NUCYRETA ER- tapentadol hydrochloride tablet, film coated,
extended release
INDICATIONS AND USAGE
NUCYRETA ® ER (TAPENTADOL) IS AN OPIOID AGONIST INDICATED FOR
THE MANAGEMENT OF: PAIN SEVERE ENOUGH TO REQUIRE DAILY,
AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH
ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
(DPN) IN ADULTS SEVERE ENOUGH TO REQUIRE DAILY,
AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH
ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
NUCYRETA ® ER (TAPENTADOL) IS AN OPIOID AGONIST INDICATED FOR
THE MANAGEMENT OF:
• PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK,
LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT
OPTIONS ARE INADEQUATE
• NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL
NEUROPATHY (DPN) IN ADULTS SEVERE ENOUGH TO REQUIRE DAILY,
AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH
ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE
NUCYRETA® ER is the first and only FDA-APPROVED LONG-ACTING
OPIOID DESIGNED TO CONTROL BOTH NOCICEPTIVE PAIN AND THE
NEUROPATHIC PAIN ASSOCIATED WITH DIABETIC PERIPHERAL NEUROPATHY
(DPN).
Limitations of Use
• Because of the risks of addiction, abuse, and misuse with
opioids, even at recommended doses, and because of the greater
risks of overdose and death with extended-release opioid
formulations, reserve NUCYRETA® ER for use in patients for whom
alternative treatment options (e.g., non-opioid analgesics or
immediate-release opioids) are ineffective, not tolerated, or
would be otherwise inadequate to provide sufficient management
of pain
• NUCYRETA® ER is not indicated as an as-needed (prn) analgesic
DOSAGE AND ADMINISTRATION
INDIVIDUALIZE DOSING BASED ON PATIENT'S PRIOR ANALGESIC
TREATMENT EXPERIENCE AND RISK FACTORS FOR ADDICTION, ABUSE, AND
MISUSE; TITRATE AS NEEDED TO PROVIDE ADEQUATE ANALGESIA AND
MINIMIZE ADVERSE REACTIONS.
FOR USE AS THE FIRST OPIOID AND IN OPIOID NON-TOLERANT PATIENTS,
INITIATE WITH 50 MG TABLET ORALLY TWICE DAILY (APPROXIMATELY
EVERY 12 HOURS).
TO CONVERT TO NUCYRETA ER FROM ANOTHER OPIOID, USE AVAILABLE
CONVERSION FACTORS TO OBTAIN ESTIMATED DOSE.
TITRATE PATIENTS WITH DOSE INCREASES OF 50 MG NO MORE THAN TWICE
DAILY EVERY THREE DAYS.
NUCYRETA ER- tapentadol hydrochloride tablet, film coated,
extended release
HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to
use NUCYRETA ® ER safely and effectively.
Maximum daily dose is 500 mg per day.
Use a gradual downward titration when NUCYRETA ER is
discontinued in a physically dependent patient.
Reduce the dose of NUCYRETA ER in patients with moderate hepatic
impairment.
NUCYRETA ER use in patients with severe renal impairment is not
recommended. Conservative initial dosing of NUCYRETA ER in
elderly patients is recommended due to possible decreased renal
and hepatic function.
Instruct patients to swallow NUCYRETA ER tablets whole.
NUCYRETA® ER IMPORTANT SAFETY INFORMATION
WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING
RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION;
NEONATAL OPIOID WITHDRAWAL SYNDROME; and INTERACTION WITH
ALCOHOL
Addiction, Abuse, and Misuse
NUCYRETA® ER exposes patients and other users to the risks of
opioid addiction, abuse, and misuse, which can lead to overdose
and death. Assess each patient's risk prior to prescribing
NUCYRETA® ER, and monitor all patients regularly for the
development of these behaviors or conditions. Life-threatening
Respiratory Depression: Serious, life-threatening, or fatal
respiratory depression may occur with use of NUCYRETA® ER.
