Metoclopramide

1. Metoclopram

Metoclopramide

 Generic name: metoclopramide (oral/injection) (MET oh KLOE pra mide)

Brand name: Metozolv ODT, Reglan
Drug class: GI stimulants, Miscellaneous antiemetics

What is metoclopramide?

Metoclopramide increases muscle contractions in the upper digestive tract. This speeds up the rate at which the stomach empties into the intestines.

Metoclopramide oral (taken by mouth) is used for 4 to 12 weeks to treat heartburn caused by gastroesophageal reflux in people who have used other medications without relief.

Metoclopramide oral is also used to treat gastroparesis (slow stomach emptying) in people with diabetes, which can cause heartburn and stomach discomfort after meals.

Metoclopramide injection is used to treat severe diabetic gastroparesis. The injection is also used to prevent nausea and vomiting caused by chemotherapy or surgery, or to aid in certain medical procedures involving the stomach or intestines.

Warnings

Do not use this medicine if you've ever had muscle movement problems after using metoclopramide or similar medicines, or if you've had a movement disorder called tardive dyskinesia. You also should not use this medicine if you've had stomach or intestinal problems (a blockage, bleeding, or a hole or tear), epilepsy or other seizure disorder, or an adrenal gland tumor (pheochromocytoma).

NEVER USE METOCLOPRAMIDE IN LARGER AMOUNTS THAN RECOMMENDED, OR FOR LONGER THAN 12 WEEKS. High doses or long-term use can cause a serious movement disorder that may not be reversible. The longer you use metoclopramide, the more likely you are to develop this movement disorder. The risk of this side effect is higher in diabetics and older adults (especially women).

Before you take metoclopramide, tell your doctor if you have kidney or liver disease, congestive heart failure, high blood pressure, diabetes, Parkinson's disease, or a history of depression.

Do not drink alcohol. It can increase some of the side effects of metoclopramide.

Stop using metoclopramide and call your doctor at once if you have tremors or uncontrolled muscle movements, fever, stiff muscles, confusion, sweating, fast or uneven heartbeats, rapid breathing, depressed mood, thoughts of suicide or hurting yourself, hallucinations, anxiety, agitation, seizure, or jaundice (yellowing of your skin or eyes).

Metoclopramide Uses:

• Injection:

  • Chemotherapy-induced nausea and vomiting, prophylaxis:

    • Prophylaxis of nausea and vomiting associated with emetogenic cancer chemotherapy.
    • Note: Injectable metoclopramide prior to moderate to higher emetic hazard chemotherapy is rarely indicated due to the potential for neurologic events and availability of more efficacious alternative agents.

  • Diabetic Gastroparesis:

    • Relief of symptoms associated with acute and recurrent diabetic gastric stasis.

• Oral:

  • Refractory Gastroesophageal reflux disease (GERD):

    • Short-term treatment having a time interval of 4 to 12 weeks in adults with documented symptomatic GERD who fail to respond to conventional therapy.

Note:

• May use metoclopramide as adjunctive therapy only if gastroparesis is confirmed.
• The American College of Gastroenterology (ACG) guidelines for the treatment of GERD recommend that diagnostic evaluation to confirm underlying gastroparesis be performed prior to considering the use of prokinetic agents.
• Furthermore, the American Gastroenterological Association (AGA) guidelines for the treatment of GERD recommend against the use of metoclopramide as monotherapy or adjunctive therapy in patients with GERD.

  • Diabetic Gastroparesis:

    • Relief of symptoms associated with acute and recurrent diabetic gastroparesis in adults.

