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Antibiotic Classification & Mechanism         11
Author: Derek Moore Topic updated on 02/17/15 12:52pm
Hemophilic Arthropathy
Overview of By Mechanism
Blood Conditions
 
Fat Embolism Syndrome
Thromboembolism (PE & DVT)
Anticoagulation
Neurologic Diseases
Multiple Sclerosis
Amyotrophic Lateral Sclerosis
(ALS)
Complex Regional Pain
Syndrome (CRPS)
Systemic Diseases
Rheumatoid Arthritis
Systemic Lupus Erythematosus
(SLE)
Lyme Disease
Acute Rheumatic Fever  
Metabolic Disease
 
Hypercalcemia
PENICILLINS CEPHALOSPORINS FLUOROQUINOLONES AMINOGLYCOSIDES MONOBACTAMS CARBAPENEMS MACROLIDES OTHER
Hypocalcemia
Hypoparathyroidism Natrual First generation Ciprofloxacin (Cipro)  Amikacin  Aztreonam      Ertapenem Azithromycin Vancomycin 
Levofloxacin Gentamicin Imienem Clarithromycin Rifampin
Hyperparathyroidism
Penicillin G Cephalothin (Levaguin)  Kanamycin Meropenem      Dirithromycin Doxycycline
Hypophosphatasia
Penicillin­VK Cefazolin (Ancef, Moxifloxacin (Avelox)  Neomycin Erythromycin Linezolid
Pseudohypoparathyroidism Kefzol)  Norfloxacin      Tobramycin      Clindamycin      Tetracycline 

Scurvy Cephapririn Trimethoprim/

Cephalexin (Keflex) sulfamethoxacole
other
Medications & Toxicity

Medications Penicillinase Second Generation

Resistant
Bisphosphonates
Methicillin Cefacor
Prophylaxis Antibiotics Nafcillin Cefotetan (Cefotan) 
Antibiotic Classification & Oxacillin other
Mechanism other
Anti­inflammatory Medications Aminopenicillins Third Generation

Analgesic Medications Ampicillin Ceftriaxone

(Rocephin) 
Anesthesia
other
Platelet­Rich Plasma
  Fourth Generation
Toxicology Cefpirome
 
Lead Toxicity Cefepime
 
Clinical Science Antibiotic Grouping By Mechanism

Clinical Studies Cell Wall Synthesis Penicillins

Cephalosporins
Statistic Definitions
Vancomycin 
Level of Evidence Beta­lactamase Inhibitors
Clinical Trial Design Carbapenems
Aztreonam
Outcome Measure Tools
Polymycin
Healthcare Worplace Bacitracin
Occupational Health Protein Synthesis Inhibitors
Legal and Ethics Inhibit 30s Subunit
Aminoglycosides (gentamicin)
Job Bank Tetracyclines 
Inhibit 50s Subunit
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4/15/2016 Antibiotic Classification & Mechanism ­ Basic Science ­ Orthobullets.com
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 Hypersensitivity
Strep. pyogenes
Aqueous penicillin G reaction
(Grp.A)**
Procaine penicillin G Step. agalactiae Hemolytic anemia
Benzathine penicillin G (Grp.B)**
Penicillin V C. perfringens(Bacilli)**

Aminopenicillins Ampicillin  Above

Above + 
Amoxicillin
↑ Gram­negative:
E. faecalis**
E. Coli**

Penicillinase­resistant­ Methicillin Above + Above + 

penicillins Nafcillin PCNase­ Interstitial nephritis
Oxacillin producingStaph.
Cloxacillin aureus
Dicloxacillin
Antipseudomonal Carbenicillin Above +  Above
penicillins 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** Coombs­positive
Some Gram­negatives: anemia (3%)
E. Coli
Klebsiella

2nd generation Cefoxitin Above + Allergic Reaction

Cefaclor ↑ Gram­negative ETOH Disulfiram
Cefuroxime reaction
3rd generation Ceftriaxone Above + Allergic Reaction
Cefotaxime ↑ Gram­negative ETOH Disulfiram
Ceftazidime Pseudomonas reaction
Cefepime (4th generation)
Other Cell Wall Inhibitors
Vancomycin     Vancomycin Red man syndrome
MRSA**
(bactericidal: disrupts Nephrotoxicity
PCN/Ceph allegies**
peptioglycan cross­linkage) S. aureus Ototoxicity
S. epidermidis

Beta­lactamase Inhibitors  Clavulanic Acid Hypersensitivity

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

Carbapenems Imipenem (+ cilastatin) Broadest activity of  

Meropenem any antibiotic
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4/15/2016 Antibiotic Classification & Mechanism ­ Basic Science ­ Orthobullets.com
Meropenem any antibiotic
Doripenem (except MRSA,
Ertapenem Mycoplasma)
Aztreonam Aztreonam Gram­negative rods  
Aerobes
Hospital­acquired
infections
Polymyxins Polymyxin B Topical Gram­negative  
Polymyxin E infections
Bacitracin Bacitracin Topical Gram­positive  
infections
Protein Synthesis Inhibition
Anti­30S ribosomal subunit
Aminoglycosides Gentamicin Aerobic Gram­ Nephrotoxicity
(bactericidal: irreversible Neomycin negatives Ototoxicity
binding to 30S)    Amikacin Enterobacteriaceae 
Tobramycin  Pseudomonas
Streptomycin
Tetracyclines  Tetracycline  Hepatotoxicity
(bacteriostatic: blocks tRNA) Doxycycline Rickettsia Tooth discoloration
Minocycline Mycoplasma Impaired growth
Demeclocycline Spirochetes (Lyme's Avoid in children <
disease) 12 years of age

