DRUGS FOR GASTROINTESTINAL SYSTEM
Functions of the GI System:
• Ingestion – food must be placed into
the mouth before it can be acted on;
this is an active, voluntary process
called ingestion.
• Propulsion – If foods are to be
processed by more than one digestive
organ, they must be propelled from one
organ to the next; swallowing is one
example of food movement that
depends largely on the propulsive
process called peristalsis (involuntary,
alternating waves of contraction and
relaxation of the muscles in the organ
wall).
• Food breakdown – mechanical
digestion prepares food for further
degradation by enzymes by physically
fragmenting the foods into smaller
pieces, and examples of mechanical
digestion are: mixing of food in the
mouth by the tongue, churning of food
in the stomach, and segmentation in
the small intestine.
• Food breakdown: chemical digestion –
the sequence of steps in which the large
food molecules are broken down into
their building blocks by enzymes is
called chemical digestion.
• Absorption – transport of digested end
products from the lumen of the GI tract
to the blood or lymph is absorption, and
for absorption to happen, the digested
foods must first enter the mucosal cells
by active or passive transport
processes.
• Defecation – is the elimination of
indigestible residues from the GI tract
via the anus in the form of feces.
Peptic Ulcer
• An ulcer is an erosion of the mucosa
layer of the GI tract, usually associated
with acute inflammation. Although
ulcers may occur in any portion of the
alimentary canal, the duodenum is the
most common site.
• The term peptic ulcer refers to a lesion
located in either the stomach (gastric)
or small intestine (duodenal)
Peptic ulcer disease is associated with the
following risk factors:
• Close family history of PUD.
• Blood group O.
• Smoking tobacco (increases gastric acid
secretion).
• Consumption of beverages and food
that contain caffeine.
• Drugs, particularly corticosteroids,
nonsteroidal anti-inflammatory drugs
(NSAIDS), and platelet inhibitors such as
aspirin and clopidogrel.
• Excessive psychological stress.
• Infection with Helicobacter pylori.
Gastroesophageal reflux disease
• (GERD) is a common condition in which
the acidic contents of the stomach
move upward into the esophagus. This
causes an intense burning (heartburn)
sometimes accompanied by belching.
• The cause of GERD is usually a
weakening of the lower esophageal
sphincter.
• GERD is associated with obesity, and
losing weight may eliminate the
symptoms. Other lifestyle changes that
can improve GERD symptoms include
elevating the head of the bed, avoiding
fatty or acidic foods, eating smaller
meals at least 3 hours before sleep, and
eliminating tobacco and alcohol use.
Proton Pump Inhibitors
• Proton pump inhibitors act by blocking
the enzyme responsible for secreting
hydrochloric acid in the stomach.
• reduce acid secretion in the stomach by
binding irreversibly to H+
• , K+ -ATPase, the enzyme that acts as a
pump to release acid (also called H+, or
protons) onto the surface of the GI
mucosa.
• The PPIs reduce acid secretion to a
greater extent than the H2-receptor
antagonists and have a longer duration
of action.
• PPIs heal more than 90% of duodenal
ulcers within 4 weeks and about 90% of
gastric ulcers in 6 to 8 weeks.
Omeprazole (Prilosec)
Therapeutic Class: Antiulcer drug
Pharmacologic Class: Proton pump
inhibitor
Actions and Uses
o It reduces acid secretion in the
stomach by binding irreversibly to
the enzyme H+, K+ -ATPase.
Although this drug can take 2 hours
to reach therapeutic levels, its
effects last up to 72 hours.
o It is used for the short-term, 4- to 8-
week therapy of active peptic ulcers
and GERD.
Administration Alert
o If possible, administer before
breakfast on an empty
stomach.
o It may be administered with
antacids.
o Capsules and tablets should not
be chewed, divided, or crushed.
o Pregnancy category C
Adverse Effects
o Adverse effects are generally minor
and include headache, nausea,
diarrhea, rash, and abdominal pain.
o Although rare, blood disorders may
occur, causing unusual fatigue and
weakness.
o Therapy is generally limited to 2
months. Atrophic gastritis and
hypomagnesemia have been
reported rarely with prolonged
treatment with PPIs.
Contraindications:
o The only contraindication is
hypersensitivity to the drug.
o OTC use is not approved for
patients under 18 years of age.
Proton Pump Inhibitors
H2 Receptor Antagonists
• Histamine has two types of receptors:
H1 and H2.
• Activation of H1 receptors produces the
classic symptoms of inflammation and
allergy, whereas the H2 receptors are
responsible for increasing acid secretion
in the stomach.
