Names and pronunciation
(ta-pen′ta-dol) Nucynta, Nucynta ER
Source page 1258
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Individual generic drug information
Extracted information for tapentadol only.
(ta-pen′ta-dol) Nucynta, Nucynta ER
Source page 1258
Func. class.: Analgesic, misc.
Source page 1258
Chem. class.: μ-Opioid receptor agonist Controlled Substance Schedule II
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ACTION: Centrally acting synthetic analgesic; μ-opioid agonist activity is thought to result in analgesia; inhibits norepinephrine uptake
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USES: Moderate to severe pain, diabetic peripheral neuropathy
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Extracted information for tapentadol only.
CONTRAINDICATIONS: Hyper- sensitivity, asthma, ileus, respiratory depression
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Black Box Warning: Respiratory depression Precautions: Pregnancy, breastfeeding, children <18 yr, increased intracranial pressure, MI (acute), severe heart dis- ease, respiratory depression, renal/ hepatic disease, GI obstruction, ulcerative colitis, sleep apnea, seizure disorder Black Box Warning: Accidental expo- sure, avoid ethanol, substance abuse, neonatal opioid withdrawal syndrome, potential for overdose, poisoning, coadministration with other CNS de- pressants Black Box Warning: These products have high potential for overdose, poi- soning; may be fatal because of respira- tory depression • Oral solution: measure using cali- brated syringe Black Box Warning: Increase: effects with other CNS depressants—alcohol, opioids, sedative/hypnotics, antipsychot- ics, skeletal muscle relaxants Increase: toxicity—MAOIs Increase: serotonin syndrome—SSRIs, SNRIs, serotonin-receptor agonists, tricyclics Black Box Warning: Do not use with al- cohol; fatal overdose may occur Drug/Herb Increase: sedative effect—kava, St. John’s wort, valerian Black Box Warning: Addiction risk, previous substance abuse: assess before using ext rel product; some may crush ext rel product and snort, inject product that is dissolved Black Box Warning: Accidental expo- sure: identify if alcohol has been used before giving this product; may be fatal if used with tapentadol; keep from pets, children; avoid coadministration with other CNS depressants Black Box Warning: Respiratory dys- function: respiratory depression, char- acter, rate, rhythm; notify prescriber if respirations are <10/min; B/P, pulse Black Box Warning: Neonatal opioid withdrawal syndrome: may be fatal; monitor neonates for irritability, hyper- activity, abnormal sleep pattern, high- pitched crying, tremors, vomiting, diar- rhea, failure to gain weight • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, including neonatal opioid withdrawal syndrome; do not breastfeed, excretion unknown Black Box Warning: Not to use with alcohol; may be fatal • To notify prescriber if pregnancy is planned or suspected, or if breastfeed ing HIGH ALERT
Source pages 1258, 1259, 1260
SIDE EFFECTS CNS: Drowsiness, dizziness, confu- sion, headache, euphoria, hallucina- tions, restlessness, syncope, anxiety, flushing, psychological dependence, insomnia, lethargy, tremors, seizures CV: Palpitations, bradycardia, hypo/ hypertension, orthostatic hypotension, sinus tachycardia GI: Nausea, vomiting, anorexia, con- stipation, cramps, gastritis, dyspepsia, biliary spasms GU: Urinary retention/frequency INTEG: Rash, urticaria, diaphoresis, pruritus RESP: Respiratory depression, cough SYST: Anaphylaxis, infection, serotonin syndrome
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INTERACTIONS
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Extracted information for tapentadol only.
DOSAGE AND ROUTES • Adult: PO 50-100 mg q4-6hr, may give 2nd dose ≥1 hr after 1st dose, max 700 mg on day 1, max 600 mg/day thereafter; ext rel 50 mg q12hr (opioid-naive), titrate to 50 mg/dose bid q3days, max 250 mg q12hr Hepatic disease • Adult: PO Immediate rel 50 mg q8hr, may titrate to response; ext rel 50 mg daily, max 100 mg/day
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Available forms: Tabs 50, 75, 100 mg; tabs ext rel 50, 100, 150, 200, 250 mg; oral solution 20 mg/mL
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Administer: • With antiemetic if nausea, vomiting occur • When pain is beginning to return; de- termine dosage interval by response • Do not crush, chew, break ext rel product, or use with alcohol; swallow whole with sufficient liquid • Preferred analgesic in those with al- tered cytochrome P450 or mild hepatic, mild to moderate renal disease • Store in light-resistant area at room temperature
Source page 1259
Extracted information for tapentadol only.
Assess: • Pain: intensity, location, type, character- istics; need for pain medication by pain/ sedation scoring; physical dependence • I&O ratio; check for decreasing out- put; may indicate urinary retention • CNS changes: dizziness, drowsiness, hal- lucinations, euphoria, LOC, pupil reaction • Serotonin syndrome: increased heart rate, shivering, sweating, dilated pupils, tremors, high B/P, hyperthermia, headache, confusion; if these occur, stop product, ad minister serotonin antagonist if needed • Seizures: history of seizures increased with SSRIs, SNRIs, tricyclic antidepressants • Allergic reactions: rash, urticaria, ana- phylaxis T
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Evaluate: • Therapeutic response: decrease in pain
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CLINICAL CONSIDERATIONS
Source page 1259
Patient and caregiver information: • To report any symptoms of CNS changes, allergic reactions, seizures, se- rotonin syndrome • That physical dependency may result from extended use • That withdrawal symptoms may occur: nausea, vomiting, cramps, fever, faint- ness, anorexia • To avoid CNS depressants, alcohol • To avoid driving, operating machinery if drowsiness, dizziness occur • To change positions slowly to decrease orthostatic hypotension • Teach patient to take as directed, not to double doses, if breakthrough pain occurs, notify provider, do not discon- tinue abruptly, gradually taper • Seizures: Teach patient that if seizure occurs, discontinue, notify provider • Not to drive or perform other hazardous activities until response is known • Orthostatic hypertension: To rise slowly to prevent orthostatic hypertension • Serotonin syndrome: Teach patient symptoms of serotonin syndrome and when to contact provider • To discuss with provider all OTC, Rx, herbals, supplements taken
Source page 1260
Extracted information for tapentadol only.
PHARMACOKINETICS Bioavailability 32%, extensively metabo- lized by liver, excreted in urine 99%, ter- minal half-life 4 hr, protein binding 20%
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Filter the extracted dose blocks for this individual drug.
• Adult: PO 50-100 mg q4-6hr, may give 2nd dose ≥1 hr after 1st dose, max 700 mg on day 1, max 600 mg/day thereafter; ext rel 50 mg q12hr (opioid-naive), titrate to 50 mg/dose bid q3days, max 250 mg q12hr Hepatic disease
Candidate age grouping · source pages 1258, 1259
• Adult: PO Immediate rel 50 mg q8hr, may titrate to response; ext rel 50 mg daily, max 100 mg/day
Candidate age grouping · source pages 1258, 1259