Introduction — significance?
First effective antimicrobials against pyogenic bacteria.
Sulphonamide core — structure?
Derived from sulphanilamide with N¹ and N⁴ substitutions.
N¹ substitution — role?
Affects solubility, pharmacokinetics.
N⁴ substitution — role?
Determines antibacterial activity.
Classification — basis?
Chemical structure and pharmacokinetics.
Prototype sulphonamide — example?
Sulfadiazine.
Spectrum — activity?
Bacteriostatic against gram-positive and negative bacteria.
Bacterial resistance — mechanism?
Increased PABA, reduced enzyme affinity, alternative pathways.
Mechanism — target enzyme?
Dihydropteroate synthase in folate synthesis.
Mode of action — process?
Competitive inhibition of PABA binding.
Bacteria unaffected?
Anaerobic bacteria resistant.
Urinary activity — significance?
Bactericidal concentrations in urine treat UTIs.
Pharmacokinetics — absorption?
Rapid, complete from GIT.
Metabolism — process?
Acetylation at N⁴ in liver.
Crystalluria — cause?
Precipitation of insoluble metabolites in urine.
Adverse effect — hypersensitivity?
Stevens-Johnson syndrome in long-acting sulphonamides.
Hemolysis risk — in?
G6PD deficiency.
Hepatitis — cause?
Drug-induced liver inflammation.
Uses — main application?
Urinary infections, topical burn treatment, ocular infections.
Cotrimoxazole — components?
Sulfamethoxazole and trimethoprim.
Trimethoprim — action?
Inhibits bacterial dihydrofolate reductase.
Synergism — effect?
Bactericidal by blocking sequential folate steps.
Spectrum — expanded?
Includes Salmonella typhi and others.
Current role —?
Limited; mainly in combination and topical applications.
Testez vos connaissances avec un QCM de 12 questions sur Sulphonamides: History, Chemistry, and Clinical Use.
1. What is the primary role or purpose of sulphonamides in antimicrobial therapy?
2. How should knowledge of sulphonamide pharmacokinetics influence clinical practice in administering these drugs?
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