|
1
|
Biedrzycki G, Wolszczak-Biedrzycka B, Dorf J, Michalak D, Żendzian-Piotrowska M, Zalewska A, Maciejczyk M. Antioxidant and Anti-Glycation Potential of H2 Receptor Antagonists-In Vitro Studies and a Systematic Literature Review. Pharmaceuticals (Basel) 2023; 16:1273. [PMID: 37765081 PMCID: PMC10535796 DOI: 10.3390/ph16091273] [Citation(s) in RCA: 0] [Impact Index Per Article: 0] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Received: 07/19/2023] [Revised: 09/05/2023] [Accepted: 09/06/2023] [Indexed: 09/29/2023] Open
Abstract
Background: Histamine H2 receptor antagonists are a group of drugs that inhibit gastric juice secretion in gastrointestinal diseases. However, there is evidence to suggest that H2 blockers have a broader spectrum of activity. The antioxidant properties of H2 blockers have not been fully elucidated, and their anti-glycation potential has not been studied to date. Therefore, this is the first study to compare the antioxidant and antiglycation potentials of the most popular H2 antagonists (ranitidine, cimetidine, and famotidine) on protein glycoxidation in vitro. Methods: Bovine serum albumin (BSA) was glycated using sugars (glucose, fructose, galactose, and ribose) as well as aldehydes (glyoxal and methylglyoxal). Results: In the analyzed group of drugs, ranitidine was the only H2 blocker that significantly inhibited BSA glycation in all tested models. The contents of protein carbonyls, protein glycoxidation products (↓dityrosine, ↓N-formylkynurenine), and early (↓Amadori products) and late-stage (↓AGEs) protein glycation products decreased in samples of glycated BSA with the addition of ranitidine relative to BSA with the addition of the glycating agents. The anti-glycation potential of ranitidine was comparable to those of aminoguanidine and Trolox. In the molecular docking analysis, ranitidine was characterized by the lowest binding energy for BSA sites and could compete with protein amino groups for the addition of carbonyl groups. H2 blockers also scavenge free radicals. The strongest antioxidant properties are found in ranitidine, which additionally has the ability to bind transition metal ions. The systematic literature review also revealed that the anti-glycation effects of ranitidine could be attributed to its antioxidant properties. Conclusions: Ranitidine showed anti-glycation and antioxidant properties. Further research is needed, particularly in patients with diseases that promote protein glycation.
Collapse
Affiliation(s)
- Grzegorz Biedrzycki
- Hospital Pharmacy, Provincial Specialist Hospital in Olsztyn, 10-900 Olsztyn, Poland
| | - Blanka Wolszczak-Biedrzycka
- Department of Psychology and Sociology of Health and Public Health, University of Warmia and Mazury in Olsztyn, 10-900 Olsztyn, Poland
| | - Justyna Dorf
- Department of Clinical Laboratory Diagnostics, Medical University of Bialystok, 15-089 Bialystok, Poland
| | - Daniel Michalak
- Students Scientific Club “Biochemistry of Civilization Diseases”, Department of Hygiene, Epidemiology and Ergonomics, Medical University of Bialystok, 15-089 Bialystok, Poland
| | | | - Anna Zalewska
- Experimental Dentistry Laboratory, Medical University of Bialystok, 15-089 Bialystok, Poland
| | - Mateusz Maciejczyk
- Department of Hygiene, Epidemiology and Ergonomics, Medical University of Bialystok, 15-089 Bialystok, Poland
| |
Collapse
|
|
2
|
Ciocalteu A, Popa P, Ionescu M, Gheonea DI. Issues and controversies in esophageal inlet patch. World J Gastroenterol 2019; 25:4061-4073. [PMID: 31435164 PMCID: PMC6700698 DOI: 10.3748/wjg.v25.i30.4061] [Citation(s) in RCA: 11] [Impact Index Per Article: 1.8] [Reference Citation Analysis] [Abstract] [Key Words] [MESH Headings] [Track Full Text] [Download PDF] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 03/12/2019] [Revised: 06/24/2019] [Accepted: 07/05/2019] [Indexed: 02/06/2023] Open
Abstract
The proximal esophagus is rarely examined, and its inspection is often inadequate. Optical chromoendoscopy techniques such as narrow band imaging improve the detection rate of inlet patches in the proximal esophagus, a region in which their prevalence is likely underestimated. Various studies have reported correlations between these esophageal marks with different issues such as Barrett's esophagus, but these findings remain controversial. Conflicting reports complicate the process of interpreting the clinical features of esophageal inlet patches and underestimate their importance. Unfortunately, the limited clinical data and statistical analyses make reaching any conclusions difficult. It is hypothesized that inlet patches are correlated with various esophageal and extraesophageal symptoms, diagnoses and the personalized therapeutic management of patients with inlet patches as well as the differential diagnosis for premalignant lesions or early cancers. Due to its potential underdiagnosis, there are no consensus guidelines for the management and follow up of inlet patches. This review focuses on questions that were raised from published literature on esophageal inlet patches in adults.
