Insulin glargine

Summary

Insulin glargine is a long-acting basal insulin analogue providing approximately 24-hour peakless glycemic control. It is used in the management of type 1 and type 2 diabetes mellitus in adults and pediatric patients. Available in standard (100 U/mL) and concentrated (300 U/mL) formulations.

Mechanism of Action

Insulin glargine is a recombinant human insulin analogue with substitutions (A21 asparagine replaced by glycine; two arginines added to B-chain C-terminus) that shift the isoelectric point, causing microprecipitation at physiological pH after subcutaneous injection, resulting in slow, prolonged, and relatively peakless absorption. It activates insulin receptors (IR-A and IR-B), stimulating glucose uptake in skeletal muscle and adipose tissue, suppressing hepatic glucose production, and inhibiting lipolysis.

Routes of Administration

Goals & Uses

• Weight management (relative)MetabolicModerate
• Reduction of hypoglycemia risk vs. NPH insulinSafety / TolerabilityHigh
• Glycemic control in type 1 diabetes mellitusEndocrine / MetabolicHigh
• Gestational diabetes / diabetes in pregnancyGlycemic ManagementModerate
• Glycemic control in type 2 diabetes mellitusEndocrine / MetabolicHigh

Contraindications

• IV or IM administrationRoute Of AdministrationHigh
• Hypoglycemic episodes (active)MetabolicHigh
• Hypersensitivity to insulin glargine or excipientsImmunologicalHigh

Adverse Effects

• Visual disturbances / retinopathy worseningOphthalmologicalUncommon
• HypoglycemiaMetabolicCommonAbnormally low blood glucose
• Peripheral edemaFluid BalanceUncommonSwelling of the arms or legs
• Injection site reactionsLocalCommon
• Allergic reactions / anaphylaxisImmunologicRare
• Weight gainMetabolicCommonIncrease in body weight

Drug Interactions

• Thiazolidinediones (e.g., pioglitazone)Moderate
• Beta-blockersModerate
• Oral antidiabetic agents (sulfonylureas, meglitinides)Moderate
• AlcoholModerate
• CorticosteroidsModerate
• Sympathomimetics (epinephrine, salbutamol)Low

Population Constraints

• PregnancyReproductive SafetyRelative
• Hepatic impairmentOrgan FunctionRelative
• Renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative
• Pediatric patients < 6 years (Toujeo 300 U/mL)AgeAbsolute

Regulatory Status

• European UnionApprovedApproved: Diabetes mellitus in adults, adolescents, and children aged 2 years and above (Lantus), Diabetes mellitus in adults (Toujeo)Lantus received EMA approval in 2000. Toujeo approved 2015. Multiple EMA-approved biosimilars available (e.g., Abasaglar, Semglee).
• United StatesApprovedApproved: Type 1 diabetes mellitus in adults and pediatric patients ≥6 years (Lantus), Type 2 diabetes mellitus in adults (Lantus, Toujeo), Type 1 diabetes in adults (Toujeo)Lantus approved April 2000; Toujeo approved February 2015; biosimilars Basaglar (2015) and Rezvoglar (2022) also approved. Multiple biosimilar applications under review.
• United KingdomApprovedApproved: Diabetes mellitus in adults, adolescents and children aged 2 years and above (Lantus), Diabetes mellitus in adults (Toujeo)Approved via MHRA; previously approved under EMA pre-Brexit. Biosimilars available on NHS. NICE guidance recommends use in appropriate patients.

First approved by the FDA in April 2000 (Lantus). A concentrated formulation (Toujeo, 300 U/mL) approved in 2015. Multiple biosimilars approved (e.g., Basaglar, Rezvoglar in the US). EMA approved Lantus in 2000; biosimilars followed. Considered a reference product for biosimilar development pathway.

Evidence & Sources

No sources recorded yet.