Gabapentinoids: Pharmacokinetics, Pharmacodynamics and Considerations for Clinical Practice
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Neurontin (Gabapentin)
Texas Prior Authorization Program Clinical Criteria Drug/Drug Class Gabapentin Clinical Criteria Information Included in this Document Neurontin (gabapentin) • Drugs requiring prior authorization: the list of drugs requiring prior authorization for this clinical criteria • Prior authorization criteria logic: a description of how the prior authorization request will be evaluated against the clinical criteria rules • Logic diagram: a visual depiction of the clinical criteria logic • Supporting tables: a collection of information associated with the steps within the criteria (diagnosis codes, procedure codes, and therapy codes); provided when applicable • References: clinical publications and sources relevant to this clinical criteria Note: Click the hyperlink to navigate directly to that section. Gralise (gabapentin Extended Release) • Drugs requiring prior authorization: the list of drugs requiring prior authorization for this clinical criteria • Prior authorization criteria logic: a description of how the prior authorization request will be evaluated against the clinical criteria rules • Logic diagram: a visual depiction of the clinical criteria logic • Supporting tables: a collection of information associated with the steps within the criteria (diagnosis codes, procedure codes, and therapy codes); provided when applicable • References: clinical publications and sources relevant to this clinical criteria Note: Click the hyperlink to navigate directly to that section. March 29, 2019 Copyright © 2019 Health Information Designs, LLC 1 Horizant -
Métrologie De La Douleur Animale Sur Modèles Expérimentaux : Développement Et Validation De Biomarqueurs Neuroprotéomiques
Université de Montréal Métrologie de la douleur animale sur modèles expérimentaux : développement et validation de biomarqueurs neuroprotéomiques. par Colombe Otis Département de biomédecine vétérinaire Faculté de médecine vétérinaire Thèse présentée à la Faculté de médecine vétérinaire en vue de l’obtention du grade de philosophiæ doctor (Ph. D.) en sciences vétérinaires option pharmacologie Août, 2017 © Colombe Otis, 2017 Résumé La douleur est un phénomène complexe et dynamique comprenant un processus primaire et sensoriel, la nociception, auquel se rajoutent des réactions de défense et d'alarme psychophysiologiques. Ceci conduit au développement d'une véritable mémoire de la douleur, individuelle et modulée (plasticité neuronale) par des expériences précédentes de douleur, incluant entre autres, des phénomènes de sensibilisation nociceptive. Pour bien comprendre les mécanismes de sensibilisation centrale, les modèles animaux mimant les pathologies humaines sont d’une importance primordi ale. Or, pour ce faire, nous avons proposé une série d'approches expérimentales translationnelles par le développement de modèles expérimentaux de douleur bovine, canine et murine afin de caractériser les atteintes du protéome spinal en fonction du niveau de douleur perçu par l'animal et d’identifier le (les) marqueur (s) potentiellement modulé (s) par la sensibilisation nociceptive. À l’aide de la neuroprotéomique, nous avons identifié sur un modèle bovin de douleur viscérale, la protéine transthyrétine (TTR) comme étant sous-exprimée dans le protéome spinal en présence de douleur et ce, vérifié également dans le modèle canin de douleur chronique liée à l’arthrose chirurgicale. Ces résultats suggèrent la possibilité d’entrevoir la TTR comme un biomarqueur potentiel de la douleur chronique. Notre découverte de la relation entre les niveaux spinaux de TTR par neuroprotéomique et l’ hypersensibilité à la douleur dans les modèles bovin et canin soutiennent l’implication de composantes inflammatoires nociceptives et immunitaires. -