Collapse
Affiliation(s)
- Adriana Ciocalteu
- Department of Gastroenterology, Research Center of Gastroenterology and Hepatology, University of Medicine and Pharmacy of Craiova, Craiova 200349, Romania
| | - Petrica Popa
- Department of Gastroenterology, Research Center of Gastroenterology and Hepatology, University of Medicine and Pharmacy of Craiova, Craiova 200349, Romania
| | - Mircea Ionescu
- Department of Anesthesiology and Intensive Care, Emergency County Hospital of Craiova, Craiova 200642, Romania
| | - Dan Ionut Gheonea
- Department of Gastroenterology, Research Center of Gastroenterology and Hepatology, University of Medicine and Pharmacy of Craiova, Craiova 200349, Romania
| |
Collapse
|
|
3
|
Evaluation of rational nonsteroidal anti-inflammatory drugs and gastro-protective agents use; association rule data mining using outpatient prescription patterns. BMC Med Inform Decis Mak 2017; 17:96. [PMID: 28676124 PMCID: PMC5496643 DOI: 10.1186/s12911-017-0496-3] [Citation(s) in RCA: 11] [Impact Index Per Article: 1.4] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Journal Information] [Subscribe] [Scholar Register] [Received: 02/01/2017] [Accepted: 06/28/2017] [Indexed: 12/03/2022] Open
Abstract
Background Nonsteroidal anti-inflammatory drugs (NSAIDs) and gastro-protective agents should be co-prescribed following a standard clinical practice guideline; however, adherence to this guideline in routine practice is unknown. This study applied an association rule model (ARM) to estimate rational NSAIDs and gastro-protective agents use in an outpatient prescriptions dataset. Methods A database of hospital outpatients from October 1st, 2013 to September 30th, 2015 was searched for any of following drugs: oral antacids (A02A), peptic ulcer and gastro-oesophageal reflux disease drugs (GORD, A02B), and anti-inflammatory and anti-rheumatic products, non-steroids or NSAIDs (M01A). Data including patient demographics, diagnoses, and drug utilization were also retrieved. An association rule model was used to analyze co-prescription of the same drug class (i.e., prescriptions within A02A-A02B, M01A) and between drug classes (A02A-A02B & M01A) using the Apriori algorithm in R. The lift value, was calculated by a ratio of confidence to expected confidence, which gave information about the association between drugs in the prescription. Results We identified a total of 404,273 patients with 2,575,331 outpatient visits in 2 fiscal years. Mean age was 48 years and 34% were male. Among A02A, A02B and M01A drug classes, 12 rules of associations were discovered with support and confidence thresholds of 1% and 50%. The highest lift was between Omeprazole and Ranitidine (340 visits); about one-third of these visits (118) were prescriptions to non-GORD patients, contrary to guidelines. Another finding was the concomitant use of COX-2 inhibitors (Etoricoxib or Celecoxib) and PPIs. 35.6% of these were for patients aged less than 60 years with no GI complication and no Aspirin, inconsistent with guidelines. Conclusions Around one-third of occasions where these medications were co-prescribed were inconsistent with guidelines. With the rapid growth of health datasets, data mining methods may help assess quality of care and concordance with guidelines and best evidence.
