1 CHAPTER 9: ANTIBIOTICS

aerobic
anaerobic
antibiotic
gram-negative
gram-positive

o
o
o
o
o
o
o
o
o
o
o
o
o
o
o

synergistic
antibiotic
by living
microorganisms,
by synthetic
manufacture, and, in
some cases,
Through genetic
engineering.
Bacteriostatic
(preventing the
growth of bacteria)
Bactericidal (killing
bacteria directly)
Aminoglycosides
Carbapenems
Cephalosporins
Fluoroquinolones,
Penicillins and
Penicillinase-resistant
drugs,
Sulfonamides,
Tetracyclines,
Disease-specific
antimycobacterials,
Antitubercular
Leprostatic drugs.
Ketolides,
Lincosamides,
lipoglycopeptides,
Macrolides, and
monobactams.
Gram-positive

Streptococcus
pneumonia
gram-negative
synergistic

bacteria that depend on oxygen for survival

bacteria that survive without oxygen, which are often seen when blood flow
is cut off to an area of the body
chemical that is able to inhibit the growth of specific bacteria or cause the
death of susceptible bacteria
bacteria that accept a negative stain and are frequently associated with
infections of the genitourinary or GI tract
bacteria that take a positive stain and are frequently associated with
infections of the respiratory tract and soft tissues
drugs that work together to increase drug effectiveness
Chemicals that inhibit specific bacteriato deal with each new threat.
Antibiotics are made in three ways:

Antibiotics may either be_.

major classes of antibiotics:

Antibiotics that do not fit into the large

antibiotic classes include_

_bacteria are those whose cell wall retains a stain known as Grams stain or
resists decolorization
with alcohol during culture and sensitivity testing.
An example of a gram-positive bacterium is_ a common cause of pneumonia
_bacteria are those whose cell walls lose a stain or are decolorized by
alcohol.
In some cases, antibiotics are given in combination because they are_,
meaning their combined effect is greater than their effect if they are given
individually

AMINOGLYCOSIDES
aminoglycosides
adverse effects

o Amikacin (Amikin),
gentamicin
(Garamycin),
o Kanamycin (Kantrex),
neomycin
(Mycifradin),
streptomycin
(generic),
tobramycin (TOBI,
Tobrex).

The_are a group of powerful antibiotics used to treat serious infections

caused by gram-negative aerobic bacilli.
Because most of these drugs have potentially serious_ , newer, less-toxic
drugs have replaced aminoglycosides in the treatment of less serious
infections.
Aminoglycosides include:

2 CHAPTER 9: ANTIBIOTICS
Therapeutic Actions and Indications
bactericidal
penicillin

The aminoglycosides are_.

Aminoglycosides are indicated for the treatment of serious infections that are
susceptible to_.

Pharmacokinetics
GI tract, 1 hour

The aminoglycosides are poorly absorbed from the _but rapidly absorbed
after intramuscular (IM) injection, reaching peak levels within_.
2 to 3 hours
These drugs have an average half-life of_.
DRUGS IN FOCUS Aminoglycosides
amikacin (Amikin)
gentamicin (Garamycin
kanamycin (Kantrex)
neomycin (Mycifradin)
streptomycin (generic)

tobramycin (TOBI, Tobrex)

Treatment of serious gram-negative infections

Treatment of Pseudomonas infections and a wide variety of gram-negative infections
Treatment of hepatic coma and to decrease gastrointestinal (GI) normal fl ora
Suppression of GI normal fl ora preoperatively; treatment of hepatic coma; topical
treatment of skin wounds
Fourth drug in combination therapy regimen for treatment of tuberculosis; treatment of
severeinfections if the organism has been shown to be sensitive to streptomycin and no
less-toxic drugs can be used
Short-term IV or IM treatment of serious infections; ocular infections caused by susceptible
bacteria; nebulizer management of cystic fibrosis and P. aeruginosa infections

Contraindications and Cautions

Renal or hepatic
disease
o Preexisting hearing
loss,
o Active infection with
herpes or
mycobacterial
infections
o Myasthenia gravis
or
o Parkinsonism
nephrotoxicity and
ototoxicity
7 to 10 days
o

Aminoglycosides are contraindicated in the following

conditions

The potential for _with amikacin is very high, so the drug is used only as long
as absolutely necessary.
Do not use kanamycin for longer Than_, because of its potential toxic effects,
which include renal damage, bone marrow depression, and GI complications.

