Tapentadol hydrochloride ER

What is Tapentadol hydrochloride ER?

• Tapentadol hydrochloride ER (NUCYNTA ER) is an opioid agonist.

Tapentadol

Tapentadol 3D

Tapentadol molecule

What are the uses of this medicine?

NUCYNTA ER is:

• A strong prescription pain medicine that contains an opioid (narcotic) that is used to manage pain severe enough to require daily around-the-clock, long-term treatment with an opioid, when other pain treatments such as non-opioid pain medicines or immediate-release opioid medicines do not treat your pain well enough or you cannot tolerate them.
• Also used to manage pain from damaged nerves (neuropathic pain) that happens with diabetes and is severe enough to require daily around-the-clock, long-term treatment with an opioid, when other pain treatments such as non-opioid pain medicines do not treat your pain well enough or you cannot tolerate them.

Limitations of Use:

• A long-acting (extended-release) opioid pain medicine that can put you at risk for overdose and death. Even if you take your dose correctly as prescribed you are at risk for opioid addiction, abuse, and misuse that can lead to death.
• Not used to treat pain that is not around-the-clock pain.

How does this medicine work?

• Tapentadol is a centrally-acting synthetic analgesic.
• The exact mechanism of action is unknown.
• Although the clinical relevance is unclear, preclinical studies have shown that tapentadol is a mu-opioid receptor (MOR) agonist and a norepinephrine reuptake inhibitor (NRI).

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Significant respiratory depression
• Acute or severe bronchial asthma or hypercarbia in an unmonitored setting or in the absence of resuscitative equipment
• Known or suspected gastrointestinal obstruction, including paralytic ileus
• Hypersensitivity (e.g. anaphylaxis, angioedema) to tapentadol or to any other ingredients of the product.
• Concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days

What drug interactions can this medicine cause?

• Concomitant use of alcohol with NUCYNTA ER can result in an increase of tapentadol plasma levels and potentially fatal overdose of tapentadol.
• Due to additive pharmacologic effect, the concomitant use of benzodiazepines or other CNS depressants, including alcohol, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death.
• The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system has resulted in serotonin syndrome
• Do not use NUCYNTA ER in patients taking MAOIs or within 14 days of stopping such treatment.
• Avoid concomitant use with butorphanol, nalbuphine, pentazocine, buprenorphine.
• Due to the risk of respiratory depression with concomitant use of skeletal muscle relaxants and opioids, consider prescribing naloxone for the emergency treatment of opioid overdose.
• Opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone.
• The concomitant use of anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus.

Is this medicine FDA approved?

• Initial U.S. Approval: 2008

How should this medicine be used?

Recommended dosage:

• Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals.
• Individualize dosing based on the severity of pain, patient response, prior analgesic experience, and risk factors for addiction, abuse, and misuse.
• Do not exceed a total daily dose of NUCYNTA ER of 500 mg.
• For opioid-naïve and opioid non-tolerant patients, initiate treatment with 50 mg tablet orally twice daily (approximately every 12 hours).
• Titrate patients with dose increases of 50 mg no more than twice daily every three days.
• Moderate Hepatic Impairment: Initiate treatment with 50 mg NUCYNTA ER no more than every 24 hours. Do not exceed 100 mg per day. Monitor closely for respiratory and central nervous system depression.
• Do not abruptly discontinue NUCYNTA ER in a physically-dependent patient because rapid discontinuation of opioid analgesics has resulted in serious withdrawal symptoms, uncontrolled pain, and suicide.

Administration:

• Do not change your dose. Take NUCYNTA ER exactly as prescribed by your healthcare provider. Use the lowest effective dose for the shortest time needed.
• Take your prescribed dose every 12 hours, at the same time every day. Do not take more than your prescribed dose in 24 hours. If you miss a dose, take your next dose at your usual time.
• Swallow NUCYNTA ER whole. Do not cut, break, chew, crush, dissolve, snort, or inject NUCYNTA ER because this may cause you to overdose and die.
• Call your healthcare provider if the dose you are taking does not control your pain.
• Do not stop taking NUCYNTA ER without talking to your healthcare provider.
• Dispose of expired, unwanted, or unused NUCYNTA ER by promptly flushing down the toilet, if a drug take-back option is not readily available. Visit www.fda.gov/drugdisposal for additional information on disposal of unused medicines.

