Motilium. When to take prokinetic medications: we relieve bloating and nausea New generation prokinetics with double action

Prokinetics- medications - stimulants of gastrointestinal motility.

Prokinetic group

For the Russian patient, only two types of prokinetics are of interest: with the active substance domperidone(motilium, motilak, etc.) and with active ingredient itopride(ganatone and itomed), as well as trimebutine, a myotropic antispasmodic, often classified as prokinetic (Alekseeva E.V. et al.).

Previously common prokinetic agents (cerucal, raglan, etc.) are considered obsolete due to the large number of side effects. For the same reasons, bromopride (bimaral), which is similar in pharmaceutical properties to metoclopramide, has not been sold in the Russian Federation for several years (it is prohibited in the USA). Cisapride (Coordinax, etc.), which was previously considered promising, was banned in 2000 in both the USA and the Russian Federation.

Other groups of drugs: 5-HT1 receptor agonists (buspirone, sumatriptan), which improve gastric accommodation after meals, motilin-like peptide ghrelin (ghrelin receptor agonist), gonadotropin-releasing hormone analogue leuprolide, kappa receptor agonists (fedotocin, azimadoline), which reduce visceral sensitivity, and others are at the stage of clinical study (Ivashkin V.T. et al.), the 5-HT 1 and 5-HT 4 agonist and the 5-HT 2 receptor antagonist cinitapride, which is registered in Spain, but not in Russia and the USA.

Promising and experimental prokinetics, but not yet registered in Russia, the USA and the European Union, include:

antagonist of muscarinic M1 and M2 receptors, as well as acetylcholinesterase inhibitor acotiamide (Maev I.V. et al.)
GABA B receptor agonists (eng. GABA B R) arbaclofen and lezogaberan (Sheptulin A.A.)
antagonist of the metabotropic glutamate-5 receptor (mGluR 5) mavoglurant (Sheptulin A.A.)
cholecystokinin receptor antagonist (CCK-A receptor) loxiglumide (Sheptulin A.A. et al., Titgat G.).

Trade names of prokinetic agents

Prokinetics - dopamine receptor antagonists

Dopamine receptor antagonists block D 2 -dopamine receptors and, thereby, have a stimulating motor function of the stomach and antiemetic effects.

D2-dopamine receptor antagonists include: metoclopramide, bromopride, domperidone, dimethpramide. Itopride is also an antagonist of D2-dopamine receptors, but it is also an inhibitor of acelinecholine and, therefore, is often not considered in the group of dopamine receptor antagonists.

The widely known prokinetics cerucal and raglan (active substance metoclopramide), the less well-known bimaral (bromopride) belong to the first generation prokinetics.

Domperidone is a second-generation prokinetic agent and, unlike metoclopramide (and bromopride), does not penetrate the blood-brain barrier and does not cause extrapyramidal disorders characteristic of metoclopramide: spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles, spasmodic torticollis , opisthotonus, muscle hypertonicity, etc. Also, unlike metoclopramide, domperidone does not cause parkinsonism: hyperkinesis, muscle rigidity. When taking domperidone, side effects of metoclopramide such as drowsiness, fatigue, tiredness, weakness, headaches, increased anxiety, confusion, and tinnitus are less common and less pronounced. That's why Domperidone is a better prokinetic agent than metoclopramide .

Prokinetics - dopamine receptor antagonists are used in the treatment of GERD, gastric and duodenal ulcers, functional dyspepsia, achalasia of the esophagus, diabetic gastroparesis, postoperative intestinal paresis, biliary dyskinesia and flatulence.

Prokinetics from this group are also used for nausea and vomiting due to diet disorders, infectious diseases, early toxicosis of pregnancy, kidney and liver diseases, myocardial infarction, traumatic brain injury, anesthesia, radiation therapy, as a prophylaxis for vomiting before endoscopy and X-ray contrast studies. Dopamine receptor antagonists have no effect on vomiting for vestibular reasons. According to the pharmacological index, prokinetic dopamine receptor antagonists belong to the group “Gastrointestinal motility stimulants, including emetics.” For ATC - to group A03FA “Gastrointestinal motility stimulants”.

Neuroleptics - antagonists of dopamine D2 receptors with prokinetic properties

Some neuroleptics, in particular sulpiride and levosulpiride, have a prokinetic effect on the organs of the digestive system, therefore, when considering gastroenterological problems, they are classified as prokinetics, which have an antiemetic effect that activates the proximal intestine (Sablin O.A., Riezzo G. et al.) . Sulpiride has been widely used in gastroenterology for a long time due to its pronounced prokinetic activity, realized through a “regulating” effect on the central nervous system. Being a selective antagonist of dopamine receptors, it has moderate antipsychotic activity in combination with some stimulating and antidepressant effects (Maev I.V. et al.). According to the pharmacological index, sulpiride and levosulpiride belong to the group “Neuroleptics”, according to ATC - to the subgroup “N05AL Benzamides” of the group “N05A Antipsychotic drugs”.

Acetylcholine agonists - stimulants of intestinal motility

Drugs in this group are most often only partially classified as prokinetics, although all of them have prokinetic properties. In Russia, the most famous of the drugs in this group is coordinax. However, its active substance, cisapride, being a cholinomimetic, can cause the development of long QT interval syndrome and, as a consequence, life-threatening heart rhythm disturbances. Therefore, although it has the best prokinetic properties among drugs in its group, cisapride is not currently recommended for use and existing permissions for its use have been revoked. In a number of CIS countries, mosapride, which is similar in mechanism of action to cisapride, has been registered. Unlike cisapride, mosapride

has little effect on potassium channel activity and therefore has a lower risk for cardiac arrhythmias.

