Multi-Systems: ABX Flashcards
(3) Mechanisms of ABX that inhibit Cell Wall Biosynthesis?
- Inhibit Peptidoglycan Cross-linking
- Inhibit Peptidoglycan Polymerization
- Inhibit Cell wall Synthesis by Binding PBP3
ABX that inhibit Membrane Potential?
-
Lipopeptides
- Daptomycin
(1) ABX that cause Cell Membrane Disruption?
-
Polymyxins
- Polymyxin A
- Polymyxin B
(10) ABX that inhibit Protein Synthesis?
- Oxazoladinones
- Tetracyclines
- Aminoglycosides
- Glycylcycline
- Chloramphenicol
- Clindamycin
- Lincosamines
- Macrolides
- Streptogramins
- Trimethoprim
(2) ABX that inhibit Folic Acid Synthesis?
(DNA Methylation)
- Sulfonamides
- Trimethoprim
(3) ABX that inhibit DNA Replication or Transplatation?
-
Fluoroquinolones (DNA Topoisomerase)
- Ciprofloxacin
- Levofloxacin
- Nitroimidazole
- Rifamycin (mRNA synthesis - RNA Polymerization)
(2) ABX that acts on the Transglycosylase enzyme
of the Cell Wall Biosynthesis?
-
Vancomycin
- D-ala D-ala portion of cell wall precursor
- Teicoplanin
(5) Sub-types of ABX that acts on the Transpeptidase
of the Cell Wall Biosynthesis?
(Inhibiting Peptidoglycan Cross-linking)
- Beta-Lactams
- Penicillins (Sensitive, Resistant)
- Cephalosporins (I, II, III, IV)
- Carbecephams
- Carbepenems
- Monobactams
(5) Penicillinase-Resistant Penicillins?
“MEt NAsty OX -OX -OX”
- Methicillin
- Nafcillin
- Oxacillin
- Cloxacillin
- Dicloxacillin
(2) Extended Range Penicillins?
“AM extended”
- Ampicillin
- Amoxicillin
- Penicillinase Sensitive
- Combine w/ Clavulanic Acid
- -> protect against β-lactamase
- “AMinoPenicillins are AMPed-up Penicillin”
Anti-Pseudomonal Penicillins?
“Pseudo-cars (2x), Never are more popular”
- Carboxylated derivatives extend range of Ampicillin to
- P. aeruginosa*; Indole-positive Proteus and Enterobacter
- Carbenicillin
- Ticarcillin
-
N-acyl derivatives
- Azlocillin
- Mezlocillin
- Piperacillin
(3) Prophylaxis during intra-abdominal surgery?
- Cefotetan (2nd)
- Cefoxitin (2nd)
- Neomycin (Bowel surgery) (Aminoglycoside)
(4) Surgery prophylaxis?
- First Generation
- Cephalexin
- Cephadrine
- Cefadroxil
- Cefazolin
(1) Used to treat Community-acquired Pneumonia?
(H. influenzae and K. pneumoniae)
- Cefuroxime
(1) Used to treat Diabetic Foot Infections?
- Cephalexin
Drugs of choice for treating?
(1) N. gonorrhea
(2) Meningitis (Adult, Children)
(1) B. burgdorferi
-
N. gonorrhea
- Ceftriaxone
-
Meningitis
- Ciprofloxacin (1st)
- Rifampin (children)
-
B. burgdorferi
- Tetracyclines
(2) ABX for Multidrug-resistant Gram-negative Infections, especially those caused by P. aeruginosa?
- Ceftazidime
- Cefoperazone
First β-lactam approved for MRSA?
Better drug Rx for MRSA?
- Ceftaroline fosamil (IV) (1st)
- Vancomycin (Better)
(3) Glycopeptide ABX?
(Inhibits Peptidoglycan Syn. –> Cell Wall Synthesis)
- Vancomycin
- Bacitracin
- Teicoplanin
Pathogenic spectrum of Vancomycin?
