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NDA 21-443 Package Insert ENJUVIA™ (synthetic conjugated estrogens, B) Tablets Rx only ESTROGENS INCREASE THE RISK OF ENDOMETRIAL CANCER Close clinical surveillance of all women taking estrogens is important. Adequate diagnostic measures, including endometrial sampling when indicated, should be undertaken to rule out malignancy in all cases of undiagnosed persistent or recurring abnormal vaginal bleeding. There is no evidence that the use of “natural” estrogens results in a different endometrial risk profile than synthetic estrogens at equivalent estrogen doses. (See WARNINGS, Malignant neoplasms, Endometrial cancer.) CARDIOVASCULAR AND OTHER RISKS Estrogens with or without progestins should not be used for the prevention of cardiovascular disease. (See WARNINGS, Cardiovascular disorders.) The Women’s Health Initiative (WHI) study reported increased risks of myocardial infarction, stroke, invasive breast cancer, pulmonary emboli, and deep vein thrombosis in postmenopausal women (50 to 79 years of age) during 5 years of treatment with oral conjugated estrogens (CE 0.625 mg) combined with medroxyprogesterone acetate (MPA 2.5 mg) relative to placebo. (See CLINICAL PHARMACOLOGY, Clinical Studies). The Women’s Health Initiative Memory Study (WHIMS), a substudy of WHI, reported increased risk of developing probable dementia in postmenopausal women 65 years of age or older during 4 years of treatment with oral conjugated estrogens plus medroxyprogesterone acetate relative to placebo. It is unknown whether this finding applies to younger postmenopausal women or to women taking estrogen alone therapy. (See CLINICAL PHARMACOLOGY, Clinical Studies.) Other doses of oral conjugated estrogens with medroxyprogesterone acetate, and other combinations and dosage forms of estrogens and progestins were not studied in the WHI clinical trials and, in the absence of comparable data, these risks should be assumed to be similar. -
Campro Catalog Stable Isotope
Introduction & Welcome Dear Valued Customer, We are pleased to present to you our Stable Isotopes Catalog which contains more than three thousand (3000) high quality labeled compounds. You will find new additions that are beneficial for your research. Campro Scientific is proud to work together with Isotec, Inc. for the distribution and marketing of their stable isotopes. We have been working with Isotec for more than twenty years and know that their products meet the highest standard. Campro Scientific was founded in 1981 and we provide services to some of the most prestigious universities, research institutes and laboratories throughout Europe. We are a research-oriented company specialized in supporting the requirements of the scientific community. We are the exclusive distributor of some of the world’s leading producers of research chemicals, radioisotopes, stable isotopes and environmental standards. We understand the requirements of our customers, and work every day to fulfill them. In working with us you are guaranteed to receive: - Excellent customer service - High quality products - Dependable service - Efficient distribution The highly educated staff at Campro’s headquarters and sales office is ready to assist you with your questions and product requirements. Feel free to call us at any time. Sincerely, Dr. Ahmad Rajabi General Manager 180/280 = unlabeled 185/285 = 15N labeled 181/281 = double labeled (13C+15N, 13C+D, 15N+18O etc.) 186/286 = 12C labeled 182/282 = d labeled 187/287 = 17O labeled 183/283 = 13C labeleld 188/288 = 18O labeled 184/284 = 16O labeled, 14N labeled 189/289 = Noble Gases Table of Contents Ordering Information.................................................................................................. page 4 - 5 Packaging Information .............................................................................................. -
Hypothalamic Principles Necessary for the Release of Ovulating Hormone from the Adenohypophysis
