MARK M CALBAN MD MPM-HSD
1-1
BACTERICIDAL
Can eradicate an infection in the abscence of
host defense mechanisms.
KILLS BACTERIA
“Very Finely Proficient At Murder”
Vancomycin, Fluoroquinolones, Penicillins,
Aminoglycosides, Metronidazole
Matrix IOP 1-2
BACTERIOSTATIC
Inhibit microbial growth but requires host
defense mechanisms.
DOES NOT KILL BACTERIA
“ECSTaTiC”
Erythromycin, Clindamycin,
Sulfamethoxazole, Trimethoprim,
Tetracycline, Chloramphenicol
Matrix IOP 1-3
MINIMUM INHIBITORY CONCENTRATION
Lowest concentration of antimicrobial
drug capable of inhibiting growth of an
organism in a defined growth medium.
Matrix IOP 1-4
EMPIRIC THERAPY
Initiation of a drug treatment before
identification of a specific pathogen.
ANTIMICROBIAL PROPHYLAXIS
Use of antimicrobial drugs to DECREASE the
risk of infection.
BACTERIAL CELL WALL
SYNTHESIS INHIBITORS
“PENICILLINS”
PENICILLINS
Binds to Penicillin Binding Proteins (PBPs)
located in the bactetial cytoplasmic
membrane.
Activates autolytic enzymes that cause
lesions in the bacterial cell wall.
PENICILLIN RESISTANCE
Enzymatic hydrolysis of the beta lactam ring
by formation of BETA LACTAMASE or
PENICILLINASE
– Staphylococcus aureus
– Beta Lactamase Inhibitors:
• CaST - Clavulanic Acid, Sulbactam,
Tazobactam
–Co-Amoxiclav, Ampicillin-Sulbactam,
Piperacillin Tazobactam
PENICILLIN RESISTANCE
Structural change in target PBPs
Methicillin Resistant Staphylococcus
aureus, Pneumococci, Enterococci
Change in the porin structures in outer
cell wall impeding access of penicillins to
PBPs.
Pseudomonas aeruginosa
PENICILLIN G
Similar Drug PENICILLIN V
Class Penicillin (Narrow Spectrum)
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses SYPHILIS
Streptococcal, Meningococcal & Pneumococcal Infxns
SE Hypersensitivity; GI Disturbances
Notes Renal Tubular Reabsorption is inhibited by PROBENECID
Inactivated by BETA LACTAMASE/PENICILLINASE
Long Acting IM Preparations - Benzathine PenG and
Procaine Penicillin
METHICILLIN (Anti-Staphylococcal)
Similar Drug METHICILLIN, OXACILLIN, CLOXACILLIN,
DICLOXACILLIN
Class Penicillin (Very Narrow Spectrum)
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Staphylococcal Infections
SE Hypersensitivity; GI Disturbances
INTERSTITIAL NEPHRITIS (METHICILLIN)
NEUTROPENIA (NAFCILLIN)
Notes Resistant to inactivation by Beta Lactamase
BILIARY CLEARANCE
AMPICILLIN (Aminopenicillin)
Similar Drug AMOXICILLIN
Class Penicillin (Extended Spectrum)
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Infections due to the following: HEELPSM
Haemophlus influenzae
Escherichia coli
Enterococci
Listeria monocytogenes
Proteus mirabilis
Salmonella spp
Moraxella catarrhalis
SE PSEUDOMEMBRANOUS COLITIS
Notes inactivation by Beta Lactamase
Ampicillin Sulbactam
Synergistic Effect with aminoglycosides
AMPED UP Penicillin
PIPERACILLIN (Anti-Pseudomonal
Penicillin)
Similar Drug TICARCILLIN, CARBENICILLIN
Class Penicillin (Anti-Pseudomonal)
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Greater activity against GRAM NEGATIVE infections
-Pseudomonas, Enterobacter, klebsiella
SE Hypersensitivity
Notes inactivation by Beta Lactamase
Synergistic with aminoglycosides against
Pseudomonas
PIPERACILLIN (Anti-Pseudomonal
Penicillin)
Similar Drug TICARCILLIN, CARBENICILLIN
Class Penicillin (Anti-Pseudomonal)
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Greater activity against GRAM NEGATIVE infections
-Pseudomonas, Enterobacter, klebsiella
SE Hypersensitivity
Notes inactivation by Beta Lactamase
Synergistic with aminogllycosides against
Pseudomonas
Anti-Pseudomonal Penicillins
“Takes Care of Pseudomonas”
-Ticarcillin, Carbenicillin, Piperacillin
1-16
CEFAZOLIN (1st Generation)
Similar Drug CEFADROXIL, CEPHALEXIN, CEPHALOTHIN,
CEPHAPIRIN, CEPHRADINE
Class Cephalosporin
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Surgical Prophylaxis
Bone Infections
Infections due to Staph and Strep
E. coli and Klebsiella pneumoniae
Skin and soft tissue infections; UTI
SE Hypersensitivity
Notes Increases nephrotoxicity with AMINOGLYCOSIDES
Which microbes are covered by
1st Generation Cephalosporins?
