1 Chemotherapeutic Agents Lecture Part 1

Notre Dame of Marbel University
College of Arts and Sciences

Nursing Department
NCM-N-106
PHARMACOLOGY
CHEMOTHERAPEUTIC
AGENTS
Nursing Department
INTENDED LEARNING OUTCOMES:

1. Identify the different actions of each drug class under the Chemotherapeutic drugs
2. Identify the common side effects of each drug class.
3. Explain the effects of each drug class.
4. Describe nursing interventions to maximize therapeutic effects and minimize
adverse effects for each drug class.
5. Relate key points for patient and family education for each drug class
Nursing Department
INTRODUCTION
Chemotherapeutic drugs are used to destroy both organisms that invade
the body (e.g., bacteria, viruses, parasites, protozoa, fungi) and abnormal
cells within the body (e.g., neoplasms, cancers).
These drugs affect cells by altering cellular function or disrupting cellular

integrity, causing cell death, or by preventing cellular reproduction,
eventually leading to cell death.
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I. THE CELL
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I. THE CELL
the basic structural unit of the body.
The cells that make up living organisms, which are
arranged into tissues and organs, all have the same
basic structure.
Each cell has a nucleus, a cell membrane, and
cytoplasm, which contains a variety of organelles
Nursing Department
I. THE CELL
A. NUCLEUS
contains all genetic material necessary for cell reproduction
and for the regulation of cellular production of proteins.
It contains a spherical mass called nucleolus.
Within this mass are dense fibers and proteins that will
eventually become ribosomes, the sites of protein synthesis.
Nursing Department
I. THE CELL
B. CELL MEMBRANE
essential for cellular integrity and is equipped with many
mechanisms for maintaining cell homeostasis.
a lipoprotein structure, mainly composed of proteins and
lipids— phospholipids, glycolipids, and cholesterol; the
bipolar arrangement of the lipids monitors substances
passing in and out of the cell.
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I. THE CELL
D. MITOCHONDRIA
“power plants” within each cell that produce energy in

the form of ATP,which allows the cell to function.
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I. THE CELL
F. LYSOSOMES
membrane-covered organelles that contain specific
digestive enzymes that can break down proteins, nucleic
acids, carbohydrates, and lipids.
are responsible for digesting worn or damaged sections
of a cell when the membrane ruptures and the cell dies.
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II. ANTI-INFECTIVE
AGENTS
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II. ANTI-INFECTIVE AGENTS

designed to target foreign organisms that have
invaded and infected the body.
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THERAPEUTIC ACTION:
interfere with biosynthesis of the pathogen cell wall.
interfere with the steps involved in protein and DNA synthesis,
functions necessary to maintain the cell and allow for cell division.
alter the permeability of the cell membrane to allow essential cellular
components to leak out
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ANTI-INFECTIVE ACTIVITY:
Bactericidal - active against the infective microorganisms
that they actually cause the death of the cells they affect.
Bacteriostatic -not as aggressive; they interfere with the

ability of the cells to reproduce or divide.
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HUMAN IMMUNE RESPONSE:
a complex interaction among chemical mediators, leukocytes, lymphocytes,
antibodies, and locally released enzymes and chemicals.
It is difficult to treat any infections for two reasons:

1. Anti-infective drugs cannot totally eliminate the pathogen without causing
severe toxicity in the host,
2. Patients do not have the immune response in place to deal with even a few
invading organisms.
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RESISTANCE:
refers to the ability over time to adapt to an anti-infective drug
and produce cells that are no longer affected by a particular
drug.
can be natural or acquired
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ACQUIRING RESISTANCE:
1. Producing an enzyme that deactivates the antimicrobial drug
2. Changing cellular permeability to prevent the drug from entering the cell
or altering transport systems.
3. Altering binding sites on the membranes which then no longer accept.
4. Producing a chemical that acts as an antagonist to the drug.
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PURPOSE:
For Treatment of Systemic Infections.
identification of the correct pathogen and selection of a drug
(sensitivity)
Combination Therapy - synergistic, which means that they are more
powerful when given in combination.
Prophylaxis - to prevent infections before they occur.
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III. ANTIBIOTICS
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A. AMINOGLYCOSIDES
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A. AMINOGLYCOSIDES
Therapeutic Actions and Indications
Bactericidal.
Inhibit protein synthesis
used to treat serious infections caused by susceptible strains of gram
negative bacteria, including Pseudomonas aeruginosa, E. coli, Proteus
species, the Klebsiella–Enterobacter– Serratia group, Citrobacter species, and
Staphylococcus.
Nursing Department
A. AMINOGLYCOSIDES
PHARMAKOKINETICS
poorly absorbed from the GI tract but rapidly absorbed after
intramuscular (IM) injection.
widely distributed throughout the body, cross the placenta and
enter breast milk, and are excreted unchanged in the urine
Nursing Department
A. AMINOGLYCOSIDES
CONTRAINDICATIONS/ CAUTIONS:
Allergy
Hepatic disease
Renal disease
Preexisting Hear loss
Herpes/ Mycobacterial Infection
myasthenia gravis or parkinsonism
Lactation
Nursing Department
A. AMINOGLYCOSIDES
ADVERSE EFFECTS:
Black box warning alerting health care professionals to the serious risk of:
ototoxicity and nephrotoxicity.
GI effects include nausea, vomiting, diarrhea, weight loss, stomatitis, and hepatic
toxicity.
Cardiac effects can include palpitations, hypotension, and hypertension
Hypersensitivity reactions include purpura, rash, urticaria, and exfoliative
dermatitis.
Nursing Department
A. AMINOGLYCOSIDES
NURSING IMPLEMENTATION:
Assessment: History and Examination, culture and sensitivity reports
Record baseline vital signs
Observe for :
OTOTOXICITY
NEPHROTOXICITY
Ensure complete course of the antibiotics as ordered.
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B. CARBAPENEMS
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B. CARBAPENEMS
are a relatively new class of broad-spectrum antibiotics
Meropenem - First drug of Class.
Bactericidal
used to treat serious infections caused by susceptible strains of S. pneumoniae,
Haemophilus infl uenzae, Moraxella catarrhalis, S. aureus, Streptococcus
pyogenes, E. coli and others.
indicated for treating serious intra-abdominal, urinary tract, skin and skin
structure, bone and joint, and gynecological infect
Nursing Department
B. CARBAPENEMS
PHARMAKOKINETICS
Rapidly absorbed if given IM
They are widely distributed throughout the body, although it is
not known whether they cross the placenta or enter breast milk.
excreted unchanged in the urine
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B. CARBAPENEMS
allergy to any of the carbanems or beta-lactams
seizure disorders
meningitis
lactation
Use caution during pregnancy
Ertapenem is not recommended for use in patients younger than
18 years of age.
Nursing Department
B. CARBAPENEMS
ADVERSE EFFECTS:
GI tract can limit the use of carbapenems in some patients.
Pseudomembranous colitis, Clostridium difficile diarrhea
nausea and vomiting can lead to serious dehydration and
electrolyte imbalances.
Superinfections can occur with any of the carbapenems.
CNS effects can include headache, dizziness, and altered mental
state.
Seizures
Nursing Department
B. CARBAPENEMS
Ensure that the patient receives a full course.
Monitor the patient regularly for signs of:
pseudomembranous colitis
severe diarrhea,
superinfections
confusion and seizures
phlebitis
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C. CEPHALOSPORINS
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C. CEPHALOSPORINS
Bactericidal and Bacteriostatic.

