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      Journal of Pain Research (submit here)

      This international, peer-reviewed Open Access journal by Dove Medical Press focuses on reporting of high-quality laboratory and clinical findings in all fields of pain research and the prevention and management of pain. Sign up for email alerts here.

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      A Randomized, Crossover, Pharmacokinetic and Adhesion Performance Study of a Lidocaine Topical System 1.8% During Physical Activity and Heat Treatment in Healthy Subjects

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          Abstract

          Purpose

          This study compares the pharmacokinetic (PK) profile, adhesion, and safety of lidocaine topical system 1.8%, a novel lidocaine topical system approved to treat postherpetic neuralgia, under conditions of heat and exercise vs normal conditions.

          Materials and Methods

          This open-label, 3-period, 3-treatment crossover study randomized 12 healthy adults to receive three lidocaine topical systems 1.8% during each of three treatment periods, with 7-day washouts between treatments. The product was applied to the mid-lower back and was removed after 12 hours. During Treatment A, subjects exercised on a bicycle for 30 minutes at 0, 2.5, 5.5, and 8.5 hours. During Treatment B, heat (temperature set at 36.7–40.3°C) was applied at 0 and 8.5 hours. Treatment C was normal conditions. The PK profile of each subject under exercise and heat conditions was compared to normal conditions. Skin irritation, adhesion, and adverse events were assessed.

          Results

          Twelve subjects completed the study. Exposure to external heat resulted in increased peak plasma concentration of lidocaine with a mean C max of 160.3±100.1 ng/mL vs 97.6±36.9 ng/mL under normal conditions, with no effect on the extent of exposure (AUC). Concentrations returned to normal within 4 hours after the heat was removed. No clinically relevant differences in absorption were observed under exercise conditions with a mean C max of 90.5±25.4 ng/mL and no effect on the extent (AUC) of lidocaine exposure was observed relative to normal conditions. No systems detached during the study. Adverse events were mild, with none leading to discontinuation.

          Conclusion

          Transient heat exposure resulted in increased lidocaine plasma concentrations compared to normal conditions, whereas exercise had no effect. The effects of heat appear to be immediate, reversible, and below systemic therapeutic threshold in antiarrhythmic treatment (1000–1500 ng/mL), and well below the safe systemic threshold of 5000 ng/mL. Lidocaine topical system 1.8% remained adhered to the skin and was well tolerated under all conditions. ClinicalTrials.gov: NCT04150536.

          Most cited references10

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          Pharmacotherapy for Neuropathic Pain: A Review

          Abstract Neuropathic pain, comprising a range of heterogeneous conditions, is often severe and difficult to manage, and this may result in a chronic condition that negatively affects the overall functioning and quality of life in patients. The pharmacotherapy of neuropathic pain is challenging and for many patients effective treatment is lacking; therefore, evidence-based recommendations are essential. Currently, there is general agreement on which drugs are appropriate for the first-line treatment of neuropathic pain, whereas debate continues regarding second- and third-line treatments. First-line drugs for neuropathic pain include antidepressants (tricyclic antidepressants and serotonin–noradrenaline reuptake inhibitors) and anticonvulsants acting at calcium channels (pregabalin and gabapentin). Second- and third-line drugs for neuropathic pain include topical lidocaine and opioids. Although efficacious in the treatment of neuropathic pain, opioids are not considered to be a first choice because of adverse drug reactions and, more recently, because of concerns about abuse, diversion, and addiction. A clear understanding of the mechanism of action of currently available drugs is an essential step towards an effective clinical approach that aims to tailor therapies both to the specific neuropathic disease and to the needs of an individual patient. This review provides an overview of current drugs available for the treatment of neuropathic pain with an emphasis on their mechanism of action. Funding Pfizer, Italy.
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            Post-herpetic Neuralgia: a Review.

