Gastro-Intestinal and Anti Emetic Drugs
Gastro-Intestinal and Anti Emetic Drugs
GIT
DRUGS USED TO TREAT
PEPTIC ULCER AND GERD
The two main causes of peptic ulcer disease are
infection with gram-negative Helicobacter pylori and
the use of non-steroidal anti-inflammatory drugs (NSAIDs).
Treatment approaches include
1) eradicating the H. pylori infection,
2) reducing secretion of gastric acid with the use of PPIs or
H2 -receptor antagonists, and/or
3) providing agents that protect the gastric mucosa from
damage, such as misoprostol and sucralfate
ANTIMICROBIAL
TREATMENT.
Patients with peptic ulcer disease (duodenal or gastric
ulcers) who are infected with H. pylori require antimicrobial
treatment.
Eradication of H. pylori results in rapid healing of active
ulcers and low recurrence rates
Currently, triple therapy consisting of a PPI combined with
amoxicillin (metronidazole may be used in penicillin-allergic
patients) plus clarithromycin is the therapy of choice.
Treatment with a single antimicrobial drug is much less
effective, results in antimicrobial resistance, and is not
recommended.
H2 -RECEPTOR
ANTAGONISTS
Gastric acid secretion is stimulated by acetylcholine,
histamine, and gastrin.
By competitively blocking the binding of histamine to H2
receptors, these agents reduce the secretion of gastric acid.
The four drugs used in the United States—cimetidine,
ranitidine [ZANTAC], Famotidine and Nizatidine—potently
inhibit (greater than 90%) basal, food-stimulated, and
nocturnal secretion of gastric acid.
Cimetidine was the first histamine H2 -receptor antagonist.
However, its utility is limited by its adverse effect profile and
drug– drug interactions
PROTON PUMP
INHIBITORS
The PPIs bind to the H+/K+-ATPase enzyme system (proton
pump) and suppress the secretion of hydrogen ions into the
gastric lumen
The available PPIs include
esomeprazole [NEXUM],
omeprazole ,
lansoprazole,
pantoprazole, and rabeprazole .
Omeprazole, esomeprazole, and lansoprazole are available
over-the counter for short-term treatment of GERD
(gastro-esophageal reflux disease)
PROSTAGLANDINS
Prostaglandin E, produced by the gastric mucosa, inhibits
secretion of acid and stimulates secretion of mucus and
bicarbonate.
A deficiency of prostaglandins is thought to be involved in
the pathogenesis of peptic ulcers.
Misoprostol, an analog of prostaglandin, is approved for the
prevention of NSAID-induced gastric ulcers.
Misoprostol is contraindicated in pregnancy, since it can
stimulate uterine contractions.
Dose-related diarrhea and nausea are the most common
adverse effects and limit the use of this agent. Thus, PPIs are
preferred agents for the prevention of NSAID-induced ulcers.
ANTACIDS
Antacids are weak bases that react with gastric acid to form
water and a salt to diminish gastric acidity. Because pepsin
is inactive at a pH greater than 4, antacids also reduce
pepsin activity