阿普唑侖
Alprazolam
別名: Xanax XR · Niravam · Alprazolam Intensol · D65 MT · U 31889 · alprazolamum
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
狗
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| For treatment of canine anxiety disorders | 0.01-0.1 mg/kg PO as needed for panic, not to exceed 4 mg/dog/day. Start with 1-2 mg (total dose) for a medium-sized dog. | PO | prn | — | 🌎 NA |
| For separation anxiety | 0.25 mg-2 mg (total dose) once daily to three times daily PO. | PO | q8-24h | — | 🌎 NA |
| For storm phobias | 0.02-0.4 mg/kg PO q4h as needed | PO | q4h | — | 🌎 NA |
| For storm phobias (adjunct) | 0.02 mg/kg PO as needed one hour before anticipated storm and every 4 hours as needed | PO | q4h | — | 🌎 NA |
| For phobias, night waking | 0.01-0.1 mg/kg or 0.25-2 mg (total dose) per dog PO q6-12h PO | PO | q6-12h | — | 🌎 NA |
| For acute anxiety | 0.05-0.1 mg/kg PO prn or three times a day. Administer 30-60 minutes prior to trigger event. | PO | prn or q8h | — | 🌎 NA |
| Anxiolysis and fear-related disorders | 0.01-0.1 mg/kg | PO | prn up to q6h | As needed | 🌍 EU |
- For storm phobias: Helps to minimize impact of experiencing a severe storm
- For storm phobias (adjunct): Used as an adjunct after behavior modification and prior clomipramine treatment
- Anxiolysis and fear-related disorders: Titrate up or down to the minimum effective dose. Best given ~30 mins before a fear-inducing event.
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| For treatment of feline anxiety disorders | 0.125-0.25 mg/kg PO q12h (Start at 0.125 mg/kg PO) | PO | q12h | — | 🌎 NA |
| For refractory house soiling | 0.1 mg/kg or 0.125-0.25 mg (total dose) per cat PO q8-12h | PO | q8-12h | — | 🌎 NA |
| For urine marking | 0.05-0.2 mg/kg PO q12-24h | PO | q12-24h | — | 🌎 NA |
| For fears/phobias/anxieties | 0.125-0.25 mg (total dose) PO once to three times a day. | PO | q8-24h | — | 🌎 NA |
| For acute anxiety | 0.05 mg/kg PO prn or three times a day. Administer 30-60 minutes prior to trigger event. | PO | prn or q8h | — | 🌎 NA |
| Anxiolysis and urine spraying | 0.125-0.25 mg/kg | PO | prn up to bid | As needed | 🌍 EU |
- Anxiolysis and urine spraying: Doses as low as 0.25 mg/cat q8-12h and as high as 0.6 mg/kg have been reported. Titrate down to minimum effective dose. High relapse rate for urine spraying upon withdrawal.
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
阿普唑侖 (Alprazolam) 是一種強效、短至中效的苯二氮平類 (benzodiazepine) 藥物，在獸醫學中主要用作抗焦慮藥和輕度鎮靜劑。它屬於第四級 (C-IV) 管制藥物。
主要臨床重點包括：
- 行為修飾：常作為輔助療法，用於治療恐慌症、雷雨恐懼症、分離焦慮以及不當排泄（例如貓咪的尿液記號行為）。
- 運動功能：與地西泮 (diazepam) 相比，低劑量的阿普唑侖對運動功能的負面影響較小，更適合需要活動的病患。
- 臨床要點：由於其具有高脂溶性，口服後起效迅速，若在觸發事件前 30-60 分鐘給藥，非常適合用於情境性焦慮（如雷雨、煙火）。
作用機制
Alprazolam exerts its effects by binding to specific benzodiazepine receptors located on the GABA-A receptor complex in the central nervous system.
- Mechanism: Binding → enhances the affinity of the receptor for gamma-aminobutyric acid (GABA) → increases the frequency of chloride channel opening → cellular hyperpolarization → decreased neuronal excitability.
- Target Areas: It primarily depresses subcortical levels of the CNS, specifically the limbic system, thalamus, and hypothalamus.
- Net Effect: This enhanced inhibitory neurotransmission produces the characteristic anxiolytic, sedative, skeletal muscle relaxant, and anticonvulsant effects.
安全性與警告
禁忌症
- Known benzodiazepine hypersensitivity
- Aggressive animals (controversial; anxiety reduction may disinhibit aggressive tendencies)
不良反應
- Sedation
- Increased appetite (polyphagia)
- Transient ataxia
- Behavior changes in cats (irritability, increased affection, depression, aberrant demeanor)
- Paradoxical CNS excitement/agitation (rare in dogs)
- Physical dependence (with chronic use)
- Impeded learning and retarded training
注意事項
Caution: Use with care in patients with hepatic or renal disease, narrow-angle glaucoma, and in debilitated or geriatric patients.
