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      Estado actual de los medicamentos con fentanilo en España Translated title: Current situation of different fentanyl delivery systems in Spain

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          Abstract

          RESUMEN El dolor es una de las principales consultas que se realiza en Atención Primaria, siendo uno de los síntomas más prevalentes en los pacientes con cáncer. Es fundamental su correcto diagnóstico y la elección de un medicamento adecuado a cada tipo de dolor. El fentanilo es un analgésico opioide ampliamente utilizado para el tratamiento del dolor intenso. Está disponible en varias formas farmacéuticas para distintas vías de administración. Las formas farmacéuticas de liberación inmediata se usan para el tratamiento del dolor irruptivo oncológico porque este tipo de dolor es de aparición súbita, intenso y de corta duración, por lo que se requiere un medicamento de inicio rápido y corta acción. Estas formas farmacéuticas son de absorción transmucosa (oral y nasal), ya que esta vía permite una absorción rápida del fármaco y una elevada biodisponibilidad. Las formas farmacéuticas con las que se puede conseguir este rápido efecto son: comprimidos para chupar con aplicador bucal integrado, comprimidos bucales y sublinguales, películas bucales y preparados intranasales. Hay que resaltar, que estos medicamentos, aunque contienen el mismo principio activo, presentan diferencias en sus perfiles farmacocinéticos, por lo que no son intercambiables. Por otro lado, las formas de liberación controlada de fentanilo comercializadas actualmente son los parches transdérmicos. Estos se usan para el tratamiento del dolor crónico o basal ya que permiten mantener niveles plasmáticos constantes del fármaco.

          Translated abstract

          SUMMARY Pain is one of the main consultations carried out in Primary Care, being one of the most prevalent symptoms in cancer patients. Its correct diagnosis and the choice of a suitable medication for each type of pain are essential. Fentanyl is an opioid analgesic widely used for the treatment of severe pain. It is available in various pharmaceutical forms for different routes of administration. Pharmaceutical forms of immediate release are used for the treatment of breakthrough cancer pain because this type of pain is sudden, intense and short-lived, so a quick-onset drug with short action is required. These pharmaceutical forms are transmucosal absorption (oral and nasal), since this route allows rapid absorption of the drug and high bioavailability. The pharmaceutical forms that achieve this rapid effect are: sucking tablets with integrated oral applicator, oral and sublingual tablets, oral films and intranasal preparations. It should be noted that these medications, although they contain the same active substance, have differences in their pharmacokinetic profiles, so they are not interchangeable. The forms of controlled release currently marketed are transdermal patches. These are used for the treatment of chronic or basal pain since they allow maintaining constant plasma levels of the drug.

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          Most cited references51

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          Breakthrough pain: definition, prevalence and characteristics.

          In the cancer population, the term breakthrough pain typically refers to a transitory flare of pain in the setting of chronic pain managed with opioid drugs. The prevalence and characteristics of this phenomenon have not been defined, and its impact on patient care is unknown. We developed operational definitions for breakthrough pain and its major characteristics, and applied these in a prospective survey of patients with cancer pain. Data were collected during a 3 month period from consecutive patients who reported moderate pain or less for more than 12 h daily and stable opioid dosing for a minimum of 2 consecutive days. Of 63 patients surveyed, 41 (64%) reported breakthrough pain, transient flares of severe or excruciating pain. Fifty-one different pains were described (median 4 pains/day; range 1-3600). Pain characteristics were extremely varied. Twenty-two (43%) pains were paroxysmal in onset; the remainder were more gradual. The duration varied from seconds to hours (median/range: 30 min/1-240 min), and 21 (41%) were both paroxysmal and brief (lancinating pain). Fifteen (29%) of the pains were related to the fixed opioid dose, occurring solely at the end of the dosing interval. Twenty-eight (55%) of the pains were precipitated; of these, 22 were caused by an action of the patient (incident pain), and 6 were associated with a non-volitional precipitant, such as flatulence. The pathophysiology of the pain was believed to be somatic in 17 (33%), visceral in 10 (20%), neuropathic in 14 (27%), and mixed in 10 (20%). Pain was related to the tumor in 42 (82%), the effects of therapy in 7 (14%), and neither in 2 (4%). Diverse interventions were employed to manage these pains, with variable efficacy. These data clarify the spectrum of breakthrough pains and indicate their importance in cancer pain management.
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            A Comprehensive Review of Rapid-Onset Opioids for Breakthrough Pain

            Breakthrough pain (BTP) is a transitory pain (reaching maximum severity in ∼15 minutes and lasting ∼60 minutes in patients with cancer) that occurs despite the management of chronic pain with long-term around-the-clock analgesia. BTP occurs in 33–65% of patients with chronic cancer pain and in ∼70% of patients with chronic noncancer pain. BTP has historically been managed with short-acting opioids; however, these medications have a pharmacokinetic profile that does not correlate with the sudden onset and short time to maximum severity of BTP. Interest in rapid-onset opioids to relieve BTP has therefore been growing. This comprehensive review aims to summarize the currently available clinical data for the approved rapid-onset opioids, which comprise different formulations of fentanyl, a μ-opioid receptor agonist with anaesthetic and analgesic properties. Administration routes for fentanyl in the management of BTP currently include the transmucosal and intranasal routes; an intrapulmonary formulation is also in development. The findings of this review suggest that the efficacy and safety of the approved rapid-onset opioids are comparable.
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              Fentanyl Formulations in the Management of Pain: An Update.

              Fentanyl is a synthetic, highly selective opioid with many desirable physicochemical properties, including a high lipophilicity and predictable pharmacokinetics. These properties have an established record in the management of pain in a variety of settings, particularly acute pain and breakthrough cancer pain. Fentanyl was initially developed for parenteral use; however, this is invasive and impractical in the outpatient setting. Unfortunately, the high first-pass metabolism of fentanyl makes oral formulations unfeasible. However, its high lipophilicity allows fentanyl to be absorbed via a number of other routes. Thus new formulations were designed to allow non-invasive methods of administration. Transmucosal and transdermal fentanyl formulations are well established, and have proven useful in the settings of breakthrough cancer pain, emergencies and in the paediatric population. The iontophoretic transdermal system was developed to provide a needle-free system of delivering bolus doses of fentanyl on demand, a novel way of delivering patient-controlled opioid analgesia. Transpulmonary administration of fentanyl remains experimental. The aim of this review is to provide an update on current non-parenteral fentanyl formulations, with attention to their particular pharmacokinetics and features relevant to clinical use in pain management.
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                Author and article information

                Journal
                ofil
                Revista de la OFIL
                Rev. OFIL·ILAPHAR
                Organización de Farmacéuticos Ibero-Latinoamericanos (Madrid, Madrid, Spain )
                1131-9429
                1699-714X
                2020
                : 30
                : 3
                : 240-250
                Affiliations
                [1] Andalucía orgnameUniversidad de Sevilla orgdiv1Facultad de Farmacia orgdiv2Departamento de Farmacia y Tecnología Farmacéutica Spain
                Article
                S1699-714X2020000300240 S1699-714X(20)03000300240
                10.4321/s1699-714x2020000300015
                b019143e-a345-479c-8eff-baccf419c767

                This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.

                History
                : 10 February 2020
                : 12 February 2020
                Page count
                Figures: 0, Tables: 0, Equations: 0, References: 54, Pages: 11
                Product

                SciELO Spain

                Categories
                Revisión

                Fentanyl,absorción transmucosa,dolor crónico,dolor irruptivo,Fentanilo,delayed release,immediate release,transmucosal absorption,chronic pain,breakthrough pain,liberación controlada,liberación inmediata

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