DOCSLIB.ORG

Salbutamol) in the Treatment of Preterm Labor

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Salbutamol) in the Treatment of Preterm Labor AL-Qadisiya Medical Journal Vol.11 No.20 2015 Effectiveness and safety of the oxytocin antagonist( atosiban) versus beta-adrenergic agonists (salbutamol) in the treatment of preterm labor. Yasamin H. Sharif Al-Shibany* ,Saba M. Swadi Al- Thuwainy * *Obstetrics and Gynecology Department Medical college / Al-Qadisia University ,Email: [email protected] , Email: [email protected] (Received 7 / 4 /2015 , Accepted 19 / 4 / 2015) الخﻻصة : التأثيرات و اﻻعراض الجانبية ﻻستتداا عاتاا اﻻسيستيبا و عتي عاضتد ضﻻتاس لووينيتيستيي الب تر عنتا ضنتتابوت الدةيتتة قالنااانتة ضتتا عاتاا النتتالبييساضي وعتي عاضتتد ضالتي لننتتتابوت البيتتا تت الدةيتة الب تتر ة لعوج حاﻻت اليﻻسة النبكرة. الطر اة: أجر ت الاااسة ضنت لى اليﻻسة و اﻷطلا التعةين الا يانية-العراق , لةلترة ضتي هت ر يتاني الثان /4102 و لغا ة ه ر ياني الثان /4102 ( عةى 011 اضرأة حاضد قعنر 01-52 ستنة( و اسلةتي التى نت الطتياا ضتتا اعتتراض لةتتيﻻسة النبكتترة و يانتتت تتترة الانتتد ضتتي 42-52 أستتبي ( ضتتا وجتتيس انابالتتات لةتترح سنتغرق 51 ثانية قنعا ≤ أاقعة انابالات لو 01 س ياة و يا اسنا عنق الرح ضي 0الى 5 س (و 1التى 5 س (لةنياات عا نة اليﻻسة وسرعة نبض الجنيي طبيعية , س ساني النر ﻻات الى ضجنيعتيي: النجنيعة اﻷولتى و عاسعا 21 ضر ﻻتة عيلجتت قعاتاا النتالبييساضي عتي طر تق ضاةتي الااتي اليا تا و النجنيعتة الثانيتة 21 ضر ﻻة عيلجت قعااااﻻسيسيبا اليا ا ضا ضرا بة هاة اﻻنابالات و اﻻعراض الجانبية لكد عااا عةى اﻻ و الجنيي لغرض سألير اليﻻسة النبكرة و ساةيد النﻻاعلات النر ر ة و الي يات لاى النياليا الداج حا ث اليﻻسة. النتتتا: : لتت كتتي عنتتاف التتتو تت ستتألير حتتاﻻت التتيﻻسة النبكتترة لنتتاة 21 ستتاعة 22% ضااقتتد20%( و 7 أ تتا 41% ضااقتتد 54%( قتتيي النجنيعتتة اﻷولتتى و الثانيتتة عةتتى التتتيال و لكتتي اﻻعتتراض الجانبيتتة ضثتتد سنتتاا نبﻻات ةب اﻻ يانت ايثر عنا النجنيعة اﻷولى الت عيلجت قعاتاا النتالبييساضي 44% ضااقتد 1%(.لت سكتي عناف التو ات النتا: اﻹحصا:ية لةنﻻاعلات النر ر ة لاى النياليا الداج حا ث اليﻻسة قيي النجنيعتيي. اﻻستتتنتاج: استتتداا عاتتاا اﻻسيستتيبا لتتا نتتتا: ضاااقتتة ﻻستتتداا عاتتاا النتتالبييساضي تت ستتألير حتتاو التتيﻻسة النبكرة و لكي لا أعنية سر ر ة ا ﻻد ضي النالبييساضي قنب ةة اﻻعراض الجانبية لاى اﻻ و الجنيي و ننصت قاستتتدااضا يتتأو لتت عوجتت لاتتاﻻت التتيﻻسة النبكتترة لتاةيتتد النﻻتتاعلات و ننتتب الي يتتات لتتاى الدتتاج حتتا ث اليﻻسة. Abstract: Background and Objectives: preterm labor complicates 5-10% of pregnancies and is a leading cause of neonatal morbidity and mortality worldwide and 70-80% of perinatal deaths occur in preterm infants. The aim of this study is to compare the effectiveness, safety and adverse effects of the oxytocin antagonist medication(atosiban) with those of beta-adrenergic agonist (salbutamol) in the treatment of patients with preterm labor. Patients and Methods: one hundred pregnant women with preterm labor were enrolled in this study from the period of( January 2014 – January 2015) at Al- Diwaniya Maternity and Pediatrics Teaching Hospital-Iraq with a gestational age of 24-34 weeks, they were randomly assigned to receive tocolytics either salbutamol (n=50) or atosiban (n=50).Salbutamol was given by(intravenous infusion 10-50 microgram)for up to 48 hour. Atosiban was given by (intravenous bolus dose of 6.75 mg then 300microgram/minute for 3 hour and 100microgram/minute for up to 48hour). Retreatment with the study drugs or alternative tocolytic agents was allowed. Main outcome measures included were tocolytic effectiveness, which was assessed in terms of number of women undelivered after 48hour and 7 days. Tocolytic safety was assessed in terms of maternal and fetal side effects and neonatal morbidity. Results: there were no significant differences between the salbutamol and the atosiban group in prolongation of pregnancy for 48 hour (44% versus 671 AL-Qadisiya Medical Journal Vol.11 No.20 2015 46%;p=0841)and 7 days(20% versus 32%;p=0.171) ,respectively. Maternal adverse events , including tachycardia occurred more frequently in the salbutamol group(22% versus 8%;p=0.050).Neonatal outcomes and complications were comparable between the two study groups(42% versus 32%;p=0.30). Conclusions: the oxytocin antagonist (atosiban) was as effective as beta- agonist(salbutamol) in delaying threatened preterm birth , and found to be better tolerated by both the mother and fetus than salbutamol , with a comparable neonatal safety profil.This study supports the clinical use of atosiban as a first line tocolytic in the treatment of preterm labor. Key words: preterm labor ,tocolytics, salbutamol , atosiban ,pregnancy outcome ,neonatal outcome. Introduction: agents act through a variety of mechanisms Preterm labor refers to the onset of uterine to decrease the availability of intracellular contractions of sufficient strength and calcium ions leading to inhibition of actin- frequency to effect progressive dilatation and myosin interaction(7).Their effectiveness in effacement of the cervix with a gestational suppression of preterm labor has been age between 24 weeks and less than 37 controversial and many of these agents are weeks of gestation , before 24 weeks the associated with serious side effects to both correct term is miscarriage rather than mother and her fetus(7).However, tocolytics preterm labor (1).Preterm labor complicates should be considered if the few days gained 5-10% of pregnancies and is a leading cause would be put to good use such as completing of neonatal morbidity and mortality a course of corticosteroids which greatly worldwide ,and 70-80% of perinatal deaths accelerate fetal lung maturity and reduce the occur in preterm infants (2).It is a major risk of respiratory distress syndrome and its public health problem in terms of loss of life sequelae as well as intraventricular from respiratory distress syndrome(RDS) and hemorrhage ,but it takes one to two days to intraventricular hemorrhage(IVH) ,long term work ,and also give time for in-utero transfer disability (cerebral palsy ,blindness ,deafness of the fetus to a tertiary center equipped for ,chronic lung disease and health care cost) high risk pregnancies with neonatal intensive both in developing and developed care unit(8). world(1,2).Preterm labor precedes about 50% Beta-adrenergic agonist drugs such as of preterm birth , but approximately 30% of salbutamol are the commonly used tocolytic preterm labor spontaneously resolves, less drugs (9).It acts through c-GMP to inhibit than 10% of women presenting with preterm uterine contractions by inhibiting the entry of contractions give birth within seven days and calcium ions into the smooth muscle of the 50% of patients hospitalized for preterm uterus and produce uterine relaxation in most labor give birth at term (3,4).For patients instance, but the onset is variable and with true preterm labor ,tocolytic therapy depends on the dosage. (9).Salbutamol is often abolishes contractions temporarily , but known to cross the placental barrier as does not remove the underlying stimulus that evidenced by the increase in fetal heart rate initiated the process of parturitions or reverse (10). It has been shown that these agents parturition changes in the uterus , and the net postpone the delivery for 24,48hours and result is that a single course of tocolytics may even 7 days, however ,such a delay has not delay delivery by hours or days ,but not been associated with a significant reduction weeks or months(5). in either perinatal mortality or Tocolytics (also called anticontraction morbidity(9,10).They are associated with medications ) are pharmacological agents serious maternal side effects