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180 Cards in this Set
- Front
- Back
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What is a chemical selective destruction of invading organisms?
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Chemotherapy
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What is the ratio of toxic dose/effective dose?
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Therapeutic Index
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What type of chemotherapy stems from the concept that substances derived from one living thing may serve to kill other living things?
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Antibiotic Chemotherapy
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What drug was discovered in 1936 and began the modern era of chemotherapy?
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Sulfanilamide
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How are chemotherapeutic agents classified?
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According to their Mechanism of Action
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What type of chemotherapeutic agents inhibit bacterial cell wall synthesis?
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Penicillin
Cephalosporins Vancomycin Bacitracin Cycloserine |
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What type of chemotherapeutic agents act directly on the cell membrane?
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Polyeene Antifungal Agents:
Nystatin Amphotericin B |
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What types of antibacterial agents affect the function of bacterial ribosomes to inhibit protein synthesis, and are bacteriostatic?
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Chloramphenicol
Tetracyclines |
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What types of antibacterial agents affect the function of bacterial ribosomes to inhibit protein synthesis, and are bacteriocidal?
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Streptomycin
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What types of chemotherapeutic agents affect nucleic acid metabolism?
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Rifampin (DNA dependent RNA polymerase)
Fluoroquinolones - Ciprofloxacin |
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What types of chemotherapeutic agents block metabolic steps essential to a microorganism?
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<u>Antimetabolites</u>:
Sulfonamides Trimethoprin |
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What chemotherapeutic agent can be either bacteriocidal or bacteriostatic depending on the environment?
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Sulfonamides
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What generally happens when you combine two bacteriostatic agents?
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Produce an Additive effect
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What generally happens when you combine 1 bacteriocidal and 1 bacteriostatic agent?
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Generally results in antagonism
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What generally happens when you add two bacteriocidal agents?
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Generally results in a synergistic effect.
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When is a microorganism said to be resistant?
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When the concentration of the drug required to weaken or kill the microorganism is greater than can be tolerated by the host.
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What type of resistance occurs in the absence of selective pressure?
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De Novo (Intrinsic) Resistance
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What are six mechanisms of resistance from chemotherapeutic agents?
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1) Absence of Target (Ergosterol's absent)
2) Alterations in Target (Pen. Binding Protein Alterations) 3) Low concentration at target (Interference with membrane passage) 4) Lack of metabolic activation (Antifungal Flucytosine -> Fluorouracil) 5) Inactivation (Penicillinases) 6) Escape from Effect (Alternate Metabolic Pathways) |
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What condition must be considered when prescribing sulfonamides and chloramphenicol?
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Glucose-6-Phosphate Dehydrogenase Deficiency (May produce Hemolysis)
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What antibiotic produces hearing loss in newborn when taken during pregnancy?
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Streptomycin
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What log cell kill is required to cure microbial infections?
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2 (99% of population is killed)
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What was the first effective chemotherapeutic agent employed systemically?
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Sulfonamides
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What types of bacteria do sulfonamides target?
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Broad-Spectrum - Gram + and Gram -
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What is the mechanism of action of sulfonamides?
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They are structural analogs and competitive antagonists of PABA (Para-Aminobenzoic Acid)
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What are sulfonamides often used in combination with?
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Trimethoprin
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How do sulfonamides not interfere with host metabolism?
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Mammalian cells use preformed folic acid.
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Which drug inhibits dihydrofolate reductase and prevents the transformation of dihydrofolate to tetrahydrofolate?
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Trimethoprim
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How is resistance to sulfonamides presented?
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Increased synthesis of PABA
Alterations in enzyme that utilizes PABA Increased capacity to destroy or inactive the drug Development of an alternative metabolic pathway for synthesis of essential metabolites |
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Where are sulfonamides absorbed?
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Gut
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Is the level of sulfonamides in urine higher or lower than serum levels?
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10-25 (?) higher
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Should you use sulfonamides on a patient with 6-glucose phosphate dehydrogenase deficiency?
