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121 Cards in this Set
- Front
- Back
Name 5 groups of B-Lactams: |
1.Penicillin
2. Cephalosporin C – (Cephalosporium acremonium) 3. Cephamycin 4. Carbapenems - pseudo 5. Monobactams - pseudo |
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TQ. What is the only second generation cephalosporin that can adequately penetrate into cerebrospinal fluid?
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cefuroxime
fur (for) ROX in the brain |
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When combining bacterioSTATic agents you can expect what kind of effect?
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Additive effect
hint: ADD :: STATS |
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Penicillinase-resistant penicillins (isOXazolyl penicillins) are most often used to treat/prevent what disease?
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Bovine staphylococcal mastitis
(can be given orally like Pen.V; unlike other Penicillins) |
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What antibiotics have the action of interfering with the cell membrane?
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Polymyxin B
Colistin (Bacitracin does not it interferes with cell wall) |
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Beta lactams (penicillins and cephalosporins), bactracin, vancomycin, and cycloserine are all examples of which type of antimicrobials?
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interfere with cell wall synthesis
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What increases the half-life of sulfonamides?
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Low urine pH
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Which penicillin is excreted mainly by bile?
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Naficillin
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What cephalosporin excreted in bile?
How about the rest of them (most)? |
Ceftriaxone and cefoperazone are excreted mainly in bile, but most cephalosporins excreted by kidney and prox.tubular secretion
- end with -one - C "own" bile -TriA(nd)X Bile OPERA.zone - Try One Operation Zone Bi LE |
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When combining bactericidal agents you can expect what kind of effect?
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Synergistic effect
Drug synergy occurs when drugs can interact in ways that enhance or magnify one or more effects, or side-effects, of those drugs. SIN:KILL SYN:CIDE |
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What is the major pathway of sulfonamide metabolism? Where?
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Acetylation in the liver and some in the lung
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What type of bacterial resistance develops slowly to sulfonamides?
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Chromosomal mediated resistance
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Which group of penicillins is more effective against gram-negative aerobic and anaerobic bacteria?
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Extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)
(there are 5: C.MAT.P. ) ~aren't natural penicillins decent against anarobes? but not pseudo.? |
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Which bacteria's cell wall is not permeable to beta-lactam antibiotics?
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Gram negative bacteria
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What antibiotics were developed from the microorganism Bacillus? (2)
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Polypeptide antibiotics (polymyxin and bacitracin)
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Which animals are sensitive to procaine penicillin, producing anaphylaxis and CNS disorders?
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Guinea pigs
Chinchillas Birds Snakes Turtles |
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What antibiotics were developed from the microorganism Actinomycetes (Streptomyces)? (3 groups & 3 drugs)
>It is a Gram + bacteria. |
1. Tetracyclines
2. Aminoglycosoides 3. Macrolides 4. Chloramphenicol 5. Ivermectin 6. Rifamycin |
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What antibiotics have the action of interfering with protein synthesis 30S ribosomal sub-unit?
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Tetracyclines
Aminoglycosides |
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What antibiotics have the action of interfering with cell wall synthesis? (1 grp., 3 drugs)
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Beta lactams
Bacitracin Vancomycin Cycloserine |
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What antibiotics have the action of interfering with the protein synthesis 50S ribosomal sub-unit?
(1 group, 2 drugs) |
Chloramphenicol
Macrolides Lincomycin (50s higher than 30 and macro means big) |
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What antibiotics have the action of interfering with nucleic acids?
(1 grp., 2 drugs) |
Fluoroquinolones
Rifampin Metronidazole forget making RNA |
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What antibiotics have the action of interfering with folate acid synthesis?
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Sulfonamides
Diaminopyrimidines |
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Which antibiotics are classified as broad spectrum? (6 grps,)
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Tetracyclines
Chloramphenicol and derivatives Macrolides and linomycins Fluoroquinolones Sulfonamides TLC Fr M S |
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Which antibiotics are classified as narrow spectrum?
(2grps, 3 drugs) |
Beta-lactams
Aminoglycosides Polymyxin B and colistin Rifampin N-A-B-P-R narrow antibiotics poor range |
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What are the three ways that transfer of resistance genes between bacteria occur?
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Conjugation
Transduction Transformation |
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What are the four biochemical mechanisms of antimicrobial resistance?
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Antimicrobial inactivation
Alteration of drug-sensitive site or drug binding site Decreased drug accumulation in the bacterium Development of an alternate metabolic pathway |
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Sulfonamides are structural analogs of what structure in bacterial organisms? Why important?
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PABA; competitvely inhibits enz. step in Folic Acid synth.
