Tapentadol Hydrochloride in Clinical Practice – To Whom, When, How, and Why?
Thanks to its specific properties, tapentadol hydrochloride ranks among the most effective opioids for managing chronic non-cancer pain. Unlike most opioids, it also exhibits an analgesic effect in neuropathic pain. The following brief overview summarizes its mechanism of action and resulting benefits, reimbursement and prescription conditions, its place in the pain management algorithm, and examples of its application in clinical practice.
Mechanism of Action and Main Benefits
Tapentadol hydrochloride, an innovative atypical opioid and representative of the latest class of opioid analgesics, is indicated for the treatment of chronic non-oncological – primarily neuropathic – pain. It offers a dual mechanism of action – synergy of agonistic activity on the µ‑opioid receptor (MOR; primarily affecting the nociceptive component of pain) and inhibition of norepinephrine reuptake (NRI; effective in mixed and neuropathic pain). The NRI effect can even outweigh the opioid effects in chronic pain conditions, especially neuropathies.
Advantages of tapentadol hydrochloride include that it is not a prodrug, so its efficacy is not dependent on metabolism. Moreover, its metabolism does not require the hepatic cytochrome system, which, together with low plasma protein binding, means a low potential for drug interactions. Due to its lower activity at the MOR, tapentadol hydrochloride also has fewer typical side effects such as constipation, vomiting, or vertigo.
It has proven effective in the therapy of acute and chronic nociceptive and mixed pain (including osteoarthritis or back pain), acute and chronic postoperative and post-traumatic pain, and in previously mentioned neuropathic pain (such as diabetic or postherpetic neuralgia). Due to its favorable safety profile, it can be used as a well-tolerated opioid with minimal risk of dependence and relatively slow development of tolerance, even in cases of gastrointestinal intolerance to opioids or opioid-induced constipation. Tapentadol hydrochloride can be used as a first-line opioid or rescue analgesic medication.
Reimbursement and Prescription
Reimbursement for tapentadol hydrochloride depends critically on the intolerance to an already used opioid. If it is used as a first-line medication, the patient pays a relatively large co-payment. However, if used as a second-line medication in cases of previous opioid intolerance, it is fully covered. As a result of these reimbursement rules, it is typically used as a second choice.
Tapentadol hydrochloride with extended release is reimbursed for the indication of severe chronic non-cancer pain in patients who have had to discontinue strong opioid therapy (oxycodone, fentanyl, buprenorphine, hydromorphone) due to associated side effects.
The range of specializations authorized to prescribe this analgesic includes algology, palliative medicine, traumatology, orthopedics, and traumatology of the locomotor system, neurology, pediatric neurology, rheumatology, pediatric rheumatology, internal medicine, and geriatrics.
Application in Clinical Practice
In the Czech Republic, tapentadol hydrochloride is available in both extended-release and immediate-release (IR) forms, allowing for comprehensive pain therapy solutions.
Typical patients might be an active forty-year-old or a senior experiencing musculoskeletal pain, most commonly in the back or large joints, who have not found relief with non-opioid analgesics. They are transitioned to a combination of tramadol/paracetamol + nonsteroidal anti-inflammatory drugs, and if this proves ineffective, they are moved to strong opioid medication (oxycodone, buprenorphine, or fentanyl). About a third of these patients experience side effects – this is where tapentadol hydrochloride comes in, initially prescribed at the lowest dose of the extended-release form (50 mg twice daily), with possible titration based on efficacy. In practice, it shows a low tendency to develop tolerance, so dosage escalation is often unnecessary. Moreover, its use in seniors is safe considering minimal drug interactions and the common presence of comorbidities. For younger individuals, it causes far less restriction in an active lifestyle.
It also proves very effective in patients with purely neuropathic pain (e.g., diabetic polyneuropathy or postherpetic neuralgia). Initially, these patients are usually treated with a combination of a weak opioid with paracetamol and an anticonvulsant; those who experience side effects from this treatment are subsequently switched to tapentadol hydrochloride. Tapentadol hydrochloride combined with pregabalin appears to be a very effective combination for neuropathic pain.
Tapentadol hydrochloride IR is also effective in cases where oxycodone IR was previously chosen. Some physicians opted to use tapentadol IR during a several-month shortage of oxycodone IR, leading to very satisfactory results. Consequently, tapentadol hydrochloride has secured an indispensable position in opioid medication within clinical practice.
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Sources:
1. Vranová V. Tapentadol Hydrochloride – an Innovative Atypical Opioid with a Unique Mechanism of Action. Remedia 2023; 33: 316–319.
2. Hakl M. Commentary: Tapentadol Hydrochloride from the Perspective of an Algologist. Remedia 2023; 33: 319–320.
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