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苄达明的药代动力学。

Pharmacokinetics of benzydamine.

作者信息

Chasseaud L F, Catanese B

出版信息

Int J Tissue React. 1985;7(3):195-204.

PMID:4044147
Abstract

Clinically, benzydamine can exert its action locally or systemically. Consequently the pharmacokinetics of this drug have been studied after its administration by several different routes. Oral doses of benzydamine are apparently well absorbed and plasma drug concentrations reach a peak fairly rapidly (e.g. 0.8 micrograms/ml after a 100-mg dose) and then decline with a half-life of about 13 h. Less than 20% of the drug is bound to plasma proteins. Assuming complete oral systemic availability, values of 193 ml/min and 213 litres respectively were calculated for the systemic clearance and volume of distribution of benzydamine. Cutaneous doses of benzydamine are more slowly absorbed and lead to peak drug levels about three-fold lower, but more persistent than those after oral administration. Although local drug concentrations are relatively large, the systemic absorption of mouthwash-gargle, vaginal and rectal doses of benzydamine is relatively low compared to oral doses: this lower absorption should greatly diminish the potential for any systemic drug side-effects when benzydamine is administered by these routes. Benzydamine is metabolized primarily by oxidation, conjugation and dealkylation.

摘要

在临床上,苄达明可在局部或全身发挥作用。因此,已经通过几种不同途径给药后研究了该药物的药代动力学。苄达明口服剂量显然吸收良好,血浆药物浓度相当迅速地达到峰值(例如,100毫克剂量后为0.8微克/毫升),然后以约13小时的半衰期下降。不到20%的药物与血浆蛋白结合。假设口服全身可用性完全,苄达明的全身清除率和分布容积分别计算为193毫升/分钟和213升。苄达明经皮肤给药吸收较慢,导致药物峰值水平比口服给药低约三倍,但比口服给药更持久。尽管局部药物浓度相对较高,但与口服剂量相比,苄达明漱口水、阴道和直肠剂量的全身吸收相对较低:当通过这些途径给药苄达明时,这种较低的吸收应大大降低任何全身性药物副作用的可能性。苄达明主要通过氧化、结合和脱烷基化进行代谢。

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F1000Res. 2025 May 22;13:350. doi: 10.12688/f1000research.144067.2. eCollection 2024.
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Pharmacology of benzydamine.苯扎氯铵的药理学。
Inflammopharmacology. 1998;6(2):95-107. doi: 10.1007/s10787-998-0026-0.
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Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms on enzyme activity.苄达明N-氧化作为反映人肝微粒体中FMO活性的指标反应以及FMO3基因多态性对酶活性的影响。
Br J Clin Pharmacol. 2000 Dec;50(6):553-61. doi: 10.1046/j.1365-2125.2000.00296.x.
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Pharmacokinetics of benzydamine in dairy cows following intravenous or intramuscular administration.苄达明在奶牛静脉注射或肌肉注射后的药代动力学
Vet Res Commun. 1993;17(4):313-23. doi: 10.1007/BF01839222.