Transdermal and Topical Drug Administration in the Treatment of Pain
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molecules Review Transdermal and Topical Drug Administration in the Treatment of Pain Wojciech Leppert 1,*, Malgorzata Malec–Milewska 2, Renata Zajaczkowska 3,4 and Jerzy Wordliczek 3,4 1 Department of Palliative Medicine, Poznan University of Medical Sciences, Osiedle Rusa 55, 61–645 Poznan, Poland 2 Department of Anesthesiology and Intensive Care, Medical Centre of Postgraduate Education, 01-813 Warsaw, Poland; [email protected] 3 Department of Interdisciplinary Intensive Care, Jagiellonian University Medical College, 31-008 Krakow, Poland; [email protected] (R.Z.); [email protected] (J.W.) 4 Department of Anesthesiology and Intensive Therapy, University Hospital, 31-501 Krakow, Poland * Correspondence: [email protected]; Tel.: +48-61-8738-303 Academic Editor: Silvia Schenone Received: 30 January 2018; Accepted: 13 March 2018; Published: 17 March 2018 Abstract: The comprehensive treatment of pain is multidimodal, with pharmacotherapy playing a key role. An effective therapy for pain depends on the intensity and type of pain, the patients’ age, comorbidities, and appropriate choice of analgesic, its dose and route of administration. This review is aimed at presenting current knowledge on analgesics administered by transdermal and topical routes for physicians, nurses, pharmacists, and other health care professionals dealing with patients suffering from pain. Analgesics administered transdermally or topically act through different mechanisms. Opioids administered transdermally are absorbed into vessels located in subcutaneous tissue and, subsequently, are conveyed in the blood to opioid receptors localized in the central and peripheral nervous system. Non–steroidal anti–inflammatory drugs (NSAIDs) applied topically render analgesia mainly through a high concentration in the structures of the joint and a provision of local anti–inflammatory effects. Topically administered drugs such as lidocaine and capsaicin in patches, capsaicin in cream, EMLA cream, and creams containing antidepressants (i.e., doxepin, amitriptyline) act mainly locally in tissues through receptors and/or ion channels. Transdermal and topical routes offer some advantages over systemic analgesic administration. Analgesics administered topically have a much better profile for adverse effects as they relieve local pain with minimal systemic effects. The transdermal route apart from the above-mentioned advantages and provision of long period of analgesia may be more convenient, especially for patients who are unable to take drugs orally. Topically and transdermally administered opioids are characterised by a lower risk of addiction compared to oral and parenteral routes. Keywords: adverse effects; analgesics; pain; topical drugs; transdermal opioids 1. Introduction Pain is defined as a subjective phenomenon that is associated with actual or potential damage to tissues. Typically, two components are found: sensory, associated with information of noxious stimuli, and emotional, which is associated with a patient reaction to painful stimuli that is often associated with psychological reactions and an individual sensitivity to pain. There are distinct types of pain regarding its time frame and pathophysiology. With respect to the former, pain may be divided into acute, which typically lasts up to three months, and chronic, which is present for a longer period of time. 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Transdermal through receptors and topical and/or route ions channelsof opioid (Figureadministration2). Transdermal are also andassociated topical routeswith a oflower opioid risk administration of addiction compar are alsoed associated to oral and with parenteral a lower riskroutes of addictionof opioid analgesics compared toadministration. oral and parenteral routes of opioid analgesics administration. Figure 1. Transdermal applicationapplication forfor systemicallysystemically