- G+ only
- Bacteriostatic against Gram-positive Cocci
-
Bactericidal for Gram-positive Rods
- Serious Penicillinase producers
- MRSA
- Enterococci
- NOT Effective against Gram negatives
- Last Resort for Pseudomembranous colitis cause by
- C. difficile* (Oral Vancomycin)
Where does Vancomycin work?
- Binds to D-Ala-D-Ala terminus of Murein Monomer
- -> D-Ala-D-Lactate. Same mode of VRE
- Inhibits Murein Polymer synthesis
- -> Inhibits Peptidoglycan formation
- Blocks attachment of Disaccharide subunits to pre-existing Cell Wall
SE of Vancomycin?
“NOT”
-
Hypersensitivity Rxn - Skin flushing or Rash
- “Red man syndrome” - rapid infusion due to Histamine release (slow infusion and pretreatment w/ antihistamines)
- Nephrotoxicity
- Ototoxicity
- Thrombophlebitis
- Neutropenia
- Tissue necrosis if given IM
Pathogen spectrum of Lipopeptide ABX?
-
Gram positive Aerobic organisms
- Complicated skin infections
- Endocarditis
- Bactericidal against VRE?
- Bacteriostatic against
- S. pneumoniae
- S. aureus
- Retains activity against Gram-positive bacteria
- Synergizes w/ Oxacillin against MRSA
Where does Lipopeptide ABX work?
- Binds to Bacterial Membranes
- Forms membrane channels in a Calcium-dependent manner leading to a rapid membrane depolarization thus inhibiting protein
- DNA and RNA synthesis
SE of Lipopeptide ABX?
- Irritation at site of Injection
- Skeletal muscle Pain and Weakness (Myopathy)
- Increase in CPK (creatine phosphokinase)
- Renal Failure
Where does Polymyxins ABX work?
- Cationic detergents (positive potential) disrupt the membranes of Gram-negative Bacteria
Pathogen spectrum of Polymyxins?
- Topical: OTC ointments
- IV: Last resort for Gram-negative infections
- Ophthalmic drops
- Otic drops
SE of Polymyxins?
- (IV) EXTREME Nephrotoxicity and Neurotoxic
- Sometimes used Internally for Multidrug resistant Strains
- Acinetobactor from the Middle East
(2) ABX that Inhibit Peptidoglycan Polymerization Synthesis?
(Glycopeptides)
-
Bactericidal
- Vancomycin
- Bacitracin
(1) ABX that Inhibits Cell Wall Synthesis by Binding PBP-3?
(Monbactam - monocyclic β-lactam)
-
Bactericidal
- Aztreonam
- Penicillin-binding-protein 3 (PBP-3)
(1) ABX that Disrupt Outer Membrane in
* *Gram-negative Bacteria**?
-
Bactericidal
- Polymyxins
ABX that inhibits Synthesis,
Para-aminobenzoic acid (PABA)
inhibit Dihydropteroate Synthetase
in Nucleotide Synthesis?
1x - Bacteriostatic
-
Bacteriostatic
- Sulfonamides
ABX that Inhibit Dihydrofolate Reductase
for Nucleotide Synthesis?
2x - Bactericidal
2x - Bacteriostatic
-
Bactericidal
- Trimethoprim (Dihydrofolate reductase)
- Sulfamethoxazole (inhibit Folate synthesis)
-
Bacteriostatic
- Trimethoprim (Dihydrofolate reductase)
- Pyrimethamine
ABX that Inhibit DNA gyrase - Type II and TYpe IV Topoisomerase?
1x - Bactericidal
-
Bactericidal
- Fluoroquinolones (must be taken w/ antacids)
ABX that Inhibit mRNA Synthesis?
1x - Bactericidal
-
Bactericidal
- Rifampin (DNA-dependent RNA polymerase)
ABX that Binds 23S, Blocks initiation of
Complex formation of 50S Ribosomal subunit?
1x - Bacteriostatic
-
Bacteriostatic
- Linezolid (Binds to 23S RNA)
ABX that Blocks release of Nascent Peptides from the Ribosome at 50S Ribosomal subunit?
