Ondansetron
Ondansetron: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Ondansetron
ATX code: A04AA01
Active ingredient: ondansetron (ondansetron)
Producer: OJSC "Novosibkhimfarm" (Russia), CJSC FarmFirma SOTEX (Russia), OJSC "Biochemist" (Russia), OJSC "Pharmstandard-UfaVITA" (Russia), MAKIZ-PHARMA, CJSC (Russia), etc.
Description and photo update: 07.01.2019
Prices in pharmacies: from 122 rubles.
Buy
Ondansetron is an antiemetic drug, serotonin receptor antagonist.
Release form and composition
Dosage forms of the drug:
- solution for intravenous (intravenous) and intramuscular (intramuscular) administration: colorless or slightly colored, transparent (2 or 4 ml each in ampoules of neutral glass; in a cardboard box of 3, 5, 10 ampoules or in a cardboard box with partitions 1 ampoule, in blister packs of 1, 3, 5, 10 ampoules, in a carton pack 1 or 2 blister packs A set with ampoules without a break ring or break point includes an ampoule knife or a scarifier for opening them);
- film-coated tablets: round, biconvex; the shell is pink, the core is white (for a dosage of 8 mg); the shell is yellow, the core is white (for a dosage of 4 mg) (10 pcs. in blisters, in a cardboard box 1 or 2 packages).
Composition for 1 ml of solution:
- active substance: ondansetron hydrochloride dihydrate (in terms of ondansetron) - 2 mg;
- auxiliary components: sodium chloride, water for injection, 1M hydrochloric acid solution to pH 3.0-4.0.
Composition for 1 tablet:
- active substance: ondansetron hydrochloride dihydrate (in terms of ondansetron) - 4 or 8 mg;
- auxiliary components: microcrystalline cellulose, sodium carboxymethyl starch, lactose (milk sugar), magnesium stearate;
- film shell: titanium dioxide, hypromellose, polysorbate 80, for a dosage of 8 mg - azorubin dye (carmoisine), for a dosage of 4 mg - quinoline yellow dye.
Pharmacological properties
Pharmacodynamics
The active component of Ondansetron is a selective serotonin receptor antagonist (5-HT3), which prevents and treats nausea / vomiting in the postoperative period, as well as caused by cytostatic chemotherapy and radiotherapy.
The use of cytotoxic drugs can increase the level of serotonin, which, by activating the vagal afferent fibers containing 5-HT 3 receptors, causes the gag reflex. Ondansetron inhibits the reflexive urge to vomit by blocking 5-HT3 receptors at the level of neurotransmission in both the central and peripheral nervous systems. The drug does not cause impaired coordination of movements, does not have a sedative effect, does not reduce working capacity, does not change the concentration of prolactin in the plasma and has anxiolytic activity.
Pharmacokinetics
Pharmacokinetic characteristics of ondansetron after intramuscular administration:
- absorption: after injection, the peak plasma concentration (T Cmax) is reached within 10 minutes;
- distribution: ondansetron binds to plasma proteins by 70–76%, its volume of distribution (V d) after parenteral administration in adult patients is ~ 140 L;
- metabolism: the drug is metabolized in the liver;
- excretion: unchanged in urine, ≤ 5% of the drug is excreted; half-life (T 1/2) ~ 3 hours, in elderly patients this indicator increases to 5 hours, and in severe liver failure - up to 15-20 hours. Severe renal failure with creatinine clearance (CC) <15 ml / min may cause an increase in the half-life by 4-5 hours, but this increase has no clinical significance.
Pharmacokinetic characteristics of ondansetron when taken orally:
- absorption: the substance is completely absorbed in the gastrointestinal tract; T Cmax is ~ 1.5 h; the bioavailability of ondansetron slightly increases with simultaneous food intake, but antacids do not affect this indicator;
- distribution: ondansetron binds to plasma proteins by 70–76%, Vd ~ 140 l;
- metabolism: the drug undergoes presystemic elimination (the effect of the first passage through the liver);
- excretion: T 1/2 is 3 hours, in elderly patients it can reach 5 hours, and with severe hepatic insufficiency - 15–20 hours. It is excreted from the systemic circulation mainly due to hepatic metabolism, which occurs with the participation of microsomal enzymes CYP1A2, CYP2D6, CYP3A4. In the urine, <5% of the administered dose is excreted unchanged.
With the repeated administration of ondansetron, its pharmacokinetic parameters do not change.