  • Off Label Use of Metoclopramide in Adults:

    • Used in aspiration prophylaxis in patients undergoing anesthesia;
    • Used in malignant inoperable partial bowel obstruction
    • Used in the prophylaxis of delayed chemotherapy-induced nausea and vomiting,  (high-risk regimen)
    • Used in refractory functional dyspepsia,
    • Used in nondiabetic gastroparesis
    • Used in hiccups
    • Used in medication-overuse headache or intractable migraine headache (status migrainosus)
    • Used in severe acute migraine, (emergency setting)
    • Used in the treatment of advanced cancer-associated nausea and vomiting
    • Used in severe or refractory pregnancy-associated, nausea and vomiting
    • Used in nausea and/or vomiting: Undifferentiated or due to a variety of medical conditions associated with acute self-limiting nausea/vomiting
    • Used in vertigo-associated nausea and vomiting
    • Used in radiation therapy-induced nausea and vomiting (rescue therapy)
    • Used in acute tension-type headache, (emergency setting)

Note: To lower the risk of tardive dyskinesia (TD), metoclopramide should not be used continuously for 12 or more than 12 weeks. Stop the treatment as soon as possible if the diagnosis of TD is made; consider the use of alternative agents.

In Canada, product information limits the total daily dose to 0.5 mg per kg except when used for prophylaxis of delayed emesis associated with cisplatin chemotherapy.

Metoclopramide (Maxolon) Dose for Aspiration prophylaxis in patients undergoing anesthesia (off-label):

Note: May be considered in patients having high hazard for aspiration:

• IV: Administer 10 mg over 1 to 2 minutes as a single dose ~30 to 60 minutes prior to induction of anesthesia;
• IT is usually given with nonparticulate antacid(s) (eg, citric acid and oral sodium citrate) and/or an H-2 receptor antagonist.

Metoclopramide Dose in the treatment of malignant inoperable partial bowel obstruction,  (off-label):

Note: Do not use in patients with confirmed or suspected complete mechanical obstruction. Often given in combination regimen (eg, with a corticosteroid, antisecretory agent, and/or anticholinergic).

• Oral, IV, SubQ: Every 4 to 6 hours use 10 mg;
• If insufficient relief with intermittent dosing, may switch to an IV or SubQ continuous infusion.

• Continuous IV or SubQ infusion (off-label):

  • Initial: 1.25 to 1.75 mg per hour;
  • Titrate as required and tolerated up to 5 mg per hour.

Metoclopramide (Maxolon) Dose as an alternative agent in the prophylaxis of Chemotherapy-induced nausea and vomiting:

Note:

• Not for routine use;
• It may be considered in selective patients (eg, patients refractory to first-line agents or patients with a history of nausea/ vomiting following low emetic risk regimens). Other agents are safer and more effective.

• Low-emetic-risk IV chemotherapy:

  • Oral: Dosing regimen dependent on expert opinion: 10 mg before chemotherapy or 10 mg every 6 hours as required.

Metoclopramide (Maxolon) Dose in the Prophylaxis of delayed emesis caused by high-emetic-risk chemotherapy regimen (alternative agent) (off-label):

Note: Routine use is not necessary for prophylaxis of delayed emesis (alternative agents recommended); however, potential alternative to neurokinin 1 (NK-1) receptor antagonist (eg, fosaprepitant, aprepitant) in patients receiving cisplatin.

• Oral: 10 to 20 mg 4 times in a day on postchemotherapy days 2 through 4; given in combination with dexamethasone.

Metoclopramide (Maxolon) Dose in the treatment of refractory functional dyspepsia (off-label):

Note: For patients unresponsive to first-line therapies (eg, Helicobacter pylori eradication, proton pump inhibitors, and/or tricyclic antidepressants). The duration of therapy should not exceed four weeks.

• Oral: 5 to 10 mg 3 to 4 times in a day administered prior to meals and at bedtime.
• A lower dose of 2 mg thrice daily (using oral liquid formulation) may provide sufficient response.

Metoclopramide (Maxolon) Dose in the treatment of Diabetic and non-diabetic Gastroparesis:

Note:

• For patients who have had an insufficient response to appropriate Starting interventions (eg, discontinuing drugs that impair GI motility, dietary therapy, improved glycemic control in diabetic gastroparesis).
• With diabetic gastroparesis, some experts suggest limiting use to severe refractory cases. Initiating treatment with an oral liquid formulation is preferred and may improve absorption.
• Oral (preferred), IM, IV, SubQ:
  • 5 to 10 mg 2 to 3 thrice times in a day considered prior to meals.
  • Titrate to the lowest effective dose;
  • The maximum dose: 40 mg per day in 4 divided doses.
  • If parenteral administration is indicated, a maximum of 30 mg per day in 3 divided doses is suggested by some experts.
  • In gastroparesis associated with anorexia nervosa, a lower oral dose of 2.5 mg considered prior to each meal and at bedtime may provide sufficient symptom relief according to some experts.

