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Opioid pharmacology

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https://www.readbyqxmd.com/read/29458047/effects-of-cytochrome-p450-single-nucleotide-polymorphisms-on-methadone-metabolism-and-pharmacodynamics
#1
REVIEW
Taha Ahmad, Monica A Valentovic, Gary O Rankin
Methadone is a synthetic, long-acting opioid with a single chiral center forming two enantiomers, (R)-methadone and (S)-methadone, each having specific pharmacological actions. Concentrations of (R)- and (S)-methadone above therapeutic levels have the ability to cause serious, life-threatening, and fatal side effects. This toxicity can be due in part to the pharmacogenetics of an individual, which influences the pharmacokinetic and pharmacodynamic properties of the drug. Methadone is primarily metabolized in the liver by cytochrome P450 (CYP) enzymes, predominately by CYP2B6, followed by CYP3A4, 2C19, 2D6, and to a lesser extent, CYP2C18, 3A7, 2C8, 2C9, 3A5, and 1A2...
February 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29457674/a-review-of-brain-stimulation-methods-to-treat-substance-use-disorders
#2
REVIEW
Alexandria S Coles, Karolina Kozak, Tony P George
BACKGROUND: Substance use disorders (SUDs) are a leading cause of disability worldwide. While several pharmacological and behavioral treatments for SUDs are available, these may not be effective for all patients. Recent studies using non-invasive neuromodulation techniques including Repetitive Transcranial Magnetic Stimulation (rTMS), Transcranial Direct Current Stimulation (tDCS), and Deep Brain Stimulation (DBS) have shown promise for SUD treatment. OBJECTIVE: Multiple studies were evaluated investigating the therapeutic potential of non-invasive brain stimulation techniques in treatment of SUDs...
February 19, 2018: American Journal on Addictions
https://www.readbyqxmd.com/read/29451744/design-synthesis-and-biological-evaluation-of-novel-bivalent-ligands-targeting-dopamine-d2-like-receptors-and-%C3%A2%C2%B5-opioid-receptor
#3
Mingcheng Qian, Lakshmi Vasudevan, Jelle Huysentruyt, Martijn D P Risseeuw, Christophe Stove, Patrick M L Vanderheyden, Kathleen Van Craenenbroeck, Serge Van Calenbergh
Nowadays, there is mounting evidence that intermolecular receptor-receptor interactions may result in altered receptor recognition, pharmacology and signaling. Heterobivalent ligands have been proven useful molecular probes for confirming and targeting heteromeric receptors. This paper describes the design and synthesis of novel heterobivalent ligands for dopamine D2-like receptors (D2-likeR) and the µ opioid receptor (µOR) and their evaluation using radioactive ligand binding and functional assays.
February 16, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29446063/direct-and-indirect-healthcare-resource-utilization-and-costs-among-migraine-patients-in-the-united-states
#4
Machaon Bonafede, Sandhya Sapra, Neel Shah, Stewart Tepper, Katherine Cappell, Pooja Desai
OBJECTIVE: The goal of this analysis was to provide a contemporary estimate of the burden of migraine, incorporating both direct and indirect costs, by comparing the costs of migraine patients to a matched group of patients without migraine in a large, nationally representative sample of commercially insured patients in the United States. BACKGROUND: Previous studies have shown that the economic burden of migraine in the United States is substantial for payers, patients, and employers...
February 15, 2018: Headache
https://www.readbyqxmd.com/read/29443722/characterizing-treatment-utilization-patterns-for-trigeminal-neuralgia-in-the-united-states
#5
Joanna M Zakrzewska, Ning Wu, John Y K Lee, Brian Werneburg, Deborah Hoffman, Ying Liu
BACKGROUND AND AIM: Trigeminal neuralgia (TN) is a rare orofacial disorder characterized by severe unilateral paroxysmal pain in the region of the fifth cranial nerve. Clinical guidelines recommend carbamazepine (only US Food and Drug Administration-approved drug for TN) and oxcarbazepine as first-line therapies. We utilized the US Truven Health MarketScan database to examine treatment patterns among patients with TN. METHODS: Included patients were aged ≥18 years, newly diagnosed with TN (≥2 TN diagnoses ≥14 days apart; no diagnosis in the prior year), continuously enrolled 1 year pre-index, with ≥3 years' follow-up post-index...
