Concise Dictionary of Pharmacological Agents Properties and Synonyms by Ian K.M. Morton King's College, London, United Kingdom and Judith M. Hall University of Surrey, Guildford, Surrey, United Kingdom KLUWER ACADEMIC PUBLISHERS DORDRECHT / BOSTON / LONDON Library of Congress Catalog Card Number: 98-67965. ISBN 075-1404-993 Published by Kluwer Academic Publishers, P.O. Box 17, 3300 AA Dordrecht, The Netherlands. Sold and distributed in North, Central and South America by Kluwer Academic Publishers, 101 Philip Drive, Norwell, MA 02061, U.S.A. In all other countries, sold and distributed by Kluwer Academic Publishers, P.O. Box 322, 3300 AH Dordrecht, The Netherlands. Printed on acid-free paper All Rights Reserved © 1999 Kluwer Academic Publishers No part of the material protected by this copyright notice may be reproduced or utilized in any form or by any means, electronic or mechanical, including photocopying, recording or by any information storage and retrieval system, without written permission from the copyright owner. Printed in the Netherlands. Introduction The purpose of this dictionary is to provide a convenient and affordable personal desk reference resource. The authors, who have many years experience in pharmacological research, teaching and editing, recognized a need for a single up-to-date volume encompassing material that hitherto could be gathered only from a well-stocked library. This book comprises two main sections: an A-Z listing of drugs and their properties; and a descriptive glossary of technical terms. The level and scope of this reference material will make it essential for pharmacologists and medicinal chemists, from the graduate student to established worker. It should also be valuable to workers in allied biomedical disciplines, such as biochemistry and physiology, medical students and science writers and editors. Scope The dictionary is centred on pharmacologically active agents. Workers in drug-related disciplines need to correctly identify individual agents from an arsenal of pharmacologically active compounds, each with a number of alternative drug names according to the country or naming convention. The A-Z Section contains details of individual drugs together with their alternative names (some 10,000 in all), classified into families according to mechanism and use. These families are the subject of descriptive articles (see below). Some of the drugs detailed here were developed for use in therapeutics, including most of those currently in clinical use (especially in the UK and USA), together with many formerly used in medicine, and some featuring in drug development programmes. Also listed are numerous agents - not themselves of therapeutic value - but important as pharmacological tools in the analysis of receptor recognition mechanisms and physiological or biochemical processes. Many compounds listed are of natural origin, including plant or animal alkaloids, antibiotics and toxins or venoms that can be used as 'chemical scalpels' in the analysis of mechanisms. The Glossary is a straightforward alphabetical reference source, explaining the meaning of some 3,000 biomedical terms. Researchers and writers in biomedical science need, at times, to understand the precise and accurate meaning of sometimes arcane terms. Collected here are definitions from pharmacology, biochemistry, molecular biology, immunology, pathology, physiology, anatomy and microbiology. We have given rather more explanation for terms that can cause confusion, for example, certain terms relating to drug receptors and to mediators, including autacoids, hormones and neurotransmitters. The rapidly evolving area of molecular biology is also covered. How to use this book The A-Z Section lists both names and families of pharmacologically active agents. Of the 10,000 cross-referenced names of these agents, about 4,000 entries