ANTIBACTERIAL (general antibacterial agents)

Synthetic Antibacterial

Sulfonamides - First marketed agents in the form of sulfonamide

MOA: inhibits dihydropteroate from adding PABA to folic acid precursor

Trimethoprim - Usually taken with sulfamethoxazole (SMX-TMP)

- Analog of dihydrofolic acid
MOA: inhibits dihydropteroate from converting dihydrofolic acid to tetrahydrofolic
acid

Quinolones - Cannot be taken with metals because quinolone will precipitate

- Cannot be exposed to sun because of phototoxicity
MOA: inhibits DNA gyrase and topoisomerase IV used for DNA replication

“-floxacins”
1. Ofloxacin - UTI, bacterial COPD, gonorrhea
2. Norfloxacin - cystitis, gonorrhea, typhoid fever
3. Ciprofloxacin - RTIs, bone infections, endocarditis
4. Moxifloxacin - RTIs, endocarditis, anthrax

Nitroheteroaromatic MOA: reduced into active NH2-OH or N radical forms which interferes with DNA or RNA
compounds
1. Metronidazole - wide variety of uses
- bacterial infections: peptic ulcer, pseudomembranous colitis
- protozoal infections: giardiasis, trichomoniasis
2. Nitrofurantoin - uncomplicated UTI

Beta-Lactam Antibiotics

Penicillin - Contain beta-lactam and thiazolidine ring

MOA: inhibits bacterial transpeptidase → blocks translocation of D-Ala-D-Ala portion
of peptidoglycan → inhibits cell wall synthesis → no cell wall → DEATH

1. Benzylpenicillins - 1st ever prototype

- Fermentation-derived (natural), unstable in acid media (not
for oral)
a. Benzylpenicillin (PEN G) - IV only
b. Phenoxypenicillin (PEN V)
2. Ampicillins - semi-synthetic, better oral absorption
a. Ampicillin
b. Amoxicillin
3. Methicillin - semi-synthetic, beta-lactamase (penicillinase) resistant, very
potent
a. Dicloxacillin
b. Oxacillin
 c. Nafcillin
4. Carboxypenicillin - semi-synthetic, broad spectrum penicillin
a. Ticarcillin - formulated with clavulanic acid
- Can be used for P. aeruginosa infection
5. Ureidopenicillin - semi-synthetic, broad spectrum penicillin
a. Piperacillin - formulated with tazobactam
- Has activity with G(+) and G(-) organisms

Beta-lactamase - DO NOT possess antibacterial activity

inhibitors - Inactivate beta-;actamase enzyme
- Suicide molecule
MOA: binds to the Ser-OH of the beta-lactamase enzyme

1. Clavulanic acid (clavam)

2. Sulbactam/Tazobactam (penam)
3. Avibactam (diazabicyclocarbamoyl sulfate)