A type of immunization that causes development of a complete and long-lasting

immunity to a certain infection through exposure of the body to the associated disease
antigen
Natural: having the disease
Artificial: receiving a vaccine or toxoid
DRUGS: Toxoids or vaccines that are administered to a host to stimulate host production
of antibodies.
Biologic antimicrobial drugs (also referred to simply as biologics) are substances such
as antitoxins, antisera, toxoids, and vaccines that are used to prevent, treat, or cure
infectious diseases. Toxoids and vaccines are known as immunizing biologics, and
they target a particular infectious microorganism.

Bacterial exotoxins that are modified or inactivated (by chemicals or heat) so that they
are no longer toxic but can still bind to host B cells to stimulate the formation of antitoxin;
toxoids are often used in the same manner as vaccines to promote artificial active
immunity in humans. They are one type of active immunizing drug (e.g., tetanus toxoid).

Vaccine: Suspensions of live, attenuated, or killed microorganisms that can promote an

artificially induced active immunity against a particular microorganism. They are another
type of active immunizing drug (e.g., tetanus vaccine).

Vaccines contain substances that trigger the formation of these antibodies against
specific pathogens. They may contain the actual live or attenuated pathogen or a killed
pathogen.

A type of immunization in which immunity to infection occurs by injecting a person with

antiserum or concentrated antibodies that directly give the host the means to fight off an
invading microorganism (artificial passive immunization). The host's immune system
therefore does not have to manufacture these antibodies. This process also occurs
when antibodies pass from mother to infant during breastfeeding or through the placenta
during pregnancy (natural passive immunization).
DRUGS: Drugs containing antibodies or antitoxins that can kill or inactivate pathogens
by binding to the associated antigens. These are directly injected into a person (host)
and provide that person with the means to fend off infection, bypassing the host's own
immune system.
Toxin: Any poison produced by a plant, animal, or microorganism that is highly toxic to
other living organisms.

Toxoid: An antiserum against a toxin (or toxoid). It is most often a purified antiserum
obtained from animals (usually horses) by injection of a toxin or toxoid so that antibodies
to the toxin (i.e., antitoxin) can be collected from the animals and used to provide
artificial passive immunity to humans exposed to a given toxin (e.g., tetanus
immunoglobulin).

Venom: A poison that is secreted by an animal (e.g., snake, insect, or spider)

Antiserum: A serum that contains antibodies. It is usually obtained from an animal that
has been immunized against a specific antigen.
Antivenin: An antiserum against a venom (poison produced by an animal) used to treat
humans or other animals that have been envenomed (e.g., by snakebite, spider bite, or
scorpion sting).

Antigens: Substances, usually proteins and foreign to a host, that stimulate the
production of antibodies and that react specifically with those antibodies. Examples of
antigens include bacterial exotoxins and viruses. An allergen (e.g., dust, pollen, mold) is
an antigen that can produce an immediate-type hypersensitivity reaction or allergy.
When the body first comes into contact with antigens (foreign proteins) from an invading
organism, specific information is imprinted into a cellular memory bank of the immune
system.

Antibodies: Immunoglobulin molecules that have an antigen-specific amino acid

sequence and are synthesized by the humoral immune system (B cells) in response to
exposure to a specific antigen. Their purpose is to attack and destroy molecules of this
antigen

Antibody Titer: The amount of an antibody needed to react with and neutralize a given
volume or amount of a specific antigen.
Immunization: The induction of immunity by administration of a vaccine or toxoid (active
immunization) or antiserum (passive immunization).

Immunoglobulins: Glycoproteins synthesized and used by the humoral immune system

(B cells) to attack and kill all substances foreign to the body. The term is synonymous
with immune globulins.

Characteristic
Artificial Type of

Active

Passive

Immunizing

Toxoid or vaccine

Immunoglobulin or antitoxin

Results from an antigen-antibody

Results from direct administration of exogenous

Mechanism of

response similar to that after

antibodies; antibody concentration will decrease

Action

antigen exposure in the natural

over time, so if exposure is expected it is wise to

disease process
To prevent development of active

continue passive immunizations

To provide temporary protection against disease in

disease in the event of exposure

individuals who are immunodeficient, those for

to a given antigen in an

whom active immunization is contraindicated, and

individuals who have at least a

those who have been exposed to or anticipate

partially functioning immune

exposure to the organism or toxin; an antibody

system
Mechanism of action. Protection

response is not stimulated in the host

Natural
Mechanism of

of owns antibodies during actual

Action

infection.

Drug

Use

Passive Immunization Drugs:

Hepatitis B

Transmission from mother to infant through placenta

or during breast feeding.

Varicella-zoster
Active Immunization Drugs:
Hepatitis b virus vaccine (recombinant)
Herpes zoster virus vaccine (live, attenuated)
Influenza virus vaccine
Pneumococcal bacterial vaccine, polyvalent
Pneumococcal thirteen-valent conjugate vaccine
Varicella virus vaccine
Passive immunizing drugs are the actual antibodies (immunoglobulins) that can kill or
inactivate the pathogen.
Adverse Effects: undesirable effects of the various immunizing drugs can range from
mild and transient to serious and even life threatening:

Body System
Minor: CNS
Minor: INTEG

Adverse Effect:
Fever, adenopathy
Minor rash, soreness at injection site,
urticarial, arthritis
Fever > 103 F encephalitis, peripheral

Severe: CNS

neuropathy, anaphylactic rxn, shock,

Severe: INTEG
Severe: RESP
Severe: Other

unconsciousness
Rash
Dyspnea
Cyanosis

Drug (Pregnancy
Category)

Pharm Class

Indications/Uses

Active
TDaP Vaccine

Mixed toxoid/vaccine

Prophylaxis against diphtheria,

tetanus, & pertussis

Hepatitis B Vaccine (C)

Influenza Virus Vaccine
(C)
Pneumococcal vaccine,
polyvalent (C)
Varicella Virus Vaccine
(C)

Viral surface antigen vaccine

Hepatitis B prophylaxis

Viral surface antigen vaccine

Influenza prophylaxis

Bacterial capsular antigenic

Streptococcus pnuemoniae

extract vaccine

prophylaxis
Prophylaxis against varicella

Live, attenuated viral vaccine

virus (causes chickenpox &

Drug (Pregnancy Category)

Passive
Hepatitis B Immunoglobulin

shingles)

Pharm Class

Indication/Uses

Pooled human

Passive Hepatitis B

immunoglobulin

prophylaxis

TDaP: are prevalent in populations of many developing countries throughout the world.
Full immunization is recommended for travelers and to those who live in those areas

Vaccine for just TD used to be given for people 7 years and older. Approved from 6

weeks 6 years as full child immunization

Due to increase in pertussis it is recommended that people get the TDaP
Booster dose required every 10 years
Available as parenteral preparations and given as DEEP IM injection
Contraindicated in people who have had prior systemic hypersensitivity rxn or
neurologic rxn to one of the ingredients

Contraindicated in people with concurrent acute or active infection but not in cases of

minor illness.
No significant studies but safe to give after first trimester
Tetanus, diphtheria & pertussis are very different conditions but a combo vaccine is
used

Hepatitis B: noninfectious viral vaccine containing hep B surface antigen made using
recombinant DNA technology with yeast and two or more organisms into an injection

Health care workers are considered high risk for Hep B exposure
Hospitals require the vaccine upon employment
Recommended that all children receive it (usually started shortly after birth)
o Adults with diabetes mellitus should get it
Contraindicated in persons who are hypersensitive to yeast
Administered IM injection in series of 3 injections

Influenza Virus Vaccine: used to prevent the flu & should be given each year before flu
season begins (single most important control measure)

FluMist given intranasally where other forms are given IM

New vaccine created each year containing atleast 3 strains chose based on recent

epidemiologic data indicating which flue virus will most likely reach North America
Latest vaccine included activity against H1N1 strain
Made from highly purified egg-grown viruses that are inactivated

Flu characteristics: abrupt onset of fever, myalgia, sore throat, and nonproductive cough

Older adults, children and adults with underlying health problems (asthma,

cardiopulmonary disease, cancer, diabetes) are at ^ risk for complications

Health care workers = high risk & kids/teens receiving long term aspirin therapy
which also puts at risk for Reyes syndrome after the flu

Death increased not just from flu but from other illnesses worsened by the flu
90%+ deaths linked to flu/pneumonia occur in people 65+

Flu Vaccine Continued: Older persons, especially those residing in nursing homes, can
avoid severe illness, secondary complications, and death by taking the influenza
vaccine. In elderly persons, the vaccine can prevent hospitalization and pneumonia up to
50% to 60% of the time and death up to 80% of the time. Achieving a high rate of
vaccination among nursing home residents can reduce the spread of infection in a
facility, thus preventing disease through herd immunity. The CDC now recommends that
all people older than 6 months of age receive the influenza vaccine.