Adverse Effects
ototoxicity and
nephrotoxicity

The drugs come with a black box warning alerting health care professionals
to
the serious risk of_.

CARBAPENEMS
carbapenems

The_ are a relatively new class of broad-spectrum antibiotics effective

against grampositive and gram-negative bacteria.

Therapeutic Actions and Indications

bactericidal
The carbapenems are _.
DRUGS IN FOCUS Carbapenems
doripenem (Doribax)
ertapenem (Invanz)
imipenem
cilastatin(Primaxin)

meropenem (Merrem IV)

Treatment of complicated intra-abdominal infections or complicated UTIs, including

pyelonephritis, caused by susceptible bacteria
Treatment of community-acquired pneumonia,complicated genitourinary infections, acute
pelvic infections, complicated intra-abdominal infections, skin and skin-structure infections
Treatment of serious respiratory, intra-abdominal, urinary tract, gynecological, bone and
joint, skin and
skin-structure infections; septicemia, endocarditis, bone and joint infections, and
polymicrobic infections
Treatment of bacterial meningitis, complicated skin and skin-structure infections, intraabdominal infections

Pharmacokinetics
IM
1 to 4 hours

These drugs are rapidly absorbed if given_ and reach peak levels at the end
of the infusion if given IV.
Carbapenems are excreted unchanged in the urine and have an average halflife of _

Contraindications and Cautions

o Known allergy to any
of the carbanems or
beta-lactams
o Seizure disorders and
lactation,
o Use caution during
pregnancy
o Test urine function

Carbapenems are contraindicated in the following conditions:

3 CHAPTER 9: ANTIBIOTICS
regularly when these
drugs are used
18 years

Ertapenem is not recommended for use in patients younger than _of age.

Adverse Effects
GI tract

Toxic effects on the _can limit the use of carbapenems in some patients.

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
DRUGS IN FOCUS Cephalosporins

First-Generation Cephalosporins
cefadroxil (generic)
cefazolin (Zolicef)
cephalexin (Kefl ex)

Treatment of UTIs, pharyngitis, and tonsillitis caused by group A betahemolyticstreptococci, as well as skin infections
Treatment of respiratory tract, skin, genitourinary (GU), biliary tract, bone, joint, and
myocardial infections, as well as sepsis
Treatment of respiratory, skin, bone, and GU infections; used for otitis media in children

Second-Generation Cephalosporins
cefaclor (Ceclor
cefoxitin (generic

cefprozil (generic)
cefuroxime (Zinacef)

Treatment of respiratory tract infections, skin infections, UTIs, otitis media, typhoid fever,
anthrax exposure
Treatment of severe infections; preoperative prophylaxis for cesarean section and
abdominal, vaginal, biliary or colorectal surgery; more effective in gynecological and intraabdominal infections than some
other agent
Treatment of pharyngitis, tonsillitis, otitis media, sinusitis, secondary bronchial infections,
and skin infections
Treatment of a wide range of infections, as listed for other second-generation drugs;
Lyme disease; preferred treatment in situations involving an anticipated switch from
parenteral to oral drug use

Third-Generation Cephalosporins
cefdinir (generic; a
suspension form is
available for children
cefotaxime (Claforan)

cefpodoxime (Vantin)
ceftazidime (Ceptaz,
Tazicef)
ceftibuten (Cedax;
available in a suspension
form for children)
ceftizoxime (Cefi zox)
Adult: 500
ceftriaxone (Rocephin)

Treatment of respiratory infections, otitis media, sinusitis, laryngitis, bronchitis, skin

infections
Treatment of moderate to severe skin,urinary tract, and respiratory tract infections; pelvic
infl ammatory disease;intra-abdominal infections; peritonitis; septicemia; bone infections;
central nervous system (CNS) infections; preoperative prophylaxis
Treatment of respiratory infections, UTIs, gonorrhea, skin infections, and otitis media
Treatment of moderate to severe skin, urinary tract, and respiratory tract infections;intraabdominal infections; septicemia; bone infections; CNS infections
Treatment of pharyngitis, tonsillitis, exacerbations of bronchitis, otitis media

