2

Name

Penicillin G

Penicillin V

Notable adverse
effects
Urticaria, severe
pruritus, fever, joint
swelling, hemolytic
anemia, nephritis, and
anaphylaxis
PSEUDOMEMBRANOUS
COLITIS due to C.
DIFFICILE. Antibiotic
mediated endogenous
infection.

-Lactams
Penicillins
Important
Indications
Drug of choice for
SYPHILIS.

Oropharyngeal
infections.

Drug
Interactions
Administered with
an
AMINOGLYCOSIDE
to treat
ENTEROCOCCAL
ENDOCARDITIS.
Oral bioavailability
significantly
reduced by food.
Should be taken 1
-2 hours before or
after meals.

Nafcillin
Oxacillin,
Cloxacillin
Dicloxacillin

Cation toxicity due to

administration as salts.

Antistaphylococcal

Ampcillin

High incidence of skin

rashes

Listeria, E. coli, M.
catarrhalis, and H.
influenzae

Syngergistic with
aminoglycosides
for Listeria and
Enterococci.

UTI, Meningitis,
Sinusitis, otitis,
and Lower Resp.
Tract infection

Given with
penicillinase
inhibitors to
improve half-life

Amoxicillin

Other info
Pneumococci, N.
gonorrheae, and S. aureus
are RESISTANT (PRSP).
PARENTERAL.

ORAL

Methicillin is the prototype,

rarely used due to
NEPHROTOXIC POTENTIAL.
Are penicillinaseRESISTANT.
Wider spectrum than
penicillin G.
Cleared partly by biliary
excretion.
Great oral bioavailability.
Highest of Pencillins.

Ureidopenicilli
n (UP) and
carboxypenicil
lin (CP)

Gram-negative
bacteremia,
pneumonia, postburn infection, and
penicillin-resitant
UTI.

Frequently used
with
aminoglycosides or
fluoroquinolones
for infections
outside urinary
tract.

UP superior against P.
aeruginosa.
CP superior against
Klebsiella.

THESE TWO ARE CALLED

GIVEN WITH
ANTIPSEUDOMONAL
AMINOGLYCOSIDE
PENICILLINS
TO TREAT
PSEUDOMONAL
INFECTION
ALL PENICILLINS (POOR PENETRATION INTO CNS UNLESS THERE IS INFLAMMATION, CROSSES PLACENTAL
BARRIER BUT NOT TERATOGENIC, POOR PENETRATION INTO BONE, EYE, AND PROSTATE). PROBENECID
INCREASES HALF-LIFE DUE TO IMPAIRED TUBULAR SECRETION.
Cephalosporins
Ge
Important
Drug
Name
Adverse effects
Other info
n
Indications
Interactions
May elicit
Drug of choice
Increased
Choice for patients
Cefazolin
hypersensitivity
from prophylaxis
nephroallergic to
(Others are Cephalexin,
reaction in patients
for orthopedic,
toxicity when
st
1
penicillin. Least
Cephapirin, cefaloridine,
allergic to
abdominal, and
given with an
toxic, does not
cefadroxil)
penicillin.
pelvic surgery
aminoglycosi
penetrate CNS.
Local pain and
(Cefazolin).
de.
thrombophlebitis in May be useful as
2nd
Cefoxitin
Have more
parenteral
Cefotetan
(Others are Cefaclor,
prophylaxis in GI
anaerobic and
preparation.
and
Cefprozil, and Cefuroxime,
sugery
gram negative
Cefamandol
Cefotetan)
(Cefoxitin).
activity than 1st
e
generation.

Drug of choice for

GONORRHEA
(Cefotriaxone
[parenteral],
cefixime [oral])

3rd

4th

Almost all
penetrate BBB
(NOT cefoperazone
and cefixime).

Useful antipseudomonal
Increased activity
activity
towards Gram(Ceftazidime)
negative.
Increased activity
Useful in treating
towards
bacterial
PNEUMOCOCCI
meningitis.
(CEFTRIAXONE
(acetaldehyd
AND
e
CEFOTAXIME)
accumulation
Cefepime
, disulfram(increased
like effect
pseudomonal
(hangover))
activity, decreaed
Also
pneumococcal)
Many cross BBB
Cefepime
antivitamin K
Cefpirome
and are efective in
Cefpirome
effects that
(increased
meningitis
thin blood
pneumococcal,
and cause
decreased
bleeding
pseudomonal
(Cefotetan)
activity)
GOOD TISSUE PENETRATION (INCLUDING BONE), LESS SUSCEPTIBLE TO PENICILLINASES. MRSA ALSO
RESISTANT TO CEPHALOSPORINS
Carbapenems
Cefotriaxone, Cefotaxime,
Cefpodoxime,
Ceftibuten, Cefdinir

Name

Adverse Effects

Imipenem/Cilastatin,
(others are meropenem,
ertapenem)

Name
Aztreonam

Name
Vancomycin
Bacitracin
Fosfomycin

Skin Rash, Seizures (high

doses), and hypotension

Indications

Drug of choice for E.

faecalis.
Penicillinase producing
gram positive and
negative bacteria.
Anaerobes and
Pseudomonas.

