Commonly Asked Questions About Tapentadol

Tapentadol, a potent opioid analgesic, is a prescription medication for managing moderate to severe pain. Its unique dual mechanism of action provides effective pain relief.

As with any medication, Tapentadol raises various questions and concerns among patients. Addressing these common queries is essential for ensuring safe and informed usage of Tapentadol and promoting well-being.

This blog answers common questions about Tapentadol to improve your understanding of this medication. We cover Tapentadol's action, dosage, side effects, and safety to help you make informed decisions and manage pain effectively.

What Is Tapentadol?

Tapentadol is a centrally-acting pain reliever that belongs to the drug class of opioid analgesics. It is a prescription medication that can only be legally obtained with a written prescription from a licensed healthcare provider. 

The popular brand names of Tapentadol are- Palexia, Nucynta, Aspadol, Tapal, and others. This analgesic is available in two formulations.

• Tapentadol Immediate Release (IR)- It is used as a short-term treatment to relieve severe acute pain.

• Tapentadol Extended Release (ER)- It is typically prescribed for the management of severe and constant around-the-clock pain that cannot be controlled with other pain-relieving drugs. 

Tapentadol Approval Dates Worldwide

Is Tapentadol A Scheduled Drug?

Yes, the Drug Enforcement Administration (DEA) has classified Tapentadol as a Schedule II drug. This means that it has a potential for abuse and dependency.

What Is Tapentadol Used For?

Tapentadol is prescribed for managing moderate to severe pain. The immediate-release and extended-release formulations of the analgesic provide options for managing different types of pain and tailoring individual treatment needs. It is used for the following conditions:

• Musculoskeletal Pain: Tapentadol manages pain associated with musculoskeletal conditions such as osteoarthritis, back pain, and joint pain.

• Fibromyalgia: It is a chronic pain disorder characterized by widespread musculoskeletal pain and other symptoms. Tapentadol manages fibromyalgia, providing effective pain relief.

• Postoperative Pain: Tapentadol effectively manages postoperative or post-surgical pain. Clinical studies suggest that it is a suitable option as a preemptive analgesic for acute postoperative pain due to its favorable safety profile [3].

• Neuropathic Pain: It effectively treats neuropathic pain, including diabetic peripheral neuropathy, postherpetic neuralgia, and other nerve-related pain conditions.

• Chronic Pain: Tapentadol may be prescribed for chronic or long-term pain conditions when other pain medications are ineffective.

• Cancer pain management: According to a study by Hans G Kress et al. Tapentadol provides effective pain relief and is well-tolerated in cancer patients.

How Does Tapentadol Work?

Tapentadol's mechanism of action (MOA) involves a dual-action approach, unlike traditional opioids. It acts as both a mu-opioid receptor agonist and a norepinephrine reuptake inhibitor.

• Tapentadol acts as a mu-opioid receptor agonist, which means it enhances the effects of opioid receptors in the brain. 

• The norepinephrine reuptake inhibitor function increases the levels of norepinephrine, a neurotransmitter involved in pain management. 

This dual action allows Tapentadol to effectively relieve moderate to severe pain by targeting two different pathways in the central nervous system.

Absorption-

After oral administration, Tapentadol is absorbed into the bloodstream. Its absorption is rapid, with peak blood levels reached within 1-2 hours for IR formulations and 4-5 hours for ER formulations. However, food can affect the rate of absorption.

Metabolism And Excretion-

Metabolism, or the breaking down process of the drug, occurs in the liver. The half-life of Tapentadol is 3.93 hours following oral consumption. 

The elimination process occurs in the kidney, and most of the drug is eliminated through urine.

How Long Does Tapentadol Take To Kick In?

Tapentadol starts working within 30 minutes of consumption, and its effects last 4 to 6 hours. However, the onset of action can vary depending on factors such as the individual's metabolism, the formulation of Tapentadol (immediate-release or extended-release), and whether it's taken with or without food.

How Long Does Tapentadol Stay In Your System?

Generally, Tapentadol stays in the system for up to 22 hours [4]. This duration can vary among individuals based on factors such as age, metabolism, dosage, body weight, or tolerance. 

