Tapentadol is a medicine used for treating severe pain. It will only be given if your doctor considers that other non-opioid painkillers are ineffective or that you are not able to tolerate them. Tapentadol is not commonly prescribed for the management of chronic (long-term) pain. People who are using tapentadol are experiencing sleepiness as a side effect. In this article, we will explore the reasons why Tapentadol users are experiencing drowsiness and give insights into its pharmacological effects.

Overview and mechanism of action of tapentadol:

Tapentadol is a synthetic painkiller that acts centrally and has a dual mechanism of action. It is an agonist of the mu-opioid receptor which additionally inhibits norepinephrine reuptake. Tapentadol stands apart from traditional opioids by inhibiting the reuptake of norepinephrine. Norepinephrine is a neurotransmitter involved in the body’s stress response and the regulation of wakefulness and alertness. Tapentadol was approved by the FDA for the first time in 2008. Later in 2011, the FDA also approved extended-release tablets of tapentadol. Tapentadol is used to treat acute pain that is sufficiently severe for the use of an opioid painkiller and for which other therapies are ineffective. Tapentadol is intended for individuals who have no other treatment alternatives due to potential risks of addiction, drug abuse, and drug misuse.

Tapentadol extended-release tablets are intended for the treatment of pain severe enough to necessitate daily, around-the-clock pain relievers and for which alternate treatment options are unsatisfactory. They are also suggested for the treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPN) in people who require daily, around-the-clock, long-term opioid medication and for whom alternate treatment alternatives are insufficient.

Reasons behind tapentadol to cause Sleepiness:

Due to some specific reasons, tapentadol users feel sleepiness and the reasons are as follows.

The effect of sleepiness:

The dual mechanism of action of tapentadol, especially the inhibition of norepinephrine reuptake causes sleepiness in tapentadol users. Because Tapentadol increases the availability of norepinephrine in the synaptic cleft by blocking norepinephrine reuptake. The increased levels of norepinephrine which are known for alertness, can paradoxically cause drowsiness in some people.

Individual Differences:

It is essential to understand that not everyone who takes Tapentadol will experience the same level of drowsiness. Individual differences will influence how the body responds to drugs. The severity of side effects can be influenced by some other factors such as overall health, drug tolerance, and the drug dose.

Tapentadol Dose:

The dose of tapentadol suggested by your physician is an important factor in managing adverse effects like sleepiness. To get the best pain relief while minimizing side effects, healthcare experts frequently start treatment with a lower dose and gradually increase it. Adjusting the dosage may help in achieving a balance between pain relief and the side effects including sleepiness.

Other Things to Think About:

Tapentadol, like any medicine, may have other side effects in addition to drowsiness. Nausea, constipation, dizziness, and headache are some of the most commonly seen adverse effects. To manage these side effects, doctors should adjust the treatment plan to according individual needs and conditions.

Potential Adverse Effects of Tapentadol other than Sleepiness:

Tapentadol, while useful in pain management, can cause the following adverse effects:

Vomiting and nausea:

Some people may experience nausea or vomiting, especially when taken Tapentadol for the first time. These symptoms can be addressed by taking the medicine with food or as instructed by your doctor.


Constipation is a typical adverse effect of several opioid medicines. Having enough hydration, including dietary fiber, and engaging in regular physical activity will all help to manage this condition.

Lightheadedness and dizziness:

Tapentadol might make you dizzy and lightheaded, especially when you change positions. Precautions such as gently moving from a seat or sleeping position may assist in reducing these consequences.


There is a chance for dependency because Tapentadol is an opioid. So it is essential to adhere to prescribed doses and talk freely with your healthcare practitioner about any concerns or changes in your reactions to the medicine.

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