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Gastro-Intestinal and Anti Emetic Drugs

The document discusses various gastrointestinal and antiemetic drugs used to treat conditions like peptic ulcer disease and GERD, highlighting treatment approaches such as eradicating H. pylori infection and using PPIs or H2-receptor antagonists. It details the mechanisms and types of medications available, including antacids, antiemetics, antimotility agents, and laxatives, along with their effects and side effects. Combination regimens and specific drug interactions are also mentioned to enhance treatment efficacy and manage adverse reactions.

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0% found this document useful (0 votes)
8 views13 pages

Gastro-Intestinal and Anti Emetic Drugs

The document discusses various gastrointestinal and antiemetic drugs used to treat conditions like peptic ulcer disease and GERD, highlighting treatment approaches such as eradicating H. pylori infection and using PPIs or H2-receptor antagonists. It details the mechanisms and types of medications available, including antacids, antiemetics, antimotility agents, and laxatives, along with their effects and side effects. Combination regimens and specific drug interactions are also mentioned to enhance treatment efficacy and manage adverse reactions.

Uploaded by

kakanas47
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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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

Adverse effects: Aluminum hydroxide tends to cause


constipation, whereas magnesium hydroxide tends to
produce diarrhea.
ANTIEMETIC DRUGS
1-Phenothiazines:such as prochlorperazine (stemitil) act by
blocking dopamine receptors.

2-5-HT3 receptor blockers: The 5-HT3 receptor antagonists


include ondansetron , granisetron. These agents selectively
block 5-HT3 receptors in the periphery (visceral vagal
afferent fibers) and in the brain. This class of agents is
important in treating emesis linked with chemotherapy,
largely because of their longer duration of action and
superior efficacy.
3-Substituted benzamides :metoclopramide [plasil] is
effective at high doses against the emetogenic drugs.
S.E :Antidopaminergic side effects, including extrapyramidal
symptoms, limit long-term high-dose use.
Metoclopramide was previously used as a prokinetic drug for
the treatment of GERD.

4-Benzodiazepines: The antiemetic potency of lorazepam


and alprazolam is low. Their beneficial effects may be due to
their sedative, anxiolytic, and amnesic properties.

5-Corticosteroids: Dexamethasone [decadron], are effective


against mildly to moderately emetogenic chemotherapy.
COMBINATION
REGIMENS
Antiemetic drugs are often combined to increase antiemetic
activity or decrease toxicity. Corticosteroids, most commonly
dexamethasone, increase antiemetic activity
antihistamines, such as diphenhydramine, are often
administered in combination with high-dose metoclopramide
to reduce extrapyramidal reactions.
ANTI- DIARRHEALS
Increased motility of the GI tract and decreased absorption
of fluid are major factors in diarrhea
A. Antimotility agents Two drugs that are widely used to
control diarrhea are diphenoxylate [entero-stop] and
loperamide [vacontil]. Both have opioid-like actions on the
gut. At the usual doses, they lack analgesic effects. Because
these drugs can contribute to toxic megacolon, they should
not be used in young children or in patients with severe
colitis.
LAXATIVES
Laxatives are commonly used for constipation to accelerate
the movement of food through the G.I tract.
Laxatives increase the potential for loss of pharmacologic
effect of poorly absorbed, delayed-acting, and extended-
release oral preparations by accelerating their transit
through the intestines.
Irritants and stimulants
1. Senna: This agent is a widely used stimulant laxative.
Taken orally, senna causes evacuation of the bowels
within 8 to 10 hours. It also causes water and electrolyte
secretion into the bowel. In combination products with
other laxatives, it is useful in treating opioid-induced
constipation.
2. Bisacodyl: Available as suppositories and enteric-coated
tablets, bisacodyl is a potent stimulant of the colon. It acts
directly on nerve fibers in the mucosa of the colon.
3. Castor oil: This agent is broken down in the small intestine
to ricinoleic acid, which is very irritating to the stomach and
promptly increases peristalsis. Pregnant patients should
avoid castor oil because it may stimulate uterine
contractions

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