DRUGS FOR UPPER RESPIRATORY  Rapidly absorbed in 15mins.

but not
DISORDERS potent to combat anaphylaxis
Upper Respiratory Disorders (URIs)
DRUGS ACTING ON UPPER RESPIRATORY
Includes : TRACT
 Common cold  Intranasal Glucocorticoids
 Acute Rhinitis
 Allergic Rhinitis 6 INTRANSAL GLUCOCPRTICOIDS
 Sinusitis 3. Antitussives
 Acute Pharyngitis o Action : suppress the cough reflex by acting
on the medullas cough center
COMMON COLD
o Treatment for nonproductive cough
TRANSMISSION OCCURS :
 COUGH – naturally protective way to
1. Touching contaminated surfaces
clear airway of secretions or any
2. Touching nose/mouth
collected material
3. Viral droplets released by sneezing
 SORE THROAT – cause coughing that
HOME REMEDIES INCLUDES :
increase throat irritation.
 Rest
4. Expectorants
 Chicken noodle soup
 Hot toddy ( tea, sugar, alchohol) o Decrease bronchial secretions so they can
 Vitamin C be elimianated by coughing
 Megadose of vitamins o Used with or without pharmacologic agents
ACUTE RHINITIS o Found in many OTC cold remedies along
 Acute inflammation of mucous with :
membrane of nose - analgesics, antihistamines,
 NOT SAME as Allergic rhinitis decongestants, antitussives
ACUTE PHARYNGITIS o Treat : cough associated with common cold,
bronchial asthma
 Inflammation of sore throat
 HYDRATION – best natural expectorant
 Caused by virus, beta hemolytic
streptococci (strep throat)
 Can occur alone or with common cold,
rhinitis or acute sinusitis
 Symptoms : elevated temperature and
cough
 Not useful in emergency situation, such
as anaphylaxis

DRUG FOR LOWER RESPIRATORY
DISORDERS
2 MAJOR CATEGORIES OF LOWER
RESPIRATORY TRACT DISORDER:
 Chronic Obstructive Pulmonary
Disease(COPD)
 Restrictive Pulmonary Disease
COPD- is caused by airway obstruction with
increased airway resistance of air flow to lung
tissues.
4 MAJOR PULMONARY DISORDERS CAUSE
COPD:
 Chronic Bronchitis
 Bronchiectasis
 Emphysema
 Asthma
Restrictive lung disease- is a decrease in total lung
capacity as a result of fluid accumulation or loss of
elasticity of the lung.
TYPES AND CAUSES OF RESTRICTIVE
PULMONARY DISEASE:
 Pulmonary edema
 Pulmonary fibrosis
 Pneumonitis
 Lung tumors
 Thoracic deformities (scoliosis)
 Disorder affecting the thoracic wall
(myasthenia gravis)
CHRONIC OBSTRUCTIVE PULMONARY
DISEASE
 Asthma is an inflammatory disorder of the
airway walls associated with a varying
amount of airway obstruction.
 -This disorder is triggered by stimuli such as
stress, allergens, and pollutants.
 -The obstruction of air passages contributes
to wheezing, coughing, dyspnea
(breathlessness), and tightness in the chest,
particularly at night or in early morning.
Bronchial Asthma- characterized by bronchospasm
(constricted bronchioles), wheezing, mucus
secretions and dyspnea.
 There is resistance to air flow caused by
obstruction of the airway.
 In acute and chronic asthma, minimal to no
changes are seen in the structure and
function of lung tissues when the disease
process is in remission.
 In chronic bronchitis, emphysema, &
bronchiectasis, there is permanent,
irreversible damage to the physical structure
of lung tissue.
Chronic bronchitis is a progressive lung disease
caused by smoking or chronic lung infections.
 Productive coughing is a response to excess
mucus production and chronic bronchial
irritation.
Hypercapnia (increased carbon dioxide retention)
Hypoxemia (decreased blood oxygen)
Bronchiectasis-the bronchioles become obstructed
by the breakdown of the epithelium of the bronchial
mucosa.
Emphysema- is a progressive lung disease caused
by cigarette smoking, atmosphere contaminants, or
lack of the alpha-antitrypsin protein that inhibits
proteolytic enzymes that destroy alveoli (air sacs).
Proteolytic enzymes are released in the lung by
bacteria or phagocytic cells.
Alveoli enlarged as many of the alveolar walls are
destroyed. Air becomes trapped in the over
expanded alveoli, leading to inadequate gas (oxygen
and carbon dioxide) exchange
Cigarette smoking is the most common risk factor
for COPD, especially with chronic bronchitis and
emphysema.
There is no cure for COPD at this time, however, it
remains preventable in most cases. Quit smoking
will slow the disease process.
Medications frequently prescribed for COPD
include the following:
 Bronchodilators such as symphatomimetics
(andrenergics, parasymphatholytic
(anticholinergic drug, atrovent), and
methylxanthines (caffeine, theophylline) are
used to assist in opening narrowed airways.
 Glucocorticoids (asteroids) are used to
decrease inflaammation.
 Leukotriene modifiers reduce inflammation
in the lung tissue, and cromolyn and
nedocromil act as anti inflammatory agents
by suppressing the release of histamine and
other mediators from mast cells.
 Expectorants are used to assist in loosening
mucus from the airway.
 Antibiotics may be prescribed to prevent
serious complications from bacteria
infections.
