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

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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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

            Interaction with benzodiazepines and other CNS depressants

            • Coadministration with benzodiazepines or other CNS depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death
            • Reserve concomitant prescribing for use in patients for whom alternative treatment options are inadequate; limit dosages and durations to the minimum required; and follow patients for signs and symptoms of respiratory depression and sedation

            Contraindications

            Hypersensitivity (eg, anaphylaxis, angioedema)

            Significant respiratory depression

            Acute or severe asthma

            Hypercarbia in unmonitored setting or in absence of resuscitative equipment

            Gastrointestinal obstruction, including suspected 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)

            Avoid dosing errors that may result from confusion between mg and mL when prescribing, dispensing, and administering oral solution; ensure the dose is communicated clearly and dispensed accurately; always use the enclosed calibrated syringe when administering drug to ensure the dose is measured and administered accurately; do not use teaspoon or tablespoon to measure a dose; a household teaspoon or tablespoon is not an adequate measuring device; health care providers should recommend a calibrated device that can measure and deliver prescribed dose accurately, and instruct caregivers to use extreme caution in measuring dosage

            In patients who may be susceptible to intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), therapy may reduce respiratory drive, and resultant CO2 retention can further increase intracranial pressure; monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy; opioids may obscure clinical course in a patient with a head injury; avoid the use in patients with impaired consciousness or coma

            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

            Cases of serotonin syndrome, a potentially life-threatening condition, reported with concomitant use of serotonergic drugs; this may occur within the recommended dosage range; the onset of symptoms generally occur within several hours to a few days of concomitant use, but may occur later than that; discontinue therapy immediately if serotonin syndrome is suspected

            Therapy may cause severe hypotension including orthostatic hypotension and syncope in ambulatory patients; there is 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 patients for signs of hypotension after initiating or titrating dosage; in patients with circulatory shock, therapy may cause vasodilation that can further reduce cardiac output and blood pressure; avoid therapy in patients with circulatory shock

            Contraindicated in patients with known or suspected gastrointestinal obstruction, including paralytic ileus; may cause spasm of sphincter of Oddi; opioids may cause increases in serum amylase; monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms

            May prevent/obscure diagnosis of acute abdominal conditions

            Avoid use of mixed agonist/antagonist (e.g., pentazocine, nalbuphine, and butorphanol) or partial agonist (e.g., buprenorphine) analgesics in patients who are receiving a full opioid agonist analgesic; mixed agonist/antagonist and partial agonist analgesics may reduce analgesic effect and/or precipitate withdrawal symptoms

            Addiction can occur in patients appropriately prescribed therapy; addiction can occur at recommended dosages and if drug is misused or abused

            While serious, life-threatening, or fatal respiratory depression can occur at any time during therapy, risk is greatest during initiation of therapy or following dosage increase; monitor patients closely for respiratory depression, especially within first 24 to 72 hr of initiating therapy with and following dosage increases; accidental ingestion of even one dose, especially by children, can result in respiratory depression and death due to overdose of opioid

            Profound sedation, respiratory depression, coma, and death may result from concomitant administration with benzodiazepines or other CNS depressants (e.g., non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol); because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate

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

            Cases of adrenal insufficiency reported with opioid use, more often following greater than one month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; if adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids; wean patient off of opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers; other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency

            Use caution in CNS depression, 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

            Prolonged use of opioid analgesics during pregnancy can cause neonatal opioid withdrawal syndrome; there are no available data in pregnant women to inform a drug associated risk for major birth defects and miscarriage; published studies with morphine use during pregnancy have not reported a clear association with opioids and major birth defects

            Prolonged use of opioid analgesics during pregnancy for medical or nonmedical purposes can result in physical dependence in the neonate and neonatal opioid withdrawal syndrome shortly after birth; the onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of drug by newborn; observe newborns for symptoms of neonatal opioid withdrawal syndrome and manage accordingly Severe fetal bradycardia reported when administered during labor; naloxone may reverse these effects; although there are no reports of fetal bradycardia earlier in pregnancy, it is possible it may occur; drug should be used in pregnancy only if clearly needed, if potential benefit outweighs risk to fetus, and if appropriate measures such as fetal monitoring are taken to detect and manage potential adverse effect on fetus

            Labor or delivery

            • Opioids cross placenta and may produce respiratory depression and psycho-physiologic effects in neonates; an opioid antagonist, such as naloxone, must be available for reversal of opioid induced respiratory depression in neonate; drug is not recommended for use in women during and immediately prior to labor, when use of shorter-acting analgesics or other analgesic techniques are more appropriate; opioid analgesics can prolong labor through actions that temporarily reduce strength, duration, and frequency of uterine contractions; however, this effect is not consistent and may be offset by an increased rate of cervical dilatation, which tends to shorten labor; monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression

            Infertility

            • Due to effects of androgen deficiency, chronic use of opioids may cause reduced fertility in females and males of reproductive potential; it is not known whether effects on fertility are reversible

            Lactation

            Drug is present in breast milk; published lactation studies report variable concentrations of drug in breast milk with administration of immediate-release formulation to nursing mothers in early postpartum period

            The developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy; capsules and any potential adverse effects on breastfed infant from therapy or from underlying maternal condition

            Monitor infants exposed to drug through breast milk for excess sedation and respiratory depression; withdrawal symptoms can occur in breastfed infants when maternal administration of an opioid analgesic is stopped, or when breast- feeding is stopped

            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
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            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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