Cerucal, 5 mg/ml 2 ml 10 pcs

CERUCAL is an antiemetic agent and is a specific blocker of dopamine (D2) and serotonin receptors. The mechanism of action is based on both central and peripheral effects of metoclopramide. Anti-emetic action is associated with blockade of brain dopamine receptors, which causes increase of irritation threshold of the vomiting center.

It has antiemetic effect, eliminates nausea and hiccups. It reduces esophageal motility, increases tone of the lower esophageal sphincter, accelerates gastric emptying, and also accelerates the movement of food through the small intestine without causing diarrhea.

Normalizes bile secretion, reduces spasm of the sphincter of Oddi, does not change its status, eliminates gall bladder dyskinesia. Stimulates the secretion of prolactin.

Pharmacokinetics

Vd is 2.2 – 3.4 L/kg.

Metabolized in the liver. The elimination half-life is from 3 to 5 hours, in chronic renal failure – 14 hours. It is excreted by kidneys during the first 24 hours unchanged and as metabolites (about 80% of single dose). It easily passes through the blood-brain barrier and is excreted with the breast milk.

Indications

Active ingredient

Composition

1 ml of solution contains:

Active substance:

metoclopramide hydrochloride monohydrate5.27 mg (equivalent to 5 mg of metoclopramide hydrochloride);

Auxiliary substances:

Sodium sulfite, 0.125 mg;

dinatrium edetate, 0.4 mg;

Sodium chloride – 8 mg;

Injection water – 991.705 mg.

How to take, the dosage

Intramuscularly or slowly intravenously.

Adults and adolescents over 14 years of age: 1 ampoule (10 mg metoclopramide) 3-4 times daily.

Children from 3 to 14 years of age: therapeutic dose is 0.1 mg metoclopramide/kg body weight; maximum daily dose is 0.5 mg metoclopramide/kg body weight.

Interaction

Incompatible with infusion solutions with an alkaline environment.

Decreases the effect of anticholinesterase agents.

It enhances absorption of antibiotics (tetracycline, ampicillin), paracetamol, levodopa, lithium and alcohol.

Decreases absorption of digoxin and cimetidine.

Accelerates the effects of alcohol and CNS depressant drugs.

No neuroleptic drugs should be prescribed concomitantly with metoclopramide to avoid possible exacerbation of extrapyramidal disorders.

May affect the effects of tricyclic antidepressants, monoamine oxidase inhibitors (MAOIs) and symptomatic agents.

Decreases the effectiveness of therapy with H2-histaminoblockers.

An increased risk of hepatotoxicity when combined with hepatotoxic agents.

Decreases the effectiveness of pergolide, levodopa.

Increases bioavailability of cyclosporine, which may require monitoring of concentrations.

Increases the concentration of bromocriptine.

If concomitant administration of cerucal with thiamine (Vitamin B1), the latter is rapidly broken down.

Special Instructions

During treatment it is necessary to refrain from driving and engaging in potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Patients are not allowed to drink alcohol during treatment.

In adolescents and patients with severe renal dysfunction the possible development of side effects is monitored; if they occur the drug is stopped.

It is not effective in vomiting of vestibular genesis.

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Contraindications

– Hypersensitivity to metoclopramide;
– pheochromocytoma (possible hypertensive crisis due to catecholamine release);
– intestinal obstruction, intestinal perforation and gastrointestinal bleeding;
– prolactin-dependent tumor;
– epilepsy and extrapyramidal motor disorders, first trimester of pregnancy and lactation, age under 2 years.

With caution: in arterial hypertension, liver function disorders, hypersensitivity to procaine and procainomide, children from 2 to 14 years of age.

In the second and third trimesters of pregnancy Cercucal is prescribed only with vital indications.
Patients with reduced renal function are prescribed the drug in reduced doses.

Because of sodium sulfite content, Cerucal should not be prescribed in patients with bronchial asthma with hypersensitivity to sulfite.

Side effects

Nervous system disorders: 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 twitches of the face, neck or shoulder muscles) may develop. Extrapyramidal disorders may occur: facial muscle spasm, trismus, rhythmic tongue protrusion, bulbar speech type, extraocular muscle spasm (including oculogyric crisis), spastic torticollis, opisthotonus, muscle hypertonus. Parkinsonism (tremor, muscle twitching, restricted mobility, 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 single cases development of severe neuroleptic syndrome is possible.

In long-term treatment with cerucal in elderly patients the development of symptoms of parkinsonism (tremor, muscle twitching, limited mobility) and tardive dyskinesias are possible.

Hematopoietic system disorders: agranulocytosis.

Cardiovascular system: supraventricular tachycardia, hypotension, hypertension.

Gastrointestinal tract: constipation, diarrhea, dry mouth.

Endocrine system disorders: with long-term use of the drug gynecomastia (enlargement of mammary glands in men), galactorrhea (spontaneous milk discharge from mammary glands) or menstrual disorders may occur; if these phenomena develop, withdraw metoclopramide.

Overdose

Symptoms: drowsiness, confusion, irritability, restlessness, seizures, extrapyramidal motor disorders, cardiovascular dysfunction with bradycardia and arterial hypo- or hypertension. In mild forms of poisoning, symptoms disappear in 24 hours after withdrawal of the drug. Depending on the severity of symptoms, it is recommended to establish surveillance of vital functions of the patient. Fatal cases of poisoning in overdose have not yet been identified.

Treatment: symptomatic. Extrapyramidal disorders are eliminated by slow administration of biperiden (doses for adults are 2.5 to 5 mg; follow the manufacturer’s recommendation). Diazepam may be used.

Pregnancy use

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

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

If it is necessary to use Cerucal during lactation, discontinuation of breastfeeding should be considered.

Similarities