Metoclopramide - full information on the drug. Metoclopramide (Metoclopramide)
Anyone who has experienced a prolonged gag reflex and nausea does not wish anyone to experience such sensations. It is with a short vomiting that the body is cleared of everything unnecessary, but if it becomes prolonged, then the situation threatens with complete dehydration. Instructions for use "Metoproclamide" claims that the drug is able to stop this symptom and significantly alleviate well-being. It begins to act within minutes of application.
Tool "Metoproclamide": release forms and composition
The drug has two forms of release. These are tablets and solution for injection. Acts quickly and effectively "Metoproclamide". The composition of the drug in tablets includes the active substance metoclopramide hydrochloride in an amount of 10 mg. As additional elements used in the creation of the pill, lactose, corn starch, talc, sodium starch glycolate, colloidal anhydrous silicon are isolated.
1 ml of solution for injection contains about 5 mg of metoclopramide hydrochloride. Auxiliary components are disodium salt of ethylenediaminetetraacetic acid, sodium acetate, sodium metabisulfite, acetic acid and water for injection.
Tablets are packaged in aluminum blisters of ten pieces. The carton contains 50 or 100 tablets, as well as instructions for the use of Metoproclamide. Inside the injection drug is poured into 2 ml ampoules. The box may contain 5 or 10 glass ampoules.
Pharmacological effect of the drug on the body
Instructions for use "Metoproclamide" describes in detail all the subtleties of the reception and effects of the drug. The remedy itself belongs to antiemetic drugs. It has a direct effect on the reduction of nausea, vomiting and hiccups. Activates the peristalsis of the gastrointestinal tract. The antiemetic effect of the drug is associated with inhibition of dopamine D2 receptors and an increase in the index of chemoreceptors in the trigger area. The drug belongs to serotonin receptor blockers. It relieves the tone of the smooth muscles of the gastric organ and increases its cholinergic reflexes. The drug promotes gastric emptying, as it does not allow the walls of the gastric organ to relax and stimulates its antral part, the upper region of the small intestine. Reduces the reaction of food in the esophagus by increasing the pressure of the esophageal sphincter in a relatively calm state. Increases clearance of gastric acid due to increased peristalsis.
Metoclopramide also activates the production of prolactin and provokes a transient increase in the rate of circulating aldosterone. A similar picture can cause temporary fluid retention in the body.
The taken tablets are absorbed from the gastrointestinal tract in a short time. Connect with blood proteins by 30%. Biotransformirovatsya in the liver. The body excretes the active substance in unchanged form and in the form of metabolites by the kidneys. The half-life of the drug is four to six hours.
"Metoproclamide": indications for use and contraindications
The drug is quite serious, it can not be used without a doctor's prescription. As a rule, the drug is used for nausea, gag reflex, hiccups, provoked by various situations. It is prescribed for atony and hypotension of the gastrointestinal environment, including postoperative, the drug "Metoproclamide". Indications for use note that the drug is effective in dyskinesia of the bile ducts belonging to the hypomotor class. It is recommended to drink tablets for reflux esophagitis, functional pyloric stenosis and flatulence. The drug is used in the complex treatment of gastric and duodenal ulcers that are in the acute stage. The drug increases the peristalsis of the gastrointestinal tract during x-ray studies. The tool facilitates the condition with duodenal sounding. Here it enhances the process of movement of the absorbed food through the small intestine and in every possible way contributes to faster emptying.
Warns that people with hypersensitivity to the active substance and its auxiliary components should not be taken Metoproclamide, instructions for use. In ampoules and tablets, the medicine is not allowed for persons who have undergone surgery on the organs of the gastrointestinal tract.
Specialists with extreme caution advise the drug to patients with bronchial asthma, having arterial hypertension and suffering from Parkinson's disease. Care should be taken to use the medicine in patients with renal or hepatic insufficiency, as well as in children and the elderly over the age of 65 years.
Can be used both orally and in injectable form, the drug "Metoproclamide". Instructions for use of the tablet advises adults to drink 5-10 mg 3-4 times a day half an hour before a meal, drinking a dragee with water.
Warns that the use of the drug "Metoproclamide" can distort laboratory parameters, instructions for use. Tablets and injections can cause changes in the level of aldosterone and prolactin in the blood. This feature must be taken into account by people when taking a blood test.
Experts do not recommend during therapy with Metoproclamide (the annotation before using the drug should be carefully studied in order to avoid undesirable consequences) to engage in activities that require increased attention and quick reactions.
Drugs that can replace Metoclopramide
To date, there are not many drugs that can replace Metoproclamide. Analogues contain the same active ingredient and have similar properties. These include:
- "Cerucal".
