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.
Mechanism: 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.
Dosing by species
- 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.
Doses are a clinical reference for licensed veterinary professionals. Always confirm against the current label and the individual patient.
Routes of administration
Contraindications
- Hypersensitivity to zafirlukast
- Acute bronchospasm or acute asthma attacks
Adverse effects
- Vomiting (dogs)
- Headache (humans)
Drug interactions
- 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
Monitoring
- Clinical efficacy
Overdose
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.
VetSheet drug reference is intended for licensed veterinary professionals as a clinical decision-support aid, not a substitute for professional judgement or the manufacturer’s current label.