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Metoclopramide Hydrochloride (MET-oh-KLOE-pra-mide HYE-droe-KLOR-ide)
Trade Name(s):   Metoclopramide Hydrochloride
  ·Tablets 5 mg
  ·Tablets 10 mg
  ·Syrup 5 mg per 5 mL
  ·Injection, solution 5 mg/mL
  Reglan
  ·Tablets 5 mg
  ·Tablets 10 mg
  ·Injection, solution 5 mg per 5 mL
APO-Metoclop
Nu-Metoclopramide

Indicates Canadian Trade Name.


Class: Antidopaminergic GI stimulant

Action: Stimulates upper GI tract motility, resulting in accelerated gastric emptying and intestinal transit, and increased resting tone of lower esophageal sphincter. Exerts antiemetic properties through antagonism of central and peripheral dopamine receptors.

Absorption:
Rapidly and well absorbed. Absolute oral bioavailability is approximately 80%; T max is 1 to 2 h (oral).
Distribution:
Approximately 30% is protein bound; Vd is approximately 3.5 L/kg.
Excretion:
Approximately 85% of dose appears in urine within 72 h (50% of the 85% is present as free or conjugated metoclopramide). The half-life is 5 to 6 h.
Onset:
Onsets are 1 to 3 h (IV), 10 to 15 ? min (IM), and 30 to 60 min (oral).
Duration:
Duration is 1 to 2 h.
Special Populations:
Renal Function Impairment - Reduced plasma Cl, renal Cl, and nonrenal Cl, and increased elimination half-life.
Hepatic Function Impairment - No data available.
Children - Prolonged Cl in neonates.
Indications:
PO Acute and recurrent diabetic gastroparesis; short-term therapy of symptomatic, documented gastroesophageal reflux disease in adults who fail to respond to conventional therapy.
Parenteral Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy; prophylaxis of postoperative nausea and vomiting when nasogastric suction is undesirable; facilitation of small bowel intubation when tube does not pass pylorus with conventional maneuvers; acute and recurrent diabetic gastric stasis; stimulation of gastric emptying and intestinal transit of barium where delayed emptying interferes with radiological examination of the stomach and/or small intestine.
Indications: Unlabeled use(s):
Migraines, opioid-induced nausea and vomiting, Tourette syndrome.

Contraindications: Patients in whom increase in GI motility could be harmful (eg, in presence of GI hemorrhage, mechanical obstruction, perforation); pheochromocytoma; epilepsy; patients receiving drugs likely to cause extrapyramidal reactions; known sensitivity or intolerance to the drug.

Interactions:
Acetaminophen, cyclosporine, ethanol, levodopa, tetracycline Metoclopramide may increase oral bioavailability or absorption of these drugs.
Anticholinergic, levodopa, opioid analgesics May decrease effect of metoclopramide on gastric emptying.
Digoxin Absorption may be diminished.
Cefprozil, cimetidine, digoxin Metoclopramide may decrease oral absorption of these drugs.
CNS depressants (eg, alcohol, anesthetics, barbiturates, opiates, sedatives) May potentiate CNS depressant effects of metoclopramide.
MAOIs Since metoclopramide releases catecholamines in patients with essential hypertension, use cautiously, if at all, in patients receiving MAOIs.
Succinylcholine and possibly mivacurium By inhibiting plasma cholinesterase, metoclopramide may prolong neuromuscular blocking effects such as respiratory depression and paralysis.
Lab Test Interferences: None well documented.

