Class Classifications Drug/Examples Mode of Action Specifics/Use/Other
Penicillin G
Natrual Penicillins Gram + Organisms, most anaerobes
Penicillin V
P Methicillin
e (no longer used)
n
i Nafcillin
c Penicillinase-resistant
Primarily gram + infections, especially Staphylococcus aureus
i penicillins
l Oxacillin
l ALL have a B-Lactam Ring = Active Site of the antibiotic
B
i Dicloxacillin
e
n • Bind to & blocks the activity of transpeptidases (aka penicilin binidng proteins) --> preventing the transpeptidatio step in
t
s Aminopenicillins Ampicillin peptidoglycan synthesis Extended Spectrum: many gram - & some gram +
a
(extended spectrum) Amoxicillin • Prevents cross-linking of peptidoglycan layers Sensiitve to B-lactamase
Carbenicillin • Bacteria can develop resistance by producing B-lactamase that cleaves the B-lactam ring Greater gram - spectrum
L Carboxypenicillins
a Ticaricillin Sensitive to B-lactamase
c Highest activity against Pseudomonas
Ureidopenicillin Piperacillin Beta Lactamase Inhibitors: Clavulanic Acid, Sublatam, Tazobactam
t Sensitive to B-lactamase
• Used in combination w/ a B-lactam antibiotic to extend the activity spectrum of the antibiotic
a
• Structural analogs of B-lactams
m Early Generation: Gram +
5 Generations • Function to inhibit the activity of B-lactamase
s Cephalosporins Later Generation: Gram -
Generally more resistant to B-lactamases • Augmentin =Amoxicillin+ Clavulanic Acid
Cell Except 4th: Extended specturm agents
Wall
Syntheis
Imipenem (given in combo w/
Inhibitors
cilastatin)
Generally limited to bacterial infections that are resistant to other drugs
Carbapenems
Broad Spectrum: Many gram +, gram -, and anaerobes
Meropenem Iminepenem:Resistance to B-lactamases
Ertapenem
Narrow Spectrum: mostly aerobic gram - rods
Monobactams Aztreonam
Aztreonam:Resistant to some B-lactamases
Binds to end of the pentapeptide chains (D-Ala D-Ala) on NAM, blocking the transglycosylation & transpeptidation steps of Structural changes in the pentapeptide chain is one way that resistance can
Vancomycin
peptidoglycan synthesis develop
Prevents dephosphorylation of bactoprenol (lipid carrier), preventing assembly & trannsport of the NAG-NAM monomers across the cell
Bacitracin Topical use only due to toxicity
membrane
An analog of phosphoenolpyruvate (PEP)
Fosfomycin
No Lactam
Inhibits MurA, preventing the formation of NAM (N-acetylmuramic acid), an essential precursor molecule for peptidoglycan synthesis
An analog of D-alanine
Cycloserine Inhibits D-alanine-D alanine synthase & alanine racemase
Prevents D-alanine from being incorporated into the pentapeptide on NAM
PolymyxinB
Polymyxin Cationic detergent disrupting membrane structure Poor selective toxicity; topical or opthalmic use only
Polymyxin E (Colistin)
Cell
Membrane
Disruption Dirsupts cell memrbane function by inserting and aggregating in the membrane, causing ion leakage that results in rapid memrane
Resistance is still relatively uncommon
Daptomycin depolarization; inhibits DNA< RNA< and prrotien syntheis
Tetracyclin
Doxycyclin Binds to the 30s subunit to prevent attachment of the aminoacyl-tRNA to the RNA-ribosome complex
Tetracyclins Contraindicated in children w/ developing teeth & pregnant women
• Prevents adding amino acids to the peptide chain, halting protein synthesis
Minocycline
30S Gentamicin
Irreversibly bind to the 30s subunit to block the initiation complex, cause misreading & premature release of mRNA from the
Tobramycin
ribosome
Aminoglycosides Streptamycin Treatment of severe infections caused by aerobic gram-negative bacilli
Amikacin • Halts protein synthesis
Neomycin
Binds to the 50S subunit --> Inhibiting peptidyl transferease
Chloramphenicol Assocated w/ causing aplastic anemia and other serious blood disorders
• Prevents elongation of the peptide chain, halting protein synthesis
Erythromycin
Protein Binds to the 50S subunit, blocking formation of the initiation complex & translocation
Synthesis Macrolides Clarithromycin Used in patients allergic to penicillins
Inhibitors Azithromycin • Prevents elongation and causes premature detachment of incomplete polypeptide chains, disrupting protein syntheis
Clindamycin Binds to the 50S subunit
Lincosamides • Has a similar mechanism of action as macrolides
50s Lincomycin • Disrupts protein synthesis
Quinupristin Binds to different sites on the 50S ribosomal subunit Separately: streptogramins A and B are bacteriostatic
Streptogramins
• Inhibition of protein synthesis at different steps Combination: Bactericidal
Dalfopristin
Linezolid
Binds to the P Site of the 50S ribosomal subunit
Oxazolidinones Limited to organisms resistant to other antibiotics
• Prevents formation of the larger ribosomal complex
Tedizolid
Sulfisoxazole
Sulfonamides: analogues of PABA; competitive inhibitors of dihydropteroate
Sulfonalimides
Sulfamethoxazole synthetase
Interferes w/ folic acid synthesis (needed for DNA synthesis)
Trimethoprim: analogue of the pteridine portion of dihydrofolic acid; inhibits
Trimethorpim enzyme dihydrofolate reductase
• Mainly used for UTIs
Antimetabolites
Individually Bacteriostatic
Bactrim Sulfamethoxazole+ Trimethoprim
Bactrim: Synergistic in combination
Prodrug that is activated by bacterial enzyme KatG (catalase-peroxidase enzyme)
Isoniazid Treatment of TB
(INH/Isonicotinylhydrazide) Active INH inhibits fatty acid synthase that interferes w/ synthesis of mycolic acids
Ciprofloxacin
Norfloxacin
Qunolones/Florquinolones Bind to & inhibit DNA gyrase (topoisomerase II) & topoisomerase IV, preventing bacterial DNA from unwinding and duplicaitng Genitourinary and respiratory infections
Levofloxacin
Moxiflocaxin
Nucelic Rifampicin (Rifampin) Inhibits DNA-dependent RNA polymerase
Acid Rifamycins Rifabutin
Synthesis Rifapentine • Prevents transcription of messenger RNA (mRNA)
Inhibitors
Pro drug
• Reduction of the nitro group of metronidazole creates the active drug that covalently binds DNA --> causing DNA breaks
Metronidazole
• Inhibits nucelic acid synthesis
