pharmacopeia
GET
/api/v1/drug/tapentadol

Boxed warning

SERIOUS AND LIFE-THREATENING RISKS FROM USE OF TAPENTADOL EXTENDED-RELEASE TABLETS Addiction, Abuse, and Misuse Because the use of tapentadol extended-release tablets expose 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 [see Warnings and Precautions (5.1) ] . Life-Threatening Respiratory Depression Serious, life-threatening, or fatal respiratory depression may occur with use of tapentadol extended-release tablets, especially during initiation or following a dosage increase. To reduce the risk of respiratory depression, proper dosing and titration of tapentadol extended-release tablets are essential. Instruct patients to swallow tapentadol extended-release tablets whole; crushing, chewing, or dissolving tapentadol extended-release tablets can cause rapid release and absorption of a potentially fatal dose of tapentadol [see Warnings and Precautions (5.2) ] . Accidental Ingestion Accidental ingestion of even one dose of tapentadol extended-release tablets, especially by children, can result in a fatal overdose of tapentadol [see Warnings and Precautions (5.2) ] .

2D structure
3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol
SMILES CC[C@@H](C1=CC(=CC=C1)O)[C@@H](C)CN(C)C
InChIKey KWTWDQCKEHXFFR-SMDDNHRTSA-N

Mechanism of action

Sourced from openFDA

Tapentadol is a centrally-acting synthetic analgesic. The exact mechanism of action is unknown.

Monoamine OxidaseOpioid

Indications

Sourced from openFDA
  • Tapentadol extended-release tablets are indicated for the management of: Severe and persistent pain in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate. Severe and persistent neuropathic pain associated with diabetic peripheral neuropathy (DPN) in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate.

Contraindications

Sourced from openFDA
  • Tapentadol extended-release tablets are contraindicated 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 [see Adverse Reactions (6.2) ] Concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days [see Drug Interactions (7) ] Significant respiratory depression ( 4 ) Acute or severe bronchial asthma ( 4 ) Known or suspected paralytic ileus ( 4 ) Hypersensitivity to tapentadol or to any other ingredients of the product ( 4 ) Concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days.contraindicated

Dosage & administration

Sourced from openFDA

Tapentadol extended-release tablets should be prescribed only by healthcare professionals who are knowledgeable about the use of extended-release/long-acting opioids and how to mitigate the associated risks. ( 2.1 ) Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals. Reserve titration to higher doses of tapentadol extended-release 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 ( 2.5 ). Initiate the dosing regimen for each patient individually, taking into account the patient's underlying cause and severity of pain, prior analgesic treatment, and response, and risk factors for addiction, abuse, and misuse. ( 5.1 ) Respiratory depression can occur at any time during opioid therapy, especially when initiating and following dosage increases with tapentadol extended-release tablets. Consider this risk when selecting an initial dose and when making dose adjustments. ( 2.1 , 5.2 ) Discuss availability of naloxone with the patient and caregiver and assess each patient's need for access to naloxone, both when initiating and renewing treatment with tapentadol extended-release tablets. Consider prescribing naloxone based on the patient's risk factors for overdose. ( 2.2 , 5.1 , 5.2 , 5.3 ) Instruct patients to swallow tapentadol extended-release tablets intact, and not to cut, break, chew, crush, or dissolve the tablets (risk of potentially fatal overdose).

Warnings & precautions

Sourced from openFDA

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. ( 5.6 ) Serotonin Syndrome with Concomitant Use of Serotonergic Drugs: Potentially life-threatening condition could result from concomitant serotonergic drug administration. Discontinue tapentadol extended-release tablets if serotonin syndrome is suspected. ( 5.7 ) Life-Threatening Respiratory Depression in Patients with Chronic Pulmonary Disease or in Elderly, Cachectic, or Debilitated Patients: Regularly evaluate, particularly during initiation and titration. ( 5.8 ) Adrenal Insufficiency : If diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid. ( 5.9 ) Severe Hypotension : Regularly evaluate during dosage initiation and titration. Avoid use of tapentadol extended-release tablets in patients with circulatory shock. ( 5.10 ) Risks of Use in Patients with Increased Intracranial Pressure, Brain Tumors, Head Injury, or Impaired Consciousness : Monitor for sedation and respiratory depression. Avoid use of tapentadol extended-release tablets in patients with impaired consciousness or coma. ( 5.11 ) 5.1 Addiction, Abuse, and Misuse Tapentadol extended-release tablets contain tapentadol, a Schedule II controlled substance.