Collapse
|
|
4
|
Flach S, Croft M, Ding J, Budhram R, Pankratz T, Pennick M, Scarfe G, Troy S, Getsy J. Pharmacokinetics, absorption, and excretion of radiolabeled revexepride: a Phase I clinical trial using a microtracer and accelerator mass spectrometry-based approach. DRUG DESIGN DEVELOPMENT AND THERAPY 2016; 10:3125-3132. [PMID: 27729771 PMCID: PMC5045912 DOI: 10.2147/dddt.s107843] [Citation(s) in RCA: 3] [Impact Index Per Article: 0.3] [Reference Citation Analysis] [Abstract] [Key Words] [Track Full Text] [Download PDF] [Figures] [Subscribe] [Scholar Register] [Indexed: 01/10/2023]
Abstract
Purpose Gastroesophageal reflux disease involves the reflux of gastric and/or duodenal content into the esophagus. Prokinetic therapies, such as the selective 5-hydroxytryptamine receptor 4 agonist revexepride, may aid gastric emptying. This Phase I study evaluated the pharmacokinetics and excretion pathways of [14C]revexepride in healthy individuals using a microtracer approach with accelerator mass spectrometry. Participants and methods Six healthy men received a single oral dose of 2 mg [14C]revexepride containing ~200 nCi of radioactivity; blood, urine, and fecal samples were collected over a 10-day period. Results Almost 100% of 14C was recovered: 38.2%±10.3% (mean ± standard deviation) was recovered in urine, and 57.3%±0.4% was recovered in feces. Blood cell uptake was low, based on the blood plasma total radioactivity ratio of 0.8. The mean revexepride renal clearance was 8.6 L/h, which was slightly higher than the typical glomerular filtration rate in healthy individuals. Time to reach maximal concentration was 1.75±1.17 hours (mean ± standard deviation). No safety signals were identified. Conclusion This study demonstrated that revexepride had rapid and moderate-to-good oral absorption. Excretion of radioactivity was completed with significant amounts in feces and urine. Renal clearance slightly exceeded the typical glomerular filtration rate, suggesting the involvement of active transportation in the renal tubules.
Collapse
Affiliation(s)
| | | | - Jie Ding
- Covance Laboratories Inc., Madison, WI, USA
| | | | | | | | | | | | | |
Collapse
|
|
5
|
Paulino N, Coutinho LA, Coutinho JR, Vilela GC, Silva Leandro VPD, Paulino AS. Antiulcerogenic Effect of Brazilian Propolis Formulation in Mice. ACTA ACUST UNITED AC 2015. [DOI: 10.4236/pp.2015.612060] [Citation(s) in RCA: 12] [Impact Index Per Article: 1.2] [Reference Citation Analysis] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/20/2022]
|
|
6
|
Fändriks L, Lönroth H, Pettersson A, Vakil N. Can famotidine and omeprazole be combined on a once-daily basis? Scand J Gastroenterol 2007; 42:689-94. [PMID: 17505990 DOI: 10.1080/00365520601026665] [Citation(s) in RCA: 13] [Impact Index Per Article: 0.7] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Indexed: 02/04/2023]
Abstract
OBJECTIVE Prompt and long-standing acid control following once-daily administration of antisecretory drugs is desirable. The objective of this study was to determine whether co-administration of a well-characterized H2-receptor antagonist, famotidine, can be combined with the proton-pump inhibitor omeprazole. MATERIAL AND METHODS Intragastric 24-h pH-metry was performed in healthy, Helicobacter pylori-negative volunteers on day 1 and after 8 days of daily administration of 20 mg omeprazole, 10 mg famotidine, or a combination of these in a three-way crossover design. RESULTS A combination of famotidine and omeprazole raised the gastric pH level to >4 in less than 1 h. The percentage of daytime with pH > 4 on day 1 was significantly higher with the combination of omeprazole and famotidine (median: 37%) than that with omeprazole alone (22%; p < 0.05). On day 8, daytime intragastric pH > 4 following treatment with omeprazole (median: 55%) or a combination of omeprazole and famotidine (61%) was superior (p < 0.05) to that with famotidine (21%). On day 1 treatment with both famotidine and the combination (famotidine and omeprazole) showed a significantly shorter time to reach a pH of 4 (medians: 93 and 63 min, respectively) compared with treatment with omeprazole alone (173 min; p < 0.05). CONCLUSIONS Compared with treatment with omeprazole alone, on day 1 famotidine and omeprazole in combination improved the duration of and time to reach intragastric pH > 4. With regard to duration with pH > 4, the combination therapy was superior to famotidine alone on day 8. The rapid acid control with an H2-receptor antagonist may be combined with the long-lasting antisecretory effect of a proton-pump inhibitor.
