Cerucal solution for intravenous and intramuscular administration 10 mg/2 ml ampoule 10 pcs. in Moscow

Compound

How does Cerucal work?

The medicine in tablet form is absorbed by the gastric mucosa within 20-30 minutes. The effect of using the solution intramuscularly is observed after 10–15 minutes. When administered intravenously - 1-3 minutes. Cerucal normalizes the tone of the muscular walls of the gastrointestinal tract, relaxes the spasm of the sphincter of Oddi, and improves the movement of bile. As a result, the evacuation of food masses from the small intestine is accelerated, physical discomfort and heaviness in the abdomen are reduced.

The antiemetic effect after a dose of Cerucal lasts up to 12 hours. The substances of the drug are partially metabolized in the liver. The drug does not accumulate in tissues and is completely eliminated from the body within 24 hours with the contents of the intestines and through the kidneys.

Directions for use and doses

Pills

Orally, approximately 30 minutes before meals, with water.

Adults: the recommended dose is 1 tablet. (10 mg metoclopramide) 3-4 times a day.

Adolescents over 14 years of age: the recommended dose is 1/2–1 tablet. 2–3 times a day.

The maximum single dose is 2 tablets. (20 mg); maximum daily dose - 6 tablets. (60 mg).

Solution for IM or IV administration

IM or slow IV.

Adults and adolescents over 14 years of age: 10 mg (1 amp.) 1–3 times a day.

Children from 2 to 14 years: therapeutic dose is 0.1 mg/kg, maximum daily dose is 0.5 mg/kg

To prepare for upper gastrointestinal examination

Adults and adolescents over 14 years of age: 1–2 amp. (10-20 mg metoclopramide) slowly over 1-2 minutes IV 10 minutes before the start of the study.

Children from 2 to 14 years: at the rate of 0.1 mg/kg, slowly, over 1–2 minutes IV, 10 minutes before the start of the study.

Prevention and treatment of nausea and vomiting caused by the use of cytostatics

Scheme 1. Short-term drip infusion (over 15 minutes) at a dose of 2 mg/kg half an hour before the start of treatment with a cytostatic agent, and then 1.5, 3.5, 5.5 and 8.5 hours after the use of cytostatics.

Scheme 2. Long-term drip infusion at a dose of 1 or 0.5 mg/kg/h, starting 2 hours before the use of a cytostatic agent, then at a dose of 0.5 or 0.25 mg/kg/h over the next 24 hours after use cytostatic agent.

The drip infusion is carried out briefly for 15 minutes after preliminary dilution of the dose of the drug Cerucal® in 50 ml of infusion solution.

The injection solution of Cerucal® can be diluted with isotonic sodium chloride solution or 5% glucose solution.

The drug Cerucal® is used throughout the entire period of treatment with cytostatic agents.

Common to both dosage forms

In case of renal dysfunction, the dose is selected according to the severity of renal dysfunction (see table).

Table

In patients with severe liver failure and ascites, the dose of the drug is halved due to an increase in T1/2.

The duration of metoclopramide therapy depends on the disease and is usually 4–6 weeks. Long-term therapy, no more than 6 months, is possible in exceptional cases.

Buy Cerucal solution intravenously and intramuscularly 5mg/ml 2ml No. 10 in pharmacies

Tradename

: Cerucal®

International nonproprietary name

: metoclopramide

Dosage form

: solution for intravenous and intramuscular administration

Compound

1 ml contains:

active ingredient metoclopramide hydrochloride monohydrate 5.270 mg (in terms of metoclopramide hydrochloride 5.000 mg);

excipients: sodium sulfite anhydrous 0.125 mg, disodium edetate 0.400 mg, sodium chloride 8.000 mg, water for injection up to 1.0 ml.

Description:

transparent colorless solution.

Pharmacotherapeutic group

Antiemetic - central dopamine receptor blocker.

pharmachologic effect

A specific blocker of dopamine receptors, weakens the sensitivity of the visceral nerves that transmit impulses from the pylorus (pylorus) and duodenum to the vomiting center. Through the hypothalamus and parasympathetic nervous system, it has a regulating and coordinating effect on the tone and motor activity of the upper gastrointestinal tract (including the tone of the lower digestive sphincter at rest). Increases the tone of the stomach and intestines, accelerates gastric emptying, reduces hyperacid stasis, prevents duodenopyloric and gastroesophageal reflux, stimulates intestinal motility.

Pharmacokinetics

The volume of distribution is 2.2-3.4 l/kg.

Metabolized in the liver. The half-life is from 3 to 5 hours, in chronic renal failure - 14 hours. It is excreted by the kidneys during the first 24 hours unchanged and in the form of metabolites (about 80% of a single dose). Easily penetrates the blood-brain barrier and is excreted in breast milk.

