NationMaster - Encyclopedia: Cimetidine

Cimetidine (INN) (IPA: [sɪˈmɛtədin, 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. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... An International Nonproprietary Name (INN) is the official non-proprietary or generic name given to a pharmaceutical substance, as designated by the World Health Organization. ... Articles with similar titles include the NATO phonetic alphabet, which has also informally been called the â€œInternational Phonetic Alphabetâ€. For information on how to read IPA transcriptions of English words, see IPA chart for English. ... An H2-receptor antagonist, often shortened to H2-antagonist, is a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. ... In anatomy, the stomach is a bean-shaped hollow muscular organ of the gastrointestinal tract involved in the second phase of digestion, following mastication. ... A benign gastric ulcer (from the antrum) of a gastrectomy specimen. ... GlaxoSmithKline plc (LSE: GSK NYSE: GSK) is a British based pharmaceutical, biological, and healthcare company. ... A trade name, also known as a trading name or a business name, is the legal name of a business, or the name which a business trades under for commercial purposes. ... The United States Food and Drug Administration (FDA) is the government agency responsible for regulating food (human and animal), dietary supplements, drugs (human and animal), cosmetics, medical devices (human and animal), biologics and blood products in the United States. ... is the 1st day of the year in the Gregorian calendar. ... Also: 1979 by Smashing Pumpkins. ...

Clinical use

Main article:H2-receptor antagonist An H2-receptor antagonist, often shortened to H2-antagonist, is a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. ...

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 (SK&F; now GlaxoSmithKline) to develop a histamine receptor antagonist to suppress stomach acid secretion. An H2-receptor antagonist, often shortened to H2-antagonist, is a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. ... GlaxoSmithKline plc (LSE: GSK NYSE: GSK) is a British based pharmaceutical, biological, and healthcare company. ... The histamine receptors are a class of G-protein coupled receptors with histamine as their endogenous ligand. ... Antagonists will block the binding of an agonist at a receptor molecule, inhibiting the signal produced by a receptor-agonist coupling. ...

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 SK&F scientists also proved the existence of histamine H₂-receptors. Also Nintendo emulator: 1964 (emulator). ... This article or section does not cite any references or sources. ... An H1 antihistamine is a histamine antagonist which serves to reduce or eliminate effects mediated by histamine, an endogenous chemical mediator released during allergic reactions, through action at the H1 receptor. ...

The SK&F 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 N^α-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 N^α-guanylhistamine, proved the existence of the H₂-receptor. Burimamide is an H2-receptor antagonist that is largely inactive at physiological pH. Clayden, J. Greeves, N. Warren, S. Wothers, P. (2001). ... A competitive antagonist is a receptor antagonist which binds to a receptor but fails to activate it. ...

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. In chemistry and biochemistry, acid dissociation constant, the acidity constant, or the acid-ionization constant () is a specific type of equilibrium constant that indicates the extent of dissociation of hydrogen ions from an acid. ... This article does not cite its references or sources. ... Nephrotoxicity is a poisonous effect of some substances, both toxins and medication, on the kidney. ... Thiourea is related to urea, where an oxygen atom is replaced by a sulfur atom. ... Guanidine is a crystalline compound of strong alkalinity formed by the oxidation of guanine. ...

Other uses

There have been two studies relating to the use of Cimetidine for treatment of warts in children. According to the studies, a daily dosage of 400mg of Cimetidine can remove over 200 warts from a 15 year old child.[1] Treatment may refer to: // Health Therapy - the act of remediation of a health problem. ... Wart is also the name of a Nintendo character, see Wart (Nintendo character). ... Dose can refer to: Dose (album), an album by the jam band Govt Mule Dose (song), a song by the band Filter Dose (magazine), a free daily Canadian magazine In medicine: Effective dose, the smallest amount of a substance required to produce a measurable effect on a living organism... A wart is generally a small, rough tumor, typically on hands and feet, that can resemble a cauliflower or a solid blister. ... For other uses, see Child (disambiguation). ...

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. [2] Lavage means washing. To lavage a joint means to wash out any blood, fluid or loose debris from inside the joint space Arthroscopic lavage is generally combined with arthroscopic debridement, where fronds of joint material or degenerative tissue are removed using a combination of injected fluid and a small vacuum...

