Included in the formulation
Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):ONLS
АТХ:A.04.A.D Other antiemetic drugs
A.04.A.D.12 Aprepitant
Pharmacodynamics:Antiemetic drug of central action. Eliminates nausea and prevents vomiting caused by chemotherapeutic drugs. Penetrates into the brain, binds to the receptors of neurokinin-1 substance P, preventing acute and delayed phases of vomiting.
Pharmacokinetics:After oral intake absorbed into the blood, the maximum concentration of the drug is achieved after 4 hours. Bioavailability of the drug: 60-65%. Penetrates through the blood-brain barrier and the placenta. The connection with plasma proteins is more than 95%.
Metabolised in the liver by oxidation.
The half-life is 9-13 hours.
When administered orally, elimination with feces. It is excreted by the kidneys by 55% with intravenous injection.
It is not removed during hemodialysis.
Indications:It is used to prevent nausea and vomiting during the course of chemotherapy.
XVIII.R10-R19.R11 Nausea and vomiting
XXI.Z40-Z54.Z51.1 Chemotherapy for neoplasm
Contraindications:Individual intolerance.
Carefully:In patients with severe liver failure, a dose adjustment is required.Treatment is carried out under the control of the amount aspartate aminotransferase, alanine aminotransferase, bilirubin (liver tests).
Pregnancy and lactation:Pregnancy and lactation: recommendations for Food and Drug Administration (US Food and Drug Administration) - Category B. When prescribing the drug, pregnant women should take into account the risk / benefit ratio. The drug penetrates into breast milk, when using aprepitant it is recommended to stop breastfeeding.
Dosing and Administration:Regardless of the food intake, the drug is taken orally 125 mg one hour prior to taking the chemotherapy drugs on the first day, then 80 mg once a day in the morning. The course of treatment is 3 days, but can be extended, depending on the scheme of application of antitumor drugs.
The highest daily dose: 160 mg.
The highest single dose: 125 mg.
Side effects:Hematopoietic system: febrile neutropenia.
Central nervous system: dizziness, headache, cognitive impairment, anxiety, euphoria.
Digestive system: anorexia, constipation, eructation.
Skin: hyperhidrosis, itching.
Allergic reactions.
Overdose.
Headache, drowsiness after taking more than 1000 mg.
Treatment is symptomatic.
Overdose:Headache, drowsiness after taking more than 1000 mg.
Treatment is symptomatic.
Interaction:The effect of the drug is not dependent on food intake.
Incompatible with warfarin. Reduces the effectiveness of oral hormonal contraceptives during treatment on a three-day schedule and for the next 28 days.
Strengthens the action of glucocorticoids (methylprednisolone, dexamethasone), in connection with which the dose of the hormone is recommended to be reduced by 50%.
Special instructions:It is recommended to use additional methods of contraception when taking aprepitant for 28 days (one cycle). Planning pregnancy no earlier than 1 month (if the drug was not taken because of chemotherapy).