Pneumococcal Vaccine, polyvalent & 13 valent: two different forms & also protect
against any other illness caused by streptococcus pneumoniae. Pneumococcus is the
common name for the bacterium S. pneumoniae the causative organism of this common
bacterial infection.

Polyvalent type used mostly in adults (designed to be effective against 23 strains)

May be recommended for pediatric pts at high risk as result of chronic illness
13 valent type routinely recommended for kids (designed to fight top 13 strains found

in pediatric cases)
2008 CDC recommended all smokers 19-64 receive it
Contraindications to the use: known drug allergy to components of the vaccine, as
well as the presence of current significant febrile illness or immunosuppressed state
as a result of drug therapy (cancer chemotherapy)

The vaccine may sometimes still be given in such cases, if it is felt that withholding

the vaccine poses an even greater risk to the patient

Herpes Zoster Vaccine: new (2008) for prevention of herpes zoster (shingles) caused by
the varicella-zoster virus that also causes chickenpox.
Recommended for patients 50+
One time vaccine can be given to pt who already had shingles
Doesnt prevent postherpetic neuralgia
Live attenuated vaccine risk of transmission from vaccinated person to others
Contraindications: hypersensitivity to neomycin, gelatin or other parts of the vaccine,

immunosuppressed pt, or pt receiving immunosuppressant therapy, pregnant women

Not used to prevent chickenpox & not given to children
Must be stored in freezer

Varicella Virus Vaccine: live attenuated virus vaccine is used to prevent varicella
(chickenpox) attenuated by passage thru human & embryonic guinea pig cell cultures

Varicella primarily occurs in children under the age of 8 or individuals with

compromised immune systems (adult HIV pt)
Estimated 10% of children over 12 are still susceptible to it
2% of adults develop varicella-zoster virus infection
50% of deaths are adult cases
o Half of these are in immunocompromised patients
Must be stored in a freezer
Contraindicated: immunocompromised pt or pt who got high doses of systemic
steroids the previous month
Avoid salicylates for 6 weeks Reyes Syndrome possibility
Given at 12 months then 2nd stage given between 4-6 years of age
o Second dose MUST be given

Hepatitis B immunoglobulin: provide passive immunity against hep b infections in

postexposure prophylaxis & treatment of pt exposed to Hep B virus or infectious
materials (blood, plasma, serum)

Prepared from humans with high titers of antibody (all donors tested for HIV first)
Pregnancy is NOT a contraindication because of the devastating possibilities of a
Hep B infection.

Immunoglobulin: available in IM or IV injection. Provides passive immunity by increasing

antibody titer and antigen antibody rxn potential.

Given to help prevent certain infections or ameliorate the disease of the infected
Pooled from blood of atleast 1000 human donors

Availability depends on donors & doctors cant give it for non FDA approved due to

shortage.
FDA Approved Uses:
o
o

Pediatric HIV infection

B-cell chronic lymphocytic

o
o
o

leukemia
Bone marrow transplant
Hepatitis A
Idiopathic thrombocytopenic
purpura

o
o
o
o

Kawasaki disease
Immunoglobulin deficiencies
Measles
Primary Immunodeficiency

o
o

Disease
Rubella
Varicella

Rh0(D) Immunoglobulin: used to suppress active antibody response for the

formation of anti-Rh0(D) antibodies in Rh0(D) negative pt exposed to Rh +
blood.

Rh- react to Rh+ as if it is foreign causes immune response rxn can be fatal
This immunoglobulin helps prevent the rxn
Most common cause maternal-fetal Rh incompatibility (postpartum)
Only mother is normally dosed
Objective is to prevent a harmful maternal immune response to a fetus during future

pregnancy if a Rh- mother becomes pregnant with Rh+ child

Prepared from plasma or serum of adults with high titer of anti Rh0(D) antibody to the

RBC antigen Rh0(D)

Contraindicated in pt who have been previous immunized with this drug in

RH0(D)/Du-positive pt.
Normally given postpartum but is category C
o

Rabies Immunoglobulin: passive immunizing drug that is administered

concurrently with rabies vaccine following suspected exposure to virus

Derived from human cells that are harvested from people who have been immunized

with a rabies vaccine

Only contraindication: allergy to the drug pt may still need to be dosed vs face

infection from a pretty much fatal infection.

Decision is made based on the probability of rabies infection given the particular
circumstances surround the animal bite
o
o
o
o
o
o
o

Tetanus immunoglobulin: passive immunization effective against tetanus

Contains antitoxin antibodies that neutralize the bacterial exotoxin produced by

clostridium tetani
Prepared from plasma of adults who are hyper immunized with the tetanus toxoid
Given as a prophylaxis to pt with tetanus prone wounds
May also be used to treat active tetanus
o
o
o
o
o
o
o
o

Varicella-zoster immunoglobulin: available only in generic form from the

American Red Cross & can be used to modify/prevent chickenpox to pt with
recent significant exposure

Best if administered within 96 hours of exposure

Candidates- high risk for serious disease or complications if they become infected
o Newborns including preemies & immunocompromised adults
If a pregnant woman gets it within 5 days of delivery VZIG is given to baby
Beneficial to mother & baby during pregnancy if given ASAP after diagnosis
Health adults (including pregnant women) are evaluated on case by case basis
Duration of protection with VZIG = 3 weeks
Prepared from plasma of donors with high titers to Varicella Zoster Virus
o
o
o
o
Active: dont want to give immunization to someone who is sick because the

body needs to work on fighting the infection and not on building immune response to the
immunization.

Patient must be:

1. In good immune health
2. No Allergies to eggs or yeast
o
o

Systemic reaction: whole body involved

Use patient immunity

Introduce deadened/weakened form of the virus

Pt gets injection & body is stimulated to form antibodies

Toxoid: for bacterial infections (deadened/weakened form)

Body has memory for future exposure

Passive: dont use the patient body

Huge immunoglobulin or gamma globulin
Not specific to disease
Immune booster
Reduce risk of getting disease

From the mother thru breast milk or placental transfusion (week 38-40)
Placental immunity passes all immunity the mother has or was exposed to as a child

to the baby
Dont rush your babys birthday!
Passive immunizing drugs may precipitate serum sickness, carefully assess patients
who have chronic illnesses, are debilitated, or are elderly. This includes measuring
vital signs, completing a physical assessment, and obtaining a medication history, as
well as examining the results of any laboratory testing ordered by the prescriber.
o
o

Labs:

o
o

WBC indicates infection

o
o
o

WBC infection is going

o
o
o
o
o
o
o
o
o

Pain: An unpleasant sensory and emotional experience associated with

actual or potential tissue damage.

Pain threshold: The level of a stimulus that results in the sensation of pain.

Pain tolerance: The amount of pain a patient can endure without its
interfering with normal function.

Acute pain: Pain that is sudden in onset, usually subsides when treated, and
typically occurs over less than a 6-week period.

Chronic pain: Persistent or recurring pain that is often difficult to treat.

Includes any pain lasting longer than 3 to 6 months, pain lasting longer than 1
month after healing of an acute injury, or pain that accompanies a nonhealing
tissue injury.

o
o

Phantom pain: Pain experienced in the area of a body part that has been
surgically or traumatically removed.

Referred pain: Pain occurring in an area away from the organ of origin.

