勞拉西泮 (Lorazepam)
Lorazepam
7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-2H-1,4-benzodiazepin-2-one
別名: Ativan · Lorazepam Intensol · BRN-07599084 · CB-8133 · Ro-7-8408 · Wy-4036 · lorazapamum · anxiedin · azurogen · bonatranquan · delormetazepam · lorazin · lorazon · lorenin · norlormetazepam · novhepar · novolorazem · oChloroxazepam · sinestron · Lorazepamum
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 |
|---|---|---|---|---|---|
| Status epilepticus (alternative to diazepam) | 0.2 mg/kg IV, IM or intranasal once | IV/IM/intranasal | once | — | 🌎 NA |
| Status epilepticus | 0.2 mg/kg IV once, followed by a bolus IV loading dose of levetiracetam at 60 mg/kg | IV | once | — | 🌎 NA |
| Fears, anxieties, phobias | 0.02-0.1 mg/kg PO once daily to three times a day | PO | q8-24h | — | 🌎 NA |
| Anxiolytic | 0.05-0.25 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Fears/anxiety | 0.02-0.5 mg/kg PO q8h | PO | q8h | — | 🌎 NA |
| Fears, anxieties, phobias, aversions | 0.02-0.1 mg/kg q8-24h | PO | q8-24h | — | 🌎 NA |
| Short-term management of anxiety disorders | 0.02-0.1 mg/kg | PO | q12-24h | Short-term | 🌍 EU |
- Fears, anxieties, phobias: May be used on an as needed basis
- Fears/anxiety: The lowest dose and frequency that alleviate the fear should be used
- Fears, anxieties, phobias, aversions: Minimally sedating, may require 4 weeks to peak effect
- Short-term management of anxiety disorders: Start at the lower end of the dose range and gradually increase as needed.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Fears/anxiety | 0.03-0.08 mg/kg PO q12h | PO | q12h | — | 🌎 NA |
| Fears, anxieties, phobias | 0.125 mg-0.25 mg total dose (¼-½ of a 0.5 mg tablet) once to twice a day | PO | q12-24h | — | 🌎 NA |
| Anxiolytic | 0.05-0.25 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| Short-term management of anxiety disorders | 0.02-0.1 mg/kg | PO | q12-24h | Short-term | 🌍 EU |
- Fears/anxiety: The lowest dose and frequency that alleviate the fear should be used
- Fears, anxieties, phobias: May be used on an as needed basis
- Short-term management of anxiety disorders: Start at the lower end of the dose range and gradually increase. Monitor closely for signs of hepatotoxicity.
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
勞拉西泮 (Lorazepam) 是一種強效的中效苯二氮平類藥物 (Benzodiazepine)，在獸醫學中主要用作行為障礙的抗焦慮藥，以及作為地西泮 (Diazepam) 的替代品來治療癲癇重積狀態。
臨床重點： 與地西泮不同，勞拉西泮直接進行葡萄糖醛酸結合反應，不會形成具活性的中間代謝物。這使其成為老年、肥胖或肝功能受損病患更安全的選擇。
- 給藥途徑多樣： 可透過多種途徑給藥，包括鼻內、肌肉注射和舌下/頰內，使其在家庭或診所的緊急癲癇管理中具有高度靈活性。
- 作用時間： 其療效似乎與地西泮相當，且可能具有更長的抗癲癇作用時間（儘管在犬隻中尚未被明確證實）。
作用機轉
Lorazepam acts as a positive allosteric modulator at the GABA-A receptor.
- It binds to the benzodiazepine site on the GABA-A receptor complex → enhances the affinity of the receptor for the inhibitory neurotransmitter gamma-aminobutyric acid (GABA).
- This increases the frequency of chloride channel openings → influx of chloride ions → hyperpolarization of the neuronal membrane → decreased neuronal excitability.
- This widespread CNS depression primarily affects the subcortical levels (limbic, thalamic, and hypothalamic), yielding 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
- Severe respiratory insufficiency (unless mechanically ventilated)
- Glaucoma
- Significant liver disease
- Significant kidney disease
- Pregnant animals
- Lactating animals
不良反應
- Increased appetite
- Increased activity/excitement (paradoxical reaction)
- Vocalization
- Somnolence
- Lethargy
- Disinhibition (potential emergence of aggression)
- Drowsiness
- Mild transient incoordination (ataxia)
- Tremor and inappetence (associated with acute withdrawal)
注意事項
Withdrawal: When using for negative behaviors, withdraw the drug gradually to avoid a rebound effect. Physical dependency has been induced in dogs; long-term regular usage requires gradual weaning.
