Naloxegol

What is Naloxegol?

• Naloxegol (Movantik) is an opioid antagonist used for the treatment of opioid-induced constipation (OIC).

What are the uses of this medicine?

• This 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?

• Naloxegol (nal ox' ee gol) is a pegylated, semisynthetic opiate receptor antagonist which is similar structurally to naltrexone, but is peripherally restricted and thus has few if any effects on the central nervous system.
• Naloxegol is a polyethylene glycol (PEG) derivative of alpha-naloxol, an opiate antagonist.
• The addition of the large PEG molecule to naloxol does not block its engagement with opioid receptors, but does prevent the drug from crossing the blood brain barrier.
• As a consequence, the opioid antagonist reverses the peripheral but not the central nervous system effects of opiates, such as pain relief and euphoria.
• In large, preregistration trials, naloxegol was found to increase spontaneous bowel movement frequency and reduce constipation related side effects of opiates used for analgesia in patients with chronic pain.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known or suspected gastrointestinal obstruction and patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal perforation.
• Patients concomitantly using strong CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole).
• known serious or severe hypersensitivity reaction to Movantik or any of its excipients.

What drug interactions can this medicine cause?

Avoid coadministration with:

• Moderate CYP3A4 inhibitors (e.g., diltiazem, erythromycin, verapamil)
• Strong CYP3A4 inducers (e.g., rifampin)
• Other opioid antagonists

Is this medicine FDA approved?

• This medicine is approved in the year 2014.

How should this medicine be used?

Recommended Dosage:

• The recommended Movantik dosage is 25 mg once daily in the morning.
• If patients are not able to tolerate Movantik, reduce the dosage to 12.5 mg once daily.

Dosage in Adult Patients with Renal Impairment

• The starting dosage for patients with creatinine clearance (CLcr) <60 mL/min (i.e., patients with moderate, severe, or end-stage renal impairment) is 12.5 mg once daily.
• If this dosage is well tolerated but OIC symptoms continue, the dosage may be increased to 25 mg once daily.

Administration

• Take Movantik exactly as your healthcare provider tells you.
• Take your prescribed dose of Movantik 1 time each day, on an empty stomach, at least 1 hour before your first meal of the day or 2 hours after the meal.
• If you cannot swallow Movantik tablets whole, Movantik can be mixed with water and taken by mouth or given through a nasogastric (NG) tube. To take Movantik by mouth:
• crush the tablet to a powder
• place your dose of Movantik in a glass that contains 4 ounces (120 mL) of water and stir
• swallow Movantik and water mixture right away
• add 4 more ounces (120 mL) of water to the glass and drink right away, to make sure that you take your full dose of Movantik.
• If you cannot swallow Movantik tablets and have a nasogastric (NG) tube, Movantik may be given as follows:
• draw up 1 ounce (30 mL) of water into a 60 mL syringe and flush the NG tube
• crush the tablet to a powder
• place your dose of Movantik in a container and mix with approximately 2 ounces (60 mL) of water
• draw up the Movantik and water into the 60 mL syringe and give the mixture through the NG tube
• add approximately 2 ounces (60 mL) of water to the same container you used to prepare your dose of Movantik
• draw up the water using the same 60 mL syringe and use all the water to flush the NG tube and any remaining medicine from the NG tube into the stomach
• Stop taking other laxatives before you start treatment with Movantik. Your healthcare provider may prescribe other laxatives if Movantik does not work after 3 days of treatment.
• Movantik 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 Movantik.
• If you take too much Movantik, call your healthcare provider or go to the nearest emergency room right away.

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

This medicine is available in fallowing doasage form:

• As Tablets: 12.5 mg and 25 mg

This medicine is available in fallowing brand namesː

• Movantik

What side effects can this medication cause?

The most common side effects of this medicine include:

• stomach (abdomen) pain
• diarrhea
• nausea
• gas
• vomiting
• headache

Movantik may cause serious side effects, including:

• Opioid withdrawal
• Severe stomach pain or diarrhea, or both severe stomach pain and diarrhea
• Tear in your stomach or intestinal wall (perforation)

What special precautions should I follow?

• Clusters of symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, irritability, and yawning have occurred in patients treated with Movantik. Consider the overall risk benefit in patients with disruptions to the blood-brain barrier. Monitor for symptoms of opioid withdrawal.
• Reports of severe abdominal pain and/or diarrhea have been reported, some of which resulted in hospitalization. Monitor for the development of symptoms after initiating treatment with Movantik and discontinue if severe symptoms develop. Consider restarting Movantik at 12.5 mg once daily if appropriate.
• Cases of gastrointestinal (GI) perforation have been reported with use of peripherally acting opioid antagonists, including Movantik. 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.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• abdominal pain
• diarrhea
• nausea

Management of overdosage:

• No antidote is known for naloxegol. Dialysis was noted to be ineffective as a means of elimination in a clinical study in patients with renal failure.
• If a patient on opioid therapy receives an overdose of naloxegol, the patient should be monitored closely for potential evidence of opioid withdrawal symptoms such as chills, rhinorrhea, diaphoresis, or reversal of central analgesic effect.
• Base treatment on the degree of opioid withdrawal symptoms, including changes in blood pressure and heart rate, and on the need for analgesia.

Can this medicine be used in pregnancy?

• Limited available data with Movantik use in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes.

Can this medicine be used in children?

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

What are the active and inactive ingredients in this medicine?

• Active ingredient: naloxegol oxalate
• Inactive ingredients: The tablet core contains mannitol, cellulose microcrystalline, croscarmellose sodium, magnesium stearate, and propyl gallate. The tablet coat contains hypromellose, titanium dioxide, polyethylene glycol, iron oxide red, and iron oxide black.

Who manufactures and distributes this medicine?

• Distributed by: AstraZeneca Pharmaceuticals LP, Wilmington

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

• Store Movantik at room temperature between 68°F to 77°F (20°C to 25°C).
• Safely throw away medicine that is out of date or that you no longer need.
• Keep Movantik and all medicines out of the reach of children.

• Dailymed label info on Naloxegol
• FDA Naloxegol

Naloxegol Resources
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Full and partial opiod agonists:

• Alfentanil
• Butorphanol
• Codeine
• Diphenoxylate
• Fentanyl
• Heroin
• Hydrocodone
• Hydromorphone
• Levorphanol
• Loperamide
• Meperidine
• Methadone
• Morphine
• Opium
• Oxycodone
• Oxymorphone
• Pentazocine
• Remifentanil
• Sufentanil
• Tramadol

Opiate antagonists:

• Nalmefene
• Naloxegol
• Naloxone
• Naltrexone