SULF-15
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SULF-15 (SULF-15).
SULF-15 is a sulfonylurea that stimulates insulin secretion from pancreatic beta cells by blocking ATP-sensitive potassium channels (K_ATP), leading to cell membrane depolarization, calcium influx, and exocytosis of insulin.
| Metabolism | Primarily metabolized by CYP2C9 to active and inactive metabolites; hepatic and renal elimination. |
| Excretion | Renal excretion accounts for 60-70% of elimination as unchanged drug; biliary/fecal excretion accounts for 20-30% as metabolites and parent compound. |
| Half-life | Terminal elimination half-life is 12-15 hours in adults with normal renal function; prolonged to >30 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 85-90% bound to albumin. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 75-90%; Intramuscular: 100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 1-5 minutes; Intramuscular: 10-15 minutes. |
| Duration of Action | Oral: 6-12 hours; Intravenous: 4-8 hours; Intramuscular: 6-10 hours. Duration increases with higher doses and in renal impairment. |
150 mg orally twice daily for 14 days.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | CrCl >50 mL/min: no adjustment; CrCl 30-50 mL/min: 75 mg twice daily; CrCl <30 mL/min: 75 mg once daily; hemodialysis: 75 mg after each dialysis session. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: not recommended. |
| Pediatric use | For children 2-12 years: 2.5 mg/kg orally twice daily (max 150 mg per dose) for 14 days; for infants <2 years: not established. |
| Geriatric use | No specific dose adjustment based on age alone; use with caution due to age-related renal decline; follow renal adjustment guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SULF-15 (SULF-15).
| Breastfeeding | SULF-15 is excreted into human breast milk with an estimated milk-to-plasma ratio of 0.8. Due to potential for serious adverse reactions in nursing infants, including nephrotoxicity and kernicterus, breastfeeding is not recommended during treatment and for 2 weeks after the last dose. |
| Teratogenic Risk | SULF-15 is contraindicated in pregnancy due to demonstrated teratogenicity in animal studies. First trimester: high risk of neural tube defects and cardiovascular malformations. Second and third trimesters: risk of fetal nephrotoxicity and oligohydramnios. Avoid in women of childbearing potential unless effective contraception is used. |
■ FDA Black Box Warning
Increased risk of cardiovascular mortality compared to diet alone or diet plus insulin, as observed in the University Group Diabetes Program (UGDP) study.
| Serious Effects |
Type 1 diabetes mellitus, diabetic ketoacidosis, hypersensitivity to sulfonylureas, severe renal or hepatic impairment (e.g., eGFR <30 mL/min/1.73 m² or Child-Pugh Class C).
| Precautions | Hypoglycemia, especially in elderly or debilitated patients, renal or hepatic impairment, and in those using other hypoglycemic agents. May cause hemolytic anemia in G6PD deficiency. Weight gain. Increased cardiovascular risk. |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN) and liver enzymes monthly. Perform fetal ultrasound every 4 weeks to assess amniotic fluid volume and fetal growth. Monitor for signs of fetal distress with non-stress test or biophysical profile after 28 weeks gestation. |
| Fertility Effects | SULF-15 has been associated with reduced fertility in animal studies, including impaired spermatogenesis in males and ovulation disruption in females. In humans, reversible oligospermia has been reported. Women may experience menstrual irregularities. Contraception is recommended during therapy. |