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Original Research

The rs662 polymorphism of paraoxonase 1 affects the difference in the inhibition of butyrylcholinesterase activity by organophosphorus pesticides in human blood

Dae Cheol Nam, Yu Mi Ha, Min Kyu Park, and Sung Kweon Cho

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Volume 54 p. 622 - 627

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 54 – No. 8/2016 (622-627)

The rs662 polymorphism of paraoxonase 1 affects the difference in the inhibition of butyrylcholinesterase activity by organophosphorus pesticides in human blood

Dae Cheol Nam¹, Yu Mi Ha², Min Kyu Park², and Sung Kweon Cho³

¹Department of Orthopaedic Surgery, Gyeongsang National University College of Medicine and Gyeongsang National University Hospital, Jinju, ²Department of Clinical Pharmacology, Dong-A University Medical Center; Department of Pharmacology, College of Medicine, Dong-A University, Busan, and ³Armed Forces Medical Research Institute, Daejeon, Republic of Korea
Objectives: Organophosphorus pesticides (OPs) are a human health hazard. OPs inhibit acetylcholinesterase (AChE) at nerve endings and accumulate acetylcholine (ACh) at these sites. High levels of ACh and long exposure promote cholinergic crisis. The hydrolysis of OPs by serum paraoxonase 1 (PON1) plays a role in cholinergic crisis in humans. Human serum PON1 can break down organophosphate before binding to ChE. We investigated the effect of PON1 polymorphisms on AChE activity after OP treatment. Methods: 50 healthy volunteers were randomly recruited with informed consent. We investigated butyrylcholinesterase (BuChE) activity changes in plasma as a biomarker of AChE after OP treatment in human blood samples immediately following blood sampling. After the standardization of BuChE activity in human blood, we correlated changes in BuChE activity with changes in blood pH. We analyzed the PON1 polymorphisms (rs854560 and rs662) of 50 participants to retrospectively investigate the interindividual variability of changes in BuChE activity. Results: Changes in BuChE activity are strongly correlated with pH changes after OP treatment (R² = 0.913). We used changes in pH as a surrogate marker for BuChE inhibition after OP treatment. OP treatment significantly decreased BuChE activity by 56.4 ± 5.1% (p < 0.001). The degree of BuChE inhibition was significantly different in the PON1 rs662 genotype (56.10 ± 4.74% vs. 57.96 ± 5.67% vs. 52.34 ± 1.51%; GG vs. GA vs. AA, respectively). Conclusion: Changes in pH can be used as a surrogate marker for the detection of BuChE inhibition after OP exposure. The rs662 polymorphism of PON1 may explain the inter-individual variability in BuChE inhibition.Correspondence to:
Sung Kweon Cho, MD, PhD
Armed Forces Medical Research Institute
90bun, Jaunro, Yuseong-gu, Daejeon, 305-878, Korea
Email: [email protected]

Bioavailability Section

Pharmacokinetic comparison between tablet of varenicline tartrate and orally disintegrating film of varenicline salicylate in healthy subjects 

Eunwoo Kim, Jun Gi Hwang, Su Jun Park, Ji Young Han, Young-Sim Choi, Se-Rin Park, Kyung-Sang Yu, Min Kyu Park, and SeungHwan Lee

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Volume 59 (2021) p. 478 - 484

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 59 – No. 6/2021 (478-484)

Pharmacokinetic comparison between tablet of varenicline tartrate and orally disintegrating film of varenicline salicylate in healthy subjects 

Eunwoo Kim¹, Jun Gi Hwang¹#², Su Jun Park³, Ji Young Han³, Young-Sim Choi², Se-Rin Park², Kyung-Sang Yu¹, Min Kyu Park², and SeungHwan Lee¹#⁴

