Chemotherapeutic Drugs Flashcards
Competitively inhibit the incorporation of PABA (para-aminobenzoic acid) into folic acid
Sulfonamide
first clinical use of sulfonamide
1936
mass production of penicillin
1941
Harmful effects of chemotherapeutic drugs have resulted from _____________ or _____________.
allergic reactions or inadvertent IV overdose
competitive enzyme inhibitor, blocks the synthesis of folic acid in bacterial cell
Sulfonamide
Sulfonamide inhibits the enzyme
Dihydropteroate synthase
Trimethoprim inhibits the enzyme
Dihydrofolate reductase
After acute overdose of antimicrobials, most agents cause only
nausea, vomiting, and diarrhea
Biological origin of Streptomycin
Streptomyces griseus
Biological origin of Gentamicin
Micromonospora purpurea
Biological origin of Tobramycin
Streptomyces tenebrarius
Biological origin of Kanamycin
Streptomyces kanamyceticus
Biological origin of Neomycin
Streptomyces fradiae
Active against Pseudomonas aeruginosa
Amikacin, Gentamicin, Tobramycin
Most ototoxic aminoglycosides
Neomycin, Kanamycin, Amikacin
Most vestibulotoxic aminoglycosides
Streptomycin, Gentamicin
Most nephrotoxic aminoglycosides
Neomycin, Tobramycin, Gentamicin
Trimethoprim poisoning can cause:
Megaloblastic anemia
Leukopenia
Granulocytopenia
Trimethoprim poisoning antidote
Leucovorin
Leucovorin other names
● Wellcovorin ● Citrovorum factor ● Folinic acid
Chemical name of Leucovorin
5-formyltetrahydrofolate
Used to treat unintentional folic acid antagonist overdose
Leucovorin
Aka Diamino-diphenyl-sulfone (DDS)
Dapsone
Dapsone is combined with
Clofazimine & Rifampin
Average elimination half-life of dapsone
30 hours
Average elimination half-life of dapsone overdose
77 hours
Disorder characterized by the presence of a higher-than-normal level of methemoglobin
Methemoglobinemia
clamps of damaged hemoglobin
Heinz-Erlich bodies
Dapsone is metabolized by 2 primary routes
● Acetylation
● CYP450 Oxidation
Dapsone toxic effects are caused by the p-450 metabolites, including
–Methemoglobinemia
–Sulfhemoglobinemia
–Heinz body hemolytic anemia
may occur owing to depletion of intracellular glutathione by oxidative metabolites
Hemolysis
Dapsone therapeutic ranges from
50-300 mg/d
Death has occurred with dapsone overdose of
1.4 g and greater
Px with ____________________ may experience greater dapsone toxicity at lower doses.
G6PD deficiency, congenital hemoglobin abnormalities, and underlying hypoxemia
form of hemoglobin that does not bind oxygen.
Methemoglobin
Decreases oxyhemoglobin saturation
Unresponsive to methylene blue
Sulfhemoglobinemia