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Uploaded byRitesh Pandav
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Pharmacology of Glucagon

Glucagon is a hormone comprised of a 29 amino acid polypeptide, discovered in 1923, that plays a vital role in increasing blood glucose levels by stimulating glycogenolysis and gluconeogenesis. Its secretion is regulated by various factors including dietary glucose and sympathetic stimulation, and it has therapeutic applications in treating severe hypoglycemia and cardiogenic shock. Glucagon is administered via injection and is contraindicated in cases of pheochromocytoma.

Health & Medicine◦
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Recombinant DNA Tech•
Presented by- Ritesh Rajendra Pandav pandavritesh@gmail.com 2020-2021 TOPIC- GLUCAGON
Glucagon Glucagon word derived from Greek word glukus (sweet) & agon (bringing). Glucagon was discovered by Murlin & Kimball in 1923, less than 2 years after the discovery of insulin. It is single chain polypeptide containing 29 amino acid, It’s MW 3500.
The amino acid sequence of Glucagon
• It is secreted by the alpha cells of the islets of Langerhans. • Commercially glucagon produced now by recombinant DNA technology.
Regulation of Secretion  Glucagon is also derived by cleavage of larger peptide prohormone.  Glucagon secretion is regulated by dietary glucose, insulin, amino acids, fatty acids, paracrine hormone & nervous system.  Amino acids stimulate both glucagon & insulin secretion
• The free fatty acids & ketones inhibits glucagon secretion. • Stimulation of sympathetic nerves or administration of sympathomimetic amines increases glucagon secretion.
Actions Glucagon causes hyperglycemia mainly by enhancing glycogenolysis & gluconeogenesis in liver. In adipose tissue, it stimulate adenylyl cyclase & increase lipolysis. In the heart glucagon increases the force of contraction.
• Glucagon has relaxant effects on the gastrointestinal tract & inhibit gastric acid production. • It plays essential role in the development of diabetic ketoacidosis. • Glucagon is considered as hormone of fuel mobilization.
Mechanism of action Glucagon interacts with a glycoprotein GPCR through Gs & activates adenylyl cyclase & increase cyclic AMP in liver, fat cells, heart & other tissues. Glucagon is inactive orally; that released from pancreas, is broken down in liver, kidney, plasma & other tissues.
Therapeutic Uses Hypoglycemia- Glucagon is used to treat severe hypoglycemia. Dose- 0.5-1.0 mg i.v. or i.m. GLUCAGON 1mg injection.
• Cardiogenic shock- Glucagon used to stimulate the heart in ß adrenergic blocker treated patients. • Glucagon is used to relax the intestinal tract to facilitate radiographic examination of GIT. ★ Contraindication– • Glucagon therapy is contraindicated in known pheochromocytoma.
References 1. KD Tripathi, Essentials of MEDICAL PHARMACOLOGY, 8th edition, 2019. 2. Laurence L. Brnton, John S. Lazo, Goodmam & Gilman’s The Pharmacological Basis of THERAPEUTICS, Eleventh edition.
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