Anti-Infective

Agents
Antibiotics:
Sulfonamides
Penicillins
Cephalosporins
Tetracyclines
Aminoglycosides
Quinolones
Macrolides
Antibiotics

• Medications used to treat

bacterial infections
• Ideally, before beginning
antibiotic therapy, the
suspected areas of infection
should be cultured to identify
the causative organism and
potential antibiotic
susceptibilities.
Antibiotics

• Empiric therapy: treatment of

an infection before specific
culture information has been
reported or obtained
• Prophylactic therapy:
treatment with antibiotics to
prevent an infection, as in intra-
abdominal surgery
Antibiotics

•Bactericidal: kill bacteria

•Bacteriostatic: inhibit growth of
susceptible bacteria, rather than
killing them immediately; will
eventually lead to bacterial
death
Antibiotics:
Sulfonamides
One of the first groups of
antibiotics
• sulfadiazine
• sulfamethizole
• sulfamethoxazole
• sulfisoxazole
Sulfonamides:
Mechanism of Action
• Bacteriostatic action
• Prevent synthesis of folic acid
required for synthesis of purines
and nucleic acid
• Does not affect human cells or
certain bacteria—they can use
preformed folic acid
 Sulfonamides:
sulfamethoxazole
Therapeutic Uses
Azo-Gantanol
• Combined with phenazopyridine
(an analgesic-anesthetic that affects the mucosa
of the urinary tract).
• Used to treat urinary tract infections (UTIs) and
to reduce the pain associated with UTIs.
Bactrim
• Combined with trimethoprim.
• Used to treat UTIs, Pneumocystis carinii
pneumonia, ear infections, bronchitis, gonorrhea,
etc.
Sulfonamides:
sulfisoxazole
Therapeutic Uses
Azo-Gantrisin
• Combined with phenazopyridine
• Used for UTIs

Pediazole
• Combined with erythromycin
• Used to treat otitis media
Sulfonamides: Side
Effects
Body System Effect
Blood Hemolytic and
aplastic anemia,
thrombocytopenia
Integumentary Photosensitivity,
exfoliative dermatitis, Stevens-
Johnson syndrome, epidermal
necrolysis
Sulfonamides: Side
Effects
Body System Effect
GI Nausea,
vomiting, diarrhea, pancreatitis
Other Convulsions,
crystalluria,
toxic nephrosis,
headache, peripheral neuritis,
urticaria
Antibiotics: Penicillins

• Natural penicillins
• Penicillinase-resistant
penicillins
• Aminopenicillins
• Extended-spectrum penicillins
Antibiotics: Penicillins

Natural penicillins
• penicillin G, penicillin V potassium

Penicillinase-resistant penicillins
• cloxacillin, dicloxacillin, methicillin,
nafcillin, oxacillin
Antibiotics: Penicillins

Aminopenicillins
• amoxicillin, ampicillin, bacampicillin

Extended-spectrum penicillins
• piperacillin, ticarcillin, carbenicillin,
mezlocillin
Antibiotics: Penicillins

• First introduced in the 1940s

• Bactericidal: inhibit cell wall
synthesis
• Kill a wide variety of bacteria
• Also called “beta-lactams”
Antibiotics: Penicillins

• Bacteria produce enzymes

capable of destroying
penicillins.

• These enzymes are known as

beta-lactamases.

• As a result, the medication is

not effective.
Antibiotics: Penicillins
• Chemicals have been
developed to inhibit these
enzymes:
• clavulanic acid
• tazobactam
• sulbactam
• These chemicals bind with
beta-lactamase and prevent
the enzyme from breaking
Antibiotics: Penicillins

• Penicillin-beta-lactamase inhibitor
combination drugs:

• ampicillin + sulbactam = Unasyn

• amoxicillin + clavulanic acid =

Augmentin

• ticarcillin + clavulanic acid =

Timentin

• piperacillin + tazobactam = Zosyn

Penicillins: Mechanism
of Action
• Penicillins enter the bacteria via the cell
wall.

• Inside the cell, they bind to penicillin-

binding protein.

• Once bound, normal cell wall synthesis is

disrupted.

• Result: bacteria cells die from cell lysis.

• Penicillins do not kill other cells in the

Penicillins: Therapeutic
Uses
• Prevention and treatment of
infections caused by
susceptible bacteria, such as:
• gram-positive bacteria
• Streptococcus, Enterococcus,
Staphylococcus species
Penicillins: Adverse
Effects
• Allergic reactions occur in 0.7%
– 8% of treatments
• urticaria, pruritus, angioedema
• 10% of allergic reactions are
life-threatening
and
• 10% of these are fatal
Penicillins: Side Effects

• Common side effects:

