Maximizing The Benefits Of Tapentadol- Recommended Dosage And Treatment Duration

 

The right Tapentadol dosage and the health impact of its long-term use are key factors that all users and physicians should take into consideration before embarking on its therapeutic journey. 

Wondering why one should care? We have a few substantial reasons to support our argument. 

The Drug Enforcement Administration (DEA) classifies Tapentadol as Schedule II controlled substance indicating its potential risk for abuse [1]. 

Tapentadol also belongs to the class of opioid analgesics, making it a higher-risk potential medication for abuse and severity of adverse effects. So, this blog meticulously looks into the FDA recommendations for Tapentadol dosage, administration, and duration of treatment to avoid any possible health issues from the pain mediation. 

 

Understanding Tapentadol- An Overview 

Tapentadol is a new class of centrally acting analgesic combining two mechanisms of action. It has clinically demonstrated a broad analgesic effect across multiple pain models and has a 30-minute onset of action. 

The analgesic effect of Tapentadol is independent of its metabolic activity, as it has no active metabolite. Following oral administration, the Tapentadol dose is principally cleared by the kidney. 

Medical Conditions Treated With Tapentadol

Scientific studies suggest that it is different from classical opioids and is thus considered a prior choice of treatment for chronic pain. The prescription use of Tapentadol in the USA was approved in 2008. 

Apart from moderate to severe chronic pain, the use of Tapentadol is also approved for diabetic neuropathic pain. 

A study from the Journal of Pain Research suggests that the Tapentadol dose can be an effective therapy for chronic back pain [2]. Another similar study from the same Journal demonstrates that Tapentadol has been tested in Cancer patients experiencing pain due to anticancer treatment. The study conveys that Tapentadol was well tolerated and effective in such patients [3]. 

 

The Recommended Starting Tapentadol Dose For Different Types Of Pain

The standard recommended dose of tapentadol for all its medically approved conditions is 100 mg. It can be taken 3–4 times daily with a dosage gap of 4–6 hours. 

The Tapentadol dose, however, may differ depending on its formulation. 

Tapentadol is available in two different formulations- Tapentadol Extended Release (ER) and Tapentadol Immediate Release (IR).  

Tapentadol ER Oral Dosing 

The Tapentadol ER strength (amount in milligrams (mg)) is the same, meaning 100 mg for beginners. 

- For Nerve Pain Caused By Diabetes

Tapentadol 50 mg twice daily is recommended for patients with neuropathic pain. One can also divide the Tapentadol 100 mg dose into two halves [4]. 

- For Pain Associated With Cancer Treatment

Suffering from pain is one of the most prevalent issues seen in patients with cancer. About two-thirds of patients report pain at an advanced stage. The predominant cause of pain in 60% of cancer patients is nociceptive; about 20% of patients suffer from neuropathic pain, and the remaining 20% show a combination of nociceptive and neuropathic pain [5]. 

The study suggests that the use of Tapentadol Prolong Release, or ER, is a well-tolerated pain medication that provides adequate pain relief in such patients. Further, Preliminary evaluations indicate that Tapentadol PR or ER may also be a suitable therapy for pain associated with oncological treatments, such as chemotherapy. However, the Tapentadol dose for such patients should be recommended by a doctor and is usually individualized [5]. 

- Clinical Trials On Tapentadol PR In The Treatment Of Cancer Pain

The table below highlights the Tapentadol dose for cancer patients and their findings to establish a preliminary dosage guidelines along with their associated health risks [5]. 

 

 

- Tapentadol ER Dosage For Patients Switching From Other Narcotic Medicines

The Tapentadol dose for people shifting from other pain medications should be determined by a physician after a thorough examination of your health, the severity of the pain, previously used narcotic analgesics, and the cause of the shift in treatment.  

The recommended dosage will then be divided into two doses during the day [4]. 

Tapentadol Immediate-Release Tablets (IR) Dosing Guidelines 

For moderate to severe pain, 100 mg of Tapentadol IR is recommended every 4 to 6 hours. 

Dosing Information For Tapentadol Oral Solution

The available and mostly recommended dosage for Tapentadol oral solution is 2.5 milliliters (mL) (equivalent to 50 milligrams [mg]), 3.75 mL (75 mg), or 5 mL (100 mg). 