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What antimicrobials!! are inhibited by sulfonamides? What are not inhibited?
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Inhibits Gram+, Gram-, and protozoa
Does not inhibit obligate anaerobes |
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What can sulfonamides be combined with to increase their spectrum of activity?
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Diaminopyrimidine
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Which sulfonamides are indicated for ophthalmic use?
Which cephalosp. are indicated for ophthalmic use? |
those with neutral or near neutral pHs (sulfacetamide)
note: cephalosporin suck penetrating vitreous humor |
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What is the major pathway of sulfonamide metabolism?
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Acetylation in the liver and some in the LUNG
SULF -> LUNG |
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Which animals are unable to acetylate sulfonamides?
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Dogs
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What are the two classifications of sulfonamide toxicity?
1+1 1+4 |
Immunologic (keratoconjunctivitis sicca)
Non-immunologic (crystalluria, hypoprothrombinemia, aplasic anemia, and thrombocytopenia) |
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What increases the half-life of sulfonamides?
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Low urine pH
sulfonamides = weak organic acid pka = 4.7 (sulfizoxazole) to 10.4 (sulfanilamide) |
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What breed of dogs reacts to sulfonamides with polyarthritis, fever, cutaneous eruptions, and hepatitis?
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Doberman Pinschers - hate sulfonamides
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What animals react to sulfonamides with hypoglycemia? (2)
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Ducks
Dogs |
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What type of bacterial resistance develops slowly to sulfonamides?
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Chromosomal mediated resistance
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What type of bacterial resistance develops rapidly to sulfonamides?
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Plasmid mediated resistance
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What are the most commonly used diaminopyrimidines (combined w/sulfonamides) used in veterinary practice? (3)
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Ormetoprim
Pyrimethamine Trimethoprim (have 'prim' or 'pyrim') Prim POT |
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What class of drugs is a lipid-soluble organic base, bacteriostatic, reversibly binds and inhibits dihydrofolate reductase, and has a low affinity towards mammalian dihydrofolate reductase?
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Diaminopyrimidines
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Which diaminopyrimidines is not degraded in rumen and can be given orally to ruminants?
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Ormethoprim
OR = oral rumen |
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How are diaminopyrimidines metabolized?
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Oxidation and conjugation in the liver
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Which class of drugs combines two bacteriostatic drugs to create a bactericidal drug?
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Potentiated Sulfonamides (Sulfonamides + Diaminopyrimidines)
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Which bacteria is not susceptible to potentiated sulfonamides?
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Pseudomonas aeruginosa
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How are potentiated sulfonamides metabolized?
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Sulfonamides acetylated and conjugated with glucoronic acid in the liver
Diaminopyrimidines are metabolized to oxide and hydroxylated metabolites in the liver |
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Which drugs interfere with the transpeptidase enzyme by binding to a PBP leading to the formation of defective cell walls that are osmotically unstable?
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Beta-lactam antibiotics - interfer w/cell walls & bactericidal
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Penicillinase-resistant penicillins (isoxazolyl penicillins) are most often used to treat/prevent what disease?
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Bovine staphylococcal mastitis
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What drugs are considered broad-spectrum penicillins (Aminopenicillins)?
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Amoxicillin
Ampicillin |
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What bacteria are susceptible to broad-spectrum penicillins (Aminopenicillins)?
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Those susceptible to natural penicillins (Active against Gram positive and Gram negative anaerobic?)
Enterobacteriaceae (E. coli, Proteus mirabilis, and Salmonella) ~e.g. Amoxicillin susceptible to B-lactamase? |
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What drugs are considered extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)? (5)
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Carbenicillin
Mezlocillin Azlocillin Ticarcillin Piperacillin C-MAT-P |
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Which group of penicillins is more effective against gram-negative aerobic and anaerobic bacteria?
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Extended spectrum/anti-pseudomonal penicillins (carboxypenicillins)
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Which penicillin should NOT be be administered via IV, because it will affect the cardiac conduction system?
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Procaine penicillin G
(also tilmicosin) PPT |
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Which penicillin is a repository salt and absorption can be prolonged for 7 or more days? (give full name)
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Benzathine penicillin G
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Naficillin is what kind of antibiotic? What's unusual about it?
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it's a penicillin; excreted in bile
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What is used when animals to be treated do not exhibit signs of disease but are in close contact with diseased animals?
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metaphylactic
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What is used for treating a clinical disease?
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therapeutic
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What is used to prevent the disease when its occurrence can be predicted?
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prophylactic
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Polymyxin B and colistin are examples of what type of antimicrobials?
