Term 1 of 106
How do lipopeptides function as antibiotics?
Lipopeptides are characterized by a peptide ring attached to a fatty acid side chain. The
fatty acid side chain is what is responsible for the antimicrobial function. The 2,4-
diaminobutyrate is protonated at physiological pH which gives the molecule a strong
positive charge. The positive charge then interacts with the negative charge of LPS,
specifically with the lipid A portion. This disrupts the outer membrane of gram negative
bacteria. From there the antibiotic can disrupt the inner membrane.
Sulfanilamide is a drug that mimics para-aminobenzoate and inhibits the function of
dihydropteroate synthase. Dihydropteroate synthase is used to produce
dihydropteroate from para-aminobenzoate. Dihydropteroate is then used to create
dihydrofolate.
Oxazolidinones bind to the 50s ribosomal subunit and inhibit the initiation complex.
Aminoglycosides bind to the 30s ribosomal subunit and cause the inhibition of tRNA
translocation from the A to the P site which will cause misreading of the mRNA. This will
cause defects in the proteins and lead to cell death.
,Term 2 of 106
What factors contribute to AMR in healthcare?
- Enhanced development of resistance to antibiotics
- Transmission of resistant bacteria to humans
- Contamination of the environment by air particles that carry antibiotics, resistance
genes, and bacteria
- Emergence of novel antibiotic resistance mechanisms
Sulfanilamide is a drug that mimics para-aminobenzoate and inhibits the function of
dihydropteroate synthase. Dihydropteroate synthase is used to produce
dihydropteroate from para-aminobenzoate. Dihydropteroate is then used to create
dihydrofolate.
Isoniazid is a prodrug that is activated by Mtb catalase peroxidase. The active form of
the drug inactivates acyl carrier protein reductase when is important for the synthesis of
mycolic acid in Mtb.
1. antibiotic usage (underuse/use/overuse)
2. lack of antibiotics
3. poor sanitation and personal hygiene
4. use of antibiotics is agriculture
5. inadequate infection controls in health care facilities
Term 3 of 106
What are the general features of Cephalosporins?
There are two distinct differences in carbapenems: there is a sulfur to carbon
substitution at the thiazolidine ring and there is also a double bond between the c2 and
c3 carbons in the 5 member ring.
Together they worked to identify a Penicillium strain that is most effective at making
penicillin. The most suitable mold strain was isolated from a cantaloupe bought on a
market in Peoria, Illinois.
Clavams mimic beta-lactam antibiotics so they can saturate beta-lactamases. Clavams
are used to enhance the ability of other beta-lactams.
Cephalosporins are more effective because they are less likely to be degraded by
penicillinases. They are also characterized by a 6 member ring attached to the beta-
lactam ring as opposed to penicillin which has a 5 member ring attached to the Beta-
lactam ring.
,Term 4 of 106
What is the proposed mechanism of action for daptomycin?
Daptomycin is believed to oligomerize inside of the bacteria membrane and affect
membrane curvature.
Daptomycin enhances the activity of other antibiotics by blocking efflux pumps.
-mycin means the drug is derived from Streptomyces and -micin means the drug is
derived from Micromonospora.
Daptomycin inhibits the synthesis of nucleic acids in bacterial cells.
Term 5 of 106
The structure of Cycloserine
, Term 6 of 106
How does tetracycline work as an antibiotic?
Sulfanilamide is a drug that mimics para-aminobenzoate and inhibits the function of
dihydropteroate synthase. Dihydropteroate synthase is used to produce
dihydropteroate from para-aminobenzoate. Dihydropteroate is then used to create
dihydrofolate.
Bacitracin was found to bind to C55PP and inhibits the dephosphorylation of C55PP. This
means that the flippase cannot cross back from the periplasm across the membrane and
into the cytoplasm. This means that the cell wall cannot continue to grow leading to cell
death.
Tetracyclines bind to the 30s subunit of the ribosomal RNA and this binding overlaps the
aminoacyl-tRNA binding site. By preventing the tRNA from binding to the ribosome the
proteins cannot be made this killing the bacteria
Rifampin binds to the RNA polymerase and prevents RNA synthesis. Rifampin binds
directly in the path of the elongating RNA molecule and sterically blocks the elongating
RNA molecule.
Term 7 of 106
What are the 5 penicillin derivatives?
Penicillin G, Penicillin V, Ampicillin, Amoxicillin, and Methicillin
Penicillin A, Penicillin B, Penicillin C, Penicillin D, and Penicillin E
Penicillin X, Penicillin Y, Penicillin Z, Penicillin W, and Penicillin Q
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