Buy Generic Maxolon (Metoclopramide) 10 mg online

 • Metoclopramide general information

      • Metoclopramide (Metoclopramide): instruction, and the use of a formula

      • Code CAS

      • substances characteristic of metoclopramide

      • Pharmacology

      • Application of the substance metoclopramide

      • Contraindications

      • Restrictions on the use

      • Application of pregnancy and breastfeeding

      • Side effects of metoclopramide substances

      • Interaction

      • Overdose

      • Dosing and Administration

      • Precautions substance metoclopramide

Maxolon Metoclopramide 10 mg
Most popular brand: Maxolon
Active ingredient: Metoclopramide
Available dosage forms: 10 mg
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Metoclopramide general information

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Metoclopramide (Metoclopramide): instruction, and the use of a formula

Code CAS

substances characteristic of metoclopramide

metoclopramide hydrochloride ; white crystalline solid, is odorless, soluble in water, ethanol. pKa ; 0.6 and 9.3. The molecular weight of 354,3.

Pharmacology

Mode of action -. Prokinetic, antiemetic, protivoikotnoe

It is an antagonist of dopamine (the D 2 ) receptors and serotonin (5 – HT 3 ) receptors (in high doses). It stimulates the motor activity of upper gastrointestinal (including adjusts the tone of the lower esophageal sphincter at rest) and normalizes its motor function. Enhances the tone and amplitude of gastric contractions (especially antral), relaxes the pyloric sphincter and the duodenal bulb, increases peristalsis and accelerates gastric emptying. It normalizes the separation of bile (increased pressure in the gallbladder and bile ducts), reduces spasm of the sphincter of Oddi, eliminates dyskinesia gallbladder.

The antiemetic activity is due to blockade of the central and peripheral D 2 – dopamine receptors, resulting in the inhibition of the trigger zone of the vomiting center and reducing the perception of signals from visceral afferent nerves. As an antiemetic effective nausea and vomiting of various etiologies, including caused by cancer chemotherapy (prevention) related to anesthesia, side effects of drugs (digitalis preparations, cytostatics, anti-TB drugs, antibiotics, morphine), diseases of the liver and kidneys, uremia, cranio – brain injury, vomiting of pregnant women, in violation of the diet. Migraine metoclopramide used to prevent nausea and gastric stasis and to stimulate suction antimigraine drugs. ingested. Metoclopramide is ineffective vomiting vestibular origin.

Suppresses the central and peripheral effects of apomorphine, increases the secretion of prolactin, causes a transient increase in levels of aldosterone (a short term fluid retention), increases the tissue sensitivity to acetylcholine (an action does not depend on vagal innervation, but eliminated holinoblokatorami).

Quickly and well absorbed after oral administration, C max is achieved through the 1 – 2 h after administration of a single dose, bioavailability ; 60 – 80%. Binding to plasma proteins ; about 30%. Easily it passes through the blood-tissue barriers, including the BBB. the placental barrier, enters the breast milk. The volume of distribution ; 3.5 l / kg. Biotransformed in the liver. T 1/2 with normal renal function is 4 – 6 hours for the kidney function ; to 14 hours. excreted by the kidneys (with ingestion of about 85% of the dose within 72 h appears in the urine in an unmodified form and in the form of sulfate and glucuronide conjugates).

Start to work through 1 – 3 minutes after the on / in the introduction, in 10 – 15 minutes after the / m, 30 – 60 min after oral administration; effect lasts 1 – 2 hours.

carcinogenicity, mutagenicity, effects on fertility

In the 77 – week study in rats receiving oral doses exceeding MRDCH about 40 times, recorded an increase in prolactin levels, which remained elevated during chronic administration. It has been found increased incidence of mammary tumors in rodents with chronic administration of prolactin – stimulus neuroleptics and metoclopramide. However, in clinical and epidemiological studies found no association between these drugs and the formation of tumors.

In the Ames test mutagenic properties were found metoclopramide.

In experiments on mice, rats and rabbits with a / c. V / m. n / a and metoclopramide administered orally at doses of 12 – 250 times the human dose, fertility disorders not detected.

