Antibiotics:

Drug

Key Clinical Features & Use

Mechanism

Side Effects

Sulfonamid
es

STATIC
Broad spectrum G+/G-Usually used with DHFR inhibitors like trimethoprim (dihydrofolate
reductase) synergistic- folate synthesis
-No longer broadly used (resistance)

Cross the placenta antibacterial

effects & unwanted side effects in
fetus
Crystalluria: drink lots of water with
PO forms
Kernicterus: a form of jaundice from
displacement of bilirubin from plasma
proteins bilirubin crosses bbb and
deposits in the basal ganglia
generalized CNS depression
-Avoid in Newborns and infants <2
months old
Blood dyscrasiasacute hemolytic
anemia, agranulocytosis, aplastic
anemia (rare but can be Fatal) do not
use topical if there is a known Hx of
blood dyscrasias
HypersensitivityStevens-Johnson
syndrome = erythema multiform
major, a severe form of erythema
multiforme characterized by bullous
eruptions on the skin & mucous
membranes; fever

Trimethoprim
(Trimpex)
Pyrimethamin
e
(Paraprim)
Methotrexate
(Rheumatrex)

Usually used with sulfonamide

-DHFRI
Antimalarial
Usually used with sulfonamide

-Inhibits the first step in

the bacterial synthesis of
folic acid
(dihydropteroate
synthase), the joining of
PABA with pteridine to form
dihydropteroic acid, the
immediate precursor of
folic acid
-Glutamate is then added to
form dihydrofolate (FH2)
which is reduced by
dihydrofolate reductase
(DHFR) to tetrahydrofolate
(FH4)
-FH4 is used in 1 Carbon
transfer reactions as in the
synthesis of thymidine
* Stops/inhibits DNA
synthesis*
-Usually used with
dihydrofolate reductase
inhibitors act
synergistically by inhibiting
another enzyme along the
same pathway
Inhibits bacterial
dihydrofolate reductase
Inhibits protozoal
dihydrofolate reductase

Sulfisoxazole
*ORAL

Prophylaxis in kids w/recurrent Otitis Media;

(Pediazole
*liquid* with erythromycin)
-Is an alternate for uncomplicated UTIs; cystitis
-Prophylaxis in kids with RECURRENT Otitis media (for acute cases,
use Amoxicillin or 2nd or 3rd generation cephalosporin)
UTIs: *note that Norfloxacin (fluoroquinolone) is only confined for UTI
use.
Community: E. coli (80%); Staph saprophyticus 10% (2nd most common)
Hospitals: E. coli 50%; Klebsiella, Proteus, Enterobacter & Serratia 40%;
Enterococcus faecalis, Staph saprophyticus & Staph aureus 10%
Available with Trimethroprim aka Co-Trimoxazole (TMP-SMX) or
Bactrim synergistically
TMP/SMZ uses: * RUG
a) UTI if local E coli resistance to TMP/SMZ is <20%; if >20% use a
fluoroquinolone (Ciprofloxacin)
b) Respiratory & GI infections
High doses for Pneumocystis carinii in AIDS
Alternate for:
Ulcerative blepharitisbacterial causes are usually S. aureus & S.

Sulfamethoxaz
ole
-ORAL
only

Sulfacetamide
(Bleph-10

-DHFRI

Used to treat psoriasis and various cancers

-DHFRI

Inhibits mammalian,
bacterial, & protozoal
DHFR
-See sulfonamide
mechanism

-See sulfonamide
mechanism
-A sulfa with a DHFRI
(dihydrofolate reductase)
provides synergism by
inhibiting 2 steps in folate
synthesis
-See sulfonamide
mechanism

Blood dyscrasias

-See sulfonamide side effects

-See sulfonamide side effects

-See sulfonamide side effects

=10%)
TOPICAL
opthalmic
preparation

Mafenide
(sulfamylon)
*TOPICAL
Blephamide

epidermidis (1st choice: polysporin ointment (bacitracin + oplymyxin B)OTC) for better G- coverage, use the aminoglycoside antibiotic
gentamicin (Garamycin) ophthalmic ointment
Bacterial conjunctivitiss. aureus, s. pneumoniae, h. influenzae &
Moraxella catarrhalis are the most common causes (use Vasosulf because
of the vasoconstrictor action) (1st choice: polysporin, for better Gcoverage, use the opthalmic form of the fluoroquinolone ciprofloxaxin
(Ciloxin))
Burns
Use limited => metabolic acidosis
Sulfacetamide + prednisolone
Treats bacteria and inflammation

Silver
sulfadiazine
(silvadedne)
TOPICAL

*first one use before Mafenide (less side-effects)

For burns to prevent sepsis

Fluoroquinolon
es

Broad spectrum CIDAL agents uses mostly for Gm - and some G+

(anaerobes?)
-floxacin ending is a fluoroquinolone
**AVOID antacids and Fe supplements: results in DECREASED FQ
absorption due to chelation (mono/divalent cations)**
*also FQ can increase/decrease bld/glc levels in DIABETICS due to insulin
or hypoglycemic drugs
*NOTE that 3rd gen are BETTER against Strept pneumonia$$$ over
2nd gen.

