tapentadol (Rx)

Brand and Other Names:Nucynta, Nucynta ER
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet, immediate release: Schedule II

  • 50mg
  • 75mg
  • 100mg

tablet, extended release: Schedule II

  • 50mg
  • 100mg
  • 150mg
  • 200mg
  • 250mg
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Acute Moderate-to-Severe Pain

Immediate-release tablet or oral solution: 50-100 mg PO q4-6hr PRN; not to exceed 700 mg on day 1 and 600 mg/day thereafter

Chronic (extended-release tablet)

  • 50-250 mg PO q12hr PRN; not to exceed 500 mg/day
  • Opioid-naive patients: 50 mg PO q12hr; titrated to optimal dosage as needed; not to exceed 500 mg/day

Chronic Severe Pain

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

50-250 mg PO q12hr PRN; not to exceed 500 mg/day

Opioid-naive patients: 50 mg PO q12hr; titrated to optimal dosage as needed; not to exceed 500 mg/day

Opioid-naive definition

  • Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression
  • Patients who are opioid tolerant are those receiving, for 1 week or longer, at least 60 mg/day PO morphine, 25 mcg/hr transdermal fentanyl, 30 mg/day PO oxycodone, 8 mg/day PO hydromorphone, 25 mg/day PO oxymorphone, or an equianalgesic dose of another opioid

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 for patients whom alternative treatment options (eg, nonopioid analgesics or immediate-release opioids) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain
  • Not indicated as a PRN analgesic

Diabetic Peripheral Neuropathy

Treatment of pain associated with diabetic peripheral neuropathy when continuous, around-the-clock opioid analgesic is needed for extended period

Extended release: 50 mg PO q12hr initially; titrated to balance individual tolerance with efficacy; typical range, 100-250 mg PO q12hr

Dosing Modifications

Renal impairment

  • CrCl ≥30 mL/min : Dosage adjustment not required
  • CrCl <30 mL/min: Not recommended

Hepatic impairment

  • Mild: Dosage adjustment not required
  • Moderate: 50 mg immediate release q8hr initially; dosing frequency not to exceed 3 times daily; alternatively, 50 mg PO q24hr extended release; not to exceed 100 mg/day
  • Severe: Not recommended

Safety and efficacy not established

Initiate dosage at lower end of range

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Interactions

Interaction Checker

and tapentadol

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Nausea (30%)

            Dizziness (24%)

            Vomiting (18%)

            Somnolence (15%)

            1-10% (selected)

            Constipation (8%)

            Pruritus (5%)

            Xerostomia (4%)

            Fatigue (3%)

            Hyperhidrosis (3%)

            Anorexia (2%)

            Dyspepsia (2%)

            Insomnia (2%)

            Postmarketing Reports

            Anaphylaxis, angioedema, anaphylactic shock

            Psychiatric disorders: Hallucinations, suicidal ideation, panic attack

            Nervous system disorders: Headache

            Gastrointestinal disorders: Diarrhea

            Cardiac disorders: Palpitations

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            Warnings

            Black Box Warnings

            Addiction, abuse, and misuse

            • Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
            • Assess each patient’s risk prior to prescribing 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
            • Monitor for respiratory depression, especially during initiation or following a dose increase Instruct patients to swallow tablet/capsule whole; crushing, chewing, or dissolving can cause rapid release and absorption of a potentially fatal dose

            Accidental exposure

            • Accidental of even 1 dose, especially by children, can result in a fatal overdose

            Neonatal opioid withdrawal syndrome

            • Prolonged use 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
            • Syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea and failure to gain weight
            • Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn
            • 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
            • Coingestion of alcohol may cause rapid release of opioid content from long-acting tablet/capsule and result in increased plasma levels and a potentially fatal overdose

            Contraindications

            Hypersensitivity (eg, anaphylaxis, angioedema)

            Significant respiratory depression

            Acute or severe asthma

            Hypercarbia in unmonitored setting or in absence of resuscitative equipment

            Paralytic ileus

            Coadministration with monoamine oxidase inhibitors (MAOIs) or use within 14 days

            Cautions

            Conditions with risk for respiratory depression (particularly in patients who are elderly or debilitated or have comorbid conditions with hypoxia, hypercarbia, or airway obstruction)

            May increase intracranial pressure

            May cause drowsiness (use with caution when driving or operating machinery)

            Instruct patients not to consume alcoholic beverages or use prescription or nonprescription products containing alcohol, other opioids, or drugs of abuse

            May cause serotonin syndrome

            May cause severe hypotension; avoid use in patients with circulatory shock or taking hypotensive agents

            May cause spasms of sphincter of Oddi

            May prevent/obscure diagnosis of acute abdominal conditions

            Potential for addiction and misuse exist

            Abrupt discontinuance may precipitate withdrawal symptoms (eg, anxiety, sweating, insomnia, rigors, pain, nausea, tremors, hallucinations)

            Use caution in adrenal insufficiency, CNS depression, head trauma, hepatic/renal impairment, hypothyroidism, prostatic hyperplasia, respiratory disease, or seizures

            Long-acting opioids

            • Schedule II opioid analgesics expose users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids due to the larger amount of active opioid present (see Black Box Warnings)
            • Addiction, abuse, and misuse risks are increased in patients with a personal or family history of substance abuse or mental illness (eg, major depression); the potential for these risks should not, however, prevent the prescribing of proper pain management in any given patient; intensive monitoring is necessary (see Black Box Warnings)
            • Serious, life-threatening, or fatal respiratory depression reported (see Black Box Warnings)
            • Accidental exposure reported, including fatalities (see Black Box Warnings)
            • Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)
            • Interactions with CNS depressants (eg, alcohol, sedatives, anxiolytics, hypnotics, neuroleptics, other opioids) can cause additive effects and increase risk for respiratory depression, profound sedation, and hypotension
            • Life-threatening respiratory depression is more likely to occur in elderly, cachectic, or debilitated patients as they may have altered pharmacokinetics or altered clearance compared to younger, healthier patients
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Unknown whether drug is distributed in breast milk; do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Mu-opioid agonist; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation; also inhibits reuptake of norepinephrine, which also affects ascending pain pathways  

            Absorption

            Bioavailability: 32% (single dose, fasting)

            Peak plasma time: Immediate release, 1.25 hr; extended release, 3-6 hr

            Distribution

            Protein bound: 20%

            Vd: 540 L (IV)

            Metabolism

            Metabolized via glucuronidation (97%)

            Elimination

            Half-life: Immediate release, 4 hr; extended release, 5-6 hr

            Excretion: Urine (99%)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
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            QL Quantity Limits
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            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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