            Post-herpetic neuralgia (PHN) is a chronic neuropathic pain condition that persists 3 months or more following an outbreak of shingles. Shingles, also known as acute herpes zoster, is associated with the reactivation of the dormant varicella zoster virus in an individual who has experienced chicken pox. PHN is associated with persistent and often refractory neuropathic pain. Patients may experience multiple types of pain including a constant deep, aching, or burning pain; a paroxysmal, lancinating pain; hyperalgesia (painful stimuli are more painful than expected); and allodynia (pain associated with typically non-painful stimuli). The pharmacological treatment of PHN may include a variety of medications including alpha-2 delta ligands (gabapentin and pregabalin), other anticonvulsants (carbamazepine), tricyclic antidepressants (amitriptyline, nortriptyline, doxepin), topical analgesics (5 % lidocaine patch, capsaicin) tramadol, or other opioids. The considerable side effect profiles of the commonly used oral medications often limit their practical use, and a combination of both topical and systemic agents may be required for optimal outcomes. Physicians and other treatment providers must tailor treatment based on the response of individual patients.
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              Practical considerations in the pharmacological treatment of postherpetic neuralgia for the primary care provider

              An estimated one million individuals in the US are diagnosed with herpes zoster (HZ; shingles) each year. Approximately 20% of these patients will develop postherpetic neuralgia (PHN), a complex HZ complication characterized by neuropathic pain isolated to the dermatome that was affected by the HZ virus. PHN is debilitating, altering physical function and quality of life, and commonly affects vulnerable populations, including the elderly and the immunocompromised. Despite the availability of an immunization for HZ prevention and several approved HZ treatments, the incidence of PHN is increasing. Furthermore, management of the neuropathic pain associated with PHN is often suboptimal, and the use of available therapeutics may be complicated by adverse effects and complex, burdensome treatment regimens, as well as by patients’ comorbidities and polypharmacy, which may lead to drug–drug interactions. Informed and comprehensive assessments of currently available pharmacological treatment options to achieve effective pain control in the primary care setting are needed. In this article, we discuss the situation in clinical practice, review currently recommended prevention and treatment options for PHN, and outline practical considerations for the management of this neuropathic pain syndrome, with a focus on optimal, individual-based treatment plans for use in the primary care setting.
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                Author and article information

                Journal
                J Pain Res
                J Pain Res
                JPR
                jpainres
                Journal of Pain Research
                Dove
                1178-7090
                10 June 2020
                2020
                : 13
                : 1359-1367
                Affiliations
                [1 ]Samuel Stratton Department of Veterans Affairs Medical Center , Albany, NY, USA
                [2 ]Albany College of Pharmacy & Health Sciences , Albany, NY, USA
                [3 ]Western New England University College of Pharmacy , Springfield, MA, USA
                [4 ]Remitigate, LLC , Delmar, NY, USA
                [5 ]Scilex Pharmaceuticals Inc ., Mountain View, CA, USA
                [6 ]Mid America PolyClinic , Overland Park, KS, USA
                Author notes
                Correspondence: Jeffrey Fudin Remitigate, LLC , Delmar, NY12054, USATel +1 518-772-4100Fax +1 518-734-0288 Email jeff@paindr.com
                Author information
                http://orcid.org/0000-0001-9929-1909
                http://orcid.org/0000-0001-6450-1988
                Article
                238268
                10.2147/JPR.S238268
                7293912
                60b5942b-db81-4c3e-8e2e-b539408cfdc1
                © 2020 Fudin et al.

                This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                History
                : 21 November 2019
                : 07 May 2020
                Page count
                Figures: 1, Tables: 5, References: 18, Pages: 9
                Funding
                The project supported by Shandong Key Research and development Program (Grant No. 2018GSF118110).
                Categories
                Original Research

                Anesthesiology & Pain management
                herpes zoster,shingles,neuropathic pain,dermal
                Anesthesiology & Pain management
                herpes zoster, shingles, neuropathic pain, dermal

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