Metabolic acidosis- inhibits carbonic

anhydrase (loss of HCO3 from kidney
tubules)
same mechanism for
sulfacetamide
Predinsolone=
glucocorticoid (steroid)
anti-inflammatory
Silver released is slowly
toxic to microorganism
-Acts with sulfonamide
mechanism
Mechanisms:
G-: Inhibit DNA gyrase
(which cuts & re-anneals
DNA fast unwinding),
prevents DNA synthesis,
replication [note:
mammalian topoisomerase
II]
G+: Inhibits Topo IV
(slightly different) function
separation of daughter
cells during replication
*Inhibits DNA replication*

Metronidazole
Ciprofloxacin
2nd gen

Anti-fungal (vaginal yeast infections)

1st choice against fluoroquinolone induced pseudomembranous colitis
against C. difficile
Fluoroquinolone; best against G- activity in the FQ grp; oral and
ophthalmic (CILOXAN) preparations, Cipro HC Otic = HC
(hydrocortisone anti-inflammatory), for ear infections

Form a reactive anion

which damages bacterial
DNA, kills C. difficile
See fluoroquinolone
mechanism

The sulfa can be absorbed if covering

a large area (larger the area the
greater the risk for systemic
absorption *blood dyscrasias)
Nausea, vomiting & diarrhea (NVD)
-Fluoroquinolones are the major cause
of C. difficile-induced diarrhea and
pseudomembranous colitis.
-C. difficile survives as spores until
antibiotics are discontinued, then it
grows without competition. Produces
two toxins: one causes fluid
production and damage to the mucosa
diarrhea, the other causes plaque
formation of the mucosa creating a
pseudomembrane on the colon wall
-Treatment= 1st choice:
Metronidzaole; 2nd choice Vancomycin
1. Phototoxicity: burning, redness,
swelling, blisters, rash, itch
2. Arthropathy: do NOT use in
prepubertal children or if pregnantdamage growing cartilage
3. Tendon rupture- higher risk over
65yo or taking steroids, even weeks
after Rx discontinued. BBW
4. CNS stimulationconvulsions and
psychosis (Rare but serious)
5. Increased cardiac conduction
(moxi-, gati-, and spar- floxacin)

See fluoroquinolone side effects 1-4

*drug rxns: INCREASES
theophylline (decrease clearance),
tizadine (inhbits CYP1A), methadone
(inhibits CYP3A4)

Gatifloxacin
3rd gen
Moxifloxacin
3rd gen

Gemifloxacin
3rd gen
Levofloxacin
3rd gen
Lomefloxacin

Fluoroquinolone; Opthalmic preparations ONLY *oral discontinued

Fluoroquinolone; oral and ophthalmic (VIGAMOX) preparations
*RESPIRATORY FQ drug
Good against anaerobes
Alternative for Bacteroides fragilis (G- rod that is part of the colons
normal flora, common cause of peritonitis in a perforated colon)
1st choice: either Ampicillin + sulbactam OR Piperacillin + Taxobactam
Fluoroquinolone; for mild-moderate community acquired pneumonia and
exacerbations of chronic bronchitis *MOST SAFE of three 3rd gen
RESPIRATORY FQ drugs$$$
Fluoroquinolone; *Active form of Ofloxacin (2nd gen), more side-effects
*also risk of acute hepatitis and fatal events (rare) *RESPIRATORY
FQ drug
Fluoroquinolone; UTIs and lower RTIs

Norfloxacin
2nd gen
Ofloxacin
2nd gen
Sparfloxacin

Fluoroquinolone; least active, low systemic levels (not enough for

systemic infections), UTI only
Fluoroquinolone

Sulbactam

-lactamase inhibitor; used synergistically with another antibiotic

Tazobactam

-lactamase inhibitor; used synergistically with another antibiotic

Clavulanate

-lactamase inhibitor; used synergistically with another antibiotic

Example: with Amoxicillin

Fluoroquinolone

PENICILLINS
*Beta-lactam Antibiotic
*CIDAL

Thiazolidine + -lactam rings form the

PCN nucleus and are required for activity,
the side chain determines their properties
and spectrums of activity
Some G- activity, MAINLY Gm +
NOTE: not all -lactamases are
penicllinases (may be cephalosporinases)
*Beta-lactamase is a general term,
pencillinase is specific term.