This group also includes: the domestically developed M-cholinomimetic aceclidine (approved for use in the USSR), reversible cholinesterase inhibitors (physiostigmine, distigmine bromide, galantamine, neostigmine monosulfate, pyridostigmine bromide), tegaserod and prucalopride.

Tegaserod and prucalopride, which are enterokinetics (prokinetics that selectively act on the intestines), were recently moved within the ATC from the section “A03 Drugs for the treatment of functional gastrointestinal disorders” to the section “A06 Laxatives”

Prokinetics - motilin receptor agonists

The hormone motilin is produced in the stomach and duodenum, increases the pressure of the lower esophageal sphincter and increases the amplitude of peristalsis in the antrum of the stomach, stimulating its emptying. Erythromycin (as well as other macrolides: azithromycin, clarithromycin, atilmotin) interact with motilin receptors, imitating the action of the physiological regulator of the gastroduodenal migratory motor complex. Erythromycin can cause powerful peristaltic contractions, similar to those of the migratory motor complex, accelerating gastric emptying of liquid and solid food, erythromycin increases the rate of gastric emptying in a number of pathological conditions, in particular gastroparesis in diabetics and patients with progressive systemic scleroderma, reduces intestinal transit time contents in the proximal colon. However, it has virtually no effect on the motility of the esophagus and, therefore, is not used in the treatment of GERD (Maev I.V. et al.). However, erythromycin, when taken for a month or more, doubles the risk of mortality associated with impaired cardiac conduction and, therefore, is not considered as a promising prokinetic agent.

Professional medical articles addressing the use of prokinetics in the treatment of gastrointestinal diseases:.

Maev I.V., Kucheryavyi Yu.A., Andreev D.N. Functional dyspepsia: epidemiology, classification, etiopathogenesis, diagnosis and treatment. - M.: ST-Print LLC, 2015.- 40 p.

Sheptulin A.A., Kurbatova A.A., Baranov S.A. Modern possibilities of using prokinetics in the treatment of patients with GERD // RZHGGK. 2018. No. 28(1). pp. 71–77.

On the website in the literature catalog there is a section “Prokinetics”, containing links to articles on the use of prokinetics in the treatment of diseases of the gastrointestinal tract.

Prokinetics - what is it? In the CIS countries, there is no consensus on which medications are included in this group, so each gastroenterologist himself determines what to include in this list and what not. Prokinetics - we will try to find out.

Definition and Brief Description

Prokinetics are a group of drugs that stimulate the motility of the digestive tube and prevent the appearance of antiperistaltic waves.

Diseases of the gastrointestinal tract are often accompanied by the reflux of chyme from the underlying parts of the intestinal tube into the overlying ones, disruption of the passage of the food bolus, or its stagnation in the intestinal segment. All these manifestations are associated with a violation of the movement of chyme through the digestive tube, which means that the symptoms can be eliminated by influencing the contractions of the smooth muscles in its walls. This is why prokinetics are needed. Their therapeutic effect is associated with blocking the ion transport mechanism (dopamine, 5-HT4 receptors, combined) or affecting the metabolism of acetylcholine. The achievement of a clinical effect occurs due to an increase in the amount of acetylcholine in the synaptic cleft or an increase in the production of cholinesterase, which enhances the decomposition of ACh, a decrease in the production of ACh by nerve endings.

Physiologically, the effects of taking the drugs are manifested in increased tone of the cardiac esophageal sphincter, evacuation of stomach contents, coordination between the antrum and duodenum, and productive intestinal motility.

First group of drugs

Prokinetics are drugs that block D2-dopamine receptors, thus stimulating the activity of gastrointestinal muscle fibers and providing an antiemetic effect. These medications include: "Metoclopramide" (first generation, representatives - "Cerucal" and "Reglan"), "Bromopride", "Domperidone" (second generation), "Dimetpramide", "Itopride".

Prokinetic drugs are used in the treatment of gastroesophageal reflux disease (GERD), gastroesophageal reflux disease, functional dyspepsia, narrowing of the esophagus after injuries and as a result of the development of adhesions, paresis of postoperative intervention in the abdominal cavity, impaired outflow of bile, and increased gas formation.

Also, prokinetics are drugs that can be used for nausea and vomiting caused by poisoning or eating disorders, diseases of viral or bacterial etiology, pregnancy in the first trimester, acute coronary insufficiency, head injuries, anesthesia, radiation and chemotherapy. They are ineffective for vomiting of vestibular origin, since they do not affect the middle ear and medulla oblongata.

Antipsychotics to help with vomiting

"Sulpiride" and "Levosulpiride", which are antipsychotics with a similar mechanism of action, also have a positive antiemetic effect, and therefore can be used in gastroenterological practice.

"Metoclopramide" (prokinetics): instructions for use

Metoclopramide is a direct smooth muscle stimulant and has all the necessary properties to achieve clinically significant results, but due to permeability through blood-histological barriers it should be used with caution. Possible side effects, such as spasm of the facial muscles, crow's feet symptom, rhythmic protrusion of the tongue, bulbar disorders, spasm of the extraocular muscles, excessive tone of the extensor muscles, Parkinson's syndrome, drowsiness, weakness, ringing in the ears, headaches, anxiety, absent-mindedness .

