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Granisetron
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| Systematic (IUPAC) name | |
| 1-methyl-N-(9-methyl-9-azabicyclo[3. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general 3. 1]non-3-yl)- indazole-3-carboxamide |
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| Identifiers | |
| CAS number | |
| ATC code | A04 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C18H24N4O |
| Mol. mass | 312. 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 A04 is a division of the Anatomical Therapeutic Chemical Classification System and is part of the A Alimentary tract and metabolism. 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 41 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 60% |
| Protein binding | 65% |
| Metabolism | Hepatic |
| Half life | 3–14 hours |
| Excretion | Renal 11–12%, faecal 38% |
| Therapeutic considerations | |
| Pregnancy cat. |
B1 (Au), |
| Legal status |
S4 (Au), POM (UK), ℞-only (U. 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 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 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 regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located S. ) |
| Routes | Oral, intravenous |
Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. In Pharmacology and Toxicology, a route Serotonin (ˌsɛrəˈtoʊnən ( 5-hydroxytryptamine, or 5-HT) is a Monoamine Neurotransmitter synthesized in serotonergic Neurons The 5-HT3 antagonists are a class of Medications which act as Receptor antagonists at the 5-hydroxytryptamine-3 receptor (5-HT3 receptor An anti-emetic is a drug that is effective against Vomiting and Nausea. Nausea ( Latin: Nausea, Greek:, " Sea-sickness " also called wamble) is the sensation of unease and discomfort Vomiting (also called throwing up, emesis) is the forceful expulsion of the contents of one's Stomach through the Mouth and sometimes the Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. The vagus nerve (ˈveɪˌgəs (VĀ-gəs (also called pneumogastric nerve or cranial nerve X) is the tenth of twelve paired Cranial nerves, and is the The medulla oblongata is the lower portion of the Brainstem. It deals with autonomic functions such as breathing and blood pressure It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors. Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates Muscarinic receptors, or mAChRs, are Acetylcholine receptors that form Metabotropic Ion channels in the Plasma membranes of certain
Granisetron was developed by chemists working at the British drug company Beecham around 1988 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. F Hoffmann–La Roche Ltd is a Swiss global health-care company which operates world-wide under two divisions Pharmaceuticals and Diagnostics. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA. The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located The United States of America —commonly referred to as the
Granisetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys. The liver is a vital organ in the human body and is present in Vertebrates and some other animals The kidneys are complicated organs that have numerous biological roles
Contents |
Indications
- Chemotherapy-induced nausea and vomiting
- 5-HT3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. Chemotherapy, in its most general sense refers to treatment of disease by chemicals that kill cells specifically those of micro-organisms or Cancer. Many times they are given intravenously about 30 minutes before beginning therapy.
- Post-operative and post-radiation nausea and vomiting
- Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis
- Treatment of Cyclic vomiting syndrome although there are no formal trials to confirm efficacy. Gastroenteritis (also known as gastro, gastric flu, and stomach flu, although unrelated to Influenza) is Inflammation of the Cyclic vomiting syndrome (US English or cyclical vomiting syndrome (UK English ( CVS) is a condition whose Symptoms are recurring attacks of intense
Adverse effects
Granisetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipations are the most commonly reported side effects associated with its use. There have been no significant drug interactions reported with this drug's use. It is broken down by the liver's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system. The liver is a vital organ in the human body and is present in Vertebrates and some other animals Cytochrome P450 (abbreviated CYP, P450, infrequently CYP450) is a very large and diverse superfamily of Hemoproteins found in all Domains
External links
References
- Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9
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