Tapentadol hydrochloride

What is Tapentadol hydrochloride?

• Tapentadol hydrochloride (Nucynta) is an opioid analgesic used for the relief of moderate to severe acute pain.

Tapentadol

Tapentadol molecule ball

What are the uses of this medicine?

• Tapentadol hydrochloride (Nucynta) is a prescription medicine that is used in adults 18 years of age or older to treat moderate to severe pain that is expected to last a short time.
• Nucynta is for short-term use only because the risks for withdrawal symptoms, abuse and addiction are higher when Nucynta is used longer.

How does this medicine work?

• Tapentadol - an orally available, synthetic benzenoid that acts as an agonist for the mu opioid receptor (mor) and inhibits the reuptake of noradrenaline, with potential anti nociceptive activity.
• Upon oral administration, tapentadol binds to the mor which enhances mor mediated signaling, interferes with the sensation of pain and results in an analgesic effect.
• Tapentadol also inhibits the reuptake of noradrenaline, which increases the levels of noradrenaline (na), activates the inhibitory alpha 2 receptors and results in an analgesic effect.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have severe lung problems
• have a gastrointestinal problem called paralytic ileus in which the intestines are not working normally.
• take a monoamine oxidase inhibitor (MAOI) medicine or have taken an MAOI within the last 14 days.

What drug interactions can this medicine cause?

• Using Nucynta with other medicines can cause serious side effects. The doses of some other medicines may need to be changed.
• Your doctor can tell you what medicines can be safely taken with Nucynta.

Especially tell your doctor if you take:

• Monoamine Oxidase Inhibitors (MAOIs).
• any medicine that makes you sleepy. Nucynta can make you sleepy and affect your breathing. Taking these medicines together can be dangerous.

Is this medicine FDA approved?

• Tapentadol was approved by the US FDA in November 2008.

How should this medicine be used?

Recommended dosage:

• As with many centrally-acting analgesic medications, the dosing regimen of Nucynta should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to monitor the patient.
• Initiate the dose by 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending upon pain intensity.
• On the first day of dosing, the second dose may be administered as soon as one hour after the first dose, if adequate pain relief is not attained with the first dose.
• Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability.
• Daily doses greater than 700 mg on the first day of therapy and 600 mg on subsequent days have not been studied and are not recommended.

Administration:

• Take Nucynta exactly as prescribed by your doctor.
• Do not change the dose of Nucynta unless your doctor tells you to. Your doctor may change your dose after seeing how the medicine affects you. Do not use Nucynta more often than prescribed.
• Follow your doctor's instructions about how to slowly stop taking Nucynta to help lessen withdrawal symptoms.
• NUCYNTA® can be taken with or without food.

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

This medicine is available in fallowing doasage form:

• As Tablets: 50 mg, 75 mg, 100 mg

This medicine is available in fallowing brand namesː

• NUCYNTA

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea
• dizziness
• vomiting
• sleepiness
• itching
• Constipation

NUCYNTA® can cause serious side effects including:

• Life-threatening breathing problems
• Physical Dependence
• Serotonin syndrome
• Seizures
• Low blood pressure

What special precautions should I follow?

• Do not drive, operate machinery, or participate in any other possibly dangerous activities until you know how you react to this medicine. Nucynta can make you sleepy.
• You should not drink alcohol while using Nucynta. Alcohol increases your chance of having dangerous side effects.
• Respiratory depression is the primary risk of mu-opioid agonists. Increased risk in elderly, debilitated patients, those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction.
• Patients receiving other mu-opioid agonist analgesics, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Nucynta may exhibit additive CNS depression. Additive CNS depressive effects when used in conjunction with alcohol, other opioids, or illicit drugs.
• Opioid analgesics can raise cerebrospinal fluid pressure as a result of respiratory depression with carbon dioxide retention. May be markedly exaggerated in the presence of head injury, other intracranial lesions.
• NUCYNTA® can be abused in a manner similar to other opioid agonists, legal or illicit. Monitor patients closely for signs of abuse and addiction.
• NUCYNTA® has not been systematically evaluated in patients with a seizure disorder, and such patients were excluded from clinical studies. Use with caution in patients with a history of seizures.
• The development of a potentially life-threatening serotonin syndrome may occur with use of Serotonin and Norepinephrine Reuptake Inhibitor (SNRI) products, including Nucynta, particularly with concomitant use of serotonergic drugs such as Selective Serotonin Reuptake Inhibitors (SSRIs), SNRIs, tricyclic antidepressants (TCAs), MAOIs and triptans, and with drugs that impair metabolism of serotonin (including MAOIs).
• Withdrawal symptoms may occur if Nucynta is discontinued abruptly. Withdrawal symptoms may be reduced by tapering Nucynta.
• NUCYNTA® should be used with caution in patients with moderate hepatic impairment.
• Like other drugs with mu-opioid agonist activity, Nucynta may cause spasm of the sphincter of Oddi and should be used with caution in patients with biliary tract disease, including acute pancreatitis.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• miosis, vomiting, cardiovascular collapse, consciousness disorders up to coma, convulsions and respiratory depression up to respiratory arrest.

Management of overdosage:

• Management of overdose should be focused on treating symptoms of mu-opioid agonism. Primary attention should be given to re-establishment of a patent airway and institution of assisted or controlled ventilation when overdose of Nucynta is suspected. Supportive measures (including oxygen and vasopressors) should be employed in the management of circulatory shock and pulmonary edema accompanying overdose as indicated. Cardiac arrest or arrhythmias may require cardiac massage or defibrillation.
• Pure opioid antagonists, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose.
• If the response to opioid antagonists is suboptimal or only brief in nature, an additional antagonist should be administered as directed by the manufacturer of the product.
• Gastrointestinal decontamination may be considered in order to eliminate unabsorbed drug.
• Gastrointestinal decontamination with activated charcoal or by gastric lavage is only recommended within 2 hours after intake.

Can this medicine be used in pregnancy?

• There are no adequate and well controlled studies ofNucynta in pregnant women.
• NUCYNTA® should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The safety and effectiveness ofNucynta in pediatric patients less than 18 years of age have not been established.
• NUCYNTA® is not recommended in this population.

What are the active and inactive ingredients in this medicine?

Active Ingredient:

• tapentadol

Inactive ingredients:

• microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, povidone, magnesium stearate, and Opadry® II, a proprietary film-coating mixture containing polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, and aluminum lake coloring.

Who manufactures and distributes this medicine?

Manufactured by: Janssen Ortho, LLC Gurabo, PR

Manufactured for:

• PriCara®, Division of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
• Raritan, NJ

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

• Store Nucynta at 59ºF to 86ºF (15ºC to 30ºC).
• Keep Nucynta tablets dry.
• Dispose of Nucynta tablets you no longer need.

• Dailymed label info on Tapentadol hydrochloride
• FDA Tapentadol hydrochloride

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