Preventive Report Appendix
Title Authors Published Journal Volume Issue Pages DOI Final Status Exclusion Reason Nasal sumatriptan is effective in treatment of migraine attacks in children: A Ahonen K.; Hamalainen ML.; Rantala H.; 2004 Neurology 62 6 883-7 10.1212/01.wnl.0000115105.05966.a7 Deemed irrelevant in initial screening Seasonal variation in migraine. Alstadhaug KB.; Salvesen R.; Bekkelund SI. Cephalalgia : an 2005 international journal 25 10 811-6 10.1111/j.1468-2982.2005.01018.x Deemed irrelevant in initial screening Flunarizine, a calcium channel blocker: a new prophylactic drug in migraine. Amery WK. 1983 Headache 23 2 70-4 10.1111/j.1526-4610.1983.hed2302070 Deemed irrelevant in initial screening Monoamine oxidase inhibitors in the control of migraine. Anthony M.; Lance JW. Proceedings of the 1970 Australian 7 45-7 Deemed irrelevant in initial screening Prostaglandins and prostaglandin receptor antagonism in migraine. Antonova M. 2013 Danish medical 60 5 B4635 Deemed irrelevant in initial screening Divalproex extended-release in adolescent migraine prophylaxis: results of a Apostol G.; Cady RK.; Laforet GA.; Robieson randomized, double-blind, placebo-controlled study. WZ.; Olson E.; Abi-Saab WM.; Saltarelli M. 2008 Headache 48 7 1012-25 10.1111/j.1526-4610.2008.01081.x Deemed irrelevant in initial screening Divalproex sodium extended-release for the prophylaxis of migraine headache in Apostol G.; Lewis DW.; Laforet GA.; adolescents: results of a stand-alone, long-term open-label safety study. Robieson WZ.; Fugate JM.; Abi-Saab WM.; 2009 Headache 49 1 45-53 10.1111/j.1526-4610.2008.01279.x Deemed irrelevant in initial screening Safety and tolerability of divalproex sodium extended-release in the prophylaxis of Apostol G.; Pakalnis A.; Laforet GA.; migraine headaches: results of an open-label extension trial in adolescents. -
Conjugation of Tryptamine to Biologically Active Carboxylic Acids in Order to Create Prodrugs
ISSN 2380-5064 | The Arsenal is published by the Augusta University Libraries | http://guides.augusta.edu/arsenal Volume 4, Issue 1 (2021) Special Edition Issue CONJUGATION OF TRYPTAMINE TO BIOLOGICALLY ACTIVE CARBOXYLIC ACIDS IN ORDER TO CREATE PRODRUGS Colin Miller, Jr. and Iryna O. Lebedyeva Citation Miller, C., Jr., & Lebedyeva, I. O. (2021). Conjugation of tryptamine to biologically active carboxylic acids in order to create prodrugs. The Arsenal: The Undergraduate Research Journal of Augusta University, 4(1), 26. http://doi.org/10.21633/issn.2380.5064/s.2021.04.01.26 © Miller, Jr. and Lebedyeva 2021. This open access article is distributed under a Creative Commons Attribution NonCommercial-NoDerivs 2.0 Generic License (https://creativecommons.org/licenses/by-nc-nd/2.0/). Conjugation of Tryptamine to Biologically Active Carboxylic Acids in Order to Create Prodrugs Presenter(s): Colin Miller, Jr. Author(s): Colin Miller Jr. and Iryna O. Lebedyeva Faculty Sponsor(s): Iryna O. Lebedyeva, PhD Affiliation(s): Department of Chemistry and Physics (Augusta Univ.) ABSTRACT A number of blood and brain barrier penetrating neurotransmitters contain polar functional groups. Gamma-aminobutyric acid (GABA) is an amino acid, which is one of the primary inhibitory neurotransmitter in the brain and a major inhibitory neurotransmitter in the spinal cord. Antiepileptic medications such as Gabapentin, Phenibut, and Pregabalin have been developed to structurally represent GABA. These drugs are usually prescribed for the treatment of neuropathic pain. Since these drugs contain a polar carboxylic acid group, it affects their ability to penetrate the blood and brain barrier. To address the low bioavailability and tendency for intramolecular cyclization of Gabapentin, its less polar prodrug Gabapentin Enacarbil has been approved in 2011. -
