Table 1

INHIBIT

CLASSIFICATION

ANTIBIOTICS
Beta-lactamase sensitive
Natural Penicillins
(narrow spectrum)

Penicillin G (Benzylpenicillin): Procainic (pain w/ IM), Benzathine ( depot IM) Penicillin V

(Phenoxymethylpenicillin): PO

Aminopenicillins (broad
spectrum)

Ampicillin (IM/IV - poorly absorbed orally; hence, risk for C. Difficile) Amoxicillin (PO)
Positively charged amino group enhances their uptake through bacterial porin (G -ve) channels.
Change in Porin Structure -> Pseudomonas becoming resistant.

Beta-lactamase resistant (very narrow spectrum) Staphylococcus aureus change in PBPs -> MRSA
Penicillins
Methicillin (no longer made)

Nafcillin

Oxacillin

Dicloxacillin

Flucloxacillin

Antipseudomonal (extended spectrum) beta-lactamase sensitive

Cell
Wall
S
y
n
t
h
e
s
i
s

Ticarcillin
Carbenicillin

Carboxypenicillins

Piperacillin
Azlocillin
Mezlocillin

Ureidopenicillins

Beta Lactams

1st Generation (long t

Cefazolin
1/2

Cephalosporins
Not effective for the LAME
bacterias
Listeria (Amoxicillin often in combination w/

2nd Generation (Better G -ve

coverage)

Aminoglycosides)

Atypicals (Macrolides, Tetracyclins)

MRSA (Vancomycin)
Enterococci (Amoxicillin often in combination

BC

3rd

Generation (Empirical Rx of
Sepsis & Meningitis, except
Cefoperazone)

w/ Aminoglycosides)

Carbapenems (Beta-lactamase resistant)

Monobactams
Beta-lactamase inhib.
Not a
Lactam

Glycopeptides

Cephalexin

Cefadroxil

Cephalotin

Cefoxitin

Cefotetan

Cefaclor

Cefonicid

Cefamandole

Cefmetazole

Cefprozil

Cefoperazone

Ceftriaxone

Ceftazidime

Cefpodoxime

Ceftizoxime

Cefotaxime

Cefixime

Ceftibuten

Cefdinir

Cefditoren

Ertapenem

Doripenem

surgical prophylaxis)

Cephadrine
Cefuroxime (1

st

to cross BBB)

4th Generation

Cefepime (Beta-lactamase resistant)

5th Generation

Ceftaroline

Meropenem

Imipenem (1 in q 2 pts suffer a seizure w/ use) + Cilastatin

(dehydropeptidase inhibitor)

Aztreonam (alternative for persons allergic to cephalosporins and infected with a G -ve rod) (Beta-lactamase resistant)
Sulbactam

Tazobactam

Clavulonic Acid

Vancomycin (Red man syndrome-

Bacitracin

Teicoplanin

Polymyxin B

Amikacin

Neomycin (contact dermatitis)

Tobramycin

histamine induced vasodilation,

ototoxicity, nephrotoxicity)

Aminoglycosides BC

30S

Gentamycin

use O2 dependent uptake system anaerobes innately resistant.

Nephrotoxicity, Ototoxicity,
Neuromuscular Blockade: Ach
release. Resistance: conjugating
enzymes (acetyltransferases)

Streptomycin
(DOC for Bubonic
plague, Tularemia)

Tetracyclins DOC for

Doxycycline DOC for Borrelia

Rickettsia, Borrelia burgdorferi.

Chelators. Resistance: PUMPS. CI;
pregnancy & children

burgdorferi (Lyme Disease)

Tetracyclin

Demeclocyclin Blocks

Minocyclin Dentistry

Tigecyclin

ADH receptor; Rx for SIADH

Chloramphenicol Phenyl group; lipid soluble. Neonates; Grey baby syndrome, Kernicterus. Dose-dependent bone marrow suppression

Protein Synthesis

Macrolide DOC: Legionella.

Erythromycin

Azithromycin

Clarithromycin

Also used for: Atypicals, C. jejuni,

MAC, H. pylori. Stim. motilin recep.
Resistance:Methylated binding site

50S

Lincosamides

Telithromycin Ketolide:
macrolide-resistant Strep.
pneumonia

Clindamycin S. Aureus,

Lincomycin

Anaerobes. Conc in Bone (Rx Osteo.)

Strong link w/ pseudo. colitis

Linezolid VRSA, VRE. Bone marrow suppression (thrombocytopenia)

Streptogramins
Floroquinolones G(-) Osteo: Pseudo A.
DNA topoisomerases
BC

UTI, STDs, travellers diarrhoea. Tendonitis; tendon

rupture. CI; pregnancy & children

Quinupristin/Dalfopristin VRSA, VRE

Ciprofloxacin (2nd)

Norfloxacin (2nd)

Ofloxacin (2nd)

Enofloxacin (2nd)

Levofloxacin (3rd)

Sparfloxacin (3rd)

Moxifloxacin (4th)

Gemifloxacin (4th)

Ag Sulfadiazine (burns)

Sulfasalazine (UC, RA)

Sulfisoxazole

Pirymethamine-sulfadiazine: Cerebral
Toxoplasmosis

Prodrug; 5-aminosalicylic acid (UC)

& sulfapyridine (RA)

Quinolones

Nalidixic acid (1st)

Sulfonamides Dihydropteroate

Sulfamethoxazole (SMX)

synthetase (not found in humans) inhibitor.

neonate; Kernicterus. Steven-Johnson syndrome

Folic acid synthesis

TMP/SMX: Nocardia (DOC),
Travellers Diarrhoea, P. Jiroveci

Sulfone

Dapsone (Diaminodiphenyl sufone, DDS) Competitive inhibitor of Dihydropteroate synthetase. SLE-like syndrome w/ slow acetylators. Used in combination with CLOFAZIMINE (binds to the
guanine bases of bacterial DNA, thereby blocking the template function of the DNA and inhibiting bacterial proliferation) &/or RIFAMPIN for Leprosy Rx. DERMATITIS HERPETIFORMIS Rx.

DHFR inhibitors

Trimethoprim (TMP)

Pirymethamine

DNA (damage) BC

Metronidazole (free radicals) DOC: C. Difficile; Pseudo. Colitis. Anaerobes. Antiprotozoal: Giardia, Trichomonas, Entamoeba.

mRNA synthesis BC

Rifampin