Means "Metoclopramide" - a medication with antiemetic effect. The Latin name for this medicine is Metoclopramide. It is produced by several pharmaceutical companies - Ellara LLC, Moscow Endocrine Plant Federal State Unitary Enterprise, FarmFirma SOTEKS CJSC, Novosibkhimpharm OJSC, Promomed Rus LLC, PROMED EXPORTS Indian company, PFK Renovation CJSC, Belarusian Borisov plant of medical preparations , Polish JSC "Pharmaceutical plant POLFARMA". A detailed description of the Metoclopramide solution will be given below.
The composition and form of the drug
The medication is available in two dosage forms - in the form of tablets and liquids for intravenous and intramuscular use. The percentage of Metoclopramide solution is 0.5%, it is poured into ampoules, in a volume of 2 ml. Glass ampoules are packed in cardboard 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.
pharmachologic effect
The solution “Metoclopramide” belongs to the category of specific blockers of serotonin (5-HT3) and dopamine (D2) receptors. It helps to suppress the activity of chemoreceptors, which are localized in the trigger section of the brain stem, and reduces the sensitivity of the visceral nerves, which are responsible for the transmission of impulses from the pylorus and duodenum to the emetic receptors. The medicine “Metoclopramide” acts on 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 medication increases the tone of the intestines and stomach, activates intestinal motility, accelerates the removal of food from the stomach, prevents the occurrence of esophageal and pyloric reflux, reduces the intensity of hyperacid stasis.
The medication 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 is uncharacteristic, m-anticholinergic, ganglioblocking, antihistamine and antiserotonin action. In addition, this substance does not change the functioning of the liver and kidneys, respiratory function, has no effect on the tone of the vessels of the brain, blood pressure in the vessels, blood formation, and secretion of the pancreas and stomach. The medication stimulates the processes of prolactin synthesis and increases the sensitivity of body tissues to acetylcholine (this effect is not determined by vagal innervation, but is stopped by anticholinergic drugs). In addition, it activates the production of aldosterone, while slowing down the excretion of potassium and sodium ions from the body.
The solution "Metoclopramide" begins to affect the digestive system approximately 10-15 minutes after administration intramuscularly and 1-3 minutes after administration intravenously, which is reflected in the rapid evacuation of gastric contents and antiemetic effect. The main element is metabolized in the liver and excreted mainly in the urine for 24–72 hours. Approximately 30% of the substance ingested is excreted unchanged. Metoclopramide easily overcomes the placental and blood-brain barriers, in some quantities it is determined in breast milk. The maximum blood levels of metoclopramide are directly proportional to the dosage taken and are usually reached after 1-2 hours.
In patients with cirrhosis of the liver, cumulation of metoclopramide may occur, which is due to a 50% decrease in plasma clearance.
Indications for appointment
The solution "Metoclopramide" in the form of injections is prescribed in the presence of the following pathological conditions:
- nausea, hiccups, vomiting, having a different nature of origin (in some cases, the medicine can 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);
- hypomotor biliary dyskinesia.
In addition to the above indications, the Metoclopramide solution is often prescribed during X-ray contrast examinations of the digestive tract (in order to enhance peristalsis) and as a medicine that facilitates duodenal sounding (in order to accelerate the process of emptying the stomach and moving food elements through the small intestine).
List of contraindications
The Metoclopramide solution has some absolute and relative contraindications. The first category includes:
- glaucoma;
- digestive bleeding;
- gastric pyloric stenosis;
- prolactin-dependent tumors;
- perforation of the walls of the intestine or stomach;
- Parkinson's disease;
- mechanical intestinal obstruction;
- pheochromocytoma;
- epilepsy;
- extrapyramidal disorders;
- vomiting due to an overdose or treatment with antipsychotics, as well as in patients with breast cancer;
- bronchial asthma with high sensitivity of the patient's body to sulfites;
- I trimester of pregnancy, lactation;
- less than 6 years old;
- high sensitivity to the components of the composition.
