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Insulin (Regular)

Human Insulin · Humulin R · Novolin R · Regular Insulin

Insulin & Glucose RegulationApproved
MW
5808g/mol
Formula
C257H383N65O77S6

Insulin (Regular) is a peptide hormone classified as a rapid-acting insulin, primarily produced by the beta cells of the pancreas. Researchers primarily study it for its role in glucose metabolism and its therapeutic applications in diabetes management. Key findings from recent studies indicate that variations in insulin dosing can significantly impact glycemic outcomes in hospitalized patients, with evidence suggesting that specific dosing strategies may mitigate risks of hypoglycemia and hyperglycemia. Additionally, pharmacokinetic and pharmacodynamic equivalence has been established between biosimilar formulations and the original Humulin® R, indicating comparable efficacy and safety profiles. Current research continues to explore the implications of concentrated insulin formulations and their potential benefits for diverse patient populations.

Overview

Übersicht

Insulin (Regular), also known as Human Insulin, Humulin R, or Novolin R, is a synthetic form of insulin produced using recombinant DNA technology. It is typically synthesized in Escherichia coli, where chemically synthesized genes for the insulin A and B chains are expressed. This synthetic insulin is classified as a peptide hormone and is crucial for regulating glucose metabolism in the body. Researchers have focused on its production and purification processes to ensure its efficacy and safety for therapeutic use. The primary physiological role of insulin is to facilitate the uptake of glucose into cells, thus lowering blood glucose levels. It is a critical hormone in the management of diabetes, particularly in patients with type 1 diabetes who lack endogenous insulin production. Research has also explored its use in managing gestational diabetes and in patients requiring insulin during stress or surgery. Insulin acts by binding to the insulin receptor, a transmembrane receptor that triggers a cascade of intracellular events, including the activation of the PI3K/Akt pathway. This leads to increased glucose uptake by cells, particularly in muscle and adipose tissue, and promotes glycogen synthesis in the liver. Pharmacokinetically, regular insulin has a relatively short half-life and is typically administered via subcutaneous injection. It has a rapid onset of action, with effects beginning within 30 minutes and peaking at 2-3 hours. The duration of action is approximately 5-8 hours. Clinically, regular insulin is widely used for the management of diabetes mellitus and is approved by regulatory agencies such as the FDA. It is available by prescription and is considered a safe and effective treatment when used according to guidelines.

Chemical profile

Chemische Struktur

FormelC257H383N65O77S6
Molekulargewicht5808g/mol
CAS-Nummer11061-68-0
PubChem CID118984375
Mechanism

Wirkmechanismus

Insulin acts on the insulin receptor, a tyrosine kinase receptor, triggering the PI3K/Akt signaling pathway. This cascade leads to increased glucose uptake in muscle and adipose tissue and promotes glycogen synthesis in the liver.

Mechanism

Signalweg

Insulin (Regular) primarily acts through the insulin receptor (IR), a receptor tyrosine kinase, which initiates signaling cascades such as the PI3K/Akt pathway and the MAPK pathway. Activation of the IR leads to increased glucose uptake via GLUT4 translocation to the plasma membrane, enhanced glycogen synthesis, and modulation of lipid metabolism, thereby promoting overall anabolic processes. While the core mechanisms are well-established, some aspects of insulin signaling and its interactions with other pathways remain to be fully elucidated.

Half-Life & Pharmacokinetics

ENEndogenous

Circulating half-life ~5-10 minutes

SCSubcutaneous

Duration of action ~5-8 hours

IVIntravenous

~5-10 minutes

POOral

Poor bioavailability due to first-pass metabolism

Regular insulin has a rapid onset and short duration of action, typically administered subcutaneously.

Storage

Temperature

Refrigerate at 2-8C

Light

Protect from light

Form

Aqueous solution: use within 28 days after opening

Notes

Do not freeze; discard if frozen.

Solubility

Löslichkeit

Soluble in water, forming a clear solution for injection.

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); regulated by the MHRA.

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.

Open Questions

Offene Forschungsfragen

Current evidence is limited regarding the optimal dosing strategies for hospitalized patients on U-500 insulin, particularly in relation to glycemic outcomes and the risk of hypoglycemia. Further research is needed through larger randomized controlled trials (RCTs) to establish effective inpatient insulin dosing protocols and to evaluate the long-term safety and efficacy of biosimilar insulins compared to established formulations like Humulin-R. Additionally, there is a need for studies focusing on specific populations, such as those with gestational diabetes or other unique clinical scenarios, to better understand the advantages and limitations of human insulin in diverse patient groups.

30 Research Publications

1,775

Total Citations

17

Human/RCT

3.9

Avg. Influence

2022

Latest

Sort
Filter
#01

Expression in Escherichia coli of chemically synthesized genes for human insulin.

Goeddel D V, et al. · Proceedings of the National Academy of Sciences of the United States of America · 1979

In VitroInfluence9.0
804
Researchers observed successful expression and purification of human insulin A and B chains in Escherichia coli, confirming the feasibility of synthesizing insulin through recombinant DNA technology.

