Antimicrobial Drugs Flashcards
Define drugs
Chemicals that affect physiology in any manner
Define chemotherapeutic agents
Drugs that act against diseases
Define antimicrobials
Drugs used for treating infections
What is chemotherapy?
The use of chemicals to selectively kill pathogens while having little or no effect on the patient
Which microbiologist is generally credited with proposing the term chemotherapy?
Paul Ehrlich
What was the name of the chemotherapeutic agent that Paul Ehrilch developed?
Magic bullet - arsenic containing compound
What disease did the ‘magic bullet’ treat?
Syphilis (salvarsan)
Which scientist is credited with reporting the antimicrobial action of penicillin secreted from Penicillium mold?
Alexander Fleming
Explain why Salvarsan and penicillin were not the first antimicrobial drugs to be widely used (2)
- Arsenic compounds are toxic to humans
- Penicillin was not made available in large enough quantities until the 1940s
What was the name of the first practical antimicrobial used to treat a wide array of bacterial infections?
Sulfanilamide
Name the bacteriologist that discovered the sulfanilamide
Gerhard Domagk
Which scientist focused on soil-dwelling bacteria?
Selman Waksman
What was the most notable species of soil-dwelling bacteria discovered by Selman Waksman?
Streptomyces
Define antibiotic
Antimicrobial agents that are produced naturally by an organism
Which scientist originally coined the term “antibiotic”?
Selman Waksman
Chemically altered antibiotics are known as ______
Semi-synthetics
Antimicrobials that are completely synthesized in a laboratory are known as ______
Synthetics
Explain the concept of selective toxicity
An effective microbial agent must be more toxic to a pathogen than to a host
How is selective toxicity possible?
Differences in the structure between the pathogen and host
Why are there far more antibacterial drugs than any other kinds of antimicrobials?
Greatest number and diversity
Why are antiviral drugs especially limited?
They are likely toxic to the host
Name 5 different targets or mechanisms of action by which antimicrobial drugs can be categorized
- Cell wall synthesis
- Cytoplasmic synthesis
- DNA / RNA synthesis
- Protein synthesis
- Metabolism
How are the sugars N-acetylglucosamine (NAG) and N-acetylmuramic acid (NAM) positioned relative to each other?
Cross-linked by short peptide chains extending between NAM subunits
What is the fundamental ‘subunit’ or ‘building block’ of peptidoglycan?
Amino acid sugars and tetrapeptides
______ polymerize NAG - NAM subunits
Transglycosylases
______ cross-link short peptide chains of neighboring NAM molecules
Transpeptidases
What are beta-lactams?
Antimicrobials that prevent cross-linking of NAM subunits
What term is used to refer to beta-lactam functional portions?
Beta-lactam rings
Name 2 examples of beta-lactams
- Penicillin
- Cephalosporin
How do beta-lactams specifically inhibit cell wall synthesis?
By irreversibly binding to transpeptidases
What occurs in the absence of correctly formed peptidoglycan in the inhibition of cell wall synthesis?
Growing bacterial cells are less resistant to the effects of osmotic pressure
What ultimate effect do beta-lactams have upon the bacterial cell - how do they kill?
They create semi-synthetic derivatives
Name an example of a semisynthetic derivative of natural penicillin
MRSA
Name 3 advantages of semisynthetic penicillins over natural penicillin
- More stable
- More readily absorbed
- Less susceptible to deactivation
What cellular target or mechanism of action does the drug vancomycin affect?
Alanine-alanine cross-bridges
Vancomycin inhibits ______
Biosynthesis
What cellular target or mechanism of action does the drug bacitracin affect?
Prevents cell wall formation
How does bacitracin specifically act?
Blocks the transport of NAG and NAM across the cytoplasmic membrane
What is bactoprenol?
Membrane localized carrier molecule
What effect does bacitracin have upon the bacterial cell - how does it kill?
Causes cell lysis due to osmotic pressure
Describe how beta-lactams, vancomycin, and bacitracin have NO effect on existing peptidoglycan
They are effective only on growing, reproducing cells - dormant cells are unaffected
How do aminoglycosides work?
Change the shape of the 30S subunit
Aminoglycosides prevent ______
Reading of mRNA codons
Name an example of an aminoglycoside
Streptomycin
How do tetracyclines work?
Block the tRNA docking site (A site)
Tetracyclines prevent _______
Amino acid binding
How does chloramphenicol work?
Blocks the enzymatic site of the 50S subunit
Chloramphenicol prevents ______
Peptide bond formation
How do macrolides work?
Bind to a different portion of the 50S subunit
Macrolides prevent ______
Translocation
Name an example of a macrolide
Erythromycin
What is translocation?
Movement of the ribosome from one codon to the next
How do antifungal polyenes work?
Disrupt the cytoplasmic membrane
What is ergosterol?
A lipid in fungal membranes
Name the 2 different polyenes
- Nystatin
- Amphotericin B
Nystatin and Amphotericin B are ______ because they attach to ergosterol
Fungicidal
______ is structurally similar to ergosterol
Cholesterol
How do sulfonamides or ‘sulfa drugs’ act as antimetabolite drugs?
They are structural analogs of PABA
What is the function of PABA in normal bacterial biochemistry?
Synthesis of nucleotides required for DNA and RNA synthesis
PABA is enzymatically converted into ______
Dihydrofolic acid
Dihydrofolic acid is enzymatically converted into ______
Tetrahydrofolic acid (THF)
How does sulfanilamide specifically inhibit folic acid synthesis in bacteria? (2)
- Sulfanilamides compete with PABA for the active site
- Folic acid enzyme is deactivated
Why are sulfa drugs safe for humans to use? (2)
- Humans do NOT synthesize THF from PABA
- Human metabolism is unaffected by sulfanilamides
The antimetabolic agent trimethoprim interferes with ______
Nucleic acid synthesis
______ distort the shapes of the nucleic acid molecules
Nucleotide analogs
Viruses are more likely than host cells to incorporate ______
Nucleotide analogs
What is the specific target of the synthetic drugs called quinones or fluoroquinolones?
Prokaryotic DNA
What process do quinones or fluoroquinolones interfere with?
DNA gyrase
What is the role of DNA gyrase?
Coiling and uncoiling of replicating DNA
What is microbial antagonism?
The competition among microbes for nutrients and space
Describe an example of microbial antagonism in normal physiology
Women taking strep throat antibiotics can develop a yeast infection from Candida albicans
What are beta-lactamases or ‘penicillinases’?
Enzymes that break the beta-lactam rings of penicillin