Zofran

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

Drugs used in chemotherapy and radiation therapy can increase the values of serotonin, which stimulates the activity of the endings of the 5-HT3 vagal axons of the afferent type, as a result of which the vomiting reflex develops. The active element of the drug slows down this reflex at the level of the CNS neurons, as well as the PNS.

Indications Zofrana

It is used to treat or prevent vomiting, as well as nausea resulting from chemotherapy or radiation therapy.

In addition, the drug can be used to prevent and treat nausea along with vomiting that appears after surgery.

[1], [2]

Release form

The release of the medication is made in the form of injection fluid - inside ampoules with a capacity of 2 or 4 ml. Inside the cell plate - 5 such ampoules; in the box - 1 record.

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

It can also be produced in the form of a syrup - inside a 50 ml bottle. Inside the box - 1 bottle complete with dosing spoon.

In addition, it is made in the form of suppositories - the first inside the strip; in the box - 1 or 2 such strips.

[3], [4], [5]

Pharmacokinetics

The drug is fully absorbed inside the intestine when administered orally, then undergoing intrahepatic metabolic processes. Indicators of plasma Cmax drug reaches after 90 minutes. The level of bioavailability is slightly increased when using drugs with food, but does not change with the introduction of antacids.

The term half-life is about 3 hours; in older people it can reach up to 5 hours, and in people with a lack of kidney function of a severe nature - up to 15-20 hours. Bound to plasma plasma by 72-76%.

With rectal use, ondansetron is recorded inside the blood after 20-60 minutes. Values Cmax reaches after 6 hours; the same 6 hours makes up the term half-life. The level of bioavailability after application in this way is 60%.

Elimination from the circulatory system is mainly implemented through intrahepatic transformation, which is carried out using several enzyme systems. Unchanged excreted not more than 5% of the portion (through the kidneys).

The pharmacokinetics of ondansetron remains unchanged when administered multiple times.

[6], [7], [8], [9],

Dosing and administration

The use of medication in the form of parenteral fluid.

In case of nausea with vomiting in connection with the conduct of emetogenic chemotherapy, as well as radiation procedures, it is necessary to prescribe the administration of 8 mg of the drug - before the session (i / m or v / v method).

Persons undergoing the procedures of highly emethogenic chemotherapy are also prescribed 1-time use of 8 mg of the substance (w / m or w / w), before performing therapeutic procedures.

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

Another intramuscular or intravenous method of using drugs at a dosage of 8 mg - at low speed, before starting chemotherapy, with the further introduction of another 2 servings (8 mg) with 3-4-hour breaks, or use (within 24 hours a) infusion having a rate of 1 mg / hour.

It is possible to increase the efficacy of the drug with the help of a one-time additional (IV) injection of 20 mg of dexamethasone Na phosphate before the start of the chemotherapy session.

The age subgroup of 0.5–17 years old, with a body surface area of up to 0.6 m ², an initial dose of 5 mg / m ² is administered in / in the method before the chemotherapy session, and then, after 12 hours Need to take 2 mg of medicinal syrup. It is required to continue treatment for another 5 consecutive days after the end of chemotherapy sessions, using the drug orally - 2 mg 2 times a day.

For children of the same age, but with a bodily surface area of 0.6-1.2 m ², the medicament is administered 1 time, in the IV dosage method of 5 mg / m ², before performing the treatment session; further, after 12 hours, 4 mg of syrup must be taken. The syrup intake course lasts for another 5 days from the end of chemotherapy - 4 mg each 2 times a day.

For children whose bodily surface equals a figure greater than 1.2 m ², the initial dose of the medication (8 mg) is used as an IV method before therapeutic sessions, and then, with a 12-hour break, syrup is used (8 mg). It is necessary to use it for another 5 days - 8 mg, 2 times a day.

In order to eliminate or prevent postoperative vomiting with nausea, an adult is administered intramuscularly or intravenously in a method of 4 mg of the substance 1-fold.

Postoperative abnormalities that occur after procedures performed under general anesthesia in children 0.5–17 years old can be prevented by intravenous injection of 0.1 mg / kg Zofran along with induction anesthesia, after it, or at the end of the operation.

The drug can be dissolved in such liquids: 5% dextrose, Ringer's solution, 10% mannitol, 0.9% NaCl, and also 0.3% ClK with 0.9% NaCl and 0, 3% ClK with 5% dextrose.

Infusion fluid is prepared immediately prior to administration. If necessary, the finished medicine can be stored for 24 hours at a temperature in the range of 2-8 ° C.

Use absorbable tablets or syrup.

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

Vomiting with nausea resulting from chemo or radiation therapy.