are short descriptions of the properties and uses of agents under their main generic drug names. Where available, all official names are given. Main articles are listed alphabetically under British Approved Names [BAN], with United States Adopted Name [USAN] , Japanese Accepted Name [JAN] and International Non-proprietary Name [INN] also provided in brackets. Some types of agents, mainly pesticides, also have certain other standard names quoted, including American National Standards Institute [ANSI], British Standards Institution [BSI] and International Standards Organization [ISO]. Individual agent's entries also give the main alternative names, alternative spellings, abbreviations, chemical names, alternative chemical forms, company codes and main British and American proprietary names that are in current use. All name variants are cross-indexed (in bold type) to the main entries. The spelling of common medical and scientific terms is in British English rather than American English: thus oestrogen, not estrogen; haemoglobin, not hemoglobin; sulphonamide, not sulfonamide. This book provides a much-needed biological companion to encyclopaedic database references, such as the Merck Index and the Dictionary of Pharmacological Agents, which extensively detail full chemical names and much other chemical material. It might be noted that the classification of drugs into families corresponds fairly closely to the latter of these books (the pharmacology of which was also our responsibility). Drug family articles form the other component of the A-Z Section. Groupings of agents are described in some 300 short articles, each with references to further reading. Family grouping is by mechanism (e.g. (3-adrenoceptor antagonists) as well as by clinical application (e.g. antihypertensive agents); these cross-references are in BOLD SMALL CAPS. The Glossary (Appendix A) contains nearly 3,000 technical terms and acronyms, with coverage of most areas that are related to drug discovery, extending to trials and licensing. There is an emphasis on the specialized nomenclature of material related to drug receptors and molecular biology. Appendix B comprises three tables: amino acid abbreviations (common natural), amino acid abbreviations (found in literature - related and unnatural) and Greek and Latin multiplicative prefixes. This is the first edition of the work. The authors welcome (via the publishers) all criticisms, corrections and suggestions for material that might be covered in subsequent editions. IKMM & JMH King's College London & University of Surrey v This page has been reformatted by Knovel to provide easier navigation. Contents Introduction vii A – Z Section 1 A 301 - Azulfidine™ 2 A 301 - AN1 2 AN 448 - Antileishmanial Agents 17 Antileprotic Agents - Azulfidine ™ 32 B 306 - BZQ 45 C6 - Cytoxan™ 59 C6 - CEENU™ 59 Cefacetrile - Clidanac 69 Climaval™ - Cytoxan™ 79 D 138 - Dytide™ 90 'E' - EXPECTORANTS 107 F 2207 - FX 703 118 G/18 - Gynol™ 127 H 33 - Hytrin BPH™ 138 I 612 - Ivermectin 149 JB 11 - Kytril™ 158 3123L - Lyxoascorbic Acid 160 M 99 - Mytelase™ 171 N 0774 - Nytol™ 188 Obidoxime Chloride - Ozagrel 206 vi Contents This page has been reformatted by Knovel to provide easier navigation. P2S - PYY 213 P2S - Picenadol Hydrochloride 213 Picloxydine - Progynova ™ 222 Proheptazine - PYY 233 Qinghaosu - Quipazine M aleate 243 R200 - Rythmodan™ 244 S 46 - Syscor™ 251 T3 - Tyzine™ 267 U 4191 - UTP 284 Vadocaine - Vumon™ 287 W 108 - Zyprexa 293 Appendices 297 Appendix A. (Glossary) 297 A - CSF 298 CSF-1 - Infarction 307 Infection - Neurogenic 319 Neurogenic inflammation - Zwitterion 326 Appendix B. (Tables) 341 JlP^ JS** m #$№!