PCN G (benzylPCN)
-only natural penicillin
still in use
*note LA: Benzathine

(Gorillacillinnot real name)

Given IM-IV, parentally (acid labile),
distributes into CNS only if the meninges
are inflamed

See fluoroquinolone
mechanism
See fluoroquinolone
mechanism

Increased cardiac conduction; See

fluoroquinolone side effects 1-4
Increased cardiac conduction,
prolongs Q-T interval in HEALTHY
people, hepatic disease (mainly
metabolized by liver)

See fluoroquinolone
mechanism

See fluoroquinolone side effects 1-4

See fluoroquinolone
mechanism

*prolongs Q-T interval in ELDERLY,

Torsades de pointes (ARRYTHYMIAS)

See fluoroquinolone
mechanism

See fluoroquinolone side effects 1-4

See fluoroquinolone
mechanism
See fluoroquinolone
mechanism
See fluoroquinolone
mechanism

See fluoroquinolone side effects 1-4

Penicillins irreversibly inhibits

transpeptidase which inhibits cell
wall synthesis lysis and killing
microorganism CIDAL
G+ cell walls contain mostly
peptidoglycan composed of 2
alternating sugars NAG (Nacetylglucosamine) and NAM (Nacetyl muramic acid)
-NAM has a D-alanine chain which
must be removed by a transpeptidase
before crosslinking of the sugars can
occur (crosslinking is essential for cell
wall synthesis) autolysins break down
for growth, but no new synthesis
Food interferes with absorption of
most PCNs so give 1 hr before meals

NOTE: PCN G is expressed in UNITS

where 1 unit = 0.6 G, or 1 million
units = 600 mg
See penicillin mechanism

See fluoroquinolone side effects 1-4

Increased cardiac conduction

Hypersensitivityfrom metabolites acting as

haptens, IgE mediated, characterized by
rashes, fever, bronchospasms, serum sickness,
Stevens-Johnson syndrome, anaphylaxis
Diarrheacommon to all antibiotics (killing
normal flora)
Superinfectionpotential risk with all
antibiotics, because of disruption of normal
microbial flora (C. difficile forms SPORES
results in (toxins) pseudomembranous colitis)
Increased risk of Seizures: penetrate BBB,
decreased renal function increases risk by
increasing penicillin levels. INHIBIT GABA
receptor (inhibitory receptor)
Jarisch-Herxheimer Reaction in 70-90% of
patients with 2 syphilis several hours after 1st
injection. Resolves spontaneously. Treat with
ASA. NOT allergic reaction, do NOT treat
like allergy otherwise pt can suffer. *fever,
chills, headache, arthralgia (Flu-like)
See penicillin side effects
***NOTE that PROCAINE is and ESTER,
some pts may have ALLERGIES to ESTER$$
*so could give Bicillin LA instead of CR.

only
-No procaine
*CR: Benzathine +
PROCAINE$$

PCN V
(phenoxymethyl PCN)

Three forms:
1. Aqueous solution for IM/IV
with Na+ and/or K+ salts, water
soluble (not for CHF)
2. Procainesuspension for IM
ONLY *local anesthetic (slows
PCN release and numbs pain)
*Bicillin CR: Benzathine +
Procaine
3. Benzathinesuspension for IM,
LONGEST acting (Bicillin LA)local anesthetic (slows) DOC for
syphilis.
Aka phenoxymethyl PCN
Acid stable form for ORAL use
Dosed in mgs

Penicillinase (lactamase): resists

PCN G and V
*Only for resistant
Staph

1. Dicloxacillin (generic)- oral

2. Oxacillin (Bactocill)- parenteral
3. Nafcillin (Nallpen)- parenteral

Ampicilin (Principen)
*also with
Sulbactam (lactamase inhibitor) as
UNASYN as IM/IV
use
Amoxicillin
*also with
Clavulanate (lactamase inhibitor) as
AUGMENTIN

