METOCLOPRAMIDE HYDROCHLORIDE
Maxolon
|
Reviewed by Dorothy
Cooper |
| September 1996
|
Dose and Administration
- 0.03-0.1 mg/kg/dose by slow IV infusion over 30
minutes, PO every 6-8 hours.
- Maximum daily dosage 0.5 mg/kg/day.
Indications
- Impaired gastric emptying and gastrointestinal motility.
- Gastroesophageal reflux.
Contraindications and Precautions
- Known hypersensitivity to metoclopramide.
- Pheochromocytoma (may precipitate hypertensive crisis).
- Caution in neonates with hepatic or renal impairment.
- Caution in neonates with conditions in which stimulation
of gastric motility may be hazardous (gastrointestinal haemorrhage, mechanical
obstruction and/or perforation).
- Concurrent use with narcotic may increase respiratory
depression, decrease gastrointestinal motility.
Clinical Pharmacology
Metoclopramide hydrochloride, a
derivative of procainamide, stimulates motility of the upper gastrointestinal
tract. Does not stimulate gastric, biliary or pancreatic secretions. Mechanism
of action is unknown. Has both dopamine antagonistic activity and peripheral
cholinergic effects. Also induces the release of prolactin.
Well absorbed from gastrointestinal
tract. Marked variation in bioavailability as a consequence of very variable
first pass metabolism. Large distribution volume (lipid soluble drug). Low
binding (13-22%) to human plasma protein. Hepatic metabolism. Elimination via
the kidney with significant fraction unchanged (40-50%). Rapid onset of action:
1-3 minutes following an IV dose (10-15 minutes IM; 30-60 minutes PO). Duration
of action 1-2 hours.
Possible Adverse Effects
- Gastrointestinal disturbances (nausea, vomiting,
diarrhoea).
- Hypotension.
- Cardiac arrhythmias.
- Restlessness, drowsiness, fatigue, anxiety, agitation.
- Dystonic reactions and extrapyramidal symptoms.
Special Considerations
- Therapy usually continued for 2-8 weeks.
- Side effects are usually mild, transient and reversible
following discontinuation of the drug.
- May increase serum levels of aldosterone and prolactin
- Management of metoclopramide overdose and/or toxicity:
discontinue metoclopramide, provide supportive therapy for side effects. May
administer diazepam or benadryl for treatment oculogyric crisis.