Monitor for respiratory depression, especially during initiation
of NUCYRETA® ER or following a dose increase. Instruct patients
to swallow NUCYRETA® ER tablets whole; crushing, chewing, or
dissolving NUCYRETA® ER tablets can cause rapid release and
absorption of a potentially fatal dose of tapentadol.
Accidental Ingestion
Accidental ingestion of even one dose of NUCYRETA® ER,
especially by children, can result in a fatal overdose of
tapentadol.
Neonatal Opioid Withdrawal Syndrome
Prolonged use of NUCYRETA® ER during pregnancy can result in
neonatal opioid withdrawal syndrome, which may be
life-threatening if not recognized and treated, and requires
management according to protocols developed by neonatology
experts. If opioid use is required for a prolonged period in a
pregnant woman, advise the patient of the risk of neonatal
opioid withdrawal syndrome and ensure that appropriate treatment
will be available.
Interaction With Alcohol
Instruct patients not to consume alcoholic beverages or use
prescription or nonprescription products that contain alcohol
while taking NUCYRETA® ER. The co-ingestion of alcohol with
NUCYRETA® ER may result in increased plasma tapentadol levels
and a potentially fatal overdose of tapentadol.
CONTRAINDICATIONS: Significant respiratory depression; acute or
severe bronchial asthma or hypercarbia in an unmonitored setting
or in the absence of resuscitative equipment; known or suspected
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
within the last 14 days.
WARNINGS AND PRECAUTIONS: Addiction, Abuse, and Misuse: NUCYRETA®
ER contains tapentadol, an opioid agonist and a Schedule II
controlled substance that can be abused in a manner similar to
other opioid agonists, legal or illicit. There is a greater risk
for overdose and death due to the larger amount of tapentadol
present in NUCYRETA® ER. Assess risk for opioid abuse or
addiction prior to prescribing NUCYRETA® ER. Addiction can occur
in patients appropriately prescribed NUCYRETA® ER at recommended
doses; in those who obtain the drug illicitly; and if the drug
is misused or abused. Therefore, routinely monitor for signs of
misuse, abuse, and addiction. Patients at increased risk (e.g.,
patients with a personal or family history of substance abuse or
mental illness) may be prescribed NUCYRETA® ER, but use in such
patients necessitates intensive counseling about the risks and
proper use along with intensive monitoring for signs of
addiction, abuse, and misuse.
Life-threatening Respiratory Depression: Can occur at any time
during the use of NUCYRETA® ER even when used as recommended.
Respiratory depression from opioid use, if not immediately
recognized and treated, may lead to respiratory arrest and
death. To reduce the risk of respiratory depression, proper
dosing and titration are essential. Overestimating the dose when
converting patients from another opioid product can result in
fatal overdose with the first dose. Management of respiratory
depression may include close observation, supportive measures,
and use of opioid antagonists, depending on the patient's
clinical status.
Neonatal Opioid Withdrawal Syndrome: Prolonged use of NUCYRETA®
ER during pregnancy can result in withdrawal signs in the
neonate, which may be life-threatening and require management
according to protocols developed by neonatology experts.
Neonatal opioid withdrawal syndrome presents as poor feeding,
irritability, hyperactivity and abnormal sleep pattern,
high-pitched cry, tremor, rigidity, seizures, vomiting,
diarrhea, and failure to gain weight.
Interactions With Central Nervous System Depressants:
Hypotension, profound sedation, coma, respiratory depression,
and death may result if NUCYRETA® ER is used concomitantly
with alcohol or other central nervous system (CNS) depressants
(e.g., sedatives, anxiolytics, hypnotics, tranquilizers, general
anesthetics, neuroleptics, other opioids). When considering the
use of NUCYRETA® ER in a patient taking a CNS depressant, assess
the duration of use of the CNS depressant and the patient's
response, including the degree of tolerance that has developed
to CNS depression. If the decision to begin NUCYRETA® ER is
made, start with NUCYRETA® ER 50 mg every 12 hours, monitor
patients for signs of sedation and respiratory depression, and
consider using a lower dose of the concomitant CNS depressant.
