Grapefruit Juice–Drug Interactions: Grapefruit Juice and Its Components Inhibit P‐Glycoprotein (ABCB1) Mediated Transport of Talinolol in Caco‐2 Cells

2007 ◽  
Vol 96 (10) ◽  
pp. 2808-2817 ◽  
Author(s):  
Whocely Victor de Castro ◽  
Susanne Mertens‐Talcott ◽  
Hartmut Derendorf ◽  
Veronika Butterweck
2021 ◽  
Vol 31 (4) ◽  
pp. 44-51
Author(s):  
A.P. Pereverzev ◽  
O.D. Ostroumova

Any drug can potentially cause adverse drug reactions (ADRs), including serious and fatal. Some of them are caused by interactions with food, in particular, fruit and berry juices. Juices have a complex chemical composition and each of the chemicals can interact with drugs. Grapefruit juice is one of the most popular and well-studed in terms of potential drug interactions juices. Grapefruit juice is an inhibitor of CYP3A enzymes in the intestine involved in the presystemic metabolism of drug substrates. Therefore, it can increase their absorption. Apple juice at a concentration of 5% significantly reduces the activity of OATP, but not the activity of P-glycoprotein, which, for example, leads to a decrease in AUC and Cmax of fexofenadine to 30- 40% relative to the concentration of fexofenadine in patients drinking only water. Taking 200 ml of grape juice can reduce the concentration of phenacetin in blood plasma and increase the ratio of AUC of paracetamol to phenacetin due to the induction of CYP1A2 activity by grape juice flavonoids or by reducing the rate of absorption of phenacetin. To prevent ADRs, it is recommended to take drugs with water and and not consume simultaneously juices that are known to interact with drugs.


Author(s):  
Taiji Miyake ◽  
Haruka Tsutsui ◽  
Kenta Haraya ◽  
Tatsuhiko Tachibana ◽  
Kayoko Morimoto ◽  
...  

2006 ◽  
Vol 26 (11) ◽  
pp. 1601-1607 ◽  
Author(s):  
Carol W Holtzman ◽  
Barbara S Wiggins ◽  
Sarah A Spinler

Author(s):  
Chetan S. Karyekar ◽  
Natalie D. Eddington ◽  
Tushar S. Garimella ◽  
Paul O. Gubbins ◽  
Thomas C. Dowling

2007 ◽  
Vol 81 (5) ◽  
pp. 631-633 ◽  
Author(s):  
B J Kirby ◽  
J D Unadkat

2021 ◽  
Vol 22 ◽  
Author(s):  
Rajkapoor Balasubramanian ◽  
Naina Mohamed Pakkir Maideen

Background: Hydroxymethyl glutaryl-CoA (HMG-CoA) reductase inhibitors (Statins) are used to treat dyslipidemia. Generally, the statins are the substrates of CYP enzymes, P-glycoprotein (P-gp), and organic anion transporting polypeptides transporters (OATP1B1). Objective: This review article focuses on the clinical significance of statins, and their interactions in real practice. Method: The databases like Medline/PubMed Central/PubMed, Google Scholar, Science Direct, Cochrane Library, Directory of open access journals (DOAJ), and reference lists were searched to identify relevant articles. Results: Most of the drug interactions of statins result in elevated plasma concentrations and toxicity of statins due to the inhibition of CYP3A4, P-gp and/or OATP1B1 transporters. The toxicity of statins includes myopathy, rhabdomyolysis, elevated liver enzymes, acute kidney injury, and diabetes. The statins like Simvastatin, Lovastatin, and Atorvastatin are substrates of CYP3A4 enzyme and P-glycoprotein and their concomitant use with the drugs inhibiting or inducing them would result in changes in plasma concentrations and toxicity/efficacy. However, the statins like Pravastatin, Rosuvastatin and Pitavastatin are not substrates of CYP enzymes and hence the concomitant use of CYP inhibitors or inducers do not affect them. Almost all the statins are the substrates of OATP1B1 transporter, and the co-prescription of inhibitors of OATP1B1 elevates the plasma concentrations and muscle toxicity of statins. Conclusion: Understanding the interacting potential of each statin will enable the prescribers, pharmacists, and other health care professionals to use statins effectively without compromising patient safety.


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