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Details

Antimetabolites
Fluoroquinolones, Antifolates, etc
36
Other
Not Applicable
12/11/2012

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Cards

Term
Nalidixic acid is a prototype
Definition
Fluoroquinolones
Term
broadly but weakly bacteriostatic against gram negative bacteria only, no longer used clinically
Definition
Nalidixic acid
Term
Fluoroquinolones
Definition
Norfloxacin, Ciprofloxacin, Ofloxacin/levofloxacin, Moxifloxacin, Trovafloxacin
Term
Relax negative supercoils/unwinds helix behind transcription bubble
Definition
Type I DNA topoisomerases
Term
DNA gyrase and topoisomerase IV in bacteria; burns ATP to reintroduce negative supercoils/rewind helix ahead of bubble
Definition
Type II DNA topoisomerases
Term
generic word for all enzymes that wind or unwind DNA
Definition
Gyrase
Term
Maintain homeostatic superhelical density
Definition
DNA topoisomerases
Term
Inhibitor of folate synthesis and metabolism
Definition
Antifolates
Term
important one-carbon carrier in several biosynthetic pathways
Definition
tetraydrofolate
Term
First group of synthetic antibacterial compounds for systemic use
Definition
Sulfonamides
Term
Sulfonamide antibiotics
Definition
Sulfamidochrysoidine, Sulfamethoxazole, Sulfacetamide, Sulfadiazine, Sulfanilamide, Dapsone (a sulfone)
Term
prodrug of Sulfamidochrysoidine
Definition
Prontosil
Term
Sulfonamides (not just antibiotics)
Definition
Sulfanilic acid, Glyburide, Celecoxib, Hydrochlorothiazide, Furosemide, Sulfasalazine
Term
sulfonylurea hypoglycemia
Definition
Glyburide
Term
COX-2 inhibitor
Definition
Celecoxib
Term
Thiazide diuretic
Definition
Hydrochlorothiazide
Term
Loop diuretic
Definition
Furosemide
Term
Topical anti-inflammatory
Definition
Sulfasalazine
Term
Used for uncomplicated UTI, Toxoplasma, Plasmodium falciparum malaria (+ pyrimethamine), Pneumocystic carinii pneumonitis in AIDS
Definition
Sulfamethoxazole/trimethoprime (SMX/TMP = 5:1)
Term
Ophthalmic drops/ointment
Definition
sulfacetamide
Term
Dermatologicals
Definition
sulfadiazine
Term
Vaginal suppository
Definition
sulfanilamide
Term
Trimethoprim (TMP), Pyrimethamine
Definition
2,4- diaminopyrimidines
Term
most selective diaminopyrimidine for bacteria (less effective alone than in combo)-- bacteriostatic
Definition
Trimethoprim
Term
diaminopyrimidine more selective for protozoans
Definition
Pyrimethamine
Term
used in combo with sulfonamide because if you block biosynthetic pathway at two points this is one way to achieve synergism
Definition
diaminopyrimidines
Term
competitive inhibitor of dihydropteroate synthetase (exogenous PABA can compete)
Definition
sulfonamides
Term
Sulfonamides spectrum of activity
Definition
Most strains of streptococci, enteric bacteria, Neisseria, H. influenza, Chlamydia, Toxoplasma, some plasmodia
Term
Fluoroquinolones biopharmaceutics
Definition
chelates aluminum, magnesium, and calcium to form insoluble complexes; inhibition of CYP450, damage developing cartilage in animals
Term
Fluoroquinolones clinical use
Definition
Gram positive coverage not considered reliable; very good gram negative coverage, important anti-pseudomonal
Term
anti-pseudomonal activity (fluoroquinolones)
Definition
pneumonia in cystic fibrosis, UTI and prostitis,
Term
Does not achieve therapeutic levels in blood, used as urinary antiseptic (excreted extremely well into kidneys, renal clearance is so massive there is no build up into bloodstream)
Definition
Norfloxacin
Term
Fluoroquinolones spectrum of activity
Definition
gram positive activity and increased gram negative activity including MRSA, streptococci, enterococci, most gram negative enteric, H. influenza, N. gonorrhoeae;
Term
active against Pseudomonas
Definition
Ciprofloxacin
Term
Fluoroquinolones inhibit:
Definition
DNA gyrase
Term
ciprofloxacin has 0-79% resistance to this within 1 year
Definition
MRSA
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