- Each 5 mL of Syrup contains: Metoclopramide hydrochloride 5 mg
- Each 1 mL of Drops contains: Metoclopramide hydrochloride 1 mg
- Each suppository contains: Metoclopramide hydrochloride 10 mg, 20 mg
ACTION AND CLINICAL PHARMACOLOGY:
Metoclopramide has antiemetic properties, which are believed to result from its action on the chemoreceptor trigger zone. A peripheral mechanism of action also may be involved.
Metoclopramide increases resting pressure in the lower esophageal sphincter and the gastric fundus, and gives rise to an increase in the amplitude of peristaltic movements in the esophagus, gastric antrum and small intestine. These actions result in hastened esophageal clearance, accelerated gastric emptying and shortened transit time through the small bowel. These effects are blocked by atropine and opioids but not by vagotomy. Metoclopramide elevates serum prolactin and also causes transient increases in circulating aldosterone levels. These effects are thought to be due to blockade of dopamine receptors at the pituitary and adrenocortical cellular level.
INDICATIONS AND CLINICAL USES:
An adjunct in the management of delayed gastric emptying associated with subacute and chronic gastritis or following vagotomy and pyloroplasty and other surgical procedures.
Metoclopramide has also been found useful as an adjunct to facilitate small bowel intubation.
Metoclopramide has been found useful as an adjunct to facilitate gastroduodenal evacuation of barium meals and improve radiological visualization of the gastroduodenal region in patients with gastric atonia, pylorospasm, spasm of the duodenal bulb, or with mechanical gastric outlet obstruction. Metoclopramide has also been shown to accelerate small bowel transit of the barium meal and to facilitate fluoroscopy of the terminal ileum.
Metoclopramide, when used preoperatively by the oral route, may be useful to reduce postoperative vomiting induced by narcotics.
Should not be used whenever stimulation of gastrointestinal motility might be dangerous; i.e., in the presence of gastrointestinal hemorrhage, mechanical obstruction or perforation. Metoclopramide is contraindicated in patients with known sensitivity or intolerance to the drug.
Metoclopramide elevates prolactin levels and the elevation persists during chronic administration. Tissue culture experiments indicate that approximately 1/3 of human breast cancers are prolactin-dependent in vitro, a factor of potential importance if the prescription of metoclopramide is contemplated in a patient with previously detected breast cancer.
Metoclopramide should not be used in patients with epilepsy or extrapyramidal symptoms unless the expected benefits outweigh the risk of increased frequency and severity of seizures or extrapyramidal reactions.
Pregnancy: The safe use of metoclopramide in pregnancy has not been established. Therefore, it should not be used in pregnant women, unless, in the opinion of the physician, the expected benefits to the patient outweigh potential risks to the fetus.
Children: Daily dose should not exceed 0.5 mg/kg, since with higher doses extrapyramidal symptoms frequently occur.
- The recommended dosage of metoclopramide should usually not be exceeded since a further increase in dosage will not produce a corresponding increase in clinical response.
- This medicine may cause tardive dyskinesia (a movement disorder). Treatment should be discontinued if the following symptoms exercised while taking this medicine: lip smacking or puckering, puffing of the cheeks, rapid or worm-like movements of the tongue, uncontrolled chewing movements, or uncontrolled movements of the arms and legs. Tardive dyskinesia may develop in patients treated with metoclopramide. The elderly, especially elderly women, appear to be at increased risk. There is no known treatment for tardive dyskinesia and is more likely to be irreversible with long-term treatment (over 12 weeks).
- Less frequently, tardive dyskinesia can develop with short term treatment at low doses; in these cases, the symptoms are more likely to disappear either partially or completely over time, once treatment has been stopped.
- Metoclopramide treatment beyond 12 weeks should be avoided, unless the benefit is judged to outweigh the risk.