Special categories of patients:
- moderate renal failure (CC = 15-60 ml / min): reduced systemic clearance and Vd, resulting in an increase in T 1/2 up to 5.4 hours, but this does not affect the effectiveness of the drug;
- severe renal impairment (patients on chronic hemodialysis): the pharmacokinetic characteristics of ondansetron practically do not change;
- severe liver dysfunctions: systemic clearance is significantly reduced, as a result of which the half-life of ondansetron is lengthened to 15–32 hours, oral bioavailability reaches 100% due to a decrease in presystemic metabolism;
- advanced age: bioavailability can increase up to 65%, half-life - up to 5 hours;
- children's age: the values of clearance and V d depend on the age category of children; dose adjustment is required taking into account the child's body weight (0.1 mg / kg, but not more than 4 mg per administration), which compensates for such changes and normalizes the systemic exposure of ondansetron;
- female sex: there is a higher absorption with oral administration of the drug, as well as a decrease in systemic clearance and V d.
Indications for use
Ondansetron is recommended for the prevention and relief of nausea and vomiting caused by cytostatic chemotherapy or radiotherapy, as well as occurring in the postoperative period.
Contraindications
Absolute:
- During pregnancy and breastfeeding;
- children under 2 years of age (for solution), up to 3 years (for tablets at a dosage of 4 mg), up to 12 years (for tablets at a dosage of 8 mg);
- individual hypersensitivity to ondansetron or other components of the drug.
Tablets in a dosage of 4 mg are prescribed with caution for hereditary lactose intolerance, congenital lactase deficiency or glucose-galactose malabsorption.
Instructions for the use of Ondansetron: method and dosage
The standard daily dose of ondansetron for adult patients is 8 to 24 mg.
Solution for i / v and i / m administration
Ondansetron solution is intended for parenteral administration (intravenous or intramuscular).
Recommended dosage regimens for cytostatic anticancer therapy:
- adult patients (with moderate emetogenicity of chemotherapy or radiotherapy): immediately before the procedure, 8 mg intravenously, slowly or intramuscularly;
- adult patients (with high emetogenicity of chemotherapy or radiotherapy): immediately before the procedure, 8 mg intravenously, slowly, after the procedure, two more intravenous injections of 8 mg, each of which is carried out with an interval of 2-4 hours, or continuous infusion at a dose of 24 mg at a rate of 1 mg / h for 24 hours, or immediately before the procedure, 16–32 mg, diluted in 50–100 ml of an infusion solution, as a 15-minute infusion;
- children over 2 years of age: immediately before the procedure, 5 mg / m 2 of body surface is injected intravenously.
To increase the effectiveness of ondansetron, a single intravenous administration of a glucocorticoid (dexamethasone 20 mg) is recommended before starting chemotherapy.
Recommended dosage regimens to prevent nausea and vomiting in the postoperative period:
- adult patients: at the beginning of the introduction of anesthesia, as well as in order to relieve nausea and vomiting that occur in the future, 4 mg once intramuscularly or intravenously slowly;
- children over 2 years of age: before or after the introduction of anesthesia to prevent postoperative nausea and vomiting, as well as to relieve nausea and vomiting that occur in the future, 0.1 mg / kg (maximum up to 4 mg) IV slowly.
Do not administer more than 4 mg of ondansetron intramuscularly to the same area of the body.
There is little experience in the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age.
To dilute the Ondansetron solution, it is allowed to use a 0.9% NaCl solution; Ringer's solution; 5% dextrose solution; 0.3% KCl solution + 0.9% NaCl solution; 0.3% KCl solution + 5% dextrose solution.
Film-coated tablets
Ondansetron tablets are taken orally.
Recommended dosage regimens for cytostatic anticancer therapy:
- adult patients and children over 12 years of age (with moderate emetogenicity of chemotherapy or radiotherapy): 1–2 hours before the start of the procedure, 8 mg each, followed by oral administration of another 8 mg after 12 hours; there are no data on the use of the drug in children under 12 years of age with radiotherapy;
- children 4-11 years of age (at moderate emetic chemotherapy or radiotherapy): for 1 / 2 h before starting the procedure for 4 mg followed by a further 4 mg inwardly after 8 hours;
- adult patients (with high emetogenicity of chemotherapy or radiotherapy): 1–2 hours before the start of the procedure, 24 mg of ondansetron simultaneously with 12 mg of dexamethasone orally; there are no data on the use of the drug in children.
In order to prevent late / prolonged vomiting, it is necessary to continue taking the pills for 5 days after the end of the main therapy 2 times a day: adults - 8 mg, children - 4 mg.
For the prevention and relief of postoperative nausea and vomiting, adult patients are prescribed 16 mg of ondansetron orally 1 hour before general anesthesia. For this purpose, the drug is prescribed to children only in the form of a solution for parenteral administration.
Side effects
- nervous system: dizziness, headache, spontaneous movement disorders and seizures;
- digestive system: dry mouth, hiccups, diarrhea / constipation; sometimes - a transient asymptomatic increase in serum transaminases;
- cardiovascular system: arrhythmias, bradycardia, chest pain (accompanied in some cases by depression of the ST segment), lowering blood pressure (blood pressure);
- organ of vision: temporary decrease in visual acuity;
- data of laboratory and instrumental studies: hypokalemia, for tablets - hypercreatininemia;
- hypersensitivity reactions: bronchospasm, laryngospasm, urticaria, angioedema, anaphylaxis;
- other reactions: a feeling of heat, flushing of the face;
- local reactions with parenteral administration: redness, burning and pain at the injection site.
