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Class/Drug MOA Coverage Adverse Effects Other Features

Cell Wall Inhibitors


PCNs:
PCN G, V
Ampicillin, Amoxicillin
Methicillin, Nafcillin
Piperacillin
Bactericidal
B-lactam abx binds to PBP
inside bacterial cell wall
inhibits cross-linkage
(transpeptidation) of cell walls
as they are made lose
structural & osmotic integrity
cell lysis
GP: S. viridans, S. pyogenes, oral
anaerobes, syphilis, Leptospira
Synergistic w/aminoglycosides
PCN G (IM): DOC for syphilis
PCN V (PO): anaerobic activity good for
dental infections
Ampicillin (IV) & amoxicillin (PO):
Amoxicillin URI due to Strep
Same GP as PCN, E. coli, Lyme disease,
GN rods (H. flue, Listeria, E. coli, Proteus,
Salmonella)
PCNase-res PCNs (PRPs): oxacillin,
cloxacillin, dicloxacillin, nafcillin
Ineffective against IC bacteria
Type I HSR: rash, angioedema,
anaphylaxis
Diarrhea
Interstitial nephritis
Indications
Otitis media
UTIs in pregnancy
Dental infections
Enterococcal infections
Listeria monocytogenes
Lyme disease
Prophylaxis against infection in
pts w/sickle cell disease
2 mechs of res: alterations in
PBPs (MRSA) or B-lactamases
Cephalosporins:
1
st
-gen (cefazolin IV,
cephalexin)
2
nd
-gen (cefaclor,
cefoxitin, cefuroxime,
cefotetan)
3
rd
-gen (ceftriaxone,
cefixime, cefotaxime,
ceftazidime)
4
th
-gen (cefepime)
5
th
-gen (ceftaroline)
Most can be given IV
All gen: S. viridans, Strep A/B/C, E. coli,
Klebsiella, Proteus
1
st
-gen: substitutes for PCN & cover
Proteus, Klebsiella, E. coli
2
nd
-gen: more GN/less GP; cover H. flue,
N. gonorrheae, Enterobacter spp
3
rd
-gen: more GN/less GP; cross BBB
can tx CNS infec
4
th
-gen: most broad-spectrum also
cover Psuedomonas, Neisseria, MSSA;
better staph coverage than 3
rd
-gen
5
th
-gen: good against MRSA
HSR: allergic cross-rxn w/PCN in
10%
2
nd
-gen: bleeding diathesis
(reversible w/vit K), disulfiram-
like rxn to alcohol
3
rd
-gen: assoc. w/abx-induced C.
diff infection
1
st
-gen: for surgical prophylaxis
or minor forms of cellulitis
Cefuroxime (2
nd
): CAP
Cefoxitin (2
nd
): abd infec (i.e.
peritonitis)
Ceftriaxone (3
rd
): gonorrhea
(IM), empiric tx of meningitis (IV)
Cefepime (4
th
): empiric therapy
in nosocomial infections, febrile
neutropenia
5
th
-gen: uncomplicated skin &
soft-tissue infections (approved)
Vancomycin Interferes w/cross-linkage of
PTG chains (diff site of action
than PCNs), damages cell
membranes
Staph infections res to other B-lactams
(MRSA) or if PCN-allergic; NOT for GN
PO form for C. diff infection
Synergistic w/aminoglycoside to tx
enterococcal infection
Fever, nephro & ototoxicity
Red man syndrome: flushing due
to infusion-induced histamine
release slow infusion, give
anti-histamines
Must f/u serum levels in
prolonged tx, adjust dose for
renal insufficiency; VRE
Carbapenems:
Imi, Erta, Dori, Mero
Synthetic B-lactams; more res
to B-lactamases & PCNases
PCN-res pneumococci, Pseudomonas,
anaerobes, Enterobacter; GN sepsis
N/V, neutropenia, reduce
seizure threshold (imipenem)
Combine imipenem w/cilastatin
to prevent renal toxicity

Monobactams:
Aztreonam
1 of the 2 rings in B-lactams;
retains res to B-lactamases
Aerobic GN rods: Pseudomonas,
Klebsiella, Serratia
Less cross-reactivity w/PCN,
good for PCN allergy

B-lactamase Inhibitors:
Sulbactam, Tazobactam,
Clavulanic acid
Combined w/PCNs to enhance
antimicrobial activity
Amoxicillin + clavulanic acid =
Augmentin
Bacitracin Inhibits transport of PTG Effective against GP Very nephrotoxic Topical only
Protein Synthesis Inhibitors (bind to BACTERIAL ribosome)
Tetracycline:
Tetracycline
Doxycycline
Minocycline

