Naldemedine

What is Naldemedine?

• Naldemedine (Symproic) is an opioid antagonist used for the treatment of opioid-induced constipation in adults with chronic non-cancer pain.

Naldemedine

Naldemedine structure

What are the uses of this medicine?

• Naldemedine (Symproic) is a prescription medicine used to treat constipation that is caused by prescription pain medicines called opioids in adults with long-lasting (chronic) pain that is not caused by active cancer.

How does this medicine work?

• Naldemedine (nal dem' e deen) is a semisynthetic opiate receptor antagonist which is similar structurally to naltrexone and blocks mu receptors in the enteric nervous system of the gastrointestinal tract resulting in an inhibition of opioid induced slowing of peristalsis.
• Naldemedine has a large polar side chain that does not block its engagement with opioid receptors, but does prevent it from crossing the blood brain barrier.
• As a consequence, naldemedine reverses the peripheral but not the central nervous system effects of opiates, such as pain relief and euphoria.
• In large preregistration trials, naldemedine was found to increase spontaneous bowel movement frequency and reduce constipation related side effects of opiates used for analgesia in patients with chronic, non-cancer pain.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have a bowel blockage (intestinal obstruction) or have a history of bowel blockage.
• are allergic to Symproic or any of the ingredients.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• amiodarone (Cordarone)
• aprepitant (Emend)
• atazanavir (Reyataz, in Evotaz)
• captopril (Capoten, in Capozide)
• carbamazepine (Tegretol)
• clarithromycin (Biaxin, in PrevPac)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• diltiazem (Cardizem, Dilacor, Tiazac)
• efavirenz (in Atripla, Sustiva)
• erythromycin (E.E.S., E-Mycin, Erythrocin)
• fluconazole (Diflucan)
• itraconazole (Onmel, Sporonax)
• ketoconazole (Nizoral)
• other opioid antagonists such as methylnaltrexone (Relistor), naloxegol (Movantik), naloxone (Evzio, in Bunavail, in Suboxone, in Zubsolv), or naltrexone (Revia, in Contrave, in Embeda, Vivitrol)
• phenytoin (Dilantin, Phenytek)
• quinidine
• rifampin (Rifadin, in Rifamate, Rifater, Rimactane)
• ritonavir (Norvir, in Kaletra, in Technivie, in Viekira)
• saquinavir (Invirase)
• verapamil (Calan, Covera, Isoptin, Verelan)
• St. John's wort

Is this medicine FDA approved?

• Naldemedine was approved for this use in the United States in 2017 and is currently available as tablets of 0.2 mg under the brand name Symproic.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of Symproic is 0.2 mg orally once daily with or without food.

Administration:

• Naldemedine comes as a tablet to take by mouth.
• Take Symproic exactly as your healthcare provider tells you to take it.
• Take your prescribed dose of Symproic 1 time each day.
• Symproic can be taken with or without food.
• Symproic has been shown to be effective in people who have taken opioid pain medicines for at least 4 weeks.
• Tell your healthcare provider if you stop taking your opioid pain medicine. If you stop taking your opioid pain medicine, you should also stop taking Symproic.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 0.2 mg naldemedine

This medicine is available in fallowing brand namesː

• Symproic

What side effects can this medication cause?

The most common side effects of this medicine include:

• stomach (abdomen) pain, diarrhea, nausea and vomiting (gastroenteritis)

Symproic may cause serious side effects, including:

• Tear in your stomach or intestinal wall (perforation)
• Opioid withdrawal
• hypersensitivity reactions

What special precautions should I follow?

• Cases of gastrointestinal perforation have been reported with use of another peripherally acting opioid antagonist in patients with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the gastrointestinal tract. Consider the overall risk benefit in patients with known or suspected lesions of the GI tract. Monitor for severe, persistent, or worsening abdominal pain; discontinue if development of symptoms.
• Clusters of symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, increased lacrimation, hot flush/flushing, pyrexia, sneezing, feeling cold, abdominal pain, diarrhea, nausea, and vomiting have occurred in patients treated with Symproic. Consider the overall risk benefit in patients with disruptions to the blood-brain barrier. Monitor symptoms of opioid withdrawal.
• Advise patients to discontinue Symproic if treatment with the opioid pain medication is also discontinued.
• Advise females of reproductive potential, who become pregnant or are planning to become pregnant, that the use of Symproic during pregnancy may precipitate opioid withdrawal in a fetus due to the undeveloped blood-brain barrier.
• Advise women that breastfeeding is not recommended during treatment with Symproic and for 3 days after the final dose.
• Naldemedine has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• abdominal pain, diarrhea, and nausea

• Dose-dependent increases in gastrointestinal-related adverse reactions, including abdominal pain, diarrhea, nausea, and vomiting, were observed.
• Also, chills, hyperhidrosis, and dizziness were reported.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• No antidote for naldemedine is known.
• Hemodialysis is not an effective means to remove naldemedine from the blood

Can this medicine be used in pregnancy?

• There are no available data with naldemedine in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.
• Taking Symproic during pregnancy may cause opioid withdrawal symptoms in your unborn baby.
• Tell your healthcare provider right away if you become pregnant during treatment with Symproic.
• Symproic should be used during pregnancy only if the potential benefit justifies the potential risk.

Can this medicine be used in children?

• The safety and effectiveness of Symproic have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active Ingredient: naldemedine tosylate
• Inactive ingredients: D-mannitol, croscarmellose sodium, magnesium stearate, hypromellose, talc, and yellow ferric oxide.

Who manufactures and distributes this medicine?

• Manufactured for: BioDelivery Sciences International, Inc. Raleigh, NC

What should I know about storage and disposal of this medication?

• Store Symproic at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Symproic in the bottle that it comes in.

• Dailymed label info on Naldemedine
• FDA Naldemedine