such pulmonary used to suppress premature labor, and they edema ,myocardial ischemia, arrhythmia are given when delivery would result in ,chest pain and death(9).Although premature birth(6).These pharmacological hyperglycemia and hypokalemia are 677 AL-Qadisiya Medical Journal Vol.11 No.20 2015 recognized complications ,so the drug used 34 weeks of pregnancy (determined by the cautiously in patients with diabetes mellitus date of the last menstrual period when known or who require surgery(9,10). or by early ultrasound)with preterm labor Atosiban is a new class of tocolytics, it is an which is defined as the persistence of ≥4 oxytocin antagonist licensed for the symptomatic uterine contractions of at least management of preterm labor (11).Oxytocin 30 second period during the 60-minutes after is believed to initiate uterine contractility by admission and despite bed rest, in the increasing the intracellular calcium presence of cervical dilatation between (0 concentration of myometrium cells through a and 3 cm ) for primigravida and between( 1 direct effect on membrane bound oxytocin and 3 cm) for multigravida , with cervical receptors. Oxytocin further stimulates uterine effacement of more than 50% with a normal contractility and initiates cervical ripening by fetal heart rate. Exclusion criteria: gestational stimulating the release of prostaglandins in age below 24 weeks or over 34 weeks the decidual and fetal membranes ,cervical dilatation greater than 3 cm (12).Atosiban is a synthetic peptide which is ,premature rupture of membranes a competitive antagonist of human oxytocin ,intrauterine growth retardation abnormal at receptor level in the uterus and potentially fetal heart rate, antepartum uterine bleeding, also in the decidual and fetal membranes and eclampsia and sever pre-eclampsia requiring administration result in a dose dependent delivery, intrauterine fetal death suspected inhibition of uterine contractility with a intrauterine infection multiple pregnancy reduction in oxytocin mediated prostaglandin ,fetal anomaly, maternal diabetes mellitus, release (13).As an antagonist
Load more

Recommended publications
  • Molecular Basis of Ligand Recognition and Activation of Human V2 Vasopressin Receptor
    bioRxiv preprint doi: https://doi.org/10.1101/2021.01.18.427077; this version posted January 18, 2021. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. Molecular basis of ligand recognition and activation of human V2 vasopressin receptor Fulai Zhou1, 12, Chenyu Ye2, 12, Xiaomin Ma3, 12, Wanchao Yin1, Qingtong Zhou4, Xinheng He1, 5, Xiaokang Zhang6, 7, Tristan I. Croll8, Dehua Yang1, 5, 9, Peiyi Wang3, 10, H. Eric Xu1, 5, 11, Ming-Wei Wang1, 2, 4, 5, 9, 11, Yi Jiang1, 5, 1. The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China 2. School of Pharmacy, Fudan University, Shanghai 201203, China 3. Cryo-EM Centre, Southern University of Science and Technology, Shenzhen 515055, China 4. School of Basic Medical Sciences, Fudan University, Shanghai 200032, China 5. University of Chinese Academy of Sciences, 100049 Beijing, China 6. Interdisciplinary Center for Brain Information, The Brain Cognition and Brain Disease Institute, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences; 7. Shenzhen-Hong Kong Institute of Brain Science-Shenzhen Fundamental Research Institutions, Shenzhen, China 8. Cambridge Institute for Medical Research, Department of Haematology, University of Cambridge, Cambridge, UK 9. The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 201203 Shanghai, China 10. Department of Biology, Southern University of Science and Technology, Shenzhen 515055, China 11. School of Life Science and Technology, ShanghaiTech University, Shanghai 201210, China 12. These authors contributed equally: Fulai Zhou, Chenyu Ye, and Xiaomin Ma.
