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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 Active Passive
Artificial Type of
Immunizing
Drug
Toxoid or vaccine Immunoglobulin or antitoxin
Mechanism of
Action
Results from an antigen-antibody
response similar to that after
antigen exposure in the natural
disease process
Results from direct administration of exogenous
antibodies; antibody concentration will decrease
over time, so if exposure is expected it is wise to
continue passive immunizations
Use
To prevent development of active
disease in the event of exposure
to a given antigen in an
individuals who have at least a
partially functioning immune
system
To provide temporary protection against disease in
individuals who are immunodeficient, those for
whom active immunization is contraindicated, and
those who have been exposed to or anticipate
exposure to the organism or toxin; an antibody
response is not stimulated in the host
Natural
Mechanism of
Action
Mechanism of action. Protection
of owns antibodies during actual
infection.
Transmission from mother to infant through placenta
or during breast feeding.
Passive Immunization Drugs:
Hepatitis B
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 Adverse Effect:
Minor: CNS Fever, adenopathy
Minor: INTEGMinor rash, soreness at injection site,
urticarial, arthritis
Severe: CNS
Fever > 103 F encephalitis, peripheral
neuropathy, anaphylactic rxn, shock,
unconsciousness
Severe: INTEG Rash
Severe: RESP Dyspnea
Severe: Other Cyanosis
Drug (Pregnancy
Category)Pharm Class Indications/Uses
Active
TDaP Vaccine Mixed toxoid/vaccineProphylaxis against diphtheria,
tetanus, & pertussis
Hepatitis B Vaccine (C) Viral surface antigen vaccine Hepatitis B prophylaxis
Influenza Virus Vaccine
(C) Viral surface antigen vaccine Influenza prophylaxis
Pneumococcal vaccine,
polyvalent (C)
Bacterial capsular antigenic
extract vaccine
Streptococcus pnuemoniae
prophylaxis
Varicella Virus Vaccine
(C) Live, attenuated viral vaccine
Prophylaxis against varicella
virus (causes chickenpox &
shingles)
Drug (Pregnancy Category) Pharm Class Indication/Uses
Passive
Hepatitis B ImmunoglobulinPooled human
immunoglobulin
Passive Hepatitis B
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 Reye’s 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
Doesn’t 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 – Reye’s 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 can’t give it for non FDA approved due to
shortage.
FDA Approved Uses:
o Pediatric HIV infection
o B-cell chronic lymphocytic
leukemia
o Bone marrow transplant
o Hepatitis A
o Idiopathic thrombocytopenic
purpura
o Kawasaki disease
o Immunoglobulin deficiencies
o Measles
o Primary Immunodeficiency
Disease
o Rubella
o 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
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
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
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
Active: don’t 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
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: don’t 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
Don’t rush your baby’s 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.
Labs:
WBC ↑ indicates infection
WBC ↓ infection is going ↓
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.
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
Deep pain: Pain that occurs in tissues below skin level; opposite of superficial pain
Central pain: Pain resulting from any disorder that causes central nervous system
damage.
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.
Opioid analgesics: Synthetic drugs that bind to opiate receptors to relieve pain.
Opioid naïve: Describes patients who are receiving opioid analgesics for the first time and
who therefore are not accustomed to their effects.
Opioid 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).
Opioid tolerant: The opposite of opioid naïve; 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.
Opioid 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.
Type of Pain Onset Duration Examples
Acute Sudden (minutes to hours)
usually sharp localized
physiological response
(SNS: tachycardia,
sweating, pallor, ↑ BP
Limited (has an end) MI, appendicitis,
dental procedures,
kidney stones,
surgical procedures
Chronic Slow (days to months) long
duration, dull, persistent,
aching
Persistent, recurring
(endless)
Arthritis, cancer, low
back pain, peripheral
neuropathy
SNS: Sympathetic Nervous System
The 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.