• The H2-receptor antagonists are
effective at suppressing the volume and
acidity of parietal cell secretions.
Ranitidine (Zantac)
Therapeutic Class: Antiulcer drug
Pharmacologic Class: H2-receptor
antagonist
Actions and Uses
o Ranitidine acts by blocking H2
receptors in the stomach to
decrease acid production.
 o Gastric ulcers require longer
therapy for healing to occur.
Intravenous (IV) and intramuscular
(IM) forms are available for the
treatment of acute, stress-induced
bleeding ulcers.
Administration Alert
o Administer after meals and monitor
liver and renal function.
Aluminum Hydroxide (AlternaGEL, others)
o Pregnancy category B.
Adverse Effects
o Adverse effects are uncommon and
mild.
o Although rare, severe reductions in
the number of red and white blood
cells and platelets are possible;
thus, periodic blood counts may be
performed.
o High doses may result in impotence
or loss of libido in men.
Contraindications
o Contraindications include
hypersensitivity to H2-receptor
antagonists, acute porphyria, and
OTC administration in children less
than 12 years of age.
H2 Receptor Antagonists
Antacids
• Antacids are alkaline, inorganic
compounds of aluminum, magnesium,
sodium, or calcium.
• Combinations of aluminum hydroxide
and magnesium hydroxide, the most
common type, are capable of rapidly
neutralizing stomach acid. Chewable
tablets and liquid formulations are
available.
• A few products combine antacids and
H2-receptor blockers into a single
tablet.
• Self-medication with antacids is safe
when taken in doses directed on the
labels. Although antacids act within 10
to 15minutes, their duration of action is
only 2 hours; thus, they must be taken
often during the day.
Therapeutic Class:
Antiheartburn agent
Pharmacologic Class: Antacid
Actions and Uses
o Aluminum hydroxide is an inorganic
agent used alone or in combination
with other antacids. Combining
aluminum compounds with
magnesium (Gaviscon, Maalox,
Mylanta) increases their
effectiveness and reduces the
potential for constipation.
Administrations Alerts
o Administer aluminum antacids at
least 2 hours before or after other
drugs because absorption could be
affected.
o Pregnancy category C
Adverse Effects
o When taken regularly or in high
doses, aluminum antacids cause
constipation.
o At high doses, aluminum
products bind with phosphate
in the GI tract and long-term
use can result in phosphate
depletion.
 o Those at risk include those who
are malnourished, alcoholics,
and those with renal disease.
Contraindications
o This drug should not be used in
patients with suspected bowel
obstruction.
Antacids
Bowel and Gastrointestinal Conditions
Laxatives
• Bowel disorders, nausea, and vomiting
are among the most common
complaints for which patients seek
medical assistance.
• These nonspecific symptoms may be
caused by a large number of infectious,
metabolic, inflammatory, neoplastic,
and neuropsychological disorders. In
addition, nausea, vomiting,
constipation, and diarrhea are the most
common adverse effects of oral
medications.
• Although symptoms often resolve
without the need for pharmacotherapy,
when severe or prolonged, these
conditions may lead to serious
consequences unless drug therapy is
initiated.
Constipation
• Constipation is a decrease in the
frequency of bowel movements. Stools
may become dry, hard, and difficult to
evacuate from the rectum without
straining.
• Constipation is not a disease but a
symptom of an underlying disorder. The
etiology of constipation may be related
to lack of exercise; insufficient food
intake, especially insoluble dietary fiber;
diminished fluid intake; or a medication
regimen that includes drugs that reduce
intestinal motility.
• Foods that can cause constipation
include alcoholic beverages, products
with a high content of refined white
flour, dairy products, and chocolate.
• Certain diseases such as
hypothyroidism, diabetes, and irritable
bowel syndrome (IBS) can cause
constipation.
• Laxatives promote the evacuation of
the bowel, or defecation, and are
widely used to prevent and treat
constipation.
• Cathartic is a related term that implies
a stronger and more complete bowel
emptying.
• Prophylactic laxative pharmacotherapy
is appropriate following abdominal
surgeries.
• The most common use for laxatives is to
treat simple, chronic constipation.
Occasionally, laxatives are administered
to accelerate the movement of ingested
toxins following poisoning or to remove
dead parasites in the intestinal tract
following anti-helminthic therapy.
1. Bulk-forming laxatives contain fiber, a
substance that absorbs water, and
increases the size of the fecal mass.
2. Saline cathartics, also called osmotic
laxatives, are not absorbed in the
intestine; they pull water into the fecal
mass to create a more watery stool.
