GLUCAGEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GLUCAGEN (GLUCAGEN).
Glucagon is a polypeptide hormone that increases blood glucose concentration by stimulating hepatic glycogenolysis and gluconeogenesis, and inhibiting glycogen synthesis. It also relaxes smooth muscle of the gastrointestinal tract.
| Metabolism | Primarily hepatic metabolism; also metabolized in the kidneys and plasma. The major metabolites are not well characterized. |
| Excretion | Renal (primarily degraded in liver, kidney, and plasma; metabolites and small amount of unchanged glucagon excreted in urine). Less than 10% excreted unchanged. |
| Half-life | 3-6 minutes (intravenous); clinical effect duration is short due to rapid degradation. |
| Protein binding | Low (less than 20%); primarily to albumin and alpha-2-macroglobulin, but binding is not clinically significant. |
| Volume of Distribution | 0.3-0.4 L/kg; approximates extracellular fluid volume, indicating limited tissue penetration. |
| Bioavailability | Intramuscular: approximately 100% (similar to intravenous); Subcutaneous: approximately 100% (but onset slower). |
| Onset of Action | Intravenous: 1 minute; Intramuscular: 8-10 minutes; Subcutaneous: 10-15 minutes. |
| Duration of Action | Intravenous: 5-20 minutes; Intramuscular: 10-40 minutes; Subcutaneous: 10-60 minutes. Duration is dose-dependent and limited by rapid metabolism. |
| Action Class | Anti-hypoglycemic agent |
| Brand Substitutes | Glugon 1mg Injection |
1 mg intramuscular, subcutaneous, or intravenous; may repeat once after 15 minutes if no response.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Children <25 kg: 0.5 mg intramuscular, subcutaneous, or intravenous; Children ≥25 kg: 1 mg intramuscular, subcutaneous, or intravenous; may repeat once after 15 minutes if no response. |
| Geriatric use | Same as adult dosing; no specific adjustment required. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GLUCAGEN (GLUCAGEN).
| Breastfeeding | It is not known whether glucagon is excreted in human breast milk. The M/P ratio has not been determined. Due to its high molecular weight and rapid degradation in the gastrointestinal tract, oral bioavailability to the infant is minimal. Glucagon is considered compatible with breastfeeding when used acutely for hypoglycemia. |
| Teratogenic Risk | Glucagon is a polypeptide hormone that does not cross the placenta in significant amounts. No teratogenic effects have been reported in animal studies. In humans, there are no adequate controlled studies in pregnant women. However, because glucagon is used in emergency hypoglycemia, the risk of fetal harm is considered low, particularly given its short-term administration. No specific trimester-associated risks are documented. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to glucagon or any component of the formulation","Patients with pheochromocytoma (risk of hypertensive crisis)","Patients with insulinoma (may cause paradoxical hypoglycemia)"]
| Precautions | ["Risk of hypoglycemia in patients with insulinoma or glucagonoma","May cause nausea and vomiting, which can lead to airway obstruction if consciousness is impaired","Hypersensitivity reactions, including anaphylaxis, have been reported","Ineffective in patients with glycogen storage disease or starvation"] |
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| Fetal Monitoring | During administration, monitor maternal blood glucose levels continuously. In pregnancy, fetal heart rate monitoring may be considered if there is maternal hypoglycemia due to potential fetal distress. Observe for signs of nausea, vomiting, or hypoglycemia recurrence. |
| Fertility Effects | No adverse effects on fertility have been reported in animal studies or human data. Glucagon is not known to impair reproductive function. |