Cerucal daily dose. Cerucal - dosage for various diseases. Method of application and dose

The drug cerucal (INN - metoclopramide) refers to antiemetic drugs of central (although there is also a peripheral component in its arsenal) action that “turns off” dopamine receptors, which in turn are important links in the process of potentiation of the gag reflex. The drug blocks dopamine (D2) receptors in the brain, which makes the vomiting center less sensitive to irritating impulses. As a result of the action of cerucal - antiemetic effect, elimination of nausea, hiccups. The drug does not allow the esophagus to “walk around”, upsetting its peristaltic impulses, mobilizes the lower esophageal sphincter to more carefully protect its passage area, increasing its tone, accelerates the passage of the food bolus through the stomach and its further movement along winding paths small intestine. At the same time, the acceleration of emptying digestive tract occurs within reasonable "pre-diarrheal" limits. The list of advantages of cerucal also includes the normalization of bile secretion, the removal of spasm of the sphincter of Oddi (this is the “gate” through which bile and pancreatic secretions enter the duodenum), elimination of gallbladder dysfunction. Cerucal stimulates the secretion of prolactin. The tablet form of the drug is rapidly absorbed in the gastrointestinal tract, its bioavailability is 60-80%.

Cerucal is available in two dosage forms: tablets and solution for intravenous and intramuscular administration.

Tablets are recommended to be taken half an hour before meals with water. Adults take 10 mg (equivalent to 1 tablet) 3-4 times a day. Adolescents aged 14 years and older are prescribed 5-10 mg (0.5-1 tablet) 2-3 times a day. Maximum dose Cerucal is 20 mg at a time and 60 mg per day. The duration of the drug course is usually 1-1.5 months. In certain situations, it is allowed to extend the treatment period up to six months. For persons with severe impaired liver function, the prescribed dose is halved. Solution for injection adults and adolescents over 14 years of age are prescribed 1 ampoule 3-4 times a day. For children in the age range between 3 and 14 years, the drug is prescribed with an eye to the patient's body weight, adhering to the following ratio: 0.1 mg of cerucal per 1 kg of body weight. Important clarification: for this age category patients, the drug is prescribed only in the form of an injection solution. Adolescents and individuals with severe renal pathologies are at risk for developing side effects associated with taking this drug. Treatment with Cerucal is incompatible with the use of alcohol.

Pharmacology

Antiemetic, helps to reduce nausea, hiccups; stimulates peristalsis of the gastrointestinal tract. The antiemetic effect is due to the blockade of dopamine D 2 receptors and an increase in the threshold of the trigger zone chemoreceptors; it is a blocker of serotonin receptors. Metoclopramide is believed to inhibit dopamine-induced relaxation of gastric smooth muscle, thus enhancing cholinergic responses in gastrointestinal smooth muscle. Helps accelerate gastric emptying by preventing the body of the stomach from relaxing and increasing the activity of the antrum and upper small intestine. It reduces the reflux of contents into the esophagus by increasing the pressure of the esophageal sphincter at rest and increases the clearance of acid from the esophagus by increasing the amplitude of its peristaltic contractions.

Metoclopramide stimulates prolactin secretion and causes a transient increase in circulating aldosterone, which may be accompanied by transient fluid retention.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. Plasma protein binding is about 30%. Biotransformed in the liver. It is excreted mainly by the kidneys both unchanged and as metabolites. T 1/2 is from 4 to 6 hours.

Release form

Tablets white color, round, flat, with a notch on one side, with a smooth surface and solid beveled edges.

Excipients: potato starch, lactose monohydrate, gelatin, magnesium stearate, precipitated silicon dioxide.

50 pcs. - dark glass bottles (1) - packs of cardboard.

Dosage

Adults inside - 5-10 mg 3-4 times / day. When vomiting severe nausea metoclopramide is administered intramuscularly or intravenously at a dose of 10 mg. Intranasally - 10-20 mg in each nostril 2-3 times / day.

Maximum doses: single when taken orally - 20 mg; daily - 60 mg (for all methods of administration).

Medium single dose for children over 6 years old is 5 mg 1-3 times / day orally or parenterally. For children under 6 years old daily dose for parenteral administration is 0.5-1 mg / kg, the frequency of administration is 1-3 times / day.

Interaction

With simultaneous use with anticholinergics, mutual weakening of the effects is possible.

With simultaneous use with neuroleptics (especially the phenothiazine series and butyrophenone derivatives), the risk of extrapyramidal reactions increases.

With simultaneous use, absorption is enhanced acetylsalicylic acid, paracetamol, ethanol.

Metoclopramide, when administered intravenously, increases the rate of absorption of diazepam and increases its maximum plasma concentration.

With simultaneous use with a slowly dissolving dosage form of digoxin, a decrease in the concentration of digoxin in the blood serum by 1/3 is possible. With simultaneous use with digoxin in a liquid dosage form or in the form of an instant dosage form, no interaction was noted.

With simultaneous use with zopiclone, the absorption of zopiclone is accelerated; with cabergoline - a decrease in the effectiveness of cabergoline is possible; with ketoprofen - the bioavailability of ketoprofen decreases.

Due to antagonism against dopamine receptors, metoclopramide can reduce the anti-Parkinsonian effect of levodopa, while it is possible to increase the bioavailability of levodopa due to the acceleration of its evacuation from the stomach under the influence of metoclopramide. The results of the interaction are ambiguous.

With simultaneous use with mexiletin, the absorption of mexiletin is accelerated; with mefloquine - the rate of absorption of mefloquine and its concentration in the blood plasma increase, while it is possible to reduce its side effects.

With simultaneous use with morphine, the absorption of morphine when taken orally is accelerated and its sedative effect is enhanced.

With simultaneous use with nitrofurantoin, the absorption of nitrofurantoin decreases.

When using metoclopramide immediately before the introduction of propofol or thiopental, it may be necessary to reduce their induction doses.

In patients receiving metoclopramide, the effects of suxamethonium chloride are enhanced and prolonged.

With simultaneous use with tolterodine, the effectiveness of metoclopramide decreases; with fluvoxamine - a case of the development of extrapyramidal disorders is described; with fluoxetine - there is a risk of developing extrapyramidal disorders; with cyclosporine - the absorption of cyclosporine increases and its concentration in the blood plasma increases.

Side effects

From the side digestive system: at the beginning of treatment, constipation, diarrhea are possible; rarely - dry mouth.

From the side of the central nervous system: at the beginning of treatment, a feeling of fatigue, drowsiness, dizziness, headache, depression, akathisia. Extrapyramidal symptoms may occur in children and young people (even after a single use of metoclopramide): facial muscle spasm, hyperkinesis, spastic torticollis (usually disappear immediately after stopping metoclopramide). At long-term use, more often in elderly patients, the phenomena of parkinsonism, dyskinesia are possible.

On the part of the hematopoietic system: at the beginning of treatment, agranulocytosis is possible.

From the side endocrine system: rarely, with prolonged use in high doses - galactorrhea, gynecomastia, disorders menstrual cycle.

Allergic reactions: rarely - skin rash.

Indications

Vomiting, nausea, hiccups various genesis. Atony and hypotension of the stomach and intestines (including postoperative); biliary dyskinesia; reflux esophagitis; flatulence; as part of complex therapy exacerbations peptic ulcer stomach and duodenum; acceleration of peristalsis during radiopaque studies of the gastrointestinal tract.

Contraindications

Bleeding from the gastrointestinal tract, mechanical intestinal obstruction, perforation of the stomach or intestines, pheochromocytoma, extrapyramidal disorders, epilepsy, prolactin-dependent tumors, glaucoma, pregnancy, lactation, simultaneous use of anticholinergic drugs, hypersensitivity to metoclopramide.

Application features

Use during 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.

Application for violations of liver function

Use with caution in patients with impaired liver function.

Application for violations of kidney function

Use with caution in patients with impaired renal function.

Use in children

Use with extreme caution in children, especially early age, because they have a significantly higher risk of developing dyskinetic syndrome.

special instructions

Use with caution in patients with bronchial asthma, arterial hypertension, impaired liver and / or kidney function, with Parkinson's disease.

With extreme caution should be used in children, especially young children, because. they have a significantly higher risk of developing dyskinetic syndrome. Metoclopramide in some cases may be effective for vomiting caused by cytotoxic drugs.

When used in elderly patients, it must be borne in mind that with long-term use of metoclopramide in high or medium doses, the most common side effects are extrapyramidal disorders, especially parkinsonism and tardive dyskinesia.

Against the background of the use of metoclopramide, data distortions are possible laboratory indicators liver function and determining the concentration of aldosterone and prolactin in blood plasma.

Influence on the ability to drive vehicles and control mechanisms

Potentially dangerous species activities requiring heightened attention, rapid psychomotor reactions.

To eliminate vestibular disorders of the brain, doctors prescribe the drug Cerucal - instructions for its use contain data on the mechanism of work and composition. The drug belongs to antiemetics, it has a central effect. Due to the active substance, it blocks the receptors responsible for motion sickness, prevents the urge to vomit in children and adults.

Medicine Cerucal

According to the accepted medical classification, Cerucal belongs to antiemetic inhibitor drugs. central action which blocks dopamine receptors. This allows you to increase the threshold of irritation of the vomiting center and prevent the urge to nausea, eliminate dyskinesia. This effect is achieved due to the work of the active substance of the drug - metoclopramide hydrochloride monohydrate.

Composition and form of release

Two forms of release of Cerucal are known - tablets for oral administration and a solution for parenteral administration:

	Tablets	injection solution
Description	White round flat with risk	Clear colorless liquid
Concentration of metoclopramide hydrochloride, mg		5 per 1 ml (10 per 1 ampoule)
	Magnesium stearate, potato starch, silicon dioxide, gelatin, lactose monohydrate	Water, sodium sulfite, sodium chloride, disodium edetate
Package	Bottles of 50 pcs.	5 ampoules of 2 ml

Pharmacological properties

The drug belongs to specific means with the effect of blockers of dopamine and serotonin receptors, eliminates nausea. The principle of operation is connected with the central and peripheral action metoclopramide. Due to the blockade of dopamine receptors in the brain, the antiemetic effect of the drug is caused, it increases the irritation threshold of the vomiting center, eliminates nausea and vomiting.

The drug does not cause diarrhea. He is also able to eliminate the symptoms of gallbladder dyskinesia, stimulate the secretion of prolactin. Tablets begin to act in half an hour, the solution - faster. The bioavailability of Cerucal in plasma is 70%, metabolism occurs in the liver, excreted by the kidneys in 6-10 hours. The drug lowers motor activity esophagus, increases the tone of the lower esophageal sphincter, accelerates the emptying of the stomach and the movement of food through small intestine.

Indications for use

In the instructions for use, the main indication for use is Cerucal for nausea. Other factors that require the use of funds are:

vomiting, hiccups, nausea;
atony, hypotension of the stomach, intestines, digestive tract;
diabetic gastroparesis;
tardive biliary dyskinesia, reflux esophagitis;
increased tone stomach;
increased peristalsis gastrointestinal tract when conducting radiopaque studies;
paresis of the stomach on the background diabetes;
facilitation of duodenal sounding (acceleration of intestinal peristalsis).

How to take Cerucal

Each pack with tablets or solution ampoules contains instructions for the use of Cerucal. Depending on the form of release, the method of use also differs. Tablets are taken orally, and the solution is used for intramuscular or intravenous administration. The course of application, regimen and duration of therapy is prescribed by a specialist, depending on the age of the patient and the severity of the tract disease.

In tablets

According to the instructions, Cerucal tablets are taken half an hour before a meal, washed down with water. for adults, the recommended dose is 1 tablet (10 mg metoclopramide) 3-4 times / day, for people over 14 years old, 0.5-1 pc. 2-3 times/day. The maximum single dose is two tablets, and the maximum daily dose is six. Treatment lasts about 4-6 weeks, sometimes it can last up to six months.

In ampoules

Cerucal injections, according to the instructions, are administered intramuscularly or slowly intravenously. Adults and adolescents over 14 years of age receive one injection ampule 3-4 times / day. Children 3-14 years of age are prescribed 0.1 mg dose of metoclopramide / kg body weight. A maximum of 0.5 mg of the active substance can be consumed per day. With problems in the work of the liver and kidneys, the dose is reduced several times.

There are two treatment regimens for Cerucal for vomiting and nausea caused by the use of cytostatic drugs:

A short-term drip infusion is carried out for 15 minutes. The dose is 2 mg/kg half an hour before taking cytotoxic drugs. The procedure is repeated 1.5, 3.5, 5.5 and 8.5 hours after taking the medication. Previously, the drug is diluted in 50 ml of infusion solution. This eliminates dyskinesia.
Long-term drip infusion at a dose of 0.5-1 mg / kg of body weight per hour. The procedure is carried out two hours before taking cytostatics, then 0.25-05 mg / kg of body weight per hour is applied over the next day. The drug can be diluted with sodium chloride solution or glucose solution. The course of treatment with injections continues throughout the course of cytostatic therapy.

special instructions

Doctors prescribe Cerucal to children with vomiting and adults with nausea. In the instructions for use, it is useful to study special instructions:

the drug reduces the concentration of attention and the speed of psychomotor reactions, which requires refraining from driving and dangerous mechanisms;
the drug is ineffective in the event of vomiting of vestibular origin;
in injections and tablets is not compatible with alcohol, during treatment it is worth refraining from taking ethanol;
at severe violations kidney function, the likelihood of side effects is high, the same applies to adolescents;
against the background of treatment with metoclopramide, the results of tests for indicators of liver function are distorted.

During pregnancy

Instructions for use Cerucal warns that the drug is contraindicated for use in the first trimester of pregnancy. This is due to the penetration of the active substance through the placenta and an increased risk of malformations. If there are vital indications, the medication can be used in the second and third trimesters of pregnancy. During lactation, it is prohibited, because it penetrates into breast milk.

Cerucal for children

Only in the form of injections is Cerucal prescribed for children aged 2-14 years. This is done for the purpose of correct and accurate dosing. Children over 14 years of age may take tablets at a dose that differs from that of an adult and depends on body weight. The instruction warns that children and adolescents have an increased risk of side effects, so their treatment with medication should be monitored by doctors.

drug interaction

Doctors prescribe Cerucal - instructions for the use of the drug contain information about its drug interaction with other medicines:

anticholinergics weaken the effect;
Metoclopramide enhances the absorption of tetracyclines, Paracetamol, Levodopa, lithium preparations, alcohol, the effect of drugs that depress the central nervous system;
changes the effects of tricyclic antidepressants;
reduces the absorption of Digoxin, Cimetidine in the intestine;
neuroleptics increase the risk of developing extrapyramidal disorders;
metoclopramide increases the bioavailability and risk of hepatotoxicity of hepatotoxic agents, reduces the effectiveness of Pergolid.

Side effects

Against the background of the use of Cerucal, the following side effects and negative reactions indicated in the instructions may develop:

fatigue, headaches;
depression;
tic-like twitching of muscles;
tremor, parkinsonism, limited muscle mobility, fever;
promotion blood pressure, change of consciousness, tachycardia;
dryness of the oral mucosa;
gynecomastia;
problems with the menstrual cycle, its slowdown or acceleration;
the risk of any adverse reactions increased in patients with impaired renal function.

Overdose

Manifestations of an overdose of Cerucal are confusion, convulsions. According to reviews, a person has bradycardia, the pressure rises or falls. Light degree symptoms of poisoning disappears a day after discontinuation of therapy, no deaths were detected. According to the instructions, the patient is assigned symptomatic treatment- extrapyramidal disorders are eliminated by the introduction of biperiden. Diazepam is used for sedation. Patients undergo gastric lavage, for the absorption of toxins give Activated carbon or sodium sulfate.

Contraindications

Cerucal is prescribed with caution in Parkinson's disease, in the second and third trimesters of pregnancy, in arterial hypertension, bronchial asthma, violations of the liver, kidneys, in old age. Contraindications for the use of the drug, according to the instructions, are:

hypersensitivity to components;
age up to 2 years for solution, up to 14 years for tablets;
pheochromocytoma;
mechanical intestinal obstruction;
stenosis of the pylorus of the stomach;
gastrointestinal bleeding;
prolactin-dependent tumor;
epilepsy, extrapyramidal symptoms;
first trimester of pregnancy, lactation.

Terms of sale and storage

You can buy Cerucal only with a prescription. It is stored in a dry, dark place away from children at temperatures up to 25 degrees for five years.

Analogues

On the shelves of domestic pharmacies you can find direct and indirect substitutes for Cerucal. The former include drugs with the same active substance in the composition, the latter - with the same therapeutic effect. Cerucal's analogs:

Metoclopramide;
Perinorm;
Metamol;
Vero-Metoclopramide;
Metoclopramide-Vial;
Metoclopramide-Eskom;
Metukal;
Brulium.

Cerucal price

You can buy Cerucal in pharmacies or through Internet sites. The cost of medicines is affected by the form of release and the percentage of markups. Approximate prices for medication in Moscow pharmacies.

Producer: Teva (Teva) Israel

ATC code: A03FA01

Farm group:

Release form: Liquid dosage forms. Injection.

General characteristics. Compound:

2 ml of the solution contains 10.54 mg of metoclopramide hydrochloride as active substance, which corresponds to 10 mg of anhydrous metoclopramide hydrochloride.

Excipients:
sodium sulfite, sodium chloride, 2HO ethylenediaminetetraacetic acid disodium salt, carbon dioxide, water for injection.

Pharmacological properties:

Metoclopramide is a specific blocker of dopamine (D2) and serotonin receptors. It has an antiemetic effect due to the effect on the chemoreceptors of the trigger zone of the medulla oblongata.

The drug has a regulating and normalizing effect on the activity of the gastrointestinal tract. Reduces the motor activity of the esophagus, increases the tone of the lower esophageal sphincter, accelerates gastric emptying, and also accelerates the movement of food through the small intestine without causing diarrhea. Stimulates the secretion of prolactin.

Metoclopramide crosses the placental and blood-brain barriers and passes into breast milk.

Indications for use:

Important! Get to know the treatment

Dosage and administration:

Cerucal solution is administered intramuscularly or intravenously. Adults are prescribed 10 mg 3-4 times a day. The maximum single dose is 20 mg, the daily dose is 60 mg. For children from 2 to 14 years of age, a single dose is 0.1 mg/kg of body weight, the highest daily dose!51; 0.5 mg/kg body weight. The frequency of administration is 1-3 times a day.

The duration of the course of treatment is determined by the doctor and is usually 4-6 weeks. In some cases, treatment can be continued up to 6 months. At kidney failure the dose of the drug should be reduced (with creatinine clearance up to 10 ml / min - 10 mg 1 time per day; from 11 to 60 ml / min - 15 mg per day, divided into 2 injections).

Prevention and treatment of nausea and vomiting associated with the use of cytostatics. Depending on the nature of the chemotherapy treatment, the daily dose ranges from 2 to 4 mg/kg of the patient's body weight. Cerucal injection solution can be diluted with isotonic sodium chloride solution or 5% glucose solution. Do not mix with alkaline infusion solutions!

Application Features:

Caution should be given to patients with arterial hypertension, Parkinson's disease, impaired liver and kidney function, elderly patients, as well as children, since they have a significantly higher risk of dyskinetic syndrome.

During pregnancy (2nd and 3rd trimesters) and children aged 2 to 14 years, the drug is prescribed for health reasons.

When using the drug, potentially hazardous activities that require increased attention, quick mental and motor reactions (driving vehicles, etc.) should be avoided.

Side effects:

At the beginning of treatment, dry mouth, fatigue, drowsiness, agitation, irritability, fear, anxiety, allergic reactions. In some cases, mainly in children, a dyskinetic syndrome may develop. With prolonged use in elderly patients, the development of phenomena, tardive dyskinesia is possible. V rare cases at long-term use drug in high doses - menstrual irregularities.

Interaction with other drugs:

The action of metoclopramide can be weakened by anticholinesterase agents. The drug enhances the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa; reduces the absorption of digoxin and cimetidine. Enhances the effect of alcohol and medicines depressing the CNS. It should not be administered simultaneously with antipsychotics, since the risk of extrapyramidal reactions increases.

Contraindications:

Bleeding from the gastrointestinal tract, pyloric stenosis, mechanical, perforation of the stomach or intestines, extrapyramidal disorders, prolactin-dependent tumors, pregnancy, childhood up to 2 years individual intolerance metoclopramide.

Overdose:

Hypersomnia may be noted. disorientation and extrapyramidal disorders. As a rule, symptoms disappear after discontinuation of the drug within 24 hours. If necessary, treatment with anticholinergics and antiparkinsonian drugs is carried out.

Storage conditions:

In a cool, dark place, out of the reach of children. Ready infusion solution can be stored at room temperature for 24 hours. Shelf life 5 years. Do not use after the expiration date.

Leave conditions:

On prescription

Package:

Preparation: CERUKAL ®

Active ingredient: metoclopramide
ATX code: A03FA01
KFG: Centrally acting antiemetic drug that blocks dopamine receptors
ICD-10 codes (indications): K21.0, K31.3, K31.8, K56, K82.8, K91.3, R11
KFU code: 11.06.02
Reg. number: P No. 012812/02
Date of registration: 26.05.06
The owner of the reg. acc.: AWD.pharma GmbH & Co.KG (Germany)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Tablets white, round, flat, with a notch on one side, with a smooth surface and solid beveled edges.

Excipients: potato starch, lactose monohydrate, gelatin, magnesium stearate, precipitated silica.
50 pcs. - dark glass bottles (1) - packs of cardboard.

Solution for intravenous and intramuscular administration transparent, colorless.

Excipients: sodium sulfite, disodium edetate (disodium ethylenediaminetetraacetate), sodium chloride, water for injections.

2 ml - colorless glass ampoules (5) - blister packs (2) - cardboard packs.

INSTRUCTION CERUKAL FOR SPECIALIST.
The description of the drug is approved by the manufacturer.

PHARMACHOLOGIC EFFECT

Antiemetic drug. A specific blocker of dopamine receptors, it weakens the sensitivity of the visceral nerves that transmit impulses from the pyloric stomach and duodenum to the vomiting center. Through the hypothalamus and parasympathetic nervous system, it has a regulatory and coordinating effect on tone and motor activity. upper division gastrointestinal tract (including the tone of the lower digestive sphincter at rest).

Increases the muscle tone of the stomach and intestines, accelerates gastric emptying, reduces hyperacid stasis, prevents pyloric and esophageal reflux. Stimulates intestinal peristalsis.

PHARMACOKINETICS

Suction

After oral administration, it is rapidly absorbed, the time to reach Cmax in blood plasma is 30-120 minutes.

Bioavailability is 60-80%.

Distribution

Penetrates through the blood-brain and placental barriers. Stands out from breast milk.

Metabolism

Metabolized in the liver.

breeding

T1 / 2 - 3-5 hours. Excreted by the kidneys during the first 24 hours unchanged and in the form of metabolites (about 80% of once taken dose).

Pharmacokinetics in special clinical situations

With impaired renal function, T 1/2 may increase up to 14 hours.

INDICATIONS

Vomiting and nausea of various origins;

Atony and hypotension of the stomach and intestines (including postoperative);

Biliary dyskinesia;

Reflux esophagitis;

Functional pyloric stenosis;

To enhance peristalsis during radiopaque studies of the gastrointestinal tract;

Paresis of the stomach in diabetes mellitus;

As a means of facilitating duodenal sounding (to accelerate the emptying of the stomach and the promotion of food through the small intestine).

DOSING MODE

Installed individually depending on clinical symptoms and age of the patient.

Adults and teenagers aged 14 and over appoint inside 10 mg 3-4 times / day.

If necessary, Cerucal can be administered intramuscularly or intravenously at a dose of 10 mg. The multiplicity of introduction - 3-4 times / day.

The average duration of the course of treatment is 4-6 weeks; in some cases - up to 6 months.

For children aged 2-14 years maximum single dose for both oral and oral administration parenteral use is 0.1 mg/kg of body weight; the maximum daily dose is 0.5 mg/kg.

Inside the drug should be taken 30 minutes before a meal.

Patients with impaired renal function dosage adjustment is required.

SIDE EFFECT

From the side of the central nervous system: sometimes there may be a feeling of fatigue, headaches, dizziness, fear, anxiety, depression, drowsiness, tinnitus; in some cases (mainly in children), dyskinetic syndrome (involuntary tic-like twitching of the muscles of the face, neck or shoulders) may develop; the appearance of extrapyramidal disorders is possible - spasm of the facial muscles, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of the extraocular muscles (including oculogiric crisis), spastic torticollis, opisthotonus, muscle hypertonicity, symptoms of parkinsonism (the risk of development in children and adolescents increases when the dose exceeds 0.5 mg / kg / day) and tardive dyskinesia (in elderly patients with chronic renal failure); in isolated cases, a severe neuroleptic syndrome may develop.

With long-term treatment with Cerucal in elderly patients, symptoms of parkinsonism and tardive dyskinesia may develop.

From the hematopoietic system: agranulocytosis.

From the side of cardio-vascular system: supraventricular tachycardia, arterial hypotension or hypertension.

From the digestive system: constipation, diarrhea, dry mouth.

From the endocrine system: rarely - with prolonged use of the drug, gynecomastia, galactorrhea or menstrual irregularities may occur (with the development of these phenomena, metoclopramide is canceled).

CONTRAINDICATIONS

Pheochromocytoma;

Intestinal obstruction;

Bleeding from the gastrointestinal tract;

Perforation of the gastrointestinal tract;

Prolactin-dependent tumor;

Epilepsy;

Extrapyramidal movement disorders;

I trimester of pregnancy;

lactation (breastfeeding);

Children's age up to 2 years;

Hypersensitivity to metoclopramide;

Hypersensitivity to sodium sulfite, especially in patients with bronchial asthma and other allergic diseases(for the injection form of Cerucal).

WITH caution the drug should be prescribed for arterial hypertension, bronchial asthma, impaired liver function, hypersensitivity to procaine and procainamide, children aged 2 to 14 years.

PREGNANCY AND LACTATION

Cerucal is contraindicated for use in the first trimester of pregnancy.

The use of Cerucal in the II and III trimesters of pregnancy is possible only under strict indications.

If it is necessary to use Cerucal during lactation, the issue of stopping breastfeeding should be resolved.

SPECIAL INSTRUCTIONS

Caution should be exercised when prescribing Cerucal to children, adolescents and patients with impaired renal function. This group of patients has an increased risk of side effects. In the event of side effects, the drug should be discontinued immediately.

Cerucal is not effective for vomiting of vestibular origin.

Against the background of the use of metoclopramide, distortions of the data of laboratory parameters of liver function and determination of the concentration of aldosterone and prolactin in plasma are possible.

During treatment, patients are prohibited from drinking alcohol.

Influence on the ability to drive vehicles and control mechanisms

Patients taking Cerucal should refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions (driving a car, working with moving mechanisms).

OVERDOSE

Symptoms: drowsiness, confusion, irritability, anxiety, convulsions, extrapyramidal movement disorders, dysfunction of the cardiovascular system with bradycardia and arterial hypo- or hypertension.

In mild forms of poisoning, symptoms disappear 24 hours after discontinuation of the drug. Depending on the severity of symptoms, monitoring of vital signs is recommended. important functions sick. Fatal cases of poisoning in overdose have not been identified.

Treatment: carry out symptomatic therapy. Extrapyramidal disorders are eliminated by slow intravenous administration of biperiden (adult doses - 2.5-5 mg). Perhaps the use of diazepam.

DRUG INTERACTIONS

With the simultaneous use of Cerucal reduces the effect of anticholinesterase drugs.

With the simultaneous use of Cerucal and neuroleptics, extrapyramidal symptoms may increase.

With the simultaneous use of Cerucal with cimetidine and digoxin, a decrease in the absorption of the latter is possible.

With the simultaneous use of Cerucal with some antibiotics (tetracycline, ampicillin), lithium preparations, paracetamol, levodopa, lithium, ethanol, the absorption of the latter increases.

Cerucal enhances the effect of ethanol and drugs that depress the central nervous system.

With the simultaneous use of Cerucal and tricyclic antidepressants, MAO inhibitors and sympathomimetic agents, their effects may change.

Cerucal reduces the effects of blockers of H 2 -histamine receptors.

Cerucal increases the risk of developing hepatotoxicity when combined with hepatotoxic agents.

Cerucal reduces the effectiveness of pergolide, levodopa.

Cerucal increases the bioavailability of cyclosporine, which may require monitoring of its plasma concentration.

Cerucal increases the concentration of bromocriptine.

Pharmaceutical interaction

When mixing solutions of Cerucal and vitamin B 1, the destruction of the vitamin occurs.

TERMS AND CONDITIONS OF DISCOUNT FROM PHARMACIES

The drug is dispensed by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a place protected from light, out of the reach of children, at a temperature not exceeding 30°C. Shelf life - 5 years.

INSTRUCTIONS
on medical use drug

Registration certificate:

Tradename:

Cerucal ®

International non-proprietary name:

metoclopramide

Dosage form:

tablets

Compound

1 tablet contains: active substance metoclopramide hydrochloride monohydrate 10.54 mg (in terms of metoclopramide hydrochloride 10.00 mg); Excipients: potato starch 36.75 mg, lactose monohydrate 76.65 mg, gelatin 2.16 mg, silicon dioxide 2.60 mg, magnesium stearate 1.30 mg.

Description:

White, round, flat tablets scored on one side.

Pharmacotherapeutic group:

Antiemetic - dopamine receptor blocker central.

ATX code: A03FA01

Pharmacological properties

Pharmacodynamics
Antiemetic, is a specific blocker of dopamine (D2) and serotonin receptors. The mechanism of action is based on both the central and peripheral effects of metoclopramide. The antiemetic effect is associated with the blockade of dopamine receptors in the brain, which causes an increase in the threshold of irritation of the vomiting center. It has an antiemetic effect, eliminates nausea and hiccups. It reduces the motor activity of the esophagus, increases the tone of the lower esophageal sphincter, accelerates gastric emptying, and also accelerates the movement of food through the small intestine without causing diarrhea. Normalizes the secretion of bile, reduces spasm of the sphincter of Oddi, does not change its status, eliminates gallbladder dyskinesia. Stimulates the secretion of prolactin.

Pharmacokinetics
After oral administration, it is rapidly absorbed, the time to reach maximum plasma concentration is 30-120 minutes. Bioavailability is 60-80%.
Metabolized in the liver. The half-life is from 3 to 5 hours, with impaired renal function it can increase up to 14 hours. It is excreted by the kidneys during the first 24 hours unchanged and in the form of metabolites (about 80% of the dose taken). It easily crosses the blood-brain barrier and is excreted in breast milk.