    [Show full text]
  • Tractocile, Atosiban
    ANNEX I SUMMARY OF PRODUCT CHARACTERISTICS 1 1. NAME OF THE MEDICINAL PRODUCT Tractocile 6.75 mg/0.9 ml solution for injection 2. QUALITATIVE AND QUANTITATIVE COMPOSITION Each vial of 0.9 ml solution contains 6.75 mg atosiban (as acetate). For a full list of excipients, see section 6.1. 3. PHARMACEUTICAL FORM Solution for injection (injection). Clear, colourless solution without particles. 4. CLINICAL PARTICULARS 4.1 Therapeutic indications Tractocile is indicated to delay imminent pre-term birth in pregnant adult women with: regular uterine contractions of at least 30 seconds duration at a rate of 4 per 30 minutes a cervical dilation of 1 to 3 cm (0-3 for nulliparas) and effacement of 50% a gestational age from 24 until 33 completed weeks a normal foetal heart rate 4.2 Posology and method of administration Posology Treatment with Tractocile should be initiated and maintained by a physician experienced in the treatment of pre-term labour. Tractocile is administered intravenously in three successive stages: an initial bolus dose (6.75 mg), performed with Tractocile 6.75 mg/0.9 ml solution for injection, immediately followed by a continuous high dose infusion (loading infusion 300 micrograms/min) of Tractocile 37.5 mg/5 ml concentrate for solution for infusion during three hours, followed by a lower dose of Tractocile 37.5 mg/5 ml concentrate for solution for infusion (subsequent infusion 100 micrograms/min) up to 45 hours. The duration of the treatment should not exceed 48 hours. The total dose given during a full course of Tractocile therapy should preferably not exceed 330.75 mg of atosiban.
    [Show full text]
  • Largescale Synthesis of Peptides
    Lars Andersson1 Lennart Blomberg1 Large-Scale Synthesis of Martin Flegel2 Ludek Lepsa2 Peptides Bo Nilsson1 Michael Verlander3 1 PolyPeptide Laboratories (Sweden) AB, Malmo, Sweden 2 PolyPeptide Laboratories SpoL, Prague, Czech Republic 3 PolyPeptide Laboratories, Inc., Torrance, CA, 90503 USA Abstract: Recent advances in the areas of formulation and delivery have rekindled the interest of the pharmaceutical community in peptides as drug candidates, which, in turn, has provided a challenge to the peptide industry to develop efficient methods for the manufacture of relatively complex peptides on scales of up to metric tons per year. This article focuses on chemical synthesis approaches for peptides, and presents an overview of the methods available and in use currently, together with a discussion of scale-up strategies. Examples of the different methods are discussed, together with solutions to some specific problems encountered during scale-up development. Finally, an overview is presented of issues common to all manufacturing methods, i.e., methods used for the large-scale purification and isolation of final bulk products and regulatory considerations to be addressed during scale-up of processes to commercial levels. © 2000 John Wiley & Sons, Inc. Biopoly 55: 227–250, 2000 Keywords: peptide synthesis; peptides as drug candidates; manufacturing; scale-up strategies INTRODUCTION and plants,5 have all combined to increase the avail- ability and lower the cost of producing peptides. For For almost half a century, since du Vigneaud first many years, however, the major obstacle to the suc- presented his pioneering synthesis of oxytocin to the cess of peptides as pharmaceuticals was their lack of world in 1953,1 the pharmaceutical community has oral bioavailability and, therefore, relatively few pep- been excited about the potential of peptides as “Na- tides reached the marketplace as approved drugs.
