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Granisetron
HCl
API (DMF filed) |
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Haorui supplies high quality Granisetron HCl API produced by our
GMP facility that has been successfully inspected by the
FDA.
We offer
competitive prices and support our products with reliable technical and
regulatory services. Granisetron HCl API is available from R&D to
commercial quantities. Please contact us for more details. |
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Dolasetron
Granisetron
base Granisetron
HCl
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Palonosetron
Ramosetron
Tropisetron |
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The
following information is provided for general information
purposes ONLY.
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What
is Granisetron HCl?
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Granisetron HCl decreases nausea and vomiting caused by chemotherapy drugs. Granisetron may be called by its brand name, Kytril. Granisetron is sometimes prescribed for other uses.
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Granisetron
HCl chemical structure
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Granisetron
hydrochloride is an antinauseant and antiemetic agent.
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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). |
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Each
1 ml of preservative-free aqueous solution contains 1.12 mg
granisetron hydrochloride equivalent to granisetron, 1.0 mg
and sodium chloride, 9.0 mg. The solution's pH ranges from 4.7
to 7.3.
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What
is Granisetron appearance?
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Granisetron
hydrochloride is a white to off-white solid that is readily
soluble in water and normal saline at 20°C. Granisetron HCl
injection is a clear, colorless, sterile, nonpyrogenic,
aqueous solution for intravenous administration.
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How is Granisetron used?
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Granisetron
comes as a tablet and a solution (liquid) to take by mouth.
Granisetron may be taken with or without food. When taken to
prevent nausea and vomiting caused by chemotherapy, the first
dose of Granisetron usually is taken 1 hour before
chemotherapy is begunWhen taken to prevent nausea and vomiting
caused by radiation, Granisetron is usually taken within 1
hour before treatment. Follow the directions on your
prescription label carefully, and ask your doctor or
pharmacist to explain any part you do not understand. Take
Granisetron exactly as directed. Do not take more or less of
it or take it more often than prescribed by your doctor.
Granisetron injections are given by qualified health care
professionals.
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Potential
side effects with Granisetron
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Headache,
Constipation or diarrhea, Weakness or decreased energy,
Abdominal pain or stomach cramps, dizziness, drowsiness
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Special
precautions for taking Granisetron
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Before
taking granisetron, tell your doctor and pharmacist if you are
allergic to granisetron, dolasetron (Anzemet), ondansetron, (Zofran),
or any other medications.
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Tell
your doctor if you are pregnant, plan to become pregnant, or
are breast-feeding. If you become pregnant while taking
granisetron, call your doctor.
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How do I take
and store Granisetron?
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Granisetron
is injected into the veins. Granisetron may also be taken by
mouth with or without food
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How
do I store Granisetron?
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Granisetron
should be kept at room at temperature, away from heat and
light.
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What
if I miss a Granisetron dose?
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Take
the missed dose as soon as possible if you take granisetron on
a regular schedule and you skip or forget to take a dose by
mouth. If it is almost time for the next dose, do not take the
missed dose but return to your regular schedule. Do not
increase your dose to make up for a missed dose. If you take
granisetron only when needed, do not take more medication than
your doctor recommends.
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Granisetron
Pharmacokinetics
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In
adult cancer patients undergoing chemotherapy and in
volunteers, infusion of a single 40 mcg/kg dose of granisetron
HCl injection produced mean pharmacokinetic data.
Pharmacokinetic Parameters in Adult Cancer Patients
Undergoing Chemotherapy and in Volunteers, Single Intravenous
40 mcg/kg dose of Granisetron HCl Injection
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Granisetron
metabolism involves N-demethylation and aromatic ring
oxidation followed by conjugation. Animal studies suggest that
some of the metabolites may also have 5-HT3 receptor
antagonist activity.
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In
vitro liver microsomal studies show that granisetron's major
route of metabolism is inhibited by ketoconazole, suggestive
of metabolism mediated by the cytochrome P-450 3A subfamily.
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Plasma
protein binding is approximately 65% and granisetron
distributes freely between plasma and red blood cells.In
healthy volunteers and adult cancer patients undergoing
chemotherapy, administration of oral granisetron HCl produced
pharmacokinetic data. |
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Granisetron
clinical pharmacology
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Granisetron
is a selective 5-hydroxytryptamine3 (5-HT3) receptor
antagonist with little or no affinity for other serotonin
receptors.
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Animal
studies demonstrate that, in binding to 5-HT3receptors,
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 high-dose cisplatin or arrested vomiting
within 5 to 30 seconds. |
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In
most human studies, granisetron has had little effect on blood
pressure, heart rate or ECG. No evidence of an effect on
plasma prolactin or aldosterone concentrations has been found
in other studies. |
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Following
single and multiple oral doses, granisetron HCl slowed colonic
transit in normal volunteers. However, granisetron HCl had no
effect on oro-cecal transit time in normal volunteers when
given as a single intravenous (IV) infusion of 50 mcg/kg or
200 mcg/kg. |
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What
other information should I know about Granisrtron?
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Keep
all appointments with your doctor and the laboratory. Do not
let anyone else take your medication. Ask your pharmacist any
questions you have about refilling your prescription.
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Disclaimer:
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Information
on this page is provided for general information purposes. You
should not make a clinical treatment decision based on
information contained in this page without consulting other
references including the package insert of the drug, textbooks
and where relevant, expert opinion. We cannot be held
responsible for any errors you make in administering drugs
mentioned on this page, nor for use of any erroneous
information contained on this page.
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