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No, it could produce acute hemolytic anemia
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Sulfadiazine
Sulfamerazine Sulfamethazine Trisulfapyrimidines Sulfisoxazole and Sulfamethoxazole are what types of drugs? |
Sulfonamides
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What sulfonamide is used routinely for urinary tract infection?
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Sulfisoxazole
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Why are long-acting sulfonamides not available in the US any longer?
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Due to the high incidence of Stevens-Johnson syndrome
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What is the mechanism of Trimethoprim?
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It is a selective inhibitor of Dihydrofolate reductase
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What must be absent with the use of trimethoprim in order to make it bacteriocidal?
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Thymine
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Which types of bacteria are targeted by Trimethoprim?
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Both Gram - and Gram +
Its Broad Spectrum |
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Which chemotherapeutic agents are inhibitors of cell wall synthesis?
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Penicillin
Cephalosporin Vancomycin Bacitracin Cycloserine |
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Which type of bacteria is most affected by penicillins?
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Gram +
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What drug inhibits the first stage of the cell wall synthesis? (Production of Cell Wall Building Blocks)
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Cycloserine
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What drug(s) inhibit the second stage of the cell wall synthesis? (Precursor transported from inside cell membrane to outside)
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Vancomycin and Bacitracin
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What drug(s) inhibit the third stage of the cell wall synthesis? (Cross linking of the cell wall)
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Penicillin and Cephalosporin
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What does Cell Death require?
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Action of Autolysin
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What are three mechanisms of resistance to Penicillin?
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Lack of accessibility to target (Gram Negative)
Production of Penicillinases (Beta-Lactamase) Alterations in Penicillin Binding Proteins |
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About what percent of penicillin is protein bound?
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33-50%
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What is the standard reference of Penicillin?
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Penicillin G
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Is oral use of Penicillin G indicated?
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Not, it is inactivated at low pH
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Which type of Pen G is used for syphyllis and rheumatic fever prophylaxis?
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Benzathine Pen G
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Which type of Pen G is used for the treatment of ghonorrea?
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Procaine Pen G
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Which type of penicillin is acid stable?
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Penicillin V
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Which drugs are penicillinase resistant penicillins?
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Methicillin
Cloxacillin Nafcillin Dicloxacillin |
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Which drugs are broad spectrum penicillins?
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Ampicillin
Amoxicillin Carbenicillin |
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Which drug is one of the last lines of defense in threatment of Methicillin-resistant S. aureus?
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Vancomycin
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Which antibiotic inhibits the intermediate stage of cell wall synthesis and is used as a topical treatment because it is too toxic for systemic use?
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Bacitracin
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Which 1st Gen drug of the cephalosporins is beta-lactamase resistant?
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Cephalothin
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Which drug of the cephalosporins is acid stable?
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Cephalexin
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Which drug of the cephalosporins is effective against otitis caused by H. influenza?
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Cefaclor
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What are the third generation drugs of the cephalosporin group?
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Cefotaxime
Ceftizoxine |
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What drugs are considered protein synthesis inhibitors?
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Tetracyclines
Chloramphenicol Aminoglycosides Macrolides Clindamycin |
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What do tetracyclines target?
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Broad Spectrum (G+ , G-, Atypical)
Bacteriostatic |
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What reduces the Oral F of Tetracyclines?
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Divalent and Trivalent metal containing products. (Milk, cheese, yogurt, kaopectate, pepto-bismol, vitamins w/iron, and calcium supplements)
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Can nursing mothers take tetracyclines?
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No, it is excreted in milk
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Which tetracyclines are short acting?
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Chlortetracycline
Tetracycline Oxytetracycline |
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Which tetracyclines are intermediate acting?
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Demeclocycline
Methacycline |
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Which tetracyclines are long acting?
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Doxycycline
Minocycline |
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What are some common adverse side effects of tetracyclines?
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GI Irritation
Photosensitivity Reactions Permanent Discoloration of Teeth |
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What is the drug of choice for cholera, rickettsiae, Lyme's disease, Chlamydial pneumonias, and vaginitis?
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Tetracyclines
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What common drug could be given for acne, or ulcers associated with H. pylori?
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Tetracyclines
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What tetracycline drug is often used systemically for periodontal disease?