Collapse
Affiliation(s)
- Lars Fändriks
- Department of Gastrosurgical Research, Sahlgrenska University Hospital, Gothenburg, Sweden.
| | | | | | | |
Collapse
|
|
7
|
Stein J, Rösch W. H2-Blocker und Antazida bei gastrointestinalen Erkrankungen. Erfolgreiche Therapie von Ulcusleiden? ACTA ACUST UNITED AC 2007; 36:38-43. [PMID: 17283749 DOI: 10.1002/pauz.200600203] [Citation(s) in RCA: 1] [Impact Index Per Article: 0.1] [Reference Citation Analysis] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/09/2022]
Affiliation(s)
- Jürgen Stein
- Medizinische Klinik-ZAFES, J.W. Goethe-Universität Frankfurt.
| | | |
Collapse
|
|
8
|
Scagliarini R, Magnani E, Praticò A, Bocchini R, Sambo P, Pazzi P. Inadequate use of acid-suppressive therapy in hospitalized patients and its implications for general practice. Dig Dis Sci 2005; 50:2307-11. [PMID: 16416179 DOI: 10.1007/s10620-005-3052-4] [Citation(s) in RCA: 29] [Impact Index Per Article: 1.5] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Submit a Manuscript] [Subscribe] [Scholar Register] [Received: 03/04/2005] [Accepted: 04/12/2005] [Indexed: 01/17/2023]
Abstract
Acid-suppressive therapy (AST) is largely prescribed in both hospital and general practice setting but few data are available on appropriateness of AST use in hospitalized patients and its fallout on prescribing in general practice. We assessed AST in patients consecutively admitted to an internal medicine department to determine the type and timing of prescription and indication for use according to widely accepted guidelines. Prescriptions were rated as indicated, acceptable, or not indicated. Overall, 58.7% of 834 admitted patients received AST, mainly proton pump inhibitors. The prescriptions were indicated in 50.1% of patients, not indicated in 41.5%, and acceptable in 6.5%. The main reason for inappropriate use was prophylaxis in low-risk patients (64.8%). On admission, 35.7% of 112 patients already on AST were judged to receive inappropriate prescription; of 348 patients discharged on AST, overuse was identified in 38.5%. No significant difference was observed for inappropriate use at admission, during hospitalization, and at discharge. In 64 inpatients (7.7%) AST, although indicated, mainly for ulcer prophylaxis in high-risk patients, was not prescribed. In conclusion, AST is substantially over-used in both hospital and general practice settings, mainly for ulcer prophylaxis in low-risk patients. On the other hand, AST is underused in a small, but not negligible proportion of high-risk patients.
Collapse
|
|
9
|
Cross LB, Justice LN. Combination drug therapy for gastroesophageal reflux disease. Ann Pharmacother 2002; 36:912-6. [PMID: 11978171 DOI: 10.1345/aph.10247] [Citation(s) in RCA: 9] [Impact Index Per Article: 0.4] [Reference Citation Analysis] [Abstract] [MESH Headings] [Track Full Text] [Journal Information] [Subscribe] [Scholar Register] [Indexed: 11/27/2022] Open
Abstract
OBJECTIVE To evaluate the role of combination therapy with proton-pump inhibitors (PPIs) and histamine(2) receptor antagonists in gastroesophageal reflux disease (GERD). DATA SOURCES Clinical literature identified through MEDLINE (January 1966-August 2001). Key search terms included gastroesophageal reflux, benzimidazoles; omeprazole; lansoprazole; pantoprazole; rabeprazole; receptor antagonists, histamine(2); therapy, combination drug; therapy, combined modality; and combinations, drug. DATA SYNTHESIS Approximately 80-90% of patients show healing of reflux esophagitis after 8 weeks of once-daily PPI therapy. Patients taking PPI therapy twice daily still have nocturnal acid breakthrough (periods of gastric pH <4 lasting for > or =60 min during the night) as much as 70% of the time. The clinical application of this finding has not been shown. One trial has shown that omeprazole in the morning plus ranitidine at bedtime is not as effective as omeprazole twice daily given before the morning and evening meals at controlling nocturnal acid breakthrough. Further, 1 small trial in healthy subjects without GERD showed that the addition of a 1-time dose of ranitidine at bedtime to a twice-daily regimen of omeprazole may decrease the occurrence of nocturnal acid breakthrough. However, the clinical significance of this finding is not clear. CONCLUSIONS No studies in patients with GERD demonstrate that the addition of histamine(2) receptor antagonists to twice-daily PPI therapy provides any further benefit above that derived from PPIs alone. The parameter used to measure the efficacy of combination regimens for GERD thus far--nocturnal acid breakthrough--has not been proven to correlate with improvement of GERD symptoms in any controlled or prospective clinical trials. Further investigation is needed to determine optimal therapy in patients refractory to standard doses of PPIs.
Collapse
Affiliation(s)
- L Brian Cross
- Department of Pharmacy Practice & Pharmacoeconomics, College of Pharmacy, University of Tennessee, 847 Monroe Avenue, Suite 205 C, Memphis, TN 38163-2109, USA.
| | | |
Collapse
|