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 result^{[citation needed]}. Adverse drug reactions were also found to be relatively common with Cimetidine, including interactions with the antimalarial medication Hydroxychloroquine^{[citation needed]}. Isozymes, (or isoenzymes) are isoforms (closely related variants) of enzymes. ... Cytochrome P450 Oxidase (CYP2E1) Cytochrome P450 oxidase (commonly abbreviated CYP) is a generic term for a large number of related, but distinct, oxidative enzymes (EC 1. ... This page is a candidate for speedy deletion. ... Cytochrome P450 2C9 (abbreviated CYP2C9), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. ... Cytochrome P450 2C19 (abbreviated CYP2C19), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. ... Cytochrome P450 2D6 (CYP2D6), a member of the cytochrome P450 mixed-function oxidase system, is one of the most important enzymes involved in the metabolism of xenobiotics in the body. ... Cytochrome P450 2E1 (abbreviated CYP2E1) (EC 1. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... A drug interaction is a situation in which a substance affects the activity of a drug, i. ... Hormonal contraception refers to birth control methods that act on the hormonal system. ... Estriol. ... Galactorrhea or galactorrhoea is the spontaneous flow of milk from the breast, unassociated with childbirth or nursing. ... Gynecomastia, or gynaecomastia, pronounced is the development of abnormally large mammary glands in males resulting in breast enlargement, which can sometimes cause secretion of milk. ... The sperm count is a measure of fertility in a man. ... An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ... Antimalarial drugs are designed to prevent or treat malaria. ... Hydroxychloroquine is an antimalarial also used to reduce inflammation and treat arthritis and lupus. ...

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 cautin is causes of hepatic impairment and cardiovascular disease^{[citation needed]}. Side effects can include dizziness, and more rarely, headache. Ranitidine (INN) (IPA: ) is a histamine H2-receptor antagonist that inhibits stomach acid production, and commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). ...

References

External links

Categories: All articles with unsourced statements | Articles with unsourced statements | Guanidines | H2 receptor antagonists | Imidazoles | Thioethers | Equine medications A benign gastric ulcer (from the antrum) of a gastrectomy specimen. ... Gastroesophageal Reflux Disease (GERD or GORD using the British Å“sophageal) is defined as chronic symptoms or mucosal damage produced by the abnormal reflux in the esophagus[1]. This is commonly due to transient or permanent changes in the barrier between the esophagus and the stomach. ... A division of the Anatomical Therapeutic Chemical Classification System A Alimentary tract and metabolism A02A Antacids A02AA Magnesium compounds A02AA01 Magnesium carbonate A02AA02 Magnesium oxide A02AA03 Magnesium peroxide A02AA04 Magnesium hydroxide A02AA05 Magnesium silicate A02AA10 Combinations A02AB Aluminium compounds A02AB01 Aluminium hydroxide A02AB02 Algeldrate A02AB03 Aluminium phosphate A02AB04 Dihydroxialumini sodium... An H2-receptor antagonist, often shortened to H2 antagonist, is a drug used to block the action of histamine on parietal cells in the stomach, decreasing acid production by these cells. ... Famotidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). ... Nizatidine is a histamine H2-receptor antagonist that inhibits stomach acid production, and commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). ... Ranitidine (INN) (IPA: ) is a histamine H2-receptor antagonist that inhibits stomach acid production, and commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD). ... Roxatidine acetate is a specific and competitive H2-receptor antagonist. ... E1 - Alprostadil I2 - Prostacyclin A prostaglandin is any member of a group of lipid compounds that are derived enzymatically from fatty acids and have important functions in the animal body. ... Synthetic prostaglandin analogues, mainly misoprostol, are used in treatment of duodenal and gastric ulcers. ... Misoprostol is a drug that is United States Food and Drug Administration (FDA)-approved for the treatment and prevention of stomach ulcers. ... Enprostil is a synthetic prostaglandin designed to resemble dinoprostone. ... Proton pump inhibitors (or PPIs) are a group of drugs whose main action is pronounced and long-lasting reduction of gastric acid production. ... Esomeprazole is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), GERD and Zollinger-Ellison syndrome. ... Lansoprazole (lan-SOE-pra-zole, INN) is a proton pump inhibitor which prevents the stomach from producing acid. ... Omeprazole (INN) (IPA: ) is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. ... Pantoprazole (brand names PantopanÂ® in Italy; ProtiumÂ®; ProtonixÂ®; PantozolÂ®; PantorÂ®; PantolocÂ®; Astropan) is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. ... Rabeprazole is an antiulcer drug in the class of proton pump inhibitors. ... Tenatoprazole (rINN, also benatoprazole) is a novel proton pump inhibitor registered for the treatment of reflux oesophagitis and peptic ulcer in Japan. ... Carbenoxolone, a synthetic derivative of glycyrrhizinic acid, is a licensed drug (in the UK) for oesophageal ulceration and inflammation. ... Sucralfate is a prescription medication used to treat peptic ulcers. ... This does not cite any references or sources. ...

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