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30 Cards in this Set

  • Front
  • Back

Chemotherapeutic agents

-chemical agents used to treat disease


-destroy pathogenic microbes or inhibit their growth within host


-most are antibiotics

Antibiotics

microbial products or their derivatives that kill susceptible microbes or inhibit their growth

Paul Ehrlich (1904)

-developed concept of selective toxicity


-identified dyes that effectively treated African sleeping sickness

Sahachiro Hato (191)

working with Ehrlich, identified arsenic compounds that effectively treated syphilis

Gerhard Domagk, Jacques, & Therese Trefouel (1935)

discovered sulfonamides and sulfa drugs

Penicillin

-FIRST discovered by Ernest Duchesne (1896) discovery lost


-accidentally discovered by Alexander Fleming 1928


-effectiveness demonstrated by Florey, Chain, and Heatley 1939

Alexander Fleming

-discovered Penicillin


-observed penicillin activity on contaminated plate and did not think it could be developed further

Streptomycin

-antibiotic active against tuberculosis


-discovered by Selman Waksman 1944 (Awarded Nobel Prize in 1952)

Later discoveries by 1953

chloramphenicol, terramycin, neomycin, and tetracyline

selective toxicity

ability of drug to kill or inhibit pathogen while damaging host as little as possible

therapeutic dose

drug level required for clinical treatment

toxic dose

drug level at which drug becomes too toxic for patient (ex. produces side effects)

therapeutic index

ratio of toxic dose to therapeutic dose

broad-spectrum drugs

attack many different pathogens

narrow-spectrum drugs

attack only a few different pathogens

Minimal Inhibitory Concentration (MIC)

lowest concentration of drug that inhibits growth of pathogen

Minimal Lethal Concentration (MLC)

lowest concentration of a drug that kills pathogen

Dilution susceptibility tests

-involves inoculating media containing different concentrations of drug

Disk Diffusion Tests

-disks impregnated with specific drugs are placed on agar plates inoculated with test microbe


-drug diffuses from disk into agar establishing concentration gradient


-observe clear zones (no growth) around disks



Kirby-Bauer method

-standardized method for disk diffusion test


-sensitivity and resistance determine using tables that relate zone diameter to degree of microbial resistance


-table values plotted and used to determine if concentration of drug reached in body will be effective

The E test

-similar to disk diffusion except uses strip rather than disk


-E-test strips contain a gradient of an antibiotic


-intersection of elliptical zone of inhibition with strip indicated MIC

How to determine concentration of drug in blood

microbiological, immunological, chemical, chromatographic, or enzymatic assays

Sulfonamides (sulfa drugs)

-inhibit folic acid synthesis


-broad spectrum

Factors influencing the effectiveness of antimicrobial drugs

-ability of drug to reach site of infection


-susceptibility of pathogen to drug


-ability of drug to reach concentrations in body that exceed MIC of pathogen

Ability of drug to reach site of infection

depends in part on mode of administration (oral, topical, parenteral routes)


-drugs can be excluded by blood clots or necrotic tissue (dead tissue)

Penicillins

most are 6-aminopenicillanic acid derivatives and differ in side chain attached to amino group


-most crucial feature of molecules is the b-lactam ring

b-lactam ring of penicillins

essential for bioactivity


-many penicillin resistant organisms produce b-lactamas (penicllinase) which hydroxlyzes a bond in this ring

Penicillin mode of action

block enzyme that catalyzes transpeptidation, prevents the synthesis of complete cell walls leading to lysis of cell


-acts only on growing bacteria that are synthesizing new peptidoglycan

Cephalosporin

-broad-spectrum antibiotics that can be used by most patients that are allergic to penicillin


-structurally and functionally similar to penicilins

Vancomycin and Teicoplanin

-glcopeptide antibiotics


-inhibit cell wall synthiesis


-vancomycin - important for treatment of antibiotic-resistant staphylococcal and ernterococcal infections