¹Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, ²Department of Clinical Pharmacology and Therapeutics, Chungbuk National University Hospital, Cheongju-si, Chungcheongbuk-do, ³CTCBIO Inc., Ansan-si, Gyeonggi-do, and ⁴Clinical Trials Center, Seoul National University Hospital, Seoul, Republic of Korea
Objective: Varenicline is an efficacious aid for smoking cessation. In this study, the pharmacokinetics and safety were compared between film-coated tablets of varenicline tartrate (reference drug) and the newly developed orally disintegrating films of varenicline salicylate (test drug), both of them contained 1 mg of varenicline.
Materials and methods: A randomized, open-label, single-dose, two-sequence, two-period crossover study was conducted in healthy male subjects. Serial blood samples were obtained for up to 72 hours in each period, with a washout period of 7 days or more. The pharmacokinetic parameters were calculated using the noncompartmental method. Safety profiles were assessed throughout the study.
Results: A total of 28 subjects completed the study. The plasma varenicline concentration-time profiles were similar for the two study drugs. The maximum plasma varenicline concentration (C_max) was 5,768.95 ng/L (mean) and 5,780.55 ng/L for the test drug and reference drug, respectively. The areas under the concentration-time curve from time 0 to the last measurable time point (AUC_0–t) were 94,086.30 h×ng/L and 89,958.55 h×ng/L for the test drug and reference drug, respectively. The geometric mean ratios (90% confidence intervals) of the test drug to the reference drug for C_max and AUC_0–t were 0.9955 (0.9488 – 1.0444) and 1.0449 (0.9848 – 1.1088), respectively, which fell within the bioequivalence range of 0.8 – 1.25. There was no difference in safety between the study drugs.
Conclusion: The pharmacokinetics and safety profiles were similar between the two study drugs. The orally disintegrating film of varenicline salicylate can be an alternative to varenicline tartrate tablets.Correspondence to:
SeungHwan Lee,  MD, PhD
Department of Clinical Pharmacology and Therapeutics
Seoul National University College of Medicine and Hospital
101 Daehak-ro, Jongno-gu,
Seoul 03080,  Republic of Korea
Email: [email protected]

Original

Comparison of the acid suppression effects between low-dose esomeprazole and famotidine in healthy subjects 

Ha-Yeon Kim, Jun Gi Hwang, Jae-Won Kim, Chang Hwan Seong, Ji Hyeon Lee, Young-sim Choi, Hyo Jin Min, Hyung Son Kim, Hye Yun Kim, Yu Kyong Kim, and Min Kyu Park

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Volume 61 (2023) p. 377 - 385

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 61 – No. 9/2023 (377-385)

Comparison of the acid suppression effects between low-dose esomeprazole and famotidine in healthy subjects 

Ha-Yeon Kim¹*, Jun Gi Hwang¹*, Jae-Won Kim¹, Chang Hwan Seong¹, Ji Hyeon Lee¹, Young-sim Choi¹, Hyo Jin Min¹, Hyung Son Kim²#³, Hye Yun Kim², Yu Kyong Kim¹, and Min Kyu Park¹

