Antiemetics for children

Vomiting is a defense mechanism by which the body tries to eliminate toxins, for example, in intestinal bacterial or viral infections in children, and, as a rule, such vomiting stops without special treatment. But there may be other reasons when it becomes necessary to use antiemetics - antiemetics for children.

Indications Antiemetic medications for children

It is important to keep in mind: there is no need to use vomiting tablets if vomiting in a child occurs due to viral infection (including rotavirus); in food poisoning and food toxic infections with the development of acute bacterial gastroenteritis, as well as intestinal helminthiasis. In these cases, antiemetics may prevent the elimination of toxins from the body.

The use of antiemetic medications for children is indicated in cases of nausea and vomiting that occur when:

• irritable bowel syndrome;
• food allergies;
• Cyclic vomiting syndrome;
• acid reflux or GERD (gastroesophageal reflux disease;
• biliary dyskinesia;
• A traumatic brain injury with a concussion;
• Acetonemic syndrome;
• viral or bacterial meningitis;
• Labyrinthitis (inflammation of the inner ear);
• motion sickness syndrome;
• after surgical interventions under general anesthesia;
• Radiation-induced intestinal lesions;
• chemotherapy for malignant neoplasms.

What antiemetics are used in pediatrics

Vomiting - with a series of contractions of the smooth muscles of the digestive tract - is initiated and controlled by the vomiting center of the medulla oblongata in response to irritation of its trigger zone receptors: dopamine DA2, serotonin 5-HT3, histamine H1, acetylcholine M1, and neurokinin-1 (NK1).

Most direct antiemetic drugs used in pediatrics are antagonists (blockers) of these receptors.

Serotonin receptor antagonists - Ondansetron (other trade names Zofran, Zofetron, Osetron, Ondanset, Emesetron, Emeset), Granisetron (Kitril), Dolasetron (Anzemet) - are prescribed only to prevent nausea and vomiting during treatment with cytostatic anticancer drugs.

In the same cases, the antiemetic drug Aprepitant or Emend, which is a selective NK1 receptor antagonist, is used. For more information, see. - Recommendations for the prevention of nausea and vomiting after chemotherapy.

The dopamine receptor antagonist Metoclopramide for vomiting in a child - as well as metoclopramide hydrochloride-containing synonyms Cerucal, Ceruglan, Gastrosil, Perinorm, Reglan, Regastrol, Metamol, etc., can be used in the same cases as in gastric peristalsis and gastroesophageal reflux. - can be used in the same cases, as well as in insufficient gastrointestinal peristalsis and gastroesophageal reflux.

Dopamine receptor blockers with prokinetic properties include not only Bromopride (Bromil, Mepramid, Modulan), which is identical to Metoclopramide, but also Domperidone (other trade names are Motilium, Motilac, Motilicum, Motoricum, Peridone, Domstal).

Due to additional cholinolytic properties, i.e. The ability to block the neurotransmitter acetylcholine, histaminergic agents such as Dimenhydrinate (Dramina, Dedalon, Aviomarin), Diprazine (Promethazine, Pipolfen) and Meclosine (Emetostop) can be used for nausea and vomiting in motion sickness syndrome in children as well as labyrinthitis.

And the drug from the group of nootropics Omarone reduces the excitability of receptors of the vestibular apparatus. Read more - Motion sickness pills

Release form

Antiemetics come in a variety of forms:

• tablets, such as Metoclopramide, Cerucal, Domperidone (Motilium, Motilac), Meclozin, etc;
• capsules - Emend;
• Diprazine (Promethazine);
• injectable solutions in ampoules, e.g. Ondansetron, Granisetron, Cerucal, Dimenhydrinate (if children are given parenteral injections);
• Domrid suspension (with domperidone);
• Motinorm syrup and Novax Domperidone (with domperidone), Susprin (with ondansetron);
• Bromopride rectal suppositories.

Pharmacodynamics

The mechanism of action of receptor antagonist drugs is due to the fact that they prevent the binding of neurotransmitters (dopamine, serotonin, histamine, acetylcholine and neurokinin) to the corresponding receptors of nerve endings in the small intestine, where they perform an important modulatory function in the release of neurotransmitters that transmit impulses of the enteric nervous system (autonomic nervous system of the gastrointestinal tract) to the vomiting center of the brain.

This is how serotonin (5-hydroxytryptamine type 3) receptor antagonists Ondansetron or Granisetron work, by blocking 5-HT3 receptor activation, because the cells lining the GI tract produce more serotonin when damaged by cytostatic anticancer drugs and radiation therapy.

D2 dopamine receptor antagonist benzamide derivative Metoclopramide (Cerucal) and benzimidazole derivative Domperidone (Motilium, Motilac, etc.) increase gastric peristalsis (i.e. Act as prokinetics, accelerating gastric emptying and alleviating symptoms of dyspepsia).) increase gastric peristalsis (i.e. Act as prokinetics, accelerating gastric emptying and relieving symptoms of dyspepsia), increase the tone of the lower esophageal sphincter and simultaneously reduce the flow of stimulating afferent signals to the trigger zone of chemoreceptors of the vomiting center, thereby preventing the response cascade of GI smooth muscle contractions.

