lunes, 16 de enero de 2017

Más de opioides / More on opioids

Enero 14, 2017. No. 2569

Oxicodona DETERx®: una nueva opción de analgésico de liberación prolongada para el tratamiento de pacientes con dolor crónico.
Oxycodone DETERx®: A Novel Abuse-Deterrent, Extended-Release Analgesic Option for the Treatment of Patients with Chronic Pain.
Pain Ther. 2016 Dec;5(2):171-186. Epub 2016 Nov 21.
BACKGROUND: Extended-release (ER) opioid analgesics are commonly used to provide safe and effective pain relief to treat pain severe enough to require around-the-clock, long-term dosing. These ER opioid formulations usually contain more drug per dosage unit than immediate-release (IR) agents, and therefore bring with them challenges related to both opioid abuse and misuse, often through manipulation of the dosage form. Oxycodone DETERx® (Xtampza® ER, Collegium Pharmaceutical, Inc.) is a novel abuse-deterrent, ER formulation developed to deter common methods of manipulation. In addition to having abuse-deterrent properties, oxycodone DETERx was developed to provide alternative modes of administration for patients with chronic pain and difficulty swallowing. SCOPE: Using published articles, abstracts, and prescribing information, data supporting the use of oxycodone DETERx are reviewed. FINDINGS: Oxycodone DETERx was effective at reducing chronic pain in patients enrolled in a pivotal clinical trial, and had a tolerability profile expected of opioids. In addition to administration of the intact capsule, oxycodone DETERx can also be administered by sprinkling directly into the mouth from a dosing cup, onto soft foods, or through nasogastric or gastrostomy tubes, thus providing flexible dosing options for patients who have difficulty swallowing. In vitro studies demonstrated the reduced ability of oxycodone DETERx to be manipulated by common techniques used by abusers to defeat the ER characteristics or prepare the formulation for injection. Pharmacokinetic studies demonstrated that the ER characteristics of oxycodone DETERx are maintained if chewed or crushed. As a result, oxycodone DETERx is currently the only ER-formulated opioid without a boxed warning against crushing or chewing. Human abuse-potential studies conducted in a population of recreational opioid users demonstrated lower drug-liking scores for oxycodone DETERx administered intranasally and orally when compared with IR oxycodone.
KEYWORDS: Abuse deterrence; Chronic pain; Drug abuse; Extended-release opioids; Opioid analgesics; Oxycodone
 ¿Es el tapentadol diferente a los opioides clásicos? Revisión de la evidencia
Is tapentadol different from classical opioids? A review of the evidence.
Br J Pain. 2016 Nov;10(4):217-221. Epub 2016 Jul 25.
Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain. The clinical studies and subsequent practice experience and surveillance support the concept of opioid and non-opioid mechanisms of action. The reduced incidence of some of the typical opioid-induced side effects, compared to equianalgesic doses of classical opioids, supports the hypothesis that tapentadol analgesia is only partially mediated by opioid agonist mechanisms. Both the pre-clinical and clinical profiles appear to be differentiated from those of classical opioids.
KEYWORDS: Tapentadol; analgesic mechanisms of action; analgesics; opioids; pain pharmacology

Papel de los opioides en el manejo de los ancianos con dolor
The Role of Opioid Analgesics in Geriatric Pain Management.
Clin Geriatr Med. 2016 Nov;32(4):725-735. doi: 10.1016/j.cger.2016.06.006. Epub 2016 Aug 9.
When possible, chronic noncancer pain (CNCP) in older adults should be managed by nonpharmacologic modalities in conjunction with nonopioid analgesics. If moderate-to-severe pain persists despite these approaches, however, nonparenteral opioids may be considered as adjunctive therapy. This article reviews the epidemiology of opioid use and their effectiveness for CNCP in older adults and summarizes important age-related changes in opioid pharmacokinetics and pharmacodynamics that increase the risks of adverse effects in the elderly. Finally, to assist clinicians with selecting appropriate therapy, the article concludes with an evidence-based approach to optimize opioid prescribing in older adults with CNCP.
KEYWORDS: Adverse drug event; Aged; Opioid; Pharmacokinetics

Farmacología de los analgésicos opioides

Analgésicos opioides
Opioid Analgesics
Maree T. Smith, Wei H. Goh

5to Curso Internacional de Anestesiología cardiotorácica, vascular, ecocardiografía y circulación extracorpórea. SMACT
Mayo 4-6, 2017, Ciudad de México
Informes Dr. Hugo Martínez Espinoza 
Regional Anesthesiology and Acute Pain Medicine Meeting
April 6-8, 2017, San Francisco, California, USA
ASRA American Society of Regional Anesthesia and Pain Medicine
California Society of Anesthesiologists
Annual Meeting April 27-30, 2017
San Francisco California
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