Tragopogon coelesyriacus is a traditional herbal medicine used for gastrointestinal disorders, mediated by its phytoconstituents. This study explores acute toxicity and gastroprotective potency of methanolic extracts of Tragopogon coelesyriacus (METC) in rats. Rats were aligned in 5 groups and pretreated with either normal saline, lansoprazole, or METC (200 and 400 mg/kg) before 5 mL/kg ethanol-induced gastric ulceration. The two-week toxicity study for METC (2 and 5 g/kg) showed no physiological alterations, behavioral changes, or morbidity in rats. Pretreatment with METC (200 and 400 mg/kg) improved gastric defense factors (mucus secretion and total stomach acidity), limiting mucosal penetrations and the lesioned areas. The histopathological results showed that METC (200 and 400 mg/kg) suppressed ethanol-induced gastric tissue alterations, indicated by increased gastric protective percentages (51.02% and 65.67%), less submucosal edema, epithelial exfoliation, lower mucous metaplasia, and necrotic areas. METC supplementation (200 and 400 mg/kg) restored the level of superoxide dismutase and catalase, while reducing the MDA by 29.84% and 48.64%, respectively. This was parallel with the anti-inflammatory effects of METC (200 and 400 mg/kg), decreasing TNF-α by 34.59%, 47.36%; IL-6 by 24.95%, 30.32%, and increasing IL-10 by 73.94%, 179.92%, respectively, relative to ulcer controls. Additionally, METC (200 and 400 mg/kg) remarkably modulated apoptotic proteins, lowering Bax by 31.10% and 45.50%, and increasing HSP 70 by 28.12 and 65.5%, respectively. The outcomes highlight the significant gastroprotective potential of Tragopogon coelesyriacus, which was mainly associated with its antioxidant, anti-inflammatory, and anti-apoptosis properties, making it a viable source for gastric ulcer management.

Gastric acid is essential for digestion, host defense, and maintenance of gastrointestinal homeostasis; however, its excessive or inappropriate secretion contributes to the development and progression of several acid-related disorders. Proton pump inhibitors (PPIs) have remained the cornerstone of acid-suppressive therapies for more than four decades owing to their potent blockade of gastric H[+]/K[+]-ATPases. This review provides a comprehensive overview of the pharmacological properties, clinical applications, and current limitations of the most widely used PPIs, including omeprazole, esomeprazole, lansoprazole, dexlansoprazole, pantoprazole, and rabeprazole. Particular emphasis is placed on their role in the management of Helicobacter pylori infection, a strong risk factor for the development of severe gastric diseases and one of the most clinically important indications for PPI-based antibiotic therapy. Beyond elevating intragastric pH to enhance antibiotic stability and efficacy, accumulating evidence indicates that PPIs exert direct antibacterial activity against H. pylori and may act synergistically with selected antibiotics. The review also discusses emerging evidence for interindividual variability in PPI metabolism, drug-drug interactions, and concerns regarding long-term adverse effects of the current treatments. Finally, it highlights potassium-competitive acid blockers (P-CABs), a newer class of acid-suppressive agents that provide sustained acid inhibition and represent a promising alternative to PPI-based regimens for H. pylori eradication.