    [Show full text]
  • Hemmo Pharmaceuticals Private Limited
    Global Supplier of Quality Peptide Products Hemmo Pharmaceuticals Private Limited Corporate Presentation Privileged & Confidential Privileged & Confidential Corporate Overview Privileged & Confidential 2 Company at a glance • Commenced operations in 1966 as a Key Highlights trading house, focusing on Oxytocin amongst other products Amongst the largest Indian peptide manufacturing company • In 1979, ventured into manufacturing of Oxytocin Competent team of 154 people including 6 PhDs, 60+ chemistry graduates/post graduates and 3 engineers • Privately held family owned company Portfolio – Generic APIs, Custom Peptides for Research and Clinical Development and Peptide • Infrastructure Fragments − State of art manufacturing facility in Developed 21 generic products in-house. Navi Mumbai, 5 more in progress − R&D facilities at Thane and Spain − Corporate office at Worli First and the only independent Indian company to have a US FDA approved peptide manufacturing site Privileged & Confidential 3 Transition from a trading house to a research based manufacturing facility Commenced Commenced Investment in State of the Art Opened R& D Expanded operations manufacturing greenfield project facility at Navi Centre in manufacturing as a trading of peptides intended for Mumbai Girona,Spain capacity House regulated markets commissioned R&D center set up in Infrastructure Mumbai 1966 1979 2005 2007 2008 2010 2011 2012 2014 2015 Oxytocin Oxytocin Desmopressin Buserelin Triptorelin Goserelin Linaclotide Glatiramer amongst Gonadorelin Decapeptide Cetrorelix
    [Show full text]
  • Oxytocin Receptor OXTR
    Oxytocin Receptor OXTR The oxytocin receptor belongs to the G-protein-coupled seven-transmembrane receptor superfamily. Its main physiological role is regulating the contraction of uterine smooth muscle at parturition and the ejection of milk from the lactating breast. The oxytocin receptors are activated in response to binding oxytocin and a similar nonapeptide, vasopressin. Oxytocin receptor triggers Gi or Gq protein-mediated signaling cascades leading to the regulation of a variety of neuroendocrine and cognitive functions. Oxytocin is a nonapeptide of the neurohypophyseal protein family that binds specifically to the oxytocin receptor to produce a multitude of central and peripheral physiological responses. In vivo, oxytocin acts as a paracrine and/or autocrine mediator of multiple biological effects. These effects are exerted primarily through interactions with G-protein-coupled oxytocin/vasopressin receptors, which, via Gq and Gi, stimulate phospholipase C-mediated hydrolysis of phosphoinositides. www.MedChemExpress.com 1 Oxytocin Receptor Agonists & Antagonists Atosiban Atosiban acetate (RW22164; RWJ22164) Cat. No.: HY-17572 (RW22164 acetate; RWJ22164 acetate) Cat. No.: HY-17572A Atosiban (RW22164; RWJ22164) is a nonapeptide Atosiban acetate (RW22164 acetate;RWJ22164 competitive vasopressin/oxytocin receptor acetate) is a nonapeptide competitive antagonist, and is a desamino-oxytocin analogue. vasopressin/oxytocin receptor antagonist, and is a Atosiban is the main tocolytic agent and has the desamino-oxytocin analogue. Atosiban is the main potential for spontaneous preterm labor research. tocolytic agent and has the potential for spontaneous preterm labor research. Purity: 99.09% Purity: 99.92% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Carbetocin Epelsiban Cat.
    [Show full text]
  • < MOH Approved Drugs List >
    Ministry Of Health Directorate General of Medical Supplies Rep_Id : App_Drugs_List_Who.rdf < MOH Approved Drugs List > DATE : 12/08/2009 Page : 1 of 108 VED Flag <S.No> < Item Code > < I T E M D E S C ROF I P- T I O N > < U N I T > DATE : ABC Flag H/C Flag Category : DRUGS 1 Ph. System : GASTRO-INTESTINAL SYSTEM 1 Main Group : ANTACIDS 1 Sub Group : ALUMINIUM COMPOUNDS 1 03000000105 ALUMINIUM HYDROXIDE GEL, DRIED 475 MG. CAPSULE Desirable Cat_C Not H/C Item 2 Sub Group : ANTACID COMPOUND PREPARATIONS 2 02000000079 ANTACID SUSPENSION (ALUMINIUM HYDROXIDE + BOTTLE Desirable MAGNESIUM HYDROXIDE OR TRISILICATE) 100 - 200 Cat_A ML. B0TTLE. H/C Item 3 03000000173 ANTACID TABLET (ALUMINIUM HYDROXIDE + TABLET/CAP Desirable MAGNESIUM HYDROXIDE OR TRISILICATE). Cat_A H/C Item 2 Main Group : ANTISPASMODICS 1 Sub Group : ANTIMUSCARINICS 4 01000000304 HYOSCINE N BUTYLBROMIDE 20MG/ML. 1ML. AMPOULE Essantial Cat_A H/C Item 5 03000000640 HYOSCINE N BUTYL BROMIDE 10MG. TABLET/CAP Essantial Cat_A H/C Item 6 020D0000063 ANTISPASMODIC DROPS 15ML-25ML. BOTTLE Desirable Cat_C Not H/C Item 2 Sub Group : OTHER ANTISPASMODIC AND MOTILITY STIMULANT 7 03000001245 MEBEVERINE HYDROCHLORIDE 100 MG - 135 MG. TABLET/CAP Essantial Cat_B Not H/C Item Ministry Of Health Directorate General of Medical Supplies Rep_Id : App_Drugs_List_Who.rdf < MOH Approved Drugs List > DATE : 12/08/2009 Page : 2 of 108 VED Flag <S.No> < Item Code > < I T E M D E S C ROF I P- T I O N > < U N I T > DATE : ABC Flag H/C Flag Category : DRUGS 1 Ph.