- "Perinorm".
- "Metukal".
- "Raglan".
- "Apo-Metoclops".
- Metamol.
- "Cerulan".
- Melomide hydrochloride.
In all of the above medicines, the main active ingredient is metoclopramide hydrochloride. Due to which it is they who are referred to as direct analogues of Metoclopramide. Medicines differ among themselves in cost and manufacturer. Some drugs are produced in European countries on modern equipment with several degrees of purification.
Should I replace Metoproclamide? Analogues are approximately the same in their effectiveness. They have identical effects on the body and, as a rule, are used in equal doses. Therefore, which remedy is better to choose or leave "Metoclopramide" should be decided by the patient after consulting a doctor.
"Cerucal" as an analogue of "Metoclopramide"
Cerucal is the direct and most common substitute for Metoclopramide. The tool removes nausea, hiccups and vomiting of various origins. It is used in radiation therapy and taking cytostatics. The medicine has contraindications and can cause a number of negative symptoms. It also passes through breast milk. The highest concentration of the active substance is observed half an hour after the use of the medication.
The cost of the medicine fluctuates around 200-300 rubles. Produce the drug in Germany and Croatia.
metoclopramide(lat. metoclopramide) - a drug for the treatment of functional disorders of the upper gastrointestinal tract (GIT), antiemetic, prokinetic of the 1st generation.
Chemical compound : 4-Amino-5-chloro-N--2-methoxybenzamide. Empirical formula C 14 H 22 ClN 3 O 2 . In medicinal preparations, it is used in the form of hydrochloride.
Metoclopramide hydrochloride is a white, odorless crystalline substance soluble in water and ethyl alcohol.
Metoclopramide is the international non-proprietary name (INN) of the drug. According to the pharmacological index, it belongs to the group "Gastrointestinal motility stimulants, including emetics." According to ATC - to the group "Gastrointestinal motility stimulants" and has the code A03FA01.
Metoclopramide blocks central dopamine D 2 receptors of the chemoreceptor trigger zone and reduces the sensitivity of afferent nerves that transmit impulses from the stomach and duodenum to the vomiting center, and also blocks peripheral dopamine D 2 receptors and, thus, eliminates dopamine inhibition of motor activity and increases tone upper GI tract. 
Therefore, as an antiemetic drug, metoclopramide is effective in nausea and vomiting of various nature, including those caused by cancer chemotherapy, associated with anesthesia, side effects of drugs, liver and kidney diseases, uremia, craniocerebral injury, vomiting of pregnant women, violation of the diet (with the exception of vomiting of vestibular origin).
Metoclopramide in high doses inhibits serotonin 5HT 3 receptors, which promote relaxation of smooth muscle tissues, and at the same time stimulates serotonin 5HT 4 receptors, which increase the contraction of muscle fibers. Thus, metoclopramide, by stimulating contractions and strengthening the tone of the smooth muscles of the walls of the hollow organs of the digestive tract, increases the duration of peristalsis of the antral part of the stomach and duodenum, does not slow down the emptying of the stomach, increases the tone of the lower esophageal sphincter, increasing pressure in the gallbladder and bile ducts, normalizes the separation of bile , reduces spasm of the sphincter of Oddi, eliminates dyskinesia of the gallbladder.
In migraine, metoclopramide is used to prevent gastric stasis and nausea, as well as to stimulate the absorption of anti-migraine drugs taken by mouth. Suppresses the central and peripheral action of apomorphine, increases the secretion of prolactin, causes a transient increase in the level of aldosterone, increases the sensitivity of tissues to acetylcholine.
Metoclopramide penetrates well through histohematic barriers, including through the blood-brain barrier (BBB), the placental barrier, and penetrates into breast milk. As a result of its penetration through the BBB, extrapyramidal disorders become possible (spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of the extraocular muscles, spastic torticollis, opisthotonus, muscle hypertonicity, etc.), as well as sedative effects, weakness, impaired mental activity and this loses to the prokinetics of the next generations (domperidone, itopride). 
Metoclopramide is rapidly and well absorbed after oral administration, the maximum concentration is reached 1-2 hours after taking a single dose, bioavailability is 60-80%. Plasma protein binding is about 30%. The half-life with normal kidney function is about 4-6 hours, with impaired renal function - up to 14 hours. After ingestion, approximately 85% of metoclopramide is excreted in the urine in unchanged form and in the form of sulfate and glucuronide conjugates within three days.
The action of metoclopramide begins 1-3 minutes after intravenous administration, 10-15 minutes after intramuscular administration, 30-60 minutes after ingestion, the effect lasts 1-2 hours.