%& <%&$$%& A 301 ^ norgestrienone. A 2774 •» delprostenate. A 3665 ~ trefentanil. A 4492 •» pentamorphone. A 4828 ^ trofosfamide. A 4942 ~ ifosfamide. A 5610 ~ azelastine. A 8103 ^ pipobroman. A 33547 •* remoxipride. A 46745 •* gestrinone. A 71623 is a substituted pentapeptide structure, a selective (CCK A -subtype) CHOLECYSTOKININ RECEPTOR AGONIST. It is an APPETITE SUPPRESSANT with low oral bioavailability, and is used as a pharmacological tool. AA 149 •» trepibutone. AA 673 ^ amlexanox. AA 861 ^ docebenone. AB 1404 •* ethchlorovynol Abbokinase™ •» saruplase; urokinase. Abbott 41070 •» gonadotrophin-releasing hormone. Abbott 43818 •» leuprorelin. Abbott 44090 •» valproic acid. Abbott 47631 •» estazolam. abciximab [BAN, USAN] (CentoRx™; ReoPro™) is a monoclonal antibody, a purified 47,615 dalton Fab fragment manufactured in mammalian cell culture. This antibody binds to the glycoprotein Ilb/IIIa (GPIIb/IIIa) receptors, members of the integrin family of adhesion receptors, and the major platelet surface receptor involved in platelet aggregation of human platelets. Acting through this mechanism, it is a PLATELET AGGREGATION INHIBITOR, and can be used parenterally as an ANTITHROMBOTIC AGENT (as an adjunct to heparin and aspirin), especially for the prevention and treatment of acute arterial occlusive disorders, including prevention of ischaemic complications in high-risk patients undergoing percutaneous transluminal coronary angioplasty. ablukast [INN, USAN] (ablukast sodium [USAN]) is a benzopyran derivative, a (LTC 4 ) LEUKOTRIENE RECEPTOR ANTAGONIST with potential as an ANTIASTHMATIC AGENT. ablukast sodium •» ablukast. AC *• ethotoin. AC 187 (acetyl-[Asn 30 ,Tyr 32 ]-salmoncalcitonin 8 .3 2 ) is an AMYLiN RECEPTOR ANTAGONIST that inhibits several metabolic actions of amylin. AC 223 ~ melinamide ABORTIFACIENTS are drugs used to induce abortion or miscarriage. A number of types of drug have been used, but commonly the PROGESTOGEN antagonist mifepristone is used (orally) and/or the prostaglandin gemeprost or dinoprostone (by the extra-amniotic route) (see PROSTANOID RECEPTOR AGONISTS) . A wide variety of the synthetic or natural agents, e.g. quinine, urea, ergot alkaloids, including ergotmetrine, and certain microbial toxins, may cause abortion (depending on dose and route of administration). See also LUTEOLYTIC AGENTS. Petrie, R.H. et al (1981) Maternal and fetal effects of uterine stimulants and relaxants. Diagn. Gynecol. Obstet., 3,111-117. Silvestre, L. et al (1990) Voluntary interruption of pregnancy with mifepristone (RU 486) and a prostaglandin analogue. A large-scale French experience N. Engl. J.Med., 322.645-648. Baulieu, E.E. (1995) The combined use of prostaglandin and antiprogestin in human fertility control. Adv. Prostaglandin. Thromboxane. Leukot. Res., 23, 55-62. ABT 077 •> zileuton. acadesine [BAN, INN] (GP 1-110) is a purine nucleoside analogue. It accumulates in the culture medium of E. coli under SULPHONAMIDE stasis, and is manufactured by Bacillus pumilus and Bacillus subtilis. It is being investigated for the management of myocardial ischaemia (it may act by influencing ischaemic cells to release adenosine, which has beneficial actions as a PLATELET AGGREGATION INHIBITOR) and also an ANTIARRHYTHMIC AGENT (with CARDIAC DEPRESSANT and VASODILATOR ACTIONS). acamprosate [BAN, INN] is related to taurine and is a GABA RECEPTOR AGONIST and PSYCHOTROPIC AGENT. It has been used in the treatment of alcoholism. acarbose [BAN, INN, USAN] (Bay g 5421; ct-GHI; Glucobay™) is an oligosaccharide isolated from the microorganisms of the Actinoplanes sp. It is an ENZYME INHIBITOR potently active against a-glucosidases and saccharases (a 'starch blocker'); and thereby delays conversion in the intestine of starch and sucrose to glucose, so slows its subsequent absorption. It can be used as an ANTIDiABETiC AGENT, usually as an adjunct to (sulphonylurea or biguanides) oral HYPOGLYCAEMICS in the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It can also be used in ANTIHYPERLIPIDAEMIC and obesity treatment. ACARICIDES are chemicals