Metoclopramide is an antiemetic medication. The Latin name for this drug is Metoclopramide. It is produced by several pharmaceutical companies - LLC "Ellara", Federal State Unitary Enterprise "Moscow Endocrine Plant", CJSC "PharmFirma SOTEKS", OJSC "Novosibkhimfarm", LLC "Promomed Rus", Indian company PROMED EXPORTS, CJSC "PFC Renewal", Belarusian Borisov Plant of Medicinal Products, Polish JSC "Pharmaceutical Plant POLFARMA". Below is a detailed description of the Metoclopramide solution.
Composition and formulation of the drug
The drug is available in two dosage forms - in the form of tablets and liquids for intravenous and intramuscular use. The percentage of the solution "Metoclopramide" is 0.5%, it is poured into ampoules, in a volume of 2 ml. Packed in glass ampoulescardboard packs of 5 or 10 pieces or 5 or 10 ampoules - in plastic or cell contour pallets, 1 or 2 pallets in a cardboard box.
In the composition of the injection solution of the drug there is an active element - metoclopramide hydrochloride.
Pharmacological action
Metoclopramide solution belongs to the category of specific blockers of serotonin (5-HT3) and dopamine (D2) receptors. It contributes to the suppression of the activity of chemoreceptors, which are localized in the trigger area of the brain stem, and reduces the sensitivity of the visceral nerves responsible for the transmission of impulses from the pylorus and duodenum to the vomiting receptors. The drug "Metoclopramide" affects the parasympathetic system and the hypothalamus, which contributes to the innervation of the digestive tract and coordinate and regulate the tone of the upper gastrointestinal tract (including the lower esophageal sphincter) and its motor activity. In addition, the drug increases the tone of the intestines and stomach, activates intestinal peristalsis, accelerates the process of removing food from the stomach, prevents the occurrence of esophageal and pyloric reflux, and reduces the intensity of hyperacid stasis.
The drug normalizes the production of bile and eliminates spasms of the sphincter of Oddi and dyskinesia of the gallbladder, without affecting the tone of the latter. For the active element, it is uncharacteristic, m-anticholinergic, ganglioblocking, antihistamine and antiserotonin action. In addition, this substance does not change the functioningliver and kidneys, respiratory function, has no effect on the vascular tone of the brain, vascular pressure, hematopoiesis, secretion of the pancreas and stomach. The drug stimulates the synthesis of prolactin and increases the sensitivity of body tissues to acetylcholine (this effect is not determined by vagal innervation, but is stopped with the help of anticholinergics). In addition, it activates the production of aldosterone, while slowing down the excretion of potassium and sodium ions from the body.
Metoclopramide solution begins to affect the digestive system approximately 10-15 minutes after intramuscular injection and 1-3 minutes after intravenous administration, which is reflected in the rapid evacuation of gastric contents and antiemetic effect. The main element is metabolized in the liver and excreted from the body, mainly in the urine for 24-72 hours. Approximately 30% of the substance that enters the body is excreted unchanged. Metoclopramide easily crosses the placental and blood-brain barriers, in a certain amount is determined in breast milk. Peak blood levels of metoclopramide are directly proportional to the dosage taken and are usually reached in 1-2 hours.
In patients with cirrhosis, metoclopramide may accumulate due to a 50% decrease in plasma clearance.
Indications for prescription
Metoclopramide solution in the form of injections is prescribed in the presence of the following pathological conditions:
- nausea, hiccups, vomiting of various origins (in somecases, the drug may be effective in the treatment of vomiting caused by the use of cytostatics or radiation therapy);
- pyloric stenosis of functional origin;
- atony or hypotension of the digestive organs, including postoperative;
- flatulence;
- reflux esophagitis;
- ulcerative changes in the duodenum and stomach (at the stage of exacerbation, simultaneously with other medications);
- dyskinesia of bile ducts by hypomotor type.
In addition to the above indications, Metoclopramide solution is often prescribed for radiopaque examinations of the digestive tract (in order to enhance peristalsis) and as a drug that facilitates duodenal sounding (in order to speed up the process of emptying the stomach and move food elements through the small intestine).
List of contraindications
Metoclopramide solution has some absolute and relative contraindications. The first category includes:
- glaucoma;
- bleeding from digestive organs;
- pyloric stenosis;
- prolactin-dependent tumors;
- perforation of the walls of the intestine or stomach;
- Parkinson's disease;
- mechanical type intestinal obstruction;
- pheochromocytoma;
- epilepsy;
- extrapyramidal disorders;
- vomiting due to overdose or treatment with neuroleptics, as well as in patients with breast cancer;
- bronchial asthma withhigh sensitivity of the patient's body to sulfites;
- I trimester of pregnancy, lactation;
- under 6 years of age;
- high sensitivity to ingredients.