As a direct-acting antihistamine, Diprazine (Promethazine) reduces the tone of intestinal smooth muscles and relieves their spasms, which are caused by the neurotransmitter histamine. In addition, this drug, being a phenothiazine derivative, has choline-blocking properties: it limits the effect of acetylcholine M1 on the corresponding receptors of the vomiting center.

In motion sickness, the antiemetic effect of Dimenhydrinate (Dedalon), an antihistamine with anticholinergic activity, lies in its ability to inhibit the activation of histamine H1 receptors of the vestibular apparatus of the inner ear.

Pharmacokinetics

After Ondnasetron injection, the drug enters the bloodstream and binds to plasma proteins by more than 70%; its total volume of distribution is 1.9 L/kg body weight. The drug is metabolized in the liver and excreted by the kidneys (with a half-life of about three hours).

Metoclopramide taken orally is completely absorbed in the digestive tract and after about one hour reaches maximum concentration in blood plasma, acting after a single dose for 12 hours. Metabolism occurs in the liver and is eliminated from the body with urine (half-life lasts about 6 hours).

After oral administration, Domperidone is rapidly absorbed in the GI tract; bioavailability does not exceed 15%; maximum concentration in blood plasma is reached after one hour (about 92% of the drug is bound to plasma proteins). Domperidone is metabolized in the liver, excreted by intestine and kidneys.

Antihistamine drug Diprazine on average 75% is bound to blood proteins, transformed in the liver, excreted with urine and feces.

When Dimenhydrinate is taken orally or injected intramuscularly, it begins to act after a maximum of half an hour, and after injection into a vein almost immediately (and the antiemetic effect lasts for 3-5 hours). Binds to blood plasma proteins about 80% of the drug. Transformation occurs in the liver, metabolites are excreted by the kidneys.

Dosing and administration

During chemotherapy Ondansetron in children is usually administered as a single intravenous injection (4 mg/kg) immediately before the administration of cytostatic drug. To prevent postoperative nausea and vomiting, a single intravenous injection (at a rate of 0.1 mg/kg) is recommended as an IM or IV injection.

Tablets Metoclopramide or Cerucal from vomiting in children 2-14 years old are taken orally no more than three times a day (before meals) in a dosage of 0,10,15 mg / kg, the maximum permissible duration of use - five days. When using the tablet form of the drug to prevent nausea and vomiting after surgery, it should be taken immediately after the end of general anesthesia.

Domperidone for vomiting in children under one year of age is prescribed at 0.25mg/kg of body weight three times a day, children under 12 years of age - 0.25-0.5mg/kg. Motilium or Motilac for vomiting in children is prescribed 10 mg (one tablet) three times a day half an hour before meals.

To prevent motion sickness and vomiting, Diprazine, Dimenhydrinate or Meclozin (Emetostop) is administered orally once (one tablet) one hour before travel.

Contraindications

Ondansetron is not used in liver insufficiency; during chemotherapy - children under four years of age; to suppress vomiting after surgery under anesthesia - children under two years of age.

Metoclopramide (Cerucal) is contraindicated in children under two years of age, in mechanical intestinal obstruction and intestinal bleeding, extrapyramidal disorders and epilepsy, as well as in bronchial asthma.

Domperidone (Motilium, Motilac) for nausea in children is contraindicated in kidney and/or liver failure, gastrointestinal bleeding, mechanical intestinal obstruction, intestinal colic.

Dimenhydrinate is not used in children under two years of age; besides similar age restriction, Diprazine is contraindicated in vomiting of unclear etiology, jaundice, renal failure, asthma and epilepsy. Meclozin (Emetostop) is not used in children under 12 years of age.

Side effects Antiemetic medications for children

Common side effects of Ondansetron and Granisetron include headache, dizziness, drowsiness, blurred vision, constipation, muscle rigidity, tachycardia, and hallucinations. Seizures, decreased liver function, abnormal heartbeat (arrhythmia, tachycardia, or bradycardia), fainting, and CNS depression may also occur.

Like other dopamine antagonists, Metoclopramide (Cerucal) may cause dizziness, diarrhea, arterial hypotension and dystonia; movement disorders, including akathisia - pathological inattentiveness; confusion and hallucinations. In addition, bradycardia, pirouette ventricular tachycardia and atrioventricular block may occur.

The use of Domperidone (Motilac, Motilium) may result in dry mouth; headache; soft tissue swelling; urticaria; muscle stiffness and movement disorders; changes in heart rate; drowsiness and feelings of weakness.

