Lesson 8 - Antimicrobials Flashcards
Chemotherapy
use of drugs to treat diseases
Antimicrobials
any drug used in treating infectious diseases
Antibiotics
substances produced by some microbes that inhibit or kill other microbes
Synthetic drugs
antimicrobial compounds synthesized in the laboratory
Selective Toxicity
An ideal in chemotherapy that an antimicrobial drug kills only pathogenic microbes without harming the host.
Historically, reminiscent of the “magic bullet” of Paul Ehrlich.
He used arsenical compound called “Salvarsan”
Alexander Fleming
discovered Penicillin extracted from Penicillium mold
Gerhard Domagk
discovered sulfanilamides
Selman Waksman
discovered Streptomycin
derived from Streptomyces bacteria
Howard Florey and Ernst Chain
performed first clinical trials of penicillin extracted from Penicillium chryseogenum
How do Penicillins and cephalosporins work?
THey destroy the peptidoglycan layer by disrupting the peptide cross bridges.
Cephalosporins
Derived from Cephalosporium acremonium
Beta lactam antibiotic like penicillin
Main ring different from penicillin
2 sites for R groups
Polypeptide Antibiotics
Bacitracin Topical application Effective against Gram-positives Blocks transport of NAG and NAM from cytoplasm Vancomycin Glycopeptide Important "last line" against antibiotic resistant S. aureus Hinders peptidoglycan elongation
Mycolic Acid Inhibitors
Antimycobacterial antibiotics
Isoniazid (INH)
inhibits mycolic acid synthesis
oral antibiotic
Ethambutol
inhibits incorporation of mycolic acid into cell wall
both are anti-tuberculosis drugs
Inhibition of Cell Wall Synthesis
Most common agents prevent cross-linkage of NAM subunits
Beta-lactams are most prominent in this group
Functional groups are beta-lactam rings
Beta-lactams bind to enzymes that cross-link NAM subunits
Bacteria have weakened cell walls and eventually lyse
Affects actively growing cells only
Inhibition of Protein Synthesis
Prokaryotic ribosomes are 70S (30S and 50S)
Eukaryotic ribosomes are 80S (40S and 60S)
Drugs can selectively target translation
Mitochondria of animals and humans contain 70S ribosomes
Can be harmful