Adverse Reactions:

cardiovascular:
Acute CHF, AV block, bradycardia, depression with suicidal ideation, fluid retention, hypertension, hypotension, supraventricular tachycardia.

cns:
Drowsiness (70%); fatigue, lassitude, restlessness (10%); akathisia; confusion; depression with suicidal ideation; dizziness; extrapyramidal symptoms; hallucinations (rare); headache; insomnia; NMS; Parkinsonian-like symptoms; tardive dyskinesia.

dermatologic:
Transient flushing of face or upper body with high IV doses.

endocrine:
Galactorrhea, gynecomastia, hyperprolactinemia.

gi:
Bowel disturbances, primarily diarrhea; nausea.

gu:
Amenorrhea, elevation of aldosterone, fluid retention, impotence, incontinence, urinary frequency.

hepatic:
Hepatotoxicity (rare).

hematologic:
Agranulocytosis, leukopenia, methemoglobinemia, neutropenia, sulfhemoglobinemia.

hypersensitivity:
Angioneurotic edema, including glossal or laryngeal edema (rare); bronchospasm; rash; urticaria.

miscellaneous:
Porphyria, visual disturbances.
Precautions:
Warning: Treatment with metoclopramide can cause tardive dyskinesia, a serious movement disorder that is often irreversible. The risk of developing tardive dyskinesia increases with duration of treatment and total cumulative dose.
Discontinue metoclopramide therapy in patients who develop signs or symptoms of tardive dyskinesia. There is no known treatment for tardive dyskinesia. In some patients, symptoms may lessen or resolve after metoclopramide treatment is stopped.
Avoid treatment with metoclopramide for longer than 12 wk in all but rare cases in which therapeutic benefit is thought to outweigh the risk of developing tardive dyskinesia.

Pregnancy: Category B .
Lactation: Excreted in breast milk.
Children: Safety and efficacy in children have not been established except to facilitate small bowel intubation. Methemoglobinemia has occurred in newborns.
Elderly: Increased risk of developing Parkinsonian-like effects or tardive dyskinesia; use lowest dose that is effective.
Carcinogenesis: Because the drug elevates serum prolactin concentration, use caution if administration of metoclopramide is considered in patient with previously detected breast cancer.
Special risk patients: Patients with NADH – cytochrome b 5 reductase deficiency are at an increased risk of developing methemoglobinemia or sulfhemoglobinemia when metoclopramide is administered. In patients with G6PD deficiency who experience metoclopramide-induced methemoglobinemia, methylete blue treatment is not recommended.
Anastomosis or closure of gut Drug could theoretically put increased pressure on suture lines after gut anastomosis or closure.
Depression Depression has occurred with or without history of depression. Symptoms have ranged from mild to severe and have included suicidal ideation and suicide.
Extrapyramidal symptoms Manifest primarily as acute dystonic reactions, occurring usually during first 24 to 48 h and more frequently in children and young adults or at higher doses.
Fluid retention/volume overload Certain patients, especially those with cirrhosis or CHF, may be at risk of developing fluid retention and volume overload.
Hypertension Use with caution.
NMS There have been rare reports of an uncommon but potentially fatal symptom complex sometimes referred to as NMS associated with metoclopramide. Clinical manifestations of NMS include altered consciousness, evidence of autonomic instability (cardiac arrhythmias, diaphoresis, irregular pulse or blood pressure, and tachycardia), hyperthermia, and muscle rigidity.
Parkinson-like symptoms Occur more commonly within first 6 mo of treatment, but also can occur after longer periods. Symptoms generally subside within 2 to 3 mo after drug discontinuation. Give drug cautiously, if at all, to patients with preexisting Parkinson disease.
Withdrawal A withdrawal period after stopping metoclopramide could include dizziness, headaches, and/or nervousness.
Overdosage: Signs & symptoms Disorientation, drowsiness, extrapyramidal reactions.

Patient/Family Education:
  • Advise patient to read the Medication Guide for metoclopramide injection before using the first time and to reread with each refill.
  • Instruct patient to take medication 30 min before meals.
  • Instruct patient to report involuntary movement of eyes, face, or limbs to health care provider.
  • Caution patient to avoid intake of alcoholic beverages.
  • Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.
  • Advise patients with diabetes that insulin dosage or timing of dosage may require adjustment.


   
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