Category : GASTROINTESTINAL

Name : METOCLOPRAMIDE     Type & Dosage : Tab. ; 10 mg Package : 100

Pharmacologic Category Dopaminergic blocking agent ; Gastrointestinal emptying ( delayed) adjunct ; Peristaltic stimulant ; Antiemetic Mechanism Of Action Dopaminergic blocking agents – GI emptying ( delayed) adjunct ; Peristaltic stimulant : It is believed that metoclopramide inhibits gastric smooth muscle relaxation produced by dopamine , thus enhancing cholinergic responses of the GI smooth muscle . It accelerates intestinal transit and gastric emptying by preventing relaxation of gastric body and increasing the phasic activity of antrum . At the same time , this action is accompanied by relaxation of the upper small intestine , resulting in an improved coordination between the body and antrum of the stomach and the upper small intestine . It decreases reflux into the esophagus by increasing the resting pressure of the lower esophageal sphincter and improves acid clearance from the esophagus by increasing amplitude of esophageal contractions. Antiemetic – Dopamine antagonist action raises the threshold of activity in the chemoreceptor trigger zone and decreases the input from afferent visceral nerves . Metoclopramide stimulates prolaction secretion and causes a transient increase in circulation aldosterone levels, which may be associated with transient fluid retention. Indications Gastroparesis (treatment ) – Metoclopramide is indicated for the relief of symptoms of acute and recurrent diabetic gastroparesis . Gastroesophageal reflux (treatment) – Oral metoclopramide is indicated in adults for the symptomatic short- term treatment of heartburn and reflux esophagitis due to delayed gastric emptying . In infants , it is used in the treatment of chronic vomiting and recurrent bronchopulmonary manifestations associated with gastroesophageal reflux. Metoclopramide is used for correcting the slow gastric emptying in postvagotomy stasis , in idiopathic stasis , and in various collagen diseases such as scleroderma . In addition , it is used for persistent functional feeding intolerance and gastric stasis in preterm infants. Side Adverse Effects a- Those indicating need for medical attention : Agranulocytosis ; Cardiovascular effects , specifically hypotension ; Hypertension ; Tachycardia ; Dystonic extrapyramidal effects ; Parkinsonian extrapyramidal effects; Tardive dyskinesia With high doses – Agitation ; Panic- like sensation ; Restless legs syndrome b- Those indicating need for medical attention only if they continue or are bothersome: Diarrhea (with high doses ) ; Drowsiness ; Restlessness ; Unusual tiredness or weakness ; Breast tenderness and swelling ; Changes in menstruation ; Constipation ; Dizziness ; Headache; Insomnia ; Mental depression ; Prolactin stimulation ; Nausea ; Skin rash ; Unusual dryness of mouth ; Unusual irritability Contraindications Hypersensitivity to metoclopramide or any component of the formulation ; GI mechanical obstruction , perforation or hemorrhage ; Pheochromocytoma ; Epilepsy Warnings Precautions Use with caution in patients with Parkinson’s disease and in patients with a history of mental depression . The frequency of extrapyramidal symptoms is higher in pediatric patients and adults < 30 years of age ; risk is increased at higher dosages . Use caution with concurrent use of other drugs associated with EPS. Metoclopramide may cause transient increase in serum aldosterone ; use with caution in patients who are at risk of fluid overload (CHF , cirrhosis) . Use with caution in patients with hypertension or following surgical anastomosis / closure . Patients with NADH- cytochrome b5 reductase deficiency are at increased risk of methemoglobinemia and / or sulfhemoglobinemia . Abrupt discontinuation may (rarely) result in withdrawal symptoms (dizziness, headache , nervousness ) . Risk of extrapyramidal effects may be increased in severe , chronic renal failure ; reduced dosage is recommended. Administration in asthmatic patients may increase risk of bronchospasm. Pregnancy FDA pregnancy category B. Extensive studies in humans have not been done . Studies in animals have not shown that metoclopramide causes adverse effects in the fetus. Breast Feeding Problems in humans have not been documented ; however , risk- benefit must be considered since metoclopramide is distributed into breast milk. Drug Interactions Concurrent use with alcohol may increase the CNS depressant effects of either alcohol or metoclopramide ; concurrent use also may accelerate gastric emptying of alcohol , thus possibly increasing its rate and extent of absorption from the small intestine . Concurret use with anticholinergics and opioid – containing medications may antagonize the effects of metoclopramide on GI motility . Prior administration of metoclopramide may decrease the emetic response to apomorphine ; also , concurrent use may potentiate the CNS depressant effects of either apomorphine or metoclopramide . Metoclopramide may increase serum prolactin concentration and interfere with effects of bromocriptine; dosage adjustment of bromocriptine may be necessary . Concurrent use with cimetidine may decrease the effect of cimetidine due to decreased absorption . Concurrent use with CNS depression – producing medications may increase the sedative effects of either these medications or metoclopramide . The decrease in gastric emptying time caused by metoclopramide may increase the bioavilability of cyclosporine ; monitoring of its concentration may be necessary . Concurrent use may decrease absorption of digoxin from stomach ; dosage adjustment of digoxin may be necessary . Metoclopramide has been reported to decrease the effectiveness of levodopa with concurrent use . Concurrent use with metoclopramide may accelerate absorption of mexiletine . Metoclopramide should be used cautiously in patients receiving MAO inhibitors, including furazolidine and procarbazine. Monitoring Parameters Periodic renal function test ; monitor for signs of hypoglycemia in patients using insulin and those being treated for gastroparesis Dietary Considerations Avoid ethanol. Administration And Dosage Treatment of diabetic gastroparesis – Oral , 10 mg 30 minutes before symptoms are likely to occur or before each meal and at bedtime , up to 4 times a day. Treatment of gastroesophageal reflux – Oral , 10 to 15 mg 30 minutes before symptoms are likely to occur or before each meal and at bedtime , up to 4 times a day . Note: In patients with renal function impairment whose creatinine clearance is less than 40 ml per minute , initial dosage should be reduced by one half . Usual adult and adolescent prescribing limits: 500 mcg (0.5 mg) per kg of body weight per day. Usual pediatric dose: GI emptying (delayed) adjunct or peristaltic stimulant – Oral , 0.1 to 0.2 mg per kg of body weight per dose , given 30 minutes before meals and at bedtime. How Supplied Tablet, 10 mg (As HCL) Oral Drop, 4 mg /1 ml (As HCL), bottles of 15 ml, with dropper (Oral drops contains sodium saccharin as sweetener) Storage Store below 30°C. Protect from light and moisture. Oral drops should be protected from freezing. References USP DI, 2004 Up To Date, Vol. 13.1 (2005) Martindale, The Complete Drug Reference, 33 rd edition 2002