What Is Glucagon?

Glucagon is a 29-amino acid peptide hormone produced by alpha cells in the pancreatic islets. It works opposite to insulin, raising blood glucose levels when they fall too low. Glucagon is critical for preventing hypoglycemia and is a life-saving emergency treatment for severe insulin reactions.

Sequence: 29 amino acids (linear) Molecular Weight: 3,483 Da Production: Pancreatic alpha cells Function: Counter-regulatory hormone to insulin Clinical Use: Emergency hypoglycemia treatment

Key Functions

  • Stimulates liver glycogenolysis (glycogen breakdown)
  • Promotes gluconeogenesis (glucose production)
  • Raises blood glucose levels
  • Inhibits glycogen synthesis
  • Emergency treatment for severe hypoglycemia

Mechanism of Action

  • Binds to glucagon receptor (GPCR) on liver cells
  • Activates adenylyl cyclase โ†’ increases cAMP
  • Activates protein kinase A
  • Stimulates glycogen breakdown and glucose release
  • Also promotes ketogenesis and lipolysis

Clinical Applications

IndicationRouteNotes
Severe hypoglycemiaIM, SC, IV, NasalEmergency treatment
Beta-blocker overdoseIVCardiac effects
Diagnostic imagingIV, IMRelaxes GI smooth muscle

Modern Glucagon Products

  • Baqsimi: Nasal spray (no injection needed)
  • Gvoke: Premixed, room-temperature stable
  • Glucagon Emergency Kit: Traditional reconstitution required
  • Dasiglucagon (Zegalogue): Stable liquid form

Glucagon in Multi-Hormone Research

Glucagon is now part of multi-agonist drug development:

  • GLP-1/glucagon dual agonists: For weight loss
  • Triple agonists: GLP-1/GIP/glucagon (e.g., retatrutide)
  • Glucagon component may enhance energy expenditure
  • Balances glucose effects of other components

Medical Use

Glucagon is a prescription medication. While generally safe for emergency hypoglycemia treatment, it has limited effect in alcohol-induced hypoglycemia or glycogen-depleted states. Proper training in administration is important for caregivers of diabetics.

Summary

Glucagon is insulin's essential partner in glucose regulation. As an emergency medication, it saves lives by rapidly reversing severe hypoglycemia. Recent drug development has also recognized glucagon's metabolic effects, incorporating it into multi-receptor agonists for obesity treatment. Modern delivery systems have made glucagon more accessible for emergency use.

โ† Insulin Next: Liraglutide โ†’