Nucelic Acid Synthesis Inhibitor Flashcards
Nucleic Acid Synthesis Inhibitors
Antifolate, Fluoroquinolones, Metronidazole, Nitrofurantoins
Antifolate drugs
Sulfonamides and Trimethoprim
Short-acting Sulfonamide
Sulfisoxazole
Intermediate-acting Sulfonamide
Sulfamethoxazole
Long-acting Sulfonamide
Sulfadoxine
PABA competing antifolate drug
Sulfonamides
Antifolate drug structurally similar to folic acid
Trimethoprim
Weakly acidic antifolate drug
Sulfonamide
Weakly basic antifolate drug
Trimethoprim
High concentrations in vaginal and prostatic fluid
Trimethoprim
Inhibited by Sulfonamides
Dihydropteroate synthase
Inhibited by Trimethoprim
Dihydrofolate reductase
SMX-TMP MOA
Sequential blockade of folate synthesis
Antifolate drug that must use preformed folic acid to cause effect
Sulfonamide
Antifolate drug resistance MOA
Increased PABA production of bacteria
Decreased sensitivity to sulfonamides
Decreased intracellular accumulation of drugs
Silver Sulfadiazine SimD
Mafenide Acetate
Sulfonamide with best eschar penetration
Silver Sulfadiazine
Precipitated by Sulfonamide use of G6PD patients
Acute hemolysis
Co-Trimoxazole coverage
Ear, Sinus, Repiratory, Urinary Tract Infections
Pneumocystic carinii
Toxoplasmosis, Nocardiosis, Typhoid, Shigella
Most common side effect of Co-trimoxazole
Hypersensitivity reactions:
TEN, EM, SJS, PAN, Exfoliative dermatitis
Fluoroquinolones MOA
inhibit topoisomerase II in Gram (-)
inhibit topoisomerase IV in Gram (+)
Fluoroquinolone resistance MOA
decreased intracellular drug accumulation
change in porin structure
point mutations in antibiotic binding regions
First Generation Fluoroquinolones
Nalidixic acid, Cinaxacin, Rosoxacin
Second Generation Fluoroquinolones
Ciprofloxacin, Ofloxacin, Norfloxacin
Third Generation Fluoroquinolones
Levofloxacin, Sparfloxacin, Grepafloxacin
Fourth Generation Fluoroquinolones
Moxifloxacin, Trovafloxacin, Gemifloxacin, Gatifloxacin
Fluoroquinolones withdrawn from market
Grepafloxacin and Gatifloxacin
First generation quinolone hypothetical clinical use
UTI
Second generation quinolone use
Gram (-) cocci, Gram (+) cocci
Mycoplasma
Third generation quinolone use
Gram (+) > Gram (-)
Streptococci, Enterococci
Fourth generation quinolone use
Broad spectrum - Anaerobes
Side effect of Fluoroquinolone
Tendinitis and Tendon rupture
Contraindication of Ciprofloxacin and Levofloxacin
Children and Pregnant
Grepafloxin side effect
Severe cardiotoxicity
Fluoroquinone causing Diabetes
Gatifloxacin
Hepatotoxic fluoroquinone
Trovafloxacin
Potentiated by Fluoroquinone
Methylxanthines
Nitroimidazole drugs
Metronidazole, Tinidazole
Antiprotozoal drug
Metronidazole
Metronidazole MOA
Reduce ferredoxin forming free radicals that disrupt ETC
Metronidazole use
Anaerobic infections below the diaphragm
Vaginitis
Pseudomembranous colitis
Nitrofuran drug
Nitrofurantoin
Forms multiple reactive intermediates when acted upon by bacterial nitrofuran reductase
Nitrofurantoin
Nitrofurantoin indication
UTI except
Proteus and Pseudomonas
Pulmonary Fibrosis Drugs
Bleomycin, Busulfan, Bromocriptine, Amiodarone, Nitrofurantoin, Methotrexate