Professional medical publications concerning the effects of metoclopramide on the gastrointestinal tract:
- Sheptulin A.A., Trukhmanov A.S., Khromov V.L. Comparative evaluation of the effectiveness of treatment of gastroesophageal reflux disease with coordinax and metoclopramide. // Russian Journal of Gastroenterology, Hepatology, Coloproctology. - 1998. - No. 4. - C. 94–97.
- Grigoriev P.Ya., Yakovenko E.P., Agafonova N.A. Cerucal in gastroenterological practice // Farmateka. 2003. - No. 10. - pp. 24–27.
Metoclopramide is used to treat:
- achalasia cardia
- chronic gastritis with a decrease in the motor-evacuation function of the stomach
- gastroptosis
- gastric ulcer with normal and low acidity and weakening of muscle tone and peristalsis
- atony and hypotension of the stomach and duodenum that developed in the postoperative period (gastroparesis)
- biliary dyskinesia hypokinetic type
Application restrictions. Bronchial asthma, arterial hypertension, hepatic or renal insufficiency, old age. With parenteral administration - age up to 14 years.
Side effects . The frequency of side effects depends on the dose and duration of taking metoclopramide. Nervous system and sense organs: restlessness (about 10%), drowsiness (about 10%, more common with high doses), unusual tiredness or weakness (about 10%). Extrapyramidal disorders, including acute dystonic reactions (0.2% at doses of 30-40 mg / day), such as convulsive twitching of the facial muscles, trismus, opisthotonus, muscle hypertonicity, spastic torticollis, spasm of the extraocular muscles, rhythmic protrusion of the tongue, bulbar type of speech; rarely - stridor and dyspnea, possibly due to laryngospasm. Parkinsonian symptoms: bradykinesia, tremor, muscle rigidity. Tardive dyskinesia, including involuntary movements of the tongue, puffing of the cheeks, uncontrolled chewing movements, uncontrolled movements of the arms and legs (in the elderly, with chronic liver failure). Insomnia, headache, dizziness, disorientation, depression, anxiety, confusion, tinnitus; rarely - hallucinations. The cardiovascular system: hypotension, hypertension, tachycardia, bradycardia, fluid retention. Digestive system: constipation, diarrhea, dry mouth; rarely - hepatotoxicity. The immune system: rarely - allergic reactions . Endocrine system: hyperprolactinemia; very rarely - galactorrhea, gynecomastia and amenorrhea. Integumentary system: urticaria, pruritus. Others: frequent urination, urinary incontinence, asymptomatic mild hyperemia of the nasal mucosa, agranulocytosis.
Antipsychotics, especially phenothiazines and butyrophenone derivatives, increase the likelihood of developing extrapyramidal disorders. With simultaneous use reduces the effectiveness of levodopa. When taken with drugs that cause CNS depression - increased sedative effect. When co-administered with cyclosporine, the reduction in gastric emptying time caused by metoclopramide may increase the bioavailability of cyclosporine. It is possible to reduce the absorption of digoxin in the stomach and accelerate the absorption of mexiletin. Accelerates the absorption of paracetamol, tetracycline. The combined use of metoclopramide with drugs containing opioids may block the effect on peristalsis. Simultaneous use with metoclopramide may reduce the effect of cimetidine due to a decrease in its absorption.
With an overdose of metoclopramide, excessive drowsiness, confusion, extrapyramidal disorders occur, disappearing within a day after stopping the drug.
Dosage and administration:
- Adults: inside - 5-10 mg 3 times a day before meals, intramuscularly or intravenously 10 mg. The maximum single dose is 20 mg, the maximum daily dose is 60 mg.
- Children over 6 years old - 2.5-5 mg 1-3 times a day, children under 6 years old - 0.5-0.1 mg / kg / day; the maximum single dose is 0.1 mg / kg.
- For patients with hepatic or renal insufficiency, the initial dose is reduced by 2 times, the subsequent dose depends on the individual patient's response.
- The duration of taking metoclopramide should not exceed 12 weeks.
- In case of hypersensitivity to procaine or procainamide, hypersensitivity to metoclopramide is possible.
- Do not take after gastrointestinal surgery as increased motility interferes with healing.
- Patients with a history of depression should only take metoclopramide if the expected benefit outweighs the potential risk.
- Extrapyramidal disorders can occur when metoclopramide is taken at therapeutic doses in people of any age, and the higher the dose of metoclopramide, the higher the likelihood of their occurrence. Extrapyramidal disorders often occur in patients younger than 30 years and in the first two days of taking the drug.
