Pharmaceutical and Veterinary Compounds and Metabolites
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Colitis Caused by Non-Steroidal Anti-Inflammatory Drugs
Postgrad Med J: first published as 10.1136/pgmj.62.730.773 on 1 August 1986. Downloaded from Postgraduate Medical Journal (1986) 62, 773-776 Colitis caused by non-steroidal anti-inflammatory drugs S. Ravi', A.C. Keat2 and E.C.B. Keat1 'Cuckfield Hospital, Cuckfield, West Sussex, and2Westminster Hospital, Horseferry Road, London SWIP2AP, UK. Summary: Four cases of acute proctocolitis associated with non-steroidal anti-inflammatory drug therapy are presented. The drugs implicated were flufenamic acid, mefenamic acid, naproxen and ibuprofen. After resolution of symptoms and signs of proctocolitis three of the four patients were subsequently rechallenged with the implicated drug: in each there was a rapid relapse. Introduction Ulcerative colitis is a disease of unknown aetiology Case reports with characteristic clinical features and a protracted course. A similar clinical picture, but running a shorter Case I and usually benign course, is occasionally seen follow- ing the administration of certain drugs. This was first A 77 year old woman was referred with intermittent noticed following the administration of antibiotics, bleeding per rectum for 6 months, associated for the often with pseudomembrane formation. Later, this last 2 months with bloody diarrhoea up to eight times was shown to be associated with infection by toxigenic daily. Previously, she had had troublesome symptoms Clostridium difficile. Until 1978, most cases were from osteoarthritis of her back and knees for which copyright. associated with treatment with clindamycin but since she had been prescribed flufenamic acid 200 mg thrice that time nearly all antibiotics have been implicated. daily. Her general health had remained good but she Other drugs capable of causing proctocolitis, though appeared pale and her haemoglobin was reduced to by different mechanisms, include phenindione (Keat & 8 g/dl. -
Testosterone, Or
COSI SIMILI, COSI DIVERSE 1. FOR A FEW ATOMS MORE: TESTOSTERONE AND DOPING A few days ago, the Tour de France winner, Floyd Landis, was found to have a high, indeed impermissible level of testosterone in his urine. Not quite, more of what was actually found in just a while. The sample was taken just after his comeback victory in a critical stage of bicycling’s premier race. If a second sample confirms the problem, Landis’s victory will be disallowed. Testosterone is the principal male sex hormone, produced mainly where… you might suspect from its name. And it is also produced in the ovaries of females. Testosterone is a so-called anabolic steroid, a class of molecules that give us a continuing lesson that almost the same is not the same. All the steroids, the class of molecules that include testosterone, have the same atomic framework – four all-carbon rings, fused together. Three are hexagons, the third ring going off at an angle to the other two. Fused to that last ring is a pentagon of carbon atoms. Call the rings A (6 carbons), B (6), C (6), D (5). Testosterone has an oxygen and a hydrogen (OH) attached to ring D, two CH3 (methyl) groups, one at the juncture of rings C and D, the other at the juncture of A and B. Finally ring A of testosterone has an oxygen attached to it as well, and there is a double bond in that ring. testosterone Testosterone is responsible for the secondary sex changes which occur in male puberty – facial and pubic hair, oiliness of skin, body odor, all that teenage boy stuff. -
Androgen Excess in Breast Cancer Development: Implications for Prevention and Treatment
26 2 Endocrine-Related G Secreto et al. Androgen excess in breast 26:2 R81–R94 Cancer cancer development REVIEW Androgen excess in breast cancer development: implications for prevention and treatment Giorgio Secreto1, Alessandro Girombelli2 and Vittorio Krogh1 1Epidemiology and Prevention Unit, Fondazione IRCCS – Istituto Nazionale dei Tumori, Milano, Italy 2Anesthesia and Critical Care Medicine, ASST – Grande Ospedale Metropolitano Niguarda, Milano, Italy Correspondence should be addressed to G Secreto: [email protected] Abstract The aim of this review is to highlight the pivotal role of androgen excess in the Key Words development of breast cancer. Available evidence suggests that testosterone f breast cancer controls breast