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20-September-2008 09:55:57 - Cimetidine Cimetidine Systematic IUPAC name 1-cyano-2-methyl-3-2-5-methyl-1H-imidazol-4-yl methylsulfanylethylguanidine Identifiers CAS number 51481-61-9 ATC code A02BA01 PubChem 2756 DrugBank APRD00568 Chemical data Formula C10H16N6S Mol. mass 252.34 g/mol Pharmacokinetic data Bioavailability 60-70% Protein binding 15-20% Metabolism Hepatic Half life 2 hours Excretion Renal Therapeutic considerations Licence data US Pregnancy cat. B1AU BUS Legal status Prescription Only S4AU POMUK OTC/â„ž-only U.S., dose-dependent Routes Oral, parenteral Cimetidine INN pronounced /sɨˈmÉ›tɨdiË?n/, /saɪ-/ is a histamine H2-receptor antagonist that inhibits the production of acid in the stomach. It is largely used in the treatment of heartburn and peptic ulcers. It is marketed by GlaxoSmithKline under the trade name Tagamet sometimes Tagamet HB or Tagamet HB200 and was approved by the Food Drug Administration for prescriptions starting January 1, 1979. Contents 1 Clinical use 2 History and development 3 Other uses 4 Shortcomings and side effects 5 Notes 6 References 7 External links Clinical use Main article:H2-receptor antagonist History and development Cimetidine was the prototypical histamine H2-receptor antagonist from which the later members of the class were developed. Cimetidine was the culmination of a project at Smith, Kline French SKF; now GlaxoSmithKline to develop a histamine receptor antagonist to suppress stomach acid secretion. This was one of the first drugs discovered using a rational drug design approach, thanks to the valiant efforts of medicinal chemists C. Robin Ganellin and Graham Durant and pharmacologist James Black at Smith, Kline, French Laboratoriesnow GlaxoSmithKline; Sir James W. Black shared the 1988 Nobel Prize in Physiology or Medicine for the discovery of propranolol and also is cred for the discovery of this drug; actually, the medicinal chemists would have made the discovery. The Organic Chemistry of Drug Design and Drug Action, Richard B. Silverman, page 159 At the time 1964 it was known that histamine was able to stimulate the secretion of stomach acid, but also that traditional antihistamines had no effect on acid production. In the process, the SKF scientists also proved the existence of histamine H2-receptors. The SKF team used a rational drug-design structure starting from the structure of histamine - the only design lead, since nothing was known of the then hypothetical H2-receptor. Hundreds of modified compounds were synthesised in an effort to develop a model of the receptor. The first breakthrough was Nα-guanylhistamine, a partial H2-receptor antagonist. From this lead the receptor model was further refined and eventually led to the development of burimamide, the first H2-receptor antagonist. Burimamide, a specific competitive antagonist at the H2-receptor 100-times more potent than Nα-guanylhistamine, proved the existence of the H2-receptor. Burimamide was still insufficiently potent for oral administration and further modification of the structure, based on modifying the pKa of the compound, lead to the development of metiamide. Metiamide was an effective agent, however it was associated with unacceptable nephrotoxicity and agranulocytosis. It was proposed that the toxicity arose from the thiourea group, and similar guanidine-analogues were investigated until the ultimate discovery of cimetidine. Cimetidine was first marketed in the United Kingdom in 1976; therefore, it took 12 years from initiation of the H2-receptor antagonist program to commercialization. Subsequent to the introduction onto the U.S. drug market, two other H2-receptor antagonists were approved, ranitidine Zantac, Glaxo Labs and famotidine Pepcid, Yamanouchi, Ltd. Cimetidine became the first drug ever to reach more than $1 billion a year in sales, thus making it the first blockbuster drug.1 Other uses A number of open label studies showed that cimetidine was effective in the treatment of common warts, but more rigorous double-blinded clinical trials showed it to be no more effective than a placebo. 2 Another study by Yokoyama et al used Cimetidine for the treatment of Chronic Calcifying Tendonitis of the shoulder. The small scale study took 16 individuals with calcifying tendonitis in one shoulder, all of which had previously attempted other forms of therapy including steroid injection and arthroscopic lavage. During the course of the study 10 patients reported an elimination of pain and 9 displayed a complete disappearance of Calcium deposits. With results being on a small scale, it has been recommended that Cimetidine, for the treatment of chronic calcifying tendonitis of the shoulder, be opened to large scale clinical trials. 1 Cimetidine has also been reported for use in treatment of colorectal cancer - it is however not approved in the US by the FDA for cancer treatment. Shortcomings and side effects Cimetidine is a known inhibitor of many isozymes of the cytochrome P450 enzyme system specifically CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4. This inhibition forms the basis of the numerous drug interactions that occur between cimetidine and other drugs. For example, cimetidine may decrease metabolism of some drugs, such as those used in hormonal contraception. Cimetidine interferes with metabolism of the hormone estrogen, enhancing estrogen activity. In women, this can lead to galactorrhea, whereas in men gynecomastia and a reduced sperm count can resultcitation needed. Adverse drug reactions were also found to be relatively common with Cimetidine, including interactions with the antimalarial medication Hydroxychloroquinecitation needed. The development of longer-acting H2-receptor antagonists with reduced adverse effects such as ranitidine proved to be the downfall of cimetidine and, whilst it is still used, it is no longer amongst the more widely used H2-receptor antagonists. Cimetidine should be used with caution in cases of hepatic impairment and cardiovascular diseasecitation needed. Side effects can include dizziness, and more rarely, headache. Notes ^ Whitney, Jake February 2006. Pharmaceutical Sales 101: Me-Too Drugs, Guernica. Retrieved on 2008-07-31. ^ Ann Pharmacother. 2007 Jul;417:1222-6. Epub 2007 May 29 References Michnovicz JJ, Galbraith RA .Cimetidine inhibits catechol estrogen metabolism in women. Metabolism. 1991 Feb;402:170-4. PMID 1988774 The Organic Chemistry of Drug Design and Drug Action, Richard B. Silverman 3.2G Case History of Rational Drug Design of a Receptor Antagonist: Cimetidine. Pages 159-165 External links American Chemical Society - National Historic Chemical Landmarks - Tagamet: A medicine that changed people's lives Tagamet HB200 v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 v d e Drugs for acid related disorders: Drugs for peptic ulcer and GERD/GORD A02B H2 antagonists Cimetidine, Famotidine, Lafutidine, Niperotidine, Nizatidine, Ranitidine, Roxatidine Prostaglandins/analogues Misoprostol, Enprostil Proton pump inhibitors Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole, Rabeprazole, Tenatoprazole Other Carbenoxolone, Cetraxate, Sucralfate, Pirenzepine, Troxipide Retrieved from http://en..org/wiki/Cimetidine Categories: Guanidines | H2 receptor antagonists | Imidazoles | Thioethers | Equine medicationsHidden categories: All articles with statements | Articles with statements since December 2007 Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Deutsch Español Français Hrvatski Italiano Nederlands 日本語 Polski Português Suomi ไทย Türkçe ä¸æ–‡ This page was last modified on 3 August 2008, at 23:2
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