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普鲁卡因酰胺在人体内的乙酰化。初步报告。

Acetylation of procaine amide in man. A preliminary communication.

作者信息

Karlsson E, Aberg G, Collste P, Molin L, Norlander B, Sjöqvist F

出版信息

Eur J Clin Pharmacol. 1975;8(1):79-81. doi: 10.1007/BF00616419.

DOI:10.1007/BF00616419
PMID:1233205
Abstract

The metabolism of procaine amide was studied in 41 cardiac patients who had achieved steady state plasma concentrations of the drug. Acetylated procaine amide accounted for 31 +/- 12% (range 16-63%) of the overall urinary recovery of the drug and is therefore a main metabolite in man. Plasma levels of the metabolite were usually lower but sometimes exceeded those of the parent compound with variations between 1 and 15 mug/ml. The metabolite had a weaker effect than procaine amide on the maximal electrical driving velocity of isolated atrial strips from guinea pig.

摘要

对41例已达到药物稳态血药浓度的心脏病患者进行了普鲁卡因胺代谢的研究。乙酰化普鲁卡因胺占该药物尿中总回收率的31±12%(范围为16 - 63%),因此是人体中的主要代谢产物。该代谢产物的血浆水平通常较低,但有时会超过母体化合物,其变化范围在1至15微克/毫升之间。该代谢产物对豚鼠离体心房条最大电驱动速度的作用比普鲁卡因胺弱。

相似文献

1
Acetylation of procaine amide in man. A preliminary communication.普鲁卡因酰胺在人体内的乙酰化。初步报告。
Eur J Clin Pharmacol. 1975;8(1):79-81. doi: 10.1007/BF00616419.
2
Acetylation of procaine amide in man studied with a new gas chromatographic method.用一种新的气相色谱法研究人体中普鲁卡因酰胺的乙酰化。
Br J Clin Pharmacol. 1974 Dec;1(6):467-75. doi: 10.1111/j.1365-2125.1974.tb01696.x.
3
Some effects of disopyramide and its N-dealkylated metabolite on isolated nerve and cardiac muscle.丙吡胺及其N-脱烷基代谢产物对离体神经和心肌的某些作用。
Eur J Pharmacol. 1978 Jun 15;49(4):389-94. doi: 10.1016/0014-2999(78)90313-8.
4
The effects of quinidine, procaine amide and pyrilamine on the membrane resting and action potential of guinea pig ventricular muscle fibers.奎尼丁、普鲁卡因酰胺和吡苄明对豚鼠心室肌纤维膜静息电位和动作电位的影响。
J Pharmacol Exp Ther. 1956 Jun;117(2):237-44.
5
[Protection offered by infusion of adrenaline on complete atrio-ventricular block induced in the guinea pig by quinidine and procaine amide].[肾上腺素输注对奎尼丁和普鲁卡因酰胺诱发豚鼠完全性房室传导阻滞的保护作用]
Folia Cardiol. 1967 Nov-Dec;26(6):326-9.
6
Clinical pharmacokinetics of procainamide.普鲁卡因胺的临床药代动力学。
Clin Pharmacokinet. 1978 Mar-Apr;3(2):97-107. doi: 10.2165/00003088-197803020-00001.
7
Polymorphic acetylation of procaine amide in healthy subjects.健康受试者中普鲁卡因胺的多态性乙酰化
Acta Med Scand. 1975 Apr;197(4):299-302. doi: 10.1111/j.0954-6820.1975.tb04921.x.
8
The effect of procaine on the passive electrical properties of guinea-pig ventricular muscle.普鲁卡因对豚鼠心室肌被动电特性的影响。
Pflugers Arch. 1978 Dec 15;378(1):1-7. doi: 10.1007/BF00581951.
9
Metabolism of procainamide and p-aminobenzoic acid in patients with chronic liver disease.慢性肝病患者中普鲁卡因胺和对氨基苯甲酸的代谢
Clin Pharmacol Ther. 1977 Nov;22(5 Pt 1):588-95. doi: 10.1002/cpt1977225part1588.
10
[Studies on the effect of quinine, quinidine, procaine and procaine amide on oxygen metabolism in isolated frog hearts].[奎宁、奎尼丁、普鲁卡因及普鲁卡因酰胺对离体蛙心氧代谢影响的研究]
Acta Physiol Pol. 1960 Sep-Dec;11:770-1.

