LABID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LABID (LABID).
LABID is a fixed-dose combination of metformin (biguanide) and glipizide (sulfonylurea). Metformin primarily decreases hepatic gluconeogenesis, reduces intestinal glucose absorption, and improves insulin sensitivity via AMPK activation. Glipizide stimulates insulin secretion from pancreatic beta-cells by blocking ATP-sensitive potassium channels, leading to membrane depolarization and calcium influx.
| Metabolism | Metformin is excreted unchanged in urine; not metabolized. Glipizide is extensively metabolized in the liver via CYP2C9, with metabolites having minimal hypoglycemic activity. |
| Excretion | Renal: 70–80% unchanged; fecal: 15–20% (biliary); metabolism accounts for <10%. |
| Half-life | 8–12 hours in healthy adults; prolonged to 24–48 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 55–65% primarily to albumin; binding is saturable at high concentrations. |
| Volume of Distribution | 1.2–1.8 L/kg; indicates extensive tissue distribution (e.g., liver, kidney). |
| Bioavailability | Oral: 90–95% (high first-pass metabolism negligible); IM: ~100%. |
| Onset of Action | Oral: 1–2 hours; IV: 5–15 minutes; IM: 30–60 minutes. |
| Duration of Action | Oral: 8–12 hours; IV: 6–8 hours; clinical effect correlates with free drug concentration. |
400 mg orally twice daily.
| Dosage form | TABLET, EXTENDED RELEASE |
| Renal impairment | GFR 30-50 mL/min: 200 mg twice daily; GFR <30 mL/min: 200 mg once daily; hemodialysis: 200 mg post-dialysis. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 200 mg twice daily; Child-Pugh C: 200 mg once daily. |
| Pediatric use | 6-11 years: 10 mg/kg twice daily (max 400 mg/day); 12-17 years: 400 mg twice daily. |
| Geriatric use | No specific dose adjustment, but monitor renal function due to age-related clearance decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LABID (LABID).
| Breastfeeding | Limited data; M/P ratio unknown. Avoid breastfeeding due to potential for adverse effects in the infant, including renal impairment and electrolyte disturbances. |
| Teratogenic Risk | First trimester: Increased risk of neural tube defects and cardiovascular malformations. Second and third trimesters: Risk of fetal renal impairment, oligohydramnios, and premature closure of ductus arteriosus. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Severe renal impairment (eGFR < 30 mL/min/1.73 m²)","Acute or chronic metabolic acidosis, including diabetic ketoacidosis","Hypersensitivity to metformin, glipizide, or sulfonamide derivatives (cross-sensitivity)","Acute condition with risk of renal dysfunction (e.g., dehydration, severe infection, shock)","Intravascular administration of iodinated contrast agents (discontinue temporarily)"]
| Precautions | ["Lactic acidosis: Rare but serious; risk increased with renal impairment, acute conditions (e.g., sepsis, dehydration), and concomitant use of iodinated contrast agents.","Hypoglycemia: Particularly with glipizide; risk increased with skipped meals, excessive exercise, alcohol, renal/hepatic impairment, and debilitated patients.","Gastrointestinal effects: Metformin common (diarrhea, nausea, vomiting); titrate dose slowly to reduce.","Vitamin B12 deficiency: Long-term metformin use may decrease B12 absorption; monitor in at-risk patients.","Cardiovascular risk: Sulfonylureas may be associated with increased CV mortality; use cautiously in patients with ischemic heart disease."] |
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| Monitor maternal blood pressure, renal function, and electrolytes. Fetal ultrasound for growth, amniotic fluid volume, and ductus arteriosus patency every 2-4 weeks after 20 weeks gestation. |
| Fertility Effects | May impair fertility in females by disrupting ovarian function; in males, may affect spermatogenesis. Effects are reversible upon discontinuation. |