Overdose
Symptoms of an overdose of ondansetron are constipation, visual impairment, decreased blood pressure and a vasovagal episode with AV (atrioventricular block) II degree. All these effects are transient and completely reversible.
It is recommended to carry out symptomatic and supportive therapy, there is no information about a specific antidote, the use of ipecac is ineffective due to the antiemetic effect of ondansetron.
special instructions
In patients with hypersensitivity to other selective 5HT3 receptor antagonists, the use of ondansetron may develop similar effects.
After using the drug, constant monitoring of patients with signs of intestinal obstruction is necessary, since ondansetron can cause constipation.
The infusion solution should be prepared immediately before use. If necessary, it is allowed to store the finished infusion solution at a temperature of 2 to 8 ° C for no more than 24 hours.
Under normal lighting or natural light, the diluted injection solution is stable for at least 24 hours, therefore, during the infusion, it is not necessary to protect the drug from light.
Influence on the ability to drive vehicles and complex mechanisms
According to psychomotor tests, ondansetron does not affect the ability to control complex mechanisms and does not have a sedative effect on the body. But it is necessary to take into account the profile of side effects on the part of the nervous system when deciding whether to engage in activities that require increased concentration of attention and increased tension of psychomotor functions.
Application during pregnancy and lactation
According to the instructions, Ondansetron is prohibited for use by pregnant and lactating women.
Pediatric use
In pediatric practice, due to insufficient data on the effectiveness and safety of therapy, the use of the drug in the form of a solution is contraindicated - for the treatment of children under 2 years of age; tablets in a dosage of 4 mg - for the treatment of children under 3 years of age; tablets in a dosage of 8 mg - for the treatment of children under 12 years of age.
With impaired renal function
Patients with impaired renal function do not need to adjust the dosage regimen or route of administration of the drug.
For violations of liver function
With moderate and severe impairment of liver function, the clearance of ondansetron is significantly reduced, and its half-life from the blood serum increases, therefore the maximum daily dose should not exceed 8 mg.
Use in the elderly
Correction of the dosage of the drug is not required for elderly patients.
Drug interactions
- inducers of cytochrome P 450 (isoenzymes CYP2D6 and CYP3A) - carbamazepine, carisoprodol, barbiturates, griseofulvin, glutethimide, dinitrogen oxide, papaverine, phenytoin (possibly other hydantoins), phenylbutazone, rifamampidicin, tolbutamidicin; inhibitors of cytochrome P 450 (isoenzymes of CYP2D6 and CYP3A) - macrolide antibiotics, allopurinol, antidepressants - monoamine oxidase inhibitors (MAO), cimetidine, chloramphenicol, oral contraceptives containing estrogens, diltiazem, flaponiramine, sodium valcholone lovastatin, ketoconazole, omeprazole, metronidazole, propranolol, quinine, quinidine, verapamil: caution is required when used together with ondansetron;
- ethanol, temazepam, furosemide and propofol: do not interact with ondansetron;
- tramadol: may reduce its analgesic effect.
Analogs
Analogs of Ondansetron are: Ondantor, Domegan, Zofran, Latran, Ondavell, Ondansetron-Teva, Ondansetron-RCRC, Ondansetron-Ferein, etc.
Terms and conditions of storage
Store in a dark place out of the reach of children. Storage temperature: tablets - up to 25 ° С, solution 15–25 ° С.
Shelf life: tablets - 2 years, solution - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ondansetron
Most reviews of Ondansetron by both patients and medical professionals indicate the high effectiveness of the drug, regardless of the dosage form. Doctors note the prevention of vomiting in 70-80% of patients due to its use.
The price of Ondansetron in pharmacies
The approximate price for Ondansetron, depending on the manufacturer, is: 8 mg tablets (10 pcs. Per pack) - 330 rubles, 4 ml ampoules (5 pcs. Per pack) - 299-352 rubles.
Ondansetron: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 2 ml 5 pcs. 122 RUB Buy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 2 ml 5 pcs. 139 RUB Buy |
|
Ondansetron solution for in. 0.2% 2ml 5 pcs. 177 r Buy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 4 ml 5 pcs. 177 r Buy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 4 ml 5 pcs. 177 r Buy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 4 ml 5 pcs. 179 r Buy |
|
Ondansetron 2 mg / ml solution for intravenous and intramuscular administration 2 ml 5 pcs. 216 r Buy |
|
Ondansetron solution for intravenous and intramuscular injection. 0.2% 4ml 5 pcs. 364 RUB Buy |
| See all offers from pharmacies |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