    [Show full text]
  • List of Pharamaceutical Peptides Available from ADI
    List of Pharamaceutical Peptides Available from ADI ADI has highly purified research grade/pharma grade pharmaceutical peptides available for small research scale or in bulk (>Kg scale). (See Details at the website) http://4adi.com/commerce/catalog/spcategory.jsp?category_id=2704 Catalog# Product Description Catalog# Product Description PP-1000 Abarelix (Acetyl-Ser-Leu-Pro-NH2; MW:1416.06) PP-1410 Growth Hormone-releasing factor, GRF (human) PP-1010 ACTH 1-24 (Adrenocorticotropic Hormone human) Acetate PP-1420 Hexarelin PP-1020 Alarelin Acetate PP-1430 Histrelin Acetate PP-1030 Angiotensin PP-1440 Lepirudin PP-1040 Angiotensin II Acetate PP-1450 Leuprolide PP-1050 Antide Acetate PP-1460 Leuprorelin Acetate PP-1060 Argipressin Acetate PP-1470 Lipopeptide Acetate PP-1070 Argireline Acetate PP-1480 Lypressin PP-1080 Atosiban Acetate PP-1490 Lysipressin Acetate PP-1090 Aviptadil PP-1500 Matrixyl Acetate PP-1100 Bivalirudin Trifluoroacetate PP-1510 Melanotan I, Acetate PP-1110 Buserelin acetate PP-1520 Melanotan II, MT-II, Acetate PP-1120 Copaxone acetate (Glatiramer acetate) PP-1530 Mechano Growth Factor, MGF, TFA PP-1130 Carbetocin acetate PP-1540 Nafarelin Acetate PP-1140 Cetrorelix Acetate PP-1550 Nesiritide Acetate PP-1150 Corticotropin-releasing factor, CRF (human, rat) Acetate PP-1560 Octreotide Acetate PP-1160 Corticotropin-releasing factor, CRF (ovine) PP-1570 Ornipressin Acetate Trifluoroacetate PP-1580 Oxytocin Acetate PP-1170 Deslorelin Acetate PP-1590 Palmitoyl Pentapeptide PP-1180 Desmopressin Acetate PP-1610 Pentagastrin Ammonium
    [Show full text]
  • The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances" WHO/EMP/RHT/TSN/2013.1
    INN Working Document 18.435 31/05/2018 Addendum1 to "The use of stems in the selection of International Nonproprietary names (INN) for pharmaceutical substances" WHO/EMP/RHT/TSN/2013.1 Programme on International Nonproprietary Names (INN) Technologies Standards and Norms (TSN) Regulation of Medicines and other health technologies (RHT) World Health Organization, Geneva © World Health Organization 2018 - All rights reserved. The contents of this document may not be reviewed, abstracted, quoted, referenced, reproduced, transmitted, distributed, translated or adapted, in part or in whole, in any form or by any means, without explicit prior authorization of the WHO INN Programme. This document contains the collective views of the INN Expert Group and does not necessarily represent the decisions or the stated policy of the World Health Organization. Addendum1 to "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances" - WHO/EMP/RHT/TSN/2013.1 1 This addendum is a cumulative list of all new stems selected by the INN Expert Group since the publication of "The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances" 2013. ------------------------------------------------------------------------------------------------------------ -apt- aptamers, classical and mirror ones (a) avacincaptad pegol (113), egaptivon pegol (111), emapticap pegol (108), lexaptepid pegol (108), olaptesed pegol (109), pegaptanib (88) (b) -vaptan stem: balovaptan (116), conivaptan
    [Show full text]
  • Effect of Intravenous Treatment with the Oxytocin Antagonist Atosiban on Circulating Progesterone in the Ewe
