ANTIBIOTICS SUMMARY
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN
Antibiotics Mechanism
Benzylpenicillin (G -lactam ring binds pencillin-
or V). binding proteins (PBPs)
break the strain ring
G: IV covalent bond with PBPs
V: PO catalytic serine covalently
inhibits X-linking of PG.
PBP have a reactive serine that is
used to X-link D-Ala-D-Ala of one
NAM to a L-lysine in another
NAM, via a pentaglycine chain
(varies).
No action on bacteria
without PG cell wall e.g.
chlamydia, mycoplasma,
atypicals.
Amoxicillin >
Ampicillin (in terms of Recall: G(-) have outer cell
bioavailability) membrane and thin PG cell
wall. May have porins.
Amox: PO or IV
Flucoxacillin and
methicillin
IV
Piperacillin
IV
Pg 1
Spectrum Important resistance S/Es or interactions
mechanism
Narrow, useless for G(-) Any -lactam can cause group I
and aerobes e.g. in gut Beta-lactamases HS (IgE-mediated) = usually
microbiome. immediate. Can be severe
anaphylaxis.
Use for Streptococci,
Neisseria, Spirochaetes. Others: Stevens Johnsons
Syndrome; toxic epidermal
necrolysis. AIHA (direct
Coombs mechanism)
Some risk of X-allergy (if very
severe allergy or SJS/TEN
contraindicate any -lactam
Abx); if not use another
penicillin / lactam Abx type
Extended spectrum Can be used in combination
aminopenicillin. Useful in Beta-lactamases with clavulanic acid =
RTI/UTI Gram (-)s e.g. co-amoxiclav.
Hib, E. coli; covers
Listeria
Antistaphylococcal - Intrinsically useless
lactamase-resistant for G(-). MRSA mecA
penicillin (bulky R grp). gene PBP2a
Best used for MSSA. altered binding site.
Some use in Streptococci Use vancomycin
(skin infections). instead.
Antipseudomonals Often in combination with
tazobactam (tazocin).
 ANTIBIOTICS SUMMARY Pg 2
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN

-lactam inhibitor Blocks beta-lactamases that

e.g. clavulanic acid, break down beta-lactam Abx,
tazobactam hence preserving spectrum of
activity.
Cefalexin In general, cephalosporins
Gen I have wider spectrum vs
penicillins.
PO
Most are active against SA
and Strept because stable to
Cefuroxime -lactamases.
Gen II
Variable spectrum vs
G (-)
Any cephalosporin does NOT
cover Listeria (actually
crosses CSF well but
intrinsically ineffective to
this bug) nor Enterococci
cover with ampicillin or
amoxicillin.
Inactive against Hib
Outpatient Rx for Resp,
UTI, soft tissue infections
Wide range of G (+) / (-) spread widely,
but NOT pseudomonas
Severe sepsis, including
urinary, respiratory and
soft tissue infections.
ESBL G(-) bacteria
e.g. Kleb and E. coli S/Es include hypersensitivity
can hydrolyse reactions; AIHA (both similar
cephalosporins. ESBL to penicillin); X-reactivity with
contains a plasmid penicillins.
encoding the enzyme
and therefore can
Increases nephrotoxicity of
affecting 1st to 3rd aminoglycosides (also cleared
generation renally).
cephalosporins.
Hence, switch to
carbapenems.

Inactive against anaerobes

cover with metronidazole
 ANTIBIOTICS SUMMARY Pg 3
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN

Wide range of G (+) / (-)

Ceftriaxone Ceftriaxone is given IV. but NOT pseudomonas Long t1/2 so once daily.
Gen III
High doses allow it to
IV attain high levels in CSF,
Gen III use for SERIOUS therefore used in severe
infections. infections including acute
bacterial meningitis

Good biliary penetration

(more lipid soluble).
Ceftazidine Similar activity to
Gen III ceftriaxone / cefotaxime.