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Periostat (Doxycycline)
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What tetracycline drug is often used topically for periodontal disease?
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Arrestin (Minocycline)
Atridox (Doxycycline) |
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What antibacterial protein synthesis inhibitor can be associated with aplastic anemia?
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Chloramphenicol
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What organisms does Chloramphenicol target?
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Gram +, Gram - Aerobes
Anaerobes (Excellent Activity) Atypical Bacteria Bacteriostatic |
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Which part of protein synthesis does chloramphenicol affect?
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Blocks the peptidyltransferase activity on the 23S RNA of the 50S subunit
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What drug is associated with Gray baby syndrome?
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Chloramphenicol
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What drug has been used for Typhoid Fever, Severe Meningitis, and Severe Pneumona?
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Chloramphenicol
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Which type of protein synthesis inhibitor chemotherapeutic agent is bacteriocidal?
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Aminoglycosides
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Which organisms do aminoglycosides target?
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Gram - (Enteric) and some Gram + (Staph and Strep)
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What are the three effects of aminoglycosides associated with binding to the 30S ribosomal subunit?
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Inhibit initiation
Premature termination Misincorporation |
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What is the method of use for aminoglycosides?
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IV, or IM
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What are the toxic effects of aminoglycosides?
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Low therapeutic index
Nephrotoxicity Ototoxicity |
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Gentamicin
Tobramycin Amikacin Netilmicin Neomycin Streptomycin and Spectinomycin Are all drugs that belong to which type of antibacterial? |
Aminoglycosides
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Which aminoglycoside is used for Pseudomonal pneumonia?
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Tobramycin
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Which aminoglycoside is used for aminoglycoside-resistant infections?
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Amikacin and Netilmicin
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Which aminoglycoside is used for TB?
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Streptomycin
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Which aminoglycoside is used for N. gonorrhea?
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Spectinomycin
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What are three types of macrolides?
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Erythromycin
Azithromycin Clarithromycin |
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Which organism is mainly targeted by macrolides?
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Aerobic Gram + cocci and bacilli
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Which macrolide has an increased activity towards H. influenzae?
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Azithromycin
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What is the mechanism of macrolides?
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Bind to 50S ribosomal subunit to block translocase activity of ribosome
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Why is erythromycin enteric-coated or ester derivatives?
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In order to avoid gastric inactivation (it is inactivated by stomach acid)
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Which macrolide is excreted unchanged in the bile?
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Azithromycin
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Which macrolide has a high potential for drug interactions?
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Erythromycin
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What are two mechanisms of resistance to macrolides?
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Acquisition of met gene (erythromycin efflux transporter)
Acquisition of erm gene (methylates a base residue in 23S RNA of ribosome) |
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How does Clindamycin differ from Erythromycin?
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Has a high activity for anaerobes
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What is the drug of choice for lung abscess, anaerobic lung and pleural space infections?
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Clindamycin
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Which antibacterial is used in certain parasitic or fungal infections of T. gondii, and P. carinii?
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Clindamycin
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What is the prototype drug of the fluoroquinolones?
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Ciprofloxacin
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What is the mechanism of fluoroquinolones?
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Inhibitor of bacterial DNA synthesis
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What are common adverse effects of fluoroquinolones?
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GI disturbances
Nausea Vomiting |
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How is Vancomycin administered?
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Parenteral
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What does Metronidazole mainly target?
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Anaerobic gram -
Clostridium species Bactericidal |
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Which drug has neurologic effects attributed to seizures?
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Metronidazole
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What topical antibacterial is used for gram + bacteria in combination with polymixin and neomycin?
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Bacitracin
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What antibiotic is a hospital grade antibiotic that is broad spectrum restricted use as a drug of last resort?
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Imipenem-cilastatin
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What is Aztreonam used for?
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Pseudomonas, Klebsiella, and Serratia
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What is the transformation of normal tissue into cancer cells?
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Carcinogenesis
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How long must a person not have recurrance after cancer-therapy before they are considered disease-free?
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5 Years
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If the tumor shrunk after therapy, how would the result be classified?
