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Insulin Glargine

Insulin & Glucose Regulation
LantusToujeoBasaglarLong-acting insulin

Overview

Insulin glargine is a synthetic long-acting insulin analog used primarily in the management of diabetes mellitus. It is produced through recombinant DNA technology in non-pathogenic strains of Escherichia coli. Chemically, it belongs to the class of peptide hormones, specifically designed to mimic the action of endogenous insulin with modifications that prolong its duration of action. Researchers have developed insulin glargine to provide a more stable and prolonged glucose-lowering effect compared to regular human insulin.

The primary physiological role of insulin glargine is to regulate blood glucose levels by facilitating cellular uptake of glucose, particularly in muscle and adipose tissue, and by inhibiting hepatic glucose production. Research areas include its efficacy in reducing HbA1c levels, its impact on hypoglycemia risk, and its role in long-term diabetes management. Studies have also explored its use in combination with other antidiabetic agents to optimize glycemic control.

Insulin glargine acts on the insulin receptor, a transmembrane receptor that triggers the insulin signaling pathway. Upon binding, it activates the receptor's intrinsic tyrosine kinase activity, leading to a cascade of phosphorylation events that promote glucose uptake and metabolism. This pathway involves key intermediates such as insulin receptor substrates (IRS) and phosphoinositide 3-kinase (PI3K), ultimately enhancing glucose transporter type 4 (GLUT4) translocation to the cell membrane.

Pharmacokinetically, insulin glargine has a prolonged half-life of approximately 24 hours when administered subcutaneously, allowing for once-daily dosing. It is metabolized in the liver and kidneys into active metabolites. Its bioavailability is nearly complete when given subcutaneously, but it is not suitable for oral administration due to degradation in the gastrointestinal tract.

Clinically, insulin glargine is widely used for both type 1 and type 2 diabetes management. It is approved by regulatory agencies such as the FDA, EMA, and TGA for this purpose. Researchers have found it effective in maintaining basal insulin levels with a reduced risk of nocturnal hypoglycemia compared to other insulins. It is available under various brand names, including Lantus, Toujeo, and Basaglar, and is subject to prescription regulations in many countries.

Mechanism of Action

Insulin glargine acts on the insulin receptor, initiating a signaling cascade that enhances glucose uptake and utilization. This involves the activation of the PI3K/AKT pathway, leading to increased translocation of GLUT4 transporters to the cell surface, facilitating glucose entry into cells.

Molecular Data

FormulaC267H404N72O78S6
Molecular Weight6063 g/mol
CAS Number160337-95-1
PubChem CID118984454

Half-Life & Pharmacokinetics

SubcutaneousApproximately 24 hours

Insulin glargine is designed for subcutaneous administration, providing a steady release over 24 hours.

Storage

Temperature

Refrigerate at 2-8°C

Light

Protect from light

Form

Aqueous solution: use within 28 days after opening

Notes

Do not freeze; discard if frozen.

Solubility

Insulin glargine is soluble in water, forming a microprecipitate at physiological pH that allows for slow absorption.

Legal Status

🇩🇪DE

Verschreibungspflichtig (prescription only); not a controlled substance under BtMG.

🇺🇸US

FDA approved; prescription required; not a controlled substance.

🇦🇺AU

TGA Schedule 4 (prescription only medicine).

🇬🇧UK

Prescription only medicine (POM) under MHRA regulations.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

7 Research Publications

A dose titration protocol for once-daily insulin glargine 300 U/mL for the treatment of diabetes mellitus in dogs.

Human

Journal of veterinary internal medicine · 2024

Researchers observed that insulin glargine 300 U/mL is effective for treating diabetes in dogs, with 92% achieving good or excellent blood sugar control. They found that most dogs could be treated with once-daily doses, although some required twice-daily doses or additional meal-time injections for optimal management.

  • 92% of diabetic dogs achieved good or excellent glycemic control.
  • Insulin glargine can be administered once daily for most dogs.
  • Some dogs may need twice-daily doses or meal-time injections for better control.
PubMed

Comparative clinical efficacy and safety of insulin glargine 300 U/ml (Toujeo) versus insulin glargine 100 U/ml in type 2 diabetes and type 1 diabetes: A systematic literature review and meta-analysis.