used to kill ticks and mites. Ticks belong to an order of the arthropods called Acarina, which also contains the mites; and chemicals used against the latter may be referred to as SCABICIDAL agents (or miticides in USA). Some ticks transmit other diseases (including Lyme disease, typhus and Rocky Mountain spotted fever), but they may themselves cause local irritation (e.g. in scabies caused by itch-mites Sarcoptes scabiei), and sometimes serious skin lesions and more general toxic manifestations, scabicidal drugs are used to kill the mites that cause scabies, in which the female mite tunnels into the top surface of the skin in order to lay eggs, causing severe irritation as she does so. Newly hatched mites, which also cause irritation with their secretions, then pass easily from person to person by direct contact; so every member of an infected household should be treated, and clothing and bedding should also be disinfected. Treatment is usually with local applications of a cream to kill the mites, but some agents can be irritant or have toxic manifestations; further resistance to many of these agents has developed in many ticks and mites. Acaricides that can, or have been used, include the halogenated hydro- carbons (e.g. dieldrin and lindane), organophosphorus compounds (e.g. malathion), carbamates (e.g.'carbaryl), pyrethroids (e.g. permethrin, phenothrin), and a number of other substances, including benzyl benzoate, crotamiton and monosulfiram. Some of these agents are also used as pediculicidal treatments against lice. Solomon, L.M. et al. (1977) Gamma benzene hexachloride toxicity: a review. Arch. Dermatol. 113. 353-357. Kunz, S.E. era/. (1994) Insecticides and acaricides: resistance and environmental impact. Rev. Sd. Tech. 13,1249-1286. Brown, S. et al. (1995) Treatment of ectoparasitic infections: review of the English-language literature, 1982-1992. Clin. Infect. Dis. 20 Suppl 1. S104-9. accelerator globulin •» factor V. Accolate™ * zafirlukast. Accupril™ •» quinapril. SMALL CAPS = drug families (by mechanism or application) bold = individual agents italic = Latin or Greek optical isomers; emphasis Accupro™ •tquinapril. AccuSite™ •» adrenaline; fluorouracil. Accutane™ ^ isotretinoin. acebutolol [BAN, INN, USAN] (acebutolol hydrochloride [JAN); Secadrex™; Sectral™) is a P-ADRENOCEPTOR ANTAGONIST showing p,-selectivity and some intrinsic (^- partial agonist activity, which is relatively lipophilic. It can be used therapeutically as an ANTIANGiNAL, ANTIARRHYTHMIC, and ANTIHYPERTENSIVE, and in ANTIGLAUCOMA TREATMENT. acebutolol hydrochloride •» acebutolol. aceclidine [INN, USAN] is an acetoxyquinuclidine analogue, a MUSCARINIC CHOLINOCEPTOR AGONIST and has been used in ANTIGLAUCOMA TREATMENT. acedapsone [BAN, INN, USAN] is a sulphone with ANTIMALARIAL and ANTILEPROTIC activity. aceglutamide [INNJAN] (acetylglutamine) has been given as a psychostimulant and NOOTROPiC AGENT in an attempt to improve memory and concentration. aceglutamide aluminium [JAN, USAN] (KW no) is an Al(III) complex, an ANTIULCEROGENIC AGENT and gastric cytoprotectant. ACE INHIBITORS (angiotensin-converting enzyme inhibitors) act by inhibiting the enzyme EC 3.4.15.1, variously known as angiotensin-converting enzyme (ACE), kininase II, dipeptidyl peptidase A. This peptidase, found in vascular endothelial cells and plasma, converts, by carboxyterminal dipeptidyl cleavage, the circulating vascular hormone angiotensin from its inactive decapeptide form angiotensin I, to the active octapeptide form, angiotensin II. Since angiotensin II is a very potent vasoconstrictor, the effect of ACE inhibitors is to cause vasodilatation with an overall hypotensive effect. Such drugs can be used as ANTIHYPERTENSIVES, and also in HEART FAILURE TREATMENT. However, drugs of this class have a number of side-effects (in particular an irritating cough), some of which