TibbsNotes – Antibacterial Table

Inhibits CLASSIFICATION ANTIBIOTICS Clinical Uses Adverse Effects Pk/Pd

Gram (+) AMPICILLIN: GI Disturbance;  PENICILLIN V – Bioavaliability
- DOC: Streptococcus pyogenes (skin & soft tissue) Pseudomonas colitis impaired by food (give 1-2hrs
- DOC: Streptococcus Pneumonia (susceptible) TICARCILLIN: Hematologic before/after), low w/o food
- DOC: Non--lactamase-producing S. aureus Disturbance  Excretion: Urine (Renal Dose
Garm (-) Common: Adjustment in Renal Failure),
- DOC: E. faecalis (NOT E. faecium)  Hypersensitivity (cross- EXCEPT:
Crystalline/Aqueous - DOC: N. Meningitidis (NOT N. Gonorrhea) reacting) oNAFCILLIN: Bile
(IV) Atypicals  Rash  EBV oOXACILLIN, etc: Bile & Urine
Natural Penicillins PENICILLIN G - DOC: Treponema pallidum (Syphillis) Rare:  AMOXICILLIN:
(Narrow Spectrum) - DOC: Leptospira spp  Anaphylactic Shock (Tx: oNot impaired by food
C Other Uses: Epinephrine) oBiovailability higher than
E - C. tetani; Actinomyces  Hemolytic Anemia Ampicillin
L - H. influenzae in high doses  Interstitial Nephritis Time-Dependent Killing
L - NOT B. fragilis Others: Bactericidal
Procaine, - S. Pyogenes (Pharyngitis, prophylaxis for reinfection)  Seizures (high doses)
Benzathine (IM) - T. Pallidum (Syphilis)  Secondary infections
W
A Penicillins PENICILLIN V (Oral) - S. Pyogenes (Pharyngitis) (replaced by AMOXICILLIN)
L NAFCILLIN (IV) METHICILLIN - DOC: MSSA
L Anti-Staphylococcal - NOT for Enterococci & Gram (-) organisms
OXACILLIN (IV) CLOXACILLIN (Oral)
S - S. Pneumoniae (most active ORAL -lactam(
AMPICILLIN [Limited Gram (-)]
Y
- Shigella spp.
N
Amino- AMOXICILLIN )Oral) AMPICILLIN (IV) - Salmonella typhi (resistance)
T - E. coli ( NOT for other enterobacteriaceae: Klebsiella,
H Enterobacter) (UTI)
E Extended-
- Listeria monocytogenes (Pneumonia in children)
S Spectrum - Pseudomonas aeruginosa (nosocomial)
I Carboxy- TICARCILLIN CARBENICILLIN - Enterobacteriaceae (broader coverage)
S - NOT active against enterococci (ex. E. Faecalis)
- Pseudomonas aeruginosa (nosocomial)
Ureido- PIPERACILLIN (IV) - Enterobacteriaceae (broader coverage inc. Klebsiella spp.)
- E. faecalis
COAMOXICLAV Coverage for: Klebsiella Pneumoniae, Bacteroides fragilis
 Diarrhea  Unreliable CNS penetration
CLAVULANIC ACID (+ Amoxicillin)

-Lactamase Inhibitors + Ticarcillin

SULBACTAM + Ampicillin
TAZOBACTAM + Piperacillin
Inhibits CLASSIFICATION ANTIBIOTICS Clinical Uses Adverse Effects Pk/Pd
- Streptococci & Staphylococci (minor skin & soft tissue infections) Common  Excretion: Urine; Except
- CEFAZOLIN – DOC: Surgical Prophylaxis (NOT for colorectal  Thrombophlebitis o CEFTRIAXONE (Bile)
1st Gen CEPHALEXIN (Oral) CEFAZOLIN (IV) procedure) Occasional o CEFOPERAZONE (Bile)
- E. coli (uncomplicated cystitis) (NOT Enterococci, Pseudomonas  Hypersensitivity  CEFOPERAZONE – DO NOT
aeruginosa, and Acinetobacter spp.  Bile sludging cross BBB
CEFUROXIME (Oral) CEFUROXIME (IV) - Broader coverage: Gram (-) (inc. -actamase-producing H.  CEFACLOR – Serum sickness
influenzae, Moraxella catarrhalis, Klebsiella spp. like reactions
CEFACLOR (Oral) CEFOTETAN (IV)
2nd Gen - Bacteroides fragilis (intraabdominal/pelvic infections)  Hematologic disturbances
- NOT against Enterococci, Pseudomonas aeruginosa, and (CEFOPERAZONE)
CEFOXITIN (IV)
Acinetobacter spp.)  Disulfiram-like reaction
CEFTRIAXONE (IV) - CEFTRIAXONE, CEFOTAXIME – DOC: Meningitis by Penicillin-  Metallic Taste
CEFPODOXIME (Oral) resistant Streptococcus pneumoniae Rare
CEFOTAXIME (IV) - CEFOPERAZONE, CEFTAZIDIME – Pseudomonas aeruginosa  Anaphylactic Shock (cross
