ZEGALOGUE (AUTOINJECTOR)
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZEGALOGUE (AUTOINJECTOR) (ZEGALOGUE (AUTOINJECTOR)).
Zegalogue (dasiglucagon) is a glucagon analog that binds to glucagon receptors, activating adenylate cyclase and increasing cAMP levels, which promotes glycogenolysis and gluconeogenesis in the liver, thereby raising blood glucose levels.
| Metabolism | Primarily metabolized via proteolytic degradation into small peptides and amino acids; not metabolized by CYP450 enzymes. |
| Excretion | Primarily hepatic metabolism followed by biliary and fecal excretion, with negligible renal elimination (<2%). |
| Half-life | 50–65 minutes (terminal elimination half-life). |
| Protein binding | Negligible (<5%); not significantly bound to plasma proteins. |
| Volume of Distribution | 0.3–0.5 L/kg, indicating distribution primarily in extracellular fluid. |
| Bioavailability | 100% after intramuscular injection (autoinjector). |
| Onset of Action | Within 1 minute after intramuscular administration. |
| Duration of Action | Approximately 20–30 minutes based on clinical efficacy in reversing neuromuscular blockade. |
0.25 mg intramuscularly (IM) as a single dose into the anterolateral thigh, repeated once after 15 minutes if necessary.
| Dosage form | SOLUTION |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Weight-based dosing: 0.01 mg/kg IM (maximum 0.25 mg) into the anterolateral thigh, repeated once after 15 minutes if necessary. |
| Geriatric use | No specific adjustment required; monitor for adverse effects due to potential comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZEGALOGUE (AUTOINJECTOR) (ZEGALOGUE (AUTOINJECTOR)).
| Breastfeeding | No data on dasiglucagon in human milk; excretion unknown. Glucagon is a peptide with low oral bioavailability; unlikely to be absorbed by infant. M/P ratio not available. Consider risk/benefit; monitor infant for hypoglycemia. |
| Teratogenic Risk | Zegalogue (dasiglucagon) is a glucagon analog; no adequate human studies exist. In animal reproduction studies, no evidence of fetal harm was observed at doses up to 600 times the MRHD. Risk cannot be ruled out; use only if clearly needed. First trimester: limited data; theoretical risk of hyperglycemia-related effects if maternal hypoglycemia not corrected. Second and third trimesters: same as first; no known teratogenicity. |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to dasiglucagon or any component of the formulation","Pheochromocytoma (risk of hypertensive crisis)","Insulinoma (risk of hypoglycemia)"]
| Precautions | ["Risk of hypoglycemia due to overdose or inadequate response","Risk of nausea and vomiting","Risk of hypersensitivity reactions including anaphylaxis","Risk of hyperglycemia in patients with pheochromocytoma or insulinoma"] |
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| Fetal Monitoring | Monitor maternal blood glucose frequently during and after administration. Fetal heart rate monitoring recommended if maternal severe hypoglycemia occurs, as it may cause fetal distress. Assess for uterine contractions if given near term. |
| Fertility Effects | No human data on fertility. Animal studies (rats) showed no impairment of fertility at doses up to 600 times MRHD. Theoretical risk from maternal hypoglycemia on conception/early pregnancy. |