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树脂和活性炭对地高辛、卡马西平和呋塞米吸收的影响。

Effects of resins and activated charcoal on the absorption of digoxin, carbamazepine and frusemide.

作者信息

Neuvonen P J, Kivistö K, Hirvisalo E L

机构信息

Department of Clinical Pharmacology, University of Helsinki, Finland.

出版信息

Br J Clin Pharmacol. 1988 Feb;25(2):229-33. doi: 10.1111/j.1365-2125.1988.tb03295.x.

Abstract
  1. The interference of resins and activated charcoal with the absorption of digoxin, carbamazepine and frusemide was studied. 2. In a cross-over study consisting of four phases, single doses of colestipol hydrochloride (10 g), cholestyramine (8 g), activated charcoal (8 g) or water only were given to six healthy volunteers immediately after the simultaneous ingestion of digoxin (0.25 mg), carbamazepine (400 mg) and frusemide (40 mg). Plasma and urine concentrations of the test drugs and the urine volumes were determined up to 72 h. 3. The absorption of digoxin was not reduced by colestipol, moderately (30-40%, P less than 0.05) reduced by cholestyramine and greatly (96%) by charcoal. 4. The absorption of carbamazepine was not decreased by cholestyramine, slightly (10%) by colestipol and greatly (90%) by activated charcoal. 5. The absorption and the diuretic effect of frusemide were significantly diminished by all agents. The bioavailability was reduced by colestipol 80%, by cholestyramine 95% and by activated charcoal 99.5%. 6. The interference with the gastrointestinal absorption of most of the basic drugs by colestipol and cholestyramine seems to be minimal. On the other hand, the resins may seriously impair the absorption of certain acidic drugs, for example frusemide.
摘要
  1. 研究了树脂和活性炭对地高辛、卡马西平和呋塞米吸收的干扰作用。2. 在一项包括四个阶段的交叉研究中,给6名健康志愿者在同时摄入地高辛(0.25毫克)、卡马西平(400毫克)和呋塞米(40毫克)后立即分别单次给予盐酸考来烯胺(10克)、考来替泊(8克)、活性炭(8克)或仅给予水。测定了长达72小时的受试药物的血浆和尿液浓度以及尿量。3. 考来烯胺未降低地高辛的吸收,考来替泊使其吸收适度降低(30 - 40%,P < 0.05),而活性炭使其吸收大幅降低(96%)。4. 考来替泊未降低卡马西平的吸收,考来烯胺使其吸收略有降低(10%),活性炭使其吸收大幅降低(90%)。5. 所有药物均显著降低了呋塞米的吸收和利尿作用。考来烯胺使生物利用度降低80%,考来替泊使其降低95%,活性炭使其降低99.5%。6. 考来替泊和考来烯胺对大多数碱性药物胃肠道吸收的干扰似乎最小。另一方面,这些树脂可能会严重损害某些酸性药物的吸收,例如呋塞米。

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