Gate Theory:
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 adjuvantsStep 3: Use of opioids for moderate or severe pain with or without nonopioids or adjuvants
7-10
4-6
1-3
OPIOIDS
Action Type ContraindicationsTeaching
NeedsOverdose Treatment
Very strong pain reliever
alleviate moderate to severe pain
Cough suppressant
Agonist – binds to pain receptor in brain
Agonist-antagonist – binds to pain receptor & causes a weaker pain response than a full agonist
Antagonist (nonanalgesic) binds to receptor doesn’t relieve pain – competes
Known drug allergySevere asthma Exercise caution:Respiratory insufficiency, Elevated intracranial pressure, morbid obesity, sleep apnea, myasthenia gravis, paralytic ileus, pregnancy *Especially with long term use or high dose
Fentanyl patch – no heating pads, proper disposal, only for opioid tolerant pt, keep away from children, do not store in warm damn places
naloxone (Narcan) given IV
naltrexone (ReVia)given PO
Used to manage overdose & addiction
Side Effects of Opioid Preventative MeasuresConstipation ↑ fluids, stool softener Nausea & Vomiting – ↓ GI peristalsis, stimulate vomiting in CNS.
Antiemetic medication
Sedation & Mental Clouding – change in mental status
Persistent drug-related sedation may be managed with decrease in dose or change in opioid drug. CNS stimulants can be ordered too
Respiratory Depression May be reversed with Naloxone and without analgesia reversal
Dry Mouth Suckers, artificial saliva drops, Pruritus – itching Diphenhydramine (Benadryl) Dysphoria or Euphoria Ongoing assessment Sleep disturbanceSexual DysfunctionAntidiuretic hormone secretion
Opioid Drugs:
Chemical Category Opioid DrugsMeperidine-like drugs Meperidine, *fentanyl, remifentanil, sufentanil, alfentanil Methadone-like drugs Methadone (treatment of detox in addicts)
Morphine-like drugsMorphine, heroin, hydromorphone, oxymorphone, levorphanol, codeine, hydrocodone, oxycodone
Other 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
Body System Opioid Induced Adverse Effect
Cardiovascular *Hypotension, flushing, bradycardia (
CNS Sedation, disorientation, euphoria, lightheadedness, dysphoria
GI Nausea, vomiting, constipation, biliary tract spasm
GenitourinaryUrinary retention (↑ in bladder tone – give low dose of opioid agonist or opioid agonist-antagonist)
INTEG *Itching, rash, wheal formation
Respiratory Respiratory depression possible & aggravation of asthma
*caused by release of histamine which causes vasodilation
Opioid Agonist Reversal DrugsGeneric Name Trade Name Adverse Effects
Naloxone (IV) Narcan↓↑ BP dysrhythmias, pulmonary edema, withdrawal
Naltrexone (PO) ReViaNervousness, headache, nausea, vomiting, pulmonary edema, withdrawal
Where x = amount of desired opioid in 24 hours and EA = equianalgesic dose obtained from the table above
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?
Step 1: Determine the 24-hour amount of oxycodone taken by this patient:80 mg × 2 doses per 24 hours = 160 mg per 24 hoursStep 2: Using the conversion table above, find the equianalgesic (EA) doses of oxycodone and parenteral morphine:15 mg oxycodone = 10 mg parenteral morphineStep 3: Use the above equation and solve for x by cross-multiplying:Where x = amount of parenteral morphine in 24 hours (solve by cross-multiplying)
Opioid Agonist
Drug RouteOnset of Action
Peak Plasma Concentration
Elimination of Half-life
Duration of Action
Morphine Sulfate
IM Rapid 30-60 mi 1.7-4.5 hr 6-7 hr
Codeine Sulfate
PO15-30 min
34-45 min 2.5-4 hr 4-6 hr
Fentanyl IV
TransdermalPO
Rapid12-24 hr5-15 min
Minutes48-72 hr
20-30 min
1.5-6 hrDelayed5-15 hr
30-60 min 13-40 hrUnknown
Meperidine HCl
IM Rapid 30-60 min 3-5 hr 2-4 hour
Methadone HCl
PO30-60 min
1.5-2 hr 25 hr 22-48 hr
Oxycodone HCl