EFFECT OF AMINOGLUTETHIMIDE ON REPRODUCTIVE PROCESSES IN FEMALE RATS W. J. EVERSOLE and D. J. THOMPSON Department of Life Sciences, Indiana State University, Terre Haute, Indiana 47809, U.S.A. (Received "òlst January 1974) Summary. Adult female rats injected subcutaneously with 100 mg aminoglutethimide phosphate (AGP)/kg/day for 4 weeks failed to become pregnant when placed in cohabitation with males during the last 2 weeks of the injection period. Lower doses depressed the fertility rate and reduced the litter size: the average litter size of three of eleven rats given 50 mg/kg/day was 4\m=.\7 young and of four of eleven rats given 25 mg was 7\m=.\0 young. Twenty-nine controls averaged 10\m=.\1/litter. Doses of 100 mg AGP/kg/day stopped vaginal cycling, prevented ovulation in adults, and delayed dissolution of the vaginal membrane in pubertal rats. Histological studies of the ovaries from rats with initial ages of 17 or 21 days which were injected with 25 to 100 mg AGP/kg/day for 2 weeks showed an increase in the number and size of vesicular follicles. Treatment of 27-day-old rats with 25 mg/kg/day for 2 weeks reduced the number of CL and three of four rats given 50 mg had ovaries lacking such bodies; all control ovaries in this group contained CL. These findings are taken as evidence that AGP inhibits ovulation but does not prevent follicular maturation. INTRODUCTION Many pharmacological compounds originally developed as anaesthetics, tranquillizers and anticonvulsants modify endocrine structures and functions (see Gaunt, Chart & Renzi, 1965). -
Mechanisms of Action of Antiepileptic Drugs
Review Mechanisms of action of antiepileptic drugs Epilepsy affects up to 1% of the general population and causes substantial disability. The management of seizures in patients with epilepsy relies heavily on antiepileptic drugs (AEDs). Phenobarbital, phenytoin, carbamazepine and valproic acid have been the primary medications used to treat epilepsy for several decades. Since 1993 several AEDs have been approved by the US FDA for use in epilepsy. The choice of the AED is based primarily on the seizure type, spectrum of clinical activity, side effect profile and patient characteristics such as age, comorbidities and concurrent medical treatments. Those AEDs with broad- spectrum activity are often found to exert an action at more than one molecular target. This article will review the proposed mechanisms of action of marketed AEDs in the US and discuss the future of AEDs in development. 1 KEYWORDS: AEDs anticonvulsant drugs antiepileptic drugs epilepsy Aaron M Cook mechanism of action seizures & Meriem K Bensalem-Owen† The therapeutic armamentarium for the treat- patients with refractory seizures. The aim of this 1UK HealthCare, 800 Rose St. H-109, ment of seizures has broadened significantly article is to discuss the past, present and future of Lexington, KY 40536-0293, USA †Author for correspondence: over the past decade [1]. Many of the newer AED pharmacology and mechanisms of action. College of Medicine, Department of anti epileptic drugs (AEDs) have clinical advan- Neurology, University of Kentucky, 800 Rose Street, Room L-455, tages over older, so-called ‘first-generation’ First-generation AEDs Lexington, KY 40536, USA AEDs in that they are more predictable in their Broadly, the mechanisms of action of AEDs can Tel.: +1 859 323 0229 Fax: +1 859 323 5943 dose–response profile and typically are associ- be categorized by their effects on the neuronal [email protected] ated with less drug–drug interactions. -
A New Robust Technique for Testing of Glucocorticosteroids in Dogs and Horses Terry E
Iowa State University Capstones, Theses and Retrospective Theses and Dissertations Dissertations 2007 A new robust technique for testing of glucocorticosteroids in dogs and horses Terry E. Webster Iowa State University Follow this and additional works at: https://lib.dr.iastate.edu/rtd Part of the Veterinary Toxicology and Pharmacology Commons Recommended Citation Webster, Terry E., "A new robust technique for testing of glucocorticosteroids in dogs and horses" (2007). Retrospective Theses and Dissertations. 