LEVEMIR
Clinical safety rating
cautionComprehensive clinical and safety monograph for LEVEMIR (LEVEMIR).
Insulin detemir is a long-acting basal insulin analogue. It binds to insulin receptors, activating downstream signaling pathways that promote glucose uptake in muscle and adipose tissue, inhibit hepatic gluconeogenesis, and suppress lipolysis and proteolysis. The myristic acid side chain enables reversible binding to albumin, resulting in slow and predictable absorption with a prolonged duration of action.
| Metabolism | Insulin detemir is extensively bound to albumin (98-99%). Hepatic metabolism is not significant; it is degraded by proteolytic enzymes into inactive metabolites. |
| Excretion | Renal: minimal, as insulin is extensively reabsorbed and degraded in the proximal tubule; hepatic metabolism: via receptor-mediated endocytosis and degradation by insulin-degrading enzyme; biliary/fecal: negligible. |
| Half-life | Terminal elimination half-life: 13–18 hours (up to 24 hours with large doses); reflects prolonged absorption from subcutaneous depot due to dihexyl-deamination modification. |
| Protein binding | Bound to albumin (>98%); also binds to insulin receptors. |
| Volume of Distribution | 0.26–0.57 L/kg; reflects distribution primarily into extracellular fluid and tissues with high insulin receptor density. |
| Bioavailability | Subcutaneous: approximately 85–90%. |
| Onset of Action | Subcutaneous: 1–2 hours. |
| Duration of Action | Subcutaneous: up to 24 hours (dose-dependent); provides a relatively flat, peakless profile for basal insulin coverage. |
| Molecular Weight | 5916 |
Subcutaneous injection: 0.2 units/kg once daily or twice daily; usual total daily dose 0.5-1.0 units/kg. Adjust based on blood glucose levels.
| Dosage form | INJECTABLE |
| Renal impairment | No specific dose adjustment recommended based on GFR; monitor glucose closely in renal impairment due to increased risk of hypoglycemia. |
| Liver impairment | No specific Child-Pugh based dose adjustments; monitor glucose closely in hepatic impairment due to altered glucose metabolism. |
| Pediatric use | Children ≥2 years: 0.2-0.5 units/kg subcutaneously once daily or twice daily; titrate based on glucose monitoring. |
| Geriatric use | Initiate at lower doses (e.g., 0.1-0.2 units/kg once daily) to minimize hypoglycemia risk; titrate cautiously. |
| 1st trimester | Insulin detemir does not cross the placenta in significant amounts and is considered safe for use during the first trimester. No increased risk of malformations has been reported. |
| 2nd trimester | Insulin detemir is safe in the second trimester. Dose adjustments may be needed due to changing insulin requirements. |
| 3rd trimester | Insulin detemir is safe in the third trimester. Close monitoring of blood glucose is essential as insulin requirements increase. |
Clinical note
Comprehensive clinical and safety monograph for LEVEMIR (LEVEMIR).
| Placental transfer | Minimal to no placental transfer due to high molecular weight and protein binding. Transfer is less than 1% of maternal serum concentration. |
| Breastfeeding | Insulin detemir is a high molecular weight protein that is not expected to pass into breast milk in significant amounts. It is considered compatible with breastfeeding. However, nursing mothers may require dose adjustments. |
| Lactation Rating | L1 (Safe) |
| Teratogenic Risk | Insulin detemir (LEVEMIR) does not cross the placenta in significant amounts; no teratogenic effects in animal studies. In humans, poor glycemic control is associated with fetal risks, but insulin detemir itself is not considered teratogenic. Risk of maternal hypoglycemia and fetal harm if dosing is poorly managed. |
| Fetal Monitoring | Monitor blood glucose levels frequently during pregnancy and postpartum. Assess HbA1c every 1-3 months. Perform fetal monitoring with ultrasound for growth and well-being, as per standard diabetes pregnancy management. Watch for maternal hypoglycemia. |
| Fertility Effects | No known adverse effects on fertility. Optimal glycemic control improves fertility outcomes in diabetic women. |
■ FDA Black Box Warning
Never share a Levemir FlexPen, PenFill cartridge, or vial between patients, even if the needle is changed. Sharing poses a risk for transmission of blood-borne pathogens.
| Common Effects | Hypoglycemia low blood glucose level Injection site allergic reaction |
| Serious Effects |
HypoglycemiaHypersensitivity to insulin detemir or any of its excipients
| Precautions | Monitor for hypoglycemia, which may be severe and life-threatening, Accidental mix-ups between insulin products can occur; verify label before administration, Changes in insulin regimen should be made cautiously and under medical supervision, Patients with renal or hepatic impairment may be at higher risk for hypoglycemia, May cause fluid retention and worsening of heart failure when used with thiazolidinediones, Hypersensitivity reactions including anaphylaxis, rash, and urticaria may occur, Hypoglycemia and hypokalemia are potential adverse effects |
| Food/Dietary | No specific food interactions, but timing of meals should be consistent to align with insulin action. Avoid large fluctuations in carbohydrate intake without dose adjustment. Alcohol may increase risk of hypoglycemia. |
| Clinical Pearls | Levemir (insulin detemir) is a long-acting basal insulin analogue with a flat action profile lasting up to 24 hours. It has a lower risk of hypoglycemia compared to NPH insulin. Dose adjustments are needed in renal or hepatic impairment. Do not mix with other insulins in the same syringe. Onset is slower than glargine; administer once or twice daily at the same time each day. |
| Patient Advice | Inject subcutaneously into abdomen, thigh, or upper arm; rotate sites within the same region. · Never mix Levemir with other insulins in the same syringe. · Do not use if solution appears cloudy or thickened; it should be clear and colorless. · Store unused vials/penfills in refrigerator (2-8°C); in-use pens can be kept at room temperature below 30°C for up to 42 days. · Monitor blood glucose regularly and watch for signs of hypo- or hyperglycemia. · Do not change insulin type or dose without consulting your healthcare provider. · Discard needles after each use; never share pens or needles. |
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