PRANDIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRANDIN (PRANDIN).
Repaglinide stimulates insulin secretion from pancreatic beta cells by binding to and closing ATP-sensitive potassium channels, leading to membrane depolarization and calcium influx.
| Metabolism | Primarily metabolized by CYP2C8 and CYP3A4 to inactive metabolites. |
| Excretion | Primarily hepatic metabolism via CYP2C8 and CYP3A4; metabolites excreted in bile (90%) and urine (10%). Less than 0.1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life: 1.0-1.5 hours. Clinically, due to rapid elimination, repaglinide requires dosing before each meal to control postprandial glucose. |
| Protein binding | >98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution (Vd): 31 L (approximately 0.44 L/kg based on 70 kg). Indicates extensive distribution into extravascular tissues. |
| Bioavailability | Oral bioavailability: 56% (under fasting conditions). Food intake does not significantly affect overall absorption but may delay time to peak concentration. |
| Onset of Action | Oral: Onset of insulin secretion occurs within 15-30 minutes following oral administration. |
| Duration of Action | Duration of action: 3-4 hours. Duration corresponds to prandial insulin release; dosing immediately before meals is recommended to cover postprandial glucose rise. |
0.5–4 mg orally 0–30 minutes before meals, typically 2–4 times daily. Maximum single dose: 4 mg. Maximum total daily dose: 16 mg.
| Dosage form | TABLET |
| Renal impairment | GFR 30–50 mL/min: initiate at 0.5 mg with meals; titrate cautiously. GFR <30 mL/min: not recommended due to increased risk of hypoglycemia. |
| Liver impairment | Child-Pugh Class A or B: no dose adjustment; use caution. Child-Pugh Class C: not studied; avoid use due to potential for reduced clearance. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | Initiate at 0.5 mg before meals; monitor renal function as elderly may have reduced GFR leading to increased hypoglycemia risk. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PRANDIN (PRANDIN).
| Breastfeeding | Unknown if excreted in human milk; M/P ratio not established. Caution advised; consider risk-benefit. |
| Teratogenic Risk | Insufficient human data; animal studies show no teratogenicity at clinically relevant doses. Risk cannot be excluded; avoid use in first trimester if possible. |
| Fetal Monitoring | Monitor maternal blood glucose closely; fetal surveillance as per standard high-risk pregnancy protocol. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Diabetic ketoacidosis with or without coma","Type 1 diabetes mellitus","Concomitant use with gemfibrozil","Known hypersensitivity to repaglinide or any excipients"]
| Precautions | ["Hypoglycemia","Cardiovascular events (possible increased risk)","Severe hepatic impairment","Hypersensitivity reactions","Macrovascular outcomes (no conclusive evidence)"] |
Loading safety data…
| Fertility Effects | No known significant impact on fertility in animal studies; no human data available. |