1x - Bactericidal
1x - Bacteriostatic
-
Bactericidal
- Quinupristin/Dalfopristin
-
Bacteriostatic
- Macrolides (Erythromycin) (Methylation 23S rRNA)
ABX that Block peptide transfer (translocation) at 50S Ribosomal subunit?
1x - Bacteriostatic
-
Bacteriostatic
- Clindamycin
ABX that inhibits Peptidyltransferase
at 50S Ribosomal subunit?
1x - Bacteriostatic
-
Bacteriostatic
- Chloramphenicol
ABX that Inhibit formation of Initiation complesx cause miscoding (misreading) of mRNA and incorrect Amino acid linking for Peptide formation?
Blocking normal Protein Synthesis at 30S Ribosomal subunit?
1x - Bactericidal
-
Bactericidal
- Aminoglycosides (Gentamicin)
ABX that Block binding of aminoacyl-tRNA and Addition of Amino Acids to the Peptide chain of 30S Ribosomal subunit?
1x - Bacteriostatic
-
Bacteriostatic
- Tetracyclines
(1) ABX that works on Dihydropteroate Synthetase
Enzyme that converts PABA –> Dihydrofolate?
(Inhibits Folate Synthesis)
- Sulfonamides
2x ABX that works on Dihydrofolate reductase
enzyme for Dihydrofolate –> THF?
- Trimethoprim
- Pyrimethamine
(1) ABX that inhibits DNA gyrase Topoisomerase II and Topoisomerase IV activity?
- Fluoroquinolones
(1) ABX that inhibits the formation of mRNA from Nucleotides through blocking DNA-dependent RNA Polymerase?
- Rifampin
(2) ABX that works on Translocase enzyme for
* *Peptide bond formation –> Translocation**?
- Macrolides (23S subunit of 50S)
- Clindamycin (50S)
(1) ABX that works on Peptidyltransferase at 50S Ribosomal subunit enzyme for Attach of AA-tRNA to Ribosome –> Peptide bond formation?
- Chloramphenicol (50S)
(1) ABX that binds to 30S, blocks Initiation Complex Formation –> Attachment of aminoacyl-tRNA to Ribosome?
- Tetracyclines (30S)
(2) ABXs that inhibit Protein synthesis
- -> Initiation of Complex formation?
- Aminoglycosides (30S)
- Linezolid (23S subunit of 50S)
(3) Different ways Bacteria protect themselves from
β-lactam drugs?
-
Inactivation via β-lactamase
- Cleaving C-N ring
- Changes in Drug target through mutation of Binding site
- Transpeptidase changes
- Decreased permeability, and Efflux pumps (G- only)
- Restricting drug entry
SEs of Penicillin?
-
Hypersensitivity
- Urticaria, Pruritus, Fever, Anaphylaxis, Joint swelling
- Rash
-
Hemolytic anemia
- Coombs-positive
Clinical use of Penicillin?
-
Gram-positive Bacteria
- S. pneumoniae
- S. pyogenes
- Actinomyces
-
Fastidious Gram-negative Bacteria
- Neisseria meningitidis
- T. pallidum
-
Gram-positive (Bactericidal)
- Clostridia, Listeria, Bacillus
- Most anaerobes EXCEPT B fragilis group
- Spirochetes: Drug of choice for Syphilis (Penicillin G)
Clinical uses of
Ampicillin and Amoxicillin (Aminopenicillins)?
“HELPS Slaughter Enterococcus”
AmOxicillin is an Oral form of Ampicillin
- Gram-positive (moderate)
- Gram-negative (moderate)
- UTIs
- Neonatal infections (+ Gentamicin)
-
HELPS Slaughter Enterococcus
- Haemophilus influenza, E coli, Listeria,
Proteus mirabilis, Salmonella, Shigella, Enterococcus
- Haemophilus influenza, E coli, Listeria,
- Used w/ Clavulanic acid –> Extends coverage by protecting against β-lactamase
- Gram-negative rods
- H influenzae, E coli, P mirabilis, Salmonella, Shigella
- 2nd Line Tx for Lyme Disease