February 13, 2018: Clinical Journal of Pain
https://www.readbyqxmd.com/read/29441714/time-dependent-regional-brain-distribution-of-methadone-and-naltrexone-in-the-treatment-of-opioid-addiction
#6
Belin G Teklezgi, Annapurna Pamreddy, Sooraj Baijnath, Hendrik G Kruger, Tricia Naicker, Nirmala D Gopal, Thavendran Govender
Opioid addiction is a serious public health concern with severe health and social implications; therefore, extensive therapeutic efforts are required to keep users drug free. The two main pharmacological interventions, in the treatment of addiction, involve management with methadone an mu (μ)-opioid agonist and treatment with naltrexone, μ-opioid, kappa (κ)-opioid and delta (δ)-opioid antagonist. MET and NAL are believed to help individuals to derive maximum benefit from treatment and undergo a full recovery...
February 14, 2018: Addiction Biology
https://www.readbyqxmd.com/read/29436434/updates-in-palliative-care-overview-and-recent-advancements-in-the-pharmacological-management-of-cancer-pain
#7
Helen Wood, Andrew Dickman, Angela Star, Jason W Boland
Pain is a common symptom in many types of cancer. Interdisciplinary team management, including pain assessment, explanation to the patient/family, treating the reversible, non-pharmacological treatments and reassessment are essential. This article focuses on the pharmacological management of cancer pain, and overviews and updates on the recent advances in this field. Both non-opioid and opioid analgesia as well as coanalgesics (adjuvants) are reviewed. Within non-opioid analgesia the risks of non-steroidal anti-inflammatory drugs (NSAIDs) are considered and recommendations for NSAIDs in patients at risk of gastrointestinal and cardiovascular toxicity are made...
February 2018: Clinical Medicine: Journal of the Royal College of Physicians of London
https://www.readbyqxmd.com/read/29436433/updates-in-palliative-care-recent-advancements-in-the-pharmacological-management-of-symptoms
#8
Angela Star, Jason W Boland
Symptom management is an important part of both palliative care and end-of-life care. This article will examine the recent research evidence about drugs commonly used for symptom management in adult patients receiving palliative care. In particular, the management of symptoms where recent palliative care-based evidence has changed recommended practice will be reviewed. This includes: breathlessness, delirium, nausea and vomiting in bowel obstruction, opioid-induced constipation and upper respiratory tract secretions...
February 2018: Clinical Medicine: Journal of the Royal College of Physicians of London
https://www.readbyqxmd.com/read/29433586/a-case-report-of-clonidine-induced-syncope-a-review-of-central-actions-of-an-old-cardiovascular-drug
#9
Alexander J Sandweiss, Christopher M Morrison, Anne Spichler, John Rozich
BACKGROUND: Clonidine is an imidazoline sympatholytic, acting on both α 2 -adrenergic and imidazoline receptors in the brainstem to induce antihypertensive and negative chronotropic effects in the vasculature and heart respectively. CASE PRESENTATION: A 69-year-old gentleman with hypertension presented to the emergency department after multiple syncopal episodes over the past 12 months. Electrocardiogram demonstrated sinus bradycardia with a heart rate of 42 beats per minute...
February 13, 2018: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29432333/buprenorphine-treatment-for-adolescents-and-young-adults-with-opioid-use-disorders-a-narrative-review
#10
Jacob T Borodovsky, Sharon Levy, Marc Fishman, Lisa A Marsch
: In the past decade, a new cohort of adolescents and young adults with opioid use disorders (OUD) has emerged. While medications and psychosocial treatments are available, few adolescents and young adults with OUD can access and remain in treatment. Effective, practical, and scalable treatment paradigms for this young population are needed. Buprenorphine is a medication with unique pharmacological and regulatory characteristics that make it a promising component of adolescent and young adult OUD treatment models...
