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

Composition:Each tablet contains:
active substance: metoclopramide hydrochloride monohydrate in terms of anhydrous metoclopramide hydrochloride - 10.00 mg; Excipients: corn starch 74.375 mg, microcrystalline cellulose 45.070 mg, purified talc 1.500 mg, magnesium stearate 0.750 mg, silicon dioxide colloid 2.500 mg, purified water.

Description:White or almost white round, flat pills, with a dividing risk on one side and engraving "PERINORM" on the other.

Pharmacotherapeutic group:Antiemetics - dopamine receptors blocker central.

ATX: & nbsp

A.03.F.A Motility stimulators GIT

A.03.F.A.01 Metoclopramide

Pharmacodynamics:The specific blocker of dopamine (D2) and sredttonin (5-HTZ) receptors, depresses the hemorrhagic receptors 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 blood, gastric and pancreatic secretion. Stimulates the secretion of prolactin. Increases the sensitivity of tissues to acetylcholine (the action does not depend on vagal innervation,but eliminated holinoblokatorami). Stimulating the secretion of aldosterone, enhances the retention of sodium ions and the excretion of potassium ions.

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 from 2.5 to 6 hours, with kidney failure - 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.
Renal failure affects the clearance of mstoclopramide. In patients with varying degrees of renal insufficiency, a decrease in creatinine clearance is associated with reduced plasma clearance, renal clearance, chain clearance, and an increase in half-life (approximately 10 hours for creatinine clearance of 10-50 ml / min and 15 hours for creatinine clearance <10 ml / min ). However, the kinetics of mstoclopramide in the presence of renal insufficiency remained linear.Reduced clearance as a result of renal failure suggests that in order to avoid accumulation of the drug, correction is necessary in the direction of reducing the maintenance dosage.
Passes through the placental and blood-brain barrier and penetrates into the mother's milk.

Indications:Adults
- prevention of nausea and vomiting caused by chemotherapy;
- prevention of nausea and vomiting caused by radiation therapy;
- symptomatic treatment of nausea and vomiting, including acute migraine;
Adolescents 15-18 years old
Prevention of nausea and vomiting caused by chemotherapy (as second-line therapy).

Contraindications:- hypersensitivity to the components of the drug;
- bleeding from the gastrointestinal tract;
- stenosis of the pylorus;
- mechanical intestinal obstruction;
- perforation of the stomach or intestines;
- conditions after operations on the gastrointestinal tract;
- pheochromocytoma (confirmed and suspected);
- epilepsy;
- glaucoma;
- extrapyramidal disorders;
- Parkinson's disease;
- Methemoglobinemia (due to taking metoclopramide or a deficiency of nicotinamide adnine dinucleotide (NADI) cytochrome b5 in history;
prolactin-dependent tumors;
- vomiting during treatment or overdose with antipsychotics and in patients with breast cancer;
- simultaneous administration with levodopa and agonists of dopaminergic receptors;
- pregnancy (III trimester)
- the period of lactation (breastfeeding);
- Children under 15 years.
Do not appoint after operations on the gastrointestinal tract (like pyloroplasty or anastomosis of the intestine), because vigorous muscle contractions prevent healing.

Carefully:- elderly age,
- renal / hepatic insufficiency,
- bronchial asthma,
- arterial hypertension,
- violation of cardiac conduction,
- violation of water-electrolyte balance,
- a bradycardia,
- simultaneous administration of drugs that extend the QT interval,
- associated neurological diseases,
- simultaneous administration of drugs that affect the central nervous system,
- depression (in the anamnesis),
- Pregnancy (I and II trimesters)

Pregnancy and lactation:Metoclopramide contraindicated in the third trimester of pregnancy due to the risk of developing extrapyramidal disorders in newborns.When using metoclopramide, pregnant women should be monitored for newborns.
Metoclopramide is excreted in breast milk. It is not recommended to use metoclopramide during breastfeeding. If necessary, use during lactation should stop breastfeeding.

Dosing and Administration:Inside 30 minutes before eating, squeezed a small amount of water. The recommended single dose is 10 mg to 3 times a day. The maximum daily dose is 30 mg.
Metoclopramide in the form of tablets is not prescribed for adolescents with a body weight of less than 61 kg.
The maximum duration of treatment is 5 days.
A 6-hour interval between taking the drug should be observed, even in the case of vomiting or if the dose has not been absorbed.
Special groups of patients.
Elderly patients.
It is possible to reduce the dose taking into account the kidney and liver function, as well as the general condition of the patient.
Patients with clinically pronounced renal insufficiency.
In patients with terminal renal failure (creatinine clearance (CK) less than 10 ml / min) daily dose is 10 mg (1 tablet).
Patients with moderate and severe renal insufficiency (creatinine clearance (CK) 11-60 ml / min) is prescribed a dose of metoclopramide twice less than usual.
Patients with hepatic impairment of severe severity.
In patients with severe hepatic insufficiency, the dose should be reduced by 50%.