C
CEFOPERAZONE (IV) - Broader coverage: Enterobacteriaceae (inc. Citrobacter spp., allerginicity)
E Cephalosporins Serratia Marcescens, Providencia spp.) (Pneumonia,  Pseudomembranous colitis
L  Interstitial nephritis
pyelonephritis)
L - CEFTRIAXONE – DOC: N. gonorrhoeae
3rd Gen - CEFTRIAXONE – DOC: MDR Salmonella typhi
W CEFIXIME (ORAL) - CEFTAZIDIME: Burkholderia capacia
CEFTAZIDIME (IV) - CEFTAZIDIME: Empirical Treatment in neutropenic febrile
A
immunocompromised patients
L - CEFTIZOXIME: Bacteroides fraglis (Intraabdominal/Pelvic
L Infections)
- CEFIXIME, CEFTAZIDIME – NOT for Sptaphylococci & Streptococci
S - Broader coverage: Enterobacteriaceae (inc. Enterobacter spp.)
Y 4th Gen CEFEPIME CEFPIROME - Pseudomonas aeruginosa (nosocomial infections)
- NOT for Enterococci, Acinetobacter spp., and anaerobes
N
T 5th Gen CEFTAROLINE - CEFTAROLINE – NOT Pseudomonas
- Aerobic Gram (-) rods (Pneumonia, Meningitis, Sepsis) Occasional - Penetrates well in CSF
H
o Pseudomonas aeruginosa  Hypersensitivity (NO - Excretion: Urine
E
Monobactam AZTREONAM (IV) o Enterobacteriaceae (inc. E. coli, Klebsiella spp., Enterobacter CROSS-ALLERGENICITY)
S spp.) Rare
I o NOT ESBLs  Pseudomembranoud colitis
S  No cross-allergenicity  NO cross-/class-resistance
Common  ERTAPENEM may be given IM
- Very broad spectrum  GI Disturbance  IMIPENEM – inactivated by
IMIPENEM (IV) DORIPENEM (IV) - DOC: ESBLs Occasional dehydropeptidases
- DOC: Serious mixed aerobic & anaerobic infections  Hypersensitivity o CILASTATIN prolongs half-
- DOC: Enterobacter spp.  Hematologic Distrubances life of IMIPENEM, maintains
Carbepenem - NOT for MRSA, Enterococci (Except IMIPENEM), and Rare therapeutic urinary
Stenotrophomonas maltophila  Seizures concentration, and
- Used for meningitis o IMIPENEM: Most decreases nephrotoxicity
MEROPENEM (IV) ERTAPENEM (IV) - Anaerobic: Aspiration pneumonia, intraabdominal infections epileptogenic  High urinary concentration
- Use with bacteria resistant to other drugs o DORIPENEM: Least  Excretion: Urine
epileptogenic
 Hallucination
 Inhibits CLASSIFICATION ANTIBIOTICS Clinical Uses Adverse Effects Pk/Pd
Common  Binds to d-ala-d-ala terminus, inhibiting transglycosylase
- DOC: MRSA (Pneumonia, Bacteremia, Endocarditis, & for Prophylaxis)  Red Man/Neck Syndrome  TELAVANCIN: disrupts bacterial cell membrane potential
VANCOMYCIN - DOC: Coagulase-negative staphylococci (Prosthetic device infections, CSF (Due to histamine release,  Passes through inflamed meninges
shunt infections, catheter-related infections infusion related flushing  Time-dependent killing
- Broad-Spectrum Gram (+)  Phlebitis  Excretion: Urine (Glomerular Filtration)
Glycopeptides - Others: Occasional o Check serum levels
o Enterococci  Ototoxicity
TEICOPLANIN TELAVANCIN* o Penicillin-resistant S. pneumoniae (Meningitis)  Nephrotoxicity
(IV, IM) o Metronidazole-resistant C. difficile (colitis)
Cell Membrane
Function  Muscle Toxicity (Myopathy)  Ca-dependent insertion of its lipid tail to the cell
- DOC: VRSA
membrane, depolarizing it with K+ efflux
- MRSA alternative
Lipopeptides DAPTOMYCIN (IV) - NOT meningitis
 Little penetration in CSF
 INACTIVATED BY LUNG SURFACTANT
- NOT FOR PNEUMONIA
 Concentration-dependent Killing
- Multidrug-resistant organisms (Pneumonia, Skin & tissue infections, Common  Attach and disrupt cell membrane (cationic agent)
Polymixin B (SC) Intraabdominal infections, Bacteremia)  Nephrotoxicity  Penetrates CSF
Polymixins - Opposite of VANCOMYCIN/DAPtOMYCIN Occasional  Excretion: Urine
