Anti-microbials IIa/b Flashcards
Cell Wall Synthesis Inhibitor Drug CLASSES (8)
Penicillins Cephalosporins Monobactams Glycopeptides Polypeptides Carbapenems Phosphoenolpyruvate Beta-lactamase inhibitor
Cell Membrane Targeting Drug CLASSES (2)
Lipopeptides
Detergents
Protein Synthesis Inhibitor Drug CLASSES (4)
Tetracyclines
Aminoglycosides
Macrolides
Others (clindamycin, chloramphenicol, linezolid)
DNA/RNA Synthesis Inhibitor drug CLASSES (4)
Sulfonamides
Trimethoprims
Fluoroquinolones
Metronidazole
Main components of bacterial cell wall
peptidoglycan
NAM-NAG-Pentapeptide repeating monomers
Penicillin Binding Proteins important for
LINKING PENTAPEPTIDE TO FORM PEPTIDOGLYCAN cell wall
Beta lactam compounds (4)
PENICILLINS
CEPHALOSPORINS
MONOBACTAMS
CARBAPENEMS
Cell wall synthesis inhibitors generally are ________
bactericidal
Penicillins MOA
Adverse effect?
bind and inhibit PBP enzymes
HYPERSENSITIVITY RXN - rash to anaphylaxis range
With hypersensitivity and penicillins, if someone has anaphylaxis hypersensitivity, what do you need to consider?
CROSS REACTIVITY with similar compounds (beta-lactam ring)
Narrow Spectrum Penicillin (2)
beta-lactamase sensisity?
Penicillin G and V
sensitive
Very narrow spectrum Penicillin (3)
beta-lactamase sensisity?
Methicillin
Nafcillin
Oxacillin
resistant
Broad spectrum Penicillins (2)
beta-lactamase sensisity?
Ampicillin
Amoxicillin
sensitive
Extended spectrum Penicillins (3)
beta-lactamase sensisity?
Piperacillin
Ticarcillin
Azlocillin
sensitive
Beta-lactamase inhibitor?
Adverse effects associated with?
CLAVULANIC ACID
Augmentin (amoxicillin + clavulanic acid)
Adverse effects are associated with whatever drug clavulanic acid is combined with
Cephalosporins MOA
Adverse effect?
Bind and inhibit PBP’s
HYPERSENSITIVITY
Changes from generation to generation of cephalosporins
INCREASE SPECTRUM OF ACTIVITY FROM 1ST TO 4TH
starts with gram positive and mores to include more gram negative
1st generation Cephalosporins (2)
beta lactamase sensitivity?
enter CNS?
Cefazolin
Cephalexin
sensitive
do not enter CNS
2nd Generation cephalosporins (3)
beta lactamase sensitivity?
enter CNS?
Cefotetan
Cefaclor
Cefuroxime
Sensitive
only cefuroxime enters CNS
3rd Generation cephalosporins (4)
beta lactamase sensitivity?
enter CNS?
Ceftriaxone
Cefotaxime
Cefdinir
Cefixime
sensitive
MOST ENTER CNS
4th Generation cephalosporins (1)
beta lactamase sensitivity?
enter CNS?
Cefepime
resistant
ENTER CNS
Monobactam MOA
Drug?
Specific for what type of bacteria?
Adverse reaction
CNS penetration?
binds to and inhibits PBP
Aztreonam
GRAM NEGATIVE
HYPERSENSITIVITY
Passes into CNS easily
Carbipenems (4)
Which is co-administered with cilastatin?
Doripenem
Imipenem*** (co-administered)
Ertapenem
Meropenem
Carbipenems MOA
Adverse reaction
beta lactamase sensitivity?
CNS penetration?
bind to and inhibit PBP’s
GI UPSET
RESISTANCE
Penetrates CNS relatively well
Glycopeptide drug?
MOA?
Adverse effect?
Good for treatment of?
Penetrate CNS?
Vancomycin
PREVENTS ELONGATION OF PEPTIDOGLYCAN CELL WALL –> binds D-ala-D-ala pentapeptide
FLUSHING - red man syndrome
resistant strains of bacteria (MRSA, enterococci, C. difficile)
does not have good CNS penetration
Polypeptide drug?
MOA?
Commonly found in?
bacitracin
blocks incorporation of amino acids and nucleic acids into cell wall
TOPICAL OINTMENTS
Phosphoenolpyruvate drug?
MOA?
Commonly used in treatment of?
