Penicillin

Natural

Antistaphyloccol
Extended spectrum
Antipseudomonal

Monobactams

Cephalosporins
1st-4th generation

Vancomycin

MOA
Inhibit the transpeptidase enzyme that assists

with cross linking of peptidoglycan chains

Resistance
By production of beta-lactamase that cleaves

the beta-lactam ring to inactivate the

metabolite
Alteration in penicillin-binding proteins
Decrease penetrability of the cell wall

Side effects: type I hypersensitivity reaction

Penicillin G (IM) and V (oral, because acid stable)

Renally excreted add probenecid to increase
blood levels
Crosses blood brain barrier with inflammation
Spectrum of activity
Gram positive
Non resistant staph and strep, anthrax
With aminoglycoside for enterococcus
Gram-negative: Neisseria meningtidis
Anaerobes: Clostridium (not B fragilis)
Spirochetes: Treponema

Methicillin (IV), nafcillin (IV), oxacillin (IV),

Dicloxacillin (PO)
Resistant to breakdown by beta-lactamase

Spectrum of activity
Beta-lactamase producing staph

Not effective against gram negative organisms

MRSA treat with vancomycin

Side effects
Methicillin: interstitial nephritis (not used

clinically).

Ampicllin (PO,IV), amoxicillin (PO)

Spectrum of activity

Covers strep
Have some gram negative coverage
H. flu
E. coli
Listeria monocytogenes
Proteus mirabillis
Salmonella
Neisseria

Beta lactam inhibitors: extend the

spectrum of activity
Clavulanate
Plus amoxicillin is Augmentin
Sulbactam
Plus ampicillin is Unasyn

Side effects:
Ampicillin: diarrhea, pseudomembranous

colitis
Ampicillin rash: infectious mono

Carbenicillin (PO), ticarcillin (IV), piperacillin (IV)

Spectrum of activity

Cover pseudomonas and some aerobic and anaerobic

gram negative rods

E.coli, Proteus, Enterobacter, Citrobacter, Serratia, Klebsiella

Side effects
GI disturbances
Prolonged bleeding time (platelet dysfunction)
Beta-lactamase inhibitors: addition adds staph staph
coverage
Clavulanate

Plus ticarcillin is Timentin

Tazobactam

Plus piperacillin is Zosyn

Aztreonam (IV)
Spectrum of activity

Active against gram-negative rods, including

pseudomonas
No activity against gram-positive rods or
anaerobes

Side effects
While is a beta-lactam, it is not

contraindicated in patients allergic to

penicillin or cephalosporins

Cefazolin (Ancef) (IV), cephalexin (Keflex)

(PO), Cephaslothin (Keflin) (IV), cefadroxil
(Duricef) (PO),
Spectrum of activity

Oral cavity anaerobes except B.fragilis

Cover some gram-negatives (used in UTI)
E.coli
Cover S. pneumoniae and H. flu but not as well

as later generations

Avoid in treating URI

Cover staph, not MRSA

Used in surgical prophylaxis

Side effects:
Diarrhea

Hypersensitivity reactions
Fever
Increased liver function tests (uncommon)

Neutropenia, thrombocytopenia

(uncommon)

Respiratory and PID

Cefaclor (Ceclor) (PO), Loracarbef (Lorabid) (PO),
Cefoxitin (Mefoxin) (IV), Cefuroxime (Zinacef, IV),
Ceftin (PO), cefotetan (Cefotan, IV), cefprozil
(Cefzil, PO)
Spectrum of activity
Increased activity against S. pneumonia, H.flu
(cefuroxime is the best for URI/sinusitis)
Active against anaerobic infection including B.
fragilis, (cefoxitin, cefotetan)
Use in PID

Spectrum of activity (continued)

Covers same gram-negatives as first

generation plus h.flu, enterobacter,

klebsiella, proteus, Neisseria species

Side effects same as first generation

Pneumonia, CNS
Ceftriaxone (Rocephin, IV),
cefixime(Suprax, PO), ceftizoxime
(Cefizox, IV), ceftazidime (fortax),
cefpodoxime (Vantin, PO),
Spectrum of activity

Against s. pneumo and h.flu

Good penetration of CNS (meningitis)

Spectrum of activity continued

Used to treat N. gonorrhoeae

Cover pseudomonas (ceftazidime,

cefepime)
Poor activity against s.aureus

Side effects
Same as first and second generation
Increased risk of enterococcal superinfection

Cefepime(Maxipime IV)
Spectrum of activity

Must be methicillin susceptible staph and

strep
Gram negative bacilli including
pseudomonas

Side effects
Same as other groups

Going from first generation to fourth,

gram positive coverage lost, gram
negative gained
Do not cover MRSA or enterococcus
Avoid alcohol

May have disulfiram-like reaction

May cause bleeding disorders

Imipenem plus cilastatin(IV), meropenem

(IV)

Cilastatin inhibits breakdown of imipenem in the

kidney

Spectrum of activity

Broad spectrum gram positive, gram negative,

anerobes

Covers 90% of clinically important bacteria

Meropenem has high activity against

pseudomonas

Side effects

Can cause seizures

Action
Inhibits bacterial cell wall synthesis; binds of

portion of cell wall precursors

Bactericidal against most bacteria (except
enterococcus)

Spectrum of activity
S. aureus (including MRSA), s.epidermidis,

strep, corynebacterium diphtheriae,

clostridium

Spectrum of activity continued

Use in endocarditis, osteomyelitis, necrotizing

fasciitis
Pseudomembranous colitis (oral
vancomycin)

No coverage against gram negative

organisms

Side effects
Red man syndrome
Histamine release
No problem if drug given slowly
Ototoxicity (can be permanent)

