Anti-bacterial drugs Beta Lactam - PENICILLINS (PCN) Inhibits bacterial cell wall synthesis (blocks assembly of peptidoglycan chains

(bactericidal).
Antimicrobial Natural Penicillins Examples Penicillin G
(IV - potassium, IM potassium, benzathine, and procaine formulation)

Gram (+) Streptococcus Enterococcus

Gram (-) Neisseria Meningococci

Penicillin VK (PO) (Pen VK)

Anti-staphylococcal Penicillins

Methicillin (IV, IM) Nafcillin (IV, IM) Oxacillin (IV, IM) Cloxacillin (IV, IM, PO) Dicloxacillin (PO)

Methicillin-Sensitive - S. Aureus (MSSA)

None

Anaerobes Additional Info Good Drug of choice for Syphilis. Renally adjusted. Best absorbed on empty stomach. Penetrates CNS well with inflamed meninges. None No Enterococcus coverage Not renally adjusted

Aminopenicillins (AminoPCN) Aminopenicillin and -lactamase inhibitor

Ampicillin (IV, PO) Amoxicillin (PO) Ampicillin/Sulbactam (IV) Amoxicillin/Clavulanate (PO) (Augmentin) COMBO

Enterococcus Listeria Streptococci (but less active than penicillins) Same as above w/ increased activity against MSSA Enterococcus Staphylococcus Streptococcus (but less active than PCN) Same as above w/ increased activity

H. pylori (excellent), E. coli, Proteus, Salmonella, H.influenzae, Bordetalla, Shigella Same as above but Sulbactam active against Acinetobacter

Pasturella Clostridium Same as AminoPCN, increased activity

Renally adjusted Best if taken on empty stomach. Amoxicillin causes less GI effects. Renally adjusted

Anti-pseudomonal Penicillins Anti-pseudomonal Penicillin--lactamase Inhibitor combination

Piperacillin (IV, IM) Ticarcillin (IV, IM) Ticarcillin/Clavulanate Piperacillin/Tazobactam COMBO

Pseudomonas Enterobacteriaceae Klebsiella Same as above w/ increased activity

Clostridium Same but increased activity

Renally adjusted Ticarcillin less active against Klebsiella than Piperacillin Renally adjusted

Anti-bacterial drugs Beta-Lactam CEPHALOSPORINS Inhibits bacterial cell wall synthesis (like PCN), (bactericidal).
Antimicrobial 1ST Generation Cephalosporins Examples Cefazolin (IV) Cefadroxil (PO) Cephalexin (PO) (Keflex) 2nd Generation Cephalosporins CefoTETAN (IV) CeFOXitin (IV) CeFURoxime (IV) CeFURoxime axetil (PO) Cefaclor (PO) Loracarbef (PO) Cefprozil (PO) 3rd Generation Cephalosporins (-xime) Cefotaxime (IV) Ceftizoxime (IV) Ceftriaxone(IV) (Rocephin) Ceftazidime(IV) Cefixime (PO) Ceftibuten (PO) Cefpodoxime (PO) Cefdinir (PO) 4th Generation Cephalosporins Cefepime (IV) Same as 1st generation but less active Gram (+) Staphylococcus Streptococcus Gram (-) Proteus E. Coli
Klebsiella

Anaerobes Additional Info None PEKSS Renally adjusted

Same as 1st generation but more active H. influenza Enterobacteraciaea Neisseria

Cefoxitin & Cefotetan possess some anaerobe coverage

PEKSS + HEN -Cefuroxime, cefprozil most effective against Strep. pneumo and H. flu -Cefuroxime axetil active against Borrelia burgdorferi (Lyme dz) Renally adjusted PEK + HEN Renally adjusted Rocephin works on shigella, salmonella, gonorrhea, PID, meningitis, pre-surgery, endocarditis, Lyme Dz

Same as 1st Same as 2nd generation but much generation. less active Serratia Ceftazidime has pseudomonas coverage.

