Description

Simple

A medication used to reduce nausea and vomiting, and treat heartburn.

Clinical

An antiemetic agent and dopamine D2 antagonist used in the treatment of gastroesophageal reflux disease, prevention of nausea and vomiting, and to stimulate gastric emptying.

Overview

Diabetic gastroparesis is a condition that causes frequent nausea and vomiting, which has a negative impact on quality of life and poses a significant burden on the healthcare system.[6] Metoclopramide is a dopamine antagonist used to treat nausea and vomiting that may be associated with diabetic gastroparesis in addition to gastroesophageal reflux disease (GERD). It can also be used to prevent nausea or vomiting associated with chemotherapy or certain surgical or diagnostic procedures.[19]

One unique property of this drug is that it does not increase gastric acid secretion. It is available in the oral tablet form or in solution, and can also be administered through the intravenous route.[17] Metoclopramide was initially approved by the FDA in 1980.[Read more

Pharmacology

Indication

Metoclopramide in the oral tablet form is used for symptomatic treatment of both acute and recurrent diabetic gastroparesis, in addition to the treatment of gastroesophageal reflux disease (GERD) in patients who have failed to respond to traditional therapy.[ Read more

Pharmacodynamic

Metoclopramide increases gastric emptying by decreasing lower esophageal sphincter (LES) pressure. It also exerts effects on the area postrema of the brain, preventing and relieving the symptoms of nausea and vomiting. In addition, this drug increases gastrointestinal motility without increasing bil... Read more

Mechanism of action

Metoclopramide causes antiemetic effects by inhibiting dopamine D2 and serotonin 5-HT3 receptors in the chemoreceptor trigger zone (CTZ) located in the area postrema of the brain.[ Read more

Absorption

Metoclopramide is rapidly absorbed in the gastrointestinal tract with an absorption rate of about 84%.[ Read more

Protein binding

Metoclopramide is 30% bound to plasma proteins, mainly to alpha-1-acid glycoprotein.[ Read more

Volume of distribution

The volume of distribution of metoclopramide is approximately 3.5 L/kg. This implies a high level of tissue distribution. Metoclopramide crosses the placental barrier and can cause extrapyramidal symptoms in the fetus.[ Read more

Clearance

The renal clearance of metoclopramide is 0.16 L/h/kg with a total clearance of 0.7 L/h/kg. Clinical studies showed that the clearance of metoclopramide may be reduced by up to 50% in patients with renal impairment.[ Read more

Half life

The mean elimination half-life of metoclopramide in people with healthy renal function ranges from 5 to 6 hours but is prolonged in patients with renal impairment. Downward dose adjustment should be considered.[ Read more

Route of elimination

About 85% of an orally administered dose was measured in the urine within 72 hours during a pharmacokinetic study. An average of 18% to 22% of 10-20 mg dose was recovered as free drug within 3 days of administration.[... Read more

Toxicity

The rat oral LD50 of metoclopramide is 750 mg/kg.[20]

Some symptoms of an overdose with metoclopramide include drowsiness, disorientation, and extrapyramidal reactions. Drugs that manage Parkinson's disease or antich... Read more

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Use of drugs that cause extrapyramidal reactions
      • Drugbank Id: DBCOND0108287
  • Regions: US
  • Patient Conditions:
      • Name: Suicidal behaviour or ideation
      • Drugbank Id: DBCOND0094352
  • Regions: US
  • Patient Conditions:
      • Name: Depression
      • Drugbank Id: DBCOND0018735
  • Regions: US
  • Patient Conditions:
      • Name: Parkinsons Disease
      • Drugbank Id: DBCOND0048101
  • Regions: US
  • Patient Conditions:
      • Name: Catecholamine-releasing paragangliomas
      • Drugbank Id: DBCOND0122494
  • Regions: US
  • Patient Conditions:
      • Name: When stimulation of gastric motility may be dangerous
      • Drugbank Id: DBCOND0122493
  • Regions: US
  • Patient Conditions:
      • Name: History of dystonia following metoclopramide use
      • Drugbank Id: DBCOND0122492
  • Regions: US
  • Patient Conditions:
      • Name: History of tardive dyskinesia
      • Drugbank Id: DBCOND0122491
  • Regions: US
  • Patient Conditions:
      • Name: Gastrointestinal Hemorrhage
      • Drugbank Id: DBCOND0031498
  • Regions: US
  • Patient Conditions:
      • Name: Mechanical gastrointestinal obstruction
      • Drugbank Id: DBCOND0107884
  • Regions: US
  • Patient Conditions:
      • Name: Pheochromocytoma
      • Drugbank Id: DBCOND0002904
  • Regions: US
  • Patient Conditions:
      • Name: Gastrointestinal Perforation
      • Drugbank Id: DBCOND0051161

Food Interactions

  • Avoid alcohol.
  • Take before a meal. Co-administration with food decreases bioavailability - take 30 minutes before meals.

