格列本脲 (Glyburide / Glibenclamide)
Glyburide
Glibenclamide
別名: DiaBeta · Micronase · Glynase PresTab · Glibenclamide · Glibenclamidum · Glybenclamide · Glybenzcyclamide · HB-419 · U-26452
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
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Non-insulin dependent diabetes mellitus (NIDDM) | 0.625 mg (1/2 of a 1.25 mg tablet) | PO | once daily | — | 🌎 NA |
| Non-insulin dependent diabetes mellitus (NIDDM) | 2.5 mg (total dose) | PO | twice a day | — | 🌎 NA |
- Non-insulin dependent diabetes mellitus (NIDDM): Initial dose
- Non-insulin dependent diabetes mellitus (NIDDM): If cat is generally well, weight loss is mild, is not ketoacidotic, and does not have peripheral neuropathy
劑量為合格獸醫專業人員的臨床參考。請務必對照最新仿單及個別病患確認。
概覽
格列本脲（Glyburide，又稱 Glibenclamide）是一種第二代磺醯脲類口服降血糖藥物。
在獸醫學中，它主要作為貓非胰島素依賴型糖尿病 (NIDDM) 的替代口服療法。
臨床重點：
- 格列吡嗪 (Glipizide) 的替代品： 當無法取得格列吡嗪，或飼主強烈希望每天僅需給藥一次時，通常會考慮使用此藥。
- 胰島素仍為首選： 雖然可以嘗試口服降血糖藥，但胰島素治療仍然是黃金標準，且通常是貓糖尿病的首選療法。
- 療效： 對於表現出明顯胰島素阻抗或胰臟 β 細胞功能已耗竭的貓，格列本脲可能無效。
作用機轉
Glyburide lowers blood glucose concentrations by stimulating the secretion of endogenous insulin from functional pancreatic beta cells.
Mechanism of Action:
- Binds to sulfonylurea receptor 1 (SUR1) subunits on ATP-sensitive potassium channels (K-ATP) in the pancreatic beta-cell membrane.
- K-ATP channel closure → cell membrane depolarization.
- Depolarization triggers the opening of voltage-dependent calcium channels → Calcium influx.
- Increased intracellular calcium promotes the exocytosis of insulin granules.
Extrapancreatic Effects: With long-term administration, glyburide may also enhance insulin activity at post-receptor sites and reduce basal hepatic glucose production.
安全性與警告
禁忌症
- Severe burns
- Severe trauma
- Severe infection
- Diabetic coma or other hypoglycemic conditions
- Major surgery
- Ketosis
- Ketoacidosis or other significant acidotic conditions
不良反應
- Vomiting
- Hypoglycemia
- Liver toxicity (icterus, increased ALT/SGPT)
- Allergic skin reactions (reported in humans)
- Arthralgia (reported in humans)
- Bone marrow suppression (reported in humans)
- Cholestatic jaundice (reported in humans)
注意事項
Caution: Glyburide should only be used when its potential benefits outweigh its risks in patients with untreated adrenal or pituitary insufficiency; thyroid, renal, or hepatic function impairment; prolonged vomiting; high fever; malnourishment or in a debilitated condition.
- Concurrent Endocrine Disease: Some patients with type II diabetes may have their disease complicated by the production of excessive amounts of cortisol or growth hormone (e.g., hyperadrenocorticism, acromegaly) that may antagonize insulin's effects. These causes should be ruled out before initiating oral antidiabetic therapy.
- Pregnancy: FDA Category C. Animal studies have shown an adverse effect on the fetus. Safety during nursing is unknown.
藥物交互作用
A disulfiram-like reaction (anorexia, nausea, vomiting) is possible
May increase plasma levels of glyburide
May potentiate hypoglycemic effect
May displace glyburide from plasma proteins
May potentiate hypoglycemic effect
May reduce efficacy
May reduce hypoglycemic efficacy
May reduce hypoglycemic efficacy
May potentiate hypoglycemic effect
May reduce hypoglycemic efficacy
May reduce hypoglycemic efficacy
May reduce hypoglycemic efficacy
May potentiate hypoglycemic effect
May displace glyburide from plasma proteins
May reduce hypoglycemic efficacy
May reduce hypoglycemic effect
May displace glyburide from plasma proteins
監測
- Physical examination (weekly during first month)
- Body weight (weekly during first month)
- Urine glucose and ketones (weekly during first month)
- Serial blood glucose exams (weekly during first month)
- Clinical signs of adverse effects (vomiting, icterus)
- Liver enzymes (ALT/SGPT) occasionally
- Complete Blood Count (CBC) occasionally
藥物動力學
半衰期
吸收
Appears to be well absorbed, though specific bioavailability data in veterinary species is lacking. Food apparently does not have an effect on the absorptive characteristics.
分佈
Distributed throughout the body, including into the brain and across the placenta.
代謝
Apparently completely metabolized, presumably in the liver.
排除
Metabolites are excreted in both the feces and the urine.
過量
Emergency Warning: Profound hypoglycemia is the greatest concern after an overdose.
- In humans, severe hypoglycemia has occurred at relatively low dosages.
- Decontamination: Gut emptying protocols should be employed when warranted and if the patient is neurologically stable.
- Treatment: Because its half-life is longer than glipizide, prolonged hypoglycemia may occur. Continuous blood glucose monitoring and treatment with parenteral glucose (IV dextrose) may be required for several days.
- Monitoring: Massive overdoses may also require additional monitoring (blood gases, serum electrolytes) and supportive therapy.
可用產品
劑型
- Micronized oral tablets
獸醫用
- None
人用標示
- Glyburide Oral Tablets: 1.25 mg, 2.5 mg, & 5 mg
- Glyburide Micronized Oral Tablets: 1.5 mg, 3 mg, 4.5 mg & 6 mg (Glynase PresTab)
- DiaBeta
- Generic formulations
- Fixed dose combinations of glyburide and metformin are also available
各地核准狀態
暫無法規資料: 🇺🇸 US · 🇪🇺 EU · 🇬🇧 UK · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Glyburide oral tablets should be stored in well-closed containers at room temperature.
飼主須知
您的獸醫已處方格列本脲來幫助控制您貓咪的糖尿病。這種藥物能幫助貓咪的胰臟釋放更多胰島素以降低血糖。
重要安全指示：
- 嚴格遵守給藥時間： 請完全按照處方給藥。如果漏服一劑，請勿跳過或在下次給藥時服用雙倍劑量。
- 注意低血糖症狀： 這是醫療緊急情況。症狀包括虛弱、步態不穩、嗜睡、肌肉抽搐、眼神呆滯或癲癇發作。如果您發現這些症狀，請將玉米糖漿或蜂蜜塗抹在貓咪的牙齦上，並立即聯繫您的獸醫。
- 注意高血糖症狀： 如果藥物效果不佳，您可能會注意到貓咪口渴增加、排尿增加或體重減輕。請向您的獸醫報告這些情況。
- 其他副作用： 如果您的貓咪開始嘔吐、食慾不振，或者您注意到牠們的眼睛或牙齦變黃（黃疸），請聯繫您的診所。
請務必按時回診，因為您的貓咪將需要頻繁進行血液和尿液檢查，特別是在治療的第一個月。
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