- Parkinsonian symptoms usually appear within the first six months of starting treatment, but may occur later. These symptoms usually disappear within 2 to 3 months after stopping metoclopramide.
- Tardive dyskinesia often develops in elderly patients, especially in women. The appearance of signs or symptoms of tardive dyskinesia is usually noted after continuous treatment for at least 1 year and may persist after discontinuation of the drug.
- Taking metoclopramide can distort laboratory parameters: liver function tests, aldosterone and prolactin levels in blood serum.
Acute and chronic diseases of the gastrointestinal tract, intoxication, stress and other causes can provoke an unpleasant phenomenon for every person - vomiting. To prevent the negative consequences of this natural reflex of the body, such as dehydration or inflammation of the esophagus, urgent measures must be taken. The drug Metoclopramide is designed to quickly eliminate attacks of eruption and alleviate the patient's condition. What is its feature?
Instructions for use Metoclopramide
The drug belongs to the group of drugs intended for the treatment of disorders in the digestive system, has a pronounced antiemetic effect. Metoclopramide is a first-generation prokinetic agent effective in functional disorders of the upper stomach and duodenum. The chemical structure of the drug is similar to dimetpramide, sulpiride.
Composition and form of release
The active ingredient of the drug is metoclopramide hydrochloride, which is a white, odorless crystalline substance. The element is soluble in water, ethanol. Pharmaceutical companies produce two forms of the drug - in the form of a dragee and a solution for injection. You can get acquainted with their detailed composition from the presented table:
| Description | Metoclopramide vomiting tablets | Solution for intramuscular injection |
| Active substance | Metoclopramide hydrochloride 10 mg |
|
| Auxiliary components | Sodium starch glycolate, lactose, magnesium stearate, colloidal anhydrous silica, povidone, corn starch | Glacial acetic acid, sodium metabisulfite, disodium salt of ethylenediaminetetraacetic acid, sodium acetate, water |
| Blister of 10 tablets | Dark colored ampoules in a plastic tray |
|
pharmachologic effect
The component neutralizes the central dopamine D2 receptors of the chemoreceptor trigger site, reduces the sensitivity of afferent nerve endings that send signals from the stomach and duodenum to the emetic block. Metoclopramide suppresses peripheral dopamine D2 impulses, eliminating the slowdown in motor activity and increasing the tone of the upper digestive tract.
Significant doses of the drug can inhibit serotonin 5HT3 receptors, designed to relax the smooth muscles of the walls of organs, and increase the contraction of muscle fibers. This effect prevents inhibition of gastric emptying, prolongs the peristalsis of the antral gastric zone, stimulates the lower esophageal sphincter. In addition, after taking the substance, the pressure in the gallbladder and ducts rises, as a result of which bile secretion increases and dyskinesia of the organ is eliminated.
The drug is widely used for migraine, its action is aimed at protecting against stasis, hiccups and nausea, and at improving the absorption of painkillers. The active ingredient blocks the activity of apomorphine, stimulates the production of prolactin, increases the level of aldosterone, increases the response of cells to acetylcholine. It perfectly passes the blood-brain and placental barrier, penetrates into breast milk, which can cause extrapyramidal disorders, such as:
- muscle spasms of the face;
- rhythmic protrusion of the tongue;
- muscle hypertonicity;
- spastic torticollis;
- lockjaw;
- stiffness of the extraocular muscles;
- opisthotonus.
The drug has a high rate of absorption in the intestine, the maximum concentration of its elements is reached 2 hours after consumption. Bioavailability is about 60-80%. Excretion of metoclopramide occurs through the kidneys, 85% of the substance is excreted in the urine in the form of glucuronide and sulfate conjugates. The effect of the drug begins 1-2 minutes after intravascular injection, 10-15 minutes with intramuscular injection, 1 hour after consumption of tablets.
Indications for use
The drug is prescribed to stop the gag reflex, nausea, hiccups, including when using cytostatics and after undergoing a course of radiation therapy. The main indications for taking the medicine are:
- excessive gas formation;
- atony, hypotension of the intestines and stomach (functional and postoperative);
- biliary dyskinesia;
- gastroesophageal reflux disease, accompanied by inflammation of the esophagus;
- ulcers of the alimentary canal;
- pyloric stenosis of functional origin;
- dyspepsia;
- improving the movement of food to the small intestine before duodenal sounding;
- acceleration of peristalsis before a diagnostic study of the digestive system.
Method of application and dosage
The standard drug treatment regimen provides for 3-4 single doses per day of 5-10 mg of the substance for an adult patient. The maximum allowable daily dose is 60 mg. Nausea tablets Metoclopramide is prescribed for oral use, and the solution is used parenterally in severe cases of illness. The recommended amount of medication for children over 15 years old is no more than 15-30 mg daily, depending on body weight.
