chemical structure of granisetron
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Kytril

Granisetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main affect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. 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. more...

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Granisetron was invented by chemists working at the British drug company Beecham around 1988 and is expected to go generic in 2007/2008. It is produced by Roche Laboratories under the trade name Kytril®. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA.

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.

Clinical Uses

  • Chemotherapy-induced nausea and vomiting
    • 5-HT3 receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. 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.

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.

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SKB sells Kytril to Roche; Famvir, Vectavir/Denavir to Novartis - Brief Article - Statistical Data Included
From Drug Store News, 9/25/00

SmithKline Beecham has signed two agreements for the divestitures of Kytril, SKB's antiemetic drug for chemotherapy, radiotherapy and post-operative associated nausea and vomiting, and the antivirals Famvir and Vectavir/Denavir. The divestitures are being undertaken to secure regulatory approval for SKB's merger with Glaxo Wellcome, which markets the antiemetic Zofran for chemotherapy and the antivirals Zovirax and Valtrex.

SKB and Roche have signed an agreement for Roche to acquire global rights to Kytril for $1.23 billion in cash. At the same time, SKB will pay Roche $400 million in cash for exclusive U.S. and Canadian rights for Coreg, the drug for congestive heart failure. SKB is currently in a co-promotion agreement with Roche to market Coreg in the United States. In 1999, U.S. sales of Coreg were $196 million.

In a separate agreement, Novartis will acquire global rights to the antivirals Famvir, indicated for the treatment of acute herpes zoster and herpes simplex, and Vectavir/Denavir, for the treatment of herpes labialis, from SKB for $1.63 billion in cash.

COPYRIGHT 2000 Lebhar-Friedman, Inc.
COPYRIGHT 2000 Gale Group

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