Granisetron concentrates 1 mg/ml 3 ml, 5 pcs.
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Granisetron is a selective antagonist of serotonin (5-hydroxytryptamine) 5-NT3 receptors located in the vagus nerve endings and trigger zone of the bottom of the IV ventricle of the brain (has almost no effect on other serotonin receptors) with a pronounced antiemetic effect.
Studies have shown that granisetron has low affinity for other types of receptors, including other types of serotonin receptors and D2-dopamine receptors. It eliminates vomiting resulting from excitation of the parasympathetic nervous system due to serotonin release by enterochromaffin cells.
Granisetron eliminates nausea and vomiting caused by cytotoxic chemotherapy, radiation therapy, and postoperative nausea and vomiting.
It does not affect plasma concentrations of prolactin and aldosterone.
Granisetron blocks potassium hERG channels of the heart, affecting myocardial repolarization. On the electrocardiogram (ECG) indices it is manifested in changes of PR, QRS and especially in prolongation of QT interval.
It has no mutagenic effect in vivo and in vitro.
When administered in high doses for a lifetime it increases the risk of hepatocellular tumors in animals.
Indications
Prevention of nausea and vomiting during cytostatic chemotherapy in adults.
The prevention and treatment of nausea and vomiting during radiation therapy in adults.
Active ingredient
Granisetron
Composition
1 ml of concentrate for preparation of solution for infusion:
The active ingredient:
granisetron hydrochloride 1.42 mg, which corresponds to the content of granisetron 1 mg
Associates:
Sodium chloride – 9 mg,
citric acid monohydrate – 2 mg, <
d/i water – up to 1 ml,
Hydrochloric acid – q.s.,
Sodium hydroxide – q.s.
How to take, the dosage
Adults, for oral administration, a single dose of 1 mg; for intravenous infusion, a single dose of 3 mg; for intravenous injection (slowly, not less than 30 seconds), a single dose of 1 mg.
The maximum dose is 9 mg/day.
In children, 40 mcg/kg (but not more than 3 mg) once by IV/ IV drip. For children over 12 years of age, a single dose of 1 mg for oral administration.
The frequency and duration of use are determined individually.
Interaction
Granisetron does not affect the activity of CYP3A4 isoenzyme (responsible for metabolism of some narcotic analgesics). The efficacy of granisetron may be enhanced by intravenous administration of dexamethasone (8-20 mg) prior to chemotherapy.
In vitro studies have shown that ketoconazole inhibits the metabolism of granisetron, which suggests the participation of CYP3A subfamily isoenzymes.
There have been no special studies on interaction with general anesthesia agents, but granisetron is well tolerated when used simultaneously with such drugs and narcotic analgesics.
In induction of “hepatic” enzymes with phenobarbital the clearance of granisetron (when administered intravenously) was increased by about one fourth.
No interaction was found when concomitant use with benzodiazepines (e.g., lorazepam), tranquilizers, neuroleptics (e.g., haloperidol), anti-ulcer drugs from the group of H2-histamine receptor blockers (e.g., cimetidine) and cytostatic drugs that cause vomiting.
In patients receiving concomitant therapy with drugs with known ability to prolong the QT interval and/or arrhythmogenic activity, the observed changes on ECG during therapy with granisetron may lead to clinically significant consequences.
As with other serotonin 5-NT3 receptor antagonists, cases of serotonin syndrome (including changes in mental state, autonomic dysfunction and nervous and muscular system disorders) have been reported when using granisetron in combination with other serotonergic drugs.
Special Instructions
Patients with signs of partial intestinal obstruction should be under medical supervision after the drug administration, since the drug may decrease intestinal motility.
Granisetron is safe for use in elderly patients and patients with renal or hepatic insufficiency.As with
other serotonin 5-NT3 receptor antagonists, changes in ECG parameters, including cases of QT interval prolongation, have been reported during granisetron therapy. These changes were not significant and, as a rule, had no clinical significance, in particular no evidence of proarrhythmogenic action.
However, in patients with pre-existing arrhythmias or diseases accompanied by cardiac conduction abnormalities, the observed changes in ECG parameters during granisetron therapy may lead to clinically significant consequences. Therefore, caution should be exercised when using the drug in patients with concomitant cardiac diseases receiving cardiotoxic chemotherapy and/or having concomitant electrolyte imbalances.
Cases of cross-sensitivity development between serotonin 5-NT3 receptor antagonists have been reported.
The patient’s condition should be monitored if it is clinically necessary to concomitantly use granisetron with other serotonergic drugs.
Patients with rare hereditary galactose intolerance, lactase deficiency, or glucose-galactose absorption disorders are not recommended to use the drug.
Influence on the ability to drive vehicles, mechanisms
There are no data on the effect of the drug on the ability to drive vehicles. However, caution should be exercised taking into account that the drug therapy was reported on occurrence of drowsiness and dizziness.
In case of these symptoms patients are advised to refrain from driving and other potentially dangerous activities that require high concentration and quick psychomotor reactions.
Contraindications
- high sensitivity to granisetron or any of the drug components in the history;
- hypersensitivity reactions to other selective serotonin 5-NT3 receptor antagonists in the history;
- breastfeeding;
- children under 12 years of age (there is insufficient data to establish an optimal dosing regimen in this age group).
Side effects
In most cases, adverse reactions when using granisetron were not severe and were tolerated by patients without interruption of therapy.
Rare and sometimes severe cases of hypersensitivity (e.g., anaphylaxis) were noted.
Immune system disorders: hypersensitivity reactions, such as skin rash, hyperthermia, bronchospasm, urticaria, itching.
Nervous system disorders: headache, insomnia, drowsiness, weakness, anxiety, anxiety, dizziness, serotonin syndrome (including changes in mental status, autonomic dysfunction and disorders of the nervous and muscular systems), extrapyramidal disorders.
Cardiovascular system: prolongation of the QT interval, arrhythmias, chest pain, decreased or increased blood pressure.
As with the use of other serotonin 5-NT3 receptor antagonists, there have been reports of electrocardiogram (ECG) parameter changes during granisetron therapy, including cases of QT interval prolongation. These changes were not significant and, as a rule, had no clinical significance, in particular, there were no signs of proarrhythmogenic action.
Digestive system disorders: constipation, abdominal pain, diarrhea, flatulence, increased “liver” transaminases activity (alanine aminotransferase (ALT), aspartate aminotransferase (AST)) usually within the normal values, dyspepsia, heartburn, change of taste.
Skin and subcutaneous fat: skin rash, edema, including facial edema.
Body in general: flu-like syndrome, including fever and chills.
Pregnancy use
Safety of treatment with granisetron during pregnancy has not been established, therefore its use is possible only in cases of extreme necessity. Breast-feeding should be discontinued if it is necessary to use during lactation.
Weight | 0.064 kg |
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Manufacturer | R-Pharm AO, Russia |
Medication form | solution for infusion |
Brand | R-Pharm AO |
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