Gastrointestinal

Drugs
Outline

• Gastrointestinal Tract • Antiulcer Drugs

Disorders
Overview of the
Gastrointestinal system
Oral Cavity The oral cavity, or mouth, starts the
digestive process by (1) breaking up food into smaller
particles; (2) adding saliva, which contains the enzyme
amylase for digesting starch (the beginning of the
digestive process); and (3) swallowing, a voluntary
movement of food that becomes involuntary (peristalsis)
in the esophagus, stomach, and intestines. Swallowing
occurs in the pharynx (throat), which connects the mouth
and esophagus.
Overview of the
Gastrointestinal system
Esophagus
The esophagus, a tube that extends from
the pharynx to the stomach, is composed
of striated muscle in its upper portion and
smooth muscle in its lower portion. The
inner lining of the esophagus is a mucous
membrane that secretes mucus.
Overview of the
Gastrointestinal system
Stomach
The stomach is a hollow organ that
lies between the esophagus and the
intestine.
Overview of the
Gastrointestinal system
Small Intestine
The small intestine begins at the
pyloric sphincter of the stomach and
extends to the ileocecal valve at the
cecum. Most drug absorption occurs
in the duodenum, but lipid-soluble
drugs and alcohol are absorbed from
the stomach.
Overview of the
Gastrointestinal system
Large Intestine

The large intestine accepts undigested

material from the small intestine, absorbs
water, secretes mucus, and with peristaltic
contractions moves the remaining intestinal
contents to the rectum for elimination.
Drugs for Gastrointestinal
Disorders
Vomiting, diarrhea, and constipation are GI problems that
frequently require drug intervention.

Nursing process is

Antiemetics used to
2 4 considered in relation

control vomiting Antidiarrheal drugs to each of these drug

groups

1 3 Laxatives
5
Emetics used to
eliminate ingested
toxins and drugs
 Vomiting
Vomiting (emesis), the expulsion of gastric
contents, has a multitude of causes,
including motion sickness, viral and
bacterial infection, food intolerance,
surgery, pregnancy, pain, shock, effects of
selected drugs (e.g., antineoplastics,
antibiotics), radiation, and disturbances of
the middle ear that affect equilibrium.
 Vomiting
Nonpharmacologic measures should be used
first when nausea and vomiting occur. If the
nonpharmacologic measures are not effective,
antiemetics are combined with
nonpharmacologic measures. The two major
groups of antiemetics are nonprescription
(antihistamines, bismuth subsalicylate, and
phosphorated carbohydrate solution) and
prescription (antihistamines, dopamine
antagonists, benzodiazepines, serotonin
antagonists, butyrophenones, glucocorticoids,
cannabinoids, and miscellaneous antiemetics).
 Vomiting
Nonpharmacologic Measures
The nonpharmacologic methods of
decreasing nausea and vomiting
include administration of weak tea, flat
soda, gelatin, Gatorade, and Pedialyte
(for use in children). Crackers and dry
toast may be helpful. When
dehydration becomes severe,
intravenous (IV) fluids are needed to
restore body fluid balance.
 Nonprescription Antiemetics
Nonprescription antiemetics (antivomiting agents) can be
purchased as over-the-counter (OTC) drugs. These
drugs are frequently used to prevent motion sickness but
have minimal effect on controlling severe vomiting
resulting from anticancer agents (antineoplastics),
radiation, and toxins.