According to the instructions, the medication “Metoclopramide” should not be used after surgical interventions on the digestive tract (pyloroplasty, intestinal anastomosis), as intense muscle contractions can 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) and children's age.
Application rules
According to the instructions, the Metoclopramide solution is administered intravenously or intramuscularly. Dosages of the drug are prescribed depending on the age category:
- adult patients: 1-3 times a day for 10-20 mg (maximum volume - 60 mg);
- children after 6 years: 1-3 mg per day, 5 mg each.
Half an hour before taking radiation therapy or cytostatics for the treatment and prevention of vomiting and nausea, this medication is administered intravenously at a dose of 2 mg / kg of patient weight. If necessary, after 2-3 hours, the introduction of the solution can be repeated. For 5-15 minutes before x-ray examination, 10-20 mg of the drug is administered intravenously. With clinically severe liver or kidney failure, the dosage should be reduced by 2 times, the next dosage depends on the individual's response to the treatment. The Latin recipe for Metoclopramide 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:
- Terminal stage (creatinine clearance less than 15 ml / min): 25% of the daily volume.
- Severe and moderate stages (creatinine clearance 15-60 ml / min): 50% of the daily dosage.
With severe manifestations of liver failure, the dosage is reduced by half.
Side effects of Metoclopramide solution
A drug can provoke the occurrence of such negative reactions:
- Heart and blood vessels: atrioventricular block.
- CNS: extrapyramidal disorders - facial muscle spasm, torticollis (spastic type), rhythmic protrusion of the tongue, bulbar type of speech, extraocular muscle spasms (oculogyric crisis), hypertonicity, muscular opistotonus, parkinsonism, dyskinesias (in case of chronic liver failure, and in elderly patients) headache, depression, anxiety, drowsiness, fatigue, tinnitus, confusion.
- Endocrine system: with prolonged treatment in high doses, gynecomastia, galactorrhea, menstrual irregularities.
- Digestive system: constipation, diarrhea, dry mouth.
- Metabolism: the development of porphyria.
- Hematopoietic system: neutropenia, sulfhemoglobinemia in adult patients, leukopenia.
- Allergic reactions: bronchospasm, angioedema, urticaria.
- Others: at the beginning of therapy - agranulocytosis, with the appointment of high doses - hyperemia of the nasal mucosa.
In the event of the above-described symptoms, its aggravation, or the development of other adverse reactions, it is recommended to consult a specialist who wrote out a prescription for Metoclopramide solution.
Signs of an overdose of the drug
The most common symptoms of drug overdose are extrapyramidal disorders, cardiac and respiratory arrest, excessive drowsiness, clouded consciousness, hallucinations, half-fainting and fainting conditions. If the patient is diagnosed with extrapyramidal symptoms, provoked by an overdose, or another reason, symptomatic treatment (benzodiazepines in children or anticholinergic antiparkinsonian medications in adults) is recommended. Depending on the clinical manifestations of the pathology, symptomatic therapy and regular monitoring of respiratory and cardiac functions are required.
Special Usage Recommendations
With vomiting of the vestibular nature of origin, the solution "Metoclopramide" in ampoules is not effective. With its use, laboratory indicators of liver function and determination of the level of aldosterone and prolactin in plasma may be distorted. Side effects in most cases occur within 36 hours after injection of the drug and disappear without additional therapy within a day after its cancellation. If possible, treatment with this remedy should be short-lived. During the use of the medication, it is not recommended to take alcoholic beverages. During treatment, caution is advised when carrying out activities using potentially dangerous mechanisms that require special attention and quick mental reactions, as well as when driving.
In pharmacies, a prescription solution of Metoclopramide is dispensed. You can get it from the attending or local medical specialist.
Use during pregnancy and lactation
The appointment of drugs based on metoclopramide in the III trimester of pregnancy is contraindicated, since this can lead to the development of extrapyramidal disorders in newborns. When prescribing a medication to pregnant women, constant monitoring of newborns should be carried out. The main substance is determined in breast milk, and therefore the period of lactation 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 with the Metoclopramide solution.
