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Yvonne D'Arcy, Bill McCarberg, Bruce Parsons, Regina Behar, Andrew Thorpe, Andrea Alexander
Neuropathic pain (NeP) is a distinct type of pain caused by damage to the nervous system itself. This often severe and chronic type of pain requires specific treatments that target the underlying pain pathophysiology. The purpose of the current narrative review is to provide an overview of pregabalin (Lyrica®) for the treatment of NeP including its effects on pain, pain-related sleep interference, and other health-related outcomes, timing of therapeutic effect, safety and tolerability, and dosing. The information provided here, along with that in our companion review [1], will help primary care providers develop more effective NeP treatment strategies...
April 20, 2017: Current Medical Research and Opinion
Amanda M Drachnik, Harshita Kumari, Collin M Mayhan, Drew A Fowler, Wei G Wycoff, Charles L Barnes, John E Adams, Carol A Deakyne, Jerry L Atwood
Solid state studies of C-butyl-resorcin[4]arene with pregabalin (Lyrica, Nervalin) in nitrobenzene yielded a cocrystal of C-butyl-resorcin[4]arene with 4-isobutylpyrrolidone-2. A combined experimental and quantum chemical investigation was implemented to further our understanding of the factors affecting the conversion process.
April 15, 2017: Journal of Pharmaceutical Sciences
Stuart M Cain, Barry Bohnet, Jeffrey LeDue, Andrew C Yung, Esperanza Garcia, John R Tyson, Sascha R A Alles, Huili Han, Arn M J M van den Maagdenberg, Piotr Kozlowski, Brian A MacVicar, Terrance P Snutch
Migraine is characterized by severe headaches that can be preceded by an aura likely caused by cortical spreading depression (SD). The antiepileptic pregabalin (Lyrica) shows clinical promise for migraine therapy, although its efficacy and mechanism of action are unclear. As detected by diffusion-weighted MRI (DW-MRI) in wild-type (WT) mice, the acute systemic administration of pregabalin increased the threshold for SD initiation in vivo. In familial hemiplegic migraine type 1 mutant mice expressing human mutations (R192Q and S218L) in the CaV2...
February 28, 2017: Proceedings of the National Academy of Sciences of the United States of America
Mathieu Poucher, Claude Cherrier, Anne-Christelle Poucher, Paolo Di Patrizio
Objective: The objective of this study was to determine current practices in the Lorraine region in the treatment of neuropathic pain and to assess the challenges faced by general practitioners (GPs). Methods: We conducted a qualitative study by the focus group technique, by constituting a balanced panel of GPs to meet diversification requirements. The number of focus groups was defined to obtain data saturation. The lead author of this study acted as an observer, while a facilitator was responsible for moderating the debate...
October 19, 2016: Santé Publique: Revue Multidisciplinaire Pour la Recherche et L'action
David H Collier, Bojena Bitman, Andrew Coles, Lyrica Liu, Sandeep Kumar, Clinton Judd
OBJECTIVES: We assessed the ability of patients with autoimmune inflammatory diseases to successfully use the investigational AutoTouch™ reusable autoinjector as well as patient preference for AutoTouch™ versus the currently marketed single-use prefilled etanercept SureClick® autoinjector. METHODS: Two multicenter studies were performed: a Home Use Study and a Patient Preference Study. In the Home Use Study, 77 patients with rheumatoid arthritis (RA) or psoriatic arthritis self-administered etanercept once weekly for 5 weeks...
January 2017: Postgraduate Medicine
Harpreet S Sidhu, Akshay Sadhotra
Antiepileptic drugs (AEDs) are extensively used worldwide to treat a wide range of disorders other than epilepsy, such as neuropathic pain, migraine, and bipolar disorder. Due to this situation more than 20 new third-generation AEDs have been introduced in the market recently. The future design of new AEDs must also have potential to help in the non-epileptic disorders. The wide acceptance of second generation AEDs for the management of various non-epileptic disorders has caused the emergence of generics in the market...
2016: Frontiers in Pharmacology
Thomas W Hamilton, Louise H Strickland, Hemant G Pandit
BACKGROUND: Total knee arthroplasty is a painful procedure, with approximately half of patients reporting severe pain during the early postoperative period. Gabapentinoids are used as an adjunct for the management of acute pain in approximately half of enhanced recovery programs. We performed a meta-analysis to assess the effectiveness and safety of gabapentinoids for the treatment of acute postoperative pain following total knee arthroplasty. METHODS: Randomized controlled trials of patients undergoing elective primary total knee arthroplasty that compared the use of the gabapentinoid class of drugs (gabapentin [Neurontin; Pfizer]) or pregabalin [Lyrica; Pfizer]) with that of placebo were retrieved, with 12 studies meeting inclusion criteria...
