Perinorm - instructions for use, dose, side effects, contraindications

Composition:Every 5 ml of oral solution contains:
active substance: metoclopramide hydrochloride in terms of anhydrous substance 5.00 mg;
Excipients: methylparaben - 6.67 mg, nropylparaben 0.50 mg, citric acid monohydrate 0.835 mg, sodium metabisulphite 2.50 mg, sorbitol 1.75 ml, glycerol 0.75 ml, quinoline yellow soluble dye 1, 60 mg, dye brilliant blue - 0.02 mg, fruit assortment essence - 0.025 ml, vanilla essence - 0.05 ml, purified water up to 5.00 ml.

Description:Transparent solution of green color; the smell of fruit platter, with a touch of vanilla.

Pharmacotherapeutic group:Antiemetics - dopamine receptors blocker central.

ATX: & nbsp

A.03.F.A Motility stimulators GIT

A.03.F.A.01 Metoclopramide

Pharmacodynamics:A specific blocker of dopamine (D2) and serogonine (5-HT3) receptors, depresses the chemoreceptors of the trigger zone of the brainstem, weakens the sensitivity of the visceral nerves that transmit pulses from the pyloric and duodenum to the vomiting center. Through the hypothalamus and the parasympathetic nervous system (the innervation of the gastrointestinal tract) has a regulating and coordinating effect on the tone and motor activity of the upper gastrointestinal tract (including the tone of the lower sphincter of the esophagus at rest). Increases the tone of the stomach and intestines, accelerates the emptying of the stomach, reduces the hyperacid stasis, prevents pyloric and esophageal reflux, stimulates intestinal peristalsis.
Normalizes the separation of bile, reduces the spasm of the sphincter of Oddi. Without changing its tone, it eliminates dyskinesia of the gallbladder. Does not affect the tone of the blood vessels of the brain, blood pressure, respiratory function, as well as kidney and liver, on hematopoiesis, gastric and pancreatic secretion. Stimulates the secretion of prolactin.Increases the sensitivity of tissues to acetylcholine (the action of nc depends on vagal innervation, but is eliminated by holinoblokatorami). Stimulating the secretion of aldosterone, enhances the retention of sodium ions Na + and the removal of potassium ions K +.

Pharmacokinetics:Quickly absorbed from the gastrointestinal tract. In connection with partial destruction in the liver after absorption, bioavailability is 75%. The volume of distribution is 3.5 l / kg. The maximum concentrations in the blood are proportional to the dose taken and are reached after 1-2 hours. Connection with plasma proteins - 13-30%. It is metabolized in the liver. The half-life period is 2.5 to 6 hours, with renal dysfunction up to 14 hours. Removal of the drug occurs mainly through the kidneys for 24-72 hours in unchanged form and in the form of conjugates. Passes through the placental and blood-brain barrier and penetrates into the mother's 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 the 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 (NADH) deficiency of cytochrome b5 in history;
prolactinoma or prolactin-dependent tumor;
- pregnancy (III trimester);
- the period of breastfeeding;
- Children under 15 years.

Carefully:When used in elderly patients.
In patients with cardiac conduction abnormality (including QT interval prolongation), water-electrolyte balance disturbance, bradycardia, in patients taking other drugs, prolonging QT interval, arterial hypertension.
In patients with concomitant neurological diseases, depression (in the anamnesis).
With renal failure of moderate and severe severity (creatinine clearance 15-60 ml / min).
With hepatic failure of severe severity.
During pregnancy (I-II trimesters).

Pregnancy and lactation:Pregnancy
Metoclopramide 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 in the use of metoclopramide at the end of pregnancy, it is impossible to exclude the possibility of developing extrapyramidal symptoms in a newborn. Metoclopramide Do not use at the end of pregnancy (during the third trimester).
Breastfeeding period
Metoclopramide in small amounts excreted in breast milk. It is impossible to exclude the possibility of developing adverse reactions in the child. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:Inside.
Adults and children start 15 years of age with a body weight of more than 60 kg The recommended dose is 10 mg to three times a day.The maximum 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 5 mg to 1-zraza per day. The maximum daily dose is 0.5 mg / kg body weight.
It is necessary to observe the minimum interval between doses of 6 hours. 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 (creatinine clearance less than 15-60 ml / min), the daily dose should be reduced by 50%.
Impaired liver function
In patients with severe hepatic insufficiency, the dose should be reduced by 50%.

