PENICILLINS CEPHALOSPORINS FLUOROQUINOLONES AMINOGLYCOSIDES MONOBACTAMS CARBAPENEMS MACROLIDES

Antibiotic Grouping By Mechanism

Natrual
Penicillin G
Penicillin-VK

Penicillinase
Resistant
Methicillin
Nafcillin
Oxacillin
other

Cell Wall Synthesis

First generation
Ciprofloxacin (Cipro)
Levofloxacin
(Levaguin)
Cephalothin
Moxifloxacin (Avelox)
Cefazolin (Ancef, Norfloxacin
Kefzol)
Cephapririn
Cephalexin
(Keflex) Protein Synthesis Inhibitors
other

Penicillins
Amikacin
Aztreonam
Cephalosporins
Gentamicin
Vancomycin
Kanamycin
Beta-lactamase Inhibitors
Neomycin
Carbapenems
Tobramycin
Aztreonam
Polymycin
Bacitracin

Ertapenem
Imienem
Meropenem

Azithromycin Vancomycin
Clarithromyci Rifampin
n
Doxycycline
Dirithromycin Linezolid
Erythromycin Tetracycline
Clindamycin Trimethoprim/
sulfamethoxac
ole

Inhibit 30s Subunit

Aminoglycosides (gentamicin)
Tetracyclines
Inhibit 50s Subunit
Macrolides
Chloramphenicol
Clindamycin
Linezolid
Streptogramins

Second
Generation
Cefacor
Cefotetan
(Cefotan)
other

Aminopenicilli Third Generation

ns
DNA Synthesis Inhibitors
Ampicillin
Ceftriaxone
(Rocephin)
RNA synthesis Inhibitors
other

Fluoroquinolones
Metronidazole
Rifampin

Mycolic Acid synthesis inhibitors

Fourth
Generation
Folic Acid synthesis inhibitors
Cefpirome
Cefepime

Isoniazid
Sulfonamides
Trimethoprim

Antibiotic Classification & Indications

Inhibits Cell Wall Synthesis
Penicillins
(bactericidal: blocks cross linking via competitive inhibition of the transpeptidase enzyme)
Class/Mechanism

Drugs

Indications (**Drug of
Choice)

OTHER

Toxicity

Penicillin

Aminopenicillins

Penicillin G
Aqueous penicillin G
Procaine penicillin G
Benzathine penicillin G
Penicillin V

Ampicillin
Amoxicillin

Strep. pyogenes
(Grp.A)**
Step. agalactiae
(Grp.B)**
C.
perfringens(Bacilli)**

Hypersensitivity
reaction
Hemolytic anemia

Above
Above +
Gram-negative:
E. faecalis**
E. Coli**

Penicillinaseresistant-penicillins

Methicillin
Nafcillin
Oxacillin
Cloxacillin
Dicloxacillin

Above +
PCNaseproducingStaph.
aureus

Antipseudomonal
penicillins

Carbenicillin
Ticarcillin
Piperacillin

Above +
Pseudomonas
aeruginosa**

Above +
Interstitial
nephritis

Above

Cephalosporins
(bactericidal: inhibits bacterial cell wall synthesis via competitive inhibition of the
transpeptidase enzyme)
1st
generation

Cefazolin
Cephalexin

Staph. aureus**
Allergic reaction
Staph. epidermidis** Coombs-positive
Some Gram-negatives: anemia (3%)
E. Coli
Klebsiella

2nd generation

Cefoxitin
Cefaclor
Cefuroxime

Above +
Gram-negative

Allergic Reaction
ETOH Disulfiram
reaction

3rd generation

Ceftriaxone
Cefotaxime
Ceftazidime
Cefepime (4th
generation)

Above +
Gram-negative
Pseudomonas

Allergic Reaction
ETOH Disulfiram
reaction

Other Cell Wall Inhibitors

Vancomycin

Vancomycin
MRSA**
PCN/Ceph allegies**
S. aureus
S. epidermidis

(bactericidal: disrupts
peptioglycan crosslinkage)
Beta-lactamase
Inhibitors

Clavulanic Acid
Sulbactam
Tazobactam

(bactericidal: blocking
cross linking)

S aureus**
S epidermis**
E.Coli**
Klebsiella**

Carbapenems

Imipenem (+ cilastatin)
Meropenem
Doripenem
Ertapenem

Broadest activity of
any antibiotic
(except MRSA,
Mycoplasma)

