异喹胍氧化表型与普萘洛尔的药代动力学和药效学之间的关系。
The relationship between debrisoquine oxidation phenotype and the pharmacokinetics and pharmacodynamics of propranolol.
作者信息
Lennard M S, Jackson P R, Freestone S, Tucker G T, Ramsay L E, Woods H F
出版信息
Br J Clin Pharmacol. 1984 Jun;17(6):679-85. doi: 10.1111/j.1365-2125.1984.tb02403.x.
Abstract
The pharmacokinetics and pharmacodynamics of propranolol (80 mg by mouth) were studied in seven extensive and four poor metabolisers of debrisoquine. Evidence for impairment of the 4'-hydroxylation of propranolol was found in poor metabolisers. However, no significant difference was detected in the oral clearance of unchanged drug between the two groups of debrisoquine oxidation phenotypes. Poor metabolisers of debrisoquine did not experience more intense or more prolonged beta-adrenoceptor blockade than extensive metabolisers of debrisoquine.
摘要
对7名异喹胍广泛代谢者和4名异喹胍代谢不良者研究了普萘洛尔（口服80毫克）的药代动力学和药效学。在代谢不良者中发现了普萘洛尔4'-羟基化受损的证据。然而，两组异喹胍氧化表型之间未观察到未改变药物口服清除率的显著差异。异喹胍代谢不良者与异喹胍广泛代谢者相比，并未经历更强烈或更持久的β-肾上腺素能受体阻滞。
相似文献
1
The relationship between debrisoquine oxidation phenotype and the pharmacokinetics and pharmacodynamics of propranolol.异喹胍氧化表型与普萘洛尔的药代动力学和药效学之间的关系。
Br J Clin Pharmacol. 1984 Jun;17(6):679-85. doi: 10.1111/j.1365-2125.1984.tb02403.x.
2
The oral clearance and beta-adrenoceptor antagonist activity of propranolol after single dose are not related to debrisoquine oxidation phenotype.单次给药后普萘洛尔的口服清除率及β-肾上腺素受体拮抗活性与异喹胍氧化表型无关。
Br J Clin Pharmacol. 1984;17 Suppl 1(Suppl 1):106S-107S. doi: 10.1111/j.1365-2125.1984.tb02441.x.
3
The polymorphic oxidation of beta-adrenoceptor antagonists. Clinical pharmacokinetic considerations.β-肾上腺素能受体拮抗剂的多态性氧化。临床药代动力学考量。
Clin Pharmacokinet. 1986 Jan-Feb;11(1):1-17. doi: 10.2165/00003088-198611010-00001.
4
Debrisoquine polymorphism and the metabolism and action of metoprolol, timolol, propranolol and atenolol.异喹胍多态性与美托洛尔、噻吗洛尔、普萘洛尔和阿替洛尔的代谢及作用
Xenobiotica. 1986 May;16(5):435-47. doi: 10.3109/00498258609050250.
5
Lack of relationship between debrisoquine oxidation phenotype and the pharmacokinetics and first dose effect of prazosin.去甲丙咪嗪氧化表型与哌唑嗪的药代动力学及首剂效应之间缺乏相关性。
Br J Clin Pharmacol. 1988 Feb;25(2):276-8. doi: 10.1111/j.1365-2125.1988.tb03303.x.
6
Timolol and atenolol: relationships between oxidation phenotype, pharmacokinetics and pharmacodynamics.噻吗洛尔和阿替洛尔：氧化表型、药代动力学与药效学之间的关系。
Br J Clin Pharmacol. 1985 Mar;19(3):329-33. doi: 10.1111/j.1365-2125.1985.tb02651.x.
7
Metabolic oxidation of methaqualone in extensive and poor metabolisers of debrisoquine.安非他明在异喹胍代谢快和代谢慢的人群中的代谢氧化作用。
Eur J Clin Pharmacol. 1982;23(2):147-50. doi: 10.1007/BF00545969.
8
Discovery of altered pharmacokinetics of CGP 15 210 G in poor hydroxylators of debrisoquine during early drug development.在药物研发早期发现去甲丙咪嗪羟化能力差的个体中CGP 15 210 G的药代动力学改变。
Br J Clin Pharmacol. 1985 Jul;20(1):81-4. doi: 10.1111/j.1365-2125.1985.tb02802.x.
9
Lack of relationship between tolbutamide metabolism and debrisoquine oxidation phenotype.甲苯磺丁脲代谢与异喹胍氧化表型之间缺乏相关性。
Eur J Clin Pharmacol. 1987;33(4):397-402. doi: 10.1007/BF00637637.
10
Defective metabolism of metoprolol in poor hydroxylators of debrisoquine.在异喹胍羟化能力差的个体中，美托洛尔代谢存在缺陷。
Br J Clin Pharmacol. 1982 Aug;14(2):301-3. doi: 10.1111/j.1365-2125.1982.tb01982.x.
引用本文的文献
1
Pediatric Beta Blocker Therapy: A Comprehensive Review of Development and Genetic Variation to Guide Precision-Based Therapy in Children, Adolescents, and Young Adults.儿科β受体阻滞剂治疗：儿童、青少年和青年精准治疗的发展和遗传变异综合综述。
Genes (Basel). 2024 Mar 20;15(3):379. doi: 10.3390/genes15030379.
2
Human CYP2D6 Is Functional in Brain In Vivo: Evidence from Humanized CYP2D6 Transgenic Mice.人 CYP2D6 在体内具有脑功能：来自人源化 CYP2D6 转基因小鼠的证据。
Mol Neurobiol. 2020 Jun;57(6):2509-2520. doi: 10.1007/s12035-020-01896-4. Epub 2020 Mar 18.