An AMINOpenicillin- Extended
Spectrum PCN: Gm (-) coverage but
still susceptible to penicillinases (like
PCN G/V). Strains resistant to PCN
also resist aminoPCNs$$$
*Oral or IV
An AMINOpenicillin (see above)
-Oral caps & pediatric drops
-used AFTER Unasyn (IV) for
peritonitis $$$ b/c Augmetin is only
ORAL (not IV) so need some fast IV first,
then can give oral to finish off after
-Uses: OM, prophylaxis before dental
procedures (no longer for mitral valve
prolapse)
Antipseudomonas PCNs against some
Gm - Pseudomonas (modest against P.
aeruginosa) and some resistant Proteus;
Still susceptible to PCNases
-Parenteral
Antipseudomonas PCN (see above)
-Parenteral
-similar to timentin

Ticarcillin +
Clavulanate
(TIMENTIN)
*ONLY available
with Clav
Piperacillin
(available alone)
- or with Tazobactam
as ZOSYN

Cephalospori
ns
*Beta-lactam
Anti-b

-lactam + dihydrothiazine ring with

side-chains
RESIST many -lactamases but not
all
*Through the generations, loss of
G+ activity better against G-

90% eliminated by tubular secretion.

Competition for secretion site (uric
acid, probenecid *used to treat
gout*) increase PCN levels

*one time 2.4mil units of Bicillin LA for

syyphillis
**NOTE: NEVER give a SUSPENSION IV,
always SOLUTION based.
*Syphillis (STD) caused by spirochete
Treponema pallidum

Food decreases absorption of most

PCNs so give 1 hr: a.c. antes cibos
(before meals) or
p.c. post cibos (after meals)
Methicillin-Resistant Staph. Aureus
(MRSA) resists DONs. *Note
Methicillin discontinued years ago

* V: Very STRONG, so can give orally b/c

resists acid

Unasyn is preferable to ampicillin for

Peritonitis due to Bacteroides fragilis, a
Gm - rod (normal flora)- common
cause of peritonitis in a perforated
colon and is a big producer of lactamases
See penicillin mechanism
Longer t

All eliminated by biliary & renal excretion

(advantage in renal or hepatic disease) *Pt
has ONE compromised organ, the other will
COMPENSATE$$$$ and eliminate.
*only PCN grp increase POWER against PCN
resistant bugs.
See penicillin side effects

See penicillin side effects

*AmOxicillin for ACUTE Otitis media,
pediatric drops.

See penicillin mechanism

See penicillin side effects

See penicillin mechanism

See penicillin side effects

*Tazobactam: beta-lactamase inhibitor

Act by the same mechanism as the PCNs

inhibit transpeptidase

Most common side effects of all cephalosporins:

Hypersensitivity- risk of cross-allergy with PCN
greatest with 1st generation; negligible with 2nd and
3rd unless prior PCN reaction
Nephrotoxicity low
Coagulation abnormalities: interferes with Vitamin

*Basically SECOND choice if PCNs

fail.
1st Generation
Cephalosporins

Resist Staph PCNase

Good against G+ and some Gorganisms: Proteus micrabilis, E. coli,
Klebsiella pneumoniae (PEcK)
1. Cefazolin (Ancef)- IV
2. Cephalexin (Keflex)- Oral
3. Cefadroxil (Duricef)- Oral

2nd Generation
Cephalosporins

Less G+ and more G1. Cefaclor (Raniclor)- q 8h; oral (See

Side Effects)
2. Cefuroxime-q 12h; Oral-Ceftin;
IV/IM-Zinacef
3. Cefoxitin (Mefoxin)- IV/IM; a
cephamycin. Active vs B. fragilis
4. Cefprozil (Cefzil)- q 12-24h; Oral
IV/IM
Best vs Meningitis (S. pneumoniae and
N. meningitidis)
Also best vs. N. gonorrhoeae

Ceftriaxone
(Rocephin)
3rd generation

Cefotaxime

Cefpodoxime

IV/ IM
Best vs Meningitis (S. pneumoniae and
N. meningitidis)
Will also cover Bacteroides
Oral use

Cefdinir

Oral use

Ceftazidime
(Fortaz)
4th Generation

IV/IM

Cefepime

4th generation cephalosporin

IV/IM for G- rods resistant to 3rd
generation Rxs
-Good CNS penetration

OTHER B
Lactams
Aztreonam
(Azactam)
Carbapenems

General increase in activity against G-

IV/IM
G- aerobes
Crosses inflamed meninges
G+/G- anaerobes, some MRSA (last
resort use)

PEcK organisms:
Proteus mirabilis: enteric, infects only when it
leaves GI tract. Generally UTIs. It is urease+
(urine alkaline, promotes stones)
E. coli: Enteric, most common cause of UTIs
and a common cause of travelers diarrhea and
diarrhea in infants (80%)
Klebsiella pneumoniae: nosocomial RTIs but
can cause UTIs
Same mechanism as the PCNs inhibit
transpeptidase enzyme
Cover PEK and H. influenzae, Neisseria
meningitidis, Neisseria gonorrhoeae HeN PEK

