Glucagon (rescue)
/ Recombinant 29-residue glucagon peptide; native glucagon receptor agonistALIAS · GlucaGen (trade) · Glucagon Emergency Kit · Recombinant glucagon · Baqsimi (intranasal) · Gvoke (auto-injector)
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Tier 1. Recombinant 29-residue glucagon is FDA-approved across multiple formulations for severe hypoglycemia rescue: the legacy lyophilised reconstitute-and-inject Glucagon Emergency Kit and GlucaGen, the ready-to-use Gvoke autoinjector and pre-filled syringe (2019), and the intranasal Baqsimi powder (2019). Pivotal non-inferiority trials versus reconstituted glucagon supported the newer formulations.
Glucagon is the 29-residue peptide hormone secreted by pancreatic alpha cells in response to hypoglycemia. Receptor binding at the hepatic glucagon receptor activates adenylate cyclase via Gs-alpha, raising intracellular cAMP and driving glycogenolysis and gluconeogenesis. The resulting rapid release of hepatic glucose into the systemic circulation is the molecular basis for severe-hypoglycemia rescue. Recombinant glucagon is sequence-identical to the endogenous human peptide.
Tier 1. The Baqsimi intranasal powder pivotal program (Rickels 2016 Diabetes Care, Pieber 2018 Diabetes Care) demonstrated non-inferiority to intramuscular reconstituted glucagon for plasma glucose recovery in adults and adolescents with type 1 diabetes during insulin-induced hypoglycemia. The Gvoke ready-to-use autoinjector program demonstrated comparable efficacy with substantially reduced administration complexity versus the legacy reconstitute-and-inject kit. The legacy product itself has decades of clinical-use evidence in severe hypoglycemia.
Common adverse events across formulations include nausea, vomiting, headache, and injection-site or nasal-administration-site reactions. Hyperglycemic rebound after rescue is expected. Glucagon is contraindicated in pheochromocytoma (catecholamine release) and insulinoma (paradoxical insulin release). Effectiveness depends on hepatic glycogen stores; in severe malnutrition, prolonged fasting, or chronic alcoholism, response may be attenuated.
Regulatory status
- FDA status:
- FDA-approved
- Compounding:
- Not eligible for compounding (approved, not in shortage)
The transition from reconstitute-and-inject to ready-to-use formulations addressed a long-standing usability problem in severe-hypoglycemia rescue; the older kit had documented administration-error rates in panic situations. The newer formulations have not changed pharmacology — only delivery. Bihormonal closed-loop systems and dasiglucagon (a stable analog) are adjacent developments that go beyond rescue dosing.