STARLIX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for STARLIX (STARLIX).
STARLIX (nateglinide) is an oral antidiabetic agent that stimulates insulin secretion from the pancreatic beta cells by binding to the sulfonylurea receptor (SUR1) on the ATP-sensitive potassium channels, causing depolarization, calcium influx, and exocytosis of insulin. It acts rapidly and has a short duration of action, primarily affecting postprandial glucose levels.
| Metabolism | Primarily metabolized by the liver via cytochrome P450 isoenzymes (CYP2C9 and CYP3A4) to inactive metabolites. Approximately 16% of the dose is excreted unchanged in the urine. |
| Excretion | Primarily hepatic metabolism via CYP2C9 and CYP3A4; ~92% excreted in feces as metabolites, ~8% in urine as metabolites; less than 1% excreted unchanged. |
| Half-life | 1-1.5 hours; short half-life supports preprandial dosing to control postprandial hyperglycemia; no accumulation with repeated dosing. |
| Protein binding | >98% bound to albumin; high binding may increase risk of hypoglycemia in hypoalbuminemic states. |
| Volume of Distribution | 0.35 L/kg; relatively small Vd indicates limited extravascular distribution, likely confined to plasma and interstitial fluid. |
| Bioavailability | Oral: ~60-70%; rapid absorption with Tmax ~1 hour; food may delay absorption but does not significantly affect extent. |
| Onset of Action | Oral: ~30 minutes; peak plasma concentrations achieved within 1 hour. |
| Duration of Action | 4-6 hours; administered 2-4 times daily before meals to cover postprandial glucose excursions. |
| Action Class | Anti-Ulcerants |
| Brand Substitutes | Ralfat Syrup, Sucratas Syrup, Dufcid Syrup, Piralfate Syrup, Scorcid 1000mg Syrup |
120 mg orally three times daily, taken 1 to 30 minutes before meals.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not recommended for use in patients with eGFR < 30 mL/min/1.73m². |
| Liver impairment | Contraindicated in patients with Child-Pugh class B or C hepatic impairment. No specific dose adjustment for Child-Pugh class A. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dosing. |
| Geriatric use | No specific dose adjustment required, but consider lower initial doses due to increased risk of hypoglycemia and reduced renal function in elderly. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for STARLIX (STARLIX).
| Breastfeeding | No published data on nateglinide in human breast milk. The molecular weight (317 g/mol) suggests potential for excretion. If used during breastfeeding, the relative infant dose is unknown; however, low oral bioavailability in nursing infants may limit systemic effects. Monitor infant for signs of hypoglycemia. M/P ratio: not available. |
| Teratogenic Risk | FDA Pregnancy Category C. In animal reproduction studies, no structural anomalies were observed at exposures up to 200 times the maximum recommended human dose. However, fetal growth retardation and delayed ossification occurred at maternally toxic doses. There are no adequate and well-controlled studies in pregnant women. Use in the first trimester: limited data, theoretical risk based on known antihyperglycemic effects may increase risk of hypoglycemia in the fetus. Second and third trimesters: can cause neonatal hypoglycemia if maternal hyperglycemia is not controlled; avoid use unless benefits outweigh risks. |
■ FDA Black Box Warning
None
| Serious Effects |
["Type 1 diabetes mellitus","Diabetic ketoacidosis","Severe hepatic impairment"]
| Precautions | ["Hypoglycemia: may occur, especially in patients with renal impairment, elderly, or those not eating regularly.","Loss of glycemic control: possible with stress, fever, infection, or surgery.","Hepatic impairment: use with caution in patients with mild-to-moderate liver disease; contraindicated in severe hepatic impairment.","Macrovascular outcomes: no conclusive evidence of benefit."] |
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| Fetal Monitoring | Monitor maternal blood glucose levels frequently (e.g., fasting and postprandial). Assess HbA1c monthly. During labor and delivery, monitor blood glucose at least hourly to prevent neonatal hypoglycemia. For the fetus, monitor growth and amniotic fluid volume via ultrasound as clinically indicated (e.g., if diabetes is poorly controlled). |
| Fertility Effects | In animal studies, nateglinide did not impair fertility at doses up to 1000 mg/kg/day (6 times human exposure). No human data on fertility effects; however, poorly controlled diabetes is associated with menstrual irregularities and impaired fertility. The drug itself is not expected to adversely affect fertility. |