A remodeled PPI with a longer half-life
Dr. George Sachs was the first to describe the molecular structure and mechanism of action of the acid-producing pumps found in the stomach lining, in the Journal of Biological Chemistry, in 1976. This discovery led to his later innovation of the first medication in the class of drugs known as the proton pump inhibitor (PPI).
The proton pump mechanism in the parietal cells, within the stomach lining, takes a non-acidic potassium ion out of the stomach and replaces it with an acidic hydrogen ion. The accumulation of hydrogen ions increases stomach acidity.
PPIs work by blocking the hydrogen/potassium adenosine triphosphatase (H+/K+ ATPase) enzyme system of the gastric parietal cell. Parietal cells have receptors for three stimulators of acid secretion, acetylcholine, gastrin, and histamine-2. While the effect of the PPI is irreversible on each individual parietal cell, permanently stopping it from pumping acid into the stomach, when these cells reach the end of their short natural life (2-5 days), the body generates new parietal cells, which are able to produce acid. This is why ongoing dosing is essential.
The PPI class of medication directly affects the proton pump, rather than using an indirect approach, such as that of the histamine-2 receptor antagonists, which were the most widely accepted acid-reducing products prior to PPI discovery. Antacids also target stomach acids but they don’t stop its production. They work by neutralizing acid in the stomach (sodium bicarbonate derivatives) and absorbing acid (calcium and magnesium salts).
The first PPI introduced into Canada was Losec®, followed by Prevacid®, Pantoloc®, Nexium®, Pariet™, and now Tecta™. While all PPIs are in the same class, each has a unique chemical profile.
A New PPI
The makers of Pantoloc® (pantoprazole sodium) have developed a brand new formulation of this medication, called Tecta™ (pantoprazole magnesium). As with Pantoloc, Tecta is indicated for the treatment of conditions where a reduction of gastric acid secretion is required, such as duodenal ulcer, gastric ulcer, reflux esophagitis, the symptoms of reflux (heartburn and acid regurgitation), and duodenal ulcers associated with infection by H. pylori.1 As pantoprazole action is distal to the receptor levels, it can inhibit gastric acid secretion irrespective of the nature of the stimulus (acetylcholine, gastrin, and histamine-2).
Tecta has the same drug interaction profile as the original pantoprazole formulation.1 This factor is of particular importance for those who are currently taking a common blood thinner, Plavix® (clopidogrel bisulfate), which physicians often prescribe to prevent recurrence of certain serious cardiac events.3 Pantoprazoles are considered a safe option for those who need to take a PPI at the same time as Plavix.
Those consuming Tecta can expect the same side effect profile as pantoprazole sodium, including headache (2.1%), diarrhea (1.6%), and nausea (1.2%).1 Tecta is contraindicated in anyone with hypersensitivity to this drug or to any ingredient in the formulation.
So how is Tecta different?
In animal studies, Tecta demonstrated a longer half-life than Pantoloc.1 This means that the drug stays in the body for a longer period-of-time, affecting new parietal cells as they form and thus its effect is longer lasting. Your doctor may prescribe Tecta for you if your current medication does not provide adequate symptom control, for example, if your symptoms prevent you from falling asleep, or if they wake you up at night.
Some patients with GERD may experience erosive esophagitis, which is damage to the lining of the esophagus caused by refluxing acid. According to the Tecta product monograph, more patients taking Tecta had their esophageal erosions healed after 4 weeks compared to those taking Pantoloc, although by 8 weeks, the two treatments had equally effective outcomes.1 All PPIs are considered very safe and effective medications. Tecta is formulated as an enteric-coated tablet, which should not be chewed or crushed and should be swallowed with fluid in the morning either before, during, or after breakfast.