basically interfere with the cell wall–building ability of
bacteria when they divide.
It is important to reserve cephalosporins for appropriate
situations because cephalosporin-resistant bacteria are
appearing in increasing numbers
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C. CEPHALOSPORINS
First-generation cephalosporins are largely effective against the same gram-positive bacteria that are affected by
penicillin G, as well as the gram-negative bacteria P. mirabilis, E. coli, and K. pneumoniae (use the letters PEcK as a
mnemonic.
Second-generation cephalosporins are effective against the previously mentioned strains, as well as H. influenzae,
Enterobacter aerogenes, and Neisseria species (remember HENPeCK)
Third-generation cephalosporins, which are effeCtive against all of the previously mentioned strains relatively weak
against gram-positive bacteria but are more potent against the gram-negative bacilli, as well as against Serratia
marcescens (remember HENPeCKS).
Fourth-generation cephalosporins are in development. The first drug of this group, cefepime (Maxipime), is active
against gram-negative and gram-positive organisms, including cephalosporin-resistant staphylococci and P.
aeruginosa.
FIRST-GENERATION CEPHALOSPORINS
SECOND-GENERATION CEPHALOSPORINS
THIRD-GENERATION CEPHALOSPORINS
THIRD-GENERATION CEPHALOSPORINS
FOURTH-GENERATION CEPHALOSPORINS
Nursing Department
C. CEPHALOSPORINS
PHARMAKOKINETICS
are well absorbed from the GI tract

others are absorbed well after IM injection or IV administration
are primarily metabolized in the liver and excreted in the urine.
These drugs cross the placenta and enter breast milk.
Nursing Department
C. CEPHALOSPORINS
allergies to cephalosporins or penicillins

Use with caution in patients with hepatic or renal impairment
use with caution in pregnant or lactating patients
Nursing Department
C. CEPHALOSPORINS
ADVERSE EFFECTS:
GI tract and include nausea, vomiting, diarrhea, anorexia, abdominal pain, and
flatulence. Pseudomembranous colitis
CNS symptoms include headache, dizziness, lethargy, and paresthesias.
Nephrotoxicity
Hepatotoxicity
Superinfection
Nursing Department
C. CEPHALOSPORINS
Monitor the patient regularly for signs:
Nephrotoxicity
Hepatotoxicity
Superinfection
Diarrhea
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D. FLUOROQUINOLONES
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D. FLUOROQUINOLONES
They interfere with the action of DNA enzymes necessary

for the growth and reproduction of the bacteria.
are indicated for treating infections caused by
susceptible strains of gram-negative bacteria, including
E. coli, P. mirabilis, K. pneumoniae, etc.
Nursing Department
. FLUOROQUINOLONES
PHARMAKOKINETICS
are absorbed from the GI tract, metabolized in the liver, and

excreted in the urine and feces.
drugs are widely distributed in the body and cross the placenta
and enter breast milk
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D. FLUOROQUINOLONES
allergy to fluoroquinolones
pregnancy
Use with caution in the presence of renal dysfunction,
Nursing Department
D. FLUOROQUINOLONES
ADVERSE EFFECTS:
most common are headache, dizziness, insomnia, and depression
GI effects include nausea, vomiting, diarrhea, and dry mouth
Box Warning was added to all drugs in this class in 2009 reporting the risk of
tendinitis and tendon rupture.
immunological effects include bone marrow depression
fever, rash, and photosensitivity
Nursing Department
D. FLUOROQUINOLONES
Monitor the patient for :
CNS: headache, dizziness, tinnitus,confusion, mental depression
GI upsets
bone marrow depression
PHOTOTOXICITY/ PHOTOSENSITIVITY
HEPATOTOXICITY
NEPHROTOXICITY
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E. PENICILLINS
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E. PENICILLINS
bactericidal effects by interfering with the ability of susceptible bacteria to
build their cell walls when they are dividing.
drugs prevent from biosynthesizing the framework of the cell wall, and
the bacteria with weakened cell walls swell and then burst from osmotic
pressure within the cell.
are indicated for the treatment of streptococcal infections, including
pharyngitis, tonsillitis, and others.
At high doses, these drugs are also used to treat meningococcal
meningitis.
Nursing Department
E. PENICILLINS
PHARMAKOKINETICS
rapidly absorbed from the GI tract, reaching peak levels

sensitive to the gastric acid levels in the stomach and should be
taken on an empty stomach to ensure adequate absorption.
enter breast milk
Nursing Department
E. PENICILLINS
allergy to penicillin and cephalosporins

pregnancy
Use with caution in the presence of renal disease,
Nursing Department
E. PENICILLINS
ADVERSE EFFECTS:
Common adverse effects include nausea, vomiting, diarrhea, abdominal pain,

