Tapentadol
NUCYNTA
Pronunciation: ta-PEN-ta-dol (nyoo-SIN-ta)
“Tape in the doll’s New scent”
pinpoint pupils → opioid
What it isMu-opioid agonist and norepinephrine reuptake inhibitor; severe nociceptive and neuropathic pain.
Why this oneUnlike tramadol, it needs no CYP2D6 activation and has little serotonergic effect, making analgesia more predictable.
What limits itDependence, respiratory depression, and constipation remain. Avoid MAOIs; noradrenergic toxicity and hypertension can result.
FDA-approved for
- pain (2008)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Moderate-to-severe acute pain | Adults | Individualized per full PI | Individualized per full PI | Individualized per full PI |
| Moderate-to-severe acute pain | Pediatric ≥6 yr and ≥40 kg, able to swallow tablets | Individualized per full PI | Individualized per full PI | Individualized per full PI |
| Moderate-to-severe acute pain, moderate hepatic impairment | Adults | 50 mg q8h (max 3 doses/24h) | 50 mg q8h | 3 doses/24h |
Renal Severe renal impairment: not recommended
Hepatic Moderate: 50 mg no more than q8h (max 3 doses/24h); severe: not recommended
Instructions
- Take with or without food
- Use lowest effective dose for shortest duration
- Do not abruptly discontinue in physically dependent patients — taper gradually
- Assess need for and consider prescribing naloxone
Available strengths
- tab 50, 75, 100 mg
- sol 20 mg/mL
- ER tab 50, 100, 150, 200, 250 mg
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma in unmonitored setting or without resuscitative equipment
- Known/suspected GI obstruction, including paralytic ileus
- MAOIs (concurrently or within 14 days) due to risk of serotonin syndrome
Cautions
- Opioid-induced hyperalgesia and allodynia
- Serotonin syndrome with concomitant serotonergic drugs
- Life-threatening respiratory depression (pulmonary disease, elderly/cachectic/debilitated)
- Adrenal insufficiency; severe hypotension
- Risk of overdose/death with benzodiazepines or other CNS depressants
Adverse reactions
- Nausea
- Vomiting
- Dizziness
- Somnolence
- Constipation
- Pruritus
- Headache
- Fatigue
Pregnancy Prolonged use may cause neonatal opioid withdrawal syndrome; may cause fetal harm
Lactation No human data; present in animal milk; monitor breastfed infants for sedation/respiratory depression
Cost
| Strength | #/mo | generic $/unit | CostPlus | |
|---|---|---|---|---|
| 50 mg | tab | per unit | $8.85/ea | not offered |
| 75 mg | tab | per unit | $10.65/ea | not offered |
| 100 mg | tab | per unit | $14.48/ea | not offered |
| 20 mg/mL | sol | per unit | not offered |
Generic entry2026
⚠ BOXED WARNINGS
- Addiction, abuse and misuse
- Life-threatening respiratory depression
- Risk from concomitant use with benzodiazepines
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityRespiratory depression, dependence and overdose; risk rises sharply with sedatives or impaired clearance.
Serotonin and MAOI
Provisional washout figures
Elevating mechanismWeak/borderline SRI
Non-elevating actionNone recorded
Exposure dependenceDose/exposure dependent; clinical relevance mainly with MAO-A inhibition
Washout BEFORE an MAOI14 days
Evidence confidenceModerate
InterpretationWeak/uncertain SRI, substantially less potent than tramadol; limited replicated data.
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