can be attributed to the fact that ACE inhibitors necessarily prolong the duration of action of, and so potentiate, bradykinin. This sensory nerve activator and hypotensive hormone is degraded to an inactive dipeptidyl cleavage product by the same enzyme (in the kinin context commonly referred to as kininase II). ACE inhibitor drugs were developed by modelling interaction with the active site of the enzyme of a snake- venom-derived bradykinin-potentiating peptide, and from this the necessary structure of non-peptide inhibitors was inferred. The first such ACE inhibitor used medicinally was captopril. Later examples in clinical use include: cilazapril, enalapril, fosinopril, lisinopril, perindopril, quinapril, ramipril, trandolapril. Several ACE inhibitors are now administered clinically as prodrugs - which have good bioavailability, but are inactive in their own right. They are then converted to the active molecule in vivo, usually by esterases (e.g. enalapril to enalaprilat, and ramipril to ramiprilat). Petrillo, E.W. et al. (1982) Angiotensin-converting enzyme inhibitors: medicinal chemistry and biological actions. Med. Res. Rev., 2, 1-41. Ondetti, MA (1991) Angiotensin converting enzyme inhibitors: An overview. Hypertension Suppl. 3,18III134-III135. Leonetti, G. et al (1995) Choosing the right ACE inhibitor: A guide to selection. Drugs, 49, 516-535. Opie, L.H. et al (1995) The discovery of captopril: From large animals to small molecules. Cardiovasc. Res., W, 18-25. acemetacin [BAN, INN, JAN] (Bay f 4975; Emflex™) is the glycolic acid ester of indomethacin (to which it is partly converted in vivo). It is one of the indole acetic acid series of CYCLOOXYGENASE INHIBITORS with NSAID ANALGESIC and ANTHNFLAMMATORY activity. It has been used orally to treat serious pain and inflammation in rheumatic disease and other musculoskeletal disorders. acenocoumarol ~ nicoumalone. acetaminophen ~ paracetamol, acetarsol [INN] is a pentavalent organic arsenical, an antisyphilitic and ANTIPROTOZOAL used in veterinary practice. acetazolamide [BAN, INN, JAN, USAN] (acetazolamide sodium [USAN]; Diamox™) is a thiadiazolesulphonamide derivative with potent CARBONIC ANHYDRASE INHIBITOR activity. Clinically, it is used for ANTIGLAUCOMA TREATMENT. It is a weak DIURETIC. It can be used to treat mountain sickness. acetazolamide sodium •» acetazolamide. acethydroximic acid •» acetohydroxamic acid, acetohexamide [BAN, INNJAN, USAN] (Dimelor™) is one of the sulphonylurea (oral) HYPOGLYCAEMiCS. It can be used as an ANTIDIABETIC in non-insulin-dependent diabetes mellitus (NIDDM). Its active metabolite is hydroxyhexamide. acetohydroxamic acid [INN, USAN] (N-acetyl- hydroxylamine; N-hydroxyacetamide; acethydroximic acid; Lithostat™) is a UREASE INHIBITOR, reversibly acting on bacterial forms of the enzyme preventing formation of ammonia from urea. It is used in adjunctive therapy in chronic urease-splitting urinary tract infection. acetomenadione •» acetomenaphthone. acetomenaphthone [BAN] (acetomenadione; menadiol diacetate; vitamin K 4 diacetate) is a naphthoquinone, a diacetate salt of menadiol, a synthetic VITAMIN and an analogue of vitamin K. It can be used as a HAEMOSTATIC prothrombogenic agent to treat haemorrhagic states in cases of deficiency. It also has VASODILATOR properties. acetomorphin * diamorphine. acetonide ^desonide. p-acetophenetidide •» phenacetin. acetophetidin ~ phenacetin. acetorphan [INN, USAN] (Tiorfan™) is a mercapto-glycine derivative, a prodrug of thiorphan, a NEUTRAL ENDOPEPTI- DASE INHIBITOR ('enkephalinase' inhibitor). It has been used as an ANALGESIC in humans, and as an ANTIDIARRHOEAL. The (S)-form is ecadotril, the (/?)