Nucynta Uses, Dosage, Side Effects, Food Interaction and all others data.

Nucynta is a centrally-acting synthetic analgesic. It is 18 times less potent than morphine in terms of binding to human mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake. Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval.

Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.

Nucynta is a centrally-acting synthetic analgesic that is 18 times less potent than morphine in binding mu-opioid receptors. It also increases norepinephrine concentrations in the brains of rats via inhibition of norepinephrine reuptake. Selective mu-opioid antagonists like naloxone can block analgesia from tapentadol. It also has not effect on the QT interval.

Trade Name Nucynta
Availability Prescription only
Generic Tapentadol
Tapentadol Other Names Tapentadol
Related Drugs Buprenex, aspirin, acetaminophen, tramadol, duloxetine, naproxen, Tylenol, oxycodone, Cymbalta, pregabalin
Weight 100mg, 50mg, 75mg, 150mg, 200mg, 250mg,
Type Oral Solution, Oral Tablet, Extended Release
Formula C14H23NO
Weight Average: 221.3385
Monoisotopic: 221.177964363
Protein binding


Groups Approved
Therapeutic Class Opioid analgesics
Available Country United States,
Last Updated: September 19, 2023 at 7:00 am


Nucynta is used for the relief of moderate to severe acute pain in patients 18 years of age or older.

Nucynta is also used to associated treatment for these conditions: Diabetic Peripheral Neuropathic Pain (DPN), Severe, Chronic Pain, Acute, moderate Pain, Acute, severe Pain, Chronic, moderate Pain

How Nucynta works

Tapendadol causes large increases in levels of extracellular norepinephrine (NE) due to a dual mechanism of action involving mu opioid receptor (MOR) agonism as well as noradrenaline reuptake inhibition.


Nucynta dosage

As with many centrally-acting analgesic medications, the dosing regimen should be individualized according to the severity of pain being treated, the previous experience with similar drugs and the ability to monitor the patient.

The dose is 50 mg, 75 mg, or 100 mg every 4 to 6 hours depending upon pain intensity. On the first day of dosing, the second dose may be administered as soon as one hour after the first dose, if adequate pain relief is not attained with the first dose. Subsequent dosing is 50 mg, 75 mg, or 100 mg every 4 to 6 hours and should be adjusted to maintain adequate analgesia with acceptable tolerability.

Daily doses greater than 700 mg on the first day of therapy and 600 mg on subsequent days have not been studied and are not recommended.

Pediatric use: The safety and effectiveness of Nucynta in pediatric patients less than 18 years of age have not been established.

Use in elderly patients: In general, recommended dosing for elderly patients with normal renal and hepatic function is the same as for younger adult patients with normal renal and hepatic function. consideration should be given to starting elderly patients with the lower range of recommended doses.

Use in Renal Disease: In patients with severe renal impairment, the safety and effectiveness of Nucynta has not been established.

Use in Hepatic Disease: Nucynta should be used with caution in patients with moderate hepatic impairment. Nucynta has not been studied in patients with severe hepatic impairment.

Side Effects

The following treatment-emergent adverse events may happen: heart rate increased, heart rate decreased, visual disturbance, abdominal discomfort, impaired gastric emptying, irritability, edema, drug withdrawal syndrome, hypersensitivity, involuntary muscle contractions, sensation of heaviness, hypoesthesia, paresthesia, disturbance in attention, sedation, dysarthria, memory impairment, ataxia, presyncope, syncope, coordination abnormal, seizure, urticaria, blood pressure decreased etc.


Oral, rabbit: LD50 = 3200 mg/kg; Oral, mouse: LD50 = 300 mg/kg; Oral, rat: LD50: 980 mg/kg; The most common reasons for discontinuation due to adverse events were dizziness, nausea, vomiting, somnolence, and headache.


Nucynta should be administered with caution to patients with conditions accompanied by hypoxia, hypercapnia respiratory problems such as: asthma, chronic obstructive pulmonary disease etc. Besides this in case of patient with sleep apnea syndrome, myxedema, kyphoscoliosis, central nervous system (CNS) depression should have to be cautious prior administration of Nucynta. Patients receiving other mu-opioid agonist analgesics, general anesthetics, phenothiazines, other tranquilizers, sedatives, hypnotics, or other CNS depressants (including alcohol) concomitantly with Nucynta may exhibit additive CNS depression.


Increased risk of serotonin syndrome with other drugs that enhance monoaminergic neurotransmission (e.g. TCAs, triptans, SSRIs, serotonin and norepinephrine reuptake inhibitors). Enhanced sedative effect with benzodiazepines, barbiturates, antipsychotics, H1-antihistamines and other opioids. Increased potential for addiction with mixed μ-opioid agonists/antagonists (e.g. nalbuphine, pentazocine) or partial μ-opioid agonists (e.g. buprenorphine). Increased systemic exposure with strong inhibitors of UGT1A6, UGT1A9 and UGT2B7 isoenzymes. Decreased efficacy with strong enzyme inducers (e.g. rifampicin, phenobarbital).

Food Interaction

  • Take with or without food. Food increases absorption, but not to a clinically significant extent.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Volume of Distribution

Following IV administration, volume of distribution is 540 ± 98 L.