Act by the same mechanism as the PCNs

inhibit transpeptidase enzyme
Highly protein bound easily displaces bilirubin
from albumin (which increases the risk of drug
interactions)
-About excreted in urine and in bile (good
if renal failure)
Same mechanism as the PCNs inhibit
transpeptidase enzyme
Parent & metabolite active
Same mechanism as the PCNs inhibit
transpeptidase enzyme
Same mechanism as the PCNs inhibit
transpeptidase enzyme
-Excreted mostly unchanged
-Binds Fe- decreases absorption and reddens
feces in infants
Same mechanism as the PCNs inhibit
transpeptidase enzyme
Act by the same mechanism as the PCNs
inhibit transpeptidase enzyme

Binds PBP-3 of G- bacteria => long unstable

filamentous bacteria => lysis
Excreted in urine unchanged- adjust dose PRN
(pro renata)
Transpeptidase activity
cilastatin inhibits dehydropeptidase: 1) prevents

K: prothrombin time [Cefmetazole, Cefoperazone,

Cefotetan, Ceftriaxone]
CAUTION: warfarin/heparin or bleeding disorders
See cephalosporins side effects

See cephalosporins side effects

1. Cefaclor associated with sx of serum sickness
(arthralgais, uticaria, glomerulonephritis, et al)

Under 3months- risk of kernicterus unless used as a

single does for Gonorrhea conjunctivitis
Hypoprothrombinemia- add vitamin K (warfarin,
heparin)
FDA warning- precipitates with Calcium in lungs
and kidnies => wait 48hours after any Ca
See cephalosporins side effects

See cephalosporins side effects

See cephalosporins side effects

Neurologic side effects: myoclonus, EEG, changes,

disorientation; causes if epileptic
See cephalosporins side effects
Neurological side effects: myclonus, EEG changes
with
increased risk if epileptic, disorientation -cauion if
epileptic
*****Renal elimination*****

Nausea, vomiting, seizures (1.5%)

Imipenem with cilastatin (Primaxin)IV/IM

Meropenem
(Merrem)
Ertapenem
(Invanz)
Doripenem
(Doribax)
OTHERS
Vancomycin
(Vancocin)

formation of nephrotoxic metabolite and 2)

Levels increase for UTIs
UTIs, Lower RTIs (S.a, E.c., K, E, H.i., etc), Intra
abdominal & gynecological infections, Bacterial
septicemia, Bone, joint, skin infections (E.f.,
S.a.& e, P.a., etc)
Seizures (0.5%)

1x/Day
Parenteral

For complicated intra-abdominal infections &

UTIs

IV for MRSA or MSSA (methicillin

Sensitive)
if allergic to B-lactams
Oral- local vs pseudomembranaous
colitis (NOT absorbed systemically)

Binds to & prevents removal of D-ala terminus

(doesnt inhibit transpeptidise, but blocks
action)

Bacitracin
(Tracin)

Cidal vs various G+ cocci and bacilli

Topical for minor cuts and scrapes

Fosfomycin
(Monurol)

Ophthalmic ointment for ulcerative

blepharitis and bacterial conjunctivitis due
to various G+/G- organisms
Short course Tx of uncomplicated UTIs in
women (all male UTIs are complicated)

Aminoglycosi 2 amino sugars in glycosidic link to

aminocyclitol ring
des

*Red Man (neck) Syndrome- flushing of upper body

& face, hypotension, tachycardia, shock
(Vancomycin releases Histamine)
Ototoxicity- can accumulate, can be permanent (hair
cells damaged and do not regenerate)
Nephrotoxicity- when used other nephrotoxic drugs
Lipid carrier (bactoprenol) transports the
Nephrotoxic
NAG/NAM complex to the outside of the cell. The
carrier starts as a pyrophosphate.
Bacitracin complexes with the pyrophosphate
preventing dephosphorylation
Inhibits enolpyruvate transferase (Blocks addition
of PEP (phospoenolpyruvate) to UDP-NAG (2nd
step cell wall synthesis))

Static: inhibit initiation (high [ ]); misreading of

mRNA (low [ ]); 3) premature termination

CIDAL

CIDAL: bacterial use of faulty proteins

Mostly for G- organisms; used
synergistically with lactams effect for G+
coverage
-Poly-cations usually very polar (not well
absorbed) and are usually given IV, some
are given orally to clean out the bowel
-All are excreted by the kidney so adjust
dose for renal function
-highest levels in renal cortex
(nephrotoxicity) and endolymph
(ototoxicity)