Use in Elderly, Cachectic, or Debilitated Patients:
Life-threatening respiratory depression is more likely to occur
in elderly, cachectic, or debilitated patients as they may have
altered pharmacokinetics or altered clearance. Because elderly
patients are more likely to have decreased renal and hepatic
function, consideration should be given to starting elderly
patients in the lower range of recommended doses. Closely
monitor these patients, particularly when initiating and
titrating NUCYRETA® ER and when given concomitantly with other
drugs that depress respiration.
Use in Patients With Chronic Pulmonary Disease: Patients with
significant chronic obstructive pulmonary disease or cor
pulmonale and patients having a substantially decreased
respiratory reserve, hypoxia, hypercarbia, or pre-existing
respiratory depression, should be monitored for respiratory
depression particularly when initiating therapy and titrating
with NUCYRETA® ER. Consider the use of alternative nonopioid
analgesics in these patients.
Hypotensive Effect: May cause severe hypotension. There is an
increased risk in patients whose ability to maintain blood
pressure has already been compromised by a reduced blood volume
or concurrent administration of certain CNS depressant drugs
(e.g., phenothiazines or general anesthetics). Monitor for signs
of hypotension during dose initiation or titration. Avoid use in
patients with circulatory shock; may cause vasodilation that can
further reduce cardiac output and blood pressure.
Use in Patients With Head Injury or Increased Intracranial
Pressure: Monitor patients who may be susceptible to the
intracranial effects of CO2 retention (e.g., those with evidence
of increased intracranial pressure or brain tumors) for signs of
sedation and respiratory depression, particularly when
initiating therapy. NUCYRETA® ER may reduce respiratory drive,
and the resultant CO2 retention can further increase
intracranial pressure. Opioids may also obscure the clinical
course in a patient with a head injury.
Seizures: May aggravate convulsions in patients with convulsive
disorders and may induce or aggravate seizures. Monitor patients
with a history of seizure disorders for worsened seizure control
during therapy.
Serotonin Syndrome: Cases of life-threatening serotonin
syndrome have been reported with the concurrent use of NUCYRETA®
ER and serotonergic drugs. Serotonergic drugs comprise selective
serotonin reuptake inhibitors (SSRIs), serotonin and
norepinephrine reuptake inhibitors (SNRIs), tricyclic
antidepressants (TCAs), triptans, drugs that affect the
serotonergic neurotransmitter system, and drugs that impair
metabolism of serotonin (including MAOIs). This may occur within
the recommended dose. Serotonin syndrome may include
mental-status changes (e.g., agitation, hallucinations, coma),
autonomic instability (e.g., tachycardia, labile blood pressure,
hyperthermia), neuromuscular aberrations (e.g., hyperreflexia,
incoordination), and/or gastrointestinal symptoms (e.g., nausea,
vomiting, diarrhea) and can be fatal. If concomitant treatment
with SSRIs, SNRIs, TCAs, or triptans is clinically warranted,
careful observation of the patient is advised, particularly when
initiating or titrating the dose.
Use in Patients With Gastrointestinal (GI) Conditions:
Contraindicated in patients with Gl obstruction including
paralytic ileus; may cause spasm of the sphincter of Oddi.
Monitor patients with biliary tract disease, including acute
pancreatitis, for worsening symptoms.
Avoidance of Withdrawal: Withdrawal symptoms (e.g., anxiety,
sweating, insomnia, restlessness, pain, nausea, tremors,
diarrhea, upper respiratory symptoms, piloerection) may occur:
• After abrupt discontinuation or a significant dose reduction
of NUCYRETA® ER in physically dependent patients. When
discontinuing NUCYRETA® ER, gradually taper the dose.