Bronchial asthma is a COPD characterized by
periods of bronchospasm resulting in wheezing and
difficulty in breathing.
Bronchospasm, or bronchoconstriction results when
the lung tissue is exposed to extrinsic or intrinsic
factors that stimulate bronchoconstrictive response.
Factors that can trigger an asthmatic attack
(bronchospasm):
 Humidity, air pressure changes, temperature
changes,smoke,fumes (exhaust, perfumes)
 Stress, emotional upset, exercise, allergy to
animal dander, dust mites,food and drugs
(e.g. aspirin, ibuprofen, beta-adrenergic
blockers).
Reactive airway disease(RAD) is a cause of
asthma resulting from sensitivity stimulation from
allergens, dust, temperature changes and cigarette
smoking.
Pathophysiology
Mast cells, found in connective tissue throughout
the body, are directly involved in the asthmatic
response, particularly to extrinsic factors.
Allergens attach themselves to mast cells and
basophils, resulting in an antigen-antibody reaction
on release of chemical mediators
(histamines,cytokines,serotonin,eosonophil
chemotatic factor anaphylaxis and leukotrienes).
These chemical mediators stimulate bronchial
constriction, musous secretions, inflammation and
pilmonary congestion.
Exposure to allergen results in bronchial
hyperresponsiveness, epithelial shedding of the
bronchial wall, mucous gland hyperlasia and
hypersecretion, leakage of plasma leading to
swelling and bronchoconstriction.
FACTORS CONTRIBUTING TO
BRONCHOCONSTRICTION
SYMPATHOMIMETICS: ALPHA- AND BETA2-
ADRENERGIC AGONISTS
Sympatomimetics increase Camp, causing dilation
of the bronchioles. The nonselective
sympathomimetic epinephrine (adrenalin), which is
an alpha, Beta, and beta, agonist is given
subcutaneously to promote bronchodilation and
elevate blood pressure.
For bronchospasm associated with chronic asthma
or COPD, selective beta2-adrenergic agonists are
given by acrosol or as a tablet. These drugs act
primarily on the beta2 receptor; therefore, side
effects are less severe than those epinephrine, which
acts on alpha, Beta1, And beta2, receptors.
Albuterol (Proventil,Ventolin)- is a selective beta2
drug that is effective for treatment and control of
asthma by causing bronchodilation with long
duration of action.
High doses or overuse of the beta2-adrenergic
agents for asthma may cause some degree of beta1
response such as nervousness, tremor and increased
pulse rate.
DO NOT CONFUSE…. drug is administred by inhalation only with
the HandiHaler device (dry-powder capsule
 Albuterol (beta2-adrenergic) with Accupril
inhaler).
(cardiovascular agent)
 Ipratropium bromide (atrovent) is used to
Metaproterenol- it has some beta1 effect but is
treat asthmatic conditions by dilating the
primary used as a beta2 agent. It can be
bronchioles. Unlike other anticholinergics,
administered orally or by inhalation with a metered-
ipratropium bromide has few systemic
dose inhaler or a nebulizer.
effects. It is administred by aerosol.
For long-term asthma treatment, beta2-
 The combination of Ipratropium bromide
adrenergic agonist are frequently administered
with albuterol sulfate (combivent) is used to
by inhalation. The effective inhalation drug dose
treat chronic bronchitis. The combination
is less than it would be by an oral route, and
has more effective and has a longer duration
there are also fewer side effects using this route.
of action than if either agent is used alone.
DO NOT CONFUSE…..
METHYLXANTHINE (XANTHINE)
 Isuprel (beta-adrenergic) and Isordil (nitrate
DERIVATIVES
vasodilation)
 The second major group of bronchodilators
USE OF AN AEROSOL INHALER
used to treat asthma is the methylxanthine
 If the patient does not use the inhaler (xanthine) derivatives, which include
properly to deliver the drug dose, the aminophylline, theophylline, and caffeine.
medication may be trapped in the upper
 Xanthines also stimulate the central nervous
airways, because of drug inhalation, mouth
system (CNS) and respiration, dilate
dryness and throat irritation could result. A
coronary and pulmonary vessels, and cause
spacer device may be attached to the inhaler
diuresis. Because of their effect on
to improve drug delivery to the lung with
respiration and pulmonary vessels, xanthines
less deposition in the mouth.
are used in the treatment of asthma.
SIDE EFFECTS AND ADVERSE REACTIONS
THEOPHYLLINE
 The side effects and adverse reaction of
 Was produced in 1936
epinephrine include tremors, dizziness,
hypertension, tachycardia, heart palpitations,  Theophylline relaxes the smooth muscles of
cardiac dysrhythmias and angina. Pt needs to bronchi, bronchioles, and pulmonary blood
monitor when epinephrine was administered. vessels by inhibiting the enzyme
phosphodiesterase, resulting in increase in
 The side effects associated with beta2-
cAMP, which promotes bronchodilation.
adrenergic drugs(e.g. albuterol) include
tremors, headaches, nervousness, increased  Theophylline has a low therapeutic index
pulse rate and palpitations (high doses). The and a narrow therapeutic range (10 to
beta2 agonists may increased blood glucose 20mcg/mL).
levels, so pt with diabetes should be taught
 The serum or plasma theophylline
to closely their serum glucose levels.
concentration level should be monitored
Anticholinergics frequently to avoid severe adverse effects.