Treatment of respiratory, gynecological, pelvic inflammatory, intra-abdominal, skin, and

bone and joint infections; also used for sepsis and meningitis
Treatment of moderate to severe skin, urinary tract, and respiratory tract infections; pelvic
infl ammatory disease; intra-abdominal infections; peritonitis; septicemia; bone infections;
CNS infections; preoperative prophylaxis; off-label use for treatment of Lyme disease

Fourth-Generation Cephalosporins
cefditoren (Spectracef)
cefepime (Maxipime)
ceftaroline (Tefl aro)gtttty

Treatment of acute exacerbations of chronic bronchitis; pharyngitis and tonsillitis; skin and
skin-structure infections
Treatment of moderate to severe skin, urinary tract, and respiratory tract infections
Treatment of skin and skin-structure infections; community-acquired pneumonia

Contraindications and Cautions

Hepatic or renal
impairment In
addition, use with
caution in pregnant or
lactating

Use with caution in patients with:

Adverse Effects
GI tract and include
nausea, vomiting,
diarrhea, anorexia,
abdominal pain, and
flatulence and
Pseudomembranous
colitis

The most common adverse effects of the cephalosporins

involve the_.

FLUOROQUINOLONES
fluoroquinolones

The _are a relatively newsynthetic class of antibiotics with a broad spectrum

of activity.
DRUGS IN FOCUS Fluoroquinolones
ciprofloxacin (Cipro)
gemifloxacin (Factive)

Treatment of infections caused by a wide spectrum of gram-negative bacteria

Treatment of acute exacerbations of chronic bronchitis, community-acquired pneumonia

4 CHAPTER 9: ANTIBIOTICS
levofloxacin (Levaquin)
moxifloxacin (Avelox)
norfloxacin (Noroxin)
ofloxacin (Floxin, Ocufl ox)

Treatment of respiratory, urinary tract, skin, and sinus infections caused by susceptible
gram-negative bacteria in adults; treatment after exposure to anthrax
Treatment of adults with sinusitis, bronchitis, or community-acquired pneumonia
Treatment of various urinary tract infections
Treatment of respiratory, skin, and urinarytract infections; pelvic infl ammatory
disease;ocular infections; otic form available for otitis media

Therapeutic Actions and Indications

passive diffusion

The fluoroquinolones enter the bacterial cell by _through channels in the cell
membrane.

Pharmacokinetics
GI tract

The fluoroquinolones are absorbed from the_, metabolized in the liver, and
excreted in the urine and feces.

Contraindications and Cautions

renal dysfunction

Use with caution in the presence of_

Adverse Effects
Headache
Dizziness
insomnia
depression related to
possible
o effects on the CNS
membranes.
o
o
o
o

These drugs are generally associated with relatively mild

adverse reactions. The most common are_

PENICILLINS AND PENICILLINASE RESISTANT ANTIBIOTICS

Therapeutic Actions and Indications
bactericidal

The penicillins and penicillinase-resistant antibiotics produce _effects by

interfering with the ability of susceptible bacteria to build their cell walls
when they are dividing
DRUGS IN FOCUS Immune SeraPenicillins and Penicillinase-Resistant Antibiotics
Penicillins
penicillin G benzathine
(Bicillin,
Permapen)
penicillin G potassium (Pfi
zerpen)
penicillin G procaine
(Wycillin)
penicillin V (Veetids)

Severe infections caused by sensitive organisms;

treatment of syphilis and erysipeloid
infections
Treatment of severe infections; used for
several days in some cases
Treatment of moderately severe infections
daily for 812 d
Used for prophylaxis for bacterial endocarditis;
Lyme disease, urinary tract infections

Extended-Spectrum Penicillins
amoxicillin (Amoxil,
Trimox)
ampicillin (Principen

nafcillin

oxacillin

Broad spectrum of uses for adults and children

Broad spectrum of activity; useful form if
switch from parenteral to oral is anticipated;
monitor for nephritis
Infections by penicillinase-producing
staphylococci as well as group A hemolytic
streptococci, plus Streptococcus viridans;
drug of choice if switch to oral form is
anticipated
Infections by penicillinase-producing staphylococci;
streptococci; drug of choice if
switch to oral form is anticipated

Pharmacokinetics
1 hour

Most of the penicillins are rapidly absorbed from the GI

tract, reaching peak levels in_.

