NCMA 216

Pharmacology
in Nursing
Chemotherapeutic
Agents
Prepared by:
Mark Joseph V. Liwanag, RN, MSN
PART 1
Anti – Microbial Agents
PART 2
Cancer Chemotherapy
Prepared by:
Mark Joseph V. Liwanag, RN, MSN
▪ involves the use of drugs to treat infectious diseases
▪ using drugs to control the growth of pathogens in
vivo.
▪ CHEMOTHERAPY
▪ refers to the use of any chemical (drug) to treat
any disease or condition.
▪ Although we most often hear the term
chemotherapy used in conjunction with cancer
(i.e., cancer chemotherapy)
▪ CHEMOTHERAPEUTIC AGENTS
▪ chemicals (drugs) used to treat diseases
▪ is any drug used to treat any condition or disease.
 INTRODUCTION
▪ ANTIMICROBIAL AGENTS: chemotherapeutic agents used to treat
infectious diseases
▪ an antimicrobial agent is any chemical (drug) used to treat an infectious
disease
▪ either by inhibiting or by killing pathogens in vivo.
▪ ANTIBACTERIAL AGENTS: Drugs used to treat bacterial diseases
▪ ANTIFUNGAL AGENTS: used to treat fungal diseases
▪ ANTIPROTOZOAL AGENTS:
Drugs used to treat protozoal
diseases
▪ ANTIVIRAL AGENTS: those
used to treat viral diseases
 INTRODUCTION:
▪ antimicrobial agents are antibiotics.
▪ ANTIBIOTICS: a substance produced by a microorganism that is effective in killing
or inhibiting the growth of other microorganisms.
▪ all antibiotics are antimicrobial agents, not all antimicrobial agents are
antibiotics
▪ Antibiotics are produced by certain moulds and
bacteria, usually those that live in soil.
▪ FUNGI (MOULDS): Penicillin and cephalosporins
▪ BACTERIA: bacitracin, erythromycin, and
chloramphenicol
▪ SEMISYNTHENTIC ANTIBIOTICS: chemically modified
to kill a wider variety of pathogens or reduce side
effects
▪ semisynthetic penicillins, such as ampicillin and
carbenicillin.
 CHARACTERISTICS OF AN IDEAL ANTIMICROBIAL
AGENT
The ideal antimicrobial agent should:
▪ Kill or inhibit the growth of pathogens
▪ Cause no damage to the host
▪ Cause no allergic reaction in the host
▪ Be stable when stored in solid or liquid
form
▪ Remain in specific tissues in the body long
enough to be effective
▪ Kill the pathogens before they mutate and
become
HOW ANTIMICROBIAL AGENTS WORK

To be acceptable, an To accomplish this, the

antimicrobial agent agent must target a
must inhibit or destroy metabolic process or
the pathogen without structure possessed by
damaging the host (i.e., the pathogen but not
the infected person) possessed by the host
The five most common mechanisms of action of antimicrobial
agents are as follows:
▪ Inhibition of cell wall synthesis

▪ Damage to cell membranes

▪ Inhibition of nucleic acid synthesis

(either DNA or RNA synthesis)

▪ Inhibition of protein synthesis

▪ Inhibition of enzyme activity

ANTIBACTERIAL AGENTS

▪ Bacteriostatic: drugs inhibit growth

of bacteria
▪ Bactericidal: agents kill bacteria

▪ Narrow-spectrum antibiotics: kill

either Gram-positive or Gram-
negative bacteria
▪ Broad-spectrum antibiotics: kill both
Gram positives and Gram negatives.
MAJOR CATEGORIES OF
ANTIBACTERIAL AGENTS
1. PENICILLINS
▪ referred to as β-lactam drugs
▪ molecular structure includes a four sided ring
structure known as a β-lactam ring

