Insulin degludec

Summary

Insulin degludec (Tresiba) is an ultra-long-acting basal insulin analogue with a duration of action exceeding 42 hours and minimal peak activity. It is approved for glycemic control in adults and children with type 1 and type 2 diabetes mellitus. Its flat action profile reduces intraday glycemic variability and nocturnal hypoglycemia risk compared to insulin glargine.

Mechanism of Action

Binds to insulin receptors on muscle, fat, and liver cells to facilitate glucose uptake and suppress hepatic glucose production. Forms soluble multi-hexamers at the injection site that slowly dissociate, releasing monomers for prolonged absorption. Ultra-long duration of action (>42 hours) with a flat, stable pharmacokinetic profile.

Routes of Administration

Goals & Uses

• Cardiovascular safety in diabetesCardiovascularHigh
• Reduction of nocturnal hypoglycemiaSafety / TolerabilityHigh
• Glycemic control in type 2 diabetesMetabolicHigh
• Glycemic control in type 1 diabetesMetabolic / EndocrineHigh
• Flexible dosing schedulePatient AdherenceModerate

Contraindications

• Hypoglycemia (during active episode)MetabolicHigh
• Hypersensitivity to insulin degludec or excipientsImmunologicHigh

Adverse Effects

• HypokalemiaElectrolyteUncommon
• HypoglycemiaMetabolicCommonAbnormally low blood glucose
• Peripheral edemaFluid BalanceUncommonSwelling of the arms or legs
• Injection site reactionsLocalCommon
• Allergic/anaphylactic reactionsImmunologicalRare
• Weight gainMetabolicCommonIncrease in body weight

Drug Interactions

• Thiazolidinediones (e.g., pioglitazone)Moderate
• Beta-blockersModerate
• Antidiabetic agents (oral/injectable)Moderate
• AlcoholModerate
• CorticosteroidsModerate
• Fluoroquinolone antibioticsModerate

Population Constraints

• PregnancyReproductive SafetyRelative
• Hepatic impairmentOrgan FunctionRelative
• Renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative
• Pediatric patients < 1 yearAgeAbsolute

Regulatory Status

• European UnionApprovedApproved: Treatment of diabetes mellitus in adults, adolescents, and children ≥1 yearEMA approved January 2013; marketed as Tresiba.
• United StatesApprovedApproved: Type 1 diabetes mellitus in adults and pediatric patients ≥1 year, Type 2 diabetes mellitus in adultsFDA approved September 2015; U-100 and U-200 formulations available.
• United KingdomApprovedApproved: Treatment of diabetes mellitus in adults, adolescents, and children ≥1 yearApproved via EMA prior to Brexit; retained in UK market post-Brexit as Tresiba.

Approved by the FDA in September 2015 for adults with diabetes, and later extended to pediatric patients (1 year and older) with type 1 diabetes. Approved by EMA in 2013. Available in U-100 and U-200 formulations.

Evidence & Sources

No sources recorded yet.