GRANISETRON HYDROCHLORIDE tablet film coated

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

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

Disponível em:

Avera McKennan Hospital

DCI (Denominação Comum Internacional):

Granisetron Hydrochloride

Composição:

Granisetron 1 mg

Tipo de prescrição:

PRESCRIPTION DRUG

Status de autorização:

Abbreviated New Drug Application

Características técnicas

GRANISETRON HYDROCHLORIDE- GRANISETRON HYDROCHLORIDE TABLET, FILM
COATED
AVERA MCKENNAN HOSPITAL
----------
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 vomiting within