Clinical value of tapentadol extended-release in painful diabetic peripheral neuropathy

Desai, B. L. M.; Freeman, Erin; Huang, Ellen; Hung, Anna; Knapp, E; Breunig, Ian M.; McPherson, Mary Lynn; Shaya, Fadia T.

doi:10.1586/17512433.2014.889562

Cited by 13 publications

(8 citation statements)

References 33 publications

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“…The treatment for painful diabetic peripheral neuropathy includes glycemic control and symptomatic pain management. Food and Drug Administration has approved only duloxetine, pregabalin and tapentadol for the treatment of painful diabetic neuropathy, but they have low efficacy and are able to cause serious side effects [3, 4]. The lack of an adequate pharmacological treatment supports the need to clarify better the diabetes-associated painful peripheral neuropathy pathogenesis to relieve this complication.…”

Section: Introductionmentioning

confidence: 99%

Possible involvement of peripheral TRP channels in the hydrogen sulfide-induced hyperalgesia in diabetic rats

et al. 2019

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BackgroundPeripheral diabetic neuropathy can be painful and its symptoms include hyperalgesia, allodynia and spontaneous pain. Hydrogen sulfide (H2S) is involved in diabetes-induced hyperalgesia and allodynia. However, the molecular target through which H2S induces hyperalgesia in diabetic animals is unclear. The aim of this study was to determine the possible involvement of transient receptor potential (TRP) channels in H2S-induced hyperalgesia in diabetic rats.ResultsStreptozotocin (STZ) injection produced hyperglycemia in rats. Intraplantar injection of NaHS (an exogenous donor of H2S, 3–100 µg/paw) induced hyperalgesia, in a time-dependent manner, in formalin-treated diabetic rats. NaHS-induced hyperalgesia was partially prevented by local intraplantar injection of capsazepine (0.3–3 µg/paw), HC-030031 (100–316 µg/paw) and SKF-96365 (10–30 µg/paw) blockers, at 21 days post-STZ injection. At the doses used, these blockers did not modify formalin-induced nociception. Moreover, capsazepine (0.3–30 µg/paw), HC-030031 (100–1000 µg/paw) and SKF-96365 (10–100 µg/paw) reduced formalin-induced nociception in diabetic rats. Contralateral injection of the highest doses used did not modify formalin-induced flinching behavior. Hyperglycemia, at 21 days, also increased protein expression of cystathionine-β-synthase enzyme (CBS) and TRPC6, but not TRPA1 nor TRPV1, channels in dorsal root ganglia (DRG). Repeated injection of NaHS enhanced CBS and TRPC6 expression, but hydroxylamine (HA) prevented the STZ-induced increase of CBS protein. In addition, daily administration of SKF-96365 diminished TRPC6 protein expression, whereas NaHS partially prevented the decrease of SKF-96365-induced TRPC6 expression. Concordantly, daily intraplantar injection of NaHS enhanced, and HA prevented STZ-induced intraepidermal fiber loss, respectively. CBS was expressed in small- and medium-sized cells of DRG and co-localized with TRPV1, TRPA1 and TRPC6 in IB4-positive neurons.ConclusionsOur data suggest that H2S leads to hyperalgesia in diabetic rats through activation of TRPV1, TRPA1 and TRPC channels and, subsequent intraepidermal fibers loss. CBS enzyme inhibitors or TRP-channel blockers could be useful for treatment of painful diabetic neuropathy.Electronic supplementary materialThe online version of this article (10.1186/s12868-018-0483-3) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

Possible involvement of peripheral TRP channels in the hydrogen sulfide-induced hyperalgesia in diabetic rats

et al. 2019

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“…The FDA approved the use of tapentadol for the treatment of diabetic neuropathic pain in 2012 due to its proved efficacy when compared to placebo. However, we still lack evidence of clinical relevance comparing tapentadol with first-line drugs, such as pregabalin, duloxetine, and tricyclic antidepressants 22,23 . Another use of tapentadol would be in acute pain after an outpatient surgical procedure.…”