In what cases is it undesirable to take prokinetics? The instructions for use say that use is undesirable in cases of hypersensitivity to the components of the drug, tumor of the adrenal cortex, intestinal obstruction, intestinal perforation and bleeding caused by it, prolactin-dependent tumor, epilepsy and up to 16 weeks of gestation, during breastfeeding, children under 5 years of age. Caution should be used in patients with reduced blood pressure clearance, bronchial asthma, and under the age of 14 years.

The medicine is swallowed half an hour before meals, one tablet at 9:00, 12:00, 15:00 and 18:00. The duration of treatment is from four to six weeks, sometimes it can be extended to six months.

If the release form is liquid, then it is administered intramuscularly or intravenously. For adults and children over 14 years old - 10 mg. Maximum at one time - 20 mg, daily dose - 60 mg. The contents of the ampoule can be diluted in an isotonic solution or in a 5% glucose solution.

"Domperidone": instructions for use

"Domperidone" is a more selective blocker of dopamine receptors; moreover, it does not penetrate the BBB, so the side effects described above do not develop when taken. But by increasing the secretion of prolactin, it provokes gynecomastia, galactorrhea and lack of menstruation. In addition, patients reported skin rash, dry mouth, diarrhea and headaches.

It is not recommended for use by people with allergic reactions to the components of the drug, bleeding from the gastrointestinal tract, intestinal obstruction, prolactinoma, during breastfeeding, under 5 years of age or weighing up to 20 kilograms. Use with caution during pregnancy, renal and/or liver failure.

Drink 10 mg twenty minutes before each meal; if necessary, you can drink it before going to bed. The maximum dose per day is 80 mg. If the treatment contains drugs that reduce the secretion of gastric juice, they should be taken separately from domperidone, separating the use with meals.

"Itopride": instructions for use

"Itopride" combines the properties of a dopamine receptor antagonist and an acetylcholinesterase blocker. Affects the hypothalamic-pituitary-adrenal system, increasing somatostatin concentrations and reducing adrenocorticotropic hormone. The negative effect is expressed in leukopenia, thrombocytopenia, hypersensitivity reactions, hyperprolactinemia, nausea, tremor, jaundice. During administration, it is necessary to monitor the condition of peripheral blood and make sure there are no side effects.

It is not recommended for people with immediate or delayed hypersensitivity, a history of gastrointestinal bleeding, obstruction of the intestinal lumen by a foreign body or compression from the outside, under the age of sixteen, during pregnancy or breastfeeding.

Take the drug orally before meals, 50 mg three times a day.

Antagonists "Acetylcholine"

This group includes:

"Aceclidine" (M-cholinomimetic);
"Physiostigmine", "Galantamine", "Tegaserod", "Prucalopride" (reversible cholinesterase inhibitors)

These drugs are only partially classified as prokinetics due to their side effects: the effect on the metabolism of potassium ions, and as a result, prolongation of the QT interval, which leads to heart rhythm disturbances. A number of medicines were withdrawn from the pharmacological market precisely for this reason.

"Aceclidine": instructions for use

Prokinetics - what are they, how and in what cases should they be used? In any case, it is necessary to consult a doctor and carefully read the instructions for use.

"Aceclidine" is used to eliminate loss of tone of the gastrointestinal tract and bladder after surgery, reduces intraocular pressure, and therefore can be used by ophthalmologists. Release form - solution for injection, 1-2 ml of 0.2% solution is administered subcutaneously. The maximum amount per dose is 0.004 g, with no more than 0.012 g per day. Side effects are ptyalism, sweating, diarrhea.

Contraindications for use are coronary artery disease, increased HDL content, bronchial asthma, hyperkinesis and other parkinsonisms, pregnancy, bleeding from the abdominal organs.

"Physiostigmine" is used mainly in ophthalmological practice, but sometimes it can also be used in gastroenterology for intestinal paresis. The medicine is injected under the skin in 0.5 - 1 ml of 0.1% solution. The maximum amount of the drug per day should not exceed 0.001 g.

Side effects include increased salivation, bronchospasm, intestinal muscle spasm, changes in heart rate, and convulsions.

Contraindications: angina pectoris, epilepsy, bronchial asthma, mechanical intestinal obstruction, peritonitis, sepsis, pregnancy.

"Galantamine": instructions for use

"Galantamine" is sometimes used as an antagonist for muscle relaxants in the postoperative period when the tone of the intestinal and bladder muscles decreases. Contraindications for use are hypersensitivity, epilepsy, bronchial asthma, blood pressure above 139/99 mmHg, COPD, mechanical blockage of the intestinal tube, decreased kidney function, age under 9 years. Restricted for use during pregnancy in cases where the potential harm outweighs the benefit. During lactation it can be transmitted to the baby through milk.

Side effects: decreased heart rate, TTP, AV block, extrasystole, nausea, vomiting, diarrhea, dyspepsia, muscle spasms, urinary incontinence, hematuria, tremor.

Can be administered subcutaneously, intramuscularly, intravenously, transcutaneously, orally. The dose is selected individually, based on the medical history, and should be adjusted by the attending physician. The average daily dose for adults is from 10 to 40 mg, divided into two to four doses.

New generation prokinetics

Today, drugs based on itopride include Ganaton, Itomed, and Pramer. Some of the newest and most effective are such new generation prokinetics as “Coordinax” and “Prepulsid”. Although they can cause serious side effects on the heart.

The most popular among gastroenterologists remains Motilium (active ingredient - domperidone), which combines the qualities of metoclopramide, but does not have its negative consequences.