(12) United States Patent (10) Patent No.: US 8,283,487 B2 Ben Moha-Lerman Et Al
USOO8283487B2 (12) United States Patent (10) Patent No.: US 8,283,487 B2 Ben Moha-Lerman et al. (45) Date of Patent: Oct. 9, 2012 (54) PROCESSES FOR THE PREPARATION AND 2003/0176398 A1 9/2003 Gallop et al. PURIFICATION OF GABAPENTIN 2004/0077553 A1* 4/2004 Gallop et al. ................... 514, 19 2005/O154057 A1 7/2005 Estrada et al. ENACARBL 2007/0049627 A1 3, 2007 Tran (75) Inventors: Elena Ben Moha-Lerman, Kiryat Ono FOREIGN PATENT DOCUMENTS (IL); Tamar Nidam, Yehud (IL); Meital WO WO O2/10O347 12/2002 Cohen, Petach-Tikva (IL); Sharon WO WO 2005/0377.84 4/2005 Avhar-Maydan, Givataym (IL); Anna Balanov, Rehovot (IL) OTHER PUBLICATIONS X. Yuan et al. “In Situ Preparation of Zinc Salts of Unsaturated (73) Assignee: Teva Pharmaceutical Industries Ltd., Carboxylic Acids to Reinforce NBR' J. Applied Polymer Science, Petach-Tikva (IL) vol. 77, p. 2740-2748 (2000). - r J. Alexander et al. “(Acyloxy)alkyl Carbamates as Novel Biorevers (*) Notice: Subject to any disclaimer, the term of this ible Prodrugs for Amines: Increased Permeation through Biological patent is extended or adjusted under 35 Membranes”.J. Med. Chem. 1988, 31, pp. 318-322. U.S.C. 154(b) by 249 days. S.M. Rahmathullah et al. “Prodrugs for Amidines: Synthesis and Anti-Pneumocystis carinii Activity of Carbamates of 2.5-Bis(4- (21) Appl. No.: 12/626,682 amidinophenyl)furan” J. Med. Chem. 1999, 42, pp. 3994-4000. (22) Filed: Nov. 26, 2009 * cited by examiner (65) Prior Publication Data Primary Examiner — Joseph K. McKane US 2010/O160665 A1 Jun. 24, 2010 Assistant Examiner — Alicia L Otton (74) Attorney, Agent, or Firm — Arent Fox LLP Related U.S. -
More Treatments on Deck for Alcohol Use Disorder
News & Analysis Medical News & Perspectives More Treatments on Deck for Alcohol Use Disorder Jeff Lyon hirteen years have passed since the Raye Z. Litten, PhD, acting director of the ment for AUD were actually prescribed an US Food and Drug Administration NIAAA’s Division of Medications Develop- AUD medication. T (FDA) last approved a new medica- ment and principal investigator of the trial, It is a complicated problem, says John tion to help the nation’s millions of people says the agency is “excited.” Rotrosen, MD, a psychiatrist and addiction withalcoholusedisorder(AUD)stopormod- Nevertheless, the science of alcohol ad- specialist at New York University School of erate their drinking. diction has seen its share of medicines that Medicine. “To a large extent primary care Only 3 such formulations exist, and 1, failed to live up to their early promise dur- physicians don’t screen for alcoholism,” he disulfiram, dates to the Prohibition era. ing full-scale testing. So Litten said the said. “When they do, they may note it, but Known commercially as Antabuse and agency isn’t putting all its eggs in one bas- don’t really do anything about it.” introduced in 1923, it makes people memo- ket. “You need as many weapons as pos- As far as the failure to prescribe exist- rably ill if they ingest alcohol, but it doesn’t sible to treat a complex disease like alcohol ing medications for AUD, Rotrosen blames stop the cravings. The other 2, naltrexone use disorder,” he said. a lack of knowledge. “A lot of doctors in and acamprosate, approved in 1994 and But therein lies a second difficulty. -