The dragee form of metoclopramide is designed for oral use, preferably half an hour before a meal. The pills are swallowed whole with water without gases. The duration of the therapeutic course is 4-6 weeks, but on the recommendation of a doctor, the use of the drug can last up to 6 months. According to the instructions, the following treatment regimens have been developed:
- adults - 1 capsule 3-4 times a day;
- adolescents 15-19 years old - 0.5-1 tablet 3 times a day;
- before the examination - 1-2 tablets once 10-15 minutes before the procedure;
Metoclopramide in ampoules
The use of injections with a solution should be intravenous and intramuscular. The substance is administered 1-3 times a day in a volume of 10-20 mg. With the joint administration of cytostatics and in the period after radiation therapy, a single dose of the drug is determined at the rate of 2 mg per kilogram of the patient's weight. Before the examination, metoclopramide is administered 15 minutes in a dosage of 10-20 mg.
special instructions
Specialists distinguish cases when the drug is prescribed with caution. These include Parkinson's disease, liver and kidney dysfunction, arterial hypertension, bronchial asthma. Older people taking pills are at risk of developing tardive dyskinesia, parkinsonism. The presence of a substance can distort data on the level of prolactin, aldosterone when conducting appropriate tests. During treatment, you should give up alcohol, driving and activities that require concentration.
metoclopramide during pregnancy
The active ingredient easily passes the placental barrier, so the drug is contraindicated in pregnant women. Part of metoclopramide is concentrated in the mammary gland, which can harm the newborn during lactation. If the expected benefit from the consumption of the drug is higher than the child's need for breast milk, then for the entire treatment period, the nursing patient is advised to refrain from breastfeeding.
Metoclopramide for children
In young children, while taking Metoclopramide, a dyskinetic syndrome may develop, and therefore the appointment of the substance to persons under 15 years of age by medical specialists is extremely rare. It is forbidden to take the component for more than 12 weeks in a row for adolescents, since there is a high probability of extrapyramidal reactions of the body.
drug interaction
With one-time therapy with neuroleptics, the risk of extrapyramidal events increases. A decrease in the therapeutic effect of the drug element is observed when cholinesterase inhibitors are taken together. The element is able to enhance the activity of histamine receptor blockers, the sedative effect of sleeping pills and the effect of ethanol on the nervous system. The drug reduces the function of Cimetidine, Digoxin, but increases the absorption of the following drugs:
- tetracycline antibiotics;
- Paracetamol;
- Acetylsalicylic acid;
- Levodopa;
- diazepam.
Side effects and overdose
The manifestation of negative consequences from taking Metoclopramide directly correlates with the amount and duration of the drug. Possible side effects include:
- dry mouth;
- constipation, diarrhea;
- leukopenia;
- sulfagemoglobinemia;
- neutropenia;
- anxiety;
- weakness;
- hyperthermia;
- depression;
- headache;
- parkinsonism;
- drowsiness;
- distraction;
- vegetative instability;
- porphyria;
- bronchospasm;
- hives;
- violation of hematopoiesis;
- failure of the menstrual cycle;
- gynecomastia;
- agranulocytosis;
- hyperemia of the nasal mucosa.
If the dosage regimen is not observed or a medical element is taken without the consent of the attending physician, extrapyramidal dysfunctions, hypersomnia, mental confusion may occur. The appearance of at least one of these symptoms requires immediate discontinuation of the medication. To avoid a repeated case of an overdose, it is necessary to correct the scheme for further use of the substance by the doctor.
Contraindications
Metoclopramide is not prescribed after pyloroplasty, intestinal anastomosis, since muscle tone slows down the healing process. Caution should be used in the treatment of children, the elderly, patients with Parkinson's disease and bronchial asthma. Absolute contraindications for drug therapy include:
- mechanical intestinal obstruction;
- internal bleeding;
- glaucoma;
- violation of the integrity of the intestine or stomach;
- epileptic syndrome;
- hypersensitivity to sulfites;
- breast tumor;
- severe renal and hepatic insufficiency;
- individual intolerance to the components of the substance;
- pheochromocytoma (due to the risk of a hypertensive crisis associated with the release of catecholamines);
- stenosis of the pylorus of the stomach;
- prolactin-dependent neoplasms;
- pregnancy;
- children's age up to 14 years.
