Chapter 20 - Antimicrobial Drugs Flashcards
Antibiotic
-a substance produced by microorganisms that in small amounts inhibits other microorganisms
Antibiotic Resistance
-formerly effective medications have less and less impact on bacteria
Narrow Spectrum of Microbial Activity
-a small range of different microbial types they affect
Broad-Spectrum Antibiotics
-have a wide range of bacteria they affect
Hydrophilic Drugs
-drugs that pass through the porin channels
-relatively small
Lipophilic Drugs
-larger
-don’t enter gram negative bacteria readily
Bactericidal
-kill microbes directly
Bacteriostatic
-prevent microbes from growing
-hosts own defences destroy the microorganism
Cell Wall Synthesis Inhibition
-bacterial cell walls have peptidoglycan
-synthesis of PG is inhibited
-cell wall is weakened and undergoes lysis
-only growing cells are affected
-ie. penicillin
Protein Synthesis Inhibition
-difference in ribosomal structure accounts for selective toxicity
-ie. chloramphenicol
Eukaryotic Cell Ribosomes
-80S
-However, mitochondria have 70S ribosomes and hence host cells may be affected
Prokaryotic Cell Ribosomes
-have 70S ribosomes
Plasma Membrane Injury
-changes in membrane permeability
-results in loss of important metabolites from the cell
Nucleic Acid Synthesis Inhibition
-interfere with DNA replication and transcription
-block bacteria RNA polymerase
Essential Metabolite Synthesis Inhibition
-competitive inhibition by a substance that closely resembles the enzyme
-ie. PABA
What part of the cell does penicillin affect?
cell wall
How do penicillin and cephalosporins act?
-they inhibit polypeptide bonds
-cause osmotic lysis
What two drugs interact with the cell wall?
penicillin and cephalosporins
What common core structure do penicillins have?
-a nucleus containing a β-lactam ring
Does penicillin affect more gram+ or gram- bacteria?
gram-positive
Which prototype do we get all penicillin species from?
-Penicillin G (natural penicillin)
Penicillin G has a ________ spectrum
narrow
Penicillin G is often the drug of choice against most _______, _______, and _______.
staphylococci, streptococci, and several spirochetes
What is a problem with penicillin G?
it has to be injected
Why can’t penicillin G be given orally?
it will be dissolved by stomach acids
Penicillin V is given…
-orally; stable in stomach acids
Penicillinase: β-lactamases
-enzymes produced by many bacteria that cleave the β-lactam ring
Which species mostly produces β-lactamase?
Staphylococcus aureus
Why were semi-synthetic penicillins developed?
in attempt to overcome disadvantages of natural penicillin
What organism is resistant to methicillin?
Methicillin-resistant Staphylococcus aureus (MRSA)
Advantage of Oxacillin
-resistant to penicillinase
Disadvantage of Oxacillin
has a narrow spectrum (gram+ only)
What are the two aminopenicillins?
ampicillin and amoxicillin
What is the advantage of ampicillin?
it has a broad spectrum of many gram- bacteria
What are the 2 main adverse effects of penicillin?
allergies and resisitance
How do cephalosporins attack?
-inhibit cell wall synthesis
Advantage of cephalosporins over penicillin?
-they are resistant to enzymes
What is the limiting factor of cephalosporins?
they are expensive because they are extracted from nature
What are cephalosporins often used to treat?
meningitis (treated by 3rd gen.)
What are cephalosporin generations?
-the semi-forms, not names
Each generation of cephalosporin has an ______ spectrum?
-increased
-ie. 5th gen is better than the 1st
What are the adverse effects of cephalosporins?
-mild GI tract symptoms (nausea, extreme vomiting)
What does chloramphenicol inhibit?
-protein synthesis
-inhibit the formation of peptide bonds (dehydration synthesis) in the polypeptide chain
How does chloramphenicol shut off protein synthesis?
-attaches to the 50S portion of the 70S prokaryotic ribosomes
What is an advantage of chloramphenicol?
-they are less expensive and have a simple structure that can be prepared in the lab
Chloramphenicol has a __________ spectrum.
broad
Chloramphenicol has a ________ size so it can…
-small size
-it can diffuse into areas of the body that are inaccessible to other drugs
Chloramphenicol can penetrate the ____
Blood brain barrier