Chemotherapeutic Agents

ANTIINFECTIVE AGENTS

 Bactericidal: substance that causes the death of

bacteria, usually by interfering with cell membrane
stability or with proteins or enzymes necessary to
maintain the cellular integrity of the bacteria.
 Bacteriostatic: substance that prevents the
replication of bacteria, usually by interfering with
proteins or enzyme systems necessary for
reproduction of the bacteria.
 Culture: sample of the bacteria (e.g., from
sputum, cell scrapings, urine) to be grown in a
laboratory to determine the species of bacteria that
causes an infection.
 Prophylaxis: treatment to prevent an infection
before it occurs, as in the use of antibiotics to
prevent bacterial endocarditis in high-risk patients
or antiprotozoal to prevent malaria.
 Resistance: ability of pathogens over time to adapt
to an anti-infective to produce cells that are no
longer affected by a particular drug Selective
toxicity: the ability to affect certain proteins or
enzyme systems that are used by the infecting
organism but not by human cells.
 Sensitivity testing: evaluation of pathogens
obtained in a culture to determine the anti-infective
ANTIBIOTICS
to which the organisms are sensitive and which
agent would be appropriate for treatment of a
particular infection.
 Aerobic: bacteria that depend on oxygen for
 Spectrum: range of bacteria against which an
survival.
antibiotic is effective (e.g., broad-spectrum
antibiotics are effective against a wide range of  Anaerobic: bacteria that survive without oxygen,
bacteria; narrow-spectrum antibiotics are effective which are often seen when blood flow is cut off to
only against very selective bacteria). an area of the body.
 Superinfection: infections that occur when  Antibiotic: chemical that is able to inhibit the
opportunistic pathogens that were kept in check by growth of specific bacteria or cause the death of
the “normal” bacteria have the opportunity to susceptible bacteria.
invade tissues and cause infections because the  Gram-negative: bacteria that accept a negative
normal flora bacteria have been destroyed by stain and are frequently associated with infections
antibiotic therapy. of the genitourinary or gastrointestinal (GI) tract.
 Gram-positive: bacteria that take a positive stain
and are frequently associated with infections of the
DRUG LIST respiratory tract and soft tissues.
 Synergistic: drugs that work together to increase
 Bacitracin drug effectiveness.
 Gentamicin
 Meropenem
 Polymyxin B
 Vancomycin
Anti-infective agents are drugs designed to target
foreign organisms that have invaded and infected the
body of a human host.
 Chemotherapeutic Agents