PO10-15 min
1 hr 2-3 hr 3-6 hr
Opioid Agonist-Antagonist (exert no action or limited action)Generic buprenorphin
ebutorph
anolnabuphine pentazocine
Trade Buprenex Stadol Nubain Talwin Opioid Antagonist
Naloxone HCl
IV < 2 min Rapid 64 min 0.5-2 hr
Naltrexone HCl
PORapid 1 hr 4-13 hr 24-72 hr
Nonopioids Acetaminophen
PO 15-30 min
0.5-2 hr 1-4 hr 3-4 hr
Acetaminophen (Nonopioid)
Action Side EffectsOverdose & Treatment
Limitation on daily amount
Blocks peripheral pain impulses by inhibition of prostaglandin synthesis (mild to moderate pain)
Lowers febrile body temp by acting on the hypothalamus – heat is dissipated by vasodilation & ↑ in peripheral blood flow
Lacks anti-inflammatory effects
Rash, nausea vomiting
Much less common but more severe: blood disorders, dyscrasias, nephrotoxicity, most concern is for hepatotoxicity
Alcohol interaction ↑ liver toxicity
Acetylcysteine is the recommended antidote for acetaminophen toxicity and works by preventing the hepatotoxic metabolites of acetaminophen from forming.Most effective if given within 10 hrs. Bad tasting with an odor of rotten eggs, and vomiting of an oral dose is common. It is recommended that the dose be repeated if vomiting occurs within 1 hour of dosing. IV formation is now available
Contraindication: known allergy, severe liver disease, genetic disease G6PD
Large amounts can cause hepatotoxicity
4000 mg limit per day 2000 mg for older adults or pt with liver dysfunction
FDA announced: max 325 mg of acetaminophen and max dose of 3000 mg/day
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 acid-related disorders.
Pepsin: An enzyme in the stomach that breaks down proteins.
Antacids H2 Blockers PPI
Actions
used to neutralize stomach acid, They do not prevent the overproduction of acid help neutralize acid secretions.
↓ hydrogen ion secretion from parietal cells, results ↑ of pH in stomach &relief of symptoms associated with hyperacidity
bind directly to the hydrogen-potassium-ATPase pump mechanism & irreversibly inhibit the action of this enzyme, = total blockage of hydrogen ion secretion from the parietal cells.
Indications
antiulcer treatment, antiflatulent, acute relief of symptoms associated with peptic ulcer, gastritis, gastric hyperacidity, and heartburn.
GERD, peptic ulcer disease, & erosive esophagitis; adjunct therapy in the control of upper GI tract bleeding;& pathologic gastric hypersecretory conditions such as Zollinger-Ellison syndrome
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 Zollinger-Ellison syndrome.
Side (Adverse) Effects
calcium antacids may lead to the development of kidney stones and increased gastric acid secretion, so they are not used as frequently as other antacids, milk of magnesia antacid may cause diarrhea, rebound hyperacidity when antacids are discontinued
Rare: but - confusion and disorientation, induce impotence and gynecomastia, may increase the secretion of prolactin from the anterior pituitary gland, thrombocytopenia
long-term users of PPIs to develop osteoporosis, Cdif infections; risk of wrist, hip, &spine fractures; & pneumonia, ↓ of magnesium
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.
Drug Action Side Effects Indications ContraindicationAntacidsAlumninum, magnesium, calcium or sodium
Neutralize stomach acid. Do not prevent production of acid
Calcium may lead to kidney stones Milk of magnesia can cause diarrhea, excessive use can cause systemic alkalosis (basic) hyperacidity when calcium containing antacid is stopped
Acute relief of symptoms associated with peptic ulcer, gastritis, hyperacidity, & heartburn
Magnesium must be avoided in pt with renal failure Electrolyte disturbances, GI obstruction
Teaching Needs
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.