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antimicrobials interfering with cell membrane
-also i think they're bactericidal |
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What has been reported in dogs and leghorn chickens receiving sulfaquinoxaline, which is due to the inhibition of vitamin K epoxide reductase?
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sulfaquinoxaline + (dogs,chickens) = hypoprothrombinemia
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Sulf. induced toxicity can be classified as ____, causing crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia
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non-immunogenic <- crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia
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diaminopyrimidines are metabolized to what (general chemical/product structure)? (2)
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oxide and hydroxylated metabolites
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What is the most common route of administration with penicillins?
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IM injection
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Isoxazolyl penicillins and V penicillin for administration via what route? Why?
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indicated for oral use because of good absorption (Isoxazolyl penicillins and V penicillin)
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How are penicillins classified?
1(+2 subgroups) 1 Admin? |
natural penicillin (G & V) and semi synthetic
G- please Give IM V- victory Over (oral) |
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How must penicillin G be administered?
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only parenteral administration
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Cephalosporins are well absorbed following what administration?
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IM or SC
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Are amoxicillin & ampicillin broad or extended spectrum penicillin?
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broad spectrum
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What is it called when DNA is acq. directly from environment and incorp. within genome thr. normal cross-over mechanism?
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transformation
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What inactivates chlorampehnicol?
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chloramphenicol acetyl transferase produced by gram positive and gram neg bacteria
(CAT anti-chlor) |
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What causes decreased permeability through the cell membrane of gram negative organisms?
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ampicillin
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What drugs sensitive to bacterial resistance via energy dependent active efflux of drug (Impaired uptake of drug)?
efflux = mechanism responsible for extrusion of toxic substances and antibiotics outside the cell |
tetracyclines and fluoroquinolones
ET F.one |
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How do bacteria synthesize their folic acid?
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using para-aminobenzoic acid
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What 2 classes of antimicrobial compounds can inhibit the synthesis of folic acid?
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sulfonamides and diaminopyrimidines
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causing depletion of the folic acid stores in bacterial cells abd are insoluble in water?
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sulfonamides
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Succinylsulfathiazole, , sulfaquinoxaline, sulfaguanidine, and <> are examples of what? How unique?
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enteric sulfonamides (e.g. phtyalylsulfathiazole); these are only sulfonamides not well absorbed orally
~slowly abs. due to poor water solub.; exerts local action in GIT! |
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What acts as topical anti-inflammatory by inhibiting prostaglandin synthesis and is used to treat rheumatoid arthritis in humans and colitis in dogs?
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5-aminosalicyclic acid (1 of 2 components of sulfasalazine, an enteric sulfonamide)
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What is hydrolyzed in the bowl by the bacteria into phtalic acid and sulfathiazole?
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phtyalylsulfathiazole
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Why must sulfonamide solutions be buffered for parenteral administration?
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prevent perivascular reactions fue to the alkalinity of most sulfonamides
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What are the 2 sulfonamides that can be used topically?
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silver sulfasiazine and mafenide
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What type of sulfonamides need to be used for opthalmic use?
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on neutral or near neutral pHs sulfonamides such as sulfacetamide
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Sulfonamide plasma protein binding is higher in cows or goats?
What drug is highly protein bound? |
15% (sulfanilamide in cows) to 90% (sulfadimethoxine in goats)
sulf-DIMEth |
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T or F: Sulfonamides cross placenta barrier and get into CSF, synovial fluid
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TRUE
CSF -> CPR's cephalosporins potentiated sulfonamides rifampin |
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Why are acetylated sulf. metabolites a problem?
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less soluble than parent compound, therefore can accum. in kidney etc. = crystal formation
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What is the primary route of excretion of sulfonamides except enteric sulfonamide?
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renal excretion
except the enteric sulfonamides |
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What urine pH favors tubular reabs. of sulfonamides thereby increasing half-life?
What other drug class affected by pH? |
low urine pH favors tubular reabs. of sulfonamides (weak acids) thereby increasing half-life
Macrolide, however, ineffective at low pH |
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Long acting sulfonamides have low or high pka?
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not sure; but i think high pka, that way they are NOT ionized at low pH
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Why would you NOT want to use Sulfonamides for mastitis treatment?
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Sulfonamides may be distributed into milk (low concentrations); not for mastitis b/c don't want people drinking antibiotics
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What drug when given orally, ; treats colitis in dogs (as anti-imflam. by inhibiting prostaglandin synth.) and rheumatoid arthr. in humans?
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Sulfasalazine (enteric sulfonamide)
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Why Folic Acid important to microbes?
