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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(0x53d8778) 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.
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
James E Frampton
Pregabalin (Lyrica(®)), a well established anxiolytic agent, has been approved in the EU for the treatment of generalized anxiety disorder (GAD) in adults. It has a distinct mechanism of action relative to other anti-anxiety agents (α2δ binding at presynaptic voltage dependent calcium channels leading to inhibition of excitatory neurotransmission), a rapid onset of effect (typically ≤1 week) and broad spectrum activity against both the psychic and somatic symptoms of GAD. In long-term studies, pregabalin maintained improvements in anxiety symptoms that occurred in response to short-term treatment and delayed the time to relapse of GAD compared with placebo...
September 2014: CNS Drugs
Marci L Chew, Christine W Alvey, Anna Plotka, Verne W Pitman, Tanja Alebic-Kolbah, Joseph M Scavone, Howard N Bockbrader
BACKGROUND: Pregabalin (Lyrica(®)) is approved as an immediate-release (IR) formulation for administration twice (BID) or three times (TID) a day depending on indication. Once daily (QD) dosing may be appropriate for ease of clinical use and patient convenience. OBJECTIVES: The objectives of this analysis were: (1) to evaluate the pharmacokinetics of pregabalin controlled-release (CR) administered with food relative to the pregabalin IR formulation administered fasted; (2) to evaluate the pharmacokinetics of a two-tablet dose of pregabalin CR compared with the equivalent one-tablet dose of pregabalin CR; and (3) to determine the safety and tolerability of multiple-dose administration of pregabalin CR and IR...
September 2014: Clinical Drug Investigation
Jan Schjøtt, Jenny Bergman
BACKGROUND: RELIS is a Norwegian network of four regional medicine-information and pharmacovigilance centers where pharmacists and clinical pharmacologists provide feedback to health care professionals in spontaneous drug-related questions and adverse drug-reaction (ADR) reports published in a question-answer pair (QAP) database (the RELIS database) and the Norwegian ADR database, respectively. OBJECTIVE: To describe the potential of RELIS's dual service to improve detection and communication of drug-safety problems...
2014: Drug, Healthcare and Patient Safety
Lingling Chu, Chisa Ohta, Zhiwei Zuo, David W C MacMillan
The direct application of carboxylic acids as a traceless activation group for radical Michael additions has been accomplished via visible light-mediated photoredox catalysis. Photon-induced oxidation of a broad series of carboxylic acids, including hydrocarbon-substituted, α-oxy, and α-amino acids, provides a versatile CO2-extrusion platform to generate Michael donors without the requirement for organometallic activation or propagation. A diverse array of Michael acceptors is amenable to this new conjugate addition strategy...
August 6, 2014: Journal of the American Chemical Society
Leslie A Wei, Brett W Davies, Eric M Hink, Vikram D Durairaj
PURPOSE: To examine the effect of a 1-time dose of pregabalin (Lyrica) on the perception of pain and analgesic consumption after oculofacial plastic surgery. METHODS: In this prospective, randomized, double-blind, placebo-controlled trial, patients presenting to the oculofacial plastic surgery service at University of Colorado Eye Center for functional eyelid surgery and who met the study criteria were consecutively enrolled between October 2011 and September 2012...
March 2015: Ophthalmic Plastic and Reconstructive Surgery
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