PEK
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
1st Generation Cephalosporins
FADer, help me FAZ my
PHarmacology boards!
CeFAdroxil
CeFAzolin
CePHalothin
CePHapirin
CePHradine
CePHalexin
CEFACLOR (2nd Generation)
Similar Drug CEFAMANDOLE, CEFMETAZOLE, CEFONICID,
CEFUROXIME, CEFPROZIL, CEFORANIDE,
CEFOXITIN, CEFOTETAN, LORACARBEF
Class Cephalosporin
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Haemophilus, Enterobacter and Neissera Infxns
SE Hypersensitivity
Notes Increases nephrotoxicity with AMINOGLYCOSIDES
Which microbes are covered by
2nd Generation Cephalosporins?
HEN PEcKS
Haemophilus influenzae
Enterobacter aerogenes
Neisseria spp
Proteus mirabilis
Escherichia coli
Klebsiella pneumoniae
Serratia marcescens
CEFOPERAZONE (3rd Generation)
Similar Drug CEFOTAXIME, CEFTAZIDIME, CEFTIZOXIME,
CEFTRIAXONE, CEFIXIME, CEFPOXIME PROXETIL,
CEFDINIR, CEFDITOREN PIVOXIL, CEFTIBUTEN,
MOXALACTAM
Class Cephalosporin
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses DECREASED GRAM (+) COVERAGE
INCREASED GRAM (-) ACTIVITY
Pseudomonas
Bacteroides
SE Hypersensitivity
DISULFIRAM REACTION - Cefoperazone
Notes SYNERGISTIC EFFECT with AMINOGLYCOSIDES
CEFEPIME (4th Generation)
Similar Drug CEFTAROLINE
Class Cephalosporin
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Wide Coverage against Gram (+) and Gram (-) Bacteria
SE Hypersensitivity
Notes Resistant to BETA LACTAMASE
Broad Gram (-) Activity
Anti-Pseudomonal
Cephalosporins
Ceftazidime
Cefepime
Cefoperazone
1-25
IMIPENEM-CILASTATIN
Similar Drug ERTAPENEM, MEROPENEM, DORIPENEM
Class CARBAPENEM
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Wide Coverage against Gram (+) and Gram (-) Bacteria
For serious infections as PNEUMONIA & SEPSIS
SE Hypersensitivity
CNS Toxicity - Confusion, Encephalopathy & Seizures
Notes “Drugs of Last Resort”
AZTREONAM
Similar Drug
Class MONOBACTAM
MOA Binds to penicillin binding protenins (PBPs);
Inhibits transpeptidation in bacteial cell wall
Uses Infections resistant to Beta Lactamases produced by
Gram (-) rods including
Klebsiella, Pseudomonas and Serratia
SE GI Upset
HEPATOTOXICITY
Notes Resistant to Beta Lactamases
NO CROSS HYPERSENSITIVITY TO PENICILLIN
No activity Vs Gram (+) Bacteria or anaerobes
For aerobic Gram (-) bacteria with hypersensitivity to
penicillins
CLAVULANIC ACID
Similar Drug SULBACTAM, TAZOBACTAM
Class BETA LACTAMASE INHIBITOR
MOA Inhibits inactivation of penicillins by beta lactamase or
penicillinase
Uses Beta Lactamase producung Gonococci, Strep, E. coli
and H. influenzae
SE Hypersensitivity
CHOLESTATIC JAUNDICE
Notes Amoxicillin-Clavulanate
Ampicillin-Sulbactam
Piperacillin-Tazobactam
VANCOMYCIN
Similar Drug TESCOPLANIN, DALBAVANCIN, TELAVANCIN
Class GLYCOPEPTIDE
MOA Inhibits CELL WALL SYNTHESIS by binding to the D-ALA-
D-ALA terminus of nascent peptidoglycan
Uses Serious Drug Resistant G (+) organisms (MRSA)
Sepsis
Endocarditis amd Meningitis
PSEUDOMEMBRANOUS COLITIS
SE RED MAN SYNDROME (Slow rate of infusion)
NEPHROTOXICITY
OTOTOXICITY
Notes Drug of Last Resort
Drugs of Last Resort
“I AM your Last Shot at Victory”
Imipenem
Amikacin
Meropenem
Linezolid
Streptogramins
Vancomycin
BACITRACIN
Similar Drug
Class PEPTIDE ANTIBIOTIC
MOA Interferes with a late stage in CELL WALL synthesis in
GRAM (+) organisms.
