Kytril Indication:

For the prevention of: nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin.

Kytril 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).

Kytril Drug Interactions:

Not Available

Kytril Food Interactions:

Take without regard to meals.

Kytril Generic Name:

Synonyms:

  • Granisetron hydrochloride
  • Granisetronum [INN-Latin]
  • Granisetron base
  • Granisetron HCl

Drug Type:

Small Molecule; Approved

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

Organisms Affected:

Humans and other mammals

Kytril to general, pharmacology

General, pharmacology..