Naldemedine

Naldemedine is used for opioid-induced constipation (OIC) in adults with chronic noncancer pain.

Naldemedine is available under the following different brand names: Symproic.

Dosages of Naldemedine:

Dosage Forms and Strengths

Tablet

• 0.2mg

Dosage Considerations – Should be Given as Follows:

Opioid-induced Constipation

• Indicated for opioid-induced constipation (OIC) in adults with chronic noncancer pain
• 0.2 mg orally once daily

Dosage Modifications

Hepatic impairment

• Mild or moderate (Child-Pugh A or B): No dose adjustment required

Safety and efficacy not established in pediatric patients

Common side effects of naldemedine include:

• Abdominal pain
• Diarrhea
• Nausea
• Vomiting
• Gastroenteritis
• Opioid withdrawal
• Other side effects of naldemedine include:
• Bronchospasm
• Rash

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

• Naldemedine has no listed severe interactions with other drugs.
• Naldemedine has serious interactions with at least 32 different drugs.
• Naldemedine has moderate interactions with at least 105 different drugs.
• Naldemedine has no listed mild interactions with other drugs.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist. Check with your physician if you have health questions or concerns.

Warnings

• This medication contains naldemedine. Do not take Symproic if you are allergic to naldemedine or any ingredients contained in this drug.
• Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

• Known or suspected gastrointestinal (GI) obstruction and patients at increased risk of recurrent obstruction, owing to the potential for GI perforation
• History of hypersensitivity to naldemedine; bronchospasm and rash reported

Effects of Drug Abuse

• No information is available

Short-Term Effects

• See "What Are Side Effects Associated with Using Naldemedine?”

Long-Term Effects

• See "What Are Side Effects Associated with Using Naldemedine?”

Cautions

• Gastrointestinal perforation
• Gastrointestinal (GI) perforation reported with the use of another PAMORA in patients with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the GI tract (e.g., peptic ulcer disease, Ogilvie syndrome, diverticular disease, infiltrative GI tract malignancies, peritoneal metastases)
• Consider risk with use in patients with these conditions or other conditions that might result in impaired integrity of the GI tract wall (e.g., Crohn’s disease)
• Monitor for severe, persistent, or worsening abdominal pain and discontinue naldemedine in patients who develop this symptom

Opioid withdrawal

• Clusters of symptoms consistent with opioid withdrawal include excessive sweating, chills, increased tearing, hot flush/flushing, fever, sneezing, feeling cold, abdominal pain, diarrhea, nausea, and vomiting
• Patients with blood-brain barrier disruption may be at increased risk for opioid withdrawal or reduced analgesia
• Take into account the overall risk-benefit profile when prescribing naldemedine in such patients
• Monitor for symptoms of opioid withdrawal

Drug interaction overview

• The substrate of CYP3A4 (major), P-gp, and UGT1A3 (minor)
• Opioid antagonists: Avoid use with another opioid antagonist
• Strong CYP3A4 inducers: Avoid coadministration, owing to the potential for decreased efficacy of naldemedine
• Moderate or strong CYP3A4 inhibitors: Monitor for potential naldemedine adverse effects, owing to increased plasma concentrations
• P-gp inhibitors: Monitor for potential naldemedine adverse effects, owing to increased plasma concentrations

Pregnancy and Lactation

• Naldemedine crosses the placenta and may precipitate opioid withdrawal in a fetus or newborn, owing to the immature fetal blood-brain barrier. There are no available data with naldemedine in pregnant women to inform a drug-associated risk of major birth defects and miscarriage. Consult your doctor.
• It is unknown if naldemedine is distributed in human breast milk. Because of the potential for serious adverse reactions, including opioid withdrawal in breastfed infants, a decision should be made to discontinue breastfeeding or discontinue naldemedine, taking into account the importance of the drug to the mother. If naldemedine is discontinued to minimize drug exposure to a breastfed infant, women may be advised that breastfeeding may be resumed 3 days after the final dose.