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ALIMENTARY TRACT AND METABOLISM › DRUGS FOR CONSTIPATION › DRUGS FOR CONSTIPATION › Peripheral opioid receptor antagonists
naldemedine
A06AH05
Forms & Strengths
- 0.2 mg tablet
- Oral formulation
Adult Dosing
- 0.2 mg once daily
- No dose adjustment for renal impairment
- No dose adjustment for mild or moderate hepatic impairment
Pediatric Dosing
- Not established for patients under 18 years old
Indications
- Opioid-induced constipation (OIC) in adult patients with chronic non-cancer pain
- Treatment of OIC in adult patients with chronic pain
Mechanism of Action
- Peripherally acting mu-receptor antagonist (PAMORA)
- Blocks mu-receptors in the gut to increase gut motility
- Does not cross the blood-brain barrier
Contraindications
- Hypersensitivity to naldemedine
- Known or suspected gastrointestinal obstruction
- Concomitant use of strong CYP3A4 inhibitors
Adverse Reactions
- Gastrointestinal adverse reactions (e.g. abdominal pain, diarrhea, nausea)
- Headache
- Increased risk of gastrointestinal adverse reactions when co-administered with another PAMORA
Drug Interactions
- Avoid concomitant use with strong CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin)
- Concomitant use with other PAMORAs may increase risk of adverse reactions
Curated Content: Needs Vetting Before Put to Clinical Use