Trade Names:Sulfadiazine- Tablets 500 mg
Exerts bacteriostatic action by competing with PABA, an essential component in folic acid synthesis, therefore preventing synthesis of folic acid needed by bacteria for growth.
Absorbed rapidly from the GI tract. A peak level of 6.04 mg per 100 mL is reached 4 h after a single 2 g oral dose (4.65 mg per 100 mL is free or active drug).
Protein binding is 38% to 48%. Diffuses into CSF, reaching concentrations of 32% to 65% of blood levels.
At least 1 acetylated form.
Excreted primarily in the urine, reaching concentrations that are 10 to 25 times higher then serum levels. About 10% of a single oral dose is excreted in the first 6 h, 50% within 24 h, and 60% to 85% in 48 to 72 h. 15% to 40% is excreted in the acetyl form.
Treatment of chancroid, trachoma, inclusion conjunctivitis, nocardiosis, UTI, toxoplasmosis encephalitis, malaria, meningococcal meningitis, acute otitis media; prophylaxis against meningococcal meningitis and recurrences of rheumatic fevers; with streptomycin as adjunctive therapy for Haemophilus influenza meningitis.
Hypersensitivity to sulfonamides; infants less than 2 mo of age (except as adjunctive therapy with pyrimethamine in treating congenital toxoplasmosis); pregnancy at term; nursing period.
PO 2 to 4 g, divided into 3 to 6 doses, every 24 h.Children older than 2 mo of age
PO Initially, one-half the 24-h dose.Maintenance
150 mg/kg or 4 g/m 2 , divided into 4 to 6 doses, every 24 h.Rheumatic Fever Prophylaxis
Under 30 kg give 500 mg every 24 h; over 30 kg give 1 g every 24 h.
Store tablets at ambient room temperature (59° to 86°F).
Effects of these agents may be enhanced by sulfadiazine.Indomethacin, probenecid, salicylates
May increase free sulfadiazine plasma levels, increasing the pharmacologic and adverse effects.
None well documented.
Headache; peripheral neuritis; mental depression; convulsions; ataxia; hallucinations; vertigo; insomnia.
Nausea; emesis; abdominal pain; diarrhea; anorexia; pancreatitis; stomatitis.
Crystalluria; stone formation; toxic nephrosis with oliguria and anuria; periarteritis nodosa; lupus erythematosus phenomenon.
Agranulocytosis; aplastic anemia; thrombocytopenia; leukopenia; hemolytic anemia; purpura; hypoprothrombinemia; methemoglobinemia.
Allergic reactions including erythema multiforme (Stevens-Johnson syndrome), generalized skin eruptions, toxic epidermal necrolysis, urticaria, serum sickness, pruritus, exfoliative dermatitis, anaphylactoid reactions, periorbital edema, conjunctival and scleral injection, photosensitization, arthralgia, allergic myocarditis, drug fever, and chills.
Category C .
Excreted in breast milk; use is contraindicated.
Contraindicated in children under 2 mo of age (except as adjunctive therapy with pyrimethamine in treating toxoplasmosis).
Use with caution in patients with renal or hepatic function impairment and those with severe allergy or bronchial asthma.
May occur if adequate fluid intake is not maintained.
Do not use drug for this infection.
May occur in G-6-PD-deficient individuals.
Severe reactions, including deaths, have been associated with hypersensitivity reactions, agranulocytosis, aplastic anemia, other blood dyscrasias, and renal and hepatic damage.
Has chemical similarities to some goitrogens, diuretics (eg, acetazolamide, thiazides), and oral hypoglycemic agents. Goiter production, diuresis, and hypoglycemia have occurred rarely in patients receiving sulfonamides; cross-sensitivity may exist.
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