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Microbiology Chapter 12 - drugs, microbes, host - the elements of chemotherapy
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antibiotic producing microbes include =
Streptomyces, Bacillus, Penicillium, and Cephalosporium
destabilize the formation of the cell wall causing bacterial cells to lyse; inhibits transpeptidase - activity of which drug?
penicillin
vancomycin and bacitracin are what type of drug with what mode of action?
non beta-lactam cell wall inhibitors
interact with phospholipids of the outer membrane- serious side effects; particularly affects gram negative - activity of what drug?
polymixin
aminoglycosides examples
streptomycin and gentamicin
are metabolic analogs of PABA and block folic acid synthesis =
sulfonamides
nitrogenous base + sugar =
nucleoside
disrupt DNA and RNA replication and cause point mutations
nucleotide analogs
enzyme that digests or breaks down protein
protease
drug that treats AIDS by blocking the production of protease, a proteolytic enzyme that helps create new viral pieces for HIV
protease inhibitor
proteins (cytokines) secreted by T cells and other cells to aid and regulate the immune response; second line of defense
interferons
helps release virions from the host cell after replication and assembly
neuraminidase
telitromycin (Ketek), new drug with different ring structure from Erythromycin; used for infection when resistant to macrolides
ketolides
linezolid (Zyvox); synthetic antimicrobial that blocks the interaction of mRNA and ribosome
Used to treat methicillin resistant Staphylococcus aureus (MRSA) and vancomycin resistant Enterococcus (VRE)
Oxazolidinones
common metabolic products of aerobic bacteria and fungi that inhibit other microbes
antibiotics
antibiotics can inhibit and/or kill bacteria in the genera _____ and _____
streptomyces, bacillus
antibiotics can inhibit and/or kill mold in the genera _____ and _____
penicillium, cephalosporium
drugs that inhibit or kill microbial cells without simultaneously damaging host tissues are described as =
selectively toxic
cell wall inhibitors, cell membrane, DNA/RNA, protein synthesis inhibitors acting on ribosomes, and metabolic pathways and products are all examples of drug _____
mechanism of action
decrease in the prevalence of infectious disease is the direct effect of _____
antibiotics
a drug’s _____ is its range of activity
spectrum
drugs that are effective on a small range of microbes are described as =
narrow-spectrum
_____ drugs target a specific cell component that is found only in certain microbes =
narrow-spectrum
drugs that are effective on a large range of microbes are described as =
broad-spectrum
_____ drugs target cell components common to most pathogens (ribosomes)
broad-spectrum
_____ and _____ block synthesis of peptidoglycan, causing the cell wall to lyse
penicillins, cephalosporins
penicillins and cephalosporins block synthesis of _____, causing the cell wall to luse
peptidoglycan
penicillins that do not penetrate the outer membrane are less effective against _____ bacteria
gram-negative
broad spectrum penicillins and cephalosporins can cross the cell walls of _____ bacteria
gram-negative
beta-lactam antimicrobials primary mode of action is =
interfere with cell wall synthesis
_____ antimicrobials primary mode of action is to interfere with cell wall synthesis
beta-lactam
greater than half of all antimicrobial drugs are _____
beta-lactam
_____ _____ _____ of all antimicrobial drugs are beta-lactams
greater than half
the most prominent beta-lactams are _____ and _____
penicillins, cephalosporins
the most prominent _____ are penicillins and cephalosporins
beta-lactams
enzyme that inactivates penicillins
penicillinase
all penicillins consist of 3 structurally similar parts: _____, _____, _____
thiazolidine ring, beta-lactam ring, variable side chain
cephalosporins account for _____ of all antibiotics administered
one third
_____ account for one third of all antibiotics administered
cephalosporins
cephalosporins have a synthetically altered _____ structure
beta-lactam
_____ are relatively broad-spectrum, resistant to most penicillinases, and cause fewer allergic reactions
cephalosporins
4 generations of _____ exist, each more effective against gram-negatives than the one before, with improvised dosing and fewer side effects
cephalosporins
_____ generations of cephalosporins exist, each more effective against _____ than the one before, with improvised dosing and fewer side effects
4, gram-negatives
first generation of cephalosporins is most effective against =
gram-positive cocci, few gram-negative
Second generation of cephalosporins is most effective against =
gram-negative bacteria
Third generation of cephalosporins is most effective against =
enteric bacteria with beta-lactamases
Fourth generation of cephalosporins is most effective against =
widest range, gram-negative and gram positive
vancomycin is _____, most effective against _____, is _____ and _____ to administer
broad-spectrum, staphylococci, toxic, hard
_____ is broad-spectrum, most effective against staphylococci, is toxic and hard to administer
vancomycin
_____ is narrow-spectrum, produced by a strain of bacillus subtilis, used topically in ointment
bacitracin
bacitracin is _____, produced by a strain of _____ _____, and is used _____ _____ _____
narrow-spectrum, bacillus subtilis, topically in ointment
polymyxin mode of action
cell membrane
polymyxins interact with _____ and cause _____ particularly in _____ bacteria
phospholipids, leakage, gram-negative
_____ interact with phospholipids and cause leakage, particularly in gram-negative bacteria
polymyxins
amphotericin B and nystatin form _____ _____ _____ on _____ membranes, which cause _____
complexes with sterols, fungal, leakage
_____ and _____ form complexes with sterols on fungal membranes, which cause leakage
amphotericin B, nystatin
amphotericin B and nystatin mode of action
cell membrane
drugs that block protein synthesis can also damage the _____ _____
eukaryotic mitochondria
drugs that block _____ could also damage the eukaryotic mitochondria
protein synthesis
_____ cause misreading of mRNA by changing the A-site conformation, blocking protein synthesis
aminoglycosides
aminoglycosides cause misreading of _____ by changing the _____ _____, blocking protein synthesis
mRNA, A-site conformation
aminoglycoside mode of action
protein synthesis
_____ block attachment of tRNA on the A acceptor site and stop further protein synthesis
tetracyclines
tetracyclines block _____ _____ _____ on the _____ _____ _____ and stop further _____ _____
attachment of tRNA, A acceptor site, protein synthesis
tetracycline mode of action
protein synthesis
STDs, rocky mountain spotted fever, lyme disease, typhus, acne, and eukaryotic parasites are all conditions/microbes that can be treated with which antimicrobial drug?