Elimination Route

Bioavailability, immediate release (IR), 86 mg: 32%; Bioavailability, extended release (ER), 86 mg: 32%; Cmax, IR: 64.2 ng/mL; Cmax, ER: 22.5 ng/mL; T max, IR: 1.5 hours; T max, ER: 5.0 hours; Nucynta accumulates following multiple repeat doses.

Half Life

Elimination half-life, IV: 4 hours.


Total clearance = 1530 ± 177 ml/min.

Elimination Route

Nucynta and its metabolites are excreted almost exclusively (99%) via the kidneys. Approximately 70% (55% O-glucuronide and 15% sulfate of tapentadol) is excreted in conjugated form. A total of 3% of drug was excreted in urine as unchanged drug.

Pregnancy & Breastfeeding use

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. This preparation should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Neonates whose mothers have been taking Nucynta should be monitored for respiratory depression.


This drug is contraindicated in patients with impaired Pulmonary Function, It is also contraindicated in patients with acute or severe bronchial asthma or hypercapnia in unmonitored settings or the absence of resuscitative equipment. This drug is contraindicated in any patient who has or is suspected of having paralytic ileus.

Acute Overdose

Symptoms: Vomiting, miosis, CV collapse, consciousness disorders up to coma, convulsions and resp depression up to resp arrest.

Management: Re-establish a patent airway and institute assisted or controlled ventilation. GI decontamination with activated charcoal or by gastric lavage may be considered within 2 hr after intake. Pure opioid receptor antagonists (e.g. naloxone) may be given as antidote.

Storage Condition

Store in a cool and dry place, protected from light and moisture. Keep the medicine out of the reach of children.

Innovators Monograph

You find simplified version here Nucynta

Nucynta contains Tapentadol see full prescribing information from innovator Nucynta Monograph, Nucynta MSDS, Nucynta FDA label


What is the use of tapentadol?

Nucynta tablets are used to treat moderate to severe acute pain (pain that begins suddenly, has a specific cause, and is expected to go away when the cause of the pain is healed). Nucynta extended-release tablets are used to treat severe neuropathic pain in people who have diabetes.

How safe is Nucynta?

Nucynta has a risk for abuse and addiction, which can lead to overdose and death.Nucynta may also cause severe, possibly fatal, To lower your risk, your doctor should have you take the smallest dose of Nucynta that works, and take it for the shortest possible time.

What are the common side effects of Nucynta?

Nucynta may cause common side effects are include:

  • headache
  • heartburn
  • stomach pain
  • dry mouth
  • excessive tiredness
  • anxiety
  • drowsiness
  • difficulty falling asleep or staying asleep
  • abnormal dreams
  • irritability
  • sudden feeling of warmth

Is Nucynta safe during pregnancy?

This may cause serious problems,if you take Nucynta regularly during your pregnancy, your baby may experience life-threatening withdrawal symptoms after birth.

Is Nucynta safe during breastfeeding?

Use is not recommended and a decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother.

Can I drink alcohol with Nucynta ?

Nucynta is a benzenoid class opioid and should not be mixed with alcohol. Doing so can lead to a variety of side effects, the least being increased dizziness and the most being death. Don’t take chances given these serious side effects. Avoid alcohol and anything containing alcohol while taking Nucynta.

How should Nucynta used?

Nucynta comes as a tablet and an extended-release tablet to take by mouth. The tablets are usually taken with or without food every 4 to 6 hours as needed. If you are taking Nucynta tablets, your doctor may tell you that you may take a second dose as soon as 1 hour after the first dose on your first day of treatment if needed to treat your pain. The extended-release tablets are taken once every 12 hours.

What should I do if I take to forget Nucynta?

If you take to forget Nucynta ,take the missed dose as soon as you remember it. Do not take a double dose to make up for a missed one.If you are taking Nucynta extended-release capsules, skip the missed dose and continue your regular dosing schedule.

How long should I take Nucynta for?

Nucynta are usually taken with or without food every 4 to 6 hours as needed.

Does Nucynta work for nerve pain?

Nucynta may also be used to help relieve nerve pain.

Can I drive after taking Nucynta?

Nucynta may make it difficult for you to drive or operate heavy machinery. If you have recently started taking an opioid medication or changed dosage, you may be at higher risk of having an accident.

How much Nucynta can I take?

Adults at first, 50 milligrams 2 times a day. Your doctor may adjust your dose as needed.Nucynta is usually not more than 500 mg per day.

Does Nucynta affect liver?

The acute exposure to Nucynta caused a dose-dependent increase in protein oxidation in liver and kidney.

Can Nucynta cause high blood pressure?

Very high blood pressure may happen.

Is Nucynta bad for my heart?

Nucynta administration can lead to serotonin syndrome, which can certainly lead to serious cardiac arrhythmia.

Does Nucynta help with anxiety?

Nucynta also to decrease of anxiety and depression scores both in patients with clinical depression and in patients with minor depressive symptoms.

Does Nucynta affect fertility?

Nucynta had no influence on male or female fertility in rats but there was reduced in utero survival at the high dose.

*** Taking medicines without doctor's advice can cause long-term problems.