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Partial Response/Remission
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What would a tumor be classified as if it was neither growing nor shrinking after therapy?
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Stable Disease
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Which phase of chemotherapy regimen seeks rapid reduction in tumor cell burden?
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Induction Therapy
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Which phase of chemotherapy regimen seeks to complete or extend initial remission?
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Consolidation Therapy
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Which phase of chemotherapy regimen seeks to sustain the remission for as long as possible?
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Maintenance Therapy
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Which tumors would you take the watch and wait approach? (No Therapy)
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Slow growing cancers (Lymphoma and some Prostate Tumors)
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What log kill would destroy the total cell population?
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9
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What may serve to recruit cells into active growth and increase sensitivity to chemotherapy?
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Surgery and Radiation
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What is an example of enhanced drug inactivation in a chemotherapeutic regimen?
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Gluthathione Redox Pathway
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What are examples of Cytotoxic Drugs?
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Alkylating agents
Antimetabolites Antitumor antibiotics Mitotic inhibitors Topoisomerase inhibitors |
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Which tissues are most affected by chemotherapy drugs?
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Those with high growth fraction -
Bone Marrow Skin Hair Follicles Gastrointestinal Tract Developing Sperm |
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When would you want to start chemotherapy treatment?
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When tumor burden is low and growth fraction is high
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How should chemotherapy drugs be administered?
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Near max individual doses
As frequently as possible |
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What cancer chemotherapeutic agent requires metabolic activation with one exception?
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Antimetabolites (the exception being Methotrexate)
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What cell cycle are antimetabolites specific to?
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S Phase
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What is the mechanism of antimetabolites?
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They interfere with metabolic steps leading to DNA synthesis
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Which type of chemotherapeutic drugs are chemically synthesized?
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Alkylating Agents
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Which type of cancer chemotherapuetic drug is not highly cell cycle specific, but is cell cycle active?
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Topoisomerase Poisons
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Which types of cancer chemotherapeutic drugs do not require metabolic activation?
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Microtubule Poisons
Topoisomerase Poisons |
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What type of cancer chemotherapeutic drug promotes DNA strand breaks?
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Topoisomerase Poisons
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Which cell cycle are Microtubule Poisons specific to?
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M phase
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What do monofunctional alkylating agents do?
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Cause DNA damage as the cell attemps to repair alkylation
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What do bifunctional alkylating agents do?
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Cross link DNA
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What are the difficulties in treating fungal infections?
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Cell structure is closely related to mammalian cells
Slow growth rate Infections can often occur in poorly vascularized tissues |
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What are four classes of drugs used to treat systemic fungal drug infections?
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Polyenes
Azoles DNA/RNA synthesis inhibitors Mitotic spindle inhibitors |
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What is the broadest spectrum of all antifungals?
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Amphotericin B (Polyene antifungal)
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What is the mechanism of polyenes?
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Binds ergosterol to create leaky membranes (pores)
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Which type of polyene has activity towards Candida, and is too toxic for systemic use?
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Nystatin
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What is the first line drug for OPC and vaginal candidaisis?
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Nystatin
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Which drug is the Azole prototype?
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Ketoconazole
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What is the mechanism of Ketoconazole?
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An Ergosterol synthesis inhibitor
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Which Azole antifungal is a strong inhibitor of CYP3A4 which leads to many drug interactions?
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Ketoconazole
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Which azole antifungal inhibits testosterone and glucocorticoid synthesis which can lead to gynecomastia in males?
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Ketoconazole
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Fluconazole is a drug of which class?
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Azole
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Which Azole antifungal is a topical use only because it is too toxic for systemic use?
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Clotrimazole
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What is the mechanism of Flucytosine?
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Inhibits DNA synthesis
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What organisms are targeted by Flucytosine?
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Narrow Spectrum (Cryptococcus and Candida)
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What is the mechanism of Griseofulvin?
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It is a mitotic spindle inhibitor which interferes with yeast cell division
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Which antifungal drug does not work when used topically and is taken orally for dermatophytic infections of hair, nails, and scalp?
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Griseofulvin (Mitotic Spindle Inhibitor)
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What was the first orally available drug for treating symptoms of HSV infection?