tetracycline
tetracycline spectrum =
broad, gram-positive and gram-negative
drugs that block metabolic pathways by competing with normal substrate for enzyme’s active site =
competitive inhibition
drugs that block metabolic pathways by having a more powerful effect in combination with each other than the sum of the effects of the individual drugs
synergistic effect
sulfonamides and trimethoprim mode of action
block metabolic pathways
sulfonamides and trimethoprim spectrum
narrow-spectrum
shigellosis, UTI, protozoan infections, burns, eye infections, PCP are all conditions/microbes that cam be treated with what drug(s)?
sulfonamides and trimethoprim (metabolic pathway inhibitors)
drugs that affect nucleic acid synthesis may block synthesis of _____, inhibit _____, or stop _____
nucleotides, replication, translation
antibacterials, antivirals, and antiprotozoan drugs are examples of drugs that affect _____ _____ synthesis
nucleic acid
chloroquine binds and cross-links the _____ _____ to treat _____ infections
double helix, malaria
_____ binds and cross-links the double helix to treat malaria infections
chloroquine
quinolones do what
inhibit DNA helicases
quinolones mode of action
nucleic acid synthesis
chloroquine mode of action
nucleic acid synthesis
one complication of antiviral chemotherapeutic agents is that _____ _____ is almost impossible due to the fact that viruses are obligate intracellular parasites
selective toxicity
why can’t antiviral chemotherapeutic agents be selectively toxic?
viruses are obligate intracellular parasites
actions of what type of drug include blocking penetration into host cell, blocking replication, transcription, or translation of viral genetic material via nucleotide analogs, inhibit proteases, and prevent maturation of viral particles?
antiviral chemotherapeutic agents
many _____ _____ mimic the structure of nucleotides and compete for sites on replicating DNA
antiviral agents
many antiviral agents mimic the structure of _____ and compete for sites on _____ _____
nucleotides, replicating DNA
acyclovir is an example of what
antiviral agent
_____ is the first drug aimed at treating AIDS, and is a thymine analog
Azidothymidine (AZT)
Azidothymidine (AZT) is the first drug aimed at treating _____, and is a _____ _____
AIDS, thymine analog
drugs that are human-based glycoproteins produced primarily by the second line of immune defense - made my fibroblasts and leukocytes =
interferons (IFN)
therapeutic benefits of _____ include: reduced healing time, reduced complications of some infections, prevents or reduces symptoms of cold and papillomavirus, slows progression of certain cancers, leukemias, and lymphomas, treats hepatitis C, genital warts, and kaposi’s sarcoma
interferons (IFN)
amantadine, rimantadine, relenza, and tamiflu are drugs used to treat _____
influenza
amantadine and rimantadine are restricted almost exclusively to _____ infections, and prevent _____
influenza A, fusion of virus with cell membrane
_____ and _____ are restricted almost exclusively to influenza A infections, and prevent fusion of virus with cell membrane
amantadine, rimantadine
relenza and tamiflu are _____ _____ drugs which block _____ in influenza A and B
broad-spectrum, neuraminidase
_____ and _____ are broad-spectrum drugs which block neuraminidase in influenza A and B
relenza, tamiflu
ketolides and oxazolidinones are newly developed _____ _____ _____
classes of antimicrobials
ketolides are most effective against gram-_____ infections in the _____ _____
positive, respiratory tract
_____ are most effective against gram-positive infections in the respiratory tract
ketolides
_____ are synthetic, broad-spectrum antimicrobials that block the interaction of mRNA and ribosome
oxazolidinones
oxazolidinones are synthetic, _____ _____ antimicrobials that block the interaction of _____ and _____
broad-spectrum, mRNA, ribosome