DRUGS FOR GASTROINTESTINAL TRACT
DISORDER
 Vomiting (emesis), the expulsion of
gastric content has a multitude of
causes
 Motion sickness
 Viral and bacterial infection
 Food intolerance
 Surgery
 Pregnancy
 Pain
 Effects of selected drugs
(antineoplastic)
 Nausea a queasy sensation, may or may
not precede the expulsion. The causes
of vomiting must be identified
 Cause of vomiting
o A. CTZ chemoreceptor trigger
zone, lies near the medulla (
drugs, toxins)
o B. vomiting center in the
medulla (odor, smell, taste)
causes vomiting when
stimulated
The vestibular center in the ear – transmits
impulse to the vomiting center
Dopamine – neurotransmitter stimulates the
CTZ
Levodopa – contains dopamine like properties
which can cause vomiting
Acetylcholine – a neurotransmitter that is also a
vomiting stimulant
How vomiting occurs??
 Vomiting center stimulated  motor
neurons respond (contraction of the
diaphragm, anterior abdomen muscle
and the stomach)  the glottis closes
 the abdominal wall moves upward
and vomiting occurs
TWO MAJOR GROUPS OF ANTIEMETICS
 Nonprescription
o Antihistamine
o Bismuth subsalicylate
o Phosphorated carbohydrate
solution
ANTIEMETICS
 Trimethobenzamide (tigan )
o Safe for pregnancy and can be
administered
o Although this drug is classified
as pregnancy category C
NON PRESCRIPTION ANTIEMETICS :
ANTIHISTAMINE
GENERIC BRAND (MOTION SICKNESS) :
 cyclizine HCL”merezine
ROUTE AND DOSAGE:
 A:PO: 50 mg q4-6 h, max 200 mg/ d
 C : 6-12 y PO : 25 mg q6-8h, max 75
mg/d
USES AND CONSIDERATION
 Used for prevention and treatment of
nausea, vomiting and motion sickness,
pregnancy category B, PB, UK, 1 ½ :13h
GENERIC BRAND
 Dimenhydrinate (Dramamine)
ROUTE AND DOSAGE
 A: PO 50 -100 mg q4-6h, max 400 mg /d
: IM/IV : 50 mg PRN ,max 300 mg/d
  C: 6-12 y PO 25-50 mg q6-8h PRN max
150 mg/d
 C 2-5 y 12.5-25 mg q6-8h PRN; max 150
mg/d
 C2-5y : 12.5 – 25 mg q6-8h PRN; max 75
mg/d
USES AND CONSIDERATIONS
 Primarily used to prevent motion
sickness, drowsiness, dizziness, dry
mouth and hypotension may occur
pregnancy category B, PB, 78% : t ½ :
35h
GENERIC BRAND
 Meclizine HCI (antivert)
ROUTE AND DOSAGE
 A/C: > 12 y : PO 25-50 mg 1h before
travel, after meal, may repeat q24h \
 Vertigo
o A : PO 25-100 mg/d in divided
doses
USES AND CONSIDERATION
 Prevention of nausea, vomiting and
dizziness, drowsiness and dry mouth
may occur pregnancy category B, PB,
UK, 1 ½ 5-6 h
Category
A  adequate and well controlled human
studies have failed to demonstrate a risk to the
fetus in the first trimester of pregnancy (and
there is no evidence of risk in later trimester
B  animal reproduction studies have failed to
demonstrate a risk to the fetus and there are no
adequate and well controlled studies in
pregnant women or animal studies have shown
an adverse effect but adequate and well
controlled studies in pregnant women have
failed to demonstrate a risk to the fetus in any
trimester
C animal reproduction studies have shown
am adverse effect on the fetus and there are no
adequate and well controlled studies in human
but potential benefits may warrant use of the
drug in pregnant women despite potential risk
D there is positive evidence of human fetal
risk based on adverse reaction data from
investigation or marketing experience or studies
in human but potential benefits may warrant
use of the drug in pregnant women despite
potential risk
GENERIC (BRAND) ‘prescription antihistamine”
 A  Hydroxyzine (vistaril)
 B  promethazine (Phenergan)
ROUTE AND DOSAGE
 A.  A PO/IM 25/100 mg tid/qid PRN:
max 400 mg/d
 A  C: IM 1.1 mg/kg q4-6h
 B  see prototype drug chart 47.1
USES AND CONSIDERATION
 For postoperative nausea and vomiting
and vertigo
 Give preoperatively with narcortics to
decrease ____
 Give hydroxyzine deep IM drowsiness
and dry mouth usually occur pregnancy