What are the most effective prokinetics? The list of drugs today includes:

"Itopride" (active ingredient) - "Ganaton", "Itomed", "Primer" (commercial names).
"Metoclopramide" - "Raglan", "Cerucal".
"Cisapride" - "Coordinax", "Prepulsid".
"Domperidone" - "Motilium", "Motilak", "Motinorm", "Passenger".

Now we know what prokinetics are. The list of them, as you can see, is very large. But remember, before using any drug you need to consult your doctor! Be healthy!

In the domestic gastroenterological literature there is no single generally accepted list of prokinetics. Different gastroenterologists define the range of prokinetic drugs differently. Many of the prokinetics can also be included in other groups (antiemetics, antidiarrheals and even antibiotics). In the “theoretical” (scientific) plan of analysis of the group of prokinetics, it is important that only a minority of the prokinetics existing in the world are present on the Russian market. However, for practical medicine this does not matter. Prokinetics that are not registered in Russia today are either prohibited (for example, by the FDA in the USA) or do not have any advantages over the approved ones. For the Russian patient, only two types of prokinetics are of interest: with the active substance domperidone(motilium, motilak, etc.) and with active ingredient itopride ().

Previously common prokinetic agents (cerucal, raglan, etc.) are considered obsolete due to the large number of side effects. For the same reasons, bromopride (bimaral), which is similar in pharmaceutical properties to metoclopramide, has not been sold in the Russian Federation for several years (it is prohibited in the USA). Cisapride (Coordinax, etc.), which was previously considered promising, was banned in 2000 in both the USA and the Russian Federation.

Trade names of prokinetic agents

Domperidone (ATC code A03FA03): Damelium, Domet, Domperidone, Domperidone Hexal, Domstal, Motilak, Motilium, Motinorm, Motonium, Passazhix

medicine with the active ingredient itopride hydrochloride: (primer on the Ukrainian pharmaceutical market)

medications with active substance (ATC code A03FA01): apo-metoclop, metamol, metoclopramide, metoclopramide 0.01 g, metoclopramide-acri, metoclopramide-promed, metoclopramide hydrochloride, metoclopramide tablets 0.01 g, perinorm, raglan, ceruglan, cerucal

medications with the active ingredient cisapride (ATC code A03FA02): coordinax, peristil, prepulsid, cisap

medicine with the active ingredient bromopride (ATC code A03FA04): bimaral

medications with the active ingredient bethanechol sold in the USA: Duvoid and Urecholine

Prokinetics - dopamine receptor antagonists

Dopamine receptor antagonists block D 2 -dopamine receptors and, thereby, have a stimulating motor function of the stomach and antiemetic effects.

The widely known prokinetics cerucal and raglan (active substance metoclopramide), the less well-known bimaral (bromopride) belong to the first generation prokinetics.
Domperidone is a second-generation prokinetic agent and, unlike metoclopramide (and bromopride), does not penetrate the blood-brain barrier and does not cause extrapyramidal disorders characteristic of metoclopramide: spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles, spastic torticollis, opisthotonus, muscle hypertonicity, etc. Also, unlike metoclopramide, domperidone does not cause parkinsonism: hyperkinesis, muscle rigidity. When taking domperidone, side effects of metoclopramide such as drowsiness, fatigue, tiredness, weakness, headaches, increased anxiety, confusion, and tinnitus are less common and less pronounced. That's why Domperidone is a better prokinetic agent than metoclopramide .

According to the pharmacological index, prokinetic dopamine receptor antagonists belong to the group “Gastrointestinal motility stimulants, including emetics.” For ATC - to group A03FA “Gastrointestinal motility stimulants”.

Acetylcholine agonists — stimulants of intestinal motility

Prokinetics - motilin receptor agonists

The hormone motilin is produced in the stomach and duodenum, increases the pressure of the lower esophageal sphincter and increases the amplitude of peristalsis in the antrum of the stomach, stimulating its emptying. Erythromycin (as well as other macrolides: azithromycin, clarithromycin, atilmotin, the latter is not approved for sale in the USA or Russia), interact with motilin receptors, imitating the action of the physiological regulator of the gastroduodenal migratory motor complex. Erythromycin can cause powerful peristaltic contractions, similar to those of the migratory motor complex, accelerating gastric emptying of liquid and solid food, erythromycin increases the rate of gastric emptying in a number of pathological conditions, in particular gastroparesis in diabetics and patients with progressive systemic scleroderma, reduces intestinal transit time contents in the proximal colon. However, it has virtually no effect on the motility of the esophagus and, therefore, is not used in the treatment of GERD (Maev I.V. et al.). However, erythromycin, when taken for a month or more, doubles the risk of mortality associated with impaired cardiac conduction and, therefore, is not considered as a promising prokinetic agent.

The table below summarizes the characteristics of the main prokinetics

Active substance	Trade marks	Mechanism of action	Prokinetic action	Antiemetic effect	QT interval prolongation	Extrapyramidal effects	Note
	tserukal, raglan, etc.	D 2 - antagonist, 5-HT 4 -agonist	expressed	expressed	does not cause	often	outdated product (not prohibited)
bromopride	bimaral	D 2 - antagonist, 5-HT 4 -agonist	expressed	expressed	does not cause	often	not allowed in the Russian Federation and the USA
domperidone	motilium, motilak, etc.	D 2 -antagonist	expressed	moderate	does not cause	rarely	most commonly used prokinetic agent
itopride		D 2 -antagonist, acetylcholine inhibitor	expressed	moderate	does not cause	rarely	new, promising prokinetic agent
cisapride	coordinatex, etc.	5-HT 4 -agonist	expressed	moderate	causes	infrequently	banned* in the USA and Russia
tegaserod	fractal, zelnorm	partial 5-HT 4 agonist	used to treat irritable bowel syndrome with constipation				banned in the USA (not sold in Russia)

*) the wording “prohibited” means that the regulatory authority initially approved the drug for use, and then, during the period of approval, issued a directive to withdraw the drug from circulation.

