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sulfadiazine
Indications:
1) treatment of urinary tract infections & nocardiosis
2) prophylaxis for rheumatic fever
3) adjunctive treatment for toxoplasmosis
4) uncomplicated malaria
5) asymptomatic meningiococcal carriers
6) chorioretinitis [2]
Dosage:
1) Toxoplasma encephalitis in HIV patients
a) acute therapy:
1] sulfadiazine 1.0-1.5 g QID plus pyrimethamine 50- 100 mg/day for 6 weeks
2] folinic acid 5-10 mg QD to offset hematologic toxicity of pyrimethamine
b) suppressive therapy:
- sulfadiazine 2-4 g/day plus pyrimethamine 25 mg/day
2) congenital toxoplasmosis:
a) newborns & infants < 2 months:
1] 100 mg/kg//day divided every 6 hours
2] plus pyrimethamine 1 mg/kg/day
3] plus folinic acid 5 mg every 3 days
4] duration of therapy 6 months
b) children > 2 months: 20-50 mg/kg QID
Tabs: 500 mg
Pharmacokinetics:
1) well absorbed orally
2) distribution
a) widely distributed:
1] pleural, peritoneal, synovial & ocular fluids
2] total body water
3] readily diffuses into CSF
4] appears in breast milk
3) protein binding: 32-56%
4) time to peak serum concentration is within 3-6 hours
5) metabolized in the liver by N-acetylation
6) elimination 1/2life 10 hours
7) eliminated in the urine
a) 43-60% as unchanged drug
b) 15-40% as metabolites
Adverse effects:
1) common (> 10%)
- fever, itching, rash, photosensitivity, dizziness, headache, anorexia, nausea/vomiting, diarrhea
2) less common (1-10%)
- granulocytopenia, leukopenia, thrombocytopenia, aplastic anemia, hemolytic anemia, hepatitis, Lyell's syndrome, Stevens-Johnson syndrome
3) uncommon (< 1%)
- crsytalluria, hematuria, thyroid function disturbance, interstitial nephritis, serum sickness-like reaction, jaundice, acute nephropathy
Interactions
drug interactions
drug adverse effects (more general classes)
monitor with carbonic anhydrase inhibitors
Related
N5-formyltetrahydrofolate (folinic acid, citrovorum factor, Fusilev)
pyrimethamine (Daraprim)
toxoplasmosis
General
sulfanilamide
Properties
MISC-INFO: elimination route KIDNEY
LIVER
1/2life 10 HOURS
pregnancy-category B
D
protein-binding 32-56%
Database Correlations
PUBCHEM cid=
References
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Deprecated Reference
- Department of Veterans Affairs, VA National Formulary
Component-of
enrofloxacin/silver sulfadiazine/sulfadiazine
pyrimethamine/sulfadiazine
sulfadiazine/sulfamerazine/sulfamethazine
sulfadiazine/trimethoprim