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  1. Pharmacology. Metoclopramide is a dopamine antagonist with antiemetic activity at the chemoreceptor trigger zone. It also accelerates GI motility and facilitates gastric emptying. The onset of effect is 1–3 minutes after intravenous administration, and therapeutic effects persist for 1–2 hours after a single dose. The drug is excreted primarily by the kidneys. The elimination half-life is about 5–6 hours but may be as long as 14.8 hours in patients with renal insufficiency and 15.4 hours in patients with cirrhosis.

  2. Indications

    1. Metoclopramide is used to prevent and control persistent nausea and vomiting, particularly when the ability to administer activated charcoal (eg, treatment of theophylline poisoning) or another oral antidotal therapy (eg, acetylcysteine for acetaminophen poisoning) is compromised.

    2. Theoretic (unproven) use to stimulate bowel activity in patients with ileus who require repeat-dose activated charcoal or whole-bowel irrigation.

  3. Contraindications

    1. Known hypersensitivity to the drug; possible cross-sensitivity with procainamide.

    2. Mechanical bowel obstruction or intestinal perforation.

    3. Pheochromocytoma (metoclopramide may cause hypertensive crisis).

  4. Adverse effects

    1. Sedation, restlessness, fatigue, and diarrhea may occur.

    2. Extrapyramidal reactions may result, particularly with high-dose treatment. Pediatric patients appear to be more susceptible. These reactions may be prevented by pretreatment with diphenhydramine (See Diphenhydramine).

    3. May increase the frequency and severity of seizures in patients with seizure disorders.

    4. Parenteral formulations that contain sulfite preservatives may precipitate bronchospasm in susceptible individuals.

    5. Use in pregnancy. FDA Category B. Not likely to cause harm when used as short-term therapy (See Introduction in Section III).

  5. Drug or laboratory interactions

    1. Additive sedation in the presence of other CNS depressants.

    2. Risk for extrapyramidal reactions may be increased in the presence of other dopamine antagonist agents (eg, haloperidol and phenothiazines).

    3. In one study involving hypertensive patients, metoclopramide enhanced the release of catecholamines. As a result, the manufacturer advises cautious use in hypertensive patients and suggests that the drug should not be used in patients taking monoamine oxidase inhibitors.

    4. Agitation, diaphoresis, and extrapyramidal movement disorder were reported in two patients taking selective serotonin reuptake inhibitors (sertraline, venlafaxine) who received IV metoclopramide.

    5. The drug may enhance the absorption of ingested drugs by promoting gastric emptying.

    6. Anticholinergic agents may inhibit bowel motility effects.

    7. Numerous IV incompatibilities: calcium gluconate, sodium bicarbonate, cimetidine, furosemide, and many antibiotic agents (eg, ampicillin, chloramphenicol, erythromycin, penicillin G potassium, tetracycline).

  6. Dosage and method of administration

    1. Low-dose therapy. Effective for mild nausea and vomiting. Give 10–20 mg IM or slowly IV (children: 0.1 mg/kg per dose).

    2. High-dose therapy. For control of severe or persistent vomiting. For adults and children, give a 1- to 2-mg/kg IV infusion over 15 minutes in 50 mL of dextrose or saline. May be repeated twice at 2- to 3-hour intervals.

      1. Metoclopramide is most effective if given before emesis or 30 minutes before administration of a nausea-inducing drug (eg, acetylcysteine).

      2. If no response to initial dose, may give additional 2 mg/kg and repeat every 2–3 hours up to maximum total dose of 12 mg/kg.

      3. Pretreatment with 50 mg (children: 1 mg/kg) of diphenhydramine (See Diphenhydramine) helps prevent extrapyramidal reactions.

      4. Reduce dose ...

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