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Acyclovir
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What is the mechanism of Acyclovir?
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It acts as a DNA chain terminator after being converted into acyclovir triphosphate by both cellular and viral molecules
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What are two other derivatives of the anti-viral Acyclovir?
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Valavyclovir
Penciclovir |
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Which antiviral used for HSV infections attains higher concentrations for longer times?
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Penciclovir
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Which antiviral drug used for HSV infections gives higher bioavailability?
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Valacyclovir
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Which antiviral medication is a 22-carbon saturated primary alcohol that inhibits fusion of human host cell with the envelope of HSV?
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Docosanol
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What drug is used for CMV Retinitis in immunocompromised hosts and as a prophylaxis in transplant patients?
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Ganciclovir
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What are two anti-influenza A only drugs? (Have no effect on Influenza B)
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Amantadine
Rimantidine |
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What is the mechanism of Amantadine and Rimantidine?
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It blocks the uncoating of virus after it enters the cell (M2 Protein interference)
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What type of drugs are Zanamivir, and Oseltmavir?
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Neuraminidase Inhibitors
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Which drugs inhibit both Influenzae A and Influenzae B?
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Zanamivir
Oseltmavir |
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What is a normal CD4+ T cell count?
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1 x 10^6 /mL
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What CD4+ T cell count indicates the first AIDS symptoms?
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<200,000 /mL
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When do you initiate drug therapy for HIV?
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When CD4+ count <200,000 cells/mL
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What are 5 classes of drugs for HIV?
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NRTI (Nucleoside reverse transcriptase Inhibitors)
Non-NRTI Protease Inhibitors Entry fusion Inhibitors Integrase strand transfer Inhibitors |
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What is the mechanism of Nucleoside Reverse Transcriptase Inhibitors?
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They are nucleoside analogues that selectively inhibit HIV Reverse Transcriptase
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How are NRTI's selective but not specific?
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They can also be incorporated into host cell DNA. Mitochondrial form of DNA Polymerase is more affected than Cellular DNA Polymerase
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What is HAART?
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Highly Active Antiretroviral Therapy: A combination of 3 HIV drugs simultaneously
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Which drugs used with HAART are chosen first?
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NRTI:
Zidovudine Abacavir Stavudine Tenofovir |
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Which drugs used with HAART are chosen second?
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Emtricitabine
Lamivudine |
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What class of drugs are Nevirapine, Delavirdine, and Efavirenz?
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Non-Nucleoside Reverse Transcriptase Inhibitors
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What class of drugs are Nevirapine, Delavirdine, and Efavirenz?
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First Generation Non-Nucleoside Reverse Transcriptase Inhibitors
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What class of drug is Etravirine?
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Second Generation Non-Nucleoside Reverse Transcriptase Inhibitors
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Which class of HIV drug is most susceptible to rapid development of drug resistance?
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NNRTIs
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What is the preferred NNRTI for starting therapy?
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Efavirenz
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What drug class do the following drugs belong to:
Saquinavir Ritonavir Indinavir Lopinavir |
HIV Protease Inhibitors, First Gen
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Which PI is often included in HAART regimens with another protease inhibitor because it increases the concentration of lopinavir?
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Ritonavir
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What second generation PI derivative is reserved as a backup for highly resistance HIV (which is also administered with ritonavir)?
|
Tipranavir
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What are two general concerns with PI's?
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They inhibit and/or induce two major families of drug metabolizing enzymes: Cytochrome P450 3A4 and UGT1A1 - Causes drug interactions
They elevate blood LDL |
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What newer derivative of PI lacks a hypercholesterolemic effect?
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Atazanavir
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What is the only AIDS drug that must be administered parenterally?
|
Enfuvirtide
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What is Enfuvirtide?
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An amino acid peptide that inhibits viral entry by preventing fusion
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What entry fusion inhibitor prevents fusion by antagonizing the chemokine coreceptor 5?
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Maraviroc
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What HIV Integrase Inhibitor is reserved for HAART regimens in patients who are resistant to at least one antiretroviral agent from each conventional class?
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Raltegravir
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