August 17, 2016: Journal of Bone and Joint Surgery. American Volume
E M Krupitsky, R D Ilyuk, A D Mikhailov, K A Kazankov, K V Rybakova, E P Skurat, O G Grishina, I A Zaplatkin, M V Vetrova, N G Neznanov
AIM: To study the efficacy and safety of pregabalin (lyrica) in the complex treatment of opioid withdrawal syndrome (OWS). MATERIAL AND METHODS: HASH(0x47966d0) STUDY DESIGN: single-blind randomized symptom-triggered protocol with an active control. Thirty-four patients were randomly assigned to two groups. The first group (n=19) received up to 600 mg a day of pregabalin for six days along with symptomatic therapy (basic and symptom-triggered)...
2016: Zhurnal Nevrologii i Psikhiatrii Imeni S.S. Korsakova
Abdel Naser Zaid, Naim Kittana, Ayman Mousa, Nadia Ghazal, Rana Bustami
BACKGROUND: Treatment of neuropathic pain has always been challenging, not only from the pharmaco-therapeutic/toxicological point of view, but also due to the unpredictable pharmacokinetic (PK) variations among different generic formulations of the same drug, which require further dose optimization. OBJECTIVES: This progressive work aims to evaluate the bioequivalence (BE) of a generic product of 150 mg pregabalin capsule (antineuropathic drug) vs. the reference brand drug Lyrica<sup>®</sup>...
September 2016: International Journal of Clinical Pharmacology and Therapeutics
Michael E Crawford, Peter Bo Poulsen, Berit Schiøttz-Christensen, Andreas Habicht, Mette Strand, Flemming W Bach
OBJECTIVE: The aim of this study was to provide evidence regarding the real-life efficacy of pregabalin in the treatment of peripheral neuropathic pain (NeP) in Denmark. METHODS: In this prospective, observational, noninterventional study, pregabalin (Lyrica(®)) was prescribed following usual clinical practice. Compared with baseline, the primary study end points after 3 months of observation were changes in 1) the average level of pain during the past week, 2) the worst level of pain during the past week, and 3) the least level of pain during the past week...
2016: Journal of Pain Research
James Offord, Lori L Isom
In the post-genomic era, the idea of using the sequence of a protein to determine its potential role as a drug target has gained currency. The goal of this approach to drug discovery is to use the sequence of a protein that is known to bind a specific ligand or drug, along with the known structure of the ligand binding site, to predict other similar proteins that are also "druggable". Gabapentin (Neurontin) and pregabalin (Lyrica) are drugs currently in the clinic that were developed based on the hypothesis that generating non-hydrolyzable analogs of GABA would lead to the development of antiepileptic agents...
July 2015: Critical Reviews in Biochemistry and Molecular Biology
Junad Khan, Hamed Alghamdi, Muhammad Moin Anwer, Eli Eliav, Vincent Ziccardi
PURPOSE: The objective of this study was to investigate the analgesic effect of a collagen conduit (Neuragen, Integra LifeSciences Corp, Plainsboro, NJ) using duloxetine (Cymbalta, Lilly, Indianapolis, IN) with or without pregabalin (Lyrica, Pfizer, NY) on pain induced by partial sciatic nerve transection in a rat model. MATERIAL AND METHODS: Adult male Sprague-Dawley rats were divided into 5 groups (n = 10 per group): group 1, nerve damage with no treatment; group 2, nerve damage treated with the application of a collagen conduit and saline; group 3, nerve damage treated with the application of a collagen conduit and duloxetine; group 4, nerve damage treated with the application of a collagen conduit and pregabalin; and group 5, nerve damage treated with the application of a collagen conduit and pregabalin plus duloxetine...
June 2016: Journal of Oral and Maxillofacial Surgery
S McNamara, S Stokes, R Kilduff, A Shine
Pregabalin (Lyrica®) is used in treating epilepsy, nerve pain and anxiety. Pregabalin was initially thought to have a low misuse potential however there are emerging reports of Pregabalin being abused. A study was commenced at the National Drug Treatment Centre's (NDTC) Drug Analysis Laboratory to determine the level of usage of Pregabalin within the addiction services population in Ireland. A total of 498 urine samples representing samples from 440 individual opioid substitution patients, initially screened by immunoassay for drugs of abuse, were subjected to further analysis for Pregabalin by Liquid Chromatography/Mass Spectrometry (LC/MS)...
