Sulfonamides, Trimethoprim and Quinolones Flashcards
Sulfonamides tend to be much more soluble at what pH?
Alkaline
What enzyme is inhibited by sulfonamide?
Dihyrdopteroate synthase
What mechanism is used by sulfonamide for its action against susceptible microorganisms?
Competitive inhibition
What drug inhibits dihydrofolate reductase?
Trimethoprim or pyrimethamine
Combination or sulfonamide and trimethoprim provides what kind of activity against microorganisms?
Synergistic activity
How do you classify sulfonamides?
- oral, absorbable
- oral, non-absorbable
- Topical
How do you classify oral, absorbable sulfonamides?
- short-acting
- intermediate-acting
- long-acting
What is the drug of choice for Pneumocystiis Jiroveci pneumonia?
Trimethoprim-sulfamethoxazole
Sulfisoxazole and sulfamethoxazole is used almost exclusively to treat what?
UTI
What is the first line therapy for the treatment of acute toxoplasmosis?
Sulfadiazine in combination with pyrimethamine
When giving sulfadiazine with pyrimethamine, you should also administer Folinic acid. Why is that?
To minimize bone marrow suppression
What drug is used for ulcerative colitis, enteritis and other inflammatory disease?
Sulfasalazine
Mafenide acetate, a sulfonamide used topically for burn sites causes metabolilc acidosis, how?
Inhibition of Carbonic Anhydrase
What is the uncommon yet serious adverse reaction of Sulfonamides?
Stevens-Johnson syndrome
Sulfadiazine when given in large doses and when fluid intakes is poor can cause crystalluria. How do you treat crystalluria?
Administration of sodium bicarbonate to alkalinize the urine and fluids to increase urine flow
What is the mechanism of action of trimethoprim?
Inhibition of bacterial dihydrofolate reductase
Is sulfonamide alone bacteriostatic or bactericidal?
Bacteriostatic
Is trimethoprim-sulfonamide bacteriostatic or bactericidal?
Bactericidal
What causes resistance to trimethoprim?
- Reduced cell permiability
- Overproduction of dihydrofolate reductase
- Production of an altered reductase with reduced drug binding
Which is more lipid soluble, therefore larger volume of distribution between sulfamethoxazole and trimethoprim?
Trimethoprim
Trimethoprim has more antimicrobial activity in prostatic and vaginal fluids than many other antimicrobial drugs, why?
Trimethorpim is a weak base and concentrates in prostatic and vaginal fluid
What are the adverse effects of trimethoprim?
Megaloblastic anemia, leukopenia and granulocytopenia
What is the mechanism of action of quinolones?
Inhibition of bacterial topoisomerase I (DNA gyrase) and topoisomerase IV
Fluoroquinolones have excellent activity against what organisms?
Gram-negative aerobic