February 9, 2018: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/29428394/the-pharmacology-of-amphetamine-and-methylphenidate-relevance-to-the-neurobiology-of-attention-deficit-hyperactivity-disorder-and-other-psychiatric-comorbidities
#11
REVIEW
Stephen V Faraone
Psychostimulants, including amphetamines and methylphenidate, are first-line pharmacotherapies for individuals with attention-deficit/hyperactivity disorder (ADHD). This review aims to educate physicians regarding differences in pharmacology and mechanisms of action between amphetamine and methylphenidate, thus enhancing physician understanding of psychostimulants and their use in managing individuals with ADHD who may have comorbid psychiatric conditions. A systematic literature review of PubMed was conducted in April 2017, focusing on cellular- and brain system-level effects of amphetamine and methylphenidate...
February 8, 2018: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/29427652/evaluating-the-abuse-potential-of-psychedelic-drugs-for-medical-use-in-humans
#12
REVIEW
David J Heal, Jane Gosden, Sharon L Smith
Psychedelics comprise drugs come from various pharmacological classes including 5-HT 2A agonists, indirect 5-HT agonists, e.g. MDMA, NMDA antagonists and κ-opioid receptor agonists. There is resurgence in developing psychedelics to treat psychiatric disorders with high unmet clinical need. Many, but not all, psychedelics are schedule 1 controlled drugs (CDs), i.e. no approved medical use. For existing psychedelics in development, regulatory approval will require a move from schedule 1 to a CD schedule for drugs with medical use, i...
February 7, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29421482/minimum-alveolar-concentration-key-concepts-and-a-review-of-its-pharmacological-reduction-in-dogs-part-2
#13
REVIEW
Rachel Reed, Thomas Doherty
OBJECTIVE: To outline the major components of the minimum alveolar concentration (MAC) and review the literature regarding pharmacological manipulation of the MAC of halothane, isoflurane, sevoflurane, enflurane, and desflurane in dogs. The pharmacological agents included are alpha-2 agonists, benzodiazepines, propofol, opioids, lidocaine, acepromazine, non-steroidal anti-inflammatory agents (NSAIDs), maropitant, and NMDA antagonists. Part 2 of this review will focus on the effect of opioids, lidocaine, NSAIDs, maropitant, acepromazine, and NMDA antagonists on MAC...
February 1, 2018: Research in Veterinary Science
https://www.readbyqxmd.com/read/29421434/differential-spinal-and-supraspinal-activation-of-glia-in-a-rat-model-of-morphine-tolerance
#14
Viljami Jokinen, Yulia Sidorova, Hanna Viisanen, Ilida Suleymanova, Henna Tiilikainen, Zhilin Li, Tuomas O Lilius, Kert Mätlik, Jenni E Anttila, Mikko Airavaara, Li Tian, Pekka V Rauhala, Eija A Kalso
Development of tolerance is a well known pharmacological characteristic of opioids and a major clinical problem. In addition to the known neuronal mechanisms of opioid tolerance, activation of glia has emerged as a potentially significant new mechanism. We studied activation of microglia and astrocytes in morphine tolerance and opioid-induced hyperalgesia in rats using immunohistochemistry, flow cytometry and RNA sequencing in spinal- and supraspinal regions. Chronic morphine treatment that induced tolerance and hyperalgesia also increased immunoreactivity of spinal microglia in the dorsal and ventral horns...
February 6, 2018: Neuroscience
https://www.readbyqxmd.com/read/29413524/mu-opioid-pharmacology-40-years-to-the-promised-land
#15
Gavril W Pasternak
Opioids continue to play a major role in medicine, but not without problems. Side effects limit their utility medically, while the potential of addiction has had a major societal impact. Pharmacologists have been trying to develop opioids lacking side effects since the first derivative, heroin, was synthesized in the 1870s. The identification of opioid receptors about 40 years ago opened up new insights into our understanding of opioid action, fueled by the molecular biology revolution of the 1980s and 1990s...