15029. https://lib.dr.iastate.edu/rtd/15029 This Thesis is brought to you for free and open access by the Iowa State University Capstones, Theses and Dissertations at Iowa State University Digital Repository. It has been accepted for inclusion in Retrospective Theses and Dissertations by an authorized administrator of Iowa State University Digital Repository. For more information, please contact [email protected]. A new robust technique for testing of glucocorticosteroids in dogs and horses by Terry E. Webster A thesis submitted to the graduate faculty in partial fulfillment of the requirements for the degree of MASTER OF SCIENCE Major: Toxicology Program o f Study Committee: Walter G. Hyde, Major Professor Steve Ensley Thomas Isenhart Iowa State University Ames, Iowa 2007 Copyright © Terry Edward Webster, 2007. All rights reserved UMI Number: 1446027 Copyright 2007 by Webster, Terry E. All rights reserved. UMI Microform 1446027 Copyright 2007 by ProQuest Information and Learning Company. All rights reserved. This microform edition is protected against unauthorized copying under Title 17, United States Code. ProQuest Information and Learning Company 300 North Zeeb Road P.O. Box 1346 Ann Arbor, MI 48106-1346 ii DEDICATION I want to dedicate this project to my wife, Jackie, and my children, Shauna, Luke and Jake for their patience and understanding without which this project would not have been possible. -
Stems for Nonproprietary Drug Names
USAN STEM LIST STEM DEFINITION EXAMPLES -abine (see -arabine, -citabine) -ac anti-inflammatory agents (acetic acid derivatives) bromfenac dexpemedolac -acetam (see -racetam) -adol or analgesics (mixed opiate receptor agonists/ tazadolene -adol- antagonists) spiradolene levonantradol -adox antibacterials (quinoline dioxide derivatives) carbadox -afenone antiarrhythmics (propafenone derivatives) alprafenone diprafenonex -afil PDE5 inhibitors tadalafil -aj- antiarrhythmics (ajmaline derivatives) lorajmine -aldrate antacid aluminum salts magaldrate -algron alpha1 - and alpha2 - adrenoreceptor agonists dabuzalgron -alol combined alpha and beta blockers labetalol medroxalol -amidis antimyloidotics tafamidis -amivir (see -vir) -ampa ionotropic non-NMDA glutamate receptors (AMPA and/or KA receptors) subgroup: -ampanel antagonists becampanel -ampator modulators forampator -anib angiogenesis inhibitors pegaptanib cediranib 1 subgroup: -siranib siRNA bevasiranib -andr- androgens nandrolone -anserin serotonin 5-HT2 receptor antagonists altanserin tropanserin adatanserin -antel anthelmintics (undefined group) carbantel subgroup: -quantel 2-deoxoparaherquamide A derivatives derquantel -antrone antineoplastics; anthraquinone derivatives pixantrone -apsel P-selectin antagonists torapsel -arabine antineoplastics (arabinofuranosyl derivatives) fazarabine fludarabine aril-, -aril, -aril- antiviral (arildone derivatives) pleconaril arildone fosarilate -arit antirheumatics (lobenzarit type) lobenzarit clobuzarit -arol anticoagulants (dicumarol type) dicumarol -
A Thesis Entitled "APPLICATIONS of GAS CHROMATOGRAPHY
A Thesis entitled "APPLICATIONS OF GAS CHROMATOGRAPHY - MASS SPECTROMETRY IN STEROID CHEMISTRY" Submitted in part fulfilment of the requirements for admittance to the degree of Doctor of Philosophy in The University of Glasgow by T.A. Baillie, B.Sc. University of Glasgow 1973. ProQuest Number: 11017930 All rights reserved INFORMATION TO ALL USERS The quality of this reproduction is dependent upon the quality of the copy submitted. In the unlikely event that the author did not send a com plete manuscript and there are missing pages, these will be noted. Also, if material had to be removed, a note will indicate the deletion. uest ProQuest 11017930 Published by ProQuest LLC(2018). Copyright of the Dissertation is held by the Author. All rights reserved. This work is protected against unauthorized copying under Title 17, United States C ode Microform Edition © ProQuest LLC. ProQuest LLC. 789 East Eisenhower Parkway P.O. Box 1346 Ann Arbor, Ml 48106- 1346 ACKNOWLEDGEMENTS I would like to express my sincere thanks to Dr. C.3.W. Brooks for his guidance and encouragement at all times, and to Professors R.A. Raphael, F.R.S., and G.W. Kirby, for the opportunity to carry out this research. Thanks are also due to my many colleagues for useful discussions, and in particular to Dr. B.S. Middleditch who was associated with me in the work described in Section 3 of this thesis. The work was carried out during the tenure of an S.R.C. Research Studentship, which is gratefully acknowledged. Finally, I would like to thank Miss 3.H. -
Japanese Flavoring Agents As Food Additives
