Chapter 187- Dapsone Flashcards
Side effects for dapsone frequently observed in G6PD patients (2)
Hemolysis
Methemoglobinemia
MOA of dapsone
- Inhibits the synthesis of dihydrofolic acid by competing with PABA for active site of dihydropteroate synthetase
- Inhibits neutrophil chemotaxis
- Inhibits release of IL8, PGD2, and TNF alpha
- Inhibits myeloperoxidase - hydrogen peroxide - halide mediated cytotoxic system
PCP prophylaxis in immunocompromised patients
Pyrimethamine + Leucovorin + Dapsone
Uses of dapsone for anrimicrobial (5)
Hansen disease Actinomycetoma Rhinosporidiosis Malaria Toxoplasmosis
FDA approved for acne
7.5% dapsone gel OD
Enzyme in azurophilic granules of neutrophils and in the lysosomes of monocytes that catalyzes conversion of hydrogen peroxide and chloride ions into hypochlorous acid
Myeloperoxidase
Metabolites of dapsone (2)
- MADDS by N-acetyltransferase
(Monoacetyl dapsone) - DDS NOH by cytochrome P450 enzymes
(Dapsone hydroxylamine)
Half life of dapsone
30 hours
2 metabolic pathways of dapsone
Acetylation
N hydroxylation
Dapsone efficacy, half life, and toxicitieesappear unrelated to rate of acetylation.
True or False
True
Dapsone hydroxylamine can be reduced back to dapsone via (2)
- MetHgb reductase in RBCs
2. Cytochrome b5 reductase in hepatocytes
Increases blood levels of dapsone
Probenecid
Trimethoprim
Reduced blood levels of Dapsone
Rifampicin
Blocks hydroxylation of dapsone
Cimetidine 400 mg TID
Omeprazole
Dapsone is contraindicated in
Patients with renal dysfunction
Uses of dapsone for antiinflammatory action
DH EED LAD CBDC Bullous SLE
As unifying feature most diseases treated with dapsone have ___ as predominant infiltrating cell.
Granulocytes (neutrophils/eosinophils)