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VOLUME 7 2 . No. 4 . AUGUST 2 0
VOLUME 72 . No.4 . AUGUST 2020 © 2020 EDIZIONI MINERVA MEDICA Minerva Pediatrica 2020 August;72(4):288-311 Online version at http://www.minervamedica.it DOI: 10.23736/S0026-4946.20.05861-2 REVIEW MANAGEMENT OF THE MAIN ENDOCRINE AND DIABETIC DISORDERS IN CHILDREN Current treatment for polycystic ovary syndrome: focus on adolescence Maria E. STREET 1 *, Francesca CIRILLO 1, Cecilia CATELLANI 1, 2, Marco DAURIZ 3, 4, Pietro LAZZERONI 1, Chiara SARTORI 1, Paolo MOGHETTI 4 1Division of Pediatric Endocrinology and Diabetology, Department of Mother and Child, Azienda USL – IRCCS di Reggio Emilia, Reggio Emilia, Italy; 2Clinical and Experimental Medicine PhD Program, University of Modena and Reggio Emilia, Modena, Italy; 3Section of Endocrinology and Diabetes, Department of Internal Medicine, Bolzano General Hospital, Bolzano, Italy; 4Division of Endocrinology, Diabetes and Metabolism, Department of Medicine, University and Hospital Trust of Verona, Verona, Italy *Corresponding author: Maria E. Street, Division of Pediatric Endocrinology and Diabetology, Department of Mother and Child, Azienda USL – IRCCS di Reggio Emilia, Viale Risorgimento 80, 42123 Reggio Emilia, Italy. E-mail: [email protected] ABSTRACT Polycystic ovary syndrome (PCOS) is the most frequent endocrine disorder in women and it is associated with an in- creased rate of infertility. Its etiology remains largely unknown, although both genetic and environmental factors play a role. PCOS is characterized by insulin resistance, metabolic disorders and low-grade chronic inflammation. To date, the treatment of PCOS is mainly symptomatic and aimed at reducing clinical signs of hyperandrogenism (hirsutism and acne), at improving menstrual cyclicity and at favoring ovulation. Since PCOS pathophysiology is still largely unknown, the therapeutic interventions currently in place are rarely cause-specific. -
Biased Versus Partial Agonism in the Search for Safer Opioid Analgesics
molecules Review Biased versus Partial Agonism in the Search for Safer Opioid Analgesics Joaquim Azevedo Neto 1 , Anna Costanzini 2 , Roberto De Giorgio 2 , David G. Lambert 3 , Chiara Ruzza 1,4,* and Girolamo Calò 1 1 Department of Biomedical and Specialty Surgical Sciences, Section of Pharmacology, University of Ferrara, 44121 Ferrara, Italy; [email protected] (J.A.N.); [email protected] (G.C.) 2 Department of Morphology, Surgery, Experimental Medicine, University of Ferrara, 44121 Ferrara, Italy; [email protected] (A.C.); [email protected] (R.D.G.) 3 Department of Cardiovascular Sciences, Anesthesia, Critical Care and Pain Management, University of Leicester, Leicester LE1 7RH, UK; [email protected] 4 Technopole of Ferrara, LTTA Laboratory for Advanced Therapies, 44122 Ferrara, Italy * Correspondence: [email protected] Academic Editor: Helmut Schmidhammer Received: 23 July 2020; Accepted: 23 August 2020; Published: 25 August 2020 Abstract: Opioids such as morphine—acting at the mu opioid receptor—are the mainstay for treatment of moderate to severe pain and have good efficacy in these indications. However, these drugs produce a plethora of unwanted adverse effects including respiratory depression, constipation, immune suppression and with prolonged treatment, tolerance, dependence and abuse liability. Studies in β-arrestin 2 gene knockout (βarr2( / )) animals indicate that morphine analgesia is potentiated − − while side effects are reduced, suggesting that drugs biased away from arrestin may manifest with a reduced-side-effect profile. However, there is controversy in this area with improvement of morphine-induced constipation and reduced respiratory effects in βarr2( / ) mice. Moreover, − − studies performed with mice genetically engineered with G-protein-biased mu receptors suggested increased sensitivity of these animals to both analgesic actions and side effects of opioid drugs. -