Nephrotoxicity (increased with other

nephrotoxic drugs)

Chloramphenicol
Tetracycline
Macrolides
Aminoglycosides
Clindamycin
Linezolid

Bacteriostatic: binds to 50S ribosomal

subunit
Metabolized in the liver and enters CNS

Good choice for brain abscess

Spectrum of action
Kills most gram-positive, gram negative, and

anaerobes
Effective against Rickettsial infections (RMSF)

Side effects
Bone marrow suppression/aplastic anemia

Gray baby syndrome

Due to inability to metabolize drug to inactive
metabolites
Present with shock, abdominal distention,
cyanosis

Decrease use due to severe side effects

Short vs. long acting

Tetracycline: t1/2 6-12 hours
Doxycycline/minocycline t1/2 16-18 hours

MOA
Bacteriostatic, bind to 30S ribosomal unit
Crosses the placenta and is in breast milk
Binds to calcium and antacids
Inhibits absorption of tetracycline
Renal excretion
Doxycycline eliminated non-renal, so safe in

renal failure

Spectrum of activity
Cover gram positive and gram negative
but not drug of choice due to increased
resistance
Covers:

Rickettisal infections
Spirochete infections (Lyme disease)
Mycoplasma pneumoneae
Chlamydial infection
Minocycline for acne

Side effects:
Hepatotoxicity

GI upset: diarrhea, nausea, vomiting

Phototoxic dermatitis
Discolored teeth/decreased bone growth

(do not give to children <8 years or pregnant

women)

Erythromycin (e-mycin)
Clarithromycin (Biaxin)
Azithromycin (Zithromax)
MOA

Bacteriostatic, bind to 50S ribosomal subunit

Hepatic metabolism
Azithromycin concentrates in tissue and

releases slowly over prolonged period (t1/2

72 hours)

Spectrum of activity
Group A strep, strep pneumo, chlamydia,

mycoplasma, .flu, legionella

Mycobacterium avium can use azithromycin

Side effects:
GI upset
Cholestatic hepatitis
Inhibits cytochrome P-45
Can lead to an increase in other drugs if
metabolized by liver

Gentamycin, Tobramycin, amikacin,

streptomycin
MOA

Poor oral absorption

Eliminated by kidneys
Bactericidal; bind to 30S ribosomal subunit

and inhibit bacterial protein synthesis

Antibiotic enters bacteria by oxygen
dependent active transport
Not effective against anaerobes

Spectrum of action
Aerobic gram negative

Tobramycin more active against

pseudomonas
Amikacin reserved for the most serious
infections
Endocarditis due to enterococcus

Side effects:
Ototoxicity
Hearing loss (usually irreversible), tinnitus,
vertigo, ataxia
Nephrotoxicity
Acute tubular necrosis
Monitor serum creatinine

PO, IV, topical

MOA

Bacteriostatic, binds to 50S ribosomal subunit

to inhibit bacterial protein synthesis

Spectrum of action

Gram positive and anaerobic bacteria

Anaerobes above the diaphragm
Will cover strep pyogenes
Alternative to pcn and ceph in allergic pt

Side effects: psedomembranous colitis

MOA
Inhibits protein synthesis, binds to 50S subunit

Spectrum of activity
MRSA, VRE, corynebacterium, listeria

Side effects:
GI upset, diarrhea, headache, rash,

thrombocytopenia

Ciprofloxacin (cipro), ofloxacin (Floxin),

norfloxacin (Noroxin), Levofloxacin
(Levaquin), moxifloxacin (Avelox)
MOA

Bactericidal; binds to bacterial enzyme DNA

gyrase
Inhibits DNA replication and RNA transcription
Undergo hepatic biotransformation and are
excreted unchanged in urine
Decreased oral absorption with ingestion of
dairy and antacids

Spectrum of action
Broad spectrum: aerobic gram positive and

gram negative bacteria

UTI: due to gram neg rods and
pseudomonas
Prostatitis: good prostate penetration
Travelers diarrhea: shigeela, salmonella,
E.coli, camplobacter
URI due to pneumococci, chlamydia,
mycoplasma, h.flu, legionella
Some coverage of mycobacterium

Side effects:
N, headache, dizzy

Sensitivity to UV light
Due to damage to growing cartilage,

contraindicated in children <18 and

pregnancy

Sulfonamides
Sulfacetaminde (Sulamyd): topical

Sulfadiazine (PO or topical)

Sulfamethoxazole (PO)

Folate reductase inhibitors

Trimethroprim (PO)
Trimethroprim-sulfamethoxazole

(Bactrim)(PO, IV)

MOA
Decreased production of essential cofactors

for the synthesis of DNA, RNA, and proteins

through the blockage of tetrahydrofolic acid
production

Spectrum of action
Allergic skin rash, steven johnson syndrome

Kernicterus: displacement of billirubin which

penetrates the CNS

Bactrim: N/V, GI upset, thrombocytopenia,
leukopenia
Avoid during pregnancy; fetotoxic

MOA
Bacteriocidal, drug reduced to toxic agents

that bind intracellular macromolecules

Metabolized in the liver

Spectrum of action
Active against nearly all anaerobic and

microaerophilic bacteria including B. fragilis

Antiparasitic

Side effects:
Disulfiram reaction

Cacinogenic potential
Metalic taste

Macrobid or macrodantin (PO)

MOA:

Causes damage to bacterial DNA

Rapidly excreted in urine

Spectrum of action
Treat UTI due to E.coli, enterococcus,

S.saprophyticus

Side effects:
N/V, hemolytic anemia, pulmonary and

hepatic toxicity