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HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to use NUCYNTA® safely and effectively. See full prescribing information for NUCYNTA®.
NUCYNTA® (tapentadol) immediate-release oral tablets C-II
Initial U.S. Approval: 2008
NUCYNTA® (tapentadol) Tablets are immediate-release film-coated tablets for oral administration. The chemical name is 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol monohydrochloride.
The molecular weight of tapentadol HCl is 257.80, and the molecular formula is C14H23NO•HCl. The n-octanol:water partition coefficient log P value is 2.87. The pKa values are 9.34 and 10.45. In addition to the active ingredient tapentadol HCl, tablets also contain the following 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.
Mechanism of Action
Tapentadol is a centrally-acting synthetic analgesic. Although its exact mechanism is unknown, analgesic efficacy is thought to be due to mu-opioid agonist activity and the inhibition of norepinephrine reuptake.
Tapentadol is a centrally-acting synthetic analgesic. It is 18 times less potent than morphine in binding to the human mu-opioid receptor and is 2-3 times less potent in producing analgesia in animal models. Tapentadol has been shown to inhibit norepinephrine reuptake in the brains of rats resulting in increased norepinephrine concentrations. In preclinical models, the analgesic activity due to the mu-opioid receptor agonist activity of tapentadol can be antagonized by selective mu-opioid antagonists (e.g., naloxone), whereas the norepinephrine reuptake inhibition is sensitive to norepinephrine modulators. Tapentadol exerts its analgesic effects without a pharmacologically active metabolite.
Effects on the cardiovascular system: There was no effect of therapeutic and supratherapeutic doses of tapentadol on the QT interval. In a randomized, double-blind, placebo- and positive-controlled crossover study, healthy subjects were administered five consecutive doses of NUCYNTA® 100 mg every 6 hours, NUCYNTA® 150 mg every 6 hours, placebo and a single oral dose of moxifloxacin. Similarly, NUCYNTA® had no relevant effect on other ECG parameters (heart rate, PR interval, QRS duration, T-wave or U-wave morphology).
INDICATIONS AND USAGE
NUCYNTA® is an opioid analgesic indicated for the relief of moderate to severe acute pain in patients 18 years of age or older.
--Impaired pulmonary function (significant respiratory depression, acute or severe bronchial asthma or hypercapnia in unmonitored settings or the absence of resuscitative equipment)
--Concomitant use with monoamine oxidase inhibitors (MAOI) or use within 14 days
WARNINGS AND PRECAUTIONS
--Respiratory depression: Increased risk in elderly, debilitated patients, those suffering from conditions accompanied by hypoxia, hypercapnia, or upper airway obstruction.
--CNS effects: Additive CNS depressive effects when used in conjunction with alcohol, other opioids, or illicit drugs.
--Elevation of intracranial pressure: May be markedly exaggerated in the presence of head injury, other intracranial lesions.
--Abuse potential may occur. Monitor patients closely for signs of abuse and addiction.
--Impaired mental/physical abilities: Caution must be used with potentially hazardous activities.
--Seizures: Use with caution in patients with a history of seizures.
--Serotonin Syndrome: Potentially life-threatening condition could result from concomitant serotonergic administration.
--Use NUCYNTA® with caution in patients currently using specified centrally-acting drugs or alcohol.
--Do not use NUCYNTA® in patients currently using or within 14 days of using a monoamine oxidase inhibitor (MAOI).
USE IN SPECIFIC POPULATIONS
--Labor and delivery: should not use during and immediately prior to labor and delivery. Monitor neonates, whose mothers have been taking NUCYNTA®, for respiratory depression.
--Nursing mothers: should not breast-feed.
--Pediatric use: safety and effectiveness not established in patients less than 18 years of age.
--Renal or hepatic impairment: not recommended in patients with severe renal or hepatic impairment. Use with caution in patients with moderate hepatic impairment.
--Elderly: care should be taken when selecting an initial dose.
The most common adverse events were nausea, dizziness, vomiting and somnolence.
To report SUSPECTED ADVERSE REACTIONS, contact Janssen Pharmaceuticals, Inc. at 1-800-526-7736 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
DOSAGE AND ADMINISTRATION
Immediate release tablets:
As with many centrally-acting analgesic medications, the dosing regimen should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to monitor the patient.
The dose is 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.
NUCYNTA® may be given with or without food.
---As with many centrally acting analgesic medications, the dosing regimen of NUCYNTA® ER should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to follow-up and provide oversight of treatment.
---The recommended NUCYNTA® ER total daily dose is 100 mg to 250 mg twice daily approximately every 12 hours. Patients not currently taking opioid analgesics should begin NUCYNTA® ER therapy with 50 mg twice a day.
---Patients receiving NUCYNTA® (immediate-release formulation) may be converted to NUCYNTA® ER by administering the same total daily dose. Administer half the total daily dose of NUCYNTA® ER approximately every 12 hours. Do not exceed the maximum daily dose of NUCYNTA® ER of 500 mg.
No dosage adjustment is recommended in patients with mild or moderate renal impairment.
NUCYNTA® has not been studied in patients with severe renal impairment. The use in this population is not recommended.
No dosage adjustment is recommended in patients with mild hepatic impairment.
NUCYNTA® should be used with caution in patients with moderate hepatic impairment. Treatment in these patients should be initiated at 50 mg with the interval between doses no less than every 8 hours (maximum of three doses in 24 hours). Further treatment should reflect maintenance of analgesia with acceptable tolerability, to be achieved by either shortening or lengthening the dosing interval [see package insert for Clinical Pharmacology (12.3)].
NUCYNTA® has not been studied in patients with severe hepatic impairment and use in this population is not recommended.
In general, recommended dosing for elderly patients with normal renal and hepatic function is the same as for younger adult patients with normal renal and hepatic function. Because elderly patients are more likely to have decreased renal and hepatic function, consideration should be given to starting elderly patients with the lower range of recommended doses.
DOSAGE FORMS AND STRENGTHS
Immediate release tablets:
Tablets: 50 mg, 75 mg, 100 mg
Extended release tablets:
Tablets: 50 mg, 100 mg, 150 mg, 200 mg, 250 mg
Package Insert data:
PRINCIPAL DISPLAY PANEL - 100 mg Tablet Bottle Label