3. Stimulant laxatives promote peristalsis
by irritating the bowel mucosa. They
are rapid acting and more likely to
cause diarrhea and cramping than the
bulk forming laxatives.
4. Stool softeners or surfactant laxatives
cause more water and fat to be
absorbed into the stools.
 5. Herbal agents are natural products that
are available OTC and are widely used
for self-treatment of constipation.
Nausea and Vomiting
6. Miscellaneous drugs include mineral
oil, which acts by lubricating the stool
and the colon mucosa.
Diarrhea
• Diarrhea may be considered a type of
body defense, rapidly and completely
eliminating the body of toxins and
pathogens. When prolonged or severe,
especially in children, diarrhea can
result in significant loss of body fluids,
and pharmacotherapy is indicated.
• Diarrhea may be caused by certain
medications, infections of the bowel,
and substances such as lactose.
• Assessing the patient’s recent travels,
dietary habits, immune system
competence, and recent drug history
may provide information about its
etiology.
Antidiarrheals
Antiemetics
• The most effective drugs for the
symptomatic treatment of diarrhea are
the opioids, which can dramatically
slow peristalsis in the colon.
• The most common opioid antidiarrheals
are codeine and diphenoxylate with
atropine (Lomotil).
• OTC drugs for diarrhea act by a number
of different mechanisms. Loperamide
(Imodium) is similar to meperidine but
it has no narcotic effects and is not
classified as a controlled substance.
• Probiotic supplements containing
Lactobacillus, a normal inhabitant of the
human gut and vagina, are sometimes
taken to correct the altered GI flora
following a serious diarrhea episode.
• Antidiarrheal medications should never
be used to treat diarrhea caused by
poisoning or infection by toxin
producing organisms.
• Nausea is an unpleasant, subjective
sensation that is accompanied by
weakness, diaphoresis, and
hyperproduction of saliva. It is
sometimes accompanied by dizziness.
Intense nausea often leads to vomiting,
or emesis.
• Vomiting is a defense mechanism used
by the body to rid itself of toxic
substances. Vomiting is a reflex
primarily controlled by the vomiting
center of the medulla of the brain,
which receives sensory signals from the
digestive tract, the inner ear, and the
chemoreceptor trigger zone (CTZ) in the
cerebral cortex.
• Once the vomiting reflex is triggered,
wavelike contractions of the stomach
quickly propel its contents upward and
out of the body.
• A large number of antiemetics are
available to treat nausea and vomiting.
• Selection of a particular agent depends
on the experience of the health care
provider and the cause of the nausea
and vomiting.
• Relief of serious nausea or vomiting,
however, requires prescription
medications.
• Patients who are receiving
antineoplastic drugs may receive three
or more antiemetics concurrently to
reduce the nausea and vomiting from
chemotherapy
Serotonin (5-HT3) Antagonists
o The serotonin antagonists
include dolasetron (Anzemet),
 granisetron (Kytril, Sancuso), therapy is sometimes treated with
ondansetron (Zofran, Zuplenz), the phenothiazines.
and palonosetron (Aloxi). o To prevent loss of the antiemetic
o These are preferred drugs for medication due to vomiting, some
the pharmacotherapy of serious of these medications are available
nausea and vomiting caused by through the intramuscular (IM), IV,
antineoplastic therapy, and/or suppository routes.
radiation therapy, or surgical o Nonphenothiazine antipsychotics
procedures. that have high antiemetic activity
o They are usually given include haloperidol (Haldol) and
prophylactically, just prior to droperidol (Inapsine).
antineoplastic therapy.
Corticosteroids
Intravenous (IV), oral, and
transdermal patch forms are o Dexamethasone (Decadron) and
available. methylprednisolone (Solu-Medrol)
o The few adverse effects include are used to prevent chemotherapy-
headache, constipation or induced and postsurgical nausea
diarrhea, and dizziness and vomiting.
o They are reserved for the short-
Antihistamines and Anticholinergics
term therapy of acute cases
o These drugs are effective for because of the potential for serious
treating simple nausea, with some long-term adverse effects.
being available OTC. For example,
nausea due to motion sickness is
effectively treated with
anticholinergics or antihistamines.
o Motion sickness is a disorder
affecting a portion of the inner ear
that is associated with significant
nausea.
o Drugs used to treat motion sickness
are most effective when taken 20 to
60 minutes before travel is
expected

Phenothiazine and Phenothiazine-like

Drugs

o The major indication for

phenothiazines relates to treating
psychoses, but they are also very
effective antiemetics.
o The serious nausea and vomiting
associated with antineoplastic