To prevent motion sickness, the antiemetic should be

taken 30 minutes before travel. These drugs are not
effective in relieving motion sickness if taken after
vomiting has occurred.
 Nonprescription Antiemetics
Selected antihistamine antiemetics—such
as dimenhydrinate, cyclizine hydrochloride,
meclizine hydrochloride, and
diphenhydramine hydrochloride—can be
purchased without a prescription to prevent
nausea, vomiting, and dizziness (vertigo)
caused by motion. These drugs inhibit
vestibular stimulation in the middle ear.
 Nonprescription Antiemetics
The side effects of antihistamine
antiemetics are similar to those of
anticholinergics and include
drowsiness, dry mouth, and
constipation.
 Nonprescription Antiemetics
Several nonprescription drugs, such as
bismuth subsalicylate, act directly on the
gastric mucosa to suppress vomiting.
They are marketed in liquid and chewable
tablet forms and can be taken for gastric
discomfort or diarrhea.
 Prescription
Antiemetics
Common prescription antiemetics are
classified into the following groups: (1)
antihistamines, (2) anticholinergics, (3)
dopamine antagonists, (4)
benzodiazepines, (5) serotonin
antagonists, (6) glucocorticoids, (7)
cannabinoids (for patients with certain
diagnoses, such as cancer), and (8)
miscellaneous
Antihistamines and
Dopamine Antagonists
Anticholinergics These agents suppress emesis by blocking
dopamine (D2 ) receptors in the CTZ
Side Effects and Adverse Reactions
Side effects include drowsiness, which
can be a major problem; dry mouth;
blurred vision caused by pupillary
dilation; tachycardia (with Phenothiazine Antiemetics
anticholinergic use); and constipation. Selected piperazine phenothiazines are used to
treat nausea and vomiting resulting from surgery,
These drugs should not be used by anesthetics, chemotherapy, and radiation sickness
patients with glaucoma.
Butyrophenones
Droperidol, like phenothiazines, block the D2 receptors
in the CTZ. They are used to treat postoperative
nausea and the vomiting and emesis associated with
toxins, cancer chemotherapy, and radiation therapy.
Like phenothiazines, droperidol is likely to cause
extrapyramidal symptoms if used for an extended time.
Hypotension may result; therefore blood pressure
should be monitored.
Benzodiazepines
Select benzodiazepines indirectly control nausea and
vomiting that may occur with cancer chemotherapy.
Lorazepam is the drug of choice. Previously,
diazepam was the preferred benzodiazepine, but
lorazepam effectively provides emesis control,
sedation, anxiety reduction, and amnesia when used
in combination with a glucocorticoid and serotonin (5-
HT3 )-receptor antagonist.
Serotonin-Receptor
Antagonists
Serotonin antagonists—ondansetron, granisetron,
dolasetron, and palonosetron—are the most effective of
all antiemetics in suppressing nausea and vomiting
caused by cancer chemotherapy–induced emesis or
emetogenic anticancer drugs.

They are also effective in preventing nausea and

vomiting before and after surgery. Common side effects
include headache, dizziness, hypotension, palpitations,
constipation, edema, and fatigue.
Glucocorticoids
(Corticosteroids)
Dexamethasone and methylprednisolone
are two agents that are effective in
suppressing emesis associated with
cancer chemotherapy.
 Cannabinoids
Cannabinoids, the active ingredients in
Cannabis, were approved for clinical use in 1985
to alleviate nausea and vomiting resulting from
cancer treatment. These agents may be
prescribed for patients receiving chemotherapy
who do not respond to or are unable to take
other antiemetics. They are contraindicated for
patients with psychiatric disorders.

Cannabinoids can be used as an appetite

stimulant for patients with acquired
immunodeficiency syndrome (AIDS).
Miscellaneous Antiemetics
Trimethobenzamide Metoclopramide
The drug suppresses suppresses emesis
impulses to the CTZ.

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 Patient Safety

Do not Confuse…
• Antivert, an antiemetic, with Axert, an antimigraine drug
•Lorazepam, which controls nausea and vomiting, with alprazolam, an anxiolytic
• Hydroxyzine, an antiemetic, with hydralazine, an antihypertensive drug
 Emetics
Emetics are drugs used to induce vomiting

