DRUGS ACTING ON THE

GASTOINTESTINAL
SYSTEM

PEPTIC ULCERS
Erosions in the lining of the stomach and
adjacent areas of the GIT
Burning pain, hours after meals
Drugs used to treat, prevent or aid in the
healing of these ulcers
Actual cause is not really known
Caused by excessive acid production->
neutralize acid or blocking PNS ->
decrease normal GI activity and
secretions
Caused by H. pylori bacteria

PEPTIC ULCERS
Drugs used to treat ulcers:
a. histamine-2 antagonists block the release of
hydrochloric acid in response to gastrin
b. antacids interact with acids at the chemical
level to neutralize them
c. proton pump inhibitors suppress the secretion
of hydrochloric acid into the lumen of the
stomach
d. antipeptic agents coat injured area in the
stomach to prevent further injury from acid
e. prostaglandins inhibit the secretion of gastrin
and increase the secretion of the stomach,
providing buffer

HISTAMINE-2 ANTAGONISTS
Selectively block H2 receptors-> located in
the parietal cells
Blocking them prevents gastrin -> prevents
release of histamine; stimulation of receptors> production of HCl acid; prevents acid reflux
cimetidine (Tagamet)- first class developed;
antiadrenergic effects; oral and parenteral
ranitidine (Zantac) longer acting; more
potent; oral and parenteral (twice a day)
famotidine (Pepcid) similar to ranitidine in
terms of actions and A/E, but it is much more
potent; can be given to children

HISTAMINE-2 ANTAGONISTS
THERAPEUTIC ACTION:
selectively block histamine-2 receptor sites -> reduction
in gastric acid secretion and pepsin production
USES:
short-term treatment of active duodenal ulcer, benign
gastric ulcer (reduction in the overall acid level can
promote healing and decrease discomfort)
prophylaxis of stress-induced ulcers and acute upper GI
bleeding (blocking acid protects the stomach lining at
risk because of decreased mucus assoc with stress)
treatment of erosive gastroesophageal reflux (decreasing
regurgitated acid-> healing, decrease pain)
relief symptoms of heartburn, acid indigestion, sour
stomach

HISTAMINE-2 ANTAGONISTS
PHARMACOKINETICS:
A: oral; D: crosses placenta and BM; M: liver; E: urine

CONTRAINDICATIONS:
allergies

CAUTIONS:
pregnancy, lactation, hepatic/renal dysfunction
care for prolonged use -> may mask more serious problems

ADVERSE EFFECTS:
diarrhea, constipation, dizziness, headache, somnolence,
confusion, arrhythmias, hypotension (IM/IV; prolonged
use); gynecomastia, impotence

ANTACIDS
inorganic chemicals -> neutralize stomach
acid; OTC
frequent administration leads to acid rebound
neutralizing the stomach contents to an
alkaline level stimulated gastrin production to
cause an increase in acid production and
return the stomach to its normal acidic state
choice of antacids depends on A?E and
absorption factors
sodium bicarbonate oldest
calcium bicarbonate causes constipation and
acid rebound

ANTACIDS
magnesium salts (Milk of Magnesia) very
effective in buffering acid; causes diarrhea; nerve
damage; coma; DOC for pregnancy and lactation
(not systemic)
aluminum salts (Amphojel) do not cause acid
rebound, but not very effective; severe
constipation, hypophosphatemia -> Ca imbalance
magaldrate (Lowsium, Riopan) combination;
decrease GI A/E, may cause rebound hyperacidity
and alkalosis; Maalox = Ca + Al buffers acid and
neither constipation and diarrhea;
MylantaII- antigas agent; 1-3 hrs after meals
antacids greatly affect the absorption of other
drugs-> separate from other meds 1-2 hrs

ANTACIDS
THERAPEUTIC ACTIONS:
neutralizes stomach acid by direct chemical
reaction

