Cerucal

General characteristics. Structure:

Active ingredient: Metoclopramidum of a hydrochloride of monohydrate of 10,540 mg (that corresponds to 10 mg of Metoclopramidum of a hydrochloride).

Auxiliary ingredients:
potato starch, lactose monohydrate, gelatin, magnesium stearate, silicon the dioxide besieged.

Description: 

white, round, flat tablets, from risky - on one party, with a smooth surface and integral, slanted edges.

Pharmacological properties:

The specific blocker of dopamine receptors, weakens sensitivity of the visceral nerves transferring impulses from a pylorus and a 12-perstny gut to the emetic center. Through a hypothalamus and a parasympathetic nervous system exerts the regulating and coordinating impact on a tone and a physical activity of an upper part of digestive tract (including a tone of the lower digestive sphincter at rest).

Raises a tone of a stomach and intestines, accelerates gastric emptying, reduces hyperacid стаз, interferes with a peloric and ezofagealny reflux, stimulates an intestines peristaltics.

Pharmacokinetics. After intake it is quickly soaked up, time of achievement of the maximum concentration in a blood plasma of 30 - 120 min. Bioavailability makes 60 - 80%.

It is metabolized in a liver. The elimination half-life from 3 to 5 hours, at renal failures can increase till 14 o'clock.

It is removed by kidneys within the first 24 hours in not changed in a look and in the form of metabolites (about 80% of once accepted dose).

Easily gets through a blood-brain barrier, it is allocated with breast milk.

Indications to use:

• vomiting and nausea of various genesis;
• atony and hypotonia of a stomach and intestines (in particular, postoperative);
• dyskinesia of biliary tract, reflux esophagitis, functional pyloric stenosis;
• for strengthening of a vermicular movement when carrying out rentgenokontrastnykh researches of a zheludochno-kishechny path;
• stomach paresis at sugar diabetes
• as the means facilitating duodenal sounding (for acceleration of gastric emptying and advance of food on a small bowel).

Route of administration and doses:

Inside, approximately in 30 minutes prior to meal.

Adults and teenagers are more senior than 14 years: 1 tablet (10 mg of Metoclopramidum) 3 - 4 times a day.

Children from 2 to 14 years: the therapeutic dose makes 0,1 mg of Metoclopramidum/kg of body weight, the maximum daily dose makes 0,5 mg of Metoclopramidum/kg of body weight.

Duration of treatment makes about 4 - 6 weeks. In some cases treatment can be continued up to 6 months.

At a renal failure the dose of drug is selected according to degree of manifestation of a renal failure.
Clearance of creatinine       Metoclopramidum Dose
to 10                  ml/min. 10 mg once a day
from 11 to 60 ml/min.          the daily dose of 15 mg divided into two receptions (10 mg + 5 mg)

Features of use:

During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

In the course of treatment by the patient alcohol intake is forbidden.

At teenagers and at patients with heavy renal failures monitor possible development of by-effects, in case of their emergence cancel drug.

It is not effective at vomiting of vestibular genesis.

Against the background of use of Metoclopramidum distortions of these laboratory indicators of function of a liver and definition of concentration of Aldosteronum and prolactin in plasma are possible.

Side effects:

From a nervous system: there can sometimes be a feeling of fatigue, headaches, dizziness, sensation of fear, concern, a depression, drowsiness, a sonitus, in some cases, mainly at children, the diskinetichesky syndrome (involuntary tikoobrazny twitchings of face muscles, a neck or shoulders) can develop. Emergence of extrapyramidal frustration is possible: a spasm of facial muscles, a lockjaw, a rhythmic protrusion of language, bulbar type of the speech, a spasm of extraocular muscles (including okulogirny crisis), a spastic wryneck, an opisthotonos, a muscle hyper tone, parkinsonism (the tremor, twitching of muscles, limited mobility, risk of development in children and teenagers increases at exceeding of a dose of 0,5 mg/kg/days) and late dyskinesia (at patients of advanced age with хроническорй a renal failure). In isolated cases development of a heavy antipsychotic syndrome is possible.

At prolonged treatment by cerucal at some patients of advanced age development of parkinsonism (a tremor, twitching of muscles, limited mobility) and late dyskinesia is possible.

From system of a hemopoiesis: agranulocytosis.

From cardiovascular system: supraventricular tachycardia, hypotension, hypertensia.

From digestive tract: a lock, diarrhea, dryness in a mouth.

From endocrine system: at prolonged use of drug in rare instances can arise a gynecomastia (increase in mammary glands at men), a galactorrhoea (the spontaneous expiration of milk from mammary glands) or disturbances of a menstrual cycle; at development of these phenomena Metoclopramidum is cancelled.

Interaction with other medicines:

• reduces action of antikholinesterazny means.
• strengthens absorption of antibiotics (tetracycline, ampicillin), paracetamol, a levodopa, lithium and alcohol.
• reduces absorption of digoxin and Cimetidinum.
• strengthens effect of alcohol and medicines, the oppressing TsNS.
• it is not necessary to appoint along with Metoclopramidum antipsychotic drugs in order to avoid possible strengthening of extrapyramidal frustration.
• can influence effect of tricyclic antidepressants, inhibitors of a monoamino-oxidase (MAO) and sympathomimetic means.
• reduces efficiency of therapy H2-gistaminoblokatorami.
• increases risk of development of a hepatotoxic at a combination with gepatotoksichny means.
• reduces efficiency of a pergolid, levodopa.
• increases bioavailability of cyclosporine that can demand control of its concentration.
• increases concentration of Bromocriptinum.

Contraindications:

• hypersensitivity to Metoclopramidum;
• a pheochromocytoma (hypertensive crisis, in connection with emission of catecholamines is possible);
• intestinal impassability;
• perforation of intestines and gastrointestinal bleeding;
• prolaktinozavisimy tumor;
• epilepsy and extrapyramidal motive frustration;
• the first trimester of pregnancy and period of a lactation,
• age up to 2 years.

With care to apply at arterial hypertension, bronchial asthma, abnormal liver functions, hypersensitivity to Procainum and procaineamide, children aged from the 2nd up to 14 years.

During 2 and 3 trimesters of pregnancy drug is appointed only according to vital indications.

The patient with the lowered function of kidneys drug is appointed in the reduced doses.

Overdose:

Symptomatology: drowsiness, confusion of consciousness, irritability, concern, spasms, extrapyramidal motive frustration, dysfunctions of cardiovascular system with bradycardia and arterial hypo - or hypertensia. At easy forms of poisonings symptoms disappear in 24 hours after medicine cancellation. Depending on weight of symptomatology it is recommended to establish observation of the vital functions of the patient.

Fatal cases of poisonings at overdose are still not revealed.

Treatment: symptomatic. Extrapyramidal frustration eliminate with slow introduction of Biperidinum (doses for adults - 2,5 – 5 mg; it is necessary to adhere to recommendations of the producer). Diazepam use is possible.

Storage conditions:

List B. To store in the place protected from light, at a temperature not above 30 °C. To store in the place, unavailable to children. Period of validity of 5 years. Not to use drug after expiry date.

Issue conditions:

According to the recipe

Packaging:

50 tablets in a bottle of dark glass of a hydrolytic class 2 with a stopper from polyethylene of low density.
1 bottle with the application instruction in a cardboard pack.