格列本脲 (Glyburide / Glibenclamide)
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。
作用機制: 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.
各物種劑量
- Non-insulin dependent diabetes mellitus (NIDDM) · 0.625 mg (1/2 of a 1.25 mg tablet) · PO · once daily · Initial dose
- Non-insulin dependent diabetes mellitus (NIDDM) · 2.5 mg (total dose) · PO · twice a day · 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。請務必對照最新藥品仿單及個別病患確認。
給藥途徑
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)
藥物相互作用
- Alcohol · A disulfiram-like reaction (anorexia, nausea, vomiting) is possible
- Azole Antifungals (ketoconazole, itraconazole, fluconazole) · May increase plasma levels of glyburide
- Beta-blockers · May potentiate hypoglycemic effect
- Chloramphenicol · May displace glyburide from plasma proteins
- Cimetidine · May potentiate hypoglycemic effect
- Corticosteroids · May reduce efficacy
- Thiazide Diuretics · May reduce hypoglycemic efficacy
- Isoniazid · May reduce hypoglycemic efficacy
- MAO Inhibitors · May potentiate hypoglycemic effect
- Niacin · May reduce hypoglycemic efficacy
- Phenothiazines · May reduce hypoglycemic efficacy
- Phenytoin · May reduce hypoglycemic efficacy
- Probenecid · May potentiate hypoglycemic effect
- Sulfonamides · 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
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.
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