Definition and Brief Description

Prokinetics are a group of drugs that stimulate the motility of the digestive tube and prevent the appearance of antiperistaltic waves.

The use of drugs is indicated for symptomatic phases, the duration of which varies, awaiting periods of clinical improvement, in which they should be suspended. Recommended drug therapy is aimed at relieving the predominant symptom. Emotional factors should be addressed in all patient groups through frank and open discussion, and an attempt should be made to educate the patient about the likely relationship of his symptoms to emotional disturbances. Psychotherapy or other methods aimed at reducing stress are often indicated, with excellent response observed in some subgroups of patients.

Current therapy Available drug treatments are aimed primarily at alleviating the predominant symptom, and the therapeutic strategy will largely depend on the nature and intensity of the symptoms, the degree of functional impairment and psychosocial factors.

Numerous studies have shown that clinical improvement during and after traditional drug therapy occurs in less than 60% of patients with dyspepsia, and there is usually no uniform response to this therapy. It should be remembered that the response to placebo is usually very high. Controlled, double-blind studies show that placebo is able to stimulate symptom improvement in a large number of patients, indicating that drug therapy is not always necessary.

First group of drugs

Antiseptics are safe medications and are the first line treatment for patients with epigastric pain syndrome. Both H2 blockers and proton pump inhibitors are widely prescribed and recommended as first-line therapy. A recent meta-analysis suggests that proton pump inhibitors should be chosen because they are more effective in relieving pain or epigastric burn. They should be used in a standard dose once a day.

Prokinetics is superior to placebo in several clinical trials and is particularly indicated for patients with postprandial discomfort syndrome. These drugs have the potential to improve various parameters of gastroduodenal motility, increasing gastric tone, antral motility and, above all, androduodenal coordination, in addition to the fact that some of them are able to relax the gastric fundus.

Prokinetic drugs are used in the treatment of gastroesophageal reflux disease (GERD), gastroesophageal reflux disease, nature, narrowing of the esophagus after injuries and as a result of the development of adhesions, paresis of postoperative intervention in the abdominal cavity, impaired outflow of bile, increased gas formation.

Symptom improvement with these drugs was 20 to 45 percentage points greater than placebo, and prokinetics should be indicated, especially for patients with postprandial symptoms. Recent observations suggest that in a select group of patients complaining of early satiety, drugs that relax the gastric fundus as 5-hydroxytryptamine agonists are useful in relieving this symptom.

Promising results have been obtained using tricyclic antidepressants or serotonin uptake inhibitors. These drugs are recommended because they have a central analgesic effect and can block the transmission of pain from the digestive tract to the brain. It is recommended to start with lower doses than usual, and if clinical improvement is observed, treatment should be continued for 6-12 months. It must be emphasized that most studies conducted using this type of therapeutic intervention were not randomized, placebo controlled and did not represent an adequate methodological design, which prevents any conclusion about the possible effectiveness of this treatment for functional dyspepsia.

Antipsychotics to help with vomiting

"Sulpiride" and "Levosulpiride", which are antipsychotics with a similar mechanism of action, also have a positive antiemetic effect, and therefore can be used in gastroenterological practice.

However, the gastroenterologist should always encourage the practice of activities or techniques involving physical and mental relaxation, such as exercise, yoga, or walking, obviously respecting each patient's preferences. Recent studies show some clinical benefit with the use of probiotics and probiotics, but more consistent and long-term results are still awaited.

However, there is still a gap between basic research and medical practice with a shortage of new drugs released for marketing. Currently, the main drugs under investigation are new prokinetics, serotonergic agents, opioid receptor agents and visceral analgesics. Other drugs, such as itopride and levosulpiride, have shown similar efficacy to traditional prokinetics in patients with dyspepsia.

"Metoclopramide" (prokinetics): instructions for use

New prokinetics, capable of acting both on digestive motility and on relaxation of the gastric fund, await our daily practice. Among these drugs, the aminothiazide derivatives motilin and ghrelin have been shown to be effective in initial trials and may soon become a new class of prokinetics. New serotonergic drugs are also being tested. Receptors capable of modulating gastrointestinal mucosa and smooth muscle function, such as capsaicin, which is a potent agonist, have great therapeutic potential.

A double-blind randomized controlled trial demonstrated significant superiority of tanspopirone citrate over placebo in relieving symptoms in patients with functional dyspepsia. Prokinetic drugs should not be routinely prescribed for the treatment of gastroesophageal reflux disease in pediatric patients.

Prokinetics should not be routinely prescribed for the treatment of gastroesophageal reflux disease in pediatric patients. Because of the multiple aspects involved in the differential diagnosis and therapeutic approach of gastroesophageal reflux disease, numerous literature reviews and ongoing updates are published by various pediatric, gastroenterology, pulmonology, and otolaryngology societies. Symptoms of gastroesophageal reflux disease are less common than symptoms of gastroesophageal reflux disease, but they are still very common.

The medicine is swallowed half an hour before meals, one tablet at 9:00, 12:00, 15:00 and 18:00. The duration of treatment is from four to six weeks, sometimes it can be extended to six months.

It is estimated that approximately 2% of children aged 3 to 9 years and 5 to 8% between 10 and 17 years present with intermittent burning sensation and acid regurgitation. A single wound burning can be detected in 17.8% of adolescents. Deficiency of the disease puts the child at risk for serious complications such as bronchospasm, esophagitis, esophageal stricture and Barrett's esophagus. However, overestimating symptoms, especially regarding the presence of regurgitation alone, can lead to overdiagnosis and overtreatment by the physician.

At that time, the initial therapeutic response was the use of a prokinetic drug, cisapride, in all age groups. There is no reference in this article to the use of other prokinetic agents such as metoclopramide, domperidone, or bethanechol.

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"Domperidone": instructions for use

Its main property is to reduce the time of postprandial reflux and is fundamentally used to control regurgitation and vomiting. Since the suspension of commercialization of cisapride, domperidone has been widely used, especially in Brazil. The magnitude and heterogeneity across the age range of the population samples assessed may have influenced the final outcome, as there is a tendency for cases of regurgitation and vomiting to resolve spontaneously in the second half of life. From the second semester towards the end of the first year, only 10% of normal infants remain with regurgitation.

Drink 10 mg twenty minutes before each meal; if necessary, you can drink it before going to bed. The maximum dose per day is 80 mg. If the treatment contains antacid drugs that reduce the secretion of gastric juice, then they should be taken separately from domperidone, separating the use with meals.

The diagnosis in question was confirmed by clinical, radiological and esophageal pH tests. Some methodological data should be considered: the mean age of patients in the domperidone group was 3.6 years, and the mean age of the placebo group was 2.4 years, which is a factor that may confound the total number of reflux events reported. The total sample included only 17 participants, a very small number that does not provide sufficient sampling power for satisfactory analysis.

Patients presented expressive symptoms but were not described in more detail. The authors also note that there are no data demonstrating a clear effect of the drug in cases of reflux disease due to endoscopically confirmed esophagitis.

"Itopride": instructions for use

Thus, serum drug levels may be increased by concomitant use of imidazole derivatives and macrolide antibiotics. These data are concerning because in Clara's publication the drug shows more consistent action, reducing regurgitation and vomiting when the dose is doubled. Metoclopramide is an antidopaminergic agent with cholinergic and serotonergic effects. The drug promotes relaxation of the pylorus, accelerates the time of gastric emptying, and increases the tone of the lower esophageal sphincter.

Take the drug orally before meals, 50 mg three times a day.

Metoclopramide should be prescribed with a pediatrician with great caution as the therapeutic dose is close to that in which there are central nervous system side effects such as; drowsiness, irritability, dystonic reactions and often extrapyramidal symptoms.

It should be remembered that due to the withdrawal of cisapride from the market in recent years, some centers have seen an increase in the availability of metoclopramide. In three studies, the drug was effective in reducing symptoms and reducing the incidence of acid reflux, but in other studies the drug was not proven to be effective. The risk of side effects was 26% in the group receiving the drug.

Antagonists "Acetylcholine"

This group includes:

"Aceclidine" (M-cholinomimetic);
"Physiostigmine", "Galantamine", "Tegaserod", "Prucalopride" (reversible cholinesterase inhibitors)

The study included 45 patients, 30 of whom were under one year of age, and data showed a reduction in symptoms and an improvement in the number of acid refluxes. The drug is a cholinergic agonist that works by directly increasing the contraction of the lower esophageal sphincter. There are potentially many risks of side effects that limit new studies on their effectiveness and safety.

Lifchtiz believes that the use of prokinetics should be analyzed with reservations. The drugs have the ability to accelerate gastric emptying and help increase the tone of the lower esophageal sphincter, which helps reduce the number of acid and non-acid reflux. Such drugs are indicated for failure of established antacid treatment, in an associated and not an isolated manner, and always with careful monitoring of side effects.

"Aceclidine": instructions for use

Prokinetics - what are they, how and in what cases should they be used? In any case, it is necessary to consult a doctor and carefully read the instructions for use.

Contraindications for use are coronary artery disease, increased HDL content, bronchial asthma, hyperkinesis and other parkinsonisms, pregnancy, bleeding from the abdominal organs.

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"Physiostigmine" is used mainly in ophthalmological practice, but sometimes it can also be used in gastroenterology when the medicine is injected under the skin with 0.5 - 1 ml of a 0.1% solution. The maximum amount of the drug per day should not exceed 0.001 g.

Side effects include increased salivation, bronchospasm, intestinal muscle spasm, changes in heart rate, and convulsions.

Contraindications: angina pectoris, epilepsy, bronchial asthma, mechanical intestinal obstruction, peritonitis, sepsis, pregnancy.

"Galantamine": instructions for use

Side effects: decreased heart rate, TTP, AV block, extrasystole, nausea, vomiting, diarrhea, dyspepsia, muscle spasms, urinary incontinence, hematuria, tremor.

New generation prokinetics

The most popular among gastroenterologists remains Motilium (the active ingredient is domperidone), which combines the qualities of metoclopramide, but does not have its negative consequences.

What are the most effective prokinetics? The list of drugs today includes:

"Itopride" (active ingredient) - "Ganaton", "Itomed", "Primer" (commercial names).
"Metoclopramide" - "Raglan", "Cerucal".
"Cisapride" - "Coordinax", "Prepulsid".
"Domperidone" - "Motilium", "Motilak", "Motinorm", "Passenger".

Now we know what prokinetics are. The list of them, as you can see, is very large. But remember, before using any drug you need to consult your doctor! Be healthy!

Attention, TODAY only!