Very little

Staphylococcus Streptococcus Coverage is better than 3rd generation but not as good as 1st generation

Same as 3rd generation with great pseudomonas coverage

Very little

Enters CNS with inflamed meninges. No enterococcal coverage Renally adjusted.

Anti-bacterial drugs Beta-Lactam - CARBAPENEMS Inhibits cell wall synthesis (-lactam ring)
Antimicrobial Carbapenem All IV Examples Imipenem/cilastatin (IV) Meropenem(IV) Ertapenem(IV) Doripenem (IV) Gram (+) Great coverage including Enterococcus MSSA Listeria (Ertapenem not active vs Listeria or Enterococcus) Gram (-)
Great coverage including: Pseudomonas Acinetobacter (Ertapenem not active vs Pseudomonas or Acinetobacter

Anaerobes Clostridium Peptococcus B. fragilis

Additional Info Penetrates well into body tissues and fluids, including CSF when the meninges are inflamed Renally adjusted Cross-reactivity in pts with PCN allergy about 50% Imipenem more gram(+) Meropenem more gram(-)

Beta-Lactam - MONOBACTAM Inhibits bacterial cell wall synthesis.

Antimicrobial Monobactam Examples Aztreonam (IV/IM) Gram (+) None Gram (-)
Pseudomonas Enterobacteriaceae

Anaerobes None

Additional Info Renally adjusted No PCN/cephalosporin cross-reactivity

GLYCOPEPTIDES Inhibits bacterial cell wall synthesis (No -lactam ring)

Antimicrobial Examples Glycopeptides Vancomycin (IV/PO) Gram (+) Great MSSA, MRSE, & MRSA Some activity against Listeria Gram (-)
Poor

Anaerobes Can be used PO for C. difficile

Additional Info Trough levels are monitored for therapeutic efficacy. Renally adjusted Can cause irreversible ototoxicity.
Red-man/Red-neck syndrome

Histamine mediated rxn (NOT allergic rxn) characterized by flushing, rash, hypotension. Associated with rapid infusion; Tx w/ antihistamines
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Anti-bacterial drugs FLUOROQUINOLONES (FQ) Target DNA gyrase to prevent relaxation and supercoiling, blocking nucleic acid synthesis.
Antimicrobial 2nd Generation FQ Examples Ofloxacin(PO, OPT, OTIC) Ciprofloxacin(IV,PO,OPT,OTIC) Levofloxacin (IV,PO) Moxifloxacin(IV,PO) Gram (+) None Gram (-) Enterobacteriaceae Cipro has pseudomonas Enterobacteriaceae Pseudomonas Anaerobes Additional Info None Atypicals - legionella, mycobacteria(diarrhea) Renally adjusted None Atypicals - Chlamydia, legionella, mycobacteria, mycoplasma pneuomiae. Moxifloxacin not renally adjusted, Levo is.

3rd Generation FQ Also known as Respiratory FQ

Streptococcus

AMINOGLYCOSIDES Binds to the 30s ribosomal subunit inhibiting protein synthesis from mRNA.
Antimicrobial Aminoglycoside Examples Gentamicin (IV, IM, ophthalmic, topical) Tobramycin (IV, IM, inhalation) Amikacin (IV, IM) Neomycin (PO, topical) Streptomycin (IV) Paromomycin / Monomycin Gram (+) Poor except when used for synergism Gram (-)
Pseudomonas E. coli Klebsiella Proteus Serratia

Anaerobes Additional Info None Tobramycin most active vs. pseudomonas. Gentamicin most active vs serratia. Renally adjusted Peak and trough monitoring for therapeutic efficacy and safety.

