What a Decade of Experience with Tapentadol Hydrochloride in Pain Treatment Has Shown
In an interview with Dr. Marek Hakl, Ph.D., from the Brno Pain Treatment Center, we focus on the role of tapentadol hydrochloride in the treatment of chronic pain. We discuss, among other things, its suitability for specific patients and the latest findings that confirm its excellent efficacy and fewer side effects compared to other opioids.
For what types of pain is tapentadol hydrochloride intended?
Primarily for the treatment of acute and chronic non-oncological pain of any origin. Besides nociceptive pain, it also has a very good effect on neuropathic pain. Compared to other opioids, it stands out primarily because of its very low incidence of side effects, not only in oral but also in transdermal forms of opioids.
How does this relate to the mechanism of action of the drug?
Tapentadol exhibits a dual mechanism of action, making it an atypical opioid. It acts as a conventional opioid on µ-opioid receptors, which is responsible for its very good analgesic effect on nociceptive pain. Additionally, it affects the reuptake of norepinephrine at nerve endings, accounting for its effect on neuropathic pain. Together, these two mechanisms give tapentadol its unique analgesic properties.
Can you specify the patients who will benefit from this drug?
Primarily, these are patients who do not tolerate other opioids. Tapentadol shows very good tolerability. Additionally, it is beneficial for patients with neuropathic pain due to its dual mechanism of action. Another advantage is that it is not metabolized in the liver via the cytochrome P450 pathway, thus avoiding negative impacts on liver function and competition for this cytochrome with other drugs.
From which clinical studies do the efficacy and safety data derive?
Many studies have been conducted, some even in the Czech Republic, in which I had the opportunity to participate. The effect of tapentadol hydrochloride was confirmed in multicentric randomized studies. The results were unequivocal, demonstrating very good efficacy and a low incidence of side effects. Among the international studies, we can cite works published by Chang et al. (2016), Christoph et al. (2010), or Überall et al. (2022).
What is the conclusion from laboratory research conducted in the Czech Republic?
Experiments were conducted on rats, which were thermally or mechanically stimulated. The outcome demonstrated an analgesic effect after administering tapentadol in both types of stimulations. In this regard, tapentadol hydrochloride appears to be the most effective opioid.
What are the side effects of the drug?
Tapentadol hydrochloride generally exhibits a very low incidence of side effects. If encountered, they are similar to other opioid medications – most commonly nausea, vomiting, vertigo, or constipation. However, unlike other opioids, their occurrence is minimal.
Does tapentadol hydrochloride have the potential to cause addiction?
As a potent opioid, it can indeed lead to dependency. We must account for the possibility of physical dependence, especially at higher doses. To avoid withdrawal syndrome when discontinuing tapentadol, we reduce the dosage gradually until complete cessation. The incidence of psychological dependence, when adhering to all principles of rational opioid prescription, is rare, and I have not personally encountered it with tapentadol.
Which interactions should be considered when prescribing?
Tapentadol hydrochloride should not be used in combination with other opioids; this rule, however, applies to all drugs in this group. In general, it has minimal interactions with other drugs. It is not a prodrug, meaning it does not need to be metabolized into an active compound, and as mentioned, it bypasses the cytochrome P450 system, so it does not compete for metabolism with other drugs at this level and has low plasma protein binding.
What are the experiences with long-term use?
Tapentadol hydrochloride has been on the Czech market for over 10 years, and experiences with its long-term administration are therefore extensive. From my own experience, I can say that it is very well tolerated with long-term use, showing minimal side effects and very little propensity for tolerance development. I have many patients who have been satisfied on the same dose of tapentadol hydrochloride for years without needing to increase or rotate opioids.
How is the drug classified in the recommendations for the treatment of chronic pain?
There is generally no first-line opioid. The initial use of an opioid is guided by personal experience. The downside of tapentadol is its double reimbursement, which limits its use as a first-line opioid. However, it has a clear position as a second-line opioid in cases where other opioids have caused side effects. Here, it proves to be an optimal drug. It also performs well in patients with impaired liver function.
What is the cost of the drug, and how is it reimbursed?
The price is slightly higher compared to other oral opioids, which led to the establishment of a dual reimbursement system. When used as a first-line treatment, there is a co-payment of several hundred crowns. For patients who experienced side effects from another opioid, increased reimbursement is available, making it co-payment free for the patient.
In summary, how does tapentadol hydrochloride affect patients' lives, and when should it not be overlooked in clinical practice?
It is undoubtedly a unique drug. It excels with minimal side effects and efficacy in neuropathic pain. These properties positively reflect in the quality of life of patients who use it. In many cases, it is the only opioid they can tolerate or that is effective for them.
Dr. Andrea Skálová
editor proLékaře.cz
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