Cerukal - instructions for use, doses, side effects, contraindications

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 with a risk on one side.

Pharmacotherapeutic group:Antiemetics - dopamine receptors blocker central.

ATX: & nbsp

A.03.F.A Motility stimulators GIT

A.03.F.A.01 Metoclopramide

Pharmacodynamics:Antiemetic, is a specific blocker of dopamine (D2) and serotonin receptors.The mechanism of action is based both on the central and peripheral effects of metoclopramide. Antiemetic action is associated with blockade of dopamine receptors of 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 sphincter of the esophagus, accelerates the emptying of the stomach, and accelerates the movement of food through the small intestine, without causing diarrhea. Normalizes the secretion of bile, reduces the spasm of the sphincter of Oddi, does not change its status, eliminates dyskinesia of the gallbladder. Stimulates the secretion of prolactin.

Pharmacokinetics:After oral intake quickly absorbed, the time to reach the maximum concentration in the blood plasma 30-120 minutes. Bioavailability is 60-80%.
Metabolised in the liver. The half-life period is from 3 to 5 hours, with violations of the kidneys can increase to 14 hours. It is excreted by the kidneys within the first 24 hours in unchanged form 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:- 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 components of the drug;
- gastrointestinal bleeding, mechanical intestinal obstruction or perforation of the wall of the stomach and intestines, conditions in which stimulation of the peristalsis of the gastrointestinal tract represents a risk;
- confirmed or suspected pheochromocytoma in connection with 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 agonists dopamine receptors;
- Methemoglobinemia due to metoclopramide or nicotinamide adenine dinucleotide (NADI) deficiency of cytochrome b5 in history;
prolactinoma or prolactin-dependent tumor;
- Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- children's age till 15 years;
- the period of breastfeeding.

Carefully:When used in elderly patients; in patients with cardiac conduction abnormality (including prolongation of the QT interval), disturbance of water electrolyte balance, bradycardia, taking other drugs, prolonging the QT interval, arterial hypertension; in patients with concomitant neurologic diseases, depression (in the anamnesis); with renal failure of moderate and severe severity (SC 15-60 ml / min); with hepatic insufficiency of severe severity; during pregnancy.

Pregnancy and lactation:Pregnancy
Numerous data obtained on the use in pregnant women (more than 1000 cases described) indicate a lack of fetotoxicity and the ability to cause malformations in the fetus. Mstocolopramide can be used during pregnancy (I-II trimesters) only if the potential benefit to the mother exceeds the potential risk to the fetus. In connection with the pharmacological features (like other neuroleptics), the use of metoclopramide at the end of pregnancy can not exclude the possibility of developing extrapyramidal symptoms in a newborn. Metoclopramide Do not use at the end of pregnancy (during the third trimester).When using metoclopramide, you should monitor the condition of the newborn.
Breastfeeding period
Metoclopramide in small amounts excreted in breast milk. It is impossible to exclude the possibility of development
adverse reactions in the child. The use of metoclopramide during breastfeeding is not recommended. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:Inside.
Adults and children over 15 years of age with a body weight of more than 60 kg
The recommended dose is I 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 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 should be observed, even in the event of vomiting. The maximum duration of treatment is 5 days.
Elderly patients
In elderly patients, a dose reduction may be required depending on the renal and hepatic function and general condition.
Renal insufficiency
In patients with terminal stage of 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 (KK 15-60 ml / min), the dose should be reduced by 50%.
Impaired liver function
In patients with hepatic insufficiency of severe severity, the dose should be reduced by 50%.

Side effects:The incidence of adverse reactions is classified as follows: very often (≥ 1/10), often (≥ 1/100 to <1/10). infrequently (≥ 1/1000 - <1/100), rarely (≥ 1/10000 - <1/1000), very rarely (<1/10000). frequency is unknown (can not be estimated based on available data).
From the side of the blood and lymphatic system: methemoglobinemia frequency is unknown, is likely due to a deficiency of the enzyme NADH-dependent cytochrome-b5 reductase, especially in neonates sulfgemoglobinemiya (usually while high-dose preparations sulfur), leukopenia, neutropenia, agranulocytosis.
From the heart: infrequent bradycardia; frequency is unknown cardiac arrest, which may be caused by bradycardia, atrioventricular block, sinus blockage, lengthening QT interval on the electrocardiogram, arrhythmia type "pirouette".
From the side 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, hyperprolactinemia; rarely - galactorrhea; frequency is unknown-ginekomastia.
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 is unknown - polyuria, incontinence.
From the genitals and the breast: 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 exceeding the recommended doses of the drug, even after a single injection), parkinsonism, akathisia: infrequently - dystonia,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.
Mental disturbance: often - depression; infrequently - hallucinations; rarely confusion.
Undesirable reactions, most common when using 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 case of developing extrapyramidal symptoms caused by an overdose or for another reason,treatment is exceptionally symptomatic (benzodiazepii in children and / or anticholinergic antiparkinsonian drugs in adults).
Symptomatic treatment and continuous monitoring of cardiac and respiratory functions are required depending on the clinical condition of the patient.
There is no specific antidote.

