Kytril
Kytril - General Information
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients. [PubChem]
Pharmacology of Kytril
Not Available
Kytril for patients
Kytril Interactions
Kytril Contraindications
KYTRIL is contraindicated in patients with known hypersensitivity to the drug or any of its components.
Additional information about Kytril
Kytril Indication: For the prevention of: nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin.
Mechanism Of Action: Kytril is a potent, selective antagonist of 5-hydroxytryptamine (serotonin) subtype 3 (5-HT 3) receptors. 5-HT 3 receptors are present peripherally on vagal nerve terminals and centrally in the area postrema of the brain. Cytotoxic drugs and radiation damage gastrointestinal mucosa, causing the release of serotonin from the enterochromaffin cells of the gastrointestinal tract. Stimulation of 5-HT 3 receptors causes transmission of sensory signals to the vomiting center via vagal afferent fibers to induce vomiting. By binding to 5-HT 3 receptors, granisetron blocks vomiting mediated by serotonin release. Kytril has little or no affinity for other serotonin receptors, including 5-HT 1, 5-HT 1A, 5-HT 1B/C, or 5-HT 2 ; for alpha 1 -, alpha 2 -, or beta-adrenoreceptors; for dopamine D 2 receptors; for histamine H 1 receptors; for benzodiazepine receptors; for picrotoxin receptors; or for opioid receptors. In most human studies, granisetron has had little effect on blood pressure, heart rate, or electrocardiogram (ECG).
Drug Interactions: Not Available
Food Interactions: Take without regard to meals.
Generic Name: Granisetron
Synonyms: Granisetron hydrochloride; Granisetronum [INN-Latin]; Granisetron base; Granisetron HCl
Drug Category: Antiemetics; Serotonin Antagonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Granisetron: Kytril;
Absorption: Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.
Toxicity (Overdose): LD50>2000 mg/kg (rat, oral)
Protein Binding: 65%
Biotransformation: Primarily hepatic; undergoes N -demethylation and aromatic ring oxidation followed by conjugation. Animal studies suggest that some of the metabolites may have 5-HT 3 receptor antagonist activity.
Half Life: 4-6 hours in healthy patients, 9-12 hours in cancer patients
Dosage Forms of Kytril: Tablet Oral
Liquid Intravenous
Chemical IUPAC Name: 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]nonan-7-yl)indazole-3-carboxamide
Chemical Formula: C18H24N4O
Granisetron on Wikipedia: https://en.wikipedia.org/wiki/Granisetron
Organisms Affected: Humans and other mammals
