Zafirlukast
Zafirlukast is an oral **leukotriene-receptor antagonist** used off-label in veterinary medicine. While theoretically promising for conditions driven by leukotriene-mediated inflammation—such as **feline asthma**, **canine atopic dermatitis**, and **inflammatory bowel disease (IBD)**—clinical efficacy in veterinary patients has been largely disappointing, limited, or not fully studied. > **Clinical Pearl:** Leukotrienes are potent inflammatory mediators produced via the lipoxygenase pathway. While blocking them is highly effective in human asthma, cats and dogs may rely on different primary inflammatory pathways (such as histamine, interleukins, or prostaglandins), which likely explains the variable and often poor clinical response to zafirlukast in these species.
กลไกการออกฤทธิ์: 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.
ขนาดยาตามชนิดสัตว์
- Adjunctive treatment of feline bronchial 'asthma' · 1-2 mg/kg PO once to twice daily · PO · q12-24h
- Adjunctive treatment of feline bronchial 'asthma' · 0.5-1 mg/kg q12-24h. · PO · q12-24h
- Adjunctive treatment of feline bronchial 'asthma' · 5 mg (total dose) per cat PO q12h. · PO · q12h
- Adjunctive treatment of mild inflammatory bowel disease · 0.15-0.2 mg/kg PO once daily. · PO · q24h · 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.
- Adjunctive treatment of atopic dermatitis · 20 mg (total dose) PO twice daily · PO · q12h · Only moderate success
- Adjunctive treatment of atopic dermatitis · 5 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). · PO · q12h · Given on an empty stomach, 1 hour before, or 2 hours after meals.
ขนาดยาเป็นข้อมูลอ้างอิงทางคลินิกสำหรับสัตวแพทย์ผู้มีใบอนุญาต โปรดตรวจสอบกับฉลากล่าสุดและผู้ป่วยแต่ละรายเสมอ
วิธีการให้ยา
ข้อห้ามใช้
- Hypersensitivity to zafirlukast
- Acute bronchospasm or acute asthma attacks
อาการไม่พึงประสงค์
- Vomiting (dogs)
- Headache (humans)
อันตรกิริยาระหว่างยา
- 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
การติดตาม
- Clinical efficacy
การได้รับยาเกินขนาด
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.
ข้อมูลอ้างอิงยาของ VetSheet มีไว้สำหรับสัตวแพทย์ผู้มีใบอนุญาตเพื่อช่วยในการตัดสินใจทางคลินิก ไม่ใช่สิ่งทดแทนการวินิจฉัยของผู้เชี่ยวชาญหรือฉลากล่าสุดของผู้ผลิต