Tigecycline (in related
class glycylcyclines)
Binds to 30S ribosome
Bacteriostatic
IC bacteria: Chlamydia, rickettsial
diseases (RMSF), Mycoplasma,
spirochetes
GN Vibrio cholera
Borrelia burgdorferi (Lyme disease)
Uncomplicated RTIs (sinusitis, bronchitis)
GI: epigastric pain, N/V
Deposits in calcified tissues
(teeth & bones of fetus if during
pregnancy, kids < 8 yo)
permanent discoloration of
teeth, stunting of growth,
skeletal deformities
Phototoxicity
Hepatotoxicity (in pregnancy)
Tigecycline: broad-spectrum,
evades res mechs that make
other tetracyclines less active
C/I
Pregnancy
Kids < 8 yo
Renal insuff (except doxy)
Dont take w/milk or antacids
(decreased absorption)
Res is common
Macrolides:
Azithromycin
Clarithromycin
Erythromycin (used less
as abx b/c of SE &
frequent dosing)
Bind to 50S ribosome
Bacteriostatic (cidal at high
dose)
IC bugs: Mycoplasma, Chlamydia,
Legionella
Clarithromycin: Staph, strep, Mycoplasma
pneumonia (DOC), Legionella (DOC), part
of H. pylori therapy, H. flue
Erythromycin: Staph, strep, alt to PCN G if
allergic (i.e. tx of chlamydia in pregnancy
to avoid tetracycline), GI stimulant
Azithromycin: H. flue, M. catarrhalis
GI: epigastric pain, N/V (esp
w/erythromycin)
Cholestasis
QT interval prolongation (esp
w/erythromycin)
C/I
Dont give erythromycin to pts
w/liver failure (metabolized in
liver)
Erythromycin & clarithromycin
interact w/many drugs due to
inhibitory effect on P450 system
Aminoglycosides:
Gentamicin,
Streptomycin
Tobramycin
Amikacin, Neomycin
Bind to 30S ribosome
Bactericidal
GN aerobes: E. coli, Pseudomonas,
Acinetobacter, Klebsiella
Combined w/ampicillin or other B-
lactams for complicated UTIs, meningitis
Combined w/anti-pseudomonal PCN to tx
No activity against anaerobes
Ototoxicity irreversible
hearing loss if infused too
quickly; baseline & follow-up
hearing tests required for pts on
long-term therapy
Nephrotoxicity renal
insufficiency or ATN; toxicity is
dose-related
Most are given IV
Check peak & trough levels to
avoid drug toxicities
Clindamycin Binds to 50S ribosome Anaerobes, GM cocci (Strep, Staph)
Can use if allergic to cephalexin (Keflex)
Abx-assoc. diarrhea (C. diff
colitis)

Chloramphenicol Binds to 50S ribosome; can
also interfere w/human
ribosomal activity can be
toxic
Anaerobes, rickettsiae
Penetrates CSF
Aplastic anemia
Gray baby syndrome: cyanosis
due to respiratory depression &
CV collapse
Inhibits P450 sytem
potentiates effect of other drugs
Linezolid GP: Strep, Enterococci, MRSA Thrombocytopenia (monitor
blood count w/prolonged
therapy)
Peripheral neuropathy
w/extended tx regimen
Inhibits MAO serotonin
syndrome when given w/pro-
serotonin agents (i.e. SSRIs)
Good oral bioavailability
Fluoroquinolones:
Levo, Cipro, Oflo, Moxi,
Gemi
Direct inhibitors of bacterial
DNA synthesis
Inhibit bacterial DNA gyrase &
topoisomerase IV blocking
replication of bacterial DNA
Bactericidal
GN: Pseudomonas, E. coli, Proteus,
Legionella, gonorrhea
GP: variable
Levo & moxi: good GP so good for CAP
Only moxi has anaerobic coverage
Cipro: UTIs, acute diarrhea due to enteric
bacteria (travelers diarrhea)
Best tx for CAP
GI: N/V/D
CNS: dizziness, headache,
lightheadedness
Nephrotoxicity
Cartilage damage in kids
Tendinitis & tendon rupture
C/I
Reduced absorption if taken w/
divalent cations (i.e. antacids
that contain Mg)
Adjust for renal insufficiency
Nursing mothers & kids
Pregnancy (cartilage damage)
TMP Inhibits DHFR blocks
bacterial DNA synthesis
Synergistic w/sulfonamides
combined w/SMX which
inhibits 2
nd
unique step in
bacterial folate synthesis
Prophylaxis & tx of PCP
S. aureus, some MRSA, UTIs, Shigella,
Salmonella
Folate def megaloblastic
anemia
Hematologic (BM suppression)
Renal (inh Cr secretion)
Hyperkalemia

Sulfonamides Analogs of PABA that inhibit
enzyme DHP synthase (needed
for folic acid) inhibits DNA
synthesis
GP & GN
Monotherapy
Silver sulfadiazine (topical soln): in burn
pts to prevent infection
Na sulfacetamide (ophthalmic ointment)
: bacterial conjunctivitis
Rash, photosensitivity
N/V/D
Stevens-Johnson syndrome
C/I n pts w/G6PD can
precipitate a hemolytic response
Metronidazole Forms cytotoxic cmpd through
redox rxn which damages DNA
Bactericidal
Anaerobes
Protozoa: E. histolytica, Giardia,
Trichomonas
PO good in tx C. diff diarrheal infection
Disulfiram-like rxn if taken
w/alcohol
Headache, metallic taste
Hepatitis, pancreatitis (rare)
Enhances effects of warfarin in
concomitant use (inhibits
warfarin metabolism)
monitor warfarin levels
Nitrofurantoin Inactivates several bacterial
enzyme systems including
acetyl-CoA
Uncomplicated lower UTIs due to E. coli
or other common community-acquired
bugs
NOT for pyelonephritis or infections
outside urinary ssytem


Quick Hits
Best abx for anaerobes: PCN (G, VK, amoxicillin, ampicillin), clindamycin, metronidazole (for abd/GI)
Best abx for MRSA: vancomycin
Indications for aminoglycoside use in tx serious infections caused by aerobic GN rods: sepsis, complicated UTI, pneumonia, osteomyelitis, complicated intra-abd infections
Best abx for GN rods (E. coli, Klebsiella, Proteus, Enterobacter, Pesudomonas): quinolones, aminoglycosides, carbapenems, piperacillin, aztreonam, cephalosporins