 Tiotropium (spiriva) is an anticholenergic Toxicity is likely to occur when the serum
drug used for maintenance treatment of level is greater than 20 mcg/mL.
bronchospasms associated with COPD. This
  Theophylline was once used as the first-line
drug for treating patients with chronic
asthma and others COPDs.
 Theophylline use has declined sharply,
because there is potential danger of serious
adverse effects. (e.g., dysrhythmias,
conclusions, cardiorespiratory collapse).
 Because of its numerous adverse reactions,
drug-drug interactions, and narrow
therapeutic drug range, it is prescribed
mostly for maintenance therapy in patients
with chronic stable asthma and other
COPDs.
 Patients who receive theophylline
3 LEUKOTRIENE MODIFIERS:
preparations need to be closely monitored
for serious side effects and drug interactions.
PHARMACOKINETICS
 Theophylline is usually well absorbed after
oral administration, oral liquids and
uncoated plain tablets.
 Theophylline can also administered in IV
fluids.
ROUTE AND DOSAGE
 Theophylline are metabolized by liver
enzymes, and 90% of drug is excreted by the
kidneys.
 Tobacco smoking increases metabolism of
theophylline drugs, thereby decreasing its
half-life.
 The half-life is also shorter in children, with
a short half-life, theophylline is readily
excreted by the kidneys.
PHARMACODYNAMICS
 Increase the level of cAMP, for oral
preparation 1-2hours for the sustained-
release form and approximately 6 hours for
the oral and IV theophylline preparations.
LEUKOTRIENE RECEPTOR ANTAGONISTS
AND SYNTHESIS INHIBITORS
 Leukotriene (LT) is a chemical mediator that
can cause inflammatory changes in the lung.
 Cysteinyl leukotriene promote an increase in
eosinophil migration, mucus production, and
airway wall edema, which result in
bronchocontion striction.
 LT receptor antagonists and LT synsthesis
inhibitors, called leukotriene modifiers, are
effective in reducing the inflammatory
symptoms of asthma triggered by allergic
and environmental stimuli.
 These drug groups are not recommended for
treatment of acute asthmatic attack. They are
used for exercise-induced asthma.
 Do not administer for acute asthmatic attack
1. ZAFIRLUKAST (ACCOLATE)
2. ZILEUTON (ZYFLO CR)
3. MONTELUKAST SODIUM
(SINGULAIR)
4. LEUKOTRIENE RECEPTOR
ANTAGONISTS
A: PO:20 mg b.i.d 1 before or 3h after meals,
max 40mg/d
C: >5 y:PO: 10mg b.i.d: max : 20mg/d
USES AND CONSIDERATIONS
For prophylaxis and maintenance therapy for
chronic asthma, reduces inflammation within
bronchial tubes and airways. Pregnancy
category: B: PB: 99% t1/2 : 10h
LEUKOTRIENE SYNTHESIS
ANTAGONISTS
ROUTE AND DOSAGE
ER:
A:PO: 1200mg b.i.d within 1h after morning
and evening meal
USES AND CONSIDERATIONS
 For prophylaxis and maintenance therapy for - disturbances of the middle ear that affect
chronic asthma. Reduces inflammation in equilibrium
airways and - nausea, a queasy sensation, may or may
decreases bronchoconstriction. Hepatotoxicity not precede the expulsion
may result; closely monitor liver enzymes. • Antiemetics can mask the underlying
Pregnancy category: C;PB 93%: t1/2 : 2.5h cause of vomiting and shouldn’t be
used until the cause has been
LEUKOTRIENE RECEPTOR
determined, unless the vomiting is so
ANTAGONISTS
severe as to cause dehydration and
ROUTE AND DOSAGE
electrolyte imbalance.
A: PO : 500 mcg/d •
USES AND CONSIDERATIONS TWO MAJOR CEREBRAL CENTERS:
• Chemoreceptor trigger zone (CTZ) –
For treatment of exacerbations in severe COPD,
which lies near the medulla
common adverse effects include diarrhea and
• Vomiting center – in the medulla,
weight loss. Contraindicated in moderate to cause when vomiting determined the
CTZ receives most of the impulses
severe liver impairment.
from drugs, toxins, and the vestibular
Pregnancy category: C, PB: 99%: t1/2 17h
center in the ear and transmits them to
DRUGS FOR GASTROINTESTINAL TRACT the vomiting center. The
DISORDERS neurotransmitter dopamine stimulates
the CTZ, which in turn stimulates the
GI TRACT DISORDERS:
vomiting center.
• Vomiting
• Levodopa, a drug with dopamine-like
• Emetics
properties, can cause vomiting by
• Diarrhea
stimulating the CTZ.
• Constipation
• The neurotransmitter acetylcholine is
VOMITING
also vomiting stimulant.
• Also called Emesis, the expulsion of
THE TWO MAJOR GROUPS OF
Gastric contents.
ANTIEMETICS ARE:
• Causes:
• Nonprescription
- sickness - Pregnancy
- Antihistamines
- viral and bacterial infection - Pain shock
- bismuth subsalicylate
- food tolerance - effect of selected drugs
- Phosphorated carbohydrate
- surgery
solution
• Prescription
- antihistamines
- dopamine antagonists
- benzodiazepines
- serotonin antagonists
- glucocorticoids
- cannabinioids
- miscellaneous antiemetics
Nonpharmacologic Measures
• Methods of decreasing nausea and
vomiting include administration of
weak tea, flat soda, gelatin, Gatorade
and Pedialyte ( for use in children ).
