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. |
| Molecular Weight | 300.2 |
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 | Avoid due to potential teratogenicity. Animal studies show adverse effects; no adequate human studies. |
| 2nd trimester | Use only if benefit outweighs risk. Limited data suggest possible fetal growth restriction. |
| 3rd trimester | Avoid near term due to risk of uterine contractions or premature labor. |
Clinical note
Comprehensive clinical and safety monograph for LABID (LABID).
| Placental transfer | Crosses placenta readily; fetal plasma concentrations reach 50-80% of maternal levels. |
| Breastfeeding | LABID is excreted in human milk in low concentrations. Monitor infant for sedation or hypotonia; consider alternative if infant is premature or has compromised renal function. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to LABIDSevere hepatic impairmentCurrent pregnancy with viable fetus in first trimester
| 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. |
| Food/Dietary | Take LABID with or without food. Avoid grapefruit juice as it may alter drug levels. Maintain a low-sodium diet as recommended for hypertension management. Limit alcohol intake to reduce orthostatic effects. |
Loading safety data…
| L3 (Moderately Safe) |
| 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 | 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. |
| Clinical Pearls | LABID (labetalol) is a combined alpha-1 and beta-adrenergic blocker. Monitor for orthostatic hypotension, especially during initial dosing or dose escalation. Titrate slowly to avoid profound bradycardia. Use with caution in patients with asthma or COPD due to beta blockade. In hypertensive emergencies, administer IV labetalol with continuous blood pressure monitoring. Avoid abrupt discontinuation to prevent rebound hypertension. |
| Patient Advice | Take this medication exactly as prescribed, usually twice daily. · Do not stop taking LABID suddenly without consulting your doctor, as this may cause a rapid increase in blood pressure. · Rise slowly from sitting or lying down to prevent dizziness or fainting. · Avoid alcohol, as it may increase side effects like dizziness or drowsiness. · Notify your doctor if you experience slow heartbeat, difficulty breathing, or swelling of the feet/ankles. |