ONDANSETRON-ALЬTFARM

Active material: Ondansetron
When ATH: A04AA01
CCF: Antiemetic drugs of the central action, blocking serotonin receptors
ICD-10 codes (testimony): R11
When CSF: 11.06.01
Manufacturer: ALTFARM Ltd. (Russia)

Pharmaceutical form, composition and packaging

Rectal Suppositories white or creamy white, torpedo-shaped, without visible inclusions on a longitudinal section.

Excipients: Witepsol N-15.

5 PC. – packings Valium planimetric (1) – packs cardboard.

Rectal Suppositories white or creamy white, torpedo-shaped, without visible inclusions on a longitudinal section.

Excipients: Witepsol N-15.

5 PC. – packings Valium planimetric (1) – packs cardboard.

Rectal Suppositories white or creamy white, torpedo-shaped, without visible inclusions on a longitudinal section.

Excipients: Witepsol N-15.

1 PC. – packings Valium planimetric (1) – inserts made of cardboard (2) – packs cardboard.

Pharmacological action

Antiemetic drugs of the central action. Selective serotonin 5HT antagonist₃-receptors.

Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in serotonin levels, which by activating vagal afferent fibers, containing serotonin 5HT₃-receptors, induces a gag reflex. Ondansetron inhibits the onset of the gag reflex by blocking serotonin 5HT₃-receptors at the level of neurons as a central, and the peripheral nervous system. Apparently, This mechanism of action is the basis for the prevention and treatment of postoperative and cytostatic chemotherapy and radiotherapy-induced nausea and vomiting..

Pharmacokinetics

Ondansetron pharmacokinetic parameters are not changed when multiple injections.

Absorption

After rectal administration, ondansetron is determined in plasma through 15-60 m. The concentration of the active substance increases linearly, C_max It reached approximately 6 h and is 20-30 ng / ml. The absolute bioavailability when administered rectally is approximately 60%. Plasma concentration decreases at a slower rate, than after ingestion (due to continued absorption).

Deduction

T_1/2 – 6 no.

Testimony

- Prevention and elimination of nausea and vomiting, caused by cytostatic chemotherapy and radiotherapy.

Dosage regimen

The drug is used rectally. To remove the suppository from the blister pack, one cell with a suppository should be broken off along the notch and separating the edges of the tape, pull them in different directions. The suppository is inserted into the anus with a pointed end, as deep as possible. For a more convenient introduction of the suppository, it is recommended to bend down, squat or lie on your side, cross-legged.

The choice of the dosage regimen is determined by the severity of the emetogenic effect of the antitumor therapy..

At moderately emetogenic chemotherapy or radiotherapy appointed 16 mg ondansetron for 1-2 hours before the start of the main therapy.

At highly emetogenic chemotherapy The recommended dose is 16 mg concomitantly with intravenous administration 20 mg dexamethasone for 1-2 h before chemotherapy.

To prevention of late or prolonged vomiting, emerging through 24 hours after the end of chemotherapy or radiotherapy, should continue taking the drug at a dose 16 mg 1 times / day for 5 days.

The drug is not recommended for use in children.

In elderly patients dose modification is not required.

In patients with renal insufficiency no dose changes required, frequency of administration or method of application.

To patients with impaired liver function daily dose of ondansetron should not exceed 8 mg.

Patients with a slow metabolism of spartein/debrisoquine do not need to adjust the daily dose or frequency of ondansetron.

Side effect

From the digestive system: Ikotech, dry mouth, constipation, diarrhea; sometimes – asymptomatic transient increase in serum aminotransferase activity.

Cardio-vascular system: chest pain (sometimes with ST segment depression), Arrhythmia, bradycardia, decrease in blood pressure.

From the nervous system: headache, dizziness, spontaneous movement disorders, convulsions.

Allergic reactions: hives, bronchospasm, laringospazm, angioedema, anaphylaxis.

Local reactions: hyperemia, pain, burning sensation in the anus and rectum after the introduction of a suppository.

Other: rush of blood to the face, feeling the heat, temporary visual impairment, kaliopenia, giperkreatininemiя.

Contraindications

- Pregnancy;

- Lactation (breast-feeding);

- Children's age;

- hypersensitivity to ondansetron or any other component of the drug.

Pregnancy and lactation

The drug is contraindicated in pregnancy and lactation (breast-feeding).

Cautions

Patients, with a history of allergic reactions to other selective serotonin 5HT blockers₃-receptors, have an increased risk of developing them while taking ondansetron.

Ondansetron may slow colonic motility, in this connection, its administration to patients with symptoms of intestinal obstruction requires special monitoring.

Overdose

There is limited experience with ondansetron overdose.. In most cases, the symptoms are similar to adverse reactions when using the drug at recommended doses..

Treatment: symptomatic and supportive therapy. No specific antidote for ondansetron is known..

Drug Interactions

There is no evidence, ondansetron that induces or inhibits the metabolism of other drugs, often prescribed in combination with it.

Ondansetron is metabolized by several cytochrome P450 isoenzymes system (CYP3A4, CYP2D6 и CYP1A2). Inhibition or decrease in the activity of one of the isoenzymes is usually normally compensated by others., in this connection, a significant decrease in the total clearance of ondansetron is unlikely. Nonetheless, caution is required when used together:

- with inducers of isoenzymes of the cytochrome P450 system (CYP2D6 и CYP3A): barbiturates, Carbamazepine, carisoprodol, glutethimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins). rifampicin, tolbutamid;

- with inhibitors of isoenzymes of the cytochrome P450 system (CYP2D6 и CYP3A): allopurinol, macrolide antibiotics, antidepressants (MAO inhibitors), chloramphenicol, cimetidine, oral contraceptives, containing estrogen, diltiazem, disulьfiram, valproic acid, sodium valproate, Erythromycin, fluconazole, ftorkhinolony, Isoniazid, ketoconazole, lovastatin, metronidazol. omeprazole, propranolol, quinidine, quinones, verapamil.

Special studies have shown, ondansetron that does not react with ethanol, temazepamom, furosemidom, tramadolom and propofolom.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, protected from light, inaccessible to children at a temperature not exceeding 25 ° C. Shelf life – 2 year.