Terms of sale and storage
The drug is in the assortment of many pharmacy chains, you can buy it with a prescription. It is necessary to store the medicine in a dry, dark place at temperatures up to +25 ºС. Keep away from children. Shelf life - 2 years, after its expiration, unused tablets or ampoules should be disposed of.
Analogues
On the pharmaceutical market, medicinal compounds are presented that have a similar structural composition and spectrum of action with Metoclopramide. It is forbidden to cancel or replace the medication without the consent of a specialist. Among the popular analogues of the component are:
- Cerucal is an effective antiemetic prescribed by physicians for impaired motility of the upper gastrointestinal tract in adults and children over 14 years of age.
- Doprokin is a dopamine antagonist that has an antipsychotic and antiemetic effect. Stimulates gastric motility. It has low permeability through the blood-brain barrier.
- Motilak - increases the duration of peristaltic contractions of the antral gastric region, eliminates attacks of vomiting and nausea. When slowing down the emptying of the stomach, the element accelerates this process.
- Reglan is a blocker of dopamine D2 receptors that successfully fights the gag reflex of any origin. It has a positive effect on the functioning of the digestive system.
- Emetron - applicable for the prevention and treatment of nausea and vomiting, provoked by the implementation of cytotoxic radio- or chemotherapy.
Metoclopramide price
The cost of a pharmaceutical product varies depending on the manufacturer and region of sale. The average price of a pack of 50 tablets ranges from 22 to 55 rubles, and 10 ampoules - from 72 to 110 rubles. You can get acquainted with the prices set for a medicine in Moscow from the table.
The drug metoclopramide is a specific blocker of serotonin or dopamine receptors. The tool prevents the emetic effect, and also helps to suppress hiccups and, as well as regulates the influence of the function of the gastrointestinal tract. Under the influence of substances, the tone and activity of the digestive organs increase. There are known cases of complete cure of such diseases of the duodenum and stomach.
Metoclopramide instructions for use
The international name is Metoclopramide (Metoclopramide).
Trade name - Metoclopramide (Metoclopramide).
Composition and forms of release
Pills(blisters) 10 mg (metoclopramide hydrochloride 10 mg). Excipients: lactose, corn starch, talc, magnesium stearate, sodium starch glycolate, silicon dioxide colloidal anhydride.
Injection 1 ml (metoclopramide hydrochloride 5 mg).
Excipients: disodium salt of ethylenediaminetetraacetic acid; sodium metabisulphite; sodium acetate; glacial acetic acid; water for injections.
In dark glass ampoules of 2 ml; in a plastic pallet 5 pcs.; in a cardboard box 1 or 2 pallets.
Pharmacological group
antiemetic - dopamine receptor antagonist central
pharmachologic effect
- antiemetic
- accelerating gastrointestinal motility
- dopamine-blocking central
Indications for the use of metoclopramide
Vomiting, nausea (narcosis, radiation therapy, diseases of the liver and kidneys, traumatic brain injury, migraines, Tourette's syndrome - generalized tics and vocalization in children, myocardial infarction, heart failure, side effects of drugs: digitalis preparations, cytostatics, antibiotics, morphine and others); vomiting of pregnant women, hiccups of various origins; atony and hypotension of the stomach and intestines (including postoperative, diabetic neuropathy); reflux esophagitis; flatulence. As part of complex therapy: peptic ulcer of the stomach and duodenum; acceleration of peristalsis during radiopaque studies of the gastrointestinal tract.
- Gastroesophageal reflux
- Gastroesophageal reflux with esophagitis
- gastrojejunal ulcer
- alcoholic liver disease
- Abnormal breathing
- Intracranial trauma
- hiccup
- peptic ulcer
- Flatulence
- Liver failure
- Head injury
- chronic hepatitis
- Fibrosis and cirrhosis of the liver
- Toxic damage to the liver
- Nausea and vomiting
- Esophagitis
- Esophageal ulcer
- Duodenal ulcer
- stomach ulcer
- Ulcerative colitis
Pharmacodynamics
A specific blocker of dopamine (D2) receptors, as well as serotonin (5-HT3) receptors, which inhibits chemoreceptors of brainstem trigger zones, weakens the sensitivity of visceral nerves that transmit impulses from the pylorus and duodenum to the vomiting center.
It has a regulating and coordinating effect on the tone and motor activity of the digestive organs through the hypothalamus and the autonomic nervous system (parasympathetic innervation of the gastrointestinal wall). As a result, it accelerates gastric emptying, prevents pyloric and esophageal reflux, and stimulates intestinal motility.
Normalizes the separation of bile, reduces spasm of the sphincter of Oddi without changing its tone, eliminates dyskinesia of the gallbladder.