▪ interfere with the synthesis of bacterial cell walls

▪ have maximum effect on bacteria that are actively
dividing.
▪ they are bactericidal drugs.
PENICILLINS
▪ NATURAL PENICILLINS: they are produced and can be
purified directly from cultures of Penicillium moulds
▪ Penicillin G and Penicillin V.
▪ effective against some Gram-positive bacteria
(especially Streptococcus spp.)
▪ some anaerobic bacteria, and some
spirochetes.
▪ few Gram-negative bacteria (e.g., N. meningitidis
and some strains of Haemophilus influenzae)
remain susceptible to natural penicillins.
▪ extended-spectrum penicillins (e.g., aminopenicillins)
are used to treat infections caused by Gram-negative
bacilli.
ANTIBIOTICS: GENERIC AND BRAND NAMES
Here is a table of commonly encountered antibiotics, their generic names,
and brand names:
Classification Generic Name Brand Name
Penicillins and Penicillinase – Resistant Antibiotics
penicillin G benzathine Bicillin, Permapen
penicillin G potassium Pfizerpen
Penicillins
penicillin G procaine Wycillin
penicillin V Veetids
Extended-Spectrum amoxicillin Amoxil, Trimox
Penicillins ampicillin Principen
Penicillinase-Resistant nafcillin
Antibiotics oxacillin
MAJOR CATEGORIES OF ANTIBACTERIAL AGENTS

CEPHALOSPORINS
▪ also β-lactam antibiotics and, like
penicillin, are produced by
moulds.
▪ interfere with cell wall synthesis
▪ are bactericidal
▪ cephalosporins are classified as
first-, second-, third-, fourth-, and
fifth- generation cephalosporins.
 MAJOR CATEGORIES OF
ANTIBACTERIAL AGENTS
CEPHALOSPORINS
First-generation agents are active primarily against
Gram-positive bacteria.

Second-generation cephalosporins have increased

activity against Gram- negative bacteria

Third-generation cephalosporins have even greater

activity against Gram negatives (including
Pseudomonas aeruginosa).
CEPHALOSPORINS
▪ Fourth-generation active against both Gram positives and Gram negatives,
including P. Aeruginosa. e.g., Cefepime
▪ Fifth-generation expanded activity against aerobic Gram-positive cocci,
including methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-
resistant Staphylococcus epidermidis MRSE e.g., Ceftaroline
MAJOR CATEGORIES OF ANTIBACTERIAL AGENTS

CARBAPENEMS
▪ powerful antibacterial
▪ target the cell envelope

▪ have excellent activity against a broad

spectrum of bacteria, including many aerobic
Gram-positive bacteria, most aerobic Gram-
negative bacteria, and most anaerobes.
▪ e.g.,imipenem &. meropenem
MAJOR CATEGORIES OF ANTIBACTERIAL AGENTS

GLYCOPEPTIDES
▪ target the cell envelope.
▪ have excellent activity against most
aerobic and anaerobic Gram-
positive bacteria.
▪ enterococci, are becoming resistant
to these drugs
▪ have a number of toxic side effects.
▪ e.g.,vancomycin
 MAJOR CATEGORIES OF
ANTIBACTERIAL AGENTS
Tetracyclines
▪ broad-spectrum drugs
▪ effect by targeting bacterial ribosomes.
▪ bacteriostatic.
▪ effective against a wide variety of
bacteria
▪ including chlamydias, mycoplasmas,
rickettsias, Vibrio cholerae
▪ spirochetes such as Borrelia spp.
and Treponema pallidum.
▪ e.g.,Doxycycline &. Tetracyclines
MAJOR CATEGORIES OF ANTIBACTERIAL AGENTS

Aminoglycosides
▪ bactericidal broad-spectrum drugs
▪ inhibit bacterial protein synthesis
▪ major factor that limits their use is their toxicity
▪ effective against a wide variety:
▪ aerobic Gram-negative bacteria
▪ used to treat infections with members of the family:
▪ Enterobacteriaceae (e.g., Escherichia coli and
▪ Enterobacter, Klebsiella, Proteus, Serratia, and Yersinia
spp.),
▪ P. aeruginosa and Vibrio cholerae.
▪ E.g., Tobramycin, Gentamicin &. Amikacin
MAJOR CATEGORIES OF ANTIBACTERIAL
AGENTS
MACROLIDES
▪ inhibit protein synthesis
▪ bacteriostatic at lower doses and bactericidal at higher
doses
▪ include erythromycin, clarithromycin, and azithromycin
▪ effective against:
▪ chlamydias, mycoplasmas,
▪ T. pallidum, and Legionella spp.
▪ Azithromycin and Erythromycin
 MAJOR CATEGORIES OF
ANTIBACTERIAL AGENTS
Fluoroquinolones
▪ bactericidal drugs
▪ inhibit DNA synthesis

