Description
Pharmacological action
Antiemetic. Selective antagonist of serotonin 5HT3 receptors. It stops vomiting that occurs when the parasympathetic nervous system is excited due to the release of serotonin by enterochromaffin cells.
Pharmacokinetics of
After iv administration in doses of 20 Ојg / kg or 40 Ојg / kg, the average Cmax in blood plasma is 13.7 Ојg / L and 42.8 Ојg / L, respectively.
Plasma Protein Binding – 65%.
Metabolized rapidly by demethylation and oxidation.
T1 / 2 is 3.1-5.9 hours. In cancer patients, T1 / 2 rises to 10-12 hours. It is excreted in the urine and feces, mainly in the form of conjugates, 8-15% is found in the urine unchanged.
Indications
Prevention and treatment of nausea and vomiting during chemotherapy with cytostatics.
Prevention and treatment of postoperative nausea and vomiting.
Contraindications
Hypersensitivity to granisetron.
Use during pregnancy and lactation
The safety of treatment with granisetron during pregnancy has not been established, therefore the use is possible only in cases of emergency. If necessary, use during lactation should stop breastfeeding.
Special instructions
Use with caution in case of symptoms of bowel obstruction.
Granisetron is not used for the treatment and prevention of postoperative nausea and vomiting in children.
Composition
Concentrate for preparation of solution for infusion transparent, colorless.
1 ml
granisetron hydrochloride 1.42 mg,
which corresponds to the content of granisetron 1 mg
Excipients: sodium chloride – 9 mg, citric acid monohydrate – 2 mg, water d / i – up to 1 ml, hydrochloric acid – qs, sodium hydroxide – qs
* Used, if necessary, in the technological process to adjust the pH value 5.3 ± 0.3.
Dosage and administration of
For adults, a single dose for oral administration is 1 mg, for intravenous infusion a single dose is 3 mg, for intravenous injection (slowly, for at least 30 sec) a single dose is 1 mg.
The maximum dose is 9 mg / day.
In children in the drip once – 40 mcg / kg (but not more than 3 mg). Children over 12 years of age for oral administration of a single dose – 1 mg.
Multiplicity and duration of use are set individually.
Side effects
Possible: transient increase in hepatic transaminase activity in the blood, constipation, headache, skin rash.
Active ingredient
Granisetron
Terms of delivery from
pharmacies Prescription
Dosage form
infusion solution