sulfonamides, trimethoprim, and quinolones Flashcards
Competitive inhibitors of Dihydropteroate synthase
Sulfonamides
Selective inhibitor of bacterial Dihydrofolate reductase
Trimethoprim
Sequential blockade of folate synthesis
Trimethoprim + Sulfamethoxazole (cotrimoxazole)
Act as substrates for dihydropteroate synthase, producing nonfunctional forms of folate
Sulfonamides
Prevents formation of active tetrahydrofolate (THF)
Trimethoprim
Sulfonamides for simple UTI
Triple sulfa, Sulfisoxazole
Drug for ocular infection
Sulfacetamide
Drug for burn infections
Mafenide, Silver Sulfadiazine
Drug for ulcerative colitis, rheumatoid arthritis
Sulfasalazine
Drug for burn wounds but causes metabolic acidosis
Mafenide acetate
First line for acute toxoplasmosis
Sulfadiazine + Pyrimethimine
Second line antimalarial agent
Sulfadoxine + Pyrimethamine (Fansinadir)
DOC for pjp, toxoplasma, nocardiosis
Co-trimoxazole
3 separate sulfonamides used to reduce the likelihood of precipitating
Triple sulfa
Adverse effects: Steven Johnson Syndrome, hemolytic anemia, granulocytopenia, thrombocytopenia, aplastic anemia, kernicterus
Sulfonamides
Adverse effects: Megaloblastic anemia, leukopenia, granulocytopenia,
Mild elevation of blood creatinine
Trimethoprim
What happens to sulfonamide when urine is acidic
Precipitates to sulfonamide crystals, decreased solubility
Sulfonamides drug interaction
Competition with warfarin and methotrexate for plasma binding
Trapped in acidic environment, good for prostatitis treatment
Trimethoprim
Interferes with bacterial DNA synthesis
Inhibits Topoisomerase II (DNA gyrase) and Topoisomerase IV
Fluoroquinolones
Activity: Gram (+), Gram (-), Enhanced activity against Anaerobes
4th gen: moxifloxacin, trovafloxacin
Activity: Slightly less active against gram (-), Greater activity against gram (+) cocci
3rd gen: levofloxacin, gatifloxacin, sparfloxacin
Activity: Greater activity against gram (-), Atypical organisms (M. pneumoniae)
2nd gen: ciprofloxacin
Activity: against common pathogens that cause UTI
1st gen: norfloxacin
Treatment for gonorrhea and chlamydia
2nd gen: ciprofloxacin, ofloxacin
Fluoroquinolone for typical and atypical pneumonia
3rd gen: levofloxacin
Fluoroquinolone that has activity against: gram (+), penicillin resistant pneumococci
3rd gen: sparfloxacin
Used in meningococcal carrier state
Tuberculosis
Prophylactic management of neutropenic patients
4th gen: moxifloxacin, trovafloxacin
Adverse effects: photosensitivity
Lomefloxacin, Pefloxacin
Adverse effects: QT prolongation
Gatifloxacin, Levofloxacin, Gemifloxacin, Moxifloxacin
Adverse effects: hyper or hypoglycemia
Gatifloxacin
Adverse effects: Hepatotoxic
Trovafloxacin
Adverse effects: Cardiac arrhythmia, photosensitivity
Sparfloxacin
Short-acting sulfonamide
Sulfisozaxole
Intermediate-acting sulfonamide
Sulfamethoxasole
Long-acting sulfonamide
Sulfadoxine
Has MRSA Activity
Co-Trimoxazole
3rd gen fluoroquinolones
Fluoroquinolone with the longest half-life
Moxifloxacin (9-10 hrs)
Earliest fluoroquinolone
Nalidixic acid
Respiratory quinolone
Levofloxacin