Drug class Drug

Aminoglycosides

beta-lactams (Penicillins through

monobactam)

Penicillin G
Penicillin V
Ampicillin/Amoxacillin
Amoxacillin + clavulanate
Penicillins
Piperacillin + tazobactam
Ticarcillin + clavulanate
Nafcillin

Cephalexin (1st generation)

Cefuroxime (2nd generation)

Cephalosporins

Ceftriaxone (3rd generation)

Cefepime (4th generation)

Meropenem
Carbapenems
Imipenam
Monobactam Aztreonam

Glycopeptide Vancomycin

Ciprofloxacin; Levofloxacin;
Fluoroquinolones Moxifloxacin

Nitroimidazole Metronidazole

INH + PZA + EMB + RIF, standard 6

Antimycobacterials month regiment for TB

Isoniazid (INH)
 Rifampin (RIF)

Pyrazinamide (PZA)

Ethambutol (EMB)

Tetracyclines Tetracycline, Doxycycline

Sulfonamides

Erythromycin, clarithromycin,
Macrolides azithromycin

Lincosamide Clindamycin

Lipopeptide Daptomycin
Oxazolidinone Linezolid

Chloramphenicol Chloramphenicol
Cidal or static Administration

Cidal, with post-antibiotic effect IV

Indirectly cidal through activation of

autolysins, and in actively growing
bacteria only

IM and IV only
oral penicillin G
oral
oral
IV only
IV only
IV only

Orally available

Parenteral
 IV, IM, not PO

cidal IV (oral for C. diff)

cidal

cidal Oral or IV

oral

cidal oral
cidal oral

cidal oral

Static oral

Static orally available

Static orally available

Static orally active

Static orally active

Cidal
Static ?

static
Mechanism Organisms affected

Inhibit protein synthesis (30s) Gram negative

Irreversibly binds to and inhibits

transpeptidase, can't form peptide bond Gram positive, some gram negative if can
between glycine and D-alanine in get through outer membrane
peptidoglycan synthesis

Gram negative coverage

Anaerobic gram negative coverage
Pseudomonas coverage
Pseudomonas coverage
S. aureus coverage

Both + and - but more active against gram

+

Both + and - but more active against gram

+

Both + and - but more active against gram

+

Both + and - but more active against gram

+

Gram positive and negative, also covers

anaerobes
Gram positive and negative, also covers
anaerobes
 Gram negative aerobes only
(aminoglycoside-like)

binds tightly to D-ala-D-ala residue during

Gram positive only
transport, can't link peptidoglycan

Inhibits DNA gyrase and topoisomerase IV, Wide range

doesn't bind human enzymes

Prodrug --> reduced by ferrodoxins to

form nitro radical --> becomes highly Anaerobes, microaerophiles; gram
active DNA alkylating agent; O2 recycles to positive and negative
inactive form so inactive in environments
with O2

Mycobacterium

pyridoxine (B6) analog that is bacteriocidal

by virtue of inhibiting mycolic acid
synthesis
bacteriocidal inhibitor of RNA polymerase

cidal prodrug (-COOH) with active form

that inhibits FA synthesis

disrupts cell wall synthesis (arabinosyl

transferase)

broad spectrum: (gram + and -),

inhibits 30s ribosomal subunit mycoplasma, rickettsiae, chlamydial
infections, acne

inhibits folate metabolism (dihyropteroate Broad spectrum

synthetase)

inhibits 50s ribosomal subunit

Anaerobic coverage, but not effective

inhibits 50s ribisomal subunit against most aerobic and gram negative
bacteria

Disrupts bacterial membrane function Gram positive

Inhibits protein synthesis

gram positive and negative, aerobic and

binds irreversibly to 50s anaerobic
Resistance mechanism Side effects

Covalent modifications to targets Nephrotoxic (6-10%); Ototoxic (2-10%)

(acetylation, phosphorylation)

Alteration of porin channels to limit access

in gram negatives; decreased affinity of
PBPs for beta-lactams (MRSA); beta- Allergy, neurotoxicity
lactamases (most common)

well tolerated

neurotoxicity, which led to its being

supplanted by meripenam
 redman syndrome' (too rapid infusion,
(VRE) - D-ala-D-ala --> D-ala-D-lactate, histamine release); thrombophlebitis (vein
inflammation related to clot); ototoxicity;
vancomycin can no longer bind increased nephrotoxicity when administered
with aminoglycoside

GI disturbances most common including

nausea, vomiting, cramping (3-17%); then
CNS effects (mild headache, dizziness, 1-
Rare because of 2 targets; cross resistance 11%); rashes, including photosensitization;
does occur achilles tendon rupture (rare); arthropathy
occurs in immature test animals, thus FQNS
not given during pregnancy and usually not
to children

Headache, nausea, dry mouth, metallic

Rare, but can have reduced compliment of taste, dark urine, Ethanol contraindicated
ferrodoxins, which is usually overcome by since inhibits EtOH metabolism and get
increased dosage acetaldehyde toxicity, rare neurotoxic effects
like seizures and convulsions

Monitor LFTs (liver function) since main

adverse event is hepatitis

HEPATOXICITY (10-20% of ptns with

subclinical evidence, clinical hep in 0.6%,
fatal in 0.2%); peripheral neuropathy
(prevented by coadministration of
pyridoxine (B6)); negative interaction with
phenytoin (inhibits metabolism); occasional
GI intolerance; rarely optic neuritis and
marrow suppression
 HEPATOTOXICITY (2.7%); orange coloration
of precious bodily fluids (tears, sweat,
urine); GI intolerance; flu-like symptoms