▪ The most commonly used fluoroquinolone,

Ciprofloxacin and Levofloxacin

▪ effective against members of the family:

▪ Enterobacteriaceae and P. aeruginosa.
 MAJOR CATEGORIES OF ANTIBACTERIAL
AGENTS
Sulfonamide
▪ drugs inhibit production of folic acid (a vitamin)
in those bacteria that require p-aminobenzoic
acid (PABA) to synthesize folic acid*

▪ Without folic acid, bacteria cannot produce

certain essential proteins and finally die
▪ called competitive inhibitors*

▪ Bacteriostatic: inhibit growth of bacteria

▪ E.g., Sulfamethoxazole + Trimethoprim
Antibiotics: Generic and Brand Names
Here is a table of commonly encountered antibiotics,
their generic names, and brand names:

Classification Generic Name Brand Name

sulfadiazine generic
Sulfonamides sulfasalazine Azulfidine
cotrimoxazole Septra, Bactrim
 MULTIDRUG THERAPY
▪ a single antimicrobial agent is not sufficient to destroy
all the pathogens that develop during the course of a
disease
▪ two or more drugs may be used simultaneously to kill
all the pathogens to prevent resistant mutant
pathogens from emerging
▪ In tuberculosis:
▪ which multidrug-resistant strains of Mycobacterium
tuberculosis are frequently encountered
▪ four drugs (isoniazid, rifampin, pyrazinamide, and
ethambutol)
ANTITUBERCULAR DRUGS
▪ Streptomycin, a parenteral antibiotic, was the first drug used
to treat TB.

▪ Isoniazid (INH), discovered in 1952, was the first oral drug

preparation effective against the tubercle bacillus.

▪ Isoniazid is a bactericidal drug that inhibits tubercle cell wall

synthesis and blocks pyridoxine (vitamin B6), which is used for
intracellular enzyme production.
ANTITUBERCULAR DRUGS
▪ It was discovered that when a combination of antitubercular drugs was
used, bacterial resistance did not occur, and the duration of treatment
was reduced from 2 years to 6 – 9 months.

▪ Different combinations of drugs can be used:

▪ Isoniazid and rifampin;
▪ isoniazid, rifampin, and ethambutol; or
▪ isoniazid, rifampin, and pyrazinamide.

▪ Rifampin and ethambutol were discovered in the early 1960s; neither

drug is effective against the tubercle bacillus when given alone.
▪ Rifampin is taken alone, bacterial resistance occurs quickly
 ANTIFUNGAL AGENTS
▪ It is much more difficult to use antimicrobial
drugs against fungal pathogens*
▪ drugs tend to be more toxic to the patient*
▪ Most antifungal agents work in one of three
ways:
▪ By binding with cell membrane sterols (e.g.,
nystatin and amphotericin B)
▪ By interfering with sterol synthesis (e.g.,
clotrimazole and miconazole)
▪ By blocking mitosis or nucleic acid
synthesis (e.g., griseofulvin and 5-
flucytosine)
 ANTIPROTOZOAL AGENTS
▪ usually quite toxic to the host and
work by:
▪ interfering with DNA and RNA
synthesis
▪ e.g., chloroquine, pentamidine,
and quinacrine
▪ interfering with protozoal
metabolism
▪ e.g., metronidazole (Flagyl)
Antimalarials - are agents used to attack Plasmodium at
various stages of its life cycle.
1. schizonticidal (acting against the red-blood-cell
phase of the life cycle),
2. gametocytocidal (acting against the gametocytes),
3. sporontocidal (acting against the parasites that are
developing in the mosquito)
4. as prophylactic or antirelapse agent.

