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RESPIRATORY SYSTEM › DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES › OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES › Leukotriene receptor antagonists
ibudilast
R03DC04
Forms & Strengths
- Oral capsule: 10 mg
- Ophthalmic solution: 0.03%
Adult Dosing
- Asthma: 10 mg orally twice daily
- Post-cataract inflammation (ophthalmic): 1 drop instilled in affected eye(s) 4 times daily
Pediatric Dosing
- Safety and efficacy in pediatric patients not established
Indications
- Bronchial asthma
- Cerebrovascular disorders
- Allergic conjunctivitis and post-operative ocular inflammation
Mechanism of Action
- Non-selective phosphodiesterase (PDE) inhibitor, with high potency against PDE3, PDE4, and PDE10
- Suppresses pro-inflammatory cytokines (TNF-alpha, IL-1beta, IL-6)
- Upregulates anti-inflammatory cytokines (IL-10)
- Acts as a glial attenuation factor and macrophage migration inhibitory factor (MIF) inhibitor
Contraindications
- Hypersensitivity to ibudilast or any component of the formulation
- Severe liver impairment
Adverse Reactions
- Gastrointestinal: nausea, vomiting, abdominal discomfort, loss of appetite
- Central nervous system: headache, dizziness, insomnia
- Cardiovascular: palpitations, flushing
- Hepatic: transient elevation of liver transaminases
Drug Interactions
- CYP3A4 inducers may decrease plasma concentrations of ibudilast
- CYP3A4 inhibitors may increase systemic exposure to ibudilast
- Additive central nervous system depression when co-administered with sedatives or alcohol
Curated Content: Needs Vetting Before Put to Clinical Use