• Duration:

  • In chronic therapy, limit the course to 12 weeks or less than 12 weeks.
  • Administer a “drug holiday” or dose reduction (eg, 5 mg two times in a day before the 2 main meals of the day) for ~2 weeks whenever clinically feasible or at least every 12 weeks (whichever is shorter) to evaluate efficacy and necessity of continued treatment.

Metoclopramide (Maxolon) Dose in the treatment of Hiccups (off-label):

Note: Limited data available. Treatment generally starts for up to 5 to 10 days. May stops treatment the day after hiccups subside; if hiccups recur, longer treatment duration may be required(eg, in palliative care).

• IV: 5 to 10 mg within every 8 hours.
• Oral: 10 mg within 6 to 8 hours.

Metoclopramide (Maxolon) Dose in the Medication-overuse headache (MOH) or intractable migraine headache (status migrainosus) (adjunctive agent) (off-label):

• Adjunct for the prevention of nausea and vomiting in patients receiving dihydroergotamine:
  • IV: Initial: 10 mg considered as soon as possible prior to dihydroergotamine; repeat as required every 8 hours, either prior to each intermittent dihydroergotamine dose or during continuous IV administration of dihydroergotamine.
  • Metoclopramide doses of up to 20 mg have been used in patients experiencing severe nausea.

Metoclopramide (Maxolon) Dose in the treatment of severe acute Migraine (emergency setting) (off-label):

Note:

• In combination with a migraine-specific agent or as monotherapy (eg, triptan).
• IV consideration may be more efficacious.
• Premedication with diphenhydramine is considered to restrict akathisia and other acute dystonic reactions.
• Restrict rapid IV administration of metoclopramide doses more than 10 mg.
• IV (preferred), IM, Oral, SubQ:
  • As a single dose(10 mg); for migraines with severe nausea and vomiting, some experts increase the dose to 20 mg.

• Alternative high-dose regimen:

  • IV: 20 mg every half an hour as necessary for up to 4 doses in combination with IV diphenhydramine.

Metoclopramide (Maxolon) Dose in the treatment of Nausea and/or vomiting:

• Undifferentiated or due to a variety of medical conditions associated with acute self-limiting nausea/vomiting (alternative agent) (off-label): Limited data available:

  • IV: 10 mg or 20 mg as a single dose; avoid rapid IV administration of doses >10 mg.
  • Oral: As a single dose(10 mg); may repeat after 4 to 6 hours if required.

Metoclopramide (Maxolon) Dose in the treatment of Advanced cancer-associated (off-label):

Note: Limited data available; dosing recommendations based primarily on expert opinion:

• Empiric therapy in patients without an identifiable etiology:

  • Oral, IV, SubQ: 10 mg administered every 6 hours.

Metoclopramide (Maxolon) Dose in the treatment of Malignancy-associated gastroparesis:

• Oral, IV, SubQ:
  • 5 to 10 mg every 6 hours or 3 to 4 times in a day before meals and at night; if required and tolerated, some experts titrate every 6 hours up to 20 mg.

Metoclopramide (Maxolon) Dose in the Palliative care setting:

• Oral, IV, SubQ:
  • Initial: 5 to 10 mg every 4 to 6 hours.
  • For severe symptoms, some experts titrate up to 100 mg/day (in divided doses) if needed.
  • If insufficient relief with intermittent dosing may switch to an IV or SubQ continuous infusion.

• Continuous IV or SubQ infusion:

  • Initial: 1.25 to 1.75 mg per hour; analyze as required and tolerated up to 5 mg per hour.

