Insulin glulisine

Summary

Insulin glulisine is a rapid-acting recombinant insulin analogue used to control postprandial blood glucose in adults and children with type 1 or type 2 diabetes mellitus. It has a faster onset and shorter duration of action than regular human insulin, allowing administration close to meals.

Mechanism of Action

Binds to insulin receptors on muscle, fat, and liver cells, stimulating glucose uptake and inhibiting hepatic glucose production. Substitution of asparagine at B3 with lysine and lysine at B29 with glutamic acid reduces self-aggregation, enabling faster absorption and onset compared to regular insulin.

Routes of Administration

Goals & Uses

• Type 1 diabetes managementEndocrine/metabolicHigh
• Type 2 diabetes managementEndocrine / MetabolicHigh
• HbA1c reductionGlycemic ManagementHigh
• Continuous subcutaneous insulin infusion (CSII)Delivery OptimizationModerate
• Postprandial glucose controlGlycemic ManagementHigh

Contraindications

• Hypersensitivity to insulin glulisine or excipientsImmunologicHigh
• HypoglycemiaMetabolicHigh

Adverse Effects

• EdemaFluid BalanceUncommonSwelling from fluid retention
• HypokalemiaElectrolyteUncommon
• HypoglycemiaMetabolicCommonAbnormally low blood glucose
• Allergic reactionsImmunologicalRare
• Injection site reactionsLocalCommon
• Weight gainMetabolicCommonIncrease in body weight

Drug Interactions

• Thiazolidinediones (e.g., pioglitazone)Moderate
• Beta-blockersModerate
• AlcoholModerate
• Sympathomimetics (e.g., epinephrine, salbutamol)Moderate
• CorticosteroidsModerate
• ACE inhibitorsLow

Population Constraints

• PregnancyReproductive SafetyRelative
• Hepatic impairmentOrgan FunctionRelative
• Renal impairmentOrgan ImpairmentRelative
• Elderly patientsAgeRelative
• Pediatric patients under 4 yearsAgeRelative

Regulatory Status

• European UnionApprovedApproved: Treatment of diabetes mellitus in adults, adolescents and children aged 6 years and aboveEMA approval 2004; Apidra marketed by Sanofi across EU member states
• United StatesApprovedApproved: Type 1 diabetes mellitus in adults and pediatric patients aged ≥4 years, Type 2 diabetes mellitus in adultsFDA approved April 2004; NDA 021629; available as Apidra (100 units/mL solution)
• United KingdomApprovedApproved: Treatment of diabetes mellitus in adults and children aged 6 years and aboveApproved via MHRA; retained post-Brexit; available on NHS prescription

Approved by the FDA in 2004 and by the EMA. Marketed under the brand name Apidra. Indicated for subcutaneous injection and continuous subcutaneous infusion (insulin pump use). Not approved for intravenous use outside of controlled clinical settings.

Evidence & Sources

No sources recorded yet.