-form is dexecadotril [INN], and the racemic form is racecadotril [INN]. acetorphine [BAN, INN] (M 183; NIH 8074; UM 501) is a derivative of etorphine and member of the thebaine series. It is an OPIOID RECEPTOR AGONIST potent as an OPIOID ANALGESIC. acetosulfone sodium [USAN] (sulfadiasulfone sodium [INN]) is a SULPHONAMIDE with ANTIBACTERIAL activity. acetoxyprogesterone •» hydroxyprogesterone. N-acetyl-2-benzyltryptamine •» luzindole acetylcholine •*• acetylcholine chloride, acetylcholine chloride [BAN, INN, USAN] (acetylchoiine; Miochol™) is a quaternary ammonium choline ester. Acetylcholine itself occurs endogenously in cholinergic neurons. Also found in plants in complexed form (e.g. in ergot). It is a neurotransmitter in the peripheral autonomic and somatic nervous systems and in the CNS. It is a MUSCARINIC CHOLINOCEPTOR AGONIST that has PARASYMPATHO- MIMETIC actions; it is a CARDIAC DEPRESSANT, has peripheral VASODILATOR actions and is a HYPOTENSIVE AGENT. It is a stimulant of gut motility and exocrine gland secretions. It is a NICOTINIC CHOLiNOCEPTOR AGONIST and can stimulate autonomic ganglia and at the skeletal neuromuscular junction. It is quickly hydrolysed in vivo by cholinesterases, which limits its clinical uses, though administered anticholinesterases potentiate endogenous acetylcholine. It can be used on local application to the eye as a MiOTiC AGENT. acetylcysteine [BAN, INN, USAN] (llube™; Mucomyst™; SMALL CAPS = drug families (by mechanism or application) bold = individual agents italic = Latin or Greek; optical isomers; emphasis Parvolex™) is used a MUCOLYTIC AGENT, which reduces the viscosity of sputum, so can be used as an EXPECTORANT in patients with disorders of the upper respiratory airways, such as chronic asthma and bronchitis. It is also used orally to treat abdominal complications associated with cystic fibrosis, and locally in the eye to increase lacrimation and mucus secretion. It is also used intravenously as an ANTIDOTE in paracetamol poisoning. acetyldigitoxin [INN] is a CARDIAC GLYCOSIDE and derivative of digoxin with CARDIAC STIMULANT actions similar to other cardiac glycosides. acetyldihydrocodeinone •* thebacon. acetylglutamine ~ aceglutamide. N-acetylhydroxylamine •» acetohydroxamic acid. /V-acetyl-5-hydroxytryptamine •» NAS. N-acety(mescaline •» mescaline acetylmethadol •» dimepheptanol. N-acetyl-5-methoxytryptamine ~ melatonin. acetylsalicylamide •» salacetamide. acetylsalicylic acid •» aspirin. acetyl-[Asn so ,Tyr 32 ]-salmon calcitonin8-32 ^ AC 187 Achromycin™ •» tetracycline. aciclovir [BAN, INN, JAN] (acyclovir [USAN]; acyclovir sodium [USAN]; Zovirax™) is a synthetic nucleoside analogue ANTI- VIRAL. It can be used orally or topically to treat infection by the herpes viruses, and is valuable in immunocompromised patients. It is also used in the form of chemical derivatives. 'Acid' -ttysergide. acifran [INN, USAN] (AY 25712) is a furancarboxylic acid derivative, an ANTIHYPERLiPIDAEMIC AGENT. acipimox [BAN, INN] (K 9321; Olbetam™) is a pyrazinecarboxylic acid derivative, used as an ANTIHYPER- LIPIDAEMIC AGENT. acitretin [BAN, INN, USAN] (Ro 10-1670; Neotigason™) is a retinoid and metabolite of etretinate. It is a topical DERMATOLOGICAL AGENT that effects epithelial proliferation, and is used topically to relieve severe psoriasis and other skin conditions. It is also an ANTICANCER AGENT active against epithelial tumours. Aclacin™ •» aclarubicin. aclarubicin [BAN, INN, USAN] (MA 144A1; NSC 208734; antibiotic MA 144A1; Aclacin™) is an (anthracycline group) ANTIBIOTIC isolated from Streptomyces galilaeus, used as an ANTICANCER AGENT for leukaemia; it shows ANTI-HIV activity. aclatonium napadisylate [BAN, INNJAN] (celatonium napadisiiate; SKF 100916J; TM 723) is a choline ester, a MUSCARINIC CHOLINOCEPTOR AGONIST with PARASYMPATHOMI- METIC actions. It has been tested in gastrointestinal disorders. Aclovate™ •» alclometasone. Acnecide™ •» benzoyl peroxide. Acnegel™ * benzoyl peroxide. Acnisal™ ~ salicylic acid aconiazide [INN] is an isoniazid analogue and an ANTITUBERCULAR and