Enter the periplasmic space of G- through porin

channels, pass through the inner membrane; flow
down electrochemical gradient (made by ETC) =>
NOT effective against anaerobes
lactams synergistic: Inhibits cell wall synthesis
to increase aminoglycoside penetration
-Calculate dose by Creatinine clearance
calculation: calculate according to lean body
mass, different for Amikacin (but same for
gentamicin and tobramycin) draw peak levels
30-60 minutes after the dose and trough just prior
to the next dose
Dosed around the clock. Now once a day due to
postantibiotic effect inhibiting bacteria
Narrow therapeutic range

Aminoglycosides attain their highest levels in

the organ they are most toxic to
1. Nephrotoxicity: damage to renal cortex,
but can regenerate=> reversible
2. Ototoxicity damage to endolymph
irreversible because sensory hair cells do not
regenerate, degeneration of the auditory
nerve can lead to permanent hearing loss
-Auditory: Tinnitus, high-frequency of hearing
loss
-Vestibular: vertigo, ataxia, loss of balance
3. Drug accumulates in fetal plasma
ototoxicity in neonates: CAUTION if
Pregnant
4. Neuromuscular blockRespiratory
paralysis: when used with/as anesthetic
blocks Ca uptake into nerve terminal => ACh
release
blocks postsynaptic ACh receptor (block
nicotinic neuromuscular junction)
Tx: IV Ca; Alternative: neostigmine

Gentamicin
Aminoglycoside
IV
Tobramycin
Aminoglycoside
IV
Amikacin
Aminoglycoside
IV
Kanamycin
Neomycin

Paromomycin

Topical cream/ointment for burns, wounds

and to prevent catheter infections
(Genoptic)- for superficial ocular infections
Interchangeable with Gentamicin
Enzyme resistant. For nosocomial
infections that resist gentamycin and
tobramycin (Big Gun)
IV only
Aminoglycoside Oral

Cockcroft-Gault (based upon clearance, lean wt, &

serum creatinine); 120-125 ml/min creatinine
cleared
Peak- 6-8 ug/ml
Trough <2ug/ml
Draw peaks 30-60 min after dose; troughs 30-60
min before
Peak- 6-8 ug/ml
Trough <2ug/ml

(AChEsterase Inhibitor)
Additional problem: Myasthenia gravisautoantibody binds ACh receptor

Possible less ototoxic than gentamycin

Peak 20-30 ug/ml

Trough <10ug/ml

Prep for bowel surgery and as a topical

anit-infectant
Aminoglycoside Oral
1st choice for amebic dysentery, an
amebiasis from Entamoeba histolytica (kill
cysts)

Tetracyclines

4 ring structure- STATIC

Broad spectrum G- and G+ - second line
agents, there is a lot of resistance and
there are side effects
-Ender go enterohepatic recycling (levels
can persist)
-Different levels of actions (duration)

Tetracycline
(sumycin)
T - 6-8h

Alternate oral or topical for inflammatory

acne
[1st Choice: topical erythromycin (a
macrolide) + benzoyl peroxide with or
without an oral antibiotic]
Used to treat chronic dilutional
hyponatremia (low Na- Natrium = sodium)
associated with Inappropriate ADH
(SIADH) secretion (action in addition to

Demeclocycline
T - 12h

Inhibit binding of aminoacyl transfer RNA to

acceptor site of ribosome inhibit protein
synthesis

Not used for antibacterial activity

Inhibits protein kinase in ducts of which ADH
depends

Absorption of all tetracyclines is decreased

by dairy products and antacids via chelation
which binds and blocks metabolism of
antibiotic
GI upsettake with food
Photosensitivity, particularly with
demeclocycline
Brown discoloration of teethPERMANENT
(due to interaction with Calcium and
Phosphate salts on enamel)
Expired Rx: Fanconi-like syndrome from
nephrotoxic epianhydrotetracycline N & V,
polyuria, glucosuria, acidosis
Dairy products and antacids: absorption
(chelation)

Doxycycline
T - 16h

Minocycline
(minocin)

antibiotic use)
Highly lipid soluble (5% absorbed)
1st choice for:
(((-Rickettsia , Chlamydia trachomatis,
Borrelia burgdorferi
Alternate for: syphilis in patients allergic
to PCN and Vibrio cholerae (1st choice is a
fluoroquinolone))))
Tx acne

