格列吡嗪
Glipizide
Glydiazinamide
別名: Glucotrol XL · Metaglip · Minodiab · CP-28720 · glipizidum · glydiazinamide · K-4024
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
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
各物種劑量
🌎 NA — North America🌍 EU — Europe
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Diabetes mellitus (non-ketotic, relatively healthy) | 2.5 mg per cat (initially), may increase to 5 mg per cat | PO | q12h | Ongoing if stable | 🌎 NA |
| Diabetes mellitus | 2.5-5 mg per cat | PO | q12h | 2-3 months trial | 🌎 NA |
| Diabetes mellitus (mild weight loss, non-ketoacidotic, no peripheral neuropathy) | 2.5 mg (total dose) | PO | q12h | — | 🌎 NA |
| Diabetes mellitus | 5 mg per cat, may increase to 7.5 mg (maximum) | PO | q12h | 4-8 weeks trial | 🌎 NA |
| Non-ketotic diabetes mellitus | 2.5-5 mg per cat | PO | q12h | — | 🌍 EU |
- Diabetes mellitus (non-ketotic, relatively healthy): Give in conjunction with a meal. Perform spot BG checks every 3-4h for initial 12-18h. Increase dose to 5 mg BID after 2 weeks if hyperglycemia persists and no adverse reactions occur.
- Diabetes mellitus: Combine with dietary fiber therapy. Evaluate every 1-2 weeks. If fasting BG remains >200 mg/dL after 2-3 months, discontinue and institute insulin.
- Diabetes mellitus: Decrease dose if hypoglycemia occurs. Response may be delayed; evaluate over 4-8 weeks before determining efficacy.
- Non-ketotic diabetes mellitus: Start at the lower end of the dose range, increasing the dose as required if no adverse effects are reported after 2 weeks.
劑量為持牌獸醫專業人員的臨床參考。請務必對照最新藥品說明書及個別病患確認。
概覽
格列吡嗪 (Glipizide) 是一種第二代口服磺醯脲類抗糖尿病藥物，主要用於人類的第二型糖尿病，但在獸醫學中也有特定應用，特別是針對貓病患。
- 貓的應用：對於仍具有功能性胰臟β細胞的單純性糖尿病貓可能有效。大約 20% 至 30% 新診斷的糖尿病貓對格列吡嗪治療有反應。
- 臨床實用性：通常保留用於飼主絕對拒絕注射胰島素（通常因為害怕針頭），或者貓在極低劑量胰島素下控制良好且飼主希望轉換為口服藥物的情況。
- 狗的限制：格列吡嗪對狗通常無效。當狗出現臨床高血糖症狀時，牠們通常已處於絕對或相對的胰島素缺乏狀態（類似人類第一型糖尿病），缺乏格列吡嗪發揮作用所需的功能性β細胞。
- 臨床要點：格列吡嗪試驗需要耐心；可能需要 4 到 8 週 才能觀察到完整的治療效果。此外，貓長期使用可能會促進胰島澱粉樣蛋白沉積增加，潛在加速剩餘β細胞的破壞。
作用機制
Glipizide lowers blood glucose concentrations by stimulating the release of endogenous insulin from the pancreas and enhancing peripheral insulin sensitivity.
- Pancreatic Mechanism: Glipizide binds to the sulfonylurea receptor 1 (SUR1) on the membrane of pancreatic β-cells → This binding closes ATP-sensitive potassium (K+) channels → Decreased potassium efflux leads to cellular depolarization → Depolarization opens voltage-dependent calcium (Ca2+) channels → Calcium influx triggers the exocytosis of insulin-containing secretory granules.
- Extrapancreatic Effects: Ongoing use enhances peripheral tissue sensitivity to circulating insulin and reduces the production of hepatic basal glucose, though the exact mechanisms for these secondary effects remain partially unexplained.
安全性與警告
禁忌症
- Severe burns, trauma, or infection
- Diabetic coma or other hypoglycemic conditions
- Major surgery
- Ketosis, ketoacidosis, or other significant acidotic conditions
- Known hypersensitivity to sulfonylureas
- Diabetic ketosis / ketoacidosis
- Hepatic impairment
- Renal impairment
- Absolute insulin deficiency (Type I diabetes)
- Insulin resistance
不良反應
- Gastrointestinal upset (anorexia, vomiting in ~15% of cats)
- Hypoglycemia (severe cases are rare)
- Hepatotoxicity (cholestatic jaundice and elevated liver enzymes in ~8% of cats)
- Increased pancreatic amyloid deposit formation
- Allergic skin reactions (reported in humans)
- Bone marrow suppression (reported in humans)
- Jaundice (hepatotoxicity)
- Skin rashes
- Fever
注意事項
Important: Glipizide should be used with extreme caution in patients with untreated adrenal or pituitary insufficiency, thyroid impairment, renal or hepatic function impairment, prolonged vomiting, high fever, malnourishment, or debilitated conditions.