ANTIBACTERIAL AGENT. aconitine is an alkaloid from monk's hood or wolfsbane (Aconitum napellus) and other Aconitum spp. (Ranunculaceae). It is a NEUROTOXIN implicated in poisoning by A. spp., especially A. chasmanthum in India. Experimen- tally, it is a SODIUM-CHANNEL ACTIVATOR that binds to Na + - channels, slows inactivation, shifts inactivation to a more negative value, and alters ion specificity. This results in repetitive firing of neurons, with marked effects on the heart including positive inotropism and arrhythmias. Aconitine (and the related alkaloid delphinine) were formerly used in medicine to promote sweating, and in liniments to relieve pain, but have proved too toxic so are now obsolete. It is used as a pharmacological tool. acrisorcin [INN, USAN] is an ANTIFUNGAL and ANTHELMINTIC. acrivastine [BAN, INN, USAN] (BW 825C; Semprex™) is a pyrrolidinyltolylpyridylacrylic acid derivative, a HiSTAMINE H 1 -RECEPTOR ANTAGONIST. It is one of the newer less sedative agents. It can be used orally for the symptomatic relief of allergic conditions, such as allergic rhinitis and urticaria. Ac-SDKP •» goralatide. Act a I™ •» alexitol ACTH •* corticotrophin. Acthar™ •» corticotrophin. Acthrel™ ^ corticotrophin-releasing factor. Actifed™ •» pseudoephedrine hydrochloride; triprolidine Actigall™ -» ursodeoxycholic acid Actilyse™ ^alteplase. Actimmune™ ^ interferon y. Actinac™ ^ chloramphenicol. Actinex™ ^ masoprocol actinomycin AIV •» dactinomycin. actinomycin B 1 ^ dactinomycin. actinomycin BIV •» dactinomycin. actinomycin C [BAN] (cactinomycin [INN, USAN]; S-67; antibiotic HBF 386; antibiotic S-67; NSC 18268) is a mixture of ANTIBIOTICS; actinomycin D, actinomycin C 2 and actinomycin C 3 . It is produced by Streptomyces chrysomallus. It has ANTIBACTERIAL activity against Gram-positive bacteria; and is also a cytotoxic agent active in ANTICANCER chemotherapy against tumours. No longer marketed. actinomycin C 1 ~ dactinomycin. actinomycin D ~ dactinomycin. actinomycin DIV •» dactinomycin. actinomycin Fo •» dactinomycin. actinomycin IV ^ dactinomycin. actinonin is a microbial product that is an ENZYME INHIBITOR With selectivity as an AMINOPEPTIDASE INHIBITOR active against aminopeptidase N (EC 3.4.11.2). It can be used as a pharmacological tool in experimental analytical studies. Activase™ -»alteplase. Acular™ •*> ketorolac trometamol. Acupan™ ^nefopam acyclovir •» aciclovir. acyclovir sodium ~ aciclovir. AD 810 ^ zonisamide AD 1590 •» bermoprofen. Adagen™ •» pegademase. Adalat™ -> nifedipine. adamexine [INN] is an adamantyl derivative, an ANTISPASMODIC and MUCOLYTIC AGENT, used in the treatment of respiratory tract disorders. Adamsite (DM; diphenylamine chloroarsine; phenarsazine chloride) is a toxic arsenical vesicant and SENSORY IRRITANT, used as war gas and riot-control agent. adapalene [BAN, INN, USAN] (CD 271; Differene™) is an adamantylnaphthoic acid derivative, a retinoid-like agent used as a topical DERMATOLOGICAL AGENT for mild to moderate acne, where it is a modulator of cell differentiation. Adapin™ -*doxepin adaprolol ^ adaprolol maleate. adaprolol maleate [USAN] (adaprolol [INN]) is a P-ADRENOCEPTOR ANTAGONIST. It can be used therapeutically as an ANTIHYPERTENSIVE. ADCA ^bisantrene SMALL CAPS = drug families (by mechanism or application) bold = individual agents italic = Latin or Greek; optical isomers; emphasis [...]