Interactions 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
Drug & Pregnancy Category
Pharm Class Usual Dosage Range
Indication
Aluminum Hydroxide (Amphojel) (A)
Aluminum containing antacid
Adult: PO 600-1500 mg 3-6xday
Hyperacidity
Aluminum Hydroxide & Magnesium (Maalox, Mylanta) (A)
Combination antacid
Adult: PO 400-2400 mg 3-6xday
Hyperacidity
Calcium Carbonate (Tums) (A)
Calcium containing antacid
Adult: PO 0.5-1.5 g prn
Hyperacidity
Magnesium Hydroxide (Milk of Magnesia) (A)
Magnesium containing antacid
Adult: PO 0.65-1.3 g prn up to 4xday
Hyperacidity (More common use – laxative)
Magnesium Salts Aluminum Salts Calcium Salts Sodium SaltsCarbonate: Gaviscon Liquid, Gaviscon Extra Strength Relief Formula Tablets
Carbonate: Basaljel
Carbonate: Tums, Maalox, Mylanta, Di-Gel
Bicarbonate: Alka-seltzer,
Hydroxide: milk of magnesia
Hydroxide: AlternaGEL, Amphojel
Citrate: Citra pH
Oxide: Mag-ox (used as magnesium supplement Trisilicate: Gaviscon tablets
Increase pH = more basic
Drug Action Side Effects Indication ContraindicationsH2 ReceptorsOTC
↑ pH of the stomach & relieve Sx linked to hyperacidity
Protypical acid secretion antagonist. ↓ but don’t totally abolish acid secretion competitively block the H2 receptor of acid-producing parietal cells, parietal cell less responsive histamine & stimulation of ACh & gastrin Up to 90% inhibition of vagal- and gastrin-stimulated acid secretion occurs when histamine is blocked
Rare: ,3% of cases ↓ BP (w/ IV admin) headache, lethargy, confusion, depression, halluicination, surred speech, agitation, increased prolactin secretion, gynecomastia (cimetidine) diarrhea, abd cramps, impotence, ↑ BUN & creatinine levels ↑ liver enzyme levels, jaundice, thrombocytopenia, rash, alopecia, sweating, flushing,
Treatment of GERD, peptic ulcer disease, erosive esophagitis, included to control upper GI bleeding, pathological gastric hyersecretory conditions (Zollinger-Ellsion syndrome)Stress ulcer prophylaxis
Known drug allergy
Liver/kidney dysfunction may warrant dose adjustment
Teaching
NeedsInteractions Cimetidine ↑ risk of interaction than other 3 especially in elderly smoking ↓ effectiveness, ↓
absorption of drugs that need acidic environment
H2 Receptor Drugs
Drug RouteOnset of Action
Peak Plasma Concentration
Elimination of Half-life
Duration of Action
cimetidine (Tagamet)
PO 15-60 min 1-2 hr 2 hr 4-5 hr
ranitidine(Zantac)
POIV
1 hrImmediate
2-4 hr< 15 min
2-3 hr 2-3hr
4-12 hr4-12 hr
famotidine (Pepcid)
POIV
1.4 hrImmediate
3 hr< 15 min
2.6-4 hr2.6-4 hr
9-12hr9-12hr
nizatidine
Drug Action Side Effect Indication Contraindication Proton Pump Inhibitors PPI
PPIs bind irreversibly to the proton pump. This inhibition prevents the movement of hydrogen ions out of the parietal cell into the stomach & blocks all gastric acid secretion. Given orally or thru NG tube & IV use
PPI stop 90%+ acid secretion which could make pt temporarily achlorhydric (without acid)
Long term use & development of osteoporosis, Cdif
Erosive esophagitis, symptomatic GERD that doesn’t respond to H2 Recepotr Agonist, Short term treatment of active duodenal ulcers, active benign gastric ulcers, hypersecretory conditions, NSAID induced ulcers, & stress ulcer prophylaxis. Used with antibiotics to treat H. Pylori infections
Known drug allergy
