Carbapenem antibiotics inhibit valproic acid transport in Caco-2 cell monolayers

Torii, Mayumi; Takiguchi, Yoshiharu; Izumi, Miyako; Fukushima, Tokuya; Yokota, Masayuki

doi:10.1016/s0378-5173(01)00916-4

Cited by 38 publications

(17 citation statements)

References 10 publications

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“…Inhibition of multidrug resistance-related protein 1 and/or canalicular multispecific organic anion transporter 2 by RIF is therefore expected to result in decreased bioavailability of CLR (Oswald et al, 2006;Giacomini et al, 2010). In addition, there exists evidence that basolateral transporters have an impact on the absorption of orally administered drugs (Torii et al, 2002). To discover intestinal uptake carriers for macrolides, further research particularly directed toward efflux transporters in the basolateral membrane of enterocytes is needed.…”

Section: Discussionmentioning

confidence: 99%

Clarithromycin Is Absorbed by an Intestinal Uptake Mechanism That Is Sensitive to Major Inhibition by Rifampicin: Results of a Short-Term Drug Interaction Study in Foals

Peters¹,

Eggers²,

Oswald³

et al. 2011

Drug Metab Dispos

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ABSTRACT:Pulmonary penetration of clarithromycin (CLR) in epithelial lining fluid (ELF) and bronchoalveolar lavage cells (BALCs) can be influenced by CYP3A4, by P-glycoprotein, and, according to our hypothesis, by a member of the organic anion-transporting protein (OATP) family, for which rifampicin (RIF) is inhibiting in single doses but inducing after long-term coadministration. To assess the partial inhibitory effect, we measured absorption and pulmonary distribution of CLR after short-term (2.5-day) coadministration of RIF, after which up-regulation is not expected. The drug interaction study was performed with five doses (12-h interval) of CLR (7.5 mg/kg) and RIF (10 mg/kg) in nine healthy foals; horse transporters are very similar in protein sequence and transcriptional regulation to the human analogs. RIF was equally distributed in ELF but reached half the plasma levels in BALCs. The deacetylated metabolite accumulated 1.4-to 6-fold in ELF and 8-to 60-fold in BALCs. CLR did not significantly influence the distribution of RIF. CLR and 14-hydroxyclarithromycin (14OH-CLR) accumulated approximately

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Section: Discussionmentioning

confidence: 99%

Clarithromycin Is Absorbed by an Intestinal Uptake Mechanism That Is Sensitive to Major Inhibition by Rifampicin: Results of a Short-Term Drug Interaction Study in Foals

Peters¹,

Eggers²,

Oswald³

et al. 2011

Drug Metab Dispos

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“…Since carbapenems are very slightly lipophilic and are hardly absorbed from the gastrointestinal tract when administered orally (20), no non-prodrug carbapenems are being developed for use as oral therapy. Based on our previous study of a suitable series of ester prodrug, we selected medoxomil ester, because of good oral absorption and the risk of formaldehyde generation from a pivoxil ester (21), although pivoxil esters of 2-aryl carbapenems also showed good oral absorption.…”

Section: Resultsmentioning

confidence: 99%

Novel Carbapenem Antibiotics for Parenteral and Oral Applications: In Vitro and In Vivo Activities of 2-Aryl Carbapenems and Their Pharmacokinetics in Laboratory Animals

Fujimoto

Koji

Hatano

et al. 2013

Antimicrob Agents Chemother

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b SM-295291 and SM-369926 are new parenteral 2-aryl carbapenems with strong activity against major causative pathogens of community-acquired infections such as methicillin-susceptible Staphylococcus aureus, Streptococcus pneumoniae (including penicillin-resistant strains), Streptococcus pyogenes, Enterococcus faecalis, Klebsiella pneumoniae, Moraxella catarrhalis, Haemophilus influenzae (including ␤-lactamase-negative ampicillin-resistant strains), and Neisseria gonorrhoeae (including ciprofloxacin-resistant strains), with MIC 90 s of <1 g/ml. Unlike tebipenem (MIC 50 , 8 g/ml), SM-295291 and SM-369926 had no activity against hospital pathogens such as Pseudomonas aeruginosa (MIC 50 , >128 g/ml). The bactericidal activities of SM-295291 and SM-369926 against penicillin-resistant S. pneumoniae and ␤-lactamase-negative ampicillin-resistant H. influenzae were equal or superior to that of tebipenem and greater than that of cefditoren. The therapeutic efficacies of intravenous administrations of SM-295291 and SM-369926 against experimentally induced infections in mice caused by penicillin-resistant S. pneumoniae and ␤-lactamase-negative ampicillin-resistant H. influenzae were equal or superior to that of tebipenem and greater than that of cefditoren, respectively, reflecting their in vitro activities. SM-295291 and SM-369926 showed intravenous pharmacokinetics similar to those of meropenem in terms of half-life in monkeys (0.4 h) and were stable against human dehydropeptidase I. SM-368589 and SM-375769, which are medoxomil esters of SM-295291 and SM-369926, respectively, showed good oral bioavailability in rats, dogs, and monkeys (4.2 to 62.3%). Thus, 2-aryl carbapenems are promising candidates that show an ideal broad spectrum for the treatment of community-acquired infections, including infections caused by penicillin-resistant S. pneumoniae and ␤-lactamase-negative ampicillin-resistant H. influenzae, have low selective pressure on antipseudomonal carbapenem-resistant nosocomial pathogens, and allow parenteral, oral, and switch therapies.

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“…Some mechanisms have been proposed for the pharmacokinetic interaction between carbapenem antibiotics and VPA 9–14. They include the suppression of enterohepatic recirculation of VPA by a decrease in the number of enteric bacteria,9 enhancement of glucuronidation of VPA as well as the suppression of VPA glucuronide hydrolysis in the liver,10–13 and direct suppression of the intestinal absorption of VPA at the basolateral membrane by carbapenem antibiotics 13,14…”

Section: Discussionmentioning

confidence: 99%

“…At present, the concomitant use of carbapenem antibiotics with VPA is prohibited in Japan. Regarding the pharmacokinetic interactions between carbapenem antibiotics and VPA, several mechanisms have been proposed focusing on the absorption process of VPA including its enterohepatic recirculation or on the enhanced hepatic metabolism of VPA 9–14. However, further study is necessary to explain the mechanism of the interaction, because the pharmacokinetic interaction between carbapenem antibiotics and VPA is observed relatively rapidly even after the intravenous administration.…”

Section: Introductionmentioning

confidence: 99%

Increased erythrocyte distribution of valproic acid in pharmacokinetic interaction with carbapenem antibiotics in rat and human

Omoda

Murakami

Yumoto

et al. 2005

Journal of Pharmaceutical Sciences

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Carbapenem antibiotics inhibit valproic acid transport in Caco-2 cell monolayers

Cited by 38 publications

References 10 publications

Clarithromycin Is Absorbed by an Intestinal Uptake Mechanism That Is Sensitive to Major Inhibition by Rifampicin: Results of a Short-Term Drug Interaction Study in Foals

Clarithromycin Is Absorbed by an Intestinal Uptake Mechanism That Is Sensitive to Major Inhibition by Rifampicin: Results of a Short-Term Drug Interaction Study in Foals

Novel Carbapenem Antibiotics for Parenteral and Oral Applications: In Vitro and In Vivo Activities of 2-Aryl Carbapenems and Their Pharmacokinetics in Laboratory Animals

Increased erythrocyte distribution of valproic acid in pharmacokinetic interaction with carbapenem antibiotics in rat and human

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