... uricosuric but to decrease synthesis of uric acid The result of its action is a decrease in blood and tissues of the relatively insoluble xanthates and of xanthic acid, so there is less formation of renal stones, and some reversal of existing crystals in tissues It is also an inhibitor of ATP synthesis from guanine and of RNA biosynthesis; it has ANTITHROMBOTIC and antiparasitic activity alloxanthine... enhance anabolic effects and minimize others See ANABOLIC AGENTS Androgen antagonists are drugs that directly inhibit the actions of androgens, or indirectly inhibit production of androgens, and are also used in medicine See ANTIANDROGENS; AROMATASE INHIBITORS Mooradian, A.D et al (1987) Biological actions of androgens Endocr Rev., 8, 1-28 Swain, S.M., et al (1990) Endocrine therapies of cancer, in Cancer... Karchmer, A.W (1995) 'Cephalosporins', in Mandell, Douglas, and Bennett's Principles and Practice of Infectious Diseases, 4th edn, (eds G.L Mandell et al.), Churchill Livingstone, New York pp 247-263 Standiford, H.C (1995) Tetracyclines and chloramphenicol', in Mandell Douglas, and Bennet's Principles and Practice of Infectious Diseases, 4th edn, (eds G.L Mandell et al.), Churchill Livingstone, New... state often results from atheroma; a degeneration of the lining of the arteries of the heart due to build-up of fatty deposits The objective is to relieve the heart of work, and to prevent spasm or to dilate coronary arteries Unloading can be achieved by stopping exercise, preventing the speeding of the heart and by dilating the coronary arteries Beta-blockers, by inhibiting the effect of adrenaline and. .. permeability and transport of fungal membrane, allowing K+-loss; and is active systemically, but only against certain fungi and not bacteria Nystatin is a polyene macrolide antibiotic used to treat fungal infections of the skin and gastrointestinal tract Griseofulvin was isolated from cultures of Penicillium griseofulvum and was eventually developed as a narrowspectrum antifungal with fungistatic properties, ... inhibitor) and by its inhibitory action both on the adrenal cortex (cholesterol to D5-pregnenalone and other biosynthetic steps), and also on peripheral aromatase, blocks the production of adrenal steroids and conversion of androgens to oestrogens It produces a state of 'chemical adrenalectomy' and is used in ANTICANCER therapy, specifically for treatment of breast cancer in postmenopausal women and sometimes... Effects of differing rates of protamine reversal of heparin anticoagulation Surgery, 119,123-128 ANTICOAGULANTS are agents that prevent the clotting of blood Blood coagulation involves the conversion of fluid blood to a solid gel or a clot The formation of a clot contributes to the process of haemostasis (see HAEMOSTATICS) The formation of fibrin filament, together with the adhesion and activation of platelets,... and severity of the epilepsy For tonic-clonic seizures (Grand MaI) as part of a syndrome of primary generalized epilepsy the drugs of choice are carbamazepine and phenytoin For absence seizures (Petit MaI), sodium valproate and ethosuximide For myoclonic seizures, sodium valproate, clonazepam and ethosuximide For other types of seizure, such as atypical absence, atonic and tonic seizures (often in childhood),... ketoconazole and miconazole They work by blocking the synthesis of ergosterol, a major constituent of the fungal membrane, and are active against most fungi and yeasts They can be used to treat infections of the skin and mucous membranes, the hair and nails, including candidiasis and thrush Some may be used systemically, though there may be hepatotoxicity (e.g miconazole, isoconazole and ketoconazole)... ANTI-HIV AGENT and an inhibitor of related retroviruses It also has IMMUNOMODULATOR properties adefovir dipivoxil •» adefovir Adenic™ ~ adenosine adenine [JAN, USAN] (vitamin B4; 6-aminopurine) is a vitamin of the B group, and is widespread throughout animal and plant tissue It is a purine component of DNA, RNA, and coenzymes and biosynthetic intermediates It has ANTIVIRAL activity, and is used as . Concise Dictionary of Pharmacological Agents Properties and Synonyms by Ian K.M. Morton King's College, London, United Kingdom and Judith . sections: an A-Z listing of drugs and their properties; and a descriptive glossary of technical terms. The level and scope of this reference