 

 

Starting Dosage Guidelines

Day 1 of taking Tapentadol - On the first day of Tapentadol dosing, the second dose should be taken within 1 hour of the first dose in cases where pain relief is not achieved from the first dose. 

Subsequent Dosing - The recommended dose of Tapentadol every 4 to 6 hours. 

 

Individualizing Tapentadol Dosage Based On Health Conditions

Tapentadol dosage adjustments are recommended for individuals with acute kidney or liver disorders. As this organ system plays a key role in the metabolism and elimination of the medication in the system, suffering from any related disorder can affect the efficacy and potency of Tapentadol. 

Renal Dose Adjustments for Tapentadol

No dosage adjustments are required for mild to moderate renal dysfunction. However, people with severe kidney disorders (CrCl less than 30 mL/min) should take the analgesic after consulting a physician. 

Clinical trials on Tapentadol Extended Release (ER) showed that taking 100 to 200 mg twice daily requires no dosage adjustments in patients with mild-to-moderate renal impairments [8]. 

The CrCl (Creatinine Clearance) test monitors the progression of renal disease. The normal CrCl range in males is 110 to 150 mL/min and 100 to 130 mL/min in females [6]. 

Hepatic Dose Adjustments

• People with Mild liver dysfunction (Child-Pugh 5-6) require no dosage adjustment for Tapentadol. 

• For patients with moderate liver dysfunction (Child-Pugh 7 to 9), an initial dose of 50 mg is recommended with a dosage gap of a minimum of 8 hours. 

• In patients with severe renal dysfunction (Child-Pugh 10-15), the use of Tapentadol 100 mg is not advisable. 

The Child-Pugh score helps in assessing the strength of treatment and the necessity of a liver transplant for patients with chronic liver disorders [7]. 

Tapentadol Dose Adjustments In Elderly People 

The use of Tapentadol tablets is not recommended for elderly people over 65 without consulting a doctor. Such people are seen to have weaker metabolic activity, thus altering the time of action and elimination of the medication. 

Tapentadol Dose In Patients With Hemodialysis

There is no clear evidence showcasing the exact impact of Tapentadol administration in patients with dialysis. 

Tapentadol is likely to be dialyzed to some extent due to its low protein binding, average water solubility, and low molecular weight [8]. 

Nucynta ER Dose- Is It Any Different? 

Nucynta ER is similar to the Extended Release formula of Tapentadol as they are formulated with the same active compound. 

Nuynta is the brand name of Tapentadol, thus, showcasing a similar working mechanism, effectiveness, and potency. 

Nucynta ER dosing guidelines

• Take the lowest dose for the shortest duration. 

• The dosing regimen of Nucynta ER should be done considering the following factors-

  • The severity of the patients

  • Prior analgesic treatment experience

  • Response time of the patient

  • History of abuse and addiction

• Patients taking Nucynta ER should be closely monitored for respiratory depression, especially within the first 24 to 72 hours of taking the initial dose or following an increase in the dosage strength. 

• Chewing, Crushing, and dissolving Nucynta ER tablets will cause an uncontrolled release of Tapentadol in the body. It can thus result in overdosing. 

Nucynta ER Dosage Strengths

The Nucynta ER dosage strengths available are 50 mg, 100 mg, 150 mg, 200mg, and 250 mg. 

 

How To Break Down Nucynta ER

Breaking or crushing Tapentadol is not advisable due to the quick release of a large amount of its active compound (Tapentadol) into the system. Moreover, the Nucynta ER tablets are formulated to resist crushing or breaking [9]. 

These Nucynta ER pills are made with an Abuse-Deterrent Formulation (ADF) that prevents an individual from crewing or breaking the pill for inhalation or intravenous (IV) abuse [9]. 

A study further supports it, suggesting that attempts to break or crush the Nucynta ER tablets resulted in minimal deformation, with the exception of using a hammer, which resulted in flattening the tablet [9]. 

A study evaluating the consequences of crushing or opening tablets and capsules suggests the following. 

• Alteration in the drug's absorption rate. 

