Tapentadol

Tapentadol tablets are indicated for the management of acute pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate in adults and pediatric patients aged 6 years and older with a body weight of at least 40kg. Limitations of Use Because of the risks of addiction, abuse, and misuse with opioids, which can occur at any dose or duration, reserve tapentadol tablets for use in patients for whom alternative treatment options [e.g., non-opioid analgesics or opioid combination products]: Have not been tolerated or are not expected to be tolerated, Have not provided adequate analgesia or are not expected to provide adequate analgesia Tapentadol tablets should not be used for an extended period of time unless the pain remains severe enough to require an opioid analgesic and for which alternative treatment options continue to be inadequate.

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). Analgesia in animal models is derived from both of these properties.

Tapentadol tablets should be prescribed only by healthcare professionals who are knowledgeable about the use of opioids and how to mitigate the associated risks. Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals. Reserve titration to higher doses of tapentadol tablets for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks. Many acute pain conditions (e.g., the pain that occurs with a number of surgical procedures or acute musculoskeletal injuries) require no more than a few days of an opioid analgesic. Clinical guidelines on opioid prescribing for some acute pain conditions are available.

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

Boxed warning (serious and life-threatening risks from use of): tapentadol TABLETS Addiction, Abuse, and Misuse Because the use of tapentadol tablets 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 and reassess all patients regularly for the development of these behaviors and conditions. Opioid-Induced Hyperalgesia and Allodynia: Opioid-Induced Hyperalgesia (OIH) occurs when an opioid analgesic paradoxically causes an increase in pain, or an increase in sensitivity to pain. If OIH is suspected, carefully consider appropriately decreasing the dose of the current opioid analgesic, or opioid rotation. Serotonin Syndrome with Concomitant Use of Serotonergic Drugs: Potentially life-threatening condition could result from concomitant serotonergic drug administration.

The following adverse reactions are discussed, or described in greater detail, in other sections: Addiction, Abuse, and Misuse Life-Threatening Respiratory Depression Interactions with Benzodiazepine or Other CNS Depressants Neonatal Opioid Withdrawal Syndrome Opioid-Induced Hyperalgesia and Allodynia Adrenal Insufficiency Severe Hypotension Gastrointestinal Adverse Reactions Seizures Withdrawal The most common adverse reactions were Adults (incidence ≥10%) were nausea, dizziness, vomiting and somnolence. Pediatric patients 6 years and older (incidence ≥5%): vomiting, constipation, nausea, pruritus, and pyrexia

Table 2 includes clinically significant drug interactions with tapentadol tablets. Table 2. Clinically Significant Drug Interactions with tapentadol Tablets Benzodiazepines and other Central Nervous System (CNS) Depressants Clinical Impact: Due to additive pharmacologic effect, the concomitant use of benzodiazepines or other CNS depressants including alcohol, increases the risk of respiratory depression, profound sedation, coma, and death [Warnings and Precautions ]. Intervention: Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Inform patients and caregivers of this potential interaction and educate them on the signs and symptoms of respiratory depression (including sedation).

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