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Download Chapter 16 Cholinesterase Inhibitors
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Sulfonamides and Trimethoprim Sulfonamides and Trimethoprim Broad-spectrum antibiotics Have closely related mechanisms Suppress bacterial growth by inhibiting tetrahydrofolic acid Sulfonamides First drugs available for systemic treatment of bacterial infection Inhibit the synthesis of folic acid (folate) More effective and less toxic drugs now available Mammalian cells do not manufacture their own folate (not affected as bacteria are affected) Primary use now: for urinary tract infection Other uses: nocardiosis, Chlamydia trachomatis, conjunction therapy for toxoplasmosis/malaria, ulcerative colitis Sulfonamides Adverse effects Hypersensitivity reactions: Stevens-Johnson syndrome Hematologic effects Kernicterus Renal damage from crystalluria Drug interactions Metabolism-related interactions Cross-hypersensitivity Fig. 88–2. Sites of action of sulfonamides and trimethoprim. Trimethoprim (Proloprim, Trimpex) Inhibits dihydrofolate reductase Uses Acute and uncomplicated urinary tract infections • Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae, Enterobacter, coagulase-negative Staphylococcus Adverse effects Hematologic effects Use in pregnancy and lactation Trimethoprim-Sulfamethoxazole Trimethoprim-sulfamethoxazole (TMP-SMZ) combo inhibits sequential steps in bacterial folic acid synthesis, making it much more powerful than TMP or SMZ alone Therapeutic uses Urinary tract infection, otitis media, bronchitis, Shigellosis, pneumonia by Pneumocystis jiroveci, Pneumocystis pneumonia, and GI infection Trimethoprim-Sulfamethoxazole Adverse effects Gastrointestinal • Nausea and vomiting Rash Hyperkalemia Hypersensitivity reactions (Stevens-Johnson syndrome) • Blood dyscrasias • Kernicterus • Renal damage: crystalluria
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