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56 Cards in this Set
- Front
- Back
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chemical substances used for therapeutic purposes
-implies chemical synthesized or modified by chemists -drugs that kills the diease |
Chemotherapeutic Agents
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metabolic products of microorganism
"against life" |
Antibiotics
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_______ envisioned "magic bullets" that seek out and destroy disease organisms.
-arsenic-phenol compound to control ________. -Found Arsphenamine given common name Salvarsan |
Paul Ehrlich
syphilis |
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________ found red dye, called what? Had an inhitory effect on staphylococci, streptococci and other Gram-positives
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Gerhard Domagk
Prontosil |
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In 1935, Jacques and Therese Trefouel group at the Pasteur Institute found the active substance within prontosil was __________.
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Sulfanilamide
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Competititive inhibitor of the synthesis of an essential metabolites --folic acid
-blocks enzyme properties |
Sulfanilamide
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Sulfanilamide looks similar to _________.
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Para-aminobenzoic acid (PABA)
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What were modern sulfonamides prescribed for?
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Gram-positive bacteria
Gram-negative urinary tract infections |
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Sulfamethoxazole + Trimethoprim (inhibitors of another step in folic acid synthesis)
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Bactrim
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Sulfisoxazole acetyl--found in creams for vaginal infections
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Gentrism
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inhibits cell wall synthesis in Mycobacterium species by inhibiting the production of mycolic acid
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Isoniazid
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DNA gyrase inhibitor blocks DNA replication
ex. Fluoroquinolnes (used in urinary tract infection) **Ciprofloxacin (Cipro) is this kind of drug |
Nalidixic acid
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effective in treating urogenital infection because it is actively excreted in the urine
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Nitrofurantoin
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What do quine, chloroquine, primaquine do?
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destroy malaria parasites
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What was the 1st antibodic discovered by Alexander Fleming?
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Penicillin
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Penicillin species that produces a substance that kills Gram-______ organisms (Staphylococci)
_________: purified, clinically tested and developed the techinques for the large-scale production of penicillin. |
Positive
Florey and Chain |
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key Beta-lactam nucleus
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Penicillin
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inhibits enzymes that make peptide cross-links in the peptidoglycan
-very effective against gram positives (Stap, Strep, clostridia, pneumococci) -at higher concentration effective against gram negative (Gonorrhea, syphilis) |
Penicillin
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Penicillin resistant bacteria produce an enzyme called _____________ (beta-lactamase) converts penicillin to penicilloic acid.
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Penicillinase
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works better against Gram-negatives than penicillin G
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Ampicillin
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acid-stable and does not bind to food
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Amoxicillin
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increased stability, good for urinary tract infection
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Carbenicillin
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What are the semisynthetic Penicillins?
-used to treat urinary tract |
1. Ampicillin
2. Amoxicillin 3. Carbenicillin |
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resemble penicillin in chemical structure
-Beta-lactam nucleus has slightly different composition |
Cephalosporins
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First cephalosporin C from fungus=Cephalosporium
What generation is this? *Works good and gram positive G+ and some G- rods -Cephalexin (_____) -Cephalothin (____) |
1st generation
-Cephalexin (Keflex) -Cephalothin (Keflin) |
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G+ and numerous G- (like H. influenzae)
-working on gram negative --Cefaclor, cefoxitin, cefuroxime |
2nd generation
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primarily against gram-negative rods* especially Pseudomonas aeruginosa
-Cefotaxime (Claforan) -Ceftriaxone (Rocephin) -Ceftazidime (Fortz) |
3rd generation
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Has greatest activity in Gram negatives
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4th generation
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group of antibiotics in which an amino group is bonded to carbohydrate molecules (glycosides) that are bonded to other carbohydrate molecules
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Aminoglycosides
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discovered by Selman A. Walksman; he found streptomycin from moldlike bacterium Streptomyces griseus
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Aminoglycosides
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Gentamicin
Kanamycin Neomycin What are these examples of? |
Aminoglycosides
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-bacteriocidal
-inhibition of protein synthesis: drug changes shape of 30S ribosomal subunit and causes code on mRNA to be read incorrectly Spectrum: kills BOTH gram - and + including Mycobacterium Considered ________ antibiotic |
Aminoglycosides
-Broad-spectrum |
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binds ribosomes and changes shape, puts in wrong codon
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Aminoglycosides
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first broad-spectrum antibiotic discovered
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Chloramphenicol
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-Inhibits gram positive and gram negative as well as rickettsiae and some fungi
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Chloramphenicol
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Isolated from Streptomyces venezuelae by John Ehrlich, Paul Burkholder, and David Gotlieb
-first synthetic antibiotic |
Chloramphenicol
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What is the mode of action of Chloramphenicol?
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Bacteriostatic, binds to the 50S ribosome particle and inhibits peptide bond formation
-small size promotes its diffusion into areas of the body that are normally inaccessible to drugs |
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affects protein synthesis by binding to ribosome and affecting peptide bond
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Chloramphenicol
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Chloramphenicol side effect:
suprression of bone marrow activity, prevents hemoglobin incorporation into RBCs. Induces condition |
Aplastic Anemia
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Chloramphenicol side effect:
Chloramphenicol accumulates in the blood of newborns which can lead to a breakdown of their cardiovascular system |
Gray Syndrome
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group of closely related broad-spectrum antibiotics
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Tetracyclines
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Bacteriostatic-inhibition of protein synthesis
-interferes w/attachment of tRNA to mRNA-ribosome complex -binds to ribosomes by blocking tRNA site (stops protein synthesis) |
Tetracyclines
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-often supress the normal intestinal microbiota causing gastrointestinal upsets and the flourishing of fungi such as Candida albicans
-in children it causes yellow-gray-brown discoloration of teeth and stunts bone growth -NOT given to pregant women |
Tetracyclines
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kills normal flora in intestines, harms gastrointestines
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Tetracyclines
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Prevents translocation; member of the group of antibiotics called MACROLIDES
-protein synthesis inhibitor, binds to 50S portion of ribosome and prevents translocation*--movement of mRNA through ribosome |
Erythomycin
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effective in treating atypical pneumonia, Legionnaires' disease, Neisseria, Chlamydia and gram positive bacterial in patients with penicillin allergy
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Erythomycin
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product of Streptomyces species
-inhibitor of cell wall synthesis gram positive bacteria (inactive against gram-negative bacteria) -last line of defense against multi-drug resistant Staphlococci |
Vancomycin
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inhibits cell wall synthesis of GRAM POSITIVES**
-last antibotic that can kill Staphlococci |
Vancomycin
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semisynthetic drug; used in treatment of tuberculosis and leprosy
-also in treatment of meningitis caused by Neisseria and Haemophilus -Mode of action: inhibition of RNA synthesis (Bacteriostatic) |
Rifampin
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inhibits RNA synthesis--binds to RNA polymerase--can kill bacteria in brain barrier
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Rifampin
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Neosporin tropical cream has _____, _______, and _________.
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1. Neomycin
2. Bacitracin 3. Polymyxin B |
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inhibits cell wall formation
-active against gram POSITIVES like staphylococci |
Bacitracin
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damages bacterial membranes; active againts gram-NEGATIVES like Pseudomonas aeruginosa
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Polymyxin B
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Bacitracin and Polymyxin B are from what species?
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Bacillus
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Antibiotic misuse and abuse
1. 2. 3. |
1. Society
2. Hospitals--MRSA and VRSA 3. Livestock feeds |
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What are the four mechanisms of antibiotic resistance?
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1. Altered metabolic pathways
2. Antibiotic inactivation 3. Reduced permeability/active export 4. Target modification |
