Pharmacokinetics of Terazosin Enantiomers in Healthy Chinese Male Subjects
ABSTRACT The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma...
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Published in | Chirality (New York, N.Y.) Vol. 24; no. 12; pp. 1047 - 1050 |
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Main Authors | , , , , , , , |
Format | Journal Article |
Language | English |
Published |
United States
Blackwell Publishing Ltd
01.12.2012
Wiley Subscription Services, Inc |
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Online Access | Get full text |
ISSN | 0899-0042 1520-636X 1520-636X |
DOI | 10.1002/chir.22095 |
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Abstract | ABSTRACT
The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)‐(R)‐terazosin at all time points were higher than those of (−)‐(S)‐terazosin. The area under the plasma concentration–time curve (AUC0–∞) and maximum plasma concentration of (+)‐(R)‐terazosin were significantly greater than those of the (−)‐(S)‐terazosin (P < 0.01, respectively). The R/S ratio of AUC0–∞ of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047–1050, 2012. © 2012 Wiley Periodicals, Inc. |
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AbstractList | The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)‐( R )‐terazosin at all time points were higher than those of (−)‐( S )‐terazosin. The area under the plasma concentration–time curve (AUC 0–∞ ) and maximum plasma concentration of (+)‐( R )‐terazosin were significantly greater than those of the (−)‐( S )‐terazosin ( P < 0.01, respectively). The R / S ratio of AUC 0–∞ of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047–1050, 2012 . © 2012 Wiley Periodicals, Inc. ABSTRACT The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)‐(R)‐terazosin at all time points were higher than those of (−)‐(S)‐terazosin. The area under the plasma concentration–time curve (AUC0–∞) and maximum plasma concentration of (+)‐(R)‐terazosin were significantly greater than those of the (−)‐(S)‐terazosin (P < 0.01, respectively). The R/S ratio of AUC0–∞ of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047–1050, 2012. © 2012 Wiley Periodicals, Inc. The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48h in 12 healthy subjects. The plasma concentrations of (+)-(R)-terazosin at all time points were higher than those of (-)-(S)-terazosin. The area under the plasma concentration-time curve (AUC0-[infin]) and maximum plasma concentration of (+)-(R)-terazosin were significantly greater than those of the (-)-(S)-terazosin (P<0.01, respectively). The R/S ratio of AUC0-[infin] of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047-1050, 2012. © 2012 Wiley Periodicals, Inc. [PUBLICATION ABSTRACT] The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48h in 12 healthy subjects. The plasma concentrations of (+)-(R)-terazosin at all time points were higher than those of (-)-(S)-terazosin. The area under the plasma concentration-time curve (AUC sub(0-[infin])) and maximum plasma concentration of (+)-(R)-terazosin were significantly greater than those of the (-)-(S)-terazosin (P<0.01, respectively). The R/S ratio of AUC sub(0-[infin]) of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. Chirality 24:1047-1050, 2012. [copy 2012 Wiley Periodicals, Inc. The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)-(R)-terazosin at all time points were higher than those of (-)-(S)-terazosin. The area under the plasma concentration-time curve (AUC(0-∞) ) and maximum plasma concentration of (+)-(R)-terazosin were significantly greater than those of the (-)-(S)-terazosin (P < 0.01, respectively). The R/S ratio of