November 2015: Irish Medical Journal
Kyu Ho Jeong, Hye Seung Woo, Chae Jin Kim, Kyung Hwa Lee, Jun Young Jeon, Sang Young Lee, Jae-Hoon Kang, Sangkil Lee, Young Wook Choi
A modified-release (MR) tablet of the anti-anxiety drug pregabalin (PRE) was prepared by hot-melt coating PRE with glyceryl behenate (GB) as a release retardant and compressing to form a matrix with microcrystalline cellulose (MCC) as a hydrophilic diluent. GB-coated PRE had a size in the range of 177-290 μm with good to acceptable flowability. Tablet hardness decreased slightly as GB content increased. PRE release from the tablet matrices was successfully modified by altering the ratio of MCC and GB, and it was found that dissolution- or diffusion-controlled release depended on the amount of GB used...
November 10, 2015: International Journal of Pharmaceutics
Caroline H Johnson, Gary J Patti, Jean-Philippe Courade, Leah P Shriver, Linh T Hoang, Marianne Manchester, Gary Siuzdak
Therapeutic options for neuropathic pain have improved over the last 20 years yet still only provide partial relief with numerous side effects. Recently, metabolomics revealed that the concentration of the endogenous metabolite N,N-dimethylsphingosine (DMS) is increased in the spinal cord in a model of neuropathic pain. Additionally, it was shown that introduction of DMS to the central nervous system (CNS) resulted in mechanical allodynia. Here, we have examined two compounds; pregabalin (Lyrica®), a drug used to treat neuropathic pain, and N-oleoylethanolamine (NOE), an endogenous endocannabinoid-like compound that is known to affect multiple lipid pathways...
September 2015: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
T Borisova, N Pozdnyakova, E Shaitanova, I Gerus, M Dudarenko, R Mironets, G Haufe, V Kukhar
Fluorinated analogs of natural substances take an essential place in the design of new biologically active compounds. New fluorinated analogs of γ-aminobutyric acid, that is, β-polyfluoroalkyl-GABAs (FGABAs), were synthesized with substituents: β-CF3-β-OH (1), β-CF3 (2); β-CF2CF2H (3). FGABAs are bioisosteres of Pregabalin (Lyrica®, Pfizer's blockbuster drug, β-i-Bu-GABA), and have lipophilicity close to this medicine. The effects of synthesized FGABAs on [(3)H]GABA uptake by isolated rat brain nerve terminals (synaptosomes) were assessed and compared with those of Pregabalin...
August 1, 2015: Bioorganic & Medicinal Chemistry
Margaret McCartney
No abstract text is available yet for this article.
May 20, 2015: BMJ: British Medical Journal
Zohre Sadeghzade, S Ali Beyramabadi, Ali Morsali
The Lyrica (Pregabalin) is a novel anticonvulsant and neuropathic pain drug, which could exist as four possible conformers. Herein, employing density functional theory (DFT), and handling the solvent effects with the PCM model, the structural parameters, energetic behavior, natural bond orbital analysis (NBO), as well as tautomerism mechanization of the Lyrica are investigated. The L1 (-OH form) is the most stable conformer of the Lyrica, which can be tautomerized to the L5 (-NH form) tautomer. The tautomerism reaction includes an intramolecular-proton transfer, which affects considerably the structural parameters and atomic charges of the L1...
March 5, 2015: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Diego Ghislieri, Kerry Gilmore, Peter H Seeberger
While continuous chemical processes have attracted both academic and industrial interest, virtually all active pharmaceutical ingredients (APIs) are still produced by using multiple distinct batch processes. To date, methods for the divergent multistep continuous production of customizable small molecules are not available. A chemical assembly system was developed, in which flow-reaction modules are linked together in an interchangeable fashion to give access to a wide breadth of chemical space. Control at three different levels--choice of starting material, reagent, or order of reaction modules--enables the synthesis of five APIs that represent three different structural classes (γ-amino acids, γ-lactams, β-amino acids), including the blockbuster drugs Lyrica and Gabapentin, in good overall yields (49-75%)...
January 7, 2015: Angewandte Chemie
Peng Xiao, Xu Zhu, Xuejian Wu
This paper aimed to discuss the curative effect and safety of curing intercostal neuralgia through paravertebral nerve block combined with pregabalin. 90 cases of patients diagnosed as intercostal neuralgia were taken as research object. Random number method was used to divide the patients that is conforming to the inclusion criteria and exclusion criteria into 3 groups. 30 cases was in group A (oral lyrica), 30 cases was in group B (paravertebral block only) and 30 cases was in group C (paravertebral block combined with pregabalin)...
September 2014: Pakistan Journal of Pharmaceutical Sciences
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