glossitis, stomatitis, gastritis, sore mouth, and furry tongue.
Superinfections, including yeast infections
Pain and inflammation at the injection site
Hypersensitivity reactions may include rash, fever, wheezing, and, with repeated
exposure, anaphylaxis .
Nursing Department
E. PENICILLINS
Assessment: History and Examination
Check culture and sensitivity reports
Examine skin and mucous membranes for any rashes or lesions and injection sites for
abscess formation
Note respiratory status as baseline
Examine the abdomen to monitor for adverse effects
Monitor renal function.
Nursing Department
F. SULFONAMIDES
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F. SULFONAMIDES
bactericidal effects by interfering with the ability of susceptible bacteria to
build their cell walls when they are dividing.
drugs prevent the bacteria from biosynthesizing the framework of the cell
wall, and the bacteria with weakened cell walls swell and then burst from
osmotic pressure within the cell.
are indicated for the treatment of streptococcal infections, including
pharyngitis, tonsillitis, and others.
At high doses, these drugs are also used to treat meningococcal
meningitis.
Nursing Department
F. SULFONAMIDES
PHARMAKOKINETICS
rapidly absorbed from the GI tract, reaching peak levels in 1

hour.
sensitive to the gastric acid levels in the stomach and should be
taken on an empty stomach to ensure adequate absorption.
enter breast milk
Nursing Department
F. SULFONAMIDES
allergy to penicillin and cephalosporins

pregnancy
Use with caution in the presence of renal disease,
Nursing Department
F. SULFONAMIDES
ADVERSE EFFECTS:
Common adverse effects include nausea, vomiting, diarrhea, abdominal pain,

glossitis, stomatitis, gastritis, sore mouth, and furry tongue.
Superinfections, including yeast infections
Pain and inflammation at the injection site
Hypersensitivity reactions may include rash, fever, wheezing, and, with repeated
exposure, anaphylaxis .
Nursing Department
F. SULFONAMIDES
Assessment: History and Examination
Check culture and sensitivity reports
Examine skin and mucous membranes for any rashes or lesions and injection sites for
abscess formation
Note respiratory status as baseline
Examine the abdomen to monitor for adverse effects
Monitor renal function.
Nursing Department
G. TETRACYCLINES
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G. TETRACYCLINES
work by inhibiting protein synthesis in a wide range of bacteria, leading to
the inability of the bacteria to multiply.
indicated for treatment of infections caused by Rickettsiae, Mycoplasma

pneumoniae, Borrelia recurrentis, H. infl uenzae, Haemophilus ducreyi,
Pasteurella pestis, ETC.
Nursing Department
G. TETRACYCLINES
PHARMAKOKINETICS
absorbed adequately, but not completely, from the GI tract.

Absorption is affected by food, iron, calcium, and other drugs in
the stomach.
cross the placenta and pass into breast milk
Nursing Department
G. TETRACYCLINES
allergy to tetracyclines or to tartrazine

pregnancy and lactation
ophthalmic preparation: patients who have fungal, mycobacterial, or
viral ocular infections
used with caution in children younger than 8 years of age
Nursing Department
G. TETRACYCLINES
ADVERSE EFFECTS:
direct irritation of the GI tract and include nausea, vomiting, diarrhea, abdominal
pain, glossitis, and dysphagia.
Fatal hepatotoxicity related to the drug’s irritating effect on the liver
Skeletal effects involve damage to the teeth and bones.
Dermatological effects include photosensitivity and rash.
Superinfections
Local effects, such as pain and stinging with topical or ocular application
Hypersensitivity reactions
Nursing Department
G. TETRACYCLINES
Monitor the patient for GI effects, bone marrow depression, rash, and superinfections.
Caution women that tetracyclines may make oral contraceptives ineffective.
note for:
teeth and skeletal growth damage
Nursing Department
H. ANTIMYCOBACTERIALS
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Mycobacteria
the group of bacteria that contain the pathogens that cause tuberculosis and
leprosy.
cause serious infectious diseases:
Mycobacterium tuberculosis - PTB
Mycobacterium leprae- LEPROSY OR HANSEN'S DISEASE
Mycobacterium avium-intracellulare -mycobacterium avium complex in AIDS
Nursing Department
ANTITUBERCULOSIS DRUGS
Treatment duration: 6 months to 2 years.
First-line drugs : Second-line drugs :