Side effects of Dimenhydrinate (Dramina) may occur in the form of dry mucous membranes in the mouth and nasopharynx, general malaise, decreased BP, headache and dizziness, impaired eye accommodation, tinnitus, drowsiness, convulsions, difficulty breathing and confusion.

The use of Promethazine (Diprazine) may cause drowsiness or hyperexcitability, dizziness and nausea, dryness and numbness in the mouth, allergic reactions in the form of urticaria, changes in blood pressure and HR, hyperhidrosis, convulsions, confusion.

Meclosin side effects include dry mouth and drowsiness, as well as increased excitability in children.

Overdose

Overdose of Domperidone (Motilium, Motilac) may lead to the development of drowsiness, weakness, disturbances of orientation in space, as well as impaired function of the extrapyramidal system with motor disorders.

In the case of an overdose of Metoclopramide (Cerucal), which, like Domperidone, is a dopamine receptor antagonist, the same symptoms are seen.

Exceeding the dose of Diprazine is manifested by facial redness, dyspnea, dilated pupils, tremor and psychomotor agitation.

Symptoms of Dimenhydrinate overdose include headache and dizziness, drowsiness, muscle weakness and impaired coordination of movements, increased HR, dilated pupils, and seizures.

Interactions with other drugs

Metoclopramide or Cerucal, as well as Domperidone (Motilium, Motilac) should not be used simultaneously with antipsychotic drugs (neuroleptics), antibiotics of macrolide group (Erythromycin, Azithromycin, Clarithromycin), neutralizing gastric acid antacids and antisecretory gastric agents of H2-histamine receptor blockers group.

Diprazine and Dimenhydrinate enhance the effects of neutroleptics, sedatives and antiepileptic drugs.

Will enterosorbents help with vomiting in children?

As a rule, in food poisoning and infectious gastroenteritis, vomiting in children is accompanied by diarrhea (diarrhea), so to bind and eliminate exogenous and endogenous toxic substances in the intestine - detoxification of the body - it is necessary to carry out enterosorption.

For this purpose, antidiarrheal drugs - enterosorbents are used: activated charcoal (Carbolong, Sorbex), Polysorb (Atoxyl), Enterosgel or Smecta (Endosorb).

Activated charcoal for vomiting children absorbs poisons and toxins from the gastrointestinal tract before they are absorbed. It is used in the form of suspension - one tablet per 10 kg of body weight.

Containing colloidal silicon dioxide (silica) Atoxil or Polysorb for vomiting in a child over one year of age is also dosed by body weight: for a child under seven years - 1.5-2 g / kg, over seven years - 2-2.5 g / kg.

Dysmectitis or Smecta for vomiting in children can be used from the age of two years. All details in the publication - Smecta for poisoning.

Intestinal adsorbent with hydrogel of methylsilicic acid Enterosgel for vomiting in a child is used in diarrhea, acute intoxication and enterocolitis.

However, it should be borne in mind that oral intestinal adsorbents can be used after vomiting has stopped, otherwise they will be useless.

Oral rehydration therapy for vomiting in a child

Children are more susceptible to the effects of fluid loss from vomiting (especially when combined with diarrhea) - disruption of water-electrolyte balance, and dehydration in children is a dangerous condition.

To replenish fluid in the body, oral rehydration therapy (ORT) is mandatory. In addition to isotonic sodium chloride solution is used Regidron for vomiting in a child, as well as Ringer-Locca solution, Glucosolan (in tablets for preparing a solution), powders in sachets for dissolving in water - Regidraton, Regisol, Gastrolit, Normohydron.

In mild dehydration in children need 50 ml of rehydration solution per kilogram of body weight, with moderate dehydration - 100 ml / kg. In severe cases, infusion of fluids in the conditions of a medical institution is carried out.

Do enzyme medications help with vomiting in children?

Why are enzyme preparations prescribed for children? To replenish the lack of pancreatic enzymes and improve digestive processes in cases of impaired external secretory function of the pancreas in cases of acute pancreatitis in children or dyspepsia, as well as in functional gastric disorder in children and pancreatic-affected cystic fibrosis.

In other cases, containing trypsin, chymotrypsin, lipase and alpha-amylase Pancreatin when a child vomits, as well as its synonyms - Pancreasim, Creon, Mezim, Enzybene - will not help reduce diarrhea and vomiting.

In lieu of a conclusion

In the treatment of children in no case can not use drugs if their expiration date (which is indicated on the package) has expired. It is also necessary to comply with the storage conditions of medicines specified in the instructions.

You can also use non-medicinal remedies to reduce nausea and antiemetic home remedies for children. The former include tea with peppermint or melissa leaves, ginger root, chamomile tea, decoction of apple peel and fresh lemon juice diluted with water (1:1). And to alleviate vomiting recommended seeds of cumin or cumin (zira): a teaspoon of seeds poured 150 ml of boiling water and insist in a closed bowl for 15-20 minutes. And several times a day, the child is given an infusion of room temperature, per reception - 30 ml (two tablespoons).