Contraindications and Cautions

renal disease

Use with caution in patients with _Although there are no adequate studies of
use during pregnancy, use in patients who are pregnant and in lactating
patients should be limited to situations in which the mother clearly would
benefit from the drug

Adverse Effects
o
o
o
o
o
o
o
o
o

Nausea,
Vomiting
Diarrhea
Abdominal pain
Glossitis
Stomatitis
Gastritis
sore mouth
And furry tongue.

The major adverse effects of penicillin therapy involve the GI tract. Common
adverse effects include _

5 CHAPTER 9: ANTIBIOTICS

SULFONAMIDES
sulfonamides

The_, or sulfa drugs , are drugs that inhibit folic acid synthesis.

Therapeutic Actions and Indications

RNA and DNA

Folic acid is necessary for the synthesis of purines and pyrimidines, which are
precursors of_.
DRUGS IN FOCUS Sulfonamides
sulfadiazine (generic)
sulfasalazine (Azulfi dine)
cotrimoxazole (Septra,
Bactrim)

Treatment of a broad spectrum of

infections
Treatment of ulcerative colitis and Crohns
disease; rheumatoid arthritis
Treatment of otitis media, bronchitis,
urinary tract infections, and pneumonitis
caused by P. carinii

Pharmacokinetics
teratogenic
3 to 6 hours

The sulfonamides are_; they are distributed into breast milk

Sulfadiazine is an oral agent slowly absorbed from the GI tract, reaching peak
levels in_.

Contraindications and Cautions

allergy to any
sulfonamide, to
sulfonylureas, or to
thiazide diuretics
during pregnancy and
during lactation
Renal disease or a
history of kidney
stone

The sulfonamides are contraindicated with any known_.

They should be used with caution in patients with _

Adverse Effects
nausea, vomiting,
diarrhea, abdominal
pain, anorexia,
stomatitis, and
hepatic injury, which
are all related to direct
irritation of the GI
tract and the death of
normal bacteria

Adverse effects associated with sulfonamides include GI effects such as_

TETRACYCLINES
tetracyclines
high concentrations

The _work by inhibiting protein synthesis in a wide range of bacteria, leading

to the inability of the bacteria to multiply
Because the affected protein is similar to a protein found in human cells,
these drugs can be toxic to humans at_.

Pharmacokinetics
GI tract
12 to 25 hours

Tetracyclines are absorbed adequately, but not completely, from the_.

Tetracyclines are concentrated in the liver and excreted unchanged in the
urine, with half-lives ranging from_.
DRUGS IN FOCUS Tetracyclines
Demeclocycline
(Declomycin)
doxycycline (Doryx,
Periostat)
minocycline (Minocin)

Tetracycline (Sumycin)

Treatment of a wide variety of infections when penicillin cannot be used

Treatment of a wide variety of infections, including travelers diarrhea and sexually
transmitted diseases; periodontal disease
Treatment of meningococcal carriers and of various uncomplicated genitourinary and
gynecological
infections
Treatment of a wide variety of infections when penicillin is contraindicated, including acne
vulgaris and minor skin infections caused by susceptible organisms

Contraindications and Cautions

Allergy,pregnancy an
lactyation

Tetracyclines are contraindicated in patients with known _to tetracyclines or

to tartrazine and during _.

Adverse Effects
nausea, vomiting,
diarrhea, abdominal
pain, glossitis, and
dysphagia.

The major adverse effects of tetracycline therapy involve direct irritation of

the GI tract and include

ANTIMYCOBACTERIALS
Mycobacteria

the group of bacteria that contain the pathogens that cause tuberculosis and
leprosyare
classified on the basis of their ability to hold a stain even in the presence of a