Indications for use

Adults

— 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. — To enhance peristalsis during X-ray contrast studies of the gastrointestinal tract.

Children

— Second line of treatment for postoperative nausea and vomiting. — Second line of prevention of delayed nausea and vomiting caused by chemotherapy.

Contraindications

— Hypersensitivity to metoclopramide and the components of the drug; - 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 antipsychotics 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 nicotinamide adenine dinucleotide (NADH) cytochrome b5 deficiency; - prolactinoma or prolactin-dependent tumor; - children under 1 year of age; - period of breastfeeding.

Carefully

When used in elderly patients; in patients with cardiac conduction disorders (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; in patients taking drugs that affect the central nervous system, depression (history); with renal failure of moderate and severe severity (creatinine clearance 15-60 ml/min); with severe liver failure; during pregnancy.

Use during pregnancy and breastfeeding

Pregnancy

Numerous data obtained on 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 characteristics (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 into breast milk. The possibility of adverse reactions in a child cannot be ruled out. The use of metoclopramide during breastfeeding is not recommended. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Directions for use and doses

Intravenous (IV) and intramuscular (IM).

IV injections should be administered as a slow bolus (at least 3 minutes).

Adults

Prevention of postoperative nausea and vomiting

Recommended single dose 10 mg (1 ampoule).

Second line treatment for postoperative nausea and vomiting. Second line prevention of delayed chemotherapy-induced nausea and vomiting

The recommended single dose of 10 mg (1 ampoule) is administered up to three times a day.

To enhance peristalsis during X-ray contrast studies of the gastrointestinal tract. As a means of facilitating duodenal intubation (to speed up gastric emptying and move food through the small intestine)

It is recommended to administer a slow (at least 3 minutes) intravenous bolus of 10-20 mg (1-2 ampoules) 10 minutes before the start of the study.

The maximum recommended daily dose is 30 mg or 0.5 mg/kg.

The period of administration of the drug in the form of injections should be as short as possible, followed by a transition to an oral or rectal dosage form.

Children's age from 1 to 18 years

Second line prevention of delayed chemotherapy-induced nausea and vomiting, second line treatment of postoperative nausea and vomiting

It is recommended to administer a slow (at least 3 minutes) intravenous bolus of 0.1-0.15 mg/kg up to 3 times a day.

The maximum daily dose is 0.5 mg/kg/day.

Dosage regimen

To enhance peristalsis during X-ray contrast studies of the gastrointestinal tract. As a means of facilitating duodenal intubation (to speed up gastric emptying and move food through the small intestine)

In children over 15 years of age

It is recommended to administer a slow (at least 3 minutes) intravenous bolus of 10-20 mg (1-2 ampoules) 10 minutes before the start of the study.

In children aged 1 to 15 years

It is recommended to administer a slow (at least 3 minutes) intravenous bolus at the rate of 0.1 mg/kg 10 minutes before the start of the study.

The maximum duration of treatment for the prevention of postoperative nausea and vomiting is 48 hours.

The maximum treatment period for preventing nausea and vomiting caused by chemotherapy is 5 days.

To avoid overdose, a minimum interval of 6 hours must be observed between doses, including in case of vomiting.

Elderly patients

In elderly patients, dose reduction may be required due to decreased renal and liver function.

Kidney 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 failure (creatinine clearance 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 common (≥ 1/10), common (≥ 1/100 - < 1/10), uncommon (≥ 1/1000 - < 1/100), rare (≥ 1/10000 - < 1/1000), very rare (< 1/10000), frequency unknown (cannot be estimated based on available data).

Disorders of 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).

Immune system disorders: uncommon - hypersensitivity; frequency unknown - anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash).

Endocrine system disorders*: uncommon - amenorrhea, hyperprolactinemia; rarely - galactorrhea; frequency unknown - gynecomastia.

*Endocrine disorders during long-term treatment are associated with hyperprolactinemia (amenorrhea, galactorrhea, gynecomastia).

Mental disorders: often - depression; infrequently - hallucinations; rarely - confusion.

Nervous system disorders: very often - drowsiness; often - asthenia, extrapyramidal disorders (especially in children and young patients and/or when recommended doses of the drug are exceeded, even after a single administration), parkinsonism, akathisia; uncommon - dystonia (including blurred vision and involuntary movement of the eye - oculogeric crisis), dyskinesia, impaired consciousness; rarely - seizures, especially in patients with epilepsy; frequency unknown - tardive dyskinesia, sometimes persistent, during or after long-term treatment, especially in elderly patients, neuroleptic malignant syndrome.