Summary Analgesics Dec2019
Status as of December 31, 2019 UPDATE STATUS: N = New, A = Advanced, C = Changed, S = Same (No Change), D = Discontinued Update Emerging treatments for acute and chronic pain Development Status, Route, Contact information Status Agent Description / Mechanism of Opioid Function / Target Indication / Other Comments Sponsor / Originator Status Route URL Action (Y/No) 2019 UPDATES / CONTINUING PRODUCTS FROM 2018 Small molecule, inhibition of 1% diacerein TWi Biotechnology / caspase-1, block activation of 1 (AC-203 / caspase-1 inhibitor Inherited Epidermolysis Bullosa Castle Creek Phase 2 No Topical www.twibiotech.com NLRP3 inflamasomes; reduced CCP-020) Pharmaceuticals IL-1beta and IL-18 Small molecule; topical NSAID Frontier 2 AB001 NSAID formulation (nondisclosed active Chronic low back pain Phase 2 No Topical www.frontierbiotech.com/en/products/1.html Biotechnologies ingredient) Small molecule; oral uricosuric / anti-inflammatory agent + febuxostat (xanthine oxidase Gout in patients taking urate- Uricosuric + 3 AC-201 CR inhibitor); inhibition of NLRP3 lowering therapy; Gout; TWi Biotechnology Phase 2 No Oral www.twibiotech.com/rAndD_11 xanthine oxidase inflammasome assembly, reduced Epidermolysis Bullosa Simplex (EBS) production of caspase-1 and cytokine IL-1Beta www.arraybiopharma.com/our-science/our-pipeline AK-1830 Small molecule; tropomyosin Array BioPharma / 4 TrkA Pain, inflammation Phase 1 No Oral www.asahi- A (ARRY-954) receptor kinase A (TrkA) inhibitor Asahi Kasei Pharma kasei.co.jp/asahi/en/news/2016/e160401_2.html www.neurosmedical.com/clinical-research; -
An Open-Label Pilot Trial of Alpha-Lipoic Acid for Weight Loss in Patients with Schizophrenia Without Diabetes Joseph C
Case Reports An Open-Label Pilot Trial of Alpha-Lipoic Acid for Weight Loss in Patients with Schizophrenia without Diabetes Joseph C. Ratliff1 , Laura B. Palmese 1, Erin L. Reutenauer 1, Cenk Tek 1 Abstract A possible mechanism of antipsychotic-induced weight gain is activation of hypothalamic monophosphate-dependent kinase (AMPK) mediated by histamine 1 receptors. Alpha-lipoic acid (ALA), a potent antioxidant, counteracts this ef- fect and may be helpful in reducing weight for patients taking antipsychotics. The objective of this open-label study was to assess the efficacy of ALA (1,200 mg) on twelve non-diabetic schizophrenia patients over ten weeks. Participants lost significant weight during the intervention (-2.2 kg±2.5 kg). ALA was well tolerated and was particularly effective for individuals taking strongly antihistaminic antipsychotics (-2.9 kg±2.6 kg vs. -0.5 kg±1.0 kg). Clinical Trial Registra- tion: NCT01355952. Key Words: Schizophrenia, Obesity, Schizoaffective Disorder, Alpha-Lipoic Acid Introduction dependent protein kinase (AMPK) in the hypothalamus Antipsychotic medications appear to induce weight (4). In the periphery, AMPK increases energy utilization; gain, which results in increased rates of obesity in schizo- AMPK activity in the hypothalamus increases appetite. phrenia (1). Schizophrenia patients have significantly short- Several highly orexigenic (stimulates appetite) antipsy- er life expectancy than the general population (2); most of chotics such as clozapine, olanzapine, and quetiapine are this excess mortality is attributed to diabetes and cardiovas- shown to activate AMPK in the hypothalamus in animal cular disease (3); weight gain is a significant contributor to studies whereas other antipsychotic medications do not (4). -