Teaching Usually work best if taken 30-60 minutes before food
NeedsInteractions 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
Proton Pump Inhibitor Drugs
Drug RouteOnset of Action
Peak Plasma Concentration
Elimination of Half-life
Duration of Action
omeprazole (Prilosec)
PO 2 hr 5 days 0.5-1 hr 1-5 days
lansoprazole (Prevacid)
PO 1.7 hr 4 wk 1-2 hour 24 hour
pantoprazole (Protonix)
PO IV
2.5 hrEnd of
infusion
2-2.5 hrEnd of
infusion
1 hr1 hf
7 days7 days
DOSAGESlansoprazole / Prevacid Pregnancy Category B
Adult: PO 30 mg dailyGERD, ulcer, erosive esophagitis
omeprazole / Prilosec Pregnancy Category C
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
Esophagitis, duodenal ulcer
Hypersecretory conditions
mg PO tidpantroprazole / ProtonixPregnancy Category B
PO/IV: 20-80 mg/day depending on indication
GERD, ulcer, stress ulcer prophylaxis
MISC Acid Controlling Drugs
Drug RouteOnset
of Action
Peak Plasma Concentration
Elimination of Half-life
Duration of Action
Use
misoprostol / Cytotec
PO 30 min 12 min 20-40 min 1-2 days
↓ NSAID induced gastric ulcers
simethicone / Mylicon
Use: ↓ the discomfort of gastric / intestinal gas
Sucralfate / Carafate
Use: Mucosal protectant in treatment of active stress ulceration & in LTC for peptic ulcers
Nursing ProcessAssessment
Nursing Diagnosis Goal Outcome Implementation:
Know GI hx, aluminum & magnesium = know full list of other meds Pay attn. to hepatic function
Constipation related to the adverse effects of aluminum-containing antacids and other drugs used to treat hyperacidity Diarrhea related to the adverse effects of magnesium-containing antacids and other drugs used to treat hyperacidity Deficient knowledge related to lack of information about antacids, H2 receptor antagonists, or PPIs,
Minimal diarrhea or constipation
Patient demonstrates adequate knowledge about use of drug
Pt states measures to help prevent constipation & diarrhea
Patient states purpose of taking antacids, H2 receptor agonists, & PPI
Chew tab completely, shake liquids before taken, Antacids must be taken with 8 oz water
including their use and potential adverse effects
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).• 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 infection–peptic 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
AdsorbentsActivated charcoal, aluminum hydroxide, bismuth subsalicylate, cholestyramine, polycarbophil
Anticholinergics (antimotility) Atropine, hyoscyamine
Opiates (antimotility) Opium tincture, paregoric, codeine, diphenoxylate, loperamide
Probiotics & intestinal flora modifiersLactobacillus acidophilus, lactobacillus GG, saccharomyces boulardii
Antidiarrheal DrugsDrug Action Side Effects Indications Contraindications
AnticholinergicSlow peristalsis
See adverse effects table
More severe
Drug allergy, acute GI condition (obstruction or colitis)
Opiates↓ bowl motility, ↓ pain of rectal spasms
See adverse effects table
More severe
Drug allergy, acute GI condition (obstruction or colitis)
Probiotics
Replenish bacteria to fight diarrhea causing bacteria
See adverse effects table
Antibiotic induced diarrhea
Drug allergy, acute GI condition (obstruction or colitis)
Adsorbents ↓ effectiveness by ↓ absorption of many drugs
The therapeutic effects of the anticholinergic can be ↓ by coadministration with antacids.