Interactions

Type in a drug name to check for interaction with Metoclopramide
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(R)-warfarin
The metabolism of (R)-warfarin can be decreased when combined with Metoclopramide.
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Metoclopramide can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of serotonin syndrome can be increased when Metoclopramide is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of sedation can be increased when Metoclopramide is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-diiodothyropropionic acid
The therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Metoclopramide.
3,5-Diiodotyrosine
The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Metoclopramide.
3,5-Dinitrocatechol
The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Metoclopramide.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of sedation can be increased when Metoclopramide is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of sedation can be increased when Metoclopramide is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of sedation can be increased when Metoclopramide is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The metabolism of 6-O-benzylguanine can be decreased when combined with Metoclopramide.
7-Nitroindazole
The risk or severity of sedation can be increased when Metoclopramide is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Metoclopramide is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
8-azaguanine
The metabolism of 8-azaguanine can be decreased when combined with Metoclopramide.
8-chlorotheophylline
The metabolism of 8-chlorotheophylline can be decreased when combined with Metoclopramide.
9-Deazaguanine
The metabolism of 9-Deazaguanine can be decreased when combined with Metoclopramide.
9-Methylguanine
The metabolism of 9-Methylguanine can be decreased when combined with Metoclopramide.
Abacavir
Abacavir may decrease the excretion rate of Metoclopramide which could result in a higher serum level.
Abaloparatide
The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Metoclopramide.
Abatacept
The metabolism of Metoclopramide can be increased when combined with Abatacept.
20 References
  1. 1 . Tonini M, Candura SM, Messori E, Rizzi CA: Therapeutic potential of drugs with mixed 5-HT4 agonist/5-HT3 antagonist action in the control of emesis. Pharmacol Res. 1995 May;31(5):257-60.PubMed: 7479521
  2. 2 . Lee A, Kuo B: Metoclopramide in the treatment of diabetic gastroparesis. Expert Rev Endocrinol Metab. 2010;5(5):653-662.PubMed: 21278804
  3. 3 . van der Meer YG, Venhuizen WA, Heyland DK, van Zanten AR: Should we stop prescribing metoclopramide as a prokinetic drug in critically ill patients? Crit Care. 2014 Sep 23;18(5):502. doi: 10.1186/s13054-014-0502-4.PubMed: 25672546
  4. 4 . Bateman DN: Clinical pharmacokinetics of metoclopramide. Clin Pharmacokinet. 1983 Nov-Dec;8(6):523-9. doi: 10.2165/00003088-198308060-00003.PubMed: 6360466
  5. 5 . Avalos DJ, Sarosiek I, Loganathan P, McCallum RW: Diabetic gastroparesis: current challenges and future prospects. Clin Exp Gastroenterol. 2018 Sep 25;11:347-363. doi: 10.2147/CEG.S131650. eCollection 2018.PubMed: 30310300
  6. 6 . Lacy BE, Crowell MD, Mathis C, Bauer D, Heinberg LJ: Gastroparesis: Quality of Life and Health Care Utilization. J Clin Gastroenterol. 2018 Jan;52(1):20-24. doi: 10.1097/MCG.0000000000000728.PubMed: 27775961
  7. 7 . Mahajan HS, Gattani S: In situ gels of Metoclopramide Hydrochloride for intranasal delivery: in vitro evaluation and in vivo pharmacokinetic study in rabbits. Drug Deliv. 2010 Jan;17(1):19-27. doi: 10.3109/10717540903447194. Epub 2009 Dec 3.PubMed: 19958151
  8. 8 . Feyer P, Jahn F, Jordan K: Prophylactic Management of Radiation-Induced Nausea and Vomiting. Biomed Res Int. 2015;2015:893013. doi: 10.1155/2015/893013. Epub 2015 Sep 3.PubMed: 26425557
  9. 9 . Eng K, Kay M: Gastrointestinal bezoars: history and current treatment paradigms. Gastroenterol Hepatol (N Y). 2012 Nov;8(11):776-8.PubMed: 24672418
  10. 10 . Wang T, Wang D: Metoclopramide for patients with intractable hiccups: a multicentre, randomised, controlled pilot study. Intern Med J. 2014 Dec;44(12a):1205-9. doi: 10.1111/imj.12542.PubMed: 25069531
  11. 11 . Najjar M, Hall T, Estupinan B: Metoclopramide for Acute Migraine Treatment in the Emergency Department: An Effective Alternative to Opioids. Cureus. 2017 Apr 20;9(4):e1181. doi: 10.7759/cureus.1181.PubMed: 28533997
  12. 12 . Webb D, Buss DC, Fifield R, Bateman DN, Routledge PA: The plasma protein binding of metoclopramide in health and renal disease. Br J Clin Pharmacol. 1986 Mar;21(3):334-6. doi: 10.1111/j.1365-2125.1986.tb05201.x.PubMed: 3964535
  13. 13 . Ross-Lee LM, Eadie MJ, Hooper WD, Bochner F: Single-dose pharmacokinetics of metoclopramide. Eur J Clin Pharmacol. 1981;20(6):465-71. doi: 10.1007/bf00542101.PubMed: 7286058
  14. 14 . McGovern EM, Grevel J, Bryson SM: Pharmacokinetics of high-dose metoclopramide in cancer patients. Clin Pharmacokinet. 1986 Nov-Dec;11(6):415-24. doi: 10.2165/00003088-198611060-00001.PubMed: 3542335
  15. 15 . Allen JC, Gralla R, Reilly L, Kellick M, Young C: Metoclopramide: dose-related toxicity and preliminary antiemetic studies in children receiving cancer chemotherapy. J Clin Oncol. 1985 Aug;3(8):1136-41. doi: 10.1200/JCO.1985.3.8.1136.PubMed: 4020411
  16. 16 . Camilleri M, Shin A: Lessons from pharmacogenetics and metoclopramide: toward the right dose of the right drug for the right patient. J Clin Gastroenterol. 2012 Jul;46(6):437-9. doi: 10.1097/MCG.0b013e3182549528.PubMed: 22688139
  17. 17 . Sasank Isola; Ninos Adams (2019). Metoclopramide, NIH StatPearls. Stat Pearls Publishing.
  18. 18 . Metoclopramide FDA label Link
  19. 19 . Reglan injection FDA label Link
  20. 20 . Metoclopramide MSDS Link