藥理分類
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somatostatin
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Somatostatin analogue
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化學結構式
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Tetradecapeptide
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cyclic octapeptide
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機轉(相同)
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- Ø 抑制secretion of growth hormone, glucagon, insulin
- Ø 直接抑制gastrin, pancreatic polypeptide, vasoactive intestinal peptide (VIP), secretin, motilin, enteroglucagon, gastric inhibitory peptide
- Ø 抑制serotonin釋放
- Ø 抑制TSH分泌
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- Ø inhibits growth hormone, glucagon, and insulin
效果比somatostatin更強:
growth hormone : 40 ×
glucagon: 11 ×
- Ø 抑制gastrin, pancreatic polypeptide, vasoactive intestinal peptide (VIP), secretin, motilin
- Ø 抑制serotonin釋放
- Ø 抑制TSH分泌
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機轉(相異)
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- Ø 是人體內自然存在的peptide,由人體的hypothalamus, CNS, peripheral nervous system, pancreatic islet cells (D cells), thyroid C cells, the adrenal medulla, and epithelial glandular and neuronal cells of theGI tract所合成,依所存在部位而有不同功能
- Ø 抑制ACTH釋放 ,e.g. Nelson's syndrome
- Ø 抑制prolactin釋放
- Ø 抑制renin, vasopressin 功效
- Ø 抑制細胞內cAMP 生成,調控Ca2+ flux, 或刺激K+ permeability
- Ø 防止因攝食碳水化合物所引致的下食道括約肌壓力減少(讓括約肌收縮力加強)
- Ø 防止因吞嚥動作所導致的下食道括約肌放鬆(讓括約肌收縮力加強)
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- Ø 合成的somatostatin相似物
- Ø 抑制luteinizing hormone's (LH) response to gonadotrophin releasing hormone (GnRH)
- Ø reduces growth hormone and/or IGF-I (somatomedin C) in acromegaly
- Ø 抑制膽囊收縮,減少膽汁分泌
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健保適應症
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食道靜脈曲張引起的嚴重急性出血。胃潰瘍、十二指腸潰瘍、出血性胃炎引起的嚴重急性出血。胰臟手術後胰臟併發症之預防。胰臟膽及腸道廔管之輔助治療
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對手術、放射線療法或dopamine作用劑療法控制無效的肢端肥大症患者,可控制其症狀,並減少生長激素及somatomedine-C的血漿值,解除與胃腸胰臟內分泌腫瘤有關的症狀,預防胰臟手術後的併發症,治療胃食道靜脈曲張出血及預防再出血
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其他適應症
(相同)
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- Ø DM
- Ø Bleeding esophageal varices
- Ø GI bleeding
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其他適應症
(相異)
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- Ø Breast ca
- Ø Glucagnoma
- Ø Chylothorax(乳糜胸)
- Ø Endoscopic retrograde cholangiopancreatography
(ECRP內視鏡逆行性膽胰造影術)
- Ø Enterocutaneous fistula
- Ø Postprandial hypotension (飯後低血壓)(預防)
- Ø Neoplastic disease(somatostatin-receptor positive)
- Ø 胰臟手術
- Ø 胰臟炎
- Ø (Infant) 持續性hyperinsulinemic hypoglycemia
- Ø Pseudocyst of pancreas
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- Ø Vasoactive intestinal peptide-secreting tumor
- Ø Neuroendocrine tumor (輔助)
- Ø Pituitary adenoma (腦下垂體腫瘤)
- Ø Insulinoma
- Ø Carcinoid syndrome (類癌症候群)
- Ø Acromegaly
- Ø AIDS - Diarrhea or other unknown diarrhea
- Ø Lymphorrhea
- Ø acute Necrotizing pancreatitis (輔助)
- Ø Polycystic ovary syndrome
- Ø Polyostotic fibrous dysplasia of bone (輔助)
- Ø Zollinger-Ellison syndrome (輔助)
- Ø Dumping syndrome (傾食症候群)
- Ø Hypothalamic obesity
- Ø Cryptosporidiosis
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藥物動力學
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t1/2 = 2~3 min
代謝:血液循環系統
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t1/2 = 1.7~1.9 hr (cirrhosis ~ 3.7 hrs)
代謝:肝臟
排除:尿液 (Clcr < 10減量 ~ 50%)
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使用劑量
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IV
Normal: 6mg/day
Infusion rate: 250μg/hr
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IV/ SC/IM
100~500 Q8H OR 100-600μg/day分2~4次使用
(可以用到1500μg/day)
- § (infusion) dilute in NS or D5W to volume of 50-200 mL; infuse over 15-30 min
- § (IV push) give over 3 min
Infusion rate: 25~50μg/hr
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泡製
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稀釋液:NS or D5W
2 amp/ 500mL → 6000μg/ 500mL→ 12μg/mL
起初20mL IV bolus, 然後維持250μg/hr輸注→ 20mL/hr
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稀釋液:NS or D5W
Volume: 50-200 mL
醫院習慣:5 amp/ 60mL NS, run 3~6 mL/hr
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副作用
(相同)
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- 1. glucose intolerance (定時監測血糖)
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副作用
(相異)
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- 1. type 1 DM:減少insulin需求量
- 2. arrhythmias, including ventricular extrasystoles
- 3. Hyponatremia
- 4. 血壓和心跳慧暫時上升,但HTN病患反而會發生血壓降低現象
- 5. 突然停藥可能造成反彈性growth hormone過度分泌(所以不能長期使用,也限制他用於支端肥大症病患)
- 6. nausea, vomiting, diarrhea, and abdominal cramps
- 7. 用於enterocutaneous fistulas病患時須小心發生反彈性 fistula output 作用
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- 1. Cholelithiasis膽結石 (22% to 33% )
- 2. Constipation, Diarrhea, Flatulence, Nausea
- 3. Pancreatitis
- 4. Hyperglycemia (1.5% to 16%), Hypoglycemia (1.5% to 3%),
- 5. Hypothyroidism
- 6. Disorder of biliary tract
- 7. Dizziness, Headache
- 8. 注射部位疼痛
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