• When dehydration becomes severe IV
fluid are needed to restore body fluid
balance.
Nonprescription Antiemetics
• anti-vomiting agents can be used 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 mins
before travel.
Antihistamine Antiemetics
• Such as dimenhydrinate (Dramamine),
cyclizine hydrocholoride (Marezine),
meclizine hydrochloride (Antivert), and
diphenhydramine hydrochloride
(bendryl) can be purchased OTC to
prevent nausea, vomiting, and dizziness
caused by motion.
SIDE EFFECTS OF
ANTIHISTAMINES ARE:
 drowsiness, dryness of the mouth, and
constipation.
Bendaryl
• Also used to prevent or alleviate
allergic reactions to drugs, insects, and
food by acting as an antagonist to
histamine1 receptors.
Bismuth subsalicylate (Pepto-Bismol)
• Act directly on the gastric mucosa to
suppress vomiting. They are marketed
in liquid chewable tablet forms and can
be taken for gastric discomfort or
diarrhea.
Phosphorated carbohydrate solution (Emetrol)
• A hyperosmolar carbohydrate, decrease
nausea and vomiting by changing the
gastric pH; it may also decrease smooth
muscle contraction of the stomach.
Prescription Antiemetics
• Common Prescription antiemetics are
classified into the following groups:
1. Antihistamines
2. Anticholinergics
3. Dopamine antagonists
4. Benzodiazepines
5. Serotonin antagonist
6. Glucocorticoids
7. Cannabinoids (for patients w/ cancer)
8. Miscellanous
Antihistamines and Anticholinergics
• Used in the treatment of nausea and
vomiting.
• Side effect and Adverse Reactions: can be a
major problem, dry mouth, drowsiness,
blurred vision caused by pupillary dilation,
tachycardia (w/anticholinergics use), and
constipation. These drugs should not be used
by patient with glaucoma.
Dopamine Antagonists
• These agents suppress emesis by blocking
dopamine2 receptors in the CTZ.
• The categories of dopamine antagonists:
- phenothiazines
- butyrophenones
- benzodiazenapines
• Common Side effects:
- extrapyramidal symptoms (EPS)
Phenothiazine Antiemetics
• Piperazine phenothiazines are used to treat
nausea and vomiting resulting from surgery,
anesthetics, chemotherapy and radiation
sickness. They act by inhibiting the CTZ.
• Chlorpromazine (Throzine) and
Prochlorperazine edisylate (Companize)
were the first phenothiazines used for both
psychosis and vomiting.
• Promethazine (Phenergan) is the most
frequently prescribed antiemetic drug, has a
sedative effect and can also be used for
motion sickness and management of nausea
and vomiting.
• Side effects and Adverse reaction: moderate
sedation, hypotension, EPS, CNS effects
(restlessness, weakness, dystonic reactions,
agitation), mild anticholinergic ( dry mouth,
urinary retention, and constipation).
Butyrophenones
• Haloperidol (Haldol) and droperidol
(Inapsine) , like phenothiazines block the
dopamine2 receptors in the CTZ.
• They are used to treat postoperative nausea
and vomiting and emesis associated with
toxins, cancer chemotherapy , radiation
therapy.
• Hypotension may result ; therefore blood
pressure should be monitored.
Benzodiazepines
• Indirectly control nausea and vomiting that
may occur with cancer chemotherapy.
• Lorazepam (Ativan) is a drug of choice.
Effectively provides emesis control,
sedation, anxiety reduction, and amnesia
when used in combination with a
glucocorticoid and serotonin 5-HT₃ receptor
antagonist.
Serotonin (5-HT₃) Receptor Antagonists
• Suppress nausea and vomiting by blocking
the serotonin receptors (5-HT₃) in the CTZ
and the afferent vagal nerve terminals in the
upper GI Tract.
• Ondansetron (Zofran), granisetron (Kytril),
dolasetron (Anzemet), and palonosetron
(Aloxi) are the most effective of all
antiemetics in suppreing nausea nad
comiting caused by cancer chemotherapy
induced emesis or emetogenic anticancer
drugs. Ondansetron, granisetron and
dolasetron do not blovk the dopamine
 receptors. These drug can be administered
orally and IV.
• Common Side effect: headache, diarrhea,
dizziness and fatigue
Glucocorticoids (Corticosteroids)
• Dexamethasone (decadron) and
methylprednisolone (Solumedrol) are two
agents that are effective in suppressing
emesis associated with cancer
chemotherapy. Because these
glucocorticoids are administered IV and for
only a short while, side effects normally
associated with glucocorticoids are
minimized.
Cannabinoids
• The active ingredients in marijuana,
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.
• Can be used as an appetite stimulant for
patients with AIDS.
• Side effects and Adverse reactions: mood
changes, euphoria, drowsiness, dizziness,
headaches, depersonalization, nightmares,
confusion, incoordination, memory lapse,
dry mouth, orthostatic hypotension or
hypertension, and tachycardia. Less
common symptoms are depression, anxiety,
and manic psychosis.
Miscellaneous Antiemetics
• Class:
- Diphenidol (Vontrol) – prevents vertigo
by inhibiting impulses to the vestibular
area
-Trimethobenzamide (Tigan)
• These drugs suppress impulses to the CTZ.