AUC(0-∞) of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects.The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)-(R)-terazosin at all time points were higher than those of (-)-(S)-terazosin. The area under the plasma concentration-time curve (AUC(0-∞) ) and maximum plasma concentration of (+)-(R)-terazosin were significantly greater than those of the (-)-(S)-terazosin (P < 0.01, respectively). The R/S ratio of AUC(0-∞) of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg terazosin, the plasma concentrations of terazosin enantiomers were measured over the course of 48 h in 12 healthy subjects. The plasma concentrations of (+)-(R)-terazosin at all time points were higher than those of (-)-(S)-terazosin. The area under the plasma concentration-time curve (AUC(0-∞) ) and maximum plasma concentration of (+)-(R)-terazosin were significantly greater than those of the (-)-(S)-terazosin (P < 0.01, respectively). The R/S ratio of AUC(0-∞) of terazosin was 1.68. For the first time, it was proven that the pharmacokinetics of terazosin was stereoselective in healthy Chinese male subjects. |
Author | Zhang, Yanan Liu, Man Wang, Xiaolin Zhao, Ting Han, Jing Zhang, Dan Yang, Man Liu, Huichen |
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BackLink | https://www.ncbi.nlm.nih.gov/pubmed/22887707$$D View this record in MEDLINE/PubMed |
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CitedBy_id | crossref_primary_10_1111_bcpt_14090 crossref_primary_10_1016_j_saa_2020_118624 crossref_primary_10_1038_aps_2013_78 crossref_primary_10_1002_adsc_202400777 crossref_primary_10_1002_chir_22505 crossref_primary_10_1246_cl_160004 |
Cites_doi | 10.1208/aapsj0901011 10.1016/S0014-2999(97)89681-1 10.1177/009127009203200605 10.1016/S0378-4347(00)00313-3 10.1016/j.chroma.2009.05.034 10.1016/S0378-4347(98)00120-0 10.1016/S0026-895X(25)09946-8 10.1002/(SICI)1097-0045(19990215)38:3<216::AID-PROS6>3.0.CO;2-0 10.1016/S0021-9673(97)00892-3 10.1016/S0026-895X(25)10156-9 10.3109/10799899509049862 |
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References | Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA. The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol 1994;45:703-708. Bansal S, DeStefano A. Key elements of bioanalytical method validation for small molecules. AAPS J 2007;9:E109-E114. Ferretti R, Gallinella B, La Torre F, Zanitti L, Turchetto L, Mosca A, Cirilli R. Direct high-performance liquid chromatography enantioseparation of terazosin on an immobilised polysaccharide-based chiral stationary phase under polar organic and reversed-phase conditions. J Chromatogr A 2009;1216:5385-5390. Achari R, Laddu A. Terazosin: a new alpha adrenoceptor blocking drug. J Clin Pharmacol 1992;32:520-523. Liu M, Zhang D, Han J, Liu H. Enantiomeric separation of terazosin by NP-HPLC. Chin J Pharm 2012;43:53-56. Ireland LM, Cain JC, Rotert G, Thomas S, Shoghi S, Hancock AA, Kerwin JF Jr. [3H]R-terazosin binds selectively to alpha1-adrenoceptors over alpha2-adrenoceptors - comparison with racemic [3H]terazosin and [3H]prazosin. Eur J Pharmacol 1997;327:79-86. Sekhar EC, Rao TR, Sekhar KR, Naidu MU, Shobha JC, Rani PU, Kumar TV, Kumar VP. Determination of terazosin in human plasma, using high-performance liquid chromatography with fluorescence detection. J Chromatogr B 1998;710:137-142. Zavitsanos AP, Alebic-Kolbah T. Enantioselective determination of terazosin in human plasma by normal phase high-performance liquid chromatography-electrospray mass spectrometry. J Chromatogr A 1998;794:45-56. Hancock AA, Buckner SA, Ireland LM, Knepper SM, Kerwin JF Jr. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res 1995;15:863-885. Bu Y, Chen D, Zhao C. Studies on pharmacokinetics and bioequivalence of terazosin hydrochloride tablets. Chin J Pharm Anal 2007;27:1361-1363. Chen J, Lu W, Gao K, Shi Z, Jiang X, Rong Z, Chen H. Studies on the bioequivalence of domestic terazosin tablet in healthy volunteers. Chin Pharm J 2003;38:446-448. Nakaki T, Nakayama M, Yamamoto S, Kato R. Alpha 1-adrenergic stimulation and beta 2-adrenergic inhibition of DNA synthesis in vascular smooth muscle cells. Mol Pharmacol 1990;37:30-36. Cheah PY, Yuen KH, Liong ML. Improved high-performance liquid chromatographic analysis of terazosin in human plasma. J Chromatogr B 2000;745:439-443. Smith P, Rhodes NP, Ke Y, Foster CS. Influence of the alpha1-adrenergic antagonist, doxazosin, on noradrenaline-induced modulation of cytoskeletal proteins in cultured hyperplastic prostatic stromal cells. Prostate 1999;38:216-227. 2009; 1216 1997; 327 1990; 37 1995; 15 1999; 38 2000; 745 1994; 45 2007; 9 2003; 38 1998; 710 1992; 32 1998; 794 2012; 43 2007; 27 e_1_2_5_15_1 e_1_2_5_14_1 e_1_2_5_16_1 e_1_2_5_11_1 e_1_2_5_7_1 e_1_2_5_10_1 e_1_2_5_6_1 e_1_2_5_5_1 e_1_2_5_12_1 e_1_2_5_4_1 Nakaki T (e_1_2_5_3_1) 1990; 37 Bu Y (e_1_2_5_8_1) 2007; 27 Liu M (e_1_2_5_13_1) 2012; 43 Chen J (e_1_2_5_9_1) 2003; 38 Forray C (e_1_2_5_2_1) 1994; 45 |
References_xml | – reference: Ireland LM, Cain JC, Rotert G, Thomas S, Shoghi S, Hancock AA, Kerwin JF Jr. [3H]R-terazosin binds selectively to alpha1-adrenoceptors over alpha2-adrenoceptors - comparison with racemic [3H]terazosin and [3H]prazosin. Eur J Pharmacol 1997;327:79-86. – reference: Bansal S, DeStefano A. Key elements of bioanalytical method validation for small molecules. AAPS J 2007;9:E109-E114. – reference: Forray C, Bard JA, Wetzel JM, Chiu G, Shapiro E, Tang R, Lepor H, Hartig PR, Weinshank RL, Branchek TA. The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype. Mol Pharmacol 1994;45:703-708. – reference: Sekhar EC, Rao TR, Sekhar KR, Naidu MU, Shobha JC, Rani PU, Kumar TV, Kumar VP. Determination of terazosin in human plasma, using high-performance liquid chromatography with fluorescence detection. J Chromatogr B 1998;710:137-142. – reference: Cheah PY, Yuen KH, Liong ML. Improved high-performance liquid chromatographic analysis of terazosin in human plasma. J Chromatogr B 2000;745:439-443. – reference: Hancock AA, Buckner SA, Ireland LM, Knepper SM, Kerwin JF Jr. Actions of terazosin and its enantiomers at subtypes of alpha 1- and alpha 2-adrenoceptors in vitro. J Recept Signal Transduct Res 1995;15:863-885. – reference: Liu M, Zhang D, Han J, Liu H. Enantiomeric separation of terazosin by NP-HPLC. Chin J Pharm 2012;43:53-56. – reference: Achari R, Laddu A. Terazosin: a new alpha adrenoceptor blocking drug. J Clin Pharmacol 1992;32:520-523. – reference: Chen J, Lu W, Gao K, Shi Z, Jiang X, Rong Z, Chen H. Studies on the bioequivalence of domestic terazosin tablet in healthy volunteers. Chin Pharm J 2003;38:446-448. – reference: Zavitsanos AP, Alebic-Kolbah T. 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The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of... The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2‐mg... The purpose of this study was to elucidate the pharmacokinetics of terazosin enantiomers in healthy Chinese male subjects. After a single oral dose of 2-mg... |
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SubjectTerms | Adult Asian Continental Ancestry Group Blood Chemical Analysis - methods Chirality Chromatography, High Pressure Liquid determination enantiomer Enantiomers Health HPLC-FD Humans Male Males Pharmacokinetics plasma Prazosin - analogs & derivatives Prazosin - blood Prazosin - chemistry Prazosin - pharmacokinetics Spectrometry, Fluorescence Stereoisomerism terazosin Young Adult |
Title | Pharmacokinetics of Terazosin Enantiomers in Healthy Chinese Male Subjects |
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