Description

Simple

A medication used to control blood sugars in diabetes.

Clinical

A modified form of fast-acting insulin used to control hyperglycemia in diabetes mellitus.

Overview

Insulin lispro is a rapid-acting form of insulin used for the treatment of hyperglycemia caused by Type 1 and Type 2 Diabetes. Insulin is prescribed for the management of diabetes mellitus to mimic the activity of endogenously produced human insulin, a peptide hormone produced by beta cells of the pancreas that promotes glucose metabolism. Insulin is released from the pancreas following a meal to promote the uptake of glucose from the blood into internal organs and tissues such as the liver, fat cells, and skeletal muscle. Absorption of glucose into cells allows for its transformation into glycogen or fat for storage. Insulin also inhibits hepatic glucose production, enhances protein synthesis, and inhibits lipolysis and proteolysis among many other functions.

Insulin is an important treatment in the management of Type 1 Diabetes (T1D) which is caused by an autoimmune reaction that destroys the beta cells of the pancreas, resulting in the body not being able to produce the insulin needed to manage circulating blood sugar levels. As a result, people with T1D rely primarily on exogenous forms of insulin, such as insulin lispro, to lower glucose levels in the blood. Insulin is also used in the treatment of Type 2 Diabetes (T2D), another form of diabetes mellitus that is a slowly progressing metabolic disorder caused by a combination of genetic and lifestyle factors that promote chronically elevated blood sugar levels. Without treatment or improvement in non-pharmacological me... Read more

Pharmacology

Indication

Insulin lispro is indicated to improve glycemic control in adults and children with diabetes mellitus.

Pharmacodynamic

Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic individuals, a basal level of insulin is supplemented with insulin spikes following meals. Increased insulin secretion following meals is responsible for the metabolic changes that occur as the body transitions from... Read more

Mechanism of action

Insulin lispro binds to the insulin receptor (IR), a heterotetrameric protein consisting of two extracellular alpha units and two transmembrane beta units. The binding of insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the beta subunit of the receptor. The bou... Read more

Absorption

Insulin lispro is rapidly absorbed following subcutaneous administration. It is also absorbed more quickly than regular human insulin. Peak serum levels occur 30-90 minutes after injection in healthy subjects. Absorption also differs depending on the site of injection. After insulin lispro was admin... Read more

Protein binding

Information currently not available.

Volume of distribution

When administered intravenously as bolus injections of 0.1 and 0.2 U/kg dose in two separate groups of healthy subjects, the mean volume of distribution of insulin lispro appeared to decrease with increase in dose (1.55 and 0.72 L/kg, respectively).

Clearance

Clearance is dose dependent. When a dose of 0.1 unit/kg and 0.2 unit/kg were administered intravenously, the mean clearance was 21.0 mL/min/kg and 9.6 mL/min/kg respectively.

Half life

After subcutaneous administration of insulin lispro, the t1/2 is shorter than that of regular human insulin (1 versus 1.5 hours, respectively).

Route of elimination

Information currently not available.

Toxicity

Inappropriately high dosages relative to food intake and/or energy expenditure may result in severe and sometimes prolonged and life-threatening hypoglycemia. Neurogenic (autonomic) signs and symptoms of hypoglycemia include trembling, palpitations, sweating, anxiety, hunger, nausea and tingling. Ne... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Flu syndrome US
  • Kind: experimental
    • Percent: 34.6
  • Kind: comparator
    • Percent: 32.6
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 33.3
  • Kind: comparator
    • Percent: 33.7
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 29.6
  • Kind: comparator
    • Percent: 22.1
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 24.7
  • Kind: comparator
    • Percent: 29.1
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 13.6
  • Kind: comparator
    • Percent: 20.9
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: 19.8
  • Kind: comparator
    • Percent: 16.3
  • Clinical Trial
    Cough increased US
  • Kind: experimental
    • Percent: 17.3
  • Kind: comparator
    • Percent: 17.4
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 15.1
  • Clinical Trial
    Surgical Procedure US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 14
  • Clinical Trial
    Fever US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 11.6
  • Clinical Trial
    Accidental injury US
  • Kind: experimental
    • Percent: 8.6
  • Kind: comparator
    • Percent: 11.6
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 11.6
  • Kind: comparator
    • Percent: 9.3
  • Clinical Trial
    Pain US
  • Kind: experimental
    • Percent: 10.8
  • Kind: comparator
    • Percent: 10
  • Clinical Trial
    Infection US
  • Kind: experimental
    • Percent: 10.1
  • Kind: comparator
    • Percent: 7.6
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 8.6
  • Kind: comparator
    • Percent: 5.8
  • Clinical Trial
    Flu syndrome US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 8.2
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 6.6
  • Kind: comparator
    • Percent: 8.2
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 7.4
  • Kind: comparator
    • Percent: 8.1
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 7.4
  • Kind: comparator
    • Percent: 8.1
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 8.1
  • Kind: comparator
    • Percent: 6.6
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 7.4
  • Kind: comparator
    • Percent: 5.8
  • Clinical Trial
    Bronchitis US
  • Kind: experimental
    • Percent: 7.4
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Surgical Procedure US
  • Kind: experimental
    • Percent: 7.4
  • Kind: comparator
    • Percent: 6.8
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 7
  • Clinical Trial
    Urinary Tract Infection US
  • Kind: experimental
    • Percent: 6.2
  • Kind: comparator
    • Percent: 4.7
  • Clinical Trial
    Infusion site reactions US
  • Kind: experimental
    • Percent: >3%
  • Kind: comparator
    • Percent: >3%
  • Clinical Trial
    Injection Site localized cutaneous amyloidosis US
    Post Marketing
    Acute painful peripheral neuropath US
    Clinical Trial
    Peripheral Edema US
    Clinical Trial
    Weight Gain US
    Clinical Trial
    Lipodystrophy US
    Clinical Trial
    Transitory, reversible ophthalmologic refraction disorder US
    Clinical Trial
    Worsening of diabetic retinopathy US
    Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Episodes of hypoglycemia
        • Drugbank Id: DBCOND0107424

    Food Interactions

    Information currently not available.