Indications for use

Prevention of postoperative nausea and vomiting.
Symptomatic treatment of nausea and vomiting, including acute migraine.
Prevention of nausea and vomiting caused by radiation therapy and chemotherapy.

Contraindications

Hypersensitivity to metoclopramide and drug components;
gastrointestinal bleeding, mechanical intestinal obstruction or perforation of the wall of the stomach and intestines, conditions in which stimulation of gastrointestinal motility poses a risk;
confirmed or suspected pheochromocytoma due to the risk of developing severe arterial hypertension;
tardive dyskinesia, which developed after treatment with neuroleptics or metoclopramide in history;
epilepsy (increased frequency and severity of seizures);
Parkinson's disease;
simultaneous use with levodopa and dopamine receptor agonists;
methemoglobinemia due to taking metoclopramide or a history of cytochrome b5 nicotinamide adenine dinucleotide (NADH) deficiency;
prolactinoma or prolactin-dependent tumor;
lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
children's age up to 15 years;
breastfeeding period.

Carefully

When used in elderly patients; in patients with impaired cardiac conduction (including prolongation of the QT interval), impaired water and electrolyte balance, bradycardia. taking other drugs that prolong the QT interval, arterial hypertension; in patients with concomitant neurological diseases, depression (in history); with renal failure of moderate and severe severity (CC 15-60 ml / min); at liver failure severe severity; during pregnancy.

Use during pregnancy and breastfeeding

Pregnancy
Numerous data obtained on the use in pregnant women (more than 1000 described cases) indicate the absence of fetotoxicity and the ability to cause malformations in the fetus. Metoclopramide can be used during pregnancy (I-II trimesters) only if potential benefit to the mother outweighs the potential risk to the fetus. In connection with pharmacological features(similar to other antipsychotics). when using metoclopramide at the end of pregnancy, the possibility of developing extrapyramidal symptoms in the newborn cannot be excluded. Metoclopramide should not be used at the end of pregnancy (during the third trimester). When using metoclopramide, the condition of the newborn should be monitored.
breastfeeding period
Metoclopramide is excreted in small amounts in breast milk. The possibility of developing adverse reactions in a child cannot be ruled out. The use of metoclopramide during breastfeeding is not recommended. If necessary, the use of the drug during lactation should stop breastfeeding.

Method of application and dose

inside.
Adults and children over 15 years of age weighing more than 60 kg
The recommended dose is 1 tablet (10 mg) up to three times a day.
The maximum recommended daily dose is 30 mg or 0.5 mg/kg body weight.
Children over 15 years of age weighing less than 60 kg
The recommended dose is 1/2 tablet (5 mg) 1-3 times a day.
The maximum recommended daily dose is 0.5 mg/kg/day.
In order to avoid overdose, it is necessary to observe a minimum interval between doses of 6 hours, even in case of vomiting.
The maximum duration of treatment is 5 days.
Elderly patients
In elderly patients, a dose reduction may be required depending on indicators of kidney and liver function and general condition.
kidney failure
In patients with terminal stage renal insufficiency (creatinine clearance less than 15 ml / min), the daily dose should be reduced by 75%.
In patients with moderate or severe renal insufficiency (CC 15-60 ml / min), the dose should be reduced by 50%.
Impaired liver function
In patients with severe hepatic insufficiency, the dose should be reduced by 50%.

Side effect

The frequency of adverse reactions is classified in the following way: very often (≥1/10), often (≥1/100 - From the blood and lymphatic system: frequency unknown - methemoglobinemia, probably associated with a deficiency of the enzyme NADH-dependent cytochrome b5 reductase. especially in newborns, sulfhemoglobinemia (most often with the simultaneous use of high doses of sulfur-containing drugs), leukopenia, neutropenia, agranulocytosis.
From the side of the heart: infrequently bradycardia: the frequency is unknown cardiac arrest, which can be caused by bradycardia, atrioventricular block, sinus node block, prolongation of the QT interval on the electrocardiogram, arrhythmia of the "pirouette" type.
From the vascular side: often - lowering blood pressure; frequency unknown - cardiogenic shock, acute increase in blood pressure in patients with pheochromocytoma.
From the endocrine system*: infrequently - amenorrhea, hyperirolactinemia: rarely - galactorrhea; frequency unknown - gynecomastia.
*Endocrine disorders during prolonged treatment are associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia).
From the gastrointestinal tract: often - nausea, diarrhea, constipation.
From the side of the kidneys and urinary tract: frequency unknown - polyuria, urinary incontinence.
From the genitals and mammary gland: unknown frequency sexual dysfunction, priapism.
From the side immune system: infrequently - hypersensitivity; frequency unknown - anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash).
From the nervous system: very often - drowsiness; often - asthenia, extrapyramidal disorders (especially in children and young patients and / or when the recommended doses of the drug are exceeded, even after a single injection), parkinsonism, akathisia: infrequently - dystopia, dyskinesia. impaired consciousness: rarely - convulsions, especially in patients with epilepsy; frequency unknown - tardive dyskinesia. sometimes persistent, during or after long-term treatment, especially in elderly patients, neuroleptic malignant syndrome.
Mental disorder: often - depression; infrequently - hallucinations; rarely confusion.
Adverse reactions most common with high doses of the drug
- Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome, akathisia developed even after a single dose of the drug, especially in children and young patients (see section " special instructions»).
- Drowsiness, decreased level of consciousness, confusion, hallucinations.