USES:
symptomatic relief of upset stomach assoc
with hyperacidity, hyperacidity assoc with
PUD, gastritis, esophagitis, gastric
hyperacidity

CONTRAINDICATIONS:
allergies

ANTACIDS
CAUTIONS:
electrolyte imbalance, GI obstruction,
allergy, renal dysfunction, pregnancy and
lactation, acid-base imbalance

ADVERSE EFFECTS:
related to acid-base levels and electrolytes;
rebound acidity; nausea, vomiting,
neuromuscular changes, headache,
irritability, muscle twitching, coma,
constipation, diarrhea, fluid retention and
CHF

PROTON PUMP INHIBITORS

suppress/inhibiting gastric acid secretion by
inhibiting hydrogen-potassium adenosine
triphosphatase (H+, K+-ATPase) enzyme system on
the secretory surface -> blocking the final step in
acid production -> lowering acid levels in the
stomach
omeprazole (Omepron) faster-acting; more
quickly excreted; used in combination therapy to
treat ulcers by H. pylori; heartburn (OTC)
esomeprazole (Nexium) longer-acting; not broken
down fast; GERD, severe erosive esophagitis
lansoprazole (Prevacid) delayed-release form, IV;
gastric ulcers, GERD, hypersecretory syndromes,
healing duodenal ulcers, eradication of H. pylori

PROTON PUMP INHIBITORS

THERAPEUTIC ACTIONS
act at specific secretory surface receptors
to prevent the final step of acid
production -? Decrease the acid level in
the stomach

USES: stated above

PHARMACOKINETICS:
A: GIT; M: liver; E: urine

PROTON PUMP INHIBITORS

CONTRAINDICATIONS: allergies
CAUTIONS: pregnancy and lactation

ADVERSE EFFECTS:
dizziness, headache, asthenia, vertigo,
insomnia, apathy, dream abnormalities,
diarrhea, abdominal pain, nausea,
vomiting, dry mouth, cough, stuffy nose,
hoarseness, epistaxis, pruritus, dry skin,
back pain, fever

ANTIPEPTIC AGENT
eroded ulcer sites in the GIT from further damage by acid
and digestive enzymes
sucralfate (Carafate)

THERAPEUTIC ACTIONS:
forms an ulcer-adherent complex at duodenal ulcer sites
-> protecting the sites against acid, pepsin and bile salts
-> prevents further breakdown of the area-> healing

USES:
short-term treatment of duodenal ulcers (reduced dose
for maintenance)

PHARMACOKINETICS:
A and M: liver; crosses placenta and BM

ANTIPEPTIC AGENT
CONTRAINDICATIONS:
allergies; renal failure; undergoing
dialysis
CAUTIONS: pregnancy and lactation

ADVERSE EFFECTS:
constipation (most common), diarrhea,
nausea, indigestion, gastric discomfort,
dry mouth, dizziness, sleepiness, vertigo,
skin rash, back pain

PROSTAGLANDIN
used to protect the lining of the stomach in situations that
may lead to serious GI complications
misoprostol(Cytotec)

THERAPEUTIC ACTIONS:
inhibits gastric acid secretion and increases bicarbonate and
mucous production in the stomach -> protecting the
stomach lining

USES:
prevent NSAID-induced gastric ulcers (at meals and at
bedtime); treatment of duodenal ulcers; abortifacient

PHARMACOKINETICS:
A: GIT; M: liver; E: urine (crosses placenta and breast milk>should not be given to pregnants)

PROSTAGLANDIN
CONTRAINDICATIONS:
Pregnancy (ensure negative pregnancy test
within 2 weeks before treatment)

CAUTIONS: allergy and lactation

ADVERSE EFFECTS:
Related to GI effects: nausea, diarrhea,
abdominal pain, flatulence, vomiting, dyspepsia,
constipation
Effects on uterus: miscarriages, excessive
bleeding, spotting, cramping, dysmenorrhea
and other menstrual disorders