Currently, a common reason for visiting doctors is problems in the gastrointestinal tract. Almost each of them is characterized by impaired motor function. However, they can appear as symptoms of a disease not related to the digestive system. In any case, there is no way to do without prokinetic drugs. The list of drugs in this group has no limiting framework. Therefore, each doctor selects a drug depending on the course of the disease. Next, let's take a closer look at what prokinetics are, a list of new generation drugs most often used for treatment.

Prokinetics: general characteristics

Medicines that change the motor activity of the intestinal tract, speed up the process of food transit and emptying, belong to this group.

As mentioned above, there is no single list of these drugs in the gastroenterological literature. Each doctor includes his own list of medications here. These include medications of other groups, such as: antiemetics, antidiarrheals, as well as some antibiotics of the macrolide group, hormonal peptides. First, let's find out what the pharmacological action of this group of drugs is.

Action of prokinetics

First of all, they activate the motility of the digestive tract and also have an antiemetic effect. Such drugs accelerate the emptying of the stomach and intestines, improve muscle tone of the gastrointestinal tract, and inhibit pyloric and esophageal reflux. Prokinetics are prescribed as monotherapy or in combination with other medications. They can be divided into several types according to the principle of action.

Types of prokinetics

The principle of action on different parts of the gastrointestinal tract differs for drugs such as prokinetics. The list of drugs should be divided into the following types:

1. Dopamine receptor blockers:

Selective 1st and 2nd generation.
Non-selective.

2. Antagonists of 5-HT3 receptors.

3. 5-HT3 receptor agonists.

And now more about these groups.

Dopamine receptor blockers

Drugs in this group are divided into selective and non-selective. Their action is that they stimulate motor function and have antiemetic properties. What are these prokinetics? The list of medications is as follows:

"Metoclopramide."
"Bromopride."
"Domperidone".
"Dimetpramide".

The main active ingredient is metoclopramide, it has been used for quite a long time. The action is as follows:

Increased activity of the lower esophageal sphincter.
Acceleration of stomach emptying.
Increasing the speed of food movement through the small and large intestines.

However, non-selective drugs can cause serious side effects.

There are widely known first-generation prokinetics. List of drugs:

"Cerucal".

"Raglan".
"Perinorm".
"Ceruglan".

One of the disadvantages is the ability to cause signs and symptoms of parkinsonism in adults and dyskinetic syndrome in children, and menstrual irregularities in women.

Second-generation selective drugs include drugs with the active ingredient domperidone. These medications do not cause severe side effects, but others may occur:

Drowsiness.
Weakness.
Anxiety.
Headache.

It is for this reason that drugs with the active substance domperidone are the best prokinetics. List of drugs:

"Motilium".
"Domidon".
"Motinorm".
"Motorix".
"Gastropom".

New generation prokinetics

Second-generation selective prokinetics include drugs with the active substance itopride hydrochloride. Such products have gained recognition due to their excellent therapeutic effect and the absence of side effects even with long-term use. Most often doctors prescribe:

"Itomed."
"Ganatom".
"Itopride."

This can be explained by the positive properties of itopride hydrochloride:

Improving the motor and evacuation function of the stomach.
Increased gallbladder activity.
Increasing the dynamism and tone of the muscles of the large and small intestines.
Promoting elimination

Intestinal prokinetics

These include prokinetics - 5-HT3 receptor agonists. The active substance is tegaserod. It has a positive effect on the motor and evacuation function of the large and small intestines. Helps normalize stool and reduce symptoms of irritable bowel.

Does not cause an increase in blood pressure and has no effect on the cardiovascular system. However, there are a fair number of side effects. The risk of stroke, angina pectoris, and anginal attack increases several times. Currently, drugs with this active substance have been discontinued in our country and in a number of other countries for further research. This includes the following prokinetics (list of drugs):

"Tegaserod."
"Zelmak".
"Fractal".

5-NT3 receptor antagonists

Prokinetics in this group are suitable for the treatment and prevention of nausea and vomiting. When taken, the residence time of food in the stomach decreases, the rate of food transit through the intestines increases, and the tone of the large intestine normalizes.

The release of acetylcholine is observed, and the motor function of the gastrointestinal tract improves. Currently, modern prokinetics are in great demand among patients and doctors. List of new generation drugs:

"Tropisetron".
"Sturgeon".
"Ondasetron".
"Silancetron".

I would like to note that 5-HT3 receptor antagonists do not have a therapeutic effect if vomiting is caused by apomorphine.

These drugs are well tolerated, although they have side effects:

Headache.
Constipation.
Flushes of blood.
Feelings of heat.

Another advantage of these drugs is that they do not have a sedative effect, do not interact with other medications, do not cause endocrine changes, and do not interfere with motor activity.

For what diseases is it prescribed?

As mentioned above, prokinetics are used in monotherapy or together with antibiotics. Doctors know that there are diseases for which the administration of prokinetics increases the effectiveness of treatment several times. This group includes:

Diseases of the digestive system with impaired motor activity.
Gastroesophageal
Peptic ulcer of the stomach (duodenum).
Idiopathic gastroparesis.
Vomiting.
Constipation.
Diabetic gastroparesis.
Flatulence.
Nausea caused by drug and radiotherapy, infection, functional disorders, poor diet.
Dyspepsia.
Biliary dyskinesia.

Who should not take it

There are contraindications for prokinetic drugs:

Hypersensitivity to the active substance.
Stomach or intestinal bleeding.
or intestines.
Intestinal obstruction.
Acute liver failure, kidney dysfunction.

