A new generation of proton pump inhibitors for injections - esomeprazole sodium

proton pump inhibitors (PPI) are the preferred drugs for the treatment of acid-related
diseases such as peptic ulcers and gastroesophageal reflux diseaseAt present, the commonly used PPIs are omeprazole, Lansorafen, Rebella, cesaprazole and Esomeprazole 5 kindsAs the first PPI drug, omeprazole has been unanimously recognized for its efficacy in the treatment of acid-relateddiseasesEssomeprazole, the commodity name Nexium, is a single isomer, or (S)-Isomer, omeprazoleDue to its metabolic advantages, essomeprazole has higher bioavailability and more consistent pharmacokinetics than omeprazole, which increases the number of drugs reaching the proton pump and has a better acid suppression effect than other PPIAlthough oral essomeprazole can achieve good clinical results, but in some patients, such as dysphagia, vomiting, acute upper gastrointestinal bleeding and surgical recovery period patients, oral administration becomes an unfeasible route of administration, intravenous drug delivery path becomes an inevitable choiceTherefore, injectable sodium esomeazole is suitable for patients who need to use PPI but cannot administer the drug orallyThe pharmacokinetic characteristics of sodium esomeprazole in injection
absorption and distribution of a single vein pathway to esomeprazole 40 mg, the highest concentration of blood (Cmax) increased with the speed of intravenous dripHowever, regardless of the speed and slowness of the drops, the blood concentration-time curve area (AUC) is always relatively constant (7.07 to 7.38 mmol/L), suggesting that its bioavailability is consistentDrug-to-drug interactionSIs For drugs whose absorption processis are affected by stomach acid, the absorption of these drugs can be increased or decreased during treatment of esomeprazole due to a decrease in stomach acidWhen esomeprazole is combined with drugs metabolized by CYP2C19 (e.gdiazepam, siplane, propylene, chlormipamin, phenytoin, etc.), the plasma concentration of these drugs may increase and appropriate doses need to be reduced The pharmacodynamic characteristics of the sodium esomeprazole in injections
mechanism of action mechanism essomeprazole and omeprazole, i.e., protonization under acidic conditions, essomeprazole into a compound with inhibited H/K -ATP enzyme activity Subsulamide, rapidly combined with the pyridine of the first-body cysteine in the AtP enzyme, to form a disulfur bond, so that the enzyme inactivated, specific inhibits the activity of H/K -ATP enzyme in the stomach wall cells to inhibit the secretion of stomach acid Acid suppression capacity Existing studies show that intravenous giving esomeprazole is consistent with oral esomeprazole acid suppression effect when repeated administration In addition, the same package of sodium esomeprazole can be used for both intravenous and intravenous drips Intravenous injection (3 minutes) and intravenous drip (30 minutes) 40 mg essomeprazole, for 10 consecutive days, the two groups of stomach acid inhibition effect is consistent In gastroesophageal reflux patients, intravenous or oral esomeprazole 40 mg/d or 20 mg/d, a total of 10 days, although intravenous drug set basic gastric acid secretion (BAO) and gastric progenitor stimulation of the largest gastric acid secretion (MAO) is higher than the oral group, but the difference is not significant, indicating that 10 days of continuous treatment, intravenous is an acceptable alternative to oral administration Studies have shown that the ability to suppress acid sacin with esomeprazole is faster and more effective than other injectable PPI Dirk et al gave health volunteers 40 mg esomeprazole or 40 mg of a single dose of protoprazole intravenously, and then continuously monitored the intra-gastric pH found that the duration of pH 4 in the first 6 hours after the two groups of medication was 3.4 and 2.1 hours, respectively, and 24 hours corresponded to 11.8 and 7.2 hours, respectively Wilder et al have shown that repeating intravenous drips of esomeprazole is faster and more effective at the same dose than the patoprazole Recent studies have also shown that the effect of intravenous application of esomeprazole inhibits the underlying state and stimulating stomach acid secretion is faster and more complete than omeprazole Clinical application sodium esomeramazole with injections gastroesophageal reflux disease for the treatment of reflux-eating esophagitis and/or patients with severe reflux symptoms Intravenous application of esomeprazole can make the cure rate of decayed esophagitis reach edited up to 80%, when gastroesophageal reflux patients have difficulty swallowing, vomiting, bleeding and other complications, intravenous giving esomeprazole can quickly and effectively inhibit the secretion of stomach acid, long-term maintenance of the stomach pH 4, so as to achieve good therapeutic results Upper gastrointestinal bleeding For non-esophageal varicose gastrointestinal bleeding treatment, usually first in the gastroscopy under the gastroscopy, after the success of the rapid use of drugs to improve the pH in the stomach to 6 or more, to promote platelet clotting and prevent thrombosis, prevent re-bleeding At present, it is recognized that it is more than 6 per cent in the stomach, with omeprazole 80 mg instant static injection, followed by 8 mg/h to maintain the acid suppression effect of intravenous drips is more ideal Esomeprazole has a better acid suppression than omeprazole and lasts longer, so there is no doubt that it will be more effective and convenient for the treatment of acute upper gastrointestinal bleeding Stress ulcer intra-gastric pH change is closely related to gastric mucosa lesions, such as effective control of stomach acid secretion and acidity in the stomach cavity, to some extent can control and cure the pathological changes of the gastric mucosa in the stress state Existing studies have shown that intravenous omeprazole can quickly improve the pH in the stomach and effectively treat stress ulcers Since essomeprazole is used longer to maintain pH 4 in the stomach, it is believed to be more effective in treating stress ulcers In short, the new generation of injectable PPI essomeprazole has unique pharmacokinetic characteristics, its acid suppression ability is faster and more effective than oral esomeprazole and other injectable PPI For patients who need to use PPI clinically but cannot administer oral medications, such as acute upper gastrointestinal bleeding and stress ulcers, injections of essomeprazole provide strong acid suppression and comprehensive protection (Ju-Yuan Lai Huamei)