LAXATIVES AND ANTIDIARRHEAL AGENTS

Drugs used to affect the motor activity of

the GIT
Can speed up or improve the movement
of intestinal contents along GIT in
constipation
Also used to increase the tone of the GIT
and to stimulate motility
Can also be used to decrease movement
along the GIT when rapid movement of
contents occur in diarrhea

LAXATIVES
Cathartic drugs, used to speed up the
passage of intestinal contents
Chemical stimulants (irritate the lining of
GIT), bulk stimulants (mechanical
stimulants), lubricants (helps to move the
contents more smoothly)

LAXATIVES: CHEMICAL STIMULANTS

cascara (generic)-intestinal evacuation;
senna (Senekot)-similar to cascara, OTC;
castor oil old, standby, thorough
evacuation, starts at the small intestines
throughout the rest of the GIT; frequent
use is not desirable -> constipation and
blocks absorption of fats
bisacodil (Dulcolax)- DOC preop; oral or
rectal

LAXATIVES: BULK STIMULANTS

rapid-acting, aggressive laxatives ->
increase the motility of GIT by increasing
the fluid in the intestinal contents
magnesium sulfate (Epsom salts)-very
potent laxative, total evacuation is needed
magnesium citrate (Citrate of Magnesia)often used to stimulate bowel evacuation
before GI tests and exams
magnesium hydroxide (Milk of Magnesia)
milder and slower-acting laxative
lactulose (Chronulac) alternative choice
for patients with CV problems

LAXATIVES: LUBRICATING LAXATIVES

hemorrhoids, rectal surgery, harmed by
straining
glycerin(Sani-Supp) suppository, no
systemic effect
mineral oil (Agoral plain) oldest; not
absorbed and forms and slippery coat
around the contents; frequent use can
interfere with absorption of fat-soluble
vitamins; leakage and staining can
develop

LAXATIVES
THERAPEUTIC ACTIONS:
direct chemical stimulation of GIT
production of bulk or increased fluid in the lumen
of the GIT
lubrication of intestinal bolus -> promote passage

USES:
short-term relief of constipation; to prevent
straining; to evacuate bowel; to remove poisons;
adjunct in anthelmintic therapy

PHARMACOKINETICS:
- A: GIT; D: castor oil is not used during pregnancy

LAXATIVES
CONTRAINDICATIONS:
appendicitis, ulcerative colitis -> can lead to
rupture or exacerbation

CAUTION: pregnancy and lactation

ADVERSE EFFECTS:
diarrhea, abdominal cramping, nausea;
dizziness, headache, weakness, sweating,
palpitations, flushing
cathartic dependence -> laxative abuse,
used over long periods of time

LAXATIVES
CONTRAINDICATIONS:
appendicitis, ulcerative colitis -> can lead
to rupture or exacerbation

CAUTION: pregnancy and lactation

ADVERSE EFFECTS:
diarrhea, abdominal cramping, nausea;
dizziness, headache, weakness, sweating,
palpitations, flushing
cathartic dependence

ANTIDIARRHEAL DRUGS
block stimulation of GIT; used for diarrhea
loperamide (Imodium) direct effect on
the muscle layers of GIT->slow peristalsis
and allow increased time for absorption of
fluid and electrolytes; slowly absorbed,
metabolized by liver, excreted by urine
and feces; crosses placenta and breast
milk
opium derivatives-> block nerve impulses
within the GIT -> stopping peristalsis and
diarrhea (diphenoxylate with atropine
[Lomotil])

ANTIDIARRHEAL DRUGS
THERAPEUTIC ACTIONS:
slow the motility of the GIT through direct
action on the lining of the GIT to inhibit
local reflexes
through direct action on the muscles of the
GIT to slow activity
actions on the CNS receptors

USES:
relief symptoms of acute and chronic
diarrhea, prevention and treatment of
travelers diarrhea