Glucagon Nasal Spray

Products

Glucagon nasal applicator was approved in the US and EU in 2019 and in many countries in 2020 (Baqsimi, single dose). Glucagon is present in the drug product as a powder for nasal administration. The applicator is stored at room temperature not above 30°C.

Structure and properties

Glucagon (C153H225N43O49S, Mr = 3483 g/mol) is a linear polypeptide of 29 amino acids that has the same structure as the hormone produced by alpha cells of the human pancreas. It exists as a white powder that is virtually insoluble in water. Glucagon can be produced by biotechnological methods.

Effects

Glucagon (ATC H04AA01) has catabolic and hyperglycemic (antihypoglycemic) properties. It increases blood glucose levels to counteract the effects of insulin. The effects are based on binding to hepatic glucagon receptors. This results in the breakdown of glycogen in the liver and the release of glucose into the bloodstream, as well as the promotion of gluconeogenesis (glucose formation). Glucagon also inhibits the movements of the digestive tract. Hepatic glycogen stores are required for it to exert its effects. Blood glucose levels begin to rise 5 minutes after administration. The mean half-life is 35 minutes.

Indications

For the treatment of severe hypoglycemia in adults, adolescents, and children 4 years of age and older with diabetes mellitus.

Dosage

According to the SmPC. The drug is administered intranasally into a nostril. The active substance enters the bloodstream through the nasal mucosa. No inhalation or deep breathing is required. Oral carbohydrates should be administered after response to therapy. Do not test the applicator before use! The U.S. SmPC mentions that if there is no response, administration can be repeated after 15 minutes with a new applicator.

Contraindications

  • Hypersensitivity
  • Pheochromocytoma

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with beta-blockers, indomethacin, and vitamin K antagonists (warfarin).

Adverse effects

Possible adverse effects include:

  • Nausea, vomiting
  • Headache
  • Irritation of the upper respiratory tract
  • Watery eyes, eye redness and itching.
  • Itching in the nose, throat.