IV But also an anti-

pseudomonal

Resistant to MOST -
Meropenem A carbapenem BROADEST spectrum - lactamases including Meropenem is stable to renal
lactam active against ESBL producing G(-)! dehydropeptidase I unlike other
IV MOST G(+) or (-) but not carbapenems (not inactivated).
MRSA! Carbapenemase Unlike other carbapenems, very
producing Klebsiella low risk of seizures.
and Carbapenemase
Producing HS reaction, rash, GI distress.
Enterococci (CPE)
oxa-48, NDM (New
Delhi metallo) now
developing.
 ANTIBIOTICS SUMMARY
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN
Glycopepetide that binds to
Vancomycin; D-Ala-D-Ala portion of PG
teichoplanin precursors, preventing
addition of new blocks to cell
IV (oral only if wall. Bactericidal.
dealing w C. diff)
Large molecules so must be
given IV (poor oral f)
Translation inhibitor
Aminoglycosides irreversible inhibition of
e.g. gentamicin initiation complex by binding
30S (bactericidal because
IV (poor oral f) cause misreading of mRNA)
but also blocks translocation.
Tetracyclines e.g. Translation inhibitor binds
doxycycline 30S to prevent attachment of
aminoacyl-tRNA.
PO Bacteriostatic.
Pg 4
Intrinsically Nephrotoxic monitor levels.
Most G(+) including ineffective against Ototoxic.
enterococci and MRSA G (-) because large Thrombophlebitis
molecule cannot Diffused flushing red man
penetrate outer syndrome (counter by anti-
membrane. histamines).
VRE: modification of 2-component system: vanH
deHydrogenase reduces pyruvate to
D-Ala-D-Ala to D-Ala-
D-Lac; vanA ligase D-Ala-D-Lac.
D-Lac. VanX cleaves D-Ala-D-Ala.
Staphylococci, most G(-) Requires O2 for uptake Streptococci susceptible IF this
including pseudomonas (active transport) drug is used with penicillin that
hence ineffective disrupts cell wall (synergism).
Drug resistant TB. against anaerobes!
Nephrotoxic (aminoglycoside
Streptococci also lack sugar so water soluble and
the transporter, so not eliminated renally) and
susceptible. ototoxic (especially if given
with loops).
Transferase enzymes
inactivates drug by NM blockade sometimes.
Ac, Phos or
Adenylation. Teratogen.
Most G(+), G(-). Do not take tetracyclines w
Weird bugs Borrelia Efflux or reduced cations (milk, antacids, iron
burgdorferi, Mycoplasma, uptake (plasmid- supplements): chelates &
Rickettsia, Chlamydia and encoded pumps). inhibit drug absorption via gut.
malarial prophylaxis. Resistance is
Ability to accumulate increasing. GI distress, teeth
intracellular is key. discolouration, bone growth
inhibition in children,
photosensitivity.
 ANTIBIOTICS SUMMARY Pg 5
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN

Macrolides e.g. Inhibit translocation by Atypical or severe Resistant in staph and All except azithromycin are
erythromycin, blocking translocation (23S pneumonias and strept mainly via P450 inhibitors (statins conc
clarithromycin, rRNA of 50S) causing intracellular bacteria such methylation of 23S increase). Also that of
azithromycin dissociation of growing as Mycoplasma, rRNA binding site. warfarin (vitamin K
peptide chain. Legionella, Chlamydia, producing bacteria loss).
PO or IV Mycobacterium avium
intracellulae. MACRO-lides:
Motility (GI); Arrhythmia
Also works for G (+) / (-) (torsades); Cholestasis; Rash;
Hib, Neisseria, eOsinophilia / Ototoxicity
Moraxella (reversible).

Azithromycin is used for

enterococci and
Chlamydia.

Clindamycin (a Translation inhibitor 50S Good soft tissue and Treat anaerobes above Pseudomembranous colitis (C.
lincosamide) blockade of peptide BONES / JOINTS diaphragm (lung difficile overgrowth)
translocation. infections (staph, strep, abscess, aspiration
PO anaerobes e.g. invasive pneumonia, oral
GAS infection). infections) vs
metronidazole below
Some protozoa PCP, Pf diaphragm.

Linezolid (an Translation inhibitor via Gram + including MRSA rRNA point mutation. BMS.
oxazolidinone) preventing formation of and VRE
initiation complex.
Bacteriostatic.
 ANTIBIOTICS SUMMARY
General key: GRAM +VE; GRAM VE; DO NOT GRAM STAIN
Fluoroquinolones Nucleic acid synthesis
e.g. ciprofloxacin, inhibitor. MoDA = DNA
moxifloxacin gyrase and DNA
topoisomerase IV inhibitor.
PO Cannot transcribe or replicate
and causes DNA damage.
Bactericidal.
Folate antagonist NA synthesis inhibitor.
e.g. sulphonamides
and trimethoprim SMX: dihydropteroate
(TMP-SMX = co- synthase inhibitor
trimoxazole)
PABA + pteridine -/-> DHP
PO
TMP: bacterial DHFRi
DHP DHF -/-> THF
purines, thymidine, met
Nitroimidazoles e.g. NA synthesis inhibitor,
metronidazole, damages DNA via toxic
nitrofurantoin metabolites (free radicals);
given orally (excellent f)
PO
Pg 6
Mutate DNA gyrase Antacids decrease gut
Ciprofloxacin (PO): (chromosome); efflux absorption. Many S/Es.
G (+) and G (-) including pumps (plasmid)
pseudomonas. Contraindicated in pregnant
women, nursing mums,
Use in GIT and UT. children < 18 distribute in
bones and block cell cycle.
Moxifloxacin: better for
staph, strep but NOT Torsades. Also lowers seizure
pseudomonas threshold.
Use for RESP infections in >60 yo tendonitis/ rupture
severe penicillin allergy. (or also in patients taking
Also use in MDR-TB. prednisone).
Multiple resistance SMX: HS (sulfa drug),
mechanisms e.g. nephrotoxic, kernicterus in
altered enzyme, infants, displace other drugs
decrease uptake, from albumin (e.g. warfarin),
increase PABA G6PD = hemolysis.
synthesis.
TMP: MEGALOBLASTIC
anaemia folinic acid
supplement alleviate.
Protozoa (Entamoeba and Only works in Disulfiram-like reaction
Giardia) and anerobes anaerobic severe flushing, tachy,
environment. R is hypotension, headache (do not
Nitrofurantoin: UTI common. drink). Metallic taste.