GVOKE PFS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GVOKE PFS (GVOKE PFS).
Glucagon receptor agonist; increases blood glucose levels by stimulating glycogenolysis and gluconeogenesis in the liver.
| Metabolism | Primarily hepatic via proteolysis; main metabolic pathway is degradation to smaller peptides and amino acids. |
| Excretion | Glucagon is primarily degraded in the liver, kidneys, and plasma by proteolytic enzymes. Renal excretion accounts for <10% as unchanged drug; metabolites are excreted in urine and bile. |
| Half-life | Terminal elimination half-life is approximately 3-6 minutes (intravenous); clinical effect wanes rapidly as glucagon is cleared, requiring continuous infusion for sustained effect. |
| Protein binding | Low; approximately 30% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.3-0.5 L/kg; distributes into extracellular fluid with minimal tissue binding. |
| Bioavailability | Not applicable for intravenous route; intramuscular and subcutaneous: near 100% as peptide is fully absorbed. |
| Onset of Action | Intravenous: 1 minute; Intramuscular: 1-10 minutes; Subcutaneous: 5-20 minutes. |
| Duration of Action | Intravenous: 5-15 minutes (hyperglycemic effect); Intramuscular: 10-30 minutes; Subcutaneous: 10-40 minutes. Duration may be prolonged in hepatic or renal impairment. |
1 mg subcutaneously as a single injection for severe hypoglycemia. May repeat once after 15 minutes if no response. For intramuscular or intravenous use: 1 mg IM or IV.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for renal impairment. GFR not a factor. |
| Liver impairment | No dose adjustment required for hepatic impairment. Child-Pugh score does not alter dosing. |
| Pediatric use | For children <25 kg: 0.5 mg subcutaneously as a single injection. For children ≥25 kg: 1 mg subcutaneously as a single injection. May repeat once after 15 minutes if no response. |
| Geriatric use | No specific dose adjustment recommended in elderly. Use same dosing as adults. Monitor closely 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 GVOKE PFS (GVOKE PFS).
| Breastfeeding | Glucagon is not orally bioavailable and is rapidly inactivated in the gastrointestinal tract. Excretion into human milk is unknown, but due to its large molecular weight (MW ~3485 Da) and rapid degradation, exposure to the nursing infant is expected to be negligible. M/P ratio is not available. Considered compatible with breastfeeding. |
| Teratogenic Risk | Glucagon (GVOKE PFS) is a polypeptide hormone that does not cross the placenta in significant amounts. There are no adequate and well-controlled studies in pregnant women. Animal reproduction studies have not been conducted. Based on its mechanism of action and limited systemic exposure, the risk of teratogenicity is considered low. However, severe maternal hypoglycemia during pregnancy can cause fetal harm, including intrauterine growth restriction, congenital anomalies, and fetal death. Use only if clearly needed. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Known hypersensitivity to glucagon or any excipients in the formulation","Pheochromocytoma (risk of hypertensive crisis)"]
| Precautions | ["Risk of hypoglycemia in patients with insulinoma or glucagonoma","Risk of hypersensitivity reactions","Risk of gastrointestinal adverse effects","Use with caution in patients with known pheochromocytoma"] |
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| Fetal Monitoring | Monitor maternal blood glucose levels before and after administration; continuous monitoring may be required until euglycemia is achieved. Assess for signs of hypoglycemia recurrence. In severe hypoglycemia, monitor for neurological status and response. Fetal heart rate monitoring is indicated in pregnant patients with hypoglycemia to detect fetal distress. |
| Fertility Effects | There are no data on the effects of glucagon on human fertility. Animal studies have not been conducted. No clinically relevant effects on fertility are expected given its use as an acute rescue medication with short duration of action. |