Aztreonam

Aztreonam

Gram-negative rods
Aerobes
Hospital-acquired
infections

Polymyxins

Polymyxin B
Polymyxin E

Topical Gram-negative
infections

Bacitracin

Bacitracin

Topical Gram-positive
infections

Red man
syndrome
Nephrotoxicity
Ototoxicity

Hypersensitivity
Reaction
Hemolytic anemia

Protein Synthesis Inhibition

Anti-30S ribosomal subunit
Aminoglycosides
(bactericidal:
irreversible binding to

Gentamicin
Neomycin
Amikacin
Tobramycin

Aerobic Gramnegatives
Enterobacteriaceae
Pseudomonas

Nephrotoxicity
Ototoxicity

30S)

Streptomycin

Tetracyclines
(bacteriostatic: blocks
tRNA)

Tetracycline
Doxycycline
Minocycline
Demeclocycline

Rickettsia
Mycoplasma
Spirochetes (Lyme's
disease)

Hepatotoxicity
Tooth
discoloration
Impaired growth
Avoid in children
< 12 years of age

Anti-50S ribosomal subunit

Macrolides
(bacteriostatic:
reversibly binds 50S)

Erythromycin
Azithromycin
Clarithromycin

Streptococcus
H. influenzae
Mycoplamsa
pneumonia

Chloramphenicol
(bacteriostatic)

Chloramphenicol

H influenzae
Bacterial Meningitis
Brain absces

Aplastic Anemia
Gray Baby
Syndrome

Bacteroides fragilis
S aureus
Coagulase-negative
Staph & Strep
Excellent Bone
Penetration

Pseudomembrano
us colitis
Hypersensitivity
Reaction

Lincosamide
Clindamycin
(bacteriostatic: inhibits
peptidyl transferase by
interfering with amino
acyl-tRNA complex)

Linezolid
(variable)

Linezolid

Resistant Grampositives

Streptogramins

Quinupristin
Dalfopristin

VRE
GAS and S. aureus skin
infections

Coumadin
Interaction
(cytochrome
P450)

DNA Synthesis Inhibitors

Fluoroquinolones
(bactericidal: inhibit DNA gyrase enzyme, inhibiting DNA synthesis)

1st
generation

Nalidixic acid

Steptococcus
Mycoplasma
Aerobic Gram +

2nd generation

Ciprofloxacin
Norfloxacin
Enoxacin
Ofloxacin
Levofloxacin

As Above
+Pseudomonas

as above

3rd generation

Gatifloxacin

As above + Grampositives

as above

4th generation

Moxifloxacin
Gemifloxacin

As above + Gramas above

positives + anaerobes

Phototoxicity
Achilles tendon
rupture
Impaired fracture
healing

Other DNA Inhibitors

Metronidazole
Metronidazole (Flagyl)
(bacteridical: metabolic
biproducts disrupt DNA)

Anaerobics

Seizures
Crebelar
dysfunction
ETOH disulfram
reaction

RNA Synthesis Inhibitors

Rifampin
(bactericidal: inhibits
RNA transcription by
inhibiting RNA
polymerase)

Rifampin

Staphylococcus
Mycobacterium (TB)

Mycolic Acids Synthesis Inhibitors

Isoniazid

Isoniazidz

TB
Latent TB

Folic acid Synthesis Inhibitors

Body fluid
discoloration
Hepatoxicity (with
INH)

Trimethoprim/Sulfona Trimethoprim/Sulfametho UTI organisms

mides
xazole (SMX)
Proteus
(bacteriostatic:
Sulfisoxazole
Enterobacter
inhibition with PABA)
Sulfadiazine

Pyrimethamine

Pyrimethamine

Malaria
T. gondii

Bacteria Overview
Gram Postive Cocci
Staphylococcus

Staph. aureus
MSSA
MRSA
Staph. epidermis
Staph saprophyticus

Streptococcus

Strep
Strep
Strep
Strep
Strep

Enterococci

E. faecalis (Group D strep)

pneumoniae
pyogenes (Group A)
agalacticae (Group B)
viridans
Bovis (Group D)

Gram Positive Bacilli

Spore Forming
Bacillus anthracis
Bacillus cereus
Clostridium tetani
Clostridium botulinum