¹Department of Clinical Pharmacology and Therapeutics, Chung-buk National University Hospital, Cheong-ju, ²Daewon Pharmaceutical Co., Ltd., Seoul, and ³Kyung Hee University, Seoul, Republic of Korea
Objective: Famotidine, an H₂ receptor antagonist (H₂RA), is mainly prescribed to alleviate the early symptoms of gastritis. Our aim was to explore the possibilities of low-dose esomeprazole as a treatment of gastritis as well as the pharmacodynamic (PD) properties of esomeprazole and famotidine.
Materials and methods: A randomized, multiple-dose, 6-sequence, 3-period crossover study was conducted with a 7-day washout between periods. For each period, the subjects were administered one dose of esomeprazole 10 mg or famotidine 20 mg or esomeprazole 20 mg each day. To evaluate the PDs, the 24-hour gastric pH was recorded after single and multiple doses. The mean percentage of time during which the gastric pH was above 4 was evaluated for PD assessment. To confirm the pharmacokinetic (PK) characteristics of esomeprazole, blood was collected for up to 24 hours after multiple doses.
Results: 26 subjects completed the study. Following the multiple doses of esomeprazole 10 mg, esomeprazole 20 mg, and famotidine 20 mg, the mean percentages of time during which the gastric pH was above 4 over the course of 24 hour were 35.77 ± 19.56%, 53.75 ± 20.55%, and 24.48 ± 17.36%, respectively. After multiple doses, the time of peak plasma concentration at steady state (t_max,ss) was 1.00 and 1.25 hours for 10 and 20 mg of esomeprazole, respectively. The geometric mean ratio and its 90% confidence interval of area under the plasma drug concentration-time curve in steady state (AUC_T,ss) and maximum concentration of drug in plasma in steady state (C_max,ss) for esomeprazole 10 mg compared to 20 mg were 0.3654 (0.3381 – 0.3948) and 0.5066 (0.4601 – 0.5579), respectively.
Conclusion: The PD parameters of esomeprazole 10 mg were comparable to those of famotidine after multiple doses. These findings provide support for further evaluating the use of 10 mg of esomeprazole as a treatment option for gastritis.

*H.Y. Kim and J.G. Hwang contributed equally to this manuscriptCorrespondence to:
Min Kyu Park, MD, PhD
Department of Clinical Pharmacology and Therapeutics
Chung-buk National University Hospital
776, 1sunhwan-ro, Seowon-gu,
Cheongju-si, Chungcheongbuk-do, 28644
Republic of Korea
Email: [email protected]

Original

Pharmacokinetic evaluation of two oral formulations of chlorpromazine in healthy subjects 

Hyo-Jin Min, Jun Gi Hwang, Young-Sim Choi, and Min Kyu Park

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p. 0 - 6

Abstract

Hyo-Jin Min¹, Jun Gi Hwang²,³, Young-Sim Choi¹, and Min Kyu Park²,³

¹Cheongju Osong National Advanced Clinical Trial Center, ChungBuk National University Hospital, ²Department of Clinical Pharmacology, ChungBuk National University College of Medicine, and ³Department of Clinical Pharmacology and Therapeutics, ChungBuk National University Hospital, Cheongju-si, Republic of Korea
Chlorpromazine is a first-generation antipsychotic agent that exerts its therapeutic effects primarily by antagonizing dopamine D2 receptors. This randomized, open-label, single-dose, two-period, two-sequence crossover study was conducted to evaluate the pharmacokinetic bioequivalence of two oral formulations of chlorpromazine 100 mg: Neomazine tablets (Whan In Pharmaceutical Co., Ltd.) and Chlorpromazine HCl tablets (Myung In Pharmaceutical Co., Ltd.). A total of 70 subjects were randomized, and 61 completed both treatment periods. Blood samples were collected at predefined intervals up to 72 hours post dose to assess pharmacokinetic parameters, including maximum plasma concentration (Cmax) and the area under the plasma concentration–time curve to the last measurable concentration (AUClast). Safety was assessed through monitoring of adverse events (AEs), clinical laboratory tests, vital signs, physical examinations, and 12-lead electrocardiograms. The geometric mean ratios (90% confidence intervals) for Cmax and AUClast were 1.0490 (0.9534 – 1.1542) and 0.9941 (0.9261 – 1.0671), respectively, falling within the accepted bioequivalence range of 0.80 – 1.25. Among the 70 subjects who received at least 1 dose, 116 AEs were reported in 48 individuals; all were mild in intensity and resolved without sequelae, and no serious AEs occurred. These findings confirm the pharmacokinetic bioequivalence and favorable tolerability of the two formulations under fasting conditions in healthy adults and support the use of Neomazine as a therapeutically equivalent and clinically interchangeable alternative to Chlorpromazine HCl. Correspondence to:
Min Kyu Park, MD, PhD, Department of Clinical Pharmacology and Therapeutics, ChungBuk National University Hospital, Cheongju-si, Republic of Korea
Email: [email protected]

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