Uses for GRAM (+) infections
SE NEPHROTOXICITY
Notes FOR TOPICAL USE ONLY DUE TO NEPHROTOXIC
EFFECT
CYCLOSERINE
Similar Drug
Class
MOA Blocks incorporation of D-Ala into the pentapeptide side
chain of the peptidoglycan
Uses Drug Resistant Tuberculosis
SE NEUROTOXICITY
Tremors
Seizures
Psychosis
Notes
CYCLOSERINE
Similar Drug
Class
MOA Blocks incorporation of D-Ala into the pentapeptide side
chain of the peptidoglycan
Uses Drug Resistant Tuberculosis
SE NEUROTOXICITY
Tremors
Seizures
Psychosis
Notes
Proten Synthesis Inhibitors
Aminoglycosides
Tetracyclines
Chloramphenicol
Erythromycin
Lincosamides
Linezolid
Streptogramins
CHLORAMPHENICOL
Similar Drug
Class PROTEIN SYNTHESIS INHIBITOR (Broad Spectrum)
MOA Inhibits TRANSPEPTIDATION (catalyzed by
transpeptidase) at 50S Subunit
BACTERIOSTATIC
Uses MENINGITIS
STREP. PNEUMONIAE
HAEMOPHILUS INFLUENZAE
NEISSERIA MENINGITIDIS
Back up for Salmonella, Rickettsia and Bacteroides
SE GRAY BABY SYNDROME
ANEMIA
Notes Inhibits many drug metabolizing enzymes causing
many drug interactions
Gray Baby Syndrome
Characterized by decreased red
blood cells, cyanosis and
cardiovascular collapse
“Gray Skin”
TETRACYCLINE
Similar Drug DOXYCYCLINE, MINOCYCLINE, TIGECYCLINE,
DEMECLOCYCLINE
Class TETRACYCLINE
MOA Binds 30S ribosomal subunit
BACTERIOSTATIC. Blocks attachment of TRNA to
acceptor site
Uses Mycoplasma pneumoniae
Chalmydia
Rickettsia
Vibrio
PUD, Lyme Disease, Malaria Prophylaxis,
Amoebiasis, SIADH (Demeclocycline), Acne, CAP,
Bronchitis (Doxycycline)
SE Tratogen - TOOTH ENAMEL
DYSPLASIA/DISCOLORATION
HEPATOTOXIC, NEPHROTOXIC, PHOTOSENSITIVITY
REVERSIBLE VESTIBULOTOXICITY (Minocycline)
Notes TIGECYCLINE has the broadest spectrum with the
least resistance
CLINDAMYCIN
Similar Drug LINCOMYCIN
Class LINCOSAMIDE
MOA Binds 50S ribosomal subunit
BACTERIOSTATIC.
Uses Skin and Soft Tissue Infections
Anaerobic Infections
Endocarditis Prophylaxis (Penicillin Allergy)
PCP Pneumonia
Toxoplasmosis
SE NEUTROPENIA
HEPATIC DYSFUNCTION
PSEUDOMEMBRANOUS ENTEROCOLITIS
Notes Cross resistance between clindamycin and macrolides
is common
Clindamycin Vs Metronidazole
CLINDAMYCIN - for anaerobic
infections ABOVE the diaphragm
METRONIDAZOLE - for anaerobic
infections BELOW the diaphragm
QUINUPRISTIN-DALFOPRISTIN
Similar Drug
Class STREPTOGRANIN
MOA Binds 50S ribosomal subunit
BACTERICIDAL.
Uses MRSA
VRSA
VRE
SE ARTHRALGIA-MYALGIA SYNDROME
Notes Inhibits CYP450 enzymes
LINEZOLID
Similar Drug
Class OXAZOLIDINONE
MOA Binds 23S ribosomal RNA of 50S subunit
BACTERIOSTATIC
Uses MRSA
VRSA
VRE
LISTERIA , CORYNEBACTERIA
SE BONE MARROW SUPPRESSION
LINEZOLID + SSRI = SEROTONIN SYNDROME
OPTIC NEURITIS
Notes -
1-42
CONCENTRATION DEPENDENT
KILLING ACTION
As the plasma level is increased
above the MIC, an increasing
proportion of bacteria are killed at a
more rapid rate
AMINOGLYCOSIDES
TIME DEPENDENT KILLING
ACTION
Efficacy is directly related to time
above MIC.
efficacy is INDEPENDENT of
concentration once the MIC has been
reached.
