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Antibiotics & Resistance
Antibiotic classes, MOAs, and resistance
12
Biology
Undergraduate 3
05/12/2006

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Term
Aminoglycosides
Definition
Includes gentamicin, streptomycin.

MOA: Inhibit protein synthesis by binding to the 30S ribosomal subunit.

Resistance: Plasmids encode enzymes to deactivate the drug; Altered 30s ribosome that will not bind drug.

Treats: Gram - bacilli
Term
Beta-lactams
Definition
Includes penicillins.

MOA: Inhibits cell wall synthesis to cause osmotic lysis of the cell.

Resistance: Altered penicillin-binding proteins will not bind drug; Outer-membrane porin shape changes—cell impermeable; Plasmid encodes b-lactamase (opens lactam ring)

Treats: Gram + and some Gram -
Term
Polymixin B
Definition
MOA: Alters cell membrane leading to cellular leakage.

Resistance: Phosphorylation of undecaprenol.

Treats: Mostly gram +
Term
Tyrocidins
Definition
Includes: tyrocidin, gramicidin.

: Interferes with cell membrane leading to cellular leakage.
Term
Macrolides
Definition
Includes: erythromycin, azithromycin

MOA: Block translation & protein synthesis by binding to the 50S ribosomal subunit.

Resistance: Changed membrane transport system prevents drug from entering the cell.

Treats: gram +
Term
Antibiotics that interfere with the 50S subunit
Definition
A. Macrolides (erythromycin, azithromycin, clarithromycin, dirithromycin) - Gram +

B. Lincosamides (lincomycin, clindamycin) - Gram + cocci

C. Chloramphenicol (chloromycetin) - Gram + and -

D. Oxazolidinones (linezolid) - Gram +

E. Streptogramins (quinupristin and dlfopristin in combination) - Most Gram +
Term
Tetracyclines
Definition
Includes: tetracycline, doxycycline

MOA: Bind to the small ribosomal subunits so as to prevent aminoacyl transfer RNA from entering the acceptor sites on the ribosome

Resistance: New membrane transport system pumps drug out of cell

Treats: Aerobic and anaerobic Gram + and –
Term
Quinolones
Definition
Includes: ciprofloxacin, levofloxacin

MOA: Inhibit nucleic acid synthesis via topoisomerases

Resistance: Not given

Treats: Most Gram -, some Gram +
Term
Sulfonamides + Trimethoprim
Definition
Includes: Sulfamethoxazole, others

MOA: Inhibit nucleic acid synthesis via cofactor tetrahydrofolate synthesis

Resistance: Not given

Treats: Gram + & -
Term
Metronidazole
Definition
MOA: Drug is activated by microbial proteins flavodoxin and feredoxin. The activated drug puts nicks in DNA strands.

Resistance: Not given

Treats: Anaerobic Gram -
Term
Nitrofurantoin
Definition
MOA: Blocks aerobic energy production and synthesis of several cellular components (DNA, RNA, cell wall, and proteins).

Resistance: Not given

Treats: Gram – and Gram +
Term
Anti-tuberculosis drugs
Definition
A. Rifampin, treats Gram +
B. Isoniazid, treats Mycobacteria
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