    Graduate Theses, Dissertations, and Problem Reports 2011 Effect of Intravenous Treatment with the Oxytocin Antagonist Atosiban on Circulating Progesterone in the Ewe Todd M. Ramboldt West Virginia University Follow this and additional works at: https://researchrepository.wvu.edu/etd Recommended Citation Ramboldt, Todd M., "Effect of Intravenous Treatment with the Oxytocin Antagonist Atosiban on Circulating Progesterone in the Ewe" (2011). Graduate Theses, Dissertations, and Problem Reports. 3323. https://researchrepository.wvu.edu/etd/3323 This Thesis is protected by copyright and/or related rights. It has been brought to you by the The Research Repository @ WVU with permission from the rights-holder(s). You are free to use this Thesis in any way that is permitted by the copyright and related rights legislation that applies to your use. For other uses you must obtain permission from the rights-holder(s) directly, unless additional rights are indicated by a Creative Commons license in the record and/ or on the work itself. This Thesis has been accepted for inclusion in WVU Graduate Theses, Dissertations, and Problem Reports collection by an authorized administrator of The Research Repository @ WVU. For more information, please contact [email protected]. Effect of Intravenous Treatment with the Oxytocin Antagonist Atosiban on Circulating Progesterone in the Ewe Todd M. Ramboldt Thesis submitted to the Davis College of Agriculture, Natural Resources and Design at West Virginia University in partial fulfillment of the requirements for the degree of Master of Science in Reproductive Physiology E. Keith Inskeep, Ph.D., Chair Robert A. Dailey, Ph.D. Jorge A. Flores, Ph.D. Faculty of Reproductive Physiology Morgantown, West Virginia 2011 Keywords: Corpus Luteum, Oxytocin, Atosiban, Progesterone, Sheep ABSTRACT Effect of Intravenous Treatment with the Oxytocin Antagonist Atosiban on Circulating Progesterone in the Ewe Todd M.
    [Show full text]
  • Biased Agonist Pharmacochaperones of the AVP V2 Receptor May Treat Congenital Nephrogenic Diabetes Insipidus
    BASIC RESEARCH www.jasn.org Biased Agonist Pharmacochaperones of the AVP V2 Receptor May Treat Congenital Nephrogenic Diabetes Insipidus Fre´de´ ric Jean-Alphonse,* Sanja Perkovska,* Marie-Ce´line Frantz,† Thierry Durroux,* Catherine Me´jean,* Denis Morin,* Ste´phanie Loison,† Dominique Bonnet,† Marcel Hibert,† Bernard Mouillac,* and Christiane Mendre* *CNRS UMR 5203, Institut de Ge´nomique fonctionnelle, INSERM U661, and Universite´ Montpellier I and II, Montpellier, France; and †CNRS UMR 7175, Institut Gilbert Laustriat, and Universite´ Louis Pasteur, Illkirch, France ABSTRACT X-linked congenital nephrogenic diabetes insipidus (cNDI) results from inactivating mutations of the human arginine vasopressin (AVP) V2 receptor (hV2R). Most of these mutations lead to intracellular retention of the hV2R, preventing its interaction with AVP and thereby limiting water reabsorption and concentration of urine. Because the majority of cNDI-hV2Rs exhibit protein misfolding, molecular chaperones hold promise as therapeutic agents; therefore, we sought to identify pharmacochaperones for hV2R that also acted as agonists. Here, we describe high-affinity nonpeptide compounds that promoted maturation and membrane rescue of L44P, A294P, and R337X cNDI mutants and restored a functional AVP-dependent cAMP signal. Contrary to pharmacochaperone antagonists, these compounds directly activated a cAMP signal upon binding to several cNDI mutants. In addition, these molecules displayed original functionally selective properties (biased agonism) toward the hV2R, being unable to recruit arrestin, trigger receptor internaliza- tion, or stimulate mitogen-activated protein kinases. These characteristics make these hV2R agonist phar- macochaperones promising therapeutic candidates for cNDI. J Am Soc Nephrol 20: 2190–2203, 2009. doi: 10.1681/ASN.2008121289 The antidiuretic hormone arginine-vasopressin congenital nephrogenic diabetes insipidus (cNDI), (AVP) is crucial for osmoregulation, cardiovascular a rare disease characterized by the kidney’s inability control, and water homeostasis.
