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扎魯司特

Zafirlukast

ICI-204219

白三烯受體拮抗劑PO

別名: Accolate · Accoleit · Aeronix · Azimax · Olmoran · Resma · Vanticon · Zafarismal · Zafirst · Zuvair · ICI-204219

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

20 mg (total dose) PO twice dailyPO· q12h
20 mg 每隻動物的固定劑量(不按體重換算)

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

適應症劑量途徑頻次療程地區
Adjunctive treatment of atopic dermatitis20 mg (total dose) PO twice dailyPOq12h🌎 NA
Adjunctive treatment of atopic dermatitis5 mg PO q12h, if the dog weighed less than 11.4 kg (25 lb); 10 mg PO q12h, if 11.4-22.3 kg (25-49 lb); 20 mg PO q12h, if 22.7-34.1 kg (50-75 lb); and 30 mg PO q12h, if greater than 34.1 kg (75 lb).POq12h🌎 NA
  • Adjunctive treatment of atopic dermatitis: Only moderate success
  • Adjunctive treatment of atopic dermatitis: Given on an empty stomach, 1 hour before, or 2 hours after meals.

適應症劑量途徑頻次療程地區
Adjunctive treatment of feline bronchial 'asthma'1-2 mg/kg PO once to twice dailyPOq12-24h🌎 NA
Adjunctive treatment of feline bronchial 'asthma'0.5-1 mg/kg q12-24h.POq12-24h🌎 NA
Adjunctive treatment of feline bronchial 'asthma'5 mg (total dose) per cat PO q12h.POq12h🌎 NA
Adjunctive treatment of mild inflammatory bowel disease0.15-0.2 mg/kg PO once daily.POq24h🌎 NA
  • Adjunctive treatment of mild inflammatory bowel disease: Author has used a combination of zafirlukast (3 months), famotidine (4 weeks), and sucralfate (2 weeks) (along with a low-allergen diet) to successfully treat a case.

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。

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概覽

扎魯司特是一種口服的​白三烯受體拮抗劑​,在獸醫學中屬仿單標示外使用。雖然理論上對於由白三烯介導的發炎疾病(如​貓氣喘​​犬異位性皮膚炎​​炎症性腸病 (IBD)​)具有潛在療效,但目前在獸醫臨床上的療效大多令人失望、有限或尚未被充分研究。

​臨床要點:​ 白三烯是透過脂氧合酶途徑產生的強效發炎介質。雖然阻斷它們在人類氣喘中非常有效,但貓和狗可能依賴其他主要的發炎途徑(如組織胺、白血球介素或前列腺素),這解釋了為什麼扎魯司特在這些物種中的臨床反應存在差異且通常不佳。

作用機制

Zafirlukast selectively and competitively inhibits leukotriene receptors, specifically targeting the LTD4 and LTE4 receptors.

  • Arachidonic acid → 5-lipoxygenase pathway → Leukotrienes (LTC4, LTD4, LTE4)
  • By blocking these receptors, zafirlukast prevents the binding of slow-reacting substance of anaphylaxis (SRS-A).
  • This inhibition reduces smooth muscle contraction (bronchoconstriction), vascular permeability, and inflammatory cell infiltration associated with allergic and asthmatic responses.

安全性與警告

禁忌症

  • Hypersensitivity to zafirlukast
  • Acute bronchospasm or acute asthma attacks

不良反應

  • Vomiting (dogs)
  • Headache (humans)

注意事項

Zafirlukast is not indicated for, and is ineffective for treating bronchospasm associated with acute asthma attacks. Patients with significantly decreased hepatic function may have reduced clearances (and increased plasma levels) of zafirlukast.

藥物相互作用

Aspirin

May significantly increase zafirlukast plasma levels

Erythromycin

May decrease the bioavailability of zafirlukast

Theophylline

May decrease plasma levels of zafirlukast

Warfarin

Zafirlukast may significantly increase the prothrombin time of patients taking warfarin

監測

  • Clinical efficacy

藥物動力學

吸收

Rapidly absorbed after oral administration (human data). Food may impair the absorption of the drug; therefore, give on an empty stomach. Peak plasma levels occur about 3 hours after dosing.

分佈

Highly bound to plasma proteins (>99%).

代謝

Extensively metabolized.

排除

Less than 10% of a dose is excreted in the urine, the rest in the feces.

過量

In dogs, doses of up to 500 mg/kg were tolerated without mortality. Overdose is generally expected to be well tolerated, but supportive care should be provided if significant gastrointestinal signs occur.

可用產品

劑型

  • Tablets (film-coated)

人用標示

  • Zafirlukast Tablets (film-coated): 10 mg & 20 mg; Accolate® (AstraZeneca); (Rx)

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

Zafirlukast tablets should be stored at room temperature and protected from light and moisture. The manufacturer states that the tablets should be dispensed only in the original, unopened container.

飼主須知

  • ​給藥方式:​ 最好在​空腹​時(飯前1小時或飯後2小時)給予,以獲得最佳吸收效果。
  • ​非急救藥物:​ 即使您的動物看起來很健康,也請規律給予此藥物。​切勿​使用此藥物來治療急性氣喘發作或突發的呼吸困難。
  • ​監測:​ 由於在獸醫學中的使用經驗有限,若發現任何不良反應(如嘔吐或嗜睡),請立即向您的獸醫師報告。

VetSheet 藥物參考供持牌獸醫專業人員作臨床決策輔助之用,不能取代專業判斷或廠方最新藥品說明書。