Cerucal tablets 10mg, No. 50

• 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.

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 starting 15 years old with a body weight of 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.
To avoid overdose, a minimum interval of 6 hours between doses must be observed, even in case of vomiting.
The maximum treatment period is 5 days.

Elderly patients
In elderly patients, a dose reduction may be required depending on the indicators of renal and hepatic function and general condition.

Renal failure
In patients with end-stage renal failure (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%.

Liver dysfunction
In patients with severe hepatic impairment, the dose should be reduced by 50%.

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.

• 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 is a risk;

• confirmed or suspected pheochromocytoma due to the risk of developing severe arterial hypertheisia;

• tardive dyskinesia, which developed after treatment with antipsychotics or metoclopramide in history;

• epilepsy (increased frequency and severity of seizures);

• Parkinson's disease;

• simultaneous use with levodopa and dopamine receptor agonists;

• a history of methemoglobinemia due to metoclopramide or nicotinamide adenine dinucleotide (NADH) deficiency;

• prolactinoma or prolactin-dependent tumor;

• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

• children under 15 years of age;

• period of breastfeeding.

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); with liver failure of severe severity; during pregnancy.

Tradename:

CerucalЃ

International non-proprietary name:

metoclopramide

Dosage form:

pills

Composition

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 - central dopamine receptor blocker.

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 a blockade of dopamine receptors in the brain, which causes an increase in the threshold of irritation of the vomiting center. Has antiemetic effect, eliminates nausea and hiccups. 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 the maximum concentration in blood plasma is 30-120 minutes. Bioavailability is 60-80%.
It is metabolized in the liver. The half-life is from 3 to 5 hours; in case of impaired renal function, it can increase 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). Easily penetrates 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 is a risk;

• confirmed or suspected pheochromocytoma due to the risk of developing severe arterial hypertheisia;

• tardive dyskinesia, which developed after treatment with antipsychotics or metoclopramide in history;

• epilepsy (increased frequency and severity of seizures);

• Parkinson's disease;

• simultaneous use with levodopa and dopamine receptor agonists;

• a history of methemoglobinemia due to metoclopramide or nicotinamide adenine dinucleotide (NADH) deficiency;

• prolactinoma or prolactin-dependent tumor;

• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

• children under 15 years of age;

• period of breastfeeding.

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); with liver failure of severe severity; during pregnancy.

Application during pregnancy and during 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 the potential benefit to the mother outweighs the potential risk to the fetus. Due to pharmacological features (like other antipsychotics). when using metoclopramide at the end of pregnancy, the likelihood of developing extrapyramidal symptoms in a newborn cannot be ruled out. Metoclopramide should not be used at the end of pregnancy (during the third trimester). When using metoclopramide, you should monitor the condition of the newborn.
Breastfeeding period
Small amounts of metoclopramide are excreted 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 administration and dosage

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 starting 15 years old with a body weight of 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.
To avoid overdose, a minimum interval of 6 hours between doses must be observed, even in case of vomiting.
The maximum treatment period is 5 days.
Elderly patients
In elderly patients, a dose reduction may be required depending on the indicators of renal and hepatic function and general condition.
Renal failure
In patients with end-stage renal disease (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%.
Liver dysfunction
In patients with severe hepatic impairment, the dose should be reduced by 50%.

Side effect

The frequency of adverse reactions is classified as follows: 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.Cardiac disorders
: infrequently bradycardia: the frequency is unknown cardiac arrest, which can be caused by bradycardia, atrioventricular block, sinus blockade for lengthening the Q interval electrocardiogram, arrhythmia type 'pirouette'.
On the part of the vessels: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 long-term 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: the frequency is unknown - polyuria, urinary incontinence.
On the part of the genitals and mammary gland: unknown frequency of sexual dysfunction, priapism.
From the 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 administration), 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 the use of high doses of the drug
- Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome and 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 disturbances, drowsiness, decreased level of consciousness, confusion, hallucinations, irritability, dizziness, bradycardia, changes in blood pressure, cardiac and respiratory arrest, abdominal pain.
Treatment
In the case of the development of extrapyramidal symptoms caused by an overdose or for another reason, the treatment is exclusively symptomatic (benzodiazepines in children and / or anticholinergic antiparkinsonian drugs in adults). Symptomatic treatment and constant monitoring of cardiac and respiratory functions are required, depending on the clinical condition of the patient. There is no specific antidote.

Interaction with other medicinal products

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 peristalsis of the gastrointestinal tract.
Medicines that depress the central nervous system (morphine derivatives, tranquilizers, H1-histamine receptor blockers, sedative antidepressants, barbiturates, clonidine and other drugs of these groups) can enhance the sedative effect under the influence of metoclopramide.
Metoclopramide enhances the effect of antipsychotics against extrapyramidal symptoms.
With the concomitant use of metoclopramide and tetrabenazine inside, there is a possibility of dopamine deficiency, which may be accompanied by an increase in muscle stiffness or muscle spasm, difficulty speaking or swallowing, anxiety, tremors, involuntary muscle movements, including facial muscles.
The use of metoclopramide with serotonergic drugs, for example, with selective serotonin reuptake inhibitors, increases the risk of developing serotonin syndrome (serotonin intoxication).
Metoclopramide reduces the bioavailability of digoxin. The concentration of digoxin in the blood plasma 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. The clinical consequences of this interaction have not been established.
Exposure of metoclopramide increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme. for example, fluoxetine and paroxetine. Although the clinical significance of this interaction has not been established, it is necessary to monitor the appearance of adverse reactions in patients.
With the concomitant use of metoclopramide with atovachone, the concentration of atovachone in the blood plasma is significantly reduced (about 50%). The 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 mexiletine and lithium.
Metoclopramide reduces the absorption of cimetidine.

special instructions

Caution should be exercised when using the drug Cerucal in elderly patients.
On the part of the nervous system, extrapyramidal disorders are possible, especially in children and young patients and / or when high doses are used, usually developing at the beginning of treatment or after a single use. The use of the drug CerucalЃ must be stopped immediately in case of extrapyramidal symptoms. Reactions are completely reversible after stopping 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 CerucalЃ, a minimum interval between doses of 6 hours must be observed, even in case of vomiting.
Long-term treatment with CerucalЃ 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.
With the use of metoclopramide simultaneously with antipsychotics, as well as with metoclopramide alone, neuroleptic malignant syndrome was noted. It is necessary to immediately stop treatment with CerucalЃ when symptoms of neuroleptic malignant syndrome appear and apply appropriate therapy.
Care must be taken when using in patients with concomitant neurological diseases and in patients taking drugs that affect the central nervous system.
When using the drug CerucalЃ, symptoms of Parkinson's disease may also occur.
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 CerucalЃ must be stopped immediately and completely and appropriate measures must be taken. Cases of severe cardiovascular side effects have been reported, including vascular insufficiency, severe bradycardia, cardiac arrest, and prolongation of the QT interval.
Care must be taken when using CerucalЃ in elderly patients, patients with cardiac disorders (including prolongation of the QT interval), patients with imbalance in 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 hepatic insufficiency, a dose reduction is recommended (see section 'Dosage and Administration').

Influence on the ability to drive vehicles and mechanisms

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

Release form

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

Storage conditions

Store in a dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

5 years. Do not use after the expiration date.

Conditions of dispensing from pharmacies

On prescription.