升糖素
Glucagon
Polypeptide hormone (29 amino acids)
別名: GlucoGen · GlucaGen HypoKit · Glucagon Emergency Kit · glucagonum · HGF
由 VetSheet 獸醫團隊審訂更新於 2026年4月5日本內容以實證獸醫文獻為本
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Insulinoma hypoglycemic crisis with insufficient response to other therapy
Glucagon 15–40 ng/kg/min CRI (constant rate infusion)
必須同時考慮的臨床上下文 (1)
- may be helpful in animals with an insufficient response to other types of therapy
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概覽
升糖素是一種由胰臟α2細胞分泌的多肽荷爾蒙。在獸醫學中，主要用於治療因胰島素瘤或胰島素過量引起的嚴重低血糖。此外，它在治療乳牛脂肪肝綜合症方面也具潛力。
作用機制
Glucagon acts as a physiological antagonist to insulin, primarily targeting the liver to increase blood glucose levels.
- Binds to specific glucagon receptors (GPCRs) on the surface of hepatocytes.
- Activates adenylate cyclase → increases intracellular cAMP → activates protein kinase A (PKA).
- This cascade stimulates glycogen phosphorylase and inhibits glycogen synthase, leading to rapid hepatic glycogenolysis (breakdown of stored glycogen into glucose) and gluconeogenesis.
- Also causes relaxation of gastrointestinal smooth muscle through poorly understood mechanisms (likely cAMP-mediated).
安全性與警告
禁忌症
- Normoglycemia
- Pheochromocytoma (in humans)
- Insulinoma (may stimulate insulin release)
不良反應
- Nausea
- Hypokalemia
- Hypersensitivity reactions (very rare)
- Vomiting (main adverse reaction reported in humans)
- Anaphylaxis (rare)
注意事項
Pheochromocytoma Warning: Glucagon should usually not be used in patients with pheochromocytoma as catecholamines may be released leading to hypertension.
- Insulinoma Caution: When used for insulinoma, it must be in a setting where blood glucose can be closely monitored. It can stimulate insulin production, potentially leading to greater rebound hypoglycemia once the drug is discontinued.
- Pregnancy/Nursing: FDA Category B in humans. As an endogenously produced hormone, it is unlikely to cause significant risk to offspring or nursing young.
藥物相互作用
May have their effects increased when glucagon is concurrently administered; this effect may be delayed. Monitor for bleeding and prothrombin activity.
監測
- Serum potassium (if used other than for acute treatment)
- Blood glucose (hourly)
- Serum potassium (if prolonged infusion)
藥物動力學
半衰期
吸收
Must be administered parenterally; destroyed in the gut after oral dosing. After IV injection, maximum glucose levels are attained within 30 minutes; hyperglycemic effects persist up to 90 minutes.
分佈
Distributes to target organs, primarily the liver.
代謝
Degraded in the plasma, liver, and kidneys.
排除
Rapidly cleared from circulation.
過量
Adverse effects seen with overdose include nausea, vomiting, diarrhea, gastric hypotonicity and, possibly, hypokalemia.
- Because glucagon's elimination half-life is so short (around 10 minutes in humans), treatment may not be necessary and would be symptomatic in nature.
- If the patient is also receiving beta-blockers, greater increases in blood pressure and heart rate may be seen.
可用產品
劑型
- Powder for injection
- 1 mg vial for reconstitution (Injectable)
人用標示
- Glucagon Powder for Injection: 1 mg (1 unit) with 1 mL diluent in vials & syringes
- GlucaGen Diagnostic Kit
- GlucaGen HypoKit
- Glucagon Emergency Kit
- Glucagen 1 mg vial for reconstitution
各地核准狀態
Human authorized product used off-label under the cascade.
POM (Prescription Only Medicine)
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儲存與穩定性
Store commercially available powder for reconstitution at room temperature between 20-25°C (68-77°F); avoid freezing and protect from light. Once reconstituted with the supplied diluent, the solution should be clear with a water-like consistency and used immediately; discard any unused portion. Discard if the solution contains any gel formation or particles.
飼主須知
緊急用途：升糖素通常在醫院環境中使用，以便持續監測寵物的血糖。
- 居家低血糖急救：雖然升糖素可用於居家緊急治療，但將口服葡萄糖漿（如玉米糖漿）塗抹在牙齦上，對於飼主來說通常更為實用且合適。
- 監測：如果您的寵物住院且正在接受升糖素連續輸注，獸醫團隊會密切監測其血糖和鉀離子濃度。
- 副作用：它通常非常安全，但偶爾可能會出現輕微噁心或嘔吐。
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