Tapentadol

What Is Tapentadol?

Tapentadol is a potent prescription medication used for the management of moderate to severe pain. As an opioid analgesic, it offers effective relief through a dual mechanism of action. This enhances its pain-relieving properties while potentially reducing the risk of tolerance compared to traditional opioids. 

History Of Tapentadol

Tapentadol is a pain medication developed by the German company Grünenthal in the late 1980s. It was designed as an improved version of Tramadol, another painkiller created by Grünenthal in 1962. 

Tapentadol was introduced to the market in 2008 after being approved by the FDA. It was classified as a Schedule II controlled substance in 2009. Johnson & Johnson then took over its marketing in the US, Canada, and Japan, while Grünenthal handled other regions.

In 2010, Grünenthal allowed Johnson & Johnson to market Tapentadol in around 80 more countries. The drug was also approved in Europe later that year. 

An extended-release version, Nucynta ER, was launched in the US in 2011 to manage chronic pain and diabetic nerve pain [1].

Tapentadol Brand Name

The popular brand names of  Tapentadol include Nucynta, Palexia, Aspadol, Tapaday, Topcynta, Yantil, Tapenta, and Tapal. 

It is important to note that generic Tapentadol tablets are not yet available. Currently, this medication is exclusively available in its branded versions.

Available Formulations

Tapentadol is prescribed in various formulations, including immediate-release and extended-release forms, to address different pain management needs. 

Immediate Release (IR) Formula- 

These are medications that are designed to dissolve instantly after intake. Eighty-five percent of these IR tablets are dissolved within thirty minutes [2]. 

Extended-Release (ER) Tablets- 

These are medications that are designed to release the active compound to release slowly over time, usually 12 or 24 hours [3].

What Is Tapentadol Used For?

Tapentadol IR tablets are used for moderate to severe acute pain. It is a type of pain that occurs suddenly and is usually sharp or intense. It typically results from injury or illness and lasts for a short period of time. Acute pain often resolves as the underlying cause heals.

Tapentadol ER tablets are recommended for chronic pain. It is a type of pain that lasts beyond 3 to 6 months. 

Tapentadol ER is advised for treating body pain caused by diabetic neuropathy and skeletomuscular pain. They are also recommended for post-surgical pain. 

Benefits of Tapentadol 

• Compared to traditional opioids like morphine or oxycodone, Tapentadol has a lower risk of experiencing side effects.
• It has a lower risk for abuse compared to other opioids. 
• One of the safest options for treating chronic pain in conditions where other treatment options do not offer effective pain relief. 

Mechanism Of Action Of Tapentadol Hydrochloride

Tapentadol works by combining two mechanisms of action. It combines mu-opioid receptor agonism with noradrenaline reuptake inhibition in the same molecule. This dual mechanism of action makes Tapentadol an effective pain medication for treating acute, chronic, and neuropathic pain. 

Μ-Opioid Receptor (MOR) Agonism

Tapentadol acts as an agonist at the μ-opioid receptors in the central nervous system (CNS). Tapentadol helps alter pain perception and reduce body pain by binding to these receptors.

Noradrenaline Reuptake Inhibition

Tapentadol also acts as a norepinephrine reuptake inhibitor. By blocking the reuptake of norepinephrine, it increases the levels of this neurotransmitter in the spinal cord. This contributes to the analgesic effects of Tapentadol by altering pain transmission pathways in the spinal cord and central nervous system.

How To Take Tapentadol? 

• The Tapentadol tablets should be swallowed with water.
• Take it as a whole without breaking or crushing it.
• Tapentadol can be taken with or without a meal. 

Tapentadol Warnings

• The use of Tapentadol has a risk for abuse and addiction. 
• Avoid taking this medication with alcohol, as it can cause breathing problems and drowsiness. 
• Before taking Tapentadol, pregnant women should talk with their doctors about the risks. As it can result in birth defects when used during pregnancy. Inform your doctor immediately if your newborn baby has any symptoms, such as-
  • Vomiting
  • Diarrhea
  • shallow breathing
  • Irritability
  • poor feeding
  • Shaking
• Before taking Tapenatdol-brand drugs, inform your doctor if you are allergic to them or if any other compounds are present in the formulation. 
• Tapentadol use can make you dizzy and drowsy. Use heavy machinery or drive with caution. 
• Before having surgery, inform your doctor about using Tapentadol. 
• Older adults may be more sensitive to side effects and, thus, should be used with caution [4]. 
• Breastfeeding mothers should take the Tapentadol dosage with caution. 
  • Avoid breastfeeding your baby for 2 to 3 hours after taking the medication. 
  • After breastfeeding, the baby should be carefully monitored for signs of unusual drowsiness, weakness,  and breathing issues. 

Tapentadol Contraindications

The use of Tapentadol is contraindicated in patients with the following health conditions- 

• Seizures
• Gallbladder disease
• Kidney or liver disease
• Mood disorders such as confusion, depression, thoughts of suicide
• History of a substance use disorder
• Intestinal problems such as blockage, constipation, and diarrhea
• Pancreatitis
• Heart disorder or a history of heart attack
• Thyroid disorder
• Severe respiratory depression
• Difficulty urinating or having an enlarged prostate.

Tapentadol Side Effects

The common side effects of Tapentadol include- 

• Nausea
• Constipation
• Sleepiness
• Vomiting
• Dizziness
• Headache
• dry mouth
• fatigue

Contact a doctor immediately if you experience any of the following severe side effects from taking Tapentadol-

• seizures
• agitation
• confusion
• fast heartbeat
• loss of coordination
• decreased sexual desire
• rash
• swelling of the eyes, face, lips, tongue, or throat
• hoarseness
• difficulty breathing or swallowing
• chest pain.

Long-Term Side Effects Of Tapentadol

Long-term use of Tapentadol can become habit-forming, causing mental and physical dependence. Long-term use of Tapentadol can also result in-

• Excess sweating 
• Decreased sense of touch or sensation 
• Cough 
• Slurred speech 
• Low sodium levels 
• low blood pressure
• Serotonin syndrome 
• Decreased libido (low sex drive) [5].

Tapentadol Withdrawal Symptoms

Sudden discontinuation of Tapentadol tablets can result in withdrawal symptoms, including-

• fever 
• chills
• loss of appetite
• joint pain
• anxiety
• Restlessness [6].

Tapentadol Options At IyrinHealth Care 

At IyrinHealth Care, we retail three of the most potent and affordable Tapentadol brands: Aspadol, Tapaday, and Topcynta. 

• 
  

  Aspadol 100mg

  $500.00
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• 
  

  Aspadol 200mg

  $199.00 – $279.00
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• 
  

  Tapaday 100mg

  $189.00 – $269.00
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• 
  

  Tapaday 200mg

  $199.00 – $279.00
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• 
  

  Topcynta 100mg

  $169.00 – $249.00
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Tapentadol Alternatives At IyrinHealth Care

Tapentadol alternatives available at IyrinHealth Care include Pregabalin and Carisoprodol. It is important to consult a doctor before making any changes to your medication regimen. Both Pregabalin and Carisoprodol belong to different drug classes and have distinct mechanisms of action.

• Pregabalin
• Carisoprodol