Drug Adverse Effects
Bismuth subsalicylateIncreased bleeding time, constipation, dark stool, confusion, tinnitus, metallic taste, blue gums
Atropine, hyoscyamine Urinary retention, impotence, headache, dizziness, anxiety, drowsiness, bradycardia, hypotension, dry skin, flushing, blurred vision
Codeine, diphenoxylateDrowsiness, dizziness, lethargy, nausea, vomiting, constipation, hypotension, urinary retention, flushing, respiratory depression
Adsorbents Drug Uses Side Effects Contraindications
Bismuth subsalicylate OTC – PO
caution pt recovering from chickenpox or flu due to risk of Reye’s Syndrome, adverse effects associated with aspirin based products. Harmless: dark tongue & stool
Anticholinergic
Belladonna alkaloid combinations
Hypersensitivity to anticholinergic, narrow angle glaucoma, GI obstruction, myasthenia gravis, paralytic ileus, toxic megacolon
OpiatesDrug Uses Side Effects ContraindicationsCodeine Rx - antidiarrheal
Diphenoxylate with atropine
Rx – antidiarrheal inhibits motility & excessive GI propulsion
Dry mouth, abd pain, tachycardia blurred vision if taken in extreme amount
Loperamide
OTC – antidiarrheal inhibits peristalsis & intestinal secretions
Ulcerative colitis, pseudomembranous colitis & acute diarrhea from E-coli
Paregoric Rx - antidiarrhealMedication error death – use = rare
Tincture of opium Rx - antidiarrheal Medication error death – use = rare
ProbioticsDrug Uses Side effects ContraindicationsLactobacillus acidophilus
Suppress growth of pathogenic bacteria improve intestinal barrier function, modulation of immune system & pain perception
Lactobacillus GG
Cause of Constipation ExampleAdverse Drug Effect Analgesics, anticholinergics, iron supplements,
aluminum & calcium antacids, opiates, calcium channel blockers
Lifestyle Poor BM habits, voluntary refusal Diet: poor fluid intake, low fiber, excessive dairyPhysical inactivity, lack of exercise, elderly Psychological factors, anxiety, stress, hypochondria
Metabolic/Endocrine disorder Diabetes mellitus, hypothyroidism, pregnancy, hypercalcemia, hypokalemia
Neurogenic disorder Autonomic neuropathy, intestinal pseudo-obstruction, MS, spinal cord lesions, Parkinson’s, stroke
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
Category Laxative Drug Bulk-forming Psyllium, methylcelluloseEmollient Docusate salts, mineral oilHyperosmotic Polyethylene glycol, lactulose, sorbitol, glycerin Saline Magnesium hydroxide, magnesium sulfate, magnesium citrate Stimulant 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
Drug Effect Bulk Emollient Hyperosmotic Saline
Stimulant
Increase peristalsis Y Y Y Y Y↑ secretion of water & electrolytes in SB
Y Y N Y Y
Inhibits absorption H2O in SB↑ permeability in SB Y Y N Y YActs only in large bowel N Y N N Y↑ water in fecal mass Y Y Y Y YSoftens fecal bass Y Y Y Y Y
Category Indication Bulk-forming Acute & chronic constipation IBS, diverticulosis Emollient Acute & chronic constipation, fecal impaction, anorectal conditions
requiring facilitation of BMHyperosmotic Chronic constipation, bowel prep for diagnostic & surg proceduresSaline Constipation, bowel prep for diagnostic & surgical proceduresStimulant Acute constipation, bowel prep for diagnostic & surg procedures
The following are some of the more common uses of laxatives:
•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.
Category Adverse EffectsBulk-forming Impaction above strictures, fluid disturbance, electrolyte imbalance,
gas formation, esophageal blockages, allergic reactionEmollient Skin rashes, decreased absorption of vitamins, lipid pneumonia,
electrolyte imbalanceHyperosmotic Abdominal bloating, electrolyte imbalance, rectal irritation Saline Magnesium toxicity (with renal insufficiency) electrolyte imbalance,
cramping, diarrhea, increase thirst Stimulant Nutrient malabsorption, skin rashes, gastric irritation, electrolyte
imbalance, discoloration in urine, rectal irritation
Drug & Pregnancy Category Type Onset of Action
bisacodyl (Dulcolax) (C) StimulantPO: 6-12 hr Rectal: 15-60 min
senna (Senokot, others) (c) Stimlant-irritant PO: 6-24 hours Psyllium (Metamucil, Fiberall,)(B) Bulk-forming PO: 12-24 hrMethylcellulose (Citrucel) (B) Bulk-forming PO: 12-24 hr
docusate sodium (Colace) docusate calcium (Surfak) (C)
Fecal softener, emollient
PO: 1-3 days
mineral oil (Kondremul Plain, Fleet Mineral Oil Enema) (B)
Emollient PO: 6-8 hr
polyethylene glycol (Colyte, GoLYTLEY, Half-lytley, Miralax) (C)
Hyperosmotic PO: 1 hr
gylcerin (Sani-Supp, Colace, Fleet Babylax) (C) Hyperosmotic PO: 16-36 min
lactulose (Enulose) (B)Hyperosmotic, disaccharide
PO: 24 hr
Magnesium citrate, magnesium sulfate (Epsom salt) (B)
Saline PO: 0.5-3 hr
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
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
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.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.