    [Show full text]
  • Anesthesia and Tocolytic / Uterotonic Therapy in Obstetrics
    First part of presentation: tocolytic therapy … a professional challenge • anesthesia: rarely involved in decision-making • expert knowledge essential ¾ basic pharmacological principles of such a therapy - potential side effects and complications ¾ taking care of pregnant women under tocolysis - secondary preterm Cesarean delivery Second part of presentation: uterotonic therapy … a professional challenge • anesthesia: always involved in decision-making ¾ Cesarean delivery … teamwork: essential component ¾ manual removal of placenta of safe patient care • expert knowledge as basis of a team approach ¾ basic pharmacological principles of such a therapy - potential side effects and complications ¾ taking care of pregnant women at risk of PPH Factors determining uterine tone Uterus contractility 2+ •Caintracellular as determining factor ¾ influx from extracellular compartment - slow voltage-dependent calcium channels ¾ release/reuptake from sarcoplasmatic reticulum • myosin light chain kinase activity as determining factor 2+ ¾ Ca dependent myosin phosphorylation Uterine contraction: contractile protein actomyosin Vercauteren M et al, Acta Anaesthesiol Scand 2009 Drugs affecting uterine contractility Tocolytic substances • β-adrenergic drugs ® ® ¾ fenoterol (Partusisten ), hexoprenaline (Gynipral ) • Calcium channel blockers ® ¾ nifedipine (Adalat ) • Oxytocin antagonists ® ¾ atosiban (Tractocile ) • Prostaglandin synthesis inhibitors (COX-1, COX-2) ® ® ¾ indomethacin (Indocid , Elmetacin ) • Magnesium sulphate • Nitroglycerine Vercauteren
    [Show full text]
  • Differential Effects of Oxytocin Receptor Antagonists, Atosiban and Nolasiban, on Oxytocin Receptor–Mediated Signaling in Human Amnion and Myometrium S
    Supplemental material to this article can be found at: http://molpharm.aspetjournals.org/content/suppl/2017/02/10/mol.116.106013.DC1 1521-0111/91/4/403–415$25.00 http://dx.doi.org/10.1124/mol.116.106013 MOLECULAR PHARMACOLOGY Mol Pharmacol 91:403–415, April 2017 Copyright ª 2017 by The Author(s) This is an open access article distributed under the CC BY-NC Attribution 4.0 International license. Differential Effects of Oxytocin Receptor Antagonists, Atosiban and Nolasiban, on Oxytocin Receptor–Mediated Signaling in Human Amnion and Myometrium s Sung Hye Kim, Oliver Pohl, Andre Chollet, Jean-Pierre Gotteland, Adam D. J. Fairhurst, Phillip R. Bennett, and Vasso Terzidou Institute of Reproductive and Developmental Biology, Hammersmith Hospital Campus (S.H.K., A.D.J.F., P.R.B., V.T.) and Chelsea and Westminster Hospital (V.T.), Imperial College London, London, United Kingdom; and ObsEva SA, Geneva, Switzerland (O.P., A.C., J.-P.G.) Downloaded from Received August 31, 2016; accepted January 30, 2017 ABSTRACT One of the most established roles of oxytocin (OT) is in inducing kinase activation in both myometrial and amnion cells. Consistent uterine contractions and labor. Apart from inducing contractions, with the activation of these inflammatory mediators, OT led to molpharm.aspetjournals.org our recent studies showed that OT can also activate proinflamma- increases in the expression of cyclooxygenase-2 and phosphor- tory pathways in both human myometrial and amnion cells, which ylated cytosolic phospholipase A2, which was reflected in prosta- suggests that the proinflammatory role of OT should be taken into glandin E2 synthesis.
    [Show full text]