Significant excretion in feces- inactive

Immunomodulatory anti-inflammatory activity:

blocks synthesis of NO and activation of microglia
neuronal damage
Might:
-improve stroke outcomes if given within 6-24
hours
-be neuroprotective in degenerative diseases

Pulmonary complications (pulmonary lupus,

hypersensitivity pneumonitis, pleural
effusions)
SLE-like syndrome. Sxs reversible
Chronic use: Nail, skin, & sclera
pigmentation (generally reversible); Black
pigmentation of thyroid (asymptomatic)
Bule-black gums from bone pigmentation
(permanent)
Similar to Tetracyclines - see Tetracyclines
side effects above

Tigecycline
(Tygacil)
NOT a
Tetracycline

Active vs tetracycline sensitive G+/Gorganisms and MRSA (due to steric

hindrance of molecule)
Parenteral use for complicated skin and
intraabdominal infections
Structurally similar to tetracycline; may
share side effects

Inhibits protein synthesis by blocking entry of

aminoacyl-tRNA to the acceptor site

Macrolides

Lactone ring + 1 more deoxy-sugars

G+ & some G-, MSSA
Mostly STATIC
1st drug effective against Legionnaires
Disease
1st choice is Azithromycin (better lung
penetration) or a parenteral
fluoroquinolone levofloxacin
-Erythromycin is the macrolide in
Pediazole (other component is
sulfisoxazole)- given for Otitis media
1st choice for Pneumonia caused by
various organisms: Campylobacter
jejuni; Corynebacterium diphtheriae;
Bordetella pertussis
USES: Community acquired pneumonia,
Legionaries disease (or use a
fluoroquinolone), mycobacterium avium
complex (MAC)
Concentrates intracellularly
USES: community acquired pneumonia,
MAC
-Also used against Helicobacter pylori

1) Inhibit translocation from A to P site

2) Release peptidly tRNA from ribosomes
3) Block formation of initiation complex
Metabolites complex with cytochrome heme Fe2+
and inhibit CYP3A, the form of P450 that also
metabolizes erythromycin inhibits metabolism of
other drugs

Inhibit CYP3A
Immunomodulatory: inhibits mRNA transcription
for proinflammatory cytokines (IL- 8, AP-1, NF-B)

CAUTION WITH colchicines- possibly fatal

Has caused low blood sugars

A macrolide derivative with increased G+

activity
Concentrates in pulmonary tissues and
WBCs
Community acquired respiratory infections
Active vs B lactam and macrolide resistant

Same mechanism as Macrolides

Inhibitrs CYP3A4, prolongs Q-T

Rarely hepatotoxic
BLACK BOX WARNING: contraindicated if
myasthenia gravis (fatal/life threatening
respiratory failure)

Erythromycin
(E-Mycin)
in Pediazole (w/
Sulfa)

Azithromycin
(Zithromax)
T = 70h
Clarithromycin
(Biaxin)

Ketolides
Extelithromycin

Prokinetic: Motilin receptor agonist: Post-op to

stimulate peristalsis; speed gastric emptying with
gastroparesis

Can prolong cardiac repolarization Torsades

de point (effect on class of K channels); the
risk is increased if used with any other drug
that inhibits CYP3A which also causes
increased levels of erythromycin
Erythromycin doubles the risk of sudden
death; increases 5X if used with diltiazem or
verapamil (also metabolized by CYP3A)

Does NOT inhibit CYP3A and is excreted

unchanged in the bile

microbes
MISCELLANEO
US
Chloramphenic
ol
(last resort; high
risk)

IV only for aerobic/anaerobic G+/G- microbes;

ophthalmic available
Limit use to resistant meningitis and other serious
infections
Alternate to doxycycline for Rocky Mt. Spotted
Fever (Rickettsia) and to fluoroquinolones or
ceftriaxone for Salmonella typhi (typhoid fever)
Also an alternate for Yersinia pestis (plague) (as
well as doxycycline)

Like tetracyclines inhibits binding of

aminoacyl-tRNA to acceptor site (A site);
CIDAL in some organisms
PROBLEM: -Also inhibits mammalian
mitochondrial protein synthesis
Erythropoietic cells are the most sensitive
(progenitor cells) => G6PDH predisposes
to hemolytic anemia
-Inhibits cytochrome p450: due to
insufficient glucuronyl transferase to
conjugate the drug, and underdeveloped
renal function (unable to eliminate the drug)

Quinupristin /
Dalfopristin
(30/70)

A streptogramin given IV for MRSA and

vancomycin resistant infections together they
are synergistic

(last resort; high

risk)

