PENICILLINS CEPHALOSPORINS FLUOROQUINOLONES AMINOGLYCOSIDES MONOBACTAMS CARBAPENEMS MACROLIDES OTHER

Natrual First generation Ciprofloxacin (Cipro) Amikacin Aztreonam Ertapenem Azithromycin Vancomycin
Levofloxacin (Levaguin) Gentamicin Imienem Clarithromycin Rifampin
Penicillin G Cephalothin Moxifloxacin (Avelox) Kanamycin Meropenem Dirithromycin Doxycycline
Penicillin-VK Cefazolin (Ancef, Norfloxacin Neomycin Erythromycin Linezolid
Kefzol) Tobramycin Clindamycin Tetracycline
Cephapririn Trimethoprim/
Cephalexin (Keflex) sulfamethoxacole
other

Penicillinase Second Generation

Resistant

Methicillin Cefacor
Nafcillin Cefotetan
Oxacillin (Cefotan)
other other

Aminopenicillins Third Generation

Ampicillin Ceftriaxone
(Rocephin)
other

Fourth Generation

Cefpirome
Cefepime

Overview of By Mechanism
Antibiotic Grouping By Mechanism

Cell Wall Synthesis Penicillins

Cephalosporins
Vancomycin
Beta-lactamase Inhibitors
Carbapenems
Aztreonam
Polymycin
Bacitracin

Protein Synthesis Inhibitors Inhibit 30s Subunit

Aminoglycosides (gentamicin)
Tetracyclines
Inhibit 50s Subunit
Macrolides
Chloramphenicol
Clindamycin
Linezolid
Streptogramins

DNA Synthesis Inhibitors Fluoroquinolones

Metronidazole

RNA synthesis Inhibitors Rifampin

Mycolic Acid synthesis inhibitors Isoniazid

Folic Acid synthesis inhibitors Sulfonamides

Trimethoprim
Antibiotic Classification & Indications

Inhibits Cell Wall Synthesis

Penicillins
(bactericidal: blocks cross linking via competitive inhibition of the transpeptidase enzyme)

Class/Mechanism Drugs Indications (**Drug of Toxicity

Choice)

Penicillin Penicillin G Strep. pyogenes Hypersensitivity

Aqueous penicillin G (Grp.A)** reaction
Procaine penicillin G Step. agalactiae Hemolytic anemia
Benzathine penicillin G (Grp.B)**
Penicillin V C. perfringens(Bacilli)**

Aminopenicillins Ampicillin Above + Above

Amoxicillin Gram-negative:
E. faecalis**
E. Coli**

Penicillinase-resistant-penicillins Methicillin Above + Above +

Nafcillin PCNase-producingStaph. Interstitial nephritis
Oxacillin aureus
Cloxacillin
Dicloxacillin

Antipseudomonal penicillins Carbenicillin Above + Above

Ticarcillin Pseudomonas
Piperacillin aeruginosa**
Cephalosporins
(bactericidal: inhibits bacterial cell wall synthesis via competitive inhibition of the transpeptidase enzyme)

1st generation Cefazolin Staph. aureus** Allergic reaction

Cephalexin Staph. epidermidis** Coombs-positive
Some Gram-negatives: anemia (3%)
E. Coli
Klebsiella

2nd generation Cefoxitin Above + Allergic Reaction

Cefaclor Gram-negative ETOH Disulfiram
Cefuroxime reaction

3rd generation Ceftriaxone Above + Allergic Reaction

Cefotaxime Gram-negative ETOH Disulfiram
Ceftazidime Pseudomonas reaction
Cefepime (4th generation)

Other Cell Wall Inhibitors

Vancomycin Vancomycin MRSA** Red man syndrome

(bactericidal: disrupts peptioglycan cross-linkage) PCN/Ceph allegies** Nephrotoxicity
S. aureus Ototoxicity
S. epidermidis

Beta-lactamase Inhibitors Clavulanic Acid S aureus** Hypersensitivity

(bactericidal: blocking cross linking) Sulbactam S epidermis** Reaction
Tazobactam E.Coli** Hemolytic anemia
Klebsiella**

Carbapenems Imipenem (+ cilastatin) Broadest activity of any

Meropenem antibiotic
Doripenem (except MRSA,
 Ertapenem Mycoplasma)

Aztreonam Aztreonam Gram-negative rods

Aerobes
Hospital-acquired
infections

Polymyxins Polymyxin B Topical Gram-negative

Polymyxin E infections

Bacitracin Bacitracin Topical Gram-positive

infections

Protein Synthesis Inhibition

Anti-30S ribosomal subunit

Aminoglycosides Gentamicin Aerobic Gram-negatives Nephrotoxicity

(bactericidal: irreversible binding to 30S) Neomycin Enterobacteriaceae Ototoxicity
Amikacin Pseudomonas
Tobramycin
Streptomycin