▪ Quinine (Qualaquine) was the first drug found to be

effective in the treatment of malaria.
▪ Chloroquine - directly toxic to parasites and decreases
the ability of the parasite to synthesize DNA.
ANTHELMINTICS - They act on metabolic pathways present in the invading worm
but are absent or significantly different in human host.
Indications
▪ Albendazole for the treatment of active lesions caused by
pork tapeworm and cystic disease of the liver, lungs, and
peritoneum caused by dog tapeworm.
▪ Ivermectin is used for the treatment of threadworm disease
or strongyloidiasis and onchocerciasis or river blindness.
▪ Mebendazole is for the treatment of diseases caused by
pinworms, roundworms, whipworms, and hookworms.
▪ Praziquantel is for treatment of a wide number of
schistosomes or flukes.
▪ Pyrantel is for treatment caused by pinworms and
roundworms.
 ANTIVIRAL AGENTS
▪ the newest weapons in antimicrobial
methodology
▪ there were no drugs for the
treatment of viral diseases*
▪ particularly difficult to develop and
use because viruses are produced
within host cells
▪ quite a few drugs have been found to
be effective in certain viral infection
 ANTIVIRAL AGENTS
▪ first antiviral agent effective against human
immunodeficiency virus (HIV)
▪ Zidovudine (also known as azidothymidine
[AZT])
▪ was introduced in 1987
▪ antiviral agents are administered
simultaneously, in combinations referred to as
“cocktails.”
▪ quite expensive, and some strains of HIV
have become resistant to some of the
drugs.
▪ e.g., Remdesivir – COVID 19 treatment
 DRUG RESISTANCE: SUPERBUGS
▪ “Superbugs”: refer to an organism
that is resistant to only one
antimicrobial agent, the term
usually refers to multidrug
resistant organisms

▪ Infections caused by superbugs

are much more difficult to treat
 ▪ note that bacteria are
not the only microbes
that have developed
resistance to drugs.

▪ Certain viruses
(including HIV, herpes
simplex viruses, and
influenza viruses),
DRUG RESISTANCE: fungi (both yeasts
SUPERBUGS and moulds),
MECHANISM BY WHICH BACTERIA BECOME RESISTANT TO
ANTIMICROBIAL AGENTS
▪ A chromosomal mutation that causes a
change in the structure of a drug-binding
site
▪ The drug cannot bind to the bacterial
cell
▪ A chromosomal mutation that causes a
change in cell membrane permeability
▪ The drug cannot pass through the cell
membrane and thus cannot enter the
cell
MECHANISM BY WHICH BACTERIA BECOME RESISTANT TO
ANTIMICROBIAL AGENTS

▪ Acquisition (by conjugation, transduction, or

transformation) of a gene that enables the
bacterium to produce an enzyme that destroys or
inactivates the drug
▪ The drug is destroyed or inactivated by the
enzyme
▪ Acquisition (by conjugation, transduction, or
transformation) of a gene that enables the
bacterium to produce an MDR pump
▪ The drug is pumped out of the cell before it can
damage or kill the cell
 HOW BACTERIA BECOME RESISTANT TO DRUGS?
▪ Some bacteria are naturally resistant to a particular antimicrobial agent
because they lack the specific target site for that drug (e.g.,
mycoplasmas)*
▪ Other bacteria are naturally resistant because the drug is unable to
cross the organism’s cell wall or cell membrane and, thus, cannot reach
its site of action (e.g., ribosomes).
▪ Such resistance is known as intrinsic
resistance.
▪ It is also possible for bacteria that were once
susceptible to a particular drug to become
resistant to it
▪ this is called acquired resistance.
 Β-LACTAMASES
▪ At the heart of every penicillin and cephalosporin
molecule is a double-ringed structure, which in penicillins
resembles a “house and garage”
▪ “garage” is called the β-lactam ring
▪ Some bacteria produce enzymes that destroy the β-
lactam ring; these enzymes are known as Β-LACTAMASES.
▪ When the β-lactam ring is destroyed, the antibiotic no
longer works.
▪ Thus, an organism that produces a β-lactamase is
resistant to antibiotics containing the β-lactam ring
(collectively referred to as β-lactam antibiotics or β-
lactams).
 1. Penicillinases destroy the β-
lactam ring in penicillins;
thus, an organism that
produces penicillinase is
resistant to penicillins.

