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西咪替丁和雷尼替丁对卡马西平和丙戊酸钠药代动力学的影响。

Effect of cimetidine and ranitidine on carbamazepine and sodium valproate pharmacokinetics.

作者信息

Webster L K, Mihaly G W, Jones D B, Smallwood R A, Phillips J A, Vajda F J

出版信息

Eur J Clin Pharmacol. 1984;27(3):341-3. doi: 10.1007/BF00542172.

DOI:10.1007/BF00542172
PMID:6096154
Abstract

The pharmacokinetics of a single oral dose (400 mg) of carbamazepine and sodium valproate were compared in peptic ulcer patients before and after four weeks of a therapeutic course of either cimetidine (1 g/day, n = 6 subjects) or ranitidine (300 mg/day, n = 6 subjects). There was a small (up to 20%) but statistically significant decrease in oral clearance of carbamazepine after cimetidine treatment. A similar fall in sodium valproate clearance in five cimetidine-treated patients was accompanied by a significantly prolonged elimination half-life. No such trends were demonstrated during ranitidine treatment. Since both anticonvulsants are partly metabolized by hepatic mixed function oxidases, an inhibition by cimetidine at this level may be responsible for the observed impairment of clearance. Thus a potentially important clinical interaction may occur in patients taking anticonvulsants and cimetidine concurrently.

摘要

在消化性溃疡患者中,比较了西咪替丁(1克/天,n = 6名受试者)或雷尼替丁(300毫克/天,n = 6名受试者)治疗四周前后,单次口服剂量400毫克卡马西平和丙戊酸钠的药代动力学。西咪替丁治疗后,卡马西平的口服清除率有小幅(高达20%)但具有统计学意义的下降。五名接受西咪替丁治疗的患者中丙戊酸清除率的类似下降伴随着消除半衰期的显著延长。雷尼替丁治疗期间未显示出此类趋势。由于两种抗惊厥药均部分通过肝脏混合功能氧化酶代谢,西咪替丁在该水平的抑制作用可能是观察到的清除率受损的原因。因此,同时服用抗惊厥药和西咪替丁的患者可能会发生潜在重要的临床相互作用。

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Effect of cimetidine and ranitidine on carbamazepine and sodium valproate pharmacokinetics.西咪替丁和雷尼替丁对卡马西平和丙戊酸钠药代动力学的影响。
Eur J Clin Pharmacol. 1984;27(3):341-3. doi: 10.1007/BF00542172.
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本文引用的文献

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Ranitidine. An updated review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in peptic ulcer disease and other allied diseases.雷尼替丁。对其药效学、药代动力学特性以及在消化性溃疡疾病和其他相关疾病中的治疗应用的最新综述。
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Clinical pharmacokinetics of drugs used in the treatment of gastrointestinal diseases (Part II).用于治疗胃肠道疾病的药物的临床药代动力学(第二部分)。
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Drug interactions with cimetidine.西咪替丁的药物相互作用。
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The interaction of cimetidine with rat liver microsomes.西咪替丁与大鼠肝微粒体的相互作用。
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Drug interactions with valproic acid.丙戊酸的药物相互作用
Drugs. 1982 Dec;24(6):543-56. doi: 10.2165/00003495-198224060-00004.
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Clinical pharmacokinetics of valproic acid.丙戊酸的临床药代动力学
Clin Pharmacokinet. 1980 Jan-Feb;5(1):67-83. doi: 10.2165/00003088-198005010-00002.
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High-pressure liquid chromatographic determination of ranitidine, a new H2-receptor antagonist, in plasma and urine.血浆和尿液中新型H2受体拮抗剂雷尼替丁的高压液相色谱测定法
J Pharm Sci. 1980 Oct;69(10):1155-7. doi: 10.1002/jps.2600691008.
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Characterization of cimetidine, ranitidine, and related structures' interaction with cytochrome P-450.西咪替丁、雷尼替丁及相关结构与细胞色素P-450相互作用的表征
Drug Metab Dispos. 1983 Mar-Apr;11(2):137-42.
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Ranitidine: a review of its pharmacology and therapeutic use in peptic ulcer disease and other allied diseases.雷尼替丁:其药理学及在消化性溃疡疾病和其他相关疾病中的治疗应用综述
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