(12) Patent Application Publication (10) Pub. No.: US 2011/0236506 A1 SCHWARTZ Et Al
US 2011 0236506A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0236506 A1 SCHWARTZ et al. (43) Pub. Date: Sep. 29, 2011 (54) PHARMACEUTICAL ASSOCIATION Publication Classification CONTAINING LIPOCACID AND (51) Int. Cl. HYDROXYCTRIC ACIDAS ACTIVE A633/24 (2006.01) INGREDIENTS A63L/385 (2006.01) A63/685 (2006.01) (75) Inventors: Laurent SCHWARTZ, Paris (FR): A63/4985 (2006.01) Adeline GUAIS-VERGNE, A63L/7056 (2006.01) Draveil (FR) A6IP35/00 (2006.01) (73) Assignees: Laurent SCHWARTZ, Paris (FR): (52) U.S. Cl. ........... 424/649; 514/440; 514/77: 514/249; BIOREBUS, Paris (FR) 514/52 (21) Appl. No.: 13/099,897 (57) ABSTRACT Pharmaceutical combination containing lipoic acid and (22) Filed: May 3, 2011 hydroxycitric acid as active ingredients. The present inven tion relates to a novel pharmaceutical combination and to the Related U.S. Application Data use thereof for producing a medicament having an antitumor (63) Continuation of application No. PCT/FR2009/ activity. According to the invention, this combination com 052110, filed on Nov. 2, 2009. prises, as active ingredients: lipoic acid or one of the pharma ceutically acceptable salts thereof, and hydroxycitric acid or (30) Foreign Application Priority Data one of the pharmaceutically acceptable salts thereof. Said active ingredients being formulated together or separately for Nov. 3, 2008 (FR) ....................................... O8574.48 a conjugated, simultaneous or separate use. Patent Application Publication Sep. 29, 2011 Sheet 1 of 9 US 2011/023650.6 A1 lipoic acid alone -29 f2 f Niger of ces i{t} v s 6 g i w 4. 6 8 i 2 Concentrations tumoi.i. -
Philadelphia
Saturday, April 18th, 2015 PCOS Awareness Symposium 2015 Philadelphia Polycystic Ovary Syndrome: Creating a Treatment Plan Katherine Sherif, MD Professor & Vice Chair, Department of Medicine Director, Jefferson Women’s Primary Care Thomas Jefferson University The Canary in the Coalmine . PCOS seems to accelerate the aging process . It is possible to reverse the aging process . Be scrupulous in your commitment to be healthy Multiple Systems . Reproductive . Endocrinologic . Cardiac . Renal (kidney) . Hepatic (liver) . Brain (mood) . Dermatologic Multiple Signs & Symptoms Irregular periods, Bleeding too much, Bleeding too little, Anxiety, Depression, Eating disorders, Weight gain, Acanthosis nigricans, Skin tags, Follicular keratitis, Hirsutism, Acne, Alopecia, Excess sweating, Seborrheic dermatitis, Hidradenitis supparativa, Fatty liver, High triglycerides, low HDL-cholesterol, Elevated glucose, Infertility, Breastfeeding problems, Poor sleep, Miscarriages, Fatigue, Endometrial cancer Multiple Pathways GnRH pulsatility Theca cell LH Progesterone 17 - OH P testosterone estrone androstenedione & TGranulosa A* Estradiol X Follicle Peripheral conversion A* = aromatase More Pathways! GnRH Insulin pulsatility Theca cell LH Progesterone 17 - OH P testosterone estrone androstenedione testosterone estradiol X ↓ SHBG Free T X Follicle Peripheral conversion The Magic Bullet The oral contraceptive pill . High doses of estrogen (ethinyl estradiol) . Increase SHBG and lower free testosterone* . Improve skin symptoms in most: . Alopecia . -
