Zofran

Zofran has an antiemetic effect. It is a selective blocker of 5-HT3 endings.

Medicines used in chemotherapy and radiation therapy can increase the levels of serotonin, which stimulates the activity of the 5-HT3 vagal axon endings of the afferent type, resulting in the development of a gag reflex. The active element of the medicine slows down this reflex at the level of neurons of the central nervous system, as well as the peripheral nervous system.

Indications Zofrana

It is used to treat or prevent vomiting and nausea that occur as a result of chemotherapy or radiation therapy.

In addition, the medication can be used to prevent and treat nausea and vomiting that occur after surgery.

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Release form

The drug is released in the form of injection liquid - inside ampoules with a capacity of 2 or 4 ml. Inside the cell plate - 5 such ampoules; in the box - 1 plate.

Also available in tablets - 10 pieces inside a blister; 1 blister in a pack.

It can also be produced as a syrup – inside 50 ml bottles. Inside the box – 1 bottle complete with a dosing spoon.

In addition, it is produced in the form of suppositories - 1 per strip; in a box - 1 or 2 such strips.

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Pharmacokinetics

The drug is fully absorbed inside the intestine when taken orally, then undergoing intrahepatic metabolic processes. The drug reaches plasma Cmax values after 90 minutes. The level of bioavailability slightly increases when taking the drug with food, but does not change when antacids are administered.

The half-life is about 3 hours; in elderly people it can reach 5 hours, and in people with severe renal insufficiency – up to 15-20 hours. It binds to intraplasmic protein by 72-76%.

When used rectally, ondansetron is registered in the blood after 20-60 minutes. Cmax values are reached after 6 hours; the half-life is also 6 hours. The bioavailability level after administration in this way is 60%.

Elimination from the circulatory system is mainly realized through intrahepatic transformation, which is carried out with the help of several enzymatic systems. No more than 5% of the portion is excreted unchanged (via the kidneys).

The pharmacokinetics of ondansetron remain unchanged with repeated administration.

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Dosing and administration

Use of a medication in the form of a parenteral liquid.

In case of nausea with vomiting in connection with emetogenic chemotherapy, as well as radiation procedures, it is necessary to prescribe the administration of 8 mg of the drug before the session (intramuscularly or intravenously).

Persons undergoing highly emetogenic chemotherapy are also prescribed a single dose of 8 mg of the substance (IM or IV) before performing treatment procedures.

In a dose of 8-32 mg, the drug is administered exclusively intravenously, over 15+ minutes, after dissolving the substance in 0.9% NaCl or another compatible infusion fluid (50-100 ml).

Another method of intramuscular or intravenous administration of the drug in a dosage of 8 mg is at a low rate, before the start of chemotherapy, with subsequent administration of 2 more portions (8 mg) with 3-4 hour breaks, or using (within 24 hours) an infusion at a rate of 1 mg/hour.

The effectiveness of the drug can be increased by a single additional (IV) injection of 20 mg of sodium dexamethasone phosphate before the start of the chemotherapy session.

For the age subgroup of 0.5-17 years, with a body surface area of up to 0.6 ^m2, the initial dose of 5 mg/ ^m2 is administered intravenously before the chemotherapy session, and then, after 12 hours, 2 mg of medicinal syrup should be taken. It is necessary to continue treatment for another 5 days after the end of the chemotherapy sessions, taking the medicine orally - 2 mg 2 times a day.

For children of the same age, but with a body surface area of 0.6-1.2 ^m2, the drug is administered once, intravenously, at a dosage of 5 mg/m2 ^, before the treatment session; then, after 12 hours, 4 mg of syrup must be taken. The course of taking the syrup lasts for another 5 days from the end of chemotherapy - 4 mg of the drug 2 times a day.

For children whose body surface area is greater than 1.2 m2 ^, the initial dose of the medication (8 mg) is administered intravenously before therapeutic sessions, and then, with a 12-hour break, syrup (8 mg) is administered. It should be taken for the next 5 days - 8 mg, 2 times a day.

To eliminate or prevent postoperative vomiting with nausea, an adult is administered 4 mg of the substance 1 time intramuscularly or intravenously.

Postoperative complications that occur after procedures performed under general anesthesia in children aged 0.5 to 17 years can be prevented by intravenous administration of 0.1 mg/kg Zofran with or after induction of anesthesia or at the end of the operation.

The medication can be dissolved in the following liquids: 5% dextrose, Ringer's solution, 10% mannitol, 0.9% NaCl, as well as 0.3% ClK with 0.9% NaCl and 0.3% ClK with 5% dextrose.

The infusion fluid is prepared immediately before administration. If necessary, the prepared medicine can be stored for 24 hours at a temperature of 2-8°C.

Use of lozenges or syrup.

Other dosage forms of Zofran are used to prevent delayed or persistent vomiting after the initial 24 hours from the end of treatment procedures.

Vomiting along with nausea that occurs as a result of chemotherapy or radiation therapy.

