HUMALOG
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HUMALOG (HUMALOG).
Insulin lispro is a rapid-acting insulin analog that lowers blood glucose by binding to insulin receptors on skeletal muscle and adipocytes, leading to increased glucose uptake and reduced hepatic glucose production.
| Metabolism | Insulin lispro is metabolized primarily by insulin-degrading enzyme (IDE) in the liver, kidney, and peripheral tissues. The exact metabolic pathway is similar to regular human insulin. |
| Excretion | Renal: 60-80% as unchanged drug; biliary/fecal: minor (<10%). |
| Half-life | Subcutaneous: 0.5-1.0 hour (insulin lispro); longer with renal impairment (up to 1.5-3 hours). |
| Protein binding | ~55% bound to albumin (insulin-specific binding proteins, negligible). |
| Volume of Distribution | 0.3-0.5 L/kg (primarily in extracellular fluid). |
| Bioavailability | Subcutaneous: 55-75% (complete but variable due to local degradation). |
| Onset of Action | Subcutaneous: 15-30 minutes; Intravenous: <5 minutes. |
| Duration of Action | Subcutaneous: 3-5 hours (rapid-acting); dose-dependent, up to 6 hours with higher doses. |
Subcutaneous injection: 0.2-1.0 units/kg/day divided into 3 or more doses, given within 15 minutes before or immediately after a meal. Typical total daily dose range 0.5-1.0 units/kg/day.
| Dosage form | INJECTABLE |
| Renal impairment | For GFR <30 mL/min: reduce starting dose by 25-50% and monitor glucose closely; no specific adjustment for GFR 30-89 mL/min. |
| Liver impairment | For Child-Pugh Class B or C: reduce starting dose by 25-50% and titrate slowly due to increased risk of hypoglycemia. |
| Pediatric use | For children <18 years: 0.1-0.2 units/kg/dose subcutaneously within 15 minutes of meals; total daily dose 0.5-1.0 units/kg/day in multiple doses. |
| Geriatric use | Initiate at lower doses (e.g., 0.2-0.4 units/kg/day) with cautious titration to avoid hypoglycemia; monitor renal function and cognitive status. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HUMALOG (HUMALOG).
| Breastfeeding | Insulin lispro is excreted into breast milk in negligible amounts and is not orally bioavailable to the infant. It is considered compatible with breastfeeding. No specific M/P ratio is available; endogenous insulin M/P ratio is <1. |
| Teratogenic Risk | Insulin lispro (Humalog) does not cross the placenta in significant amounts. No increased risk of major birth defects or miscarriage has been observed with use during pregnancy. Poorly controlled diabetes during pregnancy increases fetal risks including congenital anomalies (first trimester), macrosomia, and neonatal hypoglycemia. |
■ FDA Black Box Warning
Humalog should not be used in patients with hypoglycemia. Changes in insulin strength, manufacturer, type, or method of administration should be made under close medical supervision, as changes may increase the risk of hypoglycemia or hyperglycemia.
| Common Effects | Hypoglycemia low blood glucose level |
| Serious Effects |
["Hypersensitivity to insulin lispro or any of its excipients","During episodes of hypoglycemia"]
| Precautions | ["Hypoglycemia is the most common adverse reaction and can be life-threatening","Hypoglycemia due to insulin lispro may be more severe in patients with renal impairment, hepatic impairment, or in elderly patients","Changes in insulin regimen can lead to hyperglycemia or hypoglycemia","Patients with diabetes may experience diabetic ketoacidosis if insulin is withheld","Concomitant use with thiazolidinediones may cause fluid retention and heart failure","Risk of injection site reactions and lipodystrophy","Hypersensitivity reactions may occur"] |
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| Fetal Monitoring |
| Monitor blood glucose levels frequently. HbA1c every 1-2 months. Fetal ultrasound for growth and anatomy. Assess for maternal hypoglycemia and hyperglycemia. Monitor for signs of preterm labor and preeclampsia. |
| Fertility Effects | No known adverse effects on fertility. Proper glycemic control may normalize menstrual cycles and improve fertility in women with diabetes. |