Gabapentin Abuse Gabapentin (Neurontin®) Is Indicated for the Treatment of Epilepsy and Neuro- Pathic Pain, Including Post-Herpetic Neuralgia
November 2018 Poison Center Hotline: 1-800-222-1222 The Maryland Poison Center’s Monthly Update: News, Advances, Information Gabapentin Abuse Gabapentin (Neurontin®) is indicated for the treatment of epilepsy and neuro- pathic pain, including post-herpetic neuralgia. Gabapentin is often prescribed off -label for a variety of conditions including insomnia, anxiety, bipolar disorder, migraines, drug and alcohol addiction, and others. Off-label use exceeds use for FDA approved indications. Termed a gabapentinoid, it is an analog of γ- aminobutyric acid (GABA) that increases GABA but does not bind to GABA re- ceptors. It has a selective inhibitory effect on voltage-gated calcium channels containing the α2δ1 subunit. Its exact mechanism for epilepsy and pain is un- clear. Gabapentin is not a controlled substance as it was believed that gabapentin had no abuse potential when approved by the FDA in 1993. Overall, if used at thera- Did you know? peutic doses by patients without a substance abuse/misuse history, the risk of misuse is probably lower than that of other drugs such as benzodiazepines. There are reports of abuse of However, reports are increasing of gabapentin misuse and abuse. Motivations pregabalin (Lyrica ®), another for misuse include recreational use, mood and/or anxiety control, potentiating gabapentinoid used for the effects of drug abuse treatment, pain management, reducing cravings for neuropathic pain, post-herpetic other drugs, managing withdrawal from other drugs, substituting for other pain and fibromyalgia. drugs, and gabapentin addiction (Addiction 2016;11:1160-74). The risk of misuse Approved by the FDA in 2004, increases in people with a history of recreational drug abuse who take gabapen- pregabalin is Schedule V. -
Membrane Stabilizer Medications in the Treatment of Chronic Neuropathic Pain: a Comprehensive Review
Current Pain and Headache Reports (2019) 23: 37 https://doi.org/10.1007/s11916-019-0774-0 OTHER PAIN (A KAYE AND N VADIVELU, SECTION EDITORS) Membrane Stabilizer Medications in the Treatment of Chronic Neuropathic Pain: a Comprehensive Review Omar Viswanath1,2,3 & Ivan Urits4 & Mark R. Jones4 & Jacqueline M. Peck5 & Justin Kochanski6 & Morgan Hasegawa6 & Best Anyama7 & Alan D. Kaye7 Published online: 1 May 2019 # Springer Science+Business Media, LLC, part of Springer Nature 2019 Abstract Purpose of Review Neuropathic pain is often debilitating, severely limiting the daily lives of patients who are affected. Typically, neuropathic pain is difficult to manage and, as a result, leads to progression into a chronic condition that is, in many instances, refractory to medical management. Recent Findings Gabapentinoids, belonging to the calcium channel blocking class of drugs, have shown good efficacy in the management of chronic pain and are thus commonly utilized as first-line therapy. Various sodium channel blocking drugs, belonging to the categories of anticonvulsants and local anesthetics, have demonstrated varying degrees of efficacy in the in the treatment of neurogenic pain. Summary Though there is limited medical literature as to efficacy of any one drug, individualized multimodal therapy can provide significant analgesia to patients with chronic neuropathic pain. Keywords Neuropathic pain . Chronic pain . Ion Channel blockers . Anticonvulsants . Membrane stabilizers Introduction Neuropathic pain, which is a result of nervous system injury or lives of patients who are affected. Frequently, it is difficult to dysfunction, is often debilitating, severely limiting the daily manage and as a result leads to the progression of a chronic condition that is, in many instances, refractory to medical This article is part of the Topical Collection on Other Pain management. -
