Cerucal, solution for injection 10 mg/2 ml, 2ml x 10 ampoules — Made in Hungary — Free Delivery

Pharmacological properties

Pharmacodynamics. Metoclopramide is a central dopamine antagonist that also exhibits peripheral cholinergic activity.

Two main effects are noted: antiemetic and the effect of accelerating gastric emptying and passage through the small intestine.

The antiemetic effect is caused by the action on the central point of the brain stem (chemoreceptors - the activating zone of the vomiting center), probably due to inhibition of dopaminergic neurons. The increase in peristalsis is also partially controlled by the higher centers, but the mechanism of peripheral influence may also be partially involved, together with the activation of postganglionic cholinergic receptors and, possibly, inhibition of dopaminergic receptors in the stomach and small intestine. Through the hypothalamus and the parasympathetic nervous system, it regulates and coordinates the motor activity of the upper gastrointestinal tract. Increases the tone of the stomach and intestines, accelerates gastric emptying, reduces gastrostasis, prevents pyloric and esophageal reflux, stimulates intestinal motility. Normalizes the secretion of bile, reduces spasm of the sphincter of Oddi, does not change its tone, eliminates gallbladder dyskinesia.

Side effects mainly extend to extrapyramidal symptoms, which are based on a dopamine receptor-blocking mechanism on the central nervous system.

Long-term treatment with metoclopramide can lead to an increase in the concentration of prolactin in the blood plasma due to the absence of dopaminergic inhibition of prolactin secretion. Galactorrhea and menstrual irregularities were described in women, and gynecomastia in men, but these symptoms disappeared after discontinuation of treatment.

Pharmacokinetics. The onset of action on the gastrointestinal tract is noted within 1-3 minutes after intravenous administration and 10-15 minutes after intramuscular administration. The antiemetic effect lasts for 12 hours. 13-30% of metoclopramide binds to blood plasma proteins. The volume of distribution is 3.5 l / kg of body weight. Metabolized in the liver. T½ is 4-6 hours. Penetrates the BBB and the placental barrier, enters breast milk. Part of the dose (≈20%) is excreted in its original form, and the rest (≈80%) after metabolic transformations by the liver is excreted by the kidneys in compounds with glucuronic or sulfuric acid.

Renal failure In patients with severe renal insufficiency, creatinine clearance decreases to 70%, and T½ from the blood increases (≈10 hours for creatinine clearance of 10-50 ml / min and 15 hours for creatinine clearance of 10 ml / min).

Liver failure. In patients with liver cirrhosis, the accumulation of metoclopramide was noted, which was accompanied by a decrease in plasma clearance by 50%.

Indications

Adults

Prevention of postoperative nausea and vomiting.

Symptomatic treatment for nausea and vomiting, including those associated with acute migraines.

Prevention of nausea and vomiting caused by radiation therapy.

Children

As a second line preparation for the prevention of delayed nausea and vomiting caused by chemotherapy.

As a second-line preparation for the treatment of existing postoperative nausea and vomiting.

Application

The injection solution is administered intramuscularly or slowly intravenously.

IV metoclopramide should be used as a slow bolus injection for at least 3 minutes.

Adults

To prevent postoperative nausea and vomiting, the recommended single dose of metoclopramide is 10 mg.

For symptomatic treatment of nausea and vomiting, including those associated with acute migraines, as well as to prevent nausea and vomiting caused by radiation therapy, the recommended single dose of metoclopramide is 10 mg up to 3 times a day.

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

The use of injectable forms is carried out for a minimum period with the fastest possible transition to the use of oral or rectal forms of metoclopramide.

Children

When used to prevent postoperative nausea and vomiting, metoclopramide should be used after surgery.

The recommended dose of metoclopramide is 0.1–0.15 mg / kg up to 3 times a day. The maximum daily dose is 0.5 mg / kg. If it is necessary to continue using the preparation, at least 6-hour intervals should be observed.

The maximum duration of use of metoclopramide for treatment with established postoperative nausea and vomiting is 48 hours.

The maximum duration of use of metoclopramide to prevent delayed nausea and vomiting caused by chemotherapy is 5 days.

Elderly patients

Consideration should be given to dose reduction in the elderly due to age-related decline in renal and hepatic function.

Impaired renal function

In patients with end-stage renal dysfunction (creatinine clearance ≤15 ml / min), the dose of metoclopramide should be reduced by 75%.

In persons with moderate and severe renal impairment (creatinine clearance - 15-60 ml / min), the dose of metoclopramide should be reduced by 50%.

Liver failure

In patients with severe liver dysfunction, the dose of metoclopramide should be reduced by 50%.

Contraindications

Hypersensitivity to metoclopramide or to any other component of the preparation; gastrointestinal bleeding; mechanical intestinal obstruction; gastrointestinal perforation; confirmed or suspected pheochromocytoma, due to the risk of severe AR attacks; tardive dyskinesia due to neuroleptics.