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Dopamine Receptors, Signaling Pathways, and Drugs
Published in Nira Ben-Jonathan, Dopamine, 2020
Metoclopramide, a derivative of benzamides, binds to D2R at nanomolar affinity, has lower binding affinity to D1R, and also acts as a mixed 5-HT3R antagonist/5-HT5R agonist. Metoclopramide is used to treat nausea and vomiting that are associated with uremia, migraine headache, radiation sickness, effects of chemotherapy, labor, infection, and emetogenic drugs. Adverse side effects of metoclopramide include akathisia (restlessness), and focal dystonia, reflecting some blockade of central DARs.
Emesis
Published in Michael JG Farthing, Anne B Ballinger, Drug Therapy for Gastrointestinal and Liver Diseases, 2019
Gareth J Sanger, Paul LR Andrews
Metoclopramide has a mixed pharmacology and is used to treat nausea and vomiting, especially in gastrointestinal disorders and after cytotoxics or radiotherapy, at established conventional doses by antagonism at D2 receptors in the area postrema and by partially activating gastric enteric 5-HT4 receptors.
Information on level of drugs into breastmilk
Published in Wendy Jones, Breastfeeding and Medication, 2018
There is no licenced dose of metoclopramide to increase lactation but studies have mostly used 10 mg three times daily for 7 to 14 days followed by a tapering dosage. In 2013 the MHRA issued guidance that metoclopramide should be prescribed for no longer than five days due to underlying concerns of neurological effects such as short-term extrapyramidal disorders and tardive dyskinesia.
Gastroparesis syndromes: emerging drug targets and potential therapeutic opportunities
Published in Expert Opinion on Investigational Drugs, 2023
Le Yu Naing, Matthew Heckroth, Prateek Mathur, Thomas L Abell
Metoclopramide is currently the only drug approved by the US Food and Drug Administration (FDA) for the treatment of gastroparesis. However, in 2009 a black box warning for metoclopramide and the risk of tardive dyskinesia was issued, with the risk increasing with longer duration and higher cumulative dose. Therefore, it has been advised against the use of metoclopramide for >12 weeks except for in extraordinary circumstances[23]. Domperidone is another D2 receptor antagonist for the treatment of gastroparesis. It crosses the blood-brain barrier poorly and therefore has less frequent central adverse effects than metoclopramide. However, domperidone has been associated with significant QT prolongation, arrhythmia, and sudden cardiac death. A proposed mechanism for QT prolongation with domperidone is due to the blockade of the cardiac delayed rectifier K(+) current (I(Kr)), which is encoded by human Ether-a-go-go Related Gene (hERG)[24]. Other studies have shown that it can be used chronically with no adverse cardiac effects[25]. The FDA never approved domperidone for the US market, although it is available in most other countries. However, domperidone has been available by an investigational new drug (IND) program in the US for several years. There is continuing evidence that domperidone is safe for use in GpS [26–28].
Treatment of hiccups in stroke rehabilitation with gabapentin: A case series and focused clinical review
Published in Topics in Stroke Rehabilitation, 2021
Tiffany Got, Lilian Vivas, Cary Fan, Heather MacNeill
In acute care, he developed new onset of hiccups every 3–5 seconds, which were tiring for the patient. The patient was started on 10 mg metoclopramide with improvement. In rehabilitation, Chlopromazine 12.5 mg once a day was added for further control. However, hiccups recurred and he developed aspiration pneumonia. Since chlorpromazine was held due to interactions with the pneumonia antibiotics, gabapentin was initiated at 100 mg TID. Initially, there was no benefit, however he was titrated up to 300 mg TID and the hiccups resolved. Metoclopramide was also stopped, as hiccups had resolved. One week later, gabapentin was weaned back to 100 mg TID, however there was recurrence of mild hiccups. Accordingly, the following day, the dosage was increased back to 200 mg TID for the remaining month of stay with no recurrence. He was weaned off gabapentin at discharge. Four months later, he was seen in follow-up and reported rare hiccups.
Safety considerations when managing gastro-esophageal reflux disease in infants
Published in Expert Opinion on Drug Safety, 2021
Melina Simon, Elvira Ingrid Levy, Yvan Vandenplas
A meta-analysis on the safety of metoclopramide in infants and children revealed that data were available from 108 studies including 2699 patients [143]. In the 57 prospective studies, extrapyramidal symptoms (9%: 95% confidence interval [CI] 5–17), diarrhea (6%; 95% CI 4–9), and sedation (6%; 95% CI 3–12) were the most common side effects. In retrospective studies and case reports, 8 cases of life-threatening adverse effects were reported due to dysrhythmia, respiratory distress and even arrest, neuroleptic malignant syndrome and tardive dyskinesia [143]. In 2013, the European Medicines Agency released a statement that the risk of neurological adverse events for metoclopramide outweighed the benefit when taken for a prolonged duration at a high dose. It was advised not to use metoclopramide in children under 1 year and no longer than 5 days at a maximum dose of 0.5 mg/kg/day [142] A similar warning was made by the Food and Drug Administration in 2009 [144]. Therefore, the guidelines by NASPGHAN and ESPGHAN do not recommend the use of metoclopramide in children with GERD [9].