氯拉西泮
Clorazepate
Clorazepate dipotassium
別名: Tranxene-SD · Gen-Xene · Tranxene T-tab · Abbott-35616 · AH-3232 · 4306-CB · clorazepic acid · dipotassium clorazepate · dikalii clorazepas
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
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Adjunctive medication in the treatment of seizures (in combination with phenobarbital) | 1-2 mg/kg PO q12h, but may need to divide q12h dose and give q8h to minimize adverse effects and maintain therapeutic levels | PO | q8-12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures (in combination with phenobarbital) | 0.5-1 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 1-2 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Adjunctive medication in the treatment of seizures | 2-4 mg/kg PO twice daily, some dogs may require three times daily | PO | q8-12h | — | 🌎 NA |
| Third-line agent for seizures | 1-2 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Management of cluster seizures | 0.5-2 mg/kg two to three times daily | PO | q8-12h | 48-96 hours | 🌎 NA |
| Adjunctive therapy for fears and phobias | 11.25-22.5 mg per dog PO once to twice daily | PO | q12-24h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 22.5 mg for large dogs, 11.25 mg for medium dogs and 5.6 mg for small dogs PO | PO | prn | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.55-2.2 mg/kg PO as needed up to q8h | PO | up to q8h | — | 🌎 NA |
| Adjunctive therapy for fears and phobias | 0.2-1 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
- Adjunctive medication in the treatment of seizures (in combination with phenobarbital): No advantage gained with using sustained release products. May affect phenobarb levels; monitor 2 and 4 weeks later.
- Management of cluster seizures: Give immediately after first seizure and stop after 48-96 hours. Used only during seizure activity, not as maintenance.
- Adjunctive therapy for fears and phobias: Recommends the sustained-delivery product (Tranxene-SD).
- Adjunctive therapy for fears and phobias: Using sustained delivery product. Adjust dosage according to dog's response.
- Adjunctive therapy for fears and phobias: Titrate to clinical sedation; dose may vary for individual dogs.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Anxiolytic or for compulsive behaviors | 0.2-0.5 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Alternative drug to phenobarbital for seizures | 3.75-7.5 mg (total dose per cat) PO once to twice daily | PO | q12-24h | — | 🌎 NA |
- Alternative drug to phenobarbital for seizures: Similar precautions are necessary as described for diazepam use in cats (risk of hepatic necrosis).
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
氯拉西泮（Clorazepate）是一種苯二氮平類（Benzodiazepine）藥物，在獸醫學中主要用作輔助抗癲癇藥，以及治療與焦慮或恐懼相關的行為障礙。
- 臨床要點：它是一種前驅藥，需要胃酸環境才能迅速脫羧成為活性代謝物去甲地西泮（Nordiazepam），隨後被吸收。
- 在犬隻中，常與苯巴比妥合用治療難治性癲癇。雖然對其抗癲癇效果可能會產生耐受性，但據報導其耐受速度慢於氯硝西泮（Clonazepam）。
- 在貓咪中，可用作抗焦慮藥，有時也作為苯巴比妥的替代品來控制癲癇，但由於口服苯二氮平類藥物在貓咪中有引發特異質性肝毒性的風險，因此需要謹慎使用。
作用機轉
Benzodiazepines exert their effects by enhancing the inhibitory activity of gamma-aminobutyric acid (GABA) in the central nervous system.
- Mechanism: They bind to specific allosteric sites on the GABA-A receptor complex → increases the frequency of chloride channel opening → cellular hyperpolarization → decreased neuronal excitability.
- This depression of subcortical CNS levels (primarily limbic, thalamic, and hypothalamic) produces the characteristic anxiolytic, sedative, skeletal muscle relaxant, and anticonvulsant effects.
- Other postulated mechanisms include antagonism of serotonin and diminished release or turnover of acetylcholine in the CNS.