isoniazid (Nydrazid) ethionamide (Trecator-SC),
rifampin (Rifadin) capreomycin (Capastat),
pyrazinamide (generic) cycloserine (Seromycin)
ethambutol (Myambutol) rifabutin (Mycobutin).
streptomycin (generic),
rifapentine (Priftin).
Nursing Department
LEPROSTATIC DRUGS
Dapsone (generic)
the mainstay of leprosy treatment
inhibits folate synthesis
used for treatment of P. carinii pneumonia in AIDS patients
Adverse Effects:
CNS effects, such as neuritis, dizziness, headache, malaise,
drowsiness, and hallucinations.
irritating to the GI tract, causing nausea, vomiting, anorexia,
stomach upset, and abdominal pain.
Nursing Department
PHARMAKOKINETICS
Well absorbed from the GI tract.

metabolized in the liver and excreted in the urine
cross the placenta and pass into breast milk
Nursing Department
Isoniazid
Description
a. Bactericidal
b. Inhibits the synthesis of mycolic acids and acts to kill actively
growing organisms in the extracellular environment
c. Inhibits the growth of dormant organisms in the macrophages and
caseating granulomas
d. Is active only during cell division and is used in combination with
other antitubercular medications
Nursing Department
Isoniazid
Side and adverse effects
a. Hypersensitivity reactions
b. Peripheral neuritis
c. Neurotoxicity
d. Hepatotoxicity and hepatitis; increased liver function test levels
e. Pyridoxine deficiency
f. Irritation at injection site with intramuscular administration
g. Nausea and vomiting
h . Dry mouth
i. Dizziness
k. Vision changes
Nursing Department
Isoniazid
Contraindications and cautions
a. Contraindicated in clients with hypersensitivity or with acute liver disease
b. Use with caution in clients with chronic liver disease, alcoholism, or renal
impairment.
c. Use with caution in clients taking hepatotoxic medications because the risk for
hepatotoxicity increases.
d. Alcohol increases the risk of hepatotoxicity.
e. May increase the risk of toxicity of carbamazepine and phenytoin
g. May decrease ketoconazole concentrations
Nursing Department
Isoniazid
Nursing Interventions:
a. Assess for hypersensitivity.
b. Assess for hepatic dysfunction.
c.Monitor liver function test results.
d. Monitor for signs of hepatitis, such as anorexia, nausea, vomiting, weakness,
fatigue, dark urine
e. Monitor for tingling, numbness, or burning of the extremities.
f. Assess mental status.
g. Monitor for visual changes, and notify the HCP if they occur.
h. Assess for dizziness and initiate safety precautions.
Nursing Department
Isoniazid
i. Monitor complete blood count (CBC).
j. Administer isoniazid 1 hour before or 2 hours after a meal because food may delay
absorption.
k. Administer isoniazid at least 1 hour before antacids.
l. Administer pyridoxine as prescribed to reduce the risk of neurotoxicity.
m. To avoid tyramine-containing foods because theymaycause a reaction such as red
and itching skin, a pounding heartbeat, lightheadedness
n. To recognize the signs of neurotoxicity, hepatitis, and hepatotoxicity
o. To notify the HCP if signs of neurotoxicity, hepatitis and hepatotoxicity, or visual
changes occur
Nursing Department
Rifampicin
Description
a. Inhibits bacterial RNA synthesis
b. Binds to DNA-dependent RNA polymerase and blocks
RNA transcription
c. Used with at least 1 other antitubercular medication
Nursing Department
Rifampicin
a. Contraindicated in clients with hypersensitivity
b. Used with caution in clients with hepatic dysfunction or alcoholism
c. Use of alcohol or hepatotoxic medications may increase the risk of hepatotoxicity.
d. Decreases the effects of several medications, including oral anticoagulants, oral
hypoglycemics, chloramphenicol, digoxin, disopyramide phosphate, mexiletine,
quinidine polygalacturonate, fluconazole, methadone hydrochloride, phenytoin, and
verapamil hydrochloride
Nursing Department
Rifampicin
a. Hypersensitivity reaction, including fever, chills, shivering, headache, muscle and bone
pain, and dyspnea.
b. Heartburn, nausea, vomiting, diarrhea
c. Red-orange–colored body secretions
d. Vision changes
e. Hepatotoxicity and hepatitis
f. Increased uric acid levels
g. Blood dyscrasias
h. Colitis
Nursing Department
Rifampicin
a. Assess for hypersensitivity.
b. Evaluate CBC, uric acid, and liver function test results.
c. Assess for signs of hepatitis; if they occur, withhold the medication and notify the HCP.
d. Monitor for signs of colitis.
e. Assess for visual changes.
f. That urine, feces, sweat, and tears will be red orange and that soft contact lens can
become permanently discolored
g. To notify the HCP if jaundice (yellow eyes or skin) develops or if weakness, fatigue,
nausea, vomiting, sore throat, fever, or unusual bleedi
Nursing Department
Ethambutol
Description
a. Bacteriostatic
b. Interferes with cell metabolism and multiplication by
inhibiting 1 or more metabolites in susceptible organisms
c. Inhibits bacterial RNA synthesis and is active only during
cell division
d. Slow-acting and must be used with other bactericidal
agents
Nursing Department
Ethambutol
a. Contraindicated in clients with hypersensitivity or optic neuritis and in children
younger than 13 years
b. Used with caution in clients with renal dysfunction, gout, ocular defects, diabetic
retinopathy, cataracts, or ocular inflammatory conditions
c. Used with caution in clients taking neurotoxic medications because the risk for
neurotoxicity increases
Nursing Department
Ethambutol
a. Hypersensitivity reactions
b. Anorexia, nausea, vomiting
c. Dizziness
d. Malaise
e. Mental confusion
f. Joint pain
g. Dermatitis
h. Optic neuritis
i. Peripheral neuritis
j. Thrombocytopenia
k. Increased uric acid levels
Nursing Department
Ethambutol
a. Assess the client for hypersensitivity.
b. Evaluate results of CBC, uric acid, and renal and liver function tests.
c. Monitor for visual changes such as altered color perception and decreased visual acuity; if
changes occur, withhold the medication and notify the HCP.
d. Administer once every 24 hours and administer with food to decrease gastrointestinal
upset.
e. Monitor uric acid concentration and assess for painful or swollen joints or signs of gout.
f. Monitor intake and output and for adequate renal function.
g. Assess mental status.
h . Monitor for dizziness and initiate safety precautions.
i. Assess for peripheral neuritis (numbness, tingling, or burning of the extremities); if it occurs,
notify the HCP