Meta-Analysis

Diabetes, obesity & metabolism · 2023

Researchers found that insulin glargine 300 (Gla-300) has a lower risk of nighttime and overall low blood sugar compared to insulin glargine 100 (Gla-100) in people with type 2 diabetes. However, Gla-300 requires a higher daily dose of insulin to achieve similar results. Both insulins were found to have comparable safety and effectiveness profiles overall.

  • Gla-300 showed a lower risk of nocturnal and total hypoglycaemia in type 2 diabetes patients.
  • Patients using Gla-300 needed more insulin daily than those using Gla-100 for similar effectiveness.
  • Safety profiles of Gla-100 and Gla-300 were comparable in both type 1 and type 2 diabetes.
PubMed

Immunogenicity of LY2963016 insulin glargine and Lantus® insulin glargine in Chinese patients with type 1 or type 2 diabetes mellitus.

Human

Diabetes, obesity & metabolism · 2022

Researchers found that LY2963016 insulin glargine (LY IGlar) and Lantus® insulin glargine (IGlar) have similar immunogenicity profiles in Chinese patients with type 1 and type 2 diabetes. Both insulins showed low levels of anti-insulin antibodies, and these antibody levels did not impact clinical outcomes such as blood sugar control or safety.

  • No significant differences in anti-insulin antibody levels between LY IGlar and IGlar.
  • Both insulins resulted in low levels of antibodies (<5%) after 24 weeks of treatment.
  • Antibody levels were not linked to treatment effectiveness or safety.
PubMed

The role of Toujeo®, insulin glargine U-300, in the treatment of diabetes mellitus.

Review

Journal of the American Association of Nurse Practitioners · 2016

Researchers observed that Toujeo®, a new insulin option for diabetes treatment, is safe and effective. It may lead to fewer low blood sugar episodes and slightly less weight gain compared to another insulin, though it requires a higher dosage to achieve similar blood sugar control.

  • Toujeo® is as effective as Gla-100 but with fewer hypoglycemia incidents.
  • Patients using Toujeo® may experience less weight gain.
  • Higher doses of Toujeo® are needed to achieve the same blood sugar control as Gla-100.
PubMed

Concentrated insulin glargine (Toujeo) for diabetes.

Review

The Medical letter on drugs and therapeutics · 2015

Researchers found that Toujeo, a new formulation of insulin glargine, is just as effective as the older version in lowering blood sugar levels. They also observed that Toujeo may lead to fewer episodes of low blood sugar, known as hypoglycemia.

  • Toujeo is as effective as Lantus in lowering HbA1c.
  • Toujeo may cause less hypoglycemia.
  • Toujeo has a higher concentration of insulin.
PubMed

[Medication of the month. Insulin glargine (Lantus)].

Review

Revue medicale de Liege · 2004

Researchers found that insulin glargine (Lantus) provides a more stable and consistent release of insulin over 24 hours compared to traditional insulins. This allows for once-daily injections, which can help improve blood sugar control with a lower risk of nighttime low blood sugar. The study emphasizes the importance of integrating insulin glargine into a comprehensive diabetes management plan.

  • Insulin glargine offers a steady release of insulin, allowing for once-daily injections.
  • It improves blood sugar control while reducing the risk of nighttime hypoglycemia.
  • Optimal use of insulin glargine should be part of a broader diabetes management strategy.
PubMed

Insulin glargine (Lantus).

Review

International journal of clinical practice · 2002

Researchers observed that insulin glargine (Lantus) is a long-acting insulin that provides stable blood sugar control with a lower risk of hypoglycemia compared to traditional insulins. It is well-tolerated by patients with type 1 and type 2 diabetes, leading to higher satisfaction with treatment.

  • Insulin glargine offers consistent insulin levels without peaks, reducing the risk of low blood sugar.
  • Patients using insulin glargine reported better fasting blood glucose levels and overall treatment satisfaction.
  • It can be effectively combined with other insulin types or oral medications for better diabetes management.
PubMed

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This page is for informational and research purposes only. All information is based on published scientific literature. Nothing on this page constitutes medical advice or replaces consultation with a qualified healthcare professional.