According to the instructions, the drug "Metoclopramide" should not be used after surgical interventions on the organs of the digestive tract (pyloroplasty, intestinal anastomosis), as intense muscle contractions may interfere with healing.
Relative contraindications to the drug "Metoclopramide" should be used with caution in the presence of such pathological conditions:
- arterial hypertension;
- kidney or liver failure;
- bronchial asthma;
- II-III trimesters of pregnancy;
- elderly (after 65 years old) and children's age.
Rules of application
According to the instructions, the Metoclopramide solution is administered intravenously or intramuscularly. The dosage of the drug is prescribed depending on the age category:
- adult patients: 10-20 mg 1-3 times a day (maximum volume - 60 mg);
- children after 6 years: 1-3 times a day, 5 mg.
Half an hour before taking radiation therapy or cytostatics for the treatment and prevention of vomiting and nausea, this medical product is administered intravenously at a dosage of 2 mg / kg of the patient's weight. If necessary, after 2-3 hours, the introduction of the solution can be repeated. 5-15 minutes before X-ray examination10-20 mg of the drug is administered intravenously. In case of clinically pronounced liver or kidney failure, the dosage of the drug should be reduced by 2 times, the next dosage depends on the individual's response to the treatment. The recipe in Latin for the Metoclopramide solution will be given below.
Use for kidney and liver failure
If the patient has this pathological condition, it is necessary to adjust the dosage of Metoclopramide as follows:
- End-stage (creatinine clearance less than 15 ml/min): 25% of daily volume.
- Severe and moderate stages (creatinine clearance 15-60 ml/min): 50% of the daily dosage.
For severe manifestations of liver failure, the dosage is halved.
Side effects of Metoclopramide solution
Medication may cause these negative reactions:
- Heart and blood vessels: atrioventricular block.
- CNS: extrapyramidal disorders - spasm of the facial muscles, torticollis (spastic type), rhythmic protrusion of the tongue, bulbar type of speech, extraocular muscle spasms (oculogiric crisis), hypertonicity, muscle opisthotonus, parkinsonism, dyskinesias (with chronic liver failure and in elderly patients), headache, depression, anxiety, drowsiness, fatigue, tinnitus, confusion.
- Endocrine system: with prolonged treatment at high dosages, gynecomastia, galactorrhea, disordersmenstrual cycle.
- Digestion system: constipation, diarrhea, dry mouth.
- Metabolism: development of porphyria.
- Hematopoietic system: neutropenia, sulfhemoglobinemia in adult patients, leukopenia.
- Allergic reactions: bronchospasm, angioedema, urticaria.
- Others: at the beginning of therapy - agranulocytosis, when prescribing high doses - hyperemia of the nasal mucosa.
If the above symptoms occur, worsen or develop other adverse reactions, it is recommended to contact the specialist who wrote the prescription for the Metoclopramide solution.
Signs of drug overdose
The most common symptoms of drug overdose are extrapyramidal disorders, cardiac and respiratory arrest, excessive drowsiness, clouded consciousness, hallucinations, fainting and fainting. If a patient is diagnosed with extrapyramidal symptoms, provoked by an overdose or another cause, symptomatic treatment is recommended (benzodiazepines in children or anticholinergic antiparkinsonian drugs in adults). Depending on the clinical manifestations of the pathology, symptomatic therapy and regular monitoring of respiratory and cardiac functions are required.
Special recommendations for use
With vomiting of the vestibular nature of origin, the solution "Metoclopramide" in ampoules is not effective. When it is used, laboratory parameters of liver function and determination of the level of aldosterone andplasma prolactin. Side effects in most cases occur within 36 hours after the injection of the drug and disappear without additional therapy within a day after its cancellation. Treatment with this remedy, if possible, should be short-term. While using the medication, it is not recommended to take alcoholic beverages. During treatment, it is recommended to be careful when carrying out activities with the use of potentially dangerous mechanisms that require special attention and quick mental reactions, as well as when driving.
Metoclopramide solution is dispensed in pharmacies by prescription. You can get it from the attending or district medical specialist.
