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nalfurafine
V03AX02
Forms & Strengths
- Oral disintegrating tablets: 2.5 mcg
- Oral disintegrating tablets: 5 mcg
Adult Dosing
- Uremic pruritus: 2.5 mcg orally once daily after dialysis
- May be increased to 5 mcg orally once daily if efficacy is insufficient and tolerated
- Chronic liver disease-associated pruritus: 2.5 mcg orally once daily, may increase to 5 mcg
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of pruritus in hemodialysis patients inadequately responding to conventional treatments
- Treatment of pruritus associated with chronic liver disease
Mechanism of Action
- Selective kappa-opioid receptor agonist
- Acts primarily in the peripheral nervous system and central nervous system to modulate itch signals
- Suppresses opioid mu-receptor-mediated pruritus pathways
Contraindications
- Hypersensitivity to nalfurafine or any component of the formulation
- Severe hepatic impairment (Child-Pugh Class C)
Adverse Reactions
- Insomnia
- Somnolence
- Constipation
- Dizziness
- Nausea
- Palpitations
- Elevated liver enzymes
Drug Interactions
- Strong CYP3A4 inhibitors may increase nalfurafine exposure
- Strong CYP3A4 inducers may decrease nalfurafine efficacy
- Central nervous system depressants may potentiate somnolence and sedation
- Opioid antagonists may reverse the therapeutic effects of nalfurafine
Curated Content: Needs Vetting Before Put to Clinical Use