Application of the substance metoclopramide

Nausea, vomiting, hiccups of various origins (in some cases it may be effective in vomiting caused by radiation therapy or receiving cytostatics), functional dyspepsia, gastro – oesophageal reflux , hypotension, and atony of the stomach and duodenum (incl . postoperative), biliary dyskinesia, flatulence, exacerbation of gastric ulcer and duodenal ulcer (in the complex therapy), preparation for diagnostic gastrointestinal studies.

Contraindications

Hypersensitivity, bleeding from the gastrointestinal tract. stenosis of the pylorus, mechanical intestinal obstruction, perforation of the wall of the stomach or intestines (including state, when the gain of gastrointestinal motor activity is not desirable), glaucoma, pheochromocytoma (possible hypertensive crisis due to the release of catecholamines from the tumor), epilepsy (severity and frequency seizures may increase), Parkinson’s disease and other extrapyramidal disorders (may increase), prolaktinzavisimye tumor, a young child up to 2 years (increased risk of dyskinetic syndrome).

Restrictions on the use

Asthma (increases the risk of bronchospasm), hypertension (with on / in a possible deterioration due to catecholamine release), liver and / or kidney failure, advanced age, children under 14 years of age (for parenteral administration).

Application of pregnancy and breastfeeding

In experiments on mice, rats and rabbits with a / c. V / m. n / a and metoclopramide administered orally at doses of 12 – 250 times the human dose, the adverse effects on the fetus is not revealed.

When pregnancy is permitted only when necessary (adequate and well-controlled studies in humans have not done).

Category effects on the fetus by FDA ; B.

Although complications are not recorded in humans during the period of breastfeeding should be used with caution (passes into breast milk).

Side effects of metoclopramide substances

The frequency of side effects is correlated with the dose and duration of administration of the drug.

From the nervous system and sensory organs: restlessness (10%), drowsiness (10%, often at high doses), unusual tiredness or weakness (10%). Extrapyramidal disorders, including acute dystonic reactions (0.2% at doses of 30 – 40 mg / day), such as convulsive twitching of facial muscles, trismus, opisthotonos, muscle hypertonicity, spasmodic torticollis, a spasm of extraocular muscles (including oculogyric crisis), rhythmic protrusion tongue, bulbar type of speech; rare ; stridor and dyspnea possibly due laringospazmom. Parkinsonian symptoms: bradykinesia, tremor, muscle rigidity ; manifestation of dopamine – blocking action, the risk of children and adolescents increased in excess of the dose of 0.5 g / kg / day. Tardive dyskinesia, including involuntary movements of the tongue, bombast, uncontrolled chewing movements, uncontrolled movements of the arms and legs (see. Also “Precautions”). Insomnia, headache, dizziness, disorientation, (symptoms were moderate to severe degree and have included suicidal thoughts and suicide), anxiety, confusion, ringing in the ears; rare ; hallucinations. There are rare reports of development of neuroleptic malignant syndrome (hyperthermia, muscle rigidity, altered mental status, autonomic dysfunction) (see. Also “Precautions»).

From the cardio – vascular system and blood (blood, hemostasis): hypotension / hypertension, tachycardia / bradycardia, fluid retention.

From the digestive tract: constipation / diarrhea, dry mouth; rare ; hepatotoxicity (jaundice, abnormal liver function parameters ; if metoclopramide used in conjunction with other hepatotoxic agents).

Allergic reactions: hives.

Other: frequent urination, urinary incontinence, chronic administration of high doses of ; gynecomastia, galactorrhea, menstrual disorders, asymptomatic weak congestion of the nasal mucosa, agranulocytosis.

It has been reported about the development of methemoglobinemia in preterm and term infants born in that V / m was administered in doses of metoclopramide 1 – 2 mg / kg / day for 3 days or more.