epithelial growth through a balanced interaction between its two f ER-positive active metabolites: cell proliferation is promoted by estradiol while it is inhibited by f ER-negative dihydrotestosterone. A chronic overproduction of testosterone (e.g. ovarian stromal f androgen/estrogen balance hyperplasia) results in an increased estrogen production and cell proliferation that f androgen excess are no longer counterbalanced by dihydrotestosterone. This shift in the androgen/ f testosterone estrogen balance partakes in the genesis of ER-positive tumors. The mammary gland f estradiol is a modified apocrine gland, a fact rarely considered in breast carcinogenesis. When f dihydrotestosterone stimulated by androgens, apocrine cells synthesize epidermal growth factor (EGF) that triggers the ErbB family receptors. These include the EGF receptor and the human epithelial growth factor 2, both well known for stimulating cellular proliferation. As a result, an excessive production of androgens is capable of directly stimulating growth in apocrine and apocrine-like tumors, a subset of ER-negative/AR-positive tumors. -
Investigating the Influence of Polymers on Supersaturated
Page 1 of 45 Molecular Pharmaceutics 1 2 3 4 5 6 7 Investigating the Influence of Polymers on 8 9 10 11 12 Supersaturated Flufenamic Acid Cocrystal Solutions 13 14 15 16 1 1 2 2 1 17 Minshan Guo , Ke Wang , Noel Hamill , Keith Lorimer and Mingzhong Li * 18 19 20 1School of pharmacy, De Montfort University, Leicester, UK 21 22 23 2Almac Science, Seagoe Industrial Estate, Craigavon, UK 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 1 Molecular Pharmaceutics Page 2 of 45 1 2 3 4 5 6 7 Table of contents graphic 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 2 Page 3 of 45 Molecular Pharmaceutics 1 2 3 Abstract 4 5 6 7 The development of enabling formulations is a key stage when demonstrating the effectiveness 8 9 10 of pharmaceutical cocrystals to maximize the oral bioavailability for poorly water soluble drugs. 11 12 Inhibition of drug crystallization from a supersaturated cocrystal solution through a fundamental 13 14 understanding of the nucleation and crystal growth is important. In this study, the influence of 15 16 17 the three polymers of polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and a copolymer 18 19 of N-vinly-2-pyrrodidone (60%) and vinyl acetate (40%) (PVP-VA) on the flufenamic acid 20 21 22 (FFA) crystallization from three different supersaturated solutions of the pure FFA and two 23 24 cocrystals of FFA-NIC CO and FFA-TP CO has been investigated by measuring nucleation 25 26 induction times and desupersaturation rates in the presence and absence of seed crystals. -
Albany-Molecular-Research-Regulatory
PRODUCT CATALOGUE API COMMERCIAL US EU Japan US EU Japan API Name Site CEP India API Name Site CEP India DMF DMF DMF DMF DMF DMF A Abiraterone Malta • Benztropine Mesylate Cedarburg • Adenosine Rozzano - Quinto de' Stampi • • * Betaine Citrate Anhydrous Bon Encontre • Betametasone-17,21- Alcaftadine Spain Spain • • Dipropionate Sterile • Alclometasone-17, 21- Spain Betamethasone Acetate Spain Dipropionate • • Altrenogest Spain • • Betamethasone Base Spain Amphetamine Aspartate Rensselaer Betamethasone Benzoate Spain * Monohydrate Milled • Betamethasone Valerate Amphetamine Sulfate Rensselaer Spain * • Acetate Betamethasone-17,21- Argatroban Rozzano - Quinto de' Stampi Spain • • Dipropionate • • • Atenolol India • • Betamethasone-17-Valerate Spain • • Betamethasone-21- Atracurium Besylate Rozzano - Quinto de' Stampi Spain • Phosphate Disodium Salt • • Bromfenac Monosodium Atropine Sulfate Cedarburg Lodi * • Salt Sesquihydrate • • Azanidazole Lodi Bromocriptine Mesylate Rozzano - Quinto de' Stampi • • • • • Azelastine HCl Rozzano - Quinto de' Stampi • • Budesonide Spain • • Aztreonam Rozzano - Valle Ambrosia • • Budesonide Sterile Spain • • B Bamifylline HCl Bon Encontre • Butorphanol Tartrate Cedarburg • Beclomethasone-17, 21- Spain Capecitabine Lodi Dipropionate • C • 2 *Please contact our Accounts Managers in case you are interested in this API. 3 PRODUCT CATALOGUE API COMMERCIAL US EU Japan US EU Japan API Name Site CEP India API Name Site CEP India DMF DMF DMF DMF DMF DMF Dexamethasone-17,21- Carbimazole Bon Encontre Spain • Dipropionate -
Clomifene Citrate(BANM, Rinnm) ⊗