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used for RNA, DNA, protein synthesis? (can't synth. purines and some nucleotides w/o it)
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T or F: Although Sulfonamides primarily excreted via kidney (urine), also via tears, saliva, bile, milk, and sweat..to some extent.
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True
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Enteric sulfonamides are excreted how?
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via feces mostly, some metabolites may be reabs etc
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Sulfonamide induced toxicity can be classified as immunologic, such as what?
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keratoconjunctivitis sicca (KCS)
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Sulfonamide induced toxicity can be classified as non-immunologic, such as what?
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crystalluria, hypothrombinemia, aplastic anemia, and thrombocytopenia
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What can induce hepatic necrosis and chloestatic hepatitis in humans?
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trimethoprim-sulfadiazine and trimethoprim-sulfamethoxazole
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What is the consequence of precipitation of the sulfonamide in the glomerular filtrate of the kidney?
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crystalluria, hematuria, and renal tubular blockage
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How can aciduria be minimized?
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by keeping patient well hydrated during therapy and alkalinizing the urine
(high pH will favor elimination of Sulfonamide drug) |
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What has been reported in dogs and leghorn chickens receiving sulfaquinoxaline, which is due to the inhibition of vitamin K epoxide reductase?
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hypoprothrombinemia; blood disorder in which a deficiency of prothrombin (Factor II) results in impaired blood clotting
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What can interfere with thyroid hormone synthesis?
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sulfonamides
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First generation cephalosporing have the highest activity of the cephalosporins against what?
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gram-positive bacteria
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Beta-lactamase enz. made by what bacteria?
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gram negative bacteria
BL + N = BNL |
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Second generation cephalosporins are more effective than 1st generation in the treatment of what?
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infections caused by gram negative bacteria
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What cephalosporin drug is "new generation", has broader gram+ activity, active against beta-lactamase-producing strains as well as anerobes?
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ceftiofur
FUR ACTIVE |
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Ceftiofur is indicated for the treatment of respiratory tract infections in ____ and ____, for urinary tract infections in ____, pleuritis and peritonitis in ____, and E. coli infections in ____.
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resp. tract in cattle and pigs, urinary in dogs, perit. in horses, and E.coli in poultry
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Most cephalosporins are excreted entirely by what?
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the kidneys by glomerular filtration and proximal tubular secretion
CPT |
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Penicillin sensitive individuals are also sensitive to what?
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cephaloporins
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what beta-lactamase inhibitor acts as competitive inhibitor (preventing B-lactamase from bothering penicillin)?
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Clavulanic acid
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What are examples of penicillin G? 2+2
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sodium salt, potassium salt (benzathine, procaine)
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What form of penicillin G or ampicillin should be given when intravenous administration is indicated?
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Sodium salt
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What drug has higher bioavailibity in dog: amoxicillin or ampicillin?
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Amoxicillin
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What penicillin causes acute toxicity given IV and generally sux at life?
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Procaine
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What are examples of penicillin G?
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sodium salt, potassium salt (benzathine, procaine)
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2 CEPHLOSPORINS which have good oral absorption (most IM/SC):
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Cephalexin and cefaclor – high oral absorption
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What do these have in common?
2nd generation cephalosporin – cefuroxime 3rd generation of cephalosporin - ceftriaxone, cefotaxime, ceftazidime, ceftizoxime |
All cross BBB to CSF
notice all have x or z in them! |
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Metabolism of cephalosporins?
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LIVER – to form deacetyl derivatives
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Deacetylated metabolite of _____– longer half-life than parent compound?
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CefoTAXIME (has metabolite with long HL)
~Death and taxes |
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What cephalosporins have very ACTIVE METABOLITE?
What is it? |
Ceftiofur
Desfuroyl-ceftiofur |
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Cefoperazone, cefamandole, moxalactam inhibits vitamin K dependent pathway for the synthesis of clotting factors, this leads to what?
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hypoprothrombinemia and coagulopathy
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What beta-lactamase inhibitor is a penicillanic acid sulfone, increases the activity of beta lactam antibiotic, and can only be administered IV?
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sulbactam
Sulb.IV (AMP SS) |
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What are examples of sulbactam?
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sodium sulbactam and ampicillin
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What beta-lactam drug group is useful for serious infections, can be administered with cilastatin, and has broad spectrum action against Gram- aerobic and anaerobic bacteria?
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CARBAPENEMS - good against pseudomonas like monobactams
CARBoNO |
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What B-lactam drug group have one ring, active against gram negative bacteria like Pseudomonas, stable against B-lactamase, and used in penicillin allergic patients?
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Monobactams (aztreonam)
stable against B-lactamase |