Ulcer-Healing Drugs

H2 Receptor Antagonists:

H2-Receptor antagonists are medications used to treat a Varity of Gastrointestinal conditions such as duodenal ulcer, gastric ulcer, GERD, erosive esophagitis and zollinger-ellison syndrome.

Ranitidine:

Indications: Duodenal ulcer, benign gastric ulcer, reflux esophagitis, Zollinger­ellison syndrome, NSAID induced lesions and prevention in acid aspiration syndrome (AAS).

Contraindications: Porphyria, Disease of Liver, Gastric Cancer, Renal Disease.

Dose and Administration: By mouth: benign gastric and duodenal ulceration, chronic episodic dyspepsia, adult and child over 12 years, 150 mg twice daily or 300 mg at night for 4–8 weeks in benign gastric and duodenal ulceration, up to 6 weeks in chronic episodic dyspepsia, and up to 8 weeks in NSAID-associated ulceration (in duodenal ulcer 300 mg can be given twice daily for 4 weeks to achieve a higher healing rate); child 3–12 years, (benign gastric and duodenal ulceration) 2–4 mg/kg (max. 150 mg) twice daily for 4–8 weeks. Gastro­oesophageal reflux disease, adult and child over 12 years, 150 mg twice daily or 300 mg at night for up to 8 weeks or if necessary 12 weeks (moderate to severe, 600 mg daily in 2–4 divided doses for up to 12 weeks); long-term treatment of healed gastro-oesophageal reflux disease, 150 mg twice daily; child 3–12 years, 2.5–5 mg/kg (max. 300 mg) twice daily. Zollinger–Ellison syndrome (but see notes above), adult and child over 12 years, 150 mg 3 times daily; doses up to 6 g daily in divided doses have been used. surgical procedures, slow intravenous injection, 50 mg 45–60 minutes before induction of anaesthesia, or by mouth, 150 mg 2 hours before induction of anaesthesia and also when possible on the preceding evening. By slow intravenous: injection, adult and child over 12 years, 50 mg diluted to 20 mL and given over at least 2 minutes; may be repeated every 6–8 hours. By intravenous infusion: 25 mg/hour for 2 hours; may be repeated every 6–8 hours.

Chelates and complexes: Sucralfate:

Indications: Duodenal and non-malignant gastric ulcer, prophylaxis of duodenal ulcer recurrence and prophylaxis of gastric hemorrhage due to stress ulceration. Contraindications: Pregnant women and children. Aluminum Toxicity and Chronic Renal Failure.

Dose and Administration: Benign gastric and duodenal ulceration and chronic gastritis, adult and child over 15 years, 2 g twice daily (on rising and at bedtime) or 1 g 4 times daily 1 hour before meals and at bedtime, taken for 4–6 weeks or in resistant cases up to 12 weeks; max. 8 g daily. Prophylaxis of stress ulceration, adult and child over 15 years, 1 g 6 times daily; max. 8 g daily.

Proton Pump Inhibitors:

Proton pump inhibitors inhibit gastric acid secretion by blocking the hydrogen-potassium adenosine triphosphatase enzyme system (the ‘proton pump’) of the gastric parietal cell. Proton pump inhibitors are effective short-term treatments for gastric and duodenal ulcers; they are also used in combination with antibacterials for the eradication of Helicobacter pylori In patients with peptic ulcer bleeding, treatment with a proton pump inhibitor reduces the risk of rebleeding and the need for surgery. Side effects: The most common side effects of proton pump inhibitors are: Headache, Diarrhea, Constipation, Abdominal pain, Nausea, Rash. Interactions: Proton pump inhibitors interact with few drugs. The absorption into the body of some drugs is affected by the presence of acid in the stomach, and because PPIs reduce acid in the stomach, they may affect the absorption of these drugs. Specifically, PPIs reduce the absorption and concentration in the blood of ketoconazole and increase the absorption and concentration of digoxin. This may lead to reduce effectiveness of ketoconazole and an increase in digoxin toxicity. Proton pump inhibitors can reduce the breakdown of some drugs by the liver and lead to an increase in their concentration in the blood.

OMEPRAZOLE:

Indications: Omeprazole is used for treating acid-induced inflammation and ulcers of the stomach and duodenum; gastroesophageal reflux disease (GERD); erosive esophagitis, heartburn; prevention of upper gastrointestinal bleeding in critically ill patients; and Zollinger-Ellison Syndrome. It also is used in combination with antibiotics for eradicating H. pylori infection of the stomach. Contraindications: Severe Hepatic Disease.