Does not have parasympatholytic, antihistamine, antiserotonin and ganglioblocking action; does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as the kidneys and liver, hematopoiesis, secretion of the stomach and pancreas.
Stimulates the secretion of prolactin (similar to other dopamine receptor blockers).
The therapeutic effect of the drug in gastroenterological practice is associated with an increase in the tone of the stomach and intestines, an acceleration in the emptying of the stomach and pylorus, and a decrease in hyperacid stasis.
The onset of action on the digestive apparatus is noted 20-40 minutes after oral administration and is manifested by an acceleration of the evacuation of the contents of the stomach for about 3 hours and an antiemetic effect (lasting 12 hours).
Pharmacokinetics
After oral administration, it is rapidly and completely absorbed, reaching the maximum level in the blood plasma after 30-120 minutes. Due to partial destruction in the liver after absorption, the bioavailability of the drug is 75%. The therapeutic effect after oral administration and intravenous administration is the same.
Undergoes biotransformation in the liver. T1 / 2 - about 4-6 hours. 30% of the administered dose is excreted by the kidneys unchanged. Easily penetrates the blood-brain and placental barrier. By stimulating the secretion of aldosterone, it enhances sodium retention and potassium excretion.
Dosing regimen
Adults, before meals. Assign 5-10 mg 3-4 times a day. With vomiting, severe nausea, it is administered intramuscularly or intravenously at a dose of 10 mg. The maximum single dose is 20 mg; daily - 60 mg (for all routes of administration).
Children over 6 years old appoint 5 mg 1-3 times a day (in the form of tablets, drops, injections).
Children under 6 years old administered orally in drops or parenterally.
The daily dose for parenteral administration is 0.5-1 mg/kg of body weight; multiplicity 1-3 times. Before an x-ray examination, adults are administered 1-2 ampoules (10-20 mg) intravenously or administered orally (5-15 minutes before the start of the study) 15-30 mg. Patients with clinically severe hepatic and renal insufficiency are initially prescribed a dose that is half the usual dose, the subsequent dose depends on the patient's individual response to metoclopramide.
The action of metoclopramide begins 1-3 minutes after intravenous administration, 10-15 minutes after intramuscular administration, 30-60 minutes after ingestion, the effect lasts 1-2 hours.
The use of metoclopramide is used to treat many diseases. The correct approach to treatment methods is important, taking into account the individual characteristics of the body. As a rule, self-treatment is not recommended in order to avoid serious complications that may be caused by side effects.
Side effects
Extrapyramidal disorders, parkinsonism (hyperkinesia, muscle rigidity - a manifestation of dopamine-blocking action) in children and adolescents, increases when the daily dose of 0.5 mg / kg of body weight is exceeded. Spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of the extraocular muscles (including oculogeric crises), unnatural position of the head and shoulders, opisthotonus, muscle hypertonicity. Drowsiness, fatigue, anxiety, confusion, headache, tinnitus, dyspepsia, dry mouth, urticaria, gynecomastia, galactorrhea.
Contraindications
- hypersensitivity, bleeding in the gastrointestinal tract;
- intestinal obstruction;
- perforation of the gastrointestinal tract (including other conditions when increased motor activity of the gastrointestinal tract is undesirable);
- pheochromocytoma (hypertensive crisis due to the release of catecholamines from the tumor), epilepsy;
- vomiting in patients with breast cancer;
- use with caution in children under 14 years of age (parenteral administration).
Pregnancy and lactation
Contraindicated for use during pregnancy.
When used during lactation (breastfeeding), it should be borne in mind that metoclopramide passes into breast milk.
In experimental studies, no adverse effects of metoclopramide on the fetus have been established.
Interaction
It enhances the effect of ethanol on the central nervous system (during the period of treatment with metoclopramide, patients should not drink alcoholic beverages because of the risk of developing possible complications), the effectiveness of therapy with H2-histamine blockers for severe reflux esophagitis. Increases the absorption of acetylsalicylic acid, paracetamol, diazepam, ethanol, levodopa, tetracycline, ampicillin (due to faster evacuation of stomach contents). Reduces the absorption of digoxin and cimetidine (acceleration of intestinal motility).
special instructions
Metoclopramide is discontinued 3-4 days after operations such as pyloroplasty or intestinal anastomosis, as vigorous muscle contractions do not promote healing of sutures. Against the background of treatment, the ability to drive cars and perform work that requires concentration may be impaired. Most side effects occur within 36 hours from the start of treatment, they disappear within 24 hours after discontinuation of the drug.
Storage conditions
In a place protected from light.
Vacation from pharmacies
By prescription.
