Anti-ulcer action mechanism -
For detailed prescribing information, readers should refer to the individual drug information topics within UpToDate. Comprehensive information on drug-drug interactions can be determined using the drug interactions program.
This tool can be accessed from the UpToDate online search page or through the individual drug information topics in the section on drug interactions.
Complete information on US Food and Drug Administration FDA labeling for each drug can be accessed using the FDA searchable database. Treatment regimens for H. pylori and management of peptic ulcer disease are discussed elsewhere.
See "Treatment regimens for Helicobacter pylori in adults" and "Peptic ulcer disease: Treatment and secondary prevention". Histamine-2 receptor antagonists. Mechanism of action — Histamine-2 receptor antagonists H2RAs eg, cimetidine, famotidine, and nizatidine inhibit acid secretion by blocking H2 receptors on the parietal cell figure 1.
H2RAs are well absorbed after oral dosing; peak serum concentrations occur within one to three hours. Absorption is reduced 10 to 20 percent by concomitant antacid administration, but not by food.
Why UpToDate? Product Editorial Subscription Options Subscribe Sign in. Antacids neutralize gastric acidity and elevate the pH of the stomach. Elevated pH also inactivates pepsin, a digestive enzyme.
Calcium carbonate comes in various formations such as a tablet, a chewable tablet, a capsule, or liquid to take by mouth. It is usually taken three or four times a day. Chewable tablets should be chewed thoroughly before being swallowed; do not swallow them whole.
The patient should drink a full glass of water after taking either the regular or chewable tablets or capsules. Some liquid forms of calcium carbonate must be shaken well before use.
Do not administer calcium carbonate within hours of other medicines because calcium may decrease the effectiveness of the other medicine.
Calcium carbonate may be contraindicated in patients with preexisting kidney disease because it may cause hypercalcemia. Common side effects of calcium carbonate include constipation and rebound hyperacidity when it is discontinued.
Other interventions to prevent hyperacidity can also be recommended, such as smoking cessation and avoiding food and beverages that can cause increased acidity alcohol, high-fat or spicy foods, and caffeine. A common H2-receptor antagonist is famotidine. It is available OTC and is also often prescribed orally or as an IV injection in the hospital setting.
Other H2-receptor antagonists include cimetidine and ranitidine. Cimetidine has a high risk of drug interactions, especially in elderly patients because of its binding to cytochrome P enzymes in the liver, which affects the metabolism of other drugs.
Famotidine see Figure 7. OTC famotidine is also used to treat heartburn or sour stomach. To prevent symptoms, oral famotidine is taken 15 to 60 minutes before eating foods or drinking drinks that may cause heartburn.
Preexisting liver and kidney disease may require dosage adjustment. Famotidine is supported by evidence as safe for use in pediatric patients younger than 1 year old, as well as in geriatric patients. Patients taking the oral suspension should be instructed to shake it vigorously for 5 to 10 seconds prior to each use.
Additionally, smoking interferes with histamine antagonists and should be discouraged. A common proton pump inhibitor PPI is pantoprazole see Figure 7. It may be prescribed in various routes including orally, with an NG tube, or as an IV injection in the hospital setting.
Other PPIs include esomeprazole, lansoprazole, and omeprazole. PPIs are more powerful than antacids and H2-receptor antagonists.
Pantoprazole is used to treat damage from gastroesophageal reflux disease GERD in adults and children five years of age and older by allowing the esophagus to heal and prevent further damage.
It is also used to treat conditions where the stomach produces too much acid, such as Zollinger-Ellison syndrome in adults. PPIs may also be given in combination with antibiotics to treat H.
Pylori infections, a common cause of duodenal ulcers. PPIs inhibit the secretion of hydrochloric acid, and the antisecretory effect lasts longer than 24 hours. Packets of delayed-release granules must be mixed with applesauce or apple juice and taken by mouth or given through a feeding tube.
Consult the labeling of concomitantly used drugs to obtain further information about interactions because PPIs can interfere with the liver metabolism of other drugs. IV pantoprazole can potentially exacerbate zinc deficiency, and long-term therapy can cause hypomagnesemia, so the nurse should monitor for these deficiencies.
In addition to the considerations above, instruct patients to call their provider if their condition does not improve or gets worse, especially if bleeding occurs. Sucralfate locally covers the ulcer site in the GI tract and protects it against further attack by acid, pepsin, and bile salts.
It is minimally absorbed by the gastrointestinal tract. Administer sucralfate on an empty stomach, 2 hours after or 1 hour before meals.
Constipation may occur. Sucralfate should be cautiously used with patients with chronic renal failure or those receiving dialysis due to impaired excretion of small amounts of absorbed aluminum that can occur with sucralfate.
In addition to the considerations above, instruct patients to call their provider if their condition does not improve or gets worse. Simethicone is an antiflatulent that is commonly found in other OTC antacids see Figure 7. It is also safe for use in infants. Gas commonly occurs in the GI tract due to digestive processes and the swallowing of air.