Dose and Administration: For ulcers, GERD, erosive esophagitis and eradication of H. pylori the recommended dose for adults is 20-40 mg daily. Ulcer healing usually occurs within 4-8 weeks. H. Pylori infections are treated for 10-28 days. The usual dose for prevention of upper gastrointestinal bleeding in critically ill patients is 40 mg daily for 14 days. Omeprazole OTC is used for treating heartburn for up to two weeks, and the usual dose is 20 mg daily. For the management of Zollinger-Ellison Syndrome the starting dose for adults is 60 mg daily, and the dose is adjusted based on either the response of symptoms or the actual measurement of acid production. Doses greater than 80 mg should be divided. Doses up to 120 mg three a day in divided doses have been used in the treatment of Zollinger-Ellison Syndrome. For maximal efficacy, Omeprazole tablets should be taken before meals, swallowed whole and should not be crushed, chewed or opened.

ESOMEPRAZOLE:

Indications: Esomeprazole is approved for the treatment of gastroesophageal reflux disease (GERD) and in combination with amoxicillin and clarithromycin for the treatment of patients with ulcers and H. pylori infection. Since it is very similar to omeprazole, it also is likely that it will be used for the treatment of Zollinger-Ellison syndrome. Esomeprazole also is approved for short-term use in children ages 1-11 for GERD.

Contraindications: Atrophic Gastritis, Severe Hepatic Disease.

Dose and Administration: For GERD, 20 or 40 mg of esomeprazole is given once daily for 4-8 weeks. In children ages 1-11, the dose is 10 or 20 mg daily. For the treatment of H. pylori, 40 mg is administered once daily in combination with amoxicillin and clarithromycin for 10 days.

Esomeprazole capsules should be administered one hour before meals, swallowed whole and should not be crushed or chewed. Patients with difficulty swallowing can open the capsule and mix the pellets with applesauce. The applesauce should not be hot and the pellets should not be chewed or crushed.

PANTOPRAZOLE:

Indications: Although pantoprazole is approved for the treatment of gastroesophageal reflux disease (GERD), like other PPI’s it also is used for treating ulcers of the stomach and duodenum, and the Zollinger-Ellison Syndrome.

Contraindications: Pernicious Anemia.

Dose and Administration: For GERD the recommended dose for adults is 40 mg daily for 4-8 weeks. It generally is recommended that tablets be taken approximately 30 minutes prior to meals for maximal effectiveness. Tablets should be swallowed whole and should not be crushed, split or chewed. IV injection over at least 2 minutes or by IV infusion, duodenal ulcer, gastric ulcer and GERD, 40mg daily until oral administration can be resumed.

LANSOPRAZOLE:

Indications: Lansoprazole is used for treating ulcers of the stomach and duodenum, gastroesophageal reflux disease (GERD) and Zollinger-Ellison Syndrome.

Contraindications: Severe Hepatic Disease.

Dose and Administration: For initial treatment of duodenal ulcers the recommended dose for adults is 15 mg daily for 4 weeks. For the treatment of GERD, the recommended initial treatment is 15 mg for up to 8 weeks. For maintaining healing (long-term) in duodenal ulcer and GERD the recommended treatment is 15 mg daily. For initial treatment of severe (erosive) esophagitis and gastric ulcer, the recommended dose for adults is 30 mg daily for 4-8 weeks. For the management of Zollinger-Ellison Syndrome, the starting dose for adults is 60 mg daily, and the dose is adjusted based on response. Doses up to 180 mg have been used in some patients with Zollinger-Ellison syndrome. It is recommended that capsules be taken before meals for maximum effect. Capsules should be swallowed whole and should not be crushed, split or chewed.

RABERAZOLE:

Indications: Rabeprazole is used for treating ulcers of the stomach and duodenum, erosive or ulcerative gastroesophageal reflux disease (GERD) and Zollinger-Ellison Syndrome (in which there is overproduction of acid caused by tumors). It also is used with antibiotics for eradicating Helicobacter pylori infections of the stomach that, along with acid, are responsible for many ulcers. Contraindications: Severe Hepatic Disease.

Dose and Administration: For healing ulcerative or erosive GERD, the recommended dose for adults is 20 mg daily for 4-8 weeks. If healing does not occur after 8 weeks, another 8-week course may be considered. The recommended maintenance dose is 20 mg daily. Heartburn due to GERD is treated with 20 mg daily for 4 weeks and an additional 4 weeks if symptoms do not resolve. Ulcers are treated with 20 mg daily for 4 weeks. For the management of Zollinger-Ellison Syndrome, the starting dose for adults is 60 mg daily, and the dose is adjusted based on improvement in symptoms, healing of ulcers, or the effectiveness of acid suppression. Doses of 100 mg per day and 60 mg twice daily have been used in some patients with Zollinger-Ellison Syndrome. The regimen for eradication of Helicobacter pylori is Rabeprazole 20 mg, clarithromycin 500 mg, amoxicillin 1000 mg all given twice daily (morning and evening) for 7 days. Tablets should be swallowed whole and should not be crushed, split or chewed. Rabeprazole can be taken with or without meals since food has little effect on its absorption.