• nausea, vomiting, diarrhea,

abdominal pain

• Other side effects are less

common
Antibiotics:
Cephalosporins
• First Generation
• Second Generation
• Third Generation
• Fourth Generation
Antibiotics:
Cephalosporins
• Semisynthetic derivatives from a
fungus
• Structurally and pharmacologically
related
to penicillins
• Bactericidal action
• Broad spectrum
• Divided into groups according to their
antimicrobial activity
Cephalosporins: First
Generation
• cefadroxil
• cephalexin
• cephradine
• cefazolin
• cephalothin
• cephapirin
• Good gram-positive coverage
• Poor gram-negative coverage
Cephalosporins: First
Generation
cefazolin cephalexin
(Ancef and Kefzol) (Keflex and
Keftab)
IV and PO PO

used for surgical prophylaxis, URIs,

otitis media
Cephalosporins: Second
Generation
• cefaclor • cefonicid
• cefprozil • ceforanide
• cefamandole • cefmetazole
• cefoxitin • cefotetan
• cefuroxime

• Good gram-positive coverage

• Better gram-negative coverage than
first generation
Cephalosporins: Second
Generation
Cefoxitin cefuroxime
(Mefoxin) (Kefurox
and Ceftin)
IV and IM PO

Used prophylactically for

Surgical prophylaxis
abdominal or colorectal
surgeries Does not
kill
Cephalosporins: Third
Generation
• cefixime • ceftizoxime
• cefpodoxime proxetil • ceftriaxone
• cefoperazone • ceftazidime
• cefotaxime • moxalactam
• Most potent group against gram-
negative
• Less active against gram-positive
Cephalosporins: Third
Generation
cefixime (Suprax)
• Only oral third-generation agent
• Best of available oral cephalosporins
against
gram-negative
• Tablet and suspension

ceftriaxone (Rocephin)
• IV and IM, long half-life, once-a-day
dosing
• Easily passes meninges and diffused
into CSF
to treat CNS infections
 Cephalosporins: Third
Generation
ceftazidime (Ceptaz, Fortaz, Tazidime, Tazicef)

• IV and IM

• Excellent gram-negative coverage

• Used for difficult-to-treat organisms such as

Pseudomonas spp.

• Eliminated renally instead of biliary route

• Excellent spectrum of coverage

Cephalosporins: Fourth
Generation
cefepime (Maxipime)
• Newest cephalosporin agents.
• Broader spectrum of
antibacterial activity than
third generation, especially
against gram-positive bacteria.
Cephalosporins: Side
Effects
• similar to penicillins
Antibiotics:
Tetracyclines
• demeclocycline (Declomycin)
• oxytetracycline
• tetracycline
• doxycycline (Doryx, Doxy-Caps,
Vibramycin)
• minocycline
Antibiotics:
Tetracyclines
• Natural and semi-synthetic
• Obtained from cultures of
Streptomyces
• Bacteriostatic—inhibit bacterial
growth
• Inhibit protein synthesis
• Stop many essential functions
of the bacteria
Antibiotics:
Tetracyclines
• Bind to Ca2+ and Mg2+ and Al3+
ions to
form insoluble complexes
• Thus, dairy products, antacids,
and iron
salts reduce absorption of
tetracyclines
Tetracyclines:
Therapeutic Uses
• Wide spectrum:
• gram-negative, gram-positive,
protozoa, Mycoplasma, Rickettsia,
Chlamydia, syphilis, Lyme disease
• Demeclocycline is also used to
treat SIADH, and pleural and
pericardial effusions
Tetracyclines: Side
Effects
Strong affinity for calcium
• Discoloration of permanent teeth
and tooth
enamel in fetuses and children
• May retard fetal skeletal
development if taken
during pregnancy
Tetracyclines: Side
Effects
Alteration in intestinal flora may
result in:
• Superinfection (overgrowth of
nonsusceptible organisms such as
Candida)
• Diarrhea
• Pseudomembranous colitis
Tetracyclines: Side
Effects
May also cause:
• Vaginal moniliasis
• Gastric upset
• Enterocolitis
• Maculopapular rash
Antibiotics:
Aminoglycosides
• gentamicin (Garamycin)
• kanamycin
• neomycin
• streptomycin
• tobramycin
• amikacin (Amikin)
• netilmicin
Aminoglycosides
• Natural and semi-synthetic
• Produced from Streptomyces
• Poor oral absorption; no PO forms
• Very potent antibiotics with serious
toxicities
• Bactericidal
• Kill mostly gram-negative; some
gram-positive also
Aminoglycosides

• Used to kill gram-negative

bacteria such as
Pseudomonas spp., E. coli,
Proteus spp., Klebsiella
spp., Serratia spp.
• Often used in combination
with other antibiotics for
synergistic effect.
Aminoglycosides

• Three most common (systemic):

gentamicin, tobramycin, amikacin

• Cause serious toxicities:

• Nephrotoxicity (renal failure)

• Ototoxicity (auditory impairment

and vestibular [eighth cranial
nerve])

• Must monitor drug levels to prevent

toxicities
Aminoglycosides: Side
Effects
Ototoxicity and nephrotoxicity
are
the most significant
• Headache
• Paresthesia
• Neuromuscular blockade
• Dizziness
• Vertigo
• Skin rash
• Fever
Antibiotics: Quinolones

• ciprofloxacin (Cipro)
• enoxacin (Penetrex)
• lomefloxacin (Maxaquin)
• norfloxacin (Noroxin)
• ofloxacin (Floxin)
Quinolones