引用本文的文献

1
Acetylator phenotype and the clinical pharmacology of slow-release procainamide.乙酰化表型与普鲁卡因胺控释剂的临床药理学。
Br J Clin Pharmacol. 1976 Dec;3(6):1023-6. doi: 10.1111/j.1365-2125.1976.tb00352.x.
2
Determination of the acetylator phenotype and pharmacokinetics of some sulphonamides in man.人体中某些磺胺类药物乙酰化表型及药代动力学的测定
Clin Pharmacokinet. 1980 May-Jun;5(3):274-94. doi: 10.2165/00003088-198005030-00006.
3
Acetylation of procainamide and isoniazid by a rat liver-N-acetyl-transferase.大鼠肝脏N-乙酰转移酶对普鲁卡因胺和异烟肼的乙酰化作用。

本文引用的文献

1
The physiological disposition and cardiac effects of procaine amide.普鲁卡因酰胺的生理处置及心脏效应。
J Pharmacol Exp Ther. 1951 May;102(1):5-15.
2
A comparison of tests for antifibrillatory action.抗纤颤作用测试的比较
Br J Pharmacol Chemother. 1961 Dec;17(3):424-32. doi: 10.1111/j.1476-5381.1961.tb01129.x.
3
Procainamide induction of a systemic lupus erythematosus-like syndrome. Presentation of six cases, review of the literature, and analysis and followup of reported cases.普鲁卡因胺诱发系统性红斑狼疮样综合征。6例病例报告、文献复习以及对已报道病例的分析与随访
Eur J Drug Metab Pharmacokinet. 1981;6(2):81-4. doi: 10.1007/BF03189472.
4
Procainamide absorption studies to test the feasibility of using a sustained-release preparation.进行普鲁卡因胺吸收研究以测试使用缓释制剂的可行性。
Br J Clin Pharmacol. 1975 Dec;2(6):515-9. doi: 10.1111/j.1365-2125.1975.tb00569.x.
5
Pharmacokinetics in man of the N-acetylated metabolite of procainamide.普鲁卡因酰胺N - 乙酰化代谢产物在人体中的药代动力学。
J Pharmacokinet Biopharm. 1975 Aug;3(4):223-35. doi: 10.1007/BF01066919.
6
Comparison of the acetylation of procainamide and sulfadimidine in man.人体内普鲁卡因酰胺和磺胺二甲嘧啶乙酰化作用的比较。
Eur J Clin Pharmacol. 1976 Mar 22;09(5-6):433-8. doi: 10.1007/BF00606561.
7
Serum procainamide levels as therapeutic guides.作为治疗指导的血清普鲁卡因胺水平。
Clin Pharmacokinet. 1977 Nov-Dec;2(6):389-402. doi: 10.2165/00003088-197702060-00001.
8
Pharmacokinetics of sulphamethoxazole in man: effects of urinary pH and urine flow on metabolism and renal excretion of sulphamethoxazole and its metabolite N4-acetylsulphamethoxazole.磺胺甲恶唑在人体中的药代动力学:尿液pH值和尿流对磺胺甲恶唑及其代谢产物N4-乙酰磺胺甲恶唑代谢和肾排泄的影响。
Clin Pharmacokinet. 1978 Jul-Aug;3(4):319-29. doi: 10.2165/00003088-197803040-00005.
Medicine (Baltimore). 1969 May;48(3):217-28.
4
Inactivation of isoniazid (INH) in Swedish tuberculous patients before and during treatment with para-aminosalicylic acid (PAS).瑞典结核病患者在使用对氨基水杨酸(PAS)治疗前及治疗期间异烟肼(INH)的失活情况。
Scand J Respir Dis. 1970;51(1):61-9.
5
Genetic variations in the acetylation of isoniazid and other drugs.异烟肼及其他药物乙酰化过程中的基因变异。
Ann N Y Acad Sci. 1968 Jul 31;151(2):723-33. doi: 10.1111/j.1749-6632.1968.tb48255.x.
6
Procainamide dosage schedules, plasma concentrations, and clinical effects.普鲁卡因胺的给药方案、血浆浓度及临床效果。
JAMA. 1971 Mar 1;215(9):1454-60.
7
Pharmacokinetics of procainamide.普鲁卡因胺的药代动力学
Arch Intern Med. 1972 Sep;130(3):366-9.
8
Arrhythmia prophylaxis with procaine amide: plasma concentrations in relation to dose.普鲁卡因胺预防心律失常:血浆浓度与剂量的关系。
Acta Med Scand. 1973 Nov;194(5):405-11. doi: 10.1111/j.0954-6820.1973.tb19465.x.
9
Metabolism of procainamide in rhesus monkey and man.普鲁卡因酰胺在恒河猴和人类中的代谢。
Clin Pharmacol Ther. 1972 May-Jun;13(3):366-71. doi: 10.1002/cpt1972133366.
10
A new sustained-release tablet formulation of procainamide.
Eur J Clin Pharmacol. 1973 Dec;6(4):251-5. doi: 10.1007/BF00644741.