Section: Contentsmentioning

confidence: 99%

Tapentadol: what every doctor needs to know about this new drug

Mosele¹,

Almeida²,

Hess³

2018

Brazilian Journal of Pain

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BACKGROUND AND OBJECTIVES:Acute and chronic pain is a major problem with repercussion in our society, causing impairment in the quality of life of patients as well as socioeconomic losses, due to work absenteeism. This review aims to analyze the use of tapentadol, an analgesic not yet available in Brazil, with a dual mechanism of action, in the treatment of acute and chronic pain syndromes. CONTENTS: A review about this new drug was made on the Pubmed database using the keywords "tapentadol" and "opioids," evaluating its pharmacological and clinical aspects comparing with other current drugs in pain treatment, as well as its indications and contraindications in the management of patients with pain disorders. CONCLUSION: Tapentadol has been shown to be effective in the treatment of acute and chronic pain, with potency equivalent to the opioids currently used. In addition, it developed less tolerance, less adverse effects and better therapeutic response in chronic neuropathic pain when compared to pure μ-opioid receptors agonists. Keywords: Dual mechanism of action, Opioids, Tapentadol. RESUMO JUSTIFICATIVA E OBJETIVOS:A dor aguda e crônica consiste em um problema de grande repercussão em qualquer sociedade atual, causando degradação na qualidade de vida dos próprios pacientes e comprometimento socioeconômico pelo absenteísmo laboral. O objetivo deste estudo foi analisar o uso do tapentadol, um analgésico ainda não disponível no Brasil e com duplo mecanismo de ação, no tratamento das síndromes dolorosas agudas e crônicas. Tapentadol: what every doctor needs to know about this new drug CONTEÚDO:Foi realizada uma pesquisa na base de dados Pubmed utilizando os descritores "tapentadol" e "opioides" para revisão da literatura mundial sobre esse novo fármaco, avaliando as características farmacológicas e aspectos clínicos do seu uso na realidade atual, em comparação com os fármacos já existentes no mercado, assim como suas indicações e contraindicações no manuseio do paciente com dor. CONCLUSÃO: O tapentadol se mostrou eficaz no tratamento de dores agudas e crônicas, com potência equiparável aos opioides já comercializados. Além disso, desenvolveu menos tolerân-cia, menos efeitos adversos e melhor resposta terapêutica na dor crônica neuropática quando comparado com agonistas receptores opioides tipo μ puros. Descritores: Duplo mecanismo de ação, Opioides, Tapentadol. INTRODUCTIONPain is a problem of great proportion, involving 20 to 25% of the population with an increasing incidence. Despite the extraordinary advances in anatomy, physiology, diagnosis and pain management, more than 50% of patients report improper relief. This can be related to the neuroplasticity process of the pain pathways 1 , creating a persistent "memory" of the aggressive event and neuronal hiperexcitability 2,3 . Understanding chronic pain neurobiology is fundamental to target the treatment. Thus, the use of drugs that act on more than one pathophysiologic mechanism, as tapentadol, can be a new weapon in the therapeutic armamentarium aga...

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“…Interestingly, the rates of constipation with maintenance therapy were reportedly the same. No study has evaluated the effect of tapentadol on neuropathic cancer-related pain [64].…”

Section: Is Tapentadol the Opioid Of Choice For The Elderly Or Frail mentioning

confidence: 99%

“…Studies have demonstrated the superiority of tapentadol over placebo, but no active comparators were included [64]. Patients included in these trials were opioid non-responders [64].…”

Section: Is Tapentadol the Opioid Of Choice For The Elderly Or Frail mentioning

confidence: 99%

“…Clinical trials often excluded people taking SNRIs, TCAs, or monoamine oxidase inhibitors. In addition, trials excluded large patient groups, including those with previous stroke, transient ischemic attack, uncontrolled hypertension, other significant disease or cancer within the previous 2 years [64]; thus interactions with disease states or drugs associated with these conditions may not have been detected and could still occur. The product information advises that tapentadol is contraindicated in severe hepatic or renal impairment [52], with glucuronidation and subsequent renal excretion of the conjugate being the major route of elimination.…”

Section: Is Tapentadol the Opioid Of Choice For The Elderly Or Frail mentioning

confidence: 99%

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Pain in the Frail or Elderly Patient: Does Tapentadol Have a Role?

Veal

Peterson

2015

Drugs Aging

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Persistent pain affects the elderly disproportionally, occurring in 50% of elderly community-dwelling patients and 80% of aged care residents. The management of pain in the elderly and frail patient is complicated because of the risks posed by changes in pharmacokinetics and pharmacodynamics, polypharmacy, and drug-disease interactions. Trials evaluating the efficacy of analgesics have often excluded elderly patients and universally excluded frail patients; therefore, the true efficacy and side-effect profiles in these population groups are largely unknown, especially for long-term use. A stepwise approach is recommended to managing pain, commencing with paracetamol and adding on opioids when needed to manage pain. However, because of the short duration of clinical trials, exclusion of frail patients, and minimal inclusion of elderly patients, the decision as to which opioid should be added on to paracetamol is a difficult one. This article reviews the evidence surrounding a newer opioid, tapentadol. Tapentadol acts on both the mu receptors and on neuronal reuptake of noradrenaline, and has no significant analgesically active metabolites, which theoretically presents some advantages, particularly in comparison with tramadol. However, the evidence to support tapentadol is weak and the trials were often methodologically poor and sponsored almost universally by the drug company. Currently, there is insufficient evidence to support the use of tapentadol over other opioids, which have been on the market longer, are less expensive, and have better established safety profiles. As a first-line agent after the failure of paracetamol alone, morphine, oxycodone, fentanyl, or buprenorphine are still the preferred evidence-based choices for add-on opioid therapy for elderly or frail patients.

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Clinical value of tapentadol extended-release in painful diabetic peripheral neuropathy

Cited by 13 publications

References 33 publications

Possible involvement of peripheral TRP channels in the hydrogen sulfide-induced hyperalgesia in diabetic rats

Possible involvement of peripheral TRP channels in the hydrogen sulfide-induced hyperalgesia in diabetic rats

Tapentadol: what every doctor needs to know about this new drug

Pain in the Frail or Elderly Patient: Does Tapentadol Have a Role?

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