Fate of Insulin

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Chapter: Essential pharmacology : Insulin, Oral Hypoglycaemic Drugs and Glucagon

Insulin is distributed only extracellularly. It is a peptide; gets degraded in the g.i.t. if given orally. Injected insulin or that released from pancreas is metabolized primarily in liver and to a smaller extent in kidney and muscles.


FATE OF INSULIN

 

Insulin is distributed only extracellularly. It is a peptide; gets degraded in the g.i.t. if given orally. Injected insulin or that released from pancreas is metabolized primarily in liver and to a smaller extent in kidney and muscles. Nearly half of the insulin entering portal vein from pancreas is inactivated in the first passage through liver. Thus, normally liver is exposed to a much higher concentration (4–8 fold) of insulin than are other tissues. As noted above, degradation of insulin after receptor mediated internalization occurs to variable extents in most target cells. During biotransformation the disulfide bonds are reduced—A and B chains are separated. These are further broken down to the constituent amino acids. The plasma t½ is 5–9 min.

 

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