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Tegaserod
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| Systematic (IUPAC) name | |
| 2-((5-Methoxy-1H-indol-3-yl)methylene)-N-pentylhydrazinecarboximidamide | |
| Identifiers | |
| CAS number | |
| ATC code | A03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C16H23N5O |
| Mol. mass | 301. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug ATC code A03 is a division of the Anatomical Therapeutic Chemical Classification System and part of the A Alimentary tract and metabolism section PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 39 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | 10% |
| Protein binding | 98% |
| Metabolism | Gastric and hepatic |
| Half life | 11 ± 5 hours |
| Excretion | Fecal and renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
Withdrawn |
| Routes | Oral |
Tegaserod is a 5-HT4 agonist manufactured by Novartis and used for the management of irritable bowel syndrome and constipation. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of A drug's efficiency may be affected by the degree to which it binds to the proteins within Blood plasma. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems In Human anatomy, the stomach is a J-shaped hollow muscular organ of the Gastrointestinal tract involved in the second phase of Digestion, following The liver is a vital organ in the human body and is present in Vertebrates and some other animals The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during For a topic outline on this subject see List of basic Australia topics. The United States of America —commonly referred to as the The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons An agonist is a term used to describe a type of ligand or drug that binds and alters the activity of a receptor. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine In Gastroenterology, irritable bowel syndrome ( IBS) is a Functional bowel disorder characterized by mild to severe Abdominal pain, discomfort Constipation, costiveness, or irregularity, is a condition of the Digestive system in which a person (or animal experiences hard Feces that [1] Its use was the only drug approved by the United States Food and Drug Administration to help relieve the abdominal discomfort, bloating and constipation associated with irritable bowel syndrome. The United States of America —commonly referred to as the In Vertebrates such as Mammals the abdomen (belly constitutes the part of the body between the Thorax (chest and Pelvis. Bloating is any abnormal general Swelling, or increase in diameter of the abdominal area Its use was also approved to treat chronic idiopathic constipation. Idiopathic is an Adjective used primarily in Medicine meaning arising spontaneously or from an obscure or unknown cause. [2] It is currently marketed by Novartis under the trade names Zelnorm and Zelmac in the United States and abroad, respectively. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine
The drug functioned as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. Motility is a biological term which refers to the ability to move spontaneously and actively consuming energy in the process The enteric nervous system ( ENS) is a subdivision of the Peripheral Nervous System, that directly controls the Gastrointestinal system. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. In the Esophagus After food is chewed into a bolus it is swallowed to move it into the esophagus [3]
Withdrawal from market
On March 30, 2007, the U. Events 240 BC - 1st recorded Perihelion passage of Halley's Comet. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. S. Food and Drug Administration requested that Novartis withdraw Zelnorm from shelves. The FDA alleges a relationship between prescriptions of the drug and increased risks of heart attack or stroke. [4] An analysis of data collected on over 18,000 patients demonstrated adverse cardiovascular events in 13 of 11,614 patients treated with Zelnorm (a rate of 0. 11%) as compared with 1 of 7,031 patients treated with placebo (a rate of 0. 01%). Novartis states all of the affected patients had preexisting cardiovascular disease or risk factors for such, and further states that no causal relationship between tegaserod use and cardiovascular events has been demonstrated. [5] On the same day as the FDA announcement, Novartis Pharmaceuticals Canada announced that it was suspending marketing and sales of the drug in Canada in response to a request from Health Canada. Health Canada ( French: Santé Canada) is the department of the government of Canada with responsibility for national Public health [6] Some manufacturers in India, such as Cipla, seem to still have generic Tegaserod available in their listings[7] and some online merchants may be selling it. Cipla, originally founded as The Chemical Industrial & Pharmaceutical Laboratories is a prominent Indian Pharmaceutical company, best-known outside
References
- ^ New Data for Zelnorm. Retrieved on March 30, 2007.
- ^ FDA approves first treatment for women with irritable-bowel syndrome. Retrieved on March 30, 2007.
- ^ Rossi, S. (2004). Australian Medicines Handbook. Adelaide: Health Communication Network. ISBN ISBN 0-9578521-4-2.
- ^ Constipation drug pulled at FDA request. Retrieved on March 30, 2007.
- ^ Zelnorm. Novartis. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine Retrieved on 2007-03-30. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 240 BC - 1st recorded Perihelion passage of Halley's Comet.
- ^ Novartis suspends Canadian marketing and sales of Zelnorm in response to request from Health Canada. Health Canada ( French: Santé Canada) is the department of the government of Canada with responsibility for national Public health Retrieved on 2007-03-30. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 240 BC - 1st recorded Perihelion passage of Halley's Comet.
- ^ Cipla - Product List
http://hc-sc.gc.ca/dhp-mps/medeff/advisories-avis/public/2007/zelnorm_pc-cp_2_e.html
External links
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