Interaction

Antipsychotics (especially phenothiazines and derivatives butyrophenone) increase the likelihood of extrapyramidal disorders. In an application reduces the effectiveness of levodopa. When taken with medicines. cause CNS depression ; strengthening of sedation. When co-administered with metoclopramide caused a decrease in gastric emptying time may increase the bioavailability of cyclosporine (may need to be monitoring of cyclosporine concentrations). It may reduce the absorption of from the stomach (maybe need a dose adjustment of digoxin). It can accelerate the absorption of mexiletine. It accelerates the absorption of paracetamol, . Concomitant use with alcohol may enhance the depressant effect of alcohol or metoclopramide on the CNS. and expedite the removal of alcohol from the stomach, thus likely increasing the rate and extent of its absorption in the small intestine. The combined use of drugs. containing opioids, can block the action of metoclopramide on gastrointestinal motility. Concomitant use with metoclopramide may reduce the effect of cimetidine due to the reduction of its absorption.

Overdose

Symptoms: hypersomnia, confusion, extrapyramidal disorders.

Treatment: discontinuation of the drug (symptoms disappear within 24 hours after admission).

Dosing and Administration

Inside, in / m. I / O Adults: inside ;. 5 & ​​ndash; 10 mg 3 times a day before meals; / m or / ; 10 mg; the maximum single dose of ; 20 mg, the maximum daily ; 60 mg (for all routes of administration). Children older than 2 years ; depending on age. Patients with hepatic impairment the starting dose should be reduced by 2 times due to increased T 1/2 . If the kidney function of the dose is adjusted depending on creatinine clearance.

Precautions substance metoclopramide

Patients who have hypersensitivity to procaine or procainamide, may be sensitive to metoclopramide.

There should be appointed after operations on the digestive tract (such as pyloroplasty or intestinal anastomosis), because muscle contractions interfere with the healing of joints.

Metoclopramide can be administered to patients with a history of depression only if the expected benefit outweighs the potential risk.

Extrapyramidal disorders may occur when using metoclopramide in therapeutic doses in patients of any age (see. Also “Side effects”). More often, however, they occur in high doses. Extrapyramidal symptoms are expressed primarily as acute dystonic reactions, manifested in the first 24 – 48 h of treatment, were more frequent in adolescents and adults younger than 30 years.

parkinsonian symptoms were noted typically within the first 6 – months after the start of treatment, but can also appear after a longer period of time. These symptoms disappear, usually within 2 – 3 months after discontinuation of metoclopramide.

metoclopramide treatment can lead to the development of tardive dyskinesia . often irreversible (see. also “Side effects”). The risk of developing tardive dyskinesia and the likelihood that it will become irreversible increase with duration of treatment and total cumulative dose. With the development of the patients symptoms of tardive dyskinesia metoclopramide therapy should be discontinued. In some patients, symptoms may disappear partially or completely within a few weeks or months after discontinuation PM. Special studies on the risk of tardive dyskinesia in the treatment of metoclopramide has not been, however, in one of the published studies have reported that the incidence of this complication is about 20% among patients treated with metoclopramide at least 12 weeks. In this connection, the continuous duration of treatment is 12 weeks. except for the rare cases where the therapeutic effect is believed to outweigh the risk of developing the severe complications. Tardive dyskinesia is more common in the elderly, women and people with diabetes.

There are rare reports of potentially fatal symptom complex – neuroleptic malignant syndrome (NZS) associated with metoclopramide therapy (see also ‘Side effects’.). Clinical manifestations include NZS hyperthermia, muscle rigidity, altered mental status, and autonomic instability (irregular pulse or blood pressure is unstable. Tachycardia, sweating, arrhythmia). With the development of CIP requires the immediate withdrawal of metoclopramide and other drugs. It is not necessary for concomitant therapy, conducting intensive symptomatic treatment and monitoring.

On the background of metoclopramide may be distorted laboratory parameters ; such as liver function tests, and aldosterone levels in serum prolactin.

In the metoclopramide treatment period should not drink alcohol in order to avoid the risk of complications.

Keep in mind the possibility of reducing the concentration of attention and increase response time during treatment (better give up driving and working with potentially dangerous equipment).

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