Drug Int.
Cilastatin
inhibits
formation of
toxic
metabolite
by
inactivating
renal
dipeptidase.

Monobactams
Adverse Effects
Indications
Drug Int.
Phlebitis, skin rash,
superinfection,
Enterobacteria
Non-allergenic
vertigo
Other Cell Wall Synthesis Inhibitors (Non--Lactam)
Adverse Effects
Indication
Drug Int.
Increases
Red man, red neck
Penicillin-resistant,
aminoglycoside
syndrome
MRSA
nephrotoxicity
High nephrotoxicity,
Wide variety of gram
limited to TOPICAL
positive bacteria
APPLICATION
Gram negative UTIs
May be synergistic
with B-lactams and

Other

Metabolite
is
nephrotoxic

Other

Other

Bactoprenol
inhibition
Inihibits NAM
synthesis

quinolones in
specific tissues
Cycloserine
Daptomycin

Name
Doxycycline

Tremors, seizures,
psychosis (potential)
May cause
myopathy (CK
monitoring)

Second-line drug for

M. tuberculosis
Vancomycin-resitant
staphylococci and
enterococci

PROTEIN SYNTHESIS INHIBITORS

Tetracyclines
Adverse Effects
Indication
Drug Int.
Deposition in growing
Tetracycline of
Fecal excretion
bone and primary
choice in
teeth (staining) in
patients with
small children.
RENAL
INSUFFICIENCY.
Contraindicated for
pregnant and nursing Rocky-mountain
women (tooth enamel
spotted fever
dysplagia), and young
(rickettsiae),
children (crown
cholera, tickdeformation)
borne Lyme.

Other
Good distribution to
tissues except CSF.
Absorption impaired
by divalent cations,
antacids, dairy
products and alkaline
pH.

Superinfection and
colitis
Tetracycline
Minocycline

Kidney toxicity when

given with diuretics. IV
injection may cause
thrombophlebitis. Fatal
acute degeneration of
liver.

Malaria
PREVENTION
and amoebiasis
treatment
Helicobacter
pylori duodenal
and gastric
ulcers

Meningococcal
carrier state

Names
Amikacin
Gentamycin
Kanamycin
Necilmycin
Streptomyci
n
Tobramycin
Neomycin

Absorption impaired by
food.

ALL TETRACYCLINES
BIND TO 30S
RIBOSOMAL
SUBUNIT.

High levels achieved in

tears and saliva

Aminoglycosides
Adverse Effects
Indication
Irreversible ototoxicity and
With broad
neurotoxicity may occur with
spectrum BANY aminoglycoside.
lactam for
serious gram
Nephrotoxicity in the form of
negative bacilli
acute tubular necrosis
infection
(Gentamycin and Tobramycin
(namely P.
more commonly).
aeruginosa)

Drug Int.
Cell wall synthesis
inhibitors enhance
transport of drug
into bacterial cells.

Other
All are parenterally
administered
(except NEOMYCIN
is TOPICAL)

Block initiation
complex (IF)
formation. Cause
misreading of mRNA.

Once daily dosing

recommended to
reduce toxic
accumulation.

Amikacin and kanamycin

more prone to auditory
impairment.
Vestibular impairment more
likely with gentamycin and
tobramycin.
Crosses placenta and may
cause CN VIII damage in
fetus.
Factor V antagonism
(bleeding).
Curare-like neuromuscular
blockade.

Are active
against aerobic
and facultative
anaerobic
bacilli.

Inihibit translocation.

Inactive against
anaerobes and
gram positive
(except
staphylococci)

Renal filtration is
main excretory
mechanism.

Do not penetrate
BBB or enter
vitreous humor.

Loop diuretics may

increase ototoxicity.

Rarely used
alone, but for
Yersinia Pestis
(plague) and
tularemia they
are.

Amphotericin B,
Cephalosporins and
Vancomycin increase
odds for
nephrotoxicity.

Macrolides
Indication
Mycoplasma
infection,
community
acquired

Drug Int.
Crosses placenta,
poor BBB crossing,
accumulates in
macrophages.