 Influenza A: RNA virus that invades tissues of the

respiratory tract, causing the signs and symptoms
of the common cold or “flu”.
 Integrase inhibitor: a drug that inhibits the
activity of the virus-specific enzyme integrase, an
encoded enzyme needed for viral replication;
blocking this enzyme prevents the formation of the
HIV-1 provirus.
 Interferon: tissue hormone that is released in
response to viral invasion; blocks viral replication
nonnucleoside reverse transcriptase inhibitors:
drugs that bind to sites on the reverse transcriptase
within the cell cytoplasm, preventing RNA- and
DNA-dependent DNA polymerase activities
ANTIVIRAL AGENTS needed to carry out viral DNA synthesis; prevents
the transfer of information that allows the virus to
replicate and survive nucleoside reverse
 Acquired immunodeficiency syndrome (AIDS): transcriptase inhibitors: drugs that prevent the
collection of opportunistic infections and cancers growth of the viral DNA chain, preventing it from
that occurs when the immune system is severely inserting into the host DNA, so viral replication
depressed by a decrease in the number of cannot occur.
functioning helper T cells; caused by infection  Protease inhibitors: drugs that block the activity
with human immunodeficiency virus (HIV). of the enzyme protease in HIV; protease is
 AIDS-related complex (ARC): collection of less essential for the maturation of infectious virus, and
serious opportunistic infections with HIV its absence leads to the formation of an immature
infection; the decrease in the number of helper T and noninfective HIV particle.
cells is less severe than in fully developed AIDS.  Virus: particle of DNA or RNA surrounded by a
 CCR5 coreceptor antagonist: a drug that blocks protein coat that survives by invading a cell to alter
the receptor site on the T cell membrane that the its functioning.
HIV virus needs to interact with in order to enter
the cell.
 Cytomegalovirus (CMV): DNA virus that
accounts for many respiratory, ophthalmic, and
liver infections.
 Fusion inhibitor: a drug that prevents the fusion
of the HIV-1 virus with the human cellular
membrane, preventing it from entering the cell.
 Helper T cell: human lymphocyte that helps to
initiate immune reactions in response to tissue
invasion.
 Hepatitis B: a serious to potentially fatal viral
infection of the liver, transmitted by body fluids.
 Hepatitis C: a usually mild viral infection of the
liver that can progress to chronic inflammation;
most often seen hepatitis after blood transfusions.
 Herpes: DNA virus that accounts for many
diseases, including shingles, cold sores, genital
herpes, and encephalitis.
 Human immunodeficiency virus (HIV):
retrovirus that attacks helper T cells, leading to a
decrease in immune function and AIDS or ARC.
 Chemotherapeutic Agents
ANTIFUNGAL AGENTS
 Azoles: a group of drugs used to treat fungal
infections.
 Candida: fungus that is normally found on
mucous membranes; can cause yeast infections or
thrush of the gastrointestinal (GI) tract and vagina
in immunosuppressed patients.
 Ergosterol: steroid-type protein found in the cell
membrane of fungi; similar in configuration to
adrenal hormones and testosterone.
 Fungus: a cellular organism with a hard cell wall
that contains chitin and many polysaccharides, as
well as a cell membrane that contains ergosterols.
 Mycosis: disease caused by a fungus.
 Tinea: fungus called ringworm that causes such
infections as athlete’s foot, jock itch, and others.
Systemic Antifungals are drugs used to treat systemic
fungal infections can be toxic to the host and are not to
be used indiscriminately.
‘ 
ANTIPROTOZOAL AGENTS
 Amebiasis: amebic dysentery, which is caused by
intestinal invasion of the trophozoite stage of the
protozoan Entamoeba histolytica Anopheles
mosquito:
 Anopheles mosquito: type of mosquito that is
essential to the life cycle of injects the protozoa
into humans for further maturation.
 Cinchonism: syndrome of quinine toxicity
characterized by nausea, vomiting, tinnitus, and
vertigo.
 Giardiasis: protozoal intestinal infection that
causes severe diarrhea and epigastric distress; may
lead to serious malnutrition.
 leishmaniasis: skin, mucous membrane, or
visceral infection caused by a protozoan passed to
humans by the bites of sand flies.
 Malaria: protozoal infection with Plasmodium,
characterized by cyclic fever and chills as the
parasite is released from ruptured red blood cells;
causes serious liver, central nervous system
(CNS), heart, and lung damage.
 Plasmodium: a protozoan that causes malaria in
humans; its life cycle includes the Anopheles
mosquito, which injects protozoa into humans.
 Pneumocystis jiroveci pneumonia: opportunistic
infection that occurs when the immune system is
depressed; a frequent cause of pneumonia in
patients with AIDS and in those who are receiving
immunosuppressive therapy.
 Protozoa: single-celled organisms that pass
through several stages in their life cycle, including
at least one phase as a human parasite; found in
areas of poor sanitation and hygiene and crowded
living conditions.
Trichomoniasis: infestation with a protozoan that
causes vaginitis in women but no signs or
symptoms in men.
 Trophozoite: a developing stage of a parasite,
which uses the host for essential nutrients needed
for growth.
 Trypanosomiasis: African sleeping sickness,
which is caused by a protozoan that inflames the
CNS and is spread to humans by the bite of the
tsetse fly; also, Chagas disease, which causes a
serious cardiomyopathy after the bite of the
housefly.
Antimalarial drugs are usually given in combination
form to attack the Plasmodium at various stages of its
life cycle.
 Chemotherapeutic Agents

 Platyhelminth: flatworms, including the cestodes

or tapeworms; a worm that can live in the human
intestine or can invade other human tissues
(flukes).
 Schistosomiasis: infection with a blood fluke that
is carried by a snail; it poses a common problem in
tropical countries, where the snail is the
intermediary in the life cycle of the worm; larvae
burrow into the skin in fresh water and migrate
throughout the human body, causing a rash,
diarrhea, and liver and brain inflammation.
 Threadworm: pervasive nematode that can send
larvae into the lungs, liver, and central nervous
system (CNS); can cause severe pneumonia or
liver abscess.
 Trichinosis: disease that results from ingestion of
encysted roundworm larvae in undercooked pork;
larvae migrate throughout the body to invade
muscles, nerves, and other tissues; can cause
pneumonia, heart failure, and encephalitis.
 Whipworm: worm that attaches itself to the
intestinal mucosa and sucks blood; may cause
ANTIHELMINTIC AGENTS severe anemia and disintegration of the intestinal
mucosa.