Most to least - Hyperuricemia

(asymptomatic); non-gouty polyarthralgia
Mutations in activating enzyme (40%); HEPATOTOXICITY (dose related,
increases w alcohol); GI intolerance, gout

Most to least - optic neuritis (dose

dependent, get baseline vision and color
discrimination testing); GI; rare ones are -
gout, peripheral neuropathy, confusion and
dizziness, interstitial nephritis

GI; deposition in bone and teeth (not used

in patients under 8 years); photosensitivity;
Widespread resistance through increased hepatotoxicity (esp in pregnant women);
eflux and altered target multiple drug interactions, possible oral
contraceptive failure due to disruption of
microbial flora

Widespread resistance Allergic reactions common (skin)

GI, negative drug interactions (not azithro),

macrolides are among the least noxious
antibiotics
Infamous for association with antibiotic
associated colitis (i.e. overgrowth of C. diff
that produces toxin)
 Variety of toxicities when taken for more
than two weeks, including BM suppression,
low platelet counts, and peripheral
neuropathy

GI; dose related reversible suppression of

plasmid encoded chloramphenicol red cell production (aka dose related
anemia); gray baby syndrome in infants that
acetyltransferase --> inactivates drug still haven't developed effective glucuronic
acid conj. system
pharmakokinetics Uses

Very low Vd (0.2-0.3 L/kg), doesn't UTIs (since secreted unchanged into
perfuse well; secreted unchanged into urine)
urine

not metabolized, renal clearance; T1/2

is 30-90 minutes; large Vd but poorly
distributed into eye, prostate, CNS

Animal bites

S. aureus

Still one of most widely used antibiotics

for prophylaxis during surgery

long half life, can dose twice per day as

opposed to 4x per day for other gonorrhea
cephalosporins

renal clearance (70%) hospital acquired resistant infections

hospital acquired resistant infections

Good penetration into CNS

Trichomoniasis (T. vaginalis), amebiasis

good oral availability, good tissue (E. hystolytica), and bacterial infections
penetration including CNS (high Vd) by bacterioide speies (i.e. C. diff, H.
pylori)

Tuberculosis and Leprosy

Prophylaxis of latent Tb, treatment of

Well absorbed, good penetration (high active Tb, surgical prophylactic in
Vd), T1/2 of 80-180 min, daily or weekly combination with a beta lactam, or in
dosing regimens combination with cipro for bacterial
meningitis exposure
Well absorbed, deacylated in liver,
extnesive enterhepatic cycling, 20% of
drug appears in urine

Well absorbed from GI tract, widely

distributed (high Vd), excreted by
glomerular filtration

well absorbed from GI tract, widely

distributed, excreted by glomerular
filtration

Generally not used, exception being

when it is combined with trimethoprim
(inhibits dihydrofolate reductase) at 5:1
metabolism, fixed dose in combo known as co-
High Vd, some liver trimoxazole. This combo is consistently
excreted with urine bacteriocidal, and often first use for
UTIs, pneumocystis (pneumonia
caused by fungus), and can be used to
treat URIs

once a day dosing that penetrates well

into phagocytes (think intracellular primary indication is URIs
bacteria)

Both of daptomycin and linezolid are

expensive and relatively toxic, but are
used because they are active against
VRE and MRSA

mostly metabolized in liver
Both of daptomycin and linezolid are
expensive and relatively toxic, but are
used because they are active against
VRE and MRSA
rarely used in US due to resistance,
potential toxicity, but sometimes used
for serious rickettsial infection such as
typhus and rocky mountain fever; also
an alternative to beta lactams for
treatment of bacterial meningitis in
patients allergic to penicillin; used
topically for eye infections
Coadministrations other

Monitor plasma concentrations due to

narrow therapeutic index

Large therapeutic index, know penam

Combine with B-lactamase inhibitors and cepham structures for boards; all
mycoplasma resistant to beta-lactams
(i.e. clavinulinic acid, combined with because no cell walls, fungi also
amoxicillin is the DOC for animal bites) resistant because cell wall very
different

Used instead of methicillin which is

toxic

Only cephalosporin used on outpatient

basis due to long half life

As increase generations, more gram

negative coverage and less resistance
to beta-lactamases

Cilastatin (to prevent metabolism) original "guerilla"-cillin

Non-cross allergenic with other beta
lactams

evokes cancer in rodents at higher

doses (DNA adducts formed) and might
be a teratogen but no evidence of
cancers or birth defects in human

MDR-TB (resistance to INH and RIF);

XDR-TB (resistance to INH + RIF +
fluoroquinolones + 1-3 second line
agents)
 strong inducer of p450 enzymes which
decreases efficacy of oral-
anticoagulants and oral contraceptives

divalent cations and antacids interfere

with gut absorption

trimethoprim

almost not developed due to skeletal

muscle activity
*cephalosporins tend not to
get enterococci - this is one
of their big disadvantages

*cephalosporins tend not to

get enterococci - this is one
of their big disadvantages

*cephalosporins tend not to

get enterococci - this is one
of their big disadvantages

*cephalosporins tend not to

get enterococci - this is one
of their big disadvantages
some of the organisms you
can use it against are
Pseudomonas, Enterobacter,
E. coli, Haemophilus,
Klebsiella, Proteus, and
Serratia