Key findings

  1. 01Synthetic genes for human insulin were successfully cloned.
  2. 02Insulin peptides were purified from a precursor protein.
  3. 03The presence of insulin was confirmed using radioimmunoassay.
#02

Sequence of the human insulin gene.

In VitroInfluence9.0
491
The study demonstrated that the human insulin gene contains two intervening sequences, with potential regulatory regions identified in comparison to the rat insulin gene.
#03

Pre-meal insulin analogue insulin lispro vs Humulin R insulin treatment in young subjects with type 1 diabetes.

HumanInfluence2.0
103
Researchers observed that insulin lispro treatment resulted in fewer hypoglycemic episodes and lower postprandial glucose excursions compared to regular human insulin in young subjects with type 1 diabetes.
#04

Evolution of insulin development: focus on key parameters.

ReviewInfluence4.0
57
The study demonstrated that despite advancements in insulin development, achieving optimal glycemic control and minimizing hypoglycemic risk in diabetes patients remains a significant challenge.
#05

Concentrated insulins: the new basal insulins.

Review
51
The review highlighted that concentrated insulins, including Humulin-R U500, provide longer duration of action and reduced hypoglycemia risk compared to traditional insulins, addressing the needs of patients requiring high doses.
#06

Allergic reactions to human insulin: a review of current knowledge and treatment options.

ReviewInfluence3.0
40
The review demonstrated that while the incidence of insulin allergy has decreased, it remains a significant issue that can be life-threatening, highlighting the need for effective treatment options.
#07

Human insulin: facile synthesis by modification of porcine insulin.

In Vitro
36
Researchers observed that human insulin can be synthesized from porcine insulin through a chemical modification process, allowing for large-scale production.
#08

Availability of insulin from total parenteral nutrition solutions.

In VitroInfluence2.0
34
Researchers observed that human insulin recovery from total parenteral nutrition solutions is significantly higher than previously reported, with minimal impact from lipid addition or specific amino acid formulations.
#09

Concise synthetic routes to human insulin.

In VitroInfluence1.0
30
Researchers observed concise synthetic routes for human insulin production, achieving high yields in a single workday.
#10

Equivalent Recombinant Human Insulin Preparations and their Place in Therapy.

Review
20
Researchers observed that recombinant human insulin formulations have established bioequivalence, providing a consistent supply and replacing older animal-derived insulins in diabetes therapy.

Clinical Trials (7)

Preclinical
Phase I
Phase II
Phase III
Approved

7

Total Trials

657

Total Enrolled

Comparison on Efficacy and Safety of Three Inpatient Insulin Therapy in Type2 DM

NCT01855243COMPLETED
Sponsor

Cairo University

Enrollment

63

Started

2010

Primary outcome

Mean Daily Blood Glucose (BG) Concentration During Their Hospital Stay.

Diabetes Mellitus (DM)

Insulin Analogues and Severe Hypoglycaemia

NCT00346996Phase 4COMPLETED
Sponsor

Lise Tarnow

Enrollment

179

Started

2007

Primary outcome

Severe hypoglycaemia

Type 1 Diabetes

Insulin in Total Parenteral Nutrition

NCT02706119Phase 4COMPLETED
Sponsor

Fundación Pública Andaluza Progreso y Salud

Enrollment

163

Started

2016

Primary outcome

Basal blood glucose value before starting TPN

Diabetes Mellitus

Basal Bolus Versus Human Insulin in Hospitalized Patients With Diabetes in Paraguay

NCT02278913Phase 4COMPLETED
Sponsor

Universidad Nacional de Asunción

Enrollment

134

Started

2009

Primary outcome

Glycemic control

HyperglycemiaDiabetes

Comparison of Neutral Protamine Hagedorn (NPH) and Lantus Based Insulin Regimen in the Management of Hypoglycemia in the Hospitalized Patients in Noncritical Care Setting

NCT02189395Phase 4TERMINATED
Sponsor

Riverside University Health System Medical Center

Enrollment

52

Started

2013

Primary outcome

difference in glycemic control between treatment groups as measured by the mean daily blood glucose

Type 2 Diabetes Mellitus

AT278, NovoRapid® and Humulin® R (U500) in Glucose Clamp Study

NCT05754424Phase 1COMPLETED
Sponsor

Arecor Limited

Enrollment

41

Started

2023

Primary outcome

Area under the glucose infusion rate-time curve of insulin aspart

Diabetes Mellitus, Type 2

Comparative Glucose Clamp Study of Wockhardt's Insulin Human Regular for Injection and Novolin R, in Healthy Subjects.

NCT00596063Phase 1COMPLETED
Sponsor

Wockhardt

Enrollment

25

Started

2008

Primary outcome

The primary objective is to test for bioequivalence based on AUC0-12h and Cmax between Wockhardt's Insulin Human Regular for injection and Novolin® R

Diabetes Mellitus

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer