Effects of capsaicin on pharmacokinetics of pitavastatin in rats

  title={Effects of capsaicin on pharmacokinetics of pitavastatin in rats},
  author={Fen Chen and Xue-jia Zhai and Chao-ran Zhu and Yong-ning Lu},
  pages={171 - 176}
Abstract 1. Capsaicin (CAP) is the primary pungent principle in peppers and an inhibitor of CYP3A subfamily and P-gp. 2. Pitavastatin is mainly metabolized via glucuronidation and metabolism by hepatic CYPs is minimal. Pitavastatin is taken up by Oatp1b2 (encoded by Slco1b2) in rat. 3. The pharmacokinetics results showed that AUC and Cmax in the group pre-treated with 3 mg/kg/d CAP were increased by 1.2 fold and 1.6 fold; AUC and Cmax in the group pre-treated with 8 mg/kg/d CAP were increased… Expand
Food–drug interactions involving multiple mechanisms: A case study with effect of Capsaicin on the pharmacokinetics of Irinotecan and its main metabolites in rat
Abstract Capsaicin (CAP), the main ingredient of chili peppers, displays potent anti-tumor activity in several human cancers. Irinotecan, an anticancer agent with narrow therapeutic index, isExpand
Capsaicin pretreatment enhanced the bioavailability of fexofenadine in rats by P-glycoprotein modulation: in vitro, in situ and in vivo evaluation
Capsaicin pretreatment significantly enhanced the intestinal absorption and bioavailability of fexofenadine in rats likely by inhibition of P-gp mediated cellular efflux, suggesting that the combined use of capsaicin with P- gp substrates may require close monitoring for potential drug interactions. Expand
Effects of Phytochemical P-Glycoprotein Modulators on the Pharmacokinetics and Tissue Distribution of Doxorubicin in Mice
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Capsaicin: Current Understanding in Therapeutic Effects, Drug Interaction, and Bioavailability
Capsaicin (N-vanillyl-8-methyl-6-(E)-none amide) is a unique and significant compound from group component of capsaicinoids. This component can only be found in the plants from the Capsicum genus. ItExpand
Simultaneous determination of telmisartan and pitavastatin in rat plasma by UPLC-MS/MS: Application to pharmacokinetic interaction study.
The validated method was successfully applied to the PK study and the data did not reveal any evidence for the potential drug-drug interaction (DDI) between Tel andpitavastatin, and this information would provide the evidence for clinical rational use of Tel and Pit. Expand
Capsaicinoids enhance chemosensitivity to chemotherapeutic drugs.
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Food-drug interactions: effect of capsaicin on the pharmacokinetics of simvastatin and its active metabolite in rats.
Investigation of the pharmacokinetics of simvastatin (SV), a cytochrome P450 (CYP) 3A substrate and an important cholesterol-lowering agent, demonstrates that chronic ingestion of high doses of CAP will decrease the bioavailability of SV to a significant extent in rats. Expand
Capsaicin pretreatment increased the bioavailability of cyclosporin in rats: involvement of P-glycoprotein and CYP 3A inhibition.
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Influence of capsaicin on fluctuation of digoxin pharmacokinetics in lipopolysaccharide-treated rats
Cap decreased the absorption of digoxin by inducing CYP3A2 mRNA expression via indirect activation of PXR in LPS-treated rats by increasing the DNA-binding activity of pregnane X receptor on days 3–7 in the Cap and LPS + Cap group. Expand
Food–drug interactions: effect of capsaicin on the pharmacokinetics of galantamine in rats
It is demonstrated that the chronic ingestion of high doses of CAP will decrease the bioavailability of galantamine to a significant extent in rats and this study attempted to investigate the effect of CAP on the pharmacokinetics of Galantamine, a competitive and reversible cholinesterase inhibitor. Expand
Pharmacokinetics of pitavastatin in subjects with Child-Pugh A and B cirrhosis.
The plasma concentration of pitavastatin is increased in patients with liver cirrhosis, and caution is required, although dose reduction may not be necessary in Child-Pugh A Cirrhosis. Expand
Pitavastatin - pharmacological profile from early phase studies.
Pitavastatin has minimal drug-food and drug-drug interactions making it a treatment option in the large group of dyslipidaemic people that require multidrug therapy. Expand
Inhibition and induction of human cytochrome P450 enzymes in vitro by capsaicin
Capsaicin was evaluated in vitro against seven human drug-metabolizing cytochrome P450 (CYP) enzymes and effects on CYPs appear unlikely, given that exposure to capsaicin from either food or a topical medicine is very low and transient. Expand
Studies of the Toxicological Potential of Capsinoids, XIII: Inhibitory Effects of Capsaicin and Capsinoids on Cytochrome P450 3A4 in Human Liver Microsomes
Capsaicin was shown to inhibit cytochrome P450 3A4, probably through a mechanism-based inhibition of CYP3A4; in contrast, capsiate, dihydrocapsiate, and nordihydrocapsiates did not inhibit cy tochrome P 450 3A 4 activity and were unlikely to be mechanism- based inhibitors of CYB3A 4. Expand
Subchronic toxicity studies of capsaicin and capsicum in rats.
  • Y. Monsereenusorn
  • Chemistry, Medicine
  • Research communications in chemical pathology and pharmacology
  • 1983
It is concluded that capsaicin or capsicum, if given orally for a relatively longer period, may have a mild effect on the experimental animals. Expand
Involvement of BCRP (ABCG2) in the Biliary Excretion of Pitavastatin
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