- Broad Gram (-) coverage  Neurotoxicity  Concentration-dependent Killing
Polymixin E (COLISTIN) (IV) - NOT as monotherapy Rare - Hypersensitivity
Common Mechanisms of Resistance
 OTOTOXICITY  Transferase Enzymes
 Nephrotoxicity  Impaired entry
STREPTOMYCIN AMIKACIN - Serious Infections: Combination w/ -lactam Abs  Pregnancy: Ototoxicity  Ribosomal protection
o Gram (-) septicemia (irreversible) Pk/Pd
o GENTAMYCIN, STREPTOMYCIN: Staphylococcal & enterococcal Rare  Excretion (given oral): Feces (poor absorption)
endicarditis  Hypersensitivity,
Aminoglycosides - NOT MONOTHERAPY: P. aeruginosa (pneumonia) (although it HAS
 Excretion (IV): Urine
anaphylaxis  Poorly absorbed in tissue EXCEPT in neonates (large size,
coverage)  Neuromuscular Blockare polycationinc charge, lipid insolubility)
o Poor penetration to infected lung tissue due to low O2 (Antidote: Calcium
GENTAMYCIN TOBRAMYCIN - NOT MRSA
 SYNERGISM with -lactam Abs
Gluconate)  Antagonism with other bacteriostatic agents
 Concentration-dependent killing
o Better efficacy: single large dose
Inhibition
TETRACYCLINE - Coverage for atypicals Common Pk
of Protein 30S - DOC: Ricketssiae  Permanent teeth  Hydrophobic
Synthesis DOXYCYCLINE - Other Uses: Atypicals discoloration  Impaired by food (Except Doxy & Minocycline), antacids,
o Mycoplasma pneumoniae  Bone deformity etc.
o Chlamydia pneumoniae & C. psittuaci  Pregnancy Risk Category D  NO CSF penetration
Tetracyclines o NOT recommended for LEGIONELLA Occasional  Excretion: Bile & Urine; except DOXYCYCLINE (Bile)
o GONOCOCCAL DISEASE (+ CEFtRIAXONE)  Photosensitivity  CAN CROSS PLACENTE, EXCRETED IN MILK
MINOCYCLINE Rare
o Leptospira spp. (Mild infection, prophylaxis) Pd: Time-dependent killing
o Vibrio spp. (Cholera)  Fanconi Syndrome
o Borellia burgdorferi (Lime Disease)  Interstitial Nephritis
o Plasmodium falciparum (Prophylaxis)
- Infections caused by multidrug-resistant organisms (Skin & soft tissue  Same as tetracycline  No cross-resistance with 2nd or 1st gen tetracyclines
Glycycyclines TIGECYCLINE infections; intraabdominal infections)  Alteration of GI flora  NO CSF penetration
(IV) (3rd Gen Tetracycline) - NOT recommended as 1st line drug for pneumonia (treatment faillure)  Excretion: Bile and Urine
- NOT recommended for bacteremia
 Inhibits CLASSIFICATION ANTIBIOTICS Clinical Uses Adverse Effects Pk/Pd
- DOC: ATYPICAL PNEUMONIA – Legionella pneumoniae, Chlamydophila Common  Absorption impaired by food
pneumoniae, Chlamydophila spp.  GI Disturbance (due to MOTILIN)  NO CSF penetration
- DOC: Corynebacterium spp. (Diphteria) Occasional  Excretion: Bile
 Acute cholestatic hepatitis (estolate)  Crosses placenta; excreted in Milk
ERYTHROMYCIN - DOC: Bordetella pertussis
 Stomatitis
- Other:  Inhibitor of CYP 450
Rare
o Chlamydia trachomatis  Infantile hypertrophic pyloric stenosis
 Time-dependent killing
o Penicillin substitute for S. pyogenes with penicillin-allergy  QT interval prolongation
Macrolides  Less GI disturbance  Less affected by food
 Excretion: Urine
CLARITHROMYCIN - Most active against H. influenzae & Myobacterium avium complex  Time-dependent killing
 Inhibitor of CYP 450

 Less GI disturbance  Absorption impaired by food

AZITHROMYCIN - DOC: Bartonella henselae (Cat Scratch Disease)  Concentration-dependent killing
 Does not inhibit CYP 450
Common  Absorption not affected by food
- DOC: Community Acquired MRSA (skin and soft tissue infection)
 GI Distrubance  NO CSF penetration
o NOT for Hospital Acquired MRSA
Occasional  Can penetrate abscesses