Synonyms
Metoclopramide hydrochloride, Raglan, Cerucal, Perinorm, Clomethol, Bimaral, Comportan, Gastrobids, Imperial, Maxolon, Regastrol, Rimetin, Terperan, Viscal, Clopan, Emetizan, Legir, Maxeran, Metoclol, Moriperan, Nauzifar, Paspertine, Peraprin, Plastil, Pramin , Primperan, Primperil, Reliverin.
Similar drugs
Domstal (Domstal) Domrid / Domrid SR (Domrid / Domrid SR) Motoricum (Motoricum) Dimetpramide (Dimethpramidum) Dimetkarb (Dimetcarbum).
The article tells: for whom the drug "Metoclopramide" is intended, what it helps from and what side effects and contraindications it has.
The medicine "Metoclopramide": from what
pharmachologic effect
The drug "Metoclopramide" is included in the group of drugs with antiemetic action. The drug effectively eliminates nausea and hiccups, and also stimulates the peristalsis of the gastrointestinal system. It can be noted the speed of the drug "Metoclopramide". From what he is very much in demand by patients. So after intravenous administration, the therapeutic effect occurs after two minutes, with intramuscular injections - after a quarter of an hour. Antiemetic action lasts up to half a day.
Release form and analogues (synonyms)
The medicine is produced in the form of tablets and solution for intramuscular and intravenous administration. Both types of the drug contain 10 mg of the active substance. In the form of tablets in the same dosage as the drug "Metoclopramide", synonymous drugs are produced: Cerulan, Vero-Metoclopramide, Perinorm, Metoclopramide-Fpo, Metoclopramide-Akri.
The drug "Metoclopramide": from what is used
The main indications for prescribing the drug are:
- Reflux esophagitis;
- Flatulence;
- X-ray contrast studies of the gastrointestinal tract;
- Exacerbations of gastric ulcer;
- Pathology of the duodenum;
- Atony and hypotension of the stomach and intestines;
- Vomiting, hiccups or nausea of various origins;
- Biliary dyskinesia;
- Vomiting caused by taking cytostatics.
Contraindications
The drug should not be used when:
- Hypersensitivity;
- Prolactin-dependent tumors;
- Mechanical intestinal obstruction;
- Extrapyramidal disorders;
- Simultaneous use with anticholinergic drugs;
- epilepsy;
- Pheochromocytoma;
- Glaucoma;
- Bleeding from the gastrointestinal system.
It is forbidden to make treatment during pregnancy and breastfeeding of children. Caution is required to prescribe medication for:
- arterial hypertension;
- Parkinson's disease;
- Bronchial asthma;
- Impaired liver or kidney function;
Due to the risk of developing a dyskinetic syndrome, caution should be given to prescribing Metoclopramide to children.
Instructions for use
In tablets, 10 mg is used 3-4 times a day, maximum - 20 mg. With severe vomiting and nausea, the drug is administered intravenously or intramuscularly, usually at a dose of 10 mg. In addition, you can use the drug intranasally, instilling 10-20 mg into each nostril several times a day. The dose for children depends on age. Usually the daily dose for children under 6 years of age in tablets is 0.5-1 mg per 1 kg of weight. The drug is taken up to 3 times a day. The remedy for children over 6 years of age is prescribed up to 5 mg three times a day. Maximum for any dosage forms is used up to 60 mg. It is undesirable to use the drug "Metoclopramide" at the same time:
- With a slowly dissolving dosage form of digoxin;
- With fluoxetine and fluvoxamine due to the risk of developing extrapyramidal disorders;
- With antipsychotics, especially derivatives of butyrophenone and the phenothiazine series, due to an increased risk of extrapyramidal reactions;
- With anticholinergics due to the possible mutual weakening of the effects.
Also with caution with tolterodine, morphine, nitrofurantoin, ketoprofen, zopiclone, mefloquine, cabergoline, mexiletine due to changes in the expected therapeutic effect.
Side effects
When using the medicine, you may experience:
- menstrual irregularities, galactorrhea
- gynecomastia, as well as skin rash, are rare, with prolonged use in high doses
- agranulocytosis, usually manifesting at the beginning of treatment
- rarely - dry mouth
- at the beginning of treatment - constipation or diarrhea
- akathisia
- headache
- depression
- feeling tired
- dizziness
- drowsiness
In children, the drug can cause extrapyramidal symptoms, manifested as spastic torticollis, facial muscle spasm and hyperkinesis. In the elderly, with prolonged use, the phenomena of dyskinesia and parkinsonism are possible. During the treatment period, it is recommended to avoid potentially hazardous activities that require increased attention and rapid psychomotor reactions.