- Efficacy Loss: While initially effective, glipizide may become ineffective weeks to months after starting therapy, eventually requiring a transition to insulin.
- Concurrent Endocrine Disease: Conditions causing excessive cortisol or growth hormone production (e.g., hyperadrenocorticism, acromegaly) can antagonize insulin effects and must be ruled out before initiating therapy.
- Hepatic Monitoring: Monitor liver enzymes closely. Discontinue if ALT exceeds 500 IU/L or if icterus develops.
藥物相互作用
May cause a disulfiram-like reaction (anorexia, nausea, vomiting)
May increase plasma levels of glipizide
May potentiate hypoglycemic effect and mask signs of hypoglycemia
May displace glipizide from plasma proteins, increasing effect
May potentiate hypoglycemic effect
May antagonize insulin effects and reduce glipizide 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 glipizide from plasma proteins, increasing effect
May reduce hypoglycemic efficacy
May reduce hypoglycemic effect
May displace glipizide from plasma proteins
May enhance the hypoglycemic effects of glipizide
May enhance the hypoglycemic effects of glipizide
May enhance the hypoglycemic effects of glipizide
May enhance the hypoglycemic effects of glipizide
監測
- Physical examination and body weight (weekly during first month)
- Urine glucose and ketones
- Serial blood glucose measurements or spot checks
- Liver enzymes (ALT, AST, ALP) and bilirubin (every 1-2 weeks initially)
- Complete Blood Count (CBC)
- Clinical signs of hypoglycemia or gastrointestinal distress
- Blood glucose curves
- Fructosamine levels
- Liver enzymes (ALT, AST, ALP, Bilirubin)
- Renal function (BUN, Creatinine)
- Clinical signs of diabetes (water intake, urination, weight)
藥物動力學
半衰期
吸收
Rapidly and practically completely absorbed after oral administration. Absolute bioavailability in humans is 80-100%. Food alters the rate, but not the extent, of absorption. Transdermal administration in cats is not adequately absorbed.
分佈
Very highly bound to plasma proteins.
代謝
Primarily biotransformed in the liver to inactive metabolites.
排除
Metabolites are excreted primarily by the kidneys.
過量
Toxicity Profile: Oral LD50 is greater than 4 g/kg in all tested animal species. The primary and most dangerous consequence of an overdose is profound hypoglycemia.
Management:
- Decontamination: Employ gut-emptying protocols (emesis, activated charcoal) if the ingestion is recent and the patient is asymptomatic.
- Treatment: Monitor blood glucose closely. Administer parenteral glucose (e.g., IV dextrose bolus followed by a CRI) as needed.
- Monitoring: Because of its relatively short half-life, prolonged hypoglycemia is less likely compared to older sulfonylureas (like chlorpropamide), but blood glucose monitoring and supportive care may still be required for several days. Massive overdoses may require monitoring of blood gases and serum electrolytes.
可用產品
劑型
- Oral extended-release tablets
- Oral film-coated tablets (in combination with metformin)
- 2.5 mg oral tablets
獸醫用
- None
人用標示
- Glipizide Oral Tablets: 5 mg & 10 mg (Glucotrol, generic)
- Glipizide Oral Extended Release Tablets: 2.5 mg, 5 mg, & 10 mg (Glucotrol XL, generic)
- Glipizide/Metformin Hydrochloride Tablets: 2.5 mg/250 mg, 2.5 mg/500 mg, 5 mg/500 mg (Metaglip, generic)
- Minodiab 2.5 mg tablets
- Minodiab 5 mg tablets
- Generic Glipizide tablets
各地核准狀態
POM (Prescription Only Medicine)
POM-V (Prescription Only Medicine - Veterinarian)
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored in tight, light-resistant containers at room temperature.
飼主須知
您的獸醫師開立了格列吡嗪 (Glipizide) 來幫助控制您愛貓的糖尿病。這種藥物的作用是刺激貓咪的胰臟釋放更多胰島素。
- 耐心是關鍵：可能需要 4 到 8 週 才能看到這種藥物的完整療效。除非獸醫師指示，否則請勿自行停藥。
- 注意低血糖症狀：症狀包括虛弱、步態不穩、嗜睡、肌肉抽搐或癲癇發作。如果您觀察到這些症狀，請在貓咪的牙齦上塗抹一點玉米糖漿或蜂蜜，並立即聯繫您的獸醫師。
- 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。
- 副作用：有些貓咪可能會出現嘔吐或食慾不振，特別是在剛開始服藥時。如果嘔吐嚴重或持續超過幾天，或者您注意到眼睛/牙齦變黃（黃疸），請聯繫您的獸醫師。
- 飲食：請按照指示將此藥物與食物一起餵食，並堅持獸醫師推薦的特定飲食（通常是高蛋白/低碳水化合物或高纖維飲食）。
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