The Main Tea Eta a El Mattitauli Mali Malta
THE MAIN TEA ETA USA 20180169172A1EL MATTITAULI MALI MALTA ( 19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2018 /0169172 A1 Kariman (43 ) Pub . Date : Jun . 21 , 2018 ( 54 ) COMPOUND AND METHOD FOR A61K 31/ 437 ( 2006 .01 ) REDUCING APPETITE , FATIGUE AND PAIN A61K 9 / 48 (2006 .01 ) (52 ) U . S . CI. (71 ) Applicant : Alexander Kariman , Rockville , MD CPC . .. .. .. .. A61K 36 / 74 (2013 .01 ) ; A61K 9 / 4825 (US ) (2013 . 01 ) ; A61K 31/ 437 ( 2013 . 01 ) ; A61K ( 72 ) Inventor: Alexander Kariman , Rockville , MD 31/ 4375 (2013 .01 ) (US ) ( 57 ) ABSTRACT The disclosed invention generally relates to pharmaceutical (21 ) Appl . No. : 15 /898 , 232 and nutraceutical compounds and methods for reducing appetite , muscle fatigue and spasticity , enhancing athletic ( 22 ) Filed : Feb . 16 , 2018 performance , and treating pain associated with cancer, trauma , medical procedure , and neurological diseases and Publication Classification disorders in subjects in need thereof. The disclosed inven ( 51 ) Int. Ci. tion further relates to Kratom compounds where said com A61K 36 / 74 ( 2006 .01 ) pound contains at least some pharmacologically inactive A61K 31/ 4375 ( 2006 .01 ) component. pronuPatent Applicationolan Publication manu saJun . decor21, 2018 deSheet les 1 of 5 US 2018 /0169172 A1 reta Mitragynine 7 -OM - nitragynine *** * *momoda W . 00 . Paynantheine Speciogynine **** * * * ! 1000 co Speclociliatine Corynartheidine Figure 1 Patent Application Publication Jun . 21, 2018 Sheet 2 of 5 US 2018 /0169172 A1 -
Opioid Crisis—An Emphasis on Fentanyl Analogs
brain sciences Editorial Opioid Crisis—An Emphasis on Fentanyl Analogs Kabirullah Lutfy College of Pharmacy, Western University of Health Sciences, Pomona, CA 91766, USA; [email protected] Received: 21 July 2020; Accepted: 23 July 2020; Published: 27 July 2020 Abstract: Opioids are the mainstay for the management of moderate to severe pain. However, their acute use is associated with several side effects, ranging from nausea, itching, sedation, hypotension to respiratory depression, and death. Also, chronic use of these drugs can lead to the development of tolerance, dependence, and eventually addiction. The most serious side effect, lethality due to opioid-induced overdose, has reached the level of national emergency, i.e., the opioid crisis, which is now the forefront of medicine. In a detailed review (Novel Synthetic Opioids: The Pathologist’s Point of View), Frisoni and colleagues have discussed the side effects of novel licit and illicit fentanyl derivatives, as well as the related compounds which are more potent and faster acting than morphine and other conventional opioids (Frisoni, et al., 2018). These drugs affect the central nervous system (CNS) and can promote the development of addiction due to the quick rush they induce because of their faster entry into the brain. These drugs also arrest the cardiovascular and pulmonary systems, increasing the chance of respiratory arrest, leading to opioid-induced overdose morbidity and mortality. The respiratory arrest induced by opioids can be potentiated by other CNS depressants, such as alcohol or benzodiazepines, and therefore may occur more frequently in polydrug users. Therefore, the use of these newer fentanyl derivatives as well as other fast acting opioids should be avoided or limited to specific cases and must be kept out of the reach of children and adolescents who are more vulnerable to become addicted or overdose themselves. -
Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT
Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT Product Name : Cebranopadol Catalog Number : T5167 CAS Number : 863513-91-1 Molecular Formula : C24H27FN2O Molecular Weight : 378.48 Description: Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis of 0.9 nM, 0.7 nM, 2.6 nM, 18 nM for human NOP, μ-opioid (MOP), κ-opioid (KOP) and δ-opioid (DOP) receptor, respectively. Storage: 2 years -80°C in solvent; 3 years -20°C powder; DMSO 6 mg/mL Solubility Water Insoluble ( < 1 mg/ml refers to the product slightly soluble or insoluble ) NOP 13 nM (EC50, cell free) μ-opioid receptor 1.2 nM (EC50, cell free) Receptor (IC50) κ-opioid receptor 17 nM (EC50, cell free) δ-opioid receptor 110 nM (EC50, cell free) In vitro Activity Cebranopadol showed full agonistic efficacy at the human MOP and DOP receptors, almost full efficacy at the human NOP receptor, and partial efficacy at the human KOP receptor. In a functional [35S]GTPgS binding assay with membranes expressing the human 5-HT5A receptor, cebranopadol did not show agonistic or signirficant antagonistic effects at concentrations up to 10.0 μM [1]. In vivo Activity Cebranopadol exhibits highly potent and efficacious antinociceptive and antihypersensitive effects in several rat models of acute and chronic pain with ED50 values of 0.5-5.6 μg/kg after intravenous and 25.1 μg/kg after oral administration. Cebranopadol's duration of action is long (up to 7 hours after intravenous 12 μg/kg; >9 hours after oral 55 μg/kg in the rat tail-flick test) [1]. -
Mitochondrial Dysfunction and Chronic Inflammation in Polycystic
International Journal of Molecular Sciences Review Mitochondrial Dysfunction and Chronic Inflammation in Polycystic Ovary Syndrome Siarhei A. Dabravolski 1,*, Nikita G. Nikiforov 2,3,4, Ali H. Eid 5,6,7, Ludmila V. Nedosugova 8, Antonina V. Starodubova 9,10, Tatyana V. Popkova 11, Evgeny E. Bezsonov 4,12 and Alexander N. Orekhov 4 1 Department of Clinical Diagnostics, Vitebsk State Academy of Veterinary Medicine [UO VGAVM], 7/11 Dovatora Str., 210026 Vitebsk, Belarus 2 Center of Collective Usage, Institute of Gene Biology, Russian Academy of Sciences, 34/5 Vavilova Street, 119334 Moscow, Russia; [email protected] 3 Laboratory of Medical Genetics, Institute of Experimental Cardiology, National Medical Research Center of Cardiology, 121552 Moscow, Russia 4 Laboratory of Cellular and Molecular Pathology of Cardiovascular System, Institute of Human Morphology, 3 Tsyurupa Street, 117418 Moscow, Russia; [email protected] (E.E.B.); [email protected] (A.N.O.) 5 Department of Basic Medical Sciences, College of Medicine, QU Health, Qatar University, Doha 2713, Qatar; [email protected] 6 Biomedical and Pharmaceutical Research Unit, QU Health, Qatar University, Doha 2713, Qatar 7 Department of Pharmacology and Toxicology, Faculty of Medicine, American University of Beirut, Beirut P.O. Box 11-0236, Lebanon 8 Citation: Dabravolski, S.A.; Federal State Autonomous Educational Institution of Higher Education, I. M. Sechenov First Moscow State Nikiforov, N.G.; Eid, A.H.; Medical University (Sechenov University), 8/2 Trubenskaya Street, 119991 Moscow, Russia; [email protected] 9 Federal Research Centre for Nutrition, Biotechnology and Food Safety, 2/14 Ustinsky Passage, Nedosugova, L.V.; Starodubova, A.V.; 109240 Moscow, Russia; [email protected] Popkova, T.V.; Bezsonov, E.E.; 10 Pirogov Russian National Research Medical University, 1 Ostrovitianov Street, 117997 Moscow, Russia Orekhov, A.N. -
