HES 033: General Pharmacology - Sulfonamides
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Questions and Answers

What must happen to the dosage of sulfonamide in patients with renal failure?

  • It must be reduced. (correct)
  • It must remain unchanged.
  • It must be increased for better efficacy.
  • It must be discontinued.
  • Which drug combination is the first-line treatment for acute toxoplasmosis?

  • Dihydrofolate reductase alone
  • Sulfadiazine and pyrimethamine (correct)
  • Sulfadoxine and pyrimethamine
  • TMP-SMZ
  • Which of the following infections is TMP-SMZ primarily indicated for?

  • Pneumocystis jiroveci pneumonia (correct)
  • Influenza
  • Tuberculosis
  • Bacterial meningitis
  • What defines sulfadoxine in the context of malaria treatment?

    <p>It is a long-acting sulfonamide.</p> Signup and view all the answers

    What is the role of dihydrofolate reductase in the context of pyrimethamine treatment?

    <p>It is inhibited by pyrimethamine.</p> Signup and view all the answers

    What conditions can TMP-SMZ be used to treat, besides pneumonia?

    <p>Toxoplasmosis and nocardiosis</p> Signup and view all the answers

    In treating malaria, what is the combination of sulfadoxine and pyrimethamine commonly referred to?

    <p>Fansidar</p> Signup and view all the answers

    Which of the following conditions requires the use of sulfonamide as a second-line treatment?

    <p>Malaria</p> Signup and view all the answers

    What is the primary mechanism by which sulfonamides exert their antibacterial effect?

    <p>They inhibit dihydropteroate synthase.</p> Signup and view all the answers

    Which feature is true about the solubility of sulfonamides?

    <p>They are more soluble at alkaline pH.</p> Signup and view all the answers

    What is the effect of bacterial mutations on the effectiveness of sulfonamides?

    <p>They can lead to PABA overproduction.</p> Signup and view all the answers

    Which of the following categories includes sulfonamides that can be absorbed orally?

    <p>Oral absorbable sulfonamides</p> Signup and view all the answers

    Which of the following combinations provides synergistic activity with sulfonamides?

    <p>Sulfonamide and a dihydrofolate reductase inhibitor</p> Signup and view all the answers

    How does the protein binding of sulfonamides vary?

    <p>It can range from 20% to over 90%.</p> Signup and view all the answers

    What type of bacteria do sulfonamides primarily inhibit?

    <p>Both gram-positive and gram-negative bacteria</p> Signup and view all the answers

    Which of the following statements is true regarding the action of sulfonamides?

    <p>They are bacteriostatic.</p> Signup and view all the answers

    What is a primary adverse effect associated with sulfonamides that can lead to obstruction in the urinary tract?

    <p>Crystalluria</p> Signup and view all the answers

    Which topical sulfonamide is specifically mentioned as being effective for bacterial conjunctivitis?

    <p>Sodium sulfacetamide</p> Signup and view all the answers

    Which condition can be triggered by the absorption of mafenide acetate from burn sites?

    <p>Stevens-Johnson syndrome</p> Signup and view all the answers

    What complication may occur due to the use of sulfonamides in pregnant patients?

    <p>Kernicterus</p> Signup and view all the answers

    Which of the following sulfonamides may slow the healing of burn wounds?

    <p>Silver sulfadiazine</p> Signup and view all the answers

    What treatment is suggested for crystalluria caused by sulfonamides?

    <p>Administer sodium bicarbonate to alkalinize urine</p> Signup and view all the answers

    Which group of patients is at risk for hemolytic reactions when taking sulfonamides?

    <p>Patients with glucose-6-phosphate dehydrogenase deficiency</p> Signup and view all the answers

    Which of the following is a sulfonamide that is used in treating inflammatory bowel disorders?

    <p>Sulfasalazine</p> Signup and view all the answers

    Study Notes

    Sulfonamides Overview

    • Structural analogs of p-aminobenzoic acid (PABA), influencing their pharmacological properties.
    • Sulfonamides are synthesized by modifying the sulfanilamide nucleus with various substituents.
    • More soluble at alkaline pH; prepared as sodium salts for intravenous use.

    Mechanism of Action

    • Act as competitive inhibitors of dihydropteroate synthase, blocking folate synthesis crucial for nucleic acid production.
    • Resistance arises from bacterial mutations leading to PABA overproduction, changes in target enzyme affinity, or impaired drug permeability.

    Classification of Sulfonamides

    • Oral absorbable sulfonamides: Absorbed in the stomach and small intestine; distributed widely including CNS.
    • Non-absorbable and topical agents: Include treatments for localized infections.

    Clinical Applications

    • Fixed-drug combination TMP-SMZ is effective against Pneumocystis jiroveci pneumonia and other infections.
    • First-line treatment for acute toxoplasmosis: sulfadiazine with pyrimethamine.
    • Long-acting sulfadoxine combined with pyrimethamine is a second-line choice for malaria.
    • Sulfasalazine is used for inflammatory bowel disorders, while topical agents like sodium sulfacetamide treat conjunctivitis.

    Adverse Effects

    • Risk of crystalluria, hematuria, or renal obstruction due to precipitate formation.
    • Potential for hemolytic reactions in G6-PD deficiency patients.
    • Increased risk of kernicterus in newborns if taken late in pregnancy.

    Notable Sulfonamide Drugs

    • Sulfisoxazole, Sulfamethizole, Sulfacytine, Sulfamethoxazole, Sulfasalazine, Sodium Sulfacetamide, Mafenide, Sulfadiazine, Sulfapyridine, Sulfadoxine.

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    Description

    This quiz covers the fundamentals of sulfonamides and their pharmacological properties within the context of general pharmacology for third-year optometry students. It will explore their structural similarities to PABA, as well as the classification and characteristics of antimycobacterial and antileprotic drugs. Enhance your understanding of these essential pharmaceutical compounds.

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