- Working Animals: Benzodiazepines may impair the abilities of working or service animals.
- Aggression: Use in aggressive dogs remains controversial as it may remove anxiety-based bite inhibition.
- Pregnancy: FDA Category D in humans. May cause congenital abnormalities if administered during the first trimester. Use only when benefits clearly outweigh risks.
- Hepatic Function: Monitor hepatic enzymes, particularly in cats receiving chronic therapy, due to the risk of idiosyncratic hepatotoxicity associated with some oral benzodiazepines.
藥物相互作用
May slow the rate, but not the extent of oral absorption of alprazolam; administer 2 hours apart.
Additive CNS depression effects may occur.
Serum levels of digoxin may be increased; monitor for toxicity.
Increased alprazolam levels.
Metabolism of alprazolam may be decreased, leading to excessive sedation.
May induce hepatic microsomal enzymes and decrease the pharmacologic effects of benzodiazepines.
Alprazolam may increase levels of these drugs; concurrent use with clomipramine may improve efficacy for phobias.
Inhibits alprazolam metabolism, potentially increasing sedation and toxicity
Inhibits alprazolam metabolism
Used concurrently as an adjunct, but may have additive CNS depressant effects
監測
- Clinical efficacy (reduction in anxiety/panic)
- Adverse effects (excessive sedation, paradoxical excitation)
- Hepatic enzymes (particularly when treating cats chronically)
藥物動力學
吸收
Well absorbed orally with an intermediate onset of action. Peak plasma levels occur in 1-2 hours (in humans).
分佈
Highly lipid soluble and widely distributed throughout the body. Readily crosses the blood-brain barrier. Approximately 80% bound to plasma proteins.
代謝
Metabolized in the liver to at least two metabolites, including alpha-hydroxy-alprazolam which is pharmacologically active.
排除
Elimination half-lives range from 6-27 hours in humans.
過量
Overdoses are generally limited to CNS signs, primarily dose-dependent CNS depression.
- Clinical Signs: Ataxia, lethargy, disorientation, and vomiting. Some animals may present with a paradoxical reaction (hyperactivity, vocalization, agitation) which may be followed by CNS depression. Severe signs like hypotension, respiratory depression, and cardiac arrest are quite rare in small animals.
- Toxicity: The reported LD50 in rats is >330 mg/kg, but cardiac arrest has occurred at doses as low as 195 mg/kg.
- Treatment: Consists of standard protocols for decontamination. The decision to give activated charcoal should be weighed carefully against the risk of aspiration if the patient is sedated. Flumazenil can be used to reverse the sedative effects, but is generally reserved for cases with significant CNS and respiratory depression.
可用產品
劑型
- Extended-release oral tablets
- Orally disintegrating tablets
- Oral solution
人用標示
- Alprazolam Oral Tablets: 0.25 mg, 0.5 mg, 1 mg & 2 mg (Xanax, generic)
- Alprazolam Extended-release Oral Tablets: 0.5 mg, 1 mg, 2 mg, & 3 mg (Xanax XR, generic)
- Alprazolam Orally Disintegrating Tablets: 0.25 mg, 0.5 mg, 1 mg, & 2 mg (Niravam)
- Alprazolam Oral Solution: 1 mg/mL in 30 mL (Alprazolam Intensol)
各地核准狀態
POM (Prescription Only Medicine). Subject to controlled drug regulations depending on member state.
POM. Controlled drug.
暫無法規資料: 🇺🇸 US · 🇭🇰 HK · 🇹🇼 TW · 🇯🇵 JP · 🇰🇷 KR · 🇦🇺 AU
儲存與穩定性
Store tablets at room temperature in tight, light-resistant containers. Orally disintegrating tablets must be protected from moisture. Compounded oral suspensions (1 mg/mL in Ora-Plus/Ora-Sweet) retain >90% potency for 60 days at 5°C and 25°C, but should be protected from light.
飼主須知
- 給藥時機非常重要：對於情境性焦慮（如雷雨或煙火），請在預期事件發生前約 30 至 60 分鐘給藥，以確保藥物在寵物陷入恐慌前發揮作用。
- 餵藥方式：如果您在餵食藥丸時遇到困難，可以考慮使用口腔崩解錠。但在拿取藥片前，請確保雙手完全乾燥。
- 注意事項：如果您發現寵物出現過度嗜睡、嚴重步態不穩，或眼白、牙齦發黃（黃疸）的情況（特別是貓咪），請立即聯繫您的獸醫師。
- 行為改變：有些寵物可能會變得異常黏人、易怒，甚至變得更活躍（矛盾反應）。如果發生這種情況，請告知您的獸醫師。
- 訓練影響：此藥物可能會在訓練期間暫時減緩寵物學習新指令的能力。
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