Antibacterial Drug Class Review

“Broad-spectrum antibiotics are not a substitute for rational thought.” – anon

For all, in general learn: spectrum of activity, pharmacology, pharmacokinetics and

pharmacodynamics, and primary adverse effects

Beta-Lactams

Class effects:

MOA

Pharmacokinetics

AEs

Penicillins (PCNs)

Natural penicillins – Penicillin G, Penicillin V

Spectrum

Uses, DOC

Aminopenicillins - Ampicillin, Amoxicillin

AEs

Spectrum

Uses, DOC
 Antistaphylococcal PCNs - Nafcillin, Oxacillin, Methicillin, Dicloxacillin

PK

AEs

Spectrum

Uses, DOC

Antipseudomonal PCNs - Piperacillin, Ticarcillin, Mezlocillin, Carbenecillin

Spectrum

AEs

Uses

Beta-lactam/beta-lactamase inhibitors - Piperacillin/Tazobactam,

Amoxicillin/Clavulanate, Ampicillin/Sulbactam,

Ticarcillin/Clavulanate, Ceftolozane/tazobactam (2015)

MOA

Spectrum

Uses

Cephalosporins

MOA

Allergic cross-reactivity with PCNs

1st Generation

Cefazolin, Cephalexin, Cefadroxil, Cephalothin

 Spectrum

Uses

2nd Generation

Cefamandole, Cefuroxime, Cefoxitin, Cefotetan, Loracarbef

Spectrum

Uses

3rd Generation

Ceftriaxone, Ceftazidime, Cefotaxime, Cefpodoxime, Cefixime

Spectrum

Uses

Resistance

4th Generation

Cefepime

Spectrum

Uses

Anti-MRSA Cephalosporin (!)

Ceftaroline

Spectrum

Uses
 Cephalosporin/beta-lactamase inhibitor combination

Ceftolozane/tazobactam

Spectrum

Uses

Carbapenems – Imipenem/Cilastatin, Meropenem, Ertapenem, Doripenem

MOA

Spectrum

Uses

AEs, differences in spectrum

Allergic potential

Monobactams – Aztreonam; not quite beta-lactam

Spectrum

Allergic potential

Uses

Fluoroquinolones – Ciprofloxacin, Ofloxacin, Levofloxacin, Moxifloxacin, Gemifloxacin

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Resistance
Aminoglycosides – Gentamicin, Tobramycin, Amikacin, Neomycin, Streptomycin

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Macrolides – Erythromycin, Clarithromycin, Azithromycin; Ketolides – Telithromycin

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Non-absorbed, limited spectrum macrolide – Fidaxomicin

Pharmacokinetics

Spectrum

Uses

Tetracyclines – Tetracycline, Doxycycline, Minocycline; Glycylcyclines – Tigecycline

MOA

Pharmacokinetics

AEs
 Spectrum

Uses

Trimethoprim/Sulfamethoxazole

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Glycopeptides – Vancomycin, Teicoplanin (not in US)

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Lipoglycopeptides – Telavancin, Oritavancin, Dalbavancin

MOA

Pharmacokinetics

AEs

Spectrum

Uses
Metronidazole

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Lincosamides – Clindamycin, Lincomycin

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Nitrofurantoin

MOA

Pharmacokinetics

AEs

Spectrum

Use

Oxazolidinones – Linezolid, Tedizolid

MOA

Pharmacokinetics (Tedizolid eliminated hepatically only)

 AEs

Spectrum

Uses

Cyclic lipopeptides - Daptomycin

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Polymyxins – Colistin (colistimethate for injection), Polymyxin B

MOA

Pharmacokinetics

AEs

Spectrum

Uses

Rifamycins – Rifampin, Rifabutin, Rifaximin, Rifapentine

MOA

Pharmacokinetics

AEs

Spectrum

Uses
 Resistance

Streptogramins - Quinupristin/dalfopristin

MOA

Pharmacokinetics

AEs

Spectrum

Uses