2086 Sex Hormones and their Modulators Profasi; UK: Choragon; Ovitrelle; Pregnyl; USA: Chorex†; Choron; Gonic; who received the drug for a shorter period.6 No association be- 8. Werler MM, et al. Ovulation induction and risk of neural tube Novarel; Ovidrel; Pregnyl; Profasi; Venez.: Ovidrel; Pregnyl; Profasi†. tween gonadotrophin therapy and ovarian cancer was noted in defects. Lancet 1994; 344: 445–6. Multi-ingredient: Ger.: NeyNormin N (Revitorgan-Dilutionen N Nr this study. The conclusions of this study were only tentative, 9. Greenland S, Ackerman DL. Clomiphene citrate and neural tube 65)†; Mex.: Gonakor. defects: a pooled analysis of controlled epidemiologic studies since the numbers who developed ovarian cancer were small; it and recommendations for future studies. Fertil Steril 1995; 64: has been pointed out that a successfully achieved pregnancy may 936–41. reduce the risk of some other cancers, and that the risks and ben- 10. Whiteman D, et al. Reproductive factors, subfertility, and risk efits of the procedure are not easy to balance.7 A review8 of epi- of neural tube defects: a case-control study based on the Oxford Clomifene Citrate (BANM, rINNM) ⊗ Record Linkage Study Register. Am J Epidemiol 2000; 152: demiological and cohort studies concluded that clomifene was 823–8. Chloramiphene Citrate; Citrato de clomifeno; Clomifène, citrate not associated with any increase in the risk of ovarian cancer 11. Sørensen HT, et al. Use of clomifene during early pregnancy de; Clomifeni citras; Clomiphene Citrate (USAN); Klomifeenisi- when used for less than 12 cycles, but noted conflicting results, and risk of hypospadias: population based case-control study. -
Androgenic and Anabolic Activities of Some Newly Synthesized Epiandrosterone and Progesterone Derivatives
Scientia Pharmazeutica (Sci. Pharm.) 68, 141-1 57 (2000) O Osterreichische Apotheker-Verlagsgesellschaft m. b. H, Wien, Printed in Austria Androgenic and Anabolic Activities of Some Newly Synthesized Epiandrosterone and Progesterone Derivatives. Y. A. ~aklaai"and M. M. ~osseir'~' Abstract Derivatives of eplandrosterone and progesterone were synthesized. The androgenic and the anabolic activities of some of tlieln were investigated on prepubertal male albino rats of 21 days old by:-i determining tlie weight gain of the body, levator ani muscle, ventral prostate gland, testis, selniilal vesicles, vas deferens and epididymis, ii- esti~natioi~of serum luteinizing (LH) hor~none,iii- liistopatliological examination of the testis and ventral prostate glands. The results from this study showed that the presence of an appended substituted 2- aminopyridine ring at the C- 17 of testosterone gave the maximuin a~idrogenicactivity, whereas the presence of a substituted piperidine ring fused to ring D of 5 a- androstane exhibited tlie maxiini~inanabolic activity. However, filsio~~of a pyrazoline moiety with the ring D of 5 a- androstane led to a compo~undwith considerable androgenic and anabolic act~v~ty. Keywords: epiandrosterone, progesterone, a~idrogenicactivity, anabolic activity, prepubertal rat, inale sex accessory glands, luteinizing horinone, I~istopatl~ology Introduction A~idrogensare a class of steroids responsible for tlie primary and secondary sex characteristics of the male. In addition, these steroids have bee11 found to possess potent anabolic promoting properties. The androgens are formed by the Leydig cells of the testis which is regulated by tlie gonadotropic luteinizing hormone (LH). The latter is secreted by tlie (J - cells of the anterior pitiltary gland under tlie control of the liypotlialainic gonadotropin - releasing l~oni~one.LH polypeptide -cliaiii is bioclie~nically unique and confers the LH biological and il~~~~~l~~~ologicnlspecificity "'". -
Chemical Compounds As Carcinogenic Agents Second Supplementary Report: Literature of 1938 and 1939 Biological Considerations