Interaction:Contraindicated concurrent use of metoclopramide with levodopa or dopamine receptor agonists, in connection with the existing mutual antagonism.
Alcohol increases the sedative effect of metoclopramide.
Combinations that require caution
In connection with the prokipetic effect of metoclopramide, absorption of certain drugs may be impaired.
M-holinoblokatory and derivatives of morphine have a mutual antagonism with metoclonramid in relation to the effect on peristalsis of the gastrointestinal tract.
Drugs that depress the central nervous system (morphine derivatives, tranquilizers, H1-histamine receptor blockers, antidepressants with sedative effect, barbiturates, clonidine and other drugs of these groups) may enhance the sedation effect of metoclopramide.
Metoclopramide enhances the effect of neuroleptics on extrapyramidal symptoms.
With concomitant use of metoclopramide and tetrabenazine, there is a possibility of a dopamine deficiency, which can be accompanied by increased muscle stiffness or spasm, difficulty in speaking or swallowing, anxiety, tremor, involuntary movements of muscles, 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. It is necessary to monitor the concentration of digoxin in the blood plasma. 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 are not established.
The 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 is not established, it is necessary to monitor the occurrence of adverse reactions in patients.
With the concomitant use of metoclopramide with atovahona, the concentration of atovahona in plasma is significantly reduced (about 50%). Concomitant use of metoclopramide with atovahona 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.
Extrapyramidal disorders are possible on the part of the nervous system, especially in children and young patients and / or when high doses are used, developing usually at the beginning of treatment or after a single application. The use of CERUKAL® should be stopped immediately if extrapyramidal symptoms appear. Reactions are completely reversible after discontinuation of treatment,However, they may require symptomatic therapy (children's bezodiazepines and / or anticholinergic antiparkinsonian drugs in adults).
To avoid an overdose of Cerucal®, a minimum interval of 6 hours should be observed, even in the event of vomiting.
Long-term treatment with Cerucal® can lead to the development of tardive dyskinesia, potentially irreversible, especially in elderly patients. Duration of treatment should not exceed 3 months due to the risk of developing tardive dyskinesia. If signs of tardive dyskinesia are present, treatment should be discontinued.
When metoclopramide was used simultaneously with neuroleptics, and also with metoclopramide monotherapy, neuroleptic malignant syndrome was noted. It is necessary to immediately stop treatment with CERUKAL® with the appearance of symptoms of neuroleptic malignant syndrome 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 Cerucal®, symptoms of Parkinson's disease may also be noted.
There have been reports of the occurrence of methemoglobinemia, which could be caused by a deficiency of the enzyme NADH-dependent cytochrome-b5 reductase. In this case, taking Cerulcal® should be immediately and completely discontinued and appropriate measures taken.
There have been reports of severe cardiovascular side effects, including vascular insufficiency, severe bradycardia, cardiac arrest, and prolongation of the QT interval. Caution should be exercised when using Cerucal®, in elderly patients, patients with cardiac impairment (including QT prolongation), patients with water-electrolyte balance disorders, bradycardia, and in patients taking other drugs that extend the QT interval.
In case of renal insufficiency of moderate and severe severity and liver failure of severe severity, a dose reduction is recommended (see section "Dosing and Administration").

Effect on the ability to drive transp. cf. and fur:Care should be taken when driving vehicles and other mechanisms, becausetaking the drug may cause drowsiness and dyskinesia.

Form release / dosage:Tablets 10 mg.

Packaging:50 tablets in a bottle of brown glass, with a cork of white color from PE low density with a relief inscription "AWD".
The bottle together with the instruction for use is placed in a cardboard box.

Storage conditions:Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:5 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N012812 / 01

Date of registration:29.01.2009 / 11.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel

Manufacturer: & nbsp

PLIVA HRVATSKA, d.o.o. Croatia

Representation: & nbspTeva Teva Israel

Information update date: & nbsp2016-09-10

Illustrated instructions

Instructions

Cerucal® (Cerucal®)