Also they do not act strictly as
antihistamines, anticholinergics or
phenothiazines
• Side effects and Adverse reactions:
drowsiness and anticholinergic symptoms.
Trimethobenzamide can cause hypotension,
diarrhea and EPS.
EMETICS
• Are drugs used to induce vomiting
• When an individual has consumed certain
toxic substances, induced vomiting (emesis)
may be indicated to expel the substances
before absorption occurs.
Ipecac
• Administration of ipecac has diminished
greatly but it is still used when indicated.
• Ipecac is considered appropriate in isolated
cases for the patient who is alert and if
administered within in 60mins of poisoning.
DIARRHEA
• (frequent liquid stool), is a symptoms of an
intestinal disorder.
• Causes include;
1. foods (spicy, spoiled)
2. Fecal impaction
3. Bacteria (E.coli, salmonella or Virus
(Parvovirus, rotavirus)
4. Toxins
5. Drug reaction
 6. Laxative abuse
7. Malabsorption syndrome caused by lack of
digestive enzyme
8. Stress and anxiety
9. Bowel tumor
10. Inflammatory bowel disease
• Diarrhea can be mild to severe.
• NOTED: Antidiarrheals should not be used
for more than 2 days and should not be used
if fever is present.
Nonpharmacologic Measures
• Treatment for diarrhea is recommended until
the under lying cause can be determined.
This include use of clear liquids and oral
solutions and IV electrolyte solution.
Traveler’s Diarrhea
• Also called acute diarrhea, is usually caused
by E.coli. It lasts less than 2 days; however,
if it becomes severe, fluoroquinolone
antibiotics are usually prescribed.
• Loperamide (Imodium) may be used to slow
peristalsis and decrease the frequency of
defecation, it can also slow the exit of the
organism from the GI tract.
• Traveler’s diarrhea can be reduced by
drinking bottled water, washing fruit, and
eating cooked vegetables. Meats should be
cooked until well done.
Antidiarrheals
• For treating diarrhea and decreasing
hypermotility (increased peristalsis)
• Antidiarrheals are classified as:
1. Opiates and opiate-related agents
2. Somatostatin analogue
3. Adsorbents
4. Miscellaneous antidiarrheals
Opiates and Opiate-Related Agents
• opiates decrease intestinal motility, thereby
describing peristalsis. Constipation is a
common side effect of opium preparations.
Codeine is an example.
• Opiates are frequently combined with other
antidiarrheal agents.
• Opium antidiarrhealas can cause CNS
depression when taken w/ alcohol, sedatives
or tranquilizers. Duration of action is
2hours.
• Diphenoxylate with atropine (Lomotil) is an
opiate that has less potential for causing
drug dependence than other opiates such as
codaine.
• Difenoxin (Motofen) is an active metabolite
of diphenoxylate, but is more potent than
diphenoxylate.
• Both drugs are combined with atropine to
decrease abdominal cramping, intestinal
motility, and hypersecretion.
• Loperamide (Imodium) is structurally
related to diphenoxylate but causes less CNS
depression than dipenoxylate and difenoxin.
Is an OTC drug and it protect agains
diarrhea, reduces fecal volume & decrease
intestinal fluid and electrolyte losses.
Adsorbents
• Act by coating the wall of the GI tract and
adsorbing bacteria or toxins that cause
diarrhea.
• Adsorbent antidiarrheals include Kaolin and
pectin. These agents are combined as a mild
 or moderate antidiarrheal that can be
purchased OTC and used in combination w/
other antidiarrheals.
• Bismuth subsalicylate (Pepto-bismol) is
considered an adsorbents because its adsorbs
bacterial toxins. Can also be used as an
antacid for gastric discomfort. Is an OTC
drug used to treat traveler’s diarrhea.
• Colestipol and cholestyramine (questran) are
prescription drugs that have been used to
treat diarrhea due to excess bile acids in the
colon.
Miscellaneous Antidiarrheals
• are prescribed to control diarrhea. This
groups includes rifaximin.
CONSTIPATION
• 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.
• Causes include;
1. Fecal impaction
2. Bowel obstruction
3. Chronic laxative use
4. Neurologic disorders (paraplegia)
5. Ignoring the urge to defecate
6. Lack of exercise
7. Selected drugs, such as anticholinergics,
narcotics, certain antacids
Nonpharmacologic Measures
• Includes diet (high fiber), water, exercise
and routine bowel habits
• a “normal” number of bowl movement
ranges 1 and 3 per day to 3per week.
Laxatives
• laxatives and cathartics are used to
eliminate fecal matter.
• purgatives are “harsh” cathartics that cause
a watery stool with abdominal cramping.
• There 4 types of laxatives
- osmotics (Saline)
- stimulants (contact or irritants)
- bulk-forming
- emollients (stool softeners)
Osmotic (Saline) Laxatives
• osmotics (hypersmolar laxatives) include
salt or saline products, lactulose and
glycerin.
• Hyperosmolar salts pull water into the colon
and increase water in the feces to increases
bulk, which stimulates peristalsis.
• Saline cathartics cause a semi-formed to
watery stool according to low or high doses.
• Osmotics laxatives contain electrolyte salts,
including;
1. Sodium salts ( sodium phosphate or
Phosphoda-Soda, sodium biphophate)
2. Magnesium salts ( magnesium hydroxide
[milk of magnesia], magnesium citrate).