Fosfomycin
blocks early step in cell wall synthesis by preventing synthesis of UDP-NAM
UTI’s
Protein synthesis inhibitors are typically _______
bacteriostatic
Steps of Prokaryotic Translation
1 - tRNA binds to A site
2 - peptide bond formed
3 - newly uncharged tRNA exits
4 - now longer chain translocates to P site
Aminoglycosides (6)
streptomycin gentamicin kanamycin amikacin tobramycin neomycin
Aminoglycosides MOA?
Key adverse effects?
typically bacteriostatic or cidal?
binds to 30S RIBOSOMAL SUBUNIT - blocks formation of INITIATION COMPLEX
NEPHROTOXIC
OTOTOXIC
typically bacteriocidal
Macrolides (3)
erythromycin
clarithromycin
azithromycin
Macrolides MOA?
Key adverse effect?
typically bacteriostatic or cidal?
BINDS 50S SUBUNIT - impairs translocation of P site (step 4)
GI UPSET
bacteriocidal
Tetracyclines (4)
tetracycline
minocycline
tigecycline
doxycycline
Tetracycline MOA
key adverse effects?
typically bacteriostatic or cidal?
30S SUBUNIT BINDING - prevents binding of new tRNA to A site (step 1)
NUTRIENT INTERACTIONS - binds calcium - discoloration of bone/teeth
ECOLOGICAL EFFECTS
PHOTOSENSITIVITY
bacteriocidal
Clindamycin MOA
key adverse effect?
Spectrum?
BINDS 50S SUBUNIT - prevents formation of initiation complex (step 1) and translocation to P site (step 4)
GI –> HIGHLY ASSOCIATED WITH C. DIFFICILE
Narrow spectrum
Chloramphenicol MOA
Key adverse effects?
BINDS 50S SUBUNIT - prevents transpeptidation (step 2)
BLOOD - RBC PRODUCTION SUPPRESSION
GRAY BABY SYNDROME - glucuronic acid conjugation step inhibited
Linezolid MOA
Key adverse effect?
Good for what type of organisms?
INHIBITS PROTEIN SYNTHESIS - binds to P site of 50S RIBOSOME and inhibits very first charged tRNA from coming into complex (step 1)
BLOOD - myelosuppression (pancytopenia)
RESISTANT ORGANISMS
50 S binding drug classes (4)
Macrolides
Clindamycin
Chloramphenicol
Linezolid
30 S binding drug classes (2)
Aminoglycosides
Tetracyclines
Sulfonamides (3)
sulfadiazine
sulfamethoxazole
sulfamethizole
Sulfonamides MOA
Key adverse effect?
competitively inhibits DIHYDROPTEROATE SYNTHASE
SKIN - hypersensitivty, photosensitivity, Steven-Johnson Syndrome
Trimethoprim MOA
Key adverse effect?
Commonly used for?
Inhibits bacterial DIHYDROFOLATE REDUCTASE
BLOOD - bone marrow suppression, megaloblastic anemia, leukopenia, granulocytopenia
UTI’s (combined with sulfonamide)
TMP-SMX characteristic
common clinical use?
SYNERGISTIC ACTIVITY OF SULFONAMIDES AND TRIMETHOPRIM
UTI’s
Fluoroquinolones Group 2
active against?
Ciprofloxacin
Levofloxacin
Ofloxacin
better against gram negative, some gram positive
Fluoroquinolones MOA
Key adverse effects (3)?
clinical?
INHIBITS DNA TOPOISOMERASE II AND IV
GI
Drug-nutrient interactions - binds divalent cations
Cardio - QT prolongation
urinary, GI, respiratory, ANTHRAX, some STI’s
Fluoroquinolones group 1
characteristic?
Norfloxacin
least activity
Fluoroquinolones group 3
active against?
Gatifloxacin
Gemifloxacin
Moxifloxacin
best against gram positive
Metronidazole MOA
Key adverse effects (2)?
Activity limited to?
PRODRUG - forms REACTIVE METABOLITES that bind to DNA and disrupt function
GI
Metabolism - DISULFIRAM LIKE REACTION
ANAEROBIC BACTERIA
Daptomycin MOA
Key adverse effect(1)?
CAUSES DEPOLARIZATION OF BACTERIAL MEMBRANE - ultimately bactericidal
MUSCULOSKELETAL TOXICITY
Polymyxin B MOA
BINDS TO PHOSPHOLIPIDS - disrupts structure - specificaly LPS BINDING
rare adverse effects
TOPICAL most often