The concomitant use of ceftriaxone and proton pump inhibitors (PPIs) is common in hospital practice. However, it is unclear whether individual PPIs differ in their effects on QT interval prolongation, ventricular arrhythmia, or cardiac arrest, collectively termed as QVC events. We conducted a two-stage, real-world study. First, we screened the United States Food and Drug Administration Adverse Event Reporting System (FAERS) and the Canada Vigilance Adverse Reaction (CVAR) database with standard disproportionality measures (reporting odds ratio and proportional reporting ratio) and six drug-drug interaction (DDI) algorithms to identify combination signals that exceeded component signals. Second, we validated signal-positive combinations in the Medical Information Mart for Intensive Care IV (MIMIC-IV) intensive care unit (ICU) electronic health record (EHR) cohort by assembling adult inpatients with overlapping ceftriaxone-PPI exposures. The primary outcome was 28-day QVC events. Multivariable Cox proportional hazards models were the main analysis and complemented by propensity score matching, inverse probability of treatment weighting, and Fine-Gray competing-risk models. To address external generalisability, an additional validation was performed using ECG-ViEW II, an Asian electrocardiogram-linked real-world database. The combination of ceftriaxone and lansoprazole was significantly associated with QVC events, revealing notable DDIs (e.g., in FAERS, Ω025 = 0.54). To validate these findings, a cohort of 5,594 patients receiving ceftriaxone combined with PPIs from the MIMIC-IV database was analyzed using Cox proportional hazards models. The analyses corroborated the initial findings (lansoprazole vs. other PPIs, multivariate HR = 1.30; 95% CI: 1.10-1.54), with the risk associated with the three PPI combinations ranked as lansoprazole > pantoprazole > omeprazole. ECG-ViEW II provided supportive Asian external validation, showing a higher QVC risk for ceftriaxone plus lansoprazole than for ceftriaxone plus other PPIs. Evidence from two national pharmacovigilance systems and an ICU EHR cohort indicated that PPI choice modified cardiac safety during ceftriaxone therapy. Lansoprazole co-use confers a higher risk of QVC, whereas omeprazole appears relatively safer. Therefore, prospective confirmation is warranted.

Rabeprazole was previously defined as a small-molecule fusion inhibitor that binds the conserved hydrophobic HR1 groove of the SARS-CoV-2 spike and blocks six-helix bundle assembly. Here, we expand its antiviral spectrum and demonstrate potent activity against Nipah virus pseudotype, HCoV-229E, and RSV. Using SPR, pseudovirus neutralization, docking, and 100-ns MD simulations, we validated binding of Rabeprazole to the HR1 domains of NiV F glycoprotein and HCoV-229E spike, with a conserved fusion-inhibitory mechanism. Systematic structure-activity relationship (SAR) profiling among clinically approved PPIs revealed that Ilaprazole and Lansoprazole exhibited stronger anti-NiV potency than Rabeprazole, while Rabeprazole sulfide showed enhanced antiviral activity relative to the parent compound. Rabeprazole also inhibited live RSV and HCoV-229E infection in a dose-dependent manner. Collectively, these findings establish the HR1 groove as a druggable pan-viral target and validate benzimidazole-based PPIs as a versatile scaffold for developing orally available, broad-spectrum antivirals against phylogenetically distinct enveloped viruses that rely on class I fusion machinery.

Although Lansoprazole, a proton pump inhibitor, is quite safe, there have been occasional reports of associated neurological dysfunction. We present a middle-aged man who developed bilateral asterixis within few hours of the first dose of lansoprazole. Interestingly, the jerks disappeared rapidly after discontinuation of lansoprazole.

A 75-year-old woman presented to the emergency department of a regional hospital with progressive dyspnea for 3 months despite treatment with antibiotics and steroids in the community. There were no associated symptoms. No clear precipitating factors were identified. She did not smoke and had worked as an arable farmer but had no known exposures. Her medical history was remarkable for hypertension and a prophylactic hysterectomy 10 years previously due to a family history of ovarian cancer. Her medications included olmesartan, lansoprazole, and calcium supplements.

The causal relationship between proton pump inhibitor (PPI) use and bone health outcomes remains uncertain. This study employs a Mendelian randomization (MR) approach to investigate the potential causal association between PPI use and the risk of osteoporosis and fractures. We selected 4 representative PPIs, including omeprazole, esomeprazole, lansoprazole, and rabeprazole, for our study. Bone health outcomes were evaluated through femoral neck bone mineral density (BMD), lumbar spine BMD, and the prevalence of osteoporosis and fracture across various anatomical sites, including the upper arm and shoulder, wrist and hand, lumbar spine and pelvis, femur, and lower leg and ankle. To evaluate PPI exposure and bone health outcomes, we utilized summary statistics derived from genome-wide association studies conducted in European ancestry populations. Primary causal estimates were derived using the inverse-variance weighting (IVW) approach, supplemented by MR-Egger, weighted median, and Mendelian Randomization Pleiotropy Residual Sum and Outlier methods. To strengthen the robustness of our findings, we conducted sensitivity analyses encompassing assessments of heterogeneity, horizontal pleiotropy, and leave-one-out analyses. Lansoprazole demonstrated a significant positive causal effect on femoral neck BMD (IVW: β = 0.137, 95% confidence interval: 0.063-0.210, P = 2.73E-04), whereas no statistically significant effects were observed for lansoprazole on lumbar spine BMD, osteoporosis, or fracture risk. Esomeprazole showed a marginal causal association with an elevated risk of femur fracture (IVW: odds ratio = 1.049, 95% confidence interval: 1.004-1.096, P = .031); however, this association lost statistical significance following Bonferroni correction. Its effects on BMD, osteoporosis, and fractures at other anatomical sites remained nonsignificant. No causal associations with BMD, osteoporosis, or fracture risk were identified for either omeprazole or rabeprazole. Sensitivity analyses further reinforced the robustness and reliability of these findings. This MR analysis found no compelling evidence to support a causal association between PPI use and the risk of osteoporosis or fractures.