Somatic pain: Pain that originates from skeletal muscles, ligaments, or

joints.

Special pain situations: The general term for pain control situations that are
complex and whose treatment typically involves multiple medications, various
health care personnel, and nonpharmacologic therapeutic modalities (e.g.,
massage, chiropractic care, surgery).

Superficial pain: Pain that originates from the skin or mucous membranes;
opposite of deep pain.

Vascular pain: Pain that results from pathology of the vascular or

perivascular tissues.

Visceral pain: Pain that originates from organs or smooth muscles.

Neuropathic pain: Pain that results from a disturbance of function or pathologic

change in a nerve
o

Deep pain: Pain that occurs in tissues below skin level; opposite of superficial

pain
o

Central pain: Pain resulting from any disorder that causes central nervous system

damage.
o

Breakthrough pain: Pain that occurs between doses of pain medication.

Cancer pain: Pain resulting from any of a variety of causes related to cancer

and/or the metastasis of cancer.

o
o
oOpioid analgesics: Synthetic drugs that bind to opiate receptors to relieve pain.
o

oOpioid nave: Describes patients who are receiving opioid analgesics for the first time
and who therefore are not accustomed to their effects.
o

oOpioid tolerance: A normal physiologic condition that results from long-term opioid use,
in which larger doses of opioids are required to maintain the same level of analgesia and in
which abrupt discontinuation of the drug results in withdrawal symptoms (same as physical
dependence).
o

oOpioid tolerant: The opposite of opioid nave; describes patients who have been
receiving opioid analgesics (legally or otherwise) for a period of time (1 week or longer) and
who are at greater risk of opioid withdrawal syndrome upon sudden discontinuation.
o

oOpioid withdrawal: The signs and symptoms associated with abstinence from or
withdrawal of an opioid analgesic when the body has become physically dependent on the
substance.
o

Type

of Pain
o
Acute o

Onset

Sudden (minutes to o

hours) usually sharp

localized physiological

Duration

Examples

Limited (has

MI,

an end)

appendicitis, dental
procedures, kidney

response (SNS:

stones, surgical

tachycardia, sweating,

procedures

pallor, BP
Chron o
Slow (days to

ic

Persistent,

Arthritis,

months) long duration, dull, recurring (endless)

cancer, low back

persistent, aching

pain, peripheral
neuropathy

o
o

SNS: Sympathetic Nervous System

oThe body is also equipped with certain endogenous neurotransmitters known

as enkephalins and endorphins. These substances are produced within the body to fight
pain and are considered the body's painkillers.
oGate Theory:
o
o
o

o
o
o
o
o
o
o

World Health Organization (WHO)

Step 1: Use of nonopioids once pain has been identified and assessed (with
or without adjuvants)
Step 2: If pain persists use of opioids with or without nonopioids or
adjuvants
Step 3: Use of opioids for moderate or severe pain with or without nonopioids
or adjuvants

o
o
o
o

7-10

o
o
4-6

o
o
o

1-3

o
o
o

A
c
ti
o
n

Type

o OPIOIDS
o Contrai
ndicatio
ns

T
e
a
c
hi
n
g
N

Over
dose
Treat
ment

V
e
r
y
s
tr
o
n
g
p
a
i
n
r
e
li
e

o
o

Agoni
st
binds
to
pain
recep
tor in
brain

Agoni
stantag
onist

binds
to
pain

o
o

Known
drug
allergy
Severe
asthma
Exerci
se
cautio
n:
Respira
tory
insuffici
ency,
Elevate
d
intracra
nial

e
e
d
s
F
e
nt
a
n
yl
p
at
c
h

n
o
h
e
at
in

o
o

o
o
o

nalox
one
(Narc
an)
given
IV
naltre
xone
(ReVi
a)
given
PO
Used
to

v
e
r
o
o

a
ll
e
v
i
a
t
e
m
o
d
e
r
a
t
e
t

recep
tor &
cause
sa
weak
er
pain
respo
nse
than
a full
agoni
st
o
o

o
Antag
onist
(nona
nalge
sic)
binds
to

pressur
e,
morbid
obesity,
sleep
apnea,
myasth
enia
gravis,
paralyti
c ileus,
pregna
ncy
*Especi
ally
with
long
term
use or
high
dose

g
p
a
d
s,
pr
o
p
er
di
s
p
o
s
al
,
o
nl
y
fo
r

mana
ge
overd
ose &
addict
ion

o
s
e
v
e
r
e
p
a
i
n
o
o

C
o
u
g
h
s
u
p
p

recep
tor
does
nt
reliev
e
pain

comp
etes

o
pi
oi
d
to
le
ra
nt
pt
,
k
e
e
p
a
w
a
y
fr
o
m

r
e
s
s
a
n
t

c
hil
dr
e
n,
d
o
n
ot
st
or
e
in
w
ar
m
d
a
m
n
pl

a
c
e
s
o
o
o
o

Side Effects of Opioid

Constipation
Nausea & Vomiting GI
peristalsis, stimulate
vomiting in CNS.

Sedation & Mental Clouding

change in mental status

Respiratory Depression

o
o

Dry Mouth
Pruritus itching

o
o

Preventative Measures
fluids, stool softener

Antiemetic medication

Persistent drug-related
sedation may be managed
with decrease in dose or
change in opioid drug. CNS
stimulants can be ordered too
May be reversed with
Naloxone and without
analgesia reversal
Suckers, artificial saliva drops,
Diphenhydramine (Benadryl)

o
o

o
o
o
o

Dysphoria or Euphoria
Sleep disturbance
Sexual Dysfunction
Antidiuretic hormone
secretion

o
o
o

Ongoing assessment

o
o

Opioid Drugs:

o Chemical
Category
o
o

Meperidinelike drugs
Methadonelike drugs

Morphine-like
drugs

o
o

Other

o Opioid Drugs
o

Meperidine, *fentanyl, remifentanil, sufentanil,

alfentanil

Methadone (treatment of detox in addicts)

Morphine, heroin, hydromorphone,

oxymorphone, levorphanol, codeine,
hydrocodone, oxycodone
Tramadol, tapentadol

*Strong opioids (fentanyl, sufentanil, alfentanil) used in combo with

anesthetics for surgery

Equianalgesia refers to the ability to provide equivalent pain relief by

calculating dosages of different drugs and/or routes of administration that
provide comparable analgesia.

Opioids can cause an abnormal increase in the serum levels of amylase,

alanine aminotransferase, alkaline phosphatase, bilirubin, lipase, creatinine
kinase, and lactate dehydrogenase

o Body
Syste
m
o

Cardiov
ascular

CNS

o
o

o Opioid Induced Adverse Effect

*Hypotension, flushing, bradycardia (

Sedation, disorientation, euphoria, lightheadedness,

dysphoria

GI

Nausea, vomiting, constipation, biliary tract spasm

Genito
urinary

Urinary retention ( in bladder tone give low dose

of opioid agonist or opioid agonist-antagonist)

INTEG

*Itching, rash, wheal formation

Respira
tory

Respiratory depression possible & aggravation of

asthma

o
o

*caused by release of histamine which causes vasodilation

o

Gene
ric
Nam
e
o Nalox
one
(IV)
o Naltr
exon
e
(PO)
o
o

Opioid Agonist Reversal Drugs

Trad
o Adverse Effects
e
Nam
e

Narc
an

ReVi
a

BP dysrhythmias, pulmonary
edema, withdrawal

Nervousness, headache, nausea,

vomiting, pulmonary edema,
withdrawal

Where x = amount of desired opioid in 24 hours and EA = equianalgesic dose

obtained from the table above

o
o
o

For example: A patient with colon cancer is currently taking oral oxycodone
80 mg every 12 hours and needs to be converted to intravenous morphine
due to a bowel obstruction. What is the equivalent IV morphine dose?

o
o
o

Step 1: Determine the 24-hour amount of oxycodone taken by this patient:

80 mg 2 doses per 24 hours = 160 mg per 24 hours
Step 2: Using the conversion table above, find the equianalgesic (EA) doses
of oxycodone and parenteral morphine:
15 mg oxycodone = 10 mg parenteral morphine
Step 3: Use the above equation and solve for x by cross-multiplying:
Where x = amount of parenteral morphine in 24 hours (solve by crossmultiplying)

o
o
o

Opioid Agonist
o
o

D
r
u
g

Ro
ute

M
o
r
p
h
i
n
e

o
o

S
u
l
f

o
O

Pe
ak
Pla
sm
a
Co
nc
ent
rati
on

IM

o
R

3060
mi

El
im
in
ati
o
n
of
H
alf
lif
e

1.
74.
5
hr

o
Du

o
6-7

o
o

o
o

Action

Blocks
periphera
l pain
impulses
by
inhibition
of
prostagla
ndin
synthesis
(mild to
moderate
pain)
Lowers
febrile
body
temp by

Acetaminophen (Nonopioid)
o

Side
Effec
ts

Ras
h,
naus
ea
vomi
ting

o
o

Muc
h
less
com
mon
but
more
seve
re:
bloo
d
disor
ders,
dysc

Overdos
e&
Treatme
nt

Acetylcys
teine is
the
recomme
nded
antidote
for
acetamin
ophen
toxicity
and
works by
preventin
g the
hepatoto
xic
metabolit
es of
acetamin
ophen
from
forming.
Most
effective
if given
within 10

Limitation
on daily
amount

Contraindi
cation:
known
allergy,
severe liver
disease,
genetic
disease
G6PD

Large
amounts
can cause
hepatotoxic
ity

4000 mg

o
o

Antacid: basic compound composed of a different combo of acid-neutralizing

ionic salts

Chief cells: Cells in the stomach that secrete the gastric enzyme pepsinogen
(a precursor to pepsin).

Gastric glands: Secretory glands in the stomach containing the following cell
types: parietal, chief, mucous, endocrine, and enterochromaffin.

Gastric hyperacidity: The overproduction of stomach acid.

Hydrochloric acid (HCl): An acid secreted by the parietal cells in the lining
of the stomach that maintains the environment of the stomach at a pH of 1 to
4.

Mucous cells: Cells whose function in the stomach is to secrete mucus that
serves as a protective mucous coat against the digestive properties of HCl.
Also called surface epithelial cells.

Parietal cells: Cells in the stomach that produce and secrete HCl. These
cells are the primary site of action for many of the drugs used to treat acidrelated disorders.

Pepsin: An enzyme in the stomach that breaks down proteins.

o
o

o
A

Antacids

H2 Blockers

used to
neutralize
stomach
acid, They
do not
prevent the
overproduc
tion of acid
help
neutralize
acid
secretions.

hydrogen
ion secretion
from parietal
cells, results
of pH in
stomach
&relief of
symptoms
associated
with
hyperacidity

antiulcer
treatment,
antiflatulen
t, acute
relief of
symptoms
associated
with peptic
ulcer,
gastritis,
gastric
hyperacidit
y, and
heartburn.

calcium
antacids may
lead to the

o
I

GERD, peptic
ulcer
disease, &
erosive
esophagitis;
adjunct
therapy in the
control of
upper GI tract
bleeding;&
pathologic
gastric
hypersecretor
y conditions
such as
ZollingerEllison
syndrome

Rare: but -

PPI

bind directly to the

hydrogen-potassiumATPase pump
mechanism & irreversibly
inhibit the action of this
enzyme, = total blockage
of hydrogen ion secretion
from the parietal cells.

erosive esophagitis,
symptomatic GERD,
short-term treatment of
active duodenal ulcers
and active benign gastric
ulcers, gastric
hypersecretory
conditions, NSAID
induced ulcers, and for
stress ulcer prophylaxis,
Long-term therapeutic
uses = maintenance of
healing of erosive
esophagitis and
pathologic hypersecretory
conditions, including both
GERD and ZollingerEllison syndrome.

Peptic ulcer disease is a general term for gastric or duodenal ulcers that
involve digestion of the GI mucosa by the enzyme pepsin.

gram-negative spiral bacterium, Campylobacter pylori, was isolated from

several patients with gastritis.

The official name of the bacterium was changed to Helicobacter pylori

because it was felt to have more characteristics of the Helicobacter genus.

The bacterium is found in the GI tracts of roughly 90% of patients with

duodenal ulcers and 70% of those with gastric ulcers.

First-line therapy includes a 10- to 14-day course of a proton pump inhibitor

and the antibiotics clarithromycin and either amoxicillin or metronidazoleor a
combination of a proton pump inhibitor, bismuth subsalicylate and the
antibiotics tetracycline and metronidazole Many different combinations are
used, but all incorporate the aforementioned key drugs.

Stress-related mucosal damage is an important issue for critically ill patients.

Stress ulcer prophylaxis (or therapy to prevent severe GI damage) is
undertaken in almost every critically ill patient in an intensive care unit (ICU)
and for many patients on general medical surgical units.

D
r
u
g
A
n
t
a
c
i
d
s
A
l
u
m
n
i
n
u
m
,

Ac
tio
n

Ne
utr
aliz
e
sto
ma
ch
aci
d.
Do
not
pre
ven
t
pro
duc
tion
of

Side
Effects
Calcium
may
lead to
kidney
stones
Milk of
magnesi
a can
cause
diarrhea
,
excessiv
e use
can
cause
systemi
c
alkalosis

Indi
cati
ons

Contrai
ndicati
on

Acut
e
relie
f of
sym
pto
ms
ass
ocia
ted
with
pept
ic
ulce
r,
gast
ritis,
hyp

Magnesi
um must
be
avoided
in pt
with
renal
failure
Electroly
te
disturba
nces, GI
obstructi
on

m
a
g
n
e
s
i
u
m
,
c
a
l
c
i
u
m
o
r

aci
d

(basic)
hyperaci
dity
when
calcium
containi
ng
antacid
is
stopped

erac
idity,
&
hear
tbur
n

s
o
d
i
u
m
T
e
a
c
h
i
n
g
N
e
e
d
s

Hypercalcemia -constipation, headache, thirst, dry mouth,

appetite, irritability, & metallic taste Alkalosis is irritability, muscle
twitching, numbness & tingling, cyanosis, slow & shallow respirations,
headache, thirst, & nausea. Acid rebound occurs in stopping of
antacids that have acid-neutralizing capacity & with overuse or
misuse of antacid therapy. If acid neutralization is sudden and , the
result is an immediate in pH to alkalinity and just as rapid a in pH
to a more acidic state in the gut.

I
n
t
e
r
a
c
t
i
o
n
s

Affect adsorption of other drugs, reduces their effectiveness.

Chelation inactivates other drugs that produce insoluble complexes,
stomach pH which absorption of basic drugs & absorption of
acidic drugs, urinary pH = secretion of acid drugs and excretion
of basic drugs

o
o

Drug &
Pregna
ncy
Categor
y
Aluminu
m
Hydroxi

Pharm
Class

Usual
Dosage
Range

Indicati
on

Aluminu
m
containi

Adult:
PO
600-

Hyperac
idity

de
(Amphoj
el) (A)
Aluminu
m
Hydroxi
de &
Magnesi
um
(Maalox,
Mylanta)
(A)
Calcium
Carbona
te
(Tums)
(A)
Magnesi
um
Hydroxi
de (Milk

ng
antacid
o

Combin
ation
antacid

o
o
o
o

Calcium
containi
ng
antacid

Magnesi
um
containi
ng

1500 mg
3-6xday
Adult:
PO
4002400 mg
3-6xday

Hyperac
idity

Adult:
PO
0.5-1.5
g prn

Hyperac
idity

Adult:
PO
0.65-1.3
g prn up

Hyperac
idity
(More
common

of
Magnesi
a) (A)

antacid

to 4xday

use
laxative)

o
o
o
o
o
o

Magnesium
Salts

Carbonate:
Gaviscon
Liquid,
Gaviscon
Extra
Strength
Relief
Formula
Tablets

Alumin
um
Salts
Carbon
ate:
Basalje
l

Calci
um
Salts
Carb
onate
:
Tums
,
Maal
ox,
Mylan
ta, Di-

Sodi
um
Salts
Bicar
bonat
e:
Alkaseltze
r,

Gel
o

Hydroxide:
milk of
magnesia

Oxide: Magox (used as

magnesium
supplement
Trisilicate:
Gaviscon
tablets
o

o
o
o

Hydroxi
de:
Alterna
GEL,
Amphoj
el

Increase pH = more basic

Citrat
e:
Citra
pH

o
o

D
r
u
g
H
2
R
e
c
e
p
t
o
r
s
O
T
C

Actio
n

Side
Effect
s

Indic
ation

Contrai
ndicati
ons

Protypi
cal acid
secretio
n
antago
nist.
but
dont
totally
abolish
acid
secretio
n
competi
tively
block
the H2
recepto