• Another laxative used for bowel preparation
is polyethylene glycol (PEG), with
electrolytes, marketed as GoLYTELY.
• Lactulose, another saline laxativs that is not
absorbed, draws water into intestines to form
a soft stool. It decreases the serum ammonia
 level and is useful in liver diseases, such as
cirrhosis.
• Glycerin acts like lactulose, increasing
water in the feces in the large intestines. The
bulk that results from the increased water in
the feces stimulates peristalsis and
defecation
Stimulant (Contact) Laxatives
• increase peristalsis by irritating sensory
nerve endings in the intestinal mucosa.
• Types include those containing;
- Bisacodyl (Dulcolax)
- Senna (Senokot)
- castor oil (purgative)
• Bisacodyl and several others of the drugs
are used to empty the bowel before
diagnostic test (barium senna)
• Castor oil is a harsh laxative (purgative) that
acts on the small bowel and produces a
watery stool. Action is within 2 to 6 hrs. is
also used to correct constipation
Bulk-Forming Laxatives
• Are natural fibrous substances that promote
large, soft stool by absorbing water into the
intestine, increasing fecal bulk and
peristalsis. These agents are non-absorbable.
• Defecation usually occurs within 8 to 24
hours
• This group of laxatives does not cause
laxative dependence and may be used by
patients with diverticulosis, irritable bowel
syndrome, and ileostomy and colostomy.
• Examples of bulk-forming laxatives;
- Polycarbophil (Fibercon)
- Polyethylene glycol (Mira Lax)
- Methylcellulose (Citrucel)
- Psyllium (Netamucil)
• Patients with hypercalcemia should avoid
calcium polycarbophil because of the
significant amount of calcium in the drug.
Chloride Channel Activators
• Are a new category of laxatives used to
threat idiopathic constipation in adults.
Lubiprostone
• the first drug in category. This drug activates
chloride channels in the lining of the small
intestines, leading to an increase in intestinal
fluid secretion and motility.
• By enhancing the passage of stool, relieves
constipation, as well as accompanying
symptoms of abdominal discomfort, pain,
and bloating.
• Contraindicated for patients with history of
mechanical GI obstruction, Crohn’s disease,
diverticulitis, severe diarrhea.
• Side effects: nausea, diarrhea, headache,
abdominal distention, faltulence,.
Emollients (Stool Softeners)
• are lubricant and stool softeners (surface-
acting or wetting drugs) used to prevent
constipation. These drugs decrease straining
during defecation.
• Lubricant such as mineral oil increase water
retention in the stool.
• Mineral oil absorbs essential fat-soluble
vitamin A,D,E,K.
• stool softeners work by lowering surface
tension and promoting water accumulation
in the intestine and stool.
 • Examples of Stool Softener;
- Docusate calcium (Surfak)
- Docusate sodium (Colace)
- Docusate sodium with senna (Per-
Colace)
• Side effects: Mineral oil include nausea,
vomiting, diarrhea and abdominal cramping.
The docusate groups drugs may cause mild
cramping
• Contraindications: inflammatory disorders
of the GI tract, pregnancy, spastic colon, or
bowel obstruction. Laxatives are
contraindicated when any of these
conditions is suspected.
• Antiulcer Drugs
By: GROUP 4
Peptic Ulcer is a broad term for an ulcer occurring
in the esophagus, stomach, or duodenum within the
upper Gastrointestinal (GI) tract.
Ulcers are more specifically named according to
site of involvement : esophageal , gastric and
duodenal ulcers. Duodenal ulcers occur 10 times
more frequently than gastric and esophageal ulcers.
The release of Hydrochloric acid (HCI) from the
parietal cells of the stomach is influenced by
histamine, gastrin and acetylcholine. Peptic ulcers
occur when there is hypersecretion of hydrochloric
acid and pepsin, which erode the GI mucosal lining.
The gastric secretions in the stomach strive to
maintain a pH of 2 to 5. PEPSIN a digestive
enzyme, is activated at a pH of 2, and the acid-
pepsin complex of gastric secretions can cause
mucosal damage . If the pH of gastric secretions
increases to pH 5, the activity of pepsin declines.
The Gastric Mucosal Barrier (GMB) is a thick,
viscous, mucous material provides a barrier between
the mucosal lining and acidic gastric sessions. The
GMB maintains the integrity of mucosal lining
defense against corrosive substances.
An Esophageal ulcer results from reflux of acidic
secretions into the esophagus as a result of a
defective or incompetent cardiac sphincter.
Gastric Ulcer frequently occurs because of a
breakdown of the GMB.
Duodenal Ulcer is caused by hypersecretion of
acid from the stomach passing into the duodenum
because (1) insufficient buffers to neutralize
gastric acid in the stomach , (2) a defective or
incompetent pyloric sphincter, or (3) hypermobility
of the stomach.
Gastroesophageal reflux disease(GERD) is an
inflammation or erosion of esophageal mucosa
caused by a reflux of gastric acid content from the
stomach into the esophagus.
PREDISPOSING FACTORS IN PEPTIC
ULCER DISEASE
 The nurse needs to assist the patient in
identifying possible causes of the ulcer and
to teach ways to alleviate them. Predisposing
factors include mechanical disturbances,
genetic influences, bacterial organisms ,
environmental factors, and certain drugs.
Healing of an ulcer takes 4 to 8 weeks.