Metoclopramide (Maxolon) Dose in the treatment of severe or refractory pregnancy-associated vomiting (off-label):

Note: May be administered as an add-on or alternative therapy for nausea and vomiting when symptoms persist following initial pharmacologic therapy and IV hydration if hypovolemic.

• Oral, IV, IM:
  • Every 6 to 8 hours use 5 to 10 mg, added to current treatment regimen or as alternative therapy;
  • if feasible, give 30 half an hour before bedtime and meals.

Metoclopramide (Maxolon) Dose as an alternative agent in the treatment of Vertigo-associated (off-label):

• Oral, IV: 5 to 10 mg every six hours or as required;
• Stop as soon as severe symptoms resolve, usually after 1 to 2 days.

Metoclopramide (Maxolon) Dose as Radiation therapy-induced nausea and vomiting (rescue therapy) (alternative agent) (off-label):

• Low-emetic-risk radiation therapy (head and neck, thorax, or pelvis):

  • Oral, IV: 5 to 20 mg if required after each radiation treatment and repeated every 6 to 8 hours;
  • Based on symptom severity and remaining duration of radiation therapy, patients can receive subsequent rescue therapy as required or begin prophylactic therapy.

• Minimal-emetic-risk radiation therapy (extremities, breast):

  • Oral, IV: 5 to 20 mg if required after each radiation treatment.

Note: Restrict rapid IV consideration of doses more than 10 mg.

Metoclopramide (Maxolon) Dose as an alternative agent in the treatment of Tension-type headache, acute (emergency setting) (off-label): 

• IV: 10 mg as a single dose OR 20 mg as a single dose; premedicate with IV diphenhydramine to retain akathisia and other acute dystonic reactions.

Note: Restrict rapid IV consideration of metoclopramide doses more than 10 mg.

 

Metoclopramide (Maxolon) Dose in the treatment of Postpyloric feeding tube placement (short bowel intubation): IV:

• Patient age:

  • <6 years:
    • 0.1 mg per kg as a single dose
  • 6 to 14 years:
    • As a single dose(2.5 to 5 mg)
  • >14 years:
    • 10 mg as a single dose

Metoclopramide (Maxolon) Dose in the treatment of Gastroesophageal reflux:

Note: ESPGHAN/NASPGHAN guidelines do not allow metoclopramide for routine treatment of GERD; evaluate hazard: benefit prior to use:

• Infants, Children, and Adolescents:

  • Oral: 0.1 to 0.2 mg per kg per dose every 6 to 8 hours;
  • maximum dose: 10 mg.

Metoclopramide (Maxolon) Dose in the prevention of Postoperative nausea and vomiting:

Note: Guidelines discourage the use of metoclopramide; considered ineffective:

• Children and Adolescents:

  • IV: 0.1 to 0.5 mg per kg per dose as a single dose considered after induction or on arrival to PACU;
  • The maximum dose: 10 mg per dose.

Metoclopramide (Maxolon) Dose in the prevention of Chemotherapy-induced nausea and vomiting (CINV):

Note:

• Doses required to prevent CINV are high and should not be used first-line due to increased risk of extrapyramidal symptoms (acute dystonic reactions);
• concurrent consideration of diphenhydramine or benztropine is recommended to restrict drug-induced adverse effects.

• POGO Guidelines:

  • Infants, Children, and Adolescents:

Note: For use in patients in whom corticosteroids are contraindicated; use in combination with 5-HT-3 receptor antagonists.

• • • Initial dose: IV: 1 mg per kg as a single dose prior to chemotherapy
    • Subsequent doses: Oral: 0.0375 mg/kg/dose every 6 hours

• Alternate dosing:

  • Children and Adolescents:

    • IV: 0.1 to 0.2 mg/kg/dose prior to and then every 2 to 4 hours up to every 6 hours following chemotherapy;
    • The maximum dose: 5 doses/day;
    • another trial administered 2 mg/kg when chemotherapy was started followed by 2 mg/kg/dose 2, 6, and 12 hours later.