Poor oral
bioavailability
(highly polar
drugs)
ALL
AMINOGLYCOSID
ES BIND TO 30S
RIBOSOMAL
SUBUNIT

Skin rash more commonly

with Neomycin (topical)

Name
Erythromyci
n

Adverse Effects
Thrombophlebitis with IV
injection
Cholestatic jaundice,

Other
ALL MACROLIDES
BIND TO 50S
RIBOSOMAL
SUBUNIT.

hypersensitivity to
esterified form.
Ototoxicity (high doses)
GI distress

Azithromycin

Clarithromyc
in

GI distress

pneumonia,
Legionnaires
disease, all forms of
Chlamydial
infections,
Diphtheria and
pertussis.
More chlamydial
affinity,
mycobacterium
avium complex and
toxoplasma
Chlamydial affinity,
mycobacterium
avium complex and
toxoplasma.

Biliary excretion
and liver
metabolism
METABOLITES
INHIBIT CYP450
Stable to gastric
acid. Longest halflife and largest Vd.
Biliary excretion
Stable in gastric
acid.
Kidney excretion
and liver
metabolism.
METABOLITES
INHIBIT CYP450

Quinupristin/
dalfopristin

Hyperbillirubinemia,
arthralgia, myalgia

Linezolid

Thrombocytopenia

Vancomycinresistant
enterococcus
faecium
Multidrug resistant
gram positives

Ketolides

Penetrates
macrophages and
PMN.

INHIBIT
TRANSLOCATION.
Macrocyclic lactone
ring to which deoxy
sugars are
attached.
Macrolide
resistance in
bacteria may be
induced by
macrolides by
activation of
macrolide-inducible
methylase which
modifies ribosomal
binding site.

Name

Telithromycin

Name
Clindamycin

Adverse Effects

Indication

Drug Int.

Penicillin resistant
microbes.
Macrolide resistant
microbes.
Other protein synthesis inhibitors
Adverse Effects
Indication
Drug Int.
Neutropenia
Drug of choice for
Good tissue and
severe anaerobic
bone penetration.
Superinfection
infections in
(pseudomembrano
abdomen, female
Not to CSF.
us colitis) with C.
genital tract and
difficile.
aspiration
Biliary and urinary
pneumonia, used
excretion.
with cephalosporins
and
aminoglycosides.
Prophylaxis of
endocarditis in
valve disease
patients who are
allergic to penicillin.
Pneumocystis
carinii pneumonia
in AIDS patients
with primaquine.
AIDS related

Other
Equal to
azithromycin
against atypical
pathogens (H.
influenzae)
Other
Inhibits formation of
ribosomal initation
complex.
Interferes with
translocation
reaction.
Identical binding
site to that of
erythromycin (30S
RIBOSOMAL
SUBUNIT)

toxoplasmosis with
pyrimethamine.
Bone marrow
toxicity at high
levels (inhibits
mamallian
ribosome)
Blood dyscrasias
(aplastic anemia,
thrombocytopenia,
granulocytopenia)
Chloramphenicol

Superinfections (C.
difficile associated
diarrhea)
pseudomembranou
s colitis
Gray (Gray baby)
syndromecirculatory collapse,
cyanosis, MI,
abdominal
distension, coma
and death.
Accumlated
chloramphenicol.
(increased risk in

Rocky mountain
spotted fever and
Typhus.

Crosses BBB and

placenta readily.
60% protein bound

Back-up for
Salmonella and
pneumococcal and
meningococcal
infection in
penicillin sensitive
patients.
Ineffective for
chlamydia and P.
aeruginosa.
Topically for eye
infections

Inactivated by
hepatic UGT.
Weakly inhibits
CYP2C9 and
CYP3A4
Decreases
metabolism of anticonvulsants and
barbiturates.
Rifampin and
barbiturates
increase
metabolism of
chloramphenicol.
Decrease
sulfonylureas
metabolism.

patients with
decreased hepatic
function.

