Glucagon

Glucagon Uses, Dosage, Side Effects, Food Interaction and all others data.

Glucagon is a 29 amino acid hormone used as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia. Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose.

Glucagon was granted FDA approval on 14 November 1960.

Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and severe hypoglycemia. Glucagon raises blood sugar through activation of hepatic glucagon receptors, stimulating glycogenolysis and the release of glucose. Glucagon has a short duration of action. Glucagon may cause hyperglycemia in diabetic patients.

Trade Name Glucagon
Availability Prescription only
Generic Glucagon
Glucagon Other Names Glucagon, Glucagon (recombinant dna origin), Glucagon recombinant, Glucagon, human, Glucagon, porcine, Glucagone, Glucagonum
Related Drugs mannitol, Tubersol, arginine, Baqsimi, inulin, diazoxide, Ceretec, Gvoke, GlucaGen
Weight 1mg, , 3mg
Type Injection, Nasal Powder, Nasal
Formula C165H249N49O51S1
Weight 3767.1 Da
Protein binding

Glucagon has not been described in the literature as bound to a protein in serum.

Groups Approved
Therapeutic Class
Manufacturer
Available Country Canada, India, United States
Last Updated: September 19, 2023 at 7:00 am
Glucagon
Glucagon

Uses

Glucagon is a form of recombinant glucagon used to treat hypoglycemia in diabetes mellitus and as a part of gastrointestinal imaging procedures.

Glucagon is indicated as a diagnostic aid in radiologic exams to temporarily inhibit the movement of the gastrointestinal tract and to treat severe hypoglycemia.

Glucagon is also used to associated treatment for these conditions: Severe Hypoglycemia

How Glucagon works

Glucagon binds to the glucagon receptor activating Gsα and Gq. This activation activates adenylate cyclase, which increases intracellular cyclic AMP and activates protein kinase A. Activating Gq activates phospholipase C, increases production of inositol 1,4,5-triphosphate, and releases intracellular calcium. Protein kinase A phosphorylates glycogen phosphorylase kinase, which phosphorylates glycogen phosphorylase, which phosphorylates glycogen, causing its breakdown.

Glucagon also relaxes smooth muscle of the stomach, duodenum, small bowel, and colon.

Toxicity

Patients experiencing an overdose may present with nausea, vomiting, inhibition of GI tract motility, increased blood pressure and heart rate, and decreased serum potassium. Phentolamine may be given to control blood pressure. Treatment of glucagon overdose is largely symptomatic for nausea, vomiting, and hypokalemia.

The LD50 for intravenous glucagon in mice is 300mg/kg and in rats is 38.6mg/kg.

Food Interaction

No interactions found.

Volume of Distribution

The volume of distribution of glucagon is 0.25L/kg. The apparent volume of distribution is 885L.

Elimination Route

A 1mg intravenous dose of glucagon reaches a Cmax of 7.9ng/mL with a Tmax of 20 minutes. An intramuscular dose reaches a Cmax of 6.9ng/mL with a Tmax of 13 minutes. A 3mg dose of glucagon nasal powder reaches a Cmax of 6130pg/mL with a Tmax of 15 minutes.

Half Life

The half life of glucagon is 26 minutes for an intramuscular dose. The half life of glucagon nasal powder is approximately 35 minutes. The half life of glucagon by a subcutaneous auto-injector or pre-filled syringe is 32 minutes.

Clearance

A 1mg intravenous dose of glucagon has a clearance of 13.5mL/min/kg.

Elimination Route

Elimination of glucagon is not fully characterized in literature, however the kidney and liver appear to contribute significantly in animal models. The liver and kidney are responsible for approximately 30% of glucagon elimination each.

Innovators Monograph

You find simplified version here Glucagon

*** Taking medicines without doctor's advice can cause long-term problems.
Share