Thrombocytopenia
Avoid in third
trimester of
pregnancy

Clostridium perfringens
Clostridium difficile
Non-Spore Forming

Corynebacterium diphtheriae
Listeria monocytogenes
Gram Negative Cocci

Neisseria

Neisseria meningitidis
Neisseria gonorrhoeae
Gram Negative Bacilli

Enterics

Escherichia coli
Salmonella typhi
Salmonella enteridis
Shigella dysenteriae
Klebsiella pneumoniae
Serratia
Proteus
Campylobacter jejuni
Vibrio cholerae
Vibrio parahaemolyticus/vulnificus
Helicobacter pylori
Pseudomonas aeruginosa
Bacteroides fragilis

Respiratory bacilli

Haemophilus influenzae
Haemophilius ducreyi
Bordatella pertussis

Zoonotic bacilli

Yersinia enterocolitica
Yersinia pestis
Brucella
Francisella tularensis
Pasteurella multocida
Bartonella henselae

Other

Gardnerella vaginalis
Other Bacteria

Mycobacteria

Mycobacterium tuberculosis
Mycobacterium leprae
MOTTS

Spirochetes

Borrelia burgdorferi
Leptospira interrogans
Treponema pallidum

Chlamydiaceae

Chlamydia trachomatis
Chlamydophila
Rickettsia
Ehrlichia

Mycoplasmataceae

Mycoplasma pneumoniae
Ureaplasma urealyticum

Fungus-like Bacteria

Actinomyces israelii
Nocardia

Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze these drugs using lactamase

o confers resistance to penicillin
o e.g. E. coli, Staph epidermidis, Pseudomonas aeruginosa, Klebsiella pneumoniae
o add lactamase inhibitor e.g. clavulanic acid in amoxicillin-clavulanate (Augmentin)

Genetic mutation of mecA

o a bacterial gene encoding a penicillin-binding protein. New PBP has reduced affinity for antibiotics
o confers resistance to methicillin, oxacillin, nafcillin
o e.g. MRSA

Altered cell wall permeability

o confers resistance to tetracyclines, quinolones, trimethoprim and lactam antibiotics

Creation of biofilm barrier

o provides an environment where offending bacteria can multiply safe from the hoste immune system

Salmonella

Staph epidermidis

Active efflux pumps

o confers resistance to erythromycin and tetracycline
o e.g. msrA gene in Staph

Altered peptidoglycan subunit (altered D-alanyl-D-alanine of NAM/NAG-peptide)

o confers resistance to vancomycin
o e.g. vancomycin resistant enterococcus (VRE)

Ribosome alteration
o erm gene confer inducible resistance to MLS (macrolide lincosamide streptogranin) agents via
methylation of 23s rRNA
o demonstrate using D zone test

for inducible clindamycin resistance in Staph and beta hemolytic Strep

Penicillins

Mechanism
o interfer with bacterial cell wall synthesis

Subclassification and tested examples

o natural

penicillin G

o penicillinase-resistant

methicillin (Staphcillin)

o aminopenicillins

ampicillin (Omnipen, Polycillin)

Cephalosporins

Overview
o bactericidal

Mechanism
o disrupts the synthesis of the peptidoglycan layer of bacterial cell walls

does so through competitive inhibition on PCB (penicllin binding proteins)

peptidoglycan layer is important for cell wall structural integrity.

o same mechanicsm of action as beta-lactam antibiotics (such as penicillins)

Subclassification and tested examples

o first generation

cefazolin (Ancef, Kefzol)

o second generation

cefaclor (Ceclor)

o third generation

cefriazone (Rocephin)

o fourth generation

cefepime (Maxipime)

Fluoroquinolones

Mechanism
o blocks DNA replication via inhibition of DNA gyrase

Side effects
o inhibit early fracture healing through toxic effects on chondrocytes
o increased rates of tendinitis, with special predilection for the Achilles tendon.

tenocytes in the Achilles tendon have exhibited degenerative changes when viewed
microscopically after fluoroquinolone administration.

recent clinical studies have shown an increased relative risk of Achilles tendon rupture of 3.7.

Subclassification and tested examples

o ciprofloxacin (Cipro)
o levofloxacin (Levaquin)

Aminoglycosides

Mechanism
o bactericidal
o inhibition of bacterial protein synthesis

work by binding to the 30s ribosome subunit, leading to the misreading of mRNA. This
misreading results in the synthesis of abnormal peptides that accumulate intracellularly and
eventually lead to cell death. These antibiotics arebactericidal.