Side effects:From the hemopoietic system and lymphatic system: methemoglobinemia, sulfemoglobinemia, leukopenia, neutropenia, agranulocytosis.
From the cardiovascular system: bradycardia, cardiac arrest, atrioventricular blockade, blockade of the sinus node, prolongation of the QT interval, arrhythmia of the pirouette type, lowering of arterial pressure, cardiogenic shock, acute increase in arterial pressure in patients with pheochromocytoma.
From the endocrine system: amenorrhea, hyperprolactinaemia, gynecomastia, galactorrhea, (with prolonged admission).
From the gastrointestinal tract: nausea, diarrhea, constipation.
From the side of the kidneys and urinary tract: polyuria, incontinence.
On the part of the genitals: sexual dysfunction, priapism.
From the immune system: hypersensitivity, anaphylactic reactions (including anaphylactic shock), allergic reactions (urticaria, maculopapular rash).
From the nervous system: drowsiness, asthenia, extrapyramidal disorders, parkinsonism, akathisia, dystonia, dyskinesia, impaired consciousness, convulsions, tardive dyskinesia, neuroleptic malignant syndrome.
Disorders of the psyche: depression, hallucinations, confusion.

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 case of development of extrapyramidal symptoms caused by overdose, or for other reasons, the treatment is exceptionally symptomatic (benzodiazepines in children, 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 simultaneous use of metoclopramide with levodopa and 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 prokinetic effect of metoclopramide, absorption of certain drugs may be impaired.
M-holinoblokatory and derivatives of morphine have a mutual antagonism with metoclopramide in relation to the effect on peristalsis of the gastrointestinal tract.
Drugs that depress the central nervous system (morphine derivatives, tranquilizers, H blockers₁-gistaminovyh receptors, antidepressants with sedative effect, barbiturates, cloidin and other drugs of these groups) can enhance the sedative effect of iodine by the influence of metoclopramide. Metoclopramide intensifies the action of neuroleptics in relation to extrapyramidal symptoms. With the simultaneous use of metoclopramide and tegrabenazine, there is a possibility of a dopamine deficiency, which can be accompanied by increased muscle stiffness or spasm, difficulty speaking or swallowing, anxiety, tremors, involuntary muscle movements.
The use of metoclopramide with serotonergic drugs, for example, with selective serotonin reuptake inhibitors, increases the risk of developing serogonine syndrome (serotonin intoxication).
Metoclopramide decreases the bioavailability of digoxin and cyclosporine. It is necessary to control the concentration of digoxin and cyclosporine in the blood plasma.
The exposure of metoclopramide increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme, for example, fluoxetine and paroxetiomas.
With the simultaneous use of metoclopramide with atovahona significantly reduced the concentration of atovahona in blood plasma (about 50%). 11 simultaneous use of metoclopramide with bromocriptine increases the concentration of bromocriggine in the blood plasma.
Metoclopramide enhances the absorption of tetracycline, mexiletine and lithium, reduces the absorption of cimetidine.

Special instructions:The drug should be discontinued immediately if extrapyramidal symptoms of neuroleptic malignant syndrome appear, as well as other adverse reactions. Metoclopramide is not effective in vomiting of vestibular geeze.
Against the background of the use of metoclopramide, there may be distortions in the laboratory parameters of liver function and the determination of the concentration of aldosterone and prolactin in the plasma.
During the treatment with the drug, alcohol is not recommended.

Effect on the ability to drive transp. cf. and fur:When taking the drug should be avoided potentially dangerous activities that require increased concentration of attention, rapid mental and motor reaction.

Form release / dosage:Solution for oral administration 1 mg / ml.

Packaging:A bottle of dark glass with a screw cap of 30 ml or 100 ml. 1 vial, 1 dosage pipette in a polyethylene package and instructions for use are placed in a cardboard box.

Storage conditions:In a dry, dark place at a temperature below 25 ° C. Keep out of the reach of children.

Shelf life:3 years.
Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N015834 / 02

Date of registration:22.10.2009 / 05.03.2015

Expiration Date:Unlimited

The owner of the registration certificate:Ipka Laboratories Ltd.Ipka Laboratories Ltd. India

Manufacturer: & nbsp

IPCA LABORATORIES, Ltd. India

Information update date: & nbsp2016-09-02

Illustrated instructions

Instructions

Perinorm (Perinorm)