Tetracyclines Tetracycline Rickettsia Hepatotoxicity

(bacteriostatic: blocks tRNA) Doxycycline Mycoplasma Tooth discoloration
Minocycline Spirochetes (Lyme's Impaired growth
Demeclocycline disease) Avoid in children < 12
years of age

Anti-50S ribosomal subunit

Macrolides Erythromycin Streptococcus Coumadin Interaction

(bacteriostatic: reversibly binds 50S) Azithromycin H. influenzae (cytochrome P450)
Clarithromycin Mycoplamsa pneumonia
Chloramphenicol Chloramphenicol H influenzae Aplastic Anemia
(bacteriostatic) Bacterial Meningitis Gray Baby Syndrome
Brain absces

Lincosamide Clindamycin Bacteroides fragilis Pseudomembranous

(bacteriostatic: inhibits peptidyl transferase by S aureus colitis
interfering with amino acyl-tRNA complex) Coagulase-negative Hypersensitivity
Staph & Strep Reaction
Excellent Bone
Penetration

Linezolid Linezolid Resistant Gram-positives

(variable)

Streptogramins Quinupristin VRE

Dalfopristin GAS and S. aureus skin
infections

DNA Synthesis Inhibitors

Fluoroquinolones
(bactericidal: inhibit DNA gyrase enzyme, inhibiting DNA synthesis)

1st generation Nalidixic acid Steptococcus Phototoxicity

Mycoplasma Achilles tendon
Aerobic Gram + rupture
Impaired fracture
healing

2nd generation Ciprofloxacin As Above +Pseudomonas as above

Norfloxacin
Enoxacin
Ofloxacin
 Levofloxacin

3rd generation Gatifloxacin As above + Gram- as above

positives

4th generation Moxifloxacin As above + Gram- as above

Gemifloxacin positives + anaerobes

Other DNA Inhibitors

Metronidazole Metronidazole (Flagyl) Anaerobics Seizures

(bacteridical: metabolic biproducts disrupt DNA) Crebelar dysfunction
ETOH disulfram
reaction

RNA Synthesis Inhibitors

Rifampin Rifampin Staphylococcus Body fluid

(bactericidal: inhibits RNA transcription by Mycobacterium (TB) discoloration
inhibiting RNA polymerase) Hepatoxicity (with
INH)

Mycolic Acids Synthesis Inhibitors

Isoniazid Isoniazidz TB
Latent TB

Folic acid Synthesis Inhibitors

Trimethoprim/Sulfonamides Trimethoprim/Sulfamethoxazole UTI organisms Thrombocytopenia

(bacteriostatic: inhibition with PABA) (SMX) Proteus Avoid in third
Sulfisoxazole Enterobacter trimester of
Sulfadiazine pregnancy

Pyrimethamine Pyrimethamine Malaria

 T. gondii

Bacteria Overview

Gram Postive Cocci

Staphylococcus Staph. aureus

MSSA
MRSA
Staph. epidermis
Staph saprophyticus

Streptococcus Strep pneumoniae

Strep pyogenes (Group A)
Strep agalacticae (Group B)
Strep viridans
Strep Bovis (Group D)

Enterococci E. faecalis (Group D strep)

Gram Positive Bacilli

Spore Forming Bacillus anthracis

Bacillus cereus
Clostridium tetani
Clostridium botulinum
Clostridium perfringens
Clostridium difficile

Non-Spore Forming Corynebacterium diphtheriae

Listeria monocytogenes
Gram Negative Cocci

Neisseria Neisseria meningitidis

Neisseria gonorrhoeae

Gram Negative Bacilli

Enterics Escherichia coli

Salmonella typhi
Salmonella enteridis
Shigella dysenteriae
Klebsiella pneumoniae
Serratia
Proteus
Campylobacter jejuni
Vibrio cholerae
Vibrio parahaemolyticus/vulnificus
Helicobacter pylori
Pseudomonas aeruginosa
Bacteroides fragilis

Respiratory bacilli Haemophilus influenzae

Haemophilius ducreyi
Bordatella pertussis

Zoonotic bacilli Yersinia enterocolitica

Yersinia pestis
Brucella
Francisella tularensis
Pasteurella multocida
Bartonella henselae

Other Gardnerella vaginalis

 Other Bacteria

Mycobacteria Mycobacterium tuberculosis

Mycobacterium leprae
MOTTS

Spirochetes Borrelia burgdorferi

Leptospira interrogans
Treponema pallidum

Chlamydiaceae Chlamydia trachomatis

Chlamydophila
Rickettsia
Ehrlichia

Mycoplasmataceae Mycoplasma pneumoniae

Ureaplasma urealyticum

Fungus-like Bacteria Actinomyces israelii

Nocardia

Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze these drugs using lactamase

o confers resistance to penicillin

o e.g. E. coli, Staph epidermidis, Pseudomonas aeruginosa, Klebsiella pneumoniae

o add lactamase inhibitor e.g. clavulanic acid in amoxicillin-clavulanate (Augmentin)

 Genetic mutation of mecA

o carried by Staphylococcal cassette chromosome (SCCmec) mobile genetic unit

o a bacterial gene encoding a penicillin-binding protein (PBP2a).

