Effect of Portal Vein Ligation and Silymarin Treatment on Aspirin Metabolism and Disposition in Rats

Favari, Liliana; Soto, Claudia; Mourelle, Marisabel

doi:10.1002/(sici)1099-081x(199701)18:1<53::aid-bdd3>3.0.co;2-9

Cited by 7 publications

(2 citation statements)

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“…Leber and Man (1976) reported time‐dependent increases in total liver cytochrome P450 content in rats administered with silymarin 229 . Since that time, several other studies have analyzed the effect of silymarin or silybin on the expression of cytochrome P450 and P‐glycoprotein 192–195,198,203,230 . Recent studies also showed that anhydrosilychristin and silybin B can substantially decrease the expression of P‐glycoprotein and BCRP, but silybin A, 2,3‐dehydrosilybin (A, B, racemate), and silychristin A had no effect, while 2,3‐dehydrosilychristin only decreased the expression of BCRP 15,226 .…”

Section: Interactionsmentioning

confidence: 99%

“…The modulatory effect of silymarin on damaged livers is quite an interesting topic. Silymarin partly or almost completely normalized the pharmacokinetics of atorvastatin in rats with diabetes mellitus induced by streptozocin and the pharmacokinetics of acetylsalicylic acid in both cirrhotic rats evoked by the administration of carbon tetrachloride and in a rat model of portal hypertension 230,264,265 . On the other hand, the AUC of another compound from vastatin hypolipidemic group, pitavastatin, was increased in a rat model of nonalcoholic steatohepatitis when silymarin was given i.v 179 .…”

Section: Interactionsmentioning

confidence: 99%

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Systematic review of pharmacokinetics and potential pharmacokinetic interactions of flavonolignans from silymarin

Tvrdý

Pourová

Jirkovský

et al. 2021

Medicinal Research Reviews

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Silymarin is an extract from the seeds (fruits) of Silybum marianum that contains flavonolignans and flavonoids. Although it is frequently used as a hepatoprotective agent, its application remains somewhat debatable, in particular, due to the low oral bioavailability of flavonolignans. Moreover, there are claims of its potential interactions with concomitantly used drugs. This review aims at a systematic summary and critical assessment of known information on the pharmacokinetics of particular silymarin flavonolignans. There are two known major reasons for poor systemic oral bioavailability of flavonolignans: (1) rapid conjugation in intestinal cells or the liver and (2) efflux of parent flavonolignans or formed conjugates back to the lumen of the gastrointestinal tract by intestinal cells and rapid excretion by the liver into the bile. The metabolism of phase I appears to play a minor role, in contrast to extensive conjugation and indeed the unconjugated flavonolignans reach low plasma levels after common doses. Only about 1%–5% of the administered dose is eliminated by the kidneys. Many in vitro studies tested the inhibitory potential of silymarin and its components toward different enzymes and transporters involved in the absorption, metabolism, and excretion of xenobiotics. In most cases, effective concentrations are too high to be relevant under real biological conditions. Most human studies showed no silymarin–drug interactions explainable by these suggested interferences. More interactions were found in animal studies, likely due to the much higher doses administered.

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Section: Interactionsmentioning

confidence: 99%

Section: Interactionsmentioning

confidence: 99%