Kytril (granisetron) solution
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Nausea and vomiting associated with cancer therapy
General Information
Subjects receiving chemotherapy and radiation therapy can suffer
from severe nausea and vomiting as side effects to cancer
treatment. Kytril solution has been approved for the prevention of
nausea and vomiting associated with initial and repeat courses of
cancer therapy, including high-dose cisplatin, and nausea and
vomiting associated with radiation, including total body
irradiation and fractionated abdominal radiation. Kytril is
currently available in both tablet and injection formulations.
Kytril works by blocking the serotonin 5-HT3 receptor. When a
subjects receives chemotherapy, the hormone serotonin is released
by cells in the small intestine. Serotonin acts on the vagus nerve
to trigger nausea and vomiting. Kytril reduces this effect by
blocking receptors on the vagus nerve, reducing detrimental
stimulation by serotonin.
Side Effects
Adverse events reported in clinical trials with Kytril tablets
or Kytril injection include (but are not limited to) the
following:
- Headache
- Constipation
- Asthenia (weakness)
- Diarrhea
- Abdominal pain
- Dyspepsia (indigestion)
- Somnolence (sleepiness)
Mechanism of Action
Granisetron is a selective 5-hydroxytryptamine3 (5-HT3) receptor
antagonist with little or no affinity for other serotonin
receptors, including 5-HT1; 5-HT1A; 5-HT1B/C; 5-HT2; for alpha1-,
alpha2-, or beta-adrenoreceptors; for dopamine-D2; or for
histamine-H1; benzodiazepine; picrotoxin or opioid receptors.
Serotonin receptors of the 5-HT3 type are located peripherally
on vagal nerve terminals and centrally in the chemoreceptor trigger
zone of the area postrema. During chemotherapy that induces
vomiting, mucosal enterochromaffin cells release serotonin, which
stimulates 5- HT3 receptors. This evokes vagal afferent discharge,
inducing vomiting. Animal studies demonstrate that, in binding to
5-HT3 receptors, granisetron blocks serotonin stimulation and
subsequent vomiting after emetogenic stimuli such as cisplatin.
(from Kytril Product Information)
Additional Information