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

This medicine is available in fallowing doasage form:

• As Extended-release tablets: 50 mg, 100 mg, 150 mg, 200 mg, 250 mg

This medicine is available in fallowing brand namesː

• NUCYNTA ER ,NUCYNTA

What side effects can this medication cause?

The most common side effects of this medicine include:

• constipation
• nausea
• sleepiness
• vomiting
• tiredness
• headache
• dizziness
• abdominal pain

What special precautions should I follow?

• Do not drive or operate heavy machinery until you know how NUCYNTA ER affects you. NUCYNTA ER can make you sleepy, dizzy, or lightheaded.
• Do noy drink alcohol, or use prescription or over-the-counter medicines containing alcohol. Using products containing alcohol during treatment with NUCYNTA ER may cause you to overdose and die.
• As an opioid, NUCYNTA ER exposes users to the risks of addiction, abuse, and misuse. Because extended-release products such as NUCYNTA ER deliver the opioid over an extended period of time, there is a greater risk for overdose and death due to the larger amount of tapentadol present.
• Serious, life-threatening, or fatal respiratory depression has been reported with the use of opioids, even when used as recommended.
• Prolonged use of NUCYNTA ER during pregnancy can result in withdrawal in the neonate. Advise pregnant women using opioids for a prolonged period of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.
• Patients must not consume alcoholic beverages or prescription or non-prescription products containing alcohol while on NUCYNTA ER therapy. The use of NUCYNTA ER in patients with acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment is contraindicated.
• Cases of serotonin syndrome, a potentially life-threatening condition, have been reported during concomitant use of tapentadol with serotonergic drugs. Discontinue NUCYNTA ER if serotonin syndrome is suspected.
• Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use. If diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid.
• NUCYNTA ER may cause severe hypotension including orthostatic hypotension and syncope in ambulatory patients. Monitor during dosage initiation and titration. Avoid use of NUCYNTA ER in patients with circulatory shock.
• NUCYNTA ER is contraindicated in patients with known or suspected gastrointestinal obstruction, including paralytic ileus.
• Do not abruptly discontinue NUCYNTA ER in a patient physically dependent on opioids. When discontinuing NUCYNTA ER in a physically dependent patient, gradually taper the dosage.
• In patients who may be susceptible to the intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), NUCYNTA ER may reduce respiratory drive, and the resultant CO2 retention can further increase intracranial pressure. Monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy with NUCYNTA ER.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• respiratory depression
• somnolence progressing to stupor or coma
• skeletal muscle flaccidity
• cold and clammy skin
• constricted pupils
• pulmonary edema
• bradycardia
• hypotension
• death
• hypoxia

Management of overdosage:

• In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed.
• Employ other supportive measures (including oxygen, vasopressors) in the management of circulatory shock and pulmonary edema as indicated.
• Cardiac arrest or arrhythmias will require advanced life support techniques.
• Opioid antagonists, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose.
• For clinically significant respiratory or circulatory depression secondary to opioid overdose, administer an opioid antagonist.

Can this medicine be used in pregnancy?

• Prolonged use of opioid analgesics during pregnancy may cause neonatal opioid withdrawal syndrome.
• Available data with NUCYNTA ER are insufficient to inform a drug-associated risk for major birth defects and miscarriage.

Can this medicine be used in children?

• The safety and efficacy of NUCYNTA ER in pediatric patients less than 18 years of age have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• TAPENTADOL HYDROCHLORIDE

Inactive ingredients:

• POLYETHYLENE GLYCOL, UNSPECIFIED
• HYPROMELLOSE, UNSPECIFIED
• .ALPHA.-TOCOPHEROL
• POLYVINYL ALCOHOL, UNSPECIFIED
• TITANIUM DIOXIDE
• TALC
• SHELLAC
• PROPYLENE GLYCOL
• FERROSOFERRIC OXIDE

Who manufactures and distributes this medicine?

Distributed by:

• Collegium Pharmaceutical, Inc., 100 Technology Center Drive Suite 300, Stoughton

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

• Store at 20°C - 25°C (68°F - 77°F); excursions permitted to 15° C - 30°C (59° F - 86°F).
• Protect from moisture.
• Store NUCYNTA ER securely and dispose of properly .

• Dailymed label info on Tapentadol hydrochloride ER
• FDA Tapentadol hydrochloride ER

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