A gastric ulcer (GU) that leads to acute or persistent bleeding poses a considerable risk of fatalities. Despite their overall primacy, the current treatments for GU have major downsides of incomplete healing, antibiotic resistance, and secondary injury. To address these challenges, researchers have turned their attention to hydrogels to solve the therapeutic bottleneck of GU treatment. Based on this, we developed a β-chitin (β-ch) hydrogel incorporating Lyophilised Platelet-rich fibrin (L-PRF) with anti-ulcer drug Lansoprazole (Lns). The prepared hydrogel was characterized using FESEM and FT-IR. In vitro studies of all samples showed good controlled swelling behaviour and degradation rate. Incorporation of Lansoprazole (Lns) facilitates healing and promotes and gastric mucosal regeneration, potentially through its acid-suppressive effects, whereas the in vitro drug release study proved the sustained release of Lns from the prepared hydrogel. The in vitro growth factor release study using ELISA revealed a sustained release of TGFα and PDGF BB. The Lansoprazole incorporated hydrogels exhibited good antioxidant activity. Further, β-ch-L-PRF-Lns hydrogel was demonstrated to be biocompatible in nature, and enhanced cell attachment of β-ch -L-PRF-Lns hydrogel was also observed in intestinal cells (INT 407). The INT 407 cells exposed to Lns incorporated β-ch-L-PRF hydrogel showed enhanced cell migration. Therefore, this unique strategy accelerates regenerative processes, making it a possible effective therapeutic alternative for treating GU.

We investigated the microenvironmental pH (pHM)-modulating mechanism and intermolecular interaction of alkalizers and their impact on the aqueous stability, release profiles of drugs and alkalizers, pharmacokinetics, and intragastric pH variability in 46 healthy human subjects of lansoprazole (LAN), an acid-labile model drug. Preliminary screening of five alkalizers (CaCO3, MgO, NaHCO3, meglumine, and L-arginine) in LAN-loaded wet granules under simulated gastric fluid demonstrated that calcium carbonate (CaCO3) appeared to be the best stabilizing agent for LAN in a dose-dependent manner according to solution pH changes and drug contents. Immediate-release fixed-dose combination tablets (IFT) containing LAN and CaCO3 were prepared via a dual granulation process using a fluidized bed dryer (FBD) and/or a high shear mixer (HSM). Unlike the commercial enteric-coated granule-loaded Lanston® capsule, IFT released LAN and CaCO3 simultaneously, achieving over 90% drug release within 30 min while maintaining its aqueous stability in pH 1.2 gastric fluid via the acid-neutralizing capacity of simultaneously released CaCO3. The increased modulation of pHM and the intermolecular complex of LAN with calcium ions are crucial for stabilizing LAN under low pH conditions. The optimal IFT formulation demonstrated long-term stability for 3 years, maintaining drug content and dissolution rates while liberating impurities (<0.2%) within regulatory guidelines. IFT demonstrated bioequivalence with the commercial enteric-coated Lanston® capsule with decreased "time to reach the maximum plasma concentration" and displayed superior intragastric pH control, maintaining pH above 4 for a longer duration over 24 h in a cross-over design in 46 healthy human subjects. The current novel IFT containing acid-labile LAN and CaCO3 can be used to substitute current enteric-coated LAN tablets for the immediate release and rapid onset of LAN without chemical degradation in the gastric fluid.