Anti­50S ribosomal subunit
Macrolides Erythromycin Streptococcus
(bacteriostatic: reversibly Azithromycin H. influenzae Coumadin
binds 50S) Clarithromycin Mycoplamsa Interaction
pneumonia (cytochrome P450)

Chloramphenicol Chloramphenicol H influenzae Aplastic Anemia

(bacteriostatic) Bacterial Meningitis Gray Baby
Brain absces Syndrome
Lincosamide Clindamycin
Bacteroides fragilis Pseudomembranous
(bacteriostatic: inhibits
S aureus
peptidyl transferase by colitis
Coagulase­negative
interfering with amino acyl­ Staph & Strep Hypersensitivity
tRNA complex) Excellent Bone Reaction
Penetration

Linezolid Linezolid Resistant Gram­  

(variable) positives
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
Mycoplasma Phototoxicity
Aerobic Gram + Achilles tendon
rupture
Impaired fracture
healing 

2nd generation Ciprofloxacin As Above as above

Norfloxacin +Pseudomonas
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 Crebelar dysfunction
biproducts disrupt DNA) ETOH disulfram
reaction
RNA Synthesis Inhibitors
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4/15/2016 Antibiotic Classification & Mechanism ­ Basic Science ­ Orthobullets.com
RNA Synthesis Inhibitors
Rifampin Rifampin Staphylococcus Body fluid
(bactericidal: inhibits RNA Mycobacterium (TB)  discoloration
transcription by inhibiting RNA Hepatoxicity (with
polymerase) INH)
Mycolic Acids Synthesis Inhibitors
Isoniazid Isoniazidz TB  
Latent TB
Folic acid Synthesis Inhibitors
Trimethoprim/Sulfonamides  Trimethoprim/Sulfamethoxazole UTI organisms
(bacteriostatic: inhibition with (SMX) Proteus Thrombocytopenia
PABA) Sulfisoxazole Enterobacter Avoid in third
Sulfadiazine trimester of
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

Non­Spore 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
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4/15/2016 Antibiotic Classification & Mechanism ­ Basic Science ­ Orthobullets.com

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
Fungus­like Bacteria Actinomyces israelii
Nocardia
 
Antibiotic Resistance Mechanisms

Bacteria develop ability to hydrolyze these drugs using β lactamase
confers resistance to penicillin
e.g. E. coli, Staph epidermidis, Pseudomonas aeruginosa, Klebsiella pneumoniae
add β lactamase inhibitor e.g. clavulanic acid in amoxicillin­clavulanate (Augmentin)
Genetic mutation of mecA
a bacterial gene encoding a penicillin­binding protein. New PBP has reduced affinity for
antibiotics
confers resistance to methicillin, oxacillin, nafcillin
e.g. MRSA
Altered cell wall permeability
confers resistance to tetracyclines, quinolones, trimethoprim and β lactam antibiotics
Creation of biofilm barrier 
provides an environment where offending bacteria can multiply safe from the hoste immune
system
Salmonella
Staph epidermidis
Active efflux pumps
confers resistance to erythromycin and tetracycline
e.g. msrA gene in Staph
Altered peptidoglycan subunit (altered D­alanyl­D­alanine of NAM/NAG­peptide) 
confers resistance to vancomycin
e.g. vancomycin resistant enterococcus (VRE) 
Ribosome alteration
erm gene confer inducible resistance to MLS (macrolide lincosamide streptogranin) agents
via methylation of 23s rRNA
demonstrate using D zone test     
for inducible clindamycin resistance in Staph and beta hemolytic Strep

Penicillins

Mechanism
interfer with bacterial cell wall synthesis
Subclassification and tested examples
natural
penicillin G
penicillinase­resistant
methicillin (Staphcillin)
aminopenicillins
ampicillin (Omnipen, Polycillin)

 
Cephalosporins

Overview
bactericidal
Mechanism
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.
same mechanicsm of action as beta­lactam antibiotics (such as penicillins)
Subclassification and tested examples 
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4/15/2016 Antibiotic Classification & Mechanism ­ Basic Science ­ Orthobullets.com
Subclassification and tested examples 
first generation
cefazolin (Ancef, Kefzol)
second generation
cefaclor (Ceclor)
third generation
cefriazone (Rocephin)
fourth generation
cefepime (Maxipime)

Fluoroquinolones

Mechanism
blocks DNA replication via inhibition of DNA gyrase 
Side effects
inhibit early fracture healing through toxic effects on chondrocytes 
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 
ciprofloxacin (Cipro)
levofloxacin (Levaquin)

Aminoglycosides

Mechanism
bactericidal
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 
gentamicin (Garamycin)

Vancomycin

Coverage
gram­positive bacteria
Mechanism
bactericidal
an inhibitor of cell wall synthesis 
Resistance
increasing emergence of vancomycin­resistant enterococci has resulted in the development
of guidelines for use by the  (CDC) 
indications for vancomycin 
serious allergies to penicillins or beta­lactam 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 
Pneumococcal immunization
Haemophilus influenza type B vaccine
Meningococcal group C conjugate vaccine
Influenza immunization
Lifelong prophylactic antibiotics (oral phenoxymethylpenicillin or erythromycin)

 
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Qbank (11 Questions)

Question:  1  of 10 Next Question

TAG 

(OBQ12.53) What mechanism allows Staphylococcus epidermidis to adhere to surfaces and resist phagocytosis? 
Review Topic

1.   Creation of active efflux pumps
2.   Methylation of 23s rRNA
3.   Biofilm production
4.   Alteration of cell wall permeability
5.   Beta­lactamase production

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