 The classic symptom of peptic ulcers is
gnawing, aching, pain. With a gastric ulcer,
pain occurs 30 minutes to 1.5 hours after
eating, and with a duodenal ulcer, 2 to 3 hrs
after eating. Small, frequent meals of
nonirritating foods decreases the pain. With
treatment, pain usually subsides in 10 days;
however, the healing process may take 1 to 2
mos.
 A stress ulcer usually follows a critical
situation such as extensive trauma or major
surgery ( e.g. burns, cardiac surgery).
Prohylactic use of antiulcer drugs decreases
the incidence of stress ulcers.
HELICOBACTER PYLORI
 Helicobacter pylori, a gram-negative
bacillus , is linked with the development of
peptic ulcer and is known to cause gastritis,
gastric ulcer, and duodenal ulcer. When a
peptic ulcer recurs after antiulcer therapy,
 and the ulcer is not caused by nonsteroidal
antiinflamatory drugs (NSAIDs) such as
aspirin or ibuprofen, the patient should be
tested for the presence of the bacterium
H.pylori , which may have infected gastric
mucosa.
 There are various protocols for treating
H.pylori infection, but antibacterial agents
are the treatment of choice.
 The drug regimen eradicates more than 90%
peptic ulcer caused by H.pylori.
 Treatment to eradicate this bacterial
infection includes using a dual-,triple-, or
quadruple drug therapy program in a variety
of drug combinations such as
MEDICAL TREATMENT FOR GERD
 Also called as “reflux esophagitis” an
inflammation of the esophageal mucosa.
 caused by relflux of gastric acid content into
the esophagus.
 Its main cause is in incompetent lower
esophageal sphincter.
 Smoking tends to accelerate the disease
process.
NONPHARMACOLOGIC MEASURES FOR
MANAGING PEPTIC ULCER AND GERD
 Effective management of GERD keeps the
esophageal mucosa healed patient free from
symptoms, but GERD is a chronic disorder
that requires continues care.
ANTIULCER DRUGS
THERE ARE SEVEN GROUPS OF
ANTIULCER DRUGS:
 Tranquilizers
 Anticholinergics
 Antacids
 H2 blockers with block receptor
 PPIs
 The Pepsin inhibitor sucralfate
 The Prostaglandin E
TRANQUILIZERS
Have a minimal effect in preventing and treating
ulcers.
Reduce vagal stimulation and decrease anxiety.
Generic version of Librax, a reformulated product
of anxiolytic chlordiazepoxide(LIBRIUM)
ADVERSE EFFECTS
 Edema
 Ataxia
 Confusion
 Extrapyramidal Syndrome (EPS)
 Agranulocytosis
ANTICHOLINERGICS
 These drugs relieve pain by decreasing GI
motility and secretion.
 They act by inhibiting acetylcholine and
blocking histamine and hydrochloric acid.
 Anticholigernics delay gastric emptying
time, so they are used more frequently in
duodenal ulcer than gastric ulcer.
 Anatacids can slow the absortion of
antichloinergics.
 Anticholinergics must be taken before
meals to decrease the acid secretion that
occurs with eating.
SIDE EFFECTS AND ADVERSE EFFECTS
 Dry mouth, decreased secretions, headache,
blurred vision, drowsiness, dizziness,
lethargy, palpation, bradycardia,
tachycardia, urinary retention, and
constipation.
ANTACIDS
SYSTEMIC EFFCECT
Sodium bicarbonate
 A systemically absorbed antacids.
 Was the first antiulcer drugs. Because it has
many side effects (sodium excess, causing
hypernatremia and water retention;
metabolic alkalosis caused by excess
bicarbonate; and acid rebound)
 Is seldom used in peptic ulcer
  Example of an sodium bicarbonate
compound is Alka-Seltzer.
NONSYTEMIC EFFECT
 Are composed of alkaline salts such as
aluminum (aluminum hydroxide) and
magnesium (magnesium hydroxide,
magnesium trislicate). There are small
degree of systemic absorption with these
drugs mainly the aluminum. Magnesium
hydroxide has greater neutralizing power
than aluminum hydroxide.
 Magnesium compounds can cause diarrhea.
 Aluminum and calcium can cause
constipation.
 A combination of magnesium and aluminum
salts neutrilizes gastric acid without any
caused of severe diarrhea or constipation.
 Simenthicone ( an antigas agent) is found in
many antacids, including Mylanta Gas,
Maalox Antigas, an Mylicon.
 The ideal dosing for antacids should be 1
and 3 hours after meals (maximum acid
secretion occurs after eating) and at bedtime.
antacid should only taken when the stomach
is empty and its effective for 30 to 60
minutes before passing into duodenum.
 Drink both chewable and liquid antacids
with water.
 Antacids containing magnesium salts are
contraindicated in patients with impaired
renal function because of the risk for
hypomagnesemia.
 Prolonged use of aluminum hydroxides can
cause hypophospatemia (low serum
phospate),osteoporosis,nephrolithiasis,and
osteomalacia.
HISTAMINE2 BLOCKERS
 Patients who are taking H2 blockers like
Cimetidine can take antacids to avoid acid
reflux, but they should not take them within
an hour before or after or it can reduce the
effectiveness of the drug.
 Antihistamines that are prescribed by
doctors for the treatment of patients who
suffer from allergies are different from H2
blockers. Those go against histamines thus
reducing allergic reactions.
