Atorvastatin, simvastatin, and lovastatin are all included in the CYP3A4-substrate group despite the fact that inhibiting CYP3A4 by macrolides in healthy volunteers produced significant variation in exposure to these statins. In order to provide our website visitors and registered users with a service tailored to their individual preferences we use cookies to analyse visitor traffic and personalise content. In relation to macrolides' affinity for OATP1B3 using the same model, telithromycin showed the strongest inhibition in vitro with IC50 of 11 µM, while clarithromycin, erythromycin, and roxithromycin showed slightly similar affinities with IC50 of 32 µM, 34 µM, and 37 µM respectively. Compared with concomitant use of statins and penicillin V (52 events; IR, 5.3), however, we observed no increased risk (HR 0.93, 95% CI 0.58, 1.49).In this nationwide cohort study concomitant use of statins and macrolides was not associated with a significantly increased risk of serious renal events.These authors take responsibility for all aspects of the reliability and freedom from bias of the data presented and their discussed interpretation.We use cookies to help provide and enhance our service and tailor content and ads. Case reports suggest a drug interaction between statins and azithromycin in the development of rhabdomyolysis (11). This reduction in hepatic cholesterol synthesis is augmented by the induction of low-density lipoprotein (LDL) receptor expression which enhances the hepatic r… Die Interaktion betrifft zudem nicht alle Statine: Fluvastatin und Rosuvastatin werden hauptsächlich über CYP2… Those subjects were compared with statin users in the province prescribed another antibiotic, azithromycin, that does not block the liver enzyme the same way. Many of these inhibitors have a different affinity for CYP3A4 isoenzyme as well as the fact that many of them has different inhibitory effects on other transporters, eg, cyclosporine is a potent inhibitor of CYP3A4, P-gp, BCRP, and OATP1B1/1B3. Discuss with your cardiologist or physician the best course of action to take in regards to this … It is noteworthy to mention that from the 53 cases of rhabdomyolysis suspected to be due to azithromycin and statins combination mentioned by Strandell et al, in only three cases the reporters explicitly indicated that azithromycin was most likely to be the offending agent.The increased exposure of simvastatin, lovastatin, and atorvastatin when coadministered with clarithromycin, telithromycin, and erythromycin is evident, but the significance of this increased exposure to the development of muscle toxicity could not be established in real practice. Azithromycin does not inhibit CYP3A4 isoenzyme or is at least considered a very weak inhibitor, therefore the suspected interactions with statins could be a coincidental temporal relation. In relation to macrolides, clarithromycin, erythromycin, and telithromycin are the most offending agents, while roxithromycin has limited potential for this interaction and azithromycin appears to be safe to use with statins.The authors report no conflicts of interest in this work.The opinions expressed in all articles published here are those of the specific author(s), and do not necessarily reflect the views of Dove Medical Press Ltd or any of its employees.Dove Medical Press is part of Taylor & Francis Group, the Academic Publishing Division of Informa PLC The occurrence of each outcome in patients taking azithromycin plus a statin was compared with patients taking clarithromycin or erythromycin plus a statin. Doch Antibiotika bergen, auch wenn sie nur kurzfristig eingenommen werden, mitunter ein hohes Wechselwirkungspotential. Also, they reported 53 cases that involved azithromycin and statins, mostly simvastatin. The inhibitory effect of different macrolides on OATP1B1/1B3 transporters was evaluated in an in vitro model, the IC50 for each macrolide against OATP1B1 was 96 µM (clarithromycin), 121 µM (telithromycin), 153 µM (roxithromycin), and 217 µM (erythromycin). More than 90% of the renal clearance of pravastatin and rosuvastatin is mediated by OAT3 transporter which is responsible for their active removal from circulation.Assuming that macrolides inhibit the metabolism/clearance of statins, this may lead to increased patient exposure to statins. In line, a cohort study found concurrent use of clarithromycin and CYP3A4-metabolized statins to be associated with a doubled risk of hospitalization with rhabdomyolysis or other statin-related adverse events as compared with azithromycin-statin co-administration. Azithromycin has previously been reported to increase the bioavailability of ivermectin, a substrate for the transporter P‐glycoprotein and CYP3A4 39 . So ist beispielsweise die Interaktion zwischen Statinen und Makrolid-Antibiotika in vielen Fällen relevant.Zu den Makrolid- bzw. Among the macrolide antibiotics, azithromycin has the least risk of adverse events when co-administered with statins (12).