Japanese Flavoring Agents as Food Additives In Japan, synthetic flavoring agents are allowed to be used only when they are designated by the Minister of Health, Labour and Welfare as food additives under the Japanese Food Sanitation Act. Currently, we have identified 170 chemical substances which are commonly used as flavorings as shown in Table 1. Table 2 lists 18 groups which are also from the official list of “designated additives” and contain 3004 additional flavor materials. Each of the 18 groups in Table 2 contains substances that are similar in chemical structure. For links to a complete listing of the Japanese additives used in food: (a) Designated additives, (b) Existing food additives, (c) Natural flavoring agents and (d) Ordinary foods used as food additives - go to http://www.mhlw.go.jp/english/topics/foodsafety/foodadditives/index.html Check for Flavoring updates at http://www.jffma-jp.org/english/information.html Provided with Updated Revisions (as of April 2015) By Leffingwell & Associates Table 1. Designated additives used as flavoring substances Compound Synonym or Old name CAS Acesulfame Potassium 55589-62-3 Acetaldehyde (New as of 2006.05.16) ethanal 75-07-0 Acetophenone acetophenone 98-86-2 Acetic acid, Glacial 64-19-7 Adipic Acid 124-04-9 714229-20-6 Advantame (New as of 2015.02.20) 245650-17-3 DL-Alanine 302-72-7 Allyl cyclohexylpropionate allyl cyclohexanepropionate 2705-87-5 Allyl hexanoate allyl hexanoate 123-68-2 Allyl isothiocyanate allyl isothiocyanate 57503 (3-Amino-3-carboxypropyl)dimethylsulfonium chloride -
The Structural Biology of Oestrogen Metabolism
Journal of Steroid Biochemistry & Molecular Biology 137 (2013) 27–49 Contents lists available at ScienceDirect Journal of Steroid Biochemistry and Molecular Biology jo urnal homepage: www.elsevier.com/locate/jsbmb Review The structural biology of oestrogen metabolism ∗ Mark P. Thomas, Barry V.L. Potter Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK a r t i c l e i n f o a b s t r a c t Article history: Many enzymes catalyse reactions that have an oestrogen as a substrate and/or a product. The reac- Received 11 September 2012 tions catalysed include aromatisation, oxidation, reduction, sulfonation, desulfonation, hydroxylation Received in revised form and methoxylation. The enzymes that catalyse these reactions must all recognise and bind oestrogen but, 10 December 2012 despite this, they have diverse structures. This review looks at each of these enzymes in turn, describing Accepted 12 December 2012 the structure and discussing the mechanism of the catalysed reaction. Since oestrogen has a role in many disease states inhibition of the enzymes of oestrogen metabolism may have an impact on the state or Keywords: progression of the disease and inhibitors of these enzymes are briefly discussed. Oestrogen This article is part of a Special Issue entitled ‘CSR 2013’. Protein structure © 2012 Elsevier Ltd. Open access under CC BY license. Reaction mechanism Aromatase Sulfatase Sulfotransferase 17-Hydroxysteroid dehydrogenase Contents 1. Introduction . 27 2. Methods . 29 3. Oestrogen sulfotransferase . 29 4. Steroid sulfatase. 31 5. 17-Hydroxysteroid dehydrogenases . 33 6. Aromatase (cytochrome P450 19A1, oestrogen synthase) . 36 7. Enzymes of steroid hydroxylation . -
Impact of Wort Amino Acids on Beer Flavour: a Review
fermentation Review Impact of Wort Amino Acids on Beer Flavour: A Review Inês M. Ferreira and Luís F. Guido * LAQV/REQUIMTE, Faculdade de Ciências, Universidade do Porto, Rua do Campo Alegre, 687, 4169-007 Porto, Portugal; ines.fi[email protected] * Correspondence: [email protected]; Tel.: +351-220-402-644 Received: 3 March 2018; Accepted: 25 March 2018; Published: 28 March 2018 Abstract: The process by which beer is brewed has not changed significantly since its discovery thousands of years ago. Grain is malted, dried, crushed and mixed with hot water to produce wort. Yeast is added to the sweet, viscous wort, after which fermentation occurs. The biochemical events that occur during fermentation reflect the genotype of the yeast strain used, and its phenotypic expression is influenced by the composition of the wort and the conditions established in the fermenting vessel. Although wort is complex and not completely characterized, its content in amino acids indubitably affects the production of some minor metabolic products of