For such disorders, use such dosage schemes:

• in the case of moderate emethogenicity of the procedures, 8 mg of the drug should be used 120 minutes before the start of therapy; after 12 hours, take another 8 mg of the substance;
• in the case of severe emethogenicity, 24 mg of the drug in combination with dexamethasone (12 mg) are prescribed 120 minutes before the start of the session.

To prevent nausea with vomiting that occurs after 24 hours from the end of treatment, or prolonged vomiting, it is necessary to prolong oral use of drugs: 8 mg, 2 times a day for 5 days.

Postoperative vomiting with nausea.

Adults need to ingest 16 mg of the drug 60 minutes before the administration of anesthesia.

The use of the drug in the form of suppositories.

Vomiting, together with nausea, appearing as a result of chemotherapy or radiation therapy sessions, can be eliminated by applying the medication in the following regimens:

• moderate severity of emethogenicity requires the introduction of 16 mg of drug (1 suppository) 120 minutes before the start of the course;
• high intensity of emethogenicity requires, in conjunction with the 1st Zofran suppository, to introduce IV with the dexamethasone method (20 mg), 120 minutes before the start of therapy.

Prevention of disorders arising after 24 hours after the end of the course, or prolonged vomiting, requires the use of the medication to be prolonged - every day, for the first suppository, for a period of 5 days. Instead of suppositories, syrup or Zofran tablets can be used.

Hepatic function impairment.

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

[11], [12], [13]

Use Zofrana during pregnancy

The drug can not be used during pregnancy or lactation.

Contraindications

It is contraindicated to appoint people with intolerance regarding the components of the drug.

Caution with the introduction of injection fluid must be observed when such problems occur:

• disturbances of cardiac conduction and rhythm;
• simultaneous use of β-blockers or antiarrhythmic drugs;
• severe violations of the 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 mucous membranes, burning inside the rectum (suppositories), as well as a transient asymptomatic increase in the values of intrahepatic transaminases;
• allergy symptoms: urticaria, anaphylaxis, bronchial spasms, angioedema, laryngospasm;
• disorders in the work of the National Assembly: convulsions and spontaneous motor disorders, as well as headaches or dizziness;
• problems associated with blood circulation: pain in the sternum, lowering blood pressure levels, depression of the ST interval on an ECG, arrhythmia, or bradycardia;
• other signs: hot flashes or fever, hypokalemia, transient weakening of visual acuity and hypercreatininemia.

Disorders when using injection fluid:

• immune disorders: allergy symptoms, including anaphylaxis;
• Lesions of NA activity: headaches, convulsions, dizziness and movement disorders;
• signs associated with vision: transient visual disturbances or temporary blindness (mostly similar disorders disappear after 20 minutes);
• disorders affecting the blood flow system: arrhythmia, decrease in blood pressure values, pain in the sternum, fever, bradycardia, prolongation of the QT-segment and transient changes in ECG readings;
• problems associated with respiratory function: hiccups;
• disorders of the digestive system: transient asymptomatic increase in the values of liver transaminases or constipation;
• local signs: changes at the site of the IV injection.

[10],

Overdose

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

There is no antidote, which is why symptomatic measures are required when acute intoxication is suspected. The use of ipecac is not recommended in case of drug overdose, because it will be ineffective (due to anti-emetic properties of Zofran).

[14]

Interactions with other drugs

It is necessary to carefully combine the drug with such substances:

• CYP2D6, as well as CYP1A2 activators (among them glutetimid, rifampicin, carbamazepine with tolbutamide, papaverine, nitrous oxide and phenytoin with griseofulvin, barbiturates with carisoprodol and phenylbutazone);
• means of inhibiting the activity of CYP2D6, as well as of CYP1A2 and fluconazole with verapamil, as well as quinine, ketoconazole and metronidazole).

In addition, there is information that ondansetron is able to weaken the analgesic activity of tramadol.

[15]

Storage conditions

Zofran needs to be kept out of reach of small children, with temperature indices of no more than 30 ° C.

[16], [17], [18], [19]

Shelf life

Zofran can be used for a period of 3 years from the time the medication is sold.

[20], [21]

Application for children

You can not assign babies up to six months. Syrup and tablets can be used in patients older than 2 years of age. Suppositories in pediatrics do not use.

[22], [23], [24], [25], [26],

Analogs

Analogues of drugs are the substances Lazaran VM, Zoltem, Domegan, Osetron with Ondasol, and also Vero-Ondansetron, Setronon with Latran, Ondansetron, Emetron with Ondansetron-Teva, Emeset and Ondantor.

[27], [28], [29]

Reviews

Zofran receives positive reviews from most patients - its effects help eliminate nausea due to chemotherapy or anesthesia. Of the advantages of the drug, in addition to effectiveness, there are also several dosage forms. Of the minuses noted the presence of adverse symptoms, but they appear quite rare.

[30], [31], [32], [33]