2. Cephalosporinases destroy
the β-lactam ring in
cephalosporins; thus, an
organism that produces
cephalosporinase is resistant
THERE ARE TWO to cephalosporins. Some
bacteria produce both types
TYPES OF Β-LACTAMASES: of β-lactamases.
▪ β-lactamase inhibitor irreversibly binds to and
inactivates the β-lactamase, thus enabling the
companion drug to enter the bacterial cell and
disrupt cell wall synthesis.
▪ e.g., clavulanic acid, sulbactam, or
tazobactam
▪ Some of these special combination drugs are
▪ Clavulanic acid (clavulanate) combined with
amoxicillin (brand name, Augmentin)
▪ Clavulanic acid (clavulanate) combined with
ticarcillin (Timentin)
▪ Sulbactam combined with ampicillin
(Unasyn)
▪ Tazobactam combined with piperacillin
(Zosyn)
 SOME STRATEGIES IN THE WAR
AGAINST DRUG RESISTANCE
▪ Education is crucial—education of healthcare
professionals and, in turn, education of
patients.
▪ Patients should never pressure clinicians to
prescribe antimicrobial agents.
▪ Parents must stop demanding antibiotics
every time they have a sick child.
▪ It is important that clinicians not allow
themselves to be pressured by patients
▪ Clinicians should prescribe an inexpensive,
narrow spectrum drug whenever the
laboratory
SOME STRATEGIES IN THE WAR AGAINST
DRUG RESISTANCE
▪ Patients must take their antibiotics in the
exact manner in which they are
prescribed.
▪ It is critical that clinicians prescribe the
appropriate amount of antibiotic
necessary to cure the infection.
▪ Patients should always destroy any excess
medications and should never keep
antibiotics in their medicine cabinet.
▪ Antimicrobial agents, including antibiotics,
should be taken only when prescribed and
only under a clinician’s supervision.
▪ a clinician must initiate therapy before
laboratory results are available
▪ an effort to save the life of a patient

▪ it is sometimes necessary for the clinician

to “guess” the most likely pathogen and
the drug most likely to be effective

▪ It will be an “educated guess,” based on

the clinician’s prior experiences with the
particular type of infectious disease
 UNDESIRABLE EFFECTS OF
ANTIMICROBIAL AGENTS
▪ Listed below are some of the many reasons
why antimicrobial agents should not be used
indiscriminately.

▪ Whenever an antimicrobial agent is

administered to a patient, any organisms
within that patient that are susceptible to the
agent will die, but resistant ones will survive.

▪ patient may become allergic to the agent

 UNDESIRABLE EFFECTS OF
ANTIMICROBIAL AGENTS
▪ Many antimicrobial agents are toxic to humans, and
some are so toxic that they are administered only for
serious diseases for which no other agents are
available.
▪ chloramphenicol, which, if given in high doses for a
long period, may cause a very severe type of anemia
called aplastic anemia.
▪ streptomycin, which can damage the auditory nerve
and cause deafness.
▪ Other drugs are hepatotoxic or nephrotoxic, causing
liver or kidney damage, respectively.
 UNDESIRABLE EFFECTS OF ANTIMICROBIAL AGENTS
▪ With prolonged use, broadspectrum antibiotics may
destroy the indigenous microbiota of the mouth,
intestine, or vagina.
For example:
▪ prolonged use of oral antibiotics can result in a
superinfection of Clostridium difficile in the
colon
▪ which can lead to such diseases as antibiotic-
associated diarrhea and pseudomembranous
colitis.
▪ Yeast vaginitis often follows antibacterial therapy
▪ many bacteria of the vaginal microbiota were
destroyed, leading to a superinfection of the
indigenous yeast, Candida albicans.
These are vital nursing interventions done in patients who are taking
antibiotics:
▪ Provide safety measures to protect the patient if CNS effects (e.g.
confusion, disorientation, numbness) occur.

▪ Educate client on drug therapy to promote

understanding and compliance.

▪ Provide the following patient teaching: safety

precautions (e.g. changing positions, avoiding hazardous
tasks, ec.), drinking lots of fluids and to maintain
nutrition even though nausea and vomiting may occur,
report difficulty breathing, severe headache, fever,
diarrhea, and signs of infection.
These are vital nursing interventions done in patients who are taking
antibiotics:
▪ Check culture and sensitivity reports to ensure that this is the drug of
choice for this patient.

▪ Ensure that patient receives full course of

aminoglycosides as prescribed, divided around the clock to
increase effectiveness and decrease the risk for
development of resistant strains of bacteria.

▪ Monitor infection site and presenting signs and symptoms

throughout course of drug therapy because failure of
these manifestations to resolve may indicate the need to
reculture the site.