Sulfadiazine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

France: Adiazine; Germany: Sulfadiazin; Greece: Adiazine, Sulfadiazina; Italy: Sulfad; Malta: Sulfadiazine; Portugal: Labdiazina; Spain: Sulfadiazina; UK: Sulfadiazine.

North America

USA: Sulfadiazine.

Latin America

Argentina: Sulfadiazina; Brazil: Siglós, Suladrin, Sulfaderm.

Asia

Japan: Geben, Theradia.

Drug combinations

Chemistry

Sulfadiazine: C~10~H~10~N~4~O~2~S. Mw: 250.28. (1) Benzenesulfonamide, 4-amino-N-2-pyrimidinyl-; (2) N^1^-2-Pyrimidinylsulfanilamide. CAS-68-35-9.

Pharmacologic Category

Antibacterials; Sulfonamides. (ATC-Code: J01EC02).

Mechanism of action

Competitively inhibits bacterial synthesis of folic acid (pteroylglutamic acid) from aminobenzoic acid. Bacteriostatic in action. Inhibits only microorganisms which synthesize their own folic acid. Animal cells and bacteria capable of utilizing folic acid precursors or preformed folic acid are resistant to sulfonamides.

Therapeutic use

Urinary tract infections and nocardiosis. Toxoplasmosis. Uncomplicated attack of malaria.

Pregnancy and lactiation implications

Contraindicated in pregnant women at term. May increase risk of neonatal hyperbilirubinemia and kernicterus. Distributed into milk. Contraindicated in nursing women.

Unlabeled use

Rheumatic fever prophylaxis.

Contraindications

Hypersensitivity to sulfonamides or other chemically related drugs (e.g. sulfonylureas, thiazides). Infants <2 months of age (except as adjunctive therapy with pyrimethamine in treatment of congenital toxoplasmosis). Pregnancy at term. Nursing women. Porphyria.

Warnings and precautions

Fatalities associated with severe reactions including agranulocytosis, aplastic anemia and other blood dyscrasias occurred. Fatalities associated with severe reactions including Stevens-Johnson syndrome and toxic epidermal necrolysis occurred. Fatalities associated with hepatic necrosis occurred. Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). Risk of cross-reaction exists in allergy to any of these compounds (avoid use when previous reaction severe). Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea and pseudomembranous colitis. Use with caution in G6PD deficiency (hemolysis may occur), and in hepatic/renal impairment. Fluid intake should be maintained ≥1500 mL/day, or administer sodium bicarbonate to keep urine alkaline (more likely to cause crystalluria as it is less soluble than other sulfonamides).

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