Cardiac disorders: infrequently - bradycardia; frequency unknown - cardiac arrest, which may be caused by bradycardia, atrioventricular block, sinus node block, prolongation of the QT interval on the electrocardiogram, ari.

Vascular disorders: often - low blood pressure; frequency unknown - cardiogenic shock, acute increase in blood pressure in patients with pheochromocytoma, transient increase in blood pressure.

Gastrointestinal disorders: often - nausea, diarrhea, constipation.

Renal and urinary tract disorders: frequency unknown - polyuria, urinary incontinence.

Genital and breast disorders: unknown frequency - sexual dysfunction, priapism.

Adverse reactions most common when using high doses of the drug

— Extrapyramidal symptoms: acute dystonia and dyskinesia, parkinsonism syndrome, akathisia developed even after using 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 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 are required depending on the clinical condition of the 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-anticholinergic agents and morphine derivatives have mutual antagonism with metoclopramide in terms of their effect on gastrointestinal motility.

Medicines that depress the central nervous system (morphine derivatives, tranquilizers, H1-histamine receptor blockers, antidepressants with sedative effects, barbiturates, clonidine and other drugs of these groups) can enhance the sedative effect under the influence of metoclopramide.

Metoclopramide enhances the effect of antipsychotics on 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 speaking 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 toxicity).

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.

Metoclopramide exposure increases when used concomitantly with strong CYP2D6 inhibitors, 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 atovaquone, the concentration of atovaquone in the blood plasma is significantly reduced (about 50%). Concomitant use of metoclopramide with atovaquone 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 Cerucal® in elderly patients.

From the nervous system, extrapyramidal disorders may be observed, especially in children and young patients and/or when using high doses, usually developing at the beginning of treatment or after a single use. The use of Cerucal® should be stopped immediately if extrapyramidal symptoms occur. The reactions are completely reversible after cessation of treatment, but may require symptomatic therapy (benzodiazepines in children and/or anticholinergic antiparkinsonian drugs in adults).

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 with Cerucal® drugs may lead to the development of tardive dyskinesia, which is 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 metoclopramide was used simultaneously with neuroleptics, as well as with metoclopramide monotherapy, neuroleptic malignant syndrome was observed. It is necessary to immediately stop treatment with Cerucal® if symptoms of neuroleptic malignant syndrome appear and apply appropriate therapy.

Caution should 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 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 Cerucal® must be completely stopped immediately and appropriate measures taken.

Severe cardiovascular side effects have been reported, including vascular insufficiency, severe bradycardia, cardiac arrest, and QT prolongation.

Caution should be exercised when using the drug Cerucal® in elderly patients, patients with cardiac disorders (including prolongation of the QT interval), patients with fluid and electrolyte imbalance, bradycardia and in patients taking drugs that prolong the QT interval.

For moderate to severe renal failure and severe hepatic failure, a dose reduction is recommended (see section "Dosage and Administration").

Impact on the ability to drive vehicles and machinery

Care should be taken when driving vehicles and other machinery, because taking the drug may cause drowsiness and dyskinesia.

Release form

Solution for intravenous and intramuscular administration 5 mg/ml.

2 ml of the drug in a transparent glass ampoule (type I), with colored rings applied (top green and bottom blue) on the head of the ampoule and a white ring on the neck of the ampoule

or

in a transparent glass ampoule (type I), with colored rings applied (top green and bottom blue) on the head of the ampoule and a notch on the neck of the ampoule and a white dot above it

or in a transparent glass ampoule (type I), with colored rings applied (top green and bottom blue) on the head of the ampoule and a notch on the neck of the ampoule and a blue dot above it.

5 ampoules in an open blister pack.

2 blister packs with instructions for use are placed in a cardboard box, on which additional protective stickers can be applied

or

10 ampoules per open blister pack.

1 blister pack with instructions for use is placed in a cardboard box, on which protective stickers can additionally be applied.

Storage conditions

Store in a place protected from light at a temperature not exceeding 25°C.

Keep out of the reach of children!

Best before date

5 years. Do not use after the expiration date.

Vacation conditions

Dispensed by prescription.

Release form

Tablets, 10 mg. 50 tablets each in a brown glass bottle with a white LDPE stopper with the embossed inscription “AWD”; 1 fl. in a cardboard box.

Solution for intravenous and intramuscular administration, 5 mg/ml. 2 ml of the drug in transparent glass ampoules (type I), with colored rings applied (top - green, bottom - blue) on the head of the ampoule and a white ring on the neck of the ampoule or in transparent glass ampoules (type I), with colored rings applied rings (top - green, bottom - blue) on the head of the ampoule and a notch on the neck of the ampoule and a white dot above it. 5 ampoules in open blister packaging. 2 blister packs in a cardboard box.