TETRACYCLINES Interacts with the 30s subunit of the bacterial ribosome and prevents binding by tRNA molecules loaded
with amino acids, thereby inhibiting the protein synthesis. Antimicrobial Tetracycline Examples Minocycline (PO) Doxycycline (IV, PO) Tetracycline (IV, PO) Gram (+) Good, Staph & Strep Enterococcus CA-MRSA Gram (-)
Brucella Vibrio H. Influenzae

Anaerobes Additional Info Chlamydia & Mycoplasma Used in Lyme disease Do not use in kids < 8 y/o

Anti-bacterial drugs MACROLIDES Bind to the 50s ribosomal subunit, inhibiting protein synthesis
Antimicrobial Macrolide (A, C, E) Examples Azithromycin (IV, PO) Clarithromycin (PO) Erythromycin (IV, PO) Gram (+) Good activity against staph and strep (clarithromycin most active, azithromycin least active) Gram (-)
Some (azithromycin active against H. influenza)

Anaerobes None

Additional Info Clarithromycin has coverage against chlamydia, legionella, and mycoplasma and can leave a metallic taste in the mouth. Erythromycin is a strong CYP3A4 inhibitor and can cause GI intolerance. Macrolides can cause QT prolongation. No renal adjustment

OXAZOLIDINONES Binds to the 50S ribosomal subunit, blocking the binding site for tRNA.
Antimicrobial Oxazolidinones Examples Linezolid (IV, PO) Gram (+) Excellent coverage including: MRSA, MRSE, VRE Gram (-)
None

Anaerobes None

Additional Info Monitor CBC No renal adjustment

NITRoIMiDAZOLES - believed to work by crosslinking of DNA

Antimicrobial Nitroimdazoles Examples Metronidazole (Flagyl) Gram (+) Gram (-) H. pylori C. difficile (release toxins) Anaerobes GREAT!! Additional Info Giardia, ameba,

Anti-bacterial drugs NITROFURANS - believed to work by crosslinking of DNA

Antimicrobial Nitrofurans Examples Nitrofurantoin(MacroBID) Furazolidone (Furoxone) Gram (+) Gram (-)
E. coli (Lower UTIs) Enteritis

Anaerobes

Travelers diarrhea

Additional Info N/V, CrCl < 60 contraindic. Can cause pulm toxicity Avoid ETOH for 4 days after

CYCLIC LIPOPEPTIDES Bind to cell membrane weakening & ions leak out celling cell
Antimicrobial Lipopeptides Examples daptomycin Gram (+) MSSA, MRSA, & strep VRE enterococci Gram (-)
Poor

Anaerobes

Additional Info Effects skeletal muscle Check CK concentrations weekly Effective in staph endocarditis Not for pneumonia

LINCOsamides/MYCINS Bind to the 50s ribosomal subunit, inhibiting protein synthesis

Antimicrobial Lincomycin Examples Clindamycin (IV/PO) Gram (+) Good activity vs staph & strep Gram (-)
Poor

Anaerobes Great (C. difficile is resistant)

Additional Info Can cause the development of C.difficile infection.

FOLATE ANTAGONISTS Inhibit metabolic pathways, a folic acid synthesis antagonist, inhibiting protein synthesis.
Antimicrobial Sulfonamide Examples Gram (+) Trimethoprim/Sulfamethoxazole Some Strep and (TMP/SMZ) Staph, aka Bactrim Listeria Gram (-)
E. coli, H. influenza Proteus Klebsiella Salmonella Enterobacteriaceae S. maltophilia (Drug of choice)

Anaerobes Additional Info None Drug-Drug interactions: CYP2C9 and CYP3A4 inhibitor Stephen-Johnsons syndrome Renally adjust Leprosy
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Dapsone

Anti-bacterial drugs

POLYMIXINS (from my book only not Prof. Earley)

Antimicrobial Polymixins Examples Polymixin B Gram (+) Poor Gram (-) Good on many Acinetobacter baumannii, Pseudomonas aeroginosa & Klebsiella pneumo Anaerobes Additional Info None Older class abandoned for safer aminoglycosides; Renal toxicity; Used for bacterial resistant strains