A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache
University of South Florida Masthead Logo Scholar Commons School of Information Faculty Publications School of Information 7-2015 A Comparative Effectiveness Meta-Analysis of Drugs for the Prophylaxis of Migraine Headache Authors: Jeffrey L. Jackson, Elizabeth Cogbill, Rafael Santana-Davila, Christina Eldredge, William Collier, Andrew Gradall, Neha Sehgal, and Jessica Kuester OBJECTIVE: To compare the effectiveness and side effects of migraine prophylactic medications. DESIGN: We performed a network meta-analysis. Data were extracted independently in duplicate and quality was assessed using both the JADAD and Cochrane Risk of Bias instruments. Data were pooled and network meta-analysis performed using random effects models. DATA SOURCES: PUBMED, EMBASE, Cochrane Trial Registry, bibliography of retrieved articles through 18 May 2014. ELIGIBILITY CRITERIA FOR SELECTING STUDIES: We included randomized controlled trials of adults with migraine headaches of at least 4 weeks in duration. RESULTS: Placebo controlled trials included alpha blockers (n = 9), angiotensin converting enzyme inhibitors (n = 3), angiotensin receptor blockers (n = 3), anticonvulsants (n = 32), beta-blockers (n = 39), calcium channel blockers (n = 12), flunarizine (n = 7), serotonin reuptake inhibitors (n = 6), serotonin norepinephrine reuptake inhibitors (n = 1) serotonin agonists (n = 9) and tricyclic antidepressants (n = 11). In addition there were 53 trials comparing different drugs. Drugs with at least 3 trials that were more effective than placebo for episodic migraines -
1 Gabapentinoids in Total Joint Arthroplasty: the Clinical Practice
1 Gabapentinoids in Total Joint Arthroplasty: The Clinical Practice Guidelines of the American Association of Hip and Knee Surgeons, American Society of Regional Anesthesia and Pain Medicine, American Academy of Orthopaedic Surgeons, Hip Society, and Knee Society Charles P. Hannon MD1, Yale A. Fillingham MD2, James A. Browne MD3, Emil H Schemitsch MD FRCS(C)4, AAHKS Anesthesia & Analgesia Clinical Practice Guideline Workgroup5, Asokumar Buvanendran MD6, William G. Hamilton MD7*, Craig J. Della Valle MD1* 1Department of Orthopaedic Surgery, Rush University Medical Center, Chicago, IL, USA 2Department of Orthopaedic Surgery, Dartmouth-Hitchcock Medical Center, Lebanon, NH, USA 3Department of Orthopaedic Surgery, University of Virginia, Charlottesville, VA, USA 4Department of Surgery, University of Western Ontario, London, Ontario, Canada 5Workgroup Comprised of the following individuals: Justin T. Deen MD (Department of Orthopaedics and Rehabilitation, University of Florida College of Medicine, Gainesville, FL, USA), Greg A. Erens MD (Department of Orthopaedic Surgery, Emory University, Atlanta, GA, USA), Jess H. Lonner MD (Rothman Institute at Thomas Jefferson University, Philadelphia, PA, USA), Aidin E. Pour MD (Department of orthopaedic surgery, University of Michigan, Ann Arbor, MI, USA), Robert S. Sterling MD (Department of Orthopedic Surgery, Johns Hopkins University School of Medicine, Baltimore, MD, USA) 6Department of Anesthesiology, Rush University Medical Center, Chicago, IL, USA 7Anderson Orthopedic Research Institute, Alexandria, VA, USA *Denotes co-senior authors 2 Introduction The American Association of Hip and Knee Surgeons (AAHKS), The American Academy of Orthopaedic Surgeons (AAOS), The Hip Society, The Knee Society and The American Society of Regional Anesthesia and Pain Medicine (ASRA) have worked together to develop evidence-based guidelines on the use of gabapentinoids in primary total joint arthroplasty (TJA). -