Administration Warning: Injectable lorazepam must NOT be given intra-arterially; arteriospasm may occur resulting in necrosis.
Pregnancy: Designated FDA Category D in humans (evidence of fetal risk), but animal studies suggest relative safety at usual dosages. High doses just prior to delivery can cause 'floppy infant' syndrome.
藥物交互作用
Additive CNS effects
Decreased renal clearance of lorazepam
Increased CNS depression, irrational behavior
Decreased sedation from lorazepam
Increased lorazepam serum concentration
Inhibits the metabolism of lorazepam, potentially leading to increased plasma concentrations and prolonged sedation.
May inhibit the metabolism of lorazepam, increasing the risk of toxicity.
Additive CNS depression and sedation.
監測
- Clinical efficacy (seizure control or anxiety reduction)
- Adverse effects (CNS depression, paradoxical excitation, ataxia)
- Behavioral changes (watch for paradoxical aggression or extreme sedation)
- Liver enzymes (ALT, AST, ALP, Bilirubin), especially in cats
- Appetite and water intake
藥物動力學
半衰期
吸收
In humans, absolute bioavailability is ~90% orally. Rapidly and completely absorbed after IM dosing. Sublingual has similar bioavailability to oral, but peaks sooner. In dogs, intranasal administration reaches 30 ng/mL in 3-9 minutes.
分佈
High affinity for benzodiazepine receptors in the CNS. Brain concentrations may persist longer than serum levels. Small amounts are distributed into milk.
代謝
Converted into inactive glucuronide forms in the liver in most species. Lack of active metabolites makes it safer for patients with liver dysfunction.
排除
Dogs: Primary elimination route is via urine. Cats: Elimination is ~50% in urine (primarily as glucuronide) and 50% in feces.
過量
Overdoses of lorazepam are generally limited to CNS depression (confusion, lethargy, somnolence, decreased reflexes).
- Severe Toxicity: Very large overdoses can cause ataxia, hypotension, coma, and rarely death.
- Treatment: Standard protocols for removing/binding the drug in the gut (if orally ingested) and supportive systemic measures. Forced diuresis with IV fluids/electrolytes and mannitol may enhance excretion in patients with normal renal function.
- Antidote: Flumazenil may be considered for adjunctive treatment of serious overdoses, but it does not replace supportive therapy. Caution: Flumazenil is not recommended in patients with seizure disorders as it may induce seizures.
- Note: Analeptic agents (CNS stimulants like caffeine) are generally not recommended.
可用產品
劑型
- Concentrated Oral Solution
- Injection
- 1 mg oral tablets
- 2 mg/ml oral suspension
- 4 mg/ml injectable solution
人用標示
- Lorazepam Tablets: 0.5 mg, 1 mg, & 2 mg
- Lorazepam Concentrated Oral Solution: 2 mg/mL
- Lorazepam Injection: 2 mg/mL & 4 mg/mL
- Ativan 1 mg tablets
- Intensol 2 mg/ml oral suspension
- Lorazepam 4 mg/ml injectable solution
各地核准狀態
POM (Prescription Only Medicine). Subject to national controlled substance regulations.
POM-V / POM. Controlled Drug Schedule 4 Part 1.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Tablets should be stored in well-closed containers at room temperature (20-25°C). Oral solution and injection should be stored refrigerated (2-8°C) and protected from light. Injection must be diluted just prior to IV use with an equal volume of D5W, normal saline, or sterile water. Do not use if discolored or if a precipitate forms.
飼主須知
勞拉西泮是一種用於幫助控制寵物癲癇發作或處理嚴重焦慮和恐懼症的藥物。
- 食慾改變： 此藥物可能會增加寵物的食慾。可能需要嚴格限制飲食以防止體重不必要地增加。
- 行為改變： 請注意活動水平的變化。它可能導致嗜睡/無力，或者相反地，引起活動力增加、興奮和異常發聲。
- 請勿突然停藥： 未經獸醫指導，請勿突然停止治療。長期定期服用此藥物的動物如果沒有適當地「逐漸減量」，可能會出現戒斷症狀。
- 肝臟健康： 雖然目前尚未有動物因服用勞拉西泮而出現肝毒性的報告，但一種與其相似的藥物（地西泮）極少數情況下會引起貓的肝毒性。如果您發現寵物嘔吐、食慾不振或眼白/牙齦發黃，請立即聯繫您的獸醫。
- 餵藥技巧： 藥錠相對無味且容易在唾液中溶解。如果餵藥困難，可以將藥錠放在病患的臉頰內側，大約一分鐘後給予少量零食以幫助吞嚥。
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