6 CHAPTER 9: ANTIBIOTICS
destaining agent such as acid.

ANTITUBERCULOSIS DRUGS

o
o
o
o
o
o
o
o
o
o

are
The first-line drugs for treating tuberculosis_
isoniazid(Nydrazid),
rifampin (Rifadin),
pyrazinamide
(generic),
ethambutol
(Myambutol),
streptomycin
(generic), and
rifapentine (Priftin).
DRUGS IN FOCUS Antimycobacterials
Isoniazid(Nydrazid)
Treatment of M. tuberculosis
Rifampin (Rifadin)
Pyrazinamide
(generic)
Ethambutol
(Myambutol)
Streptomycin
(generic)
And Rifapentine
(Priftin)
Ethionamide(Trecator- Second-line treatment of M. tuberculosis
SC)
Capreomycin(Capasta
t)
Cycloserine
(Seromycin)
Rifabutin (Mycobutin)
dapsone (generic)

Treatment of leprosy

LEPROSTATIC DRUGS
dapsone (generic)

The antibiotic used to treat leprosy is_, which has been the mainstay of
leprosy treatment for
many years, although resistant strains are emerging

Therapeutic Actions and Indications

antimycobacterial
agents

Most of the _act on the DNA and/or RNA of the bacteria, leading to a lack of
growthand eventually to bacterial death

Pharmacokinetics
GI tract

The antimycobacterial agents are generally well absorbed from the_.

Contraindications and Cautions

known allergy to these
agents; in those with
severe
renal or hepatic
failure,
in those with severe
CNS dysfunction,
and in pregnancy

Antimycobacterials are contraindicated for patients with any_

.

Adverse Effects
CNS effects, such as
neuritis, dizziness,
headache, malaise,
drowsiness, and
hallucinations

_are often reported and are related to direct effects of the drugs on neurons.

OTHER ANTIBIOTICS
ketolides,
lincosamides,
lipoglycopeptides,
macrolides, and
monobactams

There are other antibiotics that do not fi t into the large antibiotic classes
These drugs are_

KETOLIDES
ketolide

The _class of antibiotics was first introduced in 2004

Therapeutic Actions and Indications

protein synthesis

The ketolides block _within susceptible bacteria, leading to cell death, which

7 CHAPTER 9: ANTIBIOTICS
makes them structurally related to the macrolide antibiotics

Pharmacokinetics
1 hour
It is rapidly absorbed through the GI tract, reaching peak levels in_.
DRUGS IN FOCUS Other Antibiotics
Ketolide
telithromycin (Ketek

Treatment of mild to moderate community-acquired pneumonia caused by susceptible

bacteria

Lincosamides
clindamycin (Cleocin
lincomycin (Lincocin

Treatment of severe infections when penicillin or other, less toxic antibiotics cannot be
used
Treatment of severe infections when penicillin or other less toxic antibiotics cannot be used

Lipoglycopeptides
televancin (Vibativ

Treatment of complicated skin and skin-structure infections

Macrolides
azithromycin (Zithromax)

clarithromycin (Biaxin
erythromycin

Treatment of mild to moderate respiratory infections and urethritis in adults and otitis
media and
pharyngitis/ tonsillitis in children
Treatment of various respiratory, skin, sinus, and maxillary infections; effective against
mycobacteria
Treatment of infections in patients allergic to penicillin

Monobactam
aztreonam (Azactam)

Treatment of gram-negative enterobacterial infections

Contraindications and Cautions

congenital prolonged
QT interval,
bradycardia, or any
proarrhythmic
condition such as
hypokalemia
with concurrent use of
pimozide, cardiac
antiarrhythmics,simva
statin,
atorvastatin, or
lovastatin
and with myasthenia
gravis, which is a
black box warning
with this drug.

with known_

Adverse Effects
nausea, vomiting,
taste alterations, and
the potential for
pseudomembranous
colitis

The adverse effects associated with telithromycin are largely secondary to

toxic effects on the GI tract:_

LINCOSAMIDES
lincosamides

The _ are similar to the macrolides but are more toxic.

Therapeutic Actions and Indications

lincosamides

The_ react at almost the same site in bacterial protein synthesis and are
effective against the same
strains of bacteria

Pharmacokinetics
2 to 3 hours, 5 hours

Clindamycin has a half-life of_.

Lincomycin has a half-life of_. It can be givenorally, IM, or IV.

Contraindications and Cautions

hepatic or renal
impairment

Use lincosamides with caution in patients with_

Adverse Effects
Severe GI reactions,
including fatal
pseudomembranous
colitis

_have occurred, limiting the usefulness of lincosamides.