How Long Does Tapentadol Stay In Urine, Blood, Hair, And Saliva?

Tapentadol stays in the urine for 3 to 4 days and in the blood for 24 to 48 hours. The drug can be detected in saliva for 5 to 6 hours, while it can last for as long as 30 days in hair.

What Are The Side Effects Of Tapentadol?

A few of the Tapentadol side effects have been mentioned below.

• Drowsiness or sleepiness

• Dizziness

• Nausea

• Vomiting

• Headache

• Itching

• Dry mouth

• Constipation

Long-term side effects of Tapentadol include-

• Gastrointestinal effects such as abdominal pain

• Breathing problems

• Blurry vision

• Memory impairment

What Is The Recommended Dosage Of Tapentadol?

Tapentadol is available in doses of 50 mg, 75 mg, or 100 mg. The standard recommended dose is 100 mg of Tapentadol, which can be taken every 4 to 6 hours, depending on the pain intensity. 

How Much Tapentadol Can I Take?

Do not exceed daily doses over 700 mg on the first day and 600 mg on subsequent days [5]. Also, do not take more than one tablet at once.

It is best to consult a healthcare professional to prescribe the appropriate dosage.

Can Tapentadol Be Taken With Other Medications?

Tapentadol can interact with certain medications to cause drug interactions that can alter efficacy and increase the risks of side effects. 

Tapentadol can interact with 379 medications; a few of them are mentioned below.

• Pregabalin

• Norflex

• Oxycodone

• Diazepam

• Xanax

• Topiramate

• Zoloft

• Albuterol

Can I Take Tapentadol With Gabapentin?

Do not take Tapentadol with Gabapentine. This interaction can cause severe side effects of drowsiness, breathing failure, and impaired cognition.

Is Tapentadol Addictive?

Tapentadol has the potential for addiction and misuse. It's crucial to use the analgesic exactly as prescribed by your healthcare provider to minimize the risk of addiction.

Is Tapentadol Safe For Long-Term Use?

Long-term use of Tapentadol can cause addiction and severe health risks. In case of necessity, it should be done only under the strict supervision of a healthcare provider. Regular monitoring and assessment are crucial in such cases.

What Are The Withdrawal Symptoms Of Tapentadol?

• Anxiety

• Sweating

• Insomnia

• Nausea

• Diarrhea

• Respiratory issues

• Hallucinations

How Long Does Tapentadol Withdrawal Last?

Tapentadol withdrawal timeline can last for a few days, or it can last longer in some individuals. 

How To Taper Off Tapentadol?

Prolonged use, abuse, or sudden discontinuation of Tapentadol can cause withdrawal symptoms. To avoid withdrawal symptoms, the tapering-off method is recommended.

To taper off Tapentadol and avoid withdrawal symptoms, it is recommended to lower the dosage of the medication and then gradually quit taking it.

When Should You Not Use Tapentadol?

The precautions to follow are provided below-

• Do not take Tapentadol if you are below 17 or above 65 years old.

• If you have any medical history of liver or kidney disease or any other condition, consult your doctor before taking Tapentadol.

• Let your doctor know about any medication you are taking or if you have a history of addiction or substance abuse.

What Are The Contraindications For Tapentadol?

Tapentadol is contraindicated in people with-

• Impaired pulmonary function or respiratory issues.

• Paralytic Ileus- It is a condition that causes paralysis or lack of movement in the muscles of the intestines.

• Patients who are taking Monoamine Oxidase Inhibitors (MAOIs). MAOIs are a class of drugs prescribed for treating depression, neurodegenerative diseases, and nervous system disorders.  

Can I Take Alcohol with Tapentadol?

Taking alcohol and Tapentadol together can cause side effects such as dizziness and, in severe cases, it can lead to death. 

Can I Take Tapentadol During Pregnancy?

Tapentadol, categorized as a Pregnancy Category C drug by the FDA, is not advised during pregnancy. Using opioids like Tapentadol during pregnancy can increase the risk of neonatal withdrawal syndrome, respiratory depression in the newborn, and possible long-term effects on the child's development.