Comparative Drug Review Gastrointestinal Remedies Tagamet And Nexium Biology Essay

Tagamet and Nexium have been two of the many common drugs these days, both which are trusted in the medical treatment of major gastric acid-related disorders like peptic ulcer disease (PUD) and gastro-esophageal reflux disease (GERD), with the respective active ingredient being cimetidine and esomerprazole.

In view with their similar uses in gastrointestinal therapies, this review addresses various major characteristics possessed by the two drugs and in an attempt to make a stunning comparison between them relating to their substances, for providing information optimizing the selection of gastric acid-related drugs at different professional medical conditions.


Both cimetidine and esomeprazole help to remedy gastrointestinal disorders by reducing the secretion of gastric acid, however, with different medicine focuses on to be acted on and mechanisms to effect a result of their actions. Cimetidine, being a histamine H2 receptor competitive antagonist (H2RA), reversibly binds to the histamine H2 receptor on the acid-secreting parietal cell of the abdominal and business lead to the production of second messenger cAMP which can ultimately result in the H+/K+-ATPase to pump more acid from the cell. Thus, the binding of histamine released by Enterochromaffin-like (ECL) skin cells in the stomach to the receptors, which stimulates gastric acid secretion, is inhibited. At the same time, with the blockage of the histamine H2 receptors by cimetidine, the effect of both gastrin- and acetylcholine-stimulated acid secretion would be reduced. All these cause the reducing of acidity in the abdomen.

Esomeprazole, being a proton pump inhibitor (PPI), serves by an completely different mechanism. Esomerprazole is a weak-base prodrug and it accumulates in the unique, highly acidic canalicular space of the active parietal cell, where the pH is less than 2. 0. As of this pH, it is converted to the energetic form of the medicine, which in turn covalently binds to 1 or even more cysteines that are seen from the luminal surface of the gastric proton pump in gastric parietal cells, the H+/K+ ATPase enzyme, the mark of which esomeprazole functions on. As a result, this irreversibly inhibits the H+/K+ ATPase enzyme, whose activity is mixed up in last step of gastric acid secretion

Therapeutic Effectiveness

Owing with their different mechanisms of action, the gastric acid-suppressive impact produced by them varies, thus leading to variant in their effectiveness for treating related diseases. In general, PPIs (e. g. esomerprazole) are stronger than H2RAs (e. g. cimetidine) because the past inhibits the H+/K+ ATPase enzyme involved in the final step of acid secretion[1], as the latter only inhibits one of the pathways involved in acid secretion. The superior acid-suppressive effect of PPI over an H2RA has been confirmed by comparative studies. [2-5]

Because of different mechanism of these two drugs, esomeprazole has an extended period than cimetidine. After changed into the effective form, Esomeprazole can bind reversibly to the H+/K+-ATPase. Because of this, esomeprazole will never be easily enzymatically metabolized and the major factor that leading to loss of aftereffect of esomeprazole is largely reliant on the production of new H+/K+-ATPase. That is reason esomeprazole has a rather long duration of influence on inhibition of acid secretion.

In conditions of therapeutic benefits, it has been shown that higher efficiency is found in PPI treatments than in H2RA treatments for an array of diseases such as peptic ulcer disease, gastroesophageal reflux disease, GI destruction triggered by non-steroidal anti-inflammatory drugs, and Zollinger-Ellison symptoms. [6 V13], as discovered by many reports. One of these aimed to research oesophagitis when a meta-analysis of 43 healing trials was conducted in patients with average or severe oesophagitis. The proportion of patients successfully treated was almost doubled with PPIs, and the rapidity of recovery and symptom alleviation were about double that with H2RAs. [14] Thus, It possessed confirmed the benefit of PPIs over H2RAs. [15]

To summarize, up for this stage, esomerprazole seems to be far better and a far more preferable choice than cimetidine for the treatment of most gastric acid-related diseases.


In reality, both cimetidine and esomeprazole are very safe plus they rarely have adverse effects which may be lethal. In a very meta-analysis of 24 double-blind placebo-controlled studies, it shows negligible difference of occurrence of side effects between cimetidine and placebo. The mostly reported undesireable effects are diarrhea, other gastrointestinal disruptions, dizziness, fatigue, rashes and headaches. Furthermore, most adverse effects of cimetidine are dose-related as the length of treatment boosts, the chance is decreased which means Cimetidine is quite secure for patients who require long-term treatment. Also, Cimetidine has significant anti-androgen effects in patient acquiring high dose and this sets some male patients in fear.

Adverse effects of Esomeprazole are infrequent as Cimetidine, however, many of its common aspect effects like pain, diarrhea and pores and skin rashes can be severe and could need to resolve on medicine discontinuation. Moreover, known increases in the prevalence of pneumonia and Campylobacter enteritis as well as a doubling of the chance of an infection with Clostridium difficile should not be overlooked because of the role of esomeprazole as a first-line medication.

What should emphasize is the fact patients still need health care professionals careful indication as if both drugs are safe. Since esomeprazole is one of the most frequently prescribed drugs and 63%, 33% and 67% of hospital inpatients in Austria, Ireland and the uk did not meet up with the criteria when planning on taking esomeprazole or other proton pump inhibitors. Because of this, it is pharmacoeconomically unfavorable and improved clinical pharmaceutical good care may be accomplished by detailed indicator by the cooperation of pharmacist and healthcare professionals. What is more, these two drugs are placed in the same Pregnancy Category by the US FDA and they're not suggested for the pregnant women. For their inhibition of parietal skin cells, secretion of intrinsic factor is reduced. As a result, both drugs can lead to mal-absorption of Supplement B12 which is important for maturation of Erythrocytes and DNA synthesis and therefore Vitamin B12 remedy may be needed.

Drug interactions

They interact with a wide variety of drugs except that they both reduce absorption of acid-dependent drugs because of the effect of bringing down of the belly pH, but in reality only drugs with a slim healing index have scientific significance. Nearly all interactions is due to binding of cimetidine to cytochrome P450 isoenzymes in the liver with subsequent inhibition of microsomal oxidative metabolism and increased bioavailability or plasma concentrations of drugs metabolised by these enzymes. These drugs are anticoagulants, phenytoin, theophylline, benzodiazepines, betal-blockers, lidocaine, Procainamide, ketoconazole and itraconazole.

Similarly, Esomeprazole inhibits the reduction of drugs metabolized by isoenzyme CYP2C19 and to a smaller amount by CYP3A4. Therefore, it increases the plasma level of clarithromycin, amoxicillin, diazepam, phenytoin, and warfarin. Furthermore, esomeprazole has a potential relationship with atazanavir which is a HIV-Protease Inhibitor to treat HIV by substantially reducing the concentration of atazanavir.


Summarizing all the above mentioned features, Nexium is seemingly an improved drug in conditions of its potency, therapeutic effects as well as its selection of application in medical conditions, comparing to Tagamet. However, its positives and negatives may be uncovered in the foreseeable future by research works, that ought to be always aware of.

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