• Fatal overdosing.

• Changing the effectiveness of the treatment. 

• Breaking or crushing the pill can make its active compound come into contact with air, light, and moisture, thus affecting the potency of the drug [10]. 

 

Tapentadol Maximum Dose And How To Titrate The Dose

The maximum Tapentadol dose on the first day of treatment is 700 mg. On subsequent days, one should not take over 600 mg of tapentadol in a day. 

The maximum Tapentadol or Nucynta ER dose is 500 mg per day [11]. 

Tapentadol ER Titration 

Beginners starting with Tapentadol therapy are generally advised to start with a low dose, which is gradually increased if needed. The main goal of using the Tapentadol titration method is to find the lowest effective dose that provides pain relief without building tolerance or dependency. 

In clinical practice, titration of a Tapentadol ER dose is done based on the following factors. 

• The severity of the patient’s pain.

• The ability of the patient to tolerate the medication. 

• The amount of supplemental opioid utilization.

The titration of the Tapentadol dose provides a significant improvement in pain with acceptable tolerability. Clinical studies show that a titration regimen with a gradual increase of 50 mg of Nucynta ER twice daily every three days is effective in pain management [12]. 

The basic rule for Tapentadol Titration is to start with the lowest effective dose or the standard recommended, which in this case is 100 mg. Following the administration, assess the pain relief and note if you experience any possible side effects from the medication. 

If you do not achieve the desired result, your doctor may increase the dose gradually, which is done every 3 days, allowing enough time to evaluate the effect of the drug. 

 

Tapentadol Dose Conversion

Some factors that are responsible for people switching from other analgesics to Tapentadol are listed below. 

• Experiencing Side effects that are difficult to manage. 

• Poor response to current medication. 

• Development of tolerance.

Conversion Of Tapentadol IR To Tapentadol ER

People converting from Tapentadol IR to ER can take the same total daily dose divided into two equal parts with 12 hours of dosage gap. 

For example, a person taking Tapentadol 100 mg four times a day (400 mg) can take 200 mg of Tapentadol ER twice daily. 

Conversion From Other Opioids

To date, there is no clinically established conversion rate from other opioid analgesics to Tapentadol. So, it is advised to start with the lowest dose of the medication, which is 50 mg every 12 hours. 

Frequent titration is advised until you find the right dose for effective pain management.

It is important to monitor the patient for symptoms of opioid withdrawal. 

 

Potential Risks Of Overdosing On Tapentadol And How To Recognize And Manage 

Taking Tapentadol IR over 600 mg and ER over 500 mg in a day can result in overdosing. Between July 2016 and September 2017, about 30% of people taking Tapentadol experienced overdosing [13]. 

A few signs of Tapentadol overdosing that can help in recognizing it at the right time are listed below.

• Respiratory Depression

• Low blood pressure 

• Cardiac Arrest 

• Shallow breathing 

• Constricted pupils

• Pulmonary edema

• Muscle stiffness 

• Bradycardia or extremely slow heart rate. 

Tapentadol Overdose Treatment 

The treatment options for Tapentadol overdose can vary depending on its severity. People experiencing respiratory depression are often given the following treatment options-

• Use of a breathing tube to keep the airway open. It also prevents the build-up of carbon dioxide in the body. 

• The use of a medication called Naloxone can also act as an antidepressant to counteract respiratory depression. It is also prescribed by physicians to regulate heart rate. 

• Using activated charcoal to empty the stomach of such patients and lower the absorption rate of the medication. 

•  Rehabilitation facilities can also help such addicts become sober and manage withdrawal symptoms effectively [13]. 

 

The Recommended Duration Of Tapentadol Treatment For Acute And Chronic Pain

The long-term use of Tapentadol is not recommended as it may increase the potency of causing addiction and overdose. Thus, being a great threat to the person’s well-being. In most cases, the continuous use of Tapentadol over three continuous weeks is not recommended. 

However, there are a few case studies that do suggest that when Tapentadol is taken correctly for a long period, there are no signs of dependency or side effects. 