Adverse reactions

Sourced from openFDA

The following serious adverse reactions are described, or described in greater detail, in other sections: Addiction, Abuse, and Misuse [see Warnings and Precautions (5.1) ] Life-Threatening Respiratory Depression [see Warnings and Precautions (5.2) ] Interaction with Benzodiazepine or Other CNS Depressants [see Warnings and Precautions (5.3) ] Neonatal Opioid Withdrawal Syndrome [see Warnings and Precautions (5.4) ] Opioid-Induced Hyperalgesia and Allodynia [see Warnings and Precautions (5.6) ] Serotonin Syndrome [see Warnings and Precautions (5.7) ] Adrenal Insufficiency [see Warnings and Precautions (5.9) ] Severe Hypotension [see Warnings and Precautions (5.10) ] Gastrointestinal Adverse Reactions [see Warnings and Precautions (5.12) ] Seizures [see Warnings and Precautions (5.13) ] Withdrawal [see Warnings and Precautions (5.14) ] The most common (≥10%) adverse reactions were nausea, constipation, dizziness, headache, and somnolence. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Hikma Pharmaceuticals USA Inc. at 1-800-962-8364 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Use in specific populations

Sourced from openFDA

Pregnancy : Based on animal data, may cause fetal harm. ( 8.1 ) Lactation: Not recommended. ( 8.2 ) Severe Hepatic or Renal Impairment: Use not recommended. ( 8.6 , 8.7 ) 8.1 Pregnancy Risk Summary Use of opioid analgesics for an extended period of time during pregnancy may cause neonatal opioid withdrawal syndrome [see Warnings and Precautions (5.4) ]. Available data with tapentadol extended-release tablets are insufficient to inform a drug-associated risk for major birth defects and miscarriage or adverse maternal outcomes. In animal reproduction studies, embryofetal mortality and structural malformations were observed with subcutaneous administration of tapentadol during organogenesis to rabbits and delays in skeletal maturation were observed in rats at exposures equivalent to and less than the maximum recommended human dose (MRHD), respectively. When administered to pregnant rats during organogenesis and through lactation, increased pup mortality was noted following oral tapentadol exposures to doses equivalent to the MRHD [see Data ] . Based on animal data, advise pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse reaction. In the U.S.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption The mean absolute bioavailability after single-dose administration (fasting) of tapentadol extended-release tablets is approximately 32% due to extensive first-pass metabolism. Maximum serum concentrations of tapentadol are observed between 3 and 6 hours after administration of tapentadol extended-release tablets.

Overdosage

Sourced from openFDA

Clinical Presentation Acute overdosage with tapentadol can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases pulmonary edema, bradycardia, hypotension, hypoglycemia, partial or complete airway obstruction, atypical snoring and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations [see Clinical Pharmacology (12.2) ] . Treatment of Overdose 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 measures. Opioid antagonists, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose. For clinically significant respiratory or circulatory depression secondary to tapentadol overdose, administer an opioid antagonist.

Approval history

Sourced from openFDA
  • Nov 20, 2008NDANDA022304Collegium Pharm Inc
  • Aug 25, 2011NDANDA200533Collegium Pharm Inc
  • Jan 27, 2026ANDAANDA214378Humanwell

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
33,133 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Death11,64335%
  2. 2Toxicity To Various Agents9,73429%
  3. 3Overdose5,88618%
  4. 4Drug Abuse1,5494.7%
  5. 5Drug Dependence1,0653.2%
  6. 6Drug Ineffective1,0113.1%
  7. 7Drug Withdrawal Syndrome Neonatal9442.8%
  8. 8Pain7502.3%
  9. 9Nausea7222.2%
  10. 10Accidental Overdose7052.1%
  11. 11Fatigue4411.3%
  12. 12Headache4101.2%
  13. 13Dizziness4091.2%
  14. 14Intentional Product Misuse3981.2%
  15. 15Somnolence3881.2%

Literature

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Recent PubMed references pinned to Tapentadol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 82 ClinicalTrials.gov registrations naming Tapentadol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Tapentadol work?
Tapentadol is a centrally-acting synthetic analgesic. The exact mechanism of action is unknown.
What is Tapentadol used for?
According to FDA labeling, Tapentadol carries indications including: Tapentadol extended-release tablets are indicated for the management of: Severe and persistent pain in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate. Severe and persistent neuropathic pain associated with diabetic peripheral neuropathy (DPN) in adults that requires an extended treatment period with a daily opioid analgesic and for which alternative treatment options are inadequate.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Tapentadol?
Tapentadol is classified as Other opioids, Opioid Agonist, Monoamine Oxidase Inhibitors, Opioid Agonists, Analgesia, Decreased GI Motility, Decreased Organized Electrical Activity, Respiratory/Pulmonary Activity Alteration.
What are the brand names for Tapentadol?
Tapentadol is marketed under brand names including Nucynta.
What are the contraindications for Tapentadol?
Tapentadol labeling lists contraindications including: Tapentadol extended-release tablets are contraindicated 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 [see Adverse Reactions (6.2) ] Concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days [see Drug Interactions (7) ] Significant respiratory depression ( 4 ) Acute or severe bronchial asthma ( 4 ) Known or suspected paralytic ileus ( 4 ) Hypersensitivity to tapentadol or to any other ingredients of the product ( 4 ) Concurrent use of monoamine oxidase inhibitors (MAOIs) or use of MAOIs within the last 14 days.. Always consult the full prescribing information and a clinician.
Note. Data for tapentadol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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