CHEMICAL COMPOUNDS AS CARCINOGENIC AGENTS SECONDSUPPLEMENTARY REPORT: LITERATURE OF 1938 AND 1939 J. W. COOK AND E. L. KENNAWAY (From the Royal Cancer Hospital (Free), London, and the University of Glasgow) BIOLOGICALCONSIDERATIONS (Continued from page 428, Jitly 1940) II. Action of Carcinogenic Compounds in Difierent Species and Tissues A number of reports of the action of carcinogenic compounds on human tis- sues have appeared. Klar (601) developed a nodule on the forearm after completion of a series of experiments with 3:4-benzpyrene. He applied a solution of the hydrocarbon (0.25 per cent in benzol) to the skin of mice with a paint brush and for at least part of the period wore rubber gloves. He also conducted experiments, of which no description is given, with the powdered hydrocarbon contained in a glass vessel. Three months after the completion of the experiments a small nodule appeared on the dorsum of the left forearm, This was excised in May 1938 and described by Professor Huckel as a “ so- called benign calcifying epithelioma.” The growth extended into the subcu- taneous fatty tissue; the connection with the superficial epithelium is not described nor is it evident in the two photomicrographs which illustrate the report. The author does not state his age. Gordonoff and Walthard (562) record the occurrence of a tumor in a labo- ratory assistant, aged forty-two, engaged in applying methylcholanthrene (0.3 per cent in benzol) to the skin of mice. The site was in the nasolabial fold, at a spot often touched by the patient when smoking. The microscopic ap- pearance was that of a “ still well delimited stage of an incipient squamous- cell sarcoma.” Cottini and Mazzone (479) deliberately applied 3 :4-benzpyrene ( 1 per cent in benzene) to the skin, generally of the arm or thigh, of 26 patients with various cutaneous diseases, usually daily for periods up to 120 days. -
Efficiency of Different Methods of Estrus Synchronization Followed by Fixed Time Artificial Insemination in Persian Downy Does
DOI: 10.21451/1984-3143-AR825 Anim. Reprod., v.14, n.2, p.413-417, Apr./Jun. 2017 Efficiency of different methods of estrus synchronization followed by fixed time artificial insemination in Persian downy does Majid Hashemi1, 2, 3, Mazaher Safdarian2 1Razi Vaccine and Serum Research Institute, Shiraz Branch, Agricultural Research, Education and Extension Organization (AREEO), Shiraz, Iran. 2Animal Science Research Department, Fars Agricultural and Natural Resource Research and Education Center, Agricultural Research, Education and Extension Organization (AREEO), Shiraz, Iran. Abstract estrus synchronization can play an important role for managing production system, allowing the density of For evaluating different methods of long term estrous mating and kidding and production of meat and milk synchronization followed by fixed time artificial during specific times of the year for strategic marketing insemination and to select the most efficient method, and other purposes (Baldassarre and Karatzas, 2004, during the breeding season 160 Persian downy does Zhao et al., 2010). In small ruminants, hormonal estrus were equally allocated to groups (n = 20/group). Estrus synchronization is achieved either by reducing the was synchronized using controlled internal drug release length of the luteal phase of the estrous cycle with devices alone (CIDR) or with equine chorionic prostaglandin F2α or by extending the cycle artificially gonadotropin (CIDR-eCG), intravaginal sponge with exogenous progesterone or more potent impregnated with 45 mg fluorgestone acetate alone progestagens (Hashemi et al., 2006, Abecia et al., (Sponge) or with eCG (Sponge-eCG), subcutaneous 2012). Progestogen administration is common and has auricular implant of 2 mg norgestomet alone (Implant) been used with or without accompanying treatments or with eCG (Implant-eCG) or two intramuscular such as gonadatropins or prostaglandin analogs. -
REVIEW Effects of Androgens on Cardiovascular Remodeling
1 REVIEW Effects of androgens on cardiovascular remodeling Yasumasa Ikeda1,2, Ken-ichi Aihara2, Sumiko Yoshida2, Masashi Akaike3 and Toshio Matsumoto2 Departments of 1Pharmacology, 2Medicine and Bioregulatory Sciences and 3Medical Education, The University of Tokushima, Graduate School of Health Biosciences, 3-18-15 Kuramoto-cho, Tokushima 770-8503, Japan (Correspondence should be addressed to K Aihara; Email: [email protected]) Abstract Androgens, the male sex hormones, exert various biological cardiovascular mortality. However, the influence of androgens effects on many target organs through the transcriptional effects on the cardiovascular system has not been fully elucidated. of the nuclear androgen receptor (AR). ARs are expressed not Toclarify this issue, we analyzed the effects of administration of only in classical target organs, such as the brain, genital organs, angiotensin II and doxorubicin, an anticancer agent, in a bone, and skeletal muscles, but also in the cardiovascular