Overdose

Symptoms
Extrapyramidal disorders, drowsiness, decreased level of consciousness, confusion, hallucinations, irritability, dizziness, bradycardia, changes in blood pressure, cardiac and respiratory arrest, abdominal pain.
Treatment
In the event of the development of extrapyramidal symptoms caused by an overdose or for another reason, treatment is exclusively symptomatic (benzodiazepines in children and / or anticholinergic antiparkinsonian drugs in adults). Symptomatic treatment and constant monitoring of cardiac and respiratory functions depending on the clinical condition patient. There is no specific antidote.

Interaction with other drugs

The simultaneous use of metoclopramide with levodopa or dopamine receptor agonists is contraindicated due to the existing mutual antagonism.
Alcohol enhances the sedative effect of metoclopramide.
Combinations requiring caution
Due to the prokinetic effect of metoclopramide, the absorption of some drugs may be impaired.
M-anticholinergics and morphine derivatives have mutual antagonism with metoclopramide in relation to the effect on the motility of the gastrointestinal tract.
Medications CNS depressants (morphine derivatives, tranquilizers, H1-histamine receptor blockers, sedative antidepressants, barbiturates, clonidine and other drugs of these groups) can increase the sedative effect under the influence of metoclopramide.
Metoclopramide enhances the effect of neuroleptics in relation to extrapyramidal symptoms.
With concomitant oral use of metoclopramide and tetrabenazine, there is a possibility of dopamine deficiency, which may be accompanied by increased muscle stiffness or spasm, difficulty in speech or swallowing, anxiety, tremor, involuntary muscle movements, including facial muscles.
The use of metoclopramide with serotonergic drugs, such as selective serotonin reuptake inhibitors, increases the risk of developing serotonin syndrome (serotonin intoxication).
Metoclopramide reduces the bioavailability of digoxin. Plasma concentrations of digoxin should be monitored.
Metoclopramide increases the bioavailability of cyclosporine (Cmax by 46% and exposure by 22%). It is necessary to carefully monitor the concentration of cyclosporine in the blood plasma. Clinical Consequences no such interaction has been established.
The exposure of metoclopramide increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme. such as fluoxetine and paroxetine. Although the clinical significance of this interaction has not been established, patients should be monitored for adverse reactions.
With the concomitant use of metoclopramide with atovachone, the concentration of atovachone in the blood plasma is significantly reduced (about 50%). Concomitant use of metoclopramide with atovachone is not recommended.
With the concomitant use of metoclopramide with bromocriptine, the concentration of bromocriptine in the blood plasma increases.
Metoclopramide enhances the absorption of tetracycline from the small intestine.
Metoclopramide enhances the absorption of mexiletin and lithium.
Metoclopramide reduces the absorption of cimetidine.

special instructions

Caution should be exercised when using Cerucal in elderly patients.
On the part of the nervous system, extrapyramidal disorders are possible, especially in children and young patients and / or when using high doses, developing, as a rule, at the beginning of treatment or after a single application. The use of the drug Cerucal ® must be immediately discontinued in case of extrapyramidal symptoms. Reactions are completely reversible upon discontinuation of treatment, but may require symptomatic therapy (benzodiazepines in children and/or anticholinergic antiparkinsonian drugs in adults).
In order to avoid an overdose of the drug Cerucal ®, it is necessary to observe a minimum interval between doses of 6 hours, even in case of vomiting.
Long term treatment drug Cerucal ® can lead to the development of tardive dyskinesia, potentially irreversible, especially in elderly patients. The duration of treatment should not exceed 3 months due to the risk of developing tardive dyskinesia. If there are signs of tardive dyskinesia, treatment should be discontinued.
When using metoclopramide simultaneously with neuroleptics, as well as with metoclopramide monotherapy, a neuroleptic malignant syndrome was noted. It is necessary to immediately stop treatment with Cerucal ® if symptoms of neuroleptic symptoms appear. malignant syndrome and apply appropriate therapy.
Caution must be exercised when used in patients with concomitant neurological diseases and in patients taking drugs that affect the central nervous system.
When using the drug Cerucal ®, symptoms of Parkinson's disease may also be noted.
Cases of methemoglobinemia have been reported, which could be caused by a deficiency of the enzyme NADH-dependent cytochrome b5 reductase. In this case, taking the drug Cerucal ® must be immediately and completely stopped and appropriate measures taken. Cases of severe cardiovascular side effects, including vascular insufficiency, severe bradycardia, cardiac arrest and prolongation of the QT interval.
Caution must be exercised when using the drug Cerucal ® in elderly patients, patients with cardiac disorders (including prolongation of the QT interval), patients with impaired water and electrolyte balance, bradycardia and in patients taking other drugs that prolong the QT interval.
In case of moderate and severe renal failure and severe liver failure, a dose reduction is recommended (see section "Method of application and doses").

Impact on ability to drive vehicles and mechanisms

Care should be taken when driving vehicles and other mechanisms. because taking the drug can cause drowsiness and dyskinesia.

Release form

Tablets 10 mg.
50 tablets in a brown glass bottle, with a white stopper made of low density PE with an embossed inscription "AWD".
The bottle, along with instructions for use, is placed in a cardboard box.