Use of the drug in childhood
The drug is prescribed to children with extreme caution. This is especially true for young children, since in this case the likelihood of dyskinetic syndrome significantly increases.
Drug interaction
With the combined use of Metoclopramide injection solution with some medical devices, the following effects may develop:
- Cholinesterase Inhibitors: Inhibition of Metoclopramide.
- Ethanol: increased effects on the central nervous system.
- Hypnotics: increased sedation.
- H2-histamine receptor blockers: increased effect of therapy.
- Digoxin, cimetidine: inhibition of absorption processes.
- Tetracycline, diazepam, ampicillin, acetylsalicylic acid, paracetamol, levodopa: increased absorption.
- Antipsychotics: 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 antagonism with respect to dopamine receptors, metoclopramide can reduce the antiparkinsonian effect of levodopa, while it is possible to increase the bioavailability of levodopa as a result of accelerating its evacuation from the stomach cavity under the influence of metoclopramide. The results of this interaction are mixed.
With concomitant use with mexiletine, the absorption of mexiletine is accelerated, with mefloquine, the absorption of mefloquine and its level in plasma is enhanced, while it is possible to reduce its side effects.
With the simultaneous use of Metoclopramide injection solution with morphine, the absorption of morphine during oral administration is accelerated and its sedative effect is enhanced.
With simultaneous administration with nitrofurantoin, absorption of nitrofurantoin decreases. With metoclopramide, prior to direct administration of thiopental or thiopental, a reduction in their induction doses may be required.
In patients receiving metoclopramide, the effects of suxamethonium chloride are prolonged and enhanced. This is important to consider.
Instructions for the solution "Metoclopramide" must be strictly observed. When combined with tolterodine, the effectiveness of the studied drug decreases, with fluvoxamine - the occurrence of extrapyramidal disorders is known, with fluoxetine - there is a possibility of the patient having extrapyramidal disorders, with cyclosporine - the absorption of cyclosporine increases and its plasma concentration increases.
Before starting the simultaneous administration of other medications, it is necessary to obtain the recommendations of a specialist.
Recipe "Metoclopramide" in Latin in solution and tablets
The doctor must prescribe the appointment in the following form:
Rp: Tabulettam Metoclopramidi 0.01 No. 10
Da.Signa: take 1 tablet. 3 times a day for nausea
Rp: Sol. Metoclopramidi 0.5% - 2 ml.
Dtd N 20 in amp.
S: 2 ml IM 3 r / d for the treatment of intestinal atony
Analogs
The most famous and common analogues of the drug "Metoclopramide" are:
- "Vero-Metoclopramide";
- "Metamol";
- "Perinorm";
- "Tserukal";
- "Metoclopramide-Eskom";
- "Metoclopramide-Vial";
- "Raglan".
A doctor should select a replacement.
The price of this drug
You can buy medicine for about 50-80 rubles (the package contains 10 ampoules of the drug). A Latin recipe for Metoclopramide should be required. The cost of the drug depends on the region and the pharmacy network.
Reviews
Patients consider this medication to be quite effective, and doctors are actively using it as antiemetic therapy. Patients who are treated with cytostatics and radiation therapy report that the Metoclopramide medicine successfully helps to eliminate nausea and vomiting. Many patients tolerate the drug well; they have no complaints 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 causes a lot of adverse reactions, and the risk of developing these complications significantly exceeds the benefit. The most common reaction to the drug in both adults and children was dizziness, visual impairment, tinnitus, cephalgia. That is, symptoms of impaired activity of the nervous system. These problems arose, as a rule, on the first day of the use of the medication, and quickly disappeared.
Doctors in reviews of the drug indicate that it is strictly forbidden to use such drugs on their own, without the appointment of a specialist. This is due to the fact that it often causes the appearance of negative effects on the body, which can entail very serious complications.