DIASONE SODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DIASONE SODIUM (DIASONE SODIUM).
Diasone sodium is a sulfone antibiotic that inhibits bacterial dihydropteroate synthase, thereby blocking folate synthesis and bacterial growth.
| Metabolism | Hepatic metabolism via acetylation and glucuronidation |
| Excretion | Renal: 70-80% as unchanged drug and metabolites; biliary/fecal: 20-30%. |
| Half-life | Terminal elimination half-life is 20-30 hours; in renal impairment, may extend to 40-60 hours, requiring dose adjustment. |
| Protein binding | 90-95% bound primarily to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.2-0.3 L/kg, indicating distribution primarily in extracellular fluid; increased in edema or third-spacing. |
| Bioavailability | Oral: 75-85% with significant first-pass metabolism; intravenous: 100%. |
| Onset of Action | Oral: 2-4 hours after single dose; intravenous: immediate (minutes). |
| Duration of Action | Oral: 6-12 hours; intravenous: 4-8 hours or shorter due to rapid redistribution. |
100-200 mg orally once daily, increased by 100 mg every 2-4 weeks up to 400 mg daily if tolerated. Usual maintenance dose is 100-200 mg daily.
| Dosage form | TABLET, DELAYED RELEASE |
| Renal impairment | No specific dose adjustment recommended; use with caution in severe renal impairment (eGFR <30 mL/min) due to potential accumulation. Monitor for adverse effects. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose by 50%. Child-Pugh C: Contraindicated. |
| Pediatric use | Not recommended for children under 12 years due to lack of safety data. For children ≥12 years, initiate at 100 mg orally daily, titrate based on response and tolerability. |
| Geriatric use | Start at lower end of dosing range (100 mg orally daily). Monitor for dizziness, hypotension, and anticholinergic effects. Caution with simultaneous use of other medications due to increased risk of drug interactions. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DIASONE SODIUM (DIASONE SODIUM).
| Breastfeeding | Distributed into breast milk; M/P ratio not established. Potential for hemolytic anemia and methemoglobinemia in nursing infants. Contraindicated in breastfeeding due to serious adverse effects. |
| Teratogenic Risk | First trimester: Crosses placenta; associated with congenital malformations including cardiovascular and neural tube defects based on animal studies and limited human data. Second and third trimesters: Risk of neonatal hemolytic anemia, methemoglobinemia, and kernicterus due to sulfone accumulation. Avoid in pregnancy unless benefit outweighs risk. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to sulfones; severe hepatic impairment; G6PD deficiency (relative).
| Precautions | May cause hemolytic anemia in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency; monitor for hypersensitivity reactions, hepatic toxicity, and peripheral neuropathy. |
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| Fetal Monitoring |
| Maternal: Complete blood count (CBC) with differential, liver function tests, and methemoglobin levels at baseline and regularly; monitor for hemolysis and hypersensitivity. Fetal/neonatal: Ultrasound for malformations; neonatal monitoring for jaundice, hemolytic anemia, and methemoglobinemia. |
| Fertility Effects | Limited data; no evidence of impaired fertility in animal studies. Potential for oligospermia or menstrual irregularities based on structural analog effects. |