 Ascaris: the most prevalent helminthic infection;

fertilized roundworm eggs are ingested, which
hatch in the small intestine and then make their
way to the lungs, where they may cause cough,
fever, and other signs of a pulmonary infiltrate.
 Cestode: tapeworm with a head and segmented
body parts that is capable of growing to several
yards in the human intestine.
 Filariasis: infection of the blood and tissues of
healthy individuals by worm embryos or filariae.
 Helminth: worm that can cause disease by
invading the human body.
 Hookworms: worms that attach themselves to the
small intestine of infected individuals, where they
suck blood from the walls of the intestine,
damaging the intestinal wall and leading to severe
anemia with lethargy, weakness, and fatigue.
 Nematode: roundworms such as the commonly
encountered pinworm, whipworm, threadworm,
Ascaris, or hookworm that cause a common
helminthic infection in humans; can cause ACTINEOPLASTIC AGENTS
intestinal obstruction as the adult worms clog the
intestinal lumen or severe pneumonia when the
larvae migrate to the lungs and form a pulmonary Alopecia: hair loss: a common adverse effect of many
infiltrate. antineoplastic drugs, which are more effective against
 Pinworm: nematode that causes a common rapidly multiplying cells, such as those of hair
helminthic infection in humans; lives in the follicles.
intestine and causes anal and possible vaginal
irritation and itching.
 Chemotherapeutic Agents

Anaplasia: loss of organization and structure; property

of cancer cells.
Angiogenesis: the generation of new blood vessels;
cancer cells release an enzyme that will cause
angiogenesis or the growth of new blood vessels to
feed the cancer cells.
Antineoplastic agent: drug used to combat cancer or
the growth of neoplasms.
Autonomy: loss of the normal controls and reactions
that inhibit growth and spreading; property of cancer
cells
Bone marrow suppression: inhibition of the blood-
forming components of the bone marrow; a common
adverse effect of many antineoplastic drugs, which are
more effective against rapidly multiplying cells, such
as those in bone marrow; seen as anemia,
thrombocytopenia, and leukopenia.
Carcinoma: tumor that originates in epithelial cells.
Metastasis: ability to enter the circulatory or
lymphatic system and travel to other areas of the body
that are conducive to growth and survival; property of
cancer cells.
Neoplasm: new or cancerous growth; occurs when
abnormal cells have the opportunity to multiply and
grow.
Sarcoma: tumor that originates in the mesenchyme
and is made up of embryonic connective tissue cells.

Antineoplastic drugs can work by affecting cell

survival or by boosting the immune system in its
efforts to combat the abnormal cells.

Systemic Antifungals

The drugs used to treat systemic fungal infections can be

toxic to the host and are not to be used indiscriminately. It is
important to get a culture of the fungus causing the infection
to ensure that the right drug is being used so that the patient
is not put at additional risk from the toxic adverse effects
associated with these drugs
 Chemotherapeutic Agents

Azole Antifungals that can be associated with the antineoplastic drugs. These
drugs are used as adjunctive therapy.
The azoles are a large group of antifungals used to treat
systemic and topical fungal infections. The azoles include
fluconazole (Diflucan), itraconazole (Sporanox),
ketoconazole (Nizoral), posaconazole (Noxafil), terbinafine
(Lamisil), voriconazole (Vfend), and the newest drug in the
class, isavuconazonium (Cresemba). Although azoles are
considered less toxic than some other antifungals, such as
amphotericin B, they may also be less effective in very
severe and progressive infections.

Antimalarials

Antimalarial drugs are usually given in combination form to

attack the Plasmodium at various stages of its life cycle.
Using this approach, it is possible to prevent the acute
malarial reaction in individuals who have been infected by
the parasite. These drugs can be schizonticidal (acting
against the red blood cell phase of the life cycle),
gametocytocidal (acting against the gametocytes),
sporontocidal (acting against the parasites that are
developing in the mosquito), or work against tissue
schizonts as prophylactic or antirelapse agents. Quinine
(Qualaquin) was the first drug found to be effective in the
treatment of malaria; it was absent from the market for a
while but is now available for the treatment of
uncomplicated malaria. Other antimalarials used today
include chloroquine (Aralen), mefloquine (generic),
primaquine (generic), and pyrimethamine (Daraprim).

Anthelmintics

The anthelmintic drugs act on metabolic pathways that are

present in the invading worm but are absent or significantly
different in the human host. Anthelmintic drugs include
albendazole (Albenza), ivermectin (Stromectol),
mebendazole (Emverm, Vermox), praziquantel (Biltricide),
and pyrantel (Antiminth, Pin-Rid, Pin-X, Reese’s Pinworm).
Box 13.2 includes information about use of these drugs
across the lifespan.

Antineoplastic Drugs

Antineoplastic drugs can work by affecting cell survival or

by boosting the immune system in its efforts to combat the
abnormal cells. Chapter 17 discusses the immune agents that
are used to combat cancer. The present chapter focuses on
those drugs that affect cell survival. The antineoplastic drugs
that are commonly used today include alkylating agents,
antimetabolites, antineoplastic antibiotics, mitotic inhibitors,
hormones and hormone modulators, cancer cell–specific
agents including protein tyrosine kinase inhibitors (which
target enzymes specific to the cancer cells), and a group of
antineoplastic agents that cannot be classified elsewhere.
Other drugs are used to combat the serious adverse effects