Overview by Mechanism

Antibiotic Grouping by Mechanism

Cell wall synthesis inhibitors Penicillins
Cephalosporins
Vancomycin
Beta-lactamase inhibitors
Carbepenems
Aztreonam
Polymycin
Bacitracin

Protein synthesis inhibitors Inhibit 30S subunit

Aminoglycosides (gentamycin)
Tetracyclines

Inhibit 50S subunit

Macrolides
Chloramphenicol
Clindamycin
Linezolid
Streptogramins

DNA synthesis inhibitors Fluoroquinolones

Metronidazole

RNA synthesis inhibitors Rifampin

Mycolic acid synthesis inhibitors Isoniazid

Folic acid synthesis inhibitors Sulfonamides

Trimethoprim

Classification & Indications

Cell Wall Synthesis Inhibitors

 Penicillins
(Bactericidal: inhibits bacterial cell wall synthesis via competitive inhibition of the transpeptidase
enzyme)
Class Name of Drug(s) Indications
Penicillin Penicillin G S. pnuemoniae
Aqueous (crystalline) S. pyogenes (group A
penicillin G strep)
Procaine penicillin G N. meningitidis
Benzathine penicillin G T. pallidum
Penicillin V L. monocytogenes
A. israelii
P. multocida

Aminopenicillins Ampicillin gram-negative

Amoxicillin coverage
Enterococci (group D
strep)
All others listed above

Penicillinase-resistant penicillins Methicillin Penicillinase-

Nafcillin producing S. aureus
Oxacillin All others listed above
Cloxacillin
Dicloxacillin

Antipseudomonal penicillins Carbenicillin P. aeruginosa

Ticarcillin Anaerobic bacteria
Piperacillin All others listed
above

Cephalosporins
(Bactericidal: inhibits bacterial cell wall synthesis via competitive inhibition of the transpeptidase
enzyme)
1st generation Cefazolin Gram-positives
Cephalexin Some gram-negatives
Skin infection
prophylaxis

2nd generation Cefoxitin Gram-positives

Cefaclor Improved gram-
Cefuroxime negative coverage
Anaerobes
3rd generation Ceftriaxone Serious gram-
Cefotaxime negative infections
Ceftazidime Meningitis
Pseudomonas

Same coverage as
cephalosporins +
expanded
Cefepime Pseudomonas
4th generation
coverage + expanded
gram-positive
coverage

Expanded gram-
positive and gram-
Ceftaroline negative coverage,
5th generation
non-suitable coverage
of Pseudomonas

Other Cell Wall Inhibitors

Vancomycin (bactericidal: Vancomycin MRSA
inhibits bacterial cell wall synthesis by Patients with PCN
disrupting peptioglycan cross linking) or ceph allergies
S aureus
S epidermidis
C. difficile

Beta-lactamase inhibitors Clavulanic acid Gram-positive

(beta-lactamse inhibitors that prevent the Sulbactam S. aureus
degradation of beta-lactam antibiotics) Tazobactam S. epidermis
Gram-negative
E. coli
Klebsiella

Carbapenems Imipenem (+ cilastatin) Broadest activity of

(Inhibits bacterial cell wall synthesis) Meropenem any antibiotic (does
Doripenem NOT cover MRSA,
Ertapenem Mycoplasma, and
some Pseudomonas)

Aztreonam Aztreonam Gram-negative rods

(inhibits bacterial cell wall synthesis) Aerobes
 Difficult-to-treat
hospital-acquired
infections

Polymyxins Polymyxin B Topical gram-negative

Polymyxin E infections

Bacitracin Bacitracin Topical gram-positive

infections

Protein Synthesis Inhibitors

Anti-30S Ribosomal Subunit
Aminoglycosides Gentamicin Severe gram-negative
(bactericidal) Neomycin infections
Amikacin Aerobes only
Tobramycin
Streptomycin

Tetracyclines (bacteriostatic) Tetracycline Chlamydia

Doxycycline Rickettsia
Minocycline Bacteria without
Demeclocycline peptidoglycan cell
walls
Spirochetes
V. cholerae
H. pylori

Anti-50S Ribosomal Subunit

Macrolides Erythromycin Outpatient URI, LRI
Azithromycin Atypical pneumonia
Clarithromycin STDs
Gram-positive cocci

Chloramphenicol Chloramphenicol H. influenzae

(bacteriostatic) Bacterial meningitis
Brain abscess
Bacteroides fragilis
Clindamycin Clindamycin Anaerobes above the
(bacteriostatic) diaphragm
Female GU
TSS
Linezolid (variable) Linezolid Resistant gram-positives
(MRSA, VRE)
Streptogramins Quinupristin VRE
Dalfopristin GAS and S. aureus
skin infections
Note: bacteriocidal
when used together

DNA Synthesis Inhibitors

Fluoroquinolones
(Bactericidal: inhibit DNA gyrase enzyme, inhibiting DNA synthesis)
1st generation Nalidixic acid Gram-negative UTIs

2nd generation Ciprofloxacin Gram-negative UTIs

Norfloxacin Gram-negative GI
Enoxacin tract
Ofloxacin Pseudomonas
Levofloxacin

3rd generation Gatifloxacin As above + gram-

positives

4th generation Moxifloxacin As above + gram-

Gemifloxacin positives + anaerobes

Other DNA Inhibitors

Metronidazole (bacteridical: Metronidazole (Flagyl) Bacteria AND
metabolic byproducts disrupt DNA) protozoa
Anaerobes below the
diaphragm
C. difficile
H. pylori

RNA Synthesis Inhibitors

Rifampin Rifampin TB
(bactericidal: inhibits RNA transcription) Leprosy
H.
influenzae prophylaxis
Antistaphylococcal

Mycolic Acids Synthesis Inhibitors

Isoniazid Isoniazid TB
Latent TB

Folic Acid Synthesis Inhibitors

Sulfonamides Sulfamethoxazole Respiratory (S.
(SMX) pneumoniae, H.
Sulfisoxazole influenzae)
Sulfadiazine GI (enterics)
UTIs
PCP and T. gondii

Trimethoprim Trimethoprim See Sulfonamides

Pyrimethamine Pyrimethamine Malaria

T. gondii

Miscellaneous
Drugs Mechanism of Action Indications and Side Effects
Uncertain mechanism: Part of RIPE therapy
potentially accumulates for TB
in cells dsirupting Can cause
Pyrazinamide
membrane potential and hyperuricemia and
fatty acid synthesis hepatoxicity

Part of RIPE therapy

for TB and used
Inhibits
for M. avium-
arabinosyltransferase
intracellulare
Ethambutol (inhibiting production of
Can cause optic
mycobacterium cell wall)
neuropathy (red-green
color blindness)

Multi-resistant gram-
positives such as
Lipopeptide that disrupts MRSA and VRE
Daptomycin cell membrane Can cause myopathy
(elevated CK and
rhabdomyolysis