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sulfadiazine

 

Classes: Sulfonamides

Dosing and uses of Sulfadiazine

 

Adult dosage forms and strengths

tablet

  • 500mg

 

Load

2-4 g PO

 

Maintenance

2-4 g/day divided 3-6x/day PO

 

Prophylaxis of Recurrent Rheumatic Fever

>30 kg: 1 g/day

<30 kg: 500 mg/day

 

Toxoplasmosis

Given with Pyrimethamine & Folinic Acid

1-1.5 g QID us. for 3-4 weeks

Prophylaxis (in patients with HIV): 0.5-1 g q6hr with pyrimethamine (25-75 mg/day PO) & folinic acid (10-25 mg/day PO)

 

Other Information

Asymptomatic meningococcal carriers: 1 g BID x2 days

Monitor: renal function, CBC

 

Other Indications & Uses

Burkholderia pseudomallei, Chlamydia trachomatis,Nocardia asteroides & brasiliensis, Mycobacterium smegmatis, Mycobacterium chelonae, Mycobacterium fortuitum

First Line:Mycobacterium smegmatis, Nocardia asteroides & brasiliensis

 

Pediatric dosage forms and strengths

tablet

  • 500mg

 

Load (>2 Months Old)

75 mg/kg PO Or

2 g/sq.meter PO

 

Maintenance (>2 Months Old)

150 mg/kg/day divided q4- 6hr PO, Or

4 g/sq. meter/day divided q4 -6hr PO

No more than 6 g/day

 

Toxoplasmosis

Given with pyrimethamine and folinic acid

100-200 mg/kg/day divided q6hr PO x3-4 weeks

Infants <2 months old: 25 mg/kg/day divided QID PO

Prophylaxis (in patients with HIV): 85-120 mg/kg/day divided BID, TID or QID with pyrimethamine (1 mg/kg or 15 mg/sq.meter daily-maximum dose 25 mg) & folinic acid (5 mg every third day)

 

Congenital Toxoplasmosis

Given with pyrimethamine and folinic acid

100 mg/kg/day divided q6hr PO x 12 months

 

Other Information

Prophylaxis of recurrent rheumatic fever: see Adult Dosing

Monitor: renal function, CBC

 

Sulfadiazine adverse (side) effects

>10%

Diarrhea (33%)

Headache (33%)

Reversible oligospermia (33%)

Anorexia

Gastric distress

Nausea

Photosensitivity

Vomiting

 

1-10%

Allergic reactions-rash

Aplastic anemia

Dizziness

Hypersensitivity

Itching

Thyroid fuction disturbance

Franulocytopenia

Thrombocytopenia

 

Frequency not defined

Lyell's syndrome

Sstevens Johnson syndrome

Rash

Fever

Granulocytopenia

Hemolytic anemia

Leukopenia

Hepatitis

Jaundice

Hematuria

Acute nephropathy

Intestinal nephritis

 

Warnings

Contraindications (additional)

Should not be used for group A beta-hemolytic strep infections

Documented megaloblastic or folate deficiency anemia, obstructive uropathy

 

Cautions (additional)

Drink 250 mL water w/ each dose & frequently throughout day while taking sulfadiazine

 

Adverse Drug Reactions

Lyell's syndrome, stevens Johnson syndrome, itching, rash, photosensitivity, thyroid function disturbance, anorexia, diarrhea, nausea, vomiting, dizziness, fever, headache, aplastic anemia, granulocytopenia, hemolytic anemia, leukopenia, thrombocytopenia, hepatitis, jaundice, hematuria, acute nephropathy, intestinal nephritis

 

Pregnancy and lactation

Pregnancy category: C

Lactation: enters breast milk; risk of kernicterus if infant <2 mo

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Sulfadiazine

Absorption: well absorbed

Distribution: sulfadiazine is distributed into most body tissues; appears to cross cell membranes freely; at a plasma concentration of 100 mcg/mL

Protein Bound: approximately 32-56%

Elimination: largely in urine; urinary concentrations usually are 10-25 times those attained in serum

 

Mechanism of action

Exerts bacteriostatic action through competitive antagonism with para-aminobenzoic acid (PABA). Microorganisms that require exogenous folic acid and do not synthesize folic acid are not susceptible to the action of sulfonamides