Metoclopramide


Description

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.[

Read more

Pharmacology

Indication

Metoclopramide in the oral tablet form is used for symptomatic treatment of both acute and recurrent... Read more

Pharmacodynamic

Metoclopramide increases gastric emptying by decreasing lower esophageal sphincter (LES) pressure. I... Read more

Mechanism of action

Metoclopramide causes antiemetic effects by inhibiting dopamine D2 and serotonin 5-HT3 receptors in... 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... 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... Read more

Half life

The mean elimination half-life of metoclopramide in people with healthy renal function ranges from 5... Read more

Route of elimination

About 85% of an orally administered dose was measured in the urine within 72 hours during a pharmaco... Read more

Toxicity

The rat oral LD50 of metoclopramide is 750 mg/kg.[ Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Drowsiness US
  • Kind: experimental
    • Percent: 70%
  • Clinical Trial
    Inability to sit still US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Pacing US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Foot tapping US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movement of extremities US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Motor restlessness US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Jitteriness US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Opisthotonus US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Trismus US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Bulbar type of speech US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Stridor US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Rarely US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Facial grimacing US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movements of limbs US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Rhythmic protrusion of tongue US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Oculogyric crisis US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Torticollis US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movement of face US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movements of the tongue US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movements of the trunk US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movement of mouth US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movement of jaw US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Bradykinesia US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Parkinsonian-like symptoms US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Cogwheel rigidity US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Mask-like facies US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 25%
  • Clinical Trial
    Involuntary movements of the trunk US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Involuntary movement of extremities US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Involuntary movement of mouth US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Involuntary movement of jaw US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Involuntary movements of the tongue US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Involuntary movement of face US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Cogwheel rigidity US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Mask-like facies US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Pacing US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Foot tapping US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Inability to sit still US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Agitation US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Jitteriness US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Motor restlessness US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Bulbar type of speech US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Rhythmic protrusion of tongue US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial
    Oculogyric crisis US
  • Kind: experimental
    • Percent: 2%
  • Clinical Trial

    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

    • Food reduces availability, take 30 minutes before meals. Avoid alcohol.

    Interactions

    Type in a drug name to check for interaction with Metoclopramide

    The metabolism of (R)-warfarin can be decreased when combined with Metoclopramide.
    The risk or severity of serotonin syndrome can be increased when Metoclopramide is combined with 2,5-Dimethoxy-4-ethylamphetamine.
    The risk or severity of sedation can be increased when Metoclopramide is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    The therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Metoclopramide.
    The therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Metoclopramide.
    The therapeutic efficacy of 3,5-Dinitrocatechol can be decreased when used in combination with Metoclopramide.
    The risk or severity of sedation can be increased when Metoclopramide is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The risk or severity of sedation can be increased when Metoclopramide is combined with 4-Methoxyamphetamine.
    The risk or severity of sedation can be increased when Metoclopramide is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of 6-O-benzylguanine can be decreased when combined with Metoclopramide.
    The risk or severity of sedation can be increased when Metoclopramide is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Metoclopramide.
    The metabolism of 8-azaguanine can be decreased when combined with Metoclopramide.
    The metabolism of 8-chlorotheophylline can be decreased when combined with Metoclopramide.
    The metabolism of 9-Deazaguanine can be decreased when combined with Metoclopramide.
    The metabolism of 9-Methylguanine can be decreased when combined with Metoclopramide.
    Abacavir may decrease the excretion rate of Metoclopramide which could result in a higher serum level.
    The therapeutic efficacy of Abaloparatide can be decreased when used in combination with Metoclopramide.
    The metabolism of Metoclopramide can be increased when combined with Abatacept.
    The serum concentration of Metoclopramide can be increased when it is combined with Abemaciclib.

    References

    • 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 . Lee A, Kuo B: Metoclopramide in the treatment of diabetic gastroparesis. Expert Rev Endocrinol Metab. 2010;5(5):653-662. [PubMed: 21278804]
    • 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 . Bateman DN: Clinical pharmacokinetics of metoclopramide. Clin Pharmacokinet. 1983 Nov-Dec;8(6):523-9. doi: 10.2165/00003088-198308060-00003. [PubMed: 6360466]
    • 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 . 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 . 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 . 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 . Eng K, Kay M: Gastrointestinal bezoars: history and current treatment paradigms. Gastroenterol Hepatol (N Y). 2012 Nov;8(11):776-8. [PubMed: 24672418]
    • 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 . 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 . 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 . 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 . 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 . 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 . 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 . Sasank Isola; Ninos Adams (2019). Metoclopramide, NIH StatPearls. Stat Pearls Publishing.
    • 18 . Metoclopramide FDA label [Link]
    • 19 . Reglan injection FDA label [Link]
    • 20 . Metoclopramide MSDS [Link]

    Recent Questions