Included in the formulation
АТХ:A.04.A.A Antagonists of serotonin 5HT3 receptors
A.04.A.A.05 Palonosetron
Pharmacodynamics:Has a high antagonistic activity against serotonin receptors. Suppresses the gag reflex due to blockade of serotonin 5HT3receptors at the level of neurons of the central and peripheral nervous system.
Warns and eliminates vomiting, provoked by chemo- and radiotherapy of malignant neoplasms.
Pharmacokinetics:With intravenous injection in the blood plasma, the concentration of the drug slowly decreases by elimination from the body. Half-distribution period is 40 hours.
The volume of distribution in the tissues is 6.9-7.9 l / kg. The connection with plasma proteins is 62%.
Elimination by the kidneys, about 50% in the form of metabolites, the activity of which is less than 1% of the activity of palonosetron.
After a single intravenous injection of palonosetron at a dose of 10 μg / kg, approximately 80% of the drug is found in the urine for 144 hours.
After a single bolus administration, the total clearance is 173 ± 73 ml / min, the renal clearance is 53 ± 29 ml / min. The half-life can be more than 100 hours (10% of patients).
Indications:It is used to prevent and elimination of vomiting caused by cytostatic radio or chemotherapy.
XVIII.R10-R19.R11 Nausea and vomiting
Contraindications:Individual intolerance.
Carefully:II-III trimester of pregnancy.
Pregnancy and lactation:Recommendations for FDA - Category B. Contraindicated in I trimester of pregnancy and lactation.
Dosing and Administration:Intravenously slowly (within 30 minutes) to 0.25 mg for 30 minutes before the start of chemotherapy.
The highest daily dose: 0.25 mg.
The highest single dose: 0.25 mg.
Side effects:Central and peripheral nervous system: headache, dizziness, drowsiness, euphoria, peripheral sensory neuropathy.
The cardiovascular system: tachycardia, supraventricular extrasystole, arterial hypertension.
Digestive system: anorexia, constipation, flatulence, hiccough.
Musculoskeletal system: arthralgia.
Dermatological reactions: itching, rash.
Sense organs: increased sensitivity of the eyes, amblyopia, diplopia, tinnitus.
Allergic reactions.
Overdose:Cases of overdose are not described.
Treatment is symptomatic.
Interaction:Clinically significant interactions are not described.
Special instructions:When taking the drug, patients should refrain from working with moving mechanisms and driving the car.