Granisetron
- Atc Codes:A04AA02
- CAS Codes:109889-09-0#107007-99-8
- PHARMGKB ID:109889-09-0#107007-99-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Granisetron, Granitron, Kytril; Belgium: Granisetron, Kytril; Bulgaria: Granisetron, Granitron, Kytril; Czech Republic: Emegar, Granegis, Granisetron, Kytril; Denmark: Granisetron, Kytril; Estonia: Granisetron, Kytril; Finland: Granisetron, Kytril; France: Granisetron, Kytril; Germany: Axigran, Granacta, Granichemia, GraniHexal, Granisetron, Kevatril, Kytril, Setravis; Greece: Dialgyl, Granisetron, Granitron, Granitryl, Kytril, Toribix; Hungary: Emegar, Gramegis, Granigen, Granisetron, Kytril; Ireland: Kytril; Italy: Granisetron, Kytril; Latvia: Granegis, Granisetron, Kytril; Lithuania: Granegis, Granisetron, Kytril; Luxembourg: Kytril; Malta: Granisetron, Kytril; Netherlands: Granisetron, Kytril; Poland: Granisetron; Portugal: Granisetron, Kytril; Romania: Granisetron, Kytril; Slovakia: Emegar, Granegis, Granisetron, Kytril, Rasetron; Slovenia: Granisetron, Kytril, Rasetron; Spain: Granisetron, Kytril; Sweden: Granisetron, Kytril; UK: Granisetron, Kytril.
North America
Canada: Granisetron, Kytril; USA: Granisetron, Kytril, Sancuso.
Latin America
Argentina: Granitron; Brazil: Granisetrona, Kytril; Mexico: Vogracen.
Asia
Japan: Granisetron, Kytril.
Drug combinations
Chemistry
Granisetron: C~18~H~24~N~4~O. Mw: 312.41. (1) 1H-Indazole-3-carboxamide, 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-, endo-; (2) 1-Methyl-N-(9-methyl-endo-9-azabicyclo[3.3.1]non-3-yl)-1H-indazole-3-carboxamide. CAS-109889-09-0 (1991).
Granisetron Hydrochloride: C~18~H~24~N~4~O HCl. Mw: 348.87. 1H-Indazole-3-carboxamide, 1-methyl-N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-, monohydrochloride, endo-. CAS-107007-99-8 (1992).
Pharmacologic Category
Antiemetics; 5-HT~3~ Receptor Antagonists. (ATC-Code: A04AA02).
Mechanism of action
Selective 5-HT~3~-receptor antagonist, blocking serotonin, both peripherally on vagal nerve terminals and centrally in chemoreceptor trigger zone.
Therapeutic use
Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including high-dose cisplatin. Prevention and treatment of postoperative nausea and vomiting. Prevention of nausea and vomiting associated with radiation, including total body irradiation and daily fractionated abdominal radiation.
Pregnancy and lactiation implications
There are no adequate, well-controlled studies in pregnant women. Teratogenic effects not observed in animal studies. Injection contains benzyl alcohol which may cross the placenta. Use only if benefit exceeds risk. Unknown whether drug is distributed into milk (caution if used in nursing women).
Unlabeled use
Contraindications
Previous hypersensitivity to granisetron, other 5-HT~3~ receptor antagonists, or any component of the formulation.
Warnings and precautions
Hypersensitivity reactions, including anaphylactic reaction, shortness of breath, hypotension, and urticaria, reported rarely. May mask progressive ileus and/or gastric distention. Allergic reactions possible. Dose-dependent increases in ECG intervals (e.g. PR, QRS duration, QT/QTc, JT) not clinically relevant; however, when used in conjunction with other agents that prolong these intervals, arrhythmia might occur. Use with caution in congenital long QT syndrome or other risk factors for QT prolongation (e.g. medications known to prolong QT interval, electrolyte abnormalities, and cumulative high-dose anthracycline therapy). Injection contains benzyl alcohol (risk of «gasping syndrome» in neonates). Mild application site reactions might occur with use of transdermal patch. For chemotherapy, should only be used in the first 24-48 hours.