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.
Treatment for IBS
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.
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.
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
Neurotransmitter (Receptor) Site in the vomiting pathway Acetylcholine (ACh) VC in brain, vestibular & labyrinthine inner ear Histamine (H2) VC in brain, vestibular & labyrinthine inner ear Seratonin GI Tract, CTZ, & VC in brain Dopamine GI Tract, CTZ in brain
Prostaglandins GI Tract
Category Antiemetic Drug Indications
Anticholinergic scopolamineMotion sickness, secretion ↓ before surgery, nausea & vomiting
Antihistamines dimenhydrinate, Motion sickness, nonproductive
diphenhydramine, meclizine
cough, sedation, rhinitis, allergy symptoms, nausea & vomiting
Antidopaminergicsprochlorperazine, premthazine, droperidol
Psychotic disorders (mania, schizophrenia, anxiety) intractable hiccups, nausea vomiting
Prokinetics metoclopramideDelayed gastric emptying gatroesophageal reflux, nausea & vomiting
Serotonin Blockers
dolasteron, granisteron, ondansteron, palonsteron
Nausea & vomiting associated with chemotheraphy & post-operative nausea & vomiting
Tetrahydrocannabinoids DronabinolNausea & vomiting associated with chemo, anorexia associated with weigh loss in patients AIDS & cancer
Category Mechanism of Action
AnticholinergicBlock ACh receptors in the vestubular nuclei & reticular formation
Antihistamines Block H1 receptors, prevent ACH from binding Antidopaminergics Block dopamine in CTZ & may also block ACh
ProkineticsBlock dopamine in CTZ or stimulate ACh receptors in GI tract
Serotonin Blockers Block serotonin receptors in GI tract, CTZ & VC
TetrahydrocannabinoidsHave inhibitor effect on reticular formation, thalamus & cerebral cortex
Antinausea Drug Adverse EffectsAnticholinergicCNS Dizziness, drowsiness, disorientationCardio Vascular TachycardiaEENT Blurred vision, dilated pupils, dry mouth
GU Difficult urination, constipation INTEG Rash, erythema Antihistamines:CNS Dizziness, drowsiness, confusion EENT Blurred vision, dilated pupils, dry mouthGU Urinary retention Antidopaminergics:Cardiovascular Orthostatic hypotension, tachycardia CNS Extrapyramidal symptoms, tardive dyskinesia, headache EENT Blurred vision, dry eyes GU Urinary retention GI Dry mouth, nausea & vomiting, anorexia, constipation Prokinetics:Cardiovascular Hypotension, supraventricular tachycardiaCNS Sedation, fatigue, restlessness, headache, dystoniaGI Dry mouth, nausea & vomiting & diarrhea
Antinausea Drugs:Serotonin Blockers:CNS Headache GI Diarrhea
Other Rash, bronchospasm, prolonged QT interval Tetrahydrocannabinoids:CNS Drowsiness, dizziness, anxiety, confusion, euphoriaEENT Visual disturbances GI Dry mouth
Anticholinergic
Drug RouteOnset of Action
Peak Plasma Concentration
Elimination of Half-life
Duration of Action
scopolamine Transdermal 1-2 hr 6-8 hr 8-9.5 hr 72 hr
(Transderm-Scop, Scopace)
Antihistamine – contraindication: shock & lactation meclizine (Antivert)
PO 1 hr Variable 6 hr 8-24 hr
Antidopaminergics:
Prochlorperazine IM30-40 min
2-4 hr 6-8 hr 3-4 hr
Promethazine IM 20 min 4.4 hr 9-16 hr 2-6 hr Prokinetics:
Metoclopramide (Regalin)
PO20-60 min
1-2.5 hr 2.5-6 hr 3-4 hr
Serotonin Blockers
Ondansetron IV15-30 min
1-1.5 hr 3.5-5 hr 6-12 hr
TetrahydrocannabinoidDronabinol PO 30-60 m 1-3 hr 19-36 hr 4-6 hr
