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利福平会降低泼尼松龙的疗效和生物利用度。

Rifampicin reduces effectiveness and bioavailability of prednisolone.

作者信息

McAllister W A, Thompson P J, Al-Habet S M, Rogers H J

出版信息

Br Med J (Clin Res Ed). 1983 Mar 19;286(6369):923-5. doi: 10.1136/bmj.286.6369.923.

DOI:10.1136/bmj.286.6369.923
PMID:6403136
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1547305/
Abstract

Rifampicin is an inducer of hepatic drug metabolising enzymes. This results in interactions with several drugs including oral anticoagulants, hypoglycaemics, and contraceptives. Concurrent treatment with prednisolone and rifampicin is given when tuberculosis coexists with a disease that is sensitive to steroids, when the diagnosis is uncertain, or occasionally in the treatment of severe tuberculosis. Two patients with respiratory disease were treated with both drugs: their condition improved considerably after rifampicin was withdrawn. Seven patients were then studied to assess the effect of rifampicin on the pharmacokinetics of prednisolone. Overall, rifampicin increased the plasma clearance of prednisolone by 45% and reduced the amount of drug available to the tissues (area under the plasma concentration time curve) by 66%. The effectiveness of prednisolone may be considerably reduced when rifampicin and prednisolone are used in combination.

摘要

利福平是肝脏药物代谢酶的诱导剂。这会导致与多种药物发生相互作用,包括口服抗凝剂、降血糖药和避孕药。当结核病与对类固醇敏感的疾病并存、诊断不确定或偶尔在治疗严重结核病时,会同时使用泼尼松龙和利福平进行治疗。两名患有呼吸系统疾病的患者接受了这两种药物的治疗:停用利福平后,他们的病情有了显著改善。随后对7名患者进行了研究,以评估利福平对泼尼松龙药代动力学的影响。总体而言,利福平使泼尼松龙的血浆清除率提高了45%,并使组织可利用的药物量(血浆浓度-时间曲线下面积)减少了66%。联合使用利福平和泼尼松龙时,泼尼松龙的有效性可能会显著降低。

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1
Rifampicin reduces effectiveness and bioavailability of prednisolone.利福平会降低泼尼松龙的疗效和生物利用度。
Br Med J (Clin Res Ed). 1983 Mar 19;286(6369):923-5. doi: 10.1136/bmj.286.6369.923.
2
Changes in prednisolone pharmacokinetics and protein binding during treatment with rifampicin.利福平治疗期间泼尼松龙药代动力学及蛋白结合率的变化。
Proc Eur Dial Transplant Assoc. 1983;19:552-7.
3
Altered prednisolone pharmacokinetics in patients treated with rifampicin.利福平治疗患者中泼尼松龙药代动力学的改变。
Acta Med Scand. 1983;213(5):339-43. doi: 10.1111/j.0954-6820.1983.tb03748.x.
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Adverse effect of rifampicin administration on steroid-dependent asthma.利福平给药对激素依赖型哮喘的不良影响。
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[Rifampicin-induced resistance to prednisolone treatment in collagen disease--a pharmacokinetic study].[利福平诱导的胶原病对泼尼松龙治疗的耐药性——一项药代动力学研究]
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[A comparative study of the accelerated metabolism of cortisol, prednisolone and dexamethasone in patients under rifampicin therapy].[利福平治疗患者中皮质醇、泼尼松龙和地塞米松代谢加速的比较研究]
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本文引用的文献

1
Pharmacokinetics of intravenous and oral prednisolone.静脉注射和口服泼尼松龙的药代动力学
Br J Clin Pharmacol. 1980 Nov;10(5):503-8. doi: 10.1111/j.1365-2125.1980.tb01796.x.
2
Differential induction of antipyrine metabolism by rifampicin.利福平对安替比林代谢的差异诱导作用。
Eur J Clin Pharmacol. 1981;21(2):155-60. doi: 10.1007/BF00637517.
3
Comparison of radioimmunoassay and thin layer chromatographic assay methods for estimation of plasma prednisolone concentrations.放射免疫分析法与薄层色谱分析法用于估算血浆泼尼松龙浓度的比较。
J Pharmacol Methods. 1981 Sep;6(2):137-42. doi: 10.1016/0160-5402(81)90036-x.
4
Changes of the smooth endoplasmic reticulum induced by rifampicin in human and guinea-pig hepatocytes.利福平诱导的人及豚鼠肝细胞滑面内质网的变化
Gut. 1971 Dec;12(12):984-7. doi: 10.1136/gut.12.12.984.
5
Kinetics of rifampicin and isoniazid administered alone and in combination to normal subjects and patients with liver disease.利福平与异烟肼单独及联合给药于正常受试者和肝病患者的动力学。
Gut. 1972 Jan;13(1):47-53. doi: 10.1136/gut.13.1.47.
6
Interaction of sodium warfarin and rifampin. Studies in man.华法林钠与利福平的相互作用。人体研究。
Ann Intern Med. 1974 Sep;81(3):337-40. doi: 10.7326/0003-4819-81-3-337.
7
Determination of drug metabolizing enzymes in needle biopsies of human liver.人肝脏穿刺活检中药物代谢酶的测定
Eur J Clin Pharmacol. 1972 Mar;4(2):65-73. doi: 10.1007/BF00562499.
8
Induction of drug metabolism in man after rifampicin treatment measured by increased hexobarbital and tolbutamide clearance.利福平治疗后通过增加己巴比妥和甲苯磺丁脲清除率来测定人体药物代谢的诱导情况。
Eur J Clin Pharmacol. 1975 Dec 19;9(2-3):219-27. doi: 10.1007/BF00614021.
9
Plasma prednisolone levels from enteric and non-enteric coated tablets estimated by an original technique.采用一种原创技术估算肠溶和非肠溶包衣片剂的血浆泼尼松龙水平。
Br J Clin Pharmacol. 1977 Oct;4(5):597-603. doi: 10.1111/j.1365-2125.1977.tb00792.x.
10
Interaction of rifampin and glucocorticoids. Adverse effect on renal allograft function.利福平与糖皮质激素的相互作用。对肾移植功能的不良影响。
JAMA. 1976 Oct 25;236(17):1958-60.