Gabapentin Enacarbil (Horizant) Monograph
Gabapentin enacarbil (Horizant) Monograph ® Gabapentin Enacarbil (Horizant ) National Drug Monograph March 2012 VA Pharmacy Benefits Management Services, Medical Advisory Panel, and VISN Pharmacist Executives The purpose of VA PBM Services drug monographs is to provide a comprehensive drug review for making formulary decisions. These documents will be updated when new clinical data warrant additional formulary discussion. Documents will be placed in the Archive section when the information is deemed to be no longer current. Executive Summary: Gabapentin enacarbil (Horizant®) is a prodrug of gabapentin which binds with high affinity to the α2δ subunit of voltage-activated calcium channels in vitro studies. It is unknown how the binding of gabapentin enacarbil (GEn) to the α2δ subunit corresponds to the treatment of restless leg syndrome (RLS) symptoms. Indication: GEn is FDA approved for treatment of RLS. Pharmacokinetics: GEn is primarily excreted by the kidneys and neither gabapentin nor GEn is substrate, inhibitor, or inducer of the major CYP450 system. In addition, GEn is not an inhibitor or substrate of p-glycoprotein in vitro. Dose: The recommended dosage is 600 mg once daily taken with food at about 5 PM. Efficacy: Several studies examining GEn have shown efficacy over placebo in patients with RLS; improvement in RLS symptoms was observed within 7 days of starting treatment.6-8, 12-14 Three studies demonstrated 1200 mg/day GEn significantly reduced International Restless Legs Syndrome (IRLS) scale total score and improved Clinical Global Impression– Improvement (CGI-I) scale compared with placebo.6-8 Two studies demonstrated efficacy at lower dose of 600 mg/day GEn; however, another study did not.7,12,13 These results are comparable to those seen with dopamine agonists.8,12 Adverse Drug Events: Commonly reported adverse effects for the approved dose of 600 mg/day GEn are somnolence, sedation and dizziness. -
Ambetter 90-Day-Maintenance Drug List- 2020
Ambetter 90-Day-Maintenance Drug List Guide to this list: What is Ambetter 90‐Day‐Maintenance Drug List? Ambetter 90‐Day‐Supply Maintenance Drug List is a list of maintenance medications that are available for 90 day supply through mail order or through our Extended Day Supply Network. How do I find a pharmacy that is participating in Extended Day Supply Network? To find a retail pharmacy that is participating in our Extended Day Supply Network please consult information available under Pharmacy Resources tab on our webpage. Alternatively, you can utilize our mail order pharmacy. Information on mail order pharmacy is available in Pharmacy Resources tab on our webpage. Are all formulary drugs covered for 90 day supply? No, certain specialty and non‐specialty drugs are excluded from 90 day supply. Please consult 90‐Day‐ Supply Maintenance Drug List for information if your drug is included. A Amitriptyline HCl Acamprosate Calcium Amlodipine Besylate Acarbose Amlodipine Besylate-Atorvastatin Calcium Acebutolol HCl Amlodipine Besylate-Benazepril HCl Acetazolamide Amlodipine Besylate-Olmesartan Medoxomil Albuterol Sulfate Amlodipine Besylate-Valsartan Alendronate Sodium Amlodipine-Valsartan-Hydrochlorothiazide Alendronate Sodium-Cholecalciferol Amoxapine Alfuzosin HCl Amphetamine-Dextroamphetamine Aliskiren Fumarate Anagrelide HCl Allopurinol Anastrozole Alogliptin Benzoate Apixaban Alosetron HCl Arformoterol Tartrate Amantadine HCl Aripiprazole Amiloride & Hydrochlorothiazide Armodafinil Amiloride HCl Asenapine Maleate Amiodarone HCl Aspirin-Dipyridamole