3
Propranolol is a mechanism-based inhibitor of CYP2D and CYP2D6 in humanized CYP2D6-transgenic mice: Effects on activity and drug responses.普萘洛尔是一种基于机制的人源化CYP2D6转基因小鼠中CYP2D和CYP2D6的抑制剂：对活性和药物反应的影响。
Br J Pharmacol. 2020 Feb;177(3):701-712. doi: 10.1111/bph.14884. Epub 2020 Jan 6.
4
Pharmacokinetic Parameters and Over-Responsiveness of Iranian Population to Propranolol.伊朗人群对普萘洛尔的药代动力学参数及过度反应性
Adv Pharm Bull. 2017 Jun;7(2):195-202. doi: 10.15171/apb.2017.024. Epub 2017 Jun 30.
5
Polymorphism of human cytochrome P450 2D6 and its clinical significance: Part I.人类细胞色素P450 2D6的多态性及其临床意义：第一部分。
Clin Pharmacokinet. 2009;48(11):689-723. doi: 10.2165/11318030-000000000-00000.
6
Use of in vitro and in vivo data to estimate the likelihood of metabolic pharmacokinetic interactions.利用体外和体内数据评估代谢性药代动力学相互作用的可能性。
Clin Pharmacokinet. 1997 Mar;32(3):210-58. doi: 10.2165/00003088-199732030-00004.
7
Interethnic differences in drug metabolism: influence of genetic and environmental factors on debrisoquine hydroxylation phenotype.药物代谢中的种族差异：遗传和环境因素对异喹胍羟基化表型的影响。
Eur J Drug Metab Pharmacokinet. 1996 Apr-Jun;21(2):129-38. doi: 10.1007/BF03190261.
8
Clinical significance of genetic influences on cardiovascular drug metabolism.基因对心血管药物代谢影响的临床意义。
Cardiovasc Drugs Ther. 1993 Jun;7(3):311-24. doi: 10.1007/BF00880154.
9
Inhibition of CYP2D6 activity by treatment with propranolol and the role of 4-hydroxy propranolol.普萘洛尔治疗对CYP2D6活性的抑制作用及4-羟基普萘洛尔的作用
Br J Clin Pharmacol. 1994 Jul;38(1):9-14. doi: 10.1111/j.1365-2125.1994.tb04315.x.
10
Identification of human CYP isoforms involved in the metabolism of propranolol enantiomers--N-desisopropylation is mediated mainly by CYP1A2.参与普萘洛尔对映体代谢的人细胞色素P450同工酶的鉴定——N-去异丙基化主要由CYP1A2介导。
Br J Clin Pharmacol. 1995 Apr;39(4):421-31. doi: 10.1111/j.1365-2125.1995.tb04472.x.
本文引用的文献
1
Effect of dose and uremia on plasma and urine profiles of propranolol metabolites.剂量和尿毒症对普萘洛尔代谢产物血浆及尿液谱的影响。
Clin Pharmacol Ther. 1980 Jun;27(6):744-55. doi: 10.1038/clpt.1980.105.
2
Oxidation phenotype--a major determinant of metoprolol metabolism and response.氧化表型——美托洛尔代谢及反应的主要决定因素。
N Engl J Med. 1982 Dec 16;307(25):1558-60. doi: 10.1056/NEJM198212163072505.
3
Plasma levels of (+) and (-)-propranolol and 4-hydroxypropranolol after administration of racemic (+/-)-propranolol in man.在人体中给予消旋（±）-普萘洛尔后（+）和（-）-普萘洛尔及4-羟基普萘洛尔的血浆水平。
Br J Clin Pharmacol. 1982 Jul;14(1):79-82. doi: 10.1111/j.1365-2125.1982.tb04937.x.
4
An automated HPLC method for the assay of propranolol and its basic metabolites in plasma and urine.一种用于测定血浆和尿液中普萘洛尔及其碱性代谢物的自动高效液相色谱法。
J Chromatogr Sci. 1982 Mar;20(3):126-31. doi: 10.1093/chromsci/20.3.126.
5
Dose-dependent elimination of propranolol and its major metabolites in humans.
J Pharm Sci. 1983 Jul;72(7):725-32. doi: 10.1002/jps.2600720703.
6
Stereoselective binding of propranolol to human plasma, alpha 1-acid glycoprotein, and albumin.普萘洛尔与人血浆、α1-酸性糖蛋白及白蛋白的立体选择性结合。
Clin Pharmacol Ther. 1983 Dec;34(6):718-23. doi: 10.1038/clpt.1983.240.
7
Identification of major sulfate conjugates in the metabolism of propranolol in dog and man.
Drug Metab Dispos. 1983 Jul-Aug;11(4):344-9.
8
[Pharmacokinetic and clinical consequences of the genetic polymorphism of oxidation].
Schweiz Med Wochenschr. 1983 Feb 26;113(8):295-7.
9
Interaction of phenobarbital with propranolol in the dog. 3. Beta blockade.
J Pharmacol Exp Ther. 1983 Jan;224(1):62-7.
10
Defective metabolism of metoprolol in poor hydroxylators of debrisoquine.在异喹胍羟化能力差的个体中，美托洛尔代谢存在缺陷。
Br J Clin Pharmacol. 1982 Aug;14(2):301-3. doi: 10.1111/j.1365-2125.1982.tb01982.x.
Zotero 插件