Pregnant and nursing mothers

I would like to say a few words about taking medications during pregnancy. Studies have shown that prokinetics tend to pass into breast milk, so breastfeeding should not be continued during treatment with such medications.

During the first trimester of pregnancy, women often experience vomiting and nausea. In this case, it is possible to prescribe medications such as prokinetics. The list of drugs for pregnant women will include only those that do not pose a threat to the life of the pregnant woman and the fetus.

The benefits from it must exceed all possible risks. Prokinetics with the active substance metoclopromide can be used from this group only as prescribed by a doctor. Prokinetics are not prescribed in subsequent trimesters of pregnancy.

Currently, drugs in this group are not prescribed during pregnancy due to the large number of side effects.

Prokinetics for children

Prokinetics with the active substance metoclopramide should be used with particular caution in children, as there is a risk of dyskinetic syndrome. It is prescribed depending on the child's weight.

If a pediatrician prescribes prokinetics, Motilium is most often included in this list. It is well tolerated and has many positive reviews. But other prokinetics may be prescribed. The list of drugs for children may also contain the following names:

"Domperidone".
"Metoclopromide."

It is worth noting that for children under 5 years of age, Motilium is recommended to be used in the form of a suspension. The medicine is prescribed depending on the child’s weight, at the rate of 2.5 ml for every 10 kg of weight. If necessary, the dose can be increased, but only for babies older than one year. The drug is also available in the form of lozenges.

Prokinetics are prescribed to children if the child has:

Vomit.
Nausea.
Esophagitis.
Slow digestion of food.
Dyspeptic symptoms.
Frequent regurgitation.
Gastroesophageal reflux.
Impaired motility of the gastrointestinal tract.

It should be noted that in the very first months of life, the child’s body and all its functions are not very developed, so all medications should be taken under the strict supervision and control of a doctor. In case of overdose, prokinetics can cause neurological side effects in infants and young children.

A herbal preparation that improves digestion and reduces gas formation in the intestines is very popular among parents of infants. This is a concentrate based on Plantex fennel fruits.

It is worth saying a few words about plant prokinetics.

Natural Helpers

The way the world works is that the cure for any ailment can be found in some plant, you just need to know which one. Thus, plant prokinetics are known that stimulate the motor function of the gastrointestinal tract. Here are some of them:

Pharmaceutical camomile.
Black elderberry.
Dill.
Oregano.
Motherwort.
Dandelion.
Melissa.
Swamp dry grass.
The plantain is big.
Alder buckthorn.

The list of plants that help improve gastrointestinal motility includes a large number of other representatives of the flora. It should also be taken into account that some vegetables and fruits have a similar effect:

Swede.
Melon.
Cabbage.
Carrot.
Beet.
Pumpkin.
Cowberry.
Grape.

The prokinetic properties of these vegetables manifest themselves very well if you take fresh juices prepared from them.

It is worth noting that you should not replace herbal medications during periods of exacerbation of diseases and without consulting a doctor.

Side effects

It is very important that new generation prokinetics have much fewer side effects than first generation drugs with the active substance metoclopramide. However, even the newest drugs have side effects:

Headache.
Increased excitability.
Dry mouth, thirst.
Spasm of the smooth muscles of the gastrointestinal tract.
Hives, rash, itching.
Hyperprolactinemia.
Babies may exhibit extrapyramidal symptoms.

After discontinuation of the drug, side effects completely disappear.

If a doctor prescribes prokinetics, the list of drugs may include several drugs with different names, but with the same active ingredient. In this case, the side effects will be the same.

Features of the use of prokinetics

Prokinetics should be prescribed very carefully to people with liver failure and poor kidney function. Such patients should be under strict medical supervision.

With long-term use of prokinetic agents, patients should also visit their doctor more often. Use prokinetics with caution in young children, especially under one year of age.

Caution should be exercised when prescribing drugs from this group to elderly patients.

When treated with prokinetics, you should not engage in work that requires increased attention and quick response.

Before taking, you should definitely consult your doctor. Your health depends on it. You should not replace a medicine with its herbal counterpart without first consulting a doctor.

The antiemetic effect of motilium is due to a combination of gastrokinetic action and blockade of chemoreceptors of the trigger zone of the vomiting center. Motilium prevents the development or reduces the severity of vomiting and nausea.

After oral administration, motilium is quickly absorbed from the gastrointestinal tract. Food or low acidity of gastric juice slows down and reduces absorption. The maximum concentration in the blood is reached after 0.5–1 hour. Motilium is found in small amounts in breast milk. It is subjected to intensive metabolism in the intestinal wall and liver with the formation of hydroxydomperidone and 2,3-dihydro-2-oxo-1-H-benzimidazole-1-propionic acid, respectively. The half-life after a single dose is 7 hours and increases in chronic renal failure. 31% is excreted by the kidneys, of which 1% is excreted unchanged and 66% is excreted by the intestines (10% unchanged). Domperidone may accumulate in patients with liver disease.

Motilium belongs to the second generation prokinetics and, unlike the first generation prokinetics: cerucal, raglan and others (the active substance metoclopramide) does not penetrate well through the blood-brain barrier (BBB). Therefore, Motilium does not cause extrapyramidal disorders: spasms of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasms of extraocular muscles, spastic torticollis, opisthotonus, muscle hypertonicity and others. Motilium does not cause parkinsonism: hyperkinesis, muscle rigidity. Motilium less frequently and to a lesser extent than Cerucal and Raglan causes side effects such as drowsiness, fatigue, tiredness, weakness, headaches, increased anxiety, confusion, and tinnitus.