2018: Advances in Pharmacology
https://www.readbyqxmd.com/read/29410385/functional-magnetic-resonance-imaging-evaluation-of-auricular-percutaneous-electrical-neural-field-stimulation-for-fibromyalgia-protocol-for-a-feasibility-study
#16
Melat Gebre, Anna Woodbury, Vitaly Napadow, Venkatagiri Krishnamurthy, Lisa C Krishnamurthy, Roman Sniecinski, Bruce Crosson
BACKGROUND: Fibromyalgia is a chronic pain state that includes widespread musculoskeletal pain, fatigue, psychiatric symptoms, cognitive and sleep disturbances, and multiple somatic symptoms. Current therapies are often insufficient or come with significant risks, and while there is an increasing demand for non-pharmacologic and especially non-opioid pain management such as that offered through complementary and alternative medicine therapies, there is currently insufficient evidence to recommend these therapies...
February 6, 2018: JMIR Research Protocols
https://www.readbyqxmd.com/read/29407363/society-of-family-planning-clinical-guidelines-pain-control-in-surgical-abortion-part-1-local-anesthesia-and-minimal-sedation
#17
REVIEW
Rebecca H Allen, Rameet Singh
Satisfactory pain control for women undergoing surgical abortion is important for patient comfort and satisfaction. Clinicians ought to be aware of the safety and efficacy of different pain control regimens. This document will focus on nonpharmacologic modalities to reduce pain and pharmacologic interventions up to the level of minimal sedation. For surgical abortion without intravenous medications, a multimodal approach to pain control may combine a dedicated emotional-support person, visual or auditory distraction, administration of local anesthesia to the cervix with buffered lidocaine, and a preoperative nonsteroidal anti-inflammatory drug...
January 30, 2018: Contraception
https://www.readbyqxmd.com/read/29404792/intrathecal-drug-delivery-and-spinal-cord-stimulation-for-the-treatment-of-cancer-pain
#18
REVIEW
Fangfang Xing, R Jason Yong, Alan David Kaye, Richard D Urman
PURPOSE OF REVIEW: The purpose of the present investigation is to summarize the body and quality of evidence including the most recent studies in support of intrathecal drug delivery systems and spinal cord stimulation for the treatment of cancer-related pain. RECENT FINDINGS: In the past 3 years, a number of prospective studies have been published supporting intrathecal drug delivery systems for cancer pain. Additional investigation with adjuvants to morphine-based analgesia including dexmedetomidine and ziconotide support drug-induced benefits of patient-controlled intrathecal analgesia...
February 5, 2018: Current Pain and Headache Reports
https://www.readbyqxmd.com/read/29403149/goals-and-objectives-to-optimize-the-value-of-an-acute-pain-service-in-perioperative-pain-management
#19
Linda Le-Wendling, Wesley Glick, Patrick Tighe
As newer pharmacologic and procedural interventions, technology, and data on outcomes in pain management are becoming available, effective acute pain management will require a dedicated Acute Pain Service (APS) to help determine the most optimal pain management plan for the patients. Goals for pain management must take into consideration the side effect profile of drugs and potential complications of procedural interventions. Multiple objective optimization is the combination of multiple different objectives for acute pain management...
December 2017: Techniques in Orthopaedics: TIO
https://www.readbyqxmd.com/read/29392233/regular-physical-activity-prevents-development-of-chronic-muscle-pain-through-modulation-of-supraspinal-opioid-and-serotonergic-mechanisms
#20
Renan G Brito, Lynn A Rasmussen, Kathleen A Sluka
Introduction: It is generally believed that exercise produces its effects by activating central opioid receptors; there are little data that support this claim. The periaqueductal gray (PAG) and rostral ventromedial medulla (RVM) are key nuclei in opioid-induced analgesia, and opioids interact with serotonin to produce analgesia. Objectives: The purpose was to examine central inhibitory mechanisms involved in analgesia produced by wheel running. Methods: C57/Black6 mice were given access to running wheels in their home cages before induction of chronic muscle hyperalgesia and compared with those without running wheels...
September 2017: Pain Reports (Baltimore, Md.)
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