• Excellent oral absorption

• Absorption reduced by
antacids
• First oral antibiotics
effective against
gram-negative bacteria
Quinolones: Mechanism
of Action
• Bactericidal
• Effective against gram-
negative organisms and
some gram-positive
organisms
• Alter DNA of bacteria,
causing death
• Do not affect human DNA
Quinolones:
Therapeutic Uses
• Lower respiratory tract
infections
• Bone and joint infections
• Infectious diarrhea
• Urinary tract infections
• Skin infections
• Sexually transmitted
diseases
Quinolones: Side
Effects
Body System Effects
CNS headache,
dizziness, fatigue,
depression, restlessness
GI nausea,
vomiting, diarrhea,
constipation, thrush,
increased liver function
studies
Quinolones: Side
Effects
Body System Effects
Integumentary rash, pruritus,
urticaria, flushing,
photosensitivity (with
lomefloxacin)
Other fever, chills, blurred
vision, tinnitus
Antibiotics: Macrolides

• erythromycin
• azithromycin (Zithromax)
• clarithromycin (Biaxin)
• dirithromycin
• troleandomycin
• bactericidal action
 Instructors may wish to
insert
EIC Image #102:

Erythromycin Formulations
Macrolides:
Therapeutic Uses
Strep infections
• Streptococcus pyogenes
(group A beta-hemolytic
streptococci)

Mild to moderate URI

• Haemophilus influenzae

Spirochetal infections
• Syphilis and Lyme disease
Macrolides: Side
Effects
GI effects, primarily with erythromycin:

• nausea, vomiting, diarrhea, hepatotoxicity,

flatulence, jaundice, anorexia

• Newer agents, azithromycin and

clarithromycin: fewer side effects, longer
duration of action,
better efficacy, better tissue penetration
Antibiotics: Nursing
Implications
• Before beginning therapy, assess drug
allergies; hepatic, liver, and cardiac
function; and other lab studies.

• Be sure to obtain thorough patient

health history, including immune
status.

• Assess for conditions that may be

contraindications to antibiotic use, or
that may indicate cautious use.

• Assess for potential drug interactions.

Antibiotics: Nursing
Implications
• It is ESSENTIAL to obtain
cultures from appropriate
sites BEFORE beginning
antibiotic therapy.
Antibiotics: Nursing
Implications
• Patients should be instructed to take
antibiotics exactly as prescribed and
for the length of time prescribed; they
should not stop taking the medication
early when they feel better.

• Assess for signs and symptoms of

superinfection: fever, perineal
itching, cough, lethargy, or any
unusual discharge.
Antibiotics: Nursing
Implications
• For safety reasons, check the
name of the medication
carefully since there are many
agents that sound alike or have
similar spellings.
Antibiotics: Nursing
Implications
• Each class of antibiotics has specific
side effects and drug interactions that
must be carefully assessed and
monitored.

• The most common side effects of

antibiotics are nausea, vomiting, and
diarrhea.

• All oral antibiotics are absorbed

better if taken with at least 6 to 8
ounces of water.
Antibiotics: Nursing
Implications
Sulfonamides
• Should be taken with at least
2400 mL of fluid
per day, unless contraindicated.
• Due to photosensitivity, avoid
sunlight and
tanning beds.
• These agents reduce the
effectiveness of
oral contraceptives.
Antibiotics: Nursing
Implications
Penicillins
• Any patient taking a penicillin should be
carefully monitored for an allergic reaction
for at least 30 minutes after its
administration.

• The effectiveness of oral penicillins is

decreased when taken with caffeine, citrus
fruit, cola beverages, fruit juices, or tomato
juice.
Antibiotics: Nursing
Implications
Cephalosporins
• Orally administered forms should
be given with food to decrease
GI upset, even though this will
delay absorption.

• Some of these agents may cause

an Antabuse-like reaction when
taken with alcohol.
Antibiotics: Nursing
Implications
Tetracyclines
• Milk products, iron preparations,
antacids, and other dairy products
should be avoided because of the
chelation and drug-binding that
occurs.
• All medications should be taken with
6 to 8 ounces of fluid, preferably
water.
• Due to photosensitivity, avoid sunlight
and
tanning beds.
Antibiotics: Nursing
Implications
Aminoglycosides
• Monitor peak and trough blood levels
of these agents to prevent
nephrotoxicity and ototoxicity.
• Symptoms of ototoxicity include
dizziness, tinnitus, and hearing loss.
• Symptoms of nephrotoxicity include
urinary casts, proteinuria, and
increased BUN and serum creatinine
levels.
Antibiotics: Nursing
Implications
Quinolones
• Should be taken with at least 3 L of
fluid per day, unless otherwise
specified
Antibiotics: Nursing
Implications
Macrolides
• These agents are highly protein-
bound and will cause severe
interactions with other protein-bound
drugs.
• The absorption of oral erythromycin
is enhanced when taken on an empty
stomach, but because
of the high incidence of GI upset,
many agents
are taken after a meal or snack.
Antibiotics: Nursing
Implications
Monitor for therapeutic effects:
• Disappearance of fever,
lethargy, drainage, and redness