Rare: ,
3% of
cases
BP (w/
IV
admin)
headach
e,
lethargy,
confusio
n,
depressi
on,
halluicin
ation,
surred
speech,
agitation

Treatm
ent of
GERD,
peptic
ulcer
diseas
e,
erosive
esopha
gitis,
include
d to
control
upper
GI
bleedin
g,
patholo

Known
drug
allergy

Liver/kidn
ey
dysfuncti
on may
warrant
dose
adjustme
nt

p
H
o
f
t
h
e
s
t
o
m
a
c
h
&
r
e
li
e
v

r of
acidproduci
ng
parietal
cells,
parietal
cell
less
respon
sive
histami
ne &
stimulat
ion of
ACh &
gastrin
Up to
90%
inhibitio
n of
vagaland
gastrinstimulat
ed acid

,
increase
d
prolactin
secretio
n,
gyneco
mastia
(cimetidi
ne)
diarrhea
, abd
cramps,
impoten
ce,
BUN &
creatinin
e levels
liver
enzyme
levels,
jaundice
,
thrombo
cytopeni
a, rash,

gical
gastric
hyerse
cretory
conditi
ons
(Zolling
erEllsion
syndro
me)
Stress
ulcer
prophyl
axis

e
S
x
li
n
k
e
d
t
o
h
y
p
e
r
a
ci
d
it
y
T

secretio
n
occurs
when
histami
ne is
blocked

alopecia
,
sweatin
g,
flushing,

e
a
c
h
i
n
g
N
e
e
d
s
I
n
t
e
r
a
c
ti
o

Cimetidine risk of interaction than other 3 especially in elderly smoking

effectiveness, absorption of drugs that need acidic environment

n
s
o
o
o

D
r
u
g

R
o
u
t
e

H2 Receptor Drugs
o

O
n
s
e
t
o
f
A
c
ti
o
n

Pe
ak
Pl
as
m
a
Co
nc
en
tra
tio
n

E
li
m
i
n
a
ti
o
n
o
f
H
a
lf
li

D
u
r
a
t
i
o
n
o
f
A
c
t
i
o

f
e
o

c
i
m
e
ti
d
i
n
e
(
T
a
g
a
m
e
t
)

P
O

1
5
6
0
m
i
n

o
o

12
hr

2
h
r

4
5
h
r

r
a
n
it
i
d
i
n
e
(
Z
a
n
t
a
c
)
f
a
m
o

P
O
o I
V

P
O
o I
V

h
r
o I
m
m
e
d
i
a
t
e

1
.
4

o
24
hr
o <
15
mi
n

2
3
h
r
2
3
h
r

4
1
2
h
r
4
1
2
h
r

3
hr
o <
15
o

2
.
6
-

9
1
2

ti
d
i
n
e

(
P
e
p
c
i
d
)
n
i
z
a
ti
d
i

h
r
o I
m
m
e
d
i
a
t
e
o
o

o
mi
n

4
h
r
2
.
6
4
h
r

h
r
9
1
2
h
r

n
e
o
o
o
o
o
o
o
o

Dr
ug

Ac
tio
n

Side
Effect

Ind
ica
tio
n

Contrai
ndicati
on

Pro
ton
Pu
mp

P
PI
s
bi
nd

PPI
stop
90%+
acid

Erosi
ve
esop
hagit
is,

Known
drug
allergy

Inh
ibit
ors
PPI

irr
ev
er
sib
ly
to
th
e
pr
ot
on
pu
m
p.
Th
is
in
hi
biti
on
pr
ev
en
ts
th
e

secretio
n which
could
make pt
tempora
rily
achlorh
ydric
(without
acid)
o
o

Long
term
use &
develop
ment of
osteopo
rosis,
Cdif

sym
ptom
atic
GER
D
that
does
nt
resp
ond
to
H2
Rece
potr
Agon
ist,
Shor
t
term
treat
ment
of
activ
e
duod
enal
ulcer
s,
activ

m
ov
e
m
en
t
of
hy
dr
og
en
io
ns
ou
t
of
th
e
pa
rie
tal
cel
l
int
o
th

e
beni
gn
gastr
ic
ulcer
s,
hype
rsecr
etory
cond
itions
,
NSAI
D
indu
ced
ulcer
s, &
stres
s
ulcer
prop
hylax
is.
Used
with
antib
iotics

e
st
o
m
ac
h
&
bl
oc
ks
all
ga
str
ic
aci
d
se
cr
eti
on
.
Gi
ve
n
or
all

to
treat
H.
Pylor
i
infec
tions

y
or
thr
u
N
G
tu
be
&
IV
us
e

Tea
chi
ng
Ne
ed
s
Int
era
cti
on
s

Usually work best if taken 30-60 minutes before food

May serum levels of diazepam & phenytoin, bleeding with use of

warfarin & PPI absorption of ketoconazole, ampicillin, iron salts,
and digoxin. risk of death if given with clopidogrel if pt has acute
coronary syndrome. Sucralfate & food may delay absorption of PPI

o
o
o
o

Dru
g

o
R

Proton Pump Inhibitor Drugs

o O
o Pe
o
n
ak
s
Pl
e
as
t
ma
o
Co
f
nc
A
ent
c
rati
ti
on
o
n

E
l
i
m
i
n
a
t
i
o
n
o
f
H
a
l
f

Duratio
n of
Action

om
epr
azo
le
(Pri
los
ec)
lan
sop
raz
ole
(Pr
eva
cid)

o
o
P

h
r

5
da
ys

o
o
o
P

1
.
7
h
r

4
wk

l
i
f
e
0
.
5
1

1-5
days

h
r
1
2
h
o
u
r

24 hour

pan
top
raz
ole
(Pr
oto
nix)

o
o
P
o
I

2
.
5
h
r
E
n
d

22.5
hr
o En
d
of
inf
usi
on
o

o
f
i
n
f
u
s
i
o
n
o

DOSAGES

h
r
1
h
f

o
o

7 days
7 days

lansoprazole /
Prevacid
Pregnancy
Category B

o
o

Adult: PO 30 mg
daily

Adult: 60 mg PO once
daily initially, then
titrated and given in
single or multiple daily
doses, with dosage
titration up to a
maximum of 120 mg
PO tid

omeprazole /
Prilosec
Pregnancy
Category C

o
o

pantroprazole
/ Protonix
Pregnancy
Category B

o
o

PO/IV: 20-80 mg/day

depending on
indication

o
o

GERD, ulcer,
erosive
esophagitis

Esophagitis,
duodenal ulcer

o
o

Hypersecretory
conditions
GERD, ulcer,
stress ulcer
prophylaxis

o
o
o

D
r

o
R

MISC Acid Controlling Drugs

o
o Pe
o E
O
ak
l

o
D

o
Us

u
g

Pl
as
m
a
Co
nc
en
tra
tio
n

i
m
i
n
a
t
i
o
n
o
f
H
a
l
f
l
i
f

e
o

m
i
s
o
p
r
o
s
t
o
l
/
C
y
t
o
t
e
c
s

o
P

o
3

12
mi
n

2
0
4
0
m
i
n

Use: the discomfort of gastric / intestinal gas

o
1-

i
m
e
t
h
i
c
o
n
e
/
M
y
l
i
c
o
n
o

Use: Mucosal protectant in treatment of active stress

u
c
r
a
l
f
a
t
e
/
C
a
r
a
f
a
t
e
o

ulceration & in LTC for peptic ulcers

o
o
o
o
o
o

A
s
s
e
s
s
m
e
n
t
K
n
o

Nursing
Diagnosis

Constipatio
n related to
the

Nursing Process
o G
oa
l

Mi
ni
m

O
ut
c
o
m
e

Impl
eme
ntati
on:

Pt
st
at

Che
w
tab

w
G
I
h
x
,
a
l
u
m
i
n
u
m
&
m
a
g

adverse
effects of
aluminumcontaining
antacids
and other
drugs used
to treat
hyperacidit
y Diarrhea
related to
the
adverse
effects of
magnesium
-containing
antacids
and other
drugs used
to treat
hyperacidit
y Deficient
knowledge

al
di
arr
he
a
or
co
ns
tip
ati
on
o
o

Pa
tie
nt
de
m
on
str
at
es

e
s
m
e
a
s
ur
e
s
to
h
el
p
pr
e
v
e
nt
c
o
n

com
plete
ly,
shak
e
liqui
ds
befo
re
take
n,
Anta
cids
must
be
take
n
with
8 oz
wate
r

n
e
s
i
u
m
=
k
n
o
w
f
u
ll
li
s
t
o

related to
lack of
information
about
antacids,
H2 receptor
antagonists
, or PPIs,
including
their use
and
potential
adverse
effects

ad
eq
ua
te
kn
o
wl
ed
ge
ab
ou
t
us
e
of
dr
ug

o
o

sti
p
at
io
n
&
di
ar
rh
e
a
P
at
ie
nt
st
at
e
s
p

f
o
t
h
e
r
m
e
d
s
P
a
y
a
t
t
n
.
t
o

ur
p
o
s
e
of
ta
ki
n
g
a
nt
a
ci
d
s,
H
2
re
c
e

h
e
p
a
ti
c
f
u
n
c
ti
o
n

pt
or
a
g
o
ni
st
s,
&
P
PI

o
o

Patient Teaching Tips:

Medications are not to be taken, unless prescribed, within 1 to 2 hours of taking an antacid
because of their impact on the absorption of many medications in the stomach.
Advise the patient to contact the prescriber immediately if he or she experiences severe or
prolonged constipation and/or diarrhea; increase in abdominal pain; abdominal distension;
nausea; vomiting; hematemesis; or black, tarry stools (a sign of possible GI tract bleeding).

o
o
o

o
o

If the patient is taking enteric-coated medications, tell the patient that the use of antacids may
promote premature dissolution of the enteric coating. Enteric coatings are used to diminish the
stomach upset caused by irritating medications, and if the coating is destroyed early in the
stomach, gastric upset may occur.
Encourage the patient to take H2 receptor antagonists exactly as prescribed. Inform the
patient that smoking decreases the drug's effectiveness. Advise that patient that H2 receptor
antagonists are not to be taken within 1 hour of antacids.
Advise the patient to take omeprazole and other PPIs before meals. Inform the patient that if
lansoprazole is being used, the granules may be sprinkled from the capsule into a tablespoon
of applesauce if needed.
Instruct the patient to follow the manufacturer's directions when taking simethicone.
Chewable forms must always be chewed thoroughly; liquid preparations need to be shaken
thoroughly before administration. Encourage patients experiencing flatulence to avoid
problematic foods (e.g., spicy, gas-producing foods) and carbonated beverages.
Sucralfate must be taken on an empty stomach, and antacids are to be avoided or, if
indicated, taken 2 hours before or 1 hour after sucralfate administration.
For a patient taking the drug regimen for the treatment of H. pylori infectionpeptic ulcer
disease, it is important to emphasize the need to take each drug, including the antibiotics,
exactly as prescribed and without fail to guarantee successful treatment. If treatment protocols
are not followed appropriately, the condition may likely recur.

Diarrhea: the passage of stools with abnormally increased frequency, fluidity,

and weight, or increased stool water excretion.

Chronic diarrhea lasts for longer than 3 to 4 weeks and is associated with
recurrent passage of diarrheal stools, possible fever, nausea, vomiting,
weight reduction, and chronic weakness.

Causes of acute diarrhea include drugs, bacteria, viruses, nutritional factors,

and protozoa. Causes of chronic diarrhea include tumors, acquired
immunodeficiency syndrome (AIDS), diabetes mellitus, hyperthyroidism,
Addison's disease, and irritable bowel syndrome (IBS).

Treatment is aimed at stopping the stool frequency, alleviating the abdominal

cramps, replenishing fluids and electrolytes, and preventing weight loss and
nutritional deficits from malabsorption.

replacement of fluids is the only treatment needed

Patients with diarrhea associated with a bacterial or parasitic infection must

not use antidiarrheal drugs, because this will cause the organism to stay in
the body longer and will prolong recovery

Category

Antidiarrheal Drugs

Adsorbents

Anticholinergics
(antimotility)

Opiates (antimotility)

Probiotics & intestinal

flora modifiers

Activated charcoal, aluminum

hydroxide, bismuth subsalicylate,
cholestyramine, polycarbophil

Atropine, hyoscyamine

Opium tincture, paregoric, codeine,

diphenoxylate, loperamide

Lactobacillus acidophilus,
lactobacillus GG, saccharomyces
boulardii

o
o
o
o
o

Antidiarrheal Drugs

o
o

Dr
ug

Act
ion

Ant
ich
olin
erg
ic

Slo
w
peri
stal
sis

Si
d
e
Ef
fe
ct
s
S
e
e
a
d
v
er
s
e
ef
fe
ct
s
ta

Indic
ation
s

Contrai
ndicati
ons

More
sever
e

Drug
allergy,
acute
GI
conditio
n
(obstru
ction or
colitis)

o
o

Opi
ate
s

Pro
bio
tics

bo
wl
mot
ility,

pai
n of
rect
al
spa
sm
s
Re
ple
nis

bl
e
S
e
e
a
d
v
er
s
e
ef
fe
ct
s
ta
bl
e
S
e
e

More
sever
e

Antibi
otic
induc

Drug
allergy,
acute
GI
conditio
n
(obstru
ction or
colitis)

Drug
allergy,
acute

h
bac
teri
a to
figh
t
diar
rhe
a
cau
sin
g
bac
teri
a

a
d
v
er
s
e
ef
fe
ct
s
ta
bl
e

GI
conditio
n
(obstru
ction or
colitis)
ed
diarrh
ea

o
o

Adsorbents effectiveness by absorption of many drugs

The therapeutic effects of the anticholinergic can be by coadministration

with antacids.

o
o

Drug

Bismuth
subsalicylate

Atropine,
hyoscyamine

Codeine,
diphenoxylat
e

o
o
o
o
o
o

o
o

Adverse Effects
Increased bleeding time, constipation, dark
stool, confusion, tinnitus, metallic taste, blue
gums
Urinary retention, impotence, headache,
dizziness, anxiety, drowsiness, bradycardia,
hypotension, dry skin, flushing, blurred vision
Drowsiness, dizziness, lethargy, nausea,
vomiting, constipation, hypotension, urinary
retention, flushing, respiratory depression

o
o
o

Drug

Bismut
h
subsali
cylate
OTC
PO

Uses

Adsorbents
o Side
Effects
o

caution pt
recoverin
g from
chickenpo
x or flu
due to risk
of Reyes
Syndrome
, adverse
effects
associate
d with
aspirin
based
products.