Inhibition Lincosamide CLINDAMYCIN o NOT for bacteremia & meningitis  Toxic Megacolon  Excretion: Bile & Urine
- Anaerobic infections ABOVE THE DIAPHARGM (eg. lung abscess) EXCEPT CNS Rare:
of Protein 50S  Crosses placenta
- Alternative for Staphylococcal infections  Esophageal ulceration
Synthesis  Time-dependent killing
Common  Prodrug
 Dose-related Anemia o Oral produces higher livel of free drug than IV
- Alternative drug for -lactam for treatment of meningitis
 Gray Baby Syndrome  CSF penetration
- Other uses:
Occasional  Metabolized in the liver (glucuronic acid conjugation)
CHLORAMPHENICOL o Salmonella typhi  GI disturbance  Excretion: Urine & bile
o Shigella spp. Rare  Crosses placenta; excreted in milk
o Ricketsia spp.  Aplastic Anemia  CYP 450 inhibitor
 Optic Neuritis  Time-dependent killing
Common  BACTERIOSTATIC but BACTERICIDAD AGAINST
- Infections caused by Multidrug-resistant Gram (+) cocci (MRSA, VRA)
 Hematologic disturbances STREPTOCOCCI
o Skin and soft tissue infections
Occasional  100% bioavailability in oral
Oxazolidinone LINEZOLID o Pneumonia
 Lactic Acidosis  CSF penetration
- Not recommended for MRSA bacteremia  Serotonin Syndrome  Excretion: Urine
- Other use: M. tuberculosis  Optic & peripheral neuropathy  Time-dependent killing
QUINUPRISTIN - Infections caused by Multidrug-resistant Gram (+) cocci (EXCEPT Enterococcus  Direct Hyperbilirubinemia  QUIINUPRISTIN-DALFOPRISTIN (30:70 ratio)
faecalis)  Arthralgia-Myalgia Syndrome  NO CSF penetration
(STREPTOGRAMIN B)
Streptogramin o Skin and soft tissue infections  Excretion: Feces
DALFOPRISTIN o Pneumonia  CYP 3A4 inhibitor
(STREPTOGRAMIN A) o Bacteremia  Concentration-dependent killing
 Inhibits CLASSIFICATION ANTIBIOTICS Clinical Uses Adverse Effects Pk/Pd
- DOC: Stenotrophomonas maltophila  SMX: Photosensitivity, Rash  Individually bacteriostatic, together, bactericidal
- DOC: Pneumocystis jiroveci pneumonia (PCP) Occasional  Mechanism of Resistance
SULFAMETH - May be used for prostatitis (prostate penetration) Hematologic Disturbances o SMX
Sulfonamides - NOR for empiric therapy for pneumonia o SMX: Aplastic Anemia, Hemolytic  Overproduction of PABA
-OXAZOLE  Overproduction of duhydropteroate
- Other: anemia (G6PD deficiency(
COTRIMO- o TMP: Megaloblastic Anemia, etc  Impaired entry
Folic Acid o Susceptible MRSA
Synthesis XAZOLE o Burholderia capacia Kernicterus o TMP
(TMP-SMX)  Overproduction of DHFR
o Salmonella typhi Urinary Tract Disturbances
 Impaired entry into the cell
DHFR TRIMETHO- o Shigella spp (REMEMBER: Penetrates prostate)
 CSF penetration, distributed in prostate & vaginal fluid
o Nocordia spp. Rare
Inhibitors PRIM  SMX: Stevens-Johnson Syndrome
 Metabolized in liver
Inhibition o Alternaive treatment for Toxoplasma gondii encephalitis (DOC:  Excretion: urine
PYRIMETHEMINE-SULFADIAZINE)  Lupus-like Syndrome  Time-dependent killing
of Nucleic
CIPROFLOXACIN - CIPROFLOXACIN: most active for gram (-); Pseudomonas coverage  Hyperglycemia  Inhibit bacterial topoisomerase II (DNA Gyrase) &
Acid
- Active against atypical organisms  Arthropathy Topoisomerase IV
Synthesis - Good against N. gonorrhoeae  Damages growing cartilage  CSF penetration and prostate penetration
- CIPROFLOXACIN, LEVOFLOXACIN: Oral step-down therapy for Pseudomonas  RETINAL DETACHMENT (Rare)  Excretion: Urine; EXCEPT:
aeruginosa  QT prolongation, torsades de pointed o GEMIFLOXACIN (Bile and urine)
- Other Uses: o MOXIFLOXACIN (Bile)
DNA Topo- Fluoro- o Salmonella typhi

 Concentration-dependent killing
iso-merases quinolones LEVOFLOXACIN o Shigella spp.