• If mixed agonist/antagonist (e.g., butorphanol, nalbuphine,
pentazocine) and partial agonist (e.g., buprenorphine)
analgesics are used in patients who have received or are
receiving NUCYRETA® ER. Avoid use with mixed
agonists/antagonists and partial agonists.
• If opioid antagonists (e.g., naloxone, nalmefene) are
administered in physically dependent patients. Administration of
the antagonist should be begun with care and by titration with
smaller than usual doses of the antagonist.
Driving and Operating Heavy Machinery: May impair the mental or
physical abilities needed to perform potentially hazardous
activities such as driving a car or operating machinery. Warn
patients not to drive or operate dangerous machinery unless they
are tolerant to the effects of NUCYRETA® ER and know how they
will react to the medication.
Hepatic Impairment: Avoid use in patients with severe hepatic
impairment (Child-Pugh Score 10 to 15). In patients with
moderate hepatic impairment (Child-Pugh Score 7-9), initiate
treatment with NUCYRETA® ER 50 mg no more than once every 24
hours, with a maximum dose of 100 mg per day. Monitor for
respiratory and CNS depression when initiating and titrating
NUCYRETA® ER.
Renal Impairment: Use in patients with severe renal impairment (CLCR
<30 mL/min) is not recommended due to accumulation of a
metabolite formed by glucuronidation of tapentadol. The clinical
relevance of the elevated metabolite is not known. DRUG INTERACTIONS
Alcohol: See BOXED WARNING.
Muscle Relaxants: Monitor patients receiving muscle relaxants
and NUCYRETA® ER for signs of respiratory depression that may be
greater than otherwise expected. Tapentadol may enhance the
neuromuscular blocking action of skeletal muscle relaxants and
produce an increased degree of respiratory depression.
Anticholinergics: Use with anticholinergic products may increase
the risk of urinary retention and/or severe constipation, which
may lead to paralytic ileus.
USE IN SPECIFIC POPULATIONS
Pregnancy/Nursing Mothers: Pregnancy Category C. NUCYRETA® ER
should be used during pregnancy only if the potential benefit
justifies the potential risk to the fetus. Neonates born to
mothers physically dependent on opioids will also be physically
dependent and may exhibit respiratory difficulties and
withdrawal symptoms. Observe newborns for symptoms of neonatal
opioid withdrawal syndrome. Withdrawal symptoms can occur in
breast-feeding infants when maternal administration of NUCYRETA®
ER is stopped.
Labor and Delivery: Opioids cross the placenta and may produce
respiratory depression in neonates. NUCYRETA® ER is not for use
in women during and immediately prior to labor, when
shorter-acting analgesics or other analgesic techniques are more
appropriate.
Use in Elderly, Renal Impairment, and Hepatic Impairment: See
WARNINGS AND PRECAUTIONS.
DRUG ABUSE AND DEPENDENCE: See BOXED WARNING
OVERDOSAGE: Institute supportive measures to manage respiratory
depression, circulatory shock, and pulmonary edema as required.
The opioid antagonists, naloxone or nalmefene, are specific
antidotes to respiratory depression.
ADVERSE REACTIONS: In clinical studies, the most common (≥10%)
adverse reactions were nausea, constipation, vomiting,
dizziness, somnolence, and headache.
Select Postmarketing Adverse Reactions: Anaphylaxis, angioedema,
and anaphylactic shock have been reported very rarely with
ingredients contained in NUCYRETA® ER. Advise patients how to
recognize such reactions and when to seek medical attention.
Panic attack has also been reported.
ADVERSE REACTIONS :The most common (≥10%) adverse reactions
were nausea, constipation, dizziness, headache, and somnolence.
Inform patients that NUCYRETA ER may cause orthostatic
hypotension and syncope. Instruct patients how to recognize
symptoms of low blood pressure and how to reduce the risk of
serious consequences should hypotension occur (e.g., sit or lie
down, carefully rise from a sitting or lying position).