Use during pregnancy and lactation
Prescribing drugs based on metoclopramide in the third trimester of pregnancy is contraindicated, as this can lead to the development of extrapyramidal disorders in newborns. When prescribing the drug to pregnant women, constant monitoring of newborns should be carried out. The main substance is determined in breast milk, and therefore the lactation period is a contraindication to the appointment of this medication. Before starting therapy, it is recommended to stop breastfeeding. This is confirmed by the instructions for use for the Metoclopramide solution.
Medication use in childhood
The remedy for children is prescribed with extreme caution. This is especially true for babiesearly age, since in this case the likelihood of a dyskinetic syndrome increases significantly.
Drug interaction
When combined use of the solution for injection "Metoclopramide" with some medical devices may develop the following effects:
- Cholinesterase inhibitors: inhibition of the action of metoclopramide.
- Ethanol: increased effects on the central nervous system.
- Sleeping pills: increased sedative effects.
- H2-histamine receptor blockers: increasing the effect of therapy.
- Digoxin, cimetidine: inhibition of absorption processes.
- Tetracycline, diazepam, ampicillin, acetylsalicylic acid, paracetamol, levodopa: increased absorption.
- Neuroleptics: increased risk of extrapyramidal symptoms.
In addition, the combined use of the drug with zopiclone accelerates the absorption of the latter, with cabergoline - a decrease in its effectiveness is possible, with ketoprofen - its bioavailability decreases.
As a result of dopamine receptor antagonism, metoclopramide can reduce the anti-Parkinsonian effect of levodopa, while it is possible to increase the bioavailability of levodopa as a result of accelerating its evacuation from the gastric cavity under the influence of metoclopramide. The results of this interaction are mixed.
When used concomitantly with mexiletine, the absorption of mexiletine is accelerated, with mefloquine, the absorption of mefloquine and its plasma level are enhanced, while its side effects may be reduced.
Whenthe simultaneous use of the solution for injection "Metoclopramide" with morphine accelerates the absorption of morphine when taken orally and enhances its sedative effect.
When administered simultaneously with nitrofurantoin, the absorption of nitrofurantoin decreases. With metoclopramide, their induction doses may need to be reduced before direct administration or thiopental.
In patients receiving metoclopramide, the effects of suxamethonium chloride are prolonged and enhanced. This is important to consider.
The instructions for the Metoclopramide solution must be strictly followed. When combined with tolterodine, the effectiveness of the studied drug decreases, with fluvoxamine - a case of extrapyramidal disorders is known, with fluoxetine - there is a possibility of extrapyramidal disorders in the patient, with cyclosporine - the absorption of cyclosporine increases and its plasma concentration increases.
Before you start taking other medicines at the same time, you need to get advice from a specialist.
Recipe for "Metoclopramide" in Latin in solution and tablets
The doctor must write out the appointment in the following form:
Rp: Tabulettam Metoclopramidi 0, 01 No. 10
Da. Signa: take 1 tab. 3 times a day for nausea
Rp: Sol. Metoclopramidi 0.5% - 2 ml.
Dtd N 20 in amp.
S: 2 ml IM 3 times a day for the treatment of intestinal atony
Analogues
The most famous and common drug analogues"Metoclopramide" are:
- "Vero-Metoclopramide";
- Metamol;
- "Perinorm";
- Cerucal;
- Metoclopramide-Eskom;
- "Metoclopramide-Vial";
- Raglan.
The doctor should select a replacement.
Price of this medicine
You can buy the medicine for about 50-80 rubles (the package contains 10 ampoules of the drug). The prescription in Latin for the solution "Metoclopramide" must be presented at the same time. The cost of the drug depends on the region and the pharmacy chain.
Reviews
Patients consider this medication quite effective, and doctors actively use it as an antiemetic therapy. Patients undergoing cytostatic treatment and radiation therapy report that the drug "Metoclopramide" successfully helps to eliminate nausea and vomiting. Many patients tolerate the drug well, they do not complain about adverse reactions.
As for the use of this tool in childhood, the reviews contain both positive and negative information about it. Parents and pediatricians note that this medicine well eliminates the signs of nausea, but it causes a lot of adverse reactions, and the risk of developing these complications significantly outweighs the benefits. The most common reactions to the drug in both adults and children were dizziness, impaired visual perception, tinnitus, and cephalalgia. That is, the symptoms of a violation of the nervous system. These problems usually occur inthe first day of the drug, and quickly disappeared.
Doctors in the reviews of the drug indicate that it is strictly forbidden to use such medicines on their own, without the appointment of a specialist. This is due to the fact that it often causes a negative effect on the body, which can lead to very serious complications.
