Gastrointestinal Drugs
Anti-ulcer drugs:
I. Histamine-2 (H2) Antagonists
- selectively block H2 receptors (located on parietal cells) blocking gastrin which causes
local release of histamine and production of hydrochloric acid (Hcl) and decrease pepsin.
Drugs
A. cimetidine (Tagamet) - first drug to be developed- has antiadrenergic effects including
gynecomastia and galactorrhea
B. ranitidine (Zantac) - longer acting and more potent than cimetidine - NOT associated
with anti-adrenergic adverse effects
Actions and indications
- short-term treatment of active duodenal ulcer or benign gastric ulcer - prophylaxis
of stress-induced ulcers and acute upper GI bleeding in critical clients - treatment
of erosive gastroesophageal reflux
- relieve symptoms of heartburn, acid indigestion and sour stomach (OTC preparations)
Contraindications and cautions
- caution for pregnancy or lactation and with hepatic or renal dysfunction
Adverse effects
GI - diarrhea or constipation
CNS - dizziness, headache, somnolence, confusion
Cardio - arrhythmias and hypotension - more commonly seen with IV or IM or with
prolonged use
- gynecomastia (more common with long term use of cimetidine) and impotence
II. Antacids
- neutralize stomach acid, available OTC; ALL antacids have adverse effects - no perfect
antacid
- giving antacid frequently causes acid rebound - nuetralizing the stomach contents to
alkaline level stimulates gastrin production to cause increased in acid production and
return stomach to its normal acidic state - therefor acid rebound causes increased intake of
antacid
- clients taking antacids should be advised to seperate them from any other drugs by 1 to 2
hours
Drugs
A. sodium bicarbonate (Bell-Ans) - oldest drug in this group - includes baking soda B.
calcium carbonate (Tums) - actually precipitated chalk
C. magnesium salts (Milk of Magnesia) - very effective in buffering acid in stomach but
can cause diarrhea
D. aluminum salts (Amphojel) - do NOT cause acid rebound but NOT very effective in
acid neutralizing
Actions and indications
- for symptomatic relief of upset stomach associated with hyperacidity as well as
hyperacidity with peptic ulcer, gastritis, gastirc hyperacidity and hiatal hernia
Contraindications and cautions
- those clients that can exacerbate by electrolyte or acid-base imbalance, GI obstruction
can cause systemic absorption, renal dysfunction can lead to electrolyte imbalance,
pregnancy or lactation
Adverse effects
- rebound acidity produce more acid in repsonse to alkaline environment is common
- use of calcium salts may lead to hypercalcemia and milk-alkali syndrome -
constipation or diarrhea
- hypophosphatemia with use of aluminum salts
- fluid retention and CHF can occur with sodium bicarbonate beacuse of high sodium
content
III. Proton pump inhibitors (gastric acid pump)
- suppress gastric acid secretion by inhibiting hydrogen-potassium adenosine
triphosphatase enzyme system on secretory surface of gastric parietal cells - blocking
final step of acid production
Drugs
A. omeprazole (Omperon) - faster acting and more quickly excreted drug; used to treat
ulcers caused by H.pylori bacteria and also for heartburn (OTC drug) B. esomeprazole
(Nexium) - longer-acting drug; NOT broken down as fast in the liver
- for treatment of GERD, severe erosive esophagitis and other hypersecretory conditions
Actions and indications
- for short-term treatment of active duodenal ulcers, GERD, erosive esophagitis and
benign active gastric ulcer
- for long-term treatment of pathological hypersecretory conditions
- also for combination with amoxicillin and clarithromycin for treatment of H. pylori
infection
Contraindications and cautions
- allergy, pregnancy or lactation
Adverse effects
CNS - dizziness and headache, sometimes asthenia (loss of strength), vertigo, insomnia,
apathy
GI - diarrhea, abdominal pain, nausea, vomiting, dry mouth and tongue atrophy
Upper resp. tract - cough, stuffy nose, hoarseness and epistaxis
IV. Laxatives
- also called cathartic drugs - spped the passage of intestinal contents through the GI tract
A. Chemical stimulants - directly stimulate nerve plexus in intestinal wall causing
increased movement and stimulation of local reflexes
Drugs
1. senna (Senokot) - may have slow or steady effect or may cause severe cramping 2.
castor oil - for thorough evacuation of intestine ; works at beginning of small intestine and
increases motility throughout the GI tract; blocks fat absorption may lead to constipation
3. bisacodyl (Dulcolax) - ofetn the drug of choice to empty the bowel pre-surgery or
diagnostic tests such as barium enema, oral or rectal
B. Bulk stimulants - rapid-acting, aggressive which increase motility of GI tract by
incrasing fluid in intestinal contents
Drugs
1. magnesium sulfate (Epsom salts) - acts by exerting a hypertonic pull against mucosal
wall, drawing fluid into intestinal contents; can be used for GI poisoning 2. magnesium
hydroxide (Milk of Magnesia) - to stimulate bulk and is milder and slower-acting; also
works by saline pull
3. lactulose (Chronulac) - alternative choice for clients with cardiovascular problems;
saltless osmotic laxative pulls fluid out of venous system 4. psyllium (Metamucil) -
gelatin-like bulk stimulant - milder and less irritating
Drugs
Three ways:
1. By direct chemical stimulation of GI tract
2. By production of bulk or increased fluid in lumen of G tract
3. By lubrication of intestinal bolus to promote passage through GI tract
- for short-term relief of constipation and prevent straining like in post-op, MI or OB
delivery
- for bowel evacuation for diagnostic procedures
- remove ingested poisons from lower GI tract
- most are available OTC but often abused becoming dependent which can develop
chronic intestinal disorders
Contraindications and cautions
- acute abdominal disorders including appendicitis, diverticulitis and ulcerative colitis
when increased motility can lead to rupture or further exacerbation of inflammation -
pregnancy or lactation
Adverse effects
GI - diarrhea, abdominal cramping and nausea
CNS - dizziness, headache and weakness some reported sweating, palpitations, and
flushing
- very common is cathartic dependence
V. Gastrointesinal stimulants
-stimulate parasympathetic activity
Drug
1. Metoclopramide (Plasil, Reglan) - blocks dopamine receptors and makes GI cells more
sensitive to acetylcholine, leading to increased GI activity and rapid movement of food
through the upper GI tract
- for relief of symptoms of GERD, prevent nausea and vomiting post-op and promote GI
movement during small bowel intubation
Actions and indications
- do NOT have local effects of laxatives to increase activity only in intestines
- indicated when more rapid movement of GI contents is desirable
Contraindications and cautions
- allergy, pregnancy or lactation
Adverse effects
- nausea, vomiting, diarrhe, intestinal spasm and cramping, others are declining BP and
heart rate, weakness and fatigue
VI. Antidiarrheal drugs
- block stimulation of GI tract are used for symptomatic relief from diarrhea
Drug
1. loperamide (Imodium) - direct effect on muscle layers of GI tract to slow peristalsis
and allow increased time for absorption of fluid and electrolytes - slowly absorbed
Contraindications and cautions
- allergy, pregnancy or lactation, GI obstruction, acute abdominal conditions or diarrhea
due to poisonings
Adverse effects
- constipation, distention, abdominal discomfort, dry mouth