When an individual has Vomiting should not be To prevent aspiration, Activated charcoal is
consumed certain toxic induced if caustic vomiting should also be given or gastric lavage
substances, induced substances such as avoided if petroleum is done when emesis is
vomiting (emesis) may ammonia, chlorine distillates are ingested; contraindicated
be indicated to expel the bleach, lye, toilet these include gasoline,
substance before cleaners, or battery acid kerosene, paint
absorption occurs. have been ingested thinners, and lighter
fluid.
Diarrhea
Travelers’ Diarrhea
• Travelers’ diarrhea, also called acute
diarrhea, is usually caused by E. coli. It
ordinarily lasts less than 2 days;
however, if it becomes severe,
fluoroquinolone antibiotics are usually
prescribed. Loperamide may be used to
slow peristalsis and decrease the
frequency of defecation, but it can also
slow the exit of the organism from the GI
tract. Travelers’ diarrhea can be reduced
by drinking bo
Antidiarrheals
Opiates and Opiate-
Related Agents
Opiates decrease intestinal
motility, thereby decreasing
peristalsis. Constipation is a
common side effect of opium
preparations. Codeine is an
example
Opiates and Opiate-
Related Agents
Opiates are frequently combined with other
antidiarrheal agents. Opium antidiarrheals can
cause CNS depression when taken with
alcohol, sedatives, or tranquilizers. The
duration of action of opiates is
approximately 2 hours.
 Opiates and Opiate-
Related Agents
Diphenoxylate with atropine is an
opiate that has less potential for
causing drug dependence than other
opiates such as codeine. Difenoxin is
an active metabolite of diphenoxylate,
but it is more potent than
diphenoxylate.
 Opiates and Opiate-
Related Agents
Loperamide is structurally related to
diphenoxylate but causes less CNS
depression than diphenoxylate and
difenoxin. It can be purchased as an OTC
drug, and it protects against diarrhea,
reduces fecal volume, and decreases
intestinal fluid and electrolyte losses.
Patients with severe hepatic impairment
should not take products that contain
diphenoxylate, difenoxin, or loperamide.
Children and older adults who take
diphenoxylate are more susceptible to
respiratory depression than are other age
groups.
Adsorbents
Adsorbents
Adsorbents act by coating
the wall of the GI tract and
adsorbing bacteria or
toxins that cause diarrhea.
Adsorbent antidiarrheals
include kaolin and pectin.
Adsorbents
Bismuth subsalicylate is considered an
adsorbent because it adsorbs bacterial
toxins. Bismuth subsalicylate is an OTC
drug commonly used to treat travelers’
diarrhea, and it can also be used as an
antacid for gastric discomfort.
Constipation
 Constipation
Constipation, the accumulation of
hard fecal material in the large
intestine, is a relatively common
complaint and a major problem for
older adults. Insufficient water intake
and poor dietary habits are
contributing factors.
Nonpharmacologic
Measures
1 2 3 4

Diet (high Water Exercise Routine

fiber) bowel
habits
 Laxatives
Laxatives and cathartics are used to eliminate
Purgatives
harsh cathartics that cause a
fecal matter. Laxatives promote a soft stool,
cathartics result in a soft to watery stool with watery stool with abdominal
some cramping, and frequently dosage cramping.
determines whether a drug acts as a laxative or
cathartic.

O T
OPPORTUNITIES
What are your goals? THREATS
What are the blockers you're facing?
Are demands shifting? How can it be improved? What are factors outside of your control?
Laxatives – Four Types
Osmotics (saline) Stimulants (contact or
irritants)

Bulk-forming Emollients (stool

softeners).
 Laxatives should be avoided if there is any
question that the patient may have intestinal
obstruction; if abdominal pain is severe; or if
symptoms of appendicitis, ulcerative colitis,
or diverticulitis are present. Most laxatives
stimulate peristalsis.
 Osmotic (Saline) Laxatives
Osmotics, hyperosmolar laxatives, include
salts or saline products, lactulose, and
glycerin. Saline products consist of sodium
or magnesium, and a small amount is
systemically absorbed.
 Stimulant (Contact)
Laxatives
Stimulant (contact or irritant) laxatives
increase peristalsis by irritating sensory
nerve endings in the intestinal mucosa.
Types include those that contain
bisacodyl, senna, and castor oil
(purgative). Bisacodyl is the most
frequently used and abused laxative and
can be purchased OTC.
 Stimulant (Contact)
Laxatives
Castor oil is a harsh laxative (purgative) that
acts on the small bowel and produces a watery
stool. The action is quick, within 2 to 6 hours, so
the laxative should not be taken at bedtime.
Castor oil is not FDA approved to correct
constipation, rather it is used mainly for bowel
preparation.
Bulk-Forming Laxatives
Polycarbophil, polyethylene glycol,
methylcellulose, and psyllium are examples of
bulk-forming laxatives. Patients with
hypercalcemia should avoid calcium
polycarbophil because of the significant amount
of calcium in the drug.
Chloride Channel
Activators

• Selective chloride channel

activators are a new
category of laxatives used to
treat idiopathic constipation
in adults.
Emollients (Stool
Softeners)
• Emollients are lubricants and stool
softeners (surface-acting or wetting
drugs) used to prevent constipation.
They are frequently prescribed for
patients after myocardial infarction or
surgery. They are also given before
administration of other laxatives in
treating fecal impaction. Docusate
calcium, docusate sodium, and
docusate sodium with senna are
examples of stool softeners.
Thank
you!