Insulin glargine binds to the insulin receptor (IR), a heterotetrameric protein consisting of 2 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 bound receptor autophosphorylates and phosphorylates numerous intracellular substrates like insulin receptor substrates (IRS) proteins, Cbl, APS, Shc and gab 1. Activation of those proteins results in the activation of downstream signal molecules as well as PI3 kinase and Akt. Akt regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC), each of that play important roles in metabolism. insulinglargine is totally soluble at pH 4, the pH of administered solution, and has low solubility at physiological pH 7.4. Upon subcuteous injection, the solution is neutralised leading to the formation of microprecipitates. small amounts of insulin glargine are released from microprecipitates giving the drug a comparatively constant concentration over time profile over 24 hours with no pronounced peak. This release mechanism permits the drug to mimic basal hormone levels within the body.
Common side effects of insulin glargine are:
Decreased blood sugar and injection site pain
Water retention in the joints and weight gain
Local allergic reactions that may occur at the injection sites are:
Severe allergic reactions are:
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