category X, PB, UK
ANTICHOLINERGIC
GENERIC (BRAND)
  Scopolamine ( Transderm scop)
ROUTE AND DOSAGE
 A. transdermal patch 1.5 mg ( 1 mg
dose over 3d) apply patch behind ear
atleast 4 h before antiemetic effect is
required
USES AND CONSIDERATION
 For motion sickness anticholinergic side
effect (dizziness, dry mouth, drowsiness
, constipation ) patch effective for 1
day. Alternate ears if using for longer
than 3 days. Wash hands after applying
disc/ patch. Wear no more than are
disc/ patch at a time. Pregnancy
category C, PB, c25%, 1 ½ 8 h
DOPAMINE ANTAGONISTS PHENOTHIAZINES
--------------------------------
Non pharmacologic measures
 Administration
o Weak tea
o Flat soda
o Gelatin
o Gatorade
o Pedialyte
Non prescription antiemetics
 Can be purchased as OTC drugs
o Dimenhydrinate (Dramamine)
o Cyclizine hydrochloride
(marezine)
o Meclizine hydrochloride
(antivert )
o Diphenhydramine
hydrochloride ( benadryl)
Antihistamine antiemetic
 Side effects:
o Similar to those of
anticholinergic
 Drowsiness
 Dryness of the mouth
 Constipation
Theses drugs inhibit vestibular stimulation in
the middle ear
Benadryl is also used to prevent or alleviate
allergic reaction to drugs, insects and food by
acting as an antagonist to histamine (H1)
receptor
ANTIEMETICS
NON PRESCIRPTION
 Cyclizine HCL (marezine)
o A: 50 mg. q4-6hr max : 200
mg/d
o C: 6-12 y/ : PO 25 mg q6-8hr.
max: 75 mg/d
 Dimenhydrinate (Dramamine )
o A: PO : 50 – 100 mg, q4-6hr,
max : 400 mg/d
o C: 6-12 y/o : PO : 25 -50 mg q6-
8hr, PRN
o Meclizine HCL (antivert)
o A/C :> y/o : PO : 25-50 mg, 1 hr,
before travel
PRESCRIPTION
 Hydroxyzine (vistaril)
o A: PO/IM : 25 -100 mg tid, PRN
o C: IM: 1 mg/kg q4-6 hr
 Promethazine (Phenergan)
  Scopolamine (transderm scop) o Benzodiazepines
transdermal patch 1.5 mg apply behind  Side effects : extrapyramidal symptoms
ear (EPS)

Prescription antiemetic DOPAMINE ANTAGONIST

Classification  Extrapyramidal symptoms

 Antihistamine
 Anticholinergic
 Dopamine antagonist
 Benzodiazepines
 Serotonin antagonist
 Glucocorticoid
 Cannabinoids ( for patient with cancer)
Prescription antiemetics
 Antihistamine and anticholinergic
o Act primarily on the vomiting
center (lower medulla
oblongata)
o Act by decreasing the
stimulation of the CTZ
(chemoreceptor trigger zone )
 medulla oblongata
 Antihistamine and anticholinergics
o Drowsiness  major problem
o Dry mouth
o Blurred vision  primarily
dilation
o Tachycardia  anticholinergic
use
o Constipation
Should not be used to patient with glaucoma
DOPAMINE ANTAGONIST
 Suppress emesis by blocking dopamine
2 receptor in the CTZ
 Categories
o Phenothiazines
o Butyrophenones
o Parkinsonism
o Dystonias
o Akathisias
o Dyskinesias
PHENOTHIAZINE ANTIEMETIC
 Piperazine phenothiazines
 Treat nausea and vomiting resulting
from :
o Surgery
o Anesthetics
o Chemotherapy
o Radiation sickness
 Piperazine phenothiazines
o Chlorpromazine (thorazine)
o Prochlorperazine (edisylate)
o the first phenothiazines used
for both psychosis and
vomiting
o promethazine (phenergan ),
introduced as antihistamine in
the 1940’s
o sedative effect, for motion
sickness, nausea and vomiting
 promethazine (Phenergan)
o CNS depressant effect when
taken with
 Alcohol
 Narcotics
 Sedative hypnotics
 General anesthetics
BUTYROPHENONES
 Haloperidol (Haldol)
  Droperidol (inapsine)
o Blocks the dopamine 2
receptors in the CTZ used to
treat post op nausea and
vomiting emesis associated
with toxins cancer
chemotherapy radiation
therapy
 Monitor BP hypotension may result
BENZODIAZEPINES
 Lorazepam (Ativan) drug of choice
o Control nausea and vomiting
that may occur with cancer
chemotherapy
 Diazepam (valium) previously preferred
benzodiazepine
 Lorazepam – sedation, anxiety
reduction, amnesia in combination with
glucocorticoids and serotonin 5 HT3
receptors antagonists.
SERATONIN (5-HT3) RECEPTOR ANTAGONISTS
 Serotonin antagonists
 Ondansetron (Zofran)
 Granisetron (kytril)
 Dolasetron (anzemet)
 Palonosetron (aloxi)
o Suppress nausea and vomiting
by blocking the serotonin
receptors (5 – HT3) in the CTZ
and the afferent vagal nerve
terminal in the upper GI tract
 Do not cause EPS as do the
phenothiazine
 Administered orally and IV
 Preventing nausea and vomiting before
and after surgery
 Side effects
o Headache
o Diarrhea
o Dizziness
o Fatigue
GLUCOCORTICOIDS (CORTICOSTEROID)
 Dexamethasone (decadron) and
methylprednisolone (solumedrol)
o Effective in suppressing emesis
associated with cancer
chemotherapy
CANNABINOIDS
 Active ingredients in marijuana
 Approved for clinical use in 1985
 Alleviate nausea and vomiting resulting
from cancer treatment
 Contraindication for patient with
psychiatric disorder
 Use as an appetite stimulant for
patient with acquired
immunodeficiency syndrome (AIDS)
MISCELLANEOUS ANTIEMETICS
 Diphenidol (vontrol) and
trimethobenzamide ( tigan)
o Do not act as antihistamine,
anticholinergic or
phenothiazine.
o Suppress impulse to the CTZ
o Prevents vertigo by inhibiting
impulse to the vestibular area
 Side effects
o Drowsiness
o (anticholinergic symptoms)
o Dry mouth
o Increased heart rate
o Urine retention
o Constipation
o Blurred vision
  Trimethobenzamide can cause
hypotension, diarrhea, EPS
NURSING CONSIDERATION ANTIEMETICS
 Assess onset, frequency amount and
contents of vomitus and the possible
causative e.g food
 Check vital signs
 Observe fro signs and symptoms of
dehydration if vomiting severe
 Mouth care after vomiting
 Issued guidelines that ipecac should no
be administered routinely
 Ipecac syrup not ipecac fluid extract –
fatal
 Should be taken with a glass of water (
do not give milk or carbonated
beverage )
 Onset of emesis 15 – 30 mins
 If vomiting is not induced give activated
charcoal absorbent
 Gastric lavage

METOCLOPRAMIDE (REGLAN)
EMETICS
 Suppress emesis by blocking the
dopamine receptor in the CTZ  Do not induced vomiting to prevent
 Used in the treatment of post operative aspiration if patient swallowed
emesis chemotherapy and radiation  Gasoline
therapy  Kerosene
 Paint thinners
DO NOT CONFUSE  Lighter fluid
 Give activated charcoal if emesis
 Antivert (antiemetic) with axert
contraindicated
(antimigraine)
 Lorazepam controls nausea and DIARRHEA
vomiting with alprazolam (anxiolytic )
 Hydroxyzine (antiemetic) with  Frequent liquid stool
hydralazine (antihypertensive )  Causes:
o Foods (spicy)
EMETICS o Fecal impaction
o Bacteria Escherichia coli,
 These are drugs used to induce
salmonella
vomiting when an individual has
o Viruses
consumed certain toxic substances
o Toxins
 Indicated to expels the substances or
o Drug reaction
drug before absorption
o Laxative abuse
IPECAC o Malabsorption syndrome
o Stress and anxiety
 2004 o Bowel tumor
 The American academy of clinical o Ulcer, colitis, crohn’s disease
toxicology  Intestinal fluid rich in water, sodium,
 European association of poisons centers potassium, bicarbonate
and clinical toxicologists
  Can cause minor or severe dehydration
and electrolytes imbalances
 Bicarbonate loss places the patient at
risk for developing metabolic acidosis
 Avoid milk and fatty foods
 Life threatening to young and adult
patient (do not compensate for the
fluid and electrolytes losses )
 Nonpharmacologic measures
 Clear fluids
 Oral solutions( Gatorade , pedialyte for
children)
TRAVELER’S DIARRHEA
 Also called acute diarrhea caused by e.
