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METOZOLV ODT

Last Updated: January 28, 2010

Manufacturer:

Salix Pharmaceuticals, Inc.

Pharmacological Class:

Prokinetic/antidopaminergic

Active Ingredient(s):

Metoclopramide (as HCl) 5mg, 10mg; orally-disintegrating tabs; mint flavored.

Indication(s):

Short-term (4–12 weeks) therapy for symptomatic refractory GERD. To relieve symptoms associated with acute and recurrent diabetic gastroparesis.

Pharmacology:

Metoclopramide is a potent dopamine receptor antagonist that promotes gastric emptying and functions as an antiemetic. Delayed gastric emptying occurs when the vagus nerve is damaged, resulting in impaired acetylcholine secretion and subsequent loss of normal contractility of the muscles of the stomach and intestines. Metoclopramide sensitizes tissues to acetylcholine to stimulate upper GI tract motility without stimulating gastric, biliary, or pancreatic secretions. It increases the tone and amplitude of gastric contraction, relaxes the pyloric sphincter and duodenal bulb, and increases peristalsis of the duodenum and jejunum to accelerate gastric emptying and intestinal transit. Metoclopramide also increases the resting tone of the lower esophageal sphincter for the management of GERD.

Metoclopramide exerts its antiemetic effects by antagonizing central and peripheral dopamine receptors. Dopamine produces nausea and vomiting by stimulating the medullary chemoreceptor trigger zone (CTZ). Metoclopramide blocks the stimulation of the CTZ by agents like l-dopa or apomorphine, which are known to increase dopamine levels or possess dopamine-like effects.

Metozolv ODT is an orally disintegrating tablet formulation of metoclopramide hydrochloride. It should be taken on an empty stomach at least 30 minutes before eating since food can decrease the peak concentration of the drug and/or time it takes to achieve the maximum drug level in the bloodstream. If inadvertently taken with food occasionally over the course of a 4- to12-week regimen, this decrease is not clinically significant.

Legal Classification:

Adults:

Allow tablet to dissolve on tongue. GERD: 10–15mg 4 times daily 30 minutes before meals and at bedtime. Intermittent symptoms: up to 20mg prior to provoking situation; max 12 weeks per therapeutic course. Diabetic gastroparesis: 10mg 4 times daily 30 minutes before meals and at bedtime for 2–8 weeks. Renal impairment: reduce dose.

Children:

Not recommended.

Contraindication(s):

When stimulation of GI motility may be dangerous (eg, obstruction, perforation, or hemorrhage). Pheochromocytoma. Epilepsy. Concomitant drugs which may cause extrapyramidal reactions (eg, antidepressants, antipsychotics, neuroleptics).

Precaution(s):

Discontinue if signs/symptoms of tardive dyskinesia develop; risk increases with duration of treatment and total cumulative dose. Parkinsonism. History of depression. Hypertension. CHF. Arrhythmia. Elderly. Pregnancy (Cat.B). Nursing mothers.

Interaction(s):

Hypertensive crisis with MAOIs. Additive sedation with alcohol, other CNS depressants. Antagonized by anticholinergics and narcotics. Monitor insulin use; may diminish gastric and accelerate intestinal absorption of drugs or food.

Adverse Reaction(s):

Headache, nausea, vomiting, fatigue, somnolence, dizziness, extrapyramidal effects, parkinsonism, tardive dyskinesia, neuroleptic malignant syndrome, hypertension.