Subclassification and tested examples

o gentamicin (Garamycin)

Vancomycin

Coverage
o gram-positive bacteria

Mechanism
o bactericidal
o an inhibitor of cell wall synthesis

Resistance
o increasing emergence of vancomycin-resistant enterococci has resulted in the development of
guidelines for use by the (CDC)
o indications for vancomycin

serious allergies to penicillins or beta-lactam antimicrobials

serious infections caused by susceptible organisms resistant to penicillins (MRSA, MRSE)

surgical prophylaxis for major procedures involving implantation of prostheses in institutions with
a high rate of MRSA or MRSE

Rifampin

Most effective against intracellular phagocytized Staphylococcus aureus in macrophages

Linezolid

Linezolid binds to the 23S portion of the 50S subunit and acts by preventing the formation of the initiation
complex between the the 30S and 50S subunits of the ribosome.

Splenectomy

Splenectomy patients or patients with functional hyposplenism require the following vaccines and/or
antibiotics

o Pneumococcal immunization
o Haemophilus influenza type B vaccine
o Meningococcal group C conjugate vaccine
o Influenza immunization
o Lifelong prophylactic antibiotics (oral phenoxymethylpenicillin or erythromycin)

Systemic Adverse Effects of Common Antibiotics and Classes

Antibiotic Class

Antibiotic Class Members

Most Common Side Effects

Additional Clinical Comments

Penicillins

penicillin, amoxicillin, amoxicillinrash, diarrhea, abdominal pain,

clavulanate, ampicillin, piperacillin- nausea/vomiting, drug fever, hypersensitivity
tazobactam, nafcillin, oxacillin
(allergic) reactions

if bloody stools, anaphylaxis, severe skin reaction,

fever occur contact health care provider
immediately; ampicillin may cause
pseudomembranous colitis

Cephalosporins

cephalexin, cefaclor, cefuroxime,

ceftibuten, cefdinir, cefixime,
ceftriaxone

rash, diarrhea, nausea/vomiting (rare),

hypersensitivity (allergic) reactions, serum
sickness, vaginal candidiasis

cross-hypersensitivity may occur in patients with

documented penicillin allergy

Aminoglycoside
s

gentamicin, tobramycin, amikacin

renal (kidney) toxicity, ototoxicity (hearing

loss), dizziness, nausea/vomiting, nystagmus

longer or multiple treatment periods may lead to

greater risk for ototoxicity, renal (kidney) toxicity

Carbapenems

meropenem, ertapenem,
doripenem, imipenem-cilastatin

diarrhea, nausea/vomiting, headache, rash,

Hypersensitivity reactions reported with
liver toxicity, eosinophilia (elevated white blood meropenem, imipenem in patients with penicillin

cells)

allergy

Antituberculosis
Agents

rifampin, rifabutin, isoniazid,

pyrazinamide, ethambutol,
dapsone

diarrhea, nausea/vomiting, anorexia,

hemolytic anemia, liver toxicity, headache,
peripheral neuropathy, dizziness, reddishorange body fluids (rifampin, rifabutin only)

sides effects vary among agents, check

individually; vitamin B6 (pyridoxine) may be taken
to help prevent peripheral neuropathy with isoniazid

Glycopeptides

vancomycin, telavancin

vancomycin: red man syndrome (flushing,

hypotension, itching); phlebitis; telavancin:
taste alteration, nausea/vomiting, headache,
dizziness

IV infusion of vancomycin over 60 minutes may

prevent red man syndrome

Macrolides

erythromycin, azithromycin,
clarithromycin

abdominal pain, diarrhea, anorexia,

nausea/vomiting, taste alterations
(clarithromycin)

high rate of gastrointestinal side effects; do not

crush, chew, break, open enteric-coated or
delayed-release pill

Sulfonamides

trimethoprin-sulfamethoxazole,
erythromycin-sulfisoxazole,
sulfadiazine

nausea/vomiting, diarrhea, anorexia,

abdominal pain, rash, photosensitivity,
headache, dizziness

Avoid prolonged sunlight exposure; use sunscreen,

wear protective clothing; antibiotic cause of Stevens
Johnson Syndrome, Toxic Epidermal Necrolysis