Individually static, together CIDAL

Linezolid

For MRSA and vancomycin resistant infections

Oral and IV
Recommended weekly CBC

Quinupristin: releases peptidyl-tRNA from

donor site of peptidyltransferase
Dalfopristin: inhibits binding of aminoacyltRNA to acceptor site and peptidyl-tRNA to
donor site peptidyl
Inhibits CYP3A metabolism of warfarin,
diazepam etc.
Prevents formation of the initiation complex

Clindamycin

1st choice for: (also vancomycin) food poisoning

from B. cereus
Alternate for: Bacteroides fragilis,
Corynebacterium diphtheriae (instead of
erythromycin)
Oral/IV/topical for acne, suppository for bacterial
vaginosis
Effective against G- organisms
Topical use only
For common bacterial infections of conjunctiva
and lids
Available alone or with other drugs, example:
-Neosporin ointment = Polymyxin B + Bacitracin +
Neomycin
-Polysporin = Polymyxin B + Bacitracin
-Polytrim = Polymyxin B + Trimethoprim
ophthalmic
Used exclusively as a single IM dose for
Gonorrhea in patients allergic to PCN or for PCN
resistant strains of gonorrhea
For travelers diarrhea from noninvasive strains of
E. coli

Inhibits translocation aa from ribosome to P

site (to growing end of peptide chain)
Penetrates tissue well (except CNS)

Ointment and cream

Alternate for Impetigo from group A strep or S.
Aureus (1st choice is dicloxacillin)

Binds bacterial isoleucyl tRNA synthetase

(does not affect mammalian form)

Polymyxin B

Spectinomycin
Rifaximin
Mupirocin

CIDAL cationic detergent

Serious and fatal blood dyscrasias limit

use to resistant meningitis and other serious
infections
-Leukopenia, thrombocytopenia and fatal
aplastic anemia
Gray Baby syndrome from inhibition of
cytochrome p450 due to 1) insufficient
glucuronyl transferase- can conjugate; 2)
underdeveloped renal function- cant
eliminate
Increased levels interfere with
mitochondrial ribosomes => depressed
respiration, CV collapse, cyanosis
Superinfection colitis (C. difficile)
Arthralgias / myalgias (30-40%)
Hyperbilirubinemia (25%)
Severe venous irritation
Vancomycin-resistant E. faecium

5-HT toxicity when with drugs that enhance

5-HT
Risk of colitis & thrombocytopenia
Chronic use- lactic acidosis and peripheral
neuropathy (irreversible); optic neuropathy
(reversible) => DO NOT use >28days
Risk of pseudomembranous colitis (C.
difficile)
Immunomodulatory activity

Very nephrotoxic and neurotoxic

(neuromuscular block) => TOPICAL ONLY

Related to aminoglycosides but STATIC

Binds DNA-dependent RNA polymerase

Flatulence, abdominal pain, urgency to

defecate

Retapamulin
(Altabax)
Nitrofurantoin
(Macrodantin)

Topical
Pleuromutilin for impetigo
Tx and prevent G+/G- UTIs
Poor systemic levels- local action in tubules

Blocks acceptor & donor sites of peptidyl

transferase
Reduced by urinary tract bacteria to
reactive intermediates that damage DNA

Daptomycin
(Cubicin)

CIDAL lipopeptide 1x/d injection for G+ & MRSA

skin infections
NOT for pneumonia (inactivated by surfactant)
IV for life threatening Plasmodium falciparum
(Quinine- sister- oral only)
Penetrates tissues & biofilm, lung cavities &
abscesses
Most G+ and many G-; staph and MRSA,
intracellular and extracellular
Used only with other Rx (careful to avoid
selection)

Depolarizes cytoplasmic membrane, inhibits

DNA, protein synthesis

Quinidine
Rifampin
(Rifadin)

Acute: fever, chills, cough, infiltrates

Chronic: malaise, DOE (Dyspnea on
exertion), altered PFTs (pulmonary function
test), pneumonitis, fibrosis
Colors urine brown
May lead to death (pulmonary reactions0
creatine kinase (CK)

Anti arrhythmic
Inhibits DNA-dependent RNA polymerase
Excreted through bile- enterohepatic
recirculation
DO NOT give for <2weeks (flu-like sys)
Enzyme inducer (CYP450) => may hasten
clearance

Red-orange color to urine, feces, saliva,

sweat, tears (stain soft contacts)
Rash, fever, nausea, vomiting
Jaundice
Hepatitis rare if normal liver; risk with
liver disease, EtOH, age