Driving or Operating Heavy Machinery
Inform patients that NUCYRETA ER may impair the ability to
perform potentially hazardous activities such as driving a car
or operating heavy machinery. Advise patients not to perform
such tasks until they know how they will react to the
medication.
Constipation
Advise patients of the potential for severe constipation,
including management instructions and when to seek medical
attention.
Anaphylaxis : Inform patients that anaphylaxis has been reported
with ingredients contained in NUCYRETA ER.
Advise patients how to recognize such a reaction and when to
seek medical attention.
NUCYRETA ER (tapentadol) Extended Release Tablets
50 mg, 100 mg, 150 mg, 200 mg, 250 mg CII
Each tablet contains tapentadol.
Excipients .Q.S.
Advise female patients that NUCYRETA ER can cause fetal harm and
to inform the prescriber if they are pregnant or plan to become
pregnant.
SWALLOW TABLETS WHOLE. DO NOT CHEW, CRUSH OR DISSOLVE. ADVISE
PATIENTS TO FLUSH THE UNUSED TABLETS DOWN THE TOILET WHEN
NUCYRETA ER IS NO LONGER NEEDED.
Store at controlled room temperature, 25°C (77°F) with
excursions
allowed from 15 to 30°C (59 to 86°F).
DOSAGE FORMS AND STRENGTHS
NUCYRETA ER (tapentadol) Extended Release Tablets
10 Tablets / 30 Tablets & 500 Tablets Packing.
Note : This product information is intended only
for residents of the India. Taj Pharmaceuticals Limited,
medicines help to treat and prevent a range of conditions—from the
most common to the most challenging—for people around the world.
Information for Health Care Professionals
*** Please consult local Prescribing
Information for any product before use. This website is an
international information resource for healthcare professionals
with an interest in disease management. This website is not
intended to replace the advice of a qualified healthcare
professional. Above brand is a trademark of the Taj group of
companies (Taj Pharmaceuticals Limited).
First and only
FDA-APPROVED LONG-ACTING OPIOID DESIGNED TO CONTROL
COMMON TYPES OF CHRONIC PAIN
Below are types of chronic pain, including diabetic peripheral
neuropathy and conditions that originate or are common to the low
back. Patients with chronic pain conditions may have both a
neuropathic and a nociceptive component.
DIABETIC PERIPHERAL NEUROPATHY (DPN):
A complication of diabetes in which high blood glucose may damage
the tiny blood vessels carrying oxygen and nutrients to the small
nerves in the hands and feet.4
INTERVERTEBRAL DISC DISEASE:
A condition typically caused by aging in which discs in the
vertebral column deteriorate or herniate, causing them to lose
fluid, elasticity, and shock-absorbing capabilities.5
RADICULOPATHY:
Nerve damage typically caused by inflammation or impingement of a
nerve root, causing weakness and/or pain radiating the length of the
nerve.6
SCIATICA:
A form of radicular nerve pain, often caused by pressure on the
nerve root at L5‑S1, causing pain that radiates down the back of the
leg.6
ARTHRITIS:
There are several forms of arthritis of the spine (known altogether
as spondyloarthropathies). These include:
OSTEOARTHRITIS:
Occurs when the cartilage that protects the bones of the spinal area
breaks down, causing bones to rub together, which leads to spurs
that press against nerves.7
ANKYLOSING SPONDYLITIS:
An inflammatory disease in which the ligaments and bones of the
spine fuse together, resulting in a stiff, fused, painful spine.8
RHEUMATOID ARTHRITIS:
Occurs when the immune system attacks soft tissue surrounding the
joints of the spine, which can place pressure on the spinal cord or
spinal nerve roots.7
SPONDYLOLISTHESIS:
A condition in which a lower vertebra slides out of place on top of
the vertebra below it, commonly between L4 and L5, causing low back
pain.8,9
Quality