A study published in 2021 evaluating the Long-Term Effectiveness and Tolerability of Tapentadol Prolonged Release suggests that effective pain relief and quality of life were reported for upto 72 weeks of treatment with stable dosing in patients with severe chronic osteoarthritis and low back pain [14]. 

A similar study in the Journal of Pain Research indicates that the use of Tapentadol Prolonged Release for long-term treatment of Pain in Children for up to 1 year showed no decline in its potency or signs of adverse effects [15]. 

It is, therefore, best to consult a doctor to determine the correct duration of treatment that is required based on your medical condition. As in most cases, the treatment length is individualized, and it varies from person to person. 

 

Long-Term Side Effects Of Tapentadol

Apart from overdose symptoms and dependency, the long-term side effects of Tapentadol may also include the following symptoms-

• Impaired gastric emptying.

• Pain in the bones

• Cough

• Blurry vision

• Dry mouth

• Coordination imbalance

• Memory impairment 

 

Tapentadol Tapering And Discontinuation

It is not advised to abruptly discontinue the intake of tapentadol, especially in people who have developed a dependency on the analgesic. Factors that should be taken into consideration while deciding how to discontinue or decrease the therapy includes-

• The dose of the Tapentadol medication. 

• Duration of the treatment. 

• Type of pain. 

• The physical and psychological

• attributes of the patient [16].

A multimodal approach to pain management should also be considered before initiating tapering, as the patient may require support to manage an increase in pain during tapering. 

Guidelines For Gradual Dosage Reduction

There is no standard tapering schedule available that is suitable for all patients. Thus each patient requires an individualized plan. The Tapentadol Tapering method is often done by tapering 10 to 25 percent of the dose every 2 to 4 weeks [16]. 

A proposed algorithm for tapering Tapentadol 200 mg from the Current Medical Research and Opinion Journal is mentioned below that can be further tailored based on the individual patients [17]. 

 

If the patient experiences an increase in body pain or severe withdrawal symptoms, they may have to go back to their previous dose until the condition is stabilized before proceeding

with a more gradual taper [16]. 

 

Tapentadol Discontinuation Challenges And Risk Factors

One of the major Tapentadol discontinuation challenges that patients and physicians, after long-term use, come across is withdrawal symptoms. 

The withdrawal symptoms of Tapentadol may vary from one person to another. Several factors, such as the metabolism, age, and functioning of the organ, may affect how your body reacts to the medication and its discontinuation. 

Some of the common symptoms of Tapentadol withdrawal include-

• Sweating

• Anxiety

• Nausea

• Diarrhea

• Vomiting

• Cravings

Managing Withdrawal Symptoms of Tapentadol

Some proven ways to manage Tapentadol withdrawal symptoms in people are listed below. It is best for such people to consult a doctor for a more individualized treatment option. 

• Medically assisted detoxification program- It gives patients with Tapentadol addiction access to medical professionals who help in cleansing the medication out of their system effectively. 

• Introducing mind-body therapies into your regime, such as meditation, yoga, and relaxation, can be useful for people going through opioid withdrawal.

• The use of medications such as Clonidine and Methadone can be effective. 

• Often, dehydration is seen in people with Tapentadol withdrawal. Thus, staying hydrated is recommended. 

 

Our Final Thoughts On Tapentadol Dosage And Treatment 

To sum up all the Tapentadol details, we can say that- 

• The recommended standard Tapentadol dosage is 100 mg, which can be taken three to four times daily with a dosage gap of 4 to 6 hours.   

• The maximum Tapentadol dose is 600 mg for the Immediate-Release formulation and 500 mg for Tapentadol ER. 

• Taking a higher dose can result in overdosage, causing adverse effects. 

• Tapentadol treatment duration is not recommended for long use as it can result in dependency. 

• Sudden discontinuation of Tapentadol treatment can cause withdrawal symptoms. Thus, Tapentadol should be discontinued after consulting a doctor and following a tapering-off method. 

• People who buy Tapentadol 100 mg online should do it only after consulting a doctor to avoid dependency. 

It is important to note that this Tapentadol dosage guideline should not be used for self-medication. It is a Schedule II controlled substance and has a high risk of causing dependency and abuse. We advise all readers to consult a physician before taking Tapentadol as their pain medication.