 

Metoclopramide (Maxolon) Pregnancy Risk Category: N

• Metoclopramide can cross over to the placenta. It is found in cord blood and amniotic liquid.
• No studies have shown that maternal use causes an increase in adverse pregnancy outcomes.
• A neonate might experience methemoglobinemia or other extrapyramidal symptoms.
• Metoclopramide may be used to treat nausea and vomiting in pregnant women if symptoms persist after initial pharmacologic treatment.
• Patients who aren’t dehydrated may receive oral or IM therapy; IV therapy should only be used if dehydration is severe.
• Metoclopramide can be used to prophylaxis nausea and vomiting that is associated with cesarean deliveries.

Breastfeeding: Metoclopramide is used

• Breast milk contains metoclopramide.
• Based on the highest concentration of breastmilk, the relative infant dosage (RID) of metoclopramide stood at 4.6%. This compares to an infant therapeutic dose of 0.5 mg/kg/day.
• Breastfeeding is acceptable when the RID of medication is below 10 percent.
• The RID for metoclopramide is calculated using 0.1565mg/per mL milk. This gives an infant’s daily intake via breastmilk at 0.023 mg/kg/day.
• This was after taking 10mg of maternal metoclopramide three times daily.
• Peak milk levels were about the same as peak maternal serum levels 2 to 3 hours after the dose.
• Metoclopramide was also found in the serum of a nursing infant.
• Two infants who had been breastfed experienced some temporary intestinal discomfort after they were exposed to breast milk. However, this is not a common problem.
• Metoclopramide can increase prolactin levels and cause galactorrhea or gynecomastia.
• It has been deemed a galactagogue for women with difficulty breastfeeding.
• Mixed results were observed in studies of metoclopramide’s efficacy as a breastfeeding aid.
• Metoclopramide does not appear to increase infant weight gain, milk production, breastfeeding duration, or breastfeeding time in any significant way compared to placebo.
• Studies that compared breastfeeding instruction and instruction with metoclopramide alone did not show a benefit to metoclopramide.
• Galactagogues should not be used if there are potential adverse maternal events.
• According to the manufacturer, the decision to stop or continue breastfeeding must be made considering the potential risks for infants and the benefits for the mother. Monitor infants breastfeeding for extrapyramidal or methemoglobinemia.
• According to the WHO, metoclopramide should not be used to treat nausea and vomiting. Long-term side effects in infants are not well documented.

 

Metoclopramide (Maxolon) Dose in Kidney Disease:

• IV:
  • CrCl ≥40 mL/minute:
    • The manufacturer’s labeling has not provided any dosage adjustments.
  • CrCl <40 mL/minute:
    • Initial: Administer ~50 percent of the normal dose.
• Oral:
  • Diabetic gastroparesis:
    • CrCl > 60 mL/minute:
      • No dosage adjustment required.
    • CrCl ≤60 mL/minute:
      • 5 mg 4 times a day (maximum: 20 mg per day).
    • ESRD:
      • 5 mg two times a day (maximum: 10 mg per day).
    • Hemodialysis and continuous ambulatory peritoneal dialysis:
      • 5 mg two times a day (maximum: 10 mg per day).

 

Metoclopramide (Maxolon) Dose in Liver disease:

• IV:
  • The manufacturer’s labeling doesn’t provide any dosage adjustments; however, metoclopramide has been used safely in patients with advanced liver disease with normal renal function.
• Oral:
  • Diabetic gastroparesis:
    • Mild impairment (Child-Pugh class A):
      • No dosage adjustment required.
    • Moderate or severe impairment (Child-Pugh class B or C):
      • 5 mg 4 times a day (maximum: 20 mg per day).