For such disorders, the following dosage regimens are used:

• in case of moderately expressed emetogenicity of the procedures, 8 mg of the drug should be used 120 minutes before the start of therapy; after 12 hours, another 8 mg of the substance should be taken;
• In case of severe emetogenicity, 24 mg of the drug is prescribed in combination with dexamethasone (12 mg) 120 minutes before the start of the session.

To prevent nausea and vomiting that occur 24 hours after the end of treatment, or prolonged vomiting, it is necessary to prolong oral administration of the drug: 8 mg, 2 times a day for 5 days.

Postoperative vomiting with nausea.

Adults should take 16 mg of the drug orally 60 minutes before the administration of anesthesia.

Use of the medicine in the form of suppositories.

Vomiting and nausea that occur as a result of chemotherapy or radiation therapy can be eliminated by using the drug in the following modes:

• moderate emetogenicity requires the administration of 16 mg of the drug (1 suppository) 120 minutes before the start of the course;
• high intensity of emetogenicity requires intravenous administration of dexamethasone (20 mg) together with the 1st Zofran suppository, 120 minutes before the start of therapy.

Prevention of disorders occurring after 24 hours from the end of the course, or prolonged vomiting requires prolongation of the use of the drug - daily, 1 suppository, for 5 days. Instead of suppositories, syrup or tablets of Zofran can be used.

Impaired liver function.

In people with liver problems, the clearance of the drug is significantly reduced and its half-life is increased. Therefore, they can use no more than 8 mg of the drug per day.

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Use Zofrana during pregnancy

The medication should not be used during pregnancy or lactation.

Contraindications

Contraindicated for use by people with intolerance to the components of the drug.

Caution should be exercised when administering injection fluid in the presence of the following problems:

• cardiac conduction and rhythm disturbances;
• concomitant use of β-blockers or antiarrhythmic drugs;
• severe disturbances in salt balance.

Side effects Zofrana

Side effects when using medicinal suppositories or syrup with tablets:

• manifestations associated with digestive function: hiccups, diarrhea or constipation, dry oral mucosa, burning inside the rectum (suppositories), as well as transient asymptomatic increase in intrahepatic transaminase levels;
• allergy symptoms: urticaria, anaphylaxis, bronchial spasms, Quincke's edema, laryngospasm;
• disorders of the nervous system: convulsions and spontaneous motor disorders, as well as headaches or dizziness;
• problems related to blood circulation: pain in the sternum area, decreased blood pressure, depression of the ST interval on the ECG, arrhythmia or bradycardia;
• Other signs include hot flashes or flushes, hypokalemia, transient decreased visual acuity, and hypercreatininemia.

Violations when using injection liquid:

• immune disorders: allergy symptoms, including anaphylaxis;
• damage to the nervous system: headaches, convulsions, dizziness and movement disorders;
• signs related to vision: transient visual impairment or temporary blindness (usually such disorders disappear after 20 minutes);
• disorders affecting the circulatory system: arrhythmia, decreased blood pressure, chest pain, fever, bradycardia, prolongation of the QT segment and transient changes in ECG readings;
• problems related to respiratory function: hiccups;
• disorders of the digestive system: transient asymptomatic increase in liver transaminase values or constipation;
• local signs: changes at the site of the intravenous injection.

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Overdose

Symptoms of poisoning are almost always similar to the side effects of the drug.

There is no antidote, so if acute intoxication is suspected, symptomatic measures must be taken. The use of ipecac in case of drug overdose is not recommended, because it will be ineffective (due to the antiemetic properties of Zofran).

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Interactions with other drugs

It is necessary to combine the medication very carefully with the following substances:

• activators of CYP2D6 enzymes, as well as CYP1A2 (including glutethimide, rifampicin, carbamazepine with tolbutamide, papaverine, nitric oxide and phenytoin with griseofulvin, barbiturates with carisoprodol and phenylbutazone);
• drugs that inhibit the activity of CYP2D6 enzymes, as well as CYP1A2 (these include chloramphenicol, diltiazem, allopurinol with disulfiram, macrolides, erythromycin, MAOIs and valproic acid, as well as cimetidine, isoniazid, lovastatin, oral contraception (estrogen-containing), quinidine with fluoroquinolones, omeprazole and fluconazole with verapamil, as well as quinine, ketoconazole and metronidazole).

In addition, there is information that ondansetron is capable of weakening the analgesic activity of tramadol.

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Storage conditions

Zofran should be stored out of the reach of small children, at a temperature no higher than 30°C.

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Shelf life

Zofran can be used for 3 years from the date of sale of the drug.

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Application for children

It should not be prescribed to infants under six months. Syrup and tablets can be used in persons over 2 years of age. Suppositories are not used in pediatrics.

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Analogues

The analogs of the drug are Lazaran VM, Zoltem, Domegan, Osetron with Ondasol, as well as Vero-Ondansetron, Setronon with Latran, Ondansetron, Emetron with Ondansetron-Teva, Emeset and Ondantor.

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Reviews

Zofran receives positive reviews from most patients - its effect helps to eliminate nausea that occurs due to chemotherapy or anesthesia. Among the advantages of the drug, in addition to its effectiveness, is the availability of several dosage forms. Among the disadvantages, the presence of side effects is noted, but they appear quite rarely.

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