Gaseous distension can also occur postoperatively. Simethicone is used to treat the symptoms of gas such as uncomfortable or painful pressure, fullness, and bloating. Simethicone works by altering the elasticity of the mucous-coated gas bubbles, which cause them to break into smaller bubbles, thus reducing pain and facilitating expulsion.
Simethicone is usually taken four times a day, after meals and at bedtime. For liquid form, shake drops before administering. Patients can be instructed about other measures to assist with gas expulsion such as changing position, ambulation, avoiding the use of straws, and tapering intake of beans and cruciferous vegetables.
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ANTI-ULCER DRUGS RVS Chaitanya Koppala. PEPTIC ULCER An Ulcer is … Erosion in the lining of the stomach or the first part of the small intestine, an area called the duodenum. Ulcers that form in the stomach are called gastric ulcers; in the duodenum, they are called duodenal ulcers.
Both types are referred to as peptic ulcers. Reduction of gastric acid secretion A H2 antihistaminics: Cimetidine, ranitidine, famotidine, roxatidine B Proton pump inhibitors: Omeprazole, esomeprazole, lansoprazole, pantoprazole, rabeprazole, dexrabeprazole C Anti cholinergic drugs: Pirenzapine, propantheline, oxyphenomium D Prostaglandin analogue: misoprostol.
Neutralization of gastric acid A Systemic : Sodium bicarbonate, sodium citrate B Non systemic: Magnesium hydroxide, mag trisilicate, aluminium hydroxide gel, magaldrate, calcium carbonate 3.
Ulcer protective : Sucralfate, colloidal bismuth subcirtrate 4. Anti H-pylori drugs: Clarithromycin, metronidazole, amoxicillin, tinidazole, tetracycline. Neuronal acetylcholine,Ach ,paracrine histamine , and endocrine gastrin factors all regulate acid secretion.
Their specific receptors M3,H2,and CCK2 receptors, respectively are on the basolateral membrane of parietal cells in the body and fundus of the stomach. The H2 receptor is a GPCR that activates the Gs- adenyl cyclase —cyclic AMP-PKA pathway.
Histamine antagonists inhibit the action of histamine on the acid-producing cells of the stomach and reduce stomach acid. H2 blockade: Block histamine induced gastric secretion, cardiac stimulation, uterine relaxation No effect on H1 responses because they are selective.
Gastric secretion: Marked inhibition of gastric secretion All phase are suppressed dose dependently. Major side effects: Bowel upset, Dry mouth, Rashes, Gynaecomastia, Impotence, Loss of libido, Decrease in sperm count.
USES: It is used in treatment of Duodenal ulcer, Gastric ulcer, Stress ulcer, GERD, Zollinger ellison syndrome Prophylaxis of aspiration pneumonia. The proton pump is the terminal stage in gastric acid secretion. Uses Peptic ulcer Bleeding peptic ulcer Stress ulcer GERD Zollinger Ellison syndrome Aspiration pneumonia Adverse effects Nausea, loose stools, headache, abdominal pain, muscle and joint pains Rashes Leucopenia Hepatic dysfunction Gynecomastia and erectile dysfunction lately observed.
SYMPTOMS OF H. SYMPTOMS Burning abdominal pain Haematemesis Melena Nausea or vomiting Unexplained weight loss Anorexia Abdominal fullness.
DIAGNOSIS Endoscopy: Flexible tube fitted with camera is threaded down the esophagus in to stomach to see the ulcer by physician Bariummeal: Barium liquid is drunk making ulcer visible on X-ray.
Test fordiagnosing H. pylori Breath test :by measuring the amount of co2 in exhaled breath. pylori antibodies by ELISA test. pylori antigen. Because of their relatively poor efficacy, side effects, and risk of blood disorders, they are rarely used today.
AGENTS THAT ENHANCE MUCOSAL DEFENSE Prostaglandin Analogs: prostaglandins are produced in the gastric mucosa and appear to serve a protective role by inhibiting acid secretion and promoting mucus and bicarbonate secretion. In addition, PGs inhibits gastrin production, increase mucosal blood flow and probably have an ill defined cytoprotective action.
DRUGS: Misoprostol. Other common side effects include: abdominal pain, nausea, flatulence, headache, dyspepsia, vomiting, and constipation.
It also attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile.
Side effects The most common side effects seen are constipation.
Anfi-ulcer stomach Anti-uulcer Anti-ulcer action mechanism that secrete different substances as part of Anti-ulcer action mechanism digestive process: parietal cells, Ketosis and Brain Function cells, Abti-ulcer surface epithelium cells. See an image of the stomach and these cells in Figure 7. Surface epithelium cells are found within the lining of the stomach and secrete mucus as a protective coating. Parietal cells and chief cells are found within the gastric glands. Parietal cells produce and secrete hydrochloric acid HCl to maintain the acidity of the environment of a pH of 1 to 4.
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