安全性與警告
禁忌症
- Hypersensitivity to benzodiazepines
- Significant liver disease/dysfunction
- Acute narrow angle glaucoma
- Fear-induced aggression (relative contraindication; may disinhibit bite inhibition)
不良反應
- Sedation (most common)
- Ataxia
- Physical dependence (with chronic use)
- Acute hepatic necrosis (idiosyncratic in cats)
- Paradoxical excitation or disinhibition of aggression
注意事項
Use with extreme caution in aggressive animals, particularly those with fear-induced aggression, as benzodiazepines can disinhibit anxiety-based bite inhibition and provoke attacks. Benzodiazepines may exacerbate myasthenia gravis. Safe use during pregnancy is not established (FDA Category D in humans; teratogenic effects noted in lab animals). The active metabolite, nordiazepam, is distributed into milk and may affect nursing neonates. Abrupt withdrawal after chronic use can precipitate severe rebound seizures.
藥物交互作用
May increase serum levels of benzodiazepines by inhibiting their metabolism.
May decrease the metabolism of benzodiazepines, leading to prolonged effects.
Additive CNS depression; may cause profound sedation or respiratory depression.
May decrease the metabolism of benzodiazepines.
Complex interaction: Clorazepate may initially increase phenobarbital serum levels. Over time, clorazepate levels may decrease, leading to decreased phenobarbital levels. Requires close monitoring.
May decrease clorazepate concentrations.
May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines.
監測
- Clinical efficacy (seizure frequency or behavioral improvement)
- Adverse effects (sedation, ataxia)
- Liver enzymes (especially critical in cats due to risk of acute hepatic necrosis)
- Phenobarbital serum levels (if used concurrently, monitor at 2 and 4 weeks after adding clorazepate)
藥物動力學
吸收
In dogs, peak serum levels generally occur within 1-2 hours.
分佈
Volume of distribution is about 1.8 L/kg after multiple dosing in dogs. Nordiazepam is distributed into milk.
代謝
Clorazepate is a prodrug that is rapidly decarboxylated in the acidic environment of the stomach to nordiazepam (active) and other metabolites.
排除
Eliminated primarily via hepatic metabolism and subsequent renal excretion of metabolites.
過量
When used alone, clorazepate overdoses are generally limited to significant CNS depression (confusion, coma, decreased reflexes, profound sedation).
- Treatment: Consists of standard protocols for removing and/or binding the drug in the gut (e.g., emesis if asymptomatic and recent, activated charcoal) and supportive systemic measures.
- The use of analeptic agents (CNS stimulants such as caffeine, amphetamines) is generally not recommended.
- Flumazenil (a specific benzodiazepine reversal agent) may be considered for very serious, life-threatening overdoses.
可用產品
劑型
- Capsules
- Sustained-release tablets
人用標示
- Clorazepate Dipotassium Tablets: 3.75 mg, 7.5 mg, & 15 mg (Tranxene T-tab; generic)
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
Clorazepate dipotassium is unstable in the presence of water. Keep the desiccant packets in the original container of the capsules and tablets. Consider adding a desiccant packet to the prescription vial when dispensing large quantities.
飼主須知
重要警告：請勿突然停止給藥。突然停藥可能會引發嚴重且危及生命的戒斷性癲癇。如果需要停藥，請務必諮詢獸醫以制定逐漸減量的計畫。
- 按時給藥是關鍵：抗癲癇治療失敗的一個主要原因是漏服藥物。請每天在固定的時間給藥。
- 貓咪飼主請注意：如果您的貓咪出現食慾不振、嘔吐，或眼白/牙齦發黃（黃疸）的現象，請立即聯繫您的獸醫，這可能表示出現了嚴重的肝臟不良反應。
- 副作用：您的寵物可能會顯得嗜睡、動作不協調或笨拙，尤其是在剛開始服藥時。這些症狀通常會在身體適應後改善。
- 儲存方式：請將藥物保存在帶有乾燥劑的原包裝容器中，因為該藥物接觸水分後會迅速降解。
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