loading model in male wild-type and AR-deficient mice. In system. Because the female sex hormones estrogens are well- this review, we focus on the actions of androgens as potential known to protect against cardiovascular disease, sex has targets for the prevention of cardiovascular diseases in males. been considered to have a significant clinical impact on Journal of Endocrinology (2012) 214, 1–10 Introduction In addition, previous studies have shown that testosterone replacement tends to increase cardiovascular risk among Cardiovascular disease remains a major cause of death in both men of all ages (Calof et al. 2005, Haddad et al. 2007, womenandmenworldwideandappearstoincrease Fernandez-Balsells et al. 2010). On the other hand, recent morbidity and mortality in industrial countries. -
Criteria to Indicate Testosterone Administration
Br. J. Sp. Med; Vol 24, No. 4 Br J Sports Med: first published as 10.1136/bjsm.24.4.253 on 1 December 1990. Downloaded from Criteria to indicate testosterone administration A.T. Kicman1, R.V. Brooks2, S.C. Collyere, D.A. Cowan', M.N. Nanjee2, G.J. Southan2 and M.J. Wheelee 'Drug Control and Teaching Centre, King's College, London University 2Department of Chemical Pathology, UMDS, London University A detection method for testosterone administration was was found to increase after an intramuscular injection developed using radioimmunoassay to measure the of testosterone heptanoate in all ten normal males, urinary ratios of testosterone (T) to epitestosterone (E) and although there was an overlap between the basal to luteinizing hormone (LH). A comparative study of the range and that obtained three days after injection. effect on these ratios of a single intramuscular injection of testosterone heptanoate followed by stimulation with The method used was radioimmunoassay as protein human chorionic gonadotrophin (HCG) in three normal hormones cannot be measured by gas liquid chroma- men was undertaken. To allow immediate investigation, a tography-mass spectrometry (GLC-MS). commercially supplied epitestosterone antiserum was In 1983, the International Olympic Committee used. This study showed that both T/E and T/LH ratios (IOC) adopted the ratio of urinary testosterone to could be used to detect testosterone administration, the epitestosterone (T/E) as the sole test for testosterone latter also being an indicator of HCG use due to doping as both these hormones could be convenient- cross-reactivity with the LH antiserum. Subsequently, an ly measured by GLC-MS. -
Estradiol (E2), Estriol (E3), Ethinylestradiol (EE2), Testosterone (TEST), Androstenedione (AND), and Progesterone
UNIVERSITY OF CINCINNATI Date: 13-Aug-2010 I, Ruth Marfil Vega , hereby submit this original work as part of the requirements for the degree of: Doctor of Philosophy in Environmental Science It is entitled: Abiotic Transformation of Estrogens in Wastewater Student Signature: Ruth Marfil Vega This work and its defense approved by: Committee Chair: Makram Suidan, PhD Makram Suidan, PhD George Sorial, PhD George Sorial, PhD Margaret Kupferle, PhD, PE Margaret Kupferle, PhD, PE Marc Mills, PhD Marc Mills, PhD 11/8/2010 1,041 Abiotic Transformation of Estrogens in Wastewater A Dissertation submitted to the Graduate School of the University of Cincinnati in partial fulfillment of the requirements for the degree of Doctor of Philosophy In the School of Energy, Environmental, Biological and Medical Engineering By Ruth Marfil-Vega B.S. Chemistry, University of Valladolid, Spain, 2001 Committee Chair: Makram T. Suidan, Ph.D. ABSTRACT The fate of seven steroids: estrone (E1), estradiol (E2), estriol (E3), ethinylestradiol (EE2), testosterone (TEST), androstenedione (AND), and progesterone (PROG), in the presence of synthetic wastewater was studied in order to establish the role abiotic processes play in the elimination of these chemicals from the environment. Comprehension of these mechanisms will foster the optimization of the existing wastewater treatment technologies and the development of sustainable alternatives. Distinctive behavior was encountered for the target compounds in accordance with their chemical structure, hence, different physico-chemical properties and reactivity. Estrogenic compounds, comprising E1, E2, E3 and EE2, were found to undergo a catalytic transformation when contacted with a model vegetable material present in the synthetic wastewater.