PBP2a has reduced affinity for antibiotics

confers resistance to methicillin, oxacillin, nafcillin

e.g. MRSA

SCCmec type IV has less genetic elements and is specific to CA-MRSA, making CA-MRSA less multi-drug resistant

Altered cell wall permeability

o confers resistance to tetracyclines, quinolones, trimethoprim and lactam antibiotics

Creation of biofilm barrier

o provides an environment where offending bacteria can multiply safe from the hoste immune system

Salmonella

Staph epidermidis

Active efflux pumps

o confers resistance to erythromycin and tetracycline

o e.g. msrA gene in Staph

Altered peptidoglycan subunit (altered D-alanyl-D-alanine of NAM/NAG-peptide)

o confers resistance to vancomycin

o e.g. vancomycin resistant enterococcus (VRE)

 Ribosome alteration

o erm gene confer inducible resistance to MLS (macrolide lincosamide streptogranin) agents via methylation of 23s rRNA

o demonstrate using D zone test

for inducible clindamycin resistance in Staph and beta hemolytic Strep

Penicillins

Mechanism

o interfer with bacterial cell wall synthesis

Subclassification and tested examples

o natural

penicillin G

o penicillinase-resistant

methicillin (Staphcillin)

o aminopenicillins

ampicillin (Omnipen, Polycillin)

Cephalosporins

Overview

o Bactericidal
 Mechanism

o disrupts the synthesis of the peptidoglycan layer of bacterial cell walls

does so through competitive inhibition on PCB (penicllin binding proteins)

peptidoglycan layer is important for cell wall structural integrity.

o same mechanicsm of action as beta-lactam antibiotics (such as penicillins)

Subclassification and tested examples

o first generation

cefazolin (Ancef, Kefzol)

o second generation

cefaclor (Ceclor)

o third generation

cefriazone (Rocephin)

o fourth generation

cefepime (Maxipime)

Fluoroquinolones

Mechanism

o blocks DNA replication via inhibition of DNA gyrase

Side effects

o inhibit early fracture healing through toxic effects on chondrocytes

 o increased rates of tendinitis, with special predilection for the Achilles tendon.

tenocytes in the Achilles tendon have exhibited degenerative changes when viewed microscopically after fluoroquinolone
administration.

recent clinical studies have shown an increased relative risk of Achilles tendon rupture of 3.7.

Subclassification and tested examples

o ciprofloxacin (Cipro)

o levofloxacin (Levaquin)

Aminoglycosides

Mechanism

o bactericidal

o inhibition of bacterial protein synthesis

work by binding to the 30s ribosome subunit, leading to the misreading of mRNA. This misreading results in the synthesis of abnormal
peptides that accumulate intracellularly and eventually lead to cell death. These antibiotics arebactericidal.

Subclassification and tested examples

o gentamicin (Garamycin)

Vancomycin

Coverage

o gram-positive bacteria

Mechanism

o bactericidal

o an inhibitor of cell wall synthesis

 Resistance

o increasing emergence of vancomycin-resistant enterococci has resulted in the development of guidelines for use by the (CDC)

o indications for vancomycin

serious allergies to penicillins or beta-lactam antimicrobials

serious infections caused by susceptible organisms resistant to penicillins (MRSA, MRSE)

surgical prophylaxis for major procedures involving implantation of prostheses in institutions with a high rate of MRSA or MRSE

Rifampin

Most effective against intracellular phagocytized Staphylococcus aureus in macrophages

Linezolid

Linezolid binds to the 23S portion of the 50S subunit and acts by preventing the formation of the initiation complex between
the the 30S and 50S subunits of the ribosome.

Splenectomy

Splenectomy patients or patients with functional hyposplenism require the following vaccines and/or antibiotics

o Pneumococcal immunization

o Haemophilus influenza type B vaccine

o Meningococcal group C conjugate vaccine

o Influenza immunization

o Lifelong prophylactic antibiotics (oral phenoxymethylpenicillin or erythromycin)

 Prepared by:

Jasher Dave C. Acabal

student