Contrai
ndicatio
ns

o
o

Bellad
onna
alkaloi
d
combi
nation
s

Harmless:
dark
tongue &
stool
Anticholinergic
o

Hyperse
nsitivity
to
anticholi
nergic,
narrow
angle
glaucom
a, GI
obstructi
on,
myasthe
nia
gravis,
paralytic
ileus,

toxic
megacol
on
o
o
o

Drug

Uses

Codeine

Dipheno
xylate
with
atropine

Rx antidiarr
heal
Rx
antidiarr
heal
inhibits
motility
&
excessi
ve GI
propulsi

Opiates
o Side
Effects
o

Dry
mouth,
abd
pain,
tachycar
dia
blurred
vision if
taken in

Contrain
dication
s

extreme
amount

on

OTC
antidiarr
heal
inhibits
peristals
is &
intestina
l
secretio
ns

Rx antidiarr
heal

Rx antidiarr
heal

Lopera
mide

Paregori
c

Tincture
of
opium

Ulcerativ
e colitis,
pseudom
embrano
us colitis
& acute
diarrhea
from Ecoli

Medicati
on error
death
use =
rare
Medicati
on error
death
use =

rare
o
o
o
o
o

Drug

Uses

Lactoba
cillus
acidophi
lus

Suppres
s growth
of
pathoge
nic
bacteria
improve
intestina
l barrier
function,
modulati

Probiotics
o Side
effects

Contrai
ndicatio
ns

on of
immune
system
& pain
percepti
on
o

o
o
o
o
o
o
o

Lactoba
cillus
GG

o
o

o
o

Cause of
Constipation
Adverse Drug
Effect

Example

Lifestyle

o
o

Analgesics, anticholinergics, iron

supplements, aluminum & calcium
antacids, opiates, calcium channel
blockers
Poor BM habits, voluntary refusal
Diet: poor fluid intake, low fiber, excessive
dairy
Physical inactivity, lack of exercise, elderly
Psychological factors, anxiety, stress,
hypochondria
Diabetes mellitus, hypothyroidism,
pregnancy, hypercalcemia, hypokalemia
Autonomic neuropathy, intestinal pseudoobstruction, MS, spinal cord lesions,
Parkinsons, stroke

o
o
o
o

o
o
Metabolic/Endocrin
e disorder
Neurogenic
disorder

o
o

o
o

Laxatives are used to treat constipation abnormal/infrequent/difficult

passage of BM

Constipation = symptom not disease. Disorder of movement thru the

colon/rectum

Ingestion digestionabsorptionstorage & removal

o
o
o
o
o
o
o
o

Categor
y
Bulkforming
Emollient
Hyperos
motic
Saline

Laxative Drug

Psyllium, methylcellulose

o
o

Docusate salts, mineral oil

Polyethylene glycol, lactulose, sorbitol, glycerin

Magnesium hydroxide, magnesium sulfate,

magnesium citrate
Stimulant
o Senna, bisacodyl
Laxatives are among the most misused OTC medications. Long-term and
often inappropriate use of laxatives may result in laxative dependence,
produce damage to the bowel, or lead to previously nonexistent intestinal
problems. With the exception of the bulk-forming type, laxatives are not to be
used for long periods
SB = small bowel
o

Drug Effect

o
Bu

o
E

Increase peristalsis

secretion of water
& electrolytes in SB
Inhibits absorption
H2O in SB
permeability in
SB
Acts only in large
bowel
water in fecal
mass
Softens fecal bass

o
Y
o
Y
o

o
Y
o
Y
o

o
Y
o
N
o
Y
o
Y

o
Y
o
Y
o
Y
o
Y

o
o
o
o
o

Hy
pe
ro
sm
oti
c

o
o

o
S

o
St

o
Y
o
Y
o

o
Y
o
Y
o

o
Y
o
N
o
Y
o
Y

o
Y
o
Y
o
Y
o
Y

o
o
o

o
o

o
o

Cate
gory
Bulkformi
ng
Emoll
ient
Hype
rosm
otic
Salin
e
Stimu
lant

Indication

Acute & chronic constipation IBS, diverticulosis

Acute & chronic constipation, fecal impaction, anorectal

conditions requiring facilitation of BM
Chronic constipation, bowel prep for diagnostic & surg
procedures

o
o

Constipation, bowel prep for diagnostic & surgical

procedures
Acute constipation, bowel prep for diagnostic & surg
procedures

o
o
o

The following are some of the more common uses of laxatives:

o
o
o
o
o
o
o
o
o
o

o
o

Facilitation of bowel movements in patients with inactive colon or anorectal

disorders
Reduction of ammonia absorption in hepatic encephalopathy (lactulose only)
Treatment of drug-induced constipation
Treatment of constipation associated with pregnancy and/or postobstetric
period
Treatment of constipation caused by reduced physical activity or poor dietary
habits
Removal of toxic substances from the body
Facilitation of defecation in megacolon
Preparation for colonic diagnostic procedures or surgery
general contraindications& precautions, including avoidance if drug allergy & caution
use in the following: acute surgical abd; appendicitis symptoms such as abd pain,
nausea, and vomiting; fecal impaction (mineral oil enemas excepted); intestinal
obstruction; and undiagnosed abd pain.

Cat
eg
ory
Bul

Adverse Effects

Impaction above strictures, fluid disturbance, electrolyte

o
o

kimbalance, gas formation, esophageal blockages, allergic

for
reaction
min
g
Em
o Skin rashes, decreased absorption of vitamins, lipid
olli
pneumonia, electrolyte imbalance
ent
Hy
o Abdominal bloating, electrolyte imbalance, rectal irritation
per
os
mot
ic
Sali
o Magnesium toxicity (with renal insufficiency) electrolyte
ne
imbalance, cramping, diarrhea, increase thirst
Sti
o Nutrient malabsorption, skin rashes, gastric irritation,
mul
electrolyte imbalance, discoloration in urine, rectal
ant
irritation
Laxatives alter intestinal function; so they can interact with other drugs, bc
many drugs are absorbed in the intestines. Bulk-forming can the absorption
of antibiotics, digoxin, salicylates, tetracyclines, & warfarin. Mineral oil can
decrease the absorption of fat-soluble vitamins (ADEK). Hyperosmotic can

cause increased CNS depression if they are given w/ barbiturates, general

anesthetics, opioids, or antipsychotics. Oral antibiotics can the effects of
lactulose. Stimulant the absorption of antibiotics, digoxin, nitrofurantoin,
salicylates, tetracyclines, & oral anticoagulants.
o Onset
o Typ
of
o Drug & Pregnancy Category
e
Actio
n
o PO: 6o Sti
12 hr
bisacodyl (Dulcolax) (C)
o Rectal
mul
ant
: 1560 min
o Sti
o PO: 6mla
senna (Senokot, others) (c)
nt24
irrit
hours
ant
Psyllium (Metamucil, Fiberall,)(B)
o Bul
o PO:
k12-24
for
hr

Methylcellulose (Citrucel) (B)

docusate sodium (Colace) docusate

calcium (Surfak) (C)

mineral oil (Kondremul Plain, Fleet

Mineral Oil Enema) (B)

polyethylene glycol (Colyte,

GoLYTLEY, Half-lytley, Miralax) (C)

min
g
o Bul
kfor
min
g
o Fec
al
soft
ene
r,
em
ollie
nt
o Em
ollie
nt
o Hyp
ero
sm

PO:
12-24
hr

PO: 13 days

PO: 68 hr

PO: 1
hr

gylcerin (Sani-Supp, Colace, Fleet

Babylax) (C)

lactulose (Enulose) (B)

Magnesium citrate, magnesium

sulfate (Epsom salt) (B)

o
o
o

otic
o Hyp
ero
sm
otic
o Hyp
ero
sm
otic,
disa
cch
arid
e
o

Sali
ne

PO:
16-36
min

PO:
24 hr

PO:
0.5-3
hr

o
o
o
o
o

Bulk-forming: OTC water retaining, total volume, normal formed stools,

action limited to GI tract, must be taken with A LOT of water, only safe long
term use
Emollient: lubricate stool, prevent water from escaping intestine, fecal
softener, do not cause BM just soften to ease passage. Contraindicated in
bowel obstruction, impaction nausea & vomiting
Hyperosmotic: increase water content of fecal matter. Results in distention,
peristalsis, & evacuation. Commonly used to treat constipation & evacuate
bowels before procedure

Lactulose: Lactulose is a synthetic derivative of the natural sugar lactose, which is not
digested in the stomach or absorbed in the small bowel. Instead it passes unchanged into
the large intestine, where it is metabolized. Colonic bacteria digest lactulose to produce
lactic acid, formic acid, and acetic acid, which creates a hyperosmotic environment that
draws water into the colon and produces a laxative effect. Also reduces ammonia serum
levels by converting it to water soluble ammonium. Contraindicated in patients on a
low-galactose die

o
o

Saline: Contain magnesium or sodium salts that osmotic pressure and

draw water into the colon, producing a watery stool, usually within 3 to 6
hours of ingestion

o
o
o
o

Stimulant: Stimulant laxatives induce intestinal peristalsis.

