Antibacterial Agents
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Created by:
sstrauss0820 on July 2, 2012
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35 terms
Terms | Definitions |
|---|---|
Red azo dye protosil | Era of systemic antibacterial chemotherapyProtected mice against systemic streptococcal infection and cured patients suffering from the disease. Protosil is cleaved, releasing p-aminobenzene sulfonamide which has antibacterial activity. |
Effective chemotherapy drugs must: | Enter the cellBind physically to a cellular structure involved in some process essential for the growth of the cell Inhibit the process in which that cell structure is involved |
Chemotherapy | The treatment of infectious diseases with chemicals or antibiotics that are inhibitory or lethal of the infecting agents. |
Selective Toxicity | The property of some antimicrobial agents to be toxic for a microorganism and nontoxic for the host. |
Antibiotic | A low-molecular-weight chemical agent produced by one organism that is harmful to other organisms. |
Antibacterial Spectrum | Range of activity of an antibacterial agent. |
Broad-Spectrum | Drug can inhibit a wide variety of gram-positive and gram-negative bacteria. |
Narrow-Spectrum | Drug is active only against a limited variety of bacteria. |
Antimicrobial drugs are either: | Bactericidal and Bacteriostatic |
Bactericidal | Drug kills the bacterial cell. |
Bacteriostatic | Drug prevents the growth of microorganisms. Must be used for a sufficient time to allow host's own defenses, such as phagocytosis and antibodies, to destroy the organisms. |
Modes of Action of Antibacterial Agents | Folic Acid synthesisDNA replication RNA synthesis Membrane disruption Protein synthesis (50S and 30S) Peptidoglycan Synthesis |
Cell Wall acting antibacterial agents | interfere with the synthesis of peptidoglycaninhibit transpeptidation Ultimately undergoes osmotic lysis |
Degradation of peptidoglycan occurs during which event: | Binary Fission; inhibition of peptidoglycan affects the daughter cells. |
Antibiotics that bind to receptors on 30S | block the binding of fmet-tRNA to the ribosomePrevent attachment of tRNA to acceptor sites Cause misreading of codons on mRNA lead to the formation of non-functional proteins |
Antibiotics that bind to receptors on 50S | Chloramphenicol blocks the action of peptidyl transferaseErythromycin blocks the translocation step |
Alteration of Cell Membranes | Especially polypeptide antibiotics, incorporate themselves into and alter bacterial cell membranes. Results in loss of important metabolites from the bacterial cell and cell death. |
Inhibition of Nucleic Acid Synthesis | Antibiotics can interfere with DNA replication and RNA transcription in bacterial cells. Mammalian DNA and RNA can be affected as well, thus limiting the use of these drugs. Inhibit bacterial DNA gyrases or topoisomerases |
Sulfonamides | antimetabolites that compete with p-aminobenzoic acid (PABA), which is the substrate for enzymatic reaction leading to synthesis of folic acid.DO NOT INTERFERE WITH MAMMALIAN CELL METABOLISM-no folic acid synthsis |
Folic Acid | Synthesized by p-aminobenzoic acid (PABA)Vitamin the functions as a coenzyme for the synthesis of the purine and pyrimidine bases of nucleic acids |
Nongenetic origin of drug resistance | loss of specific target structuresactive replication of bacteria is required |
Genetic Origin of Drug Resistance | Chromosomal resistanceResistant factor plasmid |
Chromosomal Resistance | alteration of the structure of the receptor of the drugpermeability of the drug |
Resistant factor plasmid | may carry genes for resistance to one and often several antimicrobial drugs and heavy metals.encode enzymes that degrade the drug or modify the drug Plasmid encoded proteins can pump (efflux) the drug out of the bacterial cell. |
Mechanisms of drug resistance | Bacterium may develop and altered metabolic pathway Altered structural target for the drug Production of an enzyme that destroys the drug A microbe may change its permeability to the drug Bacterium may be able to pump (efflux) out any antibiotic entering the cell Bacterium may develop an altered enzyme that still can perform its metabolic function but is less affected |
Antibiotic Sensitivity Tests | In vitro; valuable for selecting chemotherapeutic agents active against the infecting organism.Simply a measurement of the effect of the antimicrobial agent against the organism |
Selection of a drug and patients outcome are influenced by: | pharmacokinetic properties of the drugdrug toxicities site of infection patients general medical status |
Interferes with the synthesis of peptidoglycan | VancomycinBacitracin |
Inhibit transpeptidation | B-lactams: penicillins, cephalosporins, carbapenems |
EX: Antibiotics that bind to 30S | Aminoglycosides: streptomycin, kanamycin, gentmycin; tetracyclines |
EX: antibiotics that bind to 50S | ClindamycinLinezolid |
Ex: cell membrane alteration | Polymyxins, daptomycin, ketoconazole, polyenes |
DNA replication inhibition examples | QuinolonesMetronidazole |
RNA synthesis inhibition examples | Rifampin |
Antimetabolite Examples | SulfamethoxazoleDapsone Trimthoprim |
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