 

Side effects of Metoclopramide (Maxolon):

• Cardiovascular:

  • Atrioventricular Block
  • Bradycardia
  • Supraventricular Tachycardia
  • Cardiac Failure
  • Flushing
  • Hypertension
  • Hypotension

• Central Nervous System:

  • Drowsiness
  • Dizziness
  • Somnolence
  • Akathisia
  • Confusion
  • Depression
  • Dystonic Reaction
  • Lassitude
  • Restlessness
  • Fatigue
  • Headache
  • Drug-Induced Parkinson’s Disease
  • Hallucination
  • Insomnia
  • Neuroleptic Malignant Syndrome
  • Seizure
  • Suicidal Ideation
  • Tardive Dyskinesia

• Dermatologic:

  • Skin Rash
  • Urticaria

• Endocrine & Metabolic:

  • Gynecomastia
  • Hyperprolactinemia
  • Porphyria
  • Amenorrhea
  • Fluid Retention
  • Galactorrhea

• Gastrointestinal:

  • Nausea
  • Vomiting
  • Diarrhea

• Genitourinary:

  • Impotence
  • Urinary Frequency
  • Urinary Incontinence

• Hematologic & Oncologic:

  • Agranulocytosis
  • Sulfhemoglobinemia
  • Leukopenia
  • Methemoglobinemia
  • Neutropenia

• Hepatic:

  • Hepatotoxicity

• Hypersensitivity:

  • Angioedema
  • Hypersensitivity Reaction

• Neuromuscular & Skeletal:

  • Laryngospasm

• Ophthalmic:

  • Visual Disturbance

• Respiratory:

  • Bronchospasm
  • Laryngeal Edema

 

Contraindications to Metoclopramide (Maxolon):

• • • • • Hypersensitivity to metoclopramide and any component of the formulation (eg, glossal angioedema, bronchospasm and laryngeal hypersensitivity)
        • Stimulation of gastrointestinal motility (GI) may pose a danger, including perforation or hemorhage, and mechanical GI obstruction (except for when performed prior to endoscopy in order to evaluate acute upper GI bleeding).
        • History of tardive dystonia, or dyskinesia reaction metoclopramide
        • Combine with other agents that may cause extrapyramidal reactions
        • pheochromocytoma and other catecholamine-releasing paragangliomas
        • seizure disorder (eg epilepsy).

Canadian labeling: Additional contraindications that are not listed in the US labeling

• • • • • Infants less than 1 year old

Warnings & Precautions

• • • Depression in the CNS:

      • CNS depression can cause mental or physical impairments. CNS depression can lead to mental or physical impairments. Patients should not drive or operate machinery that requires mental alertness.

    • Depression

      • Both patients with and without a past have reported depression. Suicidal thoughts and suicide are common symptoms. This medication should not be used by patients with a history of depression.

    • Extrapyramidal symptoms (EPS).

      • Patients younger than 30 are at greater risk of these reactions and take higher doses than recommended.
      • Involuntary movements of the limbs and facial grimacing may occur.
      • Extrapyramidal symptoms may occur, generally as acute dystonic reaction within 24 to 48 hours after the normal adult dose (30-40 mg/day).
      • Also may present as dyspnea and stridor (may be due laryngospasm).
      • Dystonic symptoms can usually be treated with IM Diphenhydramine or benztropine. However, it is also possible for the condition to occur after longer periods. This condition can usually be reversed within two to three months.
      • You may experience motor restlessness such as agitation or jitteriness, or even insomnia. You might try starting the medication at lower doses if symptoms improve.
      • Patients who are taking metoclopramide should be restricted if they’re on antipsychotics or other drugs that could cause EPS.

    • Hyperprolactinemia

      • Metoclopramide increases prolactin levels. Hyperprolactinemia can cause hypothalamic GnRH to be suppressed, which may lead to reduced pituitary Gonadotropin secretion.
      • This can lead to a decrease in reproductive function and gonadal steroidogenesis.
      • There have been reports of amenorrhea, impotence and galactorrhea.
      • Hyperprolactinemia could potentially increase prolactin-dependent breast carcinoma.
      • There has been no evidence linking dopamine D2 receptor antagonists and human tumorigenesis.

    • Hypertension

      • It may increase blood pressure. Avoid use in hypertensive patients. Catecholamines can be released by IV administration.
      • Undiagnosed hypertensive crises have been reported in patients. Use of pheochromocytoma and other catecholamine-releasing paragangliomas is not recommended.
      • Stop treating high blood pressure patients.