Irritable bowel syndrome (IBS) is a condition of chronic intestinal discomfort

characterized by cramps, diarrhea, and/or constipation.
Women are affected more often than men.
o Tegaserod (Zelnorm) is a serotonin 5-HT4 receptor agonist & is approved
for treatment of IBS with constipation & chronic idiopathic constipation in
women younger than 55 years of age for whom no alternative therapy exists.
Tegaserod has been associated with serious adverse events including angina,
heart attacks, and stroke.
Patients must be registered with the manufacturer.
It is categorized as a pregnancy category B drug
Dosed at 6 mg twice a day for 4 to 6 weeks.
o Lubiprostone (Amitiza) is a chloride channel activator that is indicated for
the treatment of chronic idiopathic constipation and IBS with constipation in
women 18 years of age and older.
It is dosed at 24 mcg twice a day for idiopathic constipation and 8 mcg twice a
day for IBS
most common adverse effects are nausea, diarrhea, and abdominal pain.
pregnancy category C drug

contraindicated in patients with known or suspected bowel obstruction.

o
o
o Treatment for IBS
o
psyllium is moderately effective in IBS
the antidiarrheal loperamide is not more effective than placebo at reducing pain
or bloating, but it is an effective agent for the treatment of diarrhea, reducing
stool frequency, and improving stool consistency
5-hydroxytryptamine 3 (5-HT3) receptor antagonist alosetron is more effective
than placebo
alosetron is most favorable in women with severe IBS and diarrhea who have not
responded to conventional therapies
5-hydroxytryptamine 4 (5-HT4) receptor agonist tegaserod and the chloride
channel activator lubiprostone are more effective than placebo
tricyclic antidepressants and selective serotonin reuptake inhibitors are more
effective than placebo at relieving IBS symptoms, and appear to reduce
abdominal pain.
o
o
o

o
o
o
o
o
o
o
o
o
o

Emesis: The forcible emptying or expulsion of gastric and, occasionally,

intestinal contents through the mouth; also called vomiting.
Nausea: Sensation often leading to the urge to vomit.
Antiemetic drugs: Drugs given to relieve nausea and vomiting

Vomiting center: The area of the brain that is involved in stimulating the

physiologic events that lead to nausea and vomiting.

o
o

Nausea and vomiting are two gastrointestinal (GI) disorders that can be extremely

unpleasant but also can lead to more serious complications if not treated promptly
o
o
o
o

o
o
o
o

Site in the vomiting pathway

Neurotransmitter
(Receptor)
Acetylcholine (ACh)

Histamine (H2)

o
o
o

Seratonin
Dopamine
Prostaglandins

o
o
o

VC in brain, vestibular & labyrinthine

inner ear
VC in brain, vestibular & labyrinthine
inner ear
GI Tract, CTZ, & VC in brain
GI Tract, CTZ in brain
GI Tract

o
o
o
o
o
o
o
o
o

o
o
o
o
o
o
o
o

Category

Antiem
etic
Drug

Anticholinerg
ic

scopola
mine

Antihistamin
es

dimenh
ydrinat
e,
diphen
hydram
ine,
meclizi

Indications

Motion sickness, secretion

before surgery, nausea &
vomiting
Motion sickness,
nonproductive cough,
sedation, rhinitis, allergy
symptoms, nausea &
vomiting

o
o

Antidopamin
ergics

o
o

Prokinetics
o

Serotonin
Blockers

Tetrahydroca
nnabinoids

ne
prochlo
rperazi
ne,
premth
azine,
droperi
dol
metocl
oprami
de
dolaste
ron,
granist
eron,
ondans
teron,
palonst
eron
Dronab
inol

Psychotic disorders
(mania, schizophrenia,
anxiety) intractable
hiccups, nausea vomiting

Delayed gastric emptying

gatroesophageal reflux,
nausea & vomiting

Nausea & vomiting

associated with
chemotheraphy & postoperative nausea &
vomiting

Nausea & vomiting

associated with chemo,

anorexia associated with

weigh loss in patients AIDS
& cancer
o

o
o
o
o

Category
Anticholinerg
ic
Antihistamin
es
Antidopamin
ergics

Prokinetics

Serotonin
Blockers
Tetrahydroca
nnabinoids

o
o
o
o
o

Mechanism of Action
Block ACh receptors in the vestubular nuclei &
reticular formation
Block H1 receptors, prevent ACH from binding

Block dopamine in CTZ & may also block ACh

Block dopamine in CTZ or stimulate ACh

receptors in GI tract
Block serotonin receptors in GI tract, CTZ & VC

o
o

o
o

Have inhibitor effect on reticular formation,

thalamus & cerebral cortex

o
o
o
o
o
o
o
o

Antinausea Drug Adverse Effects

o
o
o
o
o
o
o
o
o
o
o

Anticho
linergic
CNS
Cardio
Vascular
EENT
GU
INTEG
Antihist
amines:
CNS
EENT
GU

o
o
o

Dizziness, drowsiness, disorientation

Tachycardia

o
o
o
o

Blurred vision, dilated pupils, dry mouth

Difficult urination, constipation
Rash, erythema

o
o
o

Dizziness, drowsiness, confusion

Blurred vision, dilated pupils, dry mouth
Urinary retention

o
o
o
o
o
o
o
o
o
o

Antidop
aminerg
ics:
Cardiov
ascular
CNS
EENT
GU
GI
Prokine
tics:
Cardiov
ascular
CNS
GI

Orthostatic hypotension, tachycardia

o
o
o
o
o

Extrapyramidal symptoms, tardive dyskinesia, headache

Blurred vision, dry eyes
Urinary retention
Dry mouth, nausea & vomiting, anorexia, constipation

Hypotension, supraventricular tachycardia

o
o

Sedation, fatigue, restlessness, headache, dystonia

Dry mouth, nausea & vomiting & diarrhea

o
o
o
o
o

Serotonin
Blockers:
CNS
GI
Other

Antinausea Drugs:

o
o
o
o

Headache
Diarrhea
Rash, bronchospasm, prolonged QT interval

o
o
o
o
o
o
o
o
o
o
o
o
o
o
o
o
o
o

Tetrahydrocan
nabinoids:
CNS
EENT
GI

o
Drowsiness, dizziness, anxiety, confusion, euphoria
Visual disturbances
Dry mouth

o
o
o

o
o

Drug

R
o

Anticholinergic
o
O

Pea
k

E
li

o
D

Pla
sma
Con
cen
trati
on

u
t
e

scop
olami
ne
(Tran
sder
m-

T
r
a
n
s
d

m
i
n
a
ti
o
n
o
f
H
a
lf
li
f
e

o
1

6-8
hr

8
9
.
5
h

o
7

Scop,
Scop
ace)
o
o

mecli
zine
(Antiv
ert)

e
r
m
r
a
l
Antihistamine contraindication: shock & lactation
o

o
1

P
O
o

Proch
lorper
azine

Prom
ethaz
ine

I
M

I
M

Vari
abl
e

6
h
r

6
8
h
r
9
1
6
h

o
8-

Antidopaminergics:
o
3

o
2

2-4
hr

4.4
hr

o
3-

o
2-

r
o
o

Meto
clopr
amid
e
(Reg
alin)

Prokinetics:
o

o
2

P
O

12.5
hr

Onda
nsetr
on

o
1

I
V

o
o

Dron
abino
l

P
O

o
3-

Serotonin Blockers
o

2
.
5
6
h
r

11.5
hr

Tetrahydrocannabinoid
o
o 1-3
3
hr

3
.
5
5
h
r
1
9
-

o
6-

o
4-

3
6
h
r
o