Tetracyclines

tetracycline, doxycycline,
minocycline

nausea/vomiting, diarrhea, anorexia,

abdominal pain, tooth discoloration in children
< 8 years, liver toxicity

Avoid prolonged sunlight exposure; use sunscreen,

wear protective clothing

Quinolones

ciprofloxacin (Cipro), levofloxacin

(Levaquin), moxifloxacin (Avelox),
ofloxacin (Floxin)

nausea/vomiting, diarrhea, abdominal pain,

headache, lethargy, insomnia, photosensitivity
(can be severe)

Avoid prolonged sunlight exposure; use sunscreen,

wear protective clothing;
moxifloxacin associated with higher rates of side
effects [shehab]; tendon rupture (rare) more
common in age > 60, with corticosteroid use, in
kidney, heart, lung translant recipients

Lincosamide

clindamycin, lincomycin

pseudomembranous colitis (may be severe),

diarrhea, nausea/vomiting, rash,
hypersensitivity, jaundice (clindamycin)

if severe diarrhea during treatment or for up to 8

weeks after treatment consult health care provider
immediately, may be pseudomembranous colitis (C.
dificile); consider use of less toxic agents

Miscellaneous

metronidazole

nausea/vomiting, dizziness, headache,

vaginal candidiasis, metallic taste

avoid alcohol use during treatment and for up to 3

days after, combined use may lead to cramps,
nausea/vomiting, flushing, headache; may discolor
urine red-brown

In a 2008 study, antibiotic side effects led to greater than 140,000 emergency department admissions per year in the United States. Roughly 50
percent of emergency visits were due to reactions to antibiotics in the penicillin class of drugs, and the other 50 percent were due to a wide variety of
antibiotics used to treat many different types of infections. In this study, children less than one year of age were found to have the highest rate of
antibiotic side effects. Allergic reactions accounted for the most common type of side effect. It was estimated that over 142,000 emergency department
visits per year were due to antibiotic adverse events, and approximately four-fifths of these events were due to allergic reactions. Allergic reactions can
typically only be prevented by avoiding the drug, although desensitization may be possible in certain circumstances for patients who have no other
antibiotic options. 1
There are also several side effects that are common to most antibiotics, regardless of class or drug. These side effects may include antibioticassociated diarrhea, yeast infections, serious allergic skin reactions, and complications from intravenous use of antibiotics.

Antibiotic-associated diarrhea - Antibiotic-associated diarrhea occurs in patients receiving antibiotics and occurs for no explainable reason.
Five to twenty-five percent of patients may develop antibiotic-associated diarrhea. The diarrhea occurs due to eradication of the normal gut flora by
the antibiotic and results in an overgrowth of infectious bacteria, such as Clostridium dificile. If the diarrhea is severe, bloody, or is accompanied by
stomach cramps of vomiting, a physician should be contacted. The most common antibiotics implicated in antibiotic-associated diarrhea are
amoxicillin-clavulanate, ampicillin, and cefixime; however, other antibiotics may lead to this side effect, including cephalosporins, fluoroquinolones,
azithromycin, clarithromycin, erythromycin, and tetracycline.2

Vaginal yeast infections or oral thrush (candida species): Antibiotics may also change the normal flora balance in the vagina, often leading
to an overgrowth of fungal species. Candida albicans is a common fungus normally present in small amounts in the vagina, mouth, gastrointestinal
tract, and on the skin and does not normally cause disease or symptoms. However, the fungus may take over when there is limited competition
from bacteria due to antibiotic treatment.

Stevens Johnson Syndrome (SJS), Toxic Epidermal Necrolysis (TEN): Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis
(TEN) are rare but serious allergic reactions to substances, often drugs, that result in serious skin and mucous membrane disorders. Antibiotics
such as sulfonamides, penicillins, cephalosporins, and fluoroquinolones may result in SJS and TEN. SJS and TEN can both cause rash, skin
peeling, and sores on the mucous membranes and may be life-threatening. 3

Injection site reactions and phlebitis: A reaction to an antibiotic can occur if the antibiotic is given intravenously in a vein. Injections site
reactions and phlebitis (vein inflammation) can occur with intravenously (IV) administered antibiotics. The vein and area with the IV needle may be
red, swollen and hot. An infection may or may not be present. Typically, the needle must be removed and reinserted elsewhere to help clear the
injection site reaction.