment of seizures and epilepsy, were simulated in humans.…”

Section: Introductionmentioning

confidence: 99%

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Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans

2023

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Rivaroxaban (RIV) is one of the direct oral anticoagulants used to prevent and treat venous and arterial thromboembolic events. Considering the therapeutic indications, RIV is likely to be concomitantly administered with various other drugs. Among these is carbamazepine (CBZ), one of the recommended first-line options to control seizures and epilepsy. RIV is a strong substrate of cytochrome P450 (CYP) enzymes and Pgp/BCRP efflux transporters. Meanwhile, CBZ is well known as a strong inducer of these enzymes and transporters. Therefore, drug–drug interaction (DDI) between CBZ and RIV is expected. This study aimed to predict the DDI profile of CBZ and RIV in humans by using a population pharmacokinetics (PK) model-based approach. We previously investigated the population PK parameters of RIV administered alone or with CBZ in rats. In this study, those parameters were extrapolated from rats to humans by using simple allometry and liver blood flow scaling, and then applied to back-simulate the PK profiles of RIV in humans (20 mg RIV per day) used alone or with CBZ (900 mg CBZ per day). Results showed that CBZ significantly reduced RIV exposure. The AUCinf and Cmax of RIV decreased by 52.3% and 41.0%, respectively, following the first RIV dose, and by 68.5% and 49.8% at the steady state. Therefore, the co-administration of CBZ and RIV warrants caution. Further studies investigating the extent of DDIs between these drugs should be conducted in humans to fully understand their safety and effects.

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Section: Resultsmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans

2023

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“…The extent of CBZ autoinduction is slightly dose sensitive but is typically resolved after 3-5 weeks of medication (Gaies et al, 2021). Only 1% of CBZ is removed through biliary excretion, thus the kidneys are responsible for the majority of excretion (Ngo et al, 2022;Methaneethorn et al, 2020).…”

Section: Pharmacokinetics: Metabolism Of Cbz In Bd Patientsmentioning

confidence: 99%

Carbamazepine and Bipolar Disorder: Pharmacodynamics, Pharmacokinetics, Pharmacogenomics, and Adverse Drug Reactions- A Comprehensive Review

P.,

Banerjee,

Bansal

et al. 2023

Asian J Pharm Pharmacol

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Bipolar disorder is a chronic recurring illness marked by swings in mood and energy. Regardless of nationality, ethnic background, or socioeconomic status, it affects more than 1% of the world's population1. It is marked by recurring episodes of mania and depression in bipolar disorder (Carvalho et al., 2020) and of hypomania and depression in bipolar disorder (Harrison et al., 2018). Patients with bipolar disorder usually have additional medical conditions in addition to their serious mental disorders (Zareifopoulos et al., 2018). There is evidence of a neurotransmission imbalance, polygenic inheritance, and illness progression in these individuals. Patients frequently take many medications at once, with varying degrees of therapeutic efficacy, especially in the case of depression. Numerous people commit suicide (Dome et al., 2019). In comparison to the general population, the suicide rate is 5-17 times greater, with a lifetime risk of 10%-20% (Miller and Black, 2020).Anticonvulsant medications are frequently prescribed for these psychiatric purposes. Although various additional anticonvulsant medications have been tested with conflicting or inconclusive results, carbamazepine, valproate, and lamotrigine are known mood stabilizers for bipolar disorder (Simonetti et al., 2020). Carbamazepine (CBZ) is a crucial second-line treatment for bipolar disorder when treatment with a conventional antipsychotic alone fails. CBZ otherwise is typically used in the treatment of seizure disorders and neuropathic pain (Sparacino et al., 2022). CBZ is structurally similar to tricyclic antidepressant imipramine. In 2002, the FDA gave CBZ the drug approved for the treatment of acute mania (Sparacino et al., 2022). Hence this review in detail discusses carbamazepine for the treatment of bipolar disorder, its underlying mechanism, and adverse effects.

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Application of physiologically‐based pharmacokinetic model approach to predict pharmacokinetics and drug–drug interaction of rivaroxaban: A case study of rivaroxaban and carbamazepine

Ngo

Yang

Shin

et al. 2022

CPT Pharmacom & Syst Pharma

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Application of physiologically‐based pharmacokinetic model approach to predict pharmacokinetics and drug–drug interaction of rivaroxaban: A case study of rivaroxaban and carbamazepine

Abstract: Jong-Hwa Lee, Hwi-yeol Yun and Jung-woo Chae contributed equally to this work as the corresponding authors.

Cited by 5 publications

References 38 publications

Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans

Application of the Population Pharmacokinetics Model-Based Approach to the Prediction of Drug–Drug Interaction between Rivaroxaban and Carbamazepine in Humans

Carbamazepine and Bipolar Disorder: Pharmacodynamics, Pharmacokinetics, Pharmacogenomics, and Adverse Drug Reactions- A Comprehensive Review

Application of physiologically‐based pharmacokinetic model approach to predict pharmacokinetics and drug–drug interaction of rivaroxaban: A case study of rivaroxaban and carbamazepine

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