coli
 Lasts less than 2 days
 If becomes severe fluoroquinolone
antibiotic are usually prescribe
 Loperamide (Imodium )  to slow
peristalsis and decrease the frequency
of defacation
 Should be avoided: drink bottled water,
washing of fruits, eat cooked
vegetables, well cooked meat
ANTIDIARRHEALS
 Opiates and opiate related agents
 Somatostatin analogue
 Adsorbent
 Miscellaneous antidiarrheal
 Opiates and opiate related agents
 Decrease intestinal motility, decreasing
peristalsis
 Side effect : constipation – common
 Codeine is an example
 Combined with other antidiarrheals
 Can cause CNS depression when takne
with alcohol, sedatives and tranquilizer
 Duration of action is approximately 2
hours
 Opiates and opiate related agents
 LOMOTIL – diphenoxylate with atropine
– less potential of causing drug
dependence
 Motofen – difenoxin – an active
metabolite of diphenoxylate, more
potent than diphenoxylate
 Both lomotil and difenoxin are
combined with atropine to decrease
abdominal cramping intestinal motility
and hypersecretion
 ADSORBENTS
o Acts by coating the wall of the
GI tract and adsorbing bacteria
or toxins that cause diarrhea
o Kaolin pectin ( kaolin with
pectin )
o A : 60 – 120 ml after eachloose
stool
o C: 6 – 12 years old 30 – 60 ml
after each loose stool OTC drug,
pregnancy category C; PB : UK,
t1/2 : UK
o These agents are combined as a
mild or moderate antidiarrheals
that can be purchased OTC and
used in combination with other
antidiarrheals
o Bismuth subsalicylate (pepto-
bismol ) OTC treat diarrhea
o A: PO : 2 tab or 30 ml q 30 – 60
min. PRN max 8 doses/ day
o pregnancy category C; PB :UK, t
½ :UK
o liquid and tablet form
 miscellaneous
o rifaximin (xifaxan)
 o A: PO : 200 mg tid for 3 days for o PEG – polyethylene glycol –
treatment of traveler’s diarrhea with electrolytes, GoLYTELY (
e. coli market name ) 3-4 liters over 3
o Pregnancy category : C ; PB : hours must be ingested
67.5 % t ½ 5-6 hrs o Keep refrigerated to make ir
more palatable
LAXATIVE o An isotonic solution, non
 Constipation absorbable substances
o Accumulation of hard fecal o Contains sodium salt and
material in the large intestine potassium chloride
o Common complaint of older o Can be used by patient with
adults renal impairment and cardiac
disorder
 Contributing factor
o Insufficient water intake  Lactulose
o Poor dietary habits o Saline laxative that is not
absorbed
 Other causes
o Draws water into the intestine
o Fecal impaction
to form stool
o Bowel obstruction
o Decreases serum ammonia
o Chronic laxative use
level, liver disease such as
o Neurologic disorder
cirrhosis
(paraplegia)
o Glycerin acts like lactulose,
o Ignoring the urge to defecate
increasing water in the large
o Lack of exercise
intestine
o Drugs such as anticholinergic,
o The bulk stimulate peristalsis
narcotics and certain antacids
and defecation
 Osmotic saline
o Side effect and adverse effect :
o Salt and saline products,
o Hypermagnesemia magnesium
lactulose and glycerin
salts
o Serum electrolytes should be
o Drowsiness
monitored to avoid electrolytes
o Weakiness
imbalance
o Paralysis
o Salts pull water into the colon
o Hypotension
and increase water in the feces
o Respiratory depression
to increase bulk which
o Flatulence
stimulates peristalsis
o Diarrhea
o Indicated for patient with good
o Abdominal cramps
renal function
o Nausea and vomiting
