GRANISETRON HYDROCHLORIDE- granisetron hydrochloride tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

Granisetron Hydrochloride (UNII: 318F6L70J8) (Granisetron - UNII:WZG3J2MCOL)

Available from:

Taro Pharmaceuticals U.S.A., Inc.

INN (International Name):

Granisetron Hydrochloride

Composition:

Granisetron 1 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Granisetron hydrochloride USP is indicated for the prevention of: - Nausea and vomiting associated with initial and repeat courses of emetogenic cancer therapy, including high-dose cisplatin. - Nausea and vomiting associated with radiation, including total body irradiation and fractionated abdominal radiation. Granisetron hydrochloride USP is contraindicated in patients with known hypersensitivity to the drug or any of its components.

Product summary:

Granisetron Hydrochloride Tablets USP, 1 mg are available as: 1 mg, round, white, film coated tablets, embossed with "T" on one side and "G1" on the other side. Bottle of 20 tablets – NDC 51672-4138-6 Bottle of 100 tablets – NDC 51672-4138-1 Unit Dose of 100 (10 ×10) – NDC 51672-4138-0 Store between 20° and 25°C (68° and 77°F) [see USP Controlled Room Temperature]. Keep container closed tightly. Protect from light. Advise patients of the possibility of serotonin syndrome with concomitant use of granisetron and another serotonergic agent such as medications to treat depression and migraines. Advise patients to seek immediate medical attention if the following symptoms occur: changes in mental status, autonomic instability, neuromuscular symptoms with or without gastrointestinal symptoms.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

GRANISETRON HYDROCHLORIDE- GRANISETRON HYDROCHLORIDE TABLET, FILM
COATED
TARO PHARMACEUTICALS U.S.A., INC.
----------
GRANIS ETRON
HYDROCHLORIDE
TABLETS USP, 1 MG
RX ONLY
DESCRIPTION
Granisetron Hydrochloride Tablets USP contain granisetron
hydrochloride USP, an antinauseant and
antiemetic agent. Chemically it is _endo_-N-(9-methyl-9-azabicyclo
[3.3.1] non-3-yl)-1-methyl-1H-
indazole-3-carboxamide hydrochloride with a molecular weight of 348.9
(312.4 free base). Its
empirical formula is C
H N O•HCl, while its chemical structure is:
Granisetron hydrochloride USP is a white to off-white solid that is
readily soluble in water and normal
saline at 20°C.
Each round, white, film coated granisetron hydrochloride tablet USP
contains 1.12 mg granisetron
hydrochloride USP equivalent to granisetron, 1 mg. Inactive
ingredients are: hypromellose 2910,
lactose monohydrate, magnesium stearate, microcrystalline cellulose,
opadry white YS-1-7003
(hypromellose, polyethylene glycol, polysorbate 80 and titanium
dioxide) and sodium starch glycolate.
CLINICAL PHARMACOLOGY
Granisetron is a selective 5-hydroxytryptamine (5-HT ) receptor
antagonist with little or no affinity for
other serotonin receptors, including 5-HT ; 5-HT
; 5-HT
; 5-HT ; for alpha
, alpha
, or beta-
adrenoreceptors; for dopamine-D ; or for histamine-H ; benzodiazepine;
picrotoxin or opioid
receptors.
Serotonin receptors of the 5-HT 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-HT receptors. This evokes
vagal afferent discharge, inducing vomiting. Animal studies
demonstrate that, in binding to 5-HT
receptors, granisetron blocks serotonin stimulation and subsequent
vomiting after emetogenic stimuli
such as cisplatin. In the ferret animal model, a single granisetron
injection prevented vomiting due to
18
24
4
3
3
1
1A
1B/C
2
1-
2-
2
1
3
3
3
high-dose cisplatin or arrested vomiti