    • Neuroleptic malignant Syndrome:

      • This could lead to neuroleptic malignant Syndrome (NMS), and even death.
      • You should monitor for signs of NMS such as hyperpyrexia and muscle rigidity, altered mental state, and autonomic instability (irregular heartbeat, blood pressure, tachycardia and diaphoresis) and elevated creatine phosphokinase and myoglobinuria.
      • Stop immediately if you feel the symptoms of NMS.

    • Proarrhythmic effects

      • Metoclopramide can cause sinus arrest (usually intravenously or in larger doses).
      • Metoclopramide is thought to have a lower torsadogenic potential.
      • However, case reports indicate that metoclopramide can cause QT prolongation or torsades d’pointes in some individuals (eg heart failure patients with renal impairment).
      • The Study of healthy male volunteers has shown that metoclopramide can reduce QT intervals and increase QT variability.
      • But, there is no evidence that metoclopramide prolongs the QT. Other than in a few cases, human data has not shown this. Evidence is not available to show a direct link between metoclopramide and the development of torsades.

    • Tardive dyskinesia [US Boxed Warn]:

      • This condition can cause tardive dyskinesia. This is a serious movement disorder that can be irreversible. With treatment duration and cumulative dose, the risk of developing tardive disorder increases.
      • If you are suffering from tardive dyskinesia, stop taking metoclopramide. Some symptoms may worsen or disappear after you stop taking metoclopramide.
      • Metoclopramide should not be used for more than 12 weeks. A higher chance of tardive dyskinesia is present.
      • Tardive dyskinesia is characterized as involuntary disfiguring movements that affect the face, tongue, trunk and extremities. These movements may appear choreoathetotic.
      • Metoclopramide may be used to mask symptoms of tardive disorder. The long-term effects of this symptomatic suppression in tardive dyskinesia remain unknown.
      • Patients who are taking antipsychotics or metoclopramide should not take metoclopramide.
      • Patients who have tardive dyskinesia symptoms or signs/symptoms should be treated immediately with metoclopramide.
      • Although there is no effective treatment for tardive dyskinesia cases that have been established, some patients may experience a partial or complete remission within weeks to months of metoclopramide being discontinued.
      • Although it is impossible to predict who will develop tardive dyskinesia, the risk of developing it increases in the elderly and especially in elderly women.

    • Cardiovascular disease

      • Patients with concomitant heart disease and kidney impairment should be careful. These patients may be at risk for QT prolongation and torsades.

    • Conditions that are edematous:

      • Patients with cirrhosis and HF are at risk of fluid overload.
      • Keep your job if you have any symptoms or other adverse events.
      • Metoclopramide temporarily increases serum aldosterone. This can increase the risk of fluid retention or volume overload.

    • Hepatic impairment

      • Patients with severe or moderate liver impairment should be cautious. The risk of adverse reactions from systemic exposure could increase. It is recommended to adjust the dosage.

    • Nicotinamide adenine nucleotide hydro (NADH),-cytochrome B5 reductase:

      • Patients suffering from NADH-cytochrome B5 reductase deficiencies are more at risk of methemoglobinemia or sulfhemoglobinemia.

    • Parkinson disease

      • Parkinson’s symptoms can be exacerbated. Patients with Parkinson’s disease and those taking antiparkinsonian medication shouldn’t use them.

    • Renal impairment

      • Patients with severe or moderate kidney impairment should be careful. Systemic exposure could lead to an increase in the risk of adverse reactions. It may be necessary to adjust the dosage.

    • Closure/Surgical anastomosis:

      • After a surgical closure/anastomosis, take care. The suture lines can be subject to pressure increases by using fertility agents.

 

Monitoring parameters:

Signs of extrapyramidal ,tardive dyskinesia, and signs and symptoms of neuroleptic malignant syndrome.

 

How to administer Metoclopramide (Maxolon)?

• • • • • Injection:
          • • • Infusions can be given via IM, direct IV push, or for short infusions (upto 15 minutes), or as continuous infusions.
              • IV push can be given with metoclopramide in lower doses (10 mg or less), for as long as 2 minutes.
              • For higher doses (more than 10 mg), 50mL of compatible solution (preferably with N) should be used and IVPB administered for 15 minutes.
              • NotificationRapid IV administration can cause an intense, temporary feeling of anxiety and restlessness. This is often followed by drowsiness.

