By Freny Menezes

Pharm. D

21 August 2022
Medically reviewed by
Kajal Jain
M. Pharm
Table of Contents

The Controlled Substances Act of the U.S. regulates the use of drugs by placing them into 1 of 5 descending schedules ranging from Schedule I to Schedule V. Tapentadol is a centrally acting, atypical analgesic with a novel mechanism of action that is a combination of μ-opioid agonist activity and norepinephrine reuptake inhibition.

The United States FDA approved Tapentadol's immediate release in December 2008 and the extended-release formulation (Nucynta ER) in August 2011. The prevalence of Tapentadol abuse and diversion (ER and IR) has been low compared with other prescription opioid compounds, mainly when considered at the population level. Continue reading for more details.

What Is The Tapentadol (Nucynta) Used For?

Tapentadol (Nucynta) is a central-acting opioid medicament of the benzenoid class for alleviating severe acute pain for a short period when other medications become intolerant. It reduces pain perception by altering the receptors of the brain.  

It increases extracellular norepinephrine (NE) due to its dual mechanism of action, i.e., it acts on mu-opioid receptor (MOR) agonist and noradrenaline reuptake inhibition. It shows its effect within 30 minutes of administration and lasts for nearly 4-6 hours.

Things To Know Before Using Tapentadol

Nucynta drug is habit-forming even at regular doses. It should be taken in the exact manner as prescribed by the doctor. Also, it should be swallowed whole with a glass of water to avoid exposure to a potentially fatal dose.

Tapentadol should not be taken if you are allergic to it or if you have-

  • Stomach or bowel obstruction
  • Severe asthma or breathing problem
  • If you have taken an MAO inhibitor (viz., Phenelzine, isocarboxazid, methylene blue injection or tranylcypromine) in the past 14 days.
  • Before taking this drug, inform your doctor if you have-
  • Urination problem
  • Alcoholism or drug addiction
  • Brain tumor or head injury
  • Problem with gallbladder, thyroid, pancreas, or adrenal gland
  • Breathing problems, sleep apnea
  • Liver or renal disorder
  • Intimate the doctor if you are breastfeeding or pregnant, as it can cause life-threatening symptoms in the baby after it is born.

Other Uses Of Tapentadol

Tapentadol (Nucynta) is an FDA-approved medicine for managing short-term (acute) pain that is severe enough to take opioid analgesics and when other pain medications become intolerant.

Tapentadol is highly useful in the following conditions-

  • Moderate to severe acute pain
  • Chronic pain
  • Tapentadol in Neuropathic pain is associated with diabetic peripheral neuropathy, which is used to treat pain due to nerve damage in diabetic patients.

In patients with chronic pain from Fibromyalgia, the increase in inhibition of endogenous pain by Tapentadol was translated into analgesia in patients with a normal CNFS. This medicine is unsafe for pregnant or breastfeeding women and should inform the healthcare practitioner.  

How To Properly Use Tapentadol?

Tapentadol (Nucynta) is an opioid analgesic that may be addictive, even at its regular dose. It should be taken in a manner as prescribed by the doctor, and instructions on the prescription label should be read carefully with all medical guides. Also, the following things should be kept in mind while taking this medicine:

  • Never self-medicate or share this medicine with another person, especially someone who has previously suffered from drug addiction. 
  • You should inform the doctor if you feel the urge to take more of this medicine.
  • Do not take any medicine containing Tapentadol or tramadol while on drug Nucynta ER extended-release tablets.
  • Do not crush or chew this tablet; instead, swallow it as a whole with a glass of water, as the outcome could be fatal.
  • This medicine should be taken at the same time interval each day and can be taken with or without food.
  • Tapentadol can cause constipation. Thus, it would be wise to talk to concerned healthcare professionals about the same before using any stool softener or laxative to prevent this side effect.
  • In case of any withdrawal symptoms are observed, stop taking drugs immediately and inform the concerned healthcare practitioner.
  • Leftover Nucynta should not be administered as its accidental or improper use can be fatal.
  • Avoid taking alcohol while on Nucynta, as dangerous effects might occur, including dizziness, drowsiness or death.

How To Store This Medication Safely? 

Tapentadol (Nucynta) is an effective drug in treating moderate to severe pain and is most effective when other drugs become intolerant. But its efficacy depends on various factors, i.e., dosage and administration time, medical history, body weight, age, tolerance, interaction with other drugs, storage of drugs, etc.

Storage of drugs is a crucial aspect of the drug control system in order to ensure that the quality of drugs is not compromised.

Tapentadol (Nucynta) should be stored at room temperature, away from moisture and heat. Also, it should be stored safely so that no one else administers it accidentally or purposely.

These pills should be kept out of reach and sight of children and pets. Also, the track of medicine should be kept properly to know how much medication is left or missing.

Tapentadol works directly on the opioid receptors in CNS and reduces the feeling of pain.
Tapentadol stays in the blood for no more than a day and in urine for 3 to 4 days, but it will remain in your hair for considerably longer.
Avoid drinking alcohol while on Tapentadol, as it may lead to drowsiness, dizziness, increased impairment, sedation, difficulty concentrating, respiratory depression, and death. 

When Should You Stop Using Tapentadol?

Nucynta drug is usually tolerated well but minor adverse effects can be observed, such as vomiting, headache, itching, dry mouth, drowsiness, and dizziness. In a few cases, there is a possibility of a life-threatening allergic reaction to the drug.

Thus, various precautions should be taken with this drug. This drug should not be self-administered and should not be stopped without a doctor's consultation. 

If this drug is stopped suddenly, a person might experience withdrawal symptoms, especially if the drug has been taken for a longer period of time. These symptoms include tremors, sweating, diarrhea, Anxiety, insomnia, and hallucinations.

Bottom Line From Practical Anxiety Solutions

Tapentadol is an opioid analgesic medication that may be habit-forming even during its regular use. Thus, it should be taken as prescribed by your healthcare practitioner. It treats moderate-to-severe acute pain, neuropathic pain, osteoarthritis pain, chronic pain, and Fibromyalgia.

It is used especially when other painkillers become intolerant. Also, precautions should be taken before taking this medication and ensure adequate storage of the drug. In case of any serious side effects are observed, seek immediate help from the healthcare practitioner.

  • Low, Ching Y., Kenneth L. McCall, and Brian J. Piper. "Declines and pronounced state-level variation in tapentadol use in the US." medRxiv (2022). Obtain On 02/11/2022
  • Darke, Shane, et al. "Characteristics of fatal tapentadol‐related toxicity in Australia." Drug and alcohol review (2022). Obtain On 02/11/2022
  • Partridge, Emma, et al. "The increasing use and abuse of tapentadol and its incorporation into a validated quantitative method." Journal of analytical toxicology 42.7 (2018): 485-490. Obtain On 02/11/2022
  • Del Águila, Manuel J. Sánchez, et al. "Practical considerations for the use of tapentadol prolonged release for the management of severe chronic pain." Clinical Therapeutics 37.1 (2015): 94-113. Obtain On 02/11/2022
What's on your mind?

Start a conversation, Post with kindness.