Side effects:From the nervous system: extrapyramidal disorders: spasm of facial musculature, trismus, rhythmic protrusion of the tongue, bulbar type of speech, spasm of extraocular muscles (including oculogic crisis), spastic torticollis, opisthotonus, muscle hypertonia; Parkinsonism (hyperkinesis, muscular rigidity); dyskinesia (in the elderly, with chronic renal failure); drowsiness, fatigue, anxiety, confusion, headache, tinnitus, depression, hallucinations, confusion.
In isolated cases, the development of malignant neuroleptic syndrome (fever, muscle contracture, altered consciousness and increased blood pressure) is possible.
From the digestive system: constipation or diarrhea, dry mouth.
Allergic reactions: urticaria, anaphylactic reactions (including anaphylactic shock).
From the endocrine system: with prolonged use in high doses - gynecomastia, galactorrhea, menstrual cycle. Endocrine disorders are associated with hyperprolactinemia.
From the hemopoietic system and lymphatic system: methemoglobinemia, sulfogemoglobinemia, agranulocytosis.
From the cardiovascular system: decrease or increase in arterial pressure, supraventricular tachycardia, bradycardia, cardiac arrest, atrioventricular blockade, blockade of the sinus node, prolongation of the QT interval, pirouette arrhythmia, cardiogenic shock.
Other: when used in high doses - hyperemia of the nasal mucosa.

Overdose:Symptoms: drowsiness, confusion, irritability, anxiety, convulsions, hallucinations, cardiac and respiratory arrest, cardiovascular system disorders, extrapyramidal disorders. As a rule, the symptomatology disappears after stopping the drug after 24 hours. Treatment: symptomatic. If necessary, treatment with holinoblokatorami and NP-Parkinsonics.

Interaction:- Strengthens the action of ethanol on the central nervous system, the sedative effect of hypnotics;
- increases the effectiveness of therapy with blockers H₂-gistaminovyh receptors;
- enhances the absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, levodopa, ethanol;
- slows the absorption of digoxin and cimetidine;
- reduces the effectiveness of pergolide;
- with simultaneous use with neuroleptics, the risk of developing extrapyramidal symptoms increases;
- anticholinesterase drugs may weaken the action of metoclopramide;
- increases the bioavailability of bromocriptine and cyclosporine;
- increases the risk of developing hepatotoxicity when taken together with hepatotoxic agents;
- simultaneous use with tricyclic antidepressants, MAO inhibitors, sympathomimetics is not recommended because of the possibility of mutual enhancement of side effects and unpredictability of changes in the expression of the action of antidepressants and sympathomimetics;
- when used simultaneously with serotonin reuptake inhibitors, as with neuroleptics, the risk of developing extrapyramidal symptoms increases;
- simultaneous use of metoclopramide with levodopa or antagonists of dopamine receptors is contraindicated in connection with the existing mutual antagonism;
- ethanol enhances the sedative effect of metoclopramide;
- m-holinoblokatory and derivatives of morphine have a mutual antagonism with metoclopramide in relation to the influence of peristalsis of the gastrointestinal tract;
- drugs that depress the central nervous system (morphine derivatives, tranquilizers, Ngystamine receptor blockers, antidepressants with sedative effect, barbiturates, clone idi and other drugs of these groups), can enhance sedative effect under the influence of metoclopramide;
- with simultaneous appointment of metoclopramide with suxamethonim, the duration of neuromuscular blockade may increase;
- Metoclopramide exposure increases with simultaneous use with potent inhibitors of the CYP2D6 isoenzyme, for example, fluoxetype and paroxystine;
- simultaneous use with drugs that have a central stimulating effect (for example, monoamine oxidase inhibitors and sympathomimetics), can lead to a change in their effect, which may require adjustment of dosages.

Special instructions:Metoclopramide is not effective in vomiting of vestibular genesis.
Against the background of the use of metoclopramide, there are possible distortions of these laboratory parameters of liver function and determination of the concentration of aldosterone and prolactin in plasma.
Most side effects occur within 36 hours of the start of treatment and take place within 24 hours after cancellation. Treatment should be as short as possible.
It should be borne in mind that with prolonged use of metoclopramide in high or medium doses in elderly patients, extrapyramidal disorders, especially parkinsonism and tardive dyskinesia, may develop.
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 (driving vehicles, etc.).

Form release / dosage:Tablets 10 mg.

Packaging:For 10 tablets in a blister Al / PVC.
For 2, 10 or 20 blisters together with the instructions for use are placed in a cardboard box.

Storage conditions:In a dry, dark place at a temperature of no higher than 25FROM. 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 / 03

Date of registration:22.10.2009 / 07.04.2015

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)