Anticholinergic drugs antagonize the effects of metoclopramide on gastrointestinal motility. Metoclopramide should not be used in conjunction with ganglioplegic or neuroleptic drugs since potentiation of effects might occur. The sedative effects of metoclopramide may be potentiated by sedatives, hypnotics, narcotics and anxiolytics.
Metoclopramide may decrease the absorption of drugs from the stomach (e.g. digoxin) whereas absorption from the small bowel may be accelerated (e.g., acetaminophen, tetracyclines, levodopa, ethanol).
Care should be exercised when metoclopramide is administered in combination with a MAO inhibitor.
Drowsiness, fatigue and lassitude occur in approximately 10% of patients at the usual recommended dosage. Less frequent adverse reactions, occurring in approximately 5% of patients are insomnia, headache, dizziness and bowel disturbances. Galactorrhea and menstrual disorders have also been reported.
The more serious adverse reactions associated with the use of metoclopramide are parkinsonism and/or other extrapyramidal reactions. These consist often of a feeling of restlessness, facial spasms, involuntary movements and in some cases, torticollis, muscular twitching, trismus, oculogyric crisis, and opisthotonos. Dystonic reactions resembling tetanus have been reported. Extrapyramidal side effects appear to occur more frequently at dosages higher than the usual recommended dosage. Tardive dyskinesia, which in some cases appears to be irreversible, has been reported after discontinuation of long-term metoclopramide therapy. Therefore, prolonged treatment with metoclopramide should be avoided.
SYMPTOMS & TREATMENT OF OVERDOSE:
Symptoms: Symptoms of overdosage may include drowsiness, disorientation and extrapyramidal reactions. Anticholinergic, antiparkinson drugs or antihistamines with anticholinergic properties such as diphenhydramine have effectively controlled extrapyramidal reactions. Symptoms are self-limiting and usually disappear within 24 hours.
Treatment: Management of overdosage consists of gastric emptying, close observation and supportive therapy.
Hemodialysis removes relatively little metoclopramide probably because of the small amount of the drug in blood relative to tissues. Similarly, continuous ambulatory peritoneal dialysis does not remove significant amounts of drug. It is unlikely that dosage would need to be adjusted to compensate for losses through dialysis. Dialysis is not likely to be an effective method of drug removal in overdose situations. Methemoglobinemia has occurred in premature and fullterm neonates who were given overdoses of metoclopramide (1 to 4 mg/kg/day orally, i.m. or i.v. for 1 to 3 or more days). Methemoglobinemia has not been reported in neonates treated with 0.5 mg/kg/day in divided doses. Methemoglobinemia can be reversed by i.v. administration of methylene blue.
DOSAGE AND ADMINISTRATION:
Note: The total adult and pediatric daily dosage must not exceed 0.5 mg/kg/body weight.
Delayed Gastric Emptying: Adults: 5 to 10 mg (1-2 spoonfuls or one 10 mg suppository) 3 or 4 times a day before meals, depending upon response and body weight.
Children (5 to 14 years): 2.5 to 5 mg (2.5 to 5 mL drops) 3 times a day before meals, depending on response and body weight.
Diagnostic Radiology: Adults: 20 mg (4 spoonfuls or one 20 mg suppository) 5 to 10 minutes before barium swallow.
Renal or Hepatic Impairment: Since metoclopramide is excreted principally through the kidneys, in those patients whose creatinine clearance is below 40 mL/min, therapy should be initiated at approximately one-half the recommended dosage. Depending upon clinical efficacy and safety considerations, the dosage may be increased or decreased as appropriate.
Metoclopramide undergoes minimal hepatic metabolism, except for simple conjugation. Its safe use has been described in patients with advanced liver disease whose renal function was normal.
- BARKABROMIDE Syrup: Bottles of 100 ml.
- BARKABROMIDE Drops: Bottles of 15 ml, 30 ml.
- BARKABROMIDE 10 mg, 20 mg Suppositories: Boxes of 10 suppositories.