fermentation which contribute to the flavour of beer. These metabolic products include higher alcohols, esters, carbonyls and sulfur-containing compounds. The formation of these products is comprehensively reviewed in this paper. Furthermore, the role of amino acids in the beer flavour, in particular their relationships with flavour active compounds, is discussed in light of recent data. Keywords: amino acids; beer; flavour; higher alcohols; esters; Vicinal Diketones (VDK); sulfur compounds 1. Introduction The process by which beer has been brewed has not changed significantly since its discovery over 2000 years ago. Although industrial equipment is used for modern commercial brewing, the principles are the same. -
Steroid Metabolites Support Evidence of Autism As a Spectrum
behavioral sciences Article Steroid Metabolites Support Evidence of Autism as a Spectrum Benedikt Andreas Gasser 1,*, Johann Kurz 2, Bernhard Dick 1,3 and Markus Georg Mohaupt 1,4 1 Department of Clinical Research, University of Bern, 3010 Berne, Switzerland; [email protected] (B.D.); [email protected] (M.G.M.) 2 Intersci Research Association, Karl Morre Gasse 10, 8430 Leibnitz, Austria; [email protected] 3 Division of Nephrology/Hypertension, University of Bern, 3010 Berne, Switzerland 4 Teaching Hospital Internal Medicine, Lindenhofgruppe, 3006 Berne, Switzerland * Correspondence: [email protected] Received: 30 March 2019; Accepted: 6 May 2019; Published: 9 May 2019 Abstract: Objectives: It is common nowadays to refer to autism as a spectrum. Increased evidence of the involvement of steroid metabolites has been shown by the presence of stronger alterations in Kanner’s syndrome compared with Asperger syndrome. Methods: 24 h urine samples were collected from 20 boys with Asperger syndrome, 21 boys with Kanner’s syndrome, and identically sized control groups, each matched for age, weight, and height for comprehensive steroid hormone metabolite analysis via gas chromatography–mass spectrometry. Results: Higher levels of most steroid metabolites were detected in boys with Kanner’s syndrome and Asperger syndrome compared to their matched controls. These differences were more pronounced in affected individuals with Kanner’s syndrome versus Asperger syndrome. Furthermore, a specific and unique pattern of alteration of androsterone, etiocholanolone, progesterone, tetrahydrocortisone, and tetrahydrocortisol was identified in boys with Kanner’s syndrome and Asperger syndrome. Interestingly, in both matched samples, only androsterone, etiocholanolone, progesterone, tetrahydrocortisone, tetrahydrocortisol, and 5a-tetrahydrocortisol groups were positively correlated. -
Mass Spec Testing for Steroid Hormone Profiles: Making an Impact on Patient Care
Mass Spec Testing for Steroid Hormone Profiles: Making an Impact on Patient Care R.J. Singh, Ph.D. Mayo Clinic Objectives •Congenital Adrenal Hyperplasia (CAH) •Sex Steroids •Cushing’s CAH New Born Screening 1 CAH CholesterolBiosynthesis of Steroids Pregnenolone 17- OH Pregnenolone DHEA ase ’ -----------------------------------------------------------------------------3SDH 17,20 desmolase 17 OH Progesterone 17-OH Progesterone Androstenedione 21 OH'ase 17b SDH ---------------------------------------------- Aromatase 21-Deoxycorti- 11-deoxycortisol Testosterone costerone 11 OH'ase Aromatase ---------------------------------------------- Estrone Corticosterone Cortisol Estradiol 17b SDH 18 OH'ase ---------------------- Cortisone --- Aldosterone STEROID PROFILE BY LC MS/MS TIC: from 051200-36 9.5e5 8 9.0e5 1. Cortisone 8.5e5 2. Cortisol, Cortisol d-4 8.0e5 3. 21-Deoxycortisol 4. Corticosterone 7.5e5 5. 11-Deoxycortisol 7.0e5 6. Androstendione 6.5e5 7. DOC 8. 17-Hydroxyprogesterone 6.0e5 17-Hydroxypregnenolone 5.5e5 9. Progesterone 5.0e5 10. Pregnenolone Intensity, cps 4.5e5 4.0e5 3.5e5 3.0e5 6 2.5e5 5 7 10 2.0e5 1.5e5 34 2 1.0e5 1 5.0e4 9 1.0 2.0 3.0 4.0 5.0 6.0 7.0 8.0 9.0 Time, min 6 2 Basics of MS Method Basics of MS Method Lack of Standardization 3 RIA vs. LC-MS/MS 14000 12000 10000 8000 6000 4000 Mayo LC/MS/MS ng/dL LC/MS/MS Mayo 2000 0 0 2000 4000 6000 8000 10000 12000 14000 Ext/RIA ng/dL Correlation Between Two Sites 4 Bland Altman Plot (N=76) 1000 + 2 SD = 801.4 500 + 1 SD = 405.8 Mean difference= 10.1 0 (ng/dL) - 1 SD = 385.6 -500