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二氮嗪

Diazoxide

7-chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide

直接血管擴張劑 / 升血糖劑POIV狗貓雪貂

別名: Proglycem · Hyperstat IV · Eudemine · Glicemin · Hypertonalum · Proglicem · Sefulken · Tensuril · diazoxidum · NSC-64198 · Sch-6783 · SRG-95213

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

經審核的 v13 劑量證據

結構化劑量計算證據

Medical management of insulinoma after stabilization of hypoglycemic crisis

5–30 mg/kgPO
  • q12h
必須同時考慮的臨床上下文 (1)
  • Once hypoglycemic crisis stabilized
textbook方案年份 2021審核 dose-audit-v13

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概覽

二氮嗪（Diazoxide）是一種非利尿性噻嗪類衍生物，在獸醫學中主要用於犬和雪貂的​胰島素瘤​（分泌胰島素的胰島細胞瘤）的內科管理。

雖然它具有強效的直接血管擴張特性（在人類中靜脈注射用於高血壓急症），但其在動物中的口服應用主要是利用其顯著的​升血糖​副作用。透過拮抗胰島素的釋放，它有助於穩定難治性低血糖患者的血糖濃度。

​臨床要點：​

  • 當單獨使用飲食管理（少量多餐）和糖皮質激素（如潑尼松）無法控制低血糖危機時，通常會結合本藥物使用。
  • 由於其結構與噻嗪類利尿劑相似，可能會引起鈉和水瀦留，但它缺乏利尿效果。

作用機制

Diazoxide exerts its hyperglycemic and vasodilatory effects via multiple mechanisms:

  • K+ ATP Channel Activation: It binds to the sulfonylurea receptor 1 (SUR1) subunit of the ATP-sensitive potassium (K+ ATP) channels on pancreatic beta cells → channel opening → cellular hyperpolarization → decreased intracellular ​calcium (Ca2+)​ influx → inhibition of insulin exocytosis from secretory granules.
  • Beta-Adrenergic Stimulation: Stimulates the release of epinephrine, which promotes hepatic glycogenolysis and inhibits peripheral cellular glucose uptake.
  • Vasodilation: Directly relaxes arteriolar smooth muscle by opening K+ ATP channels in vascular smooth muscle cells → hyperpolarization → vasodilation → decreased peripheral vascular resistance and blood pressure.

安全性與警告

禁忌症

  • Hypoglycemia secondary to insulin overdosage in diabetic patients
  • Hypersensitivity to thiazide diuretics (unless benefits outweigh risks)
  • Hypersensitivity to thiazides
  • Functional hypoglycemia (non-insulinoma)

不良反應

  • Hypersalivation
  • Tachycardia
  • Agranulocytosis
  • Aplastic anemia
  • Thrombocytopenia
  • Diabetes mellitus
  • Sodium and water retention
  • Malaise (ferrets)
  • Bone marrow suppression (ferrets)
  • Gastrointestinal upset (anorexia, vomiting, diarrhea)
  • Hyperglycemia
  • Cataracts (rare)
  • Bone marrow suppression (rare)

注意事項

Caution: Use with extreme care in patients with congestive heart failure (CHF) or renal disease due to sodium and water retention properties.

  • Hepatic Disease: Adverse effects may be more pronounced in dogs with concurrent hepatic disease.
  • Pregnancy: FDA Category C; animal studies have shown adverse effects on the fetus. Use only if benefits outweigh risks.
  • Laboratory Interference: May cause a false-negative insulin response to the glucagon-stimulation test and displace bilirubin from plasma proteins.

藥物相互作用

Alpha-adrenergic agents (e.g., phenoxybenzamine)

May decrease the effectiveness of diazoxide in increasing glucose levels

Hypotensive agents (e.g., hydralazine, prazosin)

Diazoxide may enhance the hypotensive actions of other hypotensive agents

Phenothiazines (e.g., acepromazine, chlorpromazine)

May enhance the hyperglycemic effects of diazoxide

Phenytoin

Diazoxide may increase the metabolism, or decrease the protein binding of phenytoin

Thiazide diuretics (e.g., hydrochlorothiazide)

May potentiate the hyperglycemic effects of oral diazoxide. Can be used synergistically, but caution is advised as hypotension may occur

Thiazide diureticsModerate

Potentiate hyperglycemic and hyperuricemic effects

PhenothiazinesModerate

May potentiate hyperglycemia

Alpha-adrenergic blockersModerate

May antagonize the effects of diazoxide

Highly protein-bound drugs (e.g., NSAIDs, warfarin)Moderate

Diazoxide is highly protein-bound and may displace or be displaced by other drugs, altering free drug concentrations

監測

  • Blood (serum) glucose
  • CBC (at least every 3-4 months)
  • Physical exam (monitor for clinical signs of adverse effects like edema, cataracts, or tachycardia)
  • Blood glucose
  • Electrolytes (sodium, potassium)
  • Complete blood count (CBC) periodically
  • Signs of fluid retention/edema

藥物動力學

半衰期

狗~5 hours

吸收

In humans, serum diazoxide levels peak at about 12 hours after dosing with capsules. Blood levels required for hyperglycemic effects are unknown.

分佈

Highest concentrations are found in the kidneys, with high levels also in the liver and adrenal glands. Approximately 90% is bound to plasma proteins. It crosses the placenta and enters the CNS.

代謝

Partially metabolized in the liver.

排除

Excreted as both metabolites and unchanged drug by the kidneys. Serum half-life is prolonged in patients with renal impairment.

過量

Acute overdosage may result in severe hyperglycemia and ketoacidosis.

  • Treatment: Administer insulin, intravenous fluids, and correct electrolyte imbalances.
  • Monitoring: Intensive and prolonged monitoring of blood glucose and acid-base status is highly recommended.

可用產品

劑型

  • Oral capsules
  • Oral suspension
  • 15 mg/ml injectable solution (special order)
  • 50 mg oral tablet

獸醫用

  • None

人用標示

  • Diazoxide Oral Capsules: 50 mg (Proglycem)
  • Diazoxide Oral Suspension: 50 mg/mL with sorbitol in 30 mL calibrated dropper (Proglycem)
  • Eudemine 50 mg tablet
  • Eudemine 15 mg/ml injectable solution

各地核准狀態

European Union✓ 已核准處方藥EMA

POM (Prescription Only Medicine)

United Kingdom✓ 已核准處方藥VMD

POM (Prescription Only Medicine)

暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU

儲存與穩定性

Store capsules and oral suspensions at 2-30°C and protect from light. Protect solutions/suspensions from freezing. Do not use darkened solutions/suspensions, as they may be subpotent.

飼主須知

  • ​用途​：本藥物用於預防由分泌胰島素的腫瘤（胰島素瘤）引起的危及生命的血糖下降。
  • ​給藥方式​：據報導該藥物非常苦。與食物一起給藥有助於掩蓋味道並減少嘔吐或腹瀉等胃腸道副作用。調劑藥局可能可以將其配製成無糖的調味液體。
  • ​監測​：密切觀察您的寵物是否有​高血糖​（過度口渴、排尿增加）或​低血糖​復發（虛弱、步態不穩、癲癇、嗜睡）的跡象。
  • ​副作用​：如果您發現異常出血、嚴重的嘔吐/腹瀉或腫脹（體液瀦留），請聯繫您的獸醫師。

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