RANITIDINE
Patient Teaching
 Teach patient to report pain,coughing,or
vomiting of blood.
 Advise pt. to avoid smoking, because it
can hamper effectiveness of drug.
 Remind pt. that drug must be taken
exactly as prescribed to be effective.
 Direct pt. to separate rain tide and
antacid dosage by at least 1 hour.
 Warn pt. not ot drive a motor vehicle or
engage in dangerous activities until
stabilized on drug.
 Tell pt. that drug-induced impotence and
gynecomastia are reversible.
 Educate pt. in use of relaxation
techniques to decrease anxiety
DIET
 Teach pt. to eat foods rich with vitamin
B12 to avoid deficiency as a result of
drug therapy.
 Alert pt. to avoid foods and liquids that
cause gastric irritation, such as caffeine-
 containing beverages, alcohol , and
species.
EVALUATION
• Determine effectiveness of drug therapy and
presence of any side effects or adverse
reactions.Pt should be free of pain and
healing should progress.
• PROTON PUMP INHIBITORS (GASTRIC
ACID SECRETION
INHIBITORS,GASTRIC ACID PUMP
INHIBITOR)
PPIS SUPPRESS GASTRIC ACID
SECRETION BY :
 • inhibiting the hydrogen/potassium
adenosine triphosphate(ATPase) enzyme
system located in gastric parietal cells.
• tend to inhibit gastric acid secretions up to
90%greater than the H2 blockers(histamine
antagonists)
• these agents block the final step of acid
production.
OMEPRAZOLE(PRILOSEC) was the first PPI
marketed ,
followed by lansoprazole(prevacid),
Rabeprazole (aciphex),
 These agents are effective in
suppressing
Pantoprazole (protonix),
 gastric acid secretions and are used
to treat
Esomeprazole (Nexium),
 peptic ulcer and GERD.
and dexlansoprazole (dexilant),
 a delayed-release oral capsule.
Lansoprazole
 Ulcer relief usually occurs in 1 week.
Rabeprazole
 More effective in treating duodenal ulcers
than gastric ulcers, but it is most effective
for treating GERD and hypersecretory
disease (Zollinger-Ellison syndrome).
Pantoprazole
 Is prescribed to treat short-term erosive
GERD.IV pantoprazole is also reported as
effective in treating Zollinger Ellison
syndrome.
Esomeprazole
 Has the highest success rate for healing
erosive GERD.
Omeprazole
 Promotes irreversible hydrogen or potassium
ATPase inhibition until new enzyme is
synthesized,which could take days,whereas
rabeprazole causes reversible ATPase
inhibition.
Dexlansoprazole
 Is prescribed to trat erosive esophagitis and
symptomatic nonerosive GERD.
All PIs in large doses can be combined with
antibiotic to treat H.pylori.
Two combination medications involving PPIs are
omeprazole with sodium bicarbonate(Zegerid) and
esomemprazole with naproxen(Vimovo).
Zegerid
 is the only drug given to prevent stress
ulcer in critically
ill pts. Also used to treat GERD, erosphagistis and
gastric and duodenal ulcers.
 can now be found over the counter as well.
Vimovo
 is an immediate-release PPI layered over
an entericcoated NSAID in one tablet
used to prevent NSAID-associated
gastric ulcer.
PHARMACOKINETICS and
PHARMACODYNAMICS
 The duration action for esomemprazole
is 24 hrs.These drugs have a short life
and are highly protein-bound (97%).PPIs
should usually taken before meals .
 Caution should be used in pts. with
hepatic impairement; liver enzymes
should be monitored .
 Possible side effects include
headache,dizziness,diarrhea,abdominal
pain,and rash.prolonged use of PPIs may
increase the risk for cancer,although this
has only been proven in mice,not
humans.
DRUG INTERACTION
  PPIs can enhance the action of digoxin,oral temperature in an airtight container,it will remain
anticoagulants,certain benzodiazepines, and stable for up to 2 yrs.
phenytoin,because they interfere with liver
metabolim of these drugs.
PHARMACOKINETICS and
PHARMACODYNAMICS
 The duration action for esomemprazole is
24 hrs.These drugs have a short life and are
highly protein-bound (97%).PPIs should
usually taken before meals .
 Caution should be used in pts. with hepatic
impairement; liver enzymes should be
monitored .
 Possible side effects include
headache,dizziness,diarrhea,abdominal
pain,and rash.prolonged use of PPIs may
increase the risk for cancer,although this has
only been proven in mice,not humans.
DRUG INTERACTION
 PPIs can enhance the action of digoxin,oral
anticoagulants,certain benzodiazepines, and
phenytoin,because they interfere with liver
metabolim of these drugs.
PEPSIN INHIBITOR(MUCOSAL
PROTECTIVE DRUG)
Sucralfate(Carafate)
 a complex of sulfated sucrose and aluminum
hydroxide classified as a pepsin
inhibitor/mucosal protective drug.
 it is nonabsorbable and combines with
protein to form a viscious substance that
covers the ulcer and protects it from acid
and pepsin.
 does not neutralize acid or decrease acid
secretions.
DOSAGE: 1 gram,usually 4x a day before meals
and at bedtime.if antacid is added to decrease
pain,they should be given either 30 mins.before or
30mins. After the administration of
sucralfate.because sucralfate is notsystematically
absorbed ,side effects are few:however,it can cause
constipation.if the drug is stored at room