Glucagon

Chemical formula: C₁₅₃H₂₂₅N₄₃O₄₉S  Molecular mass: 3,482.7 g/mol 

Mechanism of action

Glucagon is a hyperglycaemic agent that mobilises hepatic glycogen, which is released into the blood as glucose. Glucagon inhibits the tone and motility of the smooth muscle in the gastrointestinal tract.

Pharmacodynamic properties

Pharmacodynamic effects

When used in treatment of severe hypoglycaemia, an effect on blood glucose is usually seen within 10 minutes.

The onset of inhibitory effect on gastrointestinal motility occurs within 1 minute after an intravenous injection. Duration of action is in the range 5–20 minutes depending on the dose. The onset of effect occurs within 5–15 minutes after an intramuscular injection, with a duration of 10–40 minutes.

Pharmacokinetic properties

Metabolism

Glucagon is degraded enzymatically in the blood plasma and in the organs to which it is distributed. The liver and kidney are major sites of glucagon clearance, each organ contributing about 30% to the overall metabolic clearance rate.

Elimination

Glucagon has a short half-life in the blood of about 3–6 minutes. Metabolic clearance rate of glucagon in humans is approximately 10 ml/kg/min.

Preclinical safety data

No relevant pre-clinical data.

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