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1 Chemotherapeutic Agents Lecture Part 1

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Notre Dame of Marbel University

College of Arts and Sciences

INTENDED LEARNING OUTCOMES:

These drugs affect cells by altering cellular function or disrupting cellular

“power plants” within each cell that produce energy in

II. ANTI-INFECTIVE AGENTS

II. ANTI-INFECTIVE AGENTS

II. ANTI-INFECTIVE AGENTS

Bacteriostatic -not as aggressive; they interfere with the

II. ANTI-INFECTIVE AGENTS

It is difficult to treat any infections for two reasons:

II. ANTI-INFECTIVE AGENTS

II. ANTI-INFECTIVE AGENTS

II. ANTI-INFECTIVE AGENTS

Bactericidal and Bacteriostatic.

are well absorbed from the GI tract

allergies to cephalosporins or penicillins

They interfere with the action of DNA enzymes necessary

are absorbed from the GI tract, metabolized in the liver, and

rapidly absorbed from the GI tract, reaching peak levels

allergy to penicillin and cephalosporins

Common adverse effects include nausea, vomiting, diarrhea, abdominal pain,

rapidly absorbed from the GI tract, reaching peak levels in 1

allergy to penicillin and cephalosporins

Common adverse effects include nausea, vomiting, diarrhea, abdominal pain,

indicated for treatment of infections caused by Rickettsiae, Mycoplasma

absorbed adequately, but not completely, from the GI tract.

allergy to tetracyclines or to tartrazine

First-line drugs : Second-line drugs :

Well absorbed from the GI tract.

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