Metoclopramide (Cerukal) 10 mg, 50 pcs.

1 tablet contains:

Active substance: metoclopramide hydrochloride 10 mg;

Excipients: lactose; corn starch; purified talc; magnesium stearate; sodium starch glycolate; silicon colloidal anhydrous.

Metoclopramide - an antiemetic, helps to reduce nausea, hiccups; stimulates gastrointestinal motility. The antiemetic effect due to blockade of dopamine D2 receptors and an increase in the threshold of the trigger zone chemoreceptors is a blocker of serotonin receptors. It is believed that metoclopramide inhibits the relaxation of smooth muscle of the stomach caused by dopamine, thereby enhancing cholinergic reactions of the smooth muscles of the gastrointestinal tract. Helps to accelerate the emptying of the stomach by preventing relaxation of the body of the stomach and increasing the activity of the antrum and upper small intestine. Reduces the reflux of contents into the esophagus by increasing the pressure of the sphincter of the esophagus at rest and increases the clearance of acid from the esophagus due to an increase in the amplitude of its peristaltic contractions.

Metoclopramide stimulates the secretion of prolactin and causes a transient increase in the level of circulating aldosterone, which may be accompanied by short-term fluid retention.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the digestive tract. Plasma protein binding is about 30%. Biotransformed in the liver. It is excreted mainly by the kidneys both unchanged and in the form of metabolites. T1 / 2 is 4 to 6 hours

• vomiting, nausea, hiccups of various origins
• decreased tone of the stomach and intestines
• biliary dyskinesia
• flatulence
• preparation for diagnostic tests of the stomach and intestines.

• gastrointestinal bleeding
• intestinal obstruction
• epilepsy
• glaucoma
• hypersensitivity to the drug metoclopramide.

From the digestive system: at the beginning of treatment, constipation, diarrhea are possible; rarely - dry mouth.

From the side of the central nervous system: at the beginning of treatment, a feeling of fatigue, drowsiness, dizziness, headache, depression, akathisia are possible. Extrapyramidal symptoms may occur in children and young adults (even after a single use of metoclopramide): spasm of the facial muscles, hyperkinesis, spasmodic torticollis (usually disappear immediately after stopping the use of metoclopramide). With prolonged use, more often in elderly patients, the phenomena of parkinsonism, dyskinesia are possible.

From the hemopoietic system: at the beginning of treatment agranulocytosis is possible.

From the endocrine system: rarely, with prolonged use in high doses - galactorrhea, gynecomastia, menstrual irregularities.

Allergic reactions: rarely - skin rash.

With simultaneous use with anticholinergics, mutual attenuation of effects is possible.

With simultaneous use with antipsychotics (especially the phenothiazine series and derivatives of butyrophenone), the risk of extrapyramidal reactions increases.

With simultaneous use, the absorption of acetylsalicylic acid, paracetamol, ethanol is enhanced.

With iv administration, metoclopramide increases the absorption rate of diazepam and increases its maximum concentration in blood plasma.

With simultaneous use with a slowly dissolving dosage form of digoxin, a 1/3 decrease in the concentration of digoxin in the blood serum is possible. With simultaneous use with digoxin in a liquid dosage form or in the form of a rapidly dissolving dosage form, no interaction was noted.

With simultaneous use with zopiclone, absorption of zopiclone is accelerated; with cabergoline - a decrease in the effectiveness of cabergoline is possible; with ketoprofen - the bioavailability of ketoprofen decreases.

Due to antagonism with respect to dopamine receptors, metoclopramide can reduce the antiparkinsonian effect of levodopa, while it is possible to increase the bioavailability of levodopa due to the acceleration of its evacuation from the stomach under the influence of metoclopramide. The results of the interaction are mixed.

With simultaneous use with mexiletine, absorption of mexiletine is accelerated; with mefloquine - increases the absorption rate of mefloquine and its concentration in blood plasma, while it is possible to reduce its side effects.

With simultaneous use with morphine, absorption of morphine by ingestion is accelerated and its sedative effect is enhanced.

With simultaneous use with nitrofurantoin, the absorption of nitrofurantoin decreases.

When using metoclopramide immediately before the introduction of propofol or thiopental, it may be necessary to reduce their induction doses.

In patients receiving metoclopramide, the effects of suxamethonium chloride are enhanced and prolonged.

With simultaneous use with tolterodine, the effectiveness of metoclopramide decreases; with fluvoxamine - a case of the development of extrapyramidal disorders is described; with fluoxetine - there is a risk of extrapyramidal disorders; with cyclosporine - increases the absorption of cyclosporin and increases its concentration in blood plasma.

Tablets are taken 30 minutes before meals with a little water. Adults - 5-10 mg 3-4 times a day. The maximum single dose is 20 mg, daily - 60 mg. Children over 6 years old - 5 mg 1-3 times a day.

Hypersomnia, disorientation, and extrapyramidal disorders may occur. As a rule, the symptoms disappear after stopping the drug within 24 hours. If necessary, treatment with anticholinergics and antiparkinsonian drugs.

It is used with caution in patients with bronchial asthma, arterial hypertension, impaired liver and / or kidney function, and Parkinson's disease.

With extreme caution should be used in children, especially young children, because they have a significantly higher risk of dyskinetic syndrome. Metoclopramide in some cases may be effective for vomiting caused by cytostatics.

When used in elderly patients, it must be borne in mind that with prolonged use of metoclopramide in high or medium doses, extrapyramidal disorders, especially parkinsonism and tardive dyskinesia, are the most common side effects.

Against the background of the use of metoclopramide, distortion of the data of laboratory parameters of liver function and determination of the concentration of aldosterone and prolactin in blood plasma are possible.

Influence on the ability to drive vehicles and control mechanisms

During the treatment period, potentially hazardous activities requiring increased attention, rapid psychomotor reactions should be avoided.

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