PENICILLINS & CEPHALOSPORINS
POST ANTIBIOTIC EFFECT
Seen in aminoglycosides
Killing action continues even when
the plasma levels have declined.
Greater efficacy when administered
as a SINGLE DOSE.
PHARMACOKNETICS OF
AMINOGLYCOSIDES
NOT absorbed after oral
administration - MUST BE GIVEN IM
OR IV
Limited tissue penetration - DOESNT
CROSS THE BB
Glomerular Filtration is the major
mode of excretion
GNATS does NOT kill Anaerobes
Gentamycin
Neomycin
Amikacin
Tobramycin
Streptomycin
Nephrotoxicity
Ototoxicity
Teratogen
GENTAMICIN
Similar Drug TOBRAMYCIN
Class AMINOGLYCOSIDE
MOA Binds 30S ribosomal subunit
BACTERICIDAL
Uses AEROBIC GRAM (-) bACTERIA - E. coli, Enterobacter,
Klebsiella, Proteus, Providencia, Pseudomonas,
Serratia
ENDOCARDITIS - Staph, Strep and Enterococci
OCULAR INFECTIONS
SE REVERSIBLE NEPHROTOXICITY
IRREVERSIBLE OTOTOXICITY
NEUROMUSCULAR BLOCKADE
Notes Synergistic effect w/ BETA LACTAM ANTIBIOTics and
Vancomycin
GENTAMYCIN AND TOBRAMYCIN are the most
vestibulotoxic and nephrotoxic
AMIKACIN
Similar Drug
Class AMINOGLYCOSIDE
MOA Binds 30S ribosomal subunit
BACTERICIDAL
Uses AEROBIC GRAM (-) bACTERIA - E. coli, Enterobacter,
Klebsiella, Proteus, Providencia, Pseudomonas,
Serratia
MDRTB
SE REVERSIBLE NEPHROTOXICITY
IRREVERSIBLE OTOTOXICITY
NEUROMUSCULAR BLOCKADE
Notes Synergistic effect w/ BETA LACTAM ANTIBIOTics
LEAST RESISTANCE BUT NARROWEST
THERAPEUTIC WINDOW
STREPTOMYCIN
Similar Drug
Class AMINOGLYCOSIDE
MOA Binds 30S ribosomal subunit
BACTERICIDAL
Uses TB,TULAREMIA, BUBONIC PLAGUE, BRUCELLOSIS,
ENTEROCOCCAL ENDOCARDITIS
SE REVERSIBLE NEPHROTOXICITY
IRREVERSIBLE OTOTOXICITY
NEUROMUSCULAR BLOCKADE
CONGENITAL DEAFNESS
Notes Synergistic effect w/ BETA LACTAM ANTIBIOTics
ADMINISTERED IM
NEOMYCIN
Similar Drug KANAMYCIN, PAROMOMYCIN
Class AMINOGLYCOSIDE
MOA Binds 30S ribosomal subunit
BACTERICIDAL
Uses SKIN INFECTIONS
BOWEL PREPARATION FOR ELECTIVE SURGERY
VISCERAL LEISHMANIASIS (PAROMOMYCIN)
HEPATIC ENCEPHALOPATHY
SE REVERSIBLE NEPHROTOXICITY
IRREVERSIBLE OTOTOXICITY
NEUROMUSCULAR BLOCKADE
Notes Limited to Topical and Oral Use
Reversible Neuromuscular Blockade with Calcium
Gluconate and Neostigmine
KANAMYCIN IS MOST OTOTOXIC
SPECTINOMYCIN
Similar Drug
Class AMINOGLYCOSIDE
MOA Binds 30S ribosomal subunit
BACTERICIDAL
Uses DRUG RESISTANT GONORRHEA IN PENICILLIN
ALLERGIC PATIENTS
SE REVERSIBLE NEPHROTOXICITY
IRREVERSIBLE OTOTOXICITY
NEUROMUSCULAR BLOCKADE
ANEMIA
Notes Given IM
1-53
OTOTOXICITY
MOST OTOTOXIC: Kanamycin, Amikacin
MOST VESTIBULOTOXIC: Tobramycin,
Gentamycin
Cumulative Toxicity when used with LOOP
DIURETICS
NEPHROTOXIC
ACUTE TUBULAR NECROSIS
MOST NEPHROTOXIC
– Tobramycin
– Gentamycin
NEUROMUSCULAR BLOCKADE
CURARE-LIKE effect (non-depolarizing NM
Blockade)
Reversible with CALCIUM AND
NEOSTIGMINE
SKIN REACTIONS
Commonly from Neomycin and Streptomycin
salamat po!