Safety of Alpha-Lipoic Acid Use in Food Supplements
DTU Doc nr. 17/14450 Date 10.10.2017 Safety of alpha-lipoic acid use in food supplements The Danish Veterinary and Food Administration has asked DTU FOOD to assess the safety of alpha-lipoic acid use in food supplements in a recommended daily dose of 150-200 mg per day. Specification for alpha-lipoic acid SYNONYMS Thioctic acid 1,2-dithiolane-3-pentanoic acid; 1,2-dithiolane-3-valeric acid DEFINITION Chemical name 1,2-Dithiolan-3-pentanic acid CAS Number 1077-28-7 Chemical formula Molecular formula C8H14O2S2 Molecular weight 206.32 g/mol Content Not less than 99.0% and no more than 101.0% alpha-lipoic acid determined by gas chromatography IDENTIFICATION Identification test IR absorption. The spectrum should be in accordance with an equivalent reference spectrum 60-62° C A. Melting point 22 ° B. Specific rotation [α]D : +/- 1.0 (50 mg/ml in ethanol) PURITY Loss on drying No more than 0,2% Ashes No more than 0.1% Heavy metals No more than 10 mg/kg (by method II, Ph. US 39., 673. Mercury is not identified by this test) Lead Not more than 1 mg/kg Specification in accordance with the United States Pharmacopeia (USP) Studies in humans No studies on alpha-lipoic acid conducted in healthy subjects were identified in the literature. Healthy subjects are the target group for food supplements. Several studies conducted in different patient groups including patients with diabetic neuropathy, infertile men, overweight or obese hypertensive, diabetic or hypercholesterolemic subjects were identified (Han et al., 2012; Koh et al., 2011 ; Hahm et al., 2004; Technical University of Denmark Kemitorvet Ph. -
Treating Burning Mouth Syndrome Constance R
East Tennessee State University Digital Commons @ East Tennessee State University ETSU Faculty Works Faculty Works 1-1-2009 Treating Burning Mouth Syndrome Constance R. Sharuga East Tennessee State University Debra Dotson East Tennessee State University Tabitha Price East Tennessee State University, [email protected] Follow this and additional works at: https://dc.etsu.edu/etsu-works Part of the Dental Hygiene Commons Citation Information Sharuga, Constance R.; Dotson, Debra; and Price, Tabitha. 2009. Treating Burning Mouth Syndrome. Dimensions of Dental Hygiene. Vol.7(12). 36-39. http://www.dimensionsofdentalhygiene.com/2009/12_December/Features/ Treating_Burning_Mouth_Syndrome.aspx ISSN: 1542-7919 This Article is brought to you for free and open access by the Faculty Works at Digital Commons @ East Tennessee State University. It has been accepted for inclusion in ETSU Faculty Works by an authorized administrator of Digital Commons @ East Tennessee State University. For more information, please contact [email protected]. Treating Burning Mouth Syndrome Copyright Statement Reprinted with permission. Constance R. Sharuga, Deborah Dotson, and Tabitha Price. Treating burning mouth syndrome. Dimensions of Dental Hygiene, December 2009; 7(12):36-39. This article is available at Digital Commons @ East Tennessee State University: https://dc.etsu.edu/etsu-works/2529 7/16/2018 Dimensions of Dental Hygiene Burning mouth syndrome (BMS) is a chronic, painful condition with no clear etiology or specific, proven treatment. BMS is also known as burning tongue syndrome, glossodynia, glossopyrosis, stomatodynia, stomatopyrosis, and oral dysesthesia.1,2 The syndrome is characterized by burning and/or painful sensations of the mouth, usually in the absence of clinical or laboratory findings.3 It can occur anywhere in the mouth.