          Oral and tablet solutions:

          • • • Take half an hour before meals and bedtime.

          Tablets that can be taken orally:

          • • • Be sure to eat with an empty stomach at all times, at least 30 minutes before you eat and at bedtime.
              • Keep the packaging intact until you are ready to administer.
              • Discard any tablet that breaks or becomes brittle during handling. Place the tablet on your tongue with dry hands. It will dissolve in about one minute (range: 10 seconds to fourteen minutes).
              • Swallow saliva (formulation should be swallowed whole, as it is not intended to be taken with liquids).

          Subcutaneous administrationOff-label route has been reported as either an intermittent bolus injection (or continuous infusion).

           

Mechanism of action of Metoclopramide (Maxolon):

Metoclopramide blocks dopamine and, when taken in higher doses, also blocks serotonin receptors within the CNS’s chemoreceptor trigger area.

It enhances the response of tissues in the upper GI towards acetylcholine. This causes enhanced motility and accelerated gastric emptying. There is no stimulation of gastric or biliary secretions. It also raises the lower esophageal secretion.

Onset of action:

• Oral: 30 to 60 minutes;
• IV: 1 to 3 minutes;
• IM: 10 to 15 minutes

Duration:

• Therapeutic: 1 to 2 hours, regardless of route

Absorption:

• Oral: Rapid, well absorbed

Protein binding:

• ~30 percent

Bioavailability:

• Oral: 80 ± 15.5 percent

Half-life elimination:

• Normal renal function:
  • Neonates, PMA 31 to 40 weeks: 5.4 hours;
  • Infants: 4.15 hours (range: 2.23 to 10.3 hours);
  • Children: ~4 hours (range: 2 to 12.5 hours); half-life and clearance may be dose based;
  • Adults: 5 to 6 hours (may be dose dependent)

Time to peak, serum:

• Neonates, PMA 31 to 40 weeks: 2.45 hours;
• Infants: 2.2 hours;
• Adults: 1 to 2 hours

Excretion:

• Urine (~85 percent);
• feces

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Overdose symptoms may include drowsiness, confusion, or uncontrolled muscle movements.

 

International Brands of Metoclopramide:

• Metozolv ODT
• Reglan
• APO-Metoclop
• Metoclopramide Omega
• Metonia
• Afipran
• Ametic
• Anausin
• Balon
• Carnotprim
• Ceolat
• Cerucal
• Clomitene
• Clopamon
• Cloperan
• Clopram
• Cynovit
• Dibertil
• Dirpasid
• DO-Spertine
• Donmet
• Elitan
• Emeliv
• Emexlon
• Emperal
• Enakur
• Enzimar
• Fluccil
• Gastro-Timelets
• Gastrobi S.R.
• Gastronerton
• Gastrosil
• Imperan
• Itan
• Legir
• Macperan
• Malon
• Manosil
• Maril
• Maxeron
• Maxocol
• Maxolon
• MCP-Beta Tropfen
• MCP-ratiopharm
• Meclomid
• Meclop
• Meclopram
• Meclopstad
• Metamide
• Metlazel
• Metoclamid
• Metoclopramide-Eurogenerics
• Metoclox
• Metopram
• Metovit
• Metsil
• Migen
• Movain
• Movistal
• Nausil
• Nilatika
• Norvom
• Nutramid
• Opram
• Paspertin
• Perinorm
• Perone
• Pharmyork
• Piralen
• Plasil
• Plazilin
• Plemazol
• Polcotec
• Pramidin
• Pramin
• Premosan
• Primperan
• Primperil
• Prinparl
• Prokinyl
• Prowel
• Pulin
• Regelan
• Reglan
• Reglomar
• Regurg
• Reliveran
• Remetin
• Riamide
• Setin
• Sotatic-10
• Tricil
• Vertivom
• Vitamet
• Vomaine
• Zudaw

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