METAGLIP
Clinical safety rating: caution
Comprehensive clinical and safety monograph for METAGLIP (METAGLIP).
Metformin decreases hepatic glucose production and intestinal absorption, and improves insulin sensitivity; glipizide stimulates insulin secretion from pancreatic beta cells by inhibiting ATP-sensitive potassium channels.
| Metabolism | Metformin is excreted unchanged in urine; glipizide is metabolized by CYP2C9 to inactive metabolites. |
| Excretion | Renal: 90-95% unchanged; biliary/fecal: <5% as metabolites |
| Half-life | Terminal elimination half-life: 12-15 hours; clinically, dosing adjustments required in renal impairment with CrCl <60 mL/min |
| Protein binding | 80-90%, primarily to albumin |
| Volume of Distribution | 0.5-0.8 L/kg; reflects distribution into total body water |
| Bioavailability | Oral: 85-95% (immediate-release); 70-80% (extended-release) |
| Onset of Action | Oral: 1-2 hours; peak effect in 4-8 hours |
| Duration of Action | 12-24 hours; may be prolonged in renal impairment |
| Brand Substitutes | Tenefit-M Forte Tablet SR, Dynaglipt-M Forte Tablet SR, Tenginow M 1000 Tablet SR, Gliptel-M 1000 Tablet SR, Tenlifine M 1000 SR Tablet |
Oral: Initial 2.5 mg/250 mg once daily with breakfast, titrate gradually to maximum 20 mg/2000 mg per day in divided doses twice daily.
| Dosage form | TABLET |
| Renal impairment | eGFR 45-59 mL/min: Maximum 10 mg/1000 mg per day; eGFR 30-44 mL/min: Maximum 5 mg/500 mg per day; eGFR <30 mL/min: Contraindicated. |
| Liver impairment | Child-Pugh Class A: Use with caution, maximum 10 mg/1000 mg per day; Child-Pugh Class B: Not recommended; Child-Pugh Class C: Contraindicated. |
| Pediatric use | Not recommended for pediatric patients under 18 years due to lack of safety and efficacy data. |
| Geriatric use | Initiate at 2.5 mg/250 mg once daily; avoid use if eGFR <45 mL/min; monitor for hypoglycemia and renal function; maximum 10 mg/1000 mg per day. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for METAGLIP (METAGLIP).
| Breastfeeding | Unknown if excreted in human milk. M/P ratio not available. Due to potential for hypoglycemia in infant, not recommended during breastfeeding. |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate studies, potential risk based on animal data (skeletal and visceral malformations at high doses). Second and third trimesters: Risk of neonatal hypoglycemia and macrosomia; consider maternal hyperglycemia risks. |
| Fetal Monitoring |
■ FDA Black Box Warning
Lactic acidosis with metformin accumulation; warn about renal impairment, hepatic disease, and concomitant medications.
| Serious Effects |
Renal disease or dysfunction (e.g., serum creatinine ≥1.5 mg/dL in males, ≥1.4 mg/dL in females, or abnormal creatinine clearance); acute or chronic metabolic acidosis; concomitant use with bosentan; hypersensitivity to metformin or glipizide.
| Precautions | Lactic acidosis (metformin); hypoglycemia (glipizide); renal impairment; hepatic impairment; vitamin B12 deficiency; acute alcohol intake; surgery; radiological studies with iodinated contrast. |
Loading safety data…
| Monitor maternal blood glucose levels, HbA1c, and fetal growth via ultrasound. Assess for fetal macrosomia and neonatal hypoglycemia postpartum. |
| Fertility Effects | No human data; animal studies at high doses showed impaired fertility (prolonged estrous cycles, reduced pregnancy rate). Clinical relevance unknown. |