o E. coli (Cystitis, Pyelonephritis)
o N. meningitidis (Post-exposure prophylaxis)
- NOT for N. gonorrhoeae
- Others:
o MDR M. tuberculosis
- Only coverage: Anaerobes inc. B. fragilis & Clostridium difficile  Metallic taste  MOA only achieved in anaerobes
- DOC: Clostridium difficile colitis  Dry mouth  Loss of helical DNA structure and strand breakage
Nitro Group - Anaerobic infections BELOW THE LEVEL OF THE DIAPHRAGM (eg. intraabdominal  Urethral bleeding  CSF penetration
infection)  Darkening of urine  Excretion: Urine & Feces
Chemically
- Brain abscess  Peripheral & optic neutopathy  Penetrate abscesses
Reduced METRONIDAZOLE - Other:  Concentration-dependent killing
(DNA o Clostridium tetani
Damage) o Entamoeba histolytica
o Trichomonas vaginalis
Others
o Giardia lamblia
Synthesis of - Urinary antiseptic (uncomplicated acute cystitis)  Hemolytic anemia 
DNA, RNA, NITROFURANTOIN - NOT during renal failure  Pulmonaryinfiltration, fibrosis
and Proteins - NOT for upper tract infection (pyelonephritis)
Cell Wall   Inhibit enilpyruvate transferase
Synthesis - Uncomplicated acute cystitis  Exxcretion: Urine
FOSFOMYCIN - NOT for 1st line treatment for MDR infections
(Very Early
Stage)
 Inhibits CLASSIFICATION ANTIBIOTICS
Crystalline/Aqueous (IV)
Natural Penicillins PENICILLIN G
Procaine, Benzathine (IM)
(Narrow Spectrum)
PENICILLIN V (Oral)
NAFCILLIN (IV) METHICILLIN
C Penicillins Anti-Staphylococcal
E OXACILLIN (IV) CLOXACILLIN (Oral)
L Amino- AMOXICILLIN )Oral) AMPICILLIN (IV)
L Extended-Spectrum Carboxy- TICARCILLIN CARBENICILLIN
Ureido- PIPERACILLIN (IV)
W COAMOXICLAV
A CLAVULANIC ACID (+ Amoxicillin)
L -Lactamase Inhibitors + Ticarcillin
L SULBACTAM + Ampicillin
TAZOBACTAM + Piperacillin
S 1st Gen CEPHALEXIN (Oral) CEFAZOLIN (IV)
Y CEFUROXIME (Oral) CEFUROXIME (IV)
N 2nd Gen CEFACLOR (Oral) CEFOTETAN (IV)
T CEFOXITIN (IV)
H CEFTRIAXONE (IV)
Cephalosporins CEFPODOXIME (Oral)
E CEFOTAXIME (IV)
3rd Gen
S CEFOPERAZONE (IV)
CEFIXIME (ORAL)
I CEFTAZIDIME (IV)
S 4th Gen CEFEPIME CEFPIROME
5th Gen CEFTAROLINE
Monobactam AZTREONAM (IV)
IMIPENEM (IV) DORIPENEM (IV)
Carbepenem
MEROPENEM (IV) ERTAPENEM (IV)
VANCOMYCIN
Glycopeptides
TEICOPLANIN (IV, IM) TELAVANCIN*
Cell Membrane Function Lipopeptides DAPTOMYCIN (IV)
Polymixin B (SC)
Polymixins
Polymixin E (COLISTIN) (IV)
STREPTOMYCIN AMIKACIN
Aminoglycosides
GENTAMYCIN TOBRAMYCIN
TETRACYCLINE
30S Tetracyclines DOXYCYCLINE
MINOCYCLINE
Glycycyclines TIGECYCLINE
(IV) (3rd Gen Tetracycline)
Inhibition of Protein ERYTHROMYCIN
Synthesis
Macrolides CLARITHROMYCIN
AZITHROMYCIN
Lincosamide CLINDAMYCIN
50S
CHLORAMPHENICOL
Oxazolidinone LINEZOLID
QUINUPRISTIN (STREPTOGRAMIN B)
Streptogramin
DALFOPRISTIN (STREPTOGRAMIN A)
TibbsNotes – Antibacterial Table