Information on level of drugs into breastmilk
Wendy Jones in Breastfeeding and Medication, 2018
There are no data on the transfer of rabeprazole into breastmilk although animal studies suggest a high m/p ratio. The relevance to humans is unclear. It is 97% plasma protein bound and it is extensively metabolised in the liver by cytochrome P450 and undergoes degradation by stomach acid if not enteric coated. It also undergoes firstpass metabolism. Rabeprazole is only 52% bio-available in adults even when enteric coated due to its instability in gastric acids. Any present in milk would be virtually destroyed in the infant’s stomach prior to absorption. These factors suggest it should be compatible with breastfeeding although other safer options with more safety data on use in lactation exist. The BNF states that the manufacturer advises it should be avoided as there is no information available on the amount secreted into breastmilk.
Sitafloxacin
M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson in Kucers’ The Use of Antibiotics, 2017
A Japanese study assessed the efficacy of a sitafloxacin-based regime in 180 H. pylori–positive Japanese patients as first-line treatment (n = 45), second-line (n = 41), and third-line therapy (n = 94) (Sugimoto et al., 2015). The regimen was sitafloxacin 100 mg twice daily + rabeprazole 10 mg qid + metronidazole 250 mg twice daily for 7 days. Eradication was assessed by 13C urea breath test 8 weeks post-treatment. The overall efficacy of treatment was 92.2% (166/180) in ITT analyses, with rate of eradication varying by order of therapy: first-line 100% (45/45), second-line 92.7% (38/41), and third-line therapy 88.3% (83/94). Rates of eradication did not vary by metronidazole resistance pattern (susceptible 96.6% [28/29] vs. resistant 96.3% [77/80], p = 0.94). The authors concluded that sitafloxacin-based treatment, regardless of eradication history or metronidazole resistance status, was effective. Similarly, others have found sitafloxacin to be an effective third-line treatment option when used as part of a triple-therapy–based regimen (Murakami et al., 2013; Furuta et al., 2014; Mori et al., 2016).
Gastrointestinal diseases and pregnancy
Hung N. Winn, Frank A. Chervenak, Roberto Romero in Clinical Maternal-Fetal Medicine Online, 2021
PPIs effectively suppress gastric acid secretion by inhibiting the H+/K+ ATPase on the surface of the parietal cell. PPIs are highly effective in the treatment of PUD. Omeprazole is rated as category C during pregnancy because of embryotoxicity without teratogenicity in animal studies (19). All other PPIs, including lansoprazole, rabeprazole, pantoprazole, and esomeprazole, are classified as FDA pregnancy category B drugs. Lansoprazole is the preferred PPI during pregnancy because of lack of clinical data regarding the safety of newer PPIs. Treatment with PPIs during pregnancy should be reserved only for patients with refractory or complicated PUD, which does not respond to alternative medical therapies, including H2RAs.
Identification and genotoxicity evaluation of potential impurities in rabeprazole sodium using in silico and in vitro analyses
Published in Drug and Chemical Toxicology, 2022
Yi Du, Yinnan Wu, Yang Liu, Changhong Meng, Li Tan, Tiantian Cai, Yuxin Wang, Yihong Lu
Cumulative assays suggest that drugs for the treatment of gastroesophageal diseases may exert genotoxic and mutagenic effects. It has been reported that almost all prazoles (lansoprazole, omeprazole, pantoprazole, and rabeprazole) can induce chromosomal damages (Giovanni et al.2010, Paz et al.2020). Rabeprazole sodium, with a chemical formula of 2-[[[4-(3-methoxypropoxy)-3-methyl-2-pyri-dinyl] methyl sulfinyl]-1H-benzimidazole sodium salt, is extensively used for the treatment of duodenal ulcers, gastric ulcers, Zollinger–Ellison syndrome, anastomotic ulcer, and gastroesophageal reflux syndrome (Robinson and Horn 2003, NLM 2020a, Frazzoni et al.2017). Several analytical methods for the identification of rabeprazole sodium and its impurities have been reported (Reddy et al.2007, Rao et al.2010, Yenugu et al.2018). These impurities may originate from the active pharmaceutical ingredients or during the manufacturing and storage processes. However, only few studies have discussed the genotoxicity of impurities in rabeprazole and set a limit for these impurities (Yenugu et al. 2018). In the study, they only quantified the known genotoxic impurities, but not evaluate the genotoxicity of other impurities in rabeprazole.
Stereoselective and nonstereoselective pharmacokinetics of rabeprazole – an overview
Published in Xenobiotica, 2018
Ranjeet Prasad Dash, Rana Rais, Nuggehally R. Srinivas
Since rabeprazole differentiates itself from the rest of the class of PPIs despite higher degree of structural resemblance, we were interested to put together a consolidated review on the various aspects of its clinical pharmacokinetic disposition including the consideration of stereoselective pharmacokinetics reported in humans. The review provides a comprehensive appraisal of absorption, distribution, metabolism and excretion aspects of rabeprazole both from a racemate and from a enantiomeric point of view with the available literature data. The pharmacokinetic data from various clinical studies including drug–drug interaction studies where rabeprazole is either a perpetrator drug or victim drug has been included in a tabular summary (Table 1). The discussion section provides the overall pharmacokinetic perspectives of the use of rabeprazole in the clinical therapy.
High plasma mycophenolate acid concentration in the early phase of induction therapy predicts good renal outcome in lupus nephritis
Published in Modern Rheumatology, 2020
Tomofumi Kiyokawa, Hironari Hanaoka, Harunobu Iida, Kana Ishimori, Yukiko Takakuwa, Takahiro Okazaki, Shoichi Ozaki, Kimito Kawahata
We prospectively enrolled 10 Japanese patients with biopsy-proven LN class III or IV according to the International Society of Nephrology/Renal Pathology Society (ISN/RPS) 2003 classification, who were hospitalized at St. Marianna University Hospital between April 2016 and October 2017. All the patients completed the 6-month observation during the induction phase. Patients were enrolled if they fulfilled all the following criteria: disease that met the American College of Rheumatology (ACR) classification criteria for SLE [10], no intake of drugs known to interact with MMF, including acyclovir, ganciclovir, metronidazole, cholestyramine [11], tacrolimus, cyclosporine [12,13], magnesium- or aluminium-containing antacid [14] and rifampicin [15], and not pregnant or breastfeeding [16]. Rabeprazole was used to prevent gastric ulcer with less influence on the blood concentration of MMF and orally taken at a dose of 10 mg once a day after breakfast [17]. The study protocol was approved by the local ethics committee (Approval No. 3423), and written informed consent was obtained from all the patients before the study began.
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