丁螺環酮
Buspirone
Buspirone HCl
別名: BuSpar · MJ-9022
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 |
|---|---|---|---|---|---|
| Low-grade anxieties and fears | 1 mg/kg PO q8-24h (mild anxiety); 2.5-10 mg (total dose) per dog PO q8-24h (mild anxiety); 10-15 mg per dog PO q8-12h (more severe anxiety, thunderstorm phobia) | PO | q8-24h or q8-12h | — | 🌎 NA |
| Low-grade anxieties and fears | 1-2 mg/kg PO q12h; 5-15 mg (total dose) per dog PO q8-12h | PO | q8-12h or q12h | — | 🌎 NA |
| Low-grade anxieties and fears | 5-10 mg (total dose) PO q8-12h | PO | q8-12h | — | 🌎 NA |
| Global anxiety | 0.5-2 mg/kg PO q8-12h | PO | q8-12h | may take 2-4 weeks until effect | 🌎 NA |
| Social phobias, panic disorders | 1 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
- Social phobias, panic disorders: most useful in social phobias; may also be useful for panic disorders
貓
| 適應症 | 劑量 | 途徑 | 頻次 | 療程 | 地區 |
|---|---|---|---|---|---|
| Adjunctive treatment of low-grade anxieties/fears, spraying, overgrooming | 0.5-1 mg/kg PO q8-12h; 2.5-5 mg (total dose) per cat PO q8-12h | PO | q8-12h | 6-8 weeks | 🌎 NA |
| Adjunctive treatment of low-grade anxieties/fears, spraying, overgrooming | 2.5-5 mg (total dose) PO once a day to 3 times a day | PO | q8-24h | — | 🌎 NA |
| Urine marking | 2.5-7.5 mg (total dose) per cat PO q12h | PO | q12h | — | 🌎 NA |
| Adjunctive treatment of low-grade anxieties/fears, spraying, overgrooming | 0.5-1 mg/kg PO q12h; 2.5-7.5 mg (total dose) per cat PO q12h | PO | q12h | — | 🌎 NA |
| Social phobias, panic disorders | 0.5-1 mg/kg PO q8-12h | PO | q8-12h | — | 🌎 NA |
- Adjunctive treatment of low-grade anxieties/fears, spraying, overgrooming: some cats do well on once daily dosing
- Social phobias, panic disorders: most useful in social phobias; may also be useful for panic disorders
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
丁螺環酮 (Buspirone) 是一種屬於氮雜螺環酮 (azapirone) 類的非苯二氮平類抗焦慮藥物。主要用於獸醫學中治療犬貓的廣泛性焦慮、輕度恐懼症以及貓的噴尿標記行為。
與苯二氮平類藥物不同，它不具備鎮靜、肌肉鬆弛或抗癲癇作用，因此非常適合長期行為控制且不會造成明顯的認知或精神運動功能障礙。
臨床要點：
- 延遲起效： 此藥物需要長期給藥（通常 1 至 4 週）以改變受體密度並達到完全的臨床療效。
- 不適用於急性恐慌： 由於起效緩慢，它不適合也無法作為急性、情境恐慌（例如立即的雷雨恐懼或急性分離焦慮發作）的單一療法。
- 社交動態： 它對於與社交互動相關的焦慮特別有用，且在多貓家庭中的效果可能比單貓家庭更好。
作用機轉
Buspirone is an anxioselective agent that acts primarily as a partial agonist at serotonin (5-HT1A) receptors and as an agonist/antagonist at presynaptic dopamine (D2) receptors in the CNS.
- Serotonin Pathway: By binding to 5-HT1A autoreceptors → it slows the neuronal firing rate → decreasing the depletion of serotonin stores and modulating serotonergic tone over time.
- Receptor Specificity: It does not share mechanisms with benzodiazepines; it has no significant affinity for benzodiazepine receptors and does not affect GABA binding.
安全性與警告
禁忌症
- Severe hepatic disease (use with caution)
- Severe renal disease (use with caution)
- Aggressive animals (may reduce disinhibition)
- Working dogs (use with caution despite low sedation)
- Acute situational anxieties (as sole therapy)
不良反應
- Bradycardia
- Gastrointestinal disturbances
- Stereotypic behaviors
- Increased affection (cats)
- Paradoxical aggression/turning on attackers (previously timid cats)
- Dizziness (humans)
- Headache (humans)
- Nausea/anorexia (humans)
- Restlessness (humans)
- Tachycardia (rare)
注意事項
Buspirone should be used with caution in patients with significant renal or hepatic disease. Because buspirone may reduce disinhibition, it should be used with caution in aggressive animals. While it has far less sedating properties than many other anxiolytic drugs, it should be used with caution in working dogs. It often takes a week or more for effect, so it should not be used as the sole therapy for situational anxieties. Avoid use during nursing if possible, as it is distributed into maternal milk.
藥物交互作用
May be used in combination, but dosage reductions may be necessary to minimize adverse effects
Potentially could cause increased CNS depression
May cause increased buspirone plasma levels and adverse effects
May cause increased buspirone plasma levels and adverse effects
May cause increased buspirone plasma levels and adverse effects
May cause increased buspirone plasma levels and adverse effects
Use with buspirone is not recommended because dangerous hypertension may occur
May cause decreased buspirone plasma levels
Use with buspirone may cause increased ALT
May cause increased buspirone plasma levels
監測
- Efficacy (reduction in anxiety, spraying, or fear behaviors)
- Adverse effect profiles (GI upset, behavioral changes)
藥物動力學
吸收
In humans, rapidly and completely absorbed but high first-pass effect limits systemic bioavailability to ~5%. In cats, oral peak levels occur in about 1.4 hours, but oral bioavailability appears significantly lower than in humans. Transdermal administration (PLO-base) does not yield detectable levels.
分佈
Binding to plasma proteins is very high (95%). Highest tissue concentrations in lungs, kidneys, and fat. Distributed into maternal milk.
代謝
Hepatically metabolized to several metabolites, including one active metabolite (1-PP).
排除
Metabolites are excreted primarily in the urine.
過量
Limited information is available in veterinary species. The oral LD50 in dogs is 586 mg/kg.
Clinical Signs of Overdose:
- Vomiting
- Dizziness
- Drowsiness
- Miosis (constricted pupils)
- Gastric distention
Treatment: Standard overdose protocols (e.g., decontamination, supportive care) should be followed after ingestion has been determined.
可用產品
劑型
- Oral Tablets
人用標示
- Buspirone HCl Oral Tablets: 5 mg, 7.5 mg, 10 mg, 15 mg, and 30 mg (BuSpar, 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
Tablets should be stored in tight, light-resistant containers at room temperature. After manufacture, buspirone tablets have an expiration date of 36 months.
飼主須知
重要提示： 此藥物並非「速效藥」，需要持續給藥。
- 需要耐心： 通常需要每天服用 1 到 4 週才能看到寵物行為的明顯改善。
- 不可僅在需要時服用： 必須每天按時給藥。僅在壓力事件（如雷雨）發生時才給藥是無效的。
- 貓咪的行為改變： 如果在多貓家庭中使用，原本膽小的貓咪可能會變得更有自信，甚至可能反抗或攻擊原本欺負牠的貓咪。請密切觀察牠們的互動。
- 副作用： 通常非常安全。您可能會注意到輕微的腸胃不適、頭暈或親人程度的改變（貓咪可能會變得異常黏人）。
- 漏藥處理： 如果忘記給藥，請在想起來時盡快補給，但絕對不要一次給予雙倍劑量。
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