o Contraindicated for patient
 Stimulant (contact or irritating )
with heart failure
laxative
o High doses of salt laxatives are
used for bowel preparation
 o Increase peristalsis by irritating o Promote large soft stool by
sensory nerve endings in the absorbing water into the
intestinal mucosa intestine
o Bisacodyl (dulcolax) – most o Increasing fecal bulk and
frequently used )barium peristalsis
enema ) o Non absorbable defacation
o Senna (senokot) occurs within 8to 24 hours may
o Castor oil ( purgative) take up to 3 days for the stool
 Castor oil to be soft and well formed
o A harsh laxative (purgative) o Should be mixed in a glass of
o Acts on the small bowel and water, juice, stirred drunk
produce watery stool immediately followed by a half
o Action 2-6 hours into full glass of water
o Should not be taken at bedtime o Insufficient fluid intake can
o Used for bowel preparation not cause the drug to solidity in the
for constipation GItract intestinal obstruction
o Pharmacodynamics o Used by patient with
o Bisacodyl irritates the colon, diverticulosis irritable bowel
causing defacation , psyllium syndrome and ileostomy and
increase fecal bulk and colostomy
peristalsis o Example:
o Onset : 6 to 8 hours  Polycarbophil (fiberCon
o Suppository :15 – 60 minutes ) – contraindicated to
o Pharmacokinetics patient with
o Absorbed from the GI tract hypercalcemia
minimally, excreted in the  Polyethylene glycol
feces (miralax)
o Excretes In the urine  Methylcellulose
o Lactulose (Citrucel)
o Excessive use:  Psyllium (Metamucil)
o Fluid and electrolyte imbalance o Pharmacokinetics :
(potassium and calcium )  Metamucil is a non
o Castor oil should not be used in digestible and non
early pregnancy. It stimulates absorbent, when
uterine contraction mixed with water
o Spontaneous abortion may become viscous
result solution
o Senna can damage the nerves  There is no protein
whenprolong in use – loss of binding or half life
intestinal mucosa tone because it is not
 Bulk forming laxative absorbed
 Excretes in the feces
 o Pharmacodynamics o Encourage patient to increase
 Onset of action foe water intake (if not
Metamucil: 12 to 72 contraindicated)
hours o Advise patient to avoid overuse
 Peak of action : 1-3 of laxatives. Which can lead to
days fluid and electrolyte
 Duration of action :UK imbalances and drug
 Chloride channel activators dependence
o Used to treat idiopathic o Exercise helps to increase
constipation in adults peristalsis
o Lubiprostone – this drug o Do not chew tablet but
activates chloride channels in swallow them whole
the lining of the intestine o Teach patient to store
leading to an suppositories at less 86F (30%)
o Relieves constipation as well as o Take drug with water to
accompanying symptoms of increase absorption
abdominal discomfort o Do not take drug within 1 HR of
o Contraindicated to a patient any other drug
with a history of mechanical GI o Long term use may loose
obstruction. Crohn’s disease, bowel tone
diverticulitis severe diarrhea o
o A/E : nausea, diarrhea,
headache, abdominal
distention, and flatulence
 Emollient (stool softeners )
o Lubricant and stool softeners
(surface acting or wetting
drugs). Used to prevent
constipation
o Mineral oil (lubricant) increase
water retention in the stool
o Example:
 Docusate calcium
(surfak)
 Docusate sodium
(coface)
 Docusate sodium with
senna (peri-coface)
 Patient teaching