Name
Sulfamethoxazole
Sulfisoxazole

Daraprim

Fansidar

Sulfasalazine
Sulfacetamide
Sodium-

Glositis, stomatitis,
angioedema.
PROTEIN SYNTHESIS INHIBITORS
Sulfonamides (Inhibitors of Folate Synthesis)
Adverse Effects
Indications
Drug Int.
Photosensitivity
Useful in treating
Rarely given alone
Exfoliative
UTIs
dermatitis
Bladder infection,
Hemolytic/aplastic
ear infection,
anemia
meningitis
Granulocytopenia
First line treatment
Thrombocytopenia
for acute
toxoplasmosis
Urinary tract
DHFR inhibitor
disorder
Anti-protozoal
Precipitation of
agents
drug crystals at
Blocks folinic acid
NEUTRAL OR
Anti-malarial agent
formation
ACIDIC pH.
(crystalluria,
Ulcerative colitis,
Given ORALLY
hematuria,
enteritis and other
(NONobstruction)
inflammatory bowel
ABSORBABLE)
Prevent by
disorders
hydration and
Bacterial
Topical eye solution
alkalinize urine.
conjunctivitis
Adjunctive drug in
Topical agents

Other

Sulfadiazine
combined with
pyrimethamine
Sulfadoxine
combined with
pyrimethamine

treating trachoma
(chlamydia)

sulfacetamide

Mafenide-acetate

Name
Trimethoprim
(and
Pyrimethamine)

STEVEN-JOHNSON
SYNDROMEdetachment of
epidermis from
dermis

Prevention of sepsis
in burns and
wounds

Topical agents

KERNICTERUS in
newborns-sulfa
displace billirubin
from albumin,
allowing high
SULFONAMIDES ARE BACTERIOSTATIC
Dihydrofolate Reductase Inhibitors
Adverse Effects
Indications
Drug Int.
Megaloblastic
UTIs, Travelers
Distributes well to
anemia,
Diarrhea.
CSF.
leukopenia,
Combined with
Weak base,
granulocytopenia
sulfamethoxazole
concentrates in
AND BONE
or dapsone for
acidic
MARROW TOXICITY
prophylaxis and
environments.

Other
20-50 times more
potent than
sulfonamides

may be prevented
by folinic acid
(LEUCOVORIN)
administration.
Mammalian DHFR
inhibition (more a
problem with
pyrimethamine)

Name

Cotrimoxazole
(Trimethoprim
+Sulfamethoxazole
)

Adverse Effects

Folate deficiency
Pancytopenia in HIV
patients

treatment of
Pneumocystis

Combination Drugs
Indication
IV administration to
treat P. carinii
pneumonia
Gram negative
bacterial sepsis
Pneumonia,
travelers diarrhea,
ear infection and
UTI

Usually used in
combination with
sulfonamides.

Drug Int.

Synergistic effect
(inhibition of two
sequential steps in
THF synthesis)

Other
Broader bacterial
spectrum than
SULFAS
Prosthatic and
vaginal fluid
accumulation

Name
Nalidixic Acid

Name
Ciprofloxacin

Adverse Effects
Useful only for UTI,
systemic effective
levels were not
achieved
Adverse Effects
Reversible
arthropathies,
including tendinous
rupture.

DNA INHIBITORS
Quinolones
Indication
Prophylaxis before
transurethral
surgery
Fluoroquinolones
Indication
Drug of choice for
treatment and
prophylaxis for
ANTHRAX.
Gastroenteritis with
severe diarrhea

Levofloxacin

Norfloxacin

Effective for
chlaymidial
urethritis and
cervicitis.
Effective for
chlamydial
urethritis and
cervicitis
Least active of the
fluoroquinolones
against gram
positive and gram
negative

Drug Int.

Other
Inhibit DNA Gyrase
and Topoisomerase
IV

Drug Int.
Warfarin, caffeine,
antacids, medicines
with iron or zinc,
didanosine, and
sucralfate interfere
with
fluoroquinolones.
Bronchodilators
(theophylline,
aminophylline)
Cimetidine
interferes with
elimination

Other
Most active against
GRAM NEGATIVE (P.
aeruginosa)

Superior activity
against GRAM
POSITIVE (S.
pneumoniae)

Ofloxacin

Lomefloxacin

May worsen muscle

weakness in
myasthenia gravis
leading to death

E. coli prostatitis
and STDs, EXCEPT
SYPHILIS

UTIs and bronchitis

due to H. influenza
and M. catarrhalis
Moxifloxacin
Used for
tuberculosis and
other
mycobacterial
infections (also,
cipro and levo)
Respiratory
Gram positive and
Examples are
fluoroquinolones
gram negative
Levo-, gati-, gemi-,
atypical
moxifloxacin. Upper
pneumonias
and lower
(chlamydia,
respiratory tract
mycoplasma,
infections.
legionella)
Trovafloxacin
Intra-abdominal
infections
ALL FLUOROQUINOLONES (EXCEPT FOR MOXIFLOXACIN) ARE EFFECTIVE IN TREATING UTI EVEN WHEN
ORGANISM IS MULTI-DRUG RESISTANT (PSEUDOMONAS). ALSO EFFECTIVE FOR SALMONELLA, E.COLI,
SHIGELLA, AND CAMPYLOBACTER