VetSheet

曲唑酮

Trazodone

Trazodone hydrochloride

血清素2A拮抗劑/再攝取抑制劑 (SARI)PO狗

別名: Desyrel · Oleptro · Molipaxin · AF-1161 · trazodona · sleepeasy · Trazodone hydrochloride · Trazodonum

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

1.9 mg/kg/day-16.2 mg/kg/day (mean = 7.3 mg/kg/day)PO· daily
— 🐕

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 treatment of anxiety-related disorders (Daily medication only)1.9 mg/kg/day-16.2 mg/kg/day (mean = 7.3 mg/kg/day)POdaily—🌎 NA
Adjunctive treatment of anxiety-related disorders (As needed only)2.2 mg/kg/day- 14 mg/kg/day (mean 7.7 mg/kg/day)POPRN—🌎 NA
Adjunctive treatment of anxiety-related disorders (Daily medication and as needed)1.7 mg/kg/day-19.5 mg/kg/day (mean 7.25 mg/kg/day)POdaily and PRN—🌎 NA
Adjunctive treatment of anxiety-related disorders1 mg/kg PO q12h for 7 days, then up to 3 mg/kg PO q12h.POq12h7 days initially🌎 NA
Adjunctive treatment of anxiety-related disorders1-4.8 mg/kg PO twice daily; (titrate to effect in 1 mg increments every 7 days).POq12h—🌎 NA
Adjunctive treatment of anxiety-related disorders (Situational)typical starting dose between 2-5 mg/kg and adjusting upwards as necessary to get control (maximum dose 14 mg/kg/day).POPRN—🌎 NA
  • Adjunctive treatment of anxiety-related disorders (Daily medication only): Begin at half target dose for 3 days to build tolerance.
  • Adjunctive treatment of anxiety-related disorders (Situational): Given about an hour prior to the onset of anxiety.

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。

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概覽

曲唑酮 (Trazodone) 是一種​血清素2A拮抗劑/再攝取抑制劑 (SARI)​，在獸醫學中廣泛用作抗焦慮藥和溫和的鎮靜劑。

  • ​臨床應用​：對於情境性焦慮（如雷暴、煙火、看獸醫、旅行）以及協助術後限制活動或籠內休息非常有效。
  • ​輔助治療​：常與 SSRI（如氟西汀）或加巴噴丁 (Gabapentin) 併用，治療難治性行為障礙。
  • ​安全性​：耐受性良好，安全範圍廣，與三環類抗憂鬱藥 (TCA) 相比，其抗膽鹼能副作用較少，引發癲癇的風險也較低。
  • ​人類用途​：用於治療憂鬱症、攻擊行為、酒精或古柯鹼戒斷、偏頭痛預防及失眠。

作用機轉

Trazodone exerts its anxiolytic and sedative effects through multiple neurochemical pathways:

  • Serotonin Reuptake Inhibition: Blocks the serotonin transporter (SERT) → increases extracellular serotonin (5-HT) in the synaptic cleft.
  • 5-HT2A Receptor Antagonism: Blocks 5-HT2A receptors → prevents overstimulation by serotonin, contributing to its anxiolytic and antidepressant efficacy. Downregulation of these receptors can augment the efficacy of concurrent SSRIs.
  • Active Metabolite: Hepatic metabolism produces ​m-chlorophenylpiperazine (mCPP)​, which acts as a direct, non-selective serotonin receptor agonist.
  • Alpha-1 Adrenergic Antagonism: Blocks peripheral alpha-1 receptors → can cause mild vasodilation and hypotension.
  • Histamine (H1) Antagonism: Weak blockade of H1 receptors contributes to its sedative properties.

安全性與警告

禁忌症

  • Hypersensitivity to trazodone
  • Concurrent use of MAO inhibitors (e.g., amitraz, selegiline)
  • Glaucoma
  • History of seizures
  • Urinary retention
  • Severe liver disease

不良反應

  • Sedation
  • Lethargy
  • Ataxia
  • Cardiac conduction disturbances
  • Increased anxiety (paradoxical)
  • Aggression (paradoxical)
  • Vomiting/gagging
  • Increased excitement
  • Increased appetite
  • Colitis
  • Serotonin syndrome (rare, usually with concurrent serotonergic drugs)
  • Excitability
  • Dry mouth
  • Third eyelid protrusion (in cats)

注意事項

Cardiac & Organ Impairment: Use with caution in patients with severe cardiac disease or hepatic or renal impairment. Pregnancy: FDA Category C. Animal studies show adverse effects at very high doses (15-50X). Weigh potential risks versus benefits in pregnant or nursing animals. Serotonin Syndrome: Risk increases significantly when combined with other serotonergic drugs (e.g., SSRIs, MAOIs, TCAs).

藥物交互作用

Antihypertensive drugs

May increase reductions in blood pressure and cause hypotension

Aspirin

Increase risk for GI bleeding; monitor

Azole antifungals (e.g., ketoconazole, fluconazole)

May increase trazodone blood levels

CNS depressants

Use with trazodone may cause additive CNS depressant effects

Digoxin

Trazodone may increase digoxin levels

Macrolide antibiotics (e.g., erythromycin, clarithromycin)

May increase trazodone blood levels

Metoclopramide

Increased risk for serotonin syndrome

NSAIDs

Increased risk for GI bleeding; monitor

Phenothiazines

May increase trazodone blood levels; cause additive CNS effects

SSRI antidepressants (e.g., fluoxetine)

Increased risk for serotonin syndrome. Commonly used together, but monitor closely.

Monoamine oxidase inhibitors (MAOIs)Major

Contraindicated; high risk of serotonin syndrome

ChlorphenamineModerate

Metabolized by CYP450 2D6; potential for altered metabolism and toxicity

CimetidineModerate

Metabolized by CYP450 2D6; potential for altered metabolism and toxicity

Serotonergic substancesMajor

Increased risk of serotonin syndrome, though adjunctive therapy is sometimes used cautiously

KetoconazoleMajor

Inhibits the breakdown of trazodone, leading to increased blood levels

CarbamazepineModerate

Increases the breakdown of trazodone, leading to decreased blood levels

ItraconazoleModerate

May inhibit the breakdown of trazodone (theoretical risk based on ketoconazole similarity)

監測

  • Clinical efficacy (behavioral calming)
  • Adverse effects (sedation, GI upset, paradoxical excitement)
  • Signs of serotonin syndrome (vomiting, diarrhea, seizures, hyperthermia, hyperesthesia, mydriasis)
  • Renal function (in patients with pre-existing renal disease)
  • Signs of serotonin syndrome (tremors, agitation, hyperthermia)
  • Efficacy of anxiety reduction

藥物動力學

吸收

In humans, oral bioavailability of immediate-release tablets is about 65%. Presence of food increases absorption (AUC), decreases Cmax, and delays Tmax.

分佈

Approximately 90-95% bound to plasma proteins. Volume of distribution ranges from 0.47-0.84 L/kg (in humans).

代謝

Extensive hepatic metabolism. Oxidative cleavage via CYP3A4 forms the active metabolite m-chlorophenylpiperazine (mCCP), which is further metabolized to inactive compounds via CYP2D6.

排除

Mostly (70-75%) excreted via renal mechanisms (only 0.13% unchanged in urine). About 21% is excreted in feces.

過量

No specific information is available regarding trazodone overdoses in veterinary patients. In humans, the incidence of serious toxicity from trazodone overdose alone is low compared with tricyclic antidepressant overdoses. In the event of a substantial overdose, contact an animal poison control center for guidance. Monitor for profound sedation, ataxia, hypotension, and signs of serotonin syndrome.

可用產品

劑型

  • Oral tablets (immediate-release)
  • Oral tablets (extended-release)
  • 100 mg tablets
  • 150 mg tablets
  • 100 mg capsules
  • 150 mg capsules
  • 10 mg/ml oral liquid

人用標示

  • Trazodone Oral Tablets: 50 mg, 100 mg, 150 mg, & 300 mg; generic; (Rx)
  • Trazodone Extended-Release (24-hour) Oral Tablets: 150 mg & 300 mg; Oleptro® (Labopharm); (Rx)
  • Desyrel
  • Molipaxin

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 between 20-25°C (68-77°F); excursions are permitted to 15-30°C (59-86°F). Keep in an airtight container and protect from light.

飼主須知

  • ​給藥方式​：建議與食物一起餵食，以減少腸胃不適（如嘔吐或作嘔）。
  • ​給藥時機​：針對情境性焦慮（如看獸醫、煙火），請在預期壓力事件發生前 ​1 至 2 小時​給藥。
  • ​觀察​：請密切觀察寵物是否出現過度鎮靜、嗜睡或步態不穩（共濟失調）的情況。
  • ​矛盾反應​：在極少數情況下，寵物可能會表現出異常的興奮、焦慮增加或食慾改變。
  • ​重要警告​：未經獸醫同意，請勿將本藥與其他藥物或保健品（特別是含有雙